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Sample records for oral antifungal agents

  1. In vitro antifungal susceptibility to six antifungal agents of 229 Candida isolates from patients with diabetes mellitus.

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    Manfredi, M; McCullough, M J; Polonelli, L; Conti, S; Al-Karaawi, Z M; Vescovi, P; Porter, S R

    2006-06-01

    The most common antifungal drugs in current clinical use for the treatment of oral candidosis are polyenes and azoles, mainly used topically. Poor glycaemic control in association with other local factors, such as the presence of oral dental prostheses, salivary pH, salivary flow rate and tobacco habits, may lead to the development of oral candidosis. Topical antifungal agents are frequently used to prevent the development of candidal infections in patients with poor metabolic control, particularly in the elderly wearing dentures. The aim of this study was to assess the antifungal susceptibility of Candida isolates to six antifungal agents using a commercially available kit, Fungitest. The isolated were collected from patients affected by diabetes mellitus from two different geographic localities (London, UK, and Parma, Italy) and from a group of healthy non-diabetic subjects. No differences in antifungal susceptibility to the six agents tested were observed between Candida isolates from diabetic and non-diabetic subjects. However, differences were observed between the two geographically different diabetes mellitus populations. Oral yeast isolates from diabetes mellitus patients in the UK more often displayed resistance or intermediate resistance to fluconazole (P=0.02), miconazole (Pdiabetes mellitus patients in Italy. In addition, more C. albicans isolates were found in diabetic and non-diabetic subjects that were susceptible to fluconazole (P=0.0008 and P=0.01, respectively) than non-albicans isolates. The difference in the antifungal resistance of isolates from the two populations of diabetes mellitus patients may be related to differences in the therapeutic management of candidal infections between the two centres.

  2. Design of amphotericin B oral formulation for antifungal therapy.

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    Liu, Min; Chen, Meiwan; Yang, Zhiwen

    2017-11-01

    Amphotericin B (AmB) remains the "gold standard" for systemic antifungal therapy, even though new drugs are emerging as the attractive antifungal agents. Since AmB has negligible oral absorption as a consequence of its unfavorable physicochemical characterizations, its use is restricted to parenteral administration which is accompanied by severe side effects. As greater understanding of the gastrointestinal tract has developed, the advanced drug delivery systems are emerging with the potential to overcome the barriers of AmB oral delivery. Much research has demonstrated that oral AmB formulations such as lipid formulations may have beneficial therapeutic efficacy with reduced adverse effects and suitable for clinical application. Here we reviewed the different formulation strategies to enhance oral drug efficacy, and discussed the current trends and future perspectives for AmB oral administration in the treatment of antifungal infections.

  3. Topical antifungal agents: an update.

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    Diehl, K B

    1996-10-01

    So many topical antifungal agents have been introduced that it has become very difficult to select the proper agent for a given infection. Nonspecific agents have been available for many years, and they are still effective in many situations. These agents include Whitfield's ointment, Castellani paint, gentian violet, potassium permanganate, undecylenic acid and selenium sulfide. Specific antifungal agents include, among others, the polyenes (nystatin, amphotericin B), the imidazoles (metronidazole, clotrimazole) and the allylamines (terbinafine, naftifine). Although the choice of an antifungal agent should be based on an accurate diagnosis, many clinicians believe that topical miconazole is a relatively effective agent for the treatment of most mycotic infections. Terbinafine and other newer drugs have primary fungicidal effects. Compared with older antifungal agents, these newer drugs can be used in lower concentrations and shorter therapeutic courses. Studies are needed to evaluate the clinical efficacies and cost advantages of both newer and traditional agents.

  4. Antifungal prescribing pattern and attitude towards the treatment of oral candidiasis among dentists in Jordan.

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    Al-Shayyab, Mohammad H; Abu-Hammad, Osama A; Al-Omiri, Mahmoud K; Dar-Odeh, Najla S

    2015-08-01

    The aim of this study was to evaluate the attitude of Jordanian dentists towards the treatment of oral candidiasis and their current antifungal prescribing habits, shedding more light on the possible influence of their socio-professional factors on the pattern of prescribing and practice. A structured validated questionnaire was developed and tested; it was then emailed to a random sample of 600 Jordanian dental practitioners during the period of this cross-sectional survey. The questionnaire recorded practitioners' personal details and their attitude and prescribing of antifungal therapy for oral candidiasis. Statistical significance was based on probability values of oral candidiasis. Of the 423 questionnaires returned, only 330 were included. The attitude of respondents was significantly influenced by their experience [odds ratio (OR) = 0.14; P oral candidiasis is much better among the least-experienced dentists working in private practice. Nystatin and miconazole are the most popular choices of antifungal agents among Jordanian dentists. © 2015 FDI World Dental Federation.

  5. In vivo efficacy of SM-8668 (Sch 39304), a new oral triazole antifungal agent.

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    Tanio, T; Ichise, K; Nakajima, T; Okuda, T

    1990-06-01

    SM-8668 (Sch 39304) is a new oral antifungal agent which we evaluated in comparison with fluconazole in various fungal infection models. The prophylactic effect of SM-8668 was excellent against systemic candidiasis, aspergillosis, and cryptococcosis in mice. The 50% effective dose for SM-8668 was assessed at 10 days after infection and was 0.18, 3.7, and 5.9 mg/kg (body weight), respectively, for the above-mentioned fungal diseases. Fluconazole was about four times less effective than SM-8668 against systemic candidiasis and was only slightly effective at doses of 80 and 25 mg/kg against systemic aspergilosis and cryptococcosis, respectively. SM-8668 was also about four to eight times more active than fluconazole against vaginal candidiasis in rats and against dermatophytic infection in guinea pigs. In addition, topical SM-8668 was as effective as topical miconazole or tioconazole against skin mycosis in guinea pigs. After oral administration, SM-8668 showed a maximum concentration in serum similar to that of fluconazole in both mice and rats, but the elimination half-life and area under the serum concentration-time curve for SM-8668 were twice those for fluconazole.

  6. Penetratin and derivatives acting as antifungal agents

    NARCIS (Netherlands)

    Masman, Marcelo F.; Rodriguez, Ana M.; Raimondi, Marcela; Zacchino, Susana A.; Luiten, Paul G. M.; Somlai, Csaba; Kortvelyesi, Tamas; Penke, Botond; Enriz, Ricardo D.

    The synthesis, in vitro evaluation, and conformational study of RQIKTWFQNRRMKWKK-NH(2) (penetratin) and related derivatives acting as antifungal agents are reported. Penetratin and some of its derivatives displayed antifungal activity against the human opportunistic pathogenic standardized ATCC

  7. In Vitro Antifungal Susceptibility of Oral Candida Isolates from Patients Suffering from Caries and Chronic Periodontitis.

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    De-la-Torre, Janire; Ortiz-Samperio, María Esther; Marcos-Arias, Cristina; Marichalar-Mendia, Xabier; Eraso, Elena; Echebarria-Goicouria, María Ángeles; Aguirre-Urizar, José Manuel; Quindós, Guillermo

    2017-06-01

    Caries and chronic periodontitis are common oral diseases where a higher Candida colonization is reported. Antifungal agents could be adjuvant drugs for the therapy of both clinical conditions. The aim of the current study has been to evaluate the in vitro activities of conventional and new antifungal drugs against oral Candida isolates from patients suffering from caries and/or chronic periodontitis. In vitro activities of amphotericin B, fluconazole, itraconazole, miconazole, nystatin, posaconazole and voriconazole against 126 oral Candida isolates (75 Candida albicans, 18 Candida parapsilosis, 11 Candida dubliniensis, six Candida guilliermondii, five Candida lipolytica, five Candida glabrata, four Candida tropicalis and two Candida krusei) from 61 patients were tested by the CLSI M27-A3 method. Most antifungal drugs were highly active, and resistance was observed in less than 5% of tested isolates. Miconazole was the most active antifungal drug, being more than 98% of isolates susceptible. Fluconazole, itraconazole, and the new triazoles, posaconazole and voriconazole, were also very active. Miconazole, fluconazole and voriconazole have excellent in vitro activities against all Candida isolates and could represent suitable treatment for a hypothetically adjunctive therapy of caries and chronic periodontitis.

  8. Species distribution and in vitro antifungal susceptibility of oral yeast isolates from Tanzanian HIV-infected patients with primary and recurrent oropharyngeal candidiasis

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    Rijs Antonius JMM

    2008-08-01

    Full Text Available Abstract Background In Tanzania, little is known on the species distribution and antifungal susceptibility profiles of yeast isolates from HIV-infected patients with primary and recurrent oropharyngeal candidiasis. Methods A total of 296 clinical oral yeasts were isolated from 292 HIV-infected patients with oropharyngeal candidiasis at the Muhimbili National Hospital, Dar es Salaam, Tanzania. Identification of the yeasts was performed using standard phenotypic methods. Antifungal susceptibility to fluconazole, itraconazole, miconazole, clotrimazole, amphotericin B and nystatin was assessed using a broth microdilution format according to the guidelines of the Clinical and Laboratory Standard Institute (CLSI; M27-A2. Results Candida albicans was the most frequently isolated species from 250 (84.5% patients followed by C. glabrata from 20 (6.8% patients, and C. krusei from 10 (3.4% patients. There was no observed significant difference in species distribution between patients with primary and recurrent oropharyngeal candidiasis, but isolates cultured from patients previously treated were significantly less susceptible to the azole compounds compared to those cultured from antifungal naïve patients. Conclusion C. albicans was the most frequently isolated species from patients with oropharyngeal candidiasis. Oral yeast isolates from Tanzania had high level susceptibility to the antifungal agents tested. Recurrent oropharyngeal candidiasis and previous antifungal therapy significantly correlated with reduced susceptibility to azoles antifungal agents.

  9. Systemic Antifungal Agents: Current Status and Projected Future Developments

    NARCIS (Netherlands)

    Seyedmousavi, S.; Rafati, H.; Ilkit, M.; Tolooe, A.; Hedayati, M.T.; Verweij, P.E.

    2017-01-01

    By definition, an antifungal agent is a drug that selectively destroys fungal pathogens with minimal side effects to the host. Despite an increase in the prevalence of fungal infections particularly in immunocompromised patients, only a few classes of antifungal drugs are available for therapy, and

  10. Common drug-drug interactions in antifungal treatments for superficial fungal infections.

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    Gupta, Aditya K; Versteeg, Sarah G; Shear, Neil H

    2018-04-01

    Antifungal agents can be co-administered alongside several other medications for a variety of reasons such as the presence of comorbidities. Pharmacodynamic interactions such as synergistic and antagonistic interactions could be the result of co-administered medications. Pharmacokinetic interactions could also transpire through the inhibition of metabolizing enzymes and drug transport systems, altering the absorption, metabolism and excretion of co-administered medications. Both pharmacodynamic and pharmacokinetic interactions can result in hospitalization due to serious adverse effects associated with antifungal agents, lower therapeutic doses required to achieve desired antifungal activity, and prevent antifungal resistance. Areas covered: The objective of this review is to summarize pharmacodynamic and pharmacokinetic interactions associated with common antifungal agents used to treat superficial fungal infections. Pharmacodynamic and pharmacokinetic interactions that impact the therapeutic effects of antifungal agents and drugs that are influenced by the presence of antifungal agents was the context to which these antifungal agents were addressed. Expert opinion: The potential for drug-drug interactions is minimal for topical antifungals as opposed to oral antifungals as they have minimal exposure to other co-administered medications. Developing non-lipophilic antifungals that have unique metabolizing pathways and are topical applied are suggested properties that could help limit drug-drug interactions associated with future treatments.

  11. Antifungal stewardship considerations for adults and pediatrics.

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    Hamdy, Rana F; Zaoutis, Theoklis E; Seo, Susan K

    2017-08-18

    Antifungal stewardship refers to coordinated interventions to monitor and direct the appropriate use of antifungal agents in order to achieve the best clinical outcomes and minimize selective pressure and adverse events. Antifungal utilization has steadily risen over time in concert with the increase in number of immunocompromised adults and children at risk for invasive fungal infections (IFI). Challenges in diagnosing IFI often lead to delays in treatment and poorer outcomes. There are also emerging data linking prior antifungal exposure and suboptimal dosing to the emergence of antifungal resistance, particularly for Candida. Antimicrobial stewardship programs can take a multi-pronged bundle approach to ensure suitable prescribing of antifungals via post-prescription review and feedback and/or prior authorization. Institutional guidelines can also be developed to guide diagnostic testing in at-risk populations; appropriate choice, dose, and duration of antifungal agent; therapeutic drug monitoring; and opportunities for de-escalation and intravenous-to-oral conversion.

  12. Risk of serious skin disorders among users of oral antifungals: a population-based study

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    Duque Alberto

    2002-11-01

    Full Text Available Abstract Background Serious skin disorders have been associated with the use of oral antifungals in a number of case reports and series of cases. However the incidence of these disorders remains unknown. Methods We estimated the risk of serious skin disorders in a cohort of users of oral antifungals identified in the general population of the General Practice Research Database in the UK. The cohort included 61,858 patients, 20 to 79 years old, who had received at least one prescription for either oral fluconazole, griseofulvin, itraconazole, ketoconazole, or terbinafine. Results The background rate of serious cutaneous adverse reactions (the one corresponding to non use of oral antifungals was 3.9 per 10,000 person-years (95% CI 2.9–5.2. Incidence rates for current use were 15.4 per 10,000 person-years (1.9–55.7 for itraconazole, 11.1 (3.0–28.5 for terbinafine, 10.4 (1.3–37.5 for fluconazole, and 4.6 (0.1–25.8 for griseofulvin. Itraconazole was the antifungal associated with the highest relative risk, 3.9 (0.5–15.0, when compared to the risk among non users, followed by terbinafine and fluconazole, with relative risks of 2.8 (0.7–7.8 and 2.6 (0.3–10.1, respectively. Conclusions We conclude that cutaneous disorders associated with the use of oral antifungals in this study were all of mild severity and that the risk associated with the use of oral antifungals was slightly higher than the risk in non-users. The safety profile of terbinafine regarding cutaneous disorders is similar to other antifungals and in the very low range of risks associated with other drugs.

  13. Yeasts from the oral cavity of children with AIDS: exoenzyme production and antifungal resistance

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    Bosco Vera Lúcia

    2003-01-01

    Full Text Available The oral fungal microbiota of 30 children with AIDS, of both genders, aged from two to six years, receiving outpatient treatment, was evaluated and compared with that of a control group composed of 30 healthy subjects with matching ages and genders. Virulence factors, such as exoenzyme production, and susceptibility to five antifungal agents using an E-Test kit were evaluated. C. albicans predominated over other species in the AIDS group, showing a higher production of proteinase and phospholipase when compared with that observed in the control group. In this study few clinical manifestations of and low selectivity for C. albicans (23.3% were observed in the AIDS group. The enzymatic studies showed that 53.8% of the AIDS strains were strongly positive whereas only 33.3% of the non-AIDS strains were positive. Amphotericin B was the most effective drug among the antifungal agents tested against C. albicans. The frequency, selectivity and level of exoenzyme production by C. albicans suggest a higher pathogenicity in the AIDS children than in the control children.

  14. Management of symptomatic erosive-ulcerative lesions of oral lichen planus in an adult Egyptian population using Selenium-ACE combined with topical corticosteroids plus antifungal agent

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    Belal, Mahmoud Helmy

    2015-01-01

    Aim: Oral lichen planus (OLP) is a chronic mucocutaneous disease with an immunological etiology. This study was conducted to evaluate the effect of selenium combined with Vitamins A, C & E (Selenium-ACE) in the treatment of erosive-ulcerative OLP as an adjunctive to topical corticosteroids plus antifungal agent. Subjects and Methods: Thirty patients with a confirmed clinical and histopathologic diagnosis of OLP participated in this clinical trial. Patients were randomly allocated into one of three groups and treated as follows: (I) Topical corticosteroids, (II) topical corticosteroids plus antifungal, and (III) SE-ACE combined with topical corticosteroids plus antifungal. The patients were followed for 6 weeks. The pain and severity of the lesions were recorded at the initial and follow-up visits. All recorded data were analyzed using paired t-test and ANOVA test. A P ≤ 0.05 was considered significant. Results: The experimental groups showed a marked reduction in pain sensation and size of lesions, particularly in the final follow-up period, but there was no significant difference between the first two Groups I and II. However, healing of lesions and improvement of pain sensation was effective in Group III since a significant difference was found favoring Group III over both Groups I and II. Conclusion: No significant difference was found in treating erosive-ulcerative lesions of OLP by topical corticosteroids alone or combined with antifungal. However, when using SE-ACE in combination with topical corticosteroids plus antifungal, this approach may be effective in managing ulcerative lesions of OLP; but more research with a larger sample size and a longer evaluation period may be recommended. PMID:26681847

  15. Management of Patients with Oral Candidiasis

    DEFF Research Database (Denmark)

    Kragelund, Camilla; Reibel, Jesper; Pedersen, Anne Marie Lynge

    2016-01-01

    Oral candidal infections are medically treated with antifungal agents. In the fungal cell membrane, steroid ergosterol is the target of the antifungals on the market, but similarity with the human cell membrane may cause host toxicity and unintended reactions. Management of oral candidiasis depends...... in particular in patients with recurrent oral candidiasis. This risk can be reduced if different types of antifungal drugs are used over time or are combined. This chapter focuses on antifungal treatment of the medically compromised patient with oral candidiasis by highlighting the advantages and disadvantages...

  16. Antifungal treatment with carvacrol and eugenol of oral candidiasis in immunosuppressed rats

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    N. Chami

    Full Text Available Carvacrol and eugenol, the main (phenolic components of essential oils of some aromatic plants, were evaluated for their therapeutic efficacy in the treatment of experimental oral candidiasis induced by Candida albicans in immunosuppressed rats. This anticandidal activity was analyzed by microbiological and histopathological techniques, and it was compared with that of nystatin, which was used as a positive control. Microbiologically, carvacrol and eugenol significantly (p<0.05 reduced the number of colony forming units (CFU sampled from the oral cavity of rats treated for eight consecutive days, compared to untreated control rats. Treatment with nystatin gave similar results. Histologically, the untreated control animals showed numerous hyphae on the epithelium of the dorsal surface of the tongue. In contrast no hyphal colonization of the epithelium was seen in carvacrol-treated animals, while in rats treated with eugenol, only a few focalized zones of the dorsal surface of the tongue were occupied by hyphae. In the nystatin treated group, hyphae were found in the folds of the tongue mucosa. Thus, the histological data were confirmed by the microbiological tests for carvacrol and eugenol, but not for the nystatin-treated group. Therefore, carvacrol and eugenol could be considered as strong antifungal agents and could be proposed as therapeutic agents for oral candidiasis.

  17. Antifungal Resistance, Metabolic Routes as Drug Targets, and New Antifungal Agents: An Overview about Endemic Dimorphic Fungi

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    Juliana Alves Parente-Rocha

    2017-01-01

    Full Text Available Diseases caused by fungi can occur in healthy people, but immunocompromised patients are the major risk group for invasive fungal infections. Cases of fungal resistance and the difficulty of treatment make fungal infections a public health problem. This review explores mechanisms used by fungi to promote fungal resistance, such as the mutation or overexpression of drug targets, efflux and degradation systems, and pleiotropic drug responses. Alternative novel drug targets have been investigated; these include metabolic routes used by fungi during infection, such as trehalose and amino acid metabolism and mitochondrial proteins. An overview of new antifungal agents, including nanostructured antifungals, as well as of repositioning approaches is discussed. Studies focusing on the development of vaccines against antifungal diseases have increased in recent years, as these strategies can be applied in combination with antifungal therapy to prevent posttreatment sequelae. Studies focused on the development of a pan-fungal vaccine and antifungal drugs can improve the treatment of immunocompromised patients and reduce treatment costs.

  18. Antifungal Microbial Agents for Food Biopreservation-A Review.

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    Leyva Salas, Marcia; Mounier, Jérôme; Valence, Florence; Coton, Monika; Thierry, Anne; Coton, Emmanuel

    2017-07-08

    Food spoilage is a major issue for the food industry, leading to food waste, substantial economic losses for manufacturers and consumers, and a negative impact on brand names. Among causes, fungal contamination can be encountered at various stages of the food chain (e.g., post-harvest, during processing or storage). Fungal development leads to food sensory defects varying from visual deterioration to noticeable odor, flavor, or texture changes but can also have negative health impacts via mycotoxin production by some molds. In order to avoid microbial spoilage and thus extend product shelf life, different treatments-including fungicides and chemical preservatives-are used. In parallel, public authorities encourage the food industry to limit the use of these chemical compounds and develop natural methods for food preservation. This is accompanied by a strong societal demand for 'clean label' food products, as consumers are looking for more natural, less severely processed and safer products. In this context, microbial agents corresponding to bioprotective cultures, fermentates, culture-free supernatant or purified molecules, exhibiting antifungal activities represent a growing interest as an alternative to chemical preservation. This review presents the main fungal spoilers encountered in food products, the antifungal microorganisms tested for food bioprotection, and their mechanisms of action. A focus is made in particular on the recent in situ studies and the constraints associated with the use of antifungal microbial agents for food biopreservation.

  19. Potent Antifungal Activity of Pure Compounds from Traditional Chinese Medicine Extracts against Six Oral Candida Species and the Synergy with Fluconazole against Azole-Resistant Candida albicans

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    Zhimin Yan

    2012-01-01

    Full Text Available This study was designed to evaluate the in vitro antifungal activities of four traditional Chinese medicine (TCM extracts. The inhibitory effects of pseudolaric acid B, gentiopicrin, rhein, and alion were assessed using standard disk diffusion and broth microdilution assays. They were tested against six oral Candida species, Candida albicans, Candida glabrata, Candida tropicalis, Candida krusei, Candida dubliniensis, and Candida guilliermondii, including clinical isolates from HIV-negative, HIV-positive, and Sjögren's syndrome patients. It was found that pseudolaric acid B had the most potent antifungal effect and showed similar antifungal activity to all six Candida spp, and to isolates from HIV-negative, HIV-positive, and Sjögren's syndrome patients. The MIC values ranged from 16 to 128 μg/mL. More interestingly, a synergistic effect of pseudolaric acid B in combination with fluconazole was observed. We suggest that pseudolaric acid B might be a potential therapeutic fungicidal agent in treating oral candidiasis.

  20. Treatment of gastric candidiasis in patients with gastric ulcer disease: are antifungal agents necessary?

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    Jung, Min Kyu; Jeon, Seong Woo; Cho, Chang Min; Tak, Won Young; Kweon, Young Oh; Kim, Sung Kook; Choi, Yong Hwan

    2009-03-01

    The inadequacy of information on the treatment of gastric candidiasis with antifungal agents promoted us to evaluate patients with fungal infections who had gastric ulcers and assess the need for proton-pump inhibitors or antifungal agents. Sixteen patients were included in the study. The criterion for the diagnosis of candidiasis was finding yeast and hyphae in the tissue or an ulcer on histological sections of biopsy samples. Surface fungi were not considered infections. In all cases with benign ulcers, follow-up endoscopy performed 6 weeks after proton-pump-inhibitor treatment revealed that the ulcer had improved without antifungal medication. However, in patients with malignant ulcers, surgical resection was necessary for a definitive cure. Two patients with lymphoma received combined chemotherapy and a proton-pump inhibitor, which improved their condition. The results of this study suggest that benign ulcers with candidiasis can be effectively treated by a proton-pump inhibitor without antifungal medication. However, surgical resection should be considered for malignant ulcers with candidiasis.

  1. Probiotic Lactobacillus reuteri has antifungal effects on oral Candida species in vitro.

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    Jørgensen, Mette Rose; Kragelund, Camilla; Jensen, Peter Østrup; Keller, Mette Kirstine; Twetman, Svante

    2017-01-01

    Background: An alternative approach for managing Candida infections in the oral cavity by modulating the oral microbiota with probiotic bacteria has been proposed. Objective: The aim was to investigate the antifungal potential of the probiotic bacterium Lactobacillus reuteri (DSM 17938 and ATCC PTA 5289) against six oral Candida species ( C. albicans, C. glabrata, C. krusei, C. tropicalis, C. dubliniensis , and C. parapsilosis ). Design: The lactobacilli were tested for their ability to co-aggregate with and inhibit the growth of the yeasts assessed by spectrophotometry and the agar overlay inhibition assay. Additionally, the pH was evaluated with microsensors, and the production of hydrogen peroxide (H2O2) by the lactobacilli was verified. Results: Both L. reuteri strains showed co-aggregation abilities with the yeasts. The lactobacilli almost completely inhibited the growth of C. albicans and C. parapsilosis , but did not affect C. krusei . Statistically significant differences in co-aggregation and growth inhibition capacities between the two L. reuteri strains were observed (preuteri exhibited antifungal properties against five of the six most common oral Candida species. Further, the results reconfirms that the probiotic capacity of L. reuteri is strain specific.

  2. Drug-drug interactions of antifungal agents and implications for patient care.

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    Gubbins, Paul O; Amsden, Jarrett R

    2005-10-01

    Drug interactions in the gastrointestinal tract, liver and kidneys result from alterations in pH, ionic complexation, and interference with membrane transport proteins and enzymatic processes involved in intestinal absorption, enteric and hepatic metabolism, renal filtration and excretion. Azole antifungals can be involved in drug interactions at all the sites, by one or more of the above mechanisms. Consequently, azoles interact with a vast array of compounds. Drug-drug interactions associated with amphotericin B formulations are predictable and result from the renal toxicity and electrolyte disturbances associated with these compounds. The echinocandins are unknown cytochrome P450 substrates and to date are relatively devoid of significant drug-drug interactions. This article reviews drug interactions involving antifungal agents that affect other agents and implications for patient care are highlighted.

  3. Prospects of application of vegetable oils as antifungal agents (Literature review

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    A. A. Mikheev

    2017-04-01

    Full Text Available Purpose of work – to summarize and present modern scientific literature reviews of alternative antifungal agents usage, among which herbal medicines, and in particular herbal oils, may play significant role. Fungal infections (mycoses are one of the leading infectious diseases in the world. Besides the medical importance, pathogenic fungi play a significant role in the food industry as potential pollutants. In order to treat fungal infections and to prevent food spoilage various medications that are products of chemical synthesis are widely used and the need for them increases significantly. However, among large number of medications and herbal drugs only a small part is used to treat fungal infections and to prevent food decay, though plants contain a lot of bioactive compounds with potential antifungal properties. Therefore, question of application of vegetable oils as antifungal agents is relevant. Various plants contain oils that have the potential antifungal properties, but are often used only in gastronomic purpose. The same time those oils can be successfully used for the treatment of candidiasis and infections caused by fungi of genera Aspergillus, Trichoderma, Penicillium, Fusarium, Metrhizium, Ophiostoma, Scopulariopsis and others. Their effects are manifested like using a single vegetable oil and mixtures of oils. Conclusions. Vegetable oils usage has big perspectives due to the lack of «addictive» effect and the development of resistance in fungi of different taxa. Vegetable oils do not require considerable investments for their reception, and thanks to traditions of aromo- and herbal medicine, their usage can be more effective in contrast to traditional chemotherapeutic agents. The search and study of new medicines based on vegetable oils may be a perspective direction of modern microbiological sciences and requires further deep studies of their biological properties and mechanisms of action.

  4. Rational Discovery of (+) (S) Abscisic Acid as a Potential Antifungal Agent: a Repurposing Approach.

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    Khedr, Mohammed A; Massarotti, Alberto; Mohamed, Maged E

    2018-06-04

    Fungal infections are spreading widely worldwide, and the types of treatment are limited due to the lack of diverse therapeutic agents and their associated side effects and toxicity. The discovery of new antifungal classes is vital and critical. We discovered the antifungal activity of abscisic acid through a rational drug design methodology that included the building of homology models for fungal chorismate mutases and a pharmacophore model derived from a transition state inhibitor. Ligand-based virtual screening resulted in some hits that were filtered using molecular docking and molecular dynamic simulations studies. Both in silico methods and in vitro antifungal assays were used as tools to select and validate the abscisic acid repurposing. Abscisic acid inhibition assays confirmed the inhibitory effect of abscisic acid on chorismate mutase through the inhibition of phenylpyruvate production. The repositioning of abscisic acid, the well-known and naturally occurring plant growth regulator, as a potential antifungal agent because of its suggested action as an inhibitor to several fungal chorismate mutases was the main result of this work.

  5. In vitro susceptibility of Candida albicans clinical isolates to eight antifungal agents in Ouagadougou (Burkina Faso).

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    Zida, A; Yacouba, A; Bamba, S; Sangare, I; Sawadogo, M; Guiguemde, T; Kone, S; Traore, L K; Ouedraogo-Traore, R; Guiguemde, R T

    2017-12-01

    In recent years, the infection Candida albicans infection worldwide has risen, and the incidence of resistance to traditional antifungal therapies is also increasing. The aim of this study was to evaluate in vitro susceptibility of C. albicans clinical isolates to eight antifungal agents in Ouagadougou. A cross-sectional study was conducted from January 2013 to December 2015 at Yalgado Ouédraogo University Teaching Hospital. Two hundred seven strains have been isolated from 347 symptomatic patients received in different clinical services. Samples were cultured on Sabouraud Dextrose Agar supplemented with Cloramphenicol. Isolates were diagnosed as C. albicans using germ tube test, chlamydospore formation on Corn Meal Agar, and Api-Candida test (Biomérieux). Antifungal susceptibility testing was performed by disk diffusion method and isolates classified as susceptible, susceptible dose-dependent and resistant. Three hundred forty-seven (347) patients are included in this study. Two hundred and six (206) out of 347 collected samples (59.36%) were found positive for C. albicans. The strains were mostly isolated from vulvovaginal (49%) and oral infections (40.3%). The highest resistance rates of azoles were obtained with fluconazole (66.5%), itraconazole (52.3%) and ketoconazole (22.9%) when all clinical isolates were included. The resistance rates of fluconazole, itraconazole and ketoconazole remain highest for vulvovaginal and oral isolates. The rate of resistance to the polyene amphotericin B was 32.0% for all clinical isolates and was 56.4% for vulvovaginal strains. Resistance rate to nystatin was 6.3% for all clinical isolates. Cross-resistance analysis with data of all clinical strains revealed that the incidence of resistance to ketoconazole and itraconazole in fluconazole-resistant isolates was significantly higher than recorded for fluconazole-susceptible isolates. In vitro C. albicans antifungal susceptibility test in this study showed relatively high

  6. Tioconazole, a new imidazole-antifungal agent for the treatment of dermatomycoses. Antifungal and pharmacologic properties.

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    Marriott, M S; Baird, J R; Brammer, K W; Faulkner, J K; Halliwell, G; Jevons, S; Tarbit, M H

    1983-01-01

    Tioconazole is a new imidazole antifungal agent with broad-spectrum activity. Its in vitro activity against common dermal pathogens is generally better than miconazole by a factor of 2-8. This activity is paralleled by good topical efficacy in a guinea pig dermatomycosis model. Pharmacokinetic studies in animals have demonstrated minimal systemic exposure following dermal application. Acute general pharmacology studies have shown that the compound is well tolerated in animals and unlikely to produce side-effects in man.

  7. In-vitro Activity of 10 Antifungal Agents against 320 Dermatophyte Strains Using Microdilution Method in Tehran

    Science.gov (United States)

    Adimi, Parvaneh; Hashemi, Seyed Jamal; Mahmoudi, Mahmood; Mirhendi, Hossein; Shidfar, Mohammad Reza; Emmami, Masood; Rezaei-Matehkolaei, Ali; Gramishoar, Mohsen; Kordbacheh, Parivash

    2013-01-01

    Dermatophyte fungi are the etiologic agents of skin infections commonly referred to as ringworm. These infections are not dangerous but as a chronic cutaneous infections they may be difficult to treat and can also cause physical discomfort for patients. They are considered important as a public health problem as well. No information is available regarding the efficacy of antifungal agents against dermatophytes in Tehran. Therefore, in this study we evaluated the efficacy of 10 systemic and topical antifungal medications using CLSI broth microdilution method (M38-A). The antifungal agents used included griseofulvin, terbinafine, itraconazole, ketoconazole, fluconazole, voriconazole, clotrimazole, ciclopirox olamine, amorolfine and naftifine.Fifteen different species of dermatophytes which were mostly clinical isolates were used as follows; T. mentagrophytes, T. rubrum, E. floccosum, M. canis, T. verrucosum, T. tonsurans, M. gypseum, T. violaceum, M. ferruginum, M. fulvum, T. schoenleinii, M. racemosum, T. erinacei, T. eriotrephon and Arthroderma benhamiae. The mean number of fungi particles (conidia) inoculated was 1.25 ×10⁴ CFU/mL. Results were read after 7 days of incubation at 28 °C. According to the obtained results,itraconazole and terbinafine showed the lowest and fluconazole had the greatest MIC values for the most fungi tested. Based on the results, it is necessary to do more research and design a reliable standard method for determination of antifungal susceptibility to choose proper antibiotics with fewer side effects and decrease antifungal resistance and risk of treatment failure. PMID:24250660

  8. Antifungal activity of allylamines against agents of eumycetoma

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    Venugopal Pankajalakshmi

    1993-01-01

    Full Text Available The antifungal activity of the two allylamines naftifine and terbinafine was investigated against 22 strains of eumycetes isolated from cases of eumycetoma by agar dilution. The isolates included Madurella mycetomatis (4, M. Grisea (8, Pyrenochaeta romeroi (2, Exophiala jeanselmei (2 and Leptosphaeria tompkinsii (1 from black grain eumycetomas and Pseudalescheria boydii (3 Acremonium kiliense (1 and A. recifei (1 form pale grain eumycetomas. Terbinafine was more active than naftifine inhibiting 50% (MIC50 and 90% (MIC90 of the black grain eumycetoma agents at 0.5 and 2.5 ?g/ml respectively. The MIC50s and MIC90s of naftifine were 1 and 5 ?g/ml. For pale grain eumycetoma agents, the MIC range for terbinafine and naftifine were ??0.01 - 100 and 0.1 - 100 ?g/ml.

  9. In vitro synergistic combinations of pentamidine, polymyxin B, tigecycline and tobramycin with antifungal agents against Fusarium spp.

    Science.gov (United States)

    Pozzebon Venturini, Tarcieli; Rossato, Luana; Chassot, Francieli; Tairine Keller, Jéssica; Baldissera Piasentin, Fernanda; Morais Santurio, Janio; Hartz Alves, Sydney

    2016-08-01

    The genus Fusarium is characterized by hyaline filamentous fungi that cause infections predominantly in immunocompromised patients. The remarkable primary resistance to antifungal agents of this genus requires a search for new therapeutic possibilities. This study assessed the in vitro susceptibility of 25 clinical isolates of Fusarium against antifungal agents (amphotericin B, caspofungin, itraconazole and voriconazole) and antimicrobials (pentamidine, polymyxin B, tigecycline and tobramycin) according to the broth microdilution method (M38-A2). The interactions between antifungal and antimicrobial agents were evaluated by the microdilution checkerboard method. Pentamidine and polymyxin B showed MIC values ≥4 µg ml-1 against Fusarium spp. The highest rates of synergism were observed when amphotericin B or voriconazole was combined with tobramycin (80 % and 76 %, respectively), polymyxin B (76 % and 64 %) and pentamidine (72 % and 68 %). The most significant combinations deserve in vivo evaluations in order to verify their potential in the treatment of fusariosis.

  10. Antifungal Activity of Maytenin and Pristimerin

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    Fernanda P. Gullo

    2012-01-01

    Full Text Available Fungal infections in humans have increased alarmingly in recent years, particularly in immunocompromised individuals. Among the infections systemic candidiasis, aspergillosis, cryptococcosis, paracoccidioidomycosis, and histoplasmosis mortality are more prevalent and more severe in humans. The current high incidence of dermatophytosis is in humans, especially as the main etiologic agents Trichophyton rubrum and Trichophyton mentagrophytes. Molecules pristimerin and maytenin obtained from the plant Maytenus ilicifolia (Celastraceae are known to show various pharmacological activities. This study aimed to evaluate the spectrum of antifungal activity of maytenin and pristimerin and their cytotoxicity in human keratinocytes (NOK cells of the oral mucosa. It was concluded that the best spectrum of antifungal activity has been shown to maytenin with MIC varying from 0.12 to 125 mg/L, although it is also active with pristimerin MIC ranging between 0.12 and 250 mg/L. Regarding the toxicity, both showed to have high IC50. The SI showed high pristimerin against some species of fungi, but SI maytenin was above 1.0 for all fungi tested, showing a selective action of fungi. However, when comparing the two substances, maytenin also showed better results. The two molecules can be a possible prototype with a broad spectrum of action for the development of new antifungal agents.

  11. Antifungal Activity of Maytenin and Pristimerin

    Science.gov (United States)

    Gullo, Fernanda P.; Sardi, Janaina C. O.; Santos, Vânia A. F. F. M.; Sangalli-Leite, Fernanda; Pitangui, Nayla S.; Rossi, Suélen A.; de Paula e Silva, Ana C. A.; Soares, Luciana A.; Silva, Julhiany F.; Oliveira, Haroldo C.; Furlan, Maysa; Silva, Dulce H. S.; Bolzani, Vanderlan S.; Mendes-Giannini, Maria José S.; Fusco-Almeida, Ana Marisa

    2012-01-01

    Fungal infections in humans have increased alarmingly in recent years, particularly in immunocompromised individuals. Among the infections systemic candidiasis, aspergillosis, cryptococcosis, paracoccidioidomycosis, and histoplasmosis mortality are more prevalent and more severe in humans. The current high incidence of dermatophytosis is in humans, especially as the main etiologic agents Trichophyton rubrum and Trichophyton mentagrophytes. Molecules pristimerin and maytenin obtained from the plant Maytenus ilicifolia (Celastraceae) are known to show various pharmacological activities. This study aimed to evaluate the spectrum of antifungal activity of maytenin and pristimerin and their cytotoxicity in human keratinocytes (NOK cells of the oral mucosa). It was concluded that the best spectrum of antifungal activity has been shown to maytenin with MIC varying from 0.12 to 125 mg/L, although it is also active with pristimerin MIC ranging between 0.12 and 250 mg/L. Regarding the toxicity, both showed to have high IC50. The SI showed high pristimerin against some species of fungi, but SI maytenin was above 1.0 for all fungi tested, showing a selective action of fungi. However, when comparing the two substances, maytenin also showed better results. The two molecules can be a possible prototype with a broad spectrum of action for the development of new antifungal agents. PMID:22675379

  12. Screening of pharmacologically active small molecule compounds identifies antifungal agents against Candida biofilms

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    Takao eWatamoto

    2015-12-01

    Full Text Available Candida species have emerged as important and common opportunistic human pathogens, particularly in immunocompromised individuals. The current antifungal therapies either have toxic side effects or are insufficiently effect. The aim of this study is develop new small-molecule antifungal compounds by library screening methods using C. albicans, and to evaluate their antifungal effects on Candida biofilms and cytotoxic effects on human cells. Wild-type C. albicans strain SC5314 was used in library screening. To identify antifungal compounds, we screened a small-molecule library of 1,280 pharmacologically active compounds (LOPAC1280TM using an antifungal susceptibility test (AST. To investigate the antifungal effects of the hit compounds, ASTs were conducted using Candida strains in various growth modes, including biofilms. We tested the cytotoxicity of the hit compounds using human gingival fibroblast (hGF cells to evaluate their clinical safety. Only 35 compounds were identified by screening, which inhibited the metabolic activity of C. albicans by >50%. Of these, 26 compounds had fungistatic effects and 9 compounds had fungicidal effects on C. albicans. Five compounds, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate, ellipticine and CV-3988, had strong fungicidal effects and could inhibit the metabolic activity of Candida biofilms. However, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate and ellipticine were cytotoxic to hGF cells at low concentrations. CV-3988 showed no cytotoxicity at a fungicidal concentration.Four of the compounds identified, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate and ellipticine, had toxic effects on Candida strains and hGF cells. In contrast, CV-3988 had fungicidal effects on Candida strains, but low cytotoxic effects on hGF cells. Therefore, this screening reveals agent, CV-3988 that was previously unknown to be antifungal agent, which could be a novel therapies for superficial mucosal

  13. An Evaluation of Antifungal Agents for the Treatment of Fungal Contamination in Indoor Air Environments

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    Senthaamarai Rogawansamy

    2015-06-01

    Full Text Available Fungal contamination in indoor environments has been associated with adverse health effects for the inhabitants. Remediation of fungal contamination requires removal of the fungi present and modifying the indoor environment to become less favourable to growth.  This may include treatment of indoor environments with an antifungal agent to prevent future growth. However there are limited published data or advice on chemical agents suitable for indoor fungal remediation. The aim of this study was to assess the relative efficacies of five commercially available cleaning agents with published or anecdotal use for indoor fungal remediation. The five agents included two common multi-purpose industrial disinfectants (Cavicide® and Virkon®, 70% ethanol, vinegar (4.0%-4.2% acetic acid, and a plant-derived compound (tea tree (Melaleuca alternifolia oil tested in both a liquid and vapour form. Tea tree oil has recently generated interest for its antimicrobial efficacy in clinical settings, but has not been widely employed for fungal remediation. Each antifungal agent was assessed for fungal growth inhibition using a disc diffusion method against a representative species from two common fungal genera, (Aspergillus fumigatus and Penicillium chrysogenum, which were isolated from air samples and are commonly found in indoor air. Tea tree oil demonstrated the greatest inhibitory effect on the growth of both fungi, applied in either a liquid or vapour form. Cavicide® and Virkon® demonstrated similar, although less, growth inhibition of both genera. Vinegar (4.0%–4.2% acetic acid was found to only inhibit the growth of P. chrysogenum, while 70% ethanol was found to have no inhibitory effect on the growth of either fungi. There was a notable inhibition in sporulation, distinct from growth inhibition after exposure to tea tree oil, Virkon®, Cavicide® and vinegar. Results demonstrate that common cleaning and antifungal agents differ in their capacity to

  14. An evaluation of antifungal agents for the treatment of fungal contamination in indoor air environments.

    Science.gov (United States)

    Rogawansamy, Senthaamarai; Gaskin, Sharyn; Taylor, Michael; Pisaniello, Dino

    2015-06-02

    Fungal contamination in indoor environments has been associated with adverse health effects for the inhabitants. Remediation of fungal contamination requires removal of the fungi present and modifying the indoor environment to become less favourable to growth.  This may include treatment of indoor environments with an antifungal agent to prevent future growth. However there are limited published data or advice on chemical agents suitable for indoor fungal remediation. The aim of this study was to assess the relative efficacies of five commercially available cleaning agents with published or anecdotal use for indoor fungal remediation. The five agents included two common multi-purpose industrial disinfectants (Cavicide® and Virkon®), 70% ethanol, vinegar (4.0%-4.2% acetic acid), and a plant-derived compound (tea tree (Melaleuca alternifolia) oil) tested in both a liquid and vapour form. Tea tree oil has recently generated interest for its antimicrobial efficacy in clinical settings, but has not been widely employed for fungal remediation. Each antifungal agent was assessed for fungal growth inhibition using a disc diffusion method against a representative species from two common fungal genera, (Aspergillus fumigatus and Penicillium chrysogenum), which were isolated from air samples and are commonly found in indoor air. Tea tree oil demonstrated the greatest inhibitory effect on the growth of both fungi, applied in either a liquid or vapour form. Cavicide® and Virkon® demonstrated similar, although less, growth inhibition of both genera. Vinegar (4.0%-4.2% acetic acid) was found to only inhibit the growth of P. chrysogenum, while 70% ethanol was found to have no inhibitory effect on the growth of either fungi. There was a notable inhibition in sporulation, distinct from growth inhibition after exposure to tea tree oil, Virkon®, Cavicide® and vinegar. Results demonstrate that common cleaning and antifungal agents differ in their capacity to inhibit the growth

  15. Diagnosis of oral fungal infection in patients undergoing head and neck cancer radiation. Antifungal susceptibility of isolates

    International Nuclear Information System (INIS)

    Bulacio, L.; Paz, M.; Ramadan, S.; Ramos, L.; Marozzi, M.L.; Sortino, M.; Escovich, L.; Lopez, C.

    2008-01-01

    Radiotherapy adverse effects are very common, they contribute to development of opportunistic infections. Genus Candida is often associated with oral diseases in susceptible patients. The aim of this study was to study the presence of yeast in oral lesions, in patients receiving radiotherapy for head and neck cancer, and to evaluate antifungal susceptibility of isolates. Swabs of oral mucosal lesions of 76 patients were studied. Antifungal susceptibility of the isolates was evaluated, with ATB Fungus-3 method, which tests 5-fluorcitosine (5-FC), amphotericin B (AMB), fluconazole (FCA), itraconazole (ITR) and voriconazole (VRC); and allows the estimation of the minimum inhibitory concentration (MIC). Yeasts were isolated in 74% of samples, being Candida albicans, most frequent specie (53%), followed by C.tropicalis (24%), C.parapsilosis (14%), C.krusei (5%), C.dubliniensis (2%) and Saccharomyces cerevisiae (2%). All strains were susceptible to VRC. For other antifungals, there were resistant or dose-dependent-susceptible strains. Only C.krusei was resistant to the FCA. About AMB, 2 isolates of C. tropicalis presented a value of 2 mg/l MIC, dose with high incidence of adverse effects. These studies are important to establish early and suitable therapy, wich contribute to achieve lowers rates of disseminated forms of candidiasis, and to reduce the difficulties in food intake that carries the presence of oral lesions. (authors)

  16. Spectrum and the In Vitro Antifungal Susceptibility Pattern of Yeast Isolates in Ethiopian HIV Patients with Oropharyngeal Candidiasis.

    Science.gov (United States)

    Moges, Birhan; Bitew, Adane; Shewaamare, Aster

    2016-01-01

    Background. In Ethiopia, little is known regarding the distribution and the in vitro antifungal susceptibility profile of yeasts. Objective. This study was undertaken to determine the spectrum and the in vitro antifungal susceptibility pattern of yeasts isolated from HIV infected patients with OPC. Method. Oral pharyngeal swabs taken from oral lesions of study subjects were inoculated onto Sabouraud Dextrose Agar. Yeasts were identified by employing conventional test procedures and the susceptibility of yeasts to antifungal agents was evaluated by disk diffusion assay method. Result. One hundred and fifty-five yeast isolates were recovered of which 91 isolates were from patients that were not under HAART and 64 were from patients that were under HAART. C. albicans was the most frequently isolated species followed by C. glabrata, C. tropicalis, C. krusei, C. kefyr, Cryptococcus laurentii, and Rhodotorula species. Irrespective of yeasts isolated and identified, 5.8%, 5.8%, 12.3%, 8.4%, 0.6%, and 1.3% of the isolates were resistant to amphotericin B, clotrimazole, fluconazole, ketoconazole, miconazole, and nystatin, respectively. Conclusion. Yeast colonization rate of 69.2% and 31% resistance to six antifungal agents was documented. These highlight the need for nationwide study on the epidemiology of OPC and resistance to antifungal drugs.

  17. Spectrum and the In Vitro Antifungal Susceptibility Pattern of Yeast Isolates in Ethiopian HIV Patients with Oropharyngeal Candidiasis

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    Birhan Moges

    2016-01-01

    Full Text Available Background. In Ethiopia, little is known regarding the distribution and the in vitro antifungal susceptibility profile of yeasts. Objective. This study was undertaken to determine the spectrum and the in vitro antifungal susceptibility pattern of yeasts isolated from HIV infected patients with OPC. Method. Oral pharyngeal swabs taken from oral lesions of study subjects were inoculated onto Sabouraud Dextrose Agar. Yeasts were identified by employing conventional test procedures and the susceptibility of yeasts to antifungal agents was evaluated by disk diffusion assay method. Result. One hundred and fifty-five yeast isolates were recovered of which 91 isolates were from patients that were not under HAART and 64 were from patients that were under HAART. C. albicans was the most frequently isolated species followed by C. glabrata, C. tropicalis, C. krusei, C. kefyr, Cryptococcus laurentii, and Rhodotorula species. Irrespective of yeasts isolated and identified, 5.8%, 5.8%, 12.3%, 8.4%, 0.6%, and 1.3% of the isolates were resistant to amphotericin B, clotrimazole, fluconazole, ketoconazole, miconazole, and nystatin, respectively. Conclusion. Yeast colonization rate of 69.2% and 31% resistance to six antifungal agents was documented. These highlight the need for nationwide study on the epidemiology of OPC and resistance to antifungal drugs.

  18. Nanoparticles as safe and effective delivery systems of antifungal agents: Achievements and challenges.

    Science.gov (United States)

    Soliman, Ghareb M

    2017-05-15

    Invasive fungal infections are becoming a major health concern in several groups of patients leading to severe morbidity and mortality. Moreover, cutaneous fungal infections are a major cause of visits to outpatient dermatology clinics. Despite the availability of several effective agents in the antifungal drug arena, their therapeutic outcome is less than optimal due to limitations related to drug physicochemical properties and toxicity. For instance, poor aqueous solubility limits the formulation options and efficacy of several azole antifungal drugs while toxicity limits the benefits of many other drugs. Nanoparticles hold great promise to overcome these limitations due to their ability to enhance drug aqueous solubility, bioavailability and antifungal efficacy. Further, drug incorporation into nanoparticles could greatly reduce its toxicity. Despite these interesting nanoparticle features, there are only few marketed nanoparticle-based antifungal drug formulations. This review sheds light on different classes of nanoparticles used in antifungal drug delivery, such as lipid-based vesicles, polymeric micelles, solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions and dendrimers with emphasis on their advantages and limitations. Translation of these nanoformulations from the lab to the clinic could be facilitated by focusing the research on overcoming problems related to nanoparticle stability, drug loading and high cost of production and standardization. Copyright © 2017 Elsevier B.V. All rights reserved.

  19. Intra-antral application of an anti-fungal agent for recurrent maxillary fungal rhinosinusitis: a case report

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    Dunmade Adekunle D

    2012-08-01

    Full Text Available Abstract Introduction Fungal infection of the paranasal sinuses is an increasingly recognized entity both in immunocompetent and immunocompromised individuals. Treatment has been via use of either surgical or medical modalities, or a combination of the two. Here, we present a case of utilization of intra-antral application of an anti-fungal agent in the management of recurrent fungal sinusitis in an indigent Nigerian patient. Case presentation We present the case of a 30-year-old West African Yoruba man, an indigent Nigerian clergyman, who presented to our facility with a history of recurrent nasal discharge (about one year, recurrent nasal blockage (about five months, and right facial swelling (about one week. After intra-nasal antrostomy for debulking with a systemic anti-fungal agent, our patient had a recurrence after four months. Our patient subsequently had an intra-antral application of flumetasone and clioquinol (Locacorten®-Vioform® weekly for six weeks with improvement of symptoms and no recurrence after six months of follow-up. Conclusions We conclude that topical intra-antral application of anti-fungal agents is effective in patients with recurrent fungal maxillary sinusitis after surgical debulking.

  20. Antifungal Activity of Commercial Essential Oils and Biocides against Candida Albicans.

    Science.gov (United States)

    Serra, Elisa; Hidalgo-Bastida, Lilia Araida; Verran, Joanna; Williams, David; Malic, Sladjana

    2018-01-25

    Management of oral candidosis, most frequently caused by Candida albicans , is limited due to the relatively low number of antifungal drugs and the emergence of antifungal tolerance. In this study, the antifungal activity of a range of commercial essential oils, two terpenes, chlorhexidine and triclosan was evaluated against C. albicans in planktonic and biofilm form. In addition, cytotoxicity of the most promising compounds was assessed using murine fibroblasts and expressed as half maximal inhibitory concentrations (IC50). Antifungal activity was determined using a broth microdilution assay. The minimum inhibitory concentration (MIC) was established against planktonic cells cultured in a range of concentrations of the test agents. The minimal biofilm eradication concentration (MBEC) was determined by measuring re-growth of cells after pre-formed biofilm was treated for 24 h with the test agents. All tested commercial essential oils demonstrated anticandidal activity (MICs from 0.06% ( v / v ) to 0.4% ( v / v )) against planktonic cultures, with a noticeable increase in resistance exhibited by biofilms (MBECs > 1.5% ( v / v )). The IC50s of the commercial essential oils were lower than the MICs, while a one hour application of chlorhexidine was not cytotoxic at concentrations lower than the MIC. In conclusion, the tested commercial essential oils exhibit potential as therapeutic agents against C. albicans , although host cell cytotoxicity is a consideration when developing these new treatments.

  1. In vitro and in vivo activity of a novel antifungal small molecule against Candida infections.

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    Sarah Sze Wah Wong

    Full Text Available Candida is the most common fungal pathogen of humans worldwide and has become a major clinical problem because of the growing number of immunocompromised patients, who are susceptible to infection. Moreover, the number of available antifungals is limited, and antifungal-resistant Candida strains are emerging. New and effective antifungals are therefore urgently needed. Here, we discovered a small molecule with activity against Candida spp. both in vitro and in vivo. We screened a library of 50,240 small molecules for inhibitors of yeast-to-hypha transition, a major virulence attribute of Candida albicans. This screening identified 20 active compounds. Further examination of the in vitro antifungal and anti-biofilm properties of these compounds, using a range of Candida spp., led to the discovery of SM21, a highly potent antifungal molecule (minimum inhibitory concentration (MIC 0.2-1.6 µg/ml. In vitro, SM21 was toxic to fungi but not to various human cell lines or bacterial species and was active against Candida isolates that are resistant to existing antifungal agents. Moreover, SM21 was relatively more effective against biofilms of Candida spp. than the current antifungal agents. In vivo, SM21 prevented the death of mice in a systemic candidiasis model and was also more effective than the common antifungal nystatin at reducing the extent of tongue lesions in a mouse model of oral candidiasis. Propidium iodide uptake assay showed that SM21 affected the integrity of the cell membrane. Taken together, our results indicate that SM21 has the potential to be developed as a novel antifungal agent for clinical use.

  2. Detection and antifungal susceptibility testing of oral Candida dubliniensis from human immunodeficiency virus-infected patients

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    Chunchanur Sneha

    2009-10-01

    Full Text Available Context: Candida dubliniensis, an opportunistic yeast that has been implicated in oropharyngeal candidiasis (OPC in patients infected with Human Immunodeficiency Virus (HIV may be under-reported due to its similarity with Candida albicans. Resistance to Fluconazole is often seen in C. dubliniensis isolates from clinical specimens. Aims: To know the prevalence of C. dubliniensis in OPC in patients infected with HIV and their antifungal susceptibility pattern. Settings and Design: One hundred and thirty-two HIV seropositive individuals and 50 healthy controls were included in the study. Materials and Methods: Two oral swabs were collected from the site of the lesion from 132 HIV-infected patients. Oral rinse was obtained from 50 healthy controls. Samples were inoculated on Sabouraud′s dextrose agar (SDA medium and on HiCrome Candida Differential Agar (CHROM agar medium. Isolates were speciated by standard tests. Dark green-colored, germ tube positive isolates, which failed to grow at 420C and negative for xylose assimilation were identified as C. dubliniensis. Antifungal susceptibility test was performed by Macro broth dilution technique (National Committee for Clinical Laboratory Standards guidelines. Results and Conclusions: From 132 patients, 22 (16.3% C. dubliniensis were isolated; samples from healthy controls did not reveal their presence. Antifungal susceptibility test showed higher resistance among C. dubliniensis isolates to azoles compared to C. albicans. Five (22.7% isolates of C. dubliniensis were resistant to Fluconazole followed by four (18.2% to Ketoconazole. This study emphasizes the importance of identification and antifungal susceptibility testing of C. dubliniensis in HIV-infected patients.

  3. Neosordarin and hydroxysordarin, two new antifungal agents from Sordaria araneosa.

    Science.gov (United States)

    Davoli, Paolo; Engel, Günther; Werle, Andreas; Sterner, Olov; Anke, Timm

    2002-04-01

    Two novel antifungal agents belonging to the sordarin family have been isolated from fermentations of Sordaria araneosa by bioassay-guided purification and their structures elucidated by NMR techniques. Neosordarin (1) is closely related to the recently discovered hypoxysordarin (2), with only small differences on the aliphatic side chain acylating the hydroxyl in the 3'-position of the sordarose moiety. Hydroxysordarin (3) closely resembles sordarin (4), the only slight difference being the replacement of sordarose with altrose as the sugar unit.

  4. What Makes Oral Candidiasis Recurrent Infection? A Clinical View

    OpenAIRE

    Azmi M. G. Darwazeh; Tamer A. Darwazeh

    2014-01-01

    Clinical oral Candida infection (candidiasis) is one of the common oral mucosal infections, and its management is usually frustrating due to either treatment failure or recurrence. Historically, oral candidiasis has been branded as disease of diseased. The unsuccessful management of oral candidiasis can due to either incorrect diagnosis, failure to identify (or correct) the underlying predisposing factor(s), or inaccurate prescription of antifungal agents. Failure to properly treat oral ca...

  5. Probiotic Lactobacillus reuteri has antifungal effects on oral Candida species in vitro

    DEFF Research Database (Denmark)

    Jørgensen, Mette Rose; Kragelund, Camilla; Jensen, Peter Østrup

    2017-01-01

    Background: An alternative approach for managing Candida infections in the oral cavity by modulating the oral microbiota with probiotic bacteria has been proposed.  Objective: The aim was to investigate the antifungal potential of the probiotic bacterium Lactobacillus reuteri (DSM 17938 and ATCC...... PTA 5289) against six oral Candida species (C. albicans, C. glabrata, C. krusei, C. tropicalis, C. dubliniensis, and C. parapsilosis).  Design: The lactobacilli were tested for their ability to co-aggregate with and inhibit the growth of the yeasts assessed by spectrophotometry and the agar overlay...... inhibition assay. Additionally, the pH was evaluated with microsensors, and the production of hydrogen peroxide (H2O2) by the lactobacilli was verified.  Results: Both L. reuteri strains showed co-aggregation abilities with the yeasts. The lactobacilli almost completely inhibited the growth of C. albicans...

  6. In vitro interactions of amantadine hydrochloride, R-(-)-deprenyl hydrochloride and valproic acid sodium salt with antifungal agents against filamentous fungal species causing central nervous system infection.

    Science.gov (United States)

    Galgóczy, L; Tóth, Liliána; Virágh, M; Papp, T; Vágvölgyi, C S

    2012-12-01

    The mortality rates of fungal infections that affect the central nervous system are high in consequence of the absence of effective antifungal drugs with good penetration across the blood-brain barrier and the blood-cerebrospinal fluid barrier. In the present work in vitro antifungal activities of three good penetrating non-antifungal drugs (amantadine hydrochloride, R-(-)-deprenyl hydrochloride, valproic acid sodium salt) and their combinations with three antifungal agents (amphotericin B, itraconazole, terbinafine) were tested with broth microdilution method against eight fungal isolates belonging to Zygomycetes (Lichtheimia corymbifera, Rhizomucor miehei, Rhizopus microsporus var. rhizopodiformis, Saksenaeavasiformis) and Aspergillus genus (A. flavus, A. fumigatus, A. nidulans, A. terreus). These are known to be possible agents of central nervous fungal infections (CNFI). When used alone, the investigated nonantifungal drugs exerted slight antifungal effects. In their combinations with antifungal agents they acted antagonistically, additively and synergistically against zygomyceteous isolates. Primarily antagonistic interactions were revealed between the investigated drugs in case of Aspergilli, but additive and synergistic interactions were also observed. The additive and synergistic combinations allowed the usage of reduced concentrations of antifungal agents to inhibit the fungal growth in our study. These combinations would be a basis of an effective, less toxic therapy for treatment of CNFI.

  7. Gene Expression Response of Trichophyton rubrum during Coculture on Keratinocytes Exposed to Antifungal Agents

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    Tatiana Takahasi Komoto

    2015-01-01

    Full Text Available Trichophyton rubrum is the most common causative agent of dermatomycoses worldwide, causing infection in the stratum corneum, nails, and hair. Despite the high prevalence of these infections, little is known about the molecular mechanisms involved in the fungal-host interaction, particularly during antifungal treatment. The aim of this work was to evaluate the gene expression of T. rubrum cocultured with keratinocytes and treated with the flavonoid trans-chalcone and the glycoalkaloid α-solanine. Both substances showed a marked antifungal activity against T. rubrum strain CBS (MIC = 1.15 and 17.8 µg/mL, resp.. Cytotoxicity assay against HaCaT cells produced IC50 values of 44.18 to trans-chalcone and 61.60 µM to α-solanine. The interaction of keratinocytes with T. rubrum conidia upregulated the expression of genes involved in the glyoxylate cycle, ergosterol synthesis, and genes encoding proteases but downregulated the ABC transporter TruMDR2 gene. However, both antifungals downregulated the ERG1 and ERG11, metalloprotease 4, serine proteinase, and TruMDR2 genes. Furthermore, the trans-chalcone downregulated the genes involved in the glyoxylate pathway, isocitrate lyase, and citrate synthase. Considering the urgent need for more efficient and safer antifungals, these results contribute to a better understanding of fungal-host interactions and to the discovery of new antifungal targets.

  8. Antifungal pharmacodynamics: Latin America's perspective

    Directory of Open Access Journals (Sweden)

    Javier M. Gonzalez

    2017-01-01

    Full Text Available The current increment of invasive fungal infections and the availability of new broad-spectrum antifungal agents has increased the use of these agents by non-expert practitioners, without an impact on mortality. To improve efficacy while minimizing prescription errors and to reduce the high monetary cost to the health systems, the principles of pharmacokinetics (PK and pharmacodynamics (PD are necessary. A systematic review of the PD of antifungals agents was performed aiming at the practicing physician without expertise in this field. The initial section of this review focuses on the general concepts of antimicrobial PD. In vitro studies, fungal susceptibility and antifungal serum concentrations are related with different doses and dosing schedules, determining the PD indices and the magnitude required to obtain a specific outcome. Herein the PD of the most used antifungal drug classes in Latin America (polyenes, azoles, and echinocandins is discussed.

  9. Therapeutic strategies with oral fluoropyrimidine anticancer agent, S-1 against oral cancer.

    Science.gov (United States)

    Harada, Koji; Ferdous, Tarannum; Ueyama, Yoshiya

    2017-08-01

    Oral cancer has been recognized as a tumor with low sensitivity to anticancer agents. However, introduction of S-1, an oral cancer agent is improving treatment outcome for patients with oral cancer. In addition, S-1, as a main drug for oral cancer treatment in Japan can be easily available for outpatients. In fact, S-1 exerts high therapeutic effects with acceptable side effects. Moreover, combined chemotherapy with S-1 shows higher efficacy than S-1 alone, and combined chemo-radiotherapy with S-1 exerts remarkable therapeutic effects. Furthermore, we should consider the combined therapy of S-1 and molecular targeting agents right now as these combinations were reportedly useful for oral cancer treatment. Here, we describe our findings related to S-1 that were obtained experimentally and clinically, and favorable therapeutic strategies with S-1 against oral cancer with bibliographic considerations.

  10. Minimal inhibitory concentration distributions and epidemiological cutoff values of five antifungal agents against Sporothrix brasiliensis

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    Rodrigo Almeida-Paes

    Full Text Available BACKGROUND Sporothrix brasiliensis is the most virulent sporotrichosis agent. This species usually responds to antifungal drugs, but therapeutic failure can occur in some patients. Antifungal susceptibility tests have been performed on this species, but no clinical breakpoints (CBPs are available. In this situation, minimal inhibitory concentration (MIC distributions and epidemiological cutoff values (ECVs support the detection of identification of resistant strains. OBJECTIVES To study the MIC distributions of five antifungal drugs against S. brasiliensis and to propose tentative ECVs. METHODS MICs of amphotericin B (AMB, itraconazole (ITR, ketoconazole (KET, posaconazole (POS, and terbinafine (TRB against 335 S. brasiliensis strains were determined by the Clinical and Laboratory Standards Institute broth microdilution method. FINDINGS The proposed ECV, in µg/mL, for AMB, ITR, KET, POS, and TRB were 4.0, 2.0, 1.0, 2.0, and 0.25, respectively. Percentages of wild-type strains in our population for the above antifungal drugs were 98.48, 95.22, 95.33, 100, and 97.67%, respectively. MAIN CONCLUSIONS These ECVs will be useful to detect strains with resistance, to define CBPs, and to elaborate specific therapeutic guidelines for S. brasiliensis. Rational use of antifungals is strongly recommended to avoid the emergence of resistant strains and ensure the therapeutic effectiveness of sporotrichosis.

  11. Sustained release of a novel anti-quorum-sensing agent against oral fungal biofilms.

    Science.gov (United States)

    Feldman, Mark; Shenderovich, Julia; Al-Quntar, Abed Al Aziz; Friedman, Michael; Steinberg, Doron

    2015-04-01

    Thiazolidinedione-8 (S-8) has recently been identified as a potential anti-quorum-sensing/antibiofilm agent against bacteria and fungi. Based on these results, we investigated the possibility of incorporating S-8 in a sustained-release membrane (SRM) to increase its pharmaceutical potential against Candida albicans biofilm. We demonstrated that SRM containing S-8 inhibits fungal biofilm formation in a time-dependent manner for 72 h, due to prolonged release of S-8. Moreover, the SRM effectively delivered the agent in its active form to locations outside the membrane reservoir. In addition, eradication of mature biofilm by the SRM containing S-8 was also significant. Of note, S-8-containing SRM affected the characteristics of mature C. albicans biofilm, such as thickness, exopolysaccharide (EPS) production, and morphogenesis of fungal cells. The concept of using an antibiofilm agent with no antifungal activity incorporated into a sustained-release delivery system is new in medicine and dentistry. This concept of an SRM containing a quorum-sensing quencher with an antibiofilm effect could pave the way for combating oral fungal infectious diseases. Copyright © 2015, American Society for Microbiology. All Rights Reserved.

  12. Antifungal activity of linalool in cases of Candida spp. isolated from individuals with oral candidiasis

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    I. J. Dias

    2017-09-01

    Full Text Available Abstract This study analyzed the antifungal activity of phytoconstituents from linalool on Candida spp. strains, in vitro, isolated from patients with clinical diagnoses of oral candidiasis associated with the use of a dental prosthesis. Biological samples were collected from 12 patients using complete dentures or removable partial dentures and who presented mucous with diffuse erythematous or stippled features, indicating a clinical diagnosis of candidiasis. To identify fungal colonies of the genus Candida, samples were plated onto CHROMagar Candida®. The antifungal activity of linalool, a monoterpene unsaturated constituent of basil oil, was performed using the broth microdilution technique. Then, the minimum inhibitory concentration (MIC, the two subsequent stronger concentrations and the positive controls were subcultured on Sabouraud Dextrose Agar plates to determine the minimum fungicidal concentration (MFC. The experiments were performed in triplicate and nystatin was used as a positive control in all tests. Diagnoses of oral candidiasis were verified in eight patients (66.6% and the most prevalent fungal species was Candida albicans (37.5%, followed by Candida krusei (25.0%; and Candida tropicalis (4.2%. The best antifungal activity of linalool was observed on Candida tropicalis (MIC = 500 mg/mL, followed by Candida albicans (MIC = 1.000 mg/mL, and Candida krusei (MIC = 2.000 mg/mL.Under the study conditions and based on the results obtained, it can be concluded that the Candida strains tested were susceptible to linalool.

  13. An Evaluation of Antifungal Agents for the Treatment of Fungal Contamination in Indoor Air Environments

    OpenAIRE

    Rogawansamy, Senthaamarai; Gaskin, Sharyn; Taylor, Michael; Pisaniello, Dino

    2015-01-01

    Fungal contamination in indoor environments has been associated with adverse health effects for the inhabitants. Remediation of fungal contamination requires removal of the fungi present and modifying the indoor environment to become less favourable to growth.  This may include treatment of indoor environments with an antifungal agent to prevent future growth. However there are limited published data or advice on chemical agents suitable for indoor fungal remediation. The aim of this study wa...

  14. In vitro post-antifungal effect (PAFE) elicited by chlorhexidine gluconate on oral isolates of Candida albicans

    OpenAIRE

    Ellepola, Arjuna N.B.; Samaranayake, Lakshman P.

    2011-01-01

    The post-antifungal effect (PAFE) is defined as the suppression of growth that persists following brief exposure of yeasts and other fungi to antimycotics and subsequent removal of the drug. There is no data available on the PAFE of chlorhexidine gluconate on oral isolates of Candida albicans. As chlorhexidine gluconate is by far the commonest antiseptic mouth wash prescribed in dentistry, the main aim of this investigation was to measure the PAFE of 10 oral isolates of C. albicans following ...

  15. 21 CFR 872.6030 - Oral cavity abrasive polishing agent.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 8 2010-04-01 2010-04-01 false Oral cavity abrasive polishing agent. 872.6030... (CONTINUED) MEDICAL DEVICES DENTAL DEVICES Miscellaneous Devices § 872.6030 Oral cavity abrasive polishing agent. (a) Identification. An oral cavity abrasive polishing agent is a device in paste or powder form...

  16. In vitro antifungal susceptibility of oral candida species from Iranian HIV infected patients

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    Katiraee F

    2012-05-01

    Results: Candida albicans (50.2% was the most frequent isolated yeast, followed by C. glabrata (22%. Non-Candida albicans species were isolated from 71 (61% positive cultures. 25.7% of Candida albicans isolates were resistant to fluconazole (MIC≥64 µg/ml as were 21.9% and 16.4% to ketoconazole and clotrimazole (MIC>0.125 µg/ml, respectively. Resistance to polyene antifungals including amphotericin B and nystatin, and caspofungin were scarce. 57.7% of candida glabrata isolates were resistant to fluconazole, 31% to ketoconazole and 35% to clotrimazole. Conclusion: Screening for antifungal resistant candida isolates by disk diffusion or broth dilution methods in clinical laboratories is an ideal surveillance measure in the management of oral thrush in patients with HIV/AIDS. Although nystatin is widely used in clinical practice for HIV positive patients, there was no evidence of enhanced resistance to it. Regarding no resistance to caspofungin, its administration is suggested.

  17. Evaluation of oral abdominal contrast agent containing ferric ammonium citrate

    International Nuclear Information System (INIS)

    Shiga, Toshiko; Kawamura, Yasutaka; Iwasaki, Toshiko

    1991-01-01

    We evaluated the effectiveness of oral MRI contrast agent containing ferric ammonium citrate. Twenty patients were arbitrarily divided into 2 groups according to the given dose of 100 and 200 mg Fe of oral MRI contrast agent. MRI was performed before and immediately after ingesting 300 ml solution of oral MRI contrast agent using a 1.5 T superconducting system (GE: Signa). Each dose of 100 and 200 mg Fe of oral MRI contrast agent produced sufficient enhancement of gastrointestinal tract, enough to make clear the pancreatic contour and porta hepatis. There was no significant change in blood and urine analysis observed after taking oral MRI contrast agent. The use of ferric ammonium citrate as an oral MRI contrast agent seems to add valuable information in performing upper abdominal MRI imaging. (author)

  18. Defining the frontiers between antifungal resistance, tolerance and the concept of persistence.

    Science.gov (United States)

    Delarze, Eric; Sanglard, Dominique

    2015-11-01

    A restricted number of antifungal agents are available for the therapy of fungal diseases. With the introduction of epidemiological cut-off values for each agent in important fungal pathogens based on the distribution of minimal inhibitory concentration (MIC), the distinction between wild type and drug-resistant populations has been facilitated. Antifungal resistance has been described for all currently available antifungal agents in several pathogens and most of the associated resistance mechanisms have been deciphered at the molecular level. Clinical breakpoints for some agents have been proposed and can have predictive value for the success or failure of therapy. Tolerance to antifungals has been a much more ignored area. By definition, tolerance operates at antifungal concentrations above individual intrinsic inhibitory values. Important is that tolerance to antifungal agents favours the emergence of persister cells, which are able to survive antifungal therapy and can cause relapses. Here we will review the current knowledge on antifungal tolerance, its potential mechanisms and also evaluate the role of antifungal tolerance in the efficacy of drug treatments. Copyright © 2015 Elsevier Ltd. All rights reserved.

  19. New record of Scedosporium dehoogii from Chile: Phylogeny and susceptibility profiles to classic and novel putative antifungal agents.

    Science.gov (United States)

    Alvarez, Eduardo; Sanhueza, Camila

    Scedosporium species are considered emerging agents causing illness in immunocompromised patients. In Chile, only Scedosporium apiospermum, Scedosporium boydii and Lomentospora prolificans haven been reported previously. The study aimed to characterize genetically Scedosporium dehoogii strains from Chilean soil samples, and assessed the antifungal susceptibility profile to classic and novel putative antifungal molecules. In 2014, several samples were obtained during a survey of soil fungi in urban areas from Chile. Morphological and phylogenetic analyses of the internal transcribed spacer region (ITS), tubulin (TUB), and calmodulin (CAL) sequences were performed. In addition, the susceptibility profiles to classic antifungal and new putative antifungal molecules were determined. Four strains of Scedosporium dehoogii were isolated from soil samples. The methodology confirmed the species (reported here as a new record for Chile). Antifungal susceptibility testing demonstrates the low activity of terpenes (α-pinene and geraniol) against this species. Voriconazole (VRC), posaconazole (PSC), and the hydroxyquinolines (clioquinol, and 5,7-dibromo-8-hydroxyquinoline) showed the best antifungal activity. Our results demonstrate that Scedosporium dehoogii is present in soil samples from Chile. This study shows also that hydroxyquinolines have potential as putative antifungal molecules. Copyright © 2016 Asociación Española de Micología. Publicado por Elsevier España, S.L.U. All rights reserved.

  20. Antifungal resistance in mucorales.

    Science.gov (United States)

    Dannaoui, E

    2017-11-01

    The order Mucorales, which includes the agents of mucormycosis, comprises a large number of species. These fungi are characterised by high-level resistance to most currently available antifungal drugs. Standardised antifungal susceptibility testing methods are now available, allowing a better understanding of the in vitro activity of antifungal drugs against members of Mucorales. Such tests have made apparent that antifungal susceptibility within this group may be species-specific. Experimental animal models of mucormycosis have also been developed and are of great importance in bridging the gap between in vitro results and clinical trials. Amphotericin B, posaconazole and isavuconazole are currently the most active agents against Mucorales; however, their activity remains suboptimal and new therapeutic strategies are needed. Combination therapy could be a promising approach to overcome resistance, but further studies are required to confirm its benefits and safety for patients. Copyright © 2017 Elsevier B.V. and International Society of Chemotherapy. All rights reserved.

  1. 2016 guidelines for the use of antifungal agents in patients with invasive fungal diseases in Taiwan

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    Hsiang-Chi Kung

    2018-02-01

    Full Text Available The Infectious Diseases Society of Taiwan, Medical Foundation in Memory of Dr. Deh-Lin Cheng, Foundation of Professor Wei-Chuan Hsieh for Infectious Diseases Research and Education, and CY Lee's Research Foundation for Pediatric Infectious Diseases and Vaccines have updated the guidelines for the use of antifungal agents in adult patients with invasive fungal diseases in Taiwan. This guideline replaces the 2009 version. Recommendations are provided for Candida, Cryptococcus, Aspergillus and Mucormycetes. The focus is based on up-to-date evidence on indications for treatment or prophylaxis of the most common clinical problems. To support the recommendations in this guideline, the committee considered the rationale, purpose, local epidemiology, and key clinical features of invasive fungal diseases to select the primary and alternative antifungal agents. This is the first guideline that explicitly describes the quality and strength of the evidence to support these recommendations. The strengths of the recommendations are the quality of the evidence, the balance between benefits and harms, resource and cost. The guidelines are not intended nor recommended as a substitute for bedside judgment in the management of individual patients, the advice of qualified health care professionals, and more recent evidence concerning therapeutic efficacy and emergence of resistance. Practical considerations for individualized selection of antifungal agents include patient factors, pathogen, site of infection and drug-related factors, such as drug–drug interaction, drug-food intervention, cost and convenience. The guidelines are published in the Journal of Microbiology, Immunology and Infection and are also available on the Society website.

  2. Oral candidiasis following steroid therapy for oral lichen planus.

    Science.gov (United States)

    Marable, D R; Bowers, L M; Stout, T L; Stewart, C M; Berg, K M; Sankar, V; DeRossi, S S; Thoppay, J R; Brennan, M T

    2016-03-01

    The purpose of this multicentre study was to determine the incidence of oral candidiasis in patients treated with topical steroids for oral lichen planus (OLP) and to determine whether the application of a concurrent antifungal therapy prevented the development of an oral candidiasis in these patients. Records of 315 patients with OLP seen at four Oral Medicine practices treated for at least 2 weeks with steroids with and without the use of an antifungal regimen were retrospectively reviewed. The overall incidence of oral fungal infection in those treated with steroid therapy for OLP was 13.6%. There was no statistically significant difference in the rate of oral candidiasis development in those treated with an antifungal regimen vs those not treated prophylactically (14.3% vs 12.6%) (P = 0.68). Despite the use of various regimens, none of the preventive antifungal strategies used in this study resulted in a significant difference in the rate of development of an oral candidiasis in patients with OLP treated with steroids. © 2015 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

  3. Antifungal activity of oral (Tragacanth/acrylic acid) Amphotericin B carrier for systemic candidiasis: in vitro and in vivo study.

    Science.gov (United States)

    Mohamed, Heba A; Radwan, Rasha R; Raafat, Amany I; Ali, Amr El-Hag

    2018-02-01

    In an effort to increase the oral bioavailability of Amphotericin B (AmB), a pH-sensitive drug carrier composed of Tragacanth (Trag) and acrylic acid (AAc) was prepared using γ-irradiation. The swelling behavior of (Trag/AAc) hydrogels was characterized as a function of pH and ionic strength of the swelling medium. The obtained swelling indices revealed the ability of the prepared hydrogel to protect a loaded drug in stomach-simulated medium (Fickian behavior) and to release such drug in intestinal-simulated medium (non-Fickian behavior). In vitro release studies of the antifungal (AmB) were performed to evaluate the hydrogel potential as a drug carrier. The antifungal activity of the prepared oral formulation was investigated in a mouse model of systemic candidiasis. Data revealed that (Trag/AAc)-AmB has a potent antifungal efficacy as demonstrated by prolonging the survival time and reducing the tissue fungal burden, serum antibody titers, as well as inflammatory cytokines in kidney and liver tissues. Furthermore, in vivo toxicity of (Trag/AAc)-AmB was assessed via measuring kidney and liver functions, and results displayed the safety of this novel AmB formulation which was confirmed by histopathological examination. Overall, results indicated that the prepared (Trag/AAc)-AmB is an effective oral delivery system for AmB with better bioavailability and minimal toxicity and could represent a promising approach for improving the therapeutic index of the drug.

  4. Candida Species Biofilms’ Antifungal Resistance

    Science.gov (United States)

    Silva, Sónia; Rodrigues, Célia F.; Araújo, Daniela; Rodrigues, Maria Elisa; Henriques, Mariana

    2017-01-01

    Candida infections (candidiasis) are the most prevalent opportunistic fungal infection on humans and, as such, a major public health problem. In recent decades, candidiasis has been associated to Candida species other than Candida albicans. Moreover, biofilms have been considered the most prevalent growth form of Candida cells and a strong causative agent of the intensification of antifungal resistance. As yet, no specific resistance factor has been identified as the sole responsible for the increased recalcitrance to antifungal agents exhibited by biofilms. Instead, biofilm antifungal resistance is a complex multifactorial phenomenon, which still remains to be fully elucidated and understood. The different mechanisms, which may be responsible for the intrinsic resistance of Candida species biofilms, include the high density of cells within the biofilm, the growth and nutrient limitation, the effects of the biofilm matrix, the presence of persister cells, the antifungal resistance gene expression and the increase of sterols on the membrane of biofilm cells. Thus, this review intends to provide information on the recent advances about Candida species biofilm antifungal resistance and its implication on intensification of the candidiasis. PMID:29371527

  5. Oral Yeast Colonization and Fungal Infections in Peritoneal Dialysis Patients: A Pilot Study

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    Liliana Simões-Silva

    2017-01-01

    Full Text Available Peritonitis and exit-site infections are important complications in peritoneal dialysis (PD patients that are occasionally caused by opportunistic fungi inhabiting distant body sites. In this study, the oral yeast colonization of PD patients and the antifungal susceptibility profile of the isolated yeasts were accessed and correlated with fungal infection episodes in the following 4 years. Saliva yeast colonization was accessed in 21 PD patients and 27 healthy controls by growth in CHROMagar-Candida® and 18S rRNA/ITS sequencing. PD patients presented a lower oral yeast prevalence when compared to controls, namely, Candida albicans. Other species were also isolated, Candida glabrata and Candida carpophila. The antifungal susceptibility profiles of these isolates revealed resistance to itraconazole, variable susceptibility to caspofungin, and higher MIC values of posaconazole compared to previous reports. The 4-year longitudinal evaluation of these patients revealed Candida parapsilosis and Candida zeylanoides as PD-related exit-site infectious agents, but no correlation was found with oral yeast colonization. This pilot study suggests that oral yeast colonization may represent a limited risk for fungal infection development in PD patients. Oral yeast isolates presented a variable antifungal susceptibility profile, which may suggest resistance to some second-line drugs, highlighting the importance of antifungal susceptibility assessment in the clinical practice.

  6. The epidemiology of mycotic vulvovaginitis and the use of antifungal agents in suspected mycotic vulvovaginitis and its implications for clinical practice.

    Science.gov (United States)

    Jackson, S T; Mullings, A M; Rainford, L; Miller, A

    2005-06-01

    Data in the Caribbean documenting the speciation of yeast associated with vulvovaginitis are lacking. The widespread use of antibiotics and increased availability of antimycotic agents, both prescribed and over-the-counter, predisposes both to a change in the epidemiologic patterns and the possible development of secondary resistance among previously susceptible yeast. This study was conducted to evaluate the aetiologic agents associated with mycotic vulvovaginitis and to review the appropriateness of prescribed antifungal therapy. Of 134 positive isolates, the most frequent yeast isolate was C. albicans accounting for 78%, C. tropicalis 10%, Prototheca wickerhamii (P. wickerhamii) 5%, C. glabrata 4%, Cryptococcus albidus (C. albidus) 2% and C. lusitaniae (1%) were also isolated. Of the positive cases, 75% were treated with antifungals, 17% with antibiotics and 8% were not treated. The azole group was the most frequently prescribed antifungal (71%). Of cases with negative yeast cultures, 83% were treated with antifungals. The presence of non-albicans Candida species and other opportunistic fungi is an important finding and combined with the pattern of therapy, represents a major challenge for future empirical therapeutic and prophylactic strategies in the treatment of mycotic vulvovaginitis.

  7. Antifungal activity of redox-active benzaldehydes that target cellular antioxidation

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    Mahoney Noreen

    2011-05-01

    Full Text Available Abstract Background Disruption of cellular antioxidation systems should be an effective method for control of fungal pathogens. Such disruption can be achieved with redox-active compounds. Natural phenolic compounds can serve as potent redox cyclers that inhibit microbial growth through destabilization of cellular redox homeostasis and/or antioxidation systems. The aim of this study was to identify benzaldehydes that disrupt the fungal antioxidation system. These compounds could then function as chemosensitizing agents in concert with conventional drugs or fungicides to improve antifungal efficacy. Methods Benzaldehydes were tested as natural antifungal agents against strains of Aspergillus fumigatus, A. flavus, A. terreus and Penicillium expansum, fungi that are causative agents of human invasive aspergillosis and/or are mycotoxigenic. The yeast Saccharomyces cerevisiae was also used as a model system for identifying gene targets of benzaldehydes. The efficacy of screened compounds as effective chemosensitizers or as antifungal agents in formulations was tested with methods outlined by the Clinical Laboratory Standards Institute (CLSI. Results Several benzaldehydes are identified having potent antifungal activity. Structure-activity analysis reveals that antifungal activity increases by the presence of an ortho-hydroxyl group in the aromatic ring. Use of deletion mutants in the oxidative stress-response pathway of S. cerevisiae (sod1Δ, sod2Δ, glr1Δ and two mitogen-activated protein kinase (MAPK mutants of A. fumigatus (sakAΔ, mpkCΔ, indicates antifungal activity of the benzaldehydes is through disruption of cellular antioxidation. Certain benzaldehydes, in combination with phenylpyrroles, overcome tolerance of A. fumigatus MAPK mutants to this agent and/or increase sensitivity of fungal pathogens to mitochondrial respiration inhibitory agents. Synergistic chemosensitization greatly lowers minimum inhibitory (MIC or fungicidal (MFC

  8. Design, synthesis and molecular docking study of thienopyrimidin-4(3H-thiones as antifungal agents

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    Sanjay B. Bari

    2017-01-01

    Full Text Available In an attempt to find a new class of antimicrobial agents, a series of thienopyrimidin-4(3H-thiones 4(H1–H36 were synthesized and evaluated for in vitro antifungal activity against Candida albicans (NCIM 3471, Aspergillus niger (NCIM 545, and Penicillium chrysogenum (NCIM 709. The title compounds were synthesized by thionation of thienopyrimidin-4(3H-ones 3(H1–H36 using Lawesson’s reagent. All the compounds were characterized using elemental analytical (C, H, and N and spectral (FT-IR, 1H NMR, 13C NMR and MS data. Among the tested compounds, 5-(4-chlorophenyl-2-(pyridin-3-ylthieno[2,3-d]pyrimidine-4(3H-thione 4(H11, 2-sulfanyl-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine-4(3H-thione 4(H18, and 2-(butylsulfanyl-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine-4(3H-thione 4(H32 were identified as potentially excellent antifungal agents. They exhibited potent antifungal activity against C. albicans (MIC; 4 μg/mL, A. niger (MIC; 2 μg/mL, and P. chrysogenum (MIC; 2 μg/mL comparable with that of ketoconazole. The binding mode of compounds by SP docking studies shows that it fits well into the active site cavity of DHFR. Lipinski’s rule and in silico ADME pharmacokinetic parameters are within the acceptable range defined for human use thereby indicating their potential as drug-like molecules.

  9. Gestational Diabetes Mellitus Management with Oral Hypoglycemic Agents

    Science.gov (United States)

    Ryu, Rachel J.; Hays, Karen E.; Hebert, Mary F.

    2014-01-01

    Oral hypoglycemic agents such as glyburide (second generation sulfonylurea) and metformin (biguanide) are attractive alternatives to insulin due to lower cost, ease of administration, and better patient adherence. The majority of evidence from retrospective and prospective studies suggests comparable efficacy and safety of oral hypoglycemic agents such as glyburide and metformin as compared to insulin when used in the treatment of women with gestational diabetes mellitus (GDM). Glyburide and metformin have altered pharmacokinetics during pregnancy and both agents cross the placenta. In this article, we review the efficacy, safety and dosage of oral hypoglycemic agents for the treatment of gestational diabetes mellitus. Additional research is needed to evaluate optimal dosage for glyburide and metformin during pregnancy. Comparative studies evaluating the effects of glyburide and metformin on long-term maternal and fetal outcomes are also needed. PMID:25315294

  10. Potato dextrose agar antifungal susceptibility testing for yeasts and molds: evaluation of phosphate effect on antifungal activity of CMT-3.

    Science.gov (United States)

    Liu, Yu; Tortora, George; Ryan, Maria E; Lee, Hsi-Ming; Golub, Lorne M

    2002-05-01

    The broth macrodilution method (BMM) for antifungal susceptibility testing, approved by the National Committee for Clinical Laboratory Standards (NCCLS), was found to have deficiencies in testing of the antifungal activity of a new type of antifungal agent, a nonantibacterial chemically modified tetracycline (CMT-3). The high content of phosphate in the medium was found to greatly increase the MICs of CMT-3. To avoid the interference of phosphate in the test, a new method using potato dextrose agar (PDA) as a culture medium was developed. Eight strains of fungi, including five American Type Culture Collection strains and three clinical isolates, were used to determine the MICs of amphotericin B and itraconazole with both the BMM and the PDA methods. The MICs of the two antifungal agents determined with the PDA method showed 99% agreement with those determined with the BMM method within 1 log(2) dilution. Similarly, the overall reproducibility of the MICs with the PDA method was above 97%. Three other antifungal agents, fluconazole, ketoconazole, and CMT-3, were also tested in parallel against yeasts and molds with both the BMM and the PDA methods. The MICs of fluconazole and ketoconazole determined with the PDA method showed 100% agreement within 1 log(2) dilution of those obtained with the BMM method. However, the MICs of CMT-3 determined with the BMM method were as high as 128 times those determined with the PDA method. The effect of phosphate on the antifungal activity of CMT-3 was evaluated by adding Na2HPO4 to PDA in the new method. It was found that the MIC of CMT-3 against a Penicillium sp. increased from 0.5 microg/ml (control) to 2.0 microg/ml when the added phosphate was used at a concentration of 0.8 mg/ml, indicating a strong interference of Na2HPO4 with the antifungal activity of CMT-3. Except for fluconazole, all the other antifungal agents demonstrated clear end points among the yeasts and molds tested. Nevertheless, with its high reproducibility

  11. Susceptibility to antifungal agents of Candida spp. from blood and feces collected in Novi Sad in 3-year period (2008-2010

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    Jelesić Zora Z.

    2011-01-01

    Full Text Available Candidemia is an important emerging nosocomial infection in patients with risk factors. Candida species from nonsterile sites can give insight into the characteristics of strains that may cause invasive disease. The aim of this study was to evaluate antifungal susceptibility of Candida blood and fecal isolates in Novi Sad, Vojvodina. During a 3-year period (2008 to 2010, 424 isolates of Candida spp. were collected, 30 bloodstream isolates and 394 strains from fecal samples. In vitro susceptibility of these isolates to five antifungal agents was established using commercial ATB FUNGUS 3 (Bio-Mérieux. Predominant species was Candida albicans (6 isolates from blood and 269 from feces. Resistance to one or more antifungal agents was less common in Candida albicans (3.63% than in other species (24.83%. Resistance to itraconazole was the most commonly found in both groups of isolates, 9.64% strains from feces and 20% from blood samples. Twelve isolates were multiply resistant, usually to fluconazole, itraconazole, and voriconazole. Resistance to amphotericine B was extremely rare. Although resistance to antimycotics of Candida spp. is rare at present, continued surveillance of antifungal susceptibility is necessary in order to monitor trends, and to choose the right empiric therapy.

  12. Terbinafine: novel formulations that potentiate antifungal activities.

    Science.gov (United States)

    Ma, Y; Chen, X; Guan, S

    2015-03-01

    Terbinafine, an orally and topically active antifungal agent, has been available for the treatment of dermatophytic infections and onychomycosis for more than a decade. In addition, oral administration has been shown to be associated with drug-drug interactions, hepatotoxicity, low concentration at the infected sites, gastrointestinal and systemic side effects and other adverse effects. Since topical drug delivery can provide higher patient compliance, allow immediate access to the infected site and reduce unwanted systemic drug exposure, an improved topical drug delivery approach with high permeability, sustained release and prolonged retainment could overcome the limitations and side effects caused by oral administration. Conventional topical formulations cannot keep the drug in the targeted sites for a long duration of time and hence a novel drug delivery that can avoid the side effects while still providing sustained efficacy in treatment should be developed. This brief review of novel formulations based on polymers and nanostructure carriers provides insight into the efficacy and topical delivery of terbinafine. Copyright 2015 Prous Science, S.A.U. or its licensors. All rights reserved.

  13. Potential Applications and Antifungal Activities of Engineered Nanomaterials against Gray Mold Disease Agent Botrytis cinerea on Rose Petals

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    Yi Hao

    2017-08-01

    Full Text Available Nanoparticles (NPs have great potential for use in the fields of biomedicine, building materials, and environmental protection because of their antibacterial properties. However, there are few reports regarding the antifungal activities of NPs on plants. In this study, we evaluated the antifungal roles of NPs against Botrytis cinerea, which is a notorious worldwide fungal pathogen. Three common carbon nanomaterials, multi-walled carbon nanotubes, fullerene, and reduced graphene oxide, and three commercial metal oxidant NPs, copper oxide (CuO NPs, ferric oxide (Fe2O3 NPs, and titanium oxides (TiO2 NPs, were independently added to water-agar plates at 50 and 200-mg/L concentrations. Detached rose petals were inoculated with spores of B. cinerea and co-cultured with each of the six nanomaterials. The sizes of the lesions on infected rose petals were measured at 72 h after inoculation, and the growth of fungi on the rose petals was observed by scanning electron microscopy. The six NPs inhibited the growth of B. cinerea, but different concentrations had different effects: 50 mg/L of fullerene and CuO NPs showed the strongest antifungal properties among the treatments, while 200 mg/L of CuO and Fe2O3 showed no significant antifungal activities. Thus, NPs may have antifungal activities that prevent B. cinerea infections in plants, and they could be used as antifungal agents during the growth and post-harvesting of roses and other flowers.

  14. Genetic diversity and antifungal susceptibility profiles in causative agents of sporotrichosis

    Science.gov (United States)

    2014-01-01

    Background Sporotrichosis is a chronic subcutaneous mycosis of humans and animals, which is typically acquired by traumatic inoculation of plant material contaminated with Sporothrix propagules, or via animals, mainly felines. Sporothrix infections notably occur in outbreaks, with large epidemics currently taking place in southeastern Brazil and northeastern China. Pathogenic species include Sporothrix brasiliensis, Sporothrix schenckii s. str., Sporothrix globosa, and Sporothrix luriei, which exhibit differing geographical distribution, virulence, and resistance to antifungals. The phylogenetically remote species Sporothrix mexicana also shows a mild pathogenic potential. Methods We assessed a genetically diverse panel of 68 strains. Susceptibility profiles of medically important Sporothrix species were evaluated by measuring the MICs and MFCs for amphotericin B (AMB), fluconazole (FLC), itraconazole (ITC), voriconazole (VRC), posaconazole (PCZ), flucytosine (5FC), and caspofungin (CAS). Haplotype networks were constructed to reveal interspecific divergences within clinical Sporothrix species to evaluate genetically deviant isolates. Results ITC and PCZ were moderately effective against S. brasiliensis (MIC90 = 2 and 2 μg/mL, respectively) and S. schenckii (MIC90 = 4 and 2 μg/mL, respectively). PCZ also showed low MICs against the rare species S. mexicana. 5FC, CAS, and FLC showed no antifungal activity against any Sporothrix species. The minimum fungicidal concentration ranged from 2 to >16 μg/mL for AMB against S. brasiliensis and S. schenckii, while the MFC90 was >16 μg/mL for ITC, VRC, and PCZ. Conclusion Sporothrix species in general showed high degrees of resistance against antifungals. Evaluating a genetically diverse panel of strains revealed evidence of multidrug resistant phenotypes, underlining the need for molecular identification of etiologic agents to predict therapeutic outcome. PMID:24755107

  15. In vitro antifungal effect of mouth rinses containing chlorhexidine and thymol

    Directory of Open Access Journals (Sweden)

    Ashish Shrestha

    2011-03-01

    Conclusions: Antimicrobial agents used in the study had good in vitro activity against the two Candida species. Mouth rinses containing chlorhexidine showed superior antifungal and fungicidal activities compared to the thymol-containing mouth rinse. Both antimicrobial agents may be suggested for use as topical antifungal agents.

  16. In vitro activity of econazole in comparison with three common antifungal agents against clinical Candida strains isolated from superficial infections

    Directory of Open Access Journals (Sweden)

    Mahdi Abastabar

    2015-03-01

    Conclusion: The present study demonstrated that for Candida albicans isolates, miconazole and econazole had the best effect, but in non-albicans Candida species, itraconazole and miconazole displayed more activity than other antifungal agents.

  17. Effect of 2-Phenylethanol as Antifungal Agent and Common Antifungals (Amphotericin B, Fluconazole, and Itraconazole) on Candida Species Isolated from Chronic and Recurrent Cases of Candidal Vulvovaginitis.

    Science.gov (United States)

    Majdabadi, Niloufar; Falahati, Mehraban; Heidarie-Kohan, Fariba; Farahyar, Shirin; Rahimi-Moghaddam, Parvaneh; Ashrafi-Khozani, Mahtab; Razavi, Tandis; Mohammadnejad, Sina

    2018-04-01

    The antifungal effects of 2-phenylethanol are clearly visible through its intervention in Candida morphogenesis. Chronic and recurrent vulvovaginitis, however, does not respond to this standard experimental therapy; therefore, the study presented in this article investigated the effect of common antifungal drugs (amphotericin B [AMB], fluconazole [FLU], and itraconazole [ITC]), in combination with 2-phenylethanol, on the Candida species isolated from cases of chronic and recurrent vulvovaginitis, thereby allowing the recommendation of a more appropriate treatment option. Forty isolates from patients with chronic and recurrent vaginal candidiasis were investigated in this experimental study. The specimens were examined by direct microscopy, culturing, and PCR to identify the species. The antifungal effects of 2-phenylethanol and conventional drugs, both alone and in combination, were determined in duplicate. Finally, the findings were analyzed. In this study, 40 strains of Candida species were identified, whose agents were Candida albicans (95%) and Candida africana (5%). After 48 h, the minimum inhibitory concentration (MIC) range of the 2-phenylethanol was 800-3,200 μg/mL. Also, in the final study on the MIC levels of common antifungal drugs, AMB (0.42 μg/mL) had the lowest MIC, FLU (40.51 μg/mL) had the highest MIC, and the combination of ITC and 2-phenylethanol had the lowest fractional inhibitory concentration index (FICI) of any of the combinations (FICI range, 0.26-1.03). Combining FLU and ITC with 2-phenylethanol can effectively increase their antifungal effect.

  18. Mixtures of Quaternary Ammonium Compounds and Long-chain Fatty Acids as Antifungal Agents

    Science.gov (United States)

    Kull, F. C.; Eisman, P. C.; Sylwestrowicz, H. D.; Mayer, R. L.

    1961-01-01

    The influence of undecylenic acid on the fungistatic effect of phenoxyethyldimethyldodecylammonium bromide (Domiphen bromide) against Trichophyton mentagrophytes was investigated. The unsaturated fatty acid was found to enhance the fungistatic activity of Domiphen bromide against this organism. The ratio of concentrations of these agents has a marked influence on the results of in vitro tests for antifungal action resulting in a completely different effect than heretofore noted in combination experiments against bacteria. The enhancing phenomenon is not particular to T. mentagrophytes, it was observed also with Candida albicans. PMID:14460466

  19. Scaling adult doses of antifungal and antibacterial agents to children.

    Science.gov (United States)

    Dawson, Thomas H

    2012-06-01

    My general pharmacokinetic scaling theory is discussed for the important matter of determining pediatric dosing for existing and new therapeutic drugs when optimal, or near-optimal, dosing for adults is known. The basis for the scaling is the requirement of a time-scaled likeness of the free-drug concentration time histories of children and adults. Broad categories of single and periodic dosing are considered. The former involves the scaling of dosage, and the latter involves both the dosage and schedule. The validity of the scaling relations is demonstrated by using measurements from previously reported clinical trials with adults and children (with ages generally 1 year or older) for the relatively new antifungal agent caspofungin and for the relatively new antibacterial agent linezolid. Standard pharmacodynamic effectiveness criteria are shown to be satisfied for the scaled dosage and schedule for children to the same extent that they are for the referenced adult. Consideration of scaling from adults to children is discussed for the case of new agents where no pediatric data are available and needed parameters are determined from in vitro measurements and preclinical animal data. A connection is also made between the allometric representation of clearance data and the dosing formulas. Limitations of the scaling results for infants because of growth and maturational matters are discussed. The general conclusion from this work is that the scaling theory does indeed have application to pediatric dosing for children, for both confirmation and refinement of present practice and guidance in pediatric treatment with new therapeutic agents.

  20. Combination of Estrogen and Immunosuppressive Agents to Establish a Mouse Model of Candidiasis with Concurrent Oral and Vaginal Mucosal Infection.

    Science.gov (United States)

    Wang, Le; Wang, Chong; Mei, Huan; Shen, Yongnian; Lv, Guixia; Zeng, Rong; Zhan, Ping; Li, Dongmei; Liu, Weida

    2016-02-01

    Mouse model is an appropriate tool for pathogenic determination and study of host defenses during the fungal infection. Here, we established a mouse model of candidiasis with concurrent oral and vaginal mucosal infection. Two C. albicans strains sourced from clinical candidemia (SC5314) and mucosal infection (ATCC62342) were tested in ICR mice. The different combinational panels covering estrogen and immunosuppressive agents, cortisone, prednisolone and cyclophosphamide were used for concurrent oral and vaginal candidiasis establishment. Prednisolone in combination with estrogen proved an optimal mode for concurrent mucosal infection establishment. The model maintained for 1 week with fungal burden reached at least 10(5) cfu/g of tissue. This mouse model was evaluated by in vivo pharmacodynamics of fluconazole and host mucosal immunity of IL-17 and IL-23. Mice infected by SC5314 were cured by fluconazole. An increase in IL-23 in both oral and vaginal homogenates was observed after infection, while IL-17 only had a prominent elevation in oral tissue. This model could properly mimic complicated clinical conditions and provides a valuable means for antifungal assay in vivo and may also provide a useful method for the evaluation of host-fungal interactions.

  1. Oral yeast carriage in HIV-infected and non-infected populations in Rosario, Argentina.

    Science.gov (United States)

    Luque, A G; Biasoli, M S; Tosello, M E; Binolfi, A; Lupo, S; Magaró, H M

    2009-01-01

    The objectives of the present study were: (i) to assess the frequency of oral colonisation by Candida species in HIV-positive patients and to compare it with a population of HIV-negative individuals, (ii) to determine the prevalence of C. dubliniensis in both populations and (iii) to determine the susceptibility of C. dubliniensis and other Candida species isolated from HIV-positive patients to the most commonly used antifungal agents. Oral samples were obtained from 101 HIV-positive and 108 HIV-negative subjects. For yeast identification, we used morphology in cornmeal agar, the API 20C Aux, growth at 45 degrees C, d-xylose assimilation, morphology in sunflower seed agar and PCR. The frequency of isolation of Candida in HIV-positive patients was: C. albicans, 60.7%; C. dubliniensis, 20.2%; C. glabrata, 5.6%; C. krusei, 5.6%; C. tropicalis, 4.5%; others, <5%. The frequency of isolation of Candida in HIV-negative patients was: C. albicans, 73.9%; C. tropicalis, 15.5%; C. dubliniensis, 2.1%; C. glabrata, 2.1%; C. parapsilosis, 2.1%; others, <5%. The oral colonisation by yeast in the HIV-positive patients was higher than that in the HIV-negative subjects. The susceptibilities of 42 Candida isolates to three antifungal agents were determined. All isolates of C. dubliniensis were susceptible to fluconazole, although several individuals had been previously treated with this drug. Out of the 42 Candida isolates, 10 presented resistance to fluconazole and 10 to itraconazole. The presence of Candida species, resistant to commonly used antifungal agents, represents a potential risk in immunocompromised patients.

  2. Antifungal Screening of Bridelia ferruginea Benth (Euphorbiaceae Stem Bark Extract in Mouthwash Formulations

    Directory of Open Access Journals (Sweden)

    Aremu Olusola Isaac

    2017-06-01

    Full Text Available The plant Bridelia ferruginea Benth (Euphorbiaceae has been known for its use in the management of oral thrush ethnomedicinally in various parts of Africa, a practice which has been justified by results of certain scientific studies. The aim of this study was to develop an appropriate dosage formulation, a mouthwash and evaluate the antifungal potential of this dosage formulation against a major causative organism of oral thrush, Candida albicans. Extraction of the stem bark was carried out with boiled distilled water, the extract was formulated into mouthwashes at concentrations of 0.5, 1.0, 1.5, 2.0 and 2.5%w/v. All formulations contained viscosity imparting agent, a sweetener and a preservative. Physical characterisation, viscosity, pH and palatability of the mouthwash formulations were determined. Agar-well diffusion method was used to assess antifungal activity of the formulations against Candida albicans and Nystatin oral suspension was used as reference compound. The results showed that Bridelia ferruginea stem bark extract mouthwash solutions were brown in colour, had agreeable odour and sweet astringent taste. The pH for all concentrations was in the range 5.41-5.63. The viscosity at spindle no 2, 60rpm range between 0.226-0.238 Pa.S for all concentrations studied. The formulations had antifungal activity against Candida albicans. The highest concentration (2.5%w/v gave mean zone of inhibition of 25.50±0.71mm that was comparable with Nystatin oral suspension 28.00±1.41mm, a reference compound. The foregoing suggests that with little modification in the formulation especially the adjustment of the pH, Bridellia ferruginea mouthwash solutions may be developed into commercially useful preparations.

  3. Antifungal effect and action mechanism of antimicrobial peptide polybia-CP.

    Science.gov (United States)

    Wang, Kairong; Jia, Fengjing; Dang, Wen; Zhao, Yanyan; Zhu, Ranran; Sun, Mengyang; Qiu, Shuai; An, Xiaoping; Ma, Zelin; Zhu, Yuanyuan; Yan, Jiexi; Kong, Ziqing; Yan, Wenjin; Wang, Rui

    2016-01-01

    The incidence of life-threatening invasive fungal infections increased significantly in recent years. However, the antifungal therapeutic options are very limited. Antimicrobial peptides are a class of potential lead chemical for the development of novel antifungal agents. Antimicrobial peptide polybia-CP was purified from the venom of the social wasp Polybia paulista. In this study, we synthesized polybia-CP and determined its antifungal effects against a series of Candidian species. Our results showed that polybia-CP has potent antifungal activity and fungicidal activity against the tested fungal cells with a proposed membrane-active action mode. In addition, polybia-CP could induce the increase of cellular reactive oxygen species production, which would attribute to its antifungal activity. In conclusion, the present study suggests that polybia-CP has potential as an antifungal agent or may offer a new strategy for antifungal therapeutic option. Copyright © 2015 European Peptide Society and John Wiley & Sons, Ltd.

  4. Candidiasis and the impact of flow cytometry on antifungal drug discovery.

    Science.gov (United States)

    Ku, Tsun Sheng N; Bernardo, Stella; Walraven, Carla J; Lee, Samuel A

    2017-11-01

    Invasive candidiasis continues to be associated with significant morbidity and mortality as well as substantial health care costs nationally and globally. One of the contributing factors is the development of resistance to antifungal agents that are already in clinical use. Moreover, there are known treatment limitations with all of the available antifungal agents. Since traditional techniques in novel drug discovery are time consuming, high-throughput screening using flow cytometry presents as a potential tool to identify new antifungal agents that would be useful in the management of these patients. Areas covered: In this review, the authors discuss the use of automated high-throughput screening assays based upon flow cytometry to identify potential antifungals from a library comprised of a large number of bioactive compounds. They also review studies that employed the use of this research methodology that has identified compounds with antifungal activity. Expert opinion: High-throughput screening using flow cytometry has substantially decreased the processing time necessary for screening thousands of compounds, and has helped enhance our understanding of fungal pathogenesis. Indeed, the authors see this technology as a powerful tool to help scientists identify new antifungal agents that can be added to the clinician's arsenal in their fight against invasive candidiasis.

  5. Lactobacillus amylovorus DSM 19280 as a novel food-grade antifungal agent for bakery products.

    Science.gov (United States)

    Ryan, Liam A M; Zannini, Emanuele; Dal Bello, Fabio; Pawlowska, Agata; Koehler, Peter; Arendt, Elke K

    2011-04-29

    Mould spoilage is the main cause of substantial economic loss in bakery industry and might also cause public health problems due to the production of mycotoxins. The reduction of mould growth in bakery products is thus of crucial importance and there is great interest to develop safe and efficient strategies for this purpose. In this study Lactobacillus amylovorus DSM19280 has been shown to produce a wide spectrum of antifungal compounds active against common bread spoilage fungi. Among the indicator moulds, Aspergillus fumigatus and Fusarium culmorum were the most sensitive organisms. Several antifungal compounds were found to be present in synthetic medium inoculated with L. amylovorus DSM19280 strain, some of them being reported here for the first time. Wheat doughs fermented with L. amylovorus DSM19280 had good rheological properties and the breads thereof were of high quality as shown by rheofermentometer and texture analyser measurements. The results were compared with those obtained with a control non-antifungal L. amylovorus DSM20531(T) strain, a non-acidified and a chemically acidified dough. The quality of sourdough and bread fermented with L. amylovorus DSM 19280 was comparable to that obtained by using L. amylovorus DSM20531 (T). Additionally, breads were evaluated for the ability to retard the growth of Fusarium culmorum FST 4.05, Aspergillus niger FST4.21, Penicillium expansum FST 4.22, Penicillium roqueforti FST 4.11 and fungal flora from the bakery environment. The biological preservation of bread with L. amylovorus DSM 19280 was also compared to the most commonly used antifungal agent Calcium propionate. Breads containing sourdough fermented with L. amylovorus DSM 19280 were more effective in extending the shelf life of bread than the calcium propionate. Copyright © 2011 Elsevier B.V. All rights reserved.

  6. Synthesis and preliminary evaluation of N-acylhydrazone compounds as antibacterial and antifungal agents

    International Nuclear Information System (INIS)

    Cachiba, Thomas Haruo; Carvalho, Bruno Demartini; Carvalho, Diogo Teixeira; Cusinato, Marina; Prado, Clara Gaviao; Dias, Amanda Latercia Tranches

    2012-01-01

    We describe the synthesis and evaluation of N-acylhydrazone compounds bearing different electron-donating groups in one of its aromatic rings, obtained using a four-step synthetic route. IC 50 values against pathogenic fungi and bacteria were determined by serial microdilution. Compounds showed low activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. By contrast, a derivative with a meta-oriented electron-donating group showed significant activity (IC50) against Candida albicans (17 μM), C. krusei (34 μM) and C. tropicalis (17 μM). Results suggest this is a promising lead-compound for synthesis of potent antifungal agents. (author)

  7. Species distribution and in vitro antifungal susceptibility of oral yeast isolates from Tanzanian HIV-infected patients with primary and recurrent oropharyngeal candidiasis.

    NARCIS (Netherlands)

    Hamza, O.J.M.; Matee, M.I.N.; Moshi, M.J.; Simon, E.N.; Mugusi, F.; Mikx, F.H.M.; Palenstein Helderman, W.H. van; Rijs, A.J.M.M.; Ven, A.J.A.M. van der; Verweij, P.E.

    2008-01-01

    BACKGROUND: In Tanzania, little is known on the species distribution and antifungal susceptibility profiles of yeast isolates from HIV-infected patients with primary and recurrent oropharyngeal candidiasis. METHODS: A total of 296 clinical oral yeasts were isolated from 292 HIV-infected patients

  8. Epidemiology and antifungal resistance in invasive candidiasis

    Directory of Open Access Journals (Sweden)

    Rodloff AC

    2011-04-01

    Full Text Available Abstract The epidemiology of Candida infections has changed over the last two decades: The number of patients suffering from such infections has increased dramatically and the Candida species involved have become more numerous as Candida albicans is replaced as an infecting agent by various non-C. albicans species (NAC. At the same time, additional antifungal agents have become available. The different Candida species may vary in their susceptibility for these various antifungals. This draws more attention to in vitro susceptibility testing. Unfortunately, several different test methods exist that may deliver different results. Moreover, clinical breakpoints (CBP that classify test results into susceptible, intermediate and resistant are controver- sial between CLSI and EUCAST. Therefore, clinicians should be aware that interpretations may vary with the test system being followed by the microbiological laboratory. Thus, knowledge of actual MIC values and pharmacokinetic properties of individual antifungal agents is important in delivering appropriate therapy to patients

  9. Effect of chitosan and its derivatives as antifungal and preservative agents on postharvest green asparagus.

    Science.gov (United States)

    Qiu, Miao; Wu, Chu; Ren, Gerui; Liang, Xinle; Wang, Xiangyang; Huang, Jianying

    2014-07-15

    The antifungal activity and effect of high-molecular weight chitosan (H-chitosan), low-molecular weight chitosan (L-chitosan) and carboxymethyl chitosan (C-chitosan) coatings on postharvest green asparagus were evaluated. L-chitosan and H-chitosan efficiently inhibited the radial growth of Fusarium concentricum separated from postharvest green asparagus at 4 mg/ml, which appeared to be more effective in inhibiting spore germination and germ tube elongation than that of C-chitosan. Notably, spore germination was totally inhibited by L-chitosan and H-chitosan at 0.05 mg/ml. Coated asparagus did not show any apparent sign of phytotoxicity and maintained good quality over 28 days of cold storage, according to the weight loss and general quality aspects. Present results inferred that chitosan could act as an attractive preservative agent for postharvest green asparagus owing to its antifungal activity and its ability to stimulate some defense responses during storage. Copyright © 2014 Elsevier Ltd. All rights reserved.

  10. Sensitivity of Candida albicans to essential oils: are they an alternative to antifungal agents?

    Science.gov (United States)

    Bona, E; Cantamessa, S; Pavan, M; Novello, G; Massa, N; Rocchetti, A; Berta, G; Gamalero, E

    2016-12-01

    Candida albicans is an important opportunistic pathogen, responsible for the majority of yeast infections in humans. Essential oils, extracted from aromatic plants, are well-known antimicrobial agents, characterized by a broad spectrum of activities, including antifungal properties. The aim of this work was to assess the sensitivity of 30 different vaginal isolated strains of C. albicans to 12 essential oils, compared to the three main used drugs (clotrimazole, fluconazole and itraconazole). Thirty strains of C. albicans were isolated from vaginal swab on CHROMagar ™ Candida. The agar disc diffusion method was employed to determine the sensitivity to the essential oils. The antifungal activity of the essential oils and antifungal drugs (clotrimazole, itraconazole and fluconazole) were investigated using a microdilution method. Transmission and scanning electron microscopy analyses were performed to get a deep inside on cellular damages. Mint, basil, lavender, tea tree oil, winter savory and oregano essential oils inhibited both the growth and the activity of C. albicans more efficiently than clotrimazole. Damages induced by essential oils at the cellular level were stronger than those caused by clotrimazole. Candida albicans is more sensitive to different essential oils compared to the main used drugs. Moreover, the essential oil affected mainly the cell wall and the membranes of the yeast. The results of this work support the research for new alternatives or complementary therapies against vaginal candidiasis. © 2016 The Society for Applied Microbiology.

  11. Models hosts for the study of oral candidiasis.

    Science.gov (United States)

    Junqueira, Juliana Campos

    2012-01-01

    Oral candidiasis is an opportunistic infection caused by yeast of the Candida genus, primarily Candida albicans. It is generally associated with predisposing factors such as the use of immunosuppressive agents, antibiotics, prostheses, and xerostomia. The development of research in animal models is extremely important for understanding the nature of the fungal pathogenicity, host interactions, and treatment of oral mucosal Candida infections. Many oral candidiasis models in rats and mice have been developed with antibiotic administration, induction of xerostomia, treatment with immunosuppressive agents, or the use of germ-free animals, and all these models has both benefits and limitations. Over the past decade, invertebrate model hosts, including Galleria mellonella, Caenorhabditis elegans, and Drosophila melanogaster, have been used for the study of Candida pathogenesis. These invertebrate systems offer a number of advantages over mammalian vertebrate models, predominantly because they allow the study of strain collections without the ethical considerations associated with studies in mammals. Thus, the invertebrate models may be useful to understanding of pathogenicity of Candida isolates from the oral cavity, interactions of oral microorganisms, and study of new antifungal compounds for oral candidiasis.

  12. Quantitative structure-activity relationship of some 1-benzylbenzimidazole derivatives as antifungal agents

    Directory of Open Access Journals (Sweden)

    Podunavac-Kuzmanović Sanja O.

    2007-01-01

    Full Text Available In the present study, the antifungal activity of some 1-benzylbenzimidazole derivatives against yeast Saccharomyces cerevisiae was investigated. The tested benzimidazoles displayed in vitro antifungal activity and minimum inhibitory concentration (MIC was determined for all the compounds. Quantitative structure-activity relationship (QSAR has been used to study the relationships between the antifungal activity and lipophilicity parameter, logP, calculated by using CS Chem-Office Software version 7.0. The results are discussed on the basis of statistical data. The best QSAR model for prediction of antifungal activity of the investigated series of benzimidazoles was developed. High agreement between experimental and predicted inhibitory values was obtained. The results of this study indicate that the lipophilicity parameter has a significant effect on antifungal activity of this class of compounds, which simplify design of new biologically active molecules.

  13. Activity of Potent and Selective Host Defense Peptide Mimetics in Mouse Models of Oral Candidiasis

    Science.gov (United States)

    Ryan, Lisa K.; Freeman, Katie B.; Masso-Silva, Jorge A.; Falkovsky, Klaudia; Aloyouny, Ashwag; Markowitz, Kenneth; Hise, Amy G.; Fatahzadeh, Mahnaz; Scott, Richard W.

    2014-01-01

    There is a strong need for new broadly active antifungal agents for the treatment of oral candidiasis that not only are active against many species of Candida, including drug-resistant strains, but also evade microbial countermeasures which may lead to resistance. Host defense peptides (HDPs) can provide a foundation for the development of such agents. Toward this end, we have developed fully synthetic, small-molecule, nonpeptide mimetics of the HDPs that improve safety and other pharmaceutical properties. Here we describe the identification of several HDP mimetics that are broadly active against C. albicans and other species of Candida, rapidly fungicidal, and active against yeast and hyphal cultures and that exhibit low cytotoxicity for mammalian cells. Importantly, specificity for Candida over commensal bacteria was also evident, thereby minimizing potential damage to the endogenous microbiome which otherwise could favor fungal overgrowth. Three compounds were tested as topical agents in two different mouse models of oral candidiasis and were found to be highly active. Following single-dose administrations, total Candida burdens in tongues of infected animals were reduced up to three logs. These studies highlight the potential of HDP mimetics as a new tool in the antifungal arsenal for the treatment of oral candidiasis. PMID:24752272

  14. Nosocomial Candidiasis: Antifungal Stewardship and the Importance of Rapid Diagnosis.

    Science.gov (United States)

    Pfaller, Michael A; Castanheira, Mariana

    2016-01-01

    Candidemia and other forms of candidiasis are associated with considerable excess mortality and costs. Despite the addition of several new antifungal agents with improved spectrum and potency, the frequency of Candida infection and associated mortality have not decreased in the past two decades. The lack of rapid and sensitive diagnostic tests has led to considerable overuse of antifungal agents resulting in increased costs, selection pressure for resistance, unnecessary drug toxicity, and adverse drug interactions. Both the lack of timely diagnostic tests and emergence of antifungal resistance pose considerable problems for antifungal stewardship. Whereas antifungal stewardship with a focus on nosocomial candidiasis should be able to improve the administration of antifungal therapy in terms of drug selection, proper dose and duration, source control and de-escalation therapy, an important parameter, timeliness of antifungal therapy, remains a victim of slow and insensitive diagnostic tests. Fortunately, new proteomic and molecular diagnostic tools are improving the time to species identification and detection. In this review we will describe the potential impact that rapid diagnostic testing and antifungal stewardship can have on the management of nosocomial candidiasis. © The Author 2015. Published by Oxford University Press on behalf of The International Society for Human and Animal Mycology. All rights reserved. For permissions, please e-mail: journals.permissions@oup.com.

  15. EFFECT OF EXTRACTION METHODS ON ANTIFUNGAL ACTIVITY OF SEA CUCUMBER (Stichopus japonicus

    Directory of Open Access Journals (Sweden)

    Amir Husni

    2014-05-01

    Both SM and CS exhibited their highest antifungal activity when extracted by HRE with 70% ethanol and by HRE with water, respectively, while their highest yields were obtained when extracted by PSE with water. SM has more antifungal than potassium sorbate but weaker than propyl paraben, while CS has more antifungal than the two antifungal agents. Keywords: Antifungal, heat reflux extraction, pressurized solvent extraction, Stichopus japonicus

  16. Dynamics of Mixed- Candida Species Biofilms in Response to Antifungals.

    Science.gov (United States)

    Vipulanandan, G; Herrera, M; Wiederhold, N P; Li, X; Mintz, J; Wickes, B L; Kadosh, D

    2018-01-01

    Oral infections caused by Candida species, the most commonly isolated human fungal pathogen, are frequently associated with biofilms. Although Candida albicans is the predominant organism found in patients with oral thrush, a biofilm infection, there is an increasing incidence of oral colonization and infections caused by non- albicans Candida species, including C. glabrata, C. dubliniensis, and C. tropicalis, which are frequently more resistant to antifungal treatment. While single-species Candida biofilms have been well studied, considerably less is known about the dynamics of mixed- Candida species biofilms and how these dynamics are altered by antifungal treatment. To address these questions, we developed a quantitative polymerase chain reaction-based approach to determine the precise species composition of mixed- Candida species biofilms formed by clinical isolates and laboratory strains in the presence and absence of clinically relevant concentrations of 3 commonly used antifungals: fluconazole, caspofungin, and amphotericin B. In monospecies biofilms, fluconazole exposure favored growth of C. glabrata and C. tropicalis, while caspofungin generally favored significant growth of all species to a varying degree. Fluconazole was not effective against preformed mixed- Candida species biofilms while amphotericin B was potent. As a general trend, in mixed- Candida species biofilms, C. albicans lost dominance in the presence of antifungals. Interestingly, presence in mixed versus monospecies biofilms reduced susceptibility to amphotericin B for C. tropicalis and C. glabrata. Overall, our data suggest that antifungal treatment favors the growth of specific non- albicans Candida species in mixed- Candida species biofilms.

  17. Effect of oral antiseptic agents on phospholipase and proteinase enzymes of Candida albicans.

    Science.gov (United States)

    Uygun-Can, Banu; Kadir, Tanju; Gumru, Birsay

    2016-02-01

    Candida-associated denture stomatitis is the most prevalent form of oral candida infections among the denture wearers. Generally, antiseptic oral rinses used in the treatment of these infections are considered as an adjunct or alternative antifungal treatment. Studies have suggested that the intraoral concentrations of antiseptics decrease substantially to the sub-therapeutic levels on account of the dynamics of the oral cavity. This condition yields the question about the minimum antiseptic concentration that effect the character or pathogenesis of Candida during treatment. The extracellular phospholipase and proteinase enzymes of Candida albicans are regarded to have a crucial role in the pathogenesis of human fungal infections. Therefore, the aim of this study was to investigate the effect of different sub-therapeutic concentrations of chlorhexidine gluconate, hexetidine and triclosan on the production of these enzymes by C. albicans strains isolated from 20 patients with denture stomatitis. Phospholipase test was done by using Sabouraud dextrose agar with egg yolk, proteinase test was done by using bovine serum albumin agar. Phospholipase test was done by using Sabouraud dextrose agar with egg yolk, proteinase test was done by using bovine serum albumin agar. Exoenzyme production of 20 strains which were brief exposured to sub-therapeutic concentrations of three antiseptic agents decreased significantly compared with the strains that were not exposured with antiseptic values (pantiseptics (pantiseptic was compared, there were no significant differences between enzymatic activities (p>0.05). The results of this study show that sub-therapeutic levels of each antiseptic may modulate candidal exoenzyme production, consequently suppressing pathogenicity of C. albicans. Copyright © 2015 Elsevier Ltd. All rights reserved.

  18. 10% low density corn-oil emulsion oral contrast agent for abdominal computed tomography

    International Nuclear Information System (INIS)

    Choi, Sun Kyou; Chon, Dong Kwon; Han, Young Min; Kim, Chong Soo; Sohn, Myung Hee; Song, Ho Young; Choi, Ki Chul

    1990-01-01

    CT of the gastrointestinal tract is commonly performed after administration of a high-density diluted iodinated oral contrast material. However, because if inadequate mixing of the contrast material with the gastrointestinal contents, pseudotumor and poor mucosal visualization are frequently shown on abdominal CT. To overcome these problem, 10% corn oil emulsion (COE) is tested as an alternative oral contrast agent in 40 patients. We analyse patients tolerance, gastric mucosal visualization and discrimination of pancreas from the duodenal C-loop to 10% COE in 40 patients compared with those obtained from 35 patients, who was received high-density diluted iodinated oral contrast agent (gastrografin). The results are as follows : 1. Patients' tolerance to 10% COE is similar to that to conventional oral contrast agent. 2. Image of the gastric mucosa from patients receiving 10% COE is superior to that receiving oral contrast agent. 3. The discrimination between pancreatic head from duodenal C-loop is better in patients receiving 10% COE than in patients receiving conventional oral contrast agent. 4. In patients receiving 10% COE, differentiation of cystic masses from intestinal loops is sometimes difficult. The results of this study indicate that 10% COE may be useful oral contrast agent for optimal visualization of gastric mucosa and pancreatico-duodenal discrimination on abdominal CT

  19. Synthetic Hydroxyapatite as a Biomimetic Oral Care Agent.

    Science.gov (United States)

    Enax, Joachim; Epple, Matthias

    Human tooth enamel consists mostly of minerals, primarily hydroxyapatite, Ca10(PO4)6(OH)2, and thus synthetic hydroxyapatite can be used as a biomimetic oral care agent. This review describes the synthesis and characterization of hydroxyapatite from a chemist's perspective and provides an overview of its current use in oral care, with a focus on dentin hypersensitivity, caries, biofilm management, erosion, and enamel lesions. Reviews and original research papers published in English and German were included. The efficiency of synthetic hydroxyapatite in occluding open dentin tubules, resulting in a protection for sensitive teeth, has been well documented in a number of clinical studies. The first corresponding studies on caries, biofilm management and erosion have provided evidence for a positive effect of hydroxyapatite either as a main or synergistic agent in oral care products. However, more in situ and in vivo studies are needed due to the complexity of the oral milieu and to further clarify existing results. Due to its biocompatibility and similarity to biologically formed hydroxyapatite in natural tooth enamel, synthetic hydroxyapatite is a promising biomimetic oral care ingredient that may extend the scope of preventive dentistry.

  20. Synthesis of heterocycle-attached methylidenebenzenesulfonohydrazones as antifungal agents.

    Science.gov (United States)

    Gao, Zhinan; Lv, Min; Li, Qin; Xu, Hui

    2015-11-15

    A series of heterocycle-attached methylidenebenzenesulfonohydrazone derivatives were synthesized and evaluated for their antifungal activities against seven phytopathogenic fungi such as Fusarium graminearum, Alternaria solani, Valsa mali, Phytophthora capsici, Fusarium solani, Botrytis cinerea, and Glomerella cingulata. Compounds 7b, 8d, 9a, 9b and 9d exhibited a good and broad-spectrum of antifungal activities against at least five phytopathogenic fungi at the concentration of 100 μg/mL. It demonstrated that addition of one double bond between the phenylsulfonylhydrazone fragment and the furan ring of 6a,b,d could afford more active compounds 9a,b,d; however, introduction of the nitro group on the phenyl ring of 6a-9a gave less potent compounds 6e-9e. Copyright © 2015 Elsevier Ltd. All rights reserved.

  1. Antifungal efficacy of Punica granatum, Acacia nilotica, Cuminum cyminum and Foeniculum vulgare on Candida albicans: An in vitro study

    Directory of Open Access Journals (Sweden)

    Pai Mithun

    2010-01-01

    Full Text Available Background: The establishment and maintenance of oral microbiota is related not only to interbacterial coaggregations but also to interactions of these bacteria with yeasts. Hence, it is important for agents used in the treatment of oral diseases to have antifungal properties for effective therapy. Objective: The main purpose of this study was to evaluate the in vitro antifungal efficacy of Punica granatum, Acacia nilotica, Cuminum cyminum and Foeniculum vulgare on Candida albicans. Materials and Methods: The pomegranate peel is separated, dried and powdered. Fennel, cumin and acacia bark obtained from the tree are powdered. Candida is inoculated at 37˚C and seeded on Sabourauds agar medium. Sterilized filter papers saturated with 30 μl of the extracts are placed on the seeded plates and inoculated at 24 and 48 h. Zones of inhibition on all four sides are measured around the filter paper with a vernier caliper. The experiments were repeated on four plates, with four samples of each extract on one plate for all of the extracts. Results: All the above-mentioned ingredients showed antifungal property, with Punica granatum showing the highest inhibition of Candida albicans with a mean zone of inhibition of 22 mm. P-values <0.05 were obtained for Punica granatum when compared with the other extracts. Conclusion: The results showed the potential use of these products as cheap and convenient adjuvants to pharmaceutical antifungal products.

  2. Miconazole-loaded solid lipid nanoparticles: formulation and evaluation of a novel formula with high bioavailability and antifungal activity

    Directory of Open Access Journals (Sweden)

    Aljaeid BM

    2016-01-01

    Full Text Available Bader Mubarak Aljaeid,1 Khaled Mohamed Hosny1,2 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni Suef University, Beni Suef, Egypt Background and objective: Miconazole is a broad-spectrum antifungal drug that has poor aqueous solubility (<1 µg/mL; as a result, a reduction in its therapeutic efficacy has been reported. The aim of this study was to formulate and evaluate miconazole-loaded solid lipid nanoparticles (MN-SLNs for oral administration to find an innovative way to alleviate the disadvantages associated with commercially available capsules. Methods: MN-SLNs were prepared by hot homogenization/ultrasonication. The solubility of miconazole in different solid lipids was measured. The effect of process variables, such as surfactant types, homogenization and ultrasonication times, and the charge-inducing agent on the particle size, zeta potential, and encapsulation efficiency were determined. Furthermore, in vitro drug release, antifungal activity against Candida albicans, and in vivo pharmacokinetics were studied in rabbits. Results: The MN-SLN, consisting of 1.5% miconazole, 2% Precirol ATO5, 2.5% Cremophor RH40, 0.5% Lecinol, and 0.1% Dicetylphosphate, had an average diameter of 23 nm with a 90.2% entrapment efficiency. Furthermore, the formulation of MN-SLNs enhanced the antifungal activity compared with miconazole capsules. An in vivo pharmacokinetic study revealed that the bioavailability was enhanced by >2.5-fold. Conclusion: MN-SLN was more efficient in the treatment of candidiasis with enhanced oral bioavailability and could be a promising carrier for the oral delivery of miconazole. Keywords: miconazole, Precirol ATO5, solid lipid nanoparticles, encapsulation, Cremophor RH40, antifungal activity

  3. Evaluation of 8-Hydroxyquinoline Derivatives as Hits for Antifungal Drug Design.

    Science.gov (United States)

    Pippi, Bruna; Reginatto, Paula; Machado, Gabriella da Rosa Monte; Bergamo, Vanessa Zafaneli; Lana, Daiane Flores Dalla; Teixeira, Mario Lettieri; Franco, Lucas Lopardi; Alves, Ricardo José; Andrade, Saulo Fernandes; Fuentefria, Alexandre Meneghello

    2017-10-01

    Clioquinol is an 8-hydroxyquinoline derivative that was widely used from the 1950s to 1970s as an oral antiparasitic agent. In 1970, the oral forms were withdrawn from the market due to reports of toxicity, but topical formulations for antifungal treatment remained available. Thus, the purpose of this study was to evaluate the toxicity, anti-Candida and antidermatophyte activity and to determine pharmacodynamic characteristics of clioquinol and other 8-hydroxyquinoline derivatives (8-hydroxy-5-quinolinesulfonic acid and 8-hydroxy-7-iodo-5-quinolinesulfonic acid). Antifungal activity was tested by broth microdilution and the fungicidal or fungistatic effect was checked by a time-kill assay. Permeation and histopathological evaluation were performed in Franz diffusion cells with ear skin of pigs and examined under light microscopy. An HET-CAM test was used to determine the potential irritancy. The three compounds were active against all isolates showing anti-Candida and antidermatophyte activity, with MIC ranges of 0.031-2 μg/ml, 1-512 μg/ml, and 2-1024 μg/ml for clioquinol, 8-hydroxy-5-quinolinesulfonic acid, and 8-hydroxy-7-iodo-5-quinolinesulfonic acid, respectively. All compounds showed fungistatic effect for Candida, 8-hydroxy-5-quinolinesulfonic acid, and 8-hydroxy-7-iodo-5-quinolinesulfonic acid showed a fungicidal effect for M. canis and T. mentagrophytes, and clioquinol showed a fungicidal effect only for T. mentagrophytes. Furthermore, they presented a fungicidal effect depending on the time and concentration. The absence of lesions was observed in histopathological evaluation and no compound was irritating. Moreover, clioquinol and 8-hydroxy-5-quinolinesulfonic acid accumulated in the epithelial tissue, and 8-hydroxy-7-iodo-5-quinolinesulfonic acid had a high degree of permeation. In conclusion, 8-hydroxyquinoline derivatives showed antifungal activity and 8-hydroxy-5-quinolinesulfonic acid demonstrated the potential for antifungal drug design.

  4. Combination treatment of oral terbinafine with topical terbinafine and 10% urea ointment in hyperkeratotic type tinea pedis.

    Science.gov (United States)

    Shi, Tian-Wei; Zhang, Jiang-An; Zhang, Xian-Wei; Yu, Hong-Xing; Tang, Yong-Bo; Yu, Jian-Bin

    2014-09-01

    Hyperkeratotic-type tinea pedis is chronic and recalcitrant to topical antifungal agents. Some topical antifungal agents are effective; however, long duration of therapy is required, which often reduce the treatment compliance of patients. To seek for short period therapy of hyperkeratotic type tinea pedis, in this study, we observed the efficacy and safety of treatment of topical terbinafine and 10% urea ointment combined oral terbinafine. Participants with hyperkeratotic type tinea pedis were randomly assigned to two groups. Patients in group I were treated with oral terbinafine for 2 weeks and topical terbinafine and 10% urea ointment for 4 weeks, whereas in group II, only the above topical agents were applied for 12 weeks. Clinical improvement rates and fungal eradication rates were compared between the two groups at 24 weeks after the initiation of treatment. The group I had stopped the topical therapy 8 weeks earlier than group II. There were no significant differences in mycological eradication rates and clinical improvement rates between the two groups, besides, no major side effects were noted in both groups. The short combination therapy with oral terbinafine was effective and safe; it should be a valuable option for patients with hyperkeratotic type tinea pedis. © 2014 Blackwell Verlag GmbH.

  5. Inhibitors of amino acids biosynthesis as antifungal agents.

    Science.gov (United States)

    Jastrzębowska, Kamila; Gabriel, Iwona

    2015-02-01

    Fungal microorganisms, including the human pathogenic yeast and filamentous fungi, are able to synthesize all proteinogenic amino acids, including nine that are essential for humans. A number of enzymes catalyzing particular steps of human-essential amino acid biosynthesis are fungi specific. Numerous studies have shown that auxotrophic mutants of human pathogenic fungi impaired in biosynthesis of particular amino acids exhibit growth defect or at least reduced virulence under in vivo conditions. Several chemical compounds inhibiting activity of one of these enzymes exhibit good antifungal in vitro activity in minimal growth media, which is not always confirmed under in vivo conditions. This article provides a comprehensive overview of the present knowledge on pathways of amino acids biosynthesis in fungi, with a special emphasis put on enzymes catalyzing particular steps of these pathways as potential targets for antifungal chemotherapy.

  6. Candidal colonization, strain diversity, and antifungal susceptibility among adult diabetic patients.

    Science.gov (United States)

    Al-Attas, Safia A; Amro, Soliman O

    2010-01-01

    Candidal colonization in diabetics is a matter of debate. The aim of this study is to investigate oral candidal colonization, strain diversity, antifungal susceptibility, and the influence of local and systemic host factors on candidal colonization in adult diabetics. We conducted a case-control study that compared 150 diabetics (49 type 1, 101 type 2) with 50 healthy controls. Two salivary samples were collected, using the oral rinse sampling method: one for salivary flow rate and pH determination, and the other for candidal colonization assessment. The candidal isolates were identified and tested in vitro for antifungal susceptibility using the commercial kit, Candifast. The relationship between specific host factors and candidal colonization was also investigated. Diabetics had a higher candidal carriage rate compared to controls, but not density. Candida albicans was the most frequently isolated species, but diabetics had a variety of other candidal species present. None of the control samples were resistant to any tested antifungal, while the diabetic samples had differing resistances to azole antifungals. Although there was a significant positive correlation between glycemic control and candidal colonization in type 2 diabetics, there was a negative correlation between salivary pH and candidal carriage in the controls versus density in type 2 diabetics. Diabetic patients not only had a higher candidal carriage rate, but also a variety of candidal species that were resistant to azole antifungals. Oral candidal colonization was significantly associated with glycemic control, type of diabetes, and salivary pH.

  7. Synergy and antagonism between iron chelators and antifungal drugs in Cryptococcus.

    Science.gov (United States)

    Lai, Yu-Wen; Campbell, Leona T; Wilkins, Marc R; Pang, Chi Nam Ignatius; Chen, Sharon; Carter, Dee A

    2016-10-01

    Fungal infections remain very difficult to treat, and developing new antifungal drugs is difficult and expensive. Recent approaches therefore seek to augment existing antifungals with synergistic agents that can lower the therapeutic dose, increase efficacy and prevent resistance from developing. Iron limitation can inhibit microbial growth, and iron chelators have been employed to treat fungal infections. In this study, chequerboard testing was used to explore combinations of iron chelators with antifungal agents against pathogenic Cryptococcus spp. with the aim of determining how disruption to iron homeostasis affects antifungal susceptibility. The iron chelators ethylenediaminetetraacetic acid (EDTA), deferoxamine (DFO), deferiprone (DFP), deferasirox (DSX), ciclopirox olamine and lactoferrin (LF) were paired with the antifungal agents amphotericin B (AmB), fluconazole, itraconazole, voriconazole and caspofungin. All chelators except for DFO increased the efficacy of AmB, and significant synergy was seen between AmB and LF for all Cryptococcus strains. Addition of exogenous iron rescued cells from the antifungal effect of LF alone but could not prevent inhibition by AmB + LF, indicating that synergy was not due primarily to iron chelation but to other properties of LF that were potentiated in the presence of AmB. Significant synergy was not seen consistently for other antifungal-chelator combinations, and EDTA, DSX and DFP antagonised the activity of azole drugs in strains of Cryptococcus neoformans var. grubii. This study highlights the range of interactions that can be induced by chelators and indicates that most antifungal drugs are not enhanced by iron limitation in Cryptococcus. Copyright © 2016 Elsevier B.V. and International Society of Chemotherapy. All rights reserved.

  8. Candida albicans gastrointestinal colonization and invasion in the mouse: effect of antibacterial dosing, antifungal therapy and immunosuppression.

    Science.gov (United States)

    Kinsman, O S; Pitblado, K

    1989-12-01

    Infant mice infected with Candida albicans by the oral-intragastric route became colonized in the gut and were persistently colonized into adulthood. Faecal levels of Candida were correlated with total gastrointestinal Candida and provided a useful means of detecting yeast overgrowth or elimination. Antibacterial agents promoting Candida overgrowth when given by the oral or parenteral route included ceftriaxone, augmentin and cefoperazone. Ceftizoxime had less effect. Ceftazidime and latamoxef produced raised levels only by the oral route. Gentamicin, vancomycin and metronidazole did not affect the Candida levels. Dosing with some antibacterials promoted an increase in gastrointestinal Candida and invasion to a greater extent than immunosuppression. Antifungal therapy to reduce gastrointestinal colonization was investigated using amphotericin B, nystatin, ketoconazole, intraconazole and fluconazole. Fluconazole was most effective at reducing faecal Candida.

  9. Activity of posaconazole and other antifungal agents against Mucorales strains identified by sequencing of internal transcribed spacers.

    Science.gov (United States)

    Alastruey-Izquierdo, Ana; Castelli, Maria Victoria; Cuesta, Isabel; Monzon, Araceli; Cuenca-Estrella, Manuel; Rodriguez-Tudela, Juan Luis

    2009-04-01

    The antifungal susceptibility profiles of 77 clinical strains of Mucorales species, identified by internal transcribed spacer sequencing, were analyzed. MICs obtained at 24 and 48 h were compared. Amphotericin B was the most active agent against all isolates, except for Cunninghamella and Apophysomyces isolates. Posaconazole also showed good activity for all species but Cunninghamella bertholletiae. Voriconazole had no activity against any of the fungi tested. Terbinafine showed good activity, except for Rhizopus oryzae, Mucor circinelloides, and Rhizomucor variabilis isolates.

  10. Pharmacological interactions of anti-microbial agents in odontology.

    Science.gov (United States)

    Gómez-Moreno, Gerardo; Guardia, Javier; Cutando, Antonio; Calvo-Guirado, José-Luis

    2009-03-01

    In this third article we describe the pharmacological interactions resulting from the use of anti-microbial agents. Although the antimicrobials prescribed in odontology are generally safe they can produce interactions with other medicaments which can give rise to serious adverse reactions which are well documented in clinical studies. Antibiotics with grave and dangerous life threatening consequences are erythromycin, clarithromycin and metronidazol and the anti-fungal agents are ketoconazol and itraconazol. Regarding the capacity of the anti-microbials to reduce the efficacy of oral anti-contraceptives the clinical studies to date are inconclusive, however, it would be prudent for the oral cavity specialist to point out the risk of a possible interaction. Therefore the specialist should be aware of possible interactions as a consequence of administering an antibiotic together with other medicaments the patient may be taking.

  11. The potential of compounds isolated from Xylaria spp. as antifungal agents against anthracnose.

    Science.gov (United States)

    Elias, Luciana M; Fortkamp, Diana; Sartori, Sérgio B; Ferreira, Marília C; Gomes, Luiz H; Azevedo, João L; Montoya, Quimi V; Rodrigues, André; Ferreira, Antonio G; Lira, Simone P

    2018-03-31

    Anthracnose is a crop disease usually caused by fungi in the genus Colletotrichum or Gloeosporium. These are considered one of the main pathogens, causing significant economic losses, such as in peppers and guarana. The current forms of control include the use of resistant cultivars, sanitary pruning and fungicides. However, even with the use of some methods of controlling these cultures, the crops are not free of anthracnose. Additionally, excessive application of fungicides increases the resistance of pathogens to agrochemicals and cause harm to human health and the environment. In order to find natural antifungal agents against guarana anthracnose, endophytic fungi were isolated from Amazon guarana. The compounds piliformic acid and cytochalasin D were isolated by chromatographic techniques from two Xylaria spp., guided by assays with Colletotrichum gloeosporioides. The isolated compounds were identified by spectrometric techniques, as NMR and mass spectrometry. This is the first report that piliformic acid and cytochalasin D have antifungal activity against C. gloeosporioides with MIC 2.92 and 2.46μmolmL -1 respectively. Captan and difenoconazole were included as positive controls (MIC 16.63 and 0.02μmolmL -1 , respectively). Thus, Xylaria species presented a biotechnological potential and production of different active compounds which might be promising against anthracnose disease. Copyright © 2018 Sociedade Brasileira de Microbiologia. Published by Elsevier Editora Ltda. All rights reserved.

  12. Oral administration of amphotericin B nanoparticles: antifungal activity, bioavailability and toxicity in rats.

    Science.gov (United States)

    Radwan, Mahasen A; AlQuadeib, Bushra T; Šiller, Lidija; Wright, Matthew C; Horrocks, Benjamin

    2017-11-01

    Amphotericin B (AMB) is used most commonly in severe systemic life-threatening fungal infections. There is currently an unmet need for an efficacious (AMB) formulation amenable to oral administration with better bioavailability and lower nephrotoxicity. Novel PEGylated polylactic-polyglycolic acid copolymer (PLGA-PEG) nanoparticles (NPs) formulations of AMB were therefore studied for their ability to kill Candida albicans (C. albicans). The antifungal activity of AMB formulations was assessed in C. albicans. Its bioavalability was investigated in nine groups of rats (n = 6). Toxicity was examined by an in vitro blood hemolysis assay, and in vivo nephrotoxicity after single and multiple dosing for a week by blood urea nitrogen (BUN) and plasma creatinine (PCr) measurements. The MIC of AMB loaded to PLGA-PEG NPs against C. albicans was reduced two to threefold compared with free AMB. Novel oral AMB delivery loaded to PLGA-PEG NPs was markedly systemically available compared to Fungizone® in rats. The addition of 2% of GA to the AMB formulation significantly (p bioavailability from 1.5 to 10.5% and the relative bioavailability was > 790% that of Fungizone®. The novel AMB formulations showed minimal toxicity and better efficacy compared to Fungizone®. No nephrotoxicity in rats was detected after a week of multiple dosing of AMB NPs based on BUN and PCr, which remained at normal levels. An oral delivery system of AMB-loaded to PLGA-PEG NPs with better efficacy and minimal toxicity was formulated. The addition of glycyrrhizic acid (GA) to AMB NPs formulation resulted in a significant oral absorption and improved bioavailability in rats.

  13. Plant latex: a promising antifungal agent for post harvest disease control.

    Science.gov (United States)

    Sibi, G; Wadhavan, Rashmi; Singh, Sneha; Shukla, Abhilasha; Dhananjaya, K; Ravikumar, K R; Mallesha, H

    2013-12-01

    Bioactive compounds from plant latex are potential source of antifungic against post harvest pathogens. Latex from a total of seven plant species was investigated for its phytochemical and antifungal properties. Six fungi namely Aspergillus fumigatus, A. niger, A. terreus, F. solani, P. digitatum and R. arrhizus were isolated from infected fruits and vegetables and tested against various solvent extracts of latex. Analysis of latex extracts with phytochemical tests showed the presence of alkaloids, flavonoids, glycosides, phenols, saponins, steroids, tannins and terpenoids. Antifungal assay revealed the potential inhibitory activity of petroleum ether extracts against the postharvest fungal isolates. Various degree of sensitivity was observed irrespective of plant species studied with A. terreus and P. digitatum as the most susceptible ones. F. solani and A. fumigatus were moderately sensitive to the latex extracts tested. Among the plants, latex of Thevetia peruviana (75.2%) and Artocarpus heterophyllus (64.8%) were having potential antifungal activity against the isolates followed by Manilkara zapota (51.1%). In conclusion, use of plant latex makes interest to control postharvest fungal diseases and is fitting well with the concept of safety for human health and environment.

  14. Colonization and antifungals susceptibility patterns of Candida species isolated from hospitalized patients in ICUs and NICUs.

    Science.gov (United States)

    Zarei Mahmoudabadi, Ali; Rezaei-Matehkolaei, Ali; Navid, Mojgan; Torabizadeh, Mehdi; Mazdarani, Shahnam

    2015-07-01

    Several studies have shown that there are an increasing in invasive candidiasis during 2-3 last decades. Although, Candida albicans is considered as the most common candidiasis agents, other non-albicans such as C. glabrata, C. krusei, C. parapsilosis, and C. tropicalis were raised as infectious agents. Resistance to fluconazole among non-albicans species is an important problem for clinicians during therapy and prophylaxis. The aim of current study was to detect the Candida species from hospitalized neonatal and children in intensive care units (ICUs) and neonatal intensive care units (NICUs). In addition, the susceptibility of isolated agents were also evaluated against three antifungals. In the present study 298 samples including 98 blood samples, 100 urines and 100 swabs from oral cavity were inoculated on CHROMagar Candida. Initial detection was done according to the coloration colonies on CHROMagar Candida . Morphology on cornmeal agar, germ tube formation and growth at 45°C were confirmed isolates. Amphotericin B, fluconazole and terbinafine (Lamisil) were used for the susceptibility tests using microdilution method. In the present study 21% and 34% of urines and swabs from oral cavity were positive for Candida species, respectively. The most common species was C. albicans (62.5%) followed by C. tropicalis (15.6%), C. glabrata (6.3%) and Candida species (15.6%). Our study indicated that the most tested species of Candida, 70.3% were sensitive to fluconazole at the concentration of ≤8 μg/mL. Whereas 9 (14.1%) of isolates were resistant to amphotericine B at ≥8 μg/mL. This study demonstrates the importance of species identification and antifungals susceptibility testing for hospitalized patients in ICUs and NICUs wards.

  15. In vitro antifungal activity of hydroxychavicol isolated from Piper betle L.

    Science.gov (United States)

    Ali, Intzar; Khan, Farrah G; Suri, Krishan A; Gupta, Bishan D; Satti, Naresh K; Dutt, Prabhu; Afrin, Farhat; Qazi, Ghulam N; Khan, Inshad A

    2010-02-03

    Hydroxychavicol, isolated from the chloroform extraction of the aqueous leaf extract of Piper betle L., (Piperaceae) was investigated for its antifungal activity against 124 strains of selected fungi. The leaves of this plant have been long in use tropical countries for the preparation of traditional herbal remedies. The minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) of hydroxychavicol were determined by using broth microdilution method following CLSI guidelines. Time kill curve studies, post-antifungal effects and mutation prevention concentrations were determined against Candida species and Aspergillus species "respectively". Hydroxychavicol was also tested for its potential to inhibit and reduce the formation of Candida albicans biofilms. The membrane permeability was measured by the uptake of propidium iodide. Hydroxychavicol exhibited inhibitory effect on fungal species of clinical significance, with the MICs ranging from 15.62 to 500 microg/ml for yeasts, 125 to 500 microg/ml for Aspergillus species, and 7.81 to 62.5 microg/ml for dermatophytes where as the MFCs were found to be similar or two fold greater than the MICs. There was concentration-dependent killing of Candida albicans and Candida glabrata up to 8 x MIC. Hydroxychavicol also exhibited an extended post antifungal effect of 6.25 to 8.70 h at 4 x MIC for Candida species and suppressed the emergence of mutants of the fungal species tested at 2 x to 8 x MIC concentration. Furthermore, it also inhibited the growth of biofilm generated by C. albicans and reduced the preformed biofilms. There was increased uptake of propidium iodide by C. albicans cells when exposed to hydroxychavicol thus indicating that the membrane disruption could be the probable mode of action of hydroxychavicol. The antifungal activity exhibited by this compound warrants its use as an antifungal agent particularly for treating topical infections, as well as gargle mouthwash against oral Candida

  16. Kaempferol loaded lecithin/chitosan nanoparticles: preparation, characterization, and their potential applications as a sustainable antifungal agent.

    Science.gov (United States)

    Ilk, Sedef; Saglam, Necdet; Özgen, Mustafa

    2017-08-01

    Flavonoid compounds are strong antioxidant and antifungal agents but their applications are limited due to their poor dissolution and bioavailability. The use of nanotechnology in agriculture has received increasing attention, with the development of new formulations containing active compounds. In this study, kaempferol (KAE) was loaded into lecithin/chitosan nanoparticles (LC NPs) to determine antifungal activity compared to pure KAE against the phytopathogenic fungus Fusarium oxysporium to resolve the bioavailability problem. The influence of formulation parameters on the physicochemical properties of KAE loaded lecithin chitosan nanoparticles (KAE-LC NPs) were studied by using the electrostatic self-assembly technique. KAE-LC NPs were characterized in terms of physicochemical properties. KAE has been successfully encapsulated in LC NPs with an efficiency of 93.8 ± 4.28% and KAE-LC NPs showed good physicochemical stability. Moreover, in vitro evaluation of the KAE-LC NP system was made by the release kinetics, antioxidant and antifungal activity in a time-dependent manner against free KAE. Encapsulated KAE exhibited a significantly inhibition efficacy (67%) against Fusarium oxysporium at the end of the 60 day storage period. The results indicated that KAE-LC NP formulation could solve the problems related to the solubility and loss of KAE during use and storage. The new nanoparticle system enables the use of smaller quantities of fungicide and therefore, offers a more environmentally friendly method of controlling fungal pathogens in agriculture.

  17. Antifungal Effect of (+-Pinoresinol Isolated from Sambucus williamsii

    Directory of Open Access Journals (Sweden)

    Bomi Hwang

    2010-05-01

    Full Text Available In this study, we investigated the antifungal activity and mechanism of action of (+-pinoresinol, a biphenolic compound isolated from the herb Sambucus williamsii,used in traditional medicine. (+-Pinoresinol displays potent antifungal properties without hemolytic effects on human erythrocytes. To understand the antifungal mechanism of (+-pinoresinol, we conducted fluorescence experiments on the human pathogen Candida albicans. Fluorescence analysis using 1,6-diphenyl-1,3,5-hexatriene (DPH indicated that the (+-pinoresinol caused damage to the fungal plasma membrane. This result was confirmed by using rhodamine-labeled giant unilamellar vesicle (GUV experiments. Therefore, the present study indicates that (+-pinoresinol possesses fungicidal activities and therapeutic potential as an antifungal agent for the treatment of fungal infectious diseases in humans.

  18. Activity of Posaconazole and Other Antifungal Agents against Mucorales Strains Identified by Sequencing of Internal Transcribed Spacers▿

    Science.gov (United States)

    Alastruey-Izquierdo, Ana; Castelli, Maria Victoria; Cuesta, Isabel; Monzon, Araceli; Cuenca-Estrella, Manuel; Rodriguez-Tudela, Juan Luis

    2009-01-01

    The antifungal susceptibility profiles of 77 clinical strains of Mucorales species, identified by internal transcribed spacer sequencing, were analyzed. MICs obtained at 24 and 48 h were compared. Amphotericin B was the most active agent against all isolates, except for Cunninghamella and Apophysomyces isolates. Posaconazole also showed good activity for all species but Cunninghamella bertholletiae. Voriconazole had no activity against any of the fungi tested. Terbinafine showed good activity, except for Rhizopus oryzae, Mucor circinelloides, and Rhizomucor variabilis isolates. PMID:19171801

  19. Oral (Systemic) Botanical Agents for the Treatment of Psoriasis: A Review.

    Science.gov (United States)

    Farahnik, Benjamin; Sharma, Divya; Alban, Joseph; Sivamani, Raja

    2017-06-01

    Patients with psoriasis often use botanical therapies as part of their treatment. It is important for clinicians to be aware of the current evidence regarding these agents as they treat patients. A systematic literature search was conducted using the PubMed, MEDLINE, and EMBASE database for randomized clinical trials assessing the use of botanical therapeutics for psoriasis. The search included the following keywords: "psoriasis" and "plant" or "herbal" or "botanical." Citations within articles were also reviewed to identify relevant sources. The results were then further refined by route of administration, and the oral (systemic) botanical agents are reviewed herein. A total of 12 controlled and uncontrolled clinical trials addressing the use of oral, systemic botanical agents for psoriasis were assessed in this review. While overall evidence is limited in quantity and quality, HESA-A, curcumin, neem extract, and, to a lesser degree, Traditional Chinese Medicine seem to be the most efficacious agents. The literature addresses a large amount of studies in regards to botanicals for the treatment of psoriasis. While most agents appear to be safe, further research is necessary for evidence-based recommendation of oral botanical agents to psoriasis patients.

  20. Antibacterial and Antifungal Activities of Spices

    Science.gov (United States)

    Liu, Qing; Meng, Xiao; Li, Ya; Zhao, Cai-Ning; Tang, Guo-Yi; Li, Hua-Bin

    2017-01-01

    Infectious diseases caused by pathogens and food poisoning caused by spoilage microorganisms are threatening human health all over the world. The efficacies of some antimicrobial agents, which are currently used to extend shelf-life and increase the safety of food products in food industry and to inhibit disease-causing microorganisms in medicine, have been weakened by microbial resistance. Therefore, new antimicrobial agents that could overcome this resistance need to be discovered. Many spices—such as clove, oregano, thyme, cinnamon, and cumin—possessed significant antibacterial and antifungal activities against food spoilage bacteria like Bacillus subtilis and Pseudomonas fluorescens, pathogens like Staphylococcus aureus and Vibrio parahaemolyticus, harmful fungi like Aspergillus flavus, even antibiotic resistant microorganisms such as methicillin resistant Staphylococcus aureus. Therefore, spices have a great potential to be developed as new and safe antimicrobial agents. This review summarizes scientific studies on the antibacterial and antifungal activities of several spices and their derivatives. PMID:28621716

  1. Oral hypoglycaemic agents in 118 diabetic pregnancies

    DEFF Research Database (Denmark)

    Hellmuth, E; Damm, P; Mølsted-Pedersen, L

    2000-01-01

    AIMS: To assess maternal and neonatal complications in pregnancies of diabetic women treated with oral hypoglycaemic agents during pregnancy. METHODS: A cohort study including all consecutively registered, orally treated pregnant diabetic patients set in a diabetic obstetrical service...... at a university hospital: 50 women treated with metformin, 68 women treated with sulphonylurea during pregnancy and a reference group of 42 diabetic women treated with insulin during pregnancy. RESULTS: The prevalence of pre-eclampsia was significantly increased in the group of women treated with metformin...

  2. Epidemiology and antifungal susceptibility of Candida species in a tertiary care hospital, Kolkata, India

    Directory of Open Access Journals (Sweden)

    Partha Bhattacharjee

    2016-06-01

    Conclusion: Species-level identification of Candida and their antifungal sensitivity testing should to be performed to achieve better clinical result and to select an appropriate and effective antifungal therapy. High resistance to antifungal agents is an alarming sign to the healthcare professionals.

  3. ANTIFUNGAL SUSCEPTIBILITY TESTING: CURRENT ROLE FROM THE CLINICAL LABORATORY PERSPECTIVE

    Directory of Open Access Journals (Sweden)

    Brunella Posteraro

    2014-04-01

    Full Text Available Despite availability of many antifungal agents, antifungal clinical resistance occurs, perhaps as a result of an infecting organism found to be resistant in vitro to one or more antifungals tested. Thus, antifungal susceptibility testing (AFST results, if timely generated by the clinical microbiology and communicated to clinicians, can aid them in the therapeutic decision making, especially for difficult-to-treat invasive candidiasis and aspergillosis. Although recently refined AFST methods are commercially available to allow a close antifungal resistance surveillance in many clinical setting, novel assays, relying on short-time antifungal drug exposure of fungal isolates, are upcoming tools for AFST. Based on emerging technologies such as flow cytometry, MALDI-TOF mass spectrometry, and isothermal microcalorimetry, these assays could provide a reliable means for quicker and sensitive assessment of AFST.

  4. Effect of Incorporation of Antifungal Agents on the Ultimate Tensile Strength of Temporary Soft Denture Liners.

    Science.gov (United States)

    Neppelenbroek, Karin Hermana; Lima, Jozely Francisca Mello; Hotta, Juliana; Galitesi, Lucas Lulo; Almeida, Ana Lucia Pompéia Fraga; Urban, Vanessa Migliorini

    2018-02-01

    To investigate the ultimate tensile strength of temporary soft denture liners modified by minimum inhibitory concentrations (MICs) of antifungal agents for Candida albicans biofilm (SC5314) determined in previous microbiological research. Dumbbell-shaped specimens (n = 7) with a central cross-sectional area of 6 × 3 × 33 mm were produced by Softone and Trusoft, without (control) or with incorporation of drugs in powder form at MICs for C. albicans biofilm (per g of material powder): nystatin (0.032 g), chlorhexidine diacetate (0.064 g), ketoconazole (0.128 g), miconazole (0.256 g), and itraconazole (0.256 g). After plasticization, specimens were immersed in distilled water at 37°C for 24 hours, 7 or 14 days, and then tested in tension in a universal testing machine at 40 mm/min. Data of tensile strength (MPa) and elongation percentage (%) were submitted to 3-way ANOVA and Tukey's test (α = 0.05). At the end of 14 days, the tensile strength for both materials was significantly lower in the groups modified by miconazole and itraconazole compared to the other groups (p 0.05). After 7 and 14 days in water, miconazole and itraconazole added into both materials resulted in significantly lower elongation percentages compared to the other antifungal agents and control (p 0.05). The addition of the nystatin, chlorhexidine, and ketoconazole at MICs for C. albicans biofilm resulted in no harmful effects on the tensile strength and elongation percentage of the temporary soft denture liner materials up to 14 days. © 2017 by the American College of Prosthodontists.

  5. Identification of uncommon oral yeasts from cancer patients by MALDI-TOF mass spectrometry.

    Science.gov (United States)

    Aslani, Narges; Janbabaei, Ghasem; Abastabar, Mahdi; Meis, Jacques F; Babaeian, Mahasti; Khodavaisy, Sadegh; Boekhout, Teun; Badali, Hamid

    2018-01-08

    agents. Our findings suggest that anidulafungin should be used as antifungal of choice for prophylaxis in clinically high-risk patients with documented oral colonization or infection.

  6. Prenatal exposure to antifungal medication may change anogenital distance in male offspring

    DEFF Research Database (Denmark)

    Mogensen, Djamilla Madelung; Pihl, Maria Bergkvist; Skakkebæk, Niels Erik

    2017-01-01

    (AGDap) and penile width; measured at the base of the penis. Results: Eighty seven women had used antifungal medicine during pregnancy. Maternal use of oral fluconazole (n = 4) was associated with a 6.4 mm shorter AGDas (95% CI: -11.9;-0.9) in the male offspring. Use of antifungal vaginal tablets (n = 21...

  7. The primary applications of Gd-DTPA as an oral negative gastrointestinal contrast agent for MRCP

    International Nuclear Information System (INIS)

    Chen Yanping; Zhang Xuelin; Cheng Guanxun; Chang Renmin; Zhang Yuzhong; Cang Peng; Xia Qiong

    2003-01-01

    Objective: Using oral Gd-DTPA as a negative contrast agent to null the bowel signal during MR cholangiopancreatography (MRCP) to improve the quality of MRCP. Methods: A phantom study was performed to select the optimal concentration of Gd-DTPA to be used as an oral negative contrast agent in MRCP. 15 patients suspected of biliary tract and pancreatic disease were performed with MRCP before and after using 250 ml oral contrast agents (1:5 diluted Gd-DTPA, 1.488 g/L). All MR images were acquired using a 1.5 T whole body MR scanner (Vision Plus, Siemens). MRCP was acquired using two-dimensional single slice fast spin-echo sequence and HASTE (half-fourier acquisition single-shot fast spin echo) sequence. Results: The phantom study showed that the dilution ratio 1:5 of Gd-DTPA oral contrast agent was best in decreasing the signal intensity both in T 2 WI (59.3%) and in HASTE sequence (82.45%). All the dilution ratio of Gd-DTPA oral contrast agent decreased the signal intensity up to 90% on single slice MRCP. In all the patients the high signal intensity from the stomach and intestinal fluid was completely suppressed. The depictions of common bile duct and pancreatic duct were markedly improved by the oral contrast agent (P<0.05). Conclusion: 1:5 diluted (1.488 g/L) oral MR contrast agent Gd-DTPA can be an effective and safe negative contrast agent in eliminating signal intensity of the gastrointestinal tract, thus improving the depiction of the biliary system in MRCP

  8. Antifungal activity of tioconazole (UK-20,349), a new imidazole derivative.

    Science.gov (United States)

    Jevons, S; Gymer, G E; Brammer, K W; Cox, D A; Leeming, M R

    1979-04-01

    Tioconazole (UK-20,349), a new antifungal imidazole derivative, was compared with miconazole for activity in vitro against Candida spp., Torulopsis glabrata, Cryptococcus neoformans, Aspergillus spp., and dermatophyte fungi (Trichophyton spp. and Microsporum spp.). Tioconazole was more active than miconazole against all the fungal species examined except Aspergillus, against which both agents showed similar activity. Both tioconazole and miconazole inhibited the growth of all fungi examined at concentrations well below their quoted minimum inhibitory concentrations. Their activity against fungi in vivo was investigated in mice infected systemically with Candida albicans. Both agents significantly reduced the numbers of viable Candida cells recoverable from the kidneys of infected animals, with tioconazole producing a generally more marked reduction. After administration of a single oral dose (25 mg/kg) to beagle dogs or white mice, higher and more sustained circulating levels of bioactive drug were detectable of tioconazole than of miconazole. These observations suggest that tioconazole may have potential in the treatment of both superficial and systemic mycoses in humans.

  9. Evaluating food additives as antifungal agents against Monilinia fructicola in vitro and in hydroxypropyl methylcellulose-lipid composite edible coatings for plums.

    Science.gov (United States)

    Karaca, Hakan; Pérez-Gago, María B; Taberner, Verònica; Palou, Lluís

    2014-06-02

    Common food preservative agents were evaluated in in vitro tests for their antifungal activity against Monilinia fructicola, the most economically important pathogen causing postharvest disease of stone fruits. Radial mycelial growth was measured in Petri dishes of PDA amended with three different concentrations of the agents (0.01-0.2%, v/v) after 7 days of incubation at 25 °C. Thirteen out of fifteen agents tested completely inhibited the radial growth of the fungus at various concentrations. Among them, ammonium carbonate, ammonium bicarbonate and sodium bicarbonate were the most effective while sodium acetate and sodium formate were the least effective. The effective agents and concentrations were tested as ingredients of hydroxypropyl methylcellulose (HPMC)-lipid edible coatings against brown rot disease on plums previously inoculated with M. fructicola (curative activity). 'Friar' and 'Larry Ann' plums were inoculated with the pathogen, coated with stable edible coatings about 24h later, and incubated at 20 °C and 90% RH. Disease incidence (%) and severity (lesion diameter) were determined after 4, 6, and 8 days of incubation and the 'area under the disease progress stairs' (AUDPS) was calculated. Coatings containing bicarbonates and parabens significantly reduced brown rot incidence in plums, but potassium sorbate, used at 1.0% in the coating formulation, was the most effective agent with a reduction rate of 28.6%. All the tested coatings reduced disease severity to some extent, but coatings containing 0.1% sodium methylparaben or sodium ethylparaben or 0.2% ammonium carbonate or ammonium bicarbonate were superior to the rest, with reduction rates of 45-50%. Overall, the results showed that most of the agents tested in this study had significant antimicrobial activity against M. fructicola and the application of selected antifungal edible coatings is a promising alternative for the control of postharvest brown rot in plums. Copyright © 2014 Elsevier B

  10. Oral agents for ovulation induction:Old drugs revisited and new drugs re-evaluated

    NARCIS (Netherlands)

    Badawy, A.M.M.

    2008-01-01

    The aim of this thesis was to address a number of questions regarding oral agents used for ovulation induction. We were motivated to run the presented trials because of many reasons. Firstly, although oral agents, namely CC, have been in the market for decades, many basic aspects regarding the

  11. SHORT COMMUNICATION EVALUATION OF ANTIFUNGAL AND ...

    African Journals Online (AJOL)

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    The target substrates were characterized by UV, IR, 1H-NMR and 13C-NMR .... Also substituents like methyl, methoxy and hydroxyl, having +M effect that ... antibacterial and antifungal agents and can find use in biomedical area in near future.

  12. Antimicrobial Effect of Copper Oxide Nanoparticles on Some Oral Bacteria and Candida Species

    Directory of Open Access Journals (Sweden)

    Amiri M

    2017-03-01

    Full Text Available Statement of Problem: Acid producing bacteria including Streptococcus mutans and lactobacilli cause tooth demineralization and lead to tooth decay. Also, oral colonization of the species of Candida has been reported in many studies that are resistant to antifungal agents. Objectives: In this study, antibacterial and antifungal effects of nano-CuO were studied against some oral bacteria and yeast fungi. Materials and Methods: The minimum inhibitory concentrations (MICs of copper oxide nanoparticles (CuO NPs for oral bacterial and fungal test strains were determined in 96-well microtiter plate technique. The agar diffusion test (ADT was employed to assess the antifungal properties of nystatin. Results: The MIC50 value of CuO NPs was determined at the range of 1–10 µg/ml for S. mutans, < 1 µg/ml for L. acidophilus, and 10 µg/ml for L. casei. Higher concentrations of CuO NPs (100-1000 µg/ml were effective on the bacterial cell growth, resulting in 100% reduction in the optical density in TSB medium. The cells of Candida albicans, C. krusei and C. glabrata were treated with CuO NPs and the results showed a decrease in fungal growth at a concentration of 1-1000 µg/ml in TSB medium. The MIC50 value of CuO NPs was determined 1000 µg/ml for three species of Candida. The diameter of growth inhibition zones of 1100 µg/ml nystatin was obtained 15-21 mm for clinical isolates of three species of Candida. Conclusions: With respect to the potential bactericidal activity of CuO NPs on various cariogenic bacteria examined in this study, these NPs could be introduce as a candidate control agent for preventing dental caries or dental infections. In our study, on the other hand, Nano copper oxide had a weak effect on the candida species.

  13. Oral anticancer agent medication adherence by outpatients.

    Science.gov (United States)

    Kimura, Michio; Usami, Eiseki; Iwai, Mina; Nakao, Toshiya; Yoshimura, Tomoaki; Mori, Hiromi; Sugiyama, Tadashi; Teramachi, Hitomi

    2014-11-01

    In the present study, medication adherence and factors affecting adherence were examined in patients taking oral anticancer agents. In June 2013, 172 outpatients who had been prescribed oral anticancer agents by Ogaki Municipal Hospital (Ogaki, Gifu, Japan) completed a questionnaire survey, with answers rated on a five-point Likert scale. The factors that affect medication adherence were evaluated using a customer satisfaction (CS) analysis. For patients with good and insufficient adherence to medication, the median ages were 66 years (range, 21-85 years) and 73 years (range, 30-90 years), respectively (P=0.0004), while the median dosing time was 131 days (range, 3-3,585 days) and 219 days (24-3,465 days), respectively (P=0.0447). In 36.0% (62 out of 172) of the cases, there was insufficient medication adherence; 64.5% of those cases (40 out of 62) showed good medication compliance (4-5 point rating score). However, these patients did not fully understand the effects or side-effects of the drugs, giving a score of three points or less. The percentage of patients with good medication compliance was 87.2% (150 out of 172). Through the CS analysis, three items, the interest in the drug, the desire to consult about the drug and the condition of the patient, were extracted as items for improvement. Overall, the medication compliance of the patients taking the oral anticancer agents was good, but the medication adherence was insufficient. To improve medication adherence, a better understanding of the effectiveness and necessity of drugs and their side-effects is required. In addition, the interest of patients in their medication should be encouraged and intervention should be tailored to the condition of the patient. These steps should lead to improved medication adherence.

  14. Factors involved in patient choice of oral or vaginal treatment for vulvovaginal candidiasis

    Directory of Open Access Journals (Sweden)

    Sobel JD

    2013-12-01

    Full Text Available Jack D SobelDivision of Infectious Diseases, Wayne State University School of Medicine, Detroit, MI, USAAbstract: Vulvovaginal candidiasis (VVC is an extremely common cause of vaginal symptoms in women. Multiple antifungal products are available by either the oral or vaginal route, although no new drugs have become available for two decades. Given the therapeutic equivalence of the antimycotic agents and their routes of administration, the specific drug and formulation selected is entirely arbitrary in relation to final treatment outcome. Nevertheless, multiple factors affecting preference, both practitioner-dependent and patient-dependent, impact on selection of a specific drug and route of administration.Keywords: antifungal drugs, antimycotics, Candida vaginitis, vulvovaginal candidiasis

  15. Alterations in growth and branching of Neurospora crassa caused by sub-inhibitory concentrations of antifungal agents Alteraciones de crecimiento y ramificación en Neurospora crassa provocadas por concentraciones subinhibitorias de agentes antimicóticos

    Directory of Open Access Journals (Sweden)

    R. C. Pereira

    2009-03-01

    Full Text Available Six antifungal agents at subinhibitory concentrations were used for investigating their ability to affect the growth and branching in Neurospora crassa. Among the antifungals herein used, the azole agent ketoconazole at 0.5 μg/ml inhibited radial growth more than fluconazole at 5.0 μg/ml while amphotericin B at 0.05 μg/ml was more effective than nystatin at 0.05 μg/ml. Morphological alterations in hyphae were observed in the presence of griseofulvin, ketoconazole and terbinafine at the established concentrations. The antifungal agents were more effective on vegetative growth than on conidial germination. Terbinafine markedly reduced growth unit length (GU by 54.89%, and caused mycelia to become hyperbranched. In all cases, there was a high correlation between hyphal length and number of tips (r > 0.9. All our results showed highly significant differences by ANOVA, (p Se investigó el efecto de seis agentes antimicóticos en concentraciones subinhibitorias sobre el crecimiento y la ramificación en Neurospora crassa. El agente azólico ketoconazol a la concentración de 0,5 μg/ml inhibió el crecimiento radial más que el fluconazol a 5,0 μg/ml, y la anfotericina B a 0,05 μg/ ml fue más eficiente que 0,05 μg/ml de nistatina, entre los agentes poliénicos usados. En presencia de griseofulvina, ketoconazol y terbinafina a las concentraciones establecidas se observaron alteraciones morfológicas en las hifas. Los agentes antimicóticos fueron más eficientes sobre el crecimiento vegetativo que sobre la germinación conidial. La terbinafina redujo marcadamente (54,89% la longitud de la unidad de crecimiento y provocó la hiperramificación del micelio. En todos los casos, existió gran correlación entre la longitud y el número de ápices de las hifas (r > 0,9. Todos los resultados mostraron diferencias altamente significativas de acuerdo con ANOVA (p < 0,001, α = 0,05. Considerando que el ápice de la hifa es la principal interfase entre

  16. In vitro antifungal activity of hydroxychavicol isolated from Piper betle L

    Directory of Open Access Journals (Sweden)

    Afrin Farhat

    2010-02-01

    Full Text Available Abstract Background Hydroxychavicol, isolated from the chloroform extraction of the aqueous leaf extract of Piper betle L., (Piperaceae was investigated for its antifungal activity against 124 strains of selected fungi. The leaves of this plant have been long in use tropical countries for the preparation of traditional herbal remedies. Methods The minimum inhibitory concentration (MIC and minimum fungicidal concentration (MFC of hydroxychavicol were determined by using broth microdilution method following CLSI guidelines. Time kill curve studies, post-antifungal effects and mutation prevention concentrations were determined against Candida species and Aspergillus species "respectively". Hydroxychavicol was also tested for its potential to inhibit and reduce the formation of Candida albicans biofilms. The membrane permeability was measured by the uptake of propidium iodide. Results Hydroxychavicol exhibited inhibitory effect on fungal species of clinical significance, with the MICs ranging from 15.62 to 500 μg/ml for yeasts, 125 to 500 μg/ml for Aspergillus species, and 7.81 to 62.5 μg/ml for dermatophytes where as the MFCs were found to be similar or two fold greater than the MICs. There was concentration-dependent killing of Candida albicans and Candida glabrata up to 8 × MIC. Hydroxychavicol also exhibited an extended post antifungal effect of 6.25 to 8.70 h at 4 × MIC for Candida species and suppressed the emergence of mutants of the fungal species tested at 2 × to 8 × MIC concentration. Furthermore, it also inhibited the growth of biofilm generated by C. albicans and reduced the preformed biofilms. There was increased uptake of propidium iodide by C. albicans cells when exposed to hydroxychavicol thus indicating that the membrane disruption could be the probable mode of action of hydroxychavicol. Conclusions The antifungal activity exhibited by this compound warrants its use as an antifungal agent particularly for treating topical

  17. The In Vitro Efficacy of Essential Oils and Antifungal Drugs Against Prototheca zopfii.

    Science.gov (United States)

    Grzesiak, Barbara; Głowacka, Anna; Krukowski, Henryk; Lisowski, Andrzej; Lassa, Henryka; Sienkiewicz, Monika

    2016-08-01

    The algae of the genus Prototheca are environmental pathogens whose main reservoir is the habitat of cows. They can cause protothecosis in domestic and wild animals, as well as human beings, with the main etiological agents being Prototheca zopfii in animals and Prototheca wickerhamii in humans. The aim of the study was to evaluate the in vitro activity of selected essential oils and antifungal antibiotics against P. zopfii isolates. The material consisted of nine P. zopfii strains isolated from the milk of cows suffering from mastitis. Eight essential oils produced by POLLENA-AROMA, Poland, and nine antifungal agents were tested. The effects of essential oils on P. zopfii were evaluated by microdilution with liquid Sabouraud dextrose broth, and susceptibility to antifungal agents was tested using the disk-diffusion method. All used essential oils inhibited the activity of P. zopfii isolates, with MIC values ranging from 0.2 to 10.5 μl/ml. Cinnamon, clove, and thyme demonstrated the highest activity against the tested P. zopfii strains at concentrations ranging from 0.6 to 1.0 μl/ml. Of the antifungal agents, the tested strains were the most sensitive to nystatin (100 %). The tested essential oils can be used to complement protothecosis therapy in animals and human beings.

  18. Efficacy of oral E1210, a new broad-spectrum antifungal with a novel mechanism of action, in murine models of candidiasis, aspergillosis, and fusariosis.

    Science.gov (United States)

    Hata, Katsura; Horii, Takaaki; Miyazaki, Mamiko; Watanabe, Nao-Aki; Okubo, Miyuki; Sonoda, Jiro; Nakamoto, Kazutaka; Tanaka, Keigo; Shirotori, Syuji; Murai, Norio; Inoue, Satoshi; Matsukura, Masayuki; Abe, Shinya; Yoshimatsu, Kentaro; Asada, Makoto

    2011-10-01

    E1210 is a first-in-class, broad-spectrum antifungal with a novel mechanism of action-inhibition of fungal glycosylphosphatidylinositol biosynthesis. In this study, the efficacies of E1210 and reference antifungals were evaluated in murine models of oropharyngeal and disseminated candidiasis, pulmonary aspergillosis, and disseminated fusariosis. Oral E1210 demonstrated dose-dependent efficacy in infections caused by Candida species, Aspergillus spp., and Fusarium solani. In the treatment of oropharyngeal candidiasis, E1210 and fluconazole each caused a significantly greater reduction in the number of oral CFU than the control treatment (P candidiasis model, mice treated with E1210, fluconazole, caspofungin, or liposomal amphotericin B showed significantly higher survival rates than the control mice (P candidiasis caused by azole-resistant Candida albicans or Candida tropicalis. A 24-h delay in treatment onset minimally affected the efficacy outcome of E1210 in the treatment of disseminated candidiasis. In the Aspergillus flavus pulmonary aspergillosis model, mice treated with E1210, voriconazole, or caspofungin showed significantly higher survival rates than the control mice (P candidiasis, pulmonary aspergillosis, and disseminated fusariosis. These data suggest that further studies to determine E1210's potential for the treatment of disseminated fungal infections are indicated.

  19. Pharmacokinetic evaluation of UK-49,858, a metabolically stable triazole antifungal drug, in animals and humans.

    Science.gov (United States)

    Humphrey, M J; Jevons, S; Tarbit, M H

    1985-11-01

    The pharmacokinetic profile of UK-49,858 (fluconazole), a novel triazole antifungal agent which is being developed for oral and intravenous use, was determined in mice, rats, dogs, and humans. Comparative data following oral and intravenous administration showed that bioavailability was essentially complete in all four species. Peak concentrations in plasma of drug normalized to a 1-mg/kg dose level following oral administration, were relatively high: 0.7, 0.6, 1.1, and 1.4 micrograms/ml in mice, rats, dogs, and humans, respectively. The volumes of distribution ranged between 1.1 liter/kg in mice and 0.7 liter/kg in humans, which are approximate to the values for total body water. Whole body autoradiography studies in mice following intravenous administration of [14C]UK-49,858 demonstrated that the drug was evenly distributed throughout the tissues, including the central nervous system and the gastrointestinal tract. Plasma protein binding was low (11 to 12%) in all species. Marked species differences were observed in elimination half-lives, with mean values of 4.8, 4.0, 14, and 22 h in mice, rats, dogs, and humans, respectively. The major route of elimination of the drug was renal clearance, with about 70% of the dose being excreted unchanged in the urine in each species. Studies with [14C]UK-49,858 on metabolism and excretion (intravenous and oral) in mice and dogs showed that about 90% of the dose was recovered as unchanged drug in urine and feces, confirming the metabolic stability of the drug. This pharmacokinetic profile is markedly different from that of imidazole antifungal drugs and undoubtedly contributes to the excellent efficacy of UK-49,858 in vivo.

  20. Probiotics as Antifungals in Mucosal Candidiasis.

    Science.gov (United States)

    Matsubara, Victor H; Bandara, H M H N; Mayer, Marcia P A; Samaranayake, Lakshman P

    2016-05-01

    Candidais an opportunistic pathogen that causes mucosal and deep systemic candidiasis. The emergence of drug resistance and the side effects of currently available antifungals have restricted their use as long-term prophylactic agents for candidal infections. Given this scenario, probiotics have been suggested as a useful alternative for the management of candidiasis. We analyzed the available data on the efficacy of probiotics in candidal colonization of host surfaces. A number of well-controlled studies indicate that probiotics, particularly lactobacilli, suppressCandidagrowth and biofilm development in vitro.A few clinical trials have also shown the beneficial effects of probiotics in reducing oral, vaginal, and enteric colonization byCandida; alleviation of clinical signs and symptoms; and, in some cases, reducing the incidence of invasive fungal infection in critically ill patients. Probiotics may serve in the future as a worthy ally in the battle against chronic mucosal candidal infections. © The Author 2016. Published by Oxford University Press for the Infectious Diseases Society of America. All rights reserved. For permissions, e-mail journals.permissions@oup.com.

  1. Evaluation of 1,3-benzoxathiol-2-one Derivatives as Potential Antifungal Agents.

    Science.gov (United States)

    Terra, Luciana; de L Chazin, Eliza; de S Sanches, Paola; Saito, Max; de Souza, Marcus V N; Gomes, Claudia R B; Wardell, James L; Wardell, Solange M S V; Sathler, Plinio C; Silva, Gabriela C C; Lione, Viviane O; Kalil, Marcos; Joffily, Ana; Castro, Helena C; Vasconcelos, Thatyana R A

    2018-01-01

    Over the last few years, fungal infections have emerged as a worrisome global public health problem. Candidiasis is a disease caused by Candida species and has been a problem worldwide mainly for immunosuppressed patients. Lately, the resistant strains and side effects have been reported as important issues for treating Candidiasis, which have to be solved by identifying new drugs. The goal of this work was to synthesize a series of 1,3-benzoxathiol-2-one derivatives, XYbenzo[ d][1,3]oxathiol-2-ones, and evaluate their antifungal activity against five Candida species. In vitro antifungal screening test and minimum inhibitory concentration determination were performed according to CLSI protocols using ketoconazole as the reference drug. The cytotoxicity of the most active compounds was evaluated by hemolysis and MTT (Vero cells) assays. Compounds 2 (XY = 6-hydroxy-5-nitro, MIC = 4-32 µg/mL) and 7 (XY = 6-acetoxy-5-nitro, MIC =16-64 µg/mL) showed good results when compared with current antifungals in CLSI values (MIC = 0.04-250 µg/mL). These compounds exhibited a safer cytotoxicity as well as a lower hemolytic profile than ketoconazole. Overall, the in vitro results pointed to the potential of compounds 2 and 7 as new antifungal prototypes to be further explored. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  2. Oral Antidiabetic Agents and Cardiovascular Outcomes

    DEFF Research Database (Denmark)

    Pareek, Manan; Bhatt, Deepak L

    2018-01-01

    Cardiovascular disease is the leading cause of morbidity and mortality among patients with type 2 diabetes; however, a direct protective effect of tight glycemic control remains unproven. In fact, until 2008, when concerns related to rosiglitazone prompted regulatory agencies to mandate assessment...... of cardiovascular safety of new antidiabetic agents, little was known about how these medications affected cardiovascular outcomes. Since then, there has been a considerable increase in the number of cardiovascular trials, which employ a noninferiority design and focus on high-risk populations to establish safety...... in the shortest time possible. In this article, we summarize the 4 major cardiovascular outcome trials of oral antidiabetic agents, completed so far. These include 3 dipeptidyl peptidase-4 inhibitors (saxagliptin, alogliptin, and sitagliptin) and 1 sodium-glucose cotransporter-2 inhibitor (empagliflozin). We...

  3. Antifungal chemical compounds identified using a C. elegans pathogenicity assay.

    Directory of Open Access Journals (Sweden)

    Julia Breger

    2007-02-01

    Full Text Available There is an urgent need for the development of new antifungal agents. A facile in vivo model that evaluates libraries of chemical compounds could solve some of the main obstacles in current antifungal discovery. We show that Candida albicans, as well as other Candida species, are ingested by Caenorhabditis elegans and establish a persistent lethal infection in the C. elegans intestinal track. Importantly, key components of Candida pathogenesis in mammals, such as filament formation, are also involved in nematode killing. We devised a Candida-mediated C. elegans assay that allows high-throughput in vivo screening of chemical libraries for antifungal activities, while synchronously screening against toxic compounds. The assay is performed in liquid media using standard 96-well plate technology and allows the study of C. albicans in non-planktonic form. A screen of 1,266 compounds with known pharmaceutical activities identified 15 (approximately 1.2% that prolonged survival of C. albicans-infected nematodes and inhibited in vivo filamentation of C. albicans. Two compounds identified in the screen, caffeic acid phenethyl ester, a major active component of honeybee propolis, and the fluoroquinolone agent enoxacin exhibited antifungal activity in a murine model of candidiasis. The whole-animal C. elegans assay may help to study the molecular basis of C. albicans pathogenesis and identify antifungal compounds that most likely would not be identified by in vitro screens that target fungal growth. Compounds identified in the screen that affect the virulence of Candida in vivo can potentially be used as "probe compounds" and may have antifungal activity against other fungi.

  4. C O M B I N A T I O N A N T I F U N G A L T H E R A P Y F O R ONYCHOMYCOSIS

    Directory of Open Access Journals (Sweden)

    nur Khamidah

    2018-04-01

    Full Text Available Onychomycosis is a fungal infection of the nail unit including the nail matrix, the nail bed and the nail plate by both dermatophyte and non-dermatophyte agents. It is disturbs not only cosmetic disfigurement, but also it may have an impact on patients’ emotional, social and occupational functioning, finally affecting the overall quality of life. The incidence rate tends to increase, management of onychomycosis is still challenging. Important problems regarding antifungal monotherapy have experienced many failures and recurrences. In general, pharmacological approaches for onychomycosis can be topical or oral antifungal. Antifungal monotherapies often lead to failure treatment, also high incidence of recurrence. One strategy for this problem is a combination antifungal therapy. In vitro studies show the synergistic effect of using combination two antifungals (both oral antifungal or combination topical and oral antifungal, hence it is mycologically or clinically expected to increase the success rate of onychomycosis therapy. This review tries to evaluate the previous study exploring the effectiveness of antifungal combination therapies on onychomycosis. Two oral antifungals usually used are terbinafine as fungicidal agent and itraconazole as fungistatic agent. There is combination between topical and oral antifungal such as itraconazole or terbinafine with amorolfine or ciclopirox, also other combination like griseofulvin and amorolfone or tioconazole. All the combination therapies show better result than monotherapy alone, but it is still difficult to conclude whether antifungal combinations in onychomycosis will increase effectiveness due to variations in therapeutic duration, result definition, and statistical evaluation on existing studies. Further research is required with longer duration of observation, uniform patient criteria and definition of success, random control and blinding to minimize bias.

  5. Past, Recent Progresses and Future Perspectives of Nanotechnology Applied to Antifungal Agents.

    Science.gov (United States)

    Roque, Luis; Molpeceres, Jesus; Reis, Claudia; Rijo, Patrícia; Reis, Catarina Pinto

    2017-01-01

    Candida species remain a significant cause of nosocomial bloodstream infections, associated with prolonged hospital stay in the ICU and high healthcare cost. The incidence of Candida is very high in certain risk groups of patients (AIDS, diabetes, cancer, etc.). Recent developments of nanotechnology have strongly contributed to the design of new multifunctional drug carriers that improve drug bioavailability through a controlled and prolonged release profile or even through a more specific targeted delivery of the antifungal agent. Those types of systems have strongly increased with a progressive generation of new structures, permitting the conjunction of new materials, biomolecules, physical and chemical techniques, for better outcomes. Nanotechnology shows expanded possibilities within the medical field and in the case of the yeast infections it may overcome several issues related with the fungal proliferation or higher inhibition of the pathogen causing the infection. This review covers a period of the most representative research of Candidiasis since 1993 to the present. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  6. Azole Antifungal Resistance in Candida albicans and Emerging Non-albicans Candida Species

    Science.gov (United States)

    Whaley, Sarah G.; Berkow, Elizabeth L.; Rybak, Jeffrey M.; Nishimoto, Andrew T.; Barker, Katherine S.; Rogers, P. David

    2017-01-01

    Within the limited antifungal armamentarium, the azole antifungals are the most frequent class used to treat Candida infections. Azole antifungals such as fluconazole are often preferred treatment for many Candida infections as they are inexpensive, exhibit limited toxicity, and are available for oral administration. There is, however, extensive documentation of intrinsic and developed resistance to azole antifungals among several Candida species. As the frequency of azole resistant Candida isolates in the clinical setting increases, it is essential to elucidate the mechanisms of such resistance in order to both preserve and improve upon the azole class of antifungals for the treatment of Candida infections. This review examines azole resistance in infections caused by C. albicans as well as the emerging non-albicans Candida species C. parapsilosis, C. tropicalis, C. krusei, and C. glabrata and in particular, describes the current understanding of molecular basis of azole resistance in these fungal species. PMID:28127295

  7. Synthesis and Antifungal Activity of Novel 3-Caren-5-One Oxime Esters.

    Science.gov (United States)

    Huang, Min; Duan, Wen-Gui; Lin, Gui-Shan; Li, Kun; Hu, Qiong

    2017-09-12

    A series of novel 3-caren-5-one oxime esters were designed and synthesized by multi-step reactions in an attempt to develop potent antifungal agents. Two E - Z stereoisomers of the intermediate 3-caren-5-one oxime were separated by column chromatography for the first time. The structures of all the intermediates and target compounds were confirmed by UV-Vis, FTIR, NMR, ESI-MS, and elemental analysis. The antifungal activity of the target compounds was preliminarily evaluated by the in vitro method against Fusarium oxysporum f. sp. cucumerinum , Physalospora piricola , Alternaria solani , Cercospora arachidicola , Gibberella zeae, Rhizoeotnia solani , Bipolaris maydis , and Colleterichum orbicalare at 50 µg/mL. The target compounds exhibited best antifungal activity against P. piricola , in which compounds ( Z )- 4r (R = β -pyridyl), ( Z )- 4q (R = α -thienyl), ( E )- 4f' (R = p -F Ph), ( Z )- 4i (R = m -Me Ph), ( Z )- 4j (R = p -Me Ph), and ( Z )- 4p (R = α -furyl) had inhibition rates of 97.1%, 87.4%, 87.4%, 85.0%, 81.9%, and 77.7%, respectively, showing better antifungal activity than that of the commercial fungicide chlorothanil. Also, compound ( Z )- 4r (R = β -pyridyl) displayed remarkable antifungal activity against all the tested fungi, with inhibition rates of 76.7%, 82.7%, 97.1%, 66.3%, 74.7%, 93.9%, 76.7% and 93.3%, respectively, showing better or comparable antifungal activity than that of the commercial fungicide chlorothanil. Besides, the E-Z isomers of the target oxime esters were found to show obvious differences in antifungal activity. These results provide an encouraging framework that could lead to the development of potent novel antifungal agents.

  8. Comparison of two systemic antifungal agents, itraconazole and terbinafine, for the treatment of dermatophytosis in European hedgehogs (Erinaceus europaeus).

    Science.gov (United States)

    Bexton, Steve; Nelson, Helen

    2016-12-01

    Dermatophytosis caused by Trichophyton erinacei is a common scaling and crusting skin disease affecting European hedgehogs (Erinaceus europaeus) admitted to wildlife rescue centres. The application of topical therapy can be challenging because wild hedgehogs are subject to stress and often roll into a ball when handled. Systemic antifungal therapy is more convenient but has not been evaluated in this species. To compare the efficacy of oral itraconazole versus oral terbinafine for the treatment of dermatophytosis affecting hedgehogs. A treatment trial was undertaken in a wildlife hospital involving 165 hedgehogs with naturally occurring dermatophytosis. Animals were randomly divided into two groups and treated with either itraconazole or terbinafine orally for 28 days. The therapeutic efficacy was evaluated after 14 and 28 days by mycological culture and clinical dermatological lesion scores. Both drugs were well tolerated and clinically effective. After 14 and 28 days of treatment, the respective mycological cure rate was 36.6% and 65.9% for the itraconazole-treated group and 92.8% and 98.8% for the terbinafine-treated group. Itraconazole and terbinafine were both effective for the treatment of dermatophytosis affecting hedgehogs; however, terbinafine was more effective. © 2016 ESVD and ACVD.

  9. Topical antifungals for seborrhoeic dermatitis

    Science.gov (United States)

    Okokon, Enembe O; Verbeek, Jos H; Ruotsalainen, Jani H; Ojo, Olumuyiwa A; Bakhoya, Victor Nyange

    2015-01-01

    Background Seborrhoeic dermatitis is a chronic inflammatory skin condition that is distributed worldwide. It commonly affects the scalp, face and flexures of the body. Treatment options include antifungal drugs, steroids, calcineurin inhibitors, keratolytic agents and phototherapy. Objectives To assess the effects of antifungal agents for seborrhoeic dermatitis of the face and scalp in adolescents and adults. A secondary objective is to assess whether the same interventions are effective in the management of seborrhoeic dermatitis in patients with HIV/AIDS. Search methods We searched the following databases up to December 2014: the Cochrane Skin Group Specialised Register, the Cochrane Central Register of Controlled Trials (CENTRAL) (2014, Issue 11), MEDLINE (from 1946), EMBASE (from 1974) and Latin American Caribbean Health Sciences Literature (LILACS) (from 1982). We also searched trials registries and checked the bibliographies of published studies for further trials. Selection criteria Randomised controlled trials of topical antifungals used for treatment of seborrhoeic dermatitis in adolescents and adults, with primary outcome measures of complete clearance of symptoms and improved quality of life. Data collection and analysis Review author pairs independently assessed eligibility for inclusion, extracted study data and assessed risk of bias of included studies. We performed fixed-effect meta-analysis for studies with low statistical heterogeneity and used a random-effects model when heterogeneity was high. Main results We included 51 studies with 9052 participants. Of these, 45 trials assessed treatment outcomes at five weeks or less after commencement of treatment, and six trials assessed outcomes over a longer time frame. We believe that 24 trials had some form of conflict of interest, such as funding by pharmaceutical companies. Among the included studies were 12 ketoconazole trials (N = 3253), 11 ciclopirox trials (N = 3029), two lithium trials (N = 141

  10. Antifungal Activity of Lavandula Angustifolia and Quergues Infectoria Extracts in Comparison with Nystatin on Candida Albicans

    Directory of Open Access Journals (Sweden)

    F. Nouri

    2016-07-01

    Full Text Available Introduction & Objective: Nowadays,herbal extracts are used to treat diseases, especially infec-tious ones. Candida albicans is the most common causes of oral opportunistic infections.In this study, antifungal effects of two herbal extracts were evaluated on an oral pathogen i.e. Candida albicans. Materials & Methods: In this descriptive- analytic study, the Department of Prosthodontics, ,Tehran University of Medical Sciences, school of Dentistry the oral samples of 25 patients with denture stomatitis were collected using sterile swabs. Then the isolated candida albicans and standard candida albicans PTCC 5027 were cultured. The antifungal effect was evaluated with disk plate method. Nystatin and methanol were used as positive and negative control groups, respectively. The power of antifungal activity was evaluated with the inhibition zone diameter of each of the extracts. At the end, the data were analyzed by ANOVA and Fried-man statistical tests. Results: Results showed that extracts of Querques infectoria had great antifungal effects. There was not statistically significant difference between nystatine and Querques infectoria extract (P>0.05 however , Querques infectoria was statistically more effective than lavender extract and nystatin showed the highest antifungal activity (P <0.001. Conclusion: This study showed that plant extracts had positive effects on Candida albicans as compared to nystatin. Thus, we hope to find new herbal medicines and compounds to treat candidiasis in the future. (Sci J Hamadan Univ Med Sci 2016; 23 (2:172-178

  11. Efficacy of Oral E1210, a New Broad-Spectrum Antifungal with a Novel Mechanism of Action, in Murine Models of Candidiasis, Aspergillosis, and Fusariosis▿

    Science.gov (United States)

    Hata, Katsura; Horii, Takaaki; Miyazaki, Mamiko; Watanabe, Nao-aki; Okubo, Miyuki; Sonoda, Jiro; Nakamoto, Kazutaka; Tanaka, Keigo; Shirotori, Syuji; Murai, Norio; Inoue, Satoshi; Matsukura, Masayuki; Abe, Shinya; Yoshimatsu, Kentaro; Asada, Makoto

    2011-01-01

    E1210 is a first-in-class, broad-spectrum antifungal with a novel mechanism of action—inhibition of fungal glycosylphosphatidylinositol biosynthesis. In this study, the efficacies of E1210 and reference antifungals were evaluated in murine models of oropharyngeal and disseminated candidiasis, pulmonary aspergillosis, and disseminated fusariosis. Oral E1210 demonstrated dose-dependent efficacy in infections caused by Candida species, Aspergillus spp., and Fusarium solani. In the treatment of oropharyngeal candidiasis, E1210 and fluconazole each caused a significantly greater reduction in the number of oral CFU than the control treatment (P candidiasis model, mice treated with E1210, fluconazole, caspofungin, or liposomal amphotericin B showed significantly higher survival rates than the control mice (P candidiasis caused by azole-resistant Candida albicans or Candida tropicalis. A 24-h delay in treatment onset minimally affected the efficacy outcome of E1210 in the treatment of disseminated candidiasis. In the Aspergillus flavus pulmonary aspergillosis model, mice treated with E1210, voriconazole, or caspofungin showed significantly higher survival rates than the control mice (P candidiasis, pulmonary aspergillosis, and disseminated fusariosis. These data suggest that further studies to determine E1210's potential for the treatment of disseminated fungal infections are indicated. PMID:21788462

  12. Antifungal activities of ethanolic extract from Jatropha curcas seed cake.

    Science.gov (United States)

    Saetae, Dolaporn; Suntornsuk, Worapot

    2010-02-01

    Phorbol ester extraction was carried out from Jatropha curcas seed cake, a by-product from the bio-diesel fuel industry. Four repeated extractions from 5 g J. curcas seed cake using 15 ml of 90% (v/v) ethanol and a shaking speed of 150 rev/min gave the highest yield of phosbol esters. The ethanolic extract of J. curcas seed cake showed antifungal activities against important phytofungal pathogens: Fusarium oxysporum, Pythium aphanidermatum, Lasiodiplodia theobromae, Curvularia lunata, Fusarium semitectum, Colletotrichum capsici and Colletotrichum gloeosporiodes. The extract contained phorbol esters mainly responsible for antifungal activities. The extract could therefore be used as an antifungal agent for agricultural applications.

  13. Determination of a new promising natural antifungal product against Penicillium digitatum

    International Nuclear Information System (INIS)

    Balkan, S.

    2018-01-01

    The present study deals with the fungal infections, a great amount of food losses occur worldwide. The infections caused by Penicillium digitatum, green mold agent in Citrus fruits, are just one of those losses. In this study, determining a novel environmentally-friendly antifungal product against green mold agent is aimed. Total 39 plant species, naturally growing in Kirklareli (Turkey) were scanned in terms of antifungal activity against P. digitatum. Digitalis viridiflora, Medicago lupulina and Sambucus ebulus, inhibited the micelle development of P. digitatum completely (100%), while Lythrum salicaria, Epilobium roseum and Prunella vulgaris inhibited the micelle development over 75%. D. viridiflora has showed the least MIC value (250 mu g/ml) against P. digitatum. In SEM analysis, flattening, collapse and wrinkling effects of D. viridiflora on hyphae structure of P. digitatum were also observed during the present investigation. In the lemons treated with 8 mg/ml D. viridiflora aqueous extract, 73.99% regression in the lesion diameters has also been observed. As a result, in order to avoid green mold infection caused by P. digitatum occurring in lemon fruits, D. viridiflora can be used as a natural antifungal agent. (author)

  14. Synthesis and Antifungal Activity of Novel 3-Caren-5-One Oxime Esters

    Directory of Open Access Journals (Sweden)

    Min Huang

    2017-09-01

    Full Text Available A series of novel 3-caren-5-one oxime esters were designed and synthesized by multi-step reactions in an attempt to develop potent antifungal agents. Two E-Z stereoisomers of the intermediate 3-caren-5-one oxime were separated by column chromatography for the first time. The structures of all the intermediates and target compounds were confirmed by UV-Vis, FTIR, NMR, ESI-MS, and elemental analysis. The antifungal activity of the target compounds was preliminarily evaluated by the in vitro method against Fusarium oxysporum f. sp. cucumerinum, Physalospora piricola, Alternaria solani, Cercospora arachidicola, Gibberella zeae, Rhizoeotnia solani, Bipolaris maydis, and Colleterichum orbicalare at 50 µg/mL. The target compounds exhibited best antifungal activity against P. piricola, in which compounds (Z-4r (R = β-pyridyl, (Z-4q (R = α-thienyl, (E-4f′ (R = p-F Ph, (Z-4i (R = m-Me Ph, (Z-4j (R = p-Me Ph, and (Z-4p (R = α-furyl had inhibition rates of 97.1%, 87.4%, 87.4%, 85.0%, 81.9%, and 77.7%, respectively, showing better antifungal activity than that of the commercial fungicide chlorothanil. Also, compound (Z-4r (R = β-pyridyl displayed remarkable antifungal activity against all the tested fungi, with inhibition rates of 76.7%, 82.7%, 97.1%, 66.3%, 74.7%, 93.9%, 76.7% and 93.3%, respectively, showing better or comparable antifungal activity than that of the commercial fungicide chlorothanil. Besides, the E-Z isomers of the target oxime esters were found to show obvious differences in antifungal activity. These results provide an encouraging framework that could lead to the development of potent novel antifungal agents.

  15. 8-Amido-Bearing pseudomycin B (PSB) analogue: novel antifungal agents.

    Science.gov (United States)

    Zhang, Y Z; Sun, X; Zeckner, D J; Sachs, R K; Current, W L; Chen, S H

    2001-01-22

    During the course of a structure-activity relationship (SAR) study on novel depsinonapeptide pseudomycin B, we synthesized a total of 12 8-amidopseudomycin analogues via standard two-step sequence from either ZPSB 2 or AllocPSB 3. A number of these amides exhibited good in vitro antifungal activities.

  16. Adjuvant antifungal therapy using tissue tolerable plasma on oral mucosa and removable dentures in oral candidiasis patients: a randomised double-blinded split-mouth pilot study.

    Science.gov (United States)

    Preissner, Saskia; Kastner, Isabell; Schütte, Eyke; Hartwig, Stefan; Schmidt-Westhausen, Andrea Maria; Paris, Sebastian; Preissner, Robert; Hertel, Moritz

    2016-07-01

    Extended use of antimycotics in oral candidiasis therapy gives rise to problems related to fungal drug resistance. The aim of this pilot study was to investigate the efficacy of tissue tolerable plasma (TTP) in denture stomatitis patients. It was hypothesised that (I): erythema and (IIa): complaint remission would be accelerated and (IIb): colony forming unit (CFU) reduction would be improved. The halves of the upper jaws of eight patients were randomly assigned to control (nystatin, chlorhexidine and placebo treatment) and test sides (nystatin, chlorhexidine and TTP administered six times each 7 days). The patients and the investigators, who were different from the therapists, were both blinded. Compared to the control sides, the erythema surface was reduced significantly more extensively on the test sides between 2 and 6 weeks of antifungal therapy (P ≤ 0.05). Visual analogue scale values and the frequency of moderate or heavy growth of Candida post-treatment did not differ significantly between both sides (P > 0.05). The primary hypothesis was confirmed, which may be interpreted as an accelerated remission. As drug therapy is usually limited to the time in which signs of infection are present, TTP might help reducing antifungal use. Even though the secondary hypotheses were not confirmed, persistence of Candida might be only colonisation. © 2016 Blackwell Verlag GmbH.

  17. Oral gadopentetate dimeglumine administration as a negative gastrointestinal contrast agent to improve image quality of MR cholangiopancreatography

    International Nuclear Information System (INIS)

    Chen Yi; Xu Yikai; Zhao Yuhui; Wang Guisheng

    2008-01-01

    Objective: To choose optimal concentration and volume of Gd-DTPA solution as a oral gastrointestinal negative contrast agent for MRCP. To evaluate the role of Gd-DTPA solution in improving image quality of MRCP. Methods: In vitro experiment: Gd-DTPA solution was made with different concentrations. T 1 WI, T 2 WI, two-dimensional single slice fast spin echo sequence and three-dimensional half-fourier acquisition single-shot fast spin echo sequence were performed to measure the signal intensity of these contrast agents respectively, so Gd-DTPA solution with the optimal concentration can be decided as oral negative gastrointestinal contrast agent on MRCP. Clinical study: The Gd-DTPA solution with optimal concentration and volume was regarded as an oral negative gastrointestinal contrast agent of MRCP. Twenty- four' patients were performed with MRCP before and after (5-10 minutes and 10-15 minutes) administration of oral negative gastrointestinal contrast agent and image quality was analyzed. Statistical analysis was performed using analysis of variance with SPSS 10.0. Results: When the concentration of Gd-DTPA solution was ≤0.01 mol/L, the contrast agent was hyperintense on T 1 WI. On T 2 WI, when the concentration was ≥0.015 mol/L, it was as hypointense as basic ground; On 2D FSE MRCP images, controls were hyperintense and the contrast agent with concentration ranging from 0.0025 mol/L to 0.03 mol/L was hypointense. On 3D HEAST MRCP image, controls were hyperintense and when the concentration of Gd-DTPA was ≥0.01 mol, the contrast agent was hypointense. The Gd-DTPA solution with the concentration of 0.01 mol/L and the volume of 100 ml was chosen as MRCP oral negative gastrointestinal contrast agent. On MRCP images after oral administration of the contrast agent, in 10-15 minutes, the average grade scores within 24 patients of the intrahepatic bile duct, the common hepatic bile duct, the gall bladder, the common bile duct and pancreatic duct (the average grade

  18. Congenital malformations in offspring of diabetic women treated with oral hypoglycaemic agents during embryogenesis

    DEFF Research Database (Denmark)

    Hellmuth, E; Damm, P; Mølsted-Pedersen, L

    1994-01-01

    A markedly increased risk (50%) of congenital malformations in the offspring of women treated with oral hypoglycaemic agents during the first trimester has recently been reported. With this background, the medical records of a consecutive sample of 25 pregnant Type 2 diabetic women treated...... with oral hypoglycaemic agents during embryogenesis between 1966 and 1991 in the diabetic service of a university hospital, were studied retrospectively. None of the infants had major congenital malformations disclosed in the neonatal period (0%, 97.5% confidence interval 0.0-13.7%), but one minor...... congenital malformation was found (4.0%, 95% confidence interval 0.1-20.3%). Although this study, due to the limited number of pregnancies examined, does not exclude an association between treatment with oral hypoglycaemic agents at the time of embryogenesis and major congenital malformations...

  19. Experimental models in predicting topical antifungal efficacy: practical aspects and challenges.

    Science.gov (United States)

    Lai, J; Maibach, H I

    2009-01-01

    What are efficient screening models for improved topical antifungals? The use of minimum inhibitory concentrations (MICs) as one such parameter is discussed; we focus on the use of animal membranes for in vitro testing while highlighting the pros and cons of each model, exploring alternatives and discussing the importance of data transferability to humans and the influence of penetration kinetics in topical antifungal efficacy. Ultimately, the gold standard of testing is in vivo in humans; however, initiating with human testing, especially for novel topical antifungal agents, may be impractical, which is why we seek the ideal experimental model that most closely mimics human skin. We conclude that the pig may be an appropriate model membrane for topical antifungal testing based on its similarities in anatomical structure, physiology and permeation to human skin. Most importantly, pig and human skins appear equally permeable to several antifungals in prior in vitro and in vivo work. We do not discuss all prior work but highlight important issues in designing the protocol and parameters of the ideal experimental model for topical antifungals. Copyright 2009 S. Karger AG, Basel.

  20. A Novel Mechanistic Approach to Identify New Antifungal Lead ...

    African Journals Online (AJOL)

    Available online at http://www.tjpr.org ... The MIC of the more effective compounds, delta-decalactone and mandelonitrile ... screening which is increasingly used as a cost- ..... AD. Lanomycin and glucolanomycin, antifungal agents produced by ...

  1. The in vitro antifungal activity of sudanese medicinal plants against Madurella mycetomatis, the eumycetoma major causative agent.

    Science.gov (United States)

    Elfadil, Hassabelrasoul; Fahal, Ahmed; Kloezen, Wendy; Ahmed, Elhadi M; van de Sande, Wendy

    2015-03-01

    Eumycetoma is a debilitating chronic inflammatory fungal infection that exists worldwide but it is endemic in many tropical and subtropical regions. The major causative organism is the fungus Madurella mycetomatis. The current treatment of eumycetoma is suboptimal and characterized by low cure rate and high recurrence rates. Hence, an alternative therapy is needed to address this. Here we determined the antifungal activity of seven Sudanese medicinal plant species against Madurella mycetomatis. Of these, only three species; Boswellia papyrifera, Acacia nubica and Nigella sativa, showed some antifungal activity against M. mycetomatis and were further studied. Crude methanol, hexane and defatted methanol extracts of these species were tested for their antifungal activity. B. papyrifera had the highest antifungal activity (MIC50 of 1 ug/ml) and it was further fractionated. The crude methanol and the soluble ethyl acetate fractions of B. papyrifera showed some antifungal activity. The Gas-Liquid-Chromatography hybrid Mass-Spectrophotometer analysis of these two fractions showed the existence of beta-amyrin, beta-amyrone, beta-Sitosterol and stigmatriene. Stigmatriene had the best antifungal activity, compared to other three phytoconstituents, with an MIC-50 of 32 μg/ml. Although the antifungal activity of the identified phytoconstituents was only limited, the antifungal activity of the complete extracts is more promising, indicating synergism. Furthermore these plant extracts are also known to have anti-inflammatory activity and can stimulate wound-healing; characteristics which might also be of great value in the development of novel therapeutic drugs for this chronic inflammatory disease. Therefore further exploration of these plant species in the treatment of mycetoma is encouraging.

  2. Hypoglycaemia from misuse of oral hypoglycaemic agent in patients ...

    African Journals Online (AJOL)

    In conclusion, misuse of oral hypoglycaemic agents (OHA) to treat LUTS with subsequent presentation in hypoglycaemic coma should be of concern to the health care provider especially the urologist. It is of no benefit and constitutes drug abuse that should be discouraged. Keywords: drug abuse, hypoglycaemia, lower ...

  3. Isolation and antifungal screening of endophytic fungi from Erigeron canadensis

    Directory of Open Access Journals (Sweden)

    Xuelian Bai

    2017-07-01

    Full Text Available Sixteen fungal strains isolated from the Erigeron canadensis, one of traditional Chinese medicines used to treat the pathogenic infection and dysentery, were evaluated for their antifungal activities against one human pathogen Candida albicans, and two phytopathogens, Colletotrichum fructicola and Rhizoctonia cerealis. The bioassay results indicated that the ethyl acetate extract of the fermentation broth of these fungal endophytes had stronger antimicrobial activities. Among these endophytic strains, the ethyl acetate extracts of strains NPR003 and NPR005 showed the strongest inhibitory effects and has potential application in the discovery of new antifungal agents. This was the first report on the isolation of endophytic fungi from E. canadensis and evaluation of their antifungal activities.

  4. Extracellular phospholipase production of oral Candida albicans isolates from smokers, diabetics, asthmatics, denture wearers and healthy individuals following brief exposure to polyene, echinocandin and azole antimycotics

    Directory of Open Access Journals (Sweden)

    Arjuna N.B. Ellepola

    Full Text Available Abstract Objective Candida albicans is the primary causative agent of oral candidosis, and one of its key virulent attributes is considered to be its ability to produce extracellular phospholipases that facilitate cellular invasion. Oral candidosis can be treated with polyenes, and azoles, and the more recently introduced echinocandins. However, once administered, the intraoral concentration of these drugs tend to be sub-therapeutic and rather transient due to factors such as the diluent effect of saliva and cleansing effect of the oral musculature. Hence, intra-orally, the pathogenic yeasts may undergo a brief exposure to antifungal drugs. We, therefore, evaluated the phospholipase production of oral C. albicans isolates following brief exposure to sub-therapeutic concentrations of the foregoing antifungals. Materials and methods Fifty C. albicans oral isolates obtained from smokers, diabetics, asthmatics using steroid inhalers, partial denture wearers and healthy individuals were exposed to sub-therapeutic concentrations of nystatin, amphotericin B, caspofungin, ketoconazole and fluconazole for one hour. Thereafter the drugs were removed and the phospholipase production was determined by a plate assay using an egg yolk-agar medium. Results The phospholipase production of these isolates was significantly suppressed with a percentage reduction of 10.65, 12.14, 11.45 and 6.40% following exposure to nystatin, amphotericin B, caspofungin and ketoconazole, respectively. This suppression was not significant following exposure to fluconazole. Conclusions Despite the sub-therapeutic, intra oral, bioavailability of polyenes, echinocandins and ketoconazole, they are likely to produce a persistent antifungal effect by suppressing phospholipase production, which is a key virulent attribute of this common pathogenic yeast.

  5. Tolerability and safety of antifungal drugs

    Directory of Open Access Journals (Sweden)

    Francesco Scaglione

    2013-08-01

    Full Text Available When treating critically ill patients, as those with fungal infections, attention should be focused on the appropriate use of drugs, especially in terms of dose, safety, and tolerability. The fungal infection itself and the concomitant physiological disorders concur to increase the risk of mortality in these patients, therefore the use of any antifungal agent should be carefully evaluated, considering both the direct action on the target fungus and the adverse effects eventually caused. Among antifungal drugs, echinocandins have the greatest tolerability. In fact, unlike amphotericin B, showing nephrotoxicity, and azoles, which are hepatotoxic, the use of echinocandins doesn’t result in major adverse events.http://dx.doi.org/10.7175/rhc.v4i2s.873

  6. Antifungal activity of multifunctional Fe 3O 4-Ag nanocolloids

    Science.gov (United States)

    Chudasama, Bhupendra; Vala, Anjana K.; Andhariya, Nidhi; Upadhyay, R. V.; Mehta, R. V.

    2011-05-01

    In recent years, rapid increase has been observed in the population of microbes that are resistant to conventionally used antibiotics. Antifungal drug therapy is no exception and now resistance to many of the antifungal agents in use has emerged. Therefore, there is an inevitable and urgent medical need for antibiotics with novel antimicrobial mechanisms. Aspergillus glaucus is the potential cause of fatal brain infections and hypersensitivity pneumonitis in immunocompromised patients and leads to death despite aggressive multidrug antifungal therapy. In the present article, we describe the antifungal activity of multifunctional core-shell Fe 3O 4-Ag nanocolloids against A. glaucus isolates. Controlled experiments are also carried out with Ag nanocolloids in order to understand the role of core (Fe 3O 4) in the antifungal action. The minimum inhibitory concentration (MIC) of nanocolloids is determined by the micro-dilution method. MIC of A. glaucus is 2000 μg/mL. The result is quite promising and requires further investigations in order to develop a treatment methodology against this death causing fungus in immunocompromised patients.

  7. Antifungal activity of the lemongrass oil and citral against Candida spp.

    Directory of Open Access Journals (Sweden)

    Cristiane de Bona da Silva

    Full Text Available Superficial mycoses of the skin are among the most common dermatological infections, and causative organisms include dermatophytic, yeasts, and non-dermatophytic filamentous fungi. The treatment is limited, for many reasons, and new drugs are necessary. Numerous essential oils have been tested for both in vitro and in vivo antifungal activity and some pose much potential as antifungal agents. By using disk diffusion assay, we evaluated the antifungal activity of lemongrass oil and citral against yeasts of Candida species (Candida albicans, C. glabrata, C. krusei, C. parapsilosis and C. tropicalis. This study showed that lemongrass oil and citral have a potent in vitro activity against Candida spp.

  8. The in vitro antifungal activity of sudanese medicinal plants against Madurella mycetomatis, the eumycetoma major causative agent.

    Directory of Open Access Journals (Sweden)

    Hassabelrasoul Elfadil

    2015-03-01

    Full Text Available Eumycetoma is a debilitating chronic inflammatory fungal infection that exists worldwide but it is endemic in many tropical and subtropical regions. The major causative organism is the fungus Madurella mycetomatis. The current treatment of eumycetoma is suboptimal and characterized by low cure rate and high recurrence rates. Hence, an alternative therapy is needed to address this. Here we determined the antifungal activity of seven Sudanese medicinal plant species against Madurella mycetomatis. Of these, only three species; Boswellia papyrifera, Acacia nubica and Nigella sativa, showed some antifungal activity against M. mycetomatis and were further studied. Crude methanol, hexane and defatted methanol extracts of these species were tested for their antifungal activity. B. papyrifera had the highest antifungal activity (MIC50 of 1 ug/ml and it was further fractionated. The crude methanol and the soluble ethyl acetate fractions of B. papyrifera showed some antifungal activity. The Gas-Liquid-Chromatography hybrid Mass-Spectrophotometer analysis of these two fractions showed the existence of beta-amyrin, beta-amyrone, beta-Sitosterol and stigmatriene. Stigmatriene had the best antifungal activity, compared to other three phytoconstituents, with an MIC-50 of 32 μg/ml. Although the antifungal activity of the identified phytoconstituents was only limited, the antifungal activity of the complete extracts is more promising, indicating synergism. Furthermore these plant extracts are also known to have anti-inflammatory activity and can stimulate wound-healing; characteristics which might also be of great value in the development of novel therapeutic drugs for this chronic inflammatory disease. Therefore further exploration of these plant species in the treatment of mycetoma is encouraging.

  9. Diminished Antimicrobial Peptide and Antifungal Antibiotic Activities against Candida albicans in Denture Adhesive

    Directory of Open Access Journals (Sweden)

    Amber M. Bates

    2017-02-01

    Full Text Available The underlying causes of denture stomatitis may be related to the long-term use of adhesives, which may predispose individuals to oral candidiasis. In this study, we hypothesize that antimicrobial peptides and antifungal antibiotics have diminished anti-Candida activities in denture adhesive. To show this, nine antimicrobial peptides and five antifungal antibiotics with and without 1.0% denture adhesive were incubated with Candida albicans strains ATCC 64124 and HMV4C in radial diffusion assays. In gels with 1.0% adhesive, HNP-1, HBD2, HBD3, IP-10, LL37 (only one strain, histatin 5 (only one strain, lactoferricin B, and SMAP28 showed diminished activity against C. albicans. In gels with 1.0% adhesive, amphotericin B and chlorhexidine dihydrochloride were active against both strains of C. albicans. These results suggest that denture adhesive may inactivate innate immune mediators in the oral cavity increasing the risk of C. albicans infections, but inclusion of antifungal antibiotics to denture adhesive may aid in prevention or treatment of Candida infections and denture stomatitis.

  10. Enhancement of the antifungal activity of antimicrobial drugs by Eugenia uniflora L.

    Science.gov (United States)

    Santos, Karla K A; Matias, Edinardo F F; Tintino, Saulo R; Souza, Celestina E S; Braga, Maria F B M; Guedes, Gláucia M M; Costa, José G M; Menezes, Irwin R A; Coutinho, Henrique Douglas Melo

    2013-07-01

    Candidiasis is the most frequent infection by opportunistic fungi such as Candida albicans, Candida tropicalis, and Candida krusei. Ethanol extract from Eugenia uniflora was assayed, for its antifungal activity, either alone or combined with four selected chemotherapeutic antimicrobial agents, including anphotericin B, mebendazole, nistatin, and metronidazole against these strains. The obtained results indicated that the association of the extract of E. uniflora to metronidazole showed a potential antifungal activity against C. tropicalis. However, no synergistic activity against the other strains was observed, as observed when the extract was associated with the other, not enhancing their antifungal activity.

  11. Susceptibility to antifungal agents and enzymatic activity of Candida haemulonii and Cutaneotrichosporon dermatis isolated from soft corals on the Brazilian reefs.

    Science.gov (United States)

    Pagani, Danielle M; Heidrich, Daiane; Paulino, Gustavo V B; de Oliveira Alves, Karine; Dalbem, Paula T; de Oliveira, Caroline F; Andrade, Zélia M M; Silva, Carolini; Correia, Monica D; Scroferneker, Maria Lúcia; Valente, Patricia; Landell, Melissa Fontes

    2016-12-01

    Candida is a common fungus with the capacity to cause infections in humans. However, most studies have concentrated on clinical isolates and little is known about the identity, ecology and drug resistance of free living species/strains. Here, we isolate eight strains of Candida haemulonii and four strains of Cutaneotrichosporon dermatis from three marine cnidarian zoanthids species (Palythoa caribaeorum, Palythoa variabilis and Zoanthus sociatus) collected from Brazilian coral reefs. Strains were identified by sequencing of the D1/D2 domain LSU rDNA and ITS region. We tested these environmental isolates for their capacity to grow in media with increasing concentration of NaCl, capacity to grow in different temperatures, enzymatic activity and antifungal susceptibility. For C. haemulonii, all strains strongly produced gelatinase, esterase and albuminase and were either able to express lipase, phospholipase and keratinase, but not express urease and DNase. The strains were able to grow at 37 °C, but not at 39 °C, and except for LMS 40, all of them could grow in a 10 % NaCl medium. All isolates were resistant to all antifungals tested, with exception for ketoconazole and tioconazole (MIC = 2 µg/mL). For C. dermatis, all strains could grow at 39 °C and could not express phospholipase, keratinase or gelatinase. However, all were capable of expressing urease, lipase and esterase. Three out of four strains could grow in a 10 % NaCl medium, but none grew in a 30 % NaCl medium. The strains showed high values of minimal inhibitory concentration. LMPV 90 was resistant to tioconazole, terbinafine, fluconazole and posaconazole, and LMS 38 was resistant to all antifungal agents tested. We discuss the characterization of C. haemulonii and C. dermatis as a possible emerging pathogen due to its animal-related enzymatic arsenal and antifungal resistance.

  12. Antifungal activity of multifunctional Fe3O4-Ag nanocolloids

    International Nuclear Information System (INIS)

    Chudasama, Bhupendra; Vala, Anjana K.; Andhariya, Nidhi; Upadhyay, R.V.; Mehta, R.V.

    2011-01-01

    In recent years, rapid increase has been observed in the population of microbes that are resistant to conventionally used antibiotics. Antifungal drug therapy is no exception and now resistance to many of the antifungal agents in use has emerged. Therefore, there is an inevitable and urgent medical need for antibiotics with novel antimicrobial mechanisms. Aspergillus glaucus is the potential cause of fatal brain infections and hypersensitivity pneumonitis in immunocompromised patients and leads to death despite aggressive multidrug antifungal therapy. In the present article, we describe the antifungal activity of multifunctional core-shell Fe 3 O 4 -Ag nanocolloids against A. glaucus isolates. Controlled experiments are also carried out with Ag nanocolloids in order to understand the role of core (Fe 3 O 4 ) in the antifungal action. The minimum inhibitory concentration (MIC) of nanocolloids is determined by the micro-dilution method. MIC of A. glaucus is 2000 μg/mL. The result is quite promising and requires further investigations in order to develop a treatment methodology against this death causing fungus in immunocompromised patients. - Research Highlights: →Synthesis of Fe 3 O 4 -Ag core-shell nanocolloids. →Antifungal activity of Fe 3 O 4 -Ag nanocolloids against Aspergillus glaucus isolates. →The MIC value for A. glaucus is 2000 μg/mL. →Antifungal activity is better or comparable with most prominent antibiotics.

  13. Evaluation of potential practical oral contrast agents for pediatric magnetic resonance imaging

    International Nuclear Information System (INIS)

    Bisset, G.S. III; Cincinnati Univ., OH; Children's Hospital Medical Center, Cincinnati, OH

    1989-01-01

    Development of a practical oral contrast agent for magnetic resonance imaging is necessary to improve differentiation of bowel from adjacent structures. In order to find a readily available, inexpensive, non-toxic, palatable solution for use in the pediatric population, several formulas, milk products and a common oral sedative were evaluated in vitro. T1, T2 and signal intensity measurements were performed on a 1.5 T system. Similac with standard iron proved to be a useful high signal intensity agent on multiple pulse sequences. Early in vivo experience in four normal volunteers indicates that this agent provides excellent delineation of the stomach and duodenum from contiguous viscera. Distal small bowel visualization is less predictabel. Further clinical trials should confirm the utility of this solution, which contains a combination of iron salts and paramagnetic metallic ions. (orig.)

  14. In vitro antifungal susceptibility testing of Scopulariopsis brevicaulis strains using agar diffusion method.

    Science.gov (United States)

    Skóra, Magdalena; Macura, Anna B

    2011-01-01

    The genus Scopulariopsis is a common soil saprotroph and has been isolated from air, organic waste and also from plant, animal and human tissues. Scopulariopsis has mainly been associated in humans with superficial mycoses, but it has also been described as the cause of subcutaneous and invasive infections. The most common aetiological agent of infections in humans is Scopulariopsis brevicaulis. This species has been reported to be resistant in vitro to broad-spectrum antifungal agents available today. The aim of the study was to establish in vitro antifungal susceptibility of 35 S. brevicaulis strains against amphotericin B (AMB), flucytosine (FC), caspofungin (CAS), terbinafine (TER), ciclopirox (CIC), voriconazole (VOR), clotrimazole (CTR), miconazole (MCZ), econazole (ECO), ketoconazole (KET), itraconazole (ITR), and fluconazole (FLU). Antifungal susceptibility tests were evaluated by an agar diffusion method (Neo-Sensitabs, Rosco, Denmark). AMB, FC, CAS, ITR and FLU showed no antifungal activity against S. brevicaulis. TER, CIC, CTR, KET, VOR, ECO, and MCZ revealed inhibitory activity for S. brevicaulis, but it varied for each of the drugs. The best antifungal effect was observed for TER and CIC. All isolates had large inhibition zones for TER and CIC. CTR was also inhibitory for all tested S. brevicaulis isolates, but the diameters of inhibition zones were smaller than for TER and CIC. Nearly 89% isolates showed inhibition zones for KET and the mean diameter of the inhibition zone was comparable to CTR. The least antifungal activity exhibited VQR, ECO and MCZ. Because of the multiresistance of S. brevicaulis, infections due to this species may not respond to particular antifungal treatment and other therapeutic approaches should be considered, e.g., combined therapy and/or surgery.

  15. Correlation between Plant Secondary Metabolites and Their Antifungal Mechanisms–A Review

    DEFF Research Database (Denmark)

    Freiesleben, Sara; Jäger, Anna

    2014-01-01

    the biosynthetic group of terpenes and their antifungal mechanisms of action, all of them exhibiting their antifungal action through cell membrane disruption, although some of the terpenes also seemed to work through mitochondrial dysfunction. A clear correlation has not been demonstrated between the two other......The search for new antifungal drugs often involves secondary metabolites from plants because of their pharmacological activity against foreign pathogens. Among the modern drugs in use today about 40% are of natural origin. To distinguish the secondary metabolites they can be divided into groups...... based on their structure or biosynthetic origin. When searching for new antifungal agents it is crucial to search for a mechanism of action for which unwanted side effects can be avoided. This can be done if the mechanism of action only involves fungal cells and not mammalian cells. For that reason...

  16. Risk of Fungemia Due to Rhodotorula and Antifungal Susceptibility Testing of Rhodotorula Isolates

    OpenAIRE

    Zaas, Aimee K.; Boyce, Molly; Schell, Wiley; Lodge, Barbara Alexander; Miller, Jackie L.; Perfect, John R.

    2003-01-01

    Rhodotorula infections occur among patients with immunosuppression and/or central venous catheters. Using standardized methods (NCCLS M27-A), we determined the antifungal susceptibilities of 10 Rhodotorula bloodstream infection isolates. Patient information was collected for clinical correlation. The MICs of amphotericin B and posaconazole were the lowest, and the MICs of triazoles and echinocandins were higher than those of other antifungal agents.

  17. Computed tomography enterography: a comparison of different neutral oral contrast agents

    International Nuclear Information System (INIS)

    D'Ippolito, Giuseppe; Braga, Fernanda Angeli; Resende, Marcelo Cardoso; Bretas, Elisa Almeida Sathler; Nunes, Thiago Franchi; Rosas, George de Queiroz; Tiferes, Dario Arie

    2012-01-01

    Objective: The purpose of this study was to assess the performance of neutral oral contrast agents, comparing intestinal distension, distinction of intestinal wall, acceptance and side effects. Materials and Methods: Prospective, randomized, and double-blinded study involving 30 patients who underwent computed tomography of abdomen and pelvis with administration of neutral oral contrast agents, divided into three groups according the contrast agent type: milk, water, and polyethylene glycol. The images were consensually analyzed by two observers, considering the degree of bowel distension and intestinal wall distinction. The patients responded to a questionnaire regarding the taste of the ingested solution and on their side effects. Kruskal-Wallis and chi-square tests were employed for statistical analysis. Results: Among 40 studied intestinal segments, appropriate bowel distension (intestinal loop diameter > 2 cm) was observed in 14 segments (35%) in the milk group, 10 segments (25%) in the water group and 23 segments (57%) in the polyethylene glycol group (p = 0.01). Preparation with polyethylene glycol resulted in the best bowel distension, but it presented the worst taste and highest incidence of diarrhea as reported by patients. Conclusion: Bowel preparation with oral polyethylene glycol results in higher degree of bowel distension than with water or milk, but presents worst acceptance related to its taste and frequency of diarrhea as a side effect. (author)

  18. Computed tomography enterography: a comparison of different neutral oral contrast agents

    Energy Technology Data Exchange (ETDEWEB)

    D' Ippolito, Giuseppe, E-mail: giuseppe_dr@uol.com.br [Department of Imaging Diagnosis, Universidade Federal de Sao Paulo (UNIFESP), Sao Paulo, SP (Brazil); Braga, Fernanda Angeli; Resende, Marcelo Cardoso; Bretas, Elisa Almeida Sathler; Nunes, Thiago Franchi; Rosas, George de Queiroz; Tiferes, Dario Arie [Abdominal Imaging Section, Department of Imaging Diagnosis - Universidade Federal de Sao Paulo (Unifesp), Sao Paulo, SP (Brazil)

    2012-05-15

    Objective: The purpose of this study was to assess the performance of neutral oral contrast agents, comparing intestinal distension, distinction of intestinal wall, acceptance and side effects. Materials and Methods: Prospective, randomized, and double-blinded study involving 30 patients who underwent computed tomography of abdomen and pelvis with administration of neutral oral contrast agents, divided into three groups according the contrast agent type: milk, water, and polyethylene glycol. The images were consensually analyzed by two observers, considering the degree of bowel distension and intestinal wall distinction. The patients responded to a questionnaire regarding the taste of the ingested solution and on their side effects. Kruskal-Wallis and chi-square tests were employed for statistical analysis. Results: Among 40 studied intestinal segments, appropriate bowel distension (intestinal loop diameter > 2 cm) was observed in 14 segments (35%) in the milk group, 10 segments (25%) in the water group and 23 segments (57%) in the polyethylene glycol group (p = 0.01). Preparation with polyethylene glycol resulted in the best bowel distension, but it presented the worst taste and highest incidence of diarrhea as reported by patients. Conclusion: Bowel preparation with oral polyethylene glycol results in higher degree of bowel distension than with water or milk, but presents worst acceptance related to its taste and frequency of diarrhea as a side effect. (author)

  19. Risk of Fungemia Due to Rhodotorula and Antifungal Susceptibility Testing of Rhodotorula Isolates

    Science.gov (United States)

    Zaas, Aimee K.; Boyce, Molly; Schell, Wiley; Lodge, Barbara Alexander; Miller, Jackie L.; Perfect, John R.

    2003-01-01

    Rhodotorula infections occur among patients with immunosuppression and/or central venous catheters. Using standardized methods (NCCLS M27-A), we determined the antifungal susceptibilities of 10 Rhodotorula bloodstream infection isolates. Patient information was collected for clinical correlation. The MICs of amphotericin B and posaconazole were the lowest, and the MICs of triazoles and echinocandins were higher than those of other antifungal agents. PMID:14605170

  20. Antifungal activity of different extracts of Ageratum conyzoides for the ...

    African Journals Online (AJOL)

    Muhammad Arif Javed

    2012-06-19

    Jun 19, 2012 ... In case of aqueous extracts, the maximum reduction was observed in leaf extract (72%) ... antifungal and insecticidal agents (Hajlaoui et al., 2009). Extracts of many ..... growth reduction of mycelia of phytophthora on neem leaf.

  1. 2016 guideline strategies for the use of antifungal agents in patients with hematological malignancies or hematopoietic stem cell transplantation recipients in Taiwan.

    Science.gov (United States)

    Ko, Bor-Sheng; Chen, Wei-Ting; Kung, Hsiang-Chi; Wu, Un-In; Tang, Jih-Luh; Yao, Ming; Chen, Yee-Chun; Tien, Hwei-Fang; Chang, Shan-Chwen; Chuang, Yin-Ching; Lin, Dong-Tsamn

    2017-07-25

    The Infectious Diseases Society of Taiwan (IDST), the Hematology Society of Taiwan, the Taiwan Society of Blood and Marrow Transplantation, Medical Foundation in Memory of Dr. Deh-Lin Cheng, Foundation of Professor Wei-Chuan Hsieh for Infectious Diseases Research and Education, and CY Lee's Research Foundation for Pediatric Infectious Diseases and Vaccines cooperatively published this guideline for the use of antifungal agents in hematological patients with invasive fungal diseases (IFDs) in Taiwan. The guideline is the first one endorsed by IDST focusing on selection of antifungal strategies, including prophylaxis, empirical (or symptom-driven) and pre-emptive (or diagnostic-driven) strategy. We suggest a risk-adapted dynamic strategy and provide an algorithm to facilitate decision making in population level as well as for individual patient. Risk assessment and management accordingly is explicitly emphasized. In addition, we highlight the importance of diagnosis in each antifungal strategy among five elements of the antimicrobial stewardship (diagnosis, drug, dose, de-escalation and duration). The rationale, purpose, and key recommendations for the choice of antifungal strategy are summarized, with concise review of international guidelines or recommendation, key original articles and local epidemiology reports. We point out the interaction and influence between elements of recommendations and limitation of and gap between evidences and daily practice. The guideline balances the quality of evidence and feasibility of recommendation in clinical practice. Finally, this version introduces the concept of health economics and provides data translated from local disease burdens. All these contents hopefully facilitate transparency and accountability in medical decision-making, improvements in clinical care and health outcomes, and appropriateness of medical resource allocation. Copyright © 2017. Published by Elsevier B.V.

  2. 2016 guideline strategies for the use of antifungal agents in patients with hematological malignancies or hematopoietic stem cell transplantation recipients in Taiwan

    Directory of Open Access Journals (Sweden)

    Bor-Sheng Ko

    2018-06-01

    Full Text Available The Infectious Diseases Society of Taiwan (IDST, the Hematology Society of Taiwan, the Taiwan Society of Blood and Marrow Transplantation, Medical Foundation in Memory of Dr. Deh-Lin Cheng, Foundation of Professor Wei-Chuan Hsieh for Infectious Diseases Research and Education, and CY Lee's Research Foundation for Pediatric Infectious Diseases and Vaccines cooperatively published this guideline for the use of antifungal agents in hematological patients with invasive fungal diseases (IFDs in Taiwan. The guideline is the first one endorsed by IDST focusing on selection of antifungal strategies, including prophylaxis, empirical (or symptom-driven and pre-emptive (or diagnostic-driven strategy. We suggest a risk-adapted dynamic strategy and provide an algorithm to facilitate decision making in population level as well as for individual patient. Risk assessment and management accordingly is explicitly emphasized. In addition, we highlight the importance of diagnosis in each antifungal strategy among five elements of the antimicrobial stewardship (diagnosis, drug, dose, de-escalation and duration. The rationale, purpose, and key recommendations for the choice of antifungal strategy are summarized, with concise review of international guidelines or recommendation, key original articles and local epidemiology reports. We point out the interaction and influence between elements of recommendations and limitation of and gap between evidences and daily practice. The guideline balances the quality of evidence and feasibility of recommendation in clinical practice. Finally, this version introduces the concept of health economics and provides data translated from local disease burdens. All these contents hopefully facilitate transparency and accountability in medical decision-making, improvements in clinical care and health outcomes, and appropriateness of medical resource allocation.

  3. Enzymatic Activity and Susceptibility to Antifungal Agents of Brazilian Environmental Isolates of Hortaea werneckii.

    Science.gov (United States)

    Formoso, Andrea; Heidrich, Daiane; Felix, Ciro Ramón; Tenório, Anne Carolyne; Leite, Belize R; Pagani, Danielle M; Ortiz-Monsalve, Santiago; Ramírez-Castrillón, Mauricio; Landell, Melissa Fontes; Scroferneker, Maria L; Valente, Patricia

    2015-12-01

    Four strains of Hortaea werneckii were isolated from different substrates in Brazil (a salt marsh macrophyte, a bromeliad and a marine zoanthid) and had their identification confirmed by sequencing of the 26S rDNA D1/D2 domain or ITS region. Most of the strains were able to express amylase, lipase, esterase, pectinase and/or cellulase, enzymes that recognize components of plant cells as substrates, but did not express albuminase, keratinase, phospholipase and DNAse, whose substrates are animal-related. Urease production was positive for all isolates, while caseinase, gelatinase and laccase production were variable among the strains. All the strains grew in media containing up to 30% NaCl. We propose that the primary substrate associated with H. werneckii is plant-related, in special in saline environments, where the fungus may live as a saprophyte and decomposer. Infection of animal-associated substrates would be secondary, with the fungus acting as an opportunistic animal pathogen. All strains were resistant to fluconazole and presented high MIC for amphotericin B, while they were susceptible to all the other antifungal agents tested.

  4. Analysis, fate studies and monitoring of the antifungal agent clotrimazole in the aquatic environment.

    Science.gov (United States)

    Peschka, Manuela; Roberts, Paul H; Knepper, Thomas P

    2007-10-01

    The analysis and presence of clotrimazole, an antifungal agent with logK(OW) > 4, was thoroughly studied in the aquatic environment. For that reason analytical methods based on gas chromatography-mass spectrometry and liquid chromatography-tandem mass spectrometry were developed and validated to quantify clotrimazole with limits of quantification down to 5 and 1 ng/L, respectively. Both methods were compared in an intercalibration exercise. The complete mass-spectrometric fragmentation pattern could be elucidated with the aid of quadrupole time of flight mass spectrometry. Since clotrimazole tends to adsorb to laboratory glassware, studies on its adsorption behaviour were made to ensure the appropriate handling of water samples, e.g. pH, storage time, pretreatment of sampling vessels or material of the vials used for final extracts. The phenomena of adsorption to suspended matter were investigated while analysing different waste-water samples. Application of the methods in various investigated wastewater and surface water samples demonstrated that clotrimazole could only be detected in the low nanogram per litre range of anthropogenic influenced unfiltered water samples after acidification to pH 2.

  5. Cost-effectiveness of oral antiplatelet agents--current and future perspectives.

    Science.gov (United States)

    Arnold, Suzanne V; Cohen, David J; Magnuson, Elizabeth A

    2011-08-09

    Cardiovascular disease is both highly prevalent and exceedingly costly to treat. Several novel antiplatelet agents have been found to be effective in reducing the morbidity and mortality associated with cardiovascular disease. Understanding both the economic and the clinical implications of these novel therapies is particularly important. In this article, the results of published evaluations of the cost-effectiveness of oral antiplatelet strategies for use across a range of clinical conditions and treatment settings are reviewed. The results of these studies support the use of aspirin for primary prevention in high-risk patients and for secondary prevention in all patients with previous cardiovascular events. Although the optimal duration of dual antiplatelet therapy after an event remains uncertain, favorable cost-effectiveness estimates have been demonstrated for aspirin plus clopidogrel versus aspirin alone after a myocardial infarction or percutaneous coronary intervention. Moreover, prasugrel has been shown to be more cost-effective than clopidogrel for patients with an acute coronary syndrome and planned percutaneous coronary intervention. As novel antiplatelet agents emerge and existing agents are tested in different patient populations, the evaluation of the relative economic efficiency of these oral antiplatelet treatment strategies will continue to be instrumental to optimally inform clinical and health-policy decision-making.

  6. Genetic determinants of antifungal resistance in Candida species ...

    African Journals Online (AJOL)

    In the previous decades, it has been an increase in cases of resistance to antifungal agents used in the prophylaxis and treatment of infections caused by Candida species. The emergence of resistance to drug classes, it is usually explained by genome alterations ranging from point mutations to gain or loss of whole ...

  7. Evaluation of semisolid agar method for antifungal susceptibility test of T. rubrum

    Directory of Open Access Journals (Sweden)

    Sultana Razia

    2016-08-01

    Full Text Available Background: With increasing fungal disease many newer antifungal drugs are available with different spectrum of activ­ity. Antifungal susceptibility test will help clinicians for selection of effective drug and thereby treatment of patient. Objective: The study was undertaken to perform a simple screening drug susceptibility test of T. rnbrum by Semi Solid Agar Antifungal Susceptibility (SAAS Method: Perfonnance of susceptibility method was assessed by comparing the MICs of three commonly prescribed antifungal agents namely- tluconazole (FCZ, itraconazole (ITZ and terbinafine (TER to the CLSI (Clinical and Laboratory Standard Institute recommended M-38, a broth microdilution method. Results: In SAAS method, among twenty nine T. rubrum, twenty five (86.2% were susceptible (MIC range 0.5-64 µg/ml to Fluconazole (FCZ and four (13.7% were resistant (MIC value >64 µg/ml. In broth microdilution method, among twenty nine T. rubrum, twenty six (89.6% were susceptible (MIC range 0.3-64 µg/ml to FCZ and three (10.3% were resistant (MIC value >64 µg/ml. In case of both ITZ and TER, all were susceptible (MIC range 0.3-64 µg/ml to both methods. The SAAS method demonstrated the susceptibility pattern of T. rubrum against FCZ, ITZ and TER usually within 72 to 96 hours after organism isolation and results were concordance with the results of CLSI broth microdilution method. Conclusion: Though it is a newer method with proper standardization of the test method, SAAS method is simple and easily applicable screening method for susceptibility testing of antifungal agents against dermatophytes in any microbiology laboratories.

  8. Local, systemic, demographic, and health-related factors influencing pathogenic yeast spectrum and antifungal drug administration frequency in oral candidiasis: a retrospective study.

    Science.gov (United States)

    Hertel, Moritz; Schmidt-Westhausen, Andrea Maria; Strietzel, Frank-Peter

    2016-09-01

    In order to identify oral candidiasis patients being at risk of carrying potentially drug-resistant Candida, the aim of the study was to detect local, systemic, demographic, and health-related factors influencing (I) yeast spectrum composition and (II) antifungal administration frequency. Additionally, the aim was to investigate (III) species shift occurrence. Data from 798 patients (496 females, 302 males; mean age 59.7) with oral candidiasis diagnosed based on positive clinical and microbial findings (species identification and CFU count) between 2006 and 2011 were retrospectively analyzed using Pearson's chi(2) test and regression analysis. Among 958 isolates, Candida albicans was the most frequently detected (76.8 %). Also, species intrinsically resistant to azoles were frequently isolated (15.8 and 17.7 % of isolates and patients). (I) Infections only caused by C. albicans were significantly associated with the use of inhalation steroids (p = 0.001) and antibiotics (p = 0.04), super-infection of lichen planus (p = 0.002), and the absence of removable dentures (p oral candidiasis remains C. albicans. Nevertheless, therapeutic problems may be caused by the frequent presence of species intrinsically resistant to azoles, especially in patients wearing dentures.

  9. Antifungal activities of selected Venda medicinal plants against ...

    African Journals Online (AJOL)

    USER

    2010-05-17

    May 17, 2010 ... extracts from 30 plants used by Venda traditional healers for the ... cost of antifungal agents (Debruyne, 1997; Traeder et al., ... the use of medicinal plants is very common based on ... used to determine the activity of the plant extracts against the .... diffusion method: Table 3) as well as the two Candida.

  10. Steroid acne vs. Pityrosporum folliculitis: the incidence of Pityrosporum ovale and the effect of antifungal drugs in steroid acne.

    Science.gov (United States)

    Yu, H J; Lee, S K; Son, S J; Kim, Y S; Yang, H Y; Kim, J H

    1998-10-01

    Steroid acne is a folliculitis that can result from systemic or topical administration of steroid, and has been described as showing a similar clinical picture to Pityrosporum folliculitis, but there have been few reports about the incidence of Pityrosporum ovale and the effect of antimycotic drugs in steroid acne and other acneiform eruptions. Our purpose was to describe the association between steroid acne and P. ovale, and to confirm the superior efficacy of oral antifungal drugs over anti-acne drugs in the treatment of steroid acne. The history, clinical features direct microscopy, histopathologic analysis, and therapeutic results of 125 cases with steroid acne or other acneiform eruptions were described and compared. Over 80% of patients with acneiform eruption receiving systemic steroid revealed significant numbers of P. ovale in the lesional follicle. Furthermore, oral antifungal drug (itraconazole) showed significantly better clinical and mycologic effects than any other group of medications used in this study. Steroid acne and other acneiform eruptions showing discrete follicular papules and/or pustules localized to the upper trunk and acneiform facial skin lesions associated with multiple acneiform lesions on the body in the summer period should be suspected as Pityrosporum folliculitis. In addition, oral antifungal drugs recommended for Pityrosporum folliculitis; however, it will require a larger case-control study to confirm the superiority of antifungal therapy over anti-acne treatment.

  11. Inner conflict in patients receiving oral anticancer agents: a qualitative study.

    Science.gov (United States)

    Yagasaki, Kaori; Komatsu, Hiroko; Takahashi, Tsunehiro

    2015-04-14

    To explore the experiences of patients receiving oral anticancer agents. A qualitative study using semistructured interviews with a grounded theory approach. A university hospital in Japan. 14 patients with gastric cancer who managed their cancer with oral anticancer agents. Patients with cancer experienced inner conflict between rational belief and emotional resistance to taking medication due to confrontation with cancer, doubt regarding efficacy and concerns over potential harm attached to use of the agent. Although they perceived themselves as being adherent to medication, they reported partial non-adherent behaviours. The patients reassessed their lives through the experience of inner conflict and, ultimately, they recognised their role in medication therapy. Patients with cancer experienced inner conflict, in which considerable emotional resistance to taking their medication affected their occasional non-adherent behaviours. In patient-centred care, it is imperative that healthcare providers understand patients' inner conflict and inconsistency between their subjective view and behaviour to support patient adherence. Published by the BMJ Publishing Group Limited. For permission to use (where not already granted under a licence) please go to http://group.bmj.com/group/rights-licensing/permissions.

  12. Antifungal susceptibilities of Candida, Cryptococcus neoformans and Aspergillus fumigatus from the Asia and Western Pacific region: data from the SENTRY antifungal surveillance program (2010-2012).

    Science.gov (United States)

    Pfaller, Michael A; Messer, Shawn A; Jones, Ronald N; Castanheira, Mariana

    2015-09-01

    The SENTRY Antifungal Surveillance Program monitors global susceptibility rates of newer and established antifungal agents. We report the in vitro activity of seven antifungal agents against 496 contemporary clinical isolates of yeasts and molds. The isolates were obtained from 20 laboratories in the Asia-Western Pacific (APAC) region during 2010 through 2012. Anidulafungin, caspofungin, micafungin, fluconazole, itraconazole, posaconazole and voriconazole were susceptibility tested using CLSI methods and species-specific interpretive criteria. Sequencing of fks hot spots was performed for echinocandin-resistant strains. Isolates included 13 species of Candida (n=460), 5 species of non-Candida yeasts (21), 5 species of Aspergillus (11) and 4 other molds. Echinocandin resistance was uncommon among eight species of Candida and was only detected in three isolates of Candida glabrata, two from Australia harboring mutations in fks1 (F625S) and fks2 (S663P). Resistance to the azoles was much more common and was observed among all species with the exception of Candida dubliniensis. Fluconazole resistance rates observed with C. glabrata (6.8%) was comparable to that seen with Candida parapsilosis (5.7%) and Candida tropicalis (3.6%). Cross resistance among the triazoles was seen with each of these three species. The mold-active azoles and the echinocandins were all active against isolates of Aspergillus fumigatus. Azole resistance was not detected among the isolates of Cryptococcus neoformans. Antifungal resistance is uncommon among isolates of fungi causing invasive fungal infections in the APAC region. As in other regions of the world, emerging resistance to the echinocandins among invasive isolates of C. glabrata bears close monitoring.

  13. Inventory of oral anticancer agents : Pharmaceutical formulation aspects with focus on the solid dispersion technique

    NARCIS (Netherlands)

    Sawicki, E.; Schellens, J. H M; Beijnen, J. H.; Nuijen, B.

    2016-01-01

    Dissolution from the pharmaceutical formulation is a prerequisite for complete and consistent absorption of any orally administered drug, including anticancer agents (oncolytics). Poor dissolution of an oncolytic can result in low oral bioavailability, high variability in blood concentrations and

  14. Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.

    Science.gov (United States)

    Zhao, Shizhen; Zhang, Xiangqian; Wei, Peng; Su, Xin; Zhao, Liyu; Wu, Mengya; Hao, Chenzhou; Liu, Chunchi; Zhao, Dongmei; Cheng, Maosheng

    2017-09-08

    To further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compounds (1), a series of aromatic heterocyclic derivatives were designed, synthesized and evaluated for in vitro antifungal activity. Many of the target compounds showed good inhibitory activity against Candida albicans and Cryptococcus neoformans. In particular, the isoxazole nuclei were more suited for improving the activity against Aspergillus spp. Among these compounds, 2-F substituted analogues 23g and 23h displayed the most remarkable in vitro activity against Candida spp., C. neoformans, A. fumigatus and fluconazole-resistant C.alb. strains, which is superior or comparable to the activity of the reference drugs fluconazole and voriconazole. Notably, the compounds 23g and 23h exhibited low inhibition profiles for various isoforms of human cytochrome P450 and excellent blood plasma stability. Copyright © 2017 Elsevier Masson SAS. All rights reserved.

  15. Evaluation of antifungal efficacy of QMix 2in1 as a final irrigant: An in ...

    African Journals Online (AJOL)

    Evaluation of antifungal efficacy of QMix 2in1 as a final irrigant: An in vitro study. E Kalyoncuoglu, E Sen Tunc, S Ozer, C Keskin, K Bilgin, A Birinci. Abstract. Background: It is known that no specific antifungal agent exists at present for irrigation of infected root canals. QMix 2in1 was investigated to determine whether they ...

  16. Randomized control trial of benzydamine HCl versus sodium bicarbonate for prophylaxis of concurrent chemoradiation-induced oral mucositis.

    Science.gov (United States)

    Chitapanarux, Imjai; Tungkasamit, Tharatorn; Petsuksiri, Janjira; Kannarunimit, Danita; Katanyoo, Kanyarat; Chakkabat, Chakkapong; Setakornnukul, Jiraporn; Wongsrita, Somying; Jirawatwarakul, Naruemon; Lertbusayanukul, Chawalit; Sripan, Patumrat; Traisathit, Patrinee

    2018-03-01

    The purpose of the study is to compare the efficacy of benzydamine HCl with sodium bicarbonate in the prevention of concurrent chemoradiation-induced oral mucositis in head and neck cancer patients. Sixty locally advanced head and neck cancer patients treated with high-dose radiotherapy concurrently with platinum-based chemotherapy were randomly assigned to receive either benzydamine HCl or sodium bicarbonate from the first day of treatment to 2 weeks after the completion of treatment. The total score for mucositis, based on the Oral Mucositis Assessment Scale (OMAS), was used for the assessment, conducted weekly during the treatment period and at the fourth week of the follow-up. Pain score, all prescribed medications, and tube feeding needs were also recorded and compared. The median of total OMAS score was statistically significant lower in patients who received benzydamine HCl during concurrent chemo-radiotherapy (CCRT) than in those who received sodium bicarbonate, (p value < 0.001). There was no difference in median pain score, (p value = 0.52). Nineteen percent of patients in sodium bicarbonate arm needed oral antifungal agents whereas none in the benzydamine HCl arm required such medications, (p value = 0.06). Tube feeding needs and the compliance of CCRT were not different between the two study arms. For patients undergoing high-dose radiotherapy concurrently with platinum-based chemotherapy, using benzydamine HCl mouthwash as a preventive approach was superior to basic oral care using sodium bicarbonate mouthwash in terms of reducing the severity of oral mucositis and encouraging trend for the less need of oral antifungal drugs.

  17. Antifungal activity of gold nanoparticles prepared by solvothermal method

    Energy Technology Data Exchange (ETDEWEB)

    Ahmad, Tokeer, E-mail: tahmad3@jmi.ac.in [Nanochemistry Laboratory, Department of Chemistry, Jamia Millia Islamia, New Delhi 110025 (India); Wani, Irshad A.; Lone, Irfan H.; Ganguly, Aparna [Nanochemistry Laboratory, Department of Chemistry, Jamia Millia Islamia, New Delhi 110025 (India); Manzoor, Nikhat; Ahmad, Aijaz [Department of Biosciences, Jamia Millia Islamia, New Delhi 110025 (India); Ahmed, Jahangeer [Department of Chemistry, Michigan State University, East Lansing, MI 48824 (United States); Al-Shihri, Ayed S. [Department of Chemistry, Faculty of Science, King Khalid University, Abha 61413, P.O. Box 9004 (Saudi Arabia)

    2013-01-15

    Graphical abstract: Gold nanoparticles (7 and 15 nm) of very high surface area (329 and 269 m{sup 2}/g) have been successfully synthesized through solvothermal method by using tin chloride and sodium borohydride as reducing agents. As-prepared gold nanoparticles shows very excellent antifungal activity against Candida isolates and activity increases with decrease in the particle size. Display Omitted Highlights: ► Effect of reducing agents on the morphology of gold nanoparticles. ► Highly uniform and monodisperse gold nanoparticles (7 nm). ► Highest surface area of gold nanoparticles (329 m{sup 2/}g). ► Excellent antifungal activity of gold nanoparticles against Candida strains. -- Abstract: Gold nanoparticles have been successfully synthesized by solvothermal method using SnCl{sub 2} and NaBH{sub 4} as reducing agents. X-ray diffraction studies show highly crystalline and monophasic nature of the gold nanoparticles with face centred cubic structure. The transmission electron microscopic studies show the formation of nearly spherical gold nanoparticles of average size of 15 nm using SnCl{sub 2}, however, NaBH{sub 4} produced highly uniform, monodispersed and spherical gold nanoparticles of average grain size of 7 nm. A high surface area of 329 m{sup 2}/g for 7 nm and 269 m{sup 2}/g for 15 nm gold nanoparticles was observed. UV–vis studies assert the excitations over the visible region due to transverse and longitudinal surface plasmon modes. The gold nanoparticles exhibit excellent size dependant antifungal activity and greater biocidal action against Candida isolates for 7 nm sized gold nanoparticles restricting the transmembrane H{sup +} efflux of the Candida species than 15 nm sized gold nanoparticles.

  18. Antifungal activity of gold nanoparticles prepared by solvothermal method

    International Nuclear Information System (INIS)

    Ahmad, Tokeer; Wani, Irshad A.; Lone, Irfan H.; Ganguly, Aparna; Manzoor, Nikhat; Ahmad, Aijaz; Ahmed, Jahangeer; Al-Shihri, Ayed S.

    2013-01-01

    Graphical abstract: Gold nanoparticles (7 and 15 nm) of very high surface area (329 and 269 m 2 /g) have been successfully synthesized through solvothermal method by using tin chloride and sodium borohydride as reducing agents. As-prepared gold nanoparticles shows very excellent antifungal activity against Candida isolates and activity increases with decrease in the particle size. Display Omitted Highlights: ► Effect of reducing agents on the morphology of gold nanoparticles. ► Highly uniform and monodisperse gold nanoparticles (7 nm). ► Highest surface area of gold nanoparticles (329 m 2/ g). ► Excellent antifungal activity of gold nanoparticles against Candida strains. -- Abstract: Gold nanoparticles have been successfully synthesized by solvothermal method using SnCl 2 and NaBH 4 as reducing agents. X-ray diffraction studies show highly crystalline and monophasic nature of the gold nanoparticles with face centred cubic structure. The transmission electron microscopic studies show the formation of nearly spherical gold nanoparticles of average size of 15 nm using SnCl 2 , however, NaBH 4 produced highly uniform, monodispersed and spherical gold nanoparticles of average grain size of 7 nm. A high surface area of 329 m 2 /g for 7 nm and 269 m 2 /g for 15 nm gold nanoparticles was observed. UV–vis studies assert the excitations over the visible region due to transverse and longitudinal surface plasmon modes. The gold nanoparticles exhibit excellent size dependant antifungal activity and greater biocidal action against Candida isolates for 7 nm sized gold nanoparticles restricting the transmembrane H + efflux of the Candida species than 15 nm sized gold nanoparticles.

  19. Universal, class-specific and drug-specific reversal agents for the new oral anticoagulants.

    Science.gov (United States)

    Ansell, Jack E

    2016-02-01

    Although there is controversy about the absolute need for a reversal agent for the new direct oral anticoagulants (DOACs), the absence of such an agent is a barrier to more widespread use of these agents. For the management of major life-threatening bleeding with the DOACs, most authorities recommend the use of four factor prothrombin complex concentrates, although the evidence to support their use in terms of improving outcomes is meager. At the present time, there are three antidotes in development and poised to enter the market. Idarucizumab is a drug-specific antidote targeted to reverse the direct thrombin inhibitor, dabigatran. Andexanet alfa is a class-specific antidote targeted to reverse the oral direct factor Xa inhibitors as well as the indirect inhibitor, enoxaparin. Ciraparantag is a universal antidote targeted to reverse the direct thrombin and factor Xa inhibitors as well as the indirect inhibitor, enoxaparin.

  20. Relationship between intracranial pressure and antifungal agents levels in the CSF of patients with cryptococcal meningitis.

    Science.gov (United States)

    Wirth, Fernanda; de Azevedo, Maria Isabel; Pilla, Carmen; Aquino, Valério Rodrigues; Neto, Gustavo Wissmann; Goldani, Luciano Zubaran

    2018-04-01

    The purpose of this study was to evaluate the influence of intracranial hypertension in the cerebrospinal fluid (CSF) levels of amphotericin B and fluconazole levels of patients with cryptococcal meningitis. CSF samples and intracranial pressure were obtained by means of routine punctures performed at days 1, 7, and 14 of therapy, respectively. Amphotericin B and fluconazole CSF levels were measured by HPLC method as previously described. The minimum inhibitory concentration for amphotericin B, fluconazole, 5΄flucytosine, and voriconazole of each Cryptococcus isolate was performed according to CLSI. The predominant Cryptococcus species found was C. neoformans, and the major underlying condition was AIDS. Only one CSF sample had a detectable level for amphotericin B during the 14 days of therapy. Fluconazole CSF levels progressively increased from day 1 to day 14 of therapy for most cases. Fluconazole levels in the CSF were above the minimum inhibitory concentrations (MICs) for Cryptococcus during the initial 14 days of antifungal therapy. Variations of intracranial pressure did not affect amphotericin B and fluconazole levels in the CSF. The generalized estimating correlation (GEE) and Spearman correlation test (SCT) showed no significant correlation between the amphotericin B or fluconazole concentrations in the CSF and intracranial pressure (P = .953 and P = .093, respectively for GEE test and P = .477 and P = .847, respectively, for SCT). Combination therapy of amphotericin B with fluconazole was effective in 60% of the patients considering CSF cultures were negative in 9 of 15 patients after 14 days of therapy. Further studies are necessary to evaluate the role of intracranial hypertension on the therapeutic efficacy of different antifungal agents in patients with cryptococcal meningitis.

  1. Oral Hypoglycemic Agents Added to Insulin Monotherapy for Type 2 Diabetes

    NARCIS (Netherlands)

    Vos, Rimke C.; Rutten, Guy E.H.M.

    2017-01-01

    Clinical Question: Among patients with type 2 diabetes mellitus who do not achieve optimal glycemic control with insulin monotherapy, is the addition of oral hypoglycemic agents associated with benefits (measured by lowering of hemoglobin A1c) or adverse effects? Bottom Line: Adding a sulfonylurea

  2. Antifungal activity of multifunctional Fe{sub 3}O{sub 4}-Ag nanocolloids

    Energy Technology Data Exchange (ETDEWEB)

    Chudasama, Bhupendra, E-mail: bnchudasama@thapar.ed [School of Physics and Materials Science, Thapar University, Patiala 147004 (India); Vala, Anjana K.; Andhariya, Nidhi [Department of Physics, Bhavnagar University, Bhavnagar 364022 (India); Upadhyay, R.V. [P.D. Patel Institute of Applied Sciences, Charotar University of Science and Technology, Changa 388421 (India); Mehta, R.V. [Department of Physics, Bhavnagar University, Bhavnagar 364022 (India)

    2011-05-15

    In recent years, rapid increase has been observed in the population of microbes that are resistant to conventionally used antibiotics. Antifungal drug therapy is no exception and now resistance to many of the antifungal agents in use has emerged. Therefore, there is an inevitable and urgent medical need for antibiotics with novel antimicrobial mechanisms. Aspergillus glaucus is the potential cause of fatal brain infections and hypersensitivity pneumonitis in immunocompromised patients and leads to death despite aggressive multidrug antifungal therapy. In the present article, we describe the antifungal activity of multifunctional core-shell Fe{sub 3}O{sub 4}-Ag nanocolloids against A. glaucus isolates. Controlled experiments are also carried out with Ag nanocolloids in order to understand the role of core (Fe{sub 3}O{sub 4}) in the antifungal action. The minimum inhibitory concentration (MIC) of nanocolloids is determined by the micro-dilution method. MIC of A. glaucus is 2000 {mu}g/mL. The result is quite promising and requires further investigations in order to develop a treatment methodology against this death causing fungus in immunocompromised patients. - Research Highlights: Synthesis of Fe{sub 3}O{sub 4}-Ag core-shell nanocolloids. Antifungal activity of Fe{sub 3}O{sub 4}-Ag nanocolloids against Aspergillus glaucus isolates. The MIC value for A. glaucus is 2000 {mu}g/mL. Antifungal activity is better or comparable with most prominent antibiotics.

  3. Antifungal Efficacy of Myrtus communis Linn

    Directory of Open Access Journals (Sweden)

    Sadeghi Nejad

    2014-08-01

    Full Text Available Background The ethanolic extract of Myrtus communis Linn. leaves was assayed in vitro as a growth inhibitor against opportunistic fungi such as Candida and Aspergillus species. Myrtus communis Linn. (Family, Myrtaceae is an aromatic evergreen shrub or small tree. It is native to the Mediterranean region. Objectives This study aimed to assess antifungal activity (in vitro of the ethanolic extracts of Myrtus communis leaves as a growth inhibitor against 24 clinical isolates of Candida, including C. albicans, C. glabrata, and C. tropicalis also three species of Aspergillus, including A. niger, A. flavus, and A. terreus. Materials and Methods The ethanolic extract of myrtle leaves was prepared by maceration method and minimal inhibitory concentration (MIC of Myrtus communis leaves extract was determined by agar-well diffusion technique. Amphotericin B and clotrimazole were used as the positive control in this assay. Results The minimal inhibitory concentration (MICs values of Myrtus communis leaves extract ranged 0.625-5.0 µg/µL and 5-40 µg/µL against tested Candida spp. and Aspergillus spp., respectively. Conclusions Results revealed that the ethanolic extract of Myrtus communis leaves have antifungal potency against both pathogenic tested fungi, and it can be used as a natural antifungal agent.

  4. [Susceptibility of yeasts to antifungal agents in Kaunas University of Medicine Hospital].

    Science.gov (United States)

    Skrodeniene, Erika; Dambrauskiene, Asta; Vitkauskiene, Astra

    2006-01-01

    The aim of this study was to determine the species of yeast and their susceptibility to antifungal agents isolated from clinical specimens of patients treated in Kaunas University of Medicine Hospital. A total of 142 yeasts isolated from various clinical specimens of patients hospitalized in Kaunas University of Medicine Hospital were included in this study. All yeasts were cultivated on Sabouraud dextrose agar and identified using either CHROM agar or API 20C AUX system. The minimum inhibitory concentrations of fluconazole, itraconazole, and amphotericin B were determined by the ATB FUNGUS 2 agar microdilution test. In all clinical specimens except blood, Candida albicans was the most frequently isolated yeast (65.5%, pyeast strains showed resistance to fluconazole. Nearly one-fourth of Candida albicans strains (24.7%) and 23.2% of all isolated yeast strains showed resistance to itraconazole. Almost all of fluconazole-resistant (93.3%) and 12.6% of fluconazole-susceptible yeast were found to be resistant to itraconazole (pyeast strains were susceptible to amphotericin B. Candida albicans strains were significantly frequently resistant to fluconazole than non-albicans Candida species (15.1% and 4.1%, respectively, pyeast isolated in Kaunas University of Medicine Hospital. There was determined that yeasts resistant to fluconazole were commonly resistant to itraconazole too. All isolated yeast strains were susceptible to amphotericin B.

  5. Antifungal susceptibility profiles of 1698 yeast reference strains revealing potential emerging human pathogens.

    Directory of Open Access Journals (Sweden)

    Marie Desnos-Ollivier

    Full Text Available New molecular identification techniques and the increased number of patients with various immune defects or underlying conditions lead to the emergence and/or the description of novel species of human and animal fungal opportunistic pathogens. Antifungal susceptibility provides important information for ecological, epidemiological and therapeutic issues. The aim of this study was to assess the potential risk of the various species based on their antifungal drug resistance, keeping in mind the methodological limitations. Antifungal susceptibility profiles to the five classes of antifungal drugs (polyens, azoles, echinocandins, allylamines and antimetabolites were determined for 1698 yeast reference strains belonging to 992 species (634 Ascomycetes and 358 Basidiomycetes. Interestingly, geometric mean minimum inhibitory concentrations (MICs of all antifungal drugs tested were significantly higher for Basidiomycetes compared to Ascomycetes (p<0.001. Twenty four strains belonging to 23 species of which 19 were Basidiomycetes seem to be intrinsically "resistant" to all drugs. Comparison of the antifungal susceptibility profiles of the 4240 clinical isolates and the 315 reference strains belonging to 53 shared species showed similar results. Even in the absence of demonstrated in vitro/in vivo correlation, knowing the in vitro susceptibility to systemic antifungal agents and the putative intrinsic resistance of yeast species present in the environment is important because they could become opportunistic pathogens.

  6. Treatment modalities of oral mucositis after radiation of head and neck cancers

    International Nuclear Information System (INIS)

    Lapeyre, M.; Charra-Brunaud, C.; Kaminsky, M.C.; Geoffrois, L.; Dolivet, G.; Pourel, N.; Marchal, C.; Bey, P.; Maire, F.; Simon, M.; Toussaint, B.

    2001-01-01

    Acute mucositis is common after radiotherapy for head and neck cancers. During the past 3 decades, there was a gradual evolution in the treatment modalities for locally advanced carcinomas (concomitant radio-chemotherapy, accelerated radiotherapy). These new strategies are accompanied by an increase in early mucosal reactions. At the present time, there is no widely accepted prophylaxis or effective treatment. Many traditional remedies or new agents seem ineffective (Sucralfate, Chlorhexidine, GM-CSF, Silver nitrate, Prostaglandin, anti-oxidants, Benzydamine hydrochloride), while others seem promising (Povidone-iodine, nonabsorbable antibiotic lozenges and anti-fungal, local GM-CSF, Glutamide, Low-energy laser, corticosteroids). Radioprotectors are controversial and should be only used in experimental protocols and not in routine practice. However, some recommendations can be proposed: general prevention and global care before cancer therapy should be systematic (oral hygiene, dental and periodontal treatment, advice to avoid the use of tobacco and alcohol); frequent oral rinsing with a bland mouthwash (Povidone-iodine or others) should be used at the start of treatment because there are significant modifications of the oral microflora increased by a disturbed salivary flow; these mouthwashes could be associated with nonabsorbable antibiotic lozenges or anti-fungal topical (bicarbonates, Amphotericine B); Systematic percutaneous fluoroscopic gastrostomy should be decided before any aggressive treatments (concomitant radio-chemotherapy, accelerated radiotherapy); pain should be controlled; finally, the radiation technique should be optimized (mucosal sparing block, conformal radiotherapy and intensity modulated radiation therapy). (authors)

  7. Management of Antithrombotic Agents in Oral Surgery Maria Martinez and Dimitrios A. Tsakiris *

    Directory of Open Access Journals (Sweden)

    Maria Martinez

    2015-10-01

    Full Text Available Systemic anticoagulation with intravenous or oral anticoagulants and antiplatelet agents is an efficient treatment against thromboembolic or cardiovascular disease. Invasive dental procedures or oral surgery might be associated with bleeding complications if carried out under anticoagulants. Patients on vitamin K antagonists, new direct anticoagulants or antiplatelet agents having dental interventions with low-risk for bleeding do not need interruption of anticoagulation. In case of bleeding complications local hemostatic measures, such as local surgical sutures, fibrin glue, local antifibrinolytic treatment with tranexamic acid, or e-aminocaproic acid suffice to stop bleeding. In patients with high risk of bleeding an individual assessment of the benefit/risk ratio of interrupting anticoagulation should be carried out. Bridging the long-term anticoagulation with short-term anticoagulants should be planned according to national or international guidelines. The introduction of the newer direct oral anticoagulants having more flexible pharmacokinetic properties has facilitated bridging, allowing short-term interruption without increasing the risk of relapsing thrombotic or cardiovascular events.

  8. Effects of oral contraceptive agents and sex steroids on carbohydrate metabolism.

    Science.gov (United States)

    Kalkhoff, R K

    1972-01-01

    The article offers a general interpretation of the influence of oral contraceptive agents on glucose tolerance, emphasizing comparisons of synthetic sex hormones. Although there are conflicting reports on steroid-induced diabetes in normal women, their glucose curves are often higher when under oral contraceptive treatment, suggesting that oral contraceptives may induce a form of subclinical diabetes melitus that is reversible. Evidence from diabetic women suggests definite deliterious effects from contraceptive administration. Estradiol, estriol, and estrone may improve glucose tolerance in nondiabetic women and reduce insulin requirements in diabetics. Progesterone has little effect on carbohydrate tolerance, as did synthetic progestin. Conjugated equine estrogens (equilenine or Premarin) may provoke mild to moderate deterioration of carbohydrate tolerance. Parenterally administered natural estrogens and orally administered synthetic derivatives appear to differ sharply in their effects. Sex hormones' effects on carbohydrate metabolism likely involve interactions with insulin and endogenous glucocorticoids.

  9. Synergistic combinations of antifungals and antivirulence agents to fight against Candida albicans

    DEFF Research Database (Denmark)

    Cui, Jinhui; Ren, Biao; Tong, Yaojun

    2015-01-01

    Candida albicans, one of the pathogenic Candida species, causes high mortality rate in immunocompromised and high-risk surgical patients. In the last decade, only one new class of antifungal drug echinocandin was applied. The increased therapy failures, such as the one caused by multi-drug resist...

  10. Antifungal Potential of Host Defense Peptide Mimetics in a Mouse Model of Disseminated Candidiasis

    Directory of Open Access Journals (Sweden)

    Mobaswar Hossain Chowdhury

    2018-02-01

    Full Text Available Invasive candidiasis caused by Candida albicans and non-albicans Candida (NAC present a serious disease threat. Although the echinocandins are recommended as the first line of antifungal drug class, resistance to these agents is beginning to emerge, demonstrating the need for new antifungal agents. Host defense peptides (HDP exhibit potent antifungal activity, but as drugs they are difficult to manufacture efficiently, and they are often inactivated by serum proteins. HDP mimetics are low molecular weight non-peptide compounds that can alleviate these problems and were shown to be membrane-active against C. albicans and NAC. Here, we expand upon our previous works to describe the in vitro and in vivo activity of 11 new HDP mimetics that are active against C. albicans and NAC that are both sensitive and resistant to standard antifungal drugs. These compounds exhibit minimum inhibitory/fungicidal concentration (MIC/MFC in the µg/mL range in the presence of serum and are inhibited by divalent cations. Rapid propidium iodide influx into the yeast cells following in vitro exposure suggested that these HDP mimetics were also membrane active. The lead compounds were able to kill C. albicans in an invasive candidiasis CD-1 mouse model with some mimetic candidates decreasing kidney burden by 3–4 logs after 24 h in a dose-dependent manner. The data encouraged further development of this new anti-fungal drug class for invasive candidiasis.

  11. Macrophage Reporter Cell Assay for Screening Immunopharmacological Activity of Cell Wall-Active Antifungals

    OpenAIRE

    Lewis, Russell E.; Liao, Guangling; Young, Katherine; Douglas, Cameron; Kontoyiannis, Dimitrios P.

    2014-01-01

    Antifungal exposure can elicit immunological effects that contribute to activity in vivo, but this activity is rarely screened in vitro in a fashion analogous to MIC testing. We used RAW 264.7 murine macrophages that express a secreted embryonic alkaline phosphatase (SEAP) gene induced by transcriptional activation of NF-κB and activator protein 1 (AP-1) to develop a screen for immunopharmacological activity of cell wall-active antifungal agents. Isolates of Candida albicans and Aspergillus f...

  12. Fungal peritonitis in continuous ambulatory peritoneal dialysis: The impact of antifungal prophylaxis on patient and technique outcomes

    Directory of Open Access Journals (Sweden)

    K V Kumar

    2014-01-01

    Full Text Available Fungal peritonitis (FP is a rare, but serious complication of peritoneal dialysis. We analyzed the incidence of FP, associated risk factors and outcome of patients with FP and evaluated the role of prophylactic antifungal agent in reducing its incidence. We studied all patients with FP from January 2005 to January 2012. Study period was divided into two parts, period I (January 2005 to January 2010, when prophylactic antifungal was not used and period II (January 2010 to January 2012, when prophylactic antifungal (fluconazole was used. A total of 142 episodes of peritonitis were documented during this period of which 20 (14% were FP. During the study period I, 18 of 102 episodes of peritonitis (17.6% and in the study period II (with antifungal prophylaxis, only 2 of 40 episodes of peritonitis (5% were due to fungal infection (P = 0.04. Nine out of 20 patients (45% had prior exposure to antibiotics. Fungal isolates were Candida albicans in 65%, non-albicans Candida in 25%, Rhizopus species in 5% and Alternaria in 5% of the patients. While 12 out of 20 patients (60% recovered completely and were re-initiated on continuous ambulatory peritoneal dialysis (CAPD, 4 of them expired (20% and 4 others (20% were shifted to hemodialysis. Use of prophylactic antifungal agent significantly reduced the incidence of FP (P = 0.04. We conclude that - fluconazole when used as a prophylactic agent in the setting of bacterial peritonitis significantly reduces the incidence of subsequent FP in CAPD patients.

  13. Antifungal Effects of Bee Venom Components on Trichophyton rubrum: A Novel Approach of Bee Venom Study for Possible Emerging Antifungal Agent.

    Science.gov (United States)

    Park, Joonsoo; Kwon, Osung; An, Hyun-Jin; Park, Kwan Kyu

    2018-04-01

    Bee venom (BV) has been widely investigated for potential medical uses. Recent inadvertent uses of BV based products have shown to mitigate signs of fungal infections. However, the component mediating the antifungal effect has not been identified. This investigation compares bee venom in its whole and partial forms to evaluate the possible component responsible for the antifungal effect. Forty-eight plates inoculated with Trichophyton rubrum were allocated into four groups. The groups were treated with raw BV (RBV), melittin, apamin and BV based mist (BBM) respectively and each group was further allocated accordingly to three different concentrations. The areas were measured every other day for 14 days to evaluate the kinetic changes of the colonies. The interactions of ratio differences over interval were confirmed in groups treated with RBV and BBM. In RBV, the level of differences were achieved in groups treated with 10 mg/100 µl ( p =0.026) and 40 mg/100 µl ( p =0.000). The mean difference of ratio in groups treated with RBV was evident in day 3 and day 5. The groups that were treated with melittin or apamin did not show any significant interaction. In BBM groups, the significant levels of ratio differences over time intervals were achieved in groups treated with 200 µl/100 µl ( p =0.000) and 300 µl/100 µl ( p =0.030). The the bee venom in its whole form delivered a significant level of inhibition and we concluded that the venom in separated forms are not effective. Moreover, BV based products may exert as potential antifungal therapeutics.

  14. Antibacterial and Antifungal Activities of Punica Granatum Peel Extracts Against Oral Pathogens

    Directory of Open Access Journals (Sweden)

    Sh. Abdollahzadeh

    2011-03-01

    Full Text Available Objective: Punica granatum has been used for many years in folk medicine due to several purposes. The aim of the present study was to evaluate the effect of methanolic extract of Punica granatum peel (MEPGP against Streptococcus mutans, Staphylococcus aureus,Streptococcus salivarius, Streptococcus sanguinis, Staphylococcus epidermidis, Actynomyces viscosus, Lactobacillus acidophilus and Candida albicans.Materials and Methods: In this in vitro study, the mentioned oral organisms were cultured in blood agar and mueller-hinton media and then paper disks containing MEPGP at concentrations of 4 mg/ml, 8 mg/ml and 12 mg/ml were inserted on medias. The antimicrobialactivity was evaluated by agar disk diffusion method. The effects of three different concentrations of MEPGP against microorganisms were compared using one-way ANOVA and Tukey tests.Results: All concentrations of MEPGP had antibacterial activity against S. aureus and S.epidermidis. Only at concentration of 8 mg/ml and 12 mg/ml MEPGP was effective against L. acidophilus, S. mutans and S. salivarius. Furthermore; no concentrations ofMEPGP inhibited A. viscosus and C. albicans.Conclusion: This study suggests that MEPGP might be used as an antibacterial agent in controlling oral infections.

  15. Antibacterial and Antifungal Activities of Punica Granatum Peel Extracts Against Oral Pathogens

    Science.gov (United States)

    Abdollahzadeh, Sh.; Mashouf, RY.; Mortazavi, H.; Moghaddam, MH.; Roozbahani, N.; Vahedi, M.

    2011-01-01

    Objective: Punica granatum has been used for many years in folk medicine due to several purposes. The aim of the present study was to evaluate the effect of methanolic extract of Punica granatum peel (MEPGP) against Streptococcus mutans, Staphylococcus aureus, Streptococcus salivarius, Streptococcus sanguinis, Staphylococcus epidermidis, Actynomyces viscosus, Lactobacillus acidophilus and Candida albicans. Materials and Methods: In this in vitro study, the mentioned oral organisms were cultured in blood agar and mueller-hinton media and then paper disks containing MEPGP at concentrations of 4 mg/ml, 8 mg/ml and 12 mg/ml were inserted on medias. The antimicrobial activity was evaluated by agar disk diffusion method. The effects of three different concentrations of MEPGP against microorganisms were compared using one-way ANOVA and Tukey tests. Results: All concentrations of MEPGP had antibacterial activity against S. aureus and S. epidermidis. Only at concentration of 8 mg/ml and 12 mg/ml MEPGP was effective against L. acidophilus, S. mutans and S. salivarius. Furthermore; no concentrations of MEPGP inhibited A. viscosus and C. albicans. Conclusion: This study suggests that MEPGP might be used as an antibacterial agent in controlling oral infections. PMID:21998800

  16. Antifungal Activity of Culture Filtrates and Organic Extracts of Aspergillus spp. against Pythium ultimum

    OpenAIRE

    Rania Aydi-Ben Abdallah; Marwa Hassine; Hayfa Jabnoun-Khiareddine; Rabiaa Haouala; Mejda Daami-Remadi

    2014-01-01

    Culture filtrates, chloroform and ethyl acetate extracts of nine isolates of Aspergillus spp. (A. niger, A. terreus, A. flavus and Aspergillus sp.), isolated from soil and compost, were tested for antifungal activity against Pythium ultimum the causal agent of the potato Pythium leak. Culture filtrates showed a significant antifungal activity at the different tested concentrations. Total inhibition of the pathogen was induced by the filtrate of CH8 of Aspergillus sp., used at 10% ...

  17. Conazoles

    Directory of Open Access Journals (Sweden)

    Jan Heeres

    2010-06-01

    Full Text Available This review provides a historical overview of the analog based drug discovery of miconazole and its congeners, and is focused on marketed azole antifungals bearing the generic suffix “conazole”. The antifungal activity of miconazole, one of the first broad-spectrum antimycotic agents has been mainly restricted to topical applications. The attractive in vitro antifungal spectrum was a starting point to design more potent and especially orally active antifungal agents such as ketoconazole, itraconazole, posaconazole, fluconazole and voriconazole. The chemistry, in vitro and in vivo antifungal activity, pharmacology, and clinical applications of these marketed conazoles has been described.

  18. "Rhetoric to Reality"- Efficacy of Punica Granatum Peel Extract on Oral Candidiasis: An in vitro Study.

    Science.gov (United States)

    Madugula, Preethi; Reddy, Sudhakara; Koneru, Jyothirmai; Rao, Atla Srinivasa; Sruthi, Rayapureddi; Dalli, Divya Teja

    2017-01-01

    Global usage of synthetic drugs inadvertently has resulted in deleterious effects and antimicrobial resistance. Phytoextarcts with therapeutic properties appear to be appropriate substitutes for synthetic drugs. Punica granatum (Pomegranate) is a fruit rich in nutraceuticals and therapeutic properties that has lead to its widespread use as folk-medicine for treating innumerable diseases. To determine the in vitro antifungal efficacy of Punica granatum peel extract against the oral Candida compared with clotrimazole. An in vitro study was carried out on 60 saliva samples collected from patients confirmed by clinical and mycological examination as oral candidiasis and subjected to culture on Saborauds Dextrose Agar (SDA) medium and incubated at 37°C for 48 hours. The cultured Candida species were subjected to antifungal susceptibility test by agar well diffusion method. Punica granatum peel extract (Group-I), Ethanol (Group-II Negative control), Clotrimazole (Group-III-Positive control) were inoculated in wells and incubated. Zones of inhibitions were measured with a digital Vernier's callipers and subjected to statistical analysis. ANOVA (analysis of variance) was performed to compare inhibition zones and concentrations of all the three groups. Antifungal efficacy of Punica granatum group and Clotrimazole group were statistically significant with p-value Punica granatum approximated with that of the clotrimazole. The present research was just a venture to usual clinical approach. The results of the study reveal that MIC of peel extract of Punica granatum approximated with that of the clotrimazole. Hence, peel extract of Punica granatum may be used as a substitute for antifungal agents in clinical trials with standardization so as to minimize the deleterious effects for patient compliance.

  19. Inhibitory effects of antimicrobial agents against Fusarium species.

    Science.gov (United States)

    Kawakami, Hideaki; Inuzuka, Hiroko; Hori, Nobuhide; Takahashi, Nobumichi; Ishida, Kyoko; Mochizuki, Kiyofumi; Ohkusu, Kiyofumi; Muraosa, Yasunori; Watanabe, Akira; Kamei, Katsuhiko

    2015-08-01

    We investigated the inhibitory effects of antibacterial, biocidal, and antifungal agents against Fusarium spp. Seven Fusarium spp: four F. falciforme (Fusarium solani species complex), one Fusarium spp, one Fusarium spp. (Fusarium incarnatum-equiseti species complex), and one F. napiforme (Gibberella fujikuroi species complex), isolated from eyes with fungal keratitis were used in this study. Their susceptibility to antibacterial agents: flomoxef, imipenem, gatifloxacin, levofloxacin, moxifloxacin, gentamicin, tobramycin, and Tobracin® (contained 3,000 μg/ml of tobramycin and 25 μg/ml of benzalkonium chloride (BAK), a biocidal agent: BAK, and antifungal agents: amphotericin B, pimaricin (natamycin), fluconazole, itraconazole, miconazole, voriconazole, and micafungin, was determined by broth microdilution tests. The half-maximal inhibitory concentration (IC50), 100% inhibitory concentration (IC100), and minimum inhibitory concentration (MIC) against the Fusarium isolates were determined. BAK had the highest activity against the Fusarium spp. except for the antifungal agents. Three fluoroquinolones and two aminoglycosides had inhibitory effects against the Fusarium spp. at relatively high concentrations. Tobracin® had a higher inhibitory effect against Fusarium spp. than tobramycin alone. Amphotericin B had the highest inhibitory effect against the Fusarium spp, although it had different degrees of activity against each isolate. Our findings showed that fluoroquinolones, aminoglycosides, and BAK had some degree of inhibitory effect against the seven Fusarium isolates, although these agents had considerably lower effect than amphotericin B. However, the inhibitory effects of amphotericin B against the Fusarium spp. varied for the different isolates. Further studies for more effective medications against Fusarium, such as different combinations of antibacterial, biocidal, and antifungal agents are needed. © The Author 2015. Published by Oxford University Press on

  20. Defensins: antifungal lessons from eukaryotes

    Directory of Open Access Journals (Sweden)

    Patrícia M. Silva

    2014-03-01

    Full Text Available Over the last years, antimicrobial peptides (AMPs have been the focus of intense research towards the finding of a viable alternative to current antifungal drugs. Defensins are one of the major families of AMPs and the most represented among all eukaryotic groups, providing an important first line of host defense against pathogenic microorganisms. Several of these cysteine-stabilized peptides present a relevant effect against fungi. Defensins are the AMPs with the broader distribution across all eukaryotic kingdoms, namely, Fungi, Plantæ and Animalia, and were recently shown to have an ancestor in a bacterial organism. As a part of the host defense, defensins act as an important vehicle of information between innate and adaptive immune system and have a role in immunomodulation. This multidimensionality represents a powerful host shield, hard for microorganisms to overcome using single approach resistance strategies. Pathogenic fungi resistance to conventional antimycotic drugs is becoming a major problem. Defensins, as other AMPs, have shown to be an effective alternative to the current antimycotic therapies, demonstrating potential as novel therapeutic agents or drug leads. In this review, we summarize the current knowledge on some eukaryotic defensins with antifungal action. An overview of the main targets in the fungal cell and the mechanism of action of these AMPs (namely, the selectivity for some fungal membrane components are presented. Additionally, recent works on antifungal defensins structure, activity and citotoxicity are also reviewed.

  1. Hydroxyurea therapy in sickle cell anemia patients aids to maintain oral fungal colonization balance.

    Science.gov (United States)

    Salvia, Ana Carolina Rodrigues Danzi; Figueiredo, Maria Stella; Braga, Josefina Aparecida Pellegrini; Pereira, Daniel Freitas Alves; Brighenti, Fernanda Lourenção; Koga-Ito, C Y

    2013-08-01

    The aim of this study was to evaluate the frequency of Candida species and presence of lesions in the oral cavity of patients with sickle cell anemia (SS). The study included 30 patients diagnosed with sickle cell anemia and taking hydroxyurea for at least 90 days (SS/HU+); and 39 patients with sickle cell anemia and without hydroxyurea therapy (SS/HU-). Two control groups were constituted by healthy individuals matched to the test groups in age, gender, and oral conditions (C/HU+ for SS/HU+ and C/HU- for SS/HU-). Oral clinical examination and anamnesis were performed. Yeasts were collected by oral rinses and identified by API system. Antifungal susceptibility evaluation was performed according to the CLSI methodology. Data obtained for microorganisms counts were compared by Student's t test (SS/HU+ vs. C/HU+ and SS/HU- vs. C/HU-) using MINITAB for Windows 1.4. Significance level was set at 5%. No oral candidosis lesions were detected. Significant differences in yeasts counts were observed between SS/HU- group and the respective control, but there were no differences between SS/HU+ and C/HU+. Candida albicans was the most prevalent species in all groups. Candida famata was observed both in SS and control groups. Candida dubliniensis, Candida glabrata, Candida krusei, Candida tropicalis, Candida pelliculosa, and Candida parapsilosis were observed only in SS groups. Most strains were susceptible to all antifungal agents. Hydroxyurea therapy seems to decrease candidal counts and resistance rate in sickle cell anemia patients. However, further studies should be conducted in the future to confirm this finding. Hydroxyurea therapy in sickle cell anemia patients maintains fungal species balance in oral cavity. © 2013 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

  2. Using tools and technology to promote education and adherence to oral agents for cancer.

    Science.gov (United States)

    Burhenn, Peggy S; Smudde, Josephine

    2015-06-01

    The use of oral agents for cancer (OACs) is increasing, and oncology nurses are in an ideal position to educate patients about them and suggest methods to improve adherence. Once an OAC is ordered, the administration is the responsibility of the patient. Oncology nurses can use tools and technology to assist with education, which may promote adherence, and suggest reminder tools that can be used. Many electronic tools have been developed, such as smartphone applications, text messaging, electronic alarms, and glowing pill bottles. The researchers reviewed electronic devices, as well as traditional methods such as calendars and pillboxes, that can assist patients in remembering to take the medication they are administering at home. A literature search was compiled and websites were searched for patient education tools, reminder tools (electronic and manual), and smartphone applications. The project was part of the Oncology Nursing Society Putting Evidence Into Practice effort on oral adherence. Education alone is insufficient to promote adherence to oral medication regimens. Multicomponent interventions have demonstrated improved adherence, and tools and technology directed at improving adherence to oral agents can be used. The researchers found multiple reminder aids to assist patients in adhering to an oral regimen. They are highlighted in this article.

  3. Systematic review of natural agents for the management of oral mucositis in cancer patients

    DEFF Research Database (Denmark)

    Yarom, Noam; Ariyawardana, Anura; Hovan, Allan

    2013-01-01

    /or conflicting evidence. CONCLUSIONS: Of the various natural agents reviewed here, the available evidence supported a guideline only for two agents: a suggestion in favor of zinc and a recommendation against glutamine, in the treatment settings listed above. Well-designed studies of other natural agents......Abstract PURPOSE: The aim of this study was to review the available literature and define clinical practice guidelines for the use of natural agents for the prevention and treatment of oral mucositis. METHODS: A systematic review was conducted by the Mucositis Study Group of the Multinational...

  4. COMPARISON OF POTENCY OF ANTIFUNGAL ACTION OF DANDRUFF SHAMPOOS AND DIFFERENT PLANT EXTRACTS

    Directory of Open Access Journals (Sweden)

    Naga Padma P, Anuradha K, Divya K

    2015-04-01

    Full Text Available Context: Dandruff a very common scalp disorder with high prevalence in population is caused by numerous host factors in conjunction with Malassezia furfur. Most of the commercially available anti-dandruff hair shampoos contain some form of antifungal agent(s that appear to reduce the incidence of the disease. There are no good scientific studies done to prove the antifungal activity of commercially available hair shampoos. Aim: In this study commercially available shampoos were assessed for antifungal activity against a human dandruff isolate of M. furfur. The shampoos were Head & Shoulders, Clinic All Clear, and Pantene etc. The results demonstrated that all six of the assayed hair shampoos have some antifungal effect on growth of M. furfur. These products have poor efficacies, more side effects and give scope for recurrence of symptoms. Methods and Materials: Therefore different plant extracts that possess various active compounds which have antifungal activity could help to overcome the incidence of the disease and also avoid the emergence of resistance in the pathogen. The plant extracts were tested in different concentrations like 1:5, 1:10, 1:20 and they were hibiscus, neem, soap nut, etc. The inhibitory action was studied using agar well assay and disc diffusion method and the results indicated in percentage of inhibition. Conclusion: The study was significant as not only efficient known plant products with anti-dandruff activity could be compared with commercially available shampoos but also their better efficacies at minimum concentrations could be identified. This can help make a polyherbal mixture that could be incorporated in hair oil or shampoos for better anti-dandruff activity.

  5. “Rhetoric to Reality”- Efficacy of Punica Granatum Peel Extract on Oral Candidiasis: An in vitro Study

    Science.gov (United States)

    Reddy, Sudhakara; Koneru, Jyothirmai; Rao, Atla Srinivasa; Sruthi, Rayapureddi; Dalli, Divya Teja

    2017-01-01

    Introduction Global usage of synthetic drugs inadvertently has resulted in deleterious effects and antimicrobial resistance. Phytoextarcts with therapeutic properties appear to be appropriate substitutes for synthetic drugs. Punica granatum (Pomegranate) is a fruit rich in nutraceuticals and therapeutic properties that has lead to its widespread use as folk-medicine for treating innumerable diseases. Aim To determine the in vitro antifungal efficacy of Punica granatum peel extract against the oral Candida compared with clotrimazole. Materials and Methods An in vitro study was carried out on 60 saliva samples collected from patients confirmed by clinical and mycological examination as oral candidiasis and subjected to culture on Saborauds Dextrose Agar (SDA) medium and incubated at 37°C for 48 hours. The cultured Candida species were subjected to antifungal susceptibility test by agar well diffusion method. Punica granatum peel extract (Group-I), Ethanol (Group-II Negative control), Clotrimazole (Group-III-Positive control) were inoculated in wells and incubated. Zones of inhibitions were measured with a digital Vernier’s callipers and subjected to statistical analysis. ANOVA (analysis of variance) was performed to compare inhibition zones and concentrations of all the three groups. Results Antifungal efficacy of Punica granatum group and Clotrimazole group were statistically significant with p-value Punica granatum approximated with that of the clotrimazole. Conclusion The present research was just a venture to usual clinical approach. The results of the study reveal that MIC of peel extract of Punica granatum approximated with that of the clotrimazole. Hence, peel extract of Punica granatum may be used as a substitute for antifungal agents in clinical trials with standardization so as to minimize the deleterious effects for patient compliance. PMID:28274059

  6. The potential management of oral candidiasis using anti-biofilm therapies.

    Science.gov (United States)

    Chanda, Warren; Joseph, Thomson P; Wang, Wendong; Padhiar, Arshad A; Zhong, Mintao

    2017-09-01

    Candida albicans is a minor component of the oral microbiota and an opportunistic pathogen that takes advantage of the immunocompromised host and causes oral mucositis and oral candidiasis. This organism is able to undergo phenotypic modification from a yeast to hyphae growth phase, one of the key arsenals for immune cell evasion, tissue invasion and biofilm formation. The latter property coupled with overgrowth and immune compromising factors such as HIV/AIDS, cancer treatments, organ transplantation, diabetes, corticosteroid use, dentures, and broad-spectrum antibiotic use have modified the fungus from a normal component of the microflora to a foe of an oral cavity and resulting in reduced sensitivity towards commonly utilised antifungal agents. Hence, the need for alternative therapy to curb this plight is of importance. Making use of biomolecules produced by Streptococcus mutans, application of lactoferrin which is a nonspecific host defense factor found in saliva with metal chelating and broader antimicrobial properties, use of probiotics which have the capacity to boost the host immunity through eliciting Immunoglobulin A synthesis, and perturbing the pathogen's environment via competition of space and food, and application of photodynamic therapy can help to manage the burden of oral candidiasis. Copyright © 2017 Elsevier Ltd. All rights reserved.

  7. Synthesis, Structure Optimization and Antifungal Screening of Novel Tetrazole Ring Bearing Acyl-Hydrazones

    Directory of Open Access Journals (Sweden)

    Manzoor A. Malik

    2012-08-01

    Full Text Available Azoles are generally fungistatic, and resistance to fluconazole is emerging in several fungal pathogens. In an attempt to find novel azole antifungal agents with improved activity, a series of tetrazole ring bearing acylhydrazone derivatives were synthesized and screened for their in vitro antifungal activity. The mechanism of their antifungal activity was assessed by studying their effect on the plasma membrane using flow cytometry and determination of the levels of ergosterol, a fungal-specific sterol. Propidium iodide rapidly penetrated a majority of yeast cells when they were treated with the synthesized compounds at concentrations just above MIC, implying that fungicidal activity resulted from extensive lesions of the plasma membrane. Target compounds also caused a considerable reduction in the amount of ergosterol. The results also showed that the presence and position of different substituents on the phenyl ring of the acylhydrazone pendant seem to play a role on the antifungal activity as well as in deciding the fungistatic and fungicidal nature of the compounds.

  8. The postantifungal effect and phospholipase production of oral Candida albicans from smokers, diabetics, asthmatics, denture wearers and healthy individuals following brief exposure to subtherapeutic concentrations of chlorhexidine gluconate.

    Science.gov (United States)

    Ellepola, Arjuna N B; Joseph, Bobby K; Khan, Z U

    2014-09-01

    Candida albicans is the major aetiological agent of oral candidosis and one of its important virulent factors is the production of extracellular phospholipases, which can be modulated by subtherapeutic concentrations of antifungal agents thus decreasing their pathogenicity. Hence, considering that chlorhexidine gluconate (CG) is a common antimicrobial mouthwash used in dentistry and that its concentration in the mouth reaches subtherapeutic levels during dosage intervals due to the diluent effect of saliva and cleansing effect of the oral musculature, the postantifungal effect (PAFE) and the phospholipase production of oral C. albicans following brief exposure to subtherapeutic concentrations of CG was studied. Fifty C. albicans planktonic oral isolates obtained from smokers, diabetics, asthmatics using steroid inhalers, partial denture wearers and healthy individuals were exposed to three subtherapeutic concentrations of CG (0.005%, 0.0025% and 0.00125%) for 1 h. Isolates unexposed to CG was the control group. Thereafter the antiseptic was removed and the PAFE and phospholipase production was determined by a turbidometric method and a plate assay using an egg yolk agar medium respectively. Mean PAFE (hours) of 50 oral isolates of C. albicans following 1-h exposure to 0.005%, 0.0025% and 0.00125% CG was 6.97, 1.85 and 0.62 respectively. The phospholipase production of these isolates was significantly suppressed with a percentage reduction of 21.68, 18.20 and 14.04% following exposure to 0.005%, 0.0025% and 0.00125% CG respectively. Brief exposure of C. albicans isolates to subtherapeutic concentrations of CG would wield an antifungal effect by suppressing growth and phospholipase production, thereby quelling its pathogenicity. © 2014 Blackwell Verlag GmbH.

  9. Ebselen exerts antifungal activity by regulating glutathione (GSH) and reactive oxygen species (ROS) production in fungal cells.

    Science.gov (United States)

    Thangamani, Shankar; Eldesouky, Hassan E; Mohammad, Haroon; Pascuzzi, Pete E; Avramova, Larisa; Hazbun, Tony R; Seleem, Mohamed N

    2017-01-01

    Ebselen, an organoselenium compound and a clinically safe molecule has been reported to possess potent antifungal activity, but its antifungal mechanism of action and in vivo antifungal activity remain unclear. The antifungal effect of ebselen was tested against Candida albicans, C. glabrata, C. tropicalis, C. parapsilosis, Cryptococcus neoformans, and C. gattii clinical isolates. Chemogenomic profiling and biochemical assays were employed to identify the antifungal target of ebselen. Ebselen's antifungal activity in vivo was investigated in a Caenorhabditis elegans animal model. Ebselen exhibits potent antifungal activity against both Candida spp. and Cryptococcus spp., at concentrations ranging from 0.5 to 2μg/ml. Ebselen rapidly eradicates a high fungal inoculum within 2h of treatment. Investigation of the drug's antifungal mechanism of action indicates that ebselen depletes intracellular glutathione (GSH) levels, leading to increased production of reactive oxygen species (ROS), and thereby disturbs the redox homeostasis in fungal cells. Examination of ebselen's in vivo antifungal activity in two Caenorhabditis elegans models of infection demonstrate that ebselen is superior to conventional antifungal drugs (fluconazole, flucytosine and amphotericin) in reducing Candida and Cryptococcus fungal load. Ebselen possesses potent antifungal activity against clinically relevant isolates of both Candida and Cryptococcus by regulating GSH and ROS production. The potent in vivo antifungal activity of ebselen supports further investigation for repurposing it for use as an antifungal agent. The present study shows that ebselen targets glutathione and also support that glutathione as a potential target for antifungal drug development. Copyright © 2016 Elsevier B.V. All rights reserved.

  10. A curious case of cholestasis: oral terbinafine associated with cholestatic jaundice and subsequent erythema nodosum.

    Science.gov (United States)

    Kumar, Kartik; Gill, Anna; Shafei, Rachelle; Wright, Janine L

    2014-12-05

    Terbinafine is a commonly prescribed antifungal agent used in the treatment of trichophytic onychomycosis and chronic cutaneous mycosis that are resistant to other treatments. This case report highlights a rarely documented but important adverse hepatic reaction that was caused by the use of oral terbinafine. A woman in her thirties presented with a 3-week history of jaundice, malaise, itching, nausea, decreased appetite, weight loss, dark orange urine and intermittent non-radiating epigastric pain. She had recently finished a 3-week course of oral terbinafine for a fungal nail infection. Liver biopsy findings were consistent with chronic active hepatitis secondary to a drug reaction. A few days after initial presentation, the patient developed erythema nodosum. Delayed development of erythema nodosum secondary to terbinafine could not be excluded. 2014 BMJ Publishing Group Ltd.

  11. Antifungal and antioxidant activities of mature leaves of Myrcia splendens (Sw. DC.

    Directory of Open Access Journals (Sweden)

    F. C. Pontes

    2018-05-01

    Full Text Available Abstract In recent years, natural products with antifungal and antioxidant activities are being increasingly researched for a more sustainable alternative to the chemicals currently used for the same purpose. The plant pathogenic fungus Alternaria alternata is a causative agent of diseases in citrus, leading to huge economic losses. Antioxidants are important for the production of medicines for various diseases that may be related to the presence of free radicals, such as cancer, and in the cosmetic industry as an anti-aging agent and the food industry as preservatives. This study evaluated the antifungal and antioxidant potential of extracts of mature leaves of Myrcia splendens, a tree species that occurs in the Brazilian Cerrado. The antioxidant potential was analyzed by an assay of 1,1-diphenyl-2-picrylhydrazyl radical-scavenging method, and the antifungal activity was assessed through the evaluation of mycelial growth. Majority of the extracts exhibited a strong antioxidant activity, especially the acetonic extract (4A. The antioxidant activity may be related to the presence of phenolic compounds. However, the extracts showed no inhibitory activity of mycelial growth of the fungus tested, with the exception of dichloromethanic extract (2B, which had an inhibitory effect (10.2% at the end of testing.

  12. Synthesis Of Silver Nanoparticles Supported On Silica Using As Antifungal Agent By Gamma Irradiation

    International Nuclear Information System (INIS)

    Nguyen Thi Kim Lan; Nguyen Tue Anh; Dang Van Phu; Vo Kim Lang; Nguyen Thuy Khanh; Nguyen Quoc Hien

    2011-01-01

    Silver nanoparticles supported on silica (Ag nano/SiO 2 ) were prepared by gamma Co-60 irradiation method. The formation of Ag nano doped on silica particles was confirmed by the UV-Vis spectroscopy. The size of silver nanoparticles was characterized by transmission electron microscopy (TEM), X-ray diffraction (XRD) which showed the particle size of Ag nano to be in range of 15-30 nm for Ag + concentration 10 mM. In addition, antifungal activity of Ag nano/SiO 2 was tested against Aspergillus niger var Tieghn by plate count method. The results indicated that the antifungal efficiency of Ag nano/SiO 2 was about 64, 71, 81, 82 and 96% at the concentrations of Ag nanoparticles of 30, 50, 70, 100 and 150 ppm respectively. (author)

  13. Genetic diversity and antifungal susceptibility of Fusarium isolates in onychomycosis.

    Science.gov (United States)

    Rosa, Priscila D; Heidrich, Daiane; Corrêa, Carolina; Scroferneker, Maria Lúcia; Vettorato, Gerson; Fuentefria, Alexandre M; Goldani, Luciano Z

    2017-09-01

    Fusarium species have emerged as an important human pathogen in skin disease, onychomycosis, keratitis and invasive disease. Onychomycosis caused by Fusarium spp. The infection has been increasingly described in the immunocompetent and immunosuppressed hosts. Considering onychomycosis is a difficult to treat infection, and little is known about the genetic variability and susceptibility pattern of Fusarium spp., further studies are necessary to understand the pathogenesis and better to define the appropriate antifungal treatment for this infection. Accordingly, the objective of this study was to describe the in vitro susceptibility to different antifungal agents and the genetic diversity of 35 Fusarium isolated from patients with onychomycosis. Fusarium spp. were isolated predominantly from female Caucasians, and the most frequent anatomical location was the nail of the hallux. Results revealed that 25 (71.4%) of isolates belonged to the Fusarium solani species complex, followed by 10 (28.5%) isolates from the Fusarium oxysporum species complex. Noteworthy, the authors report the first case of Neocosmospora rubicola isolated from a patient with onychomycosis. Amphotericin B was the most effective antifungal agent against the majority of isolates (60%, MIC ≤4 μg/mL), followed by voriconazole (34.2%, MIC ≤4 μg/mL). In general, Fusarium species presented MIC values >64 μg/mL for fluconazole, itraconazole and terbinafine. Accurate pathogen identification, characterisation and susceptibility testing provide a better understanding of pathogenesis of Fusarium in onychomycosis. © 2017 Blackwell Verlag GmbH.

  14. Synthesis and antifungal evaluation of (1,2,3-triazol-4-yl)methyl nicotinate chitosan.

    Science.gov (United States)

    Qin, Yukun; Liu, Song; Xing, Ronge; Li, Kecheng; Yu, Huahua; Li, Pengcheng

    2013-10-01

    With an aim to discover novel chitosan derivatives with significant activities against crop-threatening fungi, (1,2,3-triazol-4-yl)methyl nicotinate chitosan (TAMNCS) was prepared via azide-alkyne click reaction. Its structure was characterized by FT-IR, (1)H NMR, elemental analysis, DSC, and SEM. In vitro antifungal properties of TAMNCS against Rhizoctonia solani Kühn (R. solani), Stemphylium solani weber (S. solani), and Alternaria porri (A. porri) were studied at the concentrations ranged from 0.25 mg/mL to 1.0 mg/mL. Experiments conducted displayed the derivative had obviously enhanced antifungal activity after chemical modification compared with original chitosan. Moreover, it was shown that TAMNCS can 94.2% inhibit growth of A. porri at 1.0 mg/mL, while dose at which the fungicide triadimefon had lower inhibitory index (62.2%). The primary antifungal results described here indicate this derivative may be a promising candidate as an antifungal agent. Copyright © 2013 Elsevier B.V. All rights reserved.

  15. Training should be the first step toward an antifungal stewardship program.

    Science.gov (United States)

    Valerio, Maricela; Muñoz, Patricia; Rodríguez-González, Carmen; Sanjurjo, María; Guinea, Jesús; Bouza, Emilio

    2015-04-01

    The frequency of use of systemic antifungal agents has increased significantly in most tertiary centers. However, antifungal stewardship has received very little attention. The objective of this article was to assess the knowledge of prescribing physicians in our institution as a first step in the development of an antifungal stewardship program. Attending physicians from the departments that prescribe most antifungals were invited to complete a questionnaire based on current guidelines on diagnosis and therapy of invasive candidiasis and invasive aspergillosis (IA). The survey was completed by 60.8% (200/329) of the physicians who were invited to participate. The physicians belonged to the following departments: medical (60%), pediatric (19%), intensive care (15.5%), and surgical (5.5%). The mean (±SD) score of correct responses was 5.16±1.73. In the case of candidiasis, only 55% of the physicians clearly distinguished between colonization and infection, and 17.5% knew the local rate of fluconazole resistance. Thirty-three percent knew the accepted indications for antifungal prophylaxis, and 23% the indications for empirical therapy. However, most physicians knew which antifungals to choose when starting empirical therapy (73.5%). As for aspergillosis, most physicians (67%) could differentiate between colonization and infection, and 34.5% knew the diagnostic value of galactomannan. The radiological features of IA were well recognized by 64%, but only 31.5% were aware of the first line of treatment for IA, and 36% of the recommended duration of therapy. The usefulness of antifungal levels was known by 67%. This simple, easily completed questionnaire enabled us to identify which areas of our training strategy could be improved. Copyright © 2013 Elsevier España, S.L.U. y Sociedad Española de Enfermedades Infecciosas y Microbiología Clínica. All rights reserved.

  16. Shifting to a non-vitamin K antagonist oral anticoagulation agent from vitamin K antagonist in atrial fibrillation

    DEFF Research Database (Denmark)

    Fosbøl, Emil L; Vinding, Naja Emborg; Lamberts, Morten

    2017-01-01

    Aims: After non-vitamin K antagonist (VKA) oral anticoagulation agents (NOAC) have been approved for thrombo-embolic prophylaxis in non-valvular atrial fibrillation (NVAF), utilization of oral anticoagulants (OAC) in NVAF has changed. Contemporary shifting from a VKA to a NOAC (dabigatran...

  17. Activities of Available and Investigational Antifungal Agents against Rhodotorula Species

    Science.gov (United States)

    Diekema, D. J.; Petroelje, B.; Messer, S. A.; Hollis, R. J.; Pfaller, M. A

    2005-01-01

    Rhodotorula species are emerging pathogens in immunocompromised patients. We report the in vitro activities of eight antifungals against 64 Rhodotorula isolates collected in surveillance programs between 1987 and 2003. Rhodotorula strains are resistant in vitro to fluconazole (MIC at which 50% of the isolates tested are inhibited [MIC50], >128 μg/ml) and caspofungin (MIC50, >8 μg/ml). Amphotericin B (MIC50,1 μg/ml) and flucytosine (MIC50, 0.12 μg/ml) are both active in vitro, and the new and investigational triazoles all have some in vitro activity, with ravuconazole being the most active (MIC50, 0.25 μg/ml). PMID:15635020

  18. Searching for an alternative oral contrast agent for GI tract MR imaging; in vitro phase, initial report

    International Nuclear Information System (INIS)

    Okla, W.; Szeszkowski, W.; Cieszanowski, A.; Golebiowski, M.

    2002-01-01

    MR has been recently considered to be suitable method for detection GI tract pathologies. A few substances (some of a natural origin) seem to act as an efficient oral MR contrast agents. The aim of this study is to find an alternative substance, which can be administrated orally to patients in order to enhance signal intensity (SI). The ideal agent should have a biphase pattern (high SI in T1 and low in T2), and should be nontoxic and cost effective. Phantom experiments were conducted with 1.5 T MR scanner. T1W and T2W sequences were used for initial estimation. Number of different agents such as: water, Gd-DTPA, barium sulfate, green tea, blueberry juice, cranberry juice, blackcurrant juice, and some more were evaluated. Signal intensity was measured by using elliptical region of interest (ROI). MR imaging in one patient with stomach cancer was also performed. In T1W-FFE sequence cranberry juice reached satisfactorily high signal (SI=1760.14). In T2W-TSE sequence this substance reduced signal intensity (SI=23.10) almost to background level. Blueberry juice appear to be the next substance capable to generate high signal (SI=1558.31) in T1W sequence (T1-TSE). MR examination of a patient with stomach adenocarcinoma (using blueberry juice as an oral contrast agent) satisfactorily depicted and delineated tumor mass on both: T1W and T2W images. Cranberry juice and blueberry juice seemed to act effectively as oral contrast agents for gastrointestinal MR imaging. Thus they need further exploration and trials. (author)

  19. Innovation of natural essential oil-loaded Orabase for local treatment of oral candidiasis.

    Science.gov (United States)

    Labib, Gihan S; Aldawsari, Hibah

    2015-01-01

    Oral candidiasis may be manifested in the oral cavity as either mild or severe oral fungal infection. This infection results from the overgrowth of Candida species normally existing in the oral cavity in minute amounts based on many predisposing factors. Several aspects have spurred the search for new strategies in the treatment of oral candidiasis, among which are the limited numbers of new antifungal drugs developed in recent years. Previous studies have shown that thyme and clove oils have antimycotic activities and have suggested their incorporation into pharmaceutical preparations. This study aimed to investigate the possibility of the incorporation and characterization of essential oils or their extracted active ingredients in Orabase formulations. Orabase loaded with clove oil, thyme oil, eugenol, and thymol were prepared and evaluated for their antifungal activities, pH, viscosity, erosion and water uptake characteristics, mechanical properties, in vitro release behavior, and ex vivo mucoadhesion properties. All prepared bases showed considerable antifungal activity and acceptable physical characteristics. The release pattern from loaded bases was considerably slow for all oils and active ingredients. All bases showed appreciable adhesion in the in vitro and ex vivo studies. The incorporation of essential oils in Orabase could help in future drug delivery design, with promising outcomes on patients' well-being.

  20. Antifungal Effects of Silver Nanoparticles (AgNPs) against Various Plant Pathogenic Fungi.

    Science.gov (United States)

    Kim, Sang Woo; Jung, Jin Hee; Lamsal, Kabir; Kim, Yun Seok; Min, Ji Seon; Lee, Youn Su

    2012-03-01

    This research is concerned with the fungicidal properties of nano-size silver colloidal solution used as an agent for antifungal treatment of various plant pathogens. We used WA-CV-WA13B, WA-AT-WB13R, and WA-PR-WB13R silver nanoparticles (AgNPs) at concentrations of 10, 25, 50, and 100 ppm. Eighteen different plant pathogenic fungi were treated with these AgNPs on potato dextrose agar (PDA), malt extract agar, and corn meal agar plates. We calculated fungal inhibition in order to evaluate the antifungal efficacy of silver nanoparticles against pathogens. The results indicated that AgNPs possess antifungal properties against these plant pathogens at various levels. Treatment with WA-CV-WB13R AgNPs resulted in maximum inhibition of most fungi. Results also showed that the most significant inhibition of plant pathogenic fungi was observed on PDA and 100 ppm of AgNPs.

  1. Chemical modification of antifungal polyene macrolide antibiotics

    International Nuclear Information System (INIS)

    Solovieva, S E; Olsufyeva, E N; Preobrazhenskaya, M N

    2011-01-01

    The review summarizes advances in the methods for the synthesis of polyene antibiotics (amphotericin B, partricin A, etc.) and investigations of the structure-activity relationship made in the last 15 years. State-of-the-art approaches based on the combination of the chemical synthesis and genetic engineering are considered. Emphasis is given to the design of semisynthetic antifungal agents against chemotherapy-resistant pathogens having the highest therapeutic indices. Recent results of research on the mechanisms of action of polyenes are outlined.

  2. Antifungal Activity of Bee Venom and Sweet Bee Venom against Clinically Isolated Candida albicans

    Directory of Open Access Journals (Sweden)

    Seung-Bae Lee

    2016-03-01

    Full Text Available Objectives: The purpose of this study was to investigate the antifungal effect of bee venom (BV and sweet bee venom (SBV against Candida albicans (C. albicans clinical isolates. Methods: In this study, BV and SBV were examined for antifungal activities against the Korean Collection for Type Cultures (KCTC strain and 10 clinical isolates of C. albicans. The disk diffusion method was used to measure the antifungal activity and minimum inhibitory concentration (MIC assays were performed by using a broth microdilution method. Also, a killing curve assay was conducted to investigate the kinetics of the anti- fungal action. Results: BV and SBV showed antifungal activity against 10 clinical isolates of C. albicans that were cultured from blood and the vagina by using disk diffusion method. The MIC values obtained for clinical isolates by using the broth microdilution method varied from 62.5 μg/ mL to 125 μg/mL for BV and from 15.63 μg/mL to 62.5 μg/mL for SBV. In the killing-curve assay, SBV behaved as amphotericin B, which was used as positive control, did. The antifungal efficacy of SBV was much higher than that of BV. Conclusion: BV and SBV showed antifungal activity against C. albicans clinical strains that were isolated from blood and the vagina. Especially, SBV might be a candidate for a new antifungal agent against C. albicans clinical isolates.

  3. Candida glabrata: an emerging oral opportunistic pathogen.

    Science.gov (United States)

    Li, L; Redding, S; Dongari-Bagtzoglou, A

    2007-03-01

    Following the widespread use of immunosuppressive therapy and broad-spectrum antimycotic prophylaxis, C. glabrata has emerged as an important opportunistic pathogen in the oral mucosa. In the past, studies on the virulence factors and host-pathogen interactions of this organism were scarce, but continued to rise in recent years. Denture-wearing, immunosuppression, antibiotic therapy, and aging are risk factors for oral colonization or infection with C. glabrata. Compared with C. albicans, C. glabrata exhibits lower oral keratinocyte-adherence capacity, but higher denture-surface-adherence ability. The role of extracellular hydrolase production in the virulence of this organism does not appear to be as important as it is in C. albicans pathogenesis. Although traditionally thought of as a non-transforming yeast organism, both phenotypic switching and pseudohyphal formation have recently been identified in C. glabrata, but their role in pathogenesis is not known. With the exception of granulocyte monocyte colony-stimulating factor, C. glabrata triggers a lower proinflammatory cytokine response in oral epithelial cells than does C. albicans, in a strain-dependent manner. C. glabrata is less susceptible to killing by human beta-defensins than is C. albicans and exhibits various degrees of resistance to the antifungal activity of salivary histatins and mucins. In addition, C. glabrata possesses both innate and acquired resistance against antifungal drugs, due to its ability to modify ergosterol biosynthesis, mitochondrial function, or antifungal efflux. This resistance allows for its relative overgrowth over other susceptible species and may contribute to the recent emergence of C. glabrata infections in chronically immunocompromised populations. Further investigations on the virulence and host-pathogen interactions of C. glabrata are needed to better define the pathogenesis of oral C. glabrata infection in susceptible hosts.

  4. Inhibitors of the glyoxylate cycle enzyme ICL1 in Candida albicans for potential use as antifungal agents.

    Directory of Open Access Journals (Sweden)

    Hong-Leong Cheah

    Full Text Available Candida albicans is an opportunistic pathogen that causes candidiasis in humans. In recent years, metabolic pathways in C. albicans have been explored as potential antifungal targets to treat candidiasis. The glyoxylate cycle, which enables C. albicans to survive in nutrient-limited host niches and its. Key enzymes (e.g., isocitrate lyase (ICL1, are particularly attractive antifungal targets for C. albicans. In this study, we used a new screening approach that better reflects the physiological environment that C. albicans cells experience during infection to identify potential inhibitors of ICL. Three compounds (caffeic acid (CAFF, rosmarinic acid (ROS, and apigenin (API were found to have antifungal activity against C. albicans when tested under glucose-depleted conditions. We further confirmed the inhibitory potential of these compounds against ICL using the ICL enzyme assay. Lastly, we assessed the bioavailability and toxicity of these compounds using Lipinski's rule-of-five and ADMET analysis.

  5. Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies.

    Science.gov (United States)

    Tafi, Andrea; Costi, Roberta; Botta, Maurizio; Di Santo, Roberto; Corelli, Federico; Massa, Silvio; Ciacci, Andrea; Manetti, Fabrizio; Artico, Marino

    2002-06-20

    The synthesis, anti-Candida activity, and quantitative structure-activity relationship (QSAR) studies of a series of 2,4-dichlorobenzylimidazole derivatives having a phenylpyrrole moiety (related to the antibiotic pyrrolnitrin) in the alpha-position are reported. A number of substituents on the phenyl ring, ranging from hydrophobic (tert-butyl, phenyl, or 1-pyrrolyl moiety) to basic (NH(2)), polar (CF(3), CN, SCH(3), NO(2)), or hydrogen bond donors and acceptor (OH) groups, were chosen to better understand the interaction of these compounds with cytochrome P450 14-alpha-lanosterol demethylase (P450(14DM)). Finally, the triazole counterpart of one of the imidazole compounds was synthesized and tested to investigate influence of the heterocyclic ring on biological activity. The in vitro antifungal activities of the newly synthesized azoles 10p-v,x-c' were tested against Candida albicans and Candida spp. at pH 7.2 and pH 5.6. A CoMFA model, previously derived for a series of antifungal agents belonging to chemically diverse families related to bifonazole, was applied to the new products. Because the results produced by this approach were not encouraging, Catalyst software was chosen to perform a new 3D-QSAR study. Catalyst was preferred this time because of the possibility of considering each compound as a collection of energetically reasonable conformations and of considering alternative stereoisomers. The pharmacophore model developed by Catalyst, named HYPO1, showed good performances in predicting the biological activity data, although it did not exhibit an unequivocal preference for one enantiomeric series of inhibitors relative to the other. One aromatic nitrogen with a lone pair in the ring plane (mapped by all of the considered compounds) and three aromatic ring features were recognized to have pharmacophoric relevance, whereas neither hydrogen bond acceptor nor hydrophobic features were found. These findings confirmed that the key interaction of azole

  6. Elimination of oral candidiasis may increase stimulated whole salivary flow rate.

    Science.gov (United States)

    Ohga, Noritaka; Yamazaki, Yutaka; Sato, Jun; Asaka, Takuya; Morimoto, Masahiro; Hata, Hironobu; Satoh, Chiharu; Kitagawa, Yoshimasa

    2016-11-01

    Candida infections are frequently encountered fungal infections in the oral mucosa. This study aimed to evaluate the effect of eliminating Candida spp. on stimulated whole salivary flow rate (SWS) in patients with oral candidiasis. This study involved 66 patients with oral candidiasis. Fifty-two consecutive patients, successfully treated by antifungal therapy, were available to examine the effect of elimination of oral Candida spp. on SWS (success group); the 14 patients who tested positive for Candida after therapy were retrospectively included (control group). SWS were used to measure saliva production. Moreover, tongue pain and xerostomia were evaluated using visual analog score (VAS). By eliminating oral Candida spp., SWS significantly increased in the success group after antifungal therapy [SWS: mean value 0.89±0.51ml/min (median 0.82ml/min: 0.15-2.14) to mean value 1.16±0.58ml/min (median 1.05ml/min: 0.2-2.93), Poral Candida spp. in patients with oral candidiasis. Copyright © 2016. Published by Elsevier Ltd.

  7. Invasive Fungal Infections in Patients with Hematological Malignancies: Emergence of Resistant Pathogens and New Antifungal Therapies

    Directory of Open Access Journals (Sweden)

    Maria N. Gamaletsou

    2018-02-01

    Full Text Available Invasive fungal infections caused by drug-resistant organisms are an emerging threat to heavily immunosuppressed patients with hematological malignancies. Modern early antifungal treatment strategies, such as prophylaxis and empirical and preemptive therapy, result in long-term exposure to antifungal agents, which is a major driving force for the development of resistance. The extended use of central venous catheters, the nonlinear pharmacokinetics of certain antifungal agents, neutropenia, other forms of intense immunosuppression, and drug toxicities are other contributing factors. The widespread use of agricultural and industrial fungicides with similar chemical structures and mechanisms of action has resulted in the development of environmental reservoirs for some drug-resistant fungi, especially azole-resistant Aspergillus species, which have been reported from four continents. The majority of resistant strains have the mutation TR34/L98H, a finding suggesting that the source of resistance is the environment. The global emergence of new fungal pathogens with inherent resistance, such as Candida auris, is a new public health threat. The most common mechanism of antifungal drug resistance is the induction of efflux pumps, which decrease intracellular drug concentrations. Overexpression, depletion, and alteration of the drug target are other mechanisms of resistance. Mutations in the ERG11 gene alter the protein structure of C-demethylase, reducing the efficacy of antifungal triazoles. Candida species become echinocandin-resistant by mutations in FKS genes. A shift in the epidemiology of Candida towards resistant non-albicans Candida spp. has emerged among patients with hematological malignancies. There is no definite association between antifungal resistance, as defined by elevated minimum inhibitory concentrations, and clinical outcomes in this population. Detection of genes or mutations conferring resistance with the use of molecular methods

  8. Lemon grass (Cymbopogon citratus essential oil as a potent anti-inflammatory and antifungal drugs

    Directory of Open Access Journals (Sweden)

    Mohamed Nadjib Boukhatem

    2014-09-01

    Full Text Available Background: Volatile oils obtained from lemon grass [Cymbopogon citratus (DC. Stapf, Poaceae family] are used in traditional medicine as remedies for the treatment of various diseases. Aims: In the present study, lemon grass essential oil (LGEO was evaluated for its in vivo topical and oral anti-inflammatory effects, and for its in vitro antifungal activity using both liquid and vapor phases. Methods: The chemical profile of LGEO as determined by gas chromatography–mass spectrometry analysis revealed two major components: geranial (42.2%, and neral (31.5%. The antifungal activity of LGEO was evaluated against several pathogenic yeasts and filamentous fungi using disc diffusion and vapor diffusion methods. Results: LGEO exhibited promising antifungal effect against Candida albicans, C. tropicalis, and Aspergillus niger, with different inhibition zone diameters (IZDs (35–90 mm. IZD increased with increasing oil volume. Significantly, higher anti-Candida activity was observed in the vapor phase. For the evaluation of the anti-inflammatory effect, LGEO (10 mg/kg, administered orally significantly reduced carrageenan-induced paw edema with a similar effect to that observed for oral diclofenac (50 mg/kg, which was used as the positive control. Oral administration of LGEO showed dose-dependent anti-inflammatory activity. In addition, topical application of LGEO in vivo resulted in a potent anti-inflammatory effect, as demonstrated by using the mouse model of croton oil-induced ear edema. To our knowledge, this is the first such report to be published. The topical application of LGEO at doses of 5 and 10 µL/ear significantly reduced acute ear edema induced by croton oil in 62.5 and 75% of the mice, respectively. In addition, histological analysis clearly confirmed that LGEO inhibits the skin inflammatory response in animal models. Conclusion: Results of the present study indicate that LGEO has a noteworthy potential for the development of drugs for

  9. Oral available agents in the treatment of RRMS

    Directory of Open Access Journals (Sweden)

    Aupérin T

    2013-10-01

    Full Text Available Thierry Aupérin Medical Communications, Global MS Medical Affairs, Genzyme Corporation, Cambridge, MA, USAWe read with interest the article by Drs Thöne and Ellrichmann entitled "Oral available agents in the treatment of relapsing remitting multiple sclerosis: an overview of merits and culprits" recently published in Drug, Healthcare and Patient Safety.1 The review provides a valuable overview of a number of new therapeutic options for multiple sclerosis (MS, with a focus on proposed mechanisms of action and efficacy and safety profiles of the respective agents.In reading the article, however, we did note a number of errors pertaining to teriflunomide, a once-daily oral immunomodulator approved in several countries for the treatment of relapsing forms of MS (RMS and relapsing-remitting MS (RRMS. The most significant error pertains to a statement made within the safety section, which states: "Serious adverse effects (AEs included pathological liver function, neutropenia, and trigeminal neuralgia as well as one case of progressive multifocal leukoencephalopathy (PML in a patient with systemic lupus erythematosus." We would like to draw the authors’ attention to the fact that this case of PML pertains to the use of the related drug, leflunomide, and not teriflunomide as suggested. It is important to note that leflunomide is licensed to treat active rheumatoid arthritis in adults, and has not been evaluated or approved for the treatment of MS; as such it is inappropriate to extrapolate this observation to the use of teriflunomide. Furthermore, the case of PML cited in the article is complicated by the fact that the patient received prior multiple immunosuppressant therapies before leflunomide (ie, prednisone, azathioprine, chloroquine, danazol, cyclosporin A and methotrexate, which may have contributed to the development of PML.View original paper by Thöne and Ellrichmann.

  10. Activation of Melanin Synthesis in Alternaria infectoria by Antifungal Drugs.

    Science.gov (United States)

    Fernandes, Chantal; Prados-Rosales, Rafael; Silva, Branca M A; Nakouzi-Naranjo, Antonio; Zuzarte, Mónica; Chatterjee, Subhasish; Stark, Ruth E; Casadevall, Arturo; Gonçalves, Teresa

    2015-12-28

    The importance of Alternaria species fungi to human health ranges from their role as etiological agents of serious infections with poor prognoses in immunosuppressed individuals to their association with respiratory allergic diseases. The present work focuses on Alternaria infectoria, which was used as a model organism of the genus, and was designed to unravel melanin production in response to antifungals. After we characterized the pigment produced by A. infectoria, we studied the dynamics of 1,8-dihydroxynaphthalene (DHN)-melanin production during growth, the degree of melanization in response to antifungals, and how melanization affected susceptibility to several classes of therapeutic drugs. We demonstrate that A. infectoria increased melanin deposition in cell walls in response to nikkomycin Z, caspofungin, and itraconazole but not in response to fluconazole or amphotericin B. These results indicate that A. infectoria activates DHN-melanin synthesis in response to certain antifungal drugs, possibly as a protective mechanism against these drugs. Inhibition of DHN-melanin synthesis by pyroquilon resulted in a lower minimum effective concentration (MEC) of caspofungin and enhanced morphological changes (increased hyphal balloon size), characterized by thinner and less organized A. infectoria cell walls. In summary, A. infectoria synthesizes melanin in response to certain antifungal drugs, and its susceptibility is influenced by melanization, suggesting the therapeutic potential of drug combinations that affect melanin synthesis. Copyright © 2016, American Society for Microbiology. All Rights Reserved.

  11. Essential oil of Algerian Eucalyptus citriodora: Chemical composition, antifungal activity.

    Science.gov (United States)

    Tolba, H; Moghrani, H; Benelmouffok, A; Kellou, D; Maachi, R

    2015-12-01

    Essential oil of Eucalyptus citriodora is a natural product which has been attributed for various medicinal uses. In the present investigation, E. citriodora essential oil was used to evaluate its antifungal effect against medically important dermatophytes. Essential oil from the Algerian E. citriodora leaves was analyzed by GC and GC/MS. The antifungal effect of E. citriodora essential oil was evaluated against four dermatophytes: Microsporum canis, Microsporum gypseum, Trichophyton mentagrophytes, Trichophyton rubrum using disc diffusion method, disc volatilization method, and agar dilution method. The chemical composition of the oil revealed the presence of 22 compounds accounting for 95.27% of the oil. The dominant compounds were citronellal (69.77%), citronellol (10.63%) and isopulegol (4.66%). The disc diffusion method, MIC and MFC determination, indicated that E. citriodora essential oil had a higher antifungal potential against the tested strains with inhibition zone diameter which varied from (12 to 90mm) and MIC and MFC values ranged from (0.6 to 5μL/mL and 1.25 to 5μL/mL) respectively. The M. gypseum was the most resistant to the oil. The results of the present study indicated that E. citriodora essential oil may be used as a new antifungal agent recommended by the pharmaceutical industries. Copyright © 2015 Elsevier Masson SAS. All rights reserved.

  12. Essential Oils and Antifungal Activity

    Science.gov (United States)

    Coppola, Raffaele; De Feo, Vincenzo

    2017-01-01

    Since ancient times, folk medicine and agro-food science have benefitted from the use of plant derivatives, such as essential oils, to combat different diseases, as well as to preserve food. In Nature, essential oils play a fundamental role in protecting the plant from biotic and abiotic attacks to which it may be subjected. Many researchers have analyzed in detail the modes of action of essential oils and most of their components. The purpose of this brief review is to describe the properties of essential oils, principally as antifungal agents, and their role in blocking cell communication mechanisms, fungal biofilm formation, and mycotoxin production. PMID:29099084

  13. Effect of cultivation conditions on growth and antifungal activity of ...

    African Journals Online (AJOL)

    Administrator

    Growth and production of antifungal agent by Mycena leptocephala was investigated in different culture media composition at various initial pH and temperatures. Maximum growth and activity was observed at the initial pH of 5.5 and 25oC. No detectable growth and activity was observed at pH of 3.5 and 7.5. Growth of the ...

  14. Barium sulfate suspension as a negative oral contrast agent for MR imaging

    International Nuclear Information System (INIS)

    Li, K.C.P.; Tart, R.P.; Fitzsimmons, J.R.; Storm, B.; Mao, J.

    1989-01-01

    Proton spectroscopy with linewidth measurements and MR imaging were performed on various commercially available barium sulfate suspensions as well as inorganic sulfates and barium salts. Approximately 500 mL of 20%, 40%, 60%, and 70% wt/wt single-contrast oral barium sulfate suspensions were administered to four normal volunteers, and MR imaging was performed with both a 1.5-T and a 0.15-T MR imager. As much as 80% of the small bowel and the entire colon were well visualized with the 60% or 70% wt/wt single-contrast barium sulfate suspensions. The authors conclude that barium sulfate suspensions are useful as oral MR contrast agents

  15. Resolution of disseminated fusariosis in a child with acute leukemia treated with combined antifungal therapy: a case report

    Directory of Open Access Journals (Sweden)

    Zarallo Luis

    2007-05-01

    Full Text Available Abstract Background Fusarium spp. is being isolated with increasing frequency as a pathogen in oncohematologic patients. Caspofungin and amphotericin B have been reported to have synergistic activity against Fusarium spp. Case presentation We herein report a case of disseminated fusariosis diagnosed by chest CT scan and positive blood cultures to Fusarium spp. Because the patient's clinical condition deteriorated, CRP levels increased, and blood cultures continued to yield Fusarium spp. despite liposomal amphotericin B monotherapy up to 5 mg/kg daily, treatment with caspofungin was added. Within 2 weeks of onset of combined antifungal therapy, the chest CT scan demonstrated a progressive resolution of the pulmonary lesions. Upon discontinuation of intravenous antifungals, the patient received suppressive therapy with oral voriconazole. Three months later, a chest CT scan showed no abnormalities. Twenty-five months after discontinuation of all antifungal therapy, the patient remains in complete remission of her neoplastic disease with no signs of clinical activity of the Fusarium infection. Conclusion This is the first description of successful treatment of disseminated fusariosis in a pediatric patient with acute lymphoblastic leukemia with caspofungin and amphotericin B followed by oral suppressive therapy with voriconazole.

  16. The antifungal effect of peptides from hymenoptera venom and their analogs

    Czech Academy of Sciences Publication Activity Database

    Slaninová, Jiřina; Putnová, Helena; Borovičková, Lenka; Šácha, Pavel; Čeřovský, Václav; Monincová, Lenka; Fučík, Vladimír

    2011-01-01

    Roč. 6, č. 2 (2011), s. 150-159 ISSN 1895-104X R&D Projects: GA ČR GA203/08/0536 Institutional research plan: CEZ:AV0Z40550506 Keywords : antifungal agents * candida * fluorescent microscopy * rhodamine 6G * fluorescein-labeled peptide Subject RIV: CC - Organic Chemistry Impact factor: 1.000, year: 2011

  17. Antifungal compounds from cyanobacteria.

    Science.gov (United States)

    Shishido, Tânia K; Humisto, Anu; Jokela, Jouni; Liu, Liwei; Wahlsten, Matti; Tamrakar, Anisha; Fewer, David P; Permi, Perttu; Andreote, Ana P D; Fiore, Marli F; Sivonen, Kaarina

    2015-04-13

    Cyanobacteria are photosynthetic prokaryotes found in a range of environments. They are infamous for the production of toxins, as well as bioactive compounds, which exhibit anticancer, antimicrobial and protease inhibition activities. Cyanobacteria produce a broad range of antifungals belonging to structural classes, such as peptides, polyketides and alkaloids. Here, we tested cyanobacteria from a wide variety of environments for antifungal activity. The potent antifungal macrolide scytophycin was detected in Anabaena sp. HAN21/1, Anabaena cf. cylindrica PH133, Nostoc sp. HAN11/1 and Scytonema sp. HAN3/2. To our knowledge, this is the first description of Anabaena strains that produce scytophycins. We detected antifungal glycolipopeptide hassallidin production in Anabaena spp. BIR JV1 and HAN7/1 and in Nostoc spp. 6sf Calc and CENA 219. These strains were isolated from brackish and freshwater samples collected in Brazil, the Czech Republic and Finland. In addition, three cyanobacterial strains, Fischerella sp. CENA 298, Scytonema hofmanni PCC 7110 and Nostoc sp. N107.3, produced unidentified antifungal compounds that warrant further characterization. Interestingly, all of the strains shown to produce antifungal compounds in this study belong to Nostocales or Stigonematales cyanobacterial orders.

  18. Antifungal Compounds from Cyanobacteria

    Directory of Open Access Journals (Sweden)

    Tânia K. Shishido

    2015-04-01

    Full Text Available Cyanobacteria are photosynthetic prokaryotes found in a range of environments. They are infamous for the production of toxins, as well as bioactive compounds, which exhibit anticancer, antimicrobial and protease inhibition activities. Cyanobacteria produce a broad range of antifungals belonging to structural classes, such as peptides, polyketides and alkaloids. Here, we tested cyanobacteria from a wide variety of environments for antifungal activity. The potent antifungal macrolide scytophycin was detected in Anabaena sp. HAN21/1, Anabaena cf. cylindrica PH133, Nostoc sp. HAN11/1 and Scytonema sp. HAN3/2. To our knowledge, this is the first description of Anabaena strains that produce scytophycins. We detected antifungal glycolipopeptide hassallidin production in Anabaena spp. BIR JV1 and HAN7/1 and in Nostoc spp. 6sf Calc and CENA 219. These strains were isolated from brackish and freshwater samples collected in Brazil, the Czech Republic and Finland. In addition, three cyanobacterial strains, Fischerella sp. CENA 298, Scytonema hofmanni PCC 7110 and Nostoc sp. N107.3, produced unidentified antifungal compounds that warrant further characterization. Interestingly, all of the strains shown to produce antifungal compounds in this study belong to Nostocales or Stigonematales cyanobacterial orders.

  19. In vitro and in vivo antifungal activities of selected Cameroonian dietary spices.

    Science.gov (United States)

    Dzoyem, Jean Paul; Tchuenguem, Roland T; Kuiate, Jules R; Teke, Gerald N; Kechia, Frederick A; Kuete, Victor

    2014-02-17

    Spices and herbs have been used in food since ancient times to give taste and flavor and also as food preservatives and disease remedies. In Cameroon, the use of spices and other aromatic plants as food flavoring is an integral part of dietary behavior, but relatively little is known about their antifungal potential.The present work was designed to assess the antifungal properties of extracts from spices used in Cameroonian dietary. The in vitro antifungal activities of twenty three extracts from twenty one spices were assessed by the broth micro-dilution method against eight fungi. Also, the in vivo activity of Olax subscorpioidea extract (the most active extract) was evaluated in rat model of disseminated candidiasis due to Candida albicans by estimating the fungal burden in blood and kidney. Seven extracts (30%) exhibited moderate to significant antifungal activities, inhibiting the growth of the microorganisms at concentrations ranging from 0.048 to 0.39 mg/mL. Olax subscorpioidea extract exhibited the highest antifungal activity particularly against Candida albicans and Candida tropicalis (MIC of 0.097 mg/mL and 0.048 mg/mL respectively). Sixteen extracts (70%) were weakly active (MICs > 6.25 mg/mL). Oral administration of O. subscorpioidea extract at the dose 2 g/kg of body weight (bw) to artificially infected rats revealed a drop in the number of colony forming units per milliliter (cfu/mL) of Candida albicans cells in the blood below the detection limit (100 cfu/mL) while a modest decrease was observed in the kidney. The present work shows that some of the spices studied possess interesting antifungal properties and could be used to treat candidiasis. Among the plant species tested, Olax subscorpioidea displayed the most promising result.

  20. Oral candidiasis and angular cheilitis.

    Science.gov (United States)

    Sharon, Victoria; Fazel, Nasim

    2010-01-01

    Candidiasis, an often encountered oral disease, has been increasing in frequency. Most commonly caused by the overgrowth of Candida albicans, oral candidiasis can be divided into several categories including acute and chronic forms, and angular cheilitis. Risk factors for the development of oral candidiasis include immunosuppression, wearing of dentures, pharmacotherapeutics, smoking, infancy and old age, endocrine dysfunction, and decreased salivation. Oral candidiasis may be asymptomatic. More frequently, however, it is physically uncomfortable, and the patient may complain of burning mouth, dysgeusia, dysphagia, anorexia, and weight loss, leading to nutritional deficiency and impaired quality of life. A plethora of antifungal treatments are available. The overall prognosis of oral candidiasis is good, and rarely is the condition life threatening with invasive or recalcitrant disease.

  1. Cyclization Reaction of Acyl Thiourea Chitosan: Enhanced Antifungal Properties via Structural Optimization.

    Science.gov (United States)

    Qin, Yukun; Liu, Weixiang; Xing, Ronge; Liu, Song; Li, Kecheng; Li, Pengcheng

    2018-03-06

    In this study, 3-methyl-1,2,4-triazolyl chitosan (MTACS) and 3-chloromethyl-1,2,4-triazolyl chitosan (CMTACS) were prepared via cyclization of acyl thiourea chitosan (TUCS). Their structures were confirmed by FT-IR, ¹H-NMR, elemental analysis, DSC, XRD, and SEM. The conformations were predicted using the Gaussian 09 program. Additionally, the antifungal properties of MTACS and CMTACS against Stemphylium solani weber ( S. solani ), Alternaria porri ( A. porri ), and Gloeosporium theae-sinensis ( G. theae-sinensis ) were assayed in vitro and ranged from 250 μg/mL to 1000 μg/mL. The results showed that MTACS and CMTACS exhibited enhanced inhibitory effect on the selected fungi compared to the original chitosan and TUCS. In particular, they displayed better antifungal activities against A. porri and G. theae-sinensis than that of the positive control, Triadimefon. The findings described here may lead to them being used as antifungal agents for crop protection.

  2. Cyclization Reaction of Acyl Thiourea Chitosan: Enhanced Antifungal Properties via Structural Optimization

    Directory of Open Access Journals (Sweden)

    Yukun Qin

    2018-03-01

    Full Text Available In this study, 3-methyl-1,2,4-triazolyl chitosan (MTACS and 3-chloromethyl-1,2,4-triazolyl chitosan (CMTACS were prepared via cyclization of acyl thiourea chitosan (TUCS. Their structures were confirmed by FT-IR, 1H-NMR, elemental analysis, DSC, XRD, and SEM. The conformations were predicted using the Gaussian 09 program. Additionally, the antifungal properties of MTACS and CMTACS against Stemphylium solani weber (S. solani, Alternaria porri (A. porri, and Gloeosporium theae-sinensis (G. theae-sinensis were assayed in vitro and ranged from 250 μg/mL to 1000 μg/mL. The results showed that MTACS and CMTACS exhibited enhanced inhibitory effect on the selected fungi compared to the original chitosan and TUCS. In particular, they displayed better antifungal activities against A. porri and G. theae-sinensis than that of the positive control, Triadimefon. The findings described here may lead to them being used as antifungal agents for crop protection.

  3. In vitro susceptibility patterns of clinically important Trichophyton and Epidermophyton species against nine antifungal drugs

    NARCIS (Netherlands)

    Badali, Hamid; Mohammadi, Rasoul; Mashedi, Olga; de Hoog, G Sybren; Meis, Jacques F

    Despite the common, worldwide, occurrence of dermatophytes, little information is available regarding susceptibility profiles against currently available and novel antifungal agents. A collection of sixty-eight clinical Trichophyton species and Epidermophyton floccosum were previously identified and

  4. [INVESTIGATION ON ANTIFUNGAL SUSCEPTIBILITY OF CANDIDA YEASTS IN PREGNANT PATIENTS WITH CONFIRMED VULVOVAGINAL CANDIDIASIS AND THEIR NEWBORNS.

    Science.gov (United States)

    Chokoeva, A; Kouzmanov, A; Ivanova, Z; Zisova, L; Amalie, G; Petleshkova, P; Miteva-Katrandzhieva, Ts; Krasteva, M; Uchikova, E

    Background Vulvovaginal candidiasis (VVU) is considered as a special risk factor during pregnancy, with important influence on the reproductive function of the patients and on the morbidity in the newborns from mothers with VVC. Maternal VVC is a major risk factor for the development of candida-colonization of the infant, which in turn is the first step towards the development of mucocutaneous or systemic candidiasis and Candida-septicemia in the newborn. In pregnant patients, the possible applicable local and systemic medications are limited, while the therapeutic resistance in chronic recurrent forms of VVC increases, facts that require precision of the diagnosic approach to optimize the therapeutic recommendations in pregnant patients, considered as a high risk group. The aim of this study was to investigate in vitro antifungal susceptibility of Candida yeasts to current antifungal agents in pregnant patients with confirmed VVC before the act of birth. Material and Methods Vaginal secretions of 23 healthy pregnant women with proven Candida vaginitis were taken within 48 hours before birth and the presence of yeasls of Candida was confirmed by culture examination. Between 47-72 hours after birth, samples were taken for Candida colonization of the oralmucosa and feces of their newborns. Samples were plated on Sabouraud agar and cultured in an incubator for 2 to 3 days at a temperature of 25° C. Species identification of the isolated yeasts were performed by commercial API Candida test - API 20C AUX (BioMerieux, Marcy-l'Etoile, France). Part of the isolates was identified by commercial whale AUXACOLOR (BioRad, Mames la Coquette, France). Antifungal sensitivity of isolated strains was examined by applying commercial solicitation ready kit and methods of disc diffusion and E-test, as the aim of the authors was to assess their potential for use in the diagnosis, and the correlation between them. Results Candida albicans was the prevalent etiological agent in pregnant

  5. Yeast flora of the mouth and skin during and after irradiation for oral and laryngeal cancer

    Energy Technology Data Exchange (ETDEWEB)

    Martin, M.V.; Al-Tikriti, U.; Bramley, P.A. (Sheffield Univ. (UK))

    1981-11-01

    The quantitative and qualitative changes occurring in the fungal flora of 22 patients with oral and 9 with laryngeal carcinoma were studied during and after radiation therapy. Each patient received 6000 rad of externally applied radiation in divided doses for 5 weeks. The fungal flora was isolated from the patients' oral cavity and irradiated skin sites during irradiation and 2 weeks and 4-6 months afterwards. The number and types of fungi increased in both groups of patients after the start of irradiation and persisted at high levels for at least 4-6 months after treatment. Candida albicans and C. tropicalis were the principal yeasts isolated throughout the period studied but seven other species were also identified. All the yeast isolates were sensitive in vitro to miconazole, ketoconazole, amphotericin B and nystatin. Any of these antifungal agents should be appropriate for therapy.

  6. Yeast flora of the mouth and skin during and after irradiation for oral and laryngeal cancer

    International Nuclear Information System (INIS)

    Martin, M.V.; Al-Tikriti, U.; Bramley, P.A.

    1981-01-01

    The quantitative and qualitative changes occurring in the fungal flora of 22 patients with oral and 9 with laryngeal carcinoma were studied during and after radiation therapy. Each patient received 6000 rad of externally applied radiation in divided doses for 5 weeks. The fungal flora was isolated from the patients' oral cavity and irradiated skin sites during irradiation and 2 weeks and 4-6 months afterwards. The number and types of fungi increased in both groups of patients after the start of irradiation and persisted at high levels for at least 4-6 months after treatment. Candida albicans and C. tropicalis were the principal yeasts isolated throughout the period studied but seven other species were also identified. All the yeast isolates were sensitive in vitro to miconazole, ketoconazole, amphotericin B and nystatin. Any of these antifungal agents should be appropriate for therapy. (author)

  7. Antifungal activity of the extract of Curcuma zedoaria (Christm. Roscoe, Zingiberaceae, against yeasts of the genus Candida isolated from the oral cavity of patients infected with the human immunodeficiency virus

    Directory of Open Access Journals (Sweden)

    Cristiane S. Shinobu-Mesquita

    2011-02-01

    Full Text Available Oropharyngeal candidiasis is the most common fungal infection among patients infected with the human immunodeficiency virus (HIV, and is treated empirically with topical or systemic antifungals. The objective of the present study was to investigate the possible antifungal action of the hydroalcoholic extract of Curcuma zedoaria (Christm. Roscoe, Zingiberaceae, on yeasts in this population. Samples were collected from HIV-positive patients who attended the Laboratory for Teaching and Research in Clinical Analysis at the Universidade Estadual de Maringá for routine exams. The isolated yeasts were identified at the genus and species levels through classical methodology. Next, tests of microdilution in broth were carried out to determine the profile of susceptibility of these yeasts towards the hydroalcoholic extract of C. zedoaria, following methodology standardised by the CLSI (2002. A total of 53 yeasts were identified, 49 of them C. albicans, two C. tropicalis and two C. glabrata. These yeasts were inhibited by low concentrations of the extract of C. zedoaria (between 1.95 and 15.63 μg/mL. In addition, 7.82 μg/mL inhibited 90% of the yeasts. Our results indicate a potent antifungal action for C. zedoaria and suggest more detailed studies with a view towards the practical application of this phytomedicine in topical pharmaceutical forms for the treatment of oral candidosis or candidiasis.

  8. Polymer multilayers loaded with antifungal β-peptides kill planktonic Candida albicans and reduce formation of fungal biofilms on the surfaces of flexible catheter tubes.

    Science.gov (United States)

    Raman, Namrata; Lee, Myung-Ryul; Palecek, Sean P; Lynn, David M

    2014-10-10

    Candida albicans is the most common fungal pathogen responsible for hospital-acquired infections. Most C. albicans infections are associated with the implantation of medical devices that act as points of entry for the pathogen and as substrates for the growth of fungal biofilms that are notoriously difficult to eliminate by systemic administration of conventional antifungal agents. In this study, we report a fill-and-purge approach to the layer-by-layer fabrication of biocompatible, nanoscale 'polyelectrolyte multilayers' (PEMs) on the luminal surfaces of flexible catheters, and an investigation of this platform for the localized, intraluminal release of a cationic β-peptide-based antifungal agent. We demonstrate that polyethylene catheter tubes with luminal surfaces coated with multilayers ~700nm thick fabricated from poly-l-glutamic acid (PGA) and poly-l-lysine (PLL) can be loaded, post-fabrication, by infusion with β-peptide, and that this approach promotes extended intraluminal release of this agent (over ~4months) when incubated in physiological media. The β-peptide remained potent against intraluminal inoculation of the catheters with C. albicans and substantially reduced the formation of C. albicans biofilms on the inner surfaces of film-coated catheters. Finally, we report that these β-peptide-loaded coatings exhibit antifungal activity under conditions that simulate intermittent catheter use and microbial challenge for at least three weeks. We conclude that β-peptide-loaded PEMs offer a novel and promising approach to kill C. albicans and prevent fungal biofilm formation on surfaces, with the potential to substantially reduce the incidence of device-associated infections in indwelling catheters. β-Peptides comprise a promising new class of antifungal agents that could help address problems associated with the use of conventional antifungal agents. The versatility of the layer-by-layer approach used here thus suggests additional opportunities to

  9. Candida species diversity and antifungal susceptibility patterns in oral samples of HIV/AIDS patients in Baja California, Mexico.

    Science.gov (United States)

    Clark-Ordóñez, Isadora; Callejas-Negrete, Olga A; Aréchiga-Carvajal, Elva T; Mouriño-Pérez, Rosa R

    2017-04-01

    Candidiasis is the most common opportunistic fungal infection in HIV patients. The aims of this study were to identify the prevalence of carriers of Candida, Candida species diversity, and in vitro susceptibility to antifungal drugs. In 297 HIV/AIDS patients in Baja California, Mexico, Candida strains were identified by molecular methods (PCR-RFLP) from isolates of oral rinses of patients in Tijuana, Mexicali, and Ensenada. 56.3% of patients were colonized or infected with Candida. In Tijuana, there was a significantly higher percentage of carriers (75.5%). Out of the 181 strains that were isolated, 71.8% were Candida albicans and 28.2% were non-albicans species. The most common non-albicans species was Candida tropicalis (12.2%), followed by Candida glabrata (8.3%), Candida parapsilosis (2.2%), Candida krusei (1.7%), and Candida guilliermondii (1.1%). Candida dubliniensis was not isolated. Two associated species were found in 11 patients. In Mexicali and Ensenada, there was a lower proportion of Candida carriers compared to other regions in Mexico and worldwide, however, in Tijuana, a border town with many peculiarities, a higher carrier rate was found. In this population, only a high viral load was associated with oral Candida carriers. Other factors such as gender, use of antiretroviral therapy, CD4+ T-lymphocyte levels, time since diagnosis, and alcohol/ tobacco consumption, were not associated with Candida carriers. © The Author 2016. Published by Oxford University Press on behalf of The International Society for Human and Animal Mycology. All rights reserved. For permissions, please e-mail: journals.permissions@oup.com.

  10. In Vitro Antifungal Susceptibility of Neoscytalidium dimidiatum Clinical Isolates from Malaysia.

    Science.gov (United States)

    James, Jasper Elvin; Santhanam, Jacinta; Lee, Mei Chen; Wong, Choon Xian; Sabaratnam, Parameswari; Yusoff, Hamidah; Tzar, Mohd Nizam; Razak, Mohd Fuat Abdul

    2017-04-01

    Neoscytalidium dimidiatum is an opportunistic fungus causing cutaneous infections mostly, which are difficult to treat due to antifungal resistance. In Malaysia, N. dimidiatum is associated with skin and nail infections, especially in the elderly. These infections may be mistaken for dermatophyte infections due to similar clinical appearance. In this study, Neoscytalidium isolates from cutaneous specimens, identified using morphological and molecular methods (28 Neoscytalidium dimidiatum and 1 Neoscytalidium sp.), were evaluated for susceptibility towards antifungal agents using the CLSI broth microdilution (M38-A2) and Etest methods. Amphotericin B, voriconazole, miconazole and clotrimazole showed high in vitro activity against all isolates with MIC ranging from 0.0313 to 1 µg/mL. Susceptibility towards fluconazole and itraconazole was noted in up to 10% of isolates, while ketoconazole was inactive against all isolates. Clinical breakpoints for antifungal drugs are not yet available for most filamentous fungi, including Neoscytalidium species. However, the results indicate that clinical isolates of N. dimidiatum in Malaysia were sensitive towards miconazole, clotrimazole, voriconazole and amphotericin B, in vitro.

  11. PgTeL, the lectin found in Punica granatum juice, is an antifungal agent against Candida albicans and Candida krusei.

    Science.gov (United States)

    da Silva, Pollyanna Michelle; de Moura, Maiara Celine; Gomes, Francis Soares; da Silva Trentin, Danielle; Silva de Oliveira, Ana Patrícia; de Mello, Gabriela Souto Vieira; da Rocha Pitta, Maira Galdino; de Melo Rego, Moacyr Jesus Barreto; Coelho, Luana Cassandra Breitenbach Barroso; Macedo, Alexandre José; de Figueiredo, Regina Celia Bressan Queiroz; Paiva, Patrícia Maria Guedes; Napoleão, Thiago Henrique

    2018-03-01

    The pomegranate (Punica granatum) sarcotesta contains a chitin-binding lectin (PgTeL) with antibacterial activity against human pathogenic species. In this work, the structural stability of PgTeL was evaluated by fluorimetric analysis and the lectin was evaluated for cytotoxicity to human peripheral blood mononuclear cells (PBMCs) and antifungal activity against Candida albicans and Candida krusei. PgTeL folding was impaired when lectin was incubated at pH≥6.0. On the other hand, the lectin did not undergo unfolding even when heated at 100°C. PgTeL (1, 10, and 100μg/mL) was not cytotoxic to PBMCs. Antifungal activity was detected for C. albicans (MIC: 25μg/mL; MFC: 50μg/mL) and C. krusei (MIC and MFC of 12.5μg/mL). Treatment of yeast cells with PgTeL resulted in decrease of intracellular ATP content even at sub-inhibitory concentrations (½MIC and ¼MIC) and induced lipid peroxidation. In addition, PgTeL damaged the integrity of fungal cell wall of both species, with more pronounced effects in C. krusei. The lectin showed significant antibiofilm activity on C. albicans at sub-inhibitory concentrations (0.195 and 0.39μg/mL). In conclusion, PgTeL is an anti-Candida agent whose action mechanism involves oxidative stress, energetic collapse, damage to the cell wall and rupture of yeast cells. Copyright © 2017 Elsevier B.V. All rights reserved.

  12. Study on wood vinegars for use as coagulating and antifungal agents on the production of natural rubber sheets

    Energy Technology Data Exchange (ETDEWEB)

    Baimark, Yodthong; Niamsa, Noi [Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Mahasarakham University, Mahasarakham 44150 (Thailand)

    2009-06-15

    Coagulating and antifungal properties of wood vinegars in the preparation process of Hevea brasiliensis natural rubber (NR) sheets were investigated and compared with those of formic and acetic acids. The wood vinegars produced from biomasses such as inner coconut shell, bamboo and Eucalyptus woods were evaluated. It was found that plasticity retention index, Mooney viscosity and mechanical properties of NR coagulated by wood vinegars were similar to those using acetic acid and better than using formic acid. The antifungal efficiency of coagulants determined from a fungi growth area on NR sheet surfaces was found in the following order: coconut shell wood vinegar > bamboo wood vinegar {approx} Eucalyptus wood vinegar > acetic acid {approx} formic acid. The antifungal efficiency of the wood vinegars was strongly depended upon their phenolic compound contents and confirmed through the inhibitory growth of the main fungi, Penicillium griseofulvum, on potato dextrose agar. (author)

  13. Studies on antifungal activity and elemental composition of the medicinal plant trianthema pentendra linn

    International Nuclear Information System (INIS)

    Pirzada, A.J.; Shaikh, W.; Ghaffar, S.A.

    2010-01-01

    Antifungal activity of crude solvent and aqueous extracts of the medicinal plant, Trianthema pentendra Linn., against the dermatophytic fungi, Aspergillus niger, Aspergillus flavus, Paecilomyces varioti, Microsporum gypseum and Trichophyton rubrum revealed that ethanol and aqueous extracts were the most effective antifungal agents as compared to methanol, chloroform and ethyl acetate extracts. Some basic elements, Al, Ca, Cu, Fe, Mg, Mn, P, S and Zn were also determined in the medicinal plant, T. pentendra, using atomic absorption spectrophotometry and U.V spectrophotometry. T. pentendra contained considerable amount of elements which have therapeutic effects in skin diseases. (author)

  14. Susceptibility profile of yeast-like organisms isolated from HIV/AIDS ...

    African Journals Online (AJOL)

    AIDS patients, particularly as the etiologic agent of oral thrush. Fluconazole antibiotic has been most popularly employed in treating cases of oral thrush in HIV/AIDS patients. Recent reports have recorded antifungal drug resistance amongst ...

  15. Oral hypoglycaemic agents, insulin resistance and cardiovascular disease in patients with type 2 diabetes

    DEFF Research Database (Denmark)

    Hemmingsen, Bianca; Lund, Søren S; Wetterslev, Jørn

    2009-01-01

    This article is a narrative review of the current evidence of the effects on cardiovascular disease (CVD) of oral hypoglycaemic agents that increase insulin sensitivity in patients with type 2 diabetes (T2D). In overweight T2D patients, metformin has been demonstrated to reduce CVD risk, and this......This article is a narrative review of the current evidence of the effects on cardiovascular disease (CVD) of oral hypoglycaemic agents that increase insulin sensitivity in patients with type 2 diabetes (T2D). In overweight T2D patients, metformin has been demonstrated to reduce CVD risk......, and this beneficial effect may be conserved with the combination of metformin and insulin treatment. However, the effect of glitazones on CVD is uncertain. There is conflicting evidence from large randomized trials to support a protective effect against CVD of lowering blood glucose per se but a systematic review...

  16. Effect of temperature, pH and detergents on the antifungal activity of bacterial culture filtrates against Mycosphaerella fijiensis

    Directory of Open Access Journals (Sweden)

    Eilyn Mena

    2014-01-01

    Full Text Available The bacteria associated to crops have been studied as potential biocontrol agents. However, few investigations on the interaction Musa spp. - Mycosphaerella fijiensis-Musa associated bacteria have been developed. Consequently, bacterial metabolites involved and the effect on them of physical and chemical factors remain unknown. Therefore, this study aimed to determine the effect of temperature, pH and detergents on bacterial culture filtrates with antifungal activity in vitro against Mycosphaerella fijiensis. The pathogen growth inhibition was assessed by absorbance reading at OD 565nm. It was found that the antifungal activity of the bacterial culture filtrates against M. fijiensis, varied in the presence of different values of temperature, pH, and types of detergents and this was related to the bacterial strain. The results suggested the possible protein nature of the metabolites with antifungal activity. Keywords: bacteria, biological control, antifungal metabolites

  17. Microemulsion and Microemulsion-Based Gels for Topical Antifungal Therapy with Phytochemicals.

    Science.gov (United States)

    Boonme, Prapaporn; Kaewbanjong, Jarika; Amnuaikit, Thanaporn; Andreani, Tatiana; Silva, Amélia M; Souto, Eliana B

    2016-01-01

    Skin fungal infections are regular injuries suffered by people living in tropical areas. Most common pathogens are Trichophyton, Microsporum and Epidermophyton which can cause skin lesions in many parts of body. Topical antifungal phytochemicals are commonly used to avoid systemic adverse events and are more convenient for patient application than those administered by other routes. However, the effectiveness of topical treatments in eradicating fungal infection is more limited since the stratum corneum acts as the skin barrier, resulting in long treatment duration and low patient's compliance. The goal of this work is to identify optimized drug delivery systems to improve topic clinical efficacy. Microemulsions i.e. liquid dispersions of oil and water stabilized with an interfacial film of surfactant are well known drug delivery systems. A thickening agent may be included to form microemulsion-based gels to increase skin adhesion. Microemulsions and microemulsion-based gels can be loaded with several hydrophilic and lipophilic drugs because they are composed of both water and oil phases. Microemulsions and microemulsion-based gels can also be used for the delivery of many drugs including antifungal drugs through stratum corneum due to their capacity to act as skin penetration enhancement. In addition to a comprehensive review of microemulsion and microemulsion-based gels as suitable carriers for skin delivery of various antifungal drugs, this review also aims to discuss the delivery of antifungal phytochemicals.

  18. Antifungal susceptibility and phylogeny of opportunistic members of the order mucorales.

    Science.gov (United States)

    Vitale, Roxana G; de Hoog, G Sybren; Schwarz, Patrick; Dannaoui, Eric; Deng, Shuwen; Machouart, Marie; Voigt, Kerstin; van de Sande, Wendy W J; Dolatabadi, Somayeh; Meis, Jacques F; Walther, Grit

    2012-01-01

    The in vitro susceptibilities of 66 molecularly identified strains of the Mucorales to eight antifungals (amphotericin B, terbinafine, itraconazole, posaconazole, voriconazole, caspofungin, micafungin, and 5-fluorocytosine) were tested. Molecular phylogeny was reconstructed based on the nuclear ribosomal large subunit to reveal taxon-specific susceptibility profiles. The impressive phylogenetic diversity of the Mucorales was reflected in susceptibilities differing at family, genus, and species levels. Amphotericin B was the most active drug, though somewhat less against Rhizopus and Cunninghamella species. Posaconazole was the second most effective antifungal agent but showed reduced activity in Mucor and Cunninghamella strains, while voriconazole lacked in vitro activity for most strains. Genera attributed to the Mucoraceae exhibited a wide range of MICs for posaconazole, itraconazole, and terbinafine and included resistant strains. Cunninghamella also comprised strains resistant to all azoles tested but was fully susceptible to terbinafine. In contrast, the Lichtheimiaceae completely lacked strains with reduced susceptibility for these antifungals. Syncephalastrum species exhibited susceptibility profiles similar to those of the Lichtheimiaceae. Mucor species were more resistant to azoles than Rhizopus species. Species-specific responses were obtained for terbinafine where only Rhizopus arrhizus and Mucor circinelloides were resistant. Complete or vast resistance was observed for 5-fluorocytosine, caspofungin, and micafungin. Intraspecific variability of in vitro susceptibility was found in all genera tested but was especially high in Mucor and Rhizopus for azoles and terbinafine. Accurate molecular identification of etiologic agents is compulsory to predict therapy outcome. For species of critical genera such as Mucor and Rhizopus, exhibiting high intraspecific variation, susceptibility testing before the onset of therapy is recommended.

  19. Synthesis and preliminary evaluation of N-acylhydrazone compounds as antibacterial and antifungal agents; Sintese e avaliacao preliminar da atividade antibacteriana e antifungica de derivados N-acilidrazonicos

    Energy Technology Data Exchange (ETDEWEB)

    Cachiba, Thomas Haruo; Carvalho, Bruno Demartini; Carvalho, Diogo Teixeira [Universidade Federal de Alfenas, MG (Brazil). Fac. de Ciencias Farmaceuticas. Dept. de Alimentos e Medicamentos; Cusinato, Marina; Prado, Clara Gaviao; Dias, Amanda Latercia Tranches, E-mail: diogo.carvalho@unifal-mg.edu.br [Universidade Federal de Alfenas, MG (Brazil). Inst. de Ciencias Biomedicas

    2012-07-01

    We describe the synthesis and evaluation of N-acylhydrazone compounds bearing different electron-donating groups in one of its aromatic rings, obtained using a four-step synthetic route. IC{sub 50} values against pathogenic fungi and bacteria were determined by serial microdilution. Compounds showed low activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. By contrast, a derivative with a meta-oriented electron-donating group showed significant activity (IC50) against Candida albicans (17 {mu}M), C. krusei (34 {mu}M) and C. tropicalis (17 {mu}M). Results suggest this is a promising lead-compound for synthesis of potent antifungal agents. (author)

  20. Preclinical Pharmacokinetics and Pharmacodynamic Target of SCY-078, a First-in-Class Orally Active Antifungal Glucan Synthesis Inhibitor, in Murine Models of Disseminated Candidiasis.

    Science.gov (United States)

    Wring, Stephen A; Randolph, Ryan; Park, SeongHee; Abruzzo, George; Chen, Qing; Flattery, Amy; Garrett, Graig; Peel, Michael; Outcalt, Russell; Powell, Kendall; Trucksis, Michelle; Angulo, David; Borroto-Esoda, Katyna

    2017-04-01

    SCY-078 (MK-3118) is a novel, semisynthetic derivative of enfumafungin and represents the first compound of the triterpene class of antifungals. SCY-078 exhibits potent inhibition of β-(1,3)-d-glucan synthesis, an essential cell wall component of many pathogenic fungi, including Candida spp. and Aspergillus spp. SCY-078 is currently in phase 2 clinical development for the treatment of invasive fungal diseases. In vitro disposition studies to assess solubility, intestinal permeability, and metabolic stability were predictive of good oral bioavailability. Preclinical pharmacokinetic studies were consistent with once-daily administration to humans. After intravenous delivery, plasma clearance in rodents and dogs was low, representing candidiasis, exceeded plasma by 20- to 25-fold for the area under the concentration-time curve from 0 h to infinity (AUC 0-∞ ) and C max SCY-078 achieved efficacy endpoints following oral delivery across multiple murine models of disseminated candidiasis. The pharmacokinetic/pharmacodynamic indices C max /MIC and AUC/MIC correlated with outcome. Target therapeutic exposure, expressed as the plasma AUC 0-24 , was comparable across models, with an upper value of 11.2 μg·h/ml (15.4 μM·h); the corresponding mean value for free drug AUC/MIC was ∼0.75. Overall, these results demonstrate that SCY-078 has the oral and intravenous (i.v.) pharmacokinetic properties and potency in murine infection models of disseminated candidiasis to support further investigation as a novel i.v. and oral treatment for invasive fungal diseases. Copyright © 2017 Wring et al.

  1. Preclinical Pharmacokinetics and Pharmacodynamic Target of SCY-078, a First-in-Class Orally Active Antifungal Glucan Synthesis Inhibitor, in Murine Models of Disseminated Candidiasis

    Science.gov (United States)

    Randolph, Ryan; Park, SeongHee; Abruzzo, George; Chen, Qing; Flattery, Amy; Garrett, Graig; Peel, Michael; Outcalt, Russell; Powell, Kendall; Trucksis, Michelle; Angulo, David; Borroto-Esoda, Katyna

    2017-01-01

    ABSTRACT SCY-078 (MK-3118) is a novel, semisynthetic derivative of enfumafungin and represents the first compound of the triterpene class of antifungals. SCY-078 exhibits potent inhibition of β-(1,3)-d-glucan synthesis, an essential cell wall component of many pathogenic fungi, including Candida spp. and Aspergillus spp. SCY-078 is currently in phase 2 clinical development for the treatment of invasive fungal diseases. In vitro disposition studies to assess solubility, intestinal permeability, and metabolic stability were predictive of good oral bioavailability. Preclinical pharmacokinetic studies were consistent with once-daily administration to humans. After intravenous delivery, plasma clearance in rodents and dogs was low, representing candidiasis, exceeded plasma by 20- to 25-fold for the area under the concentration-time curve from 0 h to infinity (AUC0–∞) and Cmax. SCY-078 achieved efficacy endpoints following oral delivery across multiple murine models of disseminated candidiasis. The pharmacokinetic/pharmacodynamic indices Cmax/MIC and AUC/MIC correlated with outcome. Target therapeutic exposure, expressed as the plasma AUC0–24, was comparable across models, with an upper value of 11.2 μg·h/ml (15.4 μM·h); the corresponding mean value for free drug AUC/MIC was ∼0.75. Overall, these results demonstrate that SCY-078 has the oral and intravenous (i.v.) pharmacokinetic properties and potency in murine infection models of disseminated candidiasis to support further investigation as a novel i.v. and oral treatment for invasive fungal diseases. PMID:28137806

  2. Antimicrobial and antifungal activities of the extracts and essential oils of Bidens tripartita.

    Directory of Open Access Journals (Sweden)

    Michał Tomczyk

    2008-12-01

    Full Text Available The aim of this study was to determine the antibacterial and antifungal properties of the extracts, subextracts and essential oils of Bidens tripartita flowers and herbs. In the study, twelve extracts and two essential oils were investigated for activity against different Gram-positive Bacillus subtilis, Micrococcus luteus, Staphylococcus aureus, Gram-negative bacteria Escherichia coli, E. coli (beta-laktamase+, Klebsiella pneumoniae (ESBL+, Pseudomonas aeruginosa and some fungal organisms Candida albicans, C. parapsilosis, Aspergillus fumigatus, A. terreus using a broth microdilution and disc diffusion methods. The results obtained indicate antimicrobial activity of the tested extracts (except butanolic extracts, which however did not inhibit the growth of fungi used in this study. Bacteriostatic effect of both essential oils is insignificant, but they have strong antifungal activity. These results support the use of B. tripartita to treat a microbial infections and it is indicated as an antimicrobial and antifungal agent, which may act as pharmaceuticals and preservatives.

  3. Phytochemical Analysis and Antifungal Activity of Extracts from Leaves and Fruit Residues of Brazilian Savanna Plants Aiming Its Use as Safe Fungicides.

    Science.gov (United States)

    Breda, Caroline Alves; Gasperini, Alessandra Marcon; Garcia, Vera Lucia; Monteiro, Karin Maia; Bataglion, Giovana Anceski; Eberlin, Marcos Nogueira; Duarte, Marta Cristina Teixeira

    2016-08-01

    The increasing demand for safe food without preservatives or pesticides residues has encouraged several studies on natural products with antifungal activity and low toxicity. In this study, ethanolic extracts from leaves and fruit residues (peel and seeds) of three Brazilian savanna species (Acrocomia aculeata, Campomanesia adamantium and Caryocar brasiliense) were evaluated against phytopathogenic fungi. Additionally, the most active extract was chemically characterized by ESI-MS and its oral acute toxicity was evaluated. Extracts from C. brasiliense (pequi) peel and leaves were active against Alternaria alternata, Alternaria solani and Venturia pirina with minimal inhibitory concentrations between 350 and 1000 µg/mL. When incorporated in solid media, these extracts extended the lag phase of A. alternata and A. solani and reduced the growth rate of A. solani. Pequi peel extract showed better antifungal activity and their ESI-MS analysis revealed the presence of substances widely reported as antifungal such as gallic acid, quinic acid, ellagic acid, glucogalin and corilagin. The oral acute toxicity was relatively low, being considered safe for use as a potential natural fungicide.

  4. Efficacy of steroidal vs non-steroidal agents in oral lichen planus: a randomised, open-label study.

    Science.gov (United States)

    Singh, A R; Rai, A; Aftab, M; Jain, S; Singh, M

    2017-01-01

    This study compared the therapeutic efficacy of steroidal and non-steroidal agents for treating oral lichen planus. Forty patients with clinical and/or histologically proven oral lichen planus were randomly placed into four groups and treated with topical triamcinolone, oral dapsone, topical tacrolimus or topical retinoid for three months. Pre- and post-treatment symptoms and signs were scored for each patient. Patients in all treatment groups showed significant clinical improvement after three months (p 0.05) and for topical retinoid vs topical tacrolimus (p > 0.05). Non-steroidal drugs such as dapsone, tacrolimus and retinoid are as efficacious as steroidal drugs for treating oral lichen planus, and avoid the side effects associated with steroids.

  5. Antifungal Activity of the Crude Extracts and Extracted Phenols from Gametophytes and Sporophytes of Two Species of Adiantum

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    Piyali Guha (Ghosh

    2005-12-01

    Full Text Available The water extracts and extracted phenols from gametophytes and different parts of sporophytes of the two ferns, Adiantum capillus-veneris L. and Adiantum lunulatum Burm. f., used as folkloric medicines in India, China, Tibet, America, Philippines and Italy, were investigated for their antifungal activity against Aspergillus niger and Rhizopus stolonifer. Both crude extracts and extracted phenols of gametophytes and different parts of sporophytes of both fern species were found to be bioactive against the fungal strains. Antifungal activity was found to be higher in gametophytes than different parts of sporophytes. Among the different parts of sporophyte, immature pinnule possesses highest fungistatic property. Adiantum capillus-veneris was found a better antifungal agent than Adiantum lunulatum.

  6. Candida albicans isolated from urine: Phenotypic and molecular identification, virulence factors and antifungal susceptibility

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    Laura Wiebusch

    2017-07-01

    Conclusions: C. albicans isolates from urine have a high capacity for virulence and can be associated with infectious processes. Furthermore, the high percentage of isolates resistant to itraconazole is important because this antifungal agent is commonly used to treat fungal infections in the hospital environment.

  7. In vitro antifungal susceptibility of clinical species belonging to Aspergillus genus and Rhizopus oryzae.

    Science.gov (United States)

    Kachuei, R; Khodavaisy, S; Rezaie, S; Sharifynia, S

    2016-03-01

    Among filamentous fungal pathogens, Aspergillus spp. and zygomycetes account for highest rates of morbidity and mortality among immunocompromised patients. Recently developed antifungal drugs offer the potential to improve management and therapeutic outcomes of fungal infections. The aim of this study was to analyse the in vitro activities of voriconazole, itraconazole, amphotericin B and caspofungin against clinical isolates of Aspergillus spp. and Rhizopus oryzae. The in vitro antifungal susceptibility of 54 isolates belonging to different clinical isolates of Aspergillus spp. and R. oryzae was tested for four antifungal agents using a microdilution reference method (CLSI, M38-A2). All isolates were identified by typical colony and microscopic characteristics, and also characterized by molecular methods. Caspofungin (MEC range: 0.008-0.25 and MEC50: 0.0023μg/mL) was the most active drug in vitro against Aspergillus spp., followed by voriconazole (MIC range: 0.031-8 and MIC50: 0.5μg/mL), itraconazole (MIC range: 0.031-16 and MIC50: 0.25μg/mL), and amphotericin B (MIC range: 0.125-4 and MIC50: 0.5μg/mL), in order of decreasing activity. The caspofungin, voriconazole, and itraconazole demonstrated poor in vitro activity against R. oryzae isolates evaluated, followed by amphotericin B. This study demonstrates that caspofungin had good antifungal activity and azole agents had better activity than amphotericin B against Aspergillus species. Although, azole drugs are considered ineffective against R. oryzae. This result is just from a small scale in vitro susceptibility study and we did not take other factors into consideration. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  8. The comparative study of antifungal activity of Syzygium aromaticum, Punica granatum and nystatin on Candida albicans; an in vitro study.

    Science.gov (United States)

    Mansourian, A; Boojarpour, N; Ashnagar, S; Momen Beitollahi, J; Shamshiri, A R

    2014-12-01

    Candida species are opportunistic fungi, among which, Candida albicans is the most important species responsible for infections in immunocompromised patients with invasive fungal disease. Resistance of Candida species to antifungal drugs has led scientists to pay more attention to traditional medicine herbs. Due to the limitations in the treatment of fungal diseases such as shortages, high prices, antifungal side effects and drug resistance or reduced susceptibility to fungal drugs we decided to study the antifungal effects of herbal extracts of Syzygium aromaticum and Punica granatum. Twenty-one isolates of oral C. albicans in patients with denture stomatitis referred to prosthesis department, Dental faculty of Tehran University of Medical Sciences were prepared and cultured. Plant extracts were prepared from the herbs market. Tests on patient samples and standard strains 5027ATCC (PTCC10231) yeast C. albicans were performed via well diffusion method. In addition, nystatin and methanol were used as positive and negative control, respectively. Finally, the antifungal effect of extracts using Statistical Repeated measurement ANOVA test was investigated. Both S. aromaticum and P. granatum showed noticeable antifungal activity in well method. Syzygium aromaticum showed better anti candida activity than nystatin (Pgranatum showed good antifungal effects (P-value<0.001). S. aromaticum (inhibition zone diameter: 29.62) showed better antifungal effects than nystatin (inhibition zone diameter: 28.48). Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  9. Atividade antimicrobiana, antiaderente e antifúngica in vitro de plantas medicinais brasileiras sobre microrganismos do biofilme dental e cepas do gênero Candida In vitro antimicrobial, antiadherent and antifungal activity of Brazilian medicinal plants on oral biofilm microorganisms and strains of the genus Candida

    Directory of Open Access Journals (Sweden)

    Pollianna Muniz Alves

    2009-04-01

    Full Text Available Avaliou-se in vitro a atividade antimicrobiana, antifúngica e antiaderente da aroeira-do-sertão, malva e goiabeira sobre microrganismos do biofilme dental e candidose oral. Os extratos mostraram-se eficazes, inibindo o crescimento das bactérias do biofilme dental e fungos da candidose oral, sugerindo a utilização dessas plantas como meio alternativo na terapêutica odontológica.The antimicrobial, antifungal and antiadherent activity of aroeira-do-sertão, mallow and guava tree on oral biofilm microorganisms and oral candidiasis was evaluated in vitro. The extracts were shown to be effective in inhibiting the growth of bacteria of the oral biofilm and fungi of oral candidiasis, thus suggesting that these extracts can be used as alternative means of dental therapy.

  10. Isolation and characterization of an antifungal protein from Bacillus licheniformis HS10.

    Science.gov (United States)

    Wang, Zhixin; Wang, Yunpeng; Zheng, Li; Yang, Xiaona; Liu, Hongxia; Guo, Jianhua

    2014-11-07

    Bacillus licheniformis HS10 is a good biocontrol agent against Pseudoperonospora cubensis which caused cucumber downy disease. To identify and characterize the antifungal proteins produced by B.licheniformis HS10, the proteins from HS10 were isolated by using 30-60% ammonium sulfate precipitation, and purified with column chromatography on DEAE Sepharose Fast Flow, RESOURCE Q and Sephadex G-75. And the SDS-PAGE and MALDI-TOF/TOF-MS analysis results demonstrated that the antifungal protein was a monomer with molecular weight of about 55 kDa, identified as carboxypeptidase. Our experiments also showed that the antifungal protein from B. licheniformis HS10 had significantly inhibition on eight different kinds of plant pathogenic fungi, and it was stable with good biological activity at as high as 100°C for 30 min and in pH value ranged from 6 to 10. The biological activity was negatively affected by protease K and 10mM metal cations except Ca(2+). Copyright © 2014 Elsevier Inc. All rights reserved.

  11. Non-vitamin K antagonist oral anticoagulation agents in anticoagulant naïve atrial fibrillation patients

    DEFF Research Database (Denmark)

    Olesen, Jonas Bjerring; Sørensen, Rikke; Hansen, Morten Lock

    2015-01-01

    AIMS: Non-vitamin K antagonist oral anticoagulation (NOAC) agents have been approved for stroke prophylaxis in atrial fibrillation (AF). We investigated 'real-world' information on how these drugs are being adopted. METHODS AND RESULTS: Using Danish nationwide administrative registers, we identif...

  12. The management of oral candidosis in diabetic patient with maxillary Herpes Zoster

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    Kus Harijanti

    2008-09-01

    Full Text Available Background: Oral candidosis is an infection caused by mainly Candida albicans. Candida species are common normal flora in the oral cavity and have been reported to be present in 40% to 60% of the population. Candida is predominantly an opportunistic infectious agent. Infection frequency has increased because of the presence of both local and systemic risk factors. The elderly age and diabetes mellitus may decrease the amount of saliva (xerostomia and potentially increase the risk of colonization and secondary infection by Candida. Herpes Zoster (HZ is a manifestation of the reactivation of latent varicella zoster virus. It is characterized by unilateral, painful, vesicular rash with a dermatomal distribution. The clinical manifestations of this disease can erupt to the skin and mucous membrane. If maxillary nerve is involved, the lesion can appear on unilateral facial skin and oral mucous membrane. Purpose: The purpose of this paper is to report and discuss the difficulties in managing the oral candidosis in elderly patient (57 year old male who suffered from maxillary Herpes Zoster and diabetes mellitus. Case management: At first, the patient was treated with 2% chlorhexidine gluconate and mycostatin oral suspension as topical antimycotic and reffered to dermathology clinic for viral infection treatment, however the oral candidosis did not improved. Subsequently, ketokonazole tablet was given three times daily for three weeks and regulated blood glucose level. In systemic antifungi (ketokonazole treatment the oral candidosis disappeared. Conclusion: In this case, it is conclude that the management of oral candidosis are adequate, antiviral, blood glucose level regulating and systemic antifungal therapy.

  13. Antifungal Edible Coatings for Fresh Citrus Fruit: A Review

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    Lluís Palou

    2015-12-01

    Full Text Available According to their origin, major postharvest losses of citrus fruit are caused by weight loss, fungal diseases, physiological disorders, and quarantine pests. Cold storage and postharvest treatments with conventional chemical fungicides, synthetic waxes, or combinations of them are commonly used to minimize postharvest losses. However, the repeated application of these treatments has led to important problems such as health and environmental issues associated with fungicide residues or waxes containing ammoniacal compounds, or the proliferation of resistant pathogenic fungal strains. There is, therefore, an increasing need to find non-polluting alternatives to be used as part of integrated disease management (IDM programs for preservation of fresh citrus fruit. Among them, the development of novel natural edible films and coatings with antimicrobial properties is a technological challenge for the industry and a very active research field worldwide. Chitosan and other edible coatings formulated by adding antifungal agents to composite emulsions based on polysaccharides or proteins and lipids are reviewed in this article. The most important antifungal ingredients are selected for their ability to control major citrus postharvest diseases like green and blue molds, caused by Penicillium digitatum and Penicillium italicum, respectively, and include low-toxicity or natural chemicals such as food additives, generally recognized as safe (GRAS compounds, plant extracts, or essential oils, and biological control agents such as some antagonistic strains of yeasts or bacteria.

  14. Posaconazole

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    Bhattacharya M

    2010-01-01

    Full Text Available Posaconazole is a novel second-generation Triazole oral antifungal agent. It is highly effective in the prophylaxis of invasive fungal infections in immunocompromised patients. It is used as a first-line agent as well as for salvage therapy in invasive fungal infections including aspergillosis, oropharyngeal and esophageal candidiasis. It has a good adverse effect profile. With the rising incidence of invasive fungal infections due to the HIV pandemic and medical advancements in transplantation and cancer therapy, these features make posaconazole a valuable addition in the family of antifungal agents.

  15. Identification of antifungal compounds active against Candida albicans using an improved high-throughput Caenorhabditis elegans assay.

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    Ikechukwu Okoli

    2009-09-01

    Full Text Available Candida albicans, the most common human pathogenic fungus, can establish a persistent lethal infection in the intestine of the microscopic nematode Caenorhabditis elegans. The C. elegans-C. albicans infection model was previously adapted to screen for antifungal compounds. Modifications to this screen have been made to facilitate a high-throughput assay including co-inoculation of nematodes with C. albicans and instrumentation allowing precise dispensing of worms into assay wells, eliminating two labor-intensive steps. This high-throughput method was utilized to screen a library of 3,228 compounds represented by 1,948 bioactive compounds and 1,280 small molecules derived via diversity-oriented synthesis. Nineteen compounds were identified that conferred an increase in C. elegans survival, including most known antifungal compounds within the chemical library. In addition to seven clinically used antifungal compounds, twelve compounds were identified which are not primarily used as antifungal agents, including three immunosuppressive drugs. This assay also allowed the assessment of the relative minimal inhibitory concentration, the effective concentration in vivo, and the toxicity of the compound in a single assay.

  16. Multicenter Brazilian Study of Oral Candida Species Isolated from Aids Patients

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    Priscilla de Laet Sant'Ana

    2002-03-01

    Full Text Available Oropharyngeal candidiasis continues to be considered the most common opportunistic disease in Aids patients. This study was designed to investigate species distribution, serotype and antifungal susceptibility profile among Candida spp. isolated from the oral cavity of Aids patients recruited from six Brazilian university centers. Oral swabs from 130 Aids patients were plated onto CHROMagar Candida medium and 142 isolates were recovered. Yeast isolates were identified by classical methods and serotyped using the Candida Check® system-Iatron. Antifungal susceptibility testing was performed according to the NCCLS microbroth assay. C. albicans was the most frequently isolated species (91%, and 70% of the isolates belonged to serotype A. We detected 12 episodes of co-infection (9%, including co-infection with both serotypes of C. albicans. Non-albicans species were isolated from 12 episodes, 50% of them exhibited DDS or resistance to azoles. Otherwise, only 8 out 130 isolates of C. albicans exhibited DDS or resistance to azoles. Brazilian Aids patients are infected mainly by C. albicans serotype A, most of them susceptible to all antifungal drugs.

  17. Investigation of the effect of base strength on the antifungal activity and chemical composition of the fish scales hydrolyzates

    International Nuclear Information System (INIS)

    Niaz, S.; Dil, S.

    2016-01-01

    The effect of base strength on the antifungal activity of the fish scale hydrolyzate was investigated for six types of samples prepared from the scales of Cyprinus carpio using sodium hydroxide in the range of 1-11 percent strength in the aqueous solution. Each of the sample was analyzed for its acid-base content using titration against HCl in addition to the spot test analysis for phenolic compounds. Each of these samples was analyzed using FTIR spectroscopy. Variation in chemical composition and functional group were observed with variation in the base strength. The in vitro antifungal activity of the fish scale hydrolyzates was tested against four pathogenic fungi including Acremonium, Pythium, Verticillium, and Alternaria. The antifungal assay was carried out using agar well diffusion methods. The sterilization was carried out using streptomycin while ketoconazole was used as the standard antifungal agent. Minimum inhibitory concentration was determined for the most active hydrolyzate which was obtained by 9 percent base solution. The cause of this antifungal activity was also discussed in this communication. (author)

  18. Bioavailability of voriconazole in hospitalised patients

    NARCIS (Netherlands)

    Veringa, Anette; Geling, Sanne; Span, Lambert F R; Vermeulen, Karin M; Zijlstra, Jan G; van der Werf, Tjip S; Kosterink, Jos G W; Alffenaar, Jan-Willem C

    An important element in antimicrobial stewardship programmes is early switch from intravenous (i.v.) to oral antimicrobial treatment, especially for highly bioavailable drugs. The antifungal agent voriconazole is available both in i.v. and oral formulations and bioavailability is estimated to be

  19. The Elements of Antifungal Drug Discovery

    DEFF Research Database (Denmark)

    Kjellerup, Lasse

    In this PhD thesis I will explore the development of antifungal drugs. Fungal infections are estimated to cause the death of 1.5 million patients each year. There is currently a need for new antifungal drugs as the existing drugs are hampered by lack of broad-spectrum antifungal activity, resista...

  20. Differential Antifungal Activity of Human and Cryptococcal Melanins with Structural Discrepancies

    OpenAIRE

    Néstor Correa; Néstor Correa; Néstor Correa; Cristian Covarrubias; Paula I. Rodas; Germán Hermosilla; Verónica R. Olate; Verónica R. Olate; Cristián Valdés; Wieland Meyer; Fabien Magne; Cecilia V. Tapia; Cecilia V. Tapia

    2017-01-01

    Melanin is a pigment found in all biological kingdoms, and plays a key role in protection against ultraviolet radiation, oxidizing agents, and ionizing radiation damage. Melanin exerts an antimicrobial activity against bacteria, fungi, and parasites. We demonstrated an antifungal activity of synthetic and human melanin against Candida sp. The members of the Cryptococcus neoformans and C. gattii species complexes are capsulated yeasts, which cause cryptococcosis. For both species melanin is an...

  1. Synthetic arylquinuclidine derivatives exhibit antifungal activity against Candida albicans, Candida tropicalis and Candida parapsilopsis

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    Gilbert Ian

    2011-01-01

    Full Text Available Abstract Background Sterol biosynthesis is an essential pathway for fungal survival, and is the biochemical target of many antifungal agents. The antifungal drugs most widely used to treated fungal infections are compounds that inhibit cytochrome P450-dependent C14α-demethylase (CYP51, but other enzymes of this pathway, such as squalene synthase (SQS which catalyses the first committed step in sterol biosynthesis, could be viable targets. The aim of this study was to evaluate the antifungal activity of SQS inhibitors on Candida albicans, Candida tropicalis and Candida parapsilopsis strains. Methods Ten arylquinuclidines that act as SQS inhibitors were tested as antiproliferative agents against three ATCC strains and 54 clinical isolates of Candida albicans, Candida tropicalis and Candida parapsilopsis. Also, the morphological alterations induced in the yeasts by the experimental compounds were evaluated by fluorescence and transmission electron microscopy. Results The most potent arylquinuclidine derivative (3-[1'-{4'-(benzyloxy-phenyl}]-quinuclidine-2-ene (WSP1267 had a MIC50 of 2 μg/ml for all species tested and MIC90 varying from 4 μg/ml to 8 μg/ml. Ultrathin sections of C. albicans treated with 1 μg/ml of WSP1267 showed several ultrastructural alterations, including (a loss of cell wall integrity, (b detachment of the plasma membrane from the fungal cell wall, (c accumulation of small vesicles in the periplasmic region, (d presence of large electron-dense vacuoles and (e significantly increased cell size and cell wall thickness. In addition, fluorescence microscopy of cells labelled with Nile Red showed an accumulation of lipid droplets in the cytoplasm of treated yeasts. Nuclear staining with DAPI revealed the appearance of uncommon yeast buds without a nucleus or with two nuclei. Conclusion Taken together, our data demonstrate that arylquinuclidine derivatives could be useful as lead compounds for the rational synthesis of new

  2. A new manganese-based oral contrast agent (CMC-001) for liver MRI. Pharmacological and pharmaceutical aspects

    International Nuclear Information System (INIS)

    Joergensen, Jan Troest; Rief, Matthias; Wagner, Moritz; Brismar, Torkel B.; Albiin, Nils

    2012-01-01

    Manganese is one of the most abundant metals on earth and is found as a component of more than 100 different minerals. Besides being an essential trace element in relation to the metabolic processes in the body, manganese is also a paramagnetic metal that possesses similar characteristics to gadolinium with regards to T1-weighted (T1-w) magnetic resonance imaging (MRI). Manganese, in the form of manganese (II) chloride tetrahydrate, is the active substance in a new targeted oral contrast agent, currently known as CMC-001, indicated for hepatobiliary MRI. Under physiological circumstances manganese is poorly absorbed from the intestine after oral intake, but by the use of specific absorption promoters, L-alanine and vitamin D3, it is possible to obtain a sufficiently high concentration in the liver in order to achieve a significant signal enhancing effect. In the liver manganese is exposed to a very high first-pass effect, up to 98 %, which prevents the metal from reaching the systemic circulation, thereby reducing the number of systemic side-effects. Manganese is one of the least toxic trace elements, and due to its favorable safety profile it may be an attractive alternative to gadolinium-based contrast agents for patients undergoing an MRI evaluation for liver metastases in the future. In this review the basic pharmacological and pharmaceutical aspects of this new targeted oral hepatobiliary specific contrast agent will be discussed

  3. Antifungal activity of Brazilian medicinal plants involved in popular treatment of mycoses.

    Science.gov (United States)

    Cruz, M C S; Santos, P O; Barbosa, A M; de Mélo, D L F M; Alviano, C S; Antoniolli, A R; Alviano, D S; Trindade, R C

    2007-05-04

    A survey of medicinal plants used to treat common mycoses was done in the Curituba district, Sergipe State, Brazil. One hundred inhabitants were interviewed by health agents and traditional healers. Four different plants were the most cited (more than 50% of the citations): Ziziphus joazeiro, Caesalpinia pyramidalis, Bumelia sartorum and Hymenea courbaril. The aqueous extracts obtained following traditional methods and using different parts of these plants, were submitted to drop agar diffusion tests for primary antimicrobial screening. Only the water infusion extract of Ziziphus joazeiro and Caesalpinea pyramidalis presented a significant antifungal activity against Trichophyton rubrum, Candida guilliermondii, Candida albicans, Cryptococcus neoformans and Fonsecaea pedrosoi, when compared to the antifungal agent amphotericin B. The minimal inhibitory concentration (MIC) of the bioactive extracts was evaluated by the microdilution method. Best activity with a MIC of 6.5 microg/ml for both extracts was observed against Trichophyton rubrum and Candida guilliermondii. Ziziphus joazeiro and Caesalpinea pyramidalis extracts presented also low acute toxicity in murine models. The present study validates the folk use of these plant extracts and indicates that they can be effective potential candidates for the development of new strategies to treat fungal infections.

  4. Quantitative and qualitative analysis of the antifungal activity of allicin alone and in combination with antifungal drugs.

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    Young-Sun Kim

    Full Text Available The antifungal activity of allicin and its synergistic effects with the antifungal agents flucytosine and amphotericin B (AmB were investigated in Candida albicans (C. albicans. C. albicans was treated with different conditions of compounds alone and in combination (allicin, AmB, flucytosine, allicin + AmB, allicin + flucytosine, allicin + AmB + flucytosine. After a 24-hour treatment, cells were examined by scanning electron microscopy (SEM and atomic force microscopy (AFM to measure morphological and biophysical properties associated with cell death. The clearing assay was conducted to confirm the effects of allicin. The viability of C. albicans treated by allicin alone or with one antifungal drug (AmB, flucytosine in addition was more than 40% after a 24-hr treatment, but the viability of groups treated with combinations of more than two drugs was less than 32%. When the cells were treated with allicin alone or one type of drug, the morphology of the cells did not change noticeably, but when cells were treated with combinations of drugs, there were noticeable morphological changes. In particular, cells treated with allicin + AmB had significant membrane damage (burst or collapsed membranes. Classification of cells according to their cell death phase (CDP allowed us to determine the relationship between cell viability and treatment conditions in detail. The adhesive force was decreased by the treatment in all groups compare to the control. Cells treated with AmB + allicin had a greater adhesive force than cells treated with AmB alone because of the secretion of molecules due to collapsed membranes. All cells treated with allicin or drugs were softer than the control cells. These results suggest that allicin can reduce MIC of AmB while keeping the same efficacy.

  5. Essential Oils of Myrtaceae Species Growing Wild in Tunisia: Chemical Variability and Antifungal Activity Against Biscogniauxia mediterranea, the Causative Agent of Charcoal Canker.

    Science.gov (United States)

    Yangui, Islem; Zouaoui Boutiti, Meriem; Boussaid, Mohamed; Messaoud, Chokri

    2017-07-01

    The chemical composition of five Eucalyptus species and five Myrtus communis L. populations was investigated using GC/MS and GC-FID. For Eucalyptus essential oils, 32 compounds, representing 88.56 - 96.83% of the total oil according to species, were identified. The main compounds were 1,8-cineole, α-pinene, p-cymene, γ-gurjunene, α-aromadendrene, and β-phellandrene. For Myrtle essential oils, 26 compounds, representing 93.13 - 98.91% of the total oil were identified. α-Pinene, 1,8-cineole, linalool, and myrtenyl acetate were found to be the major compounds. Principal component analysis (PCA) showed chemical differentiation between Eucalyptus species and between Myrtle populations. Biscogniauxia mediterranea, the causative agent of charcoal canker, was identified according to its morphological and molecular characteristics. Essential oils of the investigated Eucalyptus species and Myrtle populations were tested for their antifungal capacity against this fungus. The antifungal activity varied according to the essential oil composition. Biscogniauxia mediterranea exhibited powerful resistance to some essential oils including them of Eucalyptus lehmannii and Eucalyptus sideroxylon but it was very sensitive to Eucalyptus camaldulensis oil (IC 50  = 3.83 mg/ml) and M. communis oil from Zaghouan (IC 50  = 1 mg/ml). This sensitivity was found to be correlated to some essential oil compounds such as p-cymene, carvacrol, cuminaldehyde, and linalool. © 2017 Wiley-VHCA AG, Zurich, Switzerland.

  6. Pathogenesis and host defence against Mucorales: the role of cytokines and interaction with antifungal drugs.

    Science.gov (United States)

    Roilides, Emmanuel; Antachopoulos, Charalampos; Simitsopoulou, Maria

    2014-12-01

    Innate immune response, including macrophages, neutrophils and dendritic cells and their respective receptors, plays an important role in host defences against Mucorales with differential activity against specific fungal species, while adaptive immunity is not the first line of defence. A number of endogenous and exogenous factors, such as cytokines and growth factors as well as certain antifungal agents have been found that they influence innate immune response to these organisms. Used alone or especially in combination have been shown to exert antifungal effects against Mucorales species. These findings suggest novel ways of adjunctive therapy for patients with invasive mucormycosis. © 2014 Blackwell Verlag GmbH.

  7. Fluconazole for empiric antifungal therapy in cancer patients with fever and neutropenia

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    Peterson Josh F

    2006-12-01

    Full Text Available Abstract Background Several clinical trials have demonstrated the efficacy of fluconazole as empiric antifungal therapy in cancer patients with fever and neutropenia. Our objective was to assess the frequency and resource utilization associated with treatment failure in cancer patients given empiric fluconazole antifungal therapy in routine inpatient care. Methods We performed a retrospective cohort study of cancer patients treated with oral or intravenous fluconazole between 7/97 and 6/01 in a tertiary care hospital. The final study cohort included cancer patients with neutropenia (an absolute neutrophil count below 500 cells/mm3 and fever (a temperature above 38°C or 100.4°F, who were receiving at least 96 hours of parenteral antibacterial therapy prior to initiating fluconazole. Patients' responses to empiric therapy were assessed by reviewing patient charts. Results Among 103 cancer admissions with fever and neutropenia, treatment failure after initiating empiric fluconazole antifungal therapy occurred in 41% (95% confidence interval (CI 31% – 50% of admissions. Patients with a diagnosis of hematological malignancy had increased risk of treatment failure (OR = 4.6, 95% CI 1.5 – 14.8. When treatment failure occurred the mean adjusted increases in length of stay and total costs were 7.4 days (95% CI 3.3 – 11.5 and $18,925 (95% CI 3,289 – 34,563, respectively. Conclusion Treatment failure occurred in more than one-third of neutropenic cancer patients on fluconazole as empiric antifungal treatment for fever in routine clinical treatment. The increase in costs when treatment failure occurs is substantial.

  8. Effect of Oral Voriconazole on Fungal Keratitis in the Mycotic Ulcer Treatment Trial II (MUTT II): A Randomized Clinical Trial.

    Science.gov (United States)

    Prajna, N Venkatesh; Krishnan, Tiruvengada; Rajaraman, Revathi; Patel, Sushila; Srinivasan, Muthiah; Das, Manoranjan; Ray, Kathryn J; O'Brien, Kieran S; Oldenburg, Catherine E; McLeod, Stephen D; Zegans, Michael E; Porco, Travis C; Acharya, Nisha R; Lietman, Thomas M; Rose-Nussbaumer, Jennifer

    2016-12-01

    suggestion that Fusarium species might have a decreased rate of perforation or TPK in the oral voriconazole-treated arm; however, this was not a statistically significant finding after Holms-Šidák correction for multiple comparisons (effect coefficient, 0.49; 95% CI, 0.26-0.92; P = .03). Patients receiving oral voriconazole experienced a total of 58 adverse events (48.7%) compared with 28 adverse events (23.1%) in the placebo group (P < .001 after Holms-Šidák correction for multiple comparisons). There appears to be no benefit to adding oral voriconazole to topical antifungal agents in the treatment of severe filamentous fungal ulcers. All patients in this study were enrolled in India and Nepal; therefore, it is possible that organisms in this region may exhibit characteristics different from those in other regions of the world. clinicaltrials.gov Identifier: NCT00996736.

  9. Evaluation of Etest and macrodilution broth method for antifungal susceptibility testing of Candida sp strains isolated from oral cavities of AIDS patients

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    SILVA Maria do Rosário R.

    2002-01-01

    Full Text Available A comparison of the Etest and the reference broth macrodilution susceptibility test for fluconazole, ketoconazole, itraconazole and amphotericin B was performed with 59 of Candida species isolated from the oral cavities of AIDS patients. The Etest method was performed according to the manufacturer's instructions, and the reference method was performed according to National Committee for Clinical Laboratory Standards document M27-A guidelines. Our data showed that there was a good correlation between the MICs obtained by the Etest and broth dilution methods. When only the MIC results at ± 2 dilutions for both methods were considered, the agreement rates were 90.4% for itraconazole, ketoconazole and amphotericin B and 84.6% for fluconazole of the C. albicans tested. In contrast, to the reference method, the Etest method classified as susceptible three fluconazole-resistant isolates and one itraconazole-resistant isolate, representing four very major errors. These results indicate that Etest could be considered useful for antifungal sensitivity evaluation of yeasts in clinical laboratories.

  10. Perception of iron deficiency from oral mucosa alterations that show a high prevalence of Candida infection

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    Shin-Yu Lu

    2016-08-01

    Conclusion: The study demonstrates that oral mucosa alterations accompanying oral candidosis are a sensitive indicator of ID. All oral changes can be successfully ameliorated by iron therapy plus antifungals when candidosis exists. Investigating the origin of IDA is necessary, because it may be the first sign of a more serious disease, particularly malignancy.

  11. Treatment and Prevention of Oral Candidiasis in Elderly Patients.

    Science.gov (United States)

    Sakaguchi, Hideo

    2017-01-01

    The incidence of oral candidiasis has increased in the elderly in recent years. Although the increase of the elderly population plays a big role in this rise of oral candidiasis, the broader recognition that elderly people have higher infection rates for oral candidiasis is considered to be also an important factor. Oral candidiasis can be categorized into three types. Pseudomembranous oral candidiasis is characterized by the appearance of white moss, erythematous oral candidiasis by the eruption of erythema, and hyperplastic oral candidiasis by mucosal hyperplasia. Miconazole has been commonly used when treating oral candidiasis. Elderly patients, however, have a tendency to develop oral candidiasis repeatedly. It is therefore critical to take measures to prevent recurrence. We recommend the use an oral moisturizer containing hinokitiol, an antifungal substance, on a regular basis, to help prevent recurrence of oral candidiasis.

  12. Oral rinse as a potential method to culture Candida isolate from AIDS patients

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    Desiana Radithia

    2011-12-01

    Full Text Available Background: Candida isolate is easily sampled from oral cavity by swabbing directly on the candidiasis lesion, to be smeared onto slides for direct examination or cultured in a growth medium. This method is by far the gold standard for defining candidiasis diagnosis. However it is difficult to apply on sensitive patients and almost impossible on patients showing no clinical appearance of oral candidiasis. AIDS patients are very prone to candida infection and have a tendency of repetitive infection involving mixed species. As many candida species show different susceptibility to anti-fungal agents, it is necessary to identify the species causing the infection in the management of oral candidiasis. Oral rinse is a suggested method to obtain candida isolate to be cultured for further analysis such as species identification. This method is simple and less risky on infection transmission as less tools are required in the procedure. Purpose: This study aimed to assess the application of oral rinse as an alternative method to culture Candida isolate from AIDS patients. Methods: A cross-sectional observative study was conducted in HIV/AIDS in-Patient Facility of Intermediate Care Unit for Infection Disease, Dr. Soetomo Hospital Surabaya. Fourteen stadium 4 AIDS patients matching criteria were swabbed on 1/3-posterior of the tongue, and then given 10 ml phosphate buffer saline to rinse vigorously for 15 seconds. Both specimens were cultured on Sabouraud’s dextrose agar and colony growth was observed. Results: Candida colonies were able to grow from all 14 isolates (100% by both methods. Qualitatively, cultures from oral rinse specimens were more populated than cultures from swab specimens. Conclusion: Oral rinse is an applicable technique to obtain Candida species isolate. This technique is safe, easy, non-invasive, and needs less tools therefore less risky for HIV transmission.Latar belakang: Isolat Candida mudah diambil dengan cara mengusap lesi

  13. New Polyurethane Nail Lacquers for the Delivery of Terbinafine: Formulation and Antifungal Activity Evaluation.

    Science.gov (United States)

    Gregorí Valdes, Barbara S; Serro, Ana Paula; Gordo, Paulo M; Silva, Alexandra; Gonçalves, Lídia; Salgado, Ana; Marto, Joana; Baltazar, Diogo; Dos Santos, Rui Galhano; Bordado, João Moura; Ribeiro, Helena Margarida

    2017-06-01

    Onychomycosis is a fungal nail infection. The development of new topical antifungal agents for the treatment of onychomycosis has focused on formulation enhancements that optimize the pharmacological characteristics required for its effective treatment. Polyurethanes (PUs) have never been used in therapeutic nail lacquers. The aim of this work has been the development of new PU-based nail lacquers with antifungal activity containing 1.0% (wt/wt) of terbinafine hydrochloride. The biocompatibility, wettability, and the prediction of the free volume in the polymeric matrix were assessed using a human keratinocytes cell line, contact angle, and Positron Annihilation Lifetime Spectroscopy determinations, respectively. The morphology of the films obtained was confirmed by scanning electron microscopy, while the nail lacquers' bioadhesion to nails was determined by mechanical tests. Viscosity, in vitro release profiles, and antifungal activity were also assessed. This study demonstrated that PU-terbinafine-based nail lacquers have good keratinocyte compatibility, good wettability properties, and adequate free volume. They formed a homogenous film after application, with suitable adhesion to the nail plate. Furthermore, the antifungal test results demonstrated that the terbinafine released from the nail lacquer Formulation A PU 19 showed activity against dermatophytes, namely Trichophyton rubrum. Copyright © 2017 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.

  14. Synthesis and characterization of anti-bacterial and anti-fungal citrate-based mussel-inspired bioadhesives

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    Guo, Jinshan; Wang, Wei; Hu, Jianqing; Xie, Denghui; Gerhard, Ethan; Nisic, Merisa; Shan, Dingying; Qian, Guoying; Zheng, Siyang; Yang, Jian

    2016-01-01

    Bacterial and fungal infections in the use of surgical devices and medical implants remain a major concern. Traditional bioadhesives fail to incorporate anti-microbial properties, necessitating additional anti-microbial drug injection. Herein, by the introduction of the clinically used and inexpensive anti-fungal agent, 10-undecylenic acid (UA), into our recently developed injectable citrate-based mussel-inspired bioadhesives (iCMBAs), a new family of anti-bacterial and anti-fungal iCMBAs (AbAf iCs) was developed. AbAf iCs not only showed strong wet tissue adhesion strength, but also exhibited excellent in vitro cyto-compatibility, fast degradation, and strong initial and considerable long-term anti-bacterial and anti-fungal ability. For the first time, the biocompatibility and anti-microbial ability of sodium metaperiodate (PI), an oxidant used as a cross-linking initiator in the AbAf iCs system, was also thoroughly investigated. Our results suggest that the PI-based bioadhesives showed better anti-microbial properties compared to the unstable silver-based bioadhesive materials. In conclusion, AbAf iCs family can serve as excellent anti-bacterial and anti-fungal bioadhesive candidates for tissue/wound closure, wound dressing, and bone regeneration, especially when bacterial or fungal infections are a major concern. PMID:26874283

  15. Diversities in virulence, antifungal activity, pigmentation and DNA fingerprint among strains of Burkholderia glumae.

    Science.gov (United States)

    Karki, Hari S; Shrestha, Bishnu K; Han, Jae Woo; Groth, Donald E; Barphagha, Inderjit K; Rush, Milton C; Melanson, Rebecca A; Kim, Beom Seok; Ham, Jong Hyun

    2012-01-01

    Burkholderia glumae is the primary causal agent of bacterial panicle blight of rice. In this study, 11 naturally avirulent and nine virulent strains of B. glumae native to the southern United States were characterized in terms of virulence in rice and onion, toxofalvin production, antifungal activity, pigmentation and genomic structure. Virulence of B. glumae strains on rice panicles was highly correlated to virulence on onion bulb scales, suggesting that onion bulb can be a convenient alternative host system to efficiently determine the virulence of B. glumae strains. Production of toxoflavin, the phytotoxin that functions as a major virulence factor, was closely associated with the virulence phenotypes of B. glumae strains in rice. Some strains of B. glumae showed various levels of antifungal activity against Rhizoctonia solani, the causal agent of sheath blight, and pigmentation phenotypes on casamino acid-peptone-glucose (CPG) agar plates regardless of their virulence traits. Purple and yellow-green pigments were partially purified from a pigmenting strain of B. glumae, 411gr-6, and the purple pigment fraction showed a strong antifungal activity against Collectotrichum orbiculare. Genetic variations were detected among the B. glumae strains from DNA fingerprinting analyses by repetitive element sequence-based PCR (rep-PCR) for BOX-A1R-based repetitive extragenic palindromic (BOX) or enterobacterial repetitive intergenic consensus (ERIC) sequences of bacteria; and close genetic relatedness among virulent but pigment-deficient strains were revealed by clustering analyses of DNA fingerprints from BOX-and ERIC-PCR.

  16. Antimicrobial efficacy of oral topical agents on microorganisms associated with radiated head and neck cancer patients: an in vitro study.

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    Bidra, Avinash S; Tarrand, Jeffery J; Roberts, Dianna B; Rolston, Kenneth V; Chambers, Mark S

    2011-04-01

    A variety of oral topical agents have been used for prevention and management of radiotherapy-induced adverse effects. The antimicrobial nature of some of the commonly used agents is unknown. The purpose of this study was to evaluate antimicrobial efficacies of various oral topical agents on common microorganisms associated with radiated head and neck cancer patients. Seven commonly used topical oral agents-0.12% chlorhexidine with alcohol, 0.12% chlorhexidine without alcohol, baking soda-salt rinse, 0.4% stannous fluoride gel, 0.63% stannous fluoride rinse, calcium phosphate mouthrinse, and acemannan hydrogel (aloe vera) rinse-were evaluated in vitro for their antimicrobial efficacies against four common microorganisms. A combination of baking soda-salt rinse and 0.4% stannous fluoride gel was evaluated as the eighth agent. The microorganisms used were Staphylococcus aureus, group B Streptococcus, Escherichia coli, and Candida albicans. An ELISA reader was used to measure the turbidity of microbial culture wells and optical density (OD) values for each of the 960 wells recorded. Mean OD values were rank ordered based on their turbidity. One-way ANOVA with Tukey HSD post hoc analysis was used to study differences in OD values (P baking soda- salt, calcium phosphate rinse, and the combination of baking soda-salt and stannous fluoride gel. Mean OD values classified for microorganisms from lowest to highest were Escherichia coli, Staphylococcus aureus, group B Streptococcus, and Candida albicans. A significant difference among the antimicrobial efficacies of topical agents was evident for each of four microorganisms (P < .05). There was also a significant difference among the antimicrobial efficacies of the same topical agent on the four microorganisms tested (P < .05).

  17. Evaluation of date syrup as an oral negative contrast agent for MRCP.

    Science.gov (United States)

    Govindarajan, Arunkumar; Lakshmanan, Prakash Manikka; Sarawagi, Radha; Prabhakaran, Velu

    2014-11-01

    The purpose of this study was to compare the in vitro effects of date syrup with those of other contrast agents by qualitative and quantitative analysis and in vivo evaluation of the use of date syrup to improve the quality of MRCP images. Phantoms containing date syrup, ferumoxsil, pineapple juice, and water were imaged by 1.5-T MRI with T2-weighted and MRCP sequences, and signal-to-noise ratios were calculated. Biochemical analysis of date syrup was performed to find the nature of iron in it, and the iron content was quantified by energy-dispersive x-ray spectroscopy. Sixty patients underwent MRCP before and 30 minutes after ingestion of 100 mL of date syrup. Unenhanced and contrast-enhanced images were scored for gastrointestinal tract signal suppression and visualization of various pancreaticobiliary structures. In vitro evaluation showed that images obtained with date syrup had a signal-to-noise ratio comparable to that of images obtained with ferumoxsil in T2-weighted and MRCP sequences. The iron concentration in date syrup was 2.6 mg/dL, and it was in ferric form. Images obtained after oral contrast administration had statistically significant improvement in gastrointestinal tract signal suppression (p Date syrup can be used as a negative oral contrast agent for gastrointestinal tract signal suppression during MRCP and for improving visualization of various pancreaticobiliary structures.

  18. Antifungal activity and mechanism of action of monoterpenes against dermatophytes and yeasts

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    Diogo Miron

    Full Text Available Dermatomycosis causes highly frequent dermal lesions, and volatile oils have been proven to be promising as antifungal agents. The antifungal activity of geraniol, nerol, citral, neral and geranial (monoterpenes, and terbinafine and anidulafungin (control drugs against seven opportunistic pathogenic yeasts and four dermatophyte species was evaluated by the Clinical and Laboratory Standards Institute microdilution tests. Monoterpenes were more active against dermatophytes than yeasts (geometric mean of minimal inhibitory concentration (GMIC of 34.5 and 100.4 µg.ml-1, respectively. Trichophyton rubrum was the fungal species most sensitive to monoterpenes (GMIC of 22.9 µg.ml-1. The trans isomers showed higher antifungal activity than the cis. The mechanism of action was investigated evaluating damage in the fungal cell wall (Sorbitol Protection Assay and in the cell membrane (Ergosterol Affinity Assay. No changes were observed in the MIC of monoterpenes in the sorbitol protection assay.The MIC of citral and geraniol was increased from 32 to 160 µg.ml-1 when the exogenous ergosterol concentrations was zero and 250 µg.ml-1, respectively. The monoterpenes showed an affinity for ergosterol relating their mechanism of action to cell membrane destabilization.

  19. The impact of oral herpes simplex virus infection and candidiasis on chemotherapy-induced oral mucositis among patients with hematological malignancies.

    Science.gov (United States)

    Chen, Y-K; Hou, H-A; Chow, J-M; Chen, Y-C; Hsueh, P-R; Tien, H-F

    2011-06-01

    The aim of this study was to evaluate the influences of oral candidiasis and herpes simplex virus 1 (HSV-1) infections in chemotherapy-induced oral mucositis (OM). The medical records of 424 consecutive patients with hematological malignancies who had received chemotherapy at a medical center in Taiwan from January 2006 to November 2007 were retrospectively reviewed. The results of swab cultures of fungus and HSV-1 for OM were correlated with associated clinical features. Younger age, myeloid malignancies, and disease status other than complete remission before chemotherapy were significantly correlated with the development of OM. Risks of fever (p < 0.001) and bacteremia were higher in patients with OM. Among 467 episodes of OM with both swab cultures available, 221 were non-infection (47.3%) and 246 were related to either fungal infections, HSV-1 infections, or both (52.7%); of the 246 episodes, 102 were associated with fungal infections alone (21.8%), 98 with HSV-1 infections alone (21%), and 46 with both infections (9.9%). Patients who had received antifungal agents prior to OM occurrence tended to have HSV-1 infection (p < 0.001). Our results suggest that Candida albicans and HSV-1 play an important role in chemotherapy-induced OM in patients with hematological malignancies.

  20. An Antifungal Combination Matrix Identifies a Rich Pool of Adjuvant Molecules that Enhance Drug Activity against Diverse Fungal Pathogens

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    Nicole Robbins

    2015-11-01

    Full Text Available There is an urgent need to identify new treatments for fungal infections. By combining sub-lethal concentrations of the known antifungals fluconazole, caspofungin, amphotericin B, terbinafine, benomyl, and cyprodinil with ∼3,600 compounds in diverse fungal species, we generated a deep reservoir of chemical-chemical interactions termed the Antifungal Combinations Matrix (ACM. Follow-up susceptibility testing against a fluconazole-resistant isolate of C. albicans unveiled ACM combinations capable of potentiating fluconazole in this clinical strain. We used chemical genetics to elucidate the mode of action of the antimycobacterial drug clofazimine, a compound with unreported antifungal activity that synergized with several antifungals. Clofazimine induces a cell membrane stress for which the Pkc1 signaling pathway is required for tolerance. Additional tests against additional fungal pathogens, including Aspergillus fumigatus, highlighted that clofazimine exhibits efficacy as a combination agent against multiple fungi. Thus, the ACM is a rich reservoir of chemical combinations with therapeutic potential against diverse fungal pathogens.

  1. Mechanisms of antifungal and anti-aflatoxigenic properties of essential oil derived from turmeric (Curcuma longa L.) on Aspergillus flavus.

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    Hu, Yichen; Zhang, Jinming; Kong, Weijun; Zhao, Gang; Yang, Meihua

    2017-04-01

    The antifungal activity and potential mechanisms in vitro as well as anti-aflatoxigenic efficiency in vivo of natural essential oil (EO) derived from turmeric (Curcuma longa L.) against Aspergillus flavus was intensively investigated. Based on the previous chemical characterization of turmeric EO by gas chromatography-mass spectrometry, the substantially antifungal activities of turmeric EO on the mycelial growth, spore germination and aflatoxin production were observed in a dose-dependent manner. Furthermore, these antifungal effects were related to the disruption of fungal cell endomembrane system including the plasma membrane and mitochondria, specifically i.e. the inhibition of ergosterol synthesis, mitochondrial ATPase, malate dehydrogenase, and succinate dehydrogenase activities. Moreover, the down-regulation profiles of turmeric EO on the relative expression of mycotoxin genes in aflatoxin biosynthetic pathway revealed its anti-aflatoxigenic mechanism. Finally, the suppression effect of fungal contamination in maize indicated that turmeric EO has potential as an eco-friendly antifungal agent. Copyright © 2016 Elsevier Ltd. All rights reserved.

  2. Antifungal activity of salaceyin A against Colletotrichum orbiculare and Phytophthora capsici.

    Science.gov (United States)

    Park, C N; Lee, D; Kim, W; Hong, Y; Ahn, J S; Kim, B S

    2007-08-01

    The antifungal activities of novel salicylic acid derivatives, salaceyin A, 6-(9-methyldecyl) salicylic acid, and salaceyin B, 6-(9-methylundecyl) salicylic acid were evaluated against plant pathogenic fungi. Salaceyin A showed antifungal activity against Cladosporium cucumerinum, Colletotrichum orbiculare and Phytophthora capsici at 64 microg ml(-1) while salaceyin B was less effective. In vitro antifungal activities of the compounds were influenced by the experimental pH value of the MIC test medium wherein their antifungal activities were enhanced by increasingly acidic conditions. Salaceyin A showed potent in vivo control efficacy against Phytophthora blight in pepper plants. The disease was effectively suppressed at 500 microg ml(-1), which was comparable to the commercial fungicide, metalaxyl. Salaceyin A suppressed anthracnose development on cucumber leaves in a concentration dependent manner. The control efficacy of salaceyin A against C. orbiculare infection was similar to chlorothalonil when applied prior to pathogen inoculation. Since the salaceyins are derivatives of salicylic acid, a known important signal molecule critical to plant defenses against pathogen invasion, we investigated the possibility that exogenous application of the salaceyin A would activate a systemic acquired resistance against P. capsici infection and C. orbiculare development on pepper and cucumber plants respectively. The addition of 500 microg ml(-1) of salaceyin A to the plant root systems did not significantly decrease disease development in the hosts. We are led to conclude that the disease control efficacy of salaceyin A against the Phytophthora blight and anthracnose diseases, mainly originates from the direct interaction of the agent with the pathogens.

  3. Candida profiles and antifungal resistance evolution over a decade in Lebanon.

    Science.gov (United States)

    Araj, George Farah; Asmar, Rima George; Avedissian, Aline Zakaria

    2015-09-27

    Infection with and antifungal resistance of Candida species have been on the rise globally. Relevant data on these pathogens are relatively few in our region, including Lebanon, thus warranting this study. This retrospective study of Candida spp. profiles and their in vitro antifungal susceptibility was based on analysis requests for 186 Candida non-albicans and 61 C. albicans during three periods (2005-2007, 2009-2011, and 2012-2014) over the span of the last 10 years at the American University of Beirut Medical Center (AUBMC), a major tertiary care center in Lebanon. Identification of Candida was done using the API 20C AUX system, and the E-test was used to determine the minimum inhibitory concentrations (MICs) of antifungal agents. Among the 1,300-1,500 Candida isolates recovered yearly, C. albicans rates decreased from 86% in 2005 to around 60% in 2014. Simultaneously, the non-albicans rates increased from 14% in 2005 to around 40% in 2014, revealing 11 species, the most frequent of which were C. tropicalis, C. glabrata, and C. parapsilosis. All these demonstrated high resistance (35%-79%) against itraconazole, but remained uniformly susceptible (100%) to amphotericin B. Though C. albicans and the other species maintained high susceptibility against fluconazole and voriconazole, their MIC90 showed an elevated trend over time, and C. glabrata had the highest resistance rates. The observed rise in resistance among Candida spp. in Lebanon mandates the need for close surveillance and monitoring of antifungal drug resistance for both epidemiologic and treatment purposes.

  4. Chemical Composition and Antifungal Activity of Ocimum basilicum L. Essential Oil

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    Neveen Helmy Abou El-Soud

    2015-07-01

    Full Text Available BACKGROUND: The leaves of Ocimum basilicum L. (basil are used in traditional cuisine as spices; its essential oil has found a wide application in perfumery, dental products as well as antifungal agents. AIM: To assess the chemical composition as well as the in vitro antifungal activity of O. basilicum L. essential oil against Aspergillus flavus fungal growth and aflatoxin B1 production. MATERIAL AND METHODS: The essential oil of O. basilicum was obtained by hydrodistillation and analysed using gas chromatography (GC and GC coupled with mass spectrometry (GC/MS. The essential oil was tested for its effects on Aspergillus flavus (A. flavus mycelial growth and aflatoxin B1 production in Yeast Extract Sucrose (YES growth media. Aflatoxin B1 production was determined by high performance liquid chromatography (HPLC. RESULTS: Nineteen compounds, representing 96.7% of the total oil were identified. The main components were as follows: linalool (48.4%, 1,8-cineol (12.2%, eugenol (6.6%, methyl cinnamate (6.2%, α-cubebene (5.7%, caryophyllene (2.5%, β-ocimene (2.1% and α-farnesene (2.0%.The tested oil showed significant antifungal activity that was dependent on the used oil concentration. The complete inhibition of A. flavus growth was observed at 1000 ppm oil concentration, while marked inhibition of aflatoxin B1 production was observed at all oil concentrations tested (500, 750 and 1000 ppm. CONCLUSION: These results confirm the antifungal activities of O. basilicum L. oil and its potential use to cure mycotic infections and act as pharmaceutical preservative against A. flavus growth and aflatoxin B1 production.

  5. Antifungal Activity of Oleuropein against Candida albicans—The In Vitro Study

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    Nataša Zorić

    2016-11-01

    Full Text Available In the present study we investigated activity of oleuropein, a complex phenol present in large quantities in olive tree products, against opportunistic fungal pathogen Candida albicans. Oleuropein was found to have in vitro antifungal activity with a minimal inhibitory concentration (MIC value of 12.5 mg·mL−1. Morphological changes in the nuclei after staining with fluorescent DNA-binding dyes revealed that apoptosis was a primary mode of cell death in the analyzed samples treated with subinhibitory concentrations of oleuropein. Our results suggest that this antifungal agent targets virulence factors essential for establishment of the fungal infection. We noticed that oleuropein modulates morphogenetic conversion and inhibits filamentation of C. albicans. The hydrophobicity assay showed that oleuropein in sub-MIC values has significantly decreased, in both aerobic and anaerobic conditions, the cellular surface hydrophobicity (CSH of C. albicans, a factor associated with adhesion to epithelial cells. It was also demonstrated that the tested compound inhibits the activity of SAPs, cellular enzymes secreted by C. albicans, which are reported to be related to the pathogenicity of the fungi. Additionally, we detected that oleuropein causes a reduction in total sterol content in the membrane of C. albicans cells, which might be involved in the mechanism of its antifungal activity.

  6. Antifungal activity of topical microemulsion containing a thiophene derivative

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    Geovani Pereira Guimarães

    2014-06-01

    Full Text Available Fungal infections have become a major problem of worldwide concern. Yeasts belonging to the Candida genus and the pathogenic fungus Cryptococcus neoformans are responsible for different clinical manifestations, especially in immunocompromised patients. Antifungal therapies are currently based on a few chemotherapeutic agents that have problems related to effectiveness and resistance profiles. Microemulsions are isotropic, thermodynamically stable transparent systems of oil, water and surfactant that can improve the solubilization of lipophilic drugs. Taking into account the need for more effective and less toxic drugs along with the potential of thiophene derivatives as inhibitors of pathogenic fungi growth, this study aimed to evaluate the antifungal activity of a thiophene derivative (5CN05 embedded in a microemulsion (ME. The minimum inhibitory concentration (MIC was determined using the microdilution method using amphotericin B as a control. The formulations tested (ME- blank and ME-5CN05 showed physico-chemical properties that would allow their use by the topical route. 5CN05 as such exhibited moderate or weak antifungal activity against Candida species (MIC = 270-540 µg.mL-1 and good activity against C. neoformans (MIC = 17 µg.mL-1. Candida species were susceptible to ME-5CN05 (70-140 µg.mL-1, but C. neoformans was much more, presenting a MIC value of 2.2 µg.mL-1. The results of this work proved promising for the pharmaceutical industry, because they suggest an alternative therapy against C. neoformans.

  7. The Usage of Oral Anti Hyperglycemic Agent in Gestational Diabetes: Pros and Cons

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    Bram Pradipta

    2014-06-01

    Full Text Available The prevalence of gestational diabetes mellitus (GDM  is increasing as the pregnant population becomes older and more obese. Fifteen percent of GDM patients require medical intervention. Insulin is still the drug of choice because it has not been implicated as a teratogen in human pregnancies.Insulin has its disadvantages such as the need for injections, the risk of hypoglycaemia, excessive weight gain and the costs. The use of oral anti hyperglicemic agent (OAHA, traditionally contraindicated, now can be considered as an alternative for insulin which can be beneficial in developing countries. From four groups of OAHA, sulfonylurea and biguanides can be used during pregnancy. Studies and randomized controlled trial (RCT have been done and most summarized that it does not increase any maternal and perinatal morbidity. Most data also show that thereare also no differences in glycemic control or pregnancy outcomes compared with insulin. There are conflicting data shows metformin increase prevalence of preeclampsia patient and perinatal morbidity. OAHA usage, although not yet recommended internationally, can be considered in GDMpatients with uncontrolled blood sugar levels that require medical intervention but can not use insulin. Wellconducted, prospective, controlled studies regarding itsfeasibility in pregnant women with diabetes are still needed.Keywords:oral antihyperglycemic agent, gestational, diabetes

  8. Evaluating the potential of cubosomal nanoparticles for oral delivery of amphotericin B in treating fungal infection

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    Yang Z

    2014-01-01

    Full Text Available Zhiwen Yang,1,3 Meiwan Chen,2 Muhua Yang,1 Jian Chen,1 Weijun Fang,1 Ping Xu11Department of Pharmacy, Songjiang Hospital Affiliated The First People's Hospital, Shanghai Jiao Tong University, Shanghai, 2State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau, 3Shanghai Songjiang Hospital Affiliated Nanjing Medical University, Nanjing, People's Republic of ChinaAbstract: The oral administration of amphotericin B (AmB has a major drawback of poor bioavailability. The aim of this study was to investigate the potential of glyceryl monoolein (GMO cubosomes as lipid nanocarriers to improve the oral efficacy of AmB. Antifungal efficacy was determined in vivo in rats after oral administration, to investigate its therapeutic use. The human colon adenocarcinoma cell line (Caco-2 was used in vitro to evaluate transport across a model of the intestinal barrier. In vivo antifungal results showed that AmB, loaded in GMO cubosomes, could significantly enhance oral efficacy, compared against Fungizone®, and that during a 2 day course of dosage 10 mg/kg the drug reached effective therapeutic concentrations in renal tissue for treating fungal infections. In the Caco-2 transport studies, GMO cubosomes resulted in a significantly larger amount of AmB being transported into Caco-2 cells, via both clathrin- and caveolae-mediated endocytosis, but not macropinocytosis. These results suggest that GMO cubosomes, as lipid nanovectors, could facilitate the oral delivery of AmB.Keywords: glyceryl monoolein cubosomes, oral delivery, amphotericin B, antifungal activity, absorption mechanism

  9. Licochalcone A induces apoptosis in KB human oral cancer cells via a caspase-dependent FasL signaling pathway.

    Science.gov (United States)

    Kim, Jae-Sung; Park, Mi-Ra; Lee, Sook-Young; Kim, Do Kyoung; Moon, Sung-Min; Kim, Chun Sung; Cho, Seung Sik; Yoon, Goo; Im, Hee-Jeong; You, Jae-Seek; Oh, Ji-Su; Kim, Su-Gwan

    2014-02-01

    Licochalcone A (Lico-A) is a natural phenol licorice compound with multiple bioactivities, including anti-inflammatory, anti-microbial, anti-fungal and osteogenesis-inducing properties. In the present study, we investigated the Lico-A-induced apoptotic effects and examined the associated apoptosis pathway in KB human oral cancer cells. Lico-A decreased the number of viable KB oral cancer cells. However, Lico-A did not have an effect on primary normal human oral keratinocytes. In addition, the IC50 value of Lico-A was determined to be ~50 µM following dose-dependent stimulation. KB oral cancer cells stimulated with Lico-A for 24 h showed chromatin condensation by DAPI staining, genomic DNA fragmentation by agarose gel electrophoresis and a gradually increased apoptotic cell population by FACS analysis. These data suggest that Lico-A induces apoptosis in KB oral cancer cells. Additionally, Lico‑A‑induced apoptosis in KB oral cancer cells was mediated by the expression of factor associated suicide ligand (FasL) and activated caspase-8 and -3 and poly(ADP-ribose) polymerase (PARP). Furthermore, in the KB oral cancer cells co-stimulation with a caspase inhibitor (Z-VAD-fmk) and Lico-A significantly abolished the apoptotic phenomena. Our findings demonstrated that Lico‑A-induced apoptosis in KB oral cancer cells involves the extrinsic apoptotic signaling pathway, which involves a caspase-dependent FasL-mediated death receptor pathway. Our data suggest that Lico-A be developed as a chemotherapeutic agent for the management of oral cancer.

  10. Terbinafine in combination with other antifungal agents for treatment of resistant or refractory mycoses: investigating optimal dosing regimens using a physiologically based pharmacokinetic model.

    Science.gov (United States)

    Dolton, Michael J; Perera, Vidya; Pont, Lisa G; McLachlan, Andrew J

    2014-01-01

    Terbinafine is increasingly used in combination with other antifungal agents to treat resistant or refractory mycoses due to synergistic in vitro antifungal activity; high doses are commonly used, but limited data are available on systemic exposure, and no assessment of pharmacodynamic target attainment has been made. Using a physiologically based pharmacokinetic (PBPK) model for terbinafine, this study aimed to predict total and unbound terbinafine concentrations in plasma with a range of high-dose regimens and also calculate predicted pharmacodynamic parameters for terbinafine. Predicted terbinafine concentrations accumulated significantly during the first 28 days of treatment; the area under the concentration-time curve (AUC)/MIC ratios and AUC for the free, unbound fraction (fAUC)/MIC ratios increased by 54 to 62% on day 7 of treatment and by 80 to 92% on day 28 compared to day 1, depending on the dose regimen. Of the high-dose regimens investigated, 500 mg of terbinafine taken every 12 h provided the highest systemic exposure; on day 7 of treatment, the predicted AUC, maximum concentration (Cmax), and minimum concentration (Cmin) were approximately 4-fold, 1.9-fold, and 4.4-fold higher than with a standard-dose regimen of 250 mg once daily. Close agreement was seen between the concentrations predicted by the PBPK model and the observed concentrations, indicating good predictive performance. This study provides the first report of predicted terbinafine exposure in plasma with a range of high-dose regimens.

  11. Isothermal microcalorimetry for antifungal susceptibility testing of Mucorales, Fusarium spp., and Scedosporium spp.

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    Furustrand Tafin, Ulrika; Meis, Jacques F; Trampuz, Andrej

    2012-08-01

    We evaluated isothermal microcalorimetry for real-time susceptibility testing of non-Aspergillus molds. MIC and minimal effective concentration (MEC) values of Mucorales (n = 4), Fusarium spp. (n = 4), and Scedosporium spp. (n = 4) were determined by microbroth dilution according to the Clinical Laboratory Standard Institute M38-A2 guidelines. Heat production of molds was measured at 37 °C in Sabouraud dextrose broth inoculated with 2.5 × 10(4) spores/mL in the presence of amphotericin B, voriconazole, posaconazole, caspofungin, and anidulafungin. As determined by microcalorimetry, amphotericin B was the most active agent against Mucorales (MHIC 0.06-0.125 μg/mL) and Fusarium spp. (MHIC 1-4 μg/mL), whereas voriconazole was the most active agent against Scedosporium spp. (MHIC 0.25 to 8 μg/mL). The percentage of agreement (within one 2-fold dilution) between the MHIC and MIC (or MEC) was 67%, 92%, 75%, and 83% for amphotericin B, voriconazole, posaconazole, and caspofungin, respectively. Microcalorimetry provides additional information on timing of antifungal activity, enabling further investigation of drug-mold and drug-drug interaction, and optimization of antifungal treatment. Copyright © 2012 Elsevier Inc. All rights reserved.

  12. Antibacterial, antifungal, and antiviral activities of some flavonoids.

    Science.gov (United States)

    Orhan, Didem Deliorman; Ozçelik, Berrin; Ozgen, Selda; Ergun, Fatma

    2010-08-20

    Antibacterial and antifungal activities of six plant-derived flavonoids representing two different structural groups were evaluated against standard strains of Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis, Klebsiella pneumoniae, Acinetobacter baumannii, Staphylococcus aureus, Enterococcus faecalis, Bacillus subtilis and their drug-resistant isolates, as well as fungi (Candida albicans, C. krusei) using the microdilution broth method. Herpes simplex virus Type-1 and Parainfluenza-3 virus were employed for antiviral assessment of the flavonoids using Madin-Darby bovine kidney and Vero cell lines. Ampicillin, gentamycin, ofloxacin, levofloxacin, fluconazole, ketoconazole, acyclovir, and oseltamivir were used as the control agents. All tested compounds (32-128 microg/ml) showed strong antimicrobial and antifungal activities against isolated strains of P. aeruginosa, A. baumanni, S. aureus, and C. krusei. Rutin, 5,7-dimethoxyflavanone-4'-O-beta-D-glucopyranoside and 5,7,3'-trihydroxy-flavanone-4'-O-beta-D-glucopyranoside (0.2-0.05 microg/ml) were active against PI-3, while 5,7-dimethoxyflavanone-4'-O-[2''-O-(5'''-O-trans-cinnamoyl)-beta-D-apiofuranosyl]-beta-D-glucopyranoside (0.16-0.2 microg/ml) inhibited potently HSV-1. Copyright 2009 Elsevier GmbH. All rights reserved.

  13. In vitro activities of antifungal drugs against environmental Exophiala isolates and review of the literature.

    Science.gov (United States)

    Gülmez, Dolunay; Doğan, Özlem; Boral, Barış; Döğen, Aylin; İlkit, Macit; de Hoog, G Sybren; Arikan-Akdagli, Sevtap

    2018-04-03

    Exophiala is a genus of black fungi isolated worldwide from environmental and clinical specimens. Data on antifungal susceptibility of Exophiala isolates are limited and the methodology on susceptibility testing is not yet standardized. In this study, we investigated in vitro antifungal susceptibilities of environmental Exophiala isolates. A total of 87 Exophiala isolated from dishwashers or railway ties were included. CLSI M38-A2 microdilution method with modifications was used to determine antifungal susceptibility for fluconazole, voriconazole, posaconazole, itraconazole, amphotericin B, and terbinafine. Minimum inhibitory concentration (MIC) values were determined visually at 48h, 72h, and 96h. MIC-0 endpoint (complete inhibition of growth) was used for amphotericin B and azoles, except fluconazole, for which MIC-2 endpoint (~50% inhibition compared to growth control) was used. Both MIC-0 and MIC-1 (~80% inhibition compared to growth control) results were analysed for terbinafine, to enable comparison with previous studies. Fungal growth was sufficient for determination of MICs at 48h for all isolates except two Exophiala dermatitidis strains. At 72h, most active antifungal agents according to GM MIC were voriconazole and terbinafine, followed by posaconazole, itraconazole, and amphotericin B in rank order of decreasing activity. While amphotericin B displayed adequate in vitro activity despite relatively high MICs, fluconazole showed no meaningful antifungal activity against Exophiala. This article is protected by copyright. All rights reserved. This article is protected by copyright. All rights reserved.

  14. In Vitro Activity of E1210, a Novel Antifungal, against Clinically Important Yeasts and Molds▿

    Science.gov (United States)

    Miyazaki, Mamiko; Horii, Takaaki; Hata, Katsura; Watanabe, Nao-aki; Nakamoto, Kazutaka; Tanaka, Keigo; Shirotori, Syuji; Murai, Norio; Inoue, Satoshi; Matsukura, Masayuki; Abe, Shinya; Yoshimatsu, Kentaro; Asada, Makoto

    2011-01-01

    E1210 is a new antifungal compound with a novel mechanism of action and broad spectrum of antifungal activity. We investigated the in vitro antifungal activities of E1210 compared to those of fluconazole, itraconazole, voriconazole, amphotericin B, and micafungin against clinical fungal isolates. E1210 showed potent activities against most Candida spp. (MIC90 of ≤0.008 to 0.06 μg/ml), except for Candida krusei (MICs of 2 to >32 μg/ml). E1210 showed equally potent activities against fluconazole-resistant and fluconazole-susceptible Candida strains. E1210 also had potent activities against various filamentous fungi, including Aspergillus fumigatus (MIC90 of 0.13 μg/ml). E1210 was also active against Fusarium solani and some black molds. Of note, E1210 showed the greatest activities against Pseudallescheria boydii (MICs of 0.03 to 0.13 μg/ml), Scedosporium prolificans (MIC of 0.03 μg/ml), and Paecilomyces lilacinus (MICs of 0.06 μg/ml) among the compounds tested. The antifungal action of E1210 was fungistatic, but E1210 showed no trailing growth of Candida albicans, which has often been observed with fluconazole. In a cytotoxicity assay using human HK-2 cells, E1210 showed toxicity as low as that of fluconazole. Based on these results, E1210 is likely to be a promising antifungal agent for the treatment of invasive fungal infections. PMID:21825291

  15. Tavaborole, a Novel Boron-Containing Small Molecule Pharmaceutical Agent for Topical Treatment of Onychomycosis: I. Reproductive and Developmental Toxicity Studies.

    Science.gov (United States)

    Ciaravino, Vic; Coronado, Dina; Lanphear, Cheryl; Hoberman, Alan; Chanda, Sanjay

    2016-09-01

    Tavaborole is a topical antifungal agent approved by the US Food and Drug Administration for the treatment of toenail onychomycosis. As part of the nonclinical development program, reproductive and developmental toxicity studies were conducted (rat oral fertility and early embryonic development, rat (oral) and rabbit (dermal) embryo-fetal development). There were no effects on fertility or reproductive performance at doses up to 300 mg/kg/d (107 times the maximum recommended human dose [MRHD] based on mean area under the plasma concentration-time curve comparisons). In the rat embryo-fetal development toxicity studies, teratogenicity was not observed at doses up to 100 mg/kg/d (29 times the MRHD). However, several treatment-related skeletal malformations and variations were observed at 300 mg/kg/d (570 times the MRHD). In rabbit embryo-fetal development toxicity studies dosed via oral or dermal administration, the no observable adverse effect level for maternal toxicity and embryo-fetal toxicity was 50 mg/kg/d (16 times the MRHD) and 5% (26 times the MRHD), respectively. © The Author(s) 2016.

  16. Treatment modalities of oral mucositis after radiation of head and neck cancers; Prise en charge des mucites apres radiotherapie des cancers des voies aerodigestives superieures

    Energy Technology Data Exchange (ETDEWEB)

    Lapeyre, M.; Charra-Brunaud, C.; Kaminsky, M.C.; Geoffrois, L.; Dolivet, G.; Pourel, N.; Marchal, C.; Bey, P.; Maire, F.; Simon, M. [Centre Alexis-Vautrin, 54 - Vandoeuvre-les-Nancy (France); Toussaint, B. [Hopital Central, Service de Chirurgie ORL, 54 - Nancy (France)

    2001-11-01

    Acute mucositis is common after radiotherapy for head and neck cancers. During the past 3 decades, there was a gradual evolution in the treatment modalities for locally advanced carcinomas (concomitant radio-chemotherapy, accelerated radiotherapy). These new strategies are accompanied by an increase in early mucosal reactions. At the present time, there is no widely accepted prophylaxis or effective treatment. Many traditional remedies or new agents seem ineffective (Sucralfate, Chlorhexidine, GM-CSF, Silver nitrate, Prostaglandin, anti-oxidants, Benzydamine hydrochloride), while others seem promising (Povidone-iodine, nonabsorbable antibiotic lozenges and anti-fungal, local GM-CSF, Glutamide, Low-energy laser, corticosteroids). Radioprotectors are controversial and should be only used in experimental protocols and not in routine practice. However, some recommendations can be proposed: general prevention and global care before cancer therapy should be systematic (oral hygiene, dental and periodontal treatment, advice to avoid the use of tobacco and alcohol); frequent oral rinsing with a bland mouthwash (Povidone-iodine or others) should be used at the start of treatment because there are significant modifications of the oral microflora increased by a disturbed salivary flow; these mouthwashes could be associated with nonabsorbable antibiotic lozenges or anti-fungal topical (bicarbonates, Amphotericine B); Systematic percutaneous fluoroscopic gastrostomy should be decided before any aggressive treatments (concomitant radio-chemotherapy, accelerated radiotherapy); pain should be controlled; finally, the radiation technique should be optimized (mucosal sparing block, conformal radiotherapy and intensity modulated radiation therapy). (authors)

  17. Review of flavonoids: A diverse group of natural compounds with anti-Candida albicans activity in vitro.

    Science.gov (United States)

    Seleem, Dalia; Pardi, Vanessa; Murata, Ramiro Mendonça

    2017-04-01

    Flavonoids are a subdivision of polyphenols, a versatile class of natural compounds that represent secondary metabolites from higher plants and are abundant in human diet. Various protective effects of flavonoids have been reported, including antimicrobial and antifungal activities. Due to the nature of oral candidiasis and the increased use of antifungal agents, several drug-resistant strains have emerged making it impractical to rely on one standard therapeutic regime. The aim of this review is to summarize the antifungal activity of some examples of the major subclasses of flavonoids in pure extract forms against C. albicans in vitro, as reported in literature over the past 10 years (2004-2015). In addition, this review outlines the potential mechanism of actions of flavonoids studied in vitro, which may contribute to a better understanding of flavonoids as multi-targets agents in the treatment and/or prevention of oral candidiasis in clinical settings. Copyright © 2016. Published by Elsevier Ltd.

  18. In vitro and in vivo antifungal efficacy of plant based lawsone against Fusarium oxysporum species complex.

    Science.gov (United States)

    Dananjaya, S H S; Udayangani, R M C; Shin, Sang Yeop; Edussuriya, M; Nikapitiya, Chamilani; Lee, Jehee; De Zoysa, Mahanama

    2017-08-01

    Fusarium oxysporum is an ascomycete facultative fungus which generally affects to plants. However, it is recently known as a serious emerging opportunistic pathogen of human and other animals. F. oxysporum shows broad resistance to commonly used antifungal agents and therefore development of alternative therapeutic agents is required. In this study, we investigated the antifungal efficacy of plant based natural lawsone against pathogenic F. oxysporum. Antifungal susceptibility test determined the concentration dependent growth inhibition of lawsone against F. oxysporum with minimum inhibitory concentration (MIC) at 100μg/mL. Ultra-structural analysis indicates the prominent damage on cell wall of the mycelium after lawsone treatment, and suggests that it could increase the membrane permeability and disintegration of cells leading to cellular death. Propidium iodide (PI) uptake assay results showed the higher level of cell death in lawsone treated F. oxysporum which further confirms the loss of plasma membrane integrity. Also, detection of reactive oxygen species (ROS) using DCFH-DA has clearly indicated that lawsone (100μg/mL) can induce the ROS level in the filaments of F. oxysporum. MTT assay results showed the loss of viability and germination capacity of F. oxysporum spores by lawsone in concentration dependent manner. Moreover, lawsone treatment induced the mRNA expression of two autophagy related genes (ATG1 and ATG8) indicating that lawsone may activate the autophagy related pathways in F. oxysporum due to the oxidative stress generated by ROS. F. oxysporum infected zebrafish has recovered after lawsone therapy as a topical treatment suggesting that lawsone is a potential natural antifusariosis agent. Copyright © 2017 Elsevier GmbH. All rights reserved.

  19. Facile Syntheses and Molecular-Docking of Novel Substituted 3,4-Dimethyl-1H-pyrrole-2-carboxamide/carbohydrazide Analogues with Antimicrobial and Antifungal Properties

    Directory of Open Access Journals (Sweden)

    Jitendra D. Bhosale

    2018-04-01

    Full Text Available The article describes the use of facile one-pot, high-yielding reactions to synthesize substituted 3,4-dimethyl-1H-pyrrole-2-carboxamides 3a–m and carbohydrazide analogues 5a–l as potential antifungal and antimicrobial agents. The structural identity and purity of the synthesized compounds were assigned based on appropriate spectroscopic techniques. Synthesized compounds were assessed in vitro for antifungal and antibacterial activity. The compounds 5h, 5i and 5j were found to be the most potent against Aspergillus fumigatus, with MIC values of 0.039 mg/mL. The compound 5f bearing a 2, 6-dichloro group on the phenyl ring was found to be the most active broad spectrum antibacterial agent with a MIC value of 0.039 mg/mL. The mode of action of the most promising antifungal compounds (one representative from each series; 3j and 5h was established by their molecular docking with the active site of sterol 14α-demethylase. Molecular docking studies revealed a highly spontaneous binding ability of the tested compounds in the access channel away from catalytic heme iron of the enzyme, which suggested that the tested compounds inhibit this enzyme and would avoid heme iron-related deleterious side effects observed with many existing antifungal compounds.

  20. Analytical methods for determination of terbinafine hydrochloride in pharmaceuticals and biological materials

    Directory of Open Access Journals (Sweden)

    Basavaiah Kanakapura

    2016-06-01

    Full Text Available Terbinafine is a new powerful antifungal agent indicated for both oral and topical treatment of mycosessince. It is highly effective in the treatment of determatomycoses. The chemical and pharmaceutical analysis of the drug requires effective analytical methods for quality control and pharmacodynamic and pharmacokinetic studies. Ever since it was introduced as an effective antifungal agent, many methods have been developed and validated for its assay in pharmaceuticals and biological materials. This article reviews the various methods reported during the last 25 years.

  1. In vitro activity of antifungal and antiseptic agents against dermatophyte isolates from patients with tinea pedis Atividade in vitro de antifúngicos e anti-sépticos frente a dermatófitos isolados de pacientes com tinea pedis

    Directory of Open Access Journals (Sweden)

    Maria Magali Stelato Rocha Soares

    2001-06-01

    Full Text Available The in vitro activity of antifungal and antiseptic agents were evaluated against dermatophytes isolated from patients with tinea pedis. The antifungals studied were: ciclopirox olamine, cetoconazole, tolciclate and terbinafine, and the antiseptics were: povidine iodine (PVPI, propolis, Fungol®, Andriodermol®, and boric acid. The minimum inhibitory concentration (MIC or the minimal dilution concentration (MDC was determined by an agar dilution method using modified yeast nitrogen agar base, and the minimum fungicidal concentration (MFC or minimum fungicidal dilution (MFD was determined with subcultures on Sabouraud dextrose agar. All drugs studied were active against the dermatophytes at lower concentrations than those used in products and/or pharmaceutical preparations for topical use. Some antifungal agents, mainly terbinafine and tolciclate, presented higher efficacy than the other drugs, with lower MICs and MFCs values. It was concluded that the use of these antiseptic drugs represent an excellent alternative for the topical treatment of tinea pedis. For the treatment of severe cases these are the antifungal agents of choice.A atividade in vitro de antifúngicos e anti-sépticos foram avaliadas frente a dermatófitos isolados de pacientes com tinea pedis. Os antifúngicos estudados foram: ciclopirox olamine, cetoconazol, tolciclato e terbinafina, e os anti-sépticos foram: iodo povidine (PVPI, própolis, Fungol®, Andriodermol®e ácido bórico. A concentração inibitória mínima (CIM ou a diluição inibitória mínima (DIM foi determinada pelo método de diluição em ágar utilizando "yeast nitrogen" base modificado, e a concentração fungicida mínima (CFM ou diluição fungicida mínima (DFM foi determinada por subcultura em Saboraud dextrose ágar. Todas as drogas estudadas foram ativas frente aos dermatófitos em concentrações menores do que as utilizadas em produtos e/ou preparações farmacêuticas para uso tópico. Alguns

  2. Antifungal activity of secondary plant metabolites from potatoes (Solanum tuberosum L.): Glycoalkaloids and phenolic acids show synergistic effects.

    Science.gov (United States)

    Sánchez-Maldonado, A F; Schieber, A; Gänzle, M G

    2016-04-01

    To study the antifungal effects of the potato secondary metabolites α-solanine, α-chaconine, solanidine and caffeic acid, alone or combined. Resistance to glycoalkaloids varied among the fungal species tested, as derived from minimum inhibitory concentrations assays. Synergistic antifungal activity between glycoalkaloids and phenolic compounds was found. Changes in the fluidity of fungal membranes caused by potato secondary plant metabolites were determined by calculation of the generalized polarization values. The results partially explained the synergistic effect between caffeic acid and α-chaconine and supported findings on membrane disruption mechanisms from previous studies on artificial membranes. LC/MS analysis was used to determine variability and relative amounts of sterols in the different fungal species. Results suggested that the sterol pattern of fungi is related to their resistance to potato glycoalkaloids and to their taxonomy. Fungal resistance to α-chaconine and possibly other glycoalkaloids is species dependent. α-Chaconine and caffeic acid show synergistic antifungal activity. The taxonomic classification and the sterol pattern play a role in fungal resistance to glycoalkaloids. Results improve the understanding of the antifungal mode of action of potato secondary metabolites, which is essential for their potential utilization as antifungal agents in nonfood systems. © 2016 The Society for Applied Microbiology.

  3. ZnO and TiO2 nanoparticles as novel antimicrobial agents for oral hygiene: a review

    International Nuclear Information System (INIS)

    Khan, Shams Tabrez; Al-Khedhairy, Abdulaziz A.; Musarrat, Javed

    2015-01-01

    Oral cavity is inhabited by more than 25,000 different bacterial phylotypes; some of them cause systemic infections in addition to dental and periodontal diseases. Emergence of multiple antibiotic resistance among these bacteria necessitates the development of alternative antimicrobial agents that are safe, stable, and relatively economic. This review focuses on the significance of metal oxide nanoparticles, especially zinc oxide and titanium dioxide nanoparticles as supplementary antimicrobials for controlling oral infections and biofilm formation. Indeed, the ZnO NPs and TiO 2 NPs have exhibited significant antimicrobial activity against oral bacteria at concentrations which is not toxic in in vivo toxicity assays. These nanoparticles are being produced at an industrial scale for use in a variety of commercial products including food products. Thus, the application of ZnO and TiO 2 NPs as nanoantibiotics for the development of mouthwashes, dental pastes, and other oral hygiene materials is envisaged. It is also suggested that these NPs could serve as healthier, innocuous, and effective alternative for controlling both the dental biofilms and oral planktonic bacteria with lesser side effects and antibiotic resistance

  4. ZnO and TiO2 nanoparticles as novel antimicrobial agents for oral hygiene: a review

    Science.gov (United States)

    Khan, Shams Tabrez; Al-Khedhairy, Abdulaziz A.; Musarrat, Javed

    2015-06-01

    Oral cavity is inhabited by more than 25,000 different bacterial phylotypes; some of them cause systemic infections in addition to dental and periodontal diseases. Emergence of multiple antibiotic resistance among these bacteria necessitates the development of alternative antimicrobial agents that are safe, stable, and relatively economic. This review focuses on the significance of metal oxide nanoparticles, especially zinc oxide and titanium dioxide nanoparticles as supplementary antimicrobials for controlling oral infections and biofilm formation. Indeed, the ZnO NPs and TiO2 NPs have exhibited significant antimicrobial activity against oral bacteria at concentrations which is not toxic in in vivo toxicity assays. These nanoparticles are being produced at an industrial scale for use in a variety of commercial products including food products. Thus, the application of ZnO and TiO2 NPs as nanoantibiotics for the development of mouthwashes, dental pastes, and other oral hygiene materials is envisaged. It is also suggested that these NPs could serve as healthier, innocuous, and effective alternative for controlling both the dental biofilms and oral planktonic bacteria with lesser side effects and antibiotic resistance.

  5. In vitro evaluation of alternative oral contrast agents for MRI of the gastrointestinal tract

    Energy Technology Data Exchange (ETDEWEB)

    Babos, Magor [University of Szeged, Faculty of Science (Hungary); Euromedic Diagnostics Szeged, 6720 Szeged, Semmelweiss u. 6 (Hungary)], E-mail: babosmagor@yahoo.com; Schwarcz, Attila [University of Pecs, Department of Neurosurgery, Pecs Diagnostic Institute, 7624 Pecs, Retu. 2 (Hungary)], E-mail: attila.schwarcz@aok.pte.hu; Randhawa, Manjit Singh [University of Szeged, Faculty of Medicine, Department of Radiology, 6720 Szeged, Semmelweiss u. 6 (Hungary)], E-mail: majyaal@hotmail.com; Marton, Balazs [University of Szeged, Faculty of Medicine, Department of Radiology, 6720 Szeged, Semmelweiss u. 6 (Hungary)], E-mail: balazsmarton@freemail.hu; Kardos, Lilla [Euromedic Diagnostics Szeged, 6720 Szeged, Semmelweiss u. 6 (Hungary)], E-mail: medlis@tiszanet.hu; Palko, Andras [Euromedic Diagnostics Szeged, 6720 Szeged, Semmelweiss u. 6 (Hungary); University of Szeged, Faculty of Medicine, Department of Radiology, 6720 Szeged, Semmelweiss u. 6 (Hungary)], E-mail: palko@radio.szote.u-szeged.hu

    2008-01-15

    Purpose: In vitro evaluation of different materials as potential alternative oral contrast agents for small bowel MRI. Materials and methods: The T1 and T2 relaxation times of rose hip syrup, black currant extract, cocoa, iron-deferoxamine solution and a commonly used oral contrast material (1 mM Gd-DTPA) were determined in vitro at different concentrations on a 1.0 T clinical MR scanner. T1 values were obtained with an inversion prepared spoiled gradient echo sequence. T2 values were obtained using multiple echo sequences. Finally the materials were visualized on T1-, T2- and T2*-weighted MR images. Results: The relaxation times of the undiluted rose hip syrup (T1 = 110 {+-} 5 ms, T2 = 86 {+-} 3 ms), black currant extract (T1 = 55 {+-} 3 ms, T2 = 39 {+-} 2 ms) and 5 mM iron-deferoxamine solution (T1 = 104 {+-} 4 ms, T2 = 87 {+-} 2 ms) were much shorter than for a 1 mM Gd-DTPA solution (T1 = 180 {+-} 8 ms, T2 = 168 {+-} 5 ms). Dilution of black currant extract to 30% or a 3 mM iron-deferoxamine solution conducted to T1 relaxation times which are quite comparable to a 1 mM Gd-DTPA solution. Despite its much lower metal content an aqueous cocoa suspension (100 g/L) produced T2 relaxation times (T1 = 360 {+-} 21 ms, T2 = 81 {+-} 3 ms) more or less in the same range like the 5 mM iron-deferoxamine solution. Imaging of our in vitro model using clinical sequences allowed to anticipate the T1-, T2- and T2*-depiction of all used substances. Cocoa differed from all other materials with its low to moderate signal intensity on T1- and T2-weighted sequences. While all substances presented a linear 1/T1 and 1/T2 relationship towards concentration, rose hip syrup broke ranks with a disproportionately high increase of relaxation at higher concentrations. Conclusions: Rose hip syrup, black currant extract and iron-deferoxamine solution due to their positive T1 enhancement characteristics and drinkability appear to be valuable oral contrast agents for T1-weighted small bowel MRI

  6. In vitro evaluation of alternative oral contrast agents for MRI of the gastrointestinal tract

    International Nuclear Information System (INIS)

    Babos, Magor; Schwarcz, Attila; Randhawa, Manjit Singh; Marton, Balazs; Kardos, Lilla; Palko, Andras

    2008-01-01

    Purpose: In vitro evaluation of different materials as potential alternative oral contrast agents for small bowel MRI. Materials and methods: The T1 and T2 relaxation times of rose hip syrup, black currant extract, cocoa, iron-deferoxamine solution and a commonly used oral contrast material (1 mM Gd-DTPA) were determined in vitro at different concentrations on a 1.0 T clinical MR scanner. T1 values were obtained with an inversion prepared spoiled gradient echo sequence. T2 values were obtained using multiple echo sequences. Finally the materials were visualized on T1-, T2- and T2*-weighted MR images. Results: The relaxation times of the undiluted rose hip syrup (T1 = 110 ± 5 ms, T2 = 86 ± 3 ms), black currant extract (T1 = 55 ± 3 ms, T2 = 39 ± 2 ms) and 5 mM iron-deferoxamine solution (T1 = 104 ± 4 ms, T2 = 87 ± 2 ms) were much shorter than for a 1 mM Gd-DTPA solution (T1 = 180 ± 8 ms, T2 = 168 ± 5 ms). Dilution of black currant extract to 30% or a 3 mM iron-deferoxamine solution conducted to T1 relaxation times which are quite comparable to a 1 mM Gd-DTPA solution. Despite its much lower metal content an aqueous cocoa suspension (100 g/L) produced T2 relaxation times (T1 = 360 ± 21 ms, T2 = 81 ± 3 ms) more or less in the same range like the 5 mM iron-deferoxamine solution. Imaging of our in vitro model using clinical sequences allowed to anticipate the T1-, T2- and T2*-depiction of all used substances. Cocoa differed from all other materials with its low to moderate signal intensity on T1- and T2-weighted sequences. While all substances presented a linear 1/T1 and 1/T2 relationship towards concentration, rose hip syrup broke ranks with a disproportionately high increase of relaxation at higher concentrations. Conclusions: Rose hip syrup, black currant extract and iron-deferoxamine solution due to their positive T1 enhancement characteristics and drinkability appear to be valuable oral contrast agents for T1-weighted small bowel MRI. Cocoa with its

  7. Candidaemia and antifungal therapy in a French University Hospital: rough trends over a decade and possible links

    Directory of Open Access Journals (Sweden)

    Standaert Annie

    2006-05-01

    Full Text Available Abstract Background Evidence for an increased prevalence of candidaemia and for high associated mortality in the 1990s led to a number of different recommendations concerning the management of at risk patients as well as an increase in the availability and prescription of new antifungal agents. The aim of this study was to parallel in our hospital candidemia incidence with the nature of prescribed antifungal drugs between 1993 and 2003. Methods During this 10-year period we reviewed all cases of candidemia, and collected all the data about annual consumption of prescribed antifungal drugs Results Our centralised clinical mycology laboratory isolates and identifies all yeasts grown from blood cultures obtained from a 3300 bed teaching hospital. Between 1993 and 2003, 430 blood yeast isolates were identified. Examination of the trends in isolation revealed a clear decrease in number of yeast isolates recovered between 1995–2000, whereas the number of positive blood cultures in 2003 rose to 1993 levels. The relative prevalence of Candida albicans and C. glabrata was similar in 1993 and 2003 in contrast to the period 1995–2000 where an increased prevalence of C. glabrata was observed. When these quantitative and qualitative data were compared to the amount and type of antifungal agents prescribed during the same period (annual mean defined daily dose: 2662741; annual mean cost: 615629 € a single correlation was found between the decrease in number of yeast isolates, the increased prevalence of C. glabrata and the high level of prescription of fluconazole at prophylactic doses between 1995–2000. Conclusion Between 1993 and 2000, the number of cases of candidemia halved, with an increase of C. glabrata prevalence. These findings were probably linked to the use of Fluconazole prophylaxis. Although it is not possible to make any recommendations from this data the information is nevertheless interesting and may have considerable implications with

  8. Molecular basis of antifungal drug resistance in yeasts

    DEFF Research Database (Denmark)

    Morio, Florent; Jensen, Rasmus Hare; Le Pape, Patrice

    2017-01-01

    Besides inherent differences in in vitro susceptibilities, clinically-relevant yeast species may acquire resistance upon exposure to most antifungal drugs used in the clinic. In recent years, major fundamental research studies have been conducted to improve our understanding of the molecular basis...... of antifungal resistance. This topic is of major interest as antifungal resistance in yeast is clearly evolving and is correlated with clinical failure. This minireview is an overview of the most recent findings about key molecular mechanisms evolving in human pathogenic yeasts, particularly Candida spp......., in the context of antifungal drug resistance. Also included are the methods currently available for in vitro antifungal susceptibility testing and for molecular detection of mutations associated with resistance. Finally, the genetic drivers of antifungal resistance are discussed in light of the spectra...

  9. Bisbibenzyls, a new type of antifungal agent, inhibit morphogenesis switch and biofilm formation through upregulation of DPP3 in Candida albicans.

    Directory of Open Access Journals (Sweden)

    Li Zhang

    Full Text Available The yeast-to-hypha transition plays a crucial role in the pathogenesis of C. albicans. Farnesol, a quorum sensing molecule (QSM secreted by the fungal itself, could prevent the formation of hyphae and subsequently lead to the defect of biofilm formation. The DPP3, encoding phosphatase, is a key gene in regulating farnesol synthesis. In this study, we screened 24 bisbibenzyls and 2 bibenzyls that were isolated from bryophytes or chemically synthesized by using CLSI method for antifungal effect. Seven bisbibenzyls were found to have antifungal effects with IC(80 less than 32 µg/ml, and among them, plagiochin F, isoriccardin C and BS-34 were found to inhibit the hyphae and biofilm formation of C. albicans in a dose-dependent manner. To uncover the underlying relationship between morphogenesis switch and QSM formation, we measured the farnesol production by HPLC-MS and quantified Dpp3 expression by detecting the fluorescent intensity of green fluorescent protein tagged strain using Confocal Laser Scanning microscopy and Multifunction Microplate Reader. The DPP3 transcripts were determined by real-time PCR. The data indicated that the bisbibenzyls exerted antifungal effects through stimulating the synthesis of farnesol via upregulation of Dpp3, suggesting a potential antifungal application of bisbibenzyls. In addition, our assay provides a novel, visual and convenient method to measure active compounds against morphogenesis switch.

  10. Evaluation of the Efficacy of ME1111 in the Topical Treatment of Dermatophytosis in a Guinea Pig Model

    Science.gov (United States)

    Long, L.; Hager, C.

    2016-01-01

    The treatment of dermatophytoses, including onychomycosis, has come a long way over the past few decades with the introduction of oral antifungals (e.g., terbinafine and itraconazole). However, with these advancements in oral therapies come several undesirable effects, such as kidney and liver toxicity, along with drug-drug interactions. Consequently, there is a need for new topical agents that are effective against dermatophytosis. ME1111 is a topical antifungal under development. In this study, the in vivo efficacy of ME1111 was compared to that of ciclopirox in the topical treatment of dermatophytosis caused by Trichophyton mentagrophytes using a guinea pig model. Animals were treated with the topical antifungals starting at 3 days postinfection, with each agent being applied once daily for seven consecutive days. After the treatment period, the clinical and mycological efficacies were evaluated. The data showed that both antifungals demonstrated significant clinical and mycological efficacies; however, ME1111 showed clinical efficacy superior to that of ciclopirox (46.9% and 25.0%, respectively, with a P value of <0.001). The potent efficacy of ME1111 could be attributed to its properties, such as low keratin binding. PMID:26833160

  11. ArtinM offers new perspectives in the development of antifungal therapy

    Science.gov (United States)

    Ruas, Luciana P.; Carvalho, Fernanda C.; Roque-Barreira, Maria-Cristina

    2012-01-01

    The thermally dimorphic fungus Paracoccidioides brasiliensis is the causative agent of paracoccidioidomycosis (PCM), the most frequent systemic mycosis that affects the rural populations in Latin America. Despite significant developments in antifungal chemotherapy, its efficacy remains limited since drug therapy is prolonged and associated with toxic side effects and relapses. In response to these challenges, it is now recognized that several aspects of antifungal immunity can be modulated to better deal with fungal infections. A common idea for halting fungal infections has been the need to activate a cell-based, pro-inflammatory Th1 immune response to improve the fungal elimination. ArtinM, a D-mannose binding lectin from Artocarpus heterophyllus, has the property of modulating immunity against several intracellular pathogens. Here, we review the immunomodulatory activity of ArtinM during experimental PCM in mice. Both prophylactic and therapeutic protocols of ArtinM administration promotes a Th1 immune response balanced by IL-10, which outstandingly reduces the fungal load in organs of the treated mice while maintaining a controlled inflammation at the site of infection. A carbohydrate recognition-based interaction of ArtinM with Toll-like receptor 2 (TLR2) accounts for initiating the immunomodulatory effect of the lectin. The precise identification of the TLR2 N-glycan(s) targeted by ArtinM may support novel basis for the development of antifungal therapy. PMID:22715337

  12. Microwave-Assisted Synthesis and Biological Evaluation of Dihydropyrimidinone Derivatives as Anti-Inflammatory, Antibacterial, and Antifungal Agents

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    Anjna Bhatewara

    2013-01-01

    Full Text Available A simple protocol for the efficient preparation of aryl and heteroaryl substituted dihydropyrimidinone has been achieved via initial Knoevenagel, subsequent addition, and final cyclization of aldehyde, ethylcyanoacetate, and guanidine nitrate in the presence of piperidine as a catalyst in solvent-free under microwave irradiation. The synthesized compounds showed a good anti-inflammatory, antibacterial, and antifungal activity.

  13. Antifungal activity of phlorotannins against dermatophytes and yeasts: approaches to the mechanism of action and influence on Candida albicans virulence factor.

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    Graciliana Lopes

    Full Text Available In the last few decades, fungal infections, particularly nosocomial, increased all around the world. This increment stimulated the search for new antifungal agents, especially those derived from nature. Among natural products, those from marine sources have gained prominence in the last years. Purified phlorotannins extracts from three brown seaweeds (Cystoseira nodicaulis (Withering M. Roberts, Cystoseira usneoides (Linnaeus M. Roberts and Fucus spiralis Linnaeus were screened for their antifungal activity against human pathogenic yeast and filamentous fungi. The purified phlorotannins extracts from the studied seaweeds displayed fungistatic and fungicidal activity against yeast and dermatophytes, respectively, pointing to their interest as anti-dermatophyte agent. C. albicans ATCC 10231 was the most susceptible among yeast, while Epidermophyton floccosum and Trichophyton rubrum were the most susceptible among dermatophytes. Since the antifungal mechanism constitutes an important strategy for limiting the emergence of resistance to the commercially available agents, the mechanism of action of purified phlorotannins extracts was approached. C. nodicaulis and C. usneoides seem to act by affecting the ergosterol composition of the cell membrane of yeast and dermatophyte, respectively. F. spiralis influenced the dermatophyte cell wall composition by reducing the levels of chitin. Phlorotannins also seem to affect the respiratory chain function, as all of the studied species significantly increased the activity of mitochondrial dehydrogenases and increased the incorporation of rhodamine 123 by yeast cells. Phlorotannins from F. spiralis inhibited the dimorphic transition of Candida albicans, leading to the formation of pseudohyphae with diminished capacity to adhere to epithelial cells. This finding is associated with a decrease of C. albicans virulence and capacity to invade host cells and can be potentially interesting for combined antifungal

  14. Comparison of neutral oral contrast versus positive oral contrast medium in abdominal multidetector CT

    International Nuclear Information System (INIS)

    Berther, Ralph; Eckhardt, Boris; Zollikofer, Christoph L.; Patak, Michael A.; Erturk, Sukru M.

    2008-01-01

    To determine whether neutral contrast agents with water-equivalent intraluminal attenuation can improve delineation of the bowel wall and increase overall image quality for a non-selected patient population, a neutral oral contrast agent (3% mannitol) was administered to 100 patients referred for abdominal multidetector row computed tomography (MDCT). Their results were compared with those of 100 patients given a positive oral contrast agent. Qualitative and quantitative measurements were done on different levels of the gastrointestinal tract by three experienced readers. Patients given the neutral oral contrast agent showed significant better qualitative results for bowel distension (P<0.001), homogeneity of the luminal content (P<0.001), delineation of the bowel-wall to the lumen (P<0.001) and to the mesentery (P<0.001) and artifacts (P<0.001), leading to a significant better overall image quality (P<0.001) than patients receiving positive oral contrast medium. The quantitative measurements revealed significant better distension (P<0.001) and wall to lumen delineation (P<0.001) for the patients receiving neutral oral contrast medium. The present results show that the neutral oral contrast agent (mannitol) produced better distension, better homogeneity and better delineation of the bowel wall leading to a higher overall image quality than the positive oral contrast medium in a non-selected patient population. (orig.)

  15. Licochalcone A induces apoptosis in KB human oral cancer cells via a caspase-dependent FasL signaling pathway

    Science.gov (United States)

    KIM, JAE-SUNG; PARK, MI-RA; LEE, SOOK-YOUNG; KIM, DO KYOUNG; MOON, SUNG-MIN; KIM, CHUN SUNG; CHO, SEUNG SIK; YOON, GOO; IM, HEE-JEONG; YOU, JAE-SEEK; OH, JI-SU; KIM, SU-GWAN

    2014-01-01

    Licochalcone A (Lico-A) is a natural phenol licorice compound with multiple bioactivities, including anti-inflammatory, anti-microbial, anti-fungal and osteogenesis-inducing properties. In the present study, we investigated the Lico-A-induced apoptotic effects and examined the associated apoptosis pathway in KB human oral cancer cells. Lico-A decreased the number of viable KB oral cancer cells. However, Lico-A did not have an effect on primary normal human oral keratinocytes. In addition, the IC50 value of Lico-A was determined to be ~50 μM following dose-dependent stimulation. KB oral cancer cells stimulated with Lico-A for 24 h showed chromatin condensation by DAPI staining, genomic DNA fragmentation by agarose gel electrophoresis and a gradually increased apoptotic cell population by FACS analysis. These data suggest that Lico-A induces apoptosis in KB oral cancer cells. Additionally, Lico-A-induced apoptosis in KB oral cancer cells was mediated by the expression of factor associated suicide ligand (FasL) and activated caspase-8 and −3 and poly(ADP-ribose) polymerase (PARP). Furthermore, in the KB oral cancer cells co-stimulation with a caspase inhibitor (Z-VAD-fmk) and Lico-A significantly abolished the apoptotic phenomena. Our findings demonstrated that Lico-A-induced apoptosis in KB oral cancer cells involves the extrinsic apoptotic signaling pathway, which involves a caspase-dependent FasL-mediated death receptor pathway. Our data suggest that Lico-A be developed as a chemotherapeutic agent for the management of oral cancer. PMID:24337492

  16. Potential Use of Phenolic Acids as Anti-Candida Agents: A Review

    Science.gov (United States)

    Teodoro, Guilherme R.; Ellepola, Kassapa; Seneviratne, Chaminda J.; Koga-Ito, Cristiane Y.

    2015-01-01

    There has been a sharp rise in the occurrence of Candida infections and associated mortality over the last few years, due to the growing body of immunocompromised population. Limited number of currently available antifungal agents, undesirable side effects and toxicity, as well as emergence of resistant strains pose a considerable clinical challenge for the treatment of candidiasis. Therefore, molecules that derived from natural sources exhibiting considerable antifungal properties are a promising source for the development of novel anti-candidal therapy. Phenolic compounds isolated from natural sources possess antifungal properties of interest. Particularly, phenolic acids have shown promising in vitro and in vivo activity against Candida species. However, studies on their mechanism of action alone or in synergism with known antifungals are still scarce. This review attempts to discuss the potential use, proposed mechanisms of action and limitations of the phenolic acids in anti-candidal therapy. PMID:26733965

  17. Candiduria in adults and children: prevalence and antifungal susceptibility in outpatient of Jataí-GO

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    Izabela Alves de Sousa

    2014-08-01

    Full Text Available Introduction: The term candiduria refers to the presence of yeast in urine and Candida albicans is the most common agent. In general, routine laboratories do not perform identification and cultivation of yeast. Objectives: To determine the prevalence of Candida species and to evaluate the antifungal susceptibility of the species isolated in urine of outpatients Jataí-GO, between January-October 2013. Material and method: Urine samples containing fungal structures were plated out on Sabouraud agar with chloramphenicol. Differentiation was taken with the urease test, nitrogen and carbon sources assimilation, germ tube test, morphology on cornmeal agar and chromogenic agar cultivation. Susceptibility was evaluated at antifungal itraconazole, fluconazole, amphotericin B and ketoconazole. Results: 1,215 urine tests were performed, and 64 had fungal structures (5.3%. Two samples were lost, thus here we considered 62 isolates. From this total, 43 were identified as C. albicans (67.2 %, eight C. glabrata (12.5 %, five C. krusei (7.8%, three C. tropicalis (4.7%, and three could not determine the species (4.7%. Amphotericin B and ketoconazole inhibited 94.9% of the isolates. On the other hand, 55.9% and 54.2 % were resistant to itraconazole and fluconazole, respectively. The resistance rates of both fluconazole and itraconazole for C. glabrata and C. albicans, as fluconazole for C. albicans and C. krusei, showed significant differences (p < 0.05. Conclusion: These data demonstrate the importance of conducting a full identification and susceptibility to antifungal agents in samples with yeast infection.

  18. Antifungal testing and high-throughput screening of compound library against Geomyces destructans, the etiologic agent of geomycosis (WNS in bats.

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    Sudha Chaturvedi

    Full Text Available Bats in the northeastern U.S. are affected by geomycosis caused by the fungus Geomyces destructans (Gd. This infection is commonly referred to as White Nose Syndrome (WNS. Over a million hibernating bats have died since the fungus was first discovered in 2006 in a cave near Albany, New York. A population viability analysis conducted on little brown bats (Myotis lucifugus, one of six bat species infected with Gd, suggests regional extinction of this species within 20 years. The fungus Gd is a psychrophile ("cold loving", but nothing is known about how it thrives at low temperatures and what pathogenic attributes allow it to infect bats. This study aimed to determine if currently available antifungal drugs and biocides are effective against Gd. We tested five Gd strains for their susceptibility to antifungal drugs and high-throughput screened (HTS one representative strain with SpectrumPlus compound library containing 1,920 compounds. The results indicated that Gd is susceptible to a number of antifungal drugs at concentrations similar to the susceptibility range of human pathogenic fungi. Strains of Gd were susceptible to amphotericin B, fluconazole, itraconazole, ketoconazole and voriconazole. In contrast, very high MICs (minimum inhibitory concentrations of flucytosine and echinocandins were needed for growth inhibition, which were suggestive of fungal resistance to these drugs. Of the 1,920 compounds in the library, a few caused 50%--to greater than 90% inhibition of Gd growth. A number of azole antifungals, a fungicide, and some biocides caused prominent growth inhibition. Our results could provide a theoretical basis for future strategies aimed at the rehabilitation of most affected bat species and for decontamination of Gd in the cave environment.

  19. 3-Bromopyruvate: a novel antifungal agent against the human pathogen Cryptococcus neoformans.

    Science.gov (United States)

    Dyląg, Mariusz; Lis, Paweł; Niedźwiecka, Katarzyna; Ko, Young H; Pedersen, Peter L; Goffeau, Andre; Ułaszewski, Stanisław

    2013-05-03

    We have investigated the antifungal activity of the pyruvic acid analogue: 3-bromopyruvate (3-BP). Growth inhibition by 3-BP of 110 strains of yeast-like and filamentous fungi was tested by standard spot tests or microdilution method. The human pathogen Cryptococcus neoformans exhibited a low Minimal Inhibitory Concentration (MIC) of 0.12-0.15 mM 3-BP. The high toxicity of 3-BP toward C. neoformans correlated with high intracellular accumulation of 3-BP and also with low levels of intracellular ATP and glutathione. Weak cytotoxicity towards mammalian cells and lack of resistance conferred by the PDR (Pleiotropic Drug Resistance) network in the yeast Saccharomyces cerevisiae, are other properties of 3-BP that makes it a novel promising anticryptococcal drug. Copyright © 2013 Elsevier Inc. All rights reserved.

  20. In silico PASS analysis and determination of antimycobacterial, antifungal, and antioxidant efficacies of maslinic acid in an extract rich in pentacyclic triterpenoids

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    Prasad G Jamkhande

    2016-01-01

    Conclusion: This work provides scientific evidence of the antioxidant, antifungal, and antimycobacterial activities of MA, showing its potential application in the development of natural antioxidants and antimicrobial agents for the agro-food and pharmaceutical industries.

  1. Patients' oral hydration levels and incidence of immediate to short-term mild side-effects in contrast agent enhanced MRI diagnostics

    International Nuclear Information System (INIS)

    Jonker, Leon; Fallahi, Farshid

    2015-01-01

    Aim: Gadolinium-based contrast agents for radiodiagnostic purposes can lead to side effects, including nephrotoxicity in patients with renal insufficiency. This study evaluated whether the occurrence of mild side effects from gadolinium-based contrast enhanced magnetic resonance imaging (MRI) correlates to patients' oral hydration levels. Methods: Oral fluid intake levels 24 h pre- and 24 h post-MRI, as well as incidence of mild side-effects experienced 30 min and 24 h post-MRI were recorded by using a patient self-reporting questionnaire. Results: A total of 174 patients, 29 controls, 98 administered Prohance and 47 receiving Dotarem, were enrolled. Overall, the most frequently reported side-effect was headache; nausea only occurred in patients receiving contrast agent. One or more side-effects experienced 24 h following the MRI scan were reported by 10% (controls), 24% (Prohance) and 22% (Dotarem) of patients, respectively. Multivariate ordinal regression analysis showed that only male gender (OR 0.24, 95% CI 0.11–0.53) was statistically significantly associated with a decreased incidence of side-effects 30 min after MRI. At 24-h post MRI, a lack of contrast agent (OR 0.40, 95% CI 0.09–1.74) and male gender (OR 0.46, 95% CI 0.19–1.09) were associated with fewer side-effects. Conclusions: The level oral fluid intake before and after undergoing gadolinium-based contrast-enhanced MRI does not appear to markedly affect the incidence of common undesirable mild symptoms experienced shortly after the procedure. Confounding differences between patients in reporting side-effects may contribute to these findings. - Highlights: • We assess the incidence of patient-reported side-effects after contrast-enhanced MRI. • We examine the potential impact of oral hydration levels on side-effects. • Patient reported side-effects are high compared to those reported by clinicians. • Female gender and contrast agent itself are associated with increased side

  2. Evaluation of antifungal activity of standardized extract of Salvia rhytidea Benth. (Lamiaceae) against various Candida isolates.

    Science.gov (United States)

    Salari, S; Bakhshi, T; Sharififar, F; Naseri, A; Ghasemi Nejad Almani, P

    2016-12-01

    Salvia species have long been described in traditional medicine for various indications. Owing to the widespread use of this genus by ethnic populations, especially for various infections ranging from skin disease to gastrointestinal disorders, we were encouraged to determine whether Salvia rhytidea could be effective against fungal infections. Given the increased incidence of candidiasis in the past decade, limits on the use of antifungal drugs, emergence of azole-resistant Candida species and increased incidence of treatment failures, it is necessary to identify a novel agent with antifungal properties. Aim of the study was to evaluate the antifungal properties of S. rhytidea against various Candida isolates. In this study, at first rosmarinic acid content of plant extract was determined. A total of 96 Candida isolates were tested, including the following species: Candida albicans (n=42), Candida glabrata (n=16), Candida tropicalis (n=11), Candida krusei (n=9), Candida parapsilosis (n=9), Candida lusitaniae (n=7) and Candida guilliermondii (n=2). The in vitro antifungal activity of methanolic extracts of S. rhytidea Benth. was evaluated against Candida isolates and compared with that of the standard antifungal drug nystatin by using a broth microdilution method, according to CLSI. Phytochemical screening results showed that the methanolic extract of S. rhytidea Benth. was rich in flavonoids and tannins. The minimal inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) values of S. rhytidea Benth. ranged from 3.125 to>100μg/ml and 6.25 to>100μg/ml respectively. The growth inhibition value displayed that C. tropicalis, C. krusei and C. albicans isolates were most susceptible to S. rhytidea. Findings show that S. rhytidea possesses an antifungal effect against Candida isolates. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  3. Cuticular antifungals in spiders: density- and condition dependence.

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    Daniel González-Tokman

    Full Text Available Animals living in groups face a high risk of disease contagion. In many arthropod species, cuticular antimicrobials constitute the first protective barrier that prevents infections. Here we report that group-living spiders produce cuticular chemicals which inhibit fungal growth. Given that cuticular antifungals may be costly to produce, we explored whether they can be modulated according to the risk of contagion (i.e. under high densities. For this purpose, we quantified cuticular antifungal activity in the subsocial crab spider Diaea ergandros in both natural nests and experimentally manipulated nests of varying density. We quantified the body-condition of spiders to test whether antifungal activity is condition dependent, as well as the effect of spider density on body-condition. We predicted cuticular antifungal activity to increase and body-condition to decrease with high spider densities, and that antifungal activity would be inversely related to body-condition. Contrary to our predictions, antifungal activity was neither density- nor condition-dependent. However, body-condition decreased with density in natural nests, but increased in experimental nests. We suggest that pathogen pressure is so important in nature that it maintains high levels of cuticular antifungal activity in spiders, impacting negatively on individual energetic condition. Future studies should identify the chemical structure of the isolated antifungal compounds in order to understand the physiological basis of a trade-off between disease prevention and energetic condition caused by group living, and its consequences in the evolution of sociality in spiders.

  4. Cuticular antifungals in spiders: density- and condition dependence.

    Science.gov (United States)

    González-Tokman, Daniel; Ruch, Jasmin; Pulpitel, Tamara; Ponton, Fleur

    2014-01-01

    Animals living in groups face a high risk of disease contagion. In many arthropod species, cuticular antimicrobials constitute the first protective barrier that prevents infections. Here we report that group-living spiders produce cuticular chemicals which inhibit fungal growth. Given that cuticular antifungals may be costly to produce, we explored whether they can be modulated according to the risk of contagion (i.e. under high densities). For this purpose, we quantified cuticular antifungal activity in the subsocial crab spider Diaea ergandros in both natural nests and experimentally manipulated nests of varying density. We quantified the body-condition of spiders to test whether antifungal activity is condition dependent, as well as the effect of spider density on body-condition. We predicted cuticular antifungal activity to increase and body-condition to decrease with high spider densities, and that antifungal activity would be inversely related to body-condition. Contrary to our predictions, antifungal activity was neither density- nor condition-dependent. However, body-condition decreased with density in natural nests, but increased in experimental nests. We suggest that pathogen pressure is so important in nature that it maintains high levels of cuticular antifungal activity in spiders, impacting negatively on individual energetic condition. Future studies should identify the chemical structure of the isolated antifungal compounds in order to understand the physiological basis of a trade-off between disease prevention and energetic condition caused by group living, and its consequences in the evolution of sociality in spiders.

  5. Gastric stromal tumor: two-phase dynamic CT findings with water as oral contrast agents

    International Nuclear Information System (INIS)

    Lee, Se Hyo; Cho, June Sik; Shin, Kyung Sook; Jeong, Ki Ho; Park, Jin Yong; Yu, Ho Jun; Kim, Young Min; Jeon, Kwang Jin

    2000-01-01

    To evaluate two-phase dynamic CT with water as oral contrast agents in the CT diagnosis of gastric stromal tumors. We retrospectively reviewed the CT findings in 21 patients with pathologically proven gastric stromal tumors. Six were found to be benign, twelve were malignant, and there were three cases of STUMP (stromal tumor uncertain malignant potential). Two-phase dynamic CT scans with water as oral contrast agents were obtained 60-70 secs (portal phase) and 3 mins (equilibrium phase) after the start of IV contrast administration. We determined the size, growth pattern, and enhancement pattern of the tumors and overlying mucosa, the presence or absence of ulceration and necrosis, tumor extent, and lymph nod and distant metastasis. The CT and pathologic findings were correlated. All six benign tumors and three STUMP were less than 5.5 cm in size, and during the portal phase showed round endogastric masses with highly enhanced, intact overlying mucosa. Twelve malignant tumors were 4.5-15.5 cm in size (mean, 11.5 cm); an endogastric mass was seen in three cases, an exogastric mass in one, and a mixed pattern in eight. On portal phase images the tumors were not significantly enhanced, but highly enhanced feeding vessels were noted in five larger tumors (greater than 10 cm). All 12 malignant tumors showed ulceration and necrosis, and interruption of overlying mucosa was clearly seen during the portal phase. We were readily able to evaluate tumor extent during this phase, and in ten malignant tumors there was no invasion of adjacent organs. Seven malignant tumors showed air density within their necrotic portion (p less than 0.05). On equilibrium phase images, all malignant tumors showed heterogeneous enhancement due to necrosis, and poorly enhanced overlying mucosa. Dynamic CT during the portal phase with water as oral contrast agents was useful for depicting the submucosal origin of gastric stromal tumors and for evaluating the extent of malignant stromal tumors. Our

  6. In vitro susceptibility testing of dermatophytes isolated in Goiania, Brazil, against five antifungal agents by broth microdilution method Teste de suscetibilidade in vitro de dermatófitos isolados em Goiânia, Brasil, contra cinco agentes antifúngicos pelo método de microdiluição em caldo

    Directory of Open Access Journals (Sweden)

    Crystiane Rodrigues Araújo

    2009-02-01

    Full Text Available The antifungal activities of fluconazole, itraconazole, ketoconazole, terbinafine and griseofulvin were tested by broth microdilution technique, against 60 dermatophytes isolated from nail or skin specimens from Goiania city patients, Brazil. In this study, the microtiter plates were incubated at 28 ºC allowing a reading of the minimal inhibitory concentration (MIC after four days of incubation for Trichophyton mentagrophytes and five days for T. rubrum and Microsporum canis. Most of the dermatophytes had uniform patterns of susceptibility to the antifungal agents tested. Low MIC values as 0.03 µg/mL were found for 33.3%, 31.6% and 15% of isolates for itraconazole, ketoconazole and terbinafine, respectively.Atividades antifúngicas de fluconazol, itraconazol, cetoconazol, terbinafina e griseofulvina foram testadas pelo método de microdiluição em caldo contra 60 isolados de dermatófitos. Os resultados mostraram que todos os isolados produziram crescimento claramente detectável a 28 ºC e a concentração inibitória mínima (CIM foi determinada após quatro dias de incubação para Trichophyton mentagrophytes e cinco dias para T. rubrum e Microsporum canis. A maioria dos isolados teve um padrão uniforme de suscetibilidade para os agentes antifúngicos testados. Baixos valores de CIM como 0,03 µg/mL foram encontrados para 33,3%, 31,6% e 15% dos isolados para itraconazol, cetoconazol e terbinafina, respectivamente.

  7. MDCT appearance of the appendix: how does the low-density barium sulfate oral contrast agent affect it?

    Science.gov (United States)

    Yaghmai, Vahid; Aghaei-Lasboo, Anahita; Brandwein, Warren M; Tochetto, Sandra; Mafi, John N; Miller, Frank H; Nikolaidis, Paul

    2011-01-01

    We compared the effect of low-density barium sulfate neutral oral contrast agent on the diameter of normal appendix and its luminal content versus that of water on multidetector-row CT. CT scans of 24 patients who had been imaged on two separate occasions for the evaluation of pancreatic pathology, once with water and subsequently with low-density barium sulfate as the neutral oral contrast agent were evaluated (total of 48 scans). Studies were randomized and reviewed in consensus on a workstation in the stack mode by two radiologists blinded to the type of oral contrast. The appendix was measured at baseline and 10 days later to obtain an average diameter. Results of the water and low-density barium sulfate groups were compared using paired t test. Contents of the appendiceal lumen were also noted (gas, fluid, mixed, and collapsed appendix). The average diameter of the appendix for scans obtained with water and low-density barium sulfate was 4.09 ± 0.87 mm (median, 4.22 mm; range, 2.50-5.65 mm) and 4.13 ± 0.93 mm (median, 4 mm, range, 2.2-5.65 mm), respectively. This difference was not statistically significant (P = 0.69). There was no statistically significant difference in the appendiceal content when water or low-density barium sulfate were used as oral contrast (χ (2) = 4.25, P = 0.89). Low-density barium sulfate does not affect appendiceal content or diameter and, therefore, should not adversely affect evaluation of the appendix on multidetector row CT.

  8. Synthesis, Antifungal Evaluation and In Silico Study of N-(4-Halobenzyl)amides.

    Science.gov (United States)

    Montes, Ricardo Carneiro; Perez, Ana Luiza A L; Medeiros, Cássio Ilan S; Araújo, Marianna Oliveira de; Lima, Edeltrudes de Oliveira; Scotti, Marcus Tullius; Sousa, Damião Pergentino de

    2016-12-13

    A collection of 32 structurally related N -(4-halobenzyl)amides were synthesized from cinnamic and benzoic acids through coupling reactions with 4-halobenzylamines, using (benzotriazol-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate (BOP) as a coupling agent. The compounds were identified by spectroscopic methods such as infrared, ¹H- and 13 C- Nuclear Magnetic Resonance (NMR) and high-resolution mass spectrometry. The compounds were then submitted to antimicrobial tests by the minimum inhibitory concentration method (MIC) and nystatin was used as a control in the antifungal assays. The purpose of the tests was to evaluate the influence of structural changes in the cinnamic and benzoic acid substructures on the inhibitory activity against strains of Candida albicans , Candida tropicalis , and Candida krusei . A quantitative structure-activity relationship (QSAR) study with KNIME v. 3.1.0 and Volsurf v. 1.0.7 softwares were realized, showing that descriptors DRDRDR, DRDRAC, L4LgS, IW4 and DD2 influence the antifungal activity of the haloamides. In general, 10 benzamides revealed fungal sensitivity, especially a vanillic amide which enjoyed the lowest MIC. The results demonstrate that a hydroxyl group in the para position, and a methoxyl at the meta position enhance antifungal activity for the amide skeletal structure. In addition, the double bond as a spacer group appears to be important for the activity of amide structures.

  9. Oral candidosis in relation to oral immunity.

    Science.gov (United States)

    Feller, L; Khammissa, R A G; Chandran, R; Altini, M; Lemmer, J

    2014-09-01

    Symptomatic oral infection with Candida albicans is characterized by invasion of the oral epithelium by virulent hyphae that cause tissue damage releasing the inflammatory mediators that initiate and sustain local inflammation. Candida albicans triggers pattern-recognition receptors of keratinocytes, macrophages, monocytes and dendritic cells, stimulating the production of IL-1β, IL-6 and IL-23. These cytokines induce the differentiation of Th17 cells and the generation of IL-17- and/or IL-22-mediated antifungal protective immuno-inflammatory responses in infected mucosa. Some immune cells including NKT cells, γδ T cells and lymphoid cells that are innate to the oral mucosa have the capacity to produce large quantities of IL-17 in response to C. albicans, sufficient to mediate effective protective immunity against C. albicans. On the other hand, molecular structures of commensal C. albicans blastoconidia, although detected by pattern-recognition receptors, are avirulent, do not invade the oral epithelium, do not elicit inflammatory responses in a healthy host, but induce regulatory immune responses that maintain tissue tolerance to the commensal fungi. The type, specificity and sensitivity of the protective immune response towards C. albicans is determined by the outcome of the integrated interactions between the intracellular signalling pathways of specific combinations of activated pattern-recognition receptors (TLR2, TLR4, Dectin-1 and Dectin-2). IL-17-mediated protective immune response is essential for oral mucosal immunity to C. albicans infection. © 2013 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

  10. Differential Activity of the Oral Glucan Synthase Inhibitor SCY-078 against Wild-Type and Echinocandin-Resistant Strains of Candida Species.

    Science.gov (United States)

    Pfaller, Michael A; Messer, Shawn A; Rhomberg, Paul R; Borroto-Esoda, Katyna; Castanheira, Mariana

    2017-08-01

    SCY-078 (formerly MK-3118) is a novel orally active inhibitor of fungal β-(1,3)-glucan synthase (GS). SCY-078 is a derivative of enfumafungin and is structurally distinct from the echinocandin class of antifungal agents. We evaluated the in vitro activity of this compound against wild-type (WT) and echinocandin-resistant isolates containing mutations in the FKS genes of Candida spp. Against 36 Candida spp. FKS mutants tested, 30 (83.3%) were non-WT to 1 or more echinocandins, and only 9 (25.0%) were non-WT (MIC, >WT-upper limit) to SCY-078. Among C. glabrata isolates carrying FKS alterations, 84.0% were non-WT to the echinocandins versus only 24.0% for SCY-078. In contrast to the echinocandin comparators, the activity of SCY-078 was minimally affected by the presence of FKS mutations, suggesting that this agent is useful in the treatment of Candida infections due to echinocandin-resistant strains. Copyright © 2017 American Society for Microbiology.

  11. Antifungal activities of diphenyl diselenide and ebselen alone and in combination with antifungal agents against Fusarium spp.

    Science.gov (United States)

    Venturini, Tarcieli Pozzebon; Chassot, Francieli; Loreto, Érico Silva; Keller, Jéssica Tairine; Azevedo, Maria Izabel; Zeni, Gilson; Santurio, Janio Morais; Alves, Sydney Hartz

    2016-07-01

    Herein, we describe the in vitro activity of a combination of the organoselenium compounds diphenyl diselenide and ebselen alone and in combination with amphotericin B, caspofungin, itraconazole, and voriconazole against 25 clinical isolates of Fusarium spp. For this analysis, we used the broth microdilution method based on the M38-A2 technique and checkerboard microdilution method. Diphenyl diselenide (MIC range = 4-32 μg/ml) and ebselen (MIC range = 2-8 μg/ml) showed in vitro activity against the isolates tested. The most effective combinations were (synergism rates): ebselen + amphotericin B (88%), ebselen + voriconazole (80%), diphenyl diselenide + amphotericin B (72%), and diphenyl diselenide + voriconazole (64%). Combination with caspofungin resulted in low rates of synergism: ebselen + caspofungin, 36%, and diphenyl diselenide + caspofungin, 28%; combination with itraconazole demonstrated indifferent interactions. Antagonistic effects were not observed for any of the combinations tested. Our findings suggest that the antifungal potential of diphenyl diselenide and ebselen deserves further investigation in in vivo experimental models, especially in combination with amphotericin B and voriconazole. © The Author 2016. Published by Oxford University Press on behalf of The International Society for Human and Animal Mycology. All rights reserved. For permissions, please e-mail: journals.permissions@oup.com.

  12. ORAL HYPOGLYCAEMIC AGENTS IN THE MANAGEMENT OF TYPE II DIABETES MELLITUS

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    Durgaprasad M.

    2016-06-01

    Full Text Available OBJECTIVES Diabetes is fast gaining the status of a potential epidemic globally. The number of people with diabetes has risen from 108 million in 1980 to 422 million in 2014, the rise seen more rapidly in developing and under developed countries. Type 2 Diabetes Mellitus (T2DM being the most common type, accounting for an estimated 85-95% of all diabetes cases. Diabetes remains a major cause of blindness, renal failure, and cardiovascular events including heart attacks, stroke and limb amputations. 1 Being an heterogeneous disorder, many adults with T2DM have difficulty controlling their blood sugar levels and associated complications as most of available antidiabetic agents aim to achieve only normoglycaemia and relieve diabetes symptoms, such as polydipsia, polyuria, weight loss, ketoacidosis while the longterm goals to prevent the development of or slow the progression of longterm complications of the disease is often unaddressed, therefore, there remains, a significant unmet demand for new agents that will help diabetic patients achieve treatment targets without increasing the risk for weight gain or hypoglycaemia. Among the new classes of oral agents, SGLT-2 inhibitors and mTOT insulin sensitisers appear to hold some good promise. However, recent articles published describing its adverse effect profile of SGLT-2 inhibitors had put a question mark on its utility. In this article, we have reviewed the plethora of available OHAs along with the newer OHAs for managing T2DM optimally.

  13. Antifungal Activity of Gallic Acid In Vitro and In Vivo.

    Science.gov (United States)

    Li, Zhi-Jian; Liu, Meng; Dawuti, Gulina; Dou, Qin; Ma, Yu; Liu, Heng-Ge; Aibai, Silafu

    2017-07-01

    Gallic acid (GA) is a polyphenol natural compound found in many medicinal plant species, including pomegranate rind (Punica granatum L.), and has been shown to have antiinflammatory and antibacterial properties. Pomegranate rind is used to treat bacterial and fungal pathogens in Uyghur and other systems of traditional medicine, but, surprisingly, the effects of GA on antifungal activity have not yet been reported. In this study, we aimed to investigate the inhibitory effects of GA on fungal strains both in vitro and in vivo. The minimal inhibitory concentration (MIC) was determined by the NCCLS (M38-A and M27-A2) standard method in vitro, and GA was found to have a broad spectrum of antifungal activity, with MICs for all the tested dermatophyte strains between 43.75 and 83.33 μg/mL. Gallic acid was also active against three Candida strains, with MICs between 12.5 and 100.0 μg/mL. The most sensitive Candida species was Candida albicans (MIC = 12.5 μg/mL), and the most sensitive filamentous species was Trichophyton rubrum (MIC = 43.75 μg/mL), which was comparable in potency to the control, fluconazole. The mechanism of action was investigated for inhibition of ergosterol biosynthesis using an HPLC-based assay and an enzyme linked immunosorbent assay. Gallic acid reduced the activity of sterol 14α-demethylase P450 (CYP51) and squalene epoxidase in the T. rubrum membrane, respectively. In vivo model demonstrated that intraperitoneal injection administration of GA (80 mg/kg d) significantly enhanced the cure rate in a mice infection model of systemic fungal infection. Overall, our results confirm the antifungal effects of GA and suggest a mechanism of action, suggesting that GA has the potential to be developed further as a natural antifungal agent for clinical use. Copyright © 2017 John Wiley & Sons, Ltd. Copyright © 2017 John Wiley & Sons, Ltd.

  14. Differential Antifungal Activity of Human and Cryptococcal Melanins with Structural Discrepancies.

    Science.gov (United States)

    Correa, Néstor; Covarrubias, Cristian; Rodas, Paula I; Hermosilla, Germán; Olate, Verónica R; Valdés, Cristián; Meyer, Wieland; Magne, Fabien; Tapia, Cecilia V

    2017-01-01

    Melanin is a pigment found in all biological kingdoms, and plays a key role in protection against ultraviolet radiation, oxidizing agents, and ionizing radiation damage. Melanin exerts an antimicrobial activity against bacteria, fungi, and parasites. We demonstrated an antifungal activity of synthetic and human melanin against Candida sp. The members of the Cryptococcus neoformans and C. gattii species complexes are capsulated yeasts, which cause cryptococcosis. For both species melanin is an important virulence factor. To evaluate if cryptococcal and human melanins have antifungal activity against Cryptococcus species they both were assayed for their antifungal properties and physico-chemical characters. Melanin extracts from human hair and different strains of C. neoformans ( n = 4) and C. gattii ( n = 4) were investigated. The following minimum inhibitory concentrations were found for different melanins against C. neoformans and C. gattii were (average/range): 13.7/(7.8-15.6) and 19.5/(15.6-31.2) μg/mL, respectively, for human melanin; 273.4/(125->500) and 367.2/(125.5->500) μg/mL for C. neoformans melanin and 125/(62.5-250) and 156.2/(62-250) μg/mL for C. gattii melanin. Using Scanning Electron Microscopy we observed that human melanin showed a compact conformation and cryptococcal melanins exposed an amorphous conformation. Infrared spectroscopy (FTIR) showed some differences in the signals related to C-C bonds of the aromatic ring of the melanin monomers. High Performance Liquid Chromatography established differences in the chromatograms of fungal melanins extracts in comparison with human and synthetic melanin, particularly in the retention time of the main compound of fungal melanin extracts and also in the presence of minor unknown compounds. On the other hand, MALDI-TOF-MS analysis showed slight differences in the spectra, specifically the presence of a minor intensity ion in synthetic and human melanin, as well as in some fungal melanin extracts. We

  15. Combination antifungal therapy and surgery for the treatment of invasive pulmonary aspergillosis after hematopoietic stem cell transplantation

    Directory of Open Access Journals (Sweden)

    Tiziana Toffolutti

    2011-06-01

    Full Text Available An 8-year old boy, affected by severe aplastic anemia, developed a probable pulmonary invasive aspergillosis (IA early after a second unrelated allogeneic hematopoietic stem cell transplant (HSCT. He was treated promptly with the combination of liposomal amphotericin B and caspofungin. Despite the initial stabilization, the patient deteriorated and the antifungal therapy was switched to voriconazole and caspofungin. The patient gradually improved and was discharged home on day +29 post-HSCT on oral voriconazole. On day +119, a sudden episode of hemoptysis occurred and a right superior lobectomy was decided to remove the residual aspergilloma. The patient is now alive and well more than 24 months from HSCT. This case demonstrated that antifungal combination therapy and surgery are valid options to cure pulmonary IA even in patients at high-risk and severely immunosuppressed.

  16. Ficus Deltoidea: A potential source for new oral antidiabetic agent

    International Nuclear Information System (INIS)

    Zainah Adam; Juliana Mahamad Napiah; Shafii Khamis; Muhajir Hamid

    2012-01-01

    Ficus deltoidea or locally known as Mas Cotek is one of the common medicinal plant used in Malaysia. Ethno botanical approaches showed that this plant possess antidiabetic property. Previous study had shown that F. deltoidea reduced hyperglycemia in type I diabetic rats at different prandial state. This study was done to elucidate the possible antihyperglycemic mechanisms of F. deltoidea. The results showed that F. deltoidea significantly stimulated insulin secretion from pancreatic β-cells with the highest magnitude of stimulation was 7.31-fold (p 50 value was 4.15±0.25 mg/ml. Kinetic analysis of the enzyme activity revealed the F. deltoidea exhibited a mixed-type inhibition mechanism against sucrase activity. Such observations showed that F. deltoidea has the potential to be developed as new oral antidiabetic agent for the treatment of diabetes mellitus. (author)

  17. ANTIFUNGAL POTENTIAL OF PLANT SPECIES FROM BRAZILIAN CAATINGA AGAINST DERMATOPHYTES.

    Science.gov (United States)

    Biasi-Garbin, Renata Perugini; Demitto, Fernanda de Oliveira; Amaral, Renata Claro Ribeiro do; Ferreira, Magda Rhayanny Assunção; Soares, Luiz Alberto Lira; Svidzinski, Terezinha Inez Estivalet; Baeza, Lilian Cristiane; Yamada-Ogatta, Sueli Fumie

    2016-01-01

    Trichophyton rubrum and Trichophyton mentagrophytes complex, or Trichophyton spp. are the main etiologic agents of dermatophytosis, whose treatment is limited by the high cost of antifungal treatments, their various side effects, and the emergence of resistance amongst these species. This study evaluated the in vitro antidermatophytic activity of 23 crude extracts from nine plant species of semiarid vegetation (caatinga) found in Brazil. The extracts were tested at concentrations ranging from 1.95 to 1,000.0 mg/mL by broth microdilution assay against the reference strains T. rubrum ATCC 28189 and T. mentagrophytes ATCC 11481, and 33 clinical isolates of dermatophytes. All plants showed a fungicidal effect against both fungal species, with MIC/MFC values of the active extracts ranging from 15.6 to 250.0 µg/mL. Selected extracts of Eugenia uniflora (AcE), Libidibia ferrea (AE), and Persea americana (AcE) also exhibited a fungicidal effect against all clinical isolates of T. rubrum and T. mentagrophytes complex. This is the first report of the antifungal activity of Schinus terebinthifolius, Piptadenia colubrina, Parapiptadenia rigida, Mimosa ophthalmocentra, and Persea americana against both dermatophyte species.

  18. ANTIFUNGAL POTENTIAL OF PLANT SPECIES FROM BRAZILIAN CAATINGA AGAINST DERMATOPHYTES

    Science.gov (United States)

    BIASI-GARBIN, Renata Perugini; DEMITTO, Fernanda de Oliveira; do AMARAL, Renata Claro Ribeiro; FERREIRA, Magda Rhayanny Assunção; SOARES, Luiz Alberto Lira; SVIDZINSKI, Terezinha Inez Estivalet; BAEZA, Lilian Cristiane; YAMADA-OGATTA, Sueli Fumie

    2016-01-01

    Trichophyton rubrum and Trichophyton mentagrophytes complex, or Trichophyton spp. are the main etiologic agents of dermatophytosis, whose treatment is limited by the high cost of antifungal treatments, their various side effects, and the emergence of resistance amongst these species. This study evaluated the in vitro antidermatophytic activity of 23 crude extracts from nine plant species of semiarid vegetation (caatinga) found in Brazil. The extracts were tested at concentrations ranging from 1.95 to 1,000.0 mg/mL by broth microdilution assay against the reference strains T. rubrum ATCC 28189 and T. mentagrophytesATCC 11481, and 33 clinical isolates of dermatophytes. All plants showed a fungicidal effect against both fungal species, with MIC/MFC values of the active extracts ranging from 15.6 to 250.0 µg/mL. Selected extracts of Eugenia uniflora (AcE), Libidibia ferrea (AE), and Persea americana (AcE) also exhibited a fungicidal effect against all clinical isolates of T. rubrum and T. mentagrophytes complex. This is the first report of the antifungal activity of Schinus terebinthifolius, Piptadenia colubrina, Parapiptadenia rigida, Mimosa ophthalmocentra, and Persea americana against both dermatophyte species. PMID:27007561

  19. ANTIFUNGAL POTENTIAL OF PLANT SPECIES FROM BRAZILIAN CAATINGA AGAINST DERMATOPHYTES

    Directory of Open Access Journals (Sweden)

    Renata Perugini BIASI-GARBIN

    2016-01-01

    Full Text Available Trichophyton rubrum and Trichophyton mentagrophytes complex, or Trichophyton spp. are the main etiologic agents of dermatophytosis, whose treatment is limited by the high cost of antifungal treatments, their various side effects, and the emergence of resistance amongst these species. This study evaluated the in vitro antidermatophytic activity of 23 crude extracts from nine plant species of semiarid vegetation (caatinga found in Brazil. The extracts were tested at concentrations ranging from 1.95 to 1,000.0 mg/mL by broth microdilution assay against the reference strains T. rubrum ATCC 28189 and T. mentagrophytesATCC 11481, and 33 clinical isolates of dermatophytes. All plants showed a fungicidal effect against both fungal species, with MIC/MFC values of the active extracts ranging from 15.6 to 250.0 µg/mL. Selected extracts of Eugenia uniflora (AcE, Libidibia ferrea (AE, and Persea americana (AcE also exhibited a fungicidal effect against all clinical isolates of T. rubrum and T. mentagrophytes complex. This is the first report of the antifungal activity of Schinus terebinthifolius, Piptadenia colubrina, Parapiptadenia rigida, Mimosa ophthalmocentra, and Persea americana against both dermatophyte species.

  20. ZnO and TiO{sub 2} nanoparticles as novel antimicrobial agents for oral hygiene: a review

    Energy Technology Data Exchange (ETDEWEB)

    Khan, Shams Tabrez, E-mail: shamsalig75@gmail.com; Al-Khedhairy, Abdulaziz A. [King Saud University, Department of Zoology, College of Science (Saudi Arabia); Musarrat, Javed [AMU, Department of Agricultural Microbiology, Faculty of Agricultural Sciences (India)

    2015-06-15

    Oral cavity is inhabited by more than 25,000 different bacterial phylotypes; some of them cause systemic infections in addition to dental and periodontal diseases. Emergence of multiple antibiotic resistance among these bacteria necessitates the development of alternative antimicrobial agents that are safe, stable, and relatively economic. This review focuses on the significance of metal oxide nanoparticles, especially zinc oxide and titanium dioxide nanoparticles as supplementary antimicrobials for controlling oral infections and biofilm formation. Indeed, the ZnO NPs and TiO{sub 2} NPs have exhibited significant antimicrobial activity against oral bacteria at concentrations which is not toxic in in vivo toxicity assays. These nanoparticles are being produced at an industrial scale for use in a variety of commercial products including food products. Thus, the application of ZnO and TiO{sub 2} NPs as nanoantibiotics for the development of mouthwashes, dental pastes, and other oral hygiene materials is envisaged. It is also suggested that these NPs could serve as healthier, innocuous, and effective alternative for controlling both the dental biofilms and oral planktonic bacteria with lesser side effects and antibiotic resistance.

  1. Antifungal activity of medicinal plant extracts; preliminary screening studies.

    Science.gov (United States)

    Webster, Duncan; Taschereau, Pierre; Belland, René J; Sand, Crystal; Rennie, Robert P

    2008-01-04

    In the setting of HIV and organ transplantation, opportunistic fungal infections have become a common cause of morbidity and mortality. Thus antifungal therapy is playing a greater role in health care. Traditional plants are a valuable source of novel antifungals. To assess in vitro antifungal activity of aqueous plant extracts. The minimum inhibitory concentrations were determined for each extract in the setting of human pathogenic fungal isolates. Plants were harvested and identification verified. Aqueous extracts were obtained and antifungal susceptibilities determined using serial dilutional extracts with a standardized microdilution broth methodology. Twenty-three fungal isolates were cultured and exposed to the plant extracts. Five known antifungals were used as positive controls. Results were read at 48 and 72 h. Of the 14 plants analyzed, Fragaria virginiana Duchesne, Epilobium angustifolium L. and Potentilla simplex Michx. demonstrated strong antifungal potential overall. Fragaria virginiana had some degree of activity against all of the fungal pathogens. Alnus viridis DC., Betula alleghaniensis Britt. and Solidago gigantea Ait. also demonstrated a significant degree of activity against many of the yeast isolates. Fragaria virginiana, Epilobium angustifolium and Potentilla simplex demonstrate promising antifungal potential.

  2. Oropharyngeal candidiasis and resistance to antifungal drugs in patients receiving radiation for head and neck cancer

    Directory of Open Access Journals (Sweden)

    Maryam Rad DMD, MSc

    2012-04-01

    Full Text Available BACKGROUND: Oropharyngeal candidiasis is a common infection in patient receiving radiotherapy for head and neckcancer. Accurate and rapid identification of candida species is very important in clinical laboratory, because theincidence of candidiasis continues to rise after radiotherapy. The genus Candida has about 154 species that showdifferent level of resistance to antifungal drugs and have high degree of phenotypic similarity. The aim of this study wasto investigate oral yeast colonization and infection and resistance to antifungal drugs in these patients.METHODS: Thirty patients receiving a 6-week course of radiation therapy for treatment of head and neck cancer at theOncology Unit in Shafa Hospital, in 2008, were enrolled in the study. Specimens from patients were cultured weeklyfor Candida. All isolates were plated on CHROM agar and RPMI-based medium. They were subcultured and submittedfor antifungal susceptibility testing (nystatin, fluconazole, clotrimazole and ketoconazole and molecular typing.RESULTS: Infection (clinical and microbiological evidence occurred in 50% of the patients and Candida colonization(only microbiological evidence occurred in 70% of subjects in the first week. Candida albicans alone was isolated in94.9% of patient visits with positive cultures. Candida tropicalis was isolated from 5.1% of patient visits with positivecultures. All isolates were susceptible to nystatin, but did not respond to the other antifungal drugsCONCLUSIONS: The irradiation-induced changes of the intraoral environment such as xerostomia lead to increasedintraoral colonization by Candida species. All yeast isolates were susceptible to nystatin. Thus prophylactic therapywith nystatin should be considered for these patients.

  3. Antifungal susceptibility testing of vaginal candida isolates: the broth microdilution method

    Directory of Open Access Journals (Sweden)

    Mahmoudi Rad M

    2010-02-01

    Full Text Available "n Normal 0 false false false EN-US X-NONE AR-SA MicrosoftInternetExplorer4 /* Style Definitions */ table.MsoNormalTable {mso-style-name:"Table Normal"; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:yes; mso-style-priority:99; mso-style-qformat:yes; mso-style-parent:""; mso-padding-alt:0in 5.4pt 0in 5.4pt; mso-para-margin:0in; mso-para-margin-bottom:.0001pt; mso-pagination:widow-orphan; font-size:11.0pt; font-family:"Calibri","sans-serif"; mso-ascii-font-family:Calibri; mso-ascii-theme-font:minor-latin; mso-fareast-font-family:"Times New Roman"; mso-fareast-theme-font:minor-fareast; mso-hansi-font-family:Calibri; mso-hansi-theme-font:minor-latin; mso-bidi-font-family:Arial; mso-bidi-theme-font:minor-bidi;} Background: Vulvovaginal candidiasis is a common mucosal infection among immunocompetent, healthy women, and is caused by opportunistic yeasts that belong to genus Candida. In this study, we isolated and identified the Candida species in the vagina of patients who admitted in Gynecology Department of Mahdieh Hospital in Tehran, Iran to evaluate the in vitro activities of fluconazole, miconazole, itraconazole and flucytosine against 191 clinical Candida isolates by the NCCLS microdilution method."n"nMethods: 191 Candida were isolated from vaginal secretions and identified with conventional mycological methods in the diagnosis of Candida species. The identity of all strains was confirmed genotypically by multiplex PCR. In vitro susceptibility testing of vaginal Candida isolates was performed by the NCCLS broth microdilution method. The results were read at 48 h."n"nResults: Most C. albicans isolates (>90% were sensitive in vitro to the antifungal agents tested. Most C. glabrata isolates showed sensitivity to miconazole and then flucytosine while they were more resistant to Itraconazole and fluconazole. Many isolates of C. tropicalis were susceptible to miconazole and then fluconazole. They showed a little resistance to

  4. Use of alcohol vinegar in the inhibition of Candida spp. and its effect on the physical properties of acrylic resins

    OpenAIRE

    de Castro, Ricardo Dias; Mota, Ana Carolina Loureiro Gama; de Oliveira Lima, Edeltrudes; Batista, Andr? Ulisses Dantas; de Ara?jo Oliveira, Julyana; Cavalcanti, Alessandro Leite

    2015-01-01

    Background Given the high prevalence of oral candidiasis and the restricted number of antifungal agents available to control infection, this study investigated the in vitro antifungal activity of alcohol vinegar on Candida spp. and its effect on the physical properties of acrylic resins. Methods Tests to determine the Minimum Inhibitory Concentration (MIC) and Minimum Fungicidal Concentration (MFC) of vinegar alcohol (0.04?g/ml of acetic acid) and nystatin (control) were performed. The antifu...

  5. Antifungal, phytotoxic and insecticidal properties of essential oil isolated from Turkish Origanum acutidens and its three components, carvacrol, thymol and p-cymene.

    Science.gov (United States)

    Kordali, Saban; Cakir, Ahmet; Ozer, Hakan; Cakmakci, Ramazan; Kesdek, Memis; Mete, Ebru

    2008-12-01

    The chemical composition of essential oil isolated by hydrodistillation from the aerial parts of Origanum acutidens was analyzed by GC-MS. Carvacrol (87.0%), p-cymene (2.0%), linalool acetate (1.7%), borneol (1.6%) and beta-caryophyllene (1.3%) were found to be as main constituents. Antifungal, phytotoxic and insecticidal activities of the oil and its aromatic monoterpene constituents, carvacrol, p-cymene and thymol were also determined. The antifungal assays showed that O. acutidens oil, carvacrol and thymol completely inhibited mycelial growth of 17 phytopathogenic fungi and their antifungal effects were higher than commercial fungicide, benomyl. However, p-cymene possessed lower antifungal activity. The oil, carvacrol and thymol completely inhibited the seed germination and seedling growth of Amaranthus retroflexus, Chenopodium album and Rumex crispus and also showed a potent phytotoxic effect against these plants. However, p-cymene did not show any phytotoxic effect. Furthermore, O. acutidens oil showed 68.3% and 36.7% mortality against Sitophilus granarius and Tribolium confusum adults, respectively. The findings of the present study suggest that antifungal and herbicidal properties of the oil can be attributed to its major component, carvacrol, and these agents have a potential to be used as fungicide, herbicide as well as insecticide.

  6. INVESTIGATION OF ANTIFUNGAL ACTIVITY OF QUINOLINIUM DERIVATIVES

    Directory of Open Access Journals (Sweden)

    G. A. Alexandrova

    2013-01-01

    Full Text Available Abstract. Antifungal activity (Candida albicans, Candida krusei of some substituted quinolinium derivatives has been investigated. It was established that the most perspective compound for detail investigation of antifungal activity by labeled biomarkers method was N-phenylbenzoquinaldinium tetrafluoroborate.

  7. Antifungal activity of the pygidial gland secretion of Laemostenus punctatus (Coleoptera: Carabidae) against cave-dwelling micromycetes

    Science.gov (United States)

    Nenadić, Marija; Ljaljević-Grbić, Milica; Stupar, Miloš; Vukojević, Jelena; Ćirić, Ana; Tešević, Vele; Vujisić, Ljubodrag; Todosijević, Marina; Vesović, Nikola; Živković, Nemanja; Ćurčić, Srećko

    2017-06-01

    The antifungal potential of the pygidial gland secretion of the troglophilic ground beetle Laemostenus punctatus from a cave in Southeastern Serbia against cave-dwelling micromycetes, isolated from the same habitat, has been investigated. Eleven collected samples were analyzed and 32 isolates of cave-dwelling fungi were documented. A total of 14 fungal species were identified as members of the genera Aspergillus, Penicillium, Alternaria, Cladosporium, Rhizopus, Trichoderma, Arthrinium, Aureobasidium, Epicoccum, Talaromyces, and Fusarium. Five isolates were selected for testing the antifungal activity of the pygidial gland secretion: Talaromyces duclauxi, Aspergillus brunneouniseriatus, Penicillium sp., Rhizopus stolonifer, and Trichoderma viride. The microdilution method has been applied to detect minimal inhibitory concentrations (MICs) and minimal fungicidal concentrations (MFCs). The most sensitive isolate was Penicillium sp., while the other isolates demonstrated a high level of resistance to the tested agent. L. punctatus has developed a special mechanism of producing specific compounds that act synergistically within the secretion mixture, which are responsible for the antifungal action against pathogens from the cave. The results open opportunities for further research in the field of ground beetle defense against pathogens, which could have an important application in human medicine, in addition to the environmental impact, primarily.

  8. Triazole derivatives with improved in vitro antifungal activity over azole drugs

    Directory of Open Access Journals (Sweden)

    Yu S

    2014-04-01

    Full Text Available Shichong Yu,1,* Xiaoyun Chai,1,* Yanwei Wang,1 Yongbing Cao,2 Jun Zhang,3 Qiuye Wu,1 Dazhi Zhang,1 Yuanying Jiang,2 Tianhua Yan,4 Qingyan Sun11Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai, People's Republic of China; 2Drug Research Center, School of Pharmacy, Second Military Medical University, Shanghai, People's Republic of China; 3Overseas Education Faculty of the Second Military Medical University, Shanghai, People's Republic of China; 4Department of Pharmacology, School of Pharmacy, China Pharmaceutical University, Nanjing, People's Republic of China*These authors contributed equally to this workAbstract: A series of triazole antifungal agents with piperidine side chains was designed and synthesized. The results of antifungal tests against eight human pathogenic fungi in vitro showed that all the compounds exhibited moderate-to-excellent activities. Molecular docking between 8d and the active site of Candida albicans CYP51 was provided based on the computational docking results. The triazole interacts with the iron of the heme group. The difluorophenyl group is located in the S3 subsite and its fluorine atom (2-F can form H-bonds with Gly307. The side chain is oriented into the S4 subsite and formed hydrophobic and van der Waals interactions with the amino residues. Moreover, the phenyl group in the side chain interacts with the phenol group of Phe380 through the formation of π–π face-to-edge interactions.Keywords: synthesis, CYP51, molecular docking, azole agents

  9. Antifungal Poly(lactic acid Films Containing Thymol and Carvone

    Directory of Open Access Journals (Sweden)

    Boonruang Kanchana

    2016-01-01

    Full Text Available The goal of this study was to develop antifungal poly(lactic acid films for food packaging applications. The antifungal compounds, thymol and R-(--carvone were incorporated into poly(lactic acid (PLA-based polymer at 10, 15 and 20% by weight. Film converting process consists of three steps including melt blending, sheet extrusion and biaxial stretching. The incorporation of antifungal compounds into the polymer matrix resulted in decreased Tg and Tm, increased gas permeabilility, reduced tensile strength and increased elongation at break of the antifungal PLA films.

  10. Systematic review of antimicrobials, mucosal coating agents, anesthetics, and analgesics for the management of oral mucositis in cancer patients

    NARCIS (Netherlands)

    Saunders, Deborah P.; Epstein, Joel B.; Elad, Sharon; Allemano, Justin; Bossi, Paolo; van de Wetering, Marianne D.; Rao, Nikhil G.; Potting, Carin; Cheng, Karis K.; Freidank, Annette; Brennan, Michael T.; Bowen, Joanne; Dennis, Kristopher; Lalla, Rajesh V.

    2013-01-01

    The aim of this project was to develop clinical practice guidelines on the use of antimicrobials, mucosal coating agents, anesthetics, and analgesics for the prevention and management of oral mucositis (OM) in cancer patients. A systematic review of the available literature was conducted. The body

  11. Systematic review of antimicrobials, mucosal coating agents, anesthetics, and analgesics for the management of oral mucositis in cancer patients.

    NARCIS (Netherlands)

    Saunders, D.P.; Epstein, J.B.; Elad, S.; Allemano, J.; Bossi, P.; Wetering, M.D. van de; Rao, N.G.; Potting, C.M.J.; Cheng, K.K.; Freidank, A.; Brennan, M.T.; Bowen, J.; Dennis, K.; Lalla, R.V.

    2013-01-01

    PURPOSE: The aim of this project was to develop clinical practice guidelines on the use of antimicrobials, mucosal coating agents, anesthetics, and analgesics for the prevention and management of oral mucositis (OM) in cancer patients. METHODS: A systematic review of the available literature was

  12. Identification and characterization of a dual-acting antinematodal agent against the pinewood nematode, Bursaphelenchus xylophilus.

    Directory of Open Access Journals (Sweden)

    Wan-Suk Oh

    Full Text Available The pinewood nematode (PWN, Bursaphelenchus xylophilus, is a mycophagous and phytophagous pathogen responsible for the current widespread epidemic of the pine wilt disease, which has become a major threat to pine forests throughout the world. Despite the availability of several preventive trunk-injection agents, no therapeutic trunk-injection agent for eradication of PWN currently exists. In the characterization of basic physiological properties of B. xylophilus YB-1 isolates, we established a high-throughput screening (HTS method that identifies potential hits within approximately 7 h. Using this HTS method, we screened 206 compounds with known activities, mostly antifungal, for antinematodal activities and identified HWY-4213 (1-n-undecyl-2-[2-fluorphenyl] methyl-3,4-dihydro-6,7-dimethoxy-isoquinolinium chloride, a highly water-soluble protoberberine derivative, as a potent nematicidal and antifungal agent. When tested on 4 year-old pinewood seedlings that were infected with YB-1 isolates, HWY-4213 exhibited a potent therapeutic nematicidal activity. Further tests of screening 39 Caenorhabditis elegans mutants deficient in channel proteins and B. xylophilus sensitivity to Ca(2+ channel blockers suggested that HWY-4213 targets the calcium channel proteins. Our study marks a technical breakthrough by developing a novel HTS method that leads to the discovery HWY-4213 as a dual-acting antinematodal and antifungal compound.

  13. Identification and characterization of a dual-acting antinematodal agent against the pinewood nematode, Bursaphelenchus xylophilus.

    Science.gov (United States)

    Oh, Wan-Suk; Jeong, Pan-Young; Joo, Hyoe-Jin; Lee, Jeong-Eui; Moon, Yil-Seong; Cheon, Hyang-Mi; Kim, Jung-Ho; Lee, Yong-Uk; Shim, Yhong-Hee; Paik, Young-Ki

    2009-11-11

    The pinewood nematode (PWN), Bursaphelenchus xylophilus, is a mycophagous and phytophagous pathogen responsible for the current widespread epidemic of the pine wilt disease, which has become a major threat to pine forests throughout the world. Despite the availability of several preventive trunk-injection agents, no therapeutic trunk-injection agent for eradication of PWN currently exists. In the characterization of basic physiological properties of B. xylophilus YB-1 isolates, we established a high-throughput screening (HTS) method that identifies potential hits within approximately 7 h. Using this HTS method, we screened 206 compounds with known activities, mostly antifungal, for antinematodal activities and identified HWY-4213 (1-n-undecyl-2-[2-fluorphenyl] methyl-3,4-dihydro-6,7-dimethoxy-isoquinolinium chloride), a highly water-soluble protoberberine derivative, as a potent nematicidal and antifungal agent. When tested on 4 year-old pinewood seedlings that were infected with YB-1 isolates, HWY-4213 exhibited a potent therapeutic nematicidal activity. Further tests of screening 39 Caenorhabditis elegans mutants deficient in channel proteins and B. xylophilus sensitivity to Ca(2+) channel blockers suggested that HWY-4213 targets the calcium channel proteins. Our study marks a technical breakthrough by developing a novel HTS method that leads to the discovery HWY-4213 as a dual-acting antinematodal and antifungal compound.

  14. ANTIFUNGAL ACTIVITY OF SILVER NANOPARTICLES OBTAINED BY GREEN SYNTHESIS

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    Eduardo José J. MALLMANN

    2015-04-01

    Full Text Available Silver nanoparticles (AgNPs are metal structures at the nanoscale. AgNPs have exhibited antimicrobial activities against fungi and bacteria; however synthesis of AgNPs can generate toxic waste during the reaction process. Accordingly, new routes using non-toxic compounds have been researched. The proposal of the present study was to synthesize AgNPs using ribose as a reducing agent and sodium dodecyl sulfate (SDS as a stabilizer. The antifungal activity of these particles against C. albicans and C. tropicalis was also evaluated. Stable nanoparticles 12.5 ± 4.9 nm (mean ± SD in size were obtained, which showed high activity against Candida spp. and could represent an alternative for fungal infection treatment.

  15. Comparison of oral ketamine and oral midazolam as sedative agents in pediatric dentistry

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    Damle S

    2008-09-01

    Full Text Available The safe and effective treatment of uncooperative or combative preschool children with extensive dental needs is one of pediatric dentist′s ongoing challenges. The traditional methods of behavior management are no longer acceptable to parents as they are not ready to spare more time for dental treatment of their children. Keeping this in mind, the present study was designed and carried out to evaluate the sedative effects of oral ketamine and oral midazolam prior to general anesthesia. Twenty uncooperative children in the age-group of 2-6 years were selected after thorough medical examination and investigations. Informed consent was obtained from the parent. This was a randomized double-blind study. An anesthesiologist administered either 0.5 mg/kg midazolam or 5 mg/kg ketamine orally. The heart rate, respiratory rate, and oxygen saturation were recorded at regular intervals. The sedation and anxiolysis scores were also recorded. The parents were asked to answer a questionnaire at the follow-up session the next day on the surgical experience of the parent and the child and side effects experienced, if any. When the data was subjected to statistical analysis, it was observed that both drugs resulted in adequate sedation at the end of 30 min, with oral midazolam providing significantly better anxiolysis. The heart rate and respiratory rate were marginally higher with oral ketamine. The questionnaire revealed a better response with oral midazolam; side effects were more prominent with oral ketamine.

  16. Differential effects of antifungal agents on expression of genes related to formation of Candida albicans biofilms.

    Science.gov (United States)

    Chatzimoschou, Athanasios; Simitsopoulou, Maria; Antachopoulos, Charalampos; Walsh, Thomas J; Roilides, Emmanuel

    2016-01-01

    The purpose of this study was to analyse specific molecular mechanisms involved in the intrinsic resistance of C. albicans biofilms to antifungals. We investigated the transcriptional profile of three genes (BGL2, SUN41, ECE1) involved in Candida cell wall formation in response to voriconazole or anidulafungin after the production of intermediate and mature biofilms. C. albicans M61, a well-documented biofilm producer strain, was used for the development of intermediate (12 h and 18 h) and completely mature biofilms (48 h). After exposure of cells from each biofilm growth mode to voriconazole (128 and 512 mg l(-1)) or anidulafungin (0.25 and 1 mg l(-1)) for 12-24 h, total RNA samples extracted from biofilm cells were analysed by RT-PCR. The voriconazole and anidulafungin biofilm MIC was 512 and 0.5 mg l(-1) respectively. Anidulafungin caused significant up-regulation of SUN41 (3.7-9.3-fold) and BGL2 (2.2-2.8 fold) in intermediately mature biofilms; whereas, voriconazole increased gene expression in completely mature biofilms (SUN41 2.3-fold, BGL2 2.1-fold). Gene expression was primarily down-regulated by voriconazole in intermediately, but not completely mature biofilms. Both antifungals caused down-regulation of ECE1 in intermediately mature biofilms. © 2015 Blackwell Verlag GmbH.

  17. Antifungal mechanisms of ZnO and Ag nanoparticles to Sclerotinia homoeocarpa

    Science.gov (United States)

    Li, Junli; Sang, Hyunkyu; Guo, Huiyuan; Popko, James T.; He, Lili; White, Jason C.; Parkash Dhankher, Om; Jung, Geunhwa; Xing, Baoshan

    2017-04-01

    Fungicides have extensively been used to effectively combat fungal diseases on a range of plant species, but resistance to multiple active ingredients has developed in pathogens such as Sclerotinia homoeocarpa, the causal agent of dollar spot on cool-season turfgrasses. Recently, ZnO and Ag nanoparticles (NPs) have received increased attention due to their antimicrobial activities. In this study, the NPs’ toxicity and mechanisms of action were investigated as alternative antifungal agents against S. homoeocarpa isolates that varied in their resistance to demethylation inhibitor (DMI) fungicides. S. homoeocarpa isolates were treated with ZnO NPs and ZnCl2 (25-400 μg ml-1) and Ag NPs and AgNO3 (5-100 μg ml-1) to test antifungal activity of the NPs and ions. The mycelial growth of S. homoeocarpa isolates regardless of their DMI sensitivity was significantly inhibited on ZnO NPs (≥200 μg ml-1), Ag NPs (≥25 μg ml-1), Zn2+ ions (≥200 μg ml-1), and Ag+ ions (≥10 μg ml-1) amended media. Expression of stress response genes, glutathione S-transferase (Shgst1) and superoxide dismutase 2 (ShSOD2), was significantly induced in the isolates by exposure to the NPs and ions. In addition, a significant increase in the nucleic acid contents of fungal hyphae, which may be due to stress response, was observed upon treatment with Ag NPs using Raman spectroscopy. We further observed that a zinc transporter (Shzrt1) might play an important role in accumulating ZnO and Ag NPs into the cells of S. homoeocarpa due to overexpression of Shzrt1 significantly induced by ZnO or Ag NPs within 3 h of exposure. Yeast mutants complemented with Shzrt1 became more sensitive to ZnO and Ag NPs as well as Zn2+ and Ag+ ions than the control strain and resulted in increased Zn or Ag content after exposure. This is the first report of involvement of the zinc transporter in the accumulation of Zn and Ag from NP exposure in filamentous plant pathogenic fungi. Understanding the molecular

  18. Bacterial and fungal keratitis in Upper Egypt: In vitro screening of enzymes, toxins and antifungal activity

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    Abdullah A Gharamah

    2014-01-01

    Full Text Available Purpose: This work was conducted to study the ability of bacterial and fungal isolates from keratitis cases in Upper Egypt to produce enzymes, toxins, and to test the isolated fungal species sensitivity to some therapeutic agents. Materials and Methods: One hundred and fifteen patients clinically diagnosed to have microbial keratitis were investigated. From these cases, 37 bacterial isolates and 25 fungal isolates were screened for their ability to produce extra-cellular enzymes in solid media. In addition, the ability of fungal isolates to produce mycotoxins and their sensitivity to 4 antifungal agents were tested. Results: Protease, lipase, hemolysins, urease, phosphatase, and catalase were detected respectively in 48.65%, 37.84%, 59.46%, 43.24%, 67.57%, and 100% out of 37 bacterial isolates tested. Out of 25 fungal isolates tested during the present study, 80% were positive for protease, 84% for lipase and urease, 28% for blood hemolysis, and 100% for phosphatase and catalase enzymes. Thirteen fungal isolates were able to produce detectable amounts of 7 mycotoxins in culture medium (aflatoxins (B1, B2, G1, and G2, sterigmatocystin, fumagillin, diacetoxyscirpenol, zearalenone, T-2 toxin, and trichodermin. Among the antifungal agents tested in this study, terbinafine showed the highest effect against most isolates in vitro. Conclusion: In conclusion, the ability of bacterial and fungal isolates to produce extracellular enzymes and toxins may be aid in the invasion and destruction of eye tissues, which, in turn, lead to vision loss.

  19. Purification and characterisation of a novel chitinase from persimmon (Diospyros kaki) with antifungal activity.

    Science.gov (United States)

    Zhang, Jianzhi; Kopparapu, Narasimha Kumar; Yan, Qiaojuan; Yang, Shaoqing; Jiang, Zhengqiang

    2013-06-01

    A novel chitinase from the persimmon fruit was isolated, purified and characterised in this report. The Diospyros kaki chitinase (DKC) was found to be a monomer with a molecular mass of 29 kDa. It exhibited optimal activity at pH 4.5 with broad pH stability from pH 4.0-9.0. It has an optimal temperature of 60°C and thermostable up to 60°C when incubated for 30 min. The internal peptide sequences of DKC showed similarity with other reported plant chitinases. It has the ability to hydrolyse colloidal chitin into chito-oligomers such as chitotriose, chitobiose and into its monomer N-acetylglucosamine. It can be used to degrade chitin waste into useful products such as chito-oligosacchaarides. DKC exhibited antifungal activity towards pathogenic fungus Trichoderma viride. Chitinases with antifungal property can be used as biocontrol agents replacing chemical fungicides. Copyright © 2012 Elsevier Ltd. All rights reserved.

  20. Antifungal activity of rimocidin and a new rimocidin derivative BU16 produced by Streptomyces mauvecolor BU16 and their effects on pepper anthracnose.

    Science.gov (United States)

    Jeon, B J; Kim, J D; Han, J W; Kim, B S

    2016-05-01

    The objective of this study was to explore antifungal metabolites targeting fungal cell envelope and to evaluate the control efficacy against anthracnose development in pepper plants. A natural product library comprising 3000 microbial culture extracts was screened via an adenylate kinase (AK)-based cell lysis assay to detect antifungal metabolites targeting the cell envelope of plant-pathogenic fungi. The culture extract of Streptomyces mauvecolor strain BU16 displayed potent AK-releasing activity. Rimocidin and a new rimocidin derivative, BU16, were identified from the extract as active constituents. BU16 is a tetraene macrolide containing a six-membered hemiketal ring with an ethyl group side chain instead of the propyl group in rimocidin. Rimocidin and BU16 showed broad-spectrum antifungal activity against various plant-pathogenic fungi and demonstrated potent control efficacy against anthracnose development in pepper plants. Antifungal metabolites produced by S. mauvecolor strain BU16 were identified to be rimocidin and BU16. The compounds displayed potent control efficacy against pepper anthracnose. Rimocidin and BU16 would be active ingredients of disease control agents disrupting cell envelope of plant-pathogenic fungi. The structure and antifungal activity of rimocidin derivative BU16 is first described in this study. © 2016 The Society for Applied Microbiology.

  1. In vitro antifungal activity of Ocimum selloi essential oil and methylchavicol against phytopathogenic fungi1

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    Larissa Corrêa Bomfim Costa

    Full Text Available The efficacy of Ocimum selloi essential oil was evaluated for controlling the growth of mycelia and spores germination Moniliophthora perniciosa. Six compounds (99.89% of the total oil were identified by GC-MS, of which methyl chavicol, methyl eugenol, β-caryophyllene, germacrene-D, bicyclogermacrene and spathulenol. Essential oil was tested for antifungal activity, which was determined by disc diffusion and minimum inhibitory concentration (MIC determination methods. Application of the oil reduced mycelial growth in a dose dependent manner, with maximum inhibition being observed at concentration of 1,000 ppm. Such antifungal activity could be attributed to methyl chavicol since the pure compound was shown to be similarly effective against Moniliophthora perniciosa at 1,000 ppm. The oil when applied at a concentration of 1,000 ppm, reduced the spore germination of Colletotrichum gloeosporioides and M. perniciosa by 93 and 87%, respectively, but had no effect on the Alternaria alternata. It is concluded that the oil from O. selloi and its major constituent, methyl chavicol, are efficient in inhibiting M. perniciosa, but less effective against C. gloeosporioides and A. alternata. The results obtained from this work may contribute to the development of alternative anti-fungal agents to protect the cacao crop from fungal disease.

  2. Perfil de suscetibilidade a antifúngicos de dermatófitos isolados de pacientes com insuficiência renal crônica Antifungal susceptibility of dermatophytes isolated from patients with chronic renal failure

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    Cibele Massotti Magagnin

    2011-08-01

    . Treatment requires the use of topical and/or systemic antifungal drugs. The efficacy of antifungal agents for the treatment of dermatophytosis has yet to be evaluated. Studies evaluating the in vitro activity of antifungal agents are rare, particularly in filamentous fungi. OBJECTIVE: To evaluate the susceptibility profile of different species of dermatophytes isolated from patients with chronic renal failure to nine antifungal drugs available on the market for the treatment of dermatophytosis. METHODS: Twenty-six isolates of dermatophytes obtained from patients with chronic renal failure were analyzed with respect to their susceptibility to nine antifungal agents (ketoconazole, ciclopirox olamine, fluconazole, griseofulvin, itraconazole, miconazole, piroctone olamine, terbinafine and tioconazole, using the broth microdilution method proposed by the Clinical and Laboratory Standards Institute (CLSI and adapted for dermatophytes. RESULTS: Of the antifungal agents tested, the best results in terms of sensitivity were found with terbinafine and tioconazole, while the antifungal activity of fluconazole was found to be weak, particularly against strains of M. gypseum. Ciclopirox olamine, although less effective than terbinafine, also yielded satisfactory results. CONCLUSIONS: In general, the sensitivity profile of the antifungal agents tested in this study was similar to results obtained in previous studies, confirming the need to determine which species is causing the dermatophytosis given that antifungal susceptibility varies from one species to another. Furthermore, the present findings show the importance of conducting in vitro sensitivity tests, since the sensitivity profile may differ among isolates of the same species

  3. Optimization of Bacillus aerius strain JS-786 cell dry mass and its antifungal activity against Botrytis cinerea using response surface methodology

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    Shafi Jamil

    2017-01-01

    Full Text Available The optimization of fermentation conditions is necessary for field application of biological control agents. The present study was designed to optimize the fermentation conditions for the Bacillus aerius strain, JS-786 in terms of cell dry mass and its antifungal activity against Botrytis cinerea with response surface methodology. A strain of bacteria with strong antifungal activity was isolated from the phyllosphere of tomato plant and identified as B. aerius JS-786 based on the sequence homology of its 16S rRNA gene. After the success of preliminary antifungal activity tests, response surface methodology was used to optimize the fermentation conditions (medium pH, gelatin percentage, incubation period, rotatory speed and incubation temperature to maximize the cell dry mass and antifungal activity against B. cinerea. A 25 factorial central composite design was employed and multiple response optimization was used to determine the desirability of the operation. The results of regression analysis showed that at the individual level, all of the experimental parameters were significant for cell dry mass; significant results were obtained for antifungal activity pH, incubation period, rotatory speed and incubation temperature. The interactive effect of the incubation period, rotatory speed and incubation temperature was significant. Maximum cell dry mass (8.7 g/L and inhibition zone (30.4 mm were obtained at pH 6.4, gelatin 3.2%, incubation period 36.92 h, rotatory speed 163 rpm, and temperature 33.5°C. This study should help to formulate a more rational and cost-effective biological product both in terms of bacterial growth and antifungal activity.

  4. Clinico-mycological and Antifungal Susceptibility Profiles of Candiduria in A Tertiary Care Hospital From South India

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    Dinoop Korol Ponnambath

    2017-10-01

    Full Text Available Introduction: Candida is one of the common causative agent of Urinary Tract Infections (UTI worldwide. The most common reported species causing UTI is Candida albicans. Incidence of UTI due to non-albicans Candida species. is on rise in recent years because of their better adaptability and increased resistance to antifungals. Susceptibility profile reports of various Candida species. to newer azoles like voriconazole and betaglucan inhibitors (e.g., caspofungin are deficient in India, since the reference broth microdilution method is not widely utilized. In this study, a rapid reliable and easier alternative, VITEK 2 compact system was utilized to determine the antifungal susceptibility profile. Aim: To analyse the clinical and mycological profile with determination of drug susceptibility pattern of Candida isolates from urine samples. Materials and Methods: This observational study was conducted in PSG Institute of Medical Sciences and Research, during April to September 2015. Candida isolated with a colony count of ≥103 CFU/ml of urine from clinically suspected cases of UTI were included in the study. Urine samples (n=3821 from clinically suspected UTI cases (n=3821 were subjected to microscopic examination and semi quantitative estimation of yeast culture obtained by inoculated of calibrated volume of urine onto blood, Mac-conkey and HiCrome UTI agar. Clinical parameters of the cases were obtained for analysis. Speciation of Candida was performed using germ tube test, observation of morphology in corn-meal agar and pigment production in HiChrome Candida differential agar. Confirmation of the species identification and anti-fungal susceptibility profile were obtained using VITEK-2 compact system. Results: Total 101 patients were identified with significant candiduria. Community-Acquired Candiduria (CAC was seen in 11 (10.8% of the cases. 23 (22.7% cases of candiduria were associated with pyuria. Concomitant candidemia was observed in 4 (3

  5. ArtinM offers new perspectives in the development of antifungal therapy

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    Luciana Pereira Ruas

    2012-06-01

    Full Text Available The thermally dimorphic fungus Paracoccidioides brasiliensis is the causative agent of paracoccidioidomycosis (PCM, the most frequent systemic mycosis that affects the rural populations in Latin America. Despite significant developments in antifungal chemotherapy, its efficacy remains limited since drug therapy is prolonged and associated with toxic side effects and relapses. In response to these challenges, it is now recognized that several aspects of antifungal immunity can be modulated to better deal with fungal infections. A common idea for halting fungal infections has been the need to activate a cell-based, pro-inflammatory Th1 immune response to improve the fungal elimination. ArtinM, a D-mannose binding lectin from Artocarpus heterophyllus, has the property of modulating immunity against several intracellular pathogens. Here, we review the immunomodulatory activity of ArtinM during experimental PCM in mice. Both prophylactic and therapeutic protocols of ArtinM administration promotes a Th1 immune response balanced by IL-10, which outstandingly reduces the fungal load in organs of the treated mice while maintaining a controlled inflammation at the site of infection. A carbohydrate recognition based interaction of ArtinM

  6. Oral available agents in the treatment of relapsing remitting multiple sclerosis an overview of merits and culprits

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    Thöne J

    2013-02-01

    Full Text Available Jan Thöne, Gisa Ellrichmann Department of Neurology, St Josef-Hospital Bochum, Ruhr-University Bochum, Bochum, Germany Abstract: Multiple sclerosis (MS is a chronic immunological disease of the central nervous system characterized by early inflammatory demyelination and subsequent neurodegeneration. Major therapeutic progress has occurred during the past decade, in particular since the introduction of immunomodulatory agents, however, MS is still an incurable disease. In addition, parenteral application of the currently licensed drugs is associated with injection-related adverse events (AEs and low patient compliance. Thus, there remains an unmet need for the development of more effective and well tolerated oral therapies for the treatment of MS. A number of new orally administered agents including fingolimod, laquinimod, teriflunomide, cladribine, and BG-12 have been licensed recently or are currently under investigation in relapsing remitting MS patients. In multi-center, randomized, placebo-controlled phase III clinical studies, all of these agents have already shown their efficacy on both clinical disease parameters and magnetic resonance imaging-based measures of disease activity in patients with relapsing remitting MS. However, there are essential differences concerning their clinical efficacy and side-effect profiles. Additionally, the mechanisms by which these substances exert clinical efficacy have not been fully elucidated. In this article, we review the pharmaceutical properties of fingolimod, laquinimod, teriflunomide, cladribine, and BG-12; and their suggested mechanisms of action, clinical efficacy, and side-effect profiles. Keywords: cladribine, fingolimod (FTY, fumaric acid esters (BG-12, laquinimod, teriflunomide

  7. An alternative anionic bio-sustainable anti-fungal agent: Investigation of its mode of action on the fungal cell membrane.

    Science.gov (United States)

    Stenbæk, Jonas; Löf, David; Falkman, Peter; Jensen, Bo; Cárdenas, Marité

    2017-07-01

    The potential of a lactylate (the sodium caproyl lactylate or C10 lactylate), a typical food grade emulsifier, as an anionic environmental friendly anti-fungal additive was tested in growth medium and formulated in a protective coating for exterior wood. Different laboratory growth tests on the blue stain fungus Aureobasidium pullulans were performed and its interactions on a model fungal cell membrane were studied. Promising short term anti-fungal effects in growth tests were observed, although significant but less dramatic effects took place in coating test on wood panels. Scanning electron microscope analysis shows clear differences in the amount of fungal slime on the mycelium of Aureobasidium pullulans when the fungus was exposed of C10 lactylate. This could indicate an effect on the pullulan and melanin production by the fungus. Moreover, the interaction studies on model fungal cell membranes show that C10 lactylate affects the phospholipid bilayer in a similar manner to other negative charged detergents. Copyright © 2017 Elsevier Inc. All rights reserved.

  8. Comparative study on antifungal activities of chitosan nanoparticles and chitosan silver nano composites against Fusarium oxysporum species complex.

    Science.gov (United States)

    Dananjaya, S H S; Erandani, W K C U; Kim, Cheol-Hee; Nikapitiya, Chamilani; Lee, Jehee; De Zoysa, Mahanama

    2017-12-01

    Though the metal nanoparticles (NPs) have been shown favorable results against fungal diseases, erratic environmental toxicity of NPs have raised serious concerns against their applications. Hence, it is vital to modify antifungal compounds into safe substitutes over synthetic chemicals. In this study, antifungal effects of chitosan nanoparticles (CNPs) and chitosan silver nanocomposites (CAgNCs) were compared against Fusarium oxysporum species complex. CNPs and CAgNCs were synthesized, characterized and compared based on the transmission electron microscope, X-ray diffraction, UV-vis absorbance spectra, particle size distribution, zeta potential and thermal stability analysis. Ultra-structural analysis on mycelium membrane of treated F. oxysporum showed that CNPs and CAgNCs could induce a pronounced membrane damage and disruption of the mycelium surface, increase the membrane permeability, and even cell disintegration. CAgNCs showed a significantly higher radial growth inhibition than CNPs in all the tested concentrations. Both CNPs and CAgNCs were not only effective in reducing the fungal growth, but also caused morphological and ultrastructural changes in the pathogen, thereby suggesting its usage as an antifungal dispersion system to control F. oxysporum. Additionally, CNPs and CAgNCs therapy reduced the F. oxysporum infection in zebrafish. Data demonstrates biologically active CNPs and CAgNCs are promising antifungal agents against F. oxysporum. Copyright © 2017 Elsevier B.V. All rights reserved.

  9. Antifungal activity of wide band gap Thioglycolic acid capped ZnS:Mn semiconductor nanoparticles against some pathogenic fungi

    International Nuclear Information System (INIS)

    Ibrahim, Isam M.; Ali, Iftikhar M.; Dheeb, Batol Imran; Abas, Qayes A.; Asmeit Ramizy; Eisa, M.H.; Aljameel, A.I.

    2017-01-01

    The manganese doped zinc sulfide nanoparticles were synthesized by simple aqueous chemical reaction of manganese chloride, zinc acetate and thioacitamide in aqueous solution. Thioglycolic acid is used as capping agent for controlling the nanoparticle size. The main advantage of the ZnS:Mn nanoparticles of diameter ~ 2.73 nm is that the sample is prepared by using non-toxic precursors in a cost effective and eco-friendly way. The structural, morphological and chemical composition of the nanoparticles have been investigated by X-ray diffraction (XRD), Scanning Electron Microscopy (SEM) with energy dispersion spectroscopy (EDS) and Fourier transform infrared (FTIR) spectroscopy. The nanosize of the prepared nanoparticles was elucidated by Scanning Electron Microscopy (SEM). FTIR result ensures that Thioglycolic acid is well bonded on the surface of ZnS:Mn NPs. The antifungal effects of Thioglycolic acid capped ZnS:Mn nanoparticles exhibited a potent antifungal activity against tested fungal strains, so deserving further investigation for clinical applications. The antifungal property of manganese doped zinc sulphide nanoparticles is attributed to the generation of reactive oxygen species due to the interaction of nanoparticles with water. Additionally, the presence of Zn and S in the zone of inhibition area leads to perturbation of fungi cell membranes resulting in growth inhibition. - Highlights: • The manganese doped zinc sulfide nanoparticles were synthesized. • Thioglycolic acid is used as capping agent for controlling the nanoparticle size. • The structural, morphological and chemical composition of the nanoparticles has been investigated. • The presence of Zn and S in the zone of inhibition area leads to perturbation of fungi cell membranes.

  10. Antifungal activity of wide band gap Thioglycolic acid capped ZnS:Mn semiconductor nanoparticles against some pathogenic fungi

    Energy Technology Data Exchange (ETDEWEB)

    Ibrahim, Isam M.; Ali, Iftikhar M. [Department of physics, College of Science, Baghdad University, Baghdad (Iraq); Dheeb, Batol Imran [Department of Biology, College of Education, Iraqia University, Baghdad (Iraq); Abas, Qayes A. [Department of physics, College of Education, University of Anbar, Anbar (Iraq); Asmeit Ramizy, E-mail: asmat_hadithi@yahoo.com [Department of physics, College of Science, University of Anbar, Anbar (Iraq); Renewable energy Research Center, University of Anbar, Anbar (Iraq); Eisa, M.H. [Department of physics, College of Science, Sudan University of Science Technology, Khartoum 11113 (Sudan); Department of physics, College of Science, Al Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh 11623 (Saudi Arabia); Aljameel, A.I. [Department of physics, College of Science, Al Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh 11623 (Saudi Arabia)

    2017-04-01

    The manganese doped zinc sulfide nanoparticles were synthesized by simple aqueous chemical reaction of manganese chloride, zinc acetate and thioacitamide in aqueous solution. Thioglycolic acid is used as capping agent for controlling the nanoparticle size. The main advantage of the ZnS:Mn nanoparticles of diameter ~ 2.73 nm is that the sample is prepared by using non-toxic precursors in a cost effective and eco-friendly way. The structural, morphological and chemical composition of the nanoparticles have been investigated by X-ray diffraction (XRD), Scanning Electron Microscopy (SEM) with energy dispersion spectroscopy (EDS) and Fourier transform infrared (FTIR) spectroscopy. The nanosize of the prepared nanoparticles was elucidated by Scanning Electron Microscopy (SEM). FTIR result ensures that Thioglycolic acid is well bonded on the surface of ZnS:Mn NPs. The antifungal effects of Thioglycolic acid capped ZnS:Mn nanoparticles exhibited a potent antifungal activity against tested fungal strains, so deserving further investigation for clinical applications. The antifungal property of manganese doped zinc sulphide nanoparticles is attributed to the generation of reactive oxygen species due to the interaction of nanoparticles with water. Additionally, the presence of Zn and S in the zone of inhibition area leads to perturbation of fungi cell membranes resulting in growth inhibition. - Highlights: • The manganese doped zinc sulfide nanoparticles were synthesized. • Thioglycolic acid is used as capping agent for controlling the nanoparticle size. • The structural, morphological and chemical composition of the nanoparticles has been investigated. • The presence of Zn and S in the zone of inhibition area leads to perturbation of fungi cell membranes.

  11. Differential Antifungal Activity of Human and Cryptococcal Melanins with Structural Discrepancies

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    Néstor Correa

    2017-07-01

    Full Text Available Melanin is a pigment found in all biological kingdoms, and plays a key role in protection against ultraviolet radiation, oxidizing agents, and ionizing radiation damage. Melanin exerts an antimicrobial activity against bacteria, fungi, and parasites. We demonstrated an antifungal activity of synthetic and human melanin against Candida sp. The members of the Cryptococcus neoformans and C. gattii species complexes are capsulated yeasts, which cause cryptococcosis. For both species melanin is an important virulence factor. To evaluate if cryptococcal and human melanins have antifungal activity against Cryptococcus species they both were assayed for their antifungal properties and physico-chemical characters. Melanin extracts from human hair and different strains of C. neoformans (n = 4 and C. gattii (n = 4 were investigated. The following minimum inhibitory concentrations were found for different melanins against C. neoformans and C. gattii were (average/range: 13.7/(7.8–15.6 and 19.5/(15.6–31.2 μg/mL, respectively, for human melanin; 273.4/(125–>500 and 367.2/(125.5–>500 μg/mL for C. neoformans melanin and 125/(62.5–250 and 156.2/(62–250 μg/mL for C. gattii melanin. Using Scanning Electron Microscopy we observed that human melanin showed a compact conformation and cryptococcal melanins exposed an amorphous conformation. Infrared spectroscopy (FTIR showed some differences in the signals related to C-C bonds of the aromatic ring of the melanin monomers. High Performance Liquid Chromatography established differences in the chromatograms of fungal melanins extracts in comparison with human and synthetic melanin, particularly in the retention time of the main compound of fungal melanin extracts and also in the presence of minor unknown compounds. On the other hand, MALDI-TOF-MS analysis showed slight differences in the spectra, specifically the presence of a minor intensity ion in synthetic and human melanin, as well as in some fungal

  12. Oral Candidal Carriage in Subjects with Pure Vegetarian and Mixed Dietary Habits.

    Science.gov (United States)

    Patil, Shankargouda; Rao, Roopa S; Raj, A Thirumal; Sanketh, D S; Sarode, Sachin; Sarode, Gargi

    2017-07-01

    Candida albicans being a part of the normal oral microbial flora is one of the most commonly isolated species from the oral cavity. Recent studies have shown a steady rise in the number of non C. albicans species, which are relatively resistant to common antifungal agents and are being recognized as potential pathogens. It is vital to ascertain the predisposing factors leading to such a shift in the oral candidal flora. To estimate the prevalence of candidal species among vegetarians and non-vegetarians. Clinical data including age, gender, and diet preference of 238 participants were noted. Participants with a history of systemic disorders, oral prosthesis, salivary gland disorders and habits such as smoking, alcoholism, and tobacco usage were excluded from the study. The participants were asked to gargle a 10 ml solution of phosphate buffered saline for one minute before depositing the same in a sterile container. The samples were cultured using Hicrome agar media. Data analysis was carried out using Statistical Package for Social Sciences (SPSS software) version 10.5 and differences between individual groups were tested by Chi-square test. Among 238 samples, 127 (53.3%) samples were positive for Candida . The candidal prevalence in vegetarians (68.5%) was higher than non-vegetarians (40.7%). C. albicans was the most common species to be isolated in both vegetarians (35.1%) and non-vegetarians (39.2%). Candida glabrata and Candida tropicalis showed a higher prevalence in vegetarians (30.5% and 10.1%, respectively) in comparison to non-vegetarians (8.4% and 2.3%, respectively). Candida krusei was isolated only from vegetarians (4.6%). Results indicate that diet plays a major role in oral candidal prevalence and species specificity which in turn may predispose the vegetarians toward these pathogenic organisms.

  13. Resistant Microascus cirrosus pneumonia can be treated with a combination of surgery, multiple anti-fungal agents and a growth factor

    NARCIS (Netherlands)

    Ustun, Celalettin; Huls, Gerwin; Stewart, Marc; Marr, Kieren A.

    2006-01-01

    A 49-year old male with acute myelogenous leukemia relapsed eight years post allogeneic bone marrow transplantation. The patient received induction chemotherapy causing prolonged neutropenia. The patient developed pneumonia for which empirical antibacterial and antifungal therapy were started. The

  14. Magnetic resonance cholangiopancreatography (MRCP) using new negative per-oral contrast agent based on superparamagnetic iron oxide nanoparticles for extrahepatic biliary duct visualization in liver cirrhosis.

    Science.gov (United States)

    Polakova, Katerina; Mocikova, Ingrid; Purova, Dana; Tucek, Pavel; Novak, Pavel; Novotna, Katerina; Izak, Niko; Bielik, Radoslav; Zboril, Radek; Miroslav, Herman

    2016-12-01

    Magnetic resonance cholangiopancreatography (MRCP) is often used for imaging of the biliary tree and is required by surgeons before liver transplantation. Advanced liver cirrhosis and ascites in patients however present diagnostic problems for MRCP. The aim of this study was to find out if the use of our negative per-oral contrast agent containing superparamagnetic iron oxide nanoparticles (SPIO) in MRCP is helpful for imaging of hepatobiliary tree in patients with liver cirrhosis. Forty patients with liver cirrhosis were examined on a 1.5 T MR unit using standard MRCP protocol. Twenty patients (group A) underwent MRCP after administration of per-oral SPIO contrast agent 30 min before examination. In group B, twenty patients were examined without per-oral bowel preparation. Ascites was present in eleven patients from group A and in thirteen patients in group B. Four radiologists analyzed MR images for visibility and delineation of the biliary tree. χ 2 tests were used for comparison of the visibility of intrahepatic and extrahepatic biliary ducts in patients with and without ascites. Better extrahepatic biliary duct visualization and visibility of extraluminal pathologies in patients with ascites was proved after administration of SPIO contrast agent. No statistically significant difference between group A and B was found for visualization of extrahepatic biliary ducts in patients without ascites. Delineation of intrahepatic biliary ducts was independent on bowel preparation. Application of our negative per-oral SPIO contrast agent before MRCP improves the visualization of extrahepatic biliary ducts in patients with ascites which is helpful during the liver surgery, mainly in liver transplantation.

  15. Antifungal, optical, and mechanical properties of polymethylmethacrylate material incorporated with silanized zinc oxide nanoparticles

    Directory of Open Access Journals (Sweden)

    Kamonkhantikul K

    2017-03-01

    Full Text Available Krid Kamonkhantikul,1 Mansuang Arksornnukit,1 Hidekazu Takahashi2 1Department of Prosthodontics, Faculty of Dentistry, Chulalongkorn University, Bangkok, Thailand; 2Oral Biomaterials Engineering, Graduate School of Medical and Dental Sciences, Tokyo Medical and Dental University, Tokyo, Japan Background: Fungal infected denture, which is typically composed of polymethylmethacrylate (PMMA, is a common problem for a denture wearer, especially an elderly patient with limited manual dexterity. Therefore, increasing the antifungal effect of denture by incorporating surface modification nanoparticles into the PMMA, while retaining its mechanical properties, is of interest. Aim of the study: This study aimed to evaluate antifungal, optical, and mechanical properties of heat-cured PMMA incorporated with different amounts of zinc oxide nanoparticles (ZnOnps with or without methacryloxypropyltrimethoxysilane modification. Materials and methods: Specimens made from heat-cured PMMA containing 1.25, 2.5, and 5% (w/w nonsilanized (Nosi or silanized (Si ZnOnps were evaluated. Specimens without filler served as control. The fungal assay was performed placing a Candida albicans suspension on the PMMA surface for 2 h, then Sabouraud Dextrose Broth was added, and growth after 24 h was determined by counting colony forming units on agar plates. A spectrophotometer was used to measure the color in L* (brightness, a* (red-green, b* (yellow-blue and opacity of the experimental groups. Flexural strength and flexural modulus were determined using a three-point bending test on universal testing machine after 37°C water storage for 48 h and 1 month. Results: The antifungal, optical, and mechanical properties of the PMMA incorporated with ZnOnps changed depending on the amount. With the same amount of ZnOnps, the silanized groups demonstrated a greater reduction in C. albicans compared with the Nosi groups. The color difference (ΔE and opacity of the Nosi groups were

  16. Deletion of the Candida glabrata ERG3 and ERG11 genes: effect on cell viability, cell growth, sterol composition, and antifungal susceptibility.

    Science.gov (United States)

    Geber, A; Hitchcock, C A; Swartz, J E; Pullen, F S; Marsden, K E; Kwon-Chung, K J; Bennett, J E

    1995-01-01

    We have cloned and sequenced the structural genes encoding the delta 5,6 sterol desaturase (ERG3 gene) and the 14 alpha-methyl sterol demethylase (ERG11 gene) from Candida glabrata L5 (leu2). Single and double mutants of these genes were created by gene deletion. The phenotypes of these mutants, including sterol profiles, aerobic viabilities, antifungal susceptibilities, and generation times, were studied. Strain L5D (erg3 delta::LEU2) accumulated mainly ergosta-7,22-dien-3 beta-ol, was aerobically viable, and remained susceptible to antifungal agents but had a slower generation time than its parent strain. L5LUD (LEU2 erg11 delta::URA3) strains required medium supplemented with ergosterol and an anaerobic environment for growth. A spontaneous aerobically viable mutant, L5LUD40R (LEU erg11 delta::URA3), obtained from L5LUD (LEU2 erg11 delta::URA3), was found to accumulate lanosterol and obtusifoliol, was resistant to azole antifungal agents, demonstrated some increase in resistance to amphotericin B, and exhibited a 1.86-fold increase in generation time in comparison with L5 (leu2). The double-deletion mutant L5DUD61 (erg3 delta::LEU2 erg11 delta::URA3) was aerobically viable, produced mainly 14 alpha-methyl fecosterol, and had the same antifungal susceptibility pattern as L5LUD40R (LEU2 erg11 delta::URA3), and its generation time was threefold greater than that of L5 (leu2). Northern (RNA) analysis revealed that the single-deletion mutants had a marked increase in message for the undeleted ERG3 and ERG11 genes. These results indicate that differences in antifungal susceptibilities and the restoration of aerobic viability exist between the C. glabrata ergosterol mutants created in this study and those sterol mutants with similar genetic lesions previously reported for Saccharomyces cerevisiae. PMID:8593007

  17. Synthesis, X-ray Single Crystal Structure, Molecular Docking and DFT Computations on N-[(1E)-1-(2H-1,3-Benzodioxol-5-yl)-3-(1H-imidazol-1-yl)propylidene]-hydroxylamine: A New Potential Antifungal Agent Precursor.

    Science.gov (United States)

    Al-Wabli, Reem I; Al-Ghamdi, Alwah R; Ghabbour, Hazem A; Al-Agamy, Mohamed H; Monicka, James Clemy; Joe, Issac Hubert; Attia, Mohamed I

    2017-02-28

    Mycoses are serious health problem, especially in immunocompromised individuals. A new imidazole-bearing compound containing an oxime functionality was synthesized and characterized with different spectroscopic techniques to be used for the preparation of new antifungal agents. The stereochemistry of the oxime double bond was unequivocally determined via the single crystal X-ray technique. The title compound 4 , C 13 H 13 N₃O₃·C₃H₈O, crystallizes in the monoclinic space group P 2₁with a = 9.0963(3) Å, b = 14.7244(6) Å, c = 10.7035(4) Å, β = 94.298 (3)°, V = 1429.57(9) ų, Z = 2. The molecules were packed in the crystal structure by eight intermolecular hydrogen bond interactions. A comprehensive spectral analysis of the title molecule 4 has been performed based on the scaled quantum mechanical (SQM) force field obtained by density-functional theory (DFT) calculations. A molecular docking study illustrated the binding mode of the title compound 4 into its target protein. The preliminary antifungal activity of the title compound 4 was determined using a broth microdilution assay.

  18. Antifungal properties of Brazilian cerrado plants

    Directory of Open Access Journals (Sweden)

    Souza Lúcia Kioko Hasimoto e

    2002-01-01

    Full Text Available Ethanolic extracts from leaves of Hyptis ovalifolia, H. suaveolens, H. saxatilis, Hyptidendrum canum, Eugenia uniflora, E. dysenterica, Caryocar brasiliensis and Lafoensia pacari were investigated for their antifungal activity against dermatophytes. The most effective plants were H. ovalifolia and E. uniflora, while Trichophyton rubrum was the most sensitive among the four dermatophytes species evaluated. This study has demonstrated antifungal properties of Brazilian Cerrado plant extracts in "in vitro" assays.

  19. Antifungal susceptibility testing of Candida in the Clinical Laboratory: how to do it, when to do it, and how to interpret it

    Directory of Open Access Journals (Sweden)

    Esther Manso

    2014-06-01

    Full Text Available Significant changes in the management of fungaemia have occurred in the last decade with increased use of fluconazole prophylaxis, of empirical treatment and of echinocandins as first-line agents for documented disease. The emergence of drug resistance in fungal pathogens has a profound impact on human health given limited number of antifungal drugs. Antifungal resistance in Candida may be either intrinsic or acquired and may be encountered in the antifungal drug exposed but also the antifungal drug naïve patient The variation in resistance rates between centers emphasizes that it is essential to have knowledge of the local Candida species distribution and antifungal resistance rates to guide initial therapy for Candida BSI. Moreover, all Candida isolates from blood and normally sterile sites should be identified to the species level. The Clinical and Laboratory Standards Institute and European Committee on Antimicrobial Susceptibility Testing have developed breakpoints and epidemiological cutoff values that are now established for Candida spp. Clinical microbiology laboratories will be employed commercial susceptibility assays, rather than reference broth microdilution methods and comparative studies are particularly important. Vitek 2®, Etest® and Sensititre YeastOne® provided a high degree of essential agreement and comparable sensitivity and specificity to BMD-RPMI for identifying resistance to azole and echinocandins in Candida spp.

  20. Effect of ionizing energy on extracts of Quillaja saponaria to be used as an antimicrobial agent on irradiated edible coating for fresh strawberries

    Energy Technology Data Exchange (ETDEWEB)

    Zuniga, G.E., E-mail: gustavo.zuniga@usach.cl [Universidad de Santiago de Chile (USACH), Facultad de Quimica y Biologia, Depto. de Biologia, Alameda 3363, Estacion Central, Santiago (Chile); Junqueira-Goncalves, M.P., E-mail: mpaula.junqueira@usach.cl [Universidad de Santiago de Chile (USACH), Facultad Tecnologica, Depto. de Ciencia y Tecnologia de Alimentos, Ecuador 3769, Estacion Central, Santiago (Chile); Pizarro, M.; Contreras, R. [Universidad de Santiago de Chile (USACH), Facultad de Quimica y Biologia, Depto. de Biologia, Alameda 3363, Estacion Central, Santiago (Chile); Tapia, A. [Universidad de Santiago de Chile (USACH), Facultad Tecnologica, Depto. de Ciencia y Tecnologia de Alimentos, Ecuador 3769, Estacion Central, Santiago (Chile); Silva, S. [Comision Chilena de Energia Nuclear, Depto. de Aplicaciones Nucleares, Seccion Salud y Alimentos, La Reina, Santiago (Chile)

    2012-01-15

    Incorporating antimicrobial compounds into edible films or coatings provides a novel way to improve the safety and shelf life of ready-to-eat foods. Diverse studies with Quillaja saponaria Mol. (popularly named quillay) extracts have demonstrated their potential as antifungal agents against phytopathogenic fungi. Crosslinking induced by ionizing radiation is an effective method for the improvement of both barrier and mechanical properties of the edible films and coatings based on milk proteins. However there are few reports about the effects of {gamma}-radiation on plant extracts. The aim of this work was to evaluate the effect of ionizing radiation (0, 5, 10, 15, 20, 25 and 35 kGy) on extracts prepared from in vitro plants of Q. saponaria to be used as antimicrobial agent in irradiated edible coating based on calcium caseinate and whey protein isolated, and also to establish the concentration of Q. saponaria extract to be added as an antifungal agent in the coating. Gamma irradiation since 15 kGy affects negatively the antimicrobial activity and metabolites composition of extract of Q. saponaria by reducing compounds of phenolic nature. Otherwise no effect on saponins profile was observed even at higher doses. It was possible to conclude that the antifungal activity of Q. saponaria extract is mainly related to phenolic compounds content. In addition, our work also shows that to obtain an efficient antifungal protection is necessary to add a minimum concentration of 6% of the extract after the coating irradiation. - Highlights: > Antimicrobial compounds into edible coatings improve food' safety and shelf life. > Q. saponaria extract is an antifungal agent against phytopathogenic fungi. > Crosslinking induced by {gamma}-radiation over 30 kGy improves properties of the coatings. > {gamma}-radiation since 15 kGy affects the antimicrobial activity of Q. saponaria extract. > This extract should be added after the coating radiation, at a minimum of 6%.

  1. New ion-exchanged zeolite derivatives: antifungal and antimycotoxin properties against Aspergillus flavus and aflatoxin B1

    Science.gov (United States)

    Savi, Geovana D.; Cardoso, Willian A.; Furtado, Bianca G.; Bortolotto, Tiago; Da Agostin, Luciana O. V.; Nones, Janaína; Torres Zanoni, Elton; Montedo, Oscar R. K.; Angioletto, Elidio

    2017-08-01

    Zeolites are microporous crystalline hydrated aluminosilicates with absorbent and catalytic properties. This material can be used in many applications in stored-pest management such as: pesticide and fertilizer carriers, animal feed additives, mycotoxin binders and food packaging materials. Herein, four 4A zeolite forms were prepared by ion-exchange and their antifungal effect against Aspergillus flavus was highlighted. Additionally, the antimycotoxin activity and the aflatoxin B1 (AFB1) adsorption capacity of these zeolites as well as their toxic effects on Artemia sp. were investigated. The ion-exchanged zeolites with Li+ and Cu2+ showed the best antifungal activity against A. flavus, including effects on conidia germination and hyphae morphological alterations. Regarding to antimycotoxin activity, all zeolite samples efficiently inhibited the AFB1 production by A. flavus. However, the ion-exchanged zeolites exhibited better results than the 4A zeolite. On the other hand, the AFB1 adsorption capacity was only observed by the 4A zeolite and zeolite-Li+. Lastly, our data showed that all zeolites samples used at effective concentrations for antifungal and antimycotoxin assays (2 mg ml-1) showed no toxic effects towards Artemia sp. Results suggest that some these ion-exchanged zeolites have great potential as an effective fungicide and antimycotoxin agent for agricultural and food safety applications.

  2. Fisetin as a promising antifungal agent against Cryptocococcus neoformans species complex.

    Science.gov (United States)

    Reis, M P C; Carvalho, C R C; Andrade, F A; Fernandes, O F L; Arruda, W; Silva, M R R

    2016-08-01

    The aim of this study was to investigate the mechanisms of action of fisetin, a flavonol with antifungal activity previously evaluated against the Cryptococcus neoformans species complex. Ergosterol content and flow cytometry analysis were determined for the C. neoformans species complex in the presence of fisetin and ultrastructural analysis of morphology was performed on Cryptococcus gattii and C. neoformans. Decrease in the total cellular ergosterol content after exposure to fisetin ranged from 25·4% after exposure to 128 μg ml(-1) to 21·6% after exposure to 64 μg ml(-1) of fisetin compared with the control (without fisetin). The fisetin effects obtained with flow cytometry showed metabolic impairment, and alterations in its normal morphology caused by fisetin in C. neoformans cells were verified using scanning electron microscopy. Fisetin is a compound that acts in the biosynthesis of ergosterol. Flow cytometry showed that fisetin reduced viability of the metabolically active cells of C. gattii, while morphological changes explain the action of fisetin in inhibiting growth of these fungi. This study supports the idea that fisetin may represent a good starting point for the development of future therapeutic substances for cryptococcosis. © 2016 The Society for Applied Microbiology.

  3. Athlete's Foot: Clinical Update.

    Science.gov (United States)

    Ramsey, M L

    1989-10-01

    In brief: Athletes are particularly prone to athlete's foot because they are generally more exposed than others to conditions that encourage fungal growth, eg, communal showers and locker rooms. Diagnosis of athlete's foot rests on clinical suspicion and laboratory testing. Treatment may consist of topical antifungal agents and, for more resistant cases, oral griseofulvin. Preventive measures include keeping the feet dry, wearing nonocclusive leather shoes or sandals and absorbent cotton socks, and applying talcum or antifungal powder at least twice daily.

  4. Antifungal Poly(lactic acid) Films Containing Thymol and Carvone

    OpenAIRE

    Boonruang Kanchana; Chinsirikul Wannee; Hararak Bongkot; Kerddonfag Noppadon; Chonhenchob Vanee

    2016-01-01

    The goal of this study was to develop antifungal poly(lactic acid) films for food packaging applications. The antifungal compounds, thymol and R-(-)-carvone were incorporated into poly(lactic acid) (PLA)-based polymer at 10, 15 and 20% by weight. Film converting process consists of three steps including melt blending, sheet extrusion and biaxial stretching. The incorporation of antifungal compounds into the polymer matrix resulted in decreased Tg and Tm, increased gas permeabilility, reduced ...

  5. Posaconazole exhibits in vitro and in vivo synergistic antifungal activity with caspofungin or FK506 against Candida albicans.

    Directory of Open Access Journals (Sweden)

    Ying-Lien Chen

    Full Text Available The object of this study was to test whether posaconazole, a broad-spectrum antifungal agent inhibiting ergosterol biosynthesis, exhibits synergy with the β-1,3 glucan synthase inhibitor caspofungin or the calcineurin inhibitor FK506 against the human fungal pathogen Candida albicans. Although current drug treatments for Candida infection are often efficacious, the available antifungal armamentarium may not be keeping pace with the increasing incidence of drug resistant strains. The development of drug combinations or novel antifungal drugs to address emerging drug resistance is therefore of general importance. Combination drug therapies are employed to treat patients with HIV, cancer, or tuberculosis, and has considerable promise in the treatment of fungal infections like cryptococcal meningitis and C. albicans infections. Our studies reported here demonstrate that posaconazole exhibits in vitro synergy with caspofungin or FK506 against drug susceptible or resistant C. albicans strains. Furthermore, these combinations also show in vivo synergy against C. albicans strain SC5314 and its derived echinocandin-resistant mutants, which harbor an S645Y mutation in the CaFks1 β-1,3 glucan synthase drug target, suggesting potential therapeutic applicability for these combinations in the future.

  6. Antifungal Efficacy during Candida krusei Infection in Non-Conventional Models Correlates with the Yeast In Vitro Susceptibility Profile

    Science.gov (United States)

    Scorzoni, Liliana; de Lucas, Maria Pilar; Mesa-Arango, Ana Cecilia; Fusco-Almeida, Ana Marisa; Lozano, Encarnación; Cuenca-Estrella, Manuel; Mendes-Giannini, Maria Jose; Zaragoza, Oscar

    2013-01-01

    The incidence of opportunistic fungal infections has increased in recent decades due to the growing proportion of immunocompromised patients in our society. Candida krusei has been described as a causative agent of disseminated fungal infections in susceptible patients. Although its prevalence remains low among yeast infections (2–5%), its intrinsic resistance to fluconazole makes this yeast important from epidemiologic aspects. Non mammalian organisms are feasible models to study fungal virulence and drug efficacy. In this work we have used the lepidopteran Galleria mellonella and the nematode Caenorhabditis elegans as models to assess antifungal efficacy during infection by C. krusei. This yeast killed G. mellonella at 25, 30 and 37°C and reduced haemocytic density. Infected larvae melanized in a dose-dependent manner. Fluconazole did not protect against C. krusei infection, in contrast to amphotericin B, voriconazole or caspofungin. However, the doses of these antifungals required to obtain larvae protection were always higher during C. krusei infection than during C. albicans infection. Similar results were found in the model host C. elegans. Our work demonstrates that non mammalian models are useful tools to investigate in vivo antifungal efficacy and virulence of C. krusei. PMID:23555877

  7. Antifungal activity of indigenous bacillus sp. isolate Q3 against marshmallow mycobiota

    Directory of Open Access Journals (Sweden)

    Jošić Dragana Lj.

    2011-01-01

    Full Text Available Marshmallow is a host of a number of saprophytic and parasitic fungi in Serbia. The seeds of marshmallow are contaminated with fungi from different genera, especially Alternaria and Fusarium, which significantly reduced seed germination and caused seedling decay. In this study we investigate antagnonism of indigenous Bacillus sp. isolate Q3 against marshmallow mycopopulation. Bacillus sp. Q3 was isolated from maize rhizosphere, characterized by polyphasic approch and tested for plant growth promoting treats. Bacillus sp. Q3 produced antifungal metabolites with growth inhibition activity against numerous fungi in dual culture: 61.8% of Alternaria alternata, 74.8% of Myrothecium verrucaria and 33.6% of Sclerotinia sclerotiorum. That effect could be caused by different antifungal metabolites including siderophores, hydrolytic enzymes, organic acids and indole acetic acid (IAA. Suppression of natural marshmallow seed infection by Q3 isolate was observed. The seeds were immersed in different concentrations of bacterial suspension during 2h and their infections by phytopathogenic fungi were estimated. The results showed significant reduction of seed infection by Alternaria spp. The presented results indicate possible application of this isolate as promising biological agent for control of marshmallow seed pathogenic fungi.

  8. Correlation between in vitro and in vivo antifungal activities in experimental fluconazole-resistant oropharyngeal and esophageal candidiasis.

    Science.gov (United States)

    Walsh, T J; Gonzalez, C E; Piscitelli, S; Bacher, J D; Peter, J; Torres, R; Shetti, D; Katsov, V; Kligys, K; Lyman, C A

    2000-06-01

    Oropharyngeal and esophageal candidiasis (OPEC) is a frequent opportunistic mycosis in immunocompromised patients. Azole-resistant OPEC is a refractory form of this infection occurring particularly in human immunodeficiency virus (HIV)-infected patients. The procedures developed by the Antifungal Subcommittee of the National Committee for Clinical Laboratory Standards (NCCLS) are an important advance in standardization of in vitro antifungal susceptibility methodology. In order to further understand the relationship between NCCLS methodology and antifungal therapeutic response, we studied the potential correlation between in vitro susceptibility to fluconazole and in vivo response in a rabbit model of fluconazole-resistant OPEC. MICs of fluconazole were determined by NCCLS methods. Three fluconazole-susceptible (FS) (MIC, /=64 microgram/ml) isolates of Candida albicans from prospectively monitored HIV-infected children with OPEC were studied. FR isolates were recovered from children with severe OPEC refractory to fluconazole, and FS isolates were recovered from those with mucosal candidiasis responsive to fluconazole. Fluconazole at 2 mg/kg of body weight/day was administered to infected animals for 7 days. The concentrations of fluconazole in plasma were maintained above the MICs for FS isolates throughout the dosing interval. Fluconazole concentrations in the esophagus were greater than or equal to those in plasma. Rabbits infected with FS isolates and treated with fluconazole had significant reductions in oral mucosal quantitative cultures (P OPEC due to C. albicans.

  9. Water-equivalent oral contrast agents in dual-modality PET/computed tomography scanning: does a little barium make the difference?

    Science.gov (United States)

    Kinner, Sonja; Veit-Haibach, Patrick; Lauenstein, Thomas C; Bockisch, Andreas; Antoch, Gerald

    2009-03-01

    To retrospectively evaluate the performance of two water-equivalent oral contrast agents [locust bean gum (LBG)-mannitol and VoLumen] concerning their potential to distend the bowel while avoiding contrast-associated artifacts in PET/computed tomography. PET/computed tomography examinations of 30 patients with two different oral contrast agents were reviewed. Bowel distension, intraluminal density, and potential contrast-associated artifacts were assessed for stomach, jejunum, and ileum. Statistical significance was tested by Student's t-test. Distension was slightly better in the stomach with VoLumen as compared with LBG-mannitol whereas LBG-mannitol was found to slightly better distend the small bowel. This difference proved to be statistically significant for the jejunum. A statistically significant difference was detected for intraluminal density with higher densities for VoLumen. This difference, however, did not result in a higher incidence of PET artifacts with VoLumen. LBG-mannitol provides excellent bowel distension, thereby avoiding contrast-associated PET artifacts. If this solution is not available, VoLumen provides a satisfactory alternative for bowel distension without relevant PET artifacts.

  10. Oral contraceptives induced hepatotoxicity

    OpenAIRE

    B. Akshaya Srikanth; V. Manisree

    2013-01-01

    Oral Contraceptives are the pharmacological agents used to prevent pregnancy. These are divided as the combined and progestogen methods and are administered orally, transdermally, systemically and via vaginal route. All these methods contain both oestrogen and progestogen. Vigorous usage of oral contraceptives and anabolic steroids as associated with cholestasis, vascular lesions and hepatic neoplasm. Benign hepatic neoplasms are clearly associated with oral contraceptives. In this article we...

  11. Oral Administration and Detection of a Near-Infrared Molecular Imaging Agent in an Orthotopic Mouse Model for Breast Cancer Screening.

    Science.gov (United States)

    Bhatnagar, Sumit; Verma, Kirti Dhingra; Hu, Yongjun; Khera, Eshita; Priluck, Aaron; Smith, David E; Thurber, Greg M

    2018-05-07

    Molecular imaging is advantageous for screening diseases such as breast cancer by providing precise spatial information on disease-associated biomarkers, something neither blood tests nor anatomical imaging can achieve. However, the high cost and risks of ionizing radiation for several molecular imaging modalities have prevented a feasible and scalable approach for screening. Clinical studies have demonstrated the ability to detect breast tumors using nonspecific probes such as indocyanine green, but the lack of molecular information and required intravenous contrast agent does not provide a significant benefit over current noninvasive imaging techniques. Here we demonstrate that negatively charged sulfate groups, commonly used to improve solubility of near-infrared fluorophores, enable sufficient oral absorption and targeting of fluorescent molecular imaging agents for completely noninvasive detection of diseased tissue such as breast cancer. These functional groups improve the pharmacokinetic properties of affinity ligands to achieve targeting efficiencies compatible with clinical imaging devices using safe, nonionizing radiation (near-infrared light). Together, this enables development of a "disease screening pill" capable of oral absorption and systemic availability, target binding, background clearance, and imaging at clinically relevant depths for breast cancer screening. This approach should be adaptable to other molecular targets and diseases for use as a new class of screening agents.

  12. Antifungal activity of essential oils against selected terverticillate penicillia

    Directory of Open Access Journals (Sweden)

    Soňa Felšöciová

    2015-02-01

    Full Text Available The aim of this study was to screen 15 essential oils of selected plant species, viz. Lavandula angustifolia, Carum carvi, Pinus mungo var. pulmilio, Mentha piperita, Chamomilla recutita L., Pinus sylvestris, Satureia hortensis L., Origanum vulgare L., Pimpinella anisum, Rosmarinus officinalis L., Salvia officinalis L., Abietis albia etheroleum, Chamomilla recutita, L. Rausch, Thymus vulgaris L., Origanum vulgare L. for antifungal activity against five Penicillium species: Penicillium brevicompactum, Penicillium citrinum, Penicillium crustosum, Penicillium expansum and Penicillium griseofulvum. The method used for screening included the disc diffusion method. The study points out the wide spectrum of antifungal activity of essential oils against Penicillium fungi. There were five essential oils of the 15 mentioned above which showed a hopeful antifungal activity: Pimpinella anisum, Chamomilla recutita L., Thymus vulgaris, Origanum vulgare L. The most hopeful antifungal activity and killing effect against all tested penicillia was found to be Origanum vulgare L. and Pimpinella anisum. The lowest level of antifungal activity was demonstrated by the oils Pinus mungo var. pulmilio, Salvia officinalis L., Abietis albia etheroleum, Chamomilla recutita L. Rausch, Rosmarinus officinalis.

  13. Distribution and drivers of costs in type 2 diabetes mellitus treated with oral hypoglycemic agents: a retrospective claims data analysis.

    Science.gov (United States)

    Bron, Morgan; Guerin, Annie; Latremouille-Viau, Dominick; Ionescu-Ittu, Raluca; Viswanathan, Prabhakar; Lopez, Claudia; Wu, Eric Q

    2014-09-01

    To describe the distribution of costs and to identify the drivers of high costs among adult patients with type 2 diabetes mellitus (T2DM) receiving oral hypoglycemic agents. T2DM patients using oral hypoglycemic agents and having HbA1c test data were identified from the Truven MarketScan databases of Commercial and Medicare Supplemental insurance claims (2004-2010). All-cause and diabetes-related annual direct healthcare costs were measured and reported by cost components. The 25% most costly patients in the study sample were defined as high-cost patients. Drivers of high costs were identified in multivariate logistic regressions. Total 1-year all-cause costs for the 4104 study patients were $55,599,311 (mean cost per patient = $13,548). Diabetes-related costs accounted for 33.8% of all-cause costs (mean cost per patient = $4583). Medical service costs accounted for the majority of all-cause and diabetes-related total costs (63.7% and 59.5%, respectively), with a minority of patients incurring >80% of these costs (23.5% and 14.7%, respectively). Within the medical claims, inpatient admission for diabetes-complications was the strongest cost driver for both all-cause (OR = 13.5, 95% CI = 8.1-23.6) and diabetes-related costs (OR = 9.7, 95% CI = 6.3-15.1), with macrovascular complications accounting for most inpatient admissions. Other cost drivers included heavier hypoglycemic agent use, diabetes complications, and chronic diseases. The study reports a conservative estimate for the relative share of diabetes-related costs relative to total cost. The findings of this study apply mainly to T2DM patients under 65 years of age. Among the T2DM patients receiving oral hypoglycemic agents, 23.5% of patients incurred 80% of the all-cause healthcare costs, with these costs being driven by inpatient admissions, complications of diabetes, and chronic diseases. Interventions targeting inpatient admissions and/or complications of diabetes may contribute to the decrease of the

  14. Phenotypic aspects of oral strains of Candida albicans in children with down's syndrome

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    E. L. Ribeiro

    Full Text Available The aim of this article is to characterize the biological aspects of oral strains of C. albicans in children with Down's syndrome. These yeasts were analyzed as to their macromorphological and enzymatic aspects and were tested as to their in vitro susceptibility to antifungal drugs using broth microdilution to determine the minimum inhibitory concentration (MIC. The morphotyping revealed that all oral C. albicans isolates from children with Down's syndrome promoted the formation of fringes regardless of size, while the control group presented smaller fringes. All oral C. albicans strains produced proteinase, but those with phospholipolytic activity showed greater enzyme capacity in the test group. In vitro susceptibility showed that all oral C. albicans isolates were sensitive to the drugs used.

  15. Design, Synthesis and Antifungal Activity of Psoralen Derivatives

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    Xiang Yu

    2017-10-01

    Full Text Available A series of linear furanocoumarins with different substituents have been designed and synthesized. Their structures were confirmed by 1H-NMR spectroscopy, high resolution mass spectra (EI-MS, IR, and X-ray single-crystal diffraction. All of the target compounds were evaluated in vitro for their antifungal activity against Rhizoctorzia solani, Botrytis cinerea, Alternaria solani, Gibberella zeae, Cucumber anthrax, and Alternaria leaf spot at 100 μg/mL, and some of the designed compounds exhibited potential antifungal activities. Compound 3a (67.9% exhibited higher activity than the control Osthole (66.1% against Botrytis cinerea. Furthermore, compound 4b (62.4% represented equivalent antifungal activity as Osthole (69.5% against Rhizoctonia solani. The structure-activity relationship (SAR study demonstrates that linear furanocoumarin moiety has an important effect on the antifungal activity, promoting the idea of the coumarin ring as a framework that might be exploited in the future.

  16. Synergism of antifungal activity between mitochondrial respiration inhibitors and kojic acid.

    Science.gov (United States)

    Kim, Jong H; Campbell, Bruce C; Chan, Kathleen L; Mahoney, Noreen; Haff, Ronald P

    2013-01-25

    Co-application of certain types of compounds to conventional antimicrobial drugs can enhance the efficacy of the drugs through a process termed chemosensitization. We show that kojic acid (KA), a natural pyrone, is a potent chemosensitizing agent of complex III inhibitors disrupting the mitochondrial respiratory chain in fungi. Addition of KA greatly lowered the minimum inhibitory concentrations of complex III inhibitors tested against certain filamentous fungi. Efficacy of KA synergism in decreasing order was pyraclostrobin > kresoxim-methyl > antimycin A. KA was also found to be a chemosensitizer of cells to hydrogen peroxide (H₂O₂), tested as a mimic of reactive oxygen species involved in host defense during infection, against several human fungal pathogens and Penicillium strains infecting crops. In comparison, KA-mediated chemosensitization to complex III inhibitors/H₂O₂ was undetectable in other types of fungi, including Aspergillus flavus, A. parasiticus, and P. griseofulvum, among others. Of note, KA was found to function as an antioxidant, but not as an antifungal chemosensitizer in yeasts. In summary, KA could serve as an antifungal chemosensitizer to complex III inhibitors or H₂O₂ against selected human pathogens or Penicillium species. KA-mediated chemosensitization to H₂O₂ seemed specific for filamentous fungi. Thus, results indicate strain- and/or drug-specificity exist during KA chemosensitization.

  17. Onychomycosis nailed

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    Leelavathi Muthupalaniappen

    2014-04-01

    Full Text Available Fungal infection of the nail is a common condition that causes much concern because of its disfiguring appearance. Although specific treatment is available for this condition, treatment outcome is variable and persistent nail dystrophy post-treatment may cause distress to both the patient and the physician. This article describes the current available treatment options for onychomycosis, management approach and the expected treatment outcome to enhance primary care physicians’ confidence in managing this condition. Oral antifungal agents such as terbinafine and itraconazole are good treatment options for onychomycosis. Combination therapy using oral antifungal agents with topical lacquer preparations may provide added benefits. Evaluation of patient’s expectations, providing information on treatment outcome, clinical cure and recurrence rates are essential in the management of onychomycosis. This article is intended to guide primary care physicians to achieve realistic treatment goals and for a satisfactory experience in the overall management of this challenging condition.

  18. In vitro Antifungal Activity of Limonene against Trichophyton rubrum

    OpenAIRE

    Chee, Hee Youn; Kim, Hoon; Lee, Min Hee

    2009-01-01

    In this study, the antifungal activities of limonene against Trichophyton rubrum were evaluated via broth microdilution and vapor contact assays. In both assays, limonene was shown to exert a potent antifungal effect against T. rubrum. The volatile vapor of limonene at concentrations above 1 ?l/800 ml air space strongly inhibited the growth of T. rubrum. The MIC value was 0.5% v/v in the broth microdilution assay. The antifungal activity of limonene against T. rubrum was characterized as a fu...

  19. Clinical Validation of the Analysis of Fluconazole in Oral Fluid in Hospitalized Children

    NARCIS (Netherlands)

    van der Elst, Kim C. M.; van Alst, Manouche; Lub-de Hooge, Marjolijn N.; van Hateren, Kai; Kosterink, Jos G. W.; Alffenaar, Jan-Willem C.; Scholvinck, Elisabeth H.

    2014-01-01

    Fluconazole is a first-line antifungal agent for the treatment and prophylaxis of invasive candidiasis in pediatric patients. Pediatric patients are at risk of suboptimal drug exposure, due to developmental changes in gastrointestinal and renal function, metabolic capacity, and volume of

  20. An in vitro study of antifungal drug susceptibility of Candida species isolated from human immunodeficiency virus seropositive and human immunodeficiency virus seronegative individuals in Lucknow population Uttar Pradesh.

    Science.gov (United States)

    Dar, Mohammad Shafi; Sreedar, Gadiputi; Shukla, Abhilasha; Gupta, Prashant; Rehan, Ahmad Danish; George, Jiji

    2015-01-01

    Candidiasis is the most common opportunistic infection in human immunodeficiency virus (HIV) seropositive patients, starting from asymptomatic colonization to pathogenic forms and gradual colonization of non-albicans in patients with advanced immunosuppression leads to resistance for azole group of antifungal drugs with high rate of morbidity and mortality. To isolate the Candida species and determine of antifungal drug susceptibility against fluconazole, itraconazole, nystatin, amphotericin B, and clotrimazolein HIV seropositive and control individuals, with or without clinical oropharyngeal candidiasis (OPC). Includes samples from faucial region of 70 subjects with and without clinical candidiasis in HIV seropositive and controls were aseptically inoculated onto Sabaraud's Dextrose Agar media and yeasts were identified for the specific species by Corn Meal Agar, sugar fermentation and heat tolerance tests. Antifungal drug susceptibility of the isolated species was done against above-mentioned drugs by E-test and disc diffusion method. The commonly isolated species in HIV seropositive and controls were Candida albicans, Candida glabrata and Candida tropicalis Candida guilliermondii and Candida dubliniensis isolated only in HIV seropositive patients. Susceptibility against selected antifungal drugs was observed more in HIV-negative individuals whereas susceptible dose-dependent and resistance were predominant in HIV-positive patients. Resistance is the major problem in the therapy of OPC, especially in HIV seropositive patients due to aggressive and prolonged use of antifungal agents, therefore, our study emphasizes the need for antifungal drug susceptibility testing whenever antifungal treatment is desired, especially in HIV-infected subjects.

  1. In Vitro Antifungal Activities of a Series of Dication-Substituted Carbazoles, Furans, and Benzimidazoles

    Science.gov (United States)

    Del Poeta, Maurizio; Schell, Wiley A.; Dykstra, Christine C.; Jones, Susan K.; Tidwell, Richard R.; Kumar, Arvind; Boykin, David W.; Perfect, John R.

    1998-01-01

    Aromatic dicationic compounds possess antimicrobial activity against a wide range of eucaryotic pathogens, and in the present study an examination of the structures-functions of a series of compounds against fungi was performed. Sixty-seven dicationic molecules were screened for their inhibitory and fungicidal activities against Candida albicans and Cryptococcus neoformans. The MICs of a large number of compounds were comparable to those of the standard antifungal drugs amphotericin B and fluconazole. Unlike fluconazole, potent inhibitory compounds in this series were found to have excellent fungicidal activities. The MIC of one of the most potent compounds against C. albicans was 0.39 μg/ml, and it was the most potent compound against C. neoformans (MIC, ≤0.09 μg/ml). Selected compounds were also found to be active against Aspergillus fumigatus, Fusarium solani, Candida species other than C. albicans, and fluconazole-resistant strains of C. albicans and C. neoformans. Since some of these compounds have been safely given to animals, these classes of molecules have the potential to be developed as antifungal agents. PMID:9756748

  2. Diffusible and Volatile Antifungal Compounds Produced by an Antagonistic Bacillus velezensis G341 against Various Phytopathogenic Fungi

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    Seong Mi Lim

    2017-10-01

    Full Text Available The aim of this study was to identify volatile and agar-diffusible antifungal metabolites produced by Bacillus sp. G341 with strong antifungal activity against various phytopathogenic fungi. Strain G341 isolated from four-year-old roots of Korean ginseng with rot symptoms was identified as Bacillus velezensis based on 16S rDNA and gyrA sequences. Strain G341 inhibited mycelial growth of all phytopathogenic fungi tested. In vivo experiment results revealed that n-butanol extract of fermentation broth effectively controlled the development of rice sheath blight, tomato gray mold, tomato late blight, wheat leaf rust, barley powdery mildew, and red pepper anthracnose. Two antifungal compounds were isolated from strain G341 and identified as bacillomycin L and fengycin A by MS/MS analysis. Moreover, volatile compounds emitted from strain G341 were found to be able to inhibit mycelial growth of various phytopathogenic fungi. Based on volatile compound profiles of strain G341 obtained through headspace collection and analysis on GC-MS, dimethylsulfoxide, 1-butanol, and 3-hydroxy-2-butanone (acetoin were identified. Taken together, these results suggest that B. valezensis G341 can be used as a biocontrol agent for various plant diseases caused by phytopathogenic fungi.

  3. Diffusible and Volatile Antifungal Compounds Produced by an Antagonistic Bacillus velezensis G341 against Various Phytopathogenic Fungi.

    Science.gov (United States)

    Lim, Seong Mi; Yoon, Mi-Young; Choi, Gyung Ja; Choi, Yong Ho; Jang, Kyoung Soo; Shin, Teak Soo; Park, Hae Woong; Yu, Nan Hee; Kim, Young Ho; Kim, Jin-Cheol

    2017-10-01

    The aim of this study was to identify volatile and agar-diffusible antifungal metabolites produced by Bacillus sp. G341 with strong antifungal activity against various phytopathogenic fungi. Strain G341 isolated from four-year-old roots of Korean ginseng with rot symptoms was identified as Bacillus velezensis based on 16S rDNA and gyrA sequences. Strain G341 inhibited mycelial growth of all phytopathogenic fungi tested. In vivo experiment results revealed that n -butanol extract of fermentation broth effectively controlled the development of rice sheath blight, tomato gray mold, tomato late blight, wheat leaf rust, barley powdery mildew, and red pepper anthracnose. Two antifungal compounds were isolated from strain G341 and identified as bacillomycin L and fengycin A by MS/MS analysis. Moreover, volatile compounds emitted from strain G341 were found to be able to inhibit mycelial growth of various phytopathogenic fungi. Based on volatile compound profiles of strain G341 obtained through headspace collection and analysis on GC-MS, dimethylsulfoxide, 1-butanol, and 3-hydroxy-2-butanone (acetoin) were identified. Taken together, these results suggest that B. valezensis G341 can be used as a biocontrol agent for various plant diseases caused by phytopathogenic fungi.

  4. Coriandrum sativum L. (Coriander essential oil: antifungal activity and mode of action on Candida spp., and molecular targets affected in human whole-genome expression.

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    Irlan de Almeida Freires

    Full Text Available Oral candidiasis is an opportunistic fungal infection of the oral cavity with increasingly worldwide prevalence and incidence rates. Novel specifically-targeted strategies to manage this ailment have been proposed using essential oils (EO known to have antifungal properties. In this study, we aim to investigate the antifungal activity and mode of action of the EO from Coriandrum sativum L. (coriander leaves on Candida spp. In addition, we detected the molecular targets affected in whole-genome expression in human cells. The EO phytochemical profile indicates monoterpenes and sesquiterpenes as major components, which are likely to negatively impact the viability of yeast cells. There seems to be a synergistic activity of the EO chemical compounds as their isolation into fractions led to a decreased antimicrobial effect. C. sativum EO may bind to membrane ergosterol, increasing ionic permeability and causing membrane damage leading to cell death, but it does not act on cell wall biosynthesis-related pathways. This mode of action is illustrated by photomicrographs showing disruption in biofilm integrity caused by the EO at varied concentrations. The EO also inhibited Candida biofilm adherence to a polystyrene substrate at low concentrations, and decreased the proteolytic activity of Candida albicans at minimum inhibitory concentration. Finally, the EO and its selected active fraction had low cytotoxicity on human cells, with putative mechanisms affecting gene expression in pathways involving chemokines and MAP-kinase (proliferation/apoptosis, as well as adhesion proteins. These findings highlight the potential antifungal activity of the EO from C. sativum leaves and suggest avenues for future translational toxicological research.

  5. A Study on the Frequency of Fungal Rhinosinusitis and to Determine the Sensitivity of the Isolates to Antifungal Drugs in Shiraz, Iran 2012-2013

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    Parisa Badiei

    2015-06-01

    Full Text Available Abstract Background: Fungal spores are present in large amounts in the nature which may cause diseases in the susceptible individuals. Fungal rhinosinusitis has been increased during recent decades. This study aims to investigate fungal rhinosinusitis in the patients with chronic needing endoscopic sinus surgery aims and to determine the sensitivity of the isolates to rhin sinusitis antifungal agents. Materials and Methods: In cross sectional study, specimens were obtained in sterile plates containing normal saline. from the suspected cases of chronic rhinosinusitis who had undergone endoscopic sinus surgery. Microscopic experiments and Cultures were done in Sabouraud Dextrose Agar medium. Minimum inhibitory concentration (MIC of the growth of fungi for seven antifungal agents against the isolates was determined using E-Test. Results: In total, specimens from 102 immunocompetent patients were examined. Nine positive specimens were presented, consisting of 3 for Aspergillus fumigatus, 3 for Penicillium, 2 for Aspergillus flavus and 1 for Alternaria. The mean age of the patients was 38 years, with 59 males and 43 females. The isolates were most sensitive to the voriconazole and amphotericin B. Conclusion: Since the prevalence of fungal rhinosinusitis is low, unfortunately, the clinicians are not attentive enough to the condition, and they initiate antifungal therapy if the patients are not responsive to antibiotics. Early diagnosis and suitable treatment can help more efficient management of patients.

  6. Antifungal activity of indigenous Bacillus spp. isolated from soil

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    Bjelić Dragana Đ.

    2017-01-01

    Full Text Available Biocontrol using plant growth-promoting rhizobacteria (PGPR represents an alternative approach to disease management, since PGPR are known to promote growth and reduce diseases in various crops. Among the different PGPR, members of the genus Bacillus are prefered for most biotechnological uses due to their capability to form extremely resistant spores and produce a wide variety of metabolites with antimicrobial activity. The objective of this research was to identify antagonistic bacteria for management of the plant diseases. Eleven isolates of Bacillus spp. were obtained from the soil samples collected from different localities in the Province of Vojvodina. The antifungal activity of bacterial isolates against five fungal species was examined using a dual plate assay. Bacillus isolates exhibited the highest antifungal activity against Fusarium proliferatum, Fusarium oxysporum f. sp. cepae and Alternaria padwickii, while they had the least antagonistic effect on Fusarium verticillioides and Fusarium graminearum. Molecular identification showed that effective bacterial isolates were identified as Bacillus safensis (B2, Bacillus pumilus (B3, B11, Bacillus subtilis (B5, B7 and Bacillus megaterium (B8, B9. The highest antagonistic activity was exhibited by isolates B5 (from 39% to 62% reduction in fungal growth and B7 (from 40% to 71% reduction in fungal growth. These isolates of B. subtilis could be used as potential biocontrol agents of plant diseases. [Project of the Serbian Ministry of Education, Science and Technological Development, Grant no. TR-31073

  7. Abolishing coinsurance for oral antihyperglycemic agents: effects on social insurance budgets.

    Science.gov (United States)

    Athanasakis, Kostas; Skroumpelos, Anastasis G; Tsiantou, Vassiliki; Milona, Katerina; Kyriopoulos, John

    2011-02-01

    To assess the effects of abolishing coinsurance for oral antihyperglycemic agents (OAAs) on the social insurance fund budget in Greece. A mathematical model estimating the effect of a decrease in patient coinsurance rate on demand for and adherence to OAAs and the subsequent clinical and economic outcomes. Price elasticity of demand for antidiabetic agents was used to estimate quantity demand change as a result of a coinsurance rate decrease and consequent increased adherence to OAAs. Given the inverse relationship between OAA adherence and glycated hemoglobin (A1C) level, the model calculated the mean decrease in A1C level and associated cost savings based on the cost difference between patients with controlled versus uncontrolled A1C levels. A decrease in patient coinsurance rate from 25% to 0% led to an incremental increase in OAA adherence of 30.5% and a mean decrease in A1C level of 0.6%. The A1C level decrease contributed to an 18.5% "shift" of uncontrolled patients to controlled A1C levels (<7%), which in economic terms translated into savings of 324 euro per patient over a 3-year period and an investment return rate of 122.8%. A series of 1-way and 2-way sensitivity analyses were conducted to verify the robustness and validity of the outcomes. The introduction of policies aimed at abolishing coinsurance for OAAs can result in improved patient outcomes and cost savings for the healthcare system.

  8. Resposta in vitro de fungos agentes de micoses cutâneas frente aos antifúngicos sistêmicos mais utilizados na dermatologia In vitro response of cutaneous mycosis fungal agents to the most widely used systemic antifungals in dermatology

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    Lívia Maria Martins de Almeida

    2009-07-01

    Full Text Available FUNDAMENTOS - A alta frequência das micoses cutâneas justifica a necessidade de avaliar a possível contribuição da determinação do perfil de susceptibilidade aos antifúngicos in vitro. OBJETIVO - Avaliar se existe variabilidade nos isolados fúngicos quanto à susceptibilidade in vitro de fungos filamentosos, previamente isolados de micoses cutâneas, frente aos antifúngicos fluconazol, cetoconazol, itraconazol e terbinafina. MÉTODOS - Os fungos foram isolados e identificados por meio da metodologia clássica e o teste de susceptibilidade aos antifúngicos foi realizado segundo o método de microdiluição em caldo, de acordo com protocolo preconizado pelo Clinical Laboratory Standards Institute (CLSI, documento M38-A. RESULTADOS - Das 80 amostras de fungos filamentosos identificadas, o gênero Trichophyton representou 81%. As quatro drogas analisadas apresentaram grande variação nos gêneros Trichophyton e Microsporum. O gênero Fusarium foi resistente a todas as drogas testadas. A terbinafina foi o antimicótico mais eficaz contra a maioria dos isolados fúngicos. CONCLUSÃO - Houve uma grande variabilidade nos perfis de resposta aos antifúngicos testados. O estabelecimento de um método-teste de referência permitirá ao clínico maior objetividade na escolha de uma terapia adequada.BACKGROUND - The high frequency of cutaneous mycosis justify the need to evaluate the possible contribution of in vitro profile of susceptibility to antifungal agents. OBJECTIVE - To evaluate whether there is variability in in vitro susceptibility by filamentous fungi, previously isolated from cutaneous mycosis, to fluconazole, ketoconazole, itraconazole and terbinafine. METHODS - Fungi were isolated and identified by classical methods and the antifungal susceptibility test was performed using the method of broth microdilution, according to a protocol recommended by the Clinical Laboratory Standards Institute (CLSI, through M38-A document. RESULTS

  9. New Oral Hypoglycemic Agents and Cardiovascular Risk. Crossing the Metabolic Border.

    Science.gov (United States)

    Dalama, Belén; Mesa, Jordi

    2016-11-01

    Sodium-glucose cotransporter 2 inhibitors are a novel pharmacological class of oral hypoglycemic agents that lower glucose levels by increasing renal glucose excretion in an insulin-independent manner. However, this seemingly simple mechanism has more complex indirect metabolic effects. The results of randomized clinical trials have shown that these inhibitors effectively lower blood glucose and glycated hemoglobin levels without increasing the risk of hypoglycemia and, at the same time, also reduce bodyweight and systolic blood pressure. In this review, we describe the mechanism of action, efficacy, and safety of currently marketed drugs, as well as other risk factors besides glucose that can potentially be modulated positively. Recent data on empagliflozin showing a significant cardiovascular benefit have compelled us to update knowledge of this new therapeutic class for the treatment of type 2 diabetes. Copyright © 2016 Sociedad Española de Cardiología. Published by Elsevier España, S.L.U. All rights reserved.

  10. Catalytic Synthesis and Antifungal Activity of New Polychlorinated Natural Terpenes

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    Hana Ighachane

    2017-01-01

    Full Text Available Various unsaturated natural terpenes were selectively converted to the corresponding polychlorinated products in good yields using iron acetylacetonate in combination with nucleophilic cocatalyst. The synthesized compounds were evaluated for their in vitro antifungal activity. The antifungal bioassays showed that 2c and 2d possessed significant antifungal activity against Fusarium oxysporum f. sp. albedinis (Foa, Fusarium oxysporum f. sp. canariensis (Foc, and Verticillium dahliae (Vd.

  11. Outcomes of Neonatal Candidiasis: The Impact of Delayed Initiation of Antifungal Therapy

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    Heather Cahan

    2011-01-01

    Results. Sixty-three newborns with invasive neonatal candidiasis were identified. Overall mortality rate was 35%. Virtually every infant had a central venous catheter (CVC, required mechanical ventilation and previous administration of antibacterial agents. Delayed institution of antifungal therapy was associated with increased mortality. In addition, length of hospitalization, duration of prior antibacterial therapy, mechanical ventilation, and CVC use, as well as evidence of end-organ disease, were associated with an adverse outcome. Conclusions. Reliance on available laboratory tools in cases of invasive neonatal candidiasis can result in delayed diagnosis and increased mortality. A risk-factor-based approach to empirical treatment could be justified in this setting.

  12. 2-(Substituted phenyl-3,4-dihydroisoquinolin-2-iums as Novel Antifungal Lead Compounds: Biological Evaluation and Structure-Activity Relationships

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    Xin-Juan Yang

    2013-08-01

    Full Text Available The title compounds are a class of structurally simple analogues of quaternary benzo[c]phenanthridine alkaloids (QBAs. In order to develop novel QBA-like antifungal drugs, in this study, 24 of the title compounds with various substituents on the N-phenyl ring were evaluated for bioactivity against seven phytopathogenic fungi using the mycelial growth rate method and their SAR discussed. Almost all the compounds showed definite activities in vitro against each of the test fungi at 50 μg/mL and a broad antifungal spectrum. In most cases, the mono-halogenated compounds 2–12 exhibited excellent activities superior to the QBAs sanguinarine and chelerythrine. Compound 8 possessed the strongest activities on each of the fungi with EC50 values of 8.88–19.88 µg/mL and a significant concentration-dependent relationship. The SAR is as follows: the N-phenyl group is a high sensitive structural moiety for the activity and the characteristics and position of substituents intensively influence the activity. Generally, electron-withdrawing substituents remarkably enhance the activity while electron-donating substituents cause a decrease of the activity. In most cases, ortha- and para-halogenated isomers were more active than the corresponding m-halogenated isomers. Thus, the title compounds emerged as promising lead compounds for the development of novel biomimetic antifungal agrochemicals. Compounds 8 and 2 should have great potential as new broad spectrum antifungal agents for plant protection.

  13. Synthesis, Antiproliferative and Antifungal Activities of 1,2,3-Triazole-Substituted Carnosic Acid and Carnosol Derivatives

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    Mariano Walter Pertino

    2015-05-01

    Full Text Available Abietane diterpenes exhibit an array of interesting biological activities, which have generated significant interest among the pharmacological community. Starting from the abietane diterpenes carnosic acid and carnosol, twenty four new triazole derivatives were synthesized using click chemistry. The compounds differ in the length of the linker and the substituent on the triazole moiety. The compounds were assessed as antiproliferative and antifungal agents. The antiproliferative activity was determined on normal lung fibroblasts (MRC-5, gastric epithelial adenocarcinoma (AGS, lung cancer (SK-MES-1 and bladder carcinoma (J82 cells while the antifungal activity was assessed against Candida albicans ATCC 10231 and Cryptococcus neoformans ATCC 32264. The carnosic acid γ-lactone derivatives 1–3 were the most active antiproliferative compounds of the series, with IC50 values in the range of 43.4–46.9 μM and 39.2–48.9 μM for MRC-5 and AGS cells, respectively. Regarding antifungal activity, C. neoformans was the most sensitive fungus, with nine compounds inhibiting more than 50% of its fungal growth at concentrations ≤250 µg∙mL−1. Compound 22, possessing a p-Br-benzyl substituent on the triazole ring, showed the best activity (91% growth inhibition at 250 µg∙mL−1 In turn, six compounds inhibited 50% C. albicans growth at concentrations lower than 250 µg∙mL−1.

  14. Cytotoxic and Antifungal Constituents Isolated from the Metabolites of Endophytic Fungus DO14 from Dendrobium officinale

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    Ling-Shang Wu

    2015-12-01

    Full Text Available Two novel cytotoxic and antifungal constituents, (4S,6S-6-[(1S,2R-1, 2-dihydroxybutyl]-4-hydroxy-4-methoxytetrahydro-2H-pyran-2-one (1, (6S,2E-6-hydroxy-3-methoxy-5-oxodec-2-enoic acid (2, together with three known compounds, LL-P880γ (3, LL-P880α (4, and Ergosta-5,7,22-trien-3b-ol (5 were isolated from the metabolites of endophytic fungi from Dendrobium officinale. The chemical structures were determined based on spectroscopic methods. All the isolated compounds 1–5 were evaluated by cytotoxicity and antifungal effects. Our present results indicated that compounds 1–4 showed notable anti-fungal activities (minimal inhibitory concentration (MIC ≤ 50 μg/mL for all the tested pathogens including Candida albicans, Cryptococcus neoformans, Trichophyton rubrum, Aspergillus fumigatus. In addition, compounds 1–4 possessed notable cytotoxcities against human cancer cell lines of HL-60 cells with the IC50 values of below 100 μM. Besides, compounds 1, 2, 4 and 5 showed strong cytotoxities on the LOVO cell line with the IC50 values were lower than 100 μM. In conclusion, our study suggested that endophytic fungi of D. officinale are great potential resources to discover novel agents for preventing or treating pathogens and tumors.

  15. Cytotoxic and Antifungal Constituents Isolated from the Metabolites of Endophytic Fungus DO14 from Dendrobium officinale.

    Science.gov (United States)

    Wu, Ling-Shang; Jia, Min; Chen, Ling; Zhu, Bo; Dong, Hong-Xiu; Si, Jin-Ping; Peng, Wei; Han, Ting

    2015-12-22

    Two novel cytotoxic and antifungal constituents, (4S,6S)-6-[(1S,2R)-1, 2-dihydroxybutyl]-4-hydroxy-4-methoxytetrahydro-2H-pyran-2-one (1), (6S,2E)-6-hydroxy-3-methoxy-5-oxodec-2-enoic acid (2), together with three known compounds, LL-P880γ (3), LL-P880α (4), and Ergosta-5,7,22-trien-3b-ol (5) were isolated from the metabolites of endophytic fungi from Dendrobium officinale. The chemical structures were determined based on spectroscopic methods. All the isolated compounds 1-5 were evaluated by cytotoxicity and antifungal effects. Our present results indicated that compounds 1-4 showed notable anti-fungal activities (minimal inhibitory concentration (MIC) ≤ 50 μg/mL) for all the tested pathogens including Candida albicans, Cryptococcus neoformans, Trichophyton rubrum, Aspergillus fumigatus. In addition, compounds 1-4 possessed notable cytotoxcities against human cancer cell lines of HL-60 cells with the IC50 values of below 100 μM. Besides, compounds 1, 2, 4 and 5 showed strong cytotoxities on the LOVO cell line with the IC50 values were lower than 100 μM. In conclusion, our study suggested that endophytic fungi of D. officinale are great potential resources to discover novel agents for preventing or treating pathogens and tumors.

  16. Antifungal cyclic peptides from the marine sponge Microscleroderma herdmani

    Science.gov (United States)

    Screening natural product extracts from National Cancer Institute Open Repository for antifungal discovery afforded hits for bioassay-guided fractionation. Upon LC-MS analysis of column fractions with antifungal activities to generate information on chemical structure, two new cyclic hexapeptides, m...

  17. Synthesis, antioxidant, antifungal, molecular docking and ADMET studies of some thiazolyl hydrazones.

    Science.gov (United States)

    Kauthale, Sushama; Tekale, Sunil; Damale, Manoj; Sangshetti, Jaiprakash; Pawar, Rajendra

    2017-08-15

    Some thiazolyl hydrazones were synthesized by one pot reaction of thiophene-2-carbaldehyde or 2, 4-dichlorobenzaldehyde, thiosemicarbazide and various phenacyl bromides which were preliminarily screened for in vitro antioxidant and antifungal activities. Excellent DPPH and H 2 O 2 radical scavenged antioxidant activities were observed with almost all the tested compounds. Compounds 4a, 4b, 4c, 4e, 4f and 4i showed comparable DPPH scavenged antioxidant potential (90.26-96.56%) whereas H 2 O 2 scavenged antioxidant activity (90.98-92.08%) was noticeable in case of 4a and 4f; showing significant antioxidant potential comparable with the standard ascorbic acid (95.3%). In vitro antifungal activity of synthesized compounds against fungal species Candida albicance, Aspergillus niger and Aspergillus flavus was found to be moderate to good as compared with the standard fluconazole and MIC values were found in the range of 3.12-25μg/mL. Molecular docking studies revealed that the compounds 4a, 4b and 4c have a potential to become lead molecules in drug discovery process. In silico ADMET study was also performed for predicting pharmacokinetic and toxicity profile of the synthesized antioxidants which expressed good oral drug like behaviour and non-toxic nature. Copyright © 2017 Elsevier Ltd. All rights reserved.

  18. The Emerging Pathogen Candida auris: Growth Phenotype, Virulence Factors, Activity of Antifungals, and Effect of SCY-078, a Novel Glucan Synthesis Inhibitor, on Growth Morphology and Biofilm Formation.

    Science.gov (United States)

    Larkin, Emily; Hager, Christopher; Chandra, Jyotsna; Mukherjee, Pranab K; Retuerto, Mauricio; Salem, Iman; Long, Lisa; Isham, Nancy; Kovanda, Laura; Borroto-Esoda, Katyna; Wring, Steve; Angulo, David; Ghannoum, Mahmoud

    2017-05-01

    Candida auris , a new multidrug-resistant Candida spp. which is associated with invasive infection and high rates of mortality, has recently emerged. Here, we determined the virulence factors (germination, adherence, biofilm formation, phospholipase and proteinase production) of 16 C. auris isolates and their susceptibilities to 11 drugs belonging to different antifungal classes, including a novel orally bioavailable 1,3-β-d-glucan synthesis inhibitor (SCY-078). We also examined the effect of SCY-078 on the growth, ultrastructure, and biofilm-forming abilities of C. auris Our data showed that while the tested strains did not germinate, they did produce phospholipase and proteinase in a strain-dependent manner and had a significantly reduced ability to adhere and form biofilms compared to that of Candida albicans ( P = 0.01). C. auris isolates demonstrated reduced susceptibility to fluconazole and amphotericin B, while, in general, they were susceptible to the remaining drugs tested. SCY-078 had an MIC 90 of 1 mg/liter against C. auris and caused complete inhibition of the growth of C. auris and C. albicans Scanning electron microscopy analysis showed that SCY-078 interrupted C. auris cell division, with the organism forming abnormal fused fungal cells. Additionally, SCY-078 possessed potent antibiofilm activity, wherein treated biofilms demonstrated significantly reduced metabolic activity and a significantly reduced thickness compared to the untreated control ( P < 0.05 for both comparisons). Our study shows that C. auris expresses several virulence determinants (albeit to a lesser extent than C. albicans ) and is resistant to fluconazole and amphotericin B. SCY-078, the new orally bioavailable antifungal, had potent antifungal/antibiofilm activity against C. auris , indicating that further evaluation of this antifungal is warranted. Copyright © 2017 Larkin et al.

  19. In vitro antifungal activity of methanol extracts of some Indian ...

    African Journals Online (AJOL)

    STORAGESEVER

    2008-12-03

    Dec 3, 2008 ... vitro antifungal activity against some yeasts including Candida albicans (1) ATCC2091, ... Key words: medicinal plants, antifungal activity, methanol extracts, yeast, mould, Saussurea lappa. ... Caesalpinia pulcherrima.

  20. Aspergillus--classification and antifungal susceptibilities.

    Science.gov (United States)

    Buzina, Walter

    2013-01-01

    Aspergillus is one of the most important fungal genera for the man, for its industrial use, its ability to spoil food and not least its medical impact as cause of a variety of diseases. Currently hundreds of species of Aspergillus are known; nearly fifty of them are able to cause infections in humans and animals. Recently, the genus Aspergillus is subdivided into 8 subgenera and 22 sections. The spectrum of diseases caused by Aspergillus species varies from superficial cutaneous to invasive and systemic infections. All species of Aspergillus investigated so far are resistant against the antifungals fluconazole and 5-fluorocytosine, the range of susceptibilities to currently available antifungals is discussed in this paper.

  1. Quercetin Assists Fluconazole to Inhibit Biofilm Formations of Fluconazole-Resistant Candida Albicans in In Vitro and In Vivo Antifungal Managements of Vulvovaginal Candidiasis

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    Mei Gao

    2016-11-01

    Full Text Available Background: Vulvovaginal candidiasis (VVC is a common gynecological disease. Candida albicans is believed to be mainly implicated in VVC occurrence, the biofilm of which is one of the virulence factors responsible for resistance to traditional antifungal agents especially to fluconazole (FCZ. Quercetin (QCT is a dietary flavonoid and has been demonstrated to be antifungal against C. albicans biofilm. Methods: 17 C. albicans isolates including 15 clinical ones isolated from VVC patients were employed to investigate the effects of QCT and/or FCZ on the inhibition of C. albicans biofilm. Results: We observed that 64 µg/mL QCT and/or 128 µg/mL FCZ could (i be synergistic against 10 FCZ-resistant planktonic and 17 biofilm cells of C. albicans, (ii inhibit fungal adherence, cell surface hydrophobicity (CSH, flocculation, yeast-to-hypha transition, metabolism, thickness and dispersion of biofilms; (iii down-regulate the expressions of ALS1, ALS3, HWP1, SUN41, UME6 and ECE1 and up-regulate the expressions of PDE2, NRG1 and HSP90, and we also found that (iv the fungal burden was reduced in vaginal mucosa and the symptoms were alleviated in a murine VVC model after the treatments of 5 mg/kg QCT and/or 20 mg/kg FCZ. Conclusion: Together with these results, it could be demonstrated that QCT could be a favorable antifungal agent and a promising synergist with FCZ in the clinical management of VVC caused by C. albicans biofilm.

  2. In vitro antifungal activities of 26 plant extracts on mycelial growth of ...

    African Journals Online (AJOL)

    Antifungal activities of 26 plant extracts were tested against Phytophthora infestans using radial growth technique. While all tested plant extracts produced some antifungal activities Xanthium strumarium, Lauris nobilis, Salvia officinalis and Styrax officinalis were the most active plants that showed potent antifungal activity.

  3. The Hsp90 co-chaperones Sti1, Aha1, and P23 regulate adaptive responses to antifungal azoles

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    Xiaokui Gu

    2016-10-01

    Full Text Available Heat Shock Protein 90 (Hsp90 is essential for tumor progression in humans and drug resistance in fungi. However, the roles of its many co-chaperones in antifungal resistance are unknown. In this study, by susceptibility test of Neurospora crassa mutants lacking each of 18 Hsp90/Calcineurin system member genes (including 8 Hsp90 co-chaperone genes to antifungal drugs and other stresses, we demonstrate that the Hsp90 co-chaperones Sti1 (Hop1 in yeast, Aha1, and P23 (Sba1 in yeast were required for the basal resistance to antifungal azoles and heat stress. Deletion of any of them resulted in hypersensitivity to azoles and heat. Liquid chromatography–mass spectrometry (LC-MS analysis showed that the toxic sterols eburicol and 14α-methyl-3,6-diol were significantly accumulated in the sti1 and p23 deletion mutants after ketoconazole treatment, which has been shown before to led to cell membrane stress. At the transcriptional level, Aha1, Sti1, and P23 positively regulate responses to ketoconazole stress by erg11 and erg6, key genes in the ergosterol biosynthetic pathway. Aha1, Sti1, and P23 are highly conserved in fungi, and sti1 and p23 deletion also increased the susceptibility to azoles in Fusarium verticillioides. These results indicate that Hsp90-cochaperones Aha1, Sti1, and P23 are critical for the basal azole resistance and could be potential targets for developing new antifungal agents.

  4. Comparative Hepatotoxicity of Fluconazole, Ketoconazole, Itraconazole, Terbinafine, and Griseofulvin in Rats.

    Science.gov (United States)

    Khoza, Star; Moyo, Ishmael; Ncube, Denver

    2017-01-01

    Oral ketoconazole was recently the subject of regulatory safety warnings because of its association with increased risk of inducing hepatic injury. However, the relative hepatotoxicity of antifungal agents has not been clearly established. The aim of this study was to compare the hepatotoxicity induced by five commonly prescribed oral antifungal agents. Rats were treated with therapeutic oral doses of griseofulvin, fluconazole, itraconazole, ketoconazole, and terbinafine. After 14 days, only ketoconazole had significantly higher ALT levels ( p = 0.0017) and AST levels ( p = 0.0008) than the control group. After 28 days, ALT levels were highest in the rats treated with ketoconazole followed by itraconazole, fluconazole, griseofulvin, and terbinafine, respectively. The AST levels were highest in the rats treated with ketoconazole followed by itraconazole, fluconazole, terbinafine, and griseofulvin, respectively. All drugs significantly elevated ALP levels after 14 days and 28 days of treatment ( p terbinafine, and griseofulvin. However, histopathological changes revealed that fluconazole was the most hepatotoxic, followed by ketoconazole, itraconazole, terbinafine, and griseofulvin, respectively. Given the poor correlation between liver enzymes and the extent of liver injury, it is important to confirm liver injury through histological examination.

  5. Effect of Hydroxypropyl Methylcellulose-Beeswax Composite Edible Coatings Formulated with or without Antifungal Agents on Physicochemical Properties of Plums during Cold Storage

    Directory of Open Access Journals (Sweden)

    Sule Gunaydin

    2017-01-01

    Full Text Available The influence of hydroxypropyl methylcellulose- (HPMC- beeswax (BW composite edible coatings formulated with or without food additives with antifungal properties on physicochemical and sensory properties of plums (Prunus salicina cv. “Friar” stored for 11 and 22 d at 1°C followed by a shelf life period of 5 d at 20°C was evaluated. Food preservatives selected from previous research included potassium sorbate (PS, sodium methyl paraben (SMP, and sodium ethyl paraben (SEP. Emulsions had 7% of total solid content and were prepared with glycerol and stearic acid as plasticizer and emulsifier, respectively. All the coatings reduced plum weight and firmness loss and coated fruit showed higher titratable acidity, soluble solids content, and hue angle values at the end of the storage period. In addition, physiological disorders such as flesh browning and bleeding were reduced in coated samples compared to uncoated controls. Paraben-based coatings were the most effective in controlling weight loss and the SMP-based coating was the most effective in maintaining plum firmness. Respiration rate, sensory flavor, off-flavors, and fruit appearance were not adversely affected by the application of antifungal coatings. Overall, these results demonstrated the potential of selected edible coatings containing antifungal food additives to extend the postharvest life of plums, although further studies should focus on improving some properties of the coatings to enhance gas barrier properties and further increase storability.

  6. Alteration of intestinal microbiota in mice orally administered with salmon cartilage proteoglycan, a prophylactic agent.

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    Krisana Asano

    Full Text Available Proteoglycan (PG extracted from salmon nasal cartilage has potential to be a prophylactic agent. Daily oral administration of the PG attenuates systemic inflammatory response in the experimental mouse models. In this study, we applied the culture-independent approach to investigate an alteration of intestinal microbiota composition in PG-administered mice. The results indicated that the population level of bacilli increased in the small and large intestine upon PG administration. On the other hand, the population level of clostridia decreased in the large intestine. The proportion of bacteria that are able to ferment saccharides and produce short-chain fatty acids increased in the small intestine and decreased in the large intestine. Importantly, population level of probiotic lactobacilli and bacteria exhibiting the immunomodulatory effect increased in the PG-administered mice. In addition, several disease-associated bacteria decreased upon PG administration. These results provided an understanding of the specific role of PG involved in host immune modulation and supported our hypothesis that daily oral administration of PG improves the overall balance in composition of the intestinal microbial community.

  7. Effect of ionizing energy on extracts of Quillaja saponaria to be used as an antimicrobial agent on irradiated edible coating for fresh strawberries

    International Nuclear Information System (INIS)

    Zuniga, G.E.; Junqueira-Goncalves, M.P.; Pizarro, M.; Contreras, R.; Tapia, A.; Silva, S.

    2012-01-01

    Incorporating antimicrobial compounds into edible films or coatings provides a novel way to improve the safety and shelf life of ready-to-eat foods. Diverse studies with Quillaja saponaria Mol. (popularly named quillay) extracts have demonstrated their potential as antifungal agents against phytopathogenic fungi. Crosslinking induced by ionizing radiation is an effective method for the improvement of both barrier and mechanical properties of the edible films and coatings based on milk proteins. However there are few reports about the effects of γ-radiation on plant extracts. The aim of this work was to evaluate the effect of ionizing radiation (0, 5, 10, 15, 20, 25 and 35 kGy) on extracts prepared from in vitro plants of Q. saponaria to be used as antimicrobial agent in irradiated edible coating based on calcium caseinate and whey protein isolated, and also to establish the concentration of Q. saponaria extract to be added as an antifungal agent in the coating. Gamma irradiation since 15 kGy affects negatively the antimicrobial activity and metabolites composition of extract of Q. saponaria by reducing compounds of phenolic nature. Otherwise no effect on saponins profile was observed even at higher doses. It was possible to conclude that the antifungal activity of Q. saponaria extract is mainly related to phenolic compounds content. In addition, our work also shows that to obtain an efficient antifungal protection is necessary to add a minimum concentration of 6% of the extract after the coating irradiation. - Highlights: → Antimicrobial compounds into edible coatings improve food' safety and shelf life. → Q. saponaria extract is an antifungal agent against phytopathogenic fungi. → Crosslinking induced by γ-radiation over 30 kGy improves properties of the coatings. → γ-radiation since 15 kGy affects the antimicrobial activity of Q. saponaria extract. → This extract should be added after the coating radiation, at a minimum of 6%.

  8. An inter-species signaling system mediated by fusaric acid has parallel effects on antifungal metabolite production by Pseudomonas protegens Pf-5 and antibiosis of Fusarium spp.

    Science.gov (United States)

    Pseudomonas protegens strain Pf-5 is a rhizosphere bacterium that acts as a biocontrol agent of soilborne plant diseases, and produces at least seven different secondary metabolites with antifungal properties. We derived site-directed mutants of Pf-5 with single and multiple mutations in the biosynt...

  9. Mode of Antifungal Drugs Interaction with Cytochrome P- 450

    Directory of Open Access Journals (Sweden)

    M- Mahmodian

    1991-07-01

    Full Text Available Computer was used to identify the interactions of substrates and antifungal drugs with the enzyme, Cytochrome P-450; and then Molplot.bas computer program was applied to get three dimensional figures of 5-hydroxy camphor.oxidation products of camphor analogues, and antifungal drugs.Cartesian characteristics of atoms building molecules, are taken from Buildz. for program, which can calculate X,Y,Z coordinates of atoms by Zmatrix data. The other program which can calculate X,Y,Z coordinates, using fractional characteristics, is the Coord, for program that, gives our cartesian characteristics of the atoms of molecule, then by using these data, we obtain three dimensional figures and distance between active atoms in compounds under consideration. Results show that distance between two oxygen atoms in 5-exo-hydroxy- camphor and the other compounds obtained from oxidation of camphor analogues, with the distance of two oxygen atoms in antifungal compounds under discussion are equal. Therefore, we can conclude that, the antifungal molecule also interacts with enzyme's active site, by its own sites, in a similar manner to the 5-hydroxy camphor molecule, which is:"n1. Nitrogen atom (N of Imidazole and Triazole ring in antifungal molecule with Iron atom in heam molecule belonging to Cytochrome P-450 enzyme, are coordinated."n2. The other atoms such as : 0,S or N in structure of the antifungal drug are coordinated with hydrogen atom of hydroxyl group belong ing to Tyr-96 in the structure of enzyme, forming hydrogen bonding.

  10. Isolation of Bacteria with Antifungal Activity against the Phytopathogenic Fungi Stenocarpella maydis and Stenocarpella macrospora

    Science.gov (United States)

    Petatán-Sagahón, Iván; Anducho-Reyes, Miguel Angel; Silva-Rojas, Hilda Victoria; Arana-Cuenca, Ainhoa; Tellez-Jurado, Alejandro; Cárdenas-Álvarez, Isabel Oyuki; Mercado-Flores, Yuridia

    2011-01-01

    Stenocarpella maydis and Stenocarpella macrospora are the causal agents of ear rot in corn, which is one of the most destructive diseases in this crop worldwide. These fungi are important mycotoxin producers that cause different pathologies in farmed animals and represent an important risk for humans. In this work, 160 strains were isolated from soil of corn crops of which 10 showed antifungal activity against these phytopathogens, which, were identified as: Bacillus subtilis, Pseudomonas spp., Pseudomonas fluorescens, and Pantoea agglomerans by sequencing of 16S rRNA gene and the phylogenetic analysis. From cultures of each strain, extracellular filtrates were obtained and assayed to determine antifungal activity. The best filtrates were obtained in the stationary phase of B. subtilis cultures that were stable to the temperature and extreme pH values; in addition they did not show a cytotoxicity effect against brine shrimp and inhibited germination of conidia. The bacteria described in this work have the potential to be used in the control of white ear rot disease. PMID:22016606

  11. Isolation of Bacteria with Antifungal Activity against the Phytopathogenic Fungi Stenocarpella maydis and Stenocarpella macrospora

    Directory of Open Access Journals (Sweden)

    Yuridia Mercado-Flores

    2011-08-01

    Full Text Available Stenocarpella maydis and Stenocarpella macrospora are the causal agents of ear rot in corn, which is one of the most destructive diseases in this crop worldwide. These fungi are important mycotoxin producers that cause different pathologies in farmed animals and represent an important risk for humans. In this work, 160 strains were isolated from soil of corn crops of which 10 showed antifungal activity against these phytopathogens, which, were identified as: Bacillus subtilis, Pseudomonas spp., Pseudomonas fluorescens, and Pantoea agglomerans by sequencing of 16S rRNA gene and the phylogenetic analysis. From cultures of each strain, extracellular filtrates were obtained and assayed to determine antifungal activity. The best filtrates were obtained in the stationary phase of B. subtilis cultures that were stable to the temperature and extreme pH values; in addition they did not show a cytotoxicity effect against brine shrimp and inhibited germination of conidia. The bacteria described in this work have the potential to be used in the control of white ear rot disease.

  12. New insights into the structure and mode of action of Mo-CBP3, an antifungal chitin-binding protein of Moringa oleifera seeds.

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    Adelina B Batista

    Full Text Available Mo-CBP3 is a chitin-binding protein purified from Moringa oleifera Lam. seeds that displays inhibitory activity against phytopathogenic fungi. This study investigated the structural properties and the antifungal mode of action of this protein. To this end, circular dichroism spectroscopy, antifungal assays, measurements of the production of reactive oxygen species and microscopic analyses were utilized. Mo-CBP3 is composed of 30.3% α-helices, 16.3% β-sheets, 22.3% turns and 30.4% unordered forms. The Mo-CBP3 structure is highly stable and retains its antifungal activity regardless of temperature and pH. Fusarium solani was used as a model organism for studying the mechanisms by which this protein acts as an antifungal agent. Mo-CBP3 significantly inhibited spore germination and mycelial growth at 0.05 mg.mL-1. Mo-CBP3 has both fungistatic and fungicidal effects, depending on the concentration used. Binding of Mo-CBP3 to the fungal cell surface is achieved, at least in part, via electrostatic interactions, as salt was able to reduce its inhibitory effect. Mo-CBP3 induced the production of ROS and caused disorganization of both the cytoplasm and the plasma membrane in F. solani cells. Based on its high stability and specific toxicity, with broad-spectrum efficacy against important phytopathogenic fungi at low inhibitory concentrations but not to human cells, Mo-CBP3 has great potential for the development of new antifungal drugs or transgenic crops with enhanced resistance to phytopathogens.

  13. Functionalised isocoumarins as antifungal compounds: Synthesis and biological studies.

    Science.gov (United States)

    Simic, Milena; Paunovic, Nikola; Boric, Ivan; Randjelovic, Jelena; Vojnovic, Sandra; Nikodinovic-Runic, Jasmina; Pekmezovic, Marina; Savic, Vladimir

    2016-01-01

    A series of novel 3-substituted isocoumarins was prepared via Pd-catalysed coupling processes and screened in vitro for antifungal activity against Candida species. The study revealed antifungal potential of isocoumarins possessing the azole substituents, which, in some cases, showed biological properties equal to those of clinically used voriconazole. Selected compounds were also screened against voriconazole resistant Candida krusei 6258 and a clinical isolate Candida parapsilosis CA-27. Although the activity against these targets needs to be improved further, the results emphasise additional potential of this new class of antifungal compounds. Copyright © 2015 Elsevier Ltd. All rights reserved.

  14. The relationship between salivary histatin levels and oral yeast carriage.

    Science.gov (United States)

    Jainkittivong, A; Johnson, D A; Yeh, C K

    1998-06-01

    Candida species are common commensal inhabitants of the oral cavity. Human saliva contains antifungal proteins called histatins. We tested the hypothesis that oral yeast status is related to salivary histatin levels. Thirty subjects were divided into two groups based on the presence (n = 15) or absence (n = 15) of yeast on oral mucosa surfaces. Unstimulated and stimulated submandibular and sublingual and parotid saliva was collected from each subject. Salivary flow rates were measured and histatin concentrations were determined in the stimulated saliva samples. The yeast colony positive group showed lower median unstimulated parotid saliva flow rates as well as lower median concentrations of total histatins in submandibular and sublingual saliva. There was a negative correlation between yeast colony-forming units and unstimulated parotid saliva flow rates and between yeast colony-forming units and submandibular and sublingual saliva histatin concentration and secretion. The results suggest that oral yeast status may be influenced by unstimulated parotid saliva flow rates and by submandibular and sublingual histatin concentration and secretion.

  15. Metabolism and resistance of Fusarium spp. to the manzamine alkaloids via a putative retro pictet-spengler reaction and utility of the rational design of antimalarial and antifungal agents.

    Science.gov (United States)

    Kasanah, Noer; Farr, Lorelei Lucas; Gholipour, Abbas; Wedge, David E; Hamann, Mark T

    2014-08-01

    As a part of our continuing investigation of the manzamine alkaloids we studied the in vitro activity of the β-carboline containing manzamine alkaloids against Fusarium solani, Fusarium oxysporium, and Fusarium proliferatum by employing several bioassay techniques including one-dimensional direct bioautography, dilution, and plate susceptibility, and microtiter broth assays. In addition, we also studied the metabolism of the manzamine alkaloids by Fusarium spp. in order to facilitate the redesign of the compounds to prevent resistance of Fusarium spp. through metabolism. The present research reveals that the manzamine alkaloids are inactive against Fusarium spp. and the fungi transform manzamines via hydrolysis, reduction, and a retro Pictet-Spengler reaction. This is the first report to demonstrate an enzymatically retro Pictet-Spengler reaction. The results of this study reveal the utility of the rational design of metabolically stable antifungal agents from this class and the development of manzamine alkaloids as antimalarial drugs through the utilization of Fusarium's metabolic products to reconstruct the molecule.

  16. Antifungal activity of nicotine and its cobalt complex

    International Nuclear Information System (INIS)

    Zaidi, M.I.; Gul, A.

    2005-01-01

    Nicotine and its metal complex; Co(II)-nicotine were isolated from leaves of Nicotiana tabacum using various metal ions by the reported techniques and studied for their antifungal activity against fourteen different species of fungi. For comparative study, pure sample of nicotine and metal salt used for complexation; cobalt(II) chloride was also subjected to antifungal tests with the same species of fungus under similar conditions. Results indicated that nicotine had antifungal activity against all species of fungi studied except Candida albicans, Microsporum canis, Epidermophyton floccosum, Candida tropicalis, and Alternaria infectoria. Cobalt(II) nicotine was found to be effective against all selected species of fungi but ineffective against Candida solani, Penicillium notalum, Microsporum canis, Fusarium solani and Fusarium moniliforme. (author)

  17. Antibacterial and antifungal properties of guanylhydrazones

    Directory of Open Access Journals (Sweden)

    Ajdačić Vladimir

    2017-01-01

    Full Text Available A series of novel guanylhydrazones were designed, synthesized and characterized. All the compounds were screened for their antibacterial and antifungal activity. Compounds 26 and 27 showed excellent antibacterial activities against Staphylococcus aureus ATCC 25923 and Micrococcus luteus ATCC 379 with minimal inhibitory concentrations of 4 μg mL-1, and good antifungal activity against Candida parapsilosis ATCC 22019. These results suggested that the selected guanylhydrazones could serve as promising leads for improved antimicrobial development. [Project of the Ministry of Education, Science and Technological Development of the Republic of Serbia, Grant No. 172008 and Grant No. 173048

  18. Cryptic antifungal compounds active by synergism with polyene antibiotics.

    Science.gov (United States)

    Kinoshita, Hiroshi; Yoshioka, Mariko; Ihara, Fumio; Nihira, Takuya

    2016-04-01

    The majority of antifungal compounds reported so far target the cell wall or cell membrane of fungi, suggesting that other types of antibiotics cannot exert their activity because they cannot penetrate into the cells. Therefore, if the permeability of the cell membrane could be enhanced, many antibiotics might be found to have antifungal activity. We here used the polyene antibiotic nystatin, which binds to ergosterol and forms pores at the cell membrane, to enhance the cellular permeability. In the presence of nystatin, many culture extracts from entomopathogenic fungi displayed antifungal activity. Among all the active extracts, two active components were purified and identified as helvolic acid and terramide A. Because the minimum inhibitory concentration of either compound was reduced four-fold in the presence of nystatin, it can be concluded that this screening method is useful for detecting novel antifungal activity. Copyright © 2015 The Society for Biotechnology, Japan. Published by Elsevier B.V. All rights reserved.

  19. Antifungal Attributes of Lactobacillus plantarum MYS6 against Fumonisin Producing Fusarium proliferatum Associated with Poultry Feeds

    Science.gov (United States)

    Deepthi, B. V.; Poornachandra Rao, K.; Chennapa, G.; Naik, M. K.; Chandrashekara, K. T.; Sreenivasa, M. Y.

    2016-01-01

    Fumonisins, being common in occurrence in maize-based feeds, pose a great threat to animal and human health. The present study is aimed at determining the antifungal activity of Lactobacillus plantarum MYS6 against a fumonisin producing fungus, Fusarium proliferatum MYS9. The isolate was subjected to standard tests for determining its probiotic attributes and antifungal properties. L. plantarum MYS6 thrived well at pH 3.0 and 6.0, and exhibited strong resistance up to 3% bile. The isolate showed a high degree of cell surface hydrophobicity corresponding to its strong adhesion to chicken crop epithelial cells. Co-inoculation with the fungus on modified de Man Rogosa Sharpe medium revealed the inhibitory effect of L. plantarum MYS6 on fungal growth and biomass. Observation using scanning electron microscopy showed distortion of hyphal structures, swollen tips and disrupted conidia. Conidia germination inhibition assay restrained germination and showed deformed hyphae. The bioprotective feature of the isolate was evident by the inhibition of fungal development in maize-kernel treated with the cell free supernatant of L. plantarum MYS6. Both the isolate and its extracellular metabolites lowered fumonisin content in feed model up to 0.505 mg/Kg of feed and 0.3125 mg/Kg of feed respectively when compared to the level of 0.870 mg/Kg of feed in control. The major antifungal compounds produced by the isolate were 10-Octadecenoic acid, methyl ester; palmitic acid, methyl ester; heptadecanoic acid, 16-methyl ester; stearic acid and lauric acid. L. plantarum MYS6 reduced 61.7% of fumonisin possibly by a binding mechanism. These findings suggest the application of L. plantarum MYS6 as an efficient probiotic additive and biocontrol agent in feed used in poultry industry. Additionally, the antifungal metabolites pose a conspicuous inhibition of Fusarium growth and fumonisin production. PMID:27285317

  20. Antifungal Attributes of Lactobacillus plantarum MYS6 against Fumonisin Producing Fusarium proliferatum Associated with Poultry Feeds.

    Science.gov (United States)

    Deepthi, B V; Poornachandra Rao, K; Chennapa, G; Naik, M K; Chandrashekara, K T; Sreenivasa, M Y

    2016-01-01

    Fumonisins, being common in occurrence in maize-based feeds, pose a great threat to animal and human health. The present study is aimed at determining the antifungal activity of Lactobacillus plantarum MYS6 against a fumonisin producing fungus, Fusarium proliferatum MYS9. The isolate was subjected to standard tests for determining its probiotic attributes and antifungal properties. L. plantarum MYS6 thrived well at pH 3.0 and 6.0, and exhibited strong resistance up to 3% bile. The isolate showed a high degree of cell surface hydrophobicity corresponding to its strong adhesion to chicken crop epithelial cells. Co-inoculation with the fungus on modified de Man Rogosa Sharpe medium revealed the inhibitory effect of L. plantarum MYS6 on fungal growth and biomass. Observation using scanning electron microscopy showed distortion of hyphal structures, swollen tips and disrupted conidia. Conidia germination inhibition assay restrained germination and showed deformed hyphae. The bioprotective feature of the isolate was evident by the inhibition of fungal development in maize-kernel treated with the cell free supernatant of L. plantarum MYS6. Both the isolate and its extracellular metabolites lowered fumonisin content in feed model up to 0.505 mg/Kg of feed and 0.3125 mg/Kg of feed respectively when compared to the level of 0.870 mg/Kg of feed in control. The major antifungal compounds produced by the isolate were 10-Octadecenoic acid, methyl ester; palmitic acid, methyl ester; heptadecanoic acid, 16-methyl ester; stearic acid and lauric acid. L. plantarum MYS6 reduced 61.7% of fumonisin possibly by a binding mechanism. These findings suggest the application of L. plantarum MYS6 as an efficient probiotic additive and biocontrol agent in feed used in poultry industry. Additionally, the antifungal metabolites pose a conspicuous inhibition of Fusarium growth and fumonisin production.

  1. Evaluation of Antifungal Potentials and Antioxidant Capacities of Some Foliose Lichen Species

    Directory of Open Access Journals (Sweden)

    Bahar BİLGİN SÖKMEN

    2018-03-01

    Full Text Available This work is aimed to assess of antioxidant and antifungal potential of the foliose lichen species: Flavoparmelia caperata, Xanthoparmelia stenophylla and Xanthoparmelia conspersa. The antifungal activity of lichens were studied against some pathogenic fungi by disc diffusion method. The acetonitrile extracts of these lichens were obtained with Soxhlet extraction. While F. caperata exhibited maximum antifungal activity (32 mm against the C. albicans, the minimum antifungal activity (10 mm was obtained from X. stenophylla lichen against S. cerevisiae. In CUPRAC assay, absorbance values was in order of BHT>X. conspersa>F. caperata>X. stenophylla. As a result of the study, it was concluded that these lichen species may be a potential source for the development of new antifungal and antioxidant compounds.

  2. Synergism of Antifungal Activity between Mitochondrial Respiration Inhibitors and Kojic Acid

    Directory of Open Access Journals (Sweden)

    Ronald P. Haff

    2013-01-01

    Full Text Available Co-application of certain types of compounds to conventional antimicrobial drugs can enhance the efficacy of the drugs through a process termed chemosensitization. We show that kojic acid (KA, a natural pyrone, is a potent chemosensitizing agent of complex III inhibitors disrupting the mitochondrial respiratory chain in fungi. Addition of KA greatly lowered the minimum inhibitory concentrations of complex III inhibitors tested against certain filamentous fungi. Efficacy of KA synergism in decreasing order was pyraclostrobin > kresoxim-methyl > antimycin A. KA was also found to be a chemosensitizer of cells to hydrogen peroxide (H2O2, tested as a mimic of reactive oxygen species involved in host defense during infection, against several human fungal pathogens and Penicillium strains infecting crops. In comparison, KA-mediated chemosensitization to complex III inhibitors/H2O2 was undetectable in other types of fungi, including Aspergillus flavus, A. parasiticus, and P. griseofulvum, among others. Of note, KA was found to function as an antioxidant, but not as an antifungal chemosensitizer in yeasts. In summary, KA could serve as an antifungal chemosensitizer to complex III inhibitors or H2O2 against selected human pathogens or Penicillium species. KA-mediated chemosensitization to H2O2 seemed specific for filamentous fungi. Thus, results indicate strain- and/or drug-specificity exist during KA chemosensitization.

  3. Efficacy and safety of a single oral 150 mg dose of fluconazole for the treatment of vulvovaginal candidiasis in Japan.

    Science.gov (United States)

    Mikamo, Hiroshige; Matsumizu, Miyako; Nakazuru, Yoshiomi; Okayama, Akifumi; Nagashima, Masahito

    2015-07-01

    Vulvovaginal candidiasis is the second most common cause of vaginal infections following bacterial vaginosis. For the treatment of vulvovaginal candidiasis, antifungal agents are used either as topical (vaginal tablets and cream) or oral formulations. A single oral 150 mg dose of fluconazole has been recommended as the standard therapy for uncomplicated, acute vulvovaginal candidiasis in global guidelines; however, in Japan oral fluconazole therapy has not been approved. We conducted a phase 3 study to evaluate the efficacy and safety of a single oral 150 mg dose of fluconazole in Japanese subjects with vulvovaginal candidiasis for regulatory submission. A total of 157 subjects received a single oral 150 mg dose of fluconazole. Candida species (104 strains) were identified by fungal culture from 102 subjects at baseline, including Candida albicans (100 strains). The efficacy rate for the therapeutic outcome (assessed based on a comprehensive evaluation of the clinical and mycological efficacy in each subject) was 74.7% (74/99) on Day 28 in the modified Intent-To-Treat (m-ITT) population. Concerning the clinical and mycological efficacy on Day 28 in the m-ITT population, the cure, cure or improvement, and eradication rates were 81.6%, 95.9%, and 85.9%, respectively. The most common treatment-related adverse events were diarrhea and nausea (1.9% for each). No clinically significant safety issues were reported. A single oral 150 mg dose of fluconazole demonstrated excellent therapeutic efficacy and was well tolerated in Japanese subjects with vulvovaginal candidiasis. NCT01806623. Copyright © 2015 Japanese Society of Chemotherapy and The Japanese Association for Infectious Diseases. Published by Elsevier Ltd. All rights reserved.

  4. ANTI-FUNGAL ACTIVITIES OF m-IODOBENZOIC ACID AND SOME ...

    African Journals Online (AJOL)

    The anti-fungal activities of alkali and alkaline earth metal iodobenzoates were studied. Calcium iodobenzoate exhibited the highest anti-fungal activities of 74.60% inhibition for 15 ppm while sodium iodobenzoate exhibited the least inhibition of 61.64%. An optimum concentration of all the metal complexes for inhibition ...

  5. Adverse drug events in the oral cavity.

    Science.gov (United States)

    Yuan, Anna; Woo, Sook-Bin

    2015-01-01

    Adverse reactions to medications are common and may have a variety of clinical presentations in the oral cavity. Targeted therapies and the new biologic agents have revolutionized the treatment of cancers, autoimmune diseases, and inflammatory and rheumatologic diseases but have also been associated with adverse events in the oral cavity. Some examples include osteonecrosis, seen with not only bisphosphonates but also antiangiogenic agents, and the distinctive ulcers caused by mammalian target of rapamycin inhibitors. As newer therapeutic agents are approved, it is likely that more adverse drug events will be encountered. This review describes the most common clinical presentations of oral mucosal reactions to medications, namely, xerostomia, lichenoid reactions, ulcers, bullous disorders, pigmentation, fibrovascular hyperplasia, white lesions, dysesthesia, osteonecrosis, infection, angioedema, and malignancy. Oral health care providers should be familiar with such events, as they will encounter them in their practice. Copyright © 2015 Elsevier Inc. All rights reserved.

  6. Fundamental studies of oral contrast agents for MR. Comparison of manganese agent and iron agent

    International Nuclear Information System (INIS)

    Fujita, Osamu; Hiraishi, Kumiko; Suginobu, Yoshito; Takeuchi, Masayasu; Narabayashi, Isamu

    1996-01-01

    We investigated and compared signal intensity and the effect of imaging the upper abdomen with blueberry juice (B.J.), a Mn agent utilizing the properties of paramagnetic metals, and FerriSeltz (F.S.), an iron agent. Since the relaxation effect was much stronger with B.J. than with F.S., the signal intensity required of a peroral contrast agent was able to be obtained at a much lower concentration of B.J. In imaging the upper abdomen, B.J. had a positive effect on imaging in T1-weighted images, and a negative effect in T2-weighted images. F.S. had a positive imaging effect in both, and because it showed extremely high signals in T2-weighted images, motion artifact arose. (author)

  7. Safe practices and financial considerations in using oral chemotherapeutic agents.

    Science.gov (United States)

    Bartel, Sylvia B

    2007-05-01

    Safe handling practices and financial concerns associated with oral chemotherapy in non-traditional settings are discussed. Oral chemotherapy may pose a risk to patients because of a narrow therapeutic index, complex dosing regimen, dispensing by community pharmacists without prescription order review by an oncology pharmacist or nurse, or self-administration in the home or another nontraditional setting, where patient monitoring is infrequent. Errors in prescribing, dispensing, and administration and patient or caregiver misunderstandings are potential problems with the use of oral chemotherapy that need to be addressed when developing safe practices. Changes in Medicare pharmaceutical reimbursement rates and rules need to be monitored because they have the potential to affect patient care and outcomes. Patient assistance programs and advocacy groups can help alleviate financial concerns associated with oral chemotherapy. Consensus guidelines specific to safe handling of oral chemotherapy in the home or other nontraditional setting need to be developed. Also, healthcare providers must understand reimbursement and provide direction to patients when patient assistance programs or advocacy groups can assist with the financial challenges of oral chemotherapy.

  8. Antifungal activity of rice straw extract on some phytopathogenic fungi

    African Journals Online (AJOL)

    user

    2012-09-04

    Sep 4, 2012 ... antifungal properties, thus it can be used as a natural alternative approach to synthetic ..... composition and antifungal activity of essential oils of seven ... Leaf Extracts on Seed-borne Fungi of African Yam Bean Seeds,.

  9. Antifungal Activity of Endemic Salvia tigrina in Turkey | Dulger ...

    African Journals Online (AJOL)

    Ketoconazole was used as a positive reference standard to determine the sensitivity of the strains. Results: The minimum inhibitory concentration (MIC) ranged from 3.12 to 25 mg/mL. All the extracts exhibited a strong antifungal effect against the fungal cultures. The extracts exhibited greater antifungal effect against C.

  10. Antifungal and antioxidant activity of fatty acid methyl esters from vegetable oils

    Directory of Open Access Journals (Sweden)

    MARIA E.A. PINTO

    2017-08-01

    Full Text Available ABSTRACT Fatty acid methyl esters (FAMEs were obtained from vegetable oils of soybean, corn and sunflower. The current study was focused on evaluating the antifungal activity of FAMEs mainly against Paracoccidioides spp., as well as testing the interaction of these compounds with commercial antifungal drugs and also their antioxidant potential. FAMEs presented small IC50 values (1.86-9.42 μg/mL. All three FAMEs tested showed antifungal activity against isolates of Paracoccidioides spp. with MIC values ranging from 15.6-500 µg/mL. Sunflower FAMEs exhibited antifungal activity that extended also to other genera, with an MIC of 15.6 μg/mL against Candida glabrata and C. krusei and 31.2 μg/mL against C. parapsilosis. FAMEs exhibited a synergetic effect with itraconazole. The antifungal activity of the FAMEs against isolates of Paracoccidioides spp. is likely due to the presence of methyl linoleate, the major compound present in all three FAMEs. The results obtained indicate the potential of FAMEs as sources for antifungal and antioxidant activity.

  11. Production, characterization, and antifungal activity of a biosurfactant produced by Rhodotorula babjevae YS3.

    Science.gov (United States)

    Sen, Suparna; Borah, Siddhartha Narayan; Bora, Arijit; Deka, Suresh

    2017-05-30

    study reports, for the first time, the biosurfactant producing ability of R. babjevae, a relatively lesser studied yeast. The persistent surface active properties of the sophorolipid in extreme conditions advocates its applicability in diverse environmental and industrial sectors. Further, antifungal activities against plant and human pathogens opens up possibilities for development of efficient and eco-friendly antifungal agents with agricultural and biomedical applications.

  12. Evaluation of the antifungal effects of bio-oil prepared with lignocellulosic biomass using fast pyrolysis technology.

    Science.gov (United States)

    Kim, Kwang Ho; Jeong, Han Seob; Kim, Jae-Young; Han, Gyu Seong; Choi, In-Gyu; Choi, Joon Weon

    2012-10-01

    This study was performed to investigate the utility of bio-oil, produced via a fast pyrolysis process, as an antifungal agent against wood-rot fungi. Bio-oil solutions (25-100 wt.%) were prepared by diluting the bio-oil with EtOH. Wood block samples (yellow poplar and pitch pine) were treated with diluted bio-oil solutions and then subjected to a leaching process under hot water (70°C) for 72 h. After the wood block samples were thoroughly dried, they were subjected to a soil block test using Tyromyces palustris and Trametes versicolor. The antifungal effect of the 75% and 100% bio-oil solutions was the highest for both wood blocks. Scanning electron microscopy analysis indicated that some chemical components in the bio-oil solution could agglomerate together to form clusters in the inner part of the wood during the drying process, which could act as a wood preservative against fungal growth. According to GC/MS analysis, the components of the agglomerate were mainly phenolic compounds derived from lignin polymers. Copyright © 2012 Elsevier Ltd. All rights reserved.

  13. Antifungal effect of Sticophus hermanii and Holothuria atra extract and its cytotoxicity on gingiva-derived mesenchymal stem cell

    Directory of Open Access Journals (Sweden)

    Kristanti Parisihni

    2013-12-01

    Full Text Available Background: Sea cucumber had been acknowledged to have some medical properties Sticophus hermanii and Holothuria atra are species of sea cucumber which has been known to have antifungal properties thus potentially explored as therapeutic agent in oral candidiasis. Purpose: The aim of this study was to examine the antifungal property Sticophus hermanii and Holothuria atra extract against Candida albicans and its cytotoxicity to human gingiva-derived mesenchymal stem cell. Methods: The study was an experimental laboratories research with post test only control group design. Methanolic extract of Sticophus hermanii and Holothuria atra in concentrations of 1%, 0.5%; 0.25%; 0.13%, 0.07%; 0.03%, 0.02% and 0.01%; were tested its cytotoxicity on gingiva-derived mesenchymal stem cell. Cell viability were measured by MTT assay. The antifungal property against Candida albicans was tested by disk diffusion method. Data were analyzed by ANOVA followed by LSD. Results: Extract of Sticophus hermanii showed no cytotoxicity in all concentrations (p>0.05, while Holothuria atra showed toxicity in the concentration of 1% and not cytotoxic in the concentrations below (p<0.05. Both sea cucumber extract could inhibit the growth Candida albicans, in vitro, proved by the clear zone around the disc in all concentrations (p<0.05. Conclusion: Stichopus hermanii and Holothuria atra extract had the antifungal effect against Candida albicans. Sea cucumber extract were not cytotoxic togingiva-derived mesenchymal stem cell in the concentration of Sticophus hermanii ≤ 1% and Holothuria atra ≤ 0.5%.Latar belakang: Teripang telah diketahui mempunyai berbagai khasiat medis. Sticophus hermanii dan Holothuria atra adalah spesies teripang yang telah diketahui mempunyai sifat anti jamur sehingga santat potensial untuk diekplorasi sebagai agen terapeutik pada infeksi di rongga mulut. Tujuan: Tujuan dari penelitian ini adalah untuk meneliti sifat anti jamur ekstrak Sticophus hermanii

  14. In vitro control of Alternaria citri using antifungal potentials of ...

    African Journals Online (AJOL)

    In vitro control of Alternaria citri using antifungal potentials of Trichoderma species. Asma Murtaza, Shazia Shafique, Tehmina Anjum, Sobiya Shafique. Abstract. The antifungal potential of five species of Trichoderma viz., Trichoderma viride, Trichoderma aureoviride, Trichoderma reesei, Trichoderma koningii and ...

  15. Isolation of antifungally active lactobacilli from edam cheese

    DEFF Research Database (Denmark)

    Tuma, S.; Vogensen, Finn Kvist; Plocková, M.

    2007-01-01

    The antifungal activity of 322 lactobacilli strains isolated from Edam cheese at different stages of the ripening process was tested against Fusarium proliferatum M 5689 using a dual overlay spot assay. Approximately 21% of the isolates showed a certain level of inhibitory activity. Seven strains...... as Lb. paracasei and three as Lb. fermentum. Lb. paracasei ST 68 was chosen for further testing as antifungal protective adjunct for Edam cheese production.  ...

  16. Production and characterization of antifungal compounds produced by Lactobacillus plantarum IMAU10014.

    Directory of Open Access Journals (Sweden)

    HaiKuan Wang

    Full Text Available Lactobacillus plantarum IMAU10014 was isolated from koumiss that produces a broad spectrum of antifungal compounds, all of which were active against plant pathogenic fungi in an agar plate assay. Two major antifungal compounds were extracted from the cell-free supernatant broth of L. plantarum IMAU10014. 3-phenyllactic acid and Benzeneacetic acid, 2-propenyl ester were carried out by HPLC, LC-MS, GC-MS, NMR analysis. It is the first report that lactic acid bacteria produce antifungal Benzeneacetic acid, 2-propenyl ester. Of these, the antifungal products also have a broad spectrum of antifungal activity, namely against Botrytis cinerea, Glomerella cingulate, Phytophthora drechsleri Tucker, Penicillium citrinum, Penicillium digitatum and Fusarium oxysporum, which was identified by the overlay and well-diffusion assay. F. oxysporum, P. citrinum and P. drechsleri Tucker were the most sensitive among molds.

  17. Effectiveness and tolerability of second-line therapy with vildagliptin versus other oral agents in type 2 diabetes (EDGE): post-hoc subanalysis of the Belgian data.

    Science.gov (United States)

    Hoste, J; Daci, E; Mathieu, C

    2014-06-01

    To assess the efficacy and safety of vildagliptin versus other oral glucose-lowering drugs added to antidiabetic monotherapy in Belgian patients with type 2 diabetes mellitus, in comparison to the global EDGE study results. This is a pre-specified post-hoc subanalysis of the Belgian patient cohort from a worldwide 1-year observational study that compared the effectiveness and tolerability of vildagliptin to other oral antidiabetic agents in type 2 diabetes patients failing monotherapy with oral glucose-lowering agents (EDGE). A total of 1793 Belgian patients were enrolled. Physicians could add any oral antidiabetic drug and patients entered either into the vildagliptin or the comparator cohort. The primary effectiveness and tolerability endpoint was defined as the proportion of patients having a treatment response (HbA1c reduction from baseline to month 12 endpoint >0·3%) without hypoglycemia, weight gain, peripheral oedema, or gastrointestinal side-effects. In the Belgian population, 37·8% of patients in the vildagliptin group and 32·8% in the comparator group had a decrease in HbA1c of >0·3% without the predefined tolerability issues of hypoglycemia, weight gain, oedema or, gastrointestinal complaints (primary endpoint), resulting in an unadjusted odds ratio of 1·24 (95% CI: 0·96-1·61). Mean HbA1c change from baseline was -0·81% in the vildagliptin cohort and -0·75% in the comparator cohort. Overall, vildagliptin was well tolerated with similarly low incidences of total adverse events (14·9% versus 14·5% in the compactor group) and serious adverse events (2·7% versus 2·5% in the comparator group). In this EDGE subgroup of Belgian patients with type 2 diabetes who do not achieve the glycemic targets with monotherapy, a similar trend as in the global EDGE study was observed. Adding vildagliptin as a second oral glucose-lowering agent resulted in lowering HbA1c to <7% without weight gain, hypoglycemia or peripheral oedema in a higher proportion of

  18. In vitro antifungal activity of Dorstenia mannii leaf extracts (Moraceae)

    African Journals Online (AJOL)

    Owner

    The active ingredients of this plant could be an addition to the antifungal arsenal to opportunistic fungal yeast pathogens. Key words: Antifungal activity, Dorstenia mannii, yeasts, opportunistic candidiasis. INTRODUCTION. Nowadays, fungal diseases have emerged and are being increasingly recognized as important public ...

  19. Trypanocide, cytotoxic, and antifungal activities of Momordica charantia.

    Science.gov (United States)

    Santos, Karla K A; Matias, Edinardo F F; Sobral-Souza, Celestina E; Tintino, Saulo R; Morais-Braga, Maria F B; Guedes, Glaucia M M; Santos, Francisco A V; Sousa, Ana Carla A; Rolón, Miriam; Vega, Celeste; de Arias, Antonieta Rojas; Costa, José G M; Menezes, Irwin R A; Coutinho, Henrique D M

    2012-02-01

    Chagas disease, caused by Trypanosoma cruzi, is a public health problem. Currently, chemotherapy is the only available treatment for this disease, and the drugs used, nifurtimox and benzonidazol, present high toxicity levels. An alternative for replacing these drugs are natural extracts from Momordica charantia L. (Cucurbitaceae) used in traditional medicine because of their antimicrobial and biological activities. In this study, we evaluated the extract of M. charantia for its antiepimastigote, antifungal, and cytotoxic activities. An ethanol extract of leaves from M. charantia was prepared. To research in vitro antiepimastigote activity, T. cruzi CL-B5 clone was used. Epimastigotes were inoculated at a concentration of 1 × 10(5) cells/mL in 200 µl tryptose-liver infusion. For the cytotoxicity assay, J774 macrophages were used. The antifungal activity was evaluated by microdilution using strains of Candida albicans, Candida tropicalis, and Candida krusei. The effective concentration capable of killing 50% of parasites (IC(50)) was 46.06 µg/mL. The minimum inhibitory concentration (MIC) was ≤ 1024 µg/mL. Metronidazole showed a potentiation of its antifungal effect when combined with an extract of M. charantia. Our results indicate that M. charantia could be a source of plant-derived natural products with antiepimastigote and antifungal-modifying activity with moderate toxicity.

  20. Hydrogel of Ketoconazole and PAMAM Dendrimers: Formulation and Antifungal Activity

    Directory of Open Access Journals (Sweden)

    Elzbieta Tryniszewska

    2012-04-01

    Full Text Available Ketoconazole (KET, an imidazole derivative with well-known antifungal properties, is lipophilic and practically insoluble in water, therefore its clinical use has some practical disadvantages. The aim of the present study was to investigate the influence of PAMAM-NH2 and PAMAM-OH dendrimers generation 2 and generation 3 on the solubility and antifungal activity of KET and to design and evaluate KET hydrogel with PAMAM dendrimers. It was shown that the surface charge of PAMAM dendrimers strongly affects their influence on the improvement of solubility and antifungal activity of KET. The MIC and MFC values obtained by broth dilution method indicate that PAMAM-NH2 dendrimers significantly (up to 16-fold increased the antifungal activity of KET against Candida strains (e.g., in culture Candida albicans 1103059/11 MIC value was 0.008 μg/mL and 0.064 μg/mL, and MFC was 2 μg/mL and 32 μg/mL for KET in 10 mg/mL solution of PAMAM-NH2 G2 and pure KET, respectively. Antifungal activity of designed KET hydrogel with PAMAM-NH2 dendrimers measured by the plate diffusion method was definitely higher than pure KET hydrogel and than commercial available product. It was shown that the improvement of solubility and in the consequence the higher KET release from hydrogels seems to be a very significant factor affecting antifungal activity of KET in hydrogels containing PAMAM dendrimers.