WorldWideScience

Sample records for antifungal agents

  1. 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.

    2009-01-01

    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 stra

  2. Chalcone derivatives as potential antifungal agents: Synthesis, and antifungal activity

    Directory of Open Access Journals (Sweden)

    Deepa Gupta

    2015-01-01

    Full Text Available Much research has been carried out with the aim to discover the therapeutic values of chalcone derivatives. Chalcones possess wide range of pharmacological activity such as antibacterial, antimalarial, antiprotozoal, antitubercular, anticancer, and antifungal agents etc. The presence of reactive α,β-unsaturated keto group in chalcones is found to be responsible for their biological activity. The rapid developments of resistance to antifungal agents, led to design, and synthesize the new antifungal agents. The derivatives of chalcones were prepared using Claisen-Schmidt condensation scheme with appropriate tetralone and aldehyde derivatives. Ten derivatives were synthesized and were biologically screened for antifungal activity. The newly synthesized derivatives of chalcone showed antifungal activity against fungal species, Microsporum gypseum. The results so obtained were superior or comparable to ketoconazole. It was observed that none of the compounds tested showed positive results for fungi Candida albicans nor against fungi Aspergillus niger. Chalcone derivatives showed inhibitory effect against M. gypseum species of fungus. It was found that among the chalcone derivatives so synthesized, two of them, that is, 4-chloro derivative, and unsubstituted derivative of chalcone showed antifungal activity superior to ketoconazole. Thus, these can be the potential new molecule as antifungal agent.

  3. Antifungal agents in neonates: issues and recommendations.

    Science.gov (United States)

    Almirante, Benito; Rodríguez, Dolors

    2007-01-01

    Fungal infections are responsible for considerable morbidity and mortality in the neonatal period, particularly among premature neonates. Four classes of antifungal agents are commonly used in the treatment of fungal infections in pediatric patients: polyene macrolides, fluorinated pyrimidines, triazoles, and echinocandins. Due to the paucity of pediatric data, many recommendations for the use of antifungal agents in this population are derived from the experience in adults. The purpose of this article was to review the published data on fungal infections and antifungal agents, with a focus on neonatal patients, and to provide an overview of the differences in antifungal pharmacology in neonates compared with adults. Pharmacokinetic data suggest dosing differences in children versus adult patients with some antifungals, but not all agents have been fully evaluated. The available pharmacokinetic data on the amphotericin B deoxycholate formulation in neonates exhibit considerable variability; nevertheless, the dosage regimen suggested in the neonatal population is similar to that used in adults. More pharmacokinetic information is available on the liposomal and lipid complex preparations of amphotericin B and fluconazole, and it supports their use in neonates; however, the optimal dosage and duration of therapy is difficult to establish. All amphotericin-B formulations, frequently used in combination with flucytosine, are useful for treating disseminated fungal infections and Candida meningitis in neonates. Fluconazole, with potent in vitro activity against Cryptococcus neoformans and almost all Candida spp., has been used in neonates with invasive candidiasis at dosages of 6 mg/kg/day, and for antifungal prophylaxis in high-risk neonates. There are limited data on itraconazole, voriconazole, and posaconazole use in neonates. Caspofungin, which is active against Candida spp. and Aspergillus spp., requires higher doses in children relative to adults, and dosing is

  4. Lipid-based antifungal agents: current status.

    Science.gov (United States)

    Arikan, S; Rex, J H

    2001-03-01

    Immunocompromised patients are well known to be predisposed to developing invasive fungal infections. These infections are usually difficult to diagnose and more importantly, the resulting mortality rate is high. The limited number of antifungal agents available and their high rate of toxicity are the major factors complicating the issue. However, the development of lipid-based formulations of existing antifungal agents has opened a new era in antifungal therapy. The best examples are the lipid-based amphotericin B preparations, amphotericin B lipid complex (ABLC; Abelcet), amphotericin B colloidal dispersion (ABCD; Amphotec or Amphocil), and liposomal amphotericin B (AmBisome). These formulations have shown that antifungal activity is maintained while toxicity is reduced. This progress is followed by the incorporation of nystatin into liposomes. Liposomal nystatin formulation is under development and studies of it have provided encouraging data. Finally, lipid-based formulations of hamycin, miconazole, and ketoconazole have been developed but remain experimental. Advances in technology of liposomes and other lipid formulations have provided promising new tools for management of fungal infections.

  5. DYSREGULATION OF ION HOMEOSTASIS BY ANTIFUNGAL AGENTS

    Directory of Open Access Journals (Sweden)

    Yongqiang eZhang

    2012-04-01

    Full Text Available Ion signaling and transduction networks are central to fungal development and virulence because they regulate gene expression, filamentation, host association and invasion, pathogen stress response and survival. Dysregulation of ion homeostasis rapidly mediates cell death, forming the mechanistic basis by which a growing number of amphipathic but structurally unrelated compounds elicit antifungal activity. Included in this group is carvacrol, a terpenoid phenol that is a prominent component of oregano and other plant essential oils. Carvacrol triggers an early dose dependent Ca2+ burst and long lasting pH changes in the model yeast S. cerevisiae. The distinct phases of ionic transients and a robust transcriptional response that overlaps with Ca2+ stress and nutrient starvation point to specific signaling events elicited by plant terpenoid phenols, rather than a non-specific lesion of the membrane as was previously considered. We discuss the potential use of plant essential oils and other agents that disrupt ion signaling pathways as chemosensitizers to augment conventional antifungal therapy, and to convert fungistatic drugs with strong safety profiles into fungicides.

  6. Research to Identify Effective Antifungal Agents, 1993 Annual Report.

    Energy Technology Data Exchange (ETDEWEB)

    Schreck, Carl

    1993-10-01

    This study is a continuation of ``Research to Identify Effective Antifungal Agents'' sponsored by Bonneville Power Administration (Schreck et al. 1990, 1991, and 1992). The objectives of the present study were to select and evaluate candidate fungicides.

  7. Synthesis, Antifungal Activities and Qualitative Structure Activity Relationship of Carabrone Hydrazone Derivatives as Potential Antifungal Agents

    Directory of Open Access Journals (Sweden)

    Hao Wang

    2014-03-01

    Full Text Available Aimed at developing novel fungicides for relieving the ever-increasing pressure of agricultural production caused by phytopathogenic fungi, 28 new hydrazone derivatives of carabrone, a natural bioactive sesquisterpene, in three types were designed, synthesized and their antifungal activities against Botrytis cinerea and Colletotrichum lagenarium were evaluated. The result revealed that all the derivatives synthesized exhibited considerable antifungal activities in vitro and in vivo, which led to the improved activities for carabrone and its analogues and further confirmed their potential as antifungal agents.

  8. Isobolographic Analysis of Pharmacodynamic Interactions between Antifungal Agents and Ciprofloxacin against Candida albicans and Aspergillus fumigatus▿

    OpenAIRE

    Stergiopoulou, Theodouli; Meletiadis, Joseph; Sein, Tin; Papaioannidou, Paraskevi; Tsiouris, Ioannis; Roilides, Emmanuel; Walsh, Thomas J.

    2008-01-01

    Patients suffering from invasive mycoses often receive concomitant antifungal therapy and antibacterial agents. Assessment of pharmacodynamic interactions between antifungal and antibacterial agents is complicated by the absence of a common antifungal end point for both agents. Ciprofloxacin has no intrinsic antifungal activity but may interact with antifungal agents, since it inhibits DNA gyrase (topoisomerase II), which is abundant in fungi. We therefore employed isobolographic analysis ada...

  9. Antifungal activity of propolis against Fonsecaea pedrosoi, a chromoblastomycosis agent

    OpenAIRE

    2011-01-01

    Chromoblastomycosis is a subcutaneous mycosis caused by dematiaceous fungi, being Fonsecaea pedrosoi the main etiologic agent in Brazil. Propolis is a resinous material collected by honeybees, with variable composition and pharmacological properties, including antifungal activity. The antifungal activity of ethanolic extracts of propolis (EEP) obtained from different municipalities of the state of Rio Grande do Sul, Brazil, against F. pedrosoi strains was assessed. The EEP showed MIC values b...

  10. New and emerging antifungal agents: impact on respiratory infections.

    Science.gov (United States)

    Feldmesser, Marta

    2003-01-01

    Fungal pathogens are increasingly important causes of respiratory disease, yet the number of antifungal agents available for clinical use is limited. Use of amphotericin B deoxycholate is hampered by severe toxicity. Triazole agents currently available have significant drug interactions; fluconazole has a limited spectrum of activity and itraconazole was, until recently, available only in oral formulations with limited bioavailability. The development of resistance to all three agents is increasingly being recognized and some filamentous fungi are resistant to the action of all of these agents. In the past few years, new antifungal agents and new formulations of existing agents have become available.The use of liposomal amphotericin B preparations is associated with reduced, but still substantial, rates of nephrotoxicity and infusion-related reactions. An intravenous formulation of itraconazole has been introduced, and several new triazole agents have been developed, with the view of identifying agents that have enhanced potency, broader spectra of action and improved pharmacodynamic properties. One of these, voriconazole, has completed large-scale clinical trials. In addition, caspofungin, the first of a new class of agents, the echinocandins, which inhibit cell wall glucan synthesis, was approved for use in the US in 2001 as salvage therapy for invasive aspergillosis. It is hoped that the availability of these agents will have a significant impact on the morbidity and mortality of fungal respiratory infections. However, at the present time, our ability to assess their impact is limited by the problematic nature of conducting trials for antifungal therapy.

  11. Characterization of Antifungal Activity and Nail Penetration of ME1111, a New Antifungal Agent for Topical Treatment of Onychomycosis

    OpenAIRE

    Tabata, Yuji; Takei-Masuda, Naomi; Kubota, Natsuki; Takahata, Sho; Ohyama, Makoto; Kaneda, Kaori; Iida, Maiko; Maebashi, Kazunori

    2016-01-01

    Fungal nail infection (onychomycosis) is a prevalent disease in many areas of the world, with a high incidence approaching 23%. Available antifungals to treat the disease suffer from a number of disadvantages, necessitating the discovery of new efficacious and safe antifungals. Here, we evaluate the in vitro antifungal activity and nail penetration ability of ME1111, a novel antifungal agent, along with comparator drugs, including ciclopirox, amorolfine, terbinafine, and itraconazole. ME1111 ...

  12. Research to Identify Effective Antifungal Agents, 1992 Annual Report.

    Energy Technology Data Exchange (ETDEWEB)

    Schreck, Carl

    1993-03-01

    This study is a continuation of ``Research to Identify Effective Antifungal Agents'' sponsored by Bonneville Power Administration (Schreck et al. 1990 and Schreck et al. 1991). The objectives of the present study were to select and evaluate up to 10 candidate fungicides.

  13. Experimental evaluation of antifungal and antiseptic agents against Rhodotorula spp.

    Science.gov (United States)

    Preney, L; Théraud, M; Guiguen, C; Gangneux, J P

    2003-12-01

    We studied the susceptibility of 21 strains of Rhodotorula rubra and nine strains of R. glutinis to eight antifungals and tested eight antiseptic agents on one strain of R. rubra. The tested strains were susceptible to ketoconazole, 5-fluorocytosine, amphotericin B, and nystatin, intermediate to econazole and resistant to fluconazole, itraconazole and miconazole. After 5-min contact, six of the eight antiseptic agents tested showed a fungicidal activity on the tested R. rubra strain.

  14. Recent advances in topical formulation carriers of antifungal agents.

    Science.gov (United States)

    Bseiso, Eman Ahmed; Nasr, Maha; Sammour, Omaima; Abd El Gawad, Nabaweya A

    2015-01-01

    Fungal infections are amongst the most commonly encountered diseases affecting the skin. Treatment approaches include both topical and oral antifungal agents. The topical route is generally preferred due to the possible side effects of oral medication. Advances in the field of formulation may soon render outdated conventional products such as creams, ointments and gels. Several carrier systems loaded with antifungal drugs have demonstrated promising results in the treatment of skin fungal infections. Examples of these newer carriers include micelles, lipidic systems such as solid lipid nanoparticles and nanostructured lipid carriers, microemulsions and vesicular systems such as liposomes, niosomes, transfersomes, ethosomes, and penetration enhancer vesicles.

  15. Recent advances in topical formulation carriers of antifungal agents

    Directory of Open Access Journals (Sweden)

    Eman Ahmed Bseiso

    2015-01-01

    Full Text Available Fungal infections are amongst the most commonly encountered diseases affecting the skin. Treatment approaches include both topical and oral antifungal agents. The topical route is generally preferred due to the possible side effects of oral medication. Advances in the field of formulation may soon render outdated conventional products such as creams, ointments and gels. Several carrier systems loaded with antifungal drugs have demonstrated promising results in the treatment of skin fungal infections. Examples of these newer carriers include micelles, lipidic systems such as solid lipid nanoparticles and nanostructured lipid carriers, microemulsions and vesicular systems such as liposomes, niosomes, transfersomes, ethosomes, and penetration enhancer vesicles.

  16. Antiviral, antifungal and antiprotozoal agents in the cinema.

    Science.gov (United States)

    García-Sánchez, Jose Elias; García-Sánchez, E; Merino Marcos, M L

    2007-03-01

    Among the antimicrobial agents, antibacterials are the most frequently mentioned in cinematographic plots. Nevertheless, it is not uncommon to come across other antiviral agents, especially antiretrovirals and antiprotozoals. We analyzed the presence of antiviral and antifungal agents in different commercial films, both when they were merely mentioned in passing and when they played a major role in the film. This review essentially aims to address the historical portrayal of these agents in film and to list their appearances. The fictional treatments that appear in some films are not addressed.

  17. The biology and chemistry of antifungal agents: a review.

    Science.gov (United States)

    Kathiravan, Muthu K; Salake, Amol B; Chothe, Aparna S; Dudhe, Prashik B; Watode, Rahul P; Mukta, Maheshwar S; Gadhwe, Sandeep

    2012-10-01

    In recent years their has been an increased use of antifungal agents and has resulted in the development of resistance to drugs. Currently, use of standard antifungal therapies can be limited because of toxicity, low efficacy rates. Different types of mechanisms contribute to the development of resistance to antifungals. This has given raise to search for a new heterocycle with distinct action or multitargeted combination therapy. This review addresses the areas such as the underlying mechanisms, eight different targets such as ergosterol synthesis, chitin synthesis, ergosterol disruptors, glucan synthesis, squalene epoxidase, nucleic acid synthesis, protein synthesis, microtubules synthesis. The clinically employed drugs along with the current research work going on worldwide on different heterocycles are discussed. In recent advances various heterocycles including imidazole, benzimidazole etc., twenty three scaffolds and their lead identification are discussed.

  18. Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents

    Directory of Open Access Journals (Sweden)

    Bruna B. Casanova

    2015-05-01

    Full Text Available Emerging yeasts are among the most prevalent causes of systemic infections with high mortality rates and there is an urgent need to develop specific, effective and non-toxic antifungal agents to respond to this issue. In this study 35 aldehydes, hydrazones and hydrazines were obtained and their antifungal activity was evaluated against Candida species (C. parapsilosis, C. tropicalis, C. krusei, C. albicans, C. glabrata and C. lusitaneae and Trichosporon asahii, in an in vitro screening. The minimum inhibitory concentrations (MICs of the active compounds in the screening was determined against 10 clinical isolates of C. parapsilosis and 10 of T. asahii. The compounds 4-pyridin-2-ylbenzaldehyde] (13a and tert-butyl-(2Z-2-(3,4,5-trihydroxybenzylidinehydrazine carboxylate (7b showed the most promising MIC values in the range of 16–32 μg/mL and 8–16 μg/mL, respectively. The compounds’ action on the stability of the cell membrane and cell wall was evaluated, which suggested the action of the compounds on the fungal cell membrane. Cell viability of leukocytes and an alkaline comet assay were performed to evaluate the cytotoxicity. Compound 13a was not cytotoxic at the active concentrations. These results support the discovery of promising candidates for the development of new antifungal agents.

  19. Isobolographic analysis of pharmacodynamic interactions between antifungal agents and ciprofloxacin against Candida albicans and Aspergillus fumigatus.

    Science.gov (United States)

    Stergiopoulou, Theodouli; Meletiadis, Joseph; Sein, Tin; Papaioannidou, Paraskevi; Tsiouris, Ioannis; Roilides, Emmanuel; Walsh, Thomas J

    2008-06-01

    Patients suffering from invasive mycoses often receive concomitant antifungal therapy and antibacterial agents. Assessment of pharmacodynamic interactions between antifungal and antibacterial agents is complicated by the absence of a common antifungal end point for both agents. Ciprofloxacin has no intrinsic antifungal activity but may interact with antifungal agents, since it inhibits DNA gyrase (topoisomerase II), which is abundant in fungi. We therefore employed isobolographic analysis adapted to incorporate a nonactive agent in order to analyze the potential in vitro interaction between the fluoroquinolone ciprofloxacin and several representative antifungal agents against Candida albicans and Aspergillus fumigatus strains by using a microdilution checkerboard technique. In agreement with earlier in vitro studies, conventional fractional inhibitory concentration index analysis was unable to detect interactions between ciprofloxacin and antifungal agents. However, isobolographic analysis revealed significant pharmacodynamic interactions between antifungal agents and ciprofloxacin against C. albicans and A. fumigatus strains. Amphotericin B demonstrated concentration-dependent interactions for both species, with synergy (interaction indices, 0.14 to 0.81) observed at ciprofloxacin concentrations of Isobolographic analysis may help to elucidate the pharmacodynamic interactions between antifungal and non-antifungal agents and to develop better management strategies against invasive candidiasis and aspergillosis.

  20. Pyridine-grafted chitosan derivative as an antifungal agent.

    Science.gov (United States)

    Jia, Ruixiu; Duan, Yunfei; Fang, Qiang; Wang, Xiangyang; Huang, Jianying

    2016-04-01

    Pyridine moieties were introduced into chitosan by nucleophilic substitution to afford N-(1-carboxybutyl-4-pyridinium) chitosan chloride (pyridine chitosan). The resulting chitosan derivative was well characterized, and its antifungal activity was examined, based on the inhibition of mycelial growth and spore germination. The results indicated that pyridine chitosan exhibited enhanced antifungal activity by comparison with pristine chitosan. The values of the minimum inhibitory concentration and the minimal fungicidal concentration of pyridine chitosan against Fulvia fulva were 0.13 mg/ml and 1 mg/ml, respectively, while the corresponding values against Botrytis cinerea were 0.13 mg/ml and 4 mg/ml, respectively. Severe morphological changes of pyridine chitosan-treated B. cinerea were observed, indicative that pyridine chitosan could damage and deform the structure of fungal hyphae and subsequently inhibit strain growth. Non-toxicity of pyridine chitosan was demonstrated by an acute toxicity study. These results are beneficial for assessing the potential utilization of this chitosan derivative and for exploring new functional antifungal agents with chitosan in the food industry.

  1. Treatment of dermatophytosis by a new antifungal agent 'apigenin'.

    Science.gov (United States)

    Singh, Geeta; Kumar, Padma; Joshi, Suresh Chandra

    2014-08-01

    Dermatophytes are the most common causative agents of cutaneous mycosis and remain a major public health problem in spite of the availability of an increasing number of antifungal drugs. It was, therefore considered necessary to pursue the screening of different extracts (compounds) of selected traditional medicinal plants reportedly having antidermatophyte potential. The aim of this study was to isolate and identify specific compound from the most active extract (free flavonoid) of stem of Terminalia chebula of the selected plants to treat dermatophytosis induced on experimental mice. Mice which were experimentally induced with Trichophyton mentagrophytes were grouped in six of five animals each. To treat the lesions on infected mice, two concentrations of isolated apigenin ointment, i.e. 2.5 mg g(-1) (Api I) and 5 mg g(-1) (Api II), and terbinafine (standard) of concentration 5 mg g(-1) were used. Complete recovery from the infection was recorded on 12th day of treatment for reference drug Terbinafine and Api II (5 mg g(-1) ) concentration of ointment, whereas Api I (2.5 mg g(-1) ) ointment showed complete cure on 16th day of treatment. Fungal burden was also calculated by culturing skin scraping from infected mice's of different groups. Apigenin has shown potency as the infected animals recover completely by Api II comparable to the standard drug in 12th day. So Apigenin can be explored as an antifungal agent in the clinical treatment of dermatophytosis in future.

  2. Antifungal activity of allylamines against agents of eumycetoma

    Directory of Open Access Journals (Sweden)

    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.

  3. Clinical evaluation of clotrimazole. A broad-spectrum antifungal agent.

    Science.gov (United States)

    Spiekermann, P H; Young, M D

    1976-03-01

    The efficacy and safety of the broad-spectrum, topically applied antifungal agent clotrimazole were evaluated in two double-blind, multicentric trials. Ten investigators reported on a total of 1,361 cases in which a 1% solution or a 1% cream formulation was compared with its respective vehicle. Clotrimazole was therapeutically effective, as confirmed by mycological cure (negative microscopy and culture) and clinical improvement, in tinea pedis, tinea cruris, tinea corporis, pityriasis versicolor, and cutaneous candidasis. Furthermore, species identification established the efficacy of clotrimazole against Trichophyton rubrum, T mentagrophytes, Epidermophyton floccosum, Microsporum canis, Malassezia furfur (Pityrosporum orbiculare), and Candida albicans. Safety was demonstrated by the low incidence of possibly drug-related adverse experiences, namely, 19 (2.7%) of 699 patients who were treated with clotrimazole, of whom four (0.6%) discontinued treatment.

  4. Synergistic combinations of antifungals and anti-virulence agents to fight against Candida albicans

    OpenAIRE

    Cui, Jinhui; Ren, Biao; Tong, Yaojun; Dai, Huanqin; Zhang, Lixin

    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 resistance, demand innovative strategies for new effective antifungal drugs. Synergistic combinations of antifungals and anti-virulence agents highlight the pragmatic strategy to reduce the development of d...

  5. Characterization of Antifungal Activity and Nail Penetration of ME1111, a New Antifungal Agent for Topical Treatment of Onychomycosis.

    Science.gov (United States)

    Tabata, Yuji; Takei-Masuda, Naomi; Kubota, Natsuki; Takahata, Sho; Ohyama, Makoto; Kaneda, Kaori; Iida, Maiko; Maebashi, Kazunori

    2016-02-01

    Fungal nail infection (onychomycosis) is a prevalent disease in many areas of the world, with a high incidence approaching 23%. Available antifungals to treat the disease suffer from a number of disadvantages, necessitating the discovery of new efficacious and safe antifungals. Here, we evaluate the in vitro antifungal activity and nail penetration ability of ME1111, a novel antifungal agent, along with comparator drugs, including ciclopirox, amorolfine, terbinafine, and itraconazole. ME1111 showed potent antifungal activity against Trichophyton rubrum and Trichophyton mentagrophytes (the major etiologic agents of onychomycosis) strains isolated in Japan and reference fungal strains with an MIC range of 0.12 to 0.5 mg/liter and an MIC50 and MIC90 of 0.5 mg/liter for both. Importantly, none of the tested isolates showed an elevated ME1111 MIC. Moreover, the antifungal activity of ME1111 was minimally affected by 5% wool keratin powder in comparison to the other antifungals tested. The ME1111 solution was able to penetrate human nails and inhibit fungal growth in a dose-dependent manner according to the TurChub assay. In contrast, 8% ciclopirox and 5% amorolfine nail lacquers showed no activity under the same conditions. ME1111 demonstrated approximately 60-fold-greater selectivity in inhibition of Trichophyton spp. than of human cell lines. Our findings demonstrate that ME1111 possesses potent antidermatophyte activity, maintains this activity in the presence of keratin, and possesses excellent human nail permeability. These results suggest that ME1111 is a promising topical medication for the treatment of onychomycosis and therefore warrants further clinical evaluation.

  6. In vitro activities of new and conventional antifungal agents against clinical Scedosporium isolates.

    NARCIS (Netherlands)

    Meletiadis, J.; Meis, J.F.G.M.; Mouton, J.W.; Rodriguez-Tudela, J.L.; Donnelly, J.P.; Verweij, P.E.

    2002-01-01

    The susceptibilities of 13 clinical isolates of Scedosporium apiospermum and 55 clinical isolates of S. prolificans to new and conventional drugs belonging to three different classes of antifungal agents, the azoles (miconazole, itraconazole, voriconazole, UR-9825, posaconazole), the polyenes (ampho

  7. Impact of brief exposure to antifungal agents on the post-antifungal effect and hemolysin activity of oral Candida albicans

    Directory of Open Access Journals (Sweden)

    Arjuna Nishantha ELLEPOLA

    2015-08-01

    Full Text Available AbstractPost-antifungal effect (PAFE of Candida and its production of hemolysin are determinants of candidal pathogenicity. Candida albicans is the foremost aetiological agent of oral candidosis, which can be treated with polyene, azole, and echinocandin antifungals. However, once administered, the intraoral concentrations of these drugs tend to be subtherapeutic and transient due to the diluent effect of saliva and cleansing effect of the oral musculature. Hence, intra-orally, Candidamay undergo a brief exposure to antifungal drugs.Objective Therefore, the PAFE and hemolysin production of oral C. albicans isolates following brief exposure to sublethal concentrations of the foregoing antifungals were evaluated.Material and Methods A total of 50 C. albicans oral isolates obtained from smokers, diabetics, asthmatics using steroid inhalers, partial denture wearers and healthy individuals were exposed to sublethal concentrations of nystatin, amphotericin B, caspofungin, ketoconazole and fluconazole for 60 min. Thereafter, the drugs were removed and the PAFE and hemolysin production were determined by previously described turbidometric and plate assays, respectively.Results Nystatin, amphotericin B, caspofungin and ketoconazole induced mean PAFE (hours of 2.2, 2.18, 2.2 and 0.62, respectively. Fluconazole failed to produce a PAFE. Hemolysin production of these isolates was suppressed with a percentage reduction of 12.27, 13.47, 13.33, 8.53 and 4.93 following exposure to nystatin, amphotericin B, caspofungin, ketoconazole and fluconazole, respectively.Conclusions Brief exposure to sublethal concentrations of antifungal drugs appears to exert an antifungal effect by interfering with the growth as well as hemolysin production of C. albicans.

  8. In Vitro Activities of New and Conventional Antifungal Agents against Clinical Scedosporium Isolates

    OpenAIRE

    Meletiadis, Joseph; Meis, Jacques F. G. M.; Mouton, Johan W.; Rodriquez-Tudela, Juan Luis; Donnelly, J. Peter; Verweij, Paul E.

    2002-01-01

    The susceptibilities of 13 clinical isolates of Scedosporium apiospermum and 55 clinical isolates of S. prolificans to new and conventional drugs belonging to three different classes of antifungal agents, the azoles (miconazole, itraconazole, voriconazole, UR-9825, posaconazole), the polyenes (amphotericin B, nystatin and liposomal nystatin), and allylamines (terbinafine), were studied by use of proposed standard M38-P of NCCLS. Low growth-inhibitory antifungal activities were found in vitro ...

  9. Selection of antifungal agents for burn patients%烧伤患者抗真菌药物的选择

    Institute of Scientific and Technical Information of China (English)

    郇京宁

    2013-01-01

    Fungal infection is one of the serious complications of severely burned patients with high mortality.Application of antifungal agents timely and rationally is very important to control the infection.Antifungal agents including polyenes,triazoles,and echinocandins have been used widely in burned patients and are proved to be effective.Since diagnosis of fungal infection remains difficult,prophylactic and empirical therapies appear to be particularly necessary.In order to improve the efficacy and safety of antifungal agents,the factors of fungal strains,infection sites,hepatic and renal functions,and age,etc.should be considered in selecting antifungal agents.

  10. 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.

  11. Antifungal agents: mode of action, mechanisms of resistance, and correlation of these mechanisms with bacterial resistance.

    Science.gov (United States)

    Ghannoum, M A; Rice, L B

    1999-10-01

    The increased use of antibacterial and antifungal agents in recent years has resulted in the development of resistance to these drugs. The significant clinical implication of resistance has led to heightened interest in the study of antimicrobial resistance from different angles. Areas addressed include mechanisms underlying this resistance, improved methods to detect resistance when it occurs, alternate options for the treatment of infections caused by resistant organisms, and strategies to prevent and control the emergence and spread of resistance. In this review, the mode of action of antifungals and their mechanisms of resistance are discussed. Additionally, an attempt is made to discuss the correlation between fungal and bacterial resistance. Antifungals can be grouped into three classes based on their site of action: azoles, which inhibit the synthesis of ergosterol (the main fungal sterol); polyenes, which interact with fungal membrane sterols physicochemically; and 5-fluorocytosine, which inhibits macromolecular synthesis. Many different types of mechanisms contribute to the development of resistance to antifungals. These mechanisms include alteration in drug target, alteration in sterol biosynthesis, reduction in the intercellular concentration of target enzyme, and overexpression of the antifungal drug target. Although the comparison between the mechanisms of resistance to antifungals and antibacterials is necessarily limited by several factors defined in the review, a correlation between the two exists. For example, modification of enzymes which serve as targets for antimicrobial action and the involvement of membrane pumps in the extrusion of drugs are well characterized in both the eukaryotic and prokaryotic cells.

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

    Directory of Open Access Journals (Sweden)

    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. Comparison of the In Vitro Activities of Newer Triazoles and Established Antifungal Agents against Trichophyton rubrum

    NARCIS (Netherlands)

    Deng, S.; Zhang, C.; Seyedmousavi, S.; Zhu, S.; Tan, X.; Wen, Y.; Huang, X.; Lei, W.; Zhou, Z.; Fang, W.; Shen, S.; Deng, D.; Pan, W.; Liao, W.

    2015-01-01

    One hundred eleven clinical Trichophyton rubrum isolates were tested against 7 antifungal agents. The geometric mean MICs of all isolates were, in increasing order: terbinafine, 0.03 mg/liter; voriconazole, 0.05 mg/liter; posaconazole, 0.11 mg/liter; isavuconazole, 0.13 mg/liter; itraconazole, 0.26

  14. In Vitro Susceptibility of Aflatoxigenic and Non-aflatoxigenic Aspergillus flavus Strains to Conventional Antifungal Agents

    Directory of Open Access Journals (Sweden)

    Mahmoud Mahmoudi

    2012-12-01

    Full Text Available Presently appearance of resistance to antifungal agents among Aspergillus species is dramatically increasing. The objective of this study was to look at the in vitro activities of antifungal drugs against Iranian clinical (from nail, bronchoalveolar lavage, paranasal sinus isolated A. flavus strains. The susceptibility of 45 aflatoxigenic and non-aflatoxigenic Aspergillus flavus strains were evaluated to six antifungal agents (caspofungin, itraconazole, amphotericin B, ketoconazole, fluconazole, nystatin using CLSI M38-A2 broth microdilution method. The results indicated that 57.1%, 28.6% of aflatoxigenic and 25.8%, 6.5% of non-aflatoxigenic isolates were susceptible to caspofungin, amphotericin B respectively. All isolates but one aflatoxigenic strain were sensitive to ketoconazole. All 45 strains showed to be resistant to nystatin. Also 64.28%, 92.9% of aflatoxigenic and 64.51%, 100% of non-aflatoxigenic isolates were resistant to fluconazole and itraconazole in ranking order. There was no statistically significant difference between the susceptibilities of aflatoxigenic and non-aflatoxigenic strains of A. flavus to tested antifungal agents

  15. Triterpenoid glycosides from Medicago sativa as antifungal agents against Pyricularia oryzae.

    Science.gov (United States)

    Abbruscato, Pamela; Tosi, Solveig; Crispino, Laura; Biazzi, Elisa; Menin, Barbara; Picco, Anna M; Pecetti, Luciano; Avato, Pinarosa; Tava, Aldo

    2014-11-19

    The antifungal properties of saponin mixtures from alfalfa (Medicago sativa L.) tops and roots, the corresponding mixtures of prosapogenins from tops, and purified saponins and sapogenins against the causal agent of rice blast Pyricularia oryzae isolates are presented. In vitro experiments highlighted a range of activities, depending upon the assayed metabolite. The antifungal effects of the most promising prosapogenin mixture from alfalfa tops were confirmed by means of in planta tests using three different Italian cultivars of rice (Oryza sativa L. ssp. japonica), known to possess high, medium, and low blast resistance. The evidenced antifungal properties of the tested metabolites allowed some considerations on their structure-activity relationship. Results indicate that prosapogenins are active compounds to prevent the fungal attack of P. oryzae on different rice cultivars. Therefore, if properly formulated, these substances could represent a promising and environmentally friendly treatment to control rice blast.

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

    Science.gov (United States)

    Komoto, Tatiana Takahasi; Bitencourt, Tamires Aparecida; Silva, Gabriel; Beleboni, Rene Oliveira; Marins, Mozart; Fachin, Ana Lúcia

    2015-01-01

    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. PMID:26257814

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

    Directory of Open Access Journals (Sweden)

    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.

  18. Biogenic silver nanoparticles: efficient and effective antifungal agents

    Science.gov (United States)

    Netala, Vasudeva Reddy; Kotakadi, Venkata Subbaiah; Domdi, Latha; Gaddam, Susmila Aparna; Bobbu, Pushpalatha; Venkata, Sucharitha K.; Ghosh, Sukhendu Bikash; Tartte, Vijaya

    2016-04-01

    Biogenic synthesis of silver nanoparticles (AgNPs) by exploiting various plant materials is an emerging field and considered green nanotechnology as it involves simple, cost effective and ecofriendly procedure. In the present study AgNPs were successfully synthesized using aqueous callus extract of Gymnema sylvestre. The aqueous callus extract treated with 1nM silver nitrate solution resulted in the formation of AgNPs and the surface plasmon resonance (SPR) of the formed AgNPs showed a peak at 437 nm in the UV Visible spectrum. The synthesized AgNPs were characterized using Fourier transform infrared spectroscopy (FTIR), Transmission electron microscopy (TEM), and X-ray diffraction spectroscopy (XRD). FTIR spectra showed the peaks at 3333, 2928, 2361, 1600, 1357 and 1028 cm-1 which revealed the role of different functional groups possibly involved in the synthesis and stabilization of AgNPs. TEM micrograph clearly revealed the size of the AgNPs to be in the range of 3-30 nm with spherical shape and poly-dispersed nature; it is further confirmed by Particle size analysis that the stability of AgNPs is due its high negative Zeta potential (-36.1 mV). XRD pattern revealed the crystal nature of the AgNPs by showing the braggs peaks corresponding to (111), (200), (220) and (311) planes of face-centered cubic crystal phase of silver. Selected area electron diffraction pattern showed diffraction rings and confirmed the crystalline nature of synthesized AgNPs. The synthesized AgNPs exhibited effective antifungal activity against Candida albicans, Candida nonalbicans and Candida tropicalis.

  19. Antifungal Agents: Mode of Action, Mechanisms of Resistance, and Correlation of These Mechanisms with Bacterial Resistance

    OpenAIRE

    Ghannoum, Mahmoud A.; Rice, Louis B

    1999-01-01

    The increased use of antibacterial and antifungal agents in recent years has resulted in the development of resistance to these drugs. The significant clinical implication of resistance has led to heightened interest in the study of antimicrobial resistance from different angles. Areas addressed include mechanisms underlying this resistance, improved methods to detect resistance when it occurs, alternate options for the treatment of infections caused by resistant organisms, and strategies to ...

  20. Gluconic acid: an antifungal agent produced by Pseudomonas species in biological control of take-all.

    Science.gov (United States)

    Kaur, Rajvinder; Macleod, John; Foley, William; Nayudu, Murali

    2006-03-01

    Pseudomonas strain AN5 (Ps. str. AN5), a non-fluorescent Australian bacterial isolate, is an effective biological control (biocontrol) agent of the take-all disease of wheat caused by the fungus Gaeumannomyces graminis var. tritici (Ggt). Ps. str. AN5 controls Ggt by producing an antifungal compound which was purified by thin layer and column chromatography, and identified by NMR and mass spectroscopic analysis to be d-gluconic acid. Commercially bought pure gluconic acid strongly inhibited Ggt. Two different transposon mutants of Ps. str. AN5 which had lost take-all biocontrol did not produce d-gluconic acid. Gluconic acid production was restored, along with take-all biocontrol, when one of these transposon mutants was complemented with the corresponding open reading frame from wild-type genomic DNA. Gluconic acid was detected in the rhizosphere of wheat roots treated with the wild-type Ps. str. AN5, but not in untreated wheat or wheat treated with a transposon mutant strain which had lost biocontrol. The antifungal compounds phenazine-1-carboxylic acid and 2,4-diacetylphloroglucinol, produced by other Pseudomonads and previously shown to be effective in suppressing the take-all disease, were not detected in Ps. str. AN5 extracts. These results suggest that d-gluconic acid is the most significant antifungal agent produced by Ps. str. AN5 in biocontrol of take-all on wheat roots.

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

    Directory of Open Access Journals (Sweden)

    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

  2. Augmenting the Antifungal Activity of an Oxidizing Agent with Kojic Acid: Control of Penicillium Strains Infecting Crops

    Directory of Open Access Journals (Sweden)

    Jong H. Kim

    2014-11-01

    Full Text Available Oxidative treatment is one of the strategies for preventing Penicillium contamination in crops/foods. The antifungal efficacy of hydrogen peroxide (H2O2; oxidant was investigated in Penicillium strains by using kojic acid (KA as a chemosensitizing agent, which can enhance the susceptibility of pathogens to antifungal agents. Co-application of KA with H2O2 (chemosensitization resulted in the enhancement of antifungal activity of either compound, when compared to the independent application of each agent alone. Of note, heat enhanced the activity of H2O2 to a greater extent during chemosensitization, whereby the minimum inhibitory or minimum fungicidal concentrations of H2O2 was decreased up to 4 or 13 fold, respectively, at 35–45 °C (heat, when compared to that at 28 °C (normal growth temperature. However, heat didn’t increase the antifungal activity of KA, indicating specificity exists between heat and types of antifungals applied. The effect of chemosensitization was also strain-specific, where P. expansum (both parental and fludioxonil-resistant mutants or P. italicum 983 exhibited relatively higher susceptibility to the chemosensitization, comparing to other Penicillium strains tested. Collectively, chemosensitization can serve as a potent antifungal strategy to lower effective dosages of toxic antifungal substances, such as H2O2. This can lead to coincidental lowering of environmental and health risks.

  3. 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.

  4. Sordarin, an antifungal agent with a unique mode of action

    Directory of Open Access Journals (Sweden)

    2008-09-01

    Full Text Available The sordarin family of compounds, characterized by a unique tetracyclic diterpene core including a norbornene system, inhibits protein synthesis in fungi by stabilizing the ribosome/EF2 complex. This mode of action is in contrast to typical antifungals, which target the cell membrane. This unusual bioactivity makes sordarin a promising candidate for the development of new fungicidal agents, and provided the motivation for extensive research. Three total syntheses (by the Kato, Mander and Narasaka groups, modifications of the glycosyl unit, and changes to the diterpene core (Cuevas and Ciufolini models will also be discussed in this review.

  5. Synthesis and Biological Evaluation of Norcantharidin Derivatives Possessing an Aromatic Amine Moiety as Antifungal Agents

    Directory of Open Access Journals (Sweden)

    Yang Wang

    2015-12-01

    Full Text Available Based on the structure of naturally produced cantharidin, different arylamine groups were linked to the norcantharidin scaffold to provide thirty six compounds. Their structures were confirmed by melting point, 1H-NMR, 13C-NMR and HRMS-ESI studies. These synthetic compounds were tested as fungistatic agents against eight phytopathogenic fungi using the mycelium growth rate method. Of these thirty six derivatives, seven displayed stronger antifungal activity than did norcantharidin, seven showed higher activity than did cantharidin and three exhibited more significant activity than that of thiabendazole. In particular, 3-(3′-chloro-phenylcarbamoyl norcantharidate II-8 showed the most significant fungicidal activity against Sclerotinia fructigena and S. sclerotiorum, with IC50 values of 0.88 and 0.97 μg/mL, respectively. The preliminary structure-activity relationship data of these compounds revealed that: (1 the benzene ring is critical for the improvement of the spectrum of antifungal activity (3-phenylcarbamoyl norcantharidate II-1 vs norcantharidin and cantharidin; (2 among the three sites, including the C-2′, C-3′ and C-4′ positions of the phenyl ring, the presence of a halogen atom at the C-3′position of the benzene ring caused the most significant increase in antifungal activity; (3 compounds with strongly electron-drawing or electron-donating groups substitutions were found to have a poor antifungal activity; and (4 compared with fluorine, bromine and iodine, chlorine substituted at the C-3′ position of the benzene ring most greatly promoted fungistatic activity. Thus, compound II-8 has emerged as new lead structure for the development of new fungicides.

  6. 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.

  7. In vitro activities of new and conventional antifungal agents against clinical Scedosporium isolates.

    Science.gov (United States)

    Meletiadis, Joseph; Meis, Jacques F G M; Mouton, Johan W; Rodriquez-Tudela, Juan Luis; Donnelly, J Peter; Verweij, Paul E

    2002-01-01

    The susceptibilities of 13 clinical isolates of Scedosporium apiospermum and 55 clinical isolates of S. prolificans to new and conventional drugs belonging to three different classes of antifungal agents, the azoles (miconazole, itraconazole, voriconazole, UR-9825, posaconazole), the polyenes (amphotericin B, nystatin and liposomal nystatin), and allylamines (terbinafine), were studied by use of proposed standard M38-P of NCCLS. Low growth-inhibitory antifungal activities were found in vitro for most of the drugs tested against S. prolificans isolates, with the MICs at which 90% of isolates are inhibited (MIC(90)s) being >8 microg/ml; the MIC(90)s of voriconazole and UR-9825, however, were 4 microg/ml. S. apiospermum isolates were more susceptible in vitro, with the highest activity exhibited by voriconazole (MIC(90)s, 0.5 microg/ml), followed by miconazole (MIC(90)s, 1 microg/ml), UR-9825 and posaconazole (MIC(90)s, 2 microg/ml), and itraconazole (MIC(90)s, 4 microg/ml). The MICs of terbinafine, amphotericin B, and the two formulations of nystatin (for which no statistically significant differences in antifungal activities were found for the two species) for S. apiospermum isolates were high. Cross-resistance was observed among all the azoles except posaconazole and among all the polyenes except the lipid formulation. A distribution analysis was performed with the MICs of each drug and for each species. Bimodal and skewed MIC distributions were obtained, and cutoffs indicating the borders of different MIC subpopulations of the distributions were determined on the basis of the normal plot technique. These cutoffs were in many cases reproducible between 48 and 72 h.

  8. [Ajoene the main active compound of garlic (Allium sativum): a new antifungal agent].

    Science.gov (United States)

    Ledezma, Eliades; Apitz-Castro, Rafael

    2006-06-01

    The curative properties of garlic in medicine have been known for a long time. But, it was only in the last three decades when garlic properties were seriously investigated confirming its potential as therapeutic agent. Allicin, ajoene, thiosulfinates and a wide range of other organosulphurate compounds, are known to be the constituents linked to the garlic properties. Regarding the biochemical properties of these compounds, ajoene [(E,Z)-4,5,9 Trithiadodeca 1,6,11 Triene 9-oxide] is stable in water, and it can be obtained by chemical synthesis. There is evidence that some of the garlic constituents exert a wide variety of effects on different biological systems. However, ajoene is the garlic compound related to more biological activities, as showed in in vitro and in vivo systems. Those studies found that ajoene has antithrombotic, anti-tumoral,antifungal, and antiparasitic effects. This study deals with a recently described antifungal property of ajoene, and its potential use in clinical trails to treat several fungal infections.

  9. Susceptibility pattern of Malassezia species to selected plant extracts and antifungal agents

    Directory of Open Access Journals (Sweden)

    G Sibi

    2014-01-01

    Full Text Available Objective: Malassezia is associated with dandruff, seborrhoeic dermatitis, pityriasis versicolor folliculitis and atopic eczema. This study determined the susceptibility pattern of Malassezia furfur, M. globosa, M. obtusa, M. restricta, M. slooffiae and M. sympodialis isolated from patients diagnosed with dandruff against plant extracts and antifungal agents. Materials and Methods: Twenty aqueous plant extracts and five azole drugs were tested against the isolates by well diffusion and broth dilution method. Results: Among the plant extracts, Phyllanthus emblica (fruits, Hibiscus rosa sinensis (flowers and Acacia concinna (pods have demonstrated significant antidandruff activity. Minimum inhibitory concentration values revealed that ketoconazole as the most effective drug followed by itraconazole. Conclusion: M. furfur and M. globosa were found as the most susceptible organisms against the aqueous extracts of Phyllanthus emblica (fruits, Hibiscus rosa sinensis (flowers, Acacia concinna (pods and azole drugs.

  10. Turmeric powder (Curcuma longa Linn. as an antifungal agent in plant tissue culture studies

    Directory of Open Access Journals (Sweden)

    R.S. Upendra

    2011-11-01

    Full Text Available Culturing the individual plant cells, tissues (explants and organs in laboratory or in vitro on synthetic media (MS media under aseptic conditions is a usual process in plant tissue culture studies. The medium is rich in nutrients, also supports the growth of variety of microorganisms especially bacteria and fungi, which causecontamination of the medium, though the media is sterilized by autoclaving. During the process of cooling and transferring the media, the chances of fungal contamination remain high. This is avoided to the maximum extent following the good laboratory practices. A novel means could be incorporating turmeric, a well -known antifungal agent, into the media. In the present study, attempts were made to avoid fungal contamination using the media with various concentration of turmeric powder. Results of the investigation revealed that turmeric powder used at the concentrations of 0.8 g/L and 1.0 g/L in the media resulted in appreciable control of fungal contamination.

  11. Susceptibility of Clinical Candida Species Isolates to Antifungal Agents by E-Test, Southern Iran: A Five Year Study

    Directory of Open Access Journals (Sweden)

    A Alborzi

    2011-12-01

    Full Text Available Background and Objectives: The incidence of fungal infections in immunocompromised patients, especially by Candida species, has increased in recent years. This study was designed to identify Candida species and determine antifungal susceptibility patterns of 595 yeast strains isolated from various clinical specimens.Material and Methods: Identification of the isolates were determined by the API 20 C AUX kit and antifungal susceptibilities of the species to fluconazole, amphotericin B, ketoconazole, itraconazole, voriconazole, and caspofungin were determined by the agar-based E-test method.Results: Candida albicans (48% was the most frequently isolated species, followed by Candida kruzei (16.1%, Candida glabrata (13.5%, Candida kefyr (7.4%, Candida parapsilosis (4.8%, Candida tropicalis (1.7% and other species (8.5%. Resistance varies depending on the species and the respective antifungal agents. Comparing the MIC90 for all the strains, the lower MIC90 was observed for caspofungin (0.5 μg/ml. The MIC90 for all Candida species were 64 μg/ml for fluconazole, 0.75 μg/ml for amphotericin B, 4 μg/ml for ketoconazole, 4 μg/ml for itraconazole, and 2 μg/ml for voriconazole.Conclusions: Species definition and determination of antifungal susceptibility patterns are advised for the proper management and treatment of patients at risk for systemic candidiasis. Resistance to antifungal agents is an alarming sign for the emerging common nosocomial fungal infections.

  12. Biodirected synthesis of Miconazole-conjugated bacterial silver nanoparticles and their application as antifungal agents and drug delivery vehicles.

    Science.gov (United States)

    Kumar, C Ganesh; Poornachandra, Y

    2015-01-01

    The recent strategy to improve the efficacy of drugs is to combine them with metal nanoparticles for the control of microbial infections. Considering this fact, we developed a low cost and eco-friendly method for silver nanoparticles synthesis using the cell free supernatant of Delftia sp. strain KCM-006 and their application as antifungal agents and as a drug carrier. Transmission electron microscopy (TEM) and dynamic light scattering (DLS) analysis revealed the formation of spherical and monodispersed silver nanoparticles with an average size of 9.8 nm. The synthesized nanoparticles were found to be photoluminescent, highly stable and crystalline in nature having a zeta potential of -31 mV. The silver nanoparticles exhibited very good antifungal activity against various pathogenic Candida strains. Furthermore, the efficacy of nanoparticles was increased by conjugating the antifungal drug Miconazole to silver nanoparticles which exhibited significant fungicidal activity, inhibition of ergosterol biosynthesis and biofilm inhibition by increasing ROS levels. In addition, the cell viability and immunocytochemistry analysis against different normal cell lines including Chinese hamster ovary cells (CHO), human lung cell line (MRC5) and human vascular endothelial cells (HUVEC) demonstrated that these nanoparticles were non-toxic up to a concentration of 20 μM. In conclusion, these results suggest that the synthesized nanoparticles find application as both antifungal agents and drug delivery vehicles. This is a first report on the preparation of silver nanoparticles using culture supernatant from Delftia sp. and also on the conjugation of Miconazole, an antifungal drug, to the bacterial silver nanoparticles.

  13. In vitro susceptibility testing of dermatophytes isolated in Goiania, Brazil, against five antifungal agents by broth microdilution method.

    Science.gov (United States)

    Araújo, Crystiane Rodrigues; Miranda, Karla Carvalho; Fernandes, Orionalda de Fatima Lisboa; Soares, Ailton José; Silva, Maria do Rosário Rodrigues

    2009-01-01

    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 masculineC 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 microg/mL were found for 33.3%, 31.6% and 15% of isolates for itraconazole, ketoconazole and terbinafine, respectively.

  14. Exopolysaccharide matrix of developed Candida albicans biofilms after exposure to antifungal agents.

    Science.gov (United States)

    da Silva, Wander José; Gonçalves, Letícia Machado; Seneviratne, Jayampath; Parahitiyawa, Nipuna; Samaranayake, Lakshman Perera; Del Bel Cury, Altair Antoninha

    2012-01-01

    This study aimed to evaluate the effects of fluconazole or nystatin exposure on developed Candida albicans biofilms regarding their exopolysaccharide matrix. The minimal inhibitory concentration (MIC) against fluconazole or nystatin was determined for C. albicans reference strain (ATCC 90028). Poly(methlymethacrylate) resin (PMMA) specimens were fabricated according to the manufacturer's instructions and had their surface roughness measured. Biofilms were developed on specimens surfaces for 48 h and after that were exposed during 24 h to fluconazole or nystatin prepared in a medium at MIC, 10 x MIC or 100 x MIC. Metabolic activity was evaluated using an XTT assay. Production of soluble and insoluble exopolysaccharide and intracellular polysaccharides was evaluated by the phenol-sulfuric method. Confocal laser scanning microscope was used to evaluate biofilm architecture and percentage of dead/live cells. Data were analyzed statistically by ANOVA and Tukey's test at 5% significance level. The presence of fluconazole or nystatin at concentrations higher than MIC results in a great reduction of metabolic activity (p0.05). The exposure to nystatin also did not alter the exopolysaccharide matrix at all the tested concentrations (p>0.05). Biofilm architecture was not affected by either of the antifungal agents (p>0.05). Nystatin promoted higher proportion of dead cells (p<0.05). It may be concluded that fluconazole and nystatin above the MIC concentration reduced the metabolic activity of C. albicans biofilms; however, they were not able to alter the exopolysaccharide matrix and biofilm architecture.

  15. Electrochemical behavior of the antifungal agents itraconazole, posaconazole and ketoconazole at a glassy carbon electrode.

    Science.gov (United States)

    Knoth, H; Scriba, G K E; Buettner, B

    2015-06-01

    The electrochemical behavior of the azole antifungal agents itraconazole, posaconazole and ketoconazole has been investigated at a glassy carbon working electrode using cyclic voltammetry. All measurements were carried out in a supporting electrolyte solution consisting of a 1:1 (v/v) mixture of 0.1 mol L(-1) sodium phosphate buffers and acetonitrile at various substance concentrations and pH values. An amperometric cell with a three electrode system consisting of a working electrode, a palladium reference electrode and a platinum disk as the auxiliary electrode was used in all experiments. All azoles showed a similar electrochemical behavior involving two reactions. An irreversible oxidation occurred at potentials of about 0.5V. A reduction peak was detected at potentials between -0.28V and -0.14V with an associated oxidation peak, which was observed in consecutive repeated measurements at potentials between -0.03 and 0.28 V. The reduction and corresponding oxidation can be regarded as a quasi-reversible process. The proposed reaction mechanisms are an irreversible oxidation of the piperazine moiety at higher potentials as well as a reduction at lower potentials of the carbonyl group of the triazolone moiety in the case of itraconazole and posaconazole or a reduction of the methoxy group of ketoconazole.

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

    Directory of Open Access Journals (Sweden)

    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.

  17. Glucosamine-6-phosphate synthase, a novel target for antifungal agents. Molecular modelling studies in drug design.

    Science.gov (United States)

    Wojciechowski, Marek; Milewski, Sławomir; Mazerski, Jan; Borowski, Edward

    2005-01-01

    Fungal infections are a growing problem in contemporary medicine, yet only a few antifungal agents are used in clinical practice. In our laboratory we proposed the enzyme L-glutamine: D-fructose-6-phosphate amidotransferase (EC 2.6.1.16) as a new target for antifungals. The structure of this enzyme consists of two domains, N-terminal and C-terminal ones, catalysing glutamine hydrolysis and sugar-phosphate isomerisation, respectively. In our laboratory a series of potent selective inhibitors of GlcN-6-P synthase have been designed and synthesised. One group of these compounds, including the most studied N3-(4-methoxyfumaroyl)-l-2,3-diaminopropanoic acid (FMDP), behave like glutamine analogs acting as active-site-directed inactivators, blocking the N-terminal, glutamine-binding domain of the enzyme. The second group of GlcN-6-P synthase inhibitors mimic the transition state of the reaction taking place in the C-terminal sugar isomerising domain. Surprisingly, in spite of the fact that glutamine is the source of nitrogen for a number of enzymes it turned out that the glutamine analogue FMDP and its derivatives are selective against GlcN-6-P synthase and they do not block other enzymes, even belonging to the same family of glutamine amidotransferases. Our molecular modelling studies of this phenomenon revealed that even within the family of related enzymes substantial differences may exist in the geometry of the active site. In the case of the glutamine amidotransferase family the glutamine binding site of GlcN-6-P synthase fits a different region of the glutamine conformational space than other amidotransferases. Detailed analysis of the interaction pattern for the best known, so far, inhibitor of the sugar isomerising domain, namely 2-amino-2-deoxy-D-glucitol-6-phosphate (ADGP), allowed us to suggest changes in the structure of the inhibitor that should improve the interaction pattern. The novel ligand was designed and synthesised. Biological experiments confirmed

  18. Self-assembled cardanol azo derivatives as antifungal agent with chitin-binding ability.

    Science.gov (United States)

    Mahata, Denial; Mandal, Santi M; Bharti, Rashmi; Gupta, Vinay Krishna; Mandal, Mahitosh; Nag, Ahindra; Nando, Golok B

    2014-08-01

    Cardanol is a non-isoprenoic phenolic lipid-mixture of distilled cashew nut shell liquid obtained from Anacardium occidentale. Herein, cardanol is purified from cashew nut shell liquid (CNSL) and synthesized to new compounds with different azo amphiphiles. These synthesized compounds are allowed to self-assembled in hydrophobic environment and checked antifungal activity against Candida albicans. Self-assembled structure of CABA showed higher antifungal activity (16μg/mL) and chitin-binding ability in comparison to CAP and CANB. Furthermore, the self-assembled azo amphiphiles are immobilized with silver ions to prepare hydrogel which showed eight folds enhanced antifungal activity. Toxicity is reduced by several folds of self-assembled or hydrogel structure in comparison to pure compounds. Thus, the self-assembled structure of amphiphiles and their hydrogels have been found to be new macromolecules of interest with potential use as antifungal drugs.

  19. Cunninghamella bertholletiae exhibits increased resistance to human neutrophils with or without antifungal agents as compared to Rhizopus spp.

    Science.gov (United States)

    Simitsopoulou, Maria; Georgiadou, Elpiniki; Walsh, Thomas J; Roilides, Emmanuel

    2010-08-01

    Among Zygomycetes, Cunninghamella bertholletiae occurs less frequently as the etiologic agent of human disease but causes more aggressive, refractory, and fatal infections despite antifungal therapy. Little is known about the differential innate host response against Cunninghamella and other Zygomycetes in the presence of antifungal agents. We therefore studied the activity of human neutrophils (PMNs) alone or in combination with caspofungin, posaconazole (PSC), and voriconazole (VRC) against hyphae of Rhizopus oryzae, Rhizopus microsporus and C. bertholletiae. Hyphal damage was measured by XTT metabolic assay and release of IL-6, IL-8 and TNF-alpha from PMNs by ELISA. Cunninghamella bertholletiae was more resistant to PMN-induced hyphal damage than either Rhizopus spp. at effector:target (E:T) ratios of 1:1, 5:1 and 10:1 (P Rhizopus spp. (P < 0.01). No IL-6 was released from PMNs exposed to the three Zygomycetes. In comparison to R. oryzae and R. microsporus, C. bertholletiae is more resistant to PMN-induced hyphal damage with or without antifungal therapy and is more capable of suppressing release of IL-8.

  20. Candida urinary tract infection and Candida species susceptibilities to antifungal agents.

    Science.gov (United States)

    Osawa, Kayo; Shigemura, Katsumi; Yoshida, Hiroyuki; Fujisawa, Masato; Arakawa, Soichi

    2013-11-01

    The purpose of this study is to review Candida isolation from urine of urinary tract infection (UTI) patients over the recent 3 years at the Kobe University Hospital. We recorded the type of strain, the department where the patient was treated such as the intensive care unit (ICU), and combined isolation of Candida with other microorganisms. We investigated Candida isolation and susceptibilities to antifungal agents and analyzed the risk factors for combined isolation with other microorganisms. The most frequently isolated Candida was Candida albicans, which showed good (100%) susceptibilities to 5-fluorocytosine (5-FC) and fluconazole (FLCZ) but not to voriconazole (VRCZ), followed by C. glabrata. ICU was the greatest source of Candida-positive samples, and the most relevant underlying diseases of ICU patients were pneumonia followed by renal failure and post liver transplantation status. Combined isolation with other bacteria was seen in 27 cases (42.9%) in 2009, 25 (33.3%) in 2010 and 31 (31.3%) in 2011 and comparatively often seen in non-ICU patients. Other candidas than C. albicans showed significantly decreased susceptibility to FLCZ over these 3 years (P=0.004). One hundred (97.1%) of 103 ICU cases were given antibiotics at the time of Candida isolation, and the most often used antibiotics were cefazolin or meropenem. In conclusion, C. albicans was representatively isolated in Candida UTI and showed good susceptibilities to 5-FC, FLCZ and VRCZ, but other candidas than C. albicans showed significantly decreased susceptibility to FLCZ in the change of these 3 years.

  1. Synthesis and biological evaluation of novel fluconazole analogues bearing 1,3,4-oxadiazole moiety as potent antifungal agents.

    Science.gov (United States)

    Liao, Jun; Yang, Fan; Zhang, Lei; Chai, Xiaoyun; Zhao, Qingjie; Yu, Shichong; Zou, Yan; Meng, Qingguo; Wu, Qiuye

    2015-04-01

    A novel series of fluconazole based mimics incorporating 1,3,4-oxadiazole moiety were designed and synthesized. All the title compounds were characterized by (1)H-NMR, (13)C-NMR, and Q-TOF-MS. Preliminary results revealed that most of analogues exhibited significant antifungal activity against seven pathogenic fungi. Compounds 9g and 9k (MIC80 ≤ 0.125 μg/mL, respectively) were found more potent than the positive controls itraconazole and fluconazole as broad-spectrum antifungal agents. The observed docking results showed that the 1,3,4-oxadiazole moiety enhanced the affinity binding to the cytochrome P450 14α-demethylase (CYP51).

  2. Two small molecule lead compounds as new antifungal agents effective against Candida albicans and Saccharomyces cerevisiae

    Directory of Open Access Journals (Sweden)

    Yones Pilehvar-Soltanahmadi

    2014-06-01

    Full Text Available  Background: Antifungal drug resistance and few numbers of available drugs limit therapeutic options against fungal infections. The present study was designed to discover new antifungal drugs. Materials and Methods: This study was carried out in two separate steps, that is, in silico lead identification and in vitro assaying of antifungal potential. A structural data file of a ternary complex of fusicuccin (legend, C terminus of H+-ATPase and 14-3-3 regulatory protein (1o9F.pdb file was used as a model. Computational screening of a virtual 3D database of drug-like molecules was performed and selected small molecules, resembling the functional part of the ligand performing ligand docking, were tested using ArgusLab (4.0.1. Two lead compounds, 3-Cyclohexan propionic acid (CXP and 4-phenyl butyric acid (PBA were selected according to their ligation scores. Standard Strains of Candida albicans and Saccharomyces cerevisiae were used to measure the antifungal potential of the two identified lead compounds against the fungi using micro-well plate dilution assay. Results: Ligation scores for CXP and PBA were -9.33744 and -10.7259 kcal/mol, respectively, and MIC and MFC of CXP and PBA against the two yeasts were promising. Conclusion: The evidence from the present study suggests that CXP and PBA possess potentially antifungals properties. 

  3. Candida Infections, Causes, Targets, and Resistance Mechanisms: Traditional and Alternative Antifungal Agents

    Directory of Open Access Journals (Sweden)

    Claudia Spampinato

    2013-01-01

    Full Text Available The genus Candida includes about 200 different species, but only a few species are human opportunistic pathogens and cause infections when the host becomes debilitated or immunocompromised. Candida infections can be superficial or invasive. Superficial infections often affect the skin or mucous membranes and can be treated successfully with topical antifungal drugs. However, invasive fungal infections are often life-threatening, probably due to inefficient diagnostic methods and inappropriate initial antifungal therapies. Here, we briefly review our current knowledge of pathogenic species of the genus Candida and yeast infection causes and then focus on current antifungal drugs and resistance mechanisms. An overview of new therapeutic alternatives for the treatment of Candida infections is also provided.

  4. Screening of antifungal agents using ethanol precipitation and bioautography of medicinal and food plants.

    Science.gov (United States)

    Schmourlo, Gracilene; Mendonça-Filho, Ricardo R; Alviano, Celuta Sales; Costa, Sônia S

    2005-01-15

    In the search for bioactive compounds, bioautography and ethanol precipitation of macromolecules (proteins, polysaccharides, etc.) of plant aqueous extracts were associated in an antifungal screening. Thus, the supernatants, precipitates (obtained by ethanol precipitation) and aqueous extracts were investigated of medicinal and fruit bearing plants used against skin diseases by the Brazilian population. The agar diffusion and broth dilution methods were used to assess the activity against three fungi: Candida albicans, Trichophyton rubrum and Cryptococcus neoformans. The results, evaluated by the diameter of the inhibition zone of fungal growth, indicate that six plant species, among the 16 investigated, showed significant antifungal activity. The minimal inhibitory concentration (MIC) was determined on plant extracts that showed high efficacy against the tested microorganisms. The most susceptible yeast was Trichophyton rubrum and the best antifungal activity was shown by Xanthosoma sagittifolium supernatant. The bioautography was performed only for the aqueous extracts and supernatants of those plants that showed antifungal activity against Candida albicans and Cryptococcus neoformans, using n-butanol/acetic acid/water (BAW) 8:1:1 to develop silica gel TLC plates. Clear inhibition zones were observed for aqueous extracts of Schinus molle (R(f) 0.89) and Schinus terebinthifolius (R(f) 0.80) against Candida albicans, as for supernatant of Anacardium occidentale (R(f) 0.31) against Cryptococcus neoformans. The separation of macromolecules from metabolites, as in the case of Anacardium occidentale, Solanum sp. and Xanthosoma sagittifolium, enhances antifungal activity. In other cases, the antifungal activity is destroyed, as observed for Momordica charantia, Schinus molle and Schinus terebinthifolius.

  5. Voriconazole is a safe and effective anti-fungal prophylactic agent during induction therapy of acute myeloid leukemia

    Directory of Open Access Journals (Sweden)

    Akash Shah

    2016-01-01

    Full Text Available Background: Antifungal prophylaxis (AFP reduces the incidence of invasive fungal infections (IFIs during induction therapy of acute myeloid leukemia (AML. Posaconazole is considered the standard of care. Voriconazole, a generic cheaper alternative is a newer generation azole with broad anti-fungal activity. There is limited data on the use of voriconazole as a prophylactic drug. Materials and Methods: A single-center, prospective study was performed during which patients with AML undergoing induction chemotherapy received voriconazole as AFP (April 2012 to February 2014. Outcomes were compared with historical patients who received fluconazole as AFP (January 2011-March 2012, n = 66. Results: Seventy-five patients with AML (median age: 17 years [range: 1-75]; male:female 1.6:1 received voriconazole as AFP. The incidence of proven/probable/possible (ppp IFI was 6.6% (5/75. Voriconazole and fluconazole cohorts were well-matched with respect to baseline characteristics. Voriconazole (when compared to fluconazole reduced the incidence of pppIFI (5/75, 6.6% vs. 19/66, 29%; P < 0.001, need to start therapeutic (empiric + pppIFI antifungals (26/75, 34% vs. 51/66, 48%; P < 0.001 and delayed the start of therapeutic antifungals in those who needed it (day 16 vs. day 10; P < 0.001. Mortality due to IFI was also reduced with the use of voriconazole (1/75, 1.3% vs. 6/66, 9%; P = 0.0507, but this was not significant. Three patients discontinued voriconazole due to side-effects. Conclusion: Voriconazole is an effective and safe oral agent for IFI prophylaxis during induction therapy of AML. Availability of generic equivalents makes this a more economical alternative to posaconazole.

  6. Susceptibility variation of Malassezia pachydermatis to antifungal agents according to isolate source

    Directory of Open Access Journals (Sweden)

    Caroline Borges Weiler

    2013-01-01

    Full Text Available Malassezia pachydermatisis associated with dermatomycoses and otomycosis in dogs and cats. This study compared the susceptibility of M. pachydermatis isolates from sick (G1 and healthy (G2 animals to azole and polyene antifungals using the M27-A3 protocol. Isolates from G1 animals were less sensitive to amphotericin B, nystatin, fluconazole, clotrimazole and miconazole.

  7. 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.

  8. 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...

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

    Directory of Open Access Journals (Sweden)

    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.

  10. New synthesis and biological evaluation of benzothiazole derivates as antifungal agents.

    Science.gov (United States)

    Herrera Cano, Natividad; Ballari, María S; López, Abel G; Santiago, Ana N

    2015-04-15

    In search of new antifungal agrochemicals that could replace commercially available, aryl-2-mercaptobenzothiazoles were synthesized. They were prepared by two methodologies, using both photostimulated reaction and microwave assisted reaction. These reactions took place without the use of metallic catalyst by a one-pot procedure with excellent yields (70-98%). Synthesized compounds were evaluated for fungal growth inhibition against Botrytis cinerea. Most of the compounds have an excellent antifungal activity, and three of these showed a superior inhibitory effect to commercial fungicide Triadimefon. IC50 values observed for 2-(phenylthio)benzothiazole, 2-(2-chlorophenylthio)benzothiazole, and 2-(3-chlorophenyl thio)benzothiazole were 0.75, 0.69, and 0.65 μg mL(-1), respectively.

  11. Synthesis and biological evaluation of fluconazole analogs with triazole-modified scaffold as potent antifungal agents.

    Science.gov (United States)

    Hashemi, Seyedeh Mahdieh; Badali, Hamid; Irannejad, Hamid; Shokrzadeh, Mohammad; Emami, Saeed

    2015-04-01

    In order to find new azole antifungals, we have recently designed a series of triazole alcohols in which one of the 1,2,4-triazol-1-yl group in fluconazole structure has been replaced with 4-amino-5-aryl-3-mercapto-1,2,4-triazole motif. In this paper, we focused on the structural refinement of the primary lead, by removing the amino group from the structure to achieve 5-aryl-3-mercapto-1,2,4-triazole derivatives 10a-i and 11a-i. The in vitro antifungal susceptibility testing of title compounds demonstrated that most compounds had potent inhibitory activity against Candida species. Among them, 5-(2,4-dichlorophenyl)triazole analogs 10h and 11h with MIC values of fluconazole against Candida species.

  12. In vitro interactions of antifungal agents and tacrolimus against Aspergillus biofilms.

    Science.gov (United States)

    Gao, Lujuan; Sun, Yi

    2015-11-01

    Aspergillus biofilms were prepared from Aspergillus fumigatus, Aspergillus flavus, and Aspergillus terreus via a 96-well plate-based method, and the combined antifungal activity of tacrolimus with azoles or amphotericin B against Aspergillus biofilms was investigated via a broth microdilution checkerboard technique system. Our results suggest that combinations of tacrolimus with voriconazole or amphotericin B have synergistic inhibitory activity against Aspergillus biofilms. However, combinations of tacrolimus with itraconazole or posaconazole exhibit no synergistic or antagonistic effects.

  13. Topical anti-inflammatory properties of flutrimazole, a new imidazole antifungal agent.

    Science.gov (United States)

    Merlos, M; Vericat, M L; García-Rafanell, J; Forn, J

    1996-01-01

    The topical anti-inflammatory properties of flutrimazole, a new imidazole antifungal, have been evaluated. Flutrimazole inhibited mouse ear oedema induced by arachidonic acid, tetradecanoylphorbol-acetate and dithranol, with IC50 values of 3.32, 0.55 and 2.42 mumols/ear, respectively. Ketoconazole showed similar potency in arachidonic acid and dithranol models (IC50 = 3.76 and 2.41 mumols/ear) whereas it was less active against tetradecanoylphorbol acetate (IC50 = 1.96 mumols/ear). The standard anti-inflammatory sodium diclofenac was overall slightly more potent than antifungals (IC50 = 2.23, 0.57 and 0.57 mumols/ear against arachidonic acid, tetradecanoylphorbol acetate and dithranol, respectively). Both 2% flutrimazole and 2% ketoconazole creams, applied topically, inhibited carrageenan-induced rat paw oedema by about 40%. Under the same conditions, 1% flutrimazole and diclofenac creams inhibited by 26 and 54%, respectively. Flutrimazole may work through the inhibition of 5-lipoxygenase, as it inhibited LTB4 production by human granulocytes with an IC50 value of 11 microM (IC50 value for ketoconazole was 17 microM), whereas ram seminal vesicle cyclooxygenase was only inhibited by 16% at a concentration of 25 microM. Drugs such as flutrimazole, with dual anti-inflammatory/antifungal activity, may be advantageous in the treatment of topical fungal infections with an inflammatory component.

  14. Fungal peritonitis in patients undergoing peritoneal dialysis (PD) in Brazil: molecular identification, biofilm production and antifungal susceptibility of the agents.

    Science.gov (United States)

    Giacobino, Juliana; Montelli, Augusto Cezar; Barretti, Pasqual; Bruder-Nascimento, Ariane; Caramori, Jacqueline Teixeira; Barbosa, Luciano; Bagagli, Eduardo

    2016-10-01

    This paper presents data on fungal peritonitis (FP) in patients undergoing peritoneal dialysis (PD) at the University Hospital of Botucatu Medical School, São Paulo, Brazil. In a total of 422 patients, 30 developed FP, from which the medical records and the fungal isolates of 23 patient cases were studied. All patients presented abdominal pain, cloudy peritoneal effluent, needed hospitalization, had the catheter removed and were treated with fluconazole or fluconazole plus 5-flucitosine; six of them died due to FP. Concerning the agents, it was observed that Candida parapsilosis was the leading species (9/23), followed by Candida albicans (5/23), Candida orthopsilosis (4/23), Candida tropicalis (3/23), Candida guilliermondii (1/23), and Kodamaea ohmeri (1/23). All the isolates were susceptible to amphotericin B, voriconazole and caspofungin whereas C. albicans isolates were susceptible to all antifungals tested. Resistance to fluconazole was observed in three isolates of C. orthopsilosis, and dose-dependent susceptibility to this antifungal was observed in two isolates of C. parapsilosis and in the K. ohmeri isolate. Biofilm production estimates were high or moderate in most isolates, especially in C. albicans species, and low in C. parapsilosis species, with a marked variation among the isolates. This Brazilian study reinforces that FP in PD is caused by a diverse group of yeasts, most prevalently C. parapsilosis sensu stricto species. In addition, they present significant variation in susceptibility to antifungals and biofilm production, thus contributing to the complexity and severity of the clinical features.

  15. Synthesis and biological evaluation of novel phosphoramidate derivatives of coumarin as chitin synthase inhibitors and antifungal agents.

    Science.gov (United States)

    Ji, Qinggang; Ge, Zhiqiang; Ge, Zhixing; Chen, Kaizhi; Wu, Hualong; Liu, Xiaofei; Huang, Yanrong; Yuan, Lvjiang; Yang, Xiaolan; Liao, Fei

    2016-01-27

    A series of novel phosphoramidate derivatives of coumarin have been designed and synthesized as chitin synthase (CHS) inhibitors. All the synthesized compounds have been screened for their chitin synthase inhibition activity and antimicrobial activity in vitro. The bioactive assay manifested that most of the target compounds exhibited good efficacy against CHS and a variety of clinically important fungal pathogens. In particular, compound 7t with IC50 of 0.08 mM against CHS displayed stronger efficiency than the reference Polyoxin B with IC50 of 0.16 mM. In addition, the apparent Ki values of compound 7t was 0.096 mM while the Km of Chitin synthase prepared from Candida tropicalis was 3.86 mM for UDP-N-acetylglucosamine, and the result of the Ki showed that the compounds was a non-competitive inhibitor of the CHS. As far as the antifungal activity is concerned, compounds 7o, 7r and 7t were highly active against Aspergillus flavus with MIC values in the range of 1 μg/mL to 2 μg/Ml while the results of antibacterial screening showed that these compounds have negligible actions to the tested bacteria. These results indicated that the design of these compounds as antifungal agents was rational.

  16. Clerodane type diterpene as a novel antifungal agent from Polyalthia longifolia var. pendula.

    Science.gov (United States)

    Bhattacharya, Asish K; Chand, Hemender R; John, Jyothis; Deshpande, Mukund V

    2015-04-13

    Bioactivity-guided chemical examination of methanolic extract of leaves of Polyalthia longifolia var. pendula led to the isolation of the active constituent, a diterpene 1 which was identified as 16α-hydroxycleroda-3,13(14)Z-dien-15,16-olide on the basis of its spectral data. Among the tested strains, diterpene 1 was found to exhibit antifungal activities having MIC90 values of 50.3, 100.6 and 201.2 μM against Candida albicans NCIM3557, Cryptococcus neoformans NCIM3542 (human pathogens) and Neurospora crassa NCIM870 (saprophyte), respectively. Initial, structure-activity-relationship (SAR) data generated by synthesizing some derivatives revealed that the double bond between C3-C4 and the free hydroxyl group at C16 are crucial for the antifungal activity of the diterpene 1. The mode of action of 1 in C. albicans is due to compromised cell membrane permeability and also probably due to disruption of cell wall structures. The red blood cell haemolysis of all the compounds (1-4) did not show any significant haemolysis and was found to be less than 15% for all the compounds when tested at highest concentration, i.e. 1200 μM. Interestingly, all the tested compounds inhibited Y-H transition in dimorphic C. albicans NCIM3557 at much lower concentration than their MIC90 values. Determination of ROS generation by diterpene 1 using DCFH-DA and DHR123 (dihydrorhodamine) staining of C. albicans NCIM3557 indicated production of intracellular ROS as a mechanism of antifungal activity.

  17. 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.

  18. Comparison of antifungal activities of various essential oils on the Phytophthora drechsleri, the causal agent of fruit decay

    Directory of Open Access Journals (Sweden)

    Ali Mohammadi

    2015-10-01

    Full Text Available Background and Objectives: The efficacy of Mentha piperita L, Zataria multiflora Boiss and Thymus vulgaris L essential oils (EOs was evaluated for controlling the growth of Phytophthora drechsleri, the causative agent of damage to many crops that is consumed directly by humans.Materials and Methods: The EOs used in this study was purchased from Magnolia Co, Iran. The pour plate method in petri dishes containing Potato Dextrose Agar (PDA was used to evaluate the antifungal properties of EOs. The minimal inhibitory concentrations (MIC, minimum fungicidal concentration (MFC as well as mycelial growth inhibition (MGI were measured. The IC50 value (the concentration inhibited 50% of the mycelium growth was calculated by probit analysis.Results and Conclusion: The fungal growth was significantly reduced by increasing concentrations of tested EOs. The complete reduction was obtained with Shirazi thyme at all concentrations, whereas the complete reduction for peppermint and thyme was observed at 0.4% and 0.8% (v/v concentrations, respectively. Meanwhile, the minimum inhibition wasobserved when 0.1% peppermint (MGI values of 9.37% was used. The IC50, MIC and MFC values of Shirazi thyme was 0.053, 0.1% and 0.2%, respectively. Similarly, MIC and MFC values of peppermint and thyme were recorded 0.4% and 0.8%, respectively. The results obtained from this study may contribute to the development of new antifungal agents to protect the crops from this pathogenic fungus and many agricultural plant pathogens causing drastic crop losses.

  19. Carboxymethylated chitosan-stabilized copper nanoparticles: a promise to contribute a potent antifungal and antibacterial agent

    Energy Technology Data Exchange (ETDEWEB)

    Tantubay, Sangeeta, E-mail: sang.chem2@gmail.com [Indian Institute of Technology Kharagpur, Department of Chemistry (India); Mukhopadhyay, Sourav K. [Indian Institute of Technology Kharagpur, Department of Biotechnology (India); Kalita, Himani; Konar, Suraj [Indian Institute of Technology Kharagpur, Department of Chemistry (India); Dey, Satyahari [Indian Institute of Technology Kharagpur, Department of Biotechnology (India); Pathak, Amita, E-mail: ami@chem.iitkgp.ernet.in; Pramanik, Panchanan, E-mail: ppramanik1946@yahoo.in, E-mail: pramanik1946@gmail.com [Indian Institute of Technology Kharagpur, Department of Chemistry (India)

    2015-06-15

    Carboxymethylated chitosan (CMC)-stabilized copper nanoparticles (Cu-NPs) have been synthesized via chemical reduction of copper(II)–CMC complex in aqueous medium by hydrazine under microwave irradiation in ambient atmosphere. Structural morphology, phase, and chemical compositions of CMC-stabilized Cu-NPs (CMC–Cu-NPs) have been analyzed through high-resolution transmission electron microscopy, field emission scanning electron microscopy, X-ray diffraction, and X-ray photoelectron spectroscopy. Antifungal and antibacterial activities of CMC–Cu-NPs have been evaluated against Candida tropicalis and Escherichia coli through agar well diffusion method, broth microdilution assay, live–dead assay, and microscopic observation. Antimicrobial activity of spherical CMC–Cu-NPs (∼4–15 nm of diameters) has been observed to be significant for both C. tropicalis and E. coli. The cytotoxicity study indicates that CMC–Cu-NPs have no significant toxic effect against normal cell line, L929.

  20. Carboxymethylated chitosan-stabilized copper nanoparticles: a promise to contribute a potent antifungal and antibacterial agent

    Science.gov (United States)

    Tantubay, Sangeeta; Mukhopadhyay, Sourav K.; Kalita, Himani; Konar, Suraj; Dey, Satyahari; Pathak, Amita; Pramanik, Panchanan

    2015-06-01

    Carboxymethylated chitosan (CMC)-stabilized copper nanoparticles (Cu-NPs) have been synthesized via chemical reduction of copper(II)-CMC complex in aqueous medium by hydrazine under microwave irradiation in ambient atmosphere. Structural morphology, phase, and chemical compositions of CMC-stabilized Cu-NPs (CMC-Cu-NPs) have been analyzed through high-resolution transmission electron microscopy, field emission scanning electron microscopy, X-ray diffraction, and X-ray photoelectron spectroscopy. Antifungal and antibacterial activities of CMC-Cu-NPs have been evaluated against Candida tropicalis and Escherichia coli through agar well diffusion method, broth microdilution assay, live-dead assay, and microscopic observation. Antimicrobial activity of spherical CMC-Cu-NPs ( 4-15 nm of diameters) has been observed to be significant for both C. tropicalis and E. coli. The cytotoxicity study indicates that CMC-Cu-NPs have no significant toxic effect against normal cell line, L929.

  1. 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.

  2. Perillaldehyde, a Promising Antifungal Agent Used in Food Preservation, Triggers Apoptosis through a Metacaspase-Dependent Pathway in Aspergillus flavus.

    Science.gov (United States)

    Tian, Jun; Wang, Yanzhen; Lu, Zhaoqun; Sun, Chunhui; Zhang, Man; Zhu, Aihua; Peng, Xue

    2016-10-05

    In the present study, we provide detailed insights into perillaldehyde (PAE)'s mechanisms of action on Aspergillus flavus and offer evidence in favor of the induction of an apoptosis-like phenotype. Specifically, PAE's antifungal mode of action was investigated through the detection of mitochondrial membrane potential (MtΔψ) and phosphatidylserine (PS) exposure, as well as intracellular Ca(2+) level, reactive oxygen species accumulation, and metacaspase activation. This was done by way of fluorometry, measuring DNA fragmentation, and condensation by fluorescent microscopy. Furthermore, we searched for phenotypic changes characteristic of apoptosis by transmission electron microscopy and flow cytometry, determining the amount of cytochrome c released using Western blotting. Results indicated that cultivation of A. flavus in the presence of PAE caused depolarization of MtΔψ, rapid DNA condensation, large-scale DNA fragmentation, and an elevation of intracellular Ca(2+) level. The percentage of early apoptotic cells with exposure of PS were 27.4% and 48.7%, respectively, after 9 h incubations with 0.25 and 0.5 μL/mL of PAE. The percentage of stained cells with activated intracellular metacaspases exposed to PAE at concentrations of 0.25 and 0.5 μL/mL compared with control subjects were increased by 28.4 ± 3.25% and 37.9 ± 4.24%, respectively. The above results has revealed that PAE induces fungal apoptosis through a caspase-dependent mitochondrial pathway. In all, our findings provide a novel mechanism for exploring a possible antifungal agent used in food preservation.

  3. Synthesis and Biological Evaluation of New Eugenol Mannich Bases as Promising Antifungal Agents.

    Science.gov (United States)

    Abrão, Pedro Henrique O; Pizi, Rafael B; de Souza, Thiago B; Silva, Naiara C; Fregnan, Antonio M; Silva, Fernanda N; Coelho, Luiz Felipe L; Malaquias, Luiz Cosme C; Dias, Amanda Latercia T; Dias, Danielle F; Veloso, Marcia P; Carvalho, Diogo T

    2015-10-01

    New Mannich base-type eugenol derivatives were synthesized and evaluated for their anticandidal activity using a broth microdilution assay. Among the synthesized compounds, 4-allyl-2-methoxy-6-(morpholin-4-ylmethyl) phenyl benzoate (7) and 4-{5-allyl-2-[(4-chlorobenzoyl)oxy]-3-methoxybenzyl}morpholin-4-ium chloride (8) were found to be the most effective antifungal compounds with low IC50 values, some of them well below those of reference drug fluconazole. The most significant IC50 values were those of 7 against C. glabrata (1.23 μm), C. albicans and C. krusei (both 0.63 μm). Additionally, the synthesized compounds were evaluated for their in vitro cytotoxic effects on human mononuclear cells. As result, the cytotoxic activity of eugenol in eukaryotic cells decreased with the introduction of the morpholinyl group. Given these findings, we point out compounds 7 and 8 as the most promising derivatives because they showed potency values greater than those of eugenol and fluconazole and they also presented high selectivity indexes.

  4. [Molecular epidemiologic surveillance and antifungal agent sensitivity of Candida albicans isolated from anesthesia intensive care units].

    Science.gov (United States)

    Gülay, Zeynep; Ergon, Cem; Ozkütük, Aydan; Yücesoy, Mine; Biçmen, Meral

    2002-01-01

    Patients in intensive care units (ICU) are at risk of nosocomial infections. The incidence of nosocomial fungal infections has increased in parallel with the increase of nosocomial infections. Candida albicans is the most frequent pathogenic species among the fungi. The aim of this study was to make an epidemiological surveillance of C. albicans urine isolates which were isolated from patients who were hospitalized in ICU between June 2000 and October 2001 by antifungal susceptibility testing and Randomly Amplified Polymorphic DNA (RAPD) analysis. For this purpose, 38 C. albicans which were isolated from 29 patients were investigated for amphotericin B and fluconazole susceptibility with the microdilution method. The range of minimal inhibitory concentration (MIC) of amphotericin B was between 0.25-1 microgram/ml and MIC50 value was 0.5 microgram/ml and none of the isolates had high (MIC > 1 microgram/ml) MIC values. The MIC values for fluconazole varied between 0.25-16 micrograms/ml and MIC50 value was 1 microgram/ml. While none of the isolates was resistant to fluconazole, two isolates were detected as dose dependent susceptible. RAPD analysis was performed with two different primers in order to investigate clonal relationship, and 22 patterns were detected with one of the primers and 24 patterns were detected with the other. In conclusion, it is thought that the origin of the C. albicans urine isolates were mostly endogenous but exogenous spread might also be considered as isolates that were clonally related were isolated from different patients at the same time interval.

  5. 9-O-butyl-13-(4-isopropylbenzyl)berberine, KR-72, is a potent antifungal agent that inhibits the growth of Cryptococcus neoformans by regulating gene expression.

    Science.gov (United States)

    Bang, Soohyun; Kwon, Hyojeong; Hwang, Hyun Sook; Park, Ki Duk; Kim, Sung Uk; Bahn, Yong-Sun

    2014-01-01

    In this study we explored the mode of action of KR-72, a 9-O-butyl-13-(4-isopropylbenzyl)berberine derivative previously shown to exhibit potent antifungal activity against a variety of human fungal pathogens. The DNA microarray data revealed that KR-72 treatment significantly changed the transcription profiles of C. neoformans, affecting the expression of more than 2,000 genes. Genes involved in translation and transcription were mostly upregulated, whereas those involved in the cytoskeleton, intracellular trafficking, and lipid metabolism were downregulated. KR-72 also exhibited a strong synergistic effect with the antifungal agent FK506. KR-72 treatment regulated the expression of several essential genes, including ECM16, NOP14, HSP10 and MGE1, which are required for C. neoformans growth. The KR-72-mediated induction of MGE1 also likely reduced the viability of C. neoformans by impairing cell cycle or the DNA repair system. In conclusion, KR-72 showed antifungal activity by modulating diverse biological processes through a mode of action distinct from those of clinically available antifungal drugs such as polyene and azole drugs.

  6. Expansion of a recent class of broad-spectrum antifungal agents: the echinocandins

    Directory of Open Access Journals (Sweden)

    Roberto Manfredi

    2009-09-01

    Full Text Available The echinocandins show comparable efficacy in the treatment of candidemia and invasive candidiasis. Caspofungin and micafungin appear to be similarly efficacious in salvage therapy in aspergillosis; anidulafungin has excellent in vitro activity against Aspergillus species but as yet there are no sufficient clinical data for anidulafungin in this disease state. Each drug has minor advantages and disadvantages compared to the others of the same classe; however, there are large differences in the approved indications for the different drugs. The formulary selection process should consider the direct and indirect costs of the single agents; the characteristics of the patient population at risk for invasive mycosis, such as frequent use of interacting drugs and the burden of monitoring plasma drug levels of drugs; and the implications of using products for indications which have not been still approved (off-label indications.

  7. 医院2010-2012年抗真菌药使用分析%Use of antifungal agents from 2010 to 2012

    Institute of Scientific and Technical Information of China (English)

    刘蔚

    2015-01-01

    目的 评价2010-2012年抗真菌药物使用情况.方法 利用计算机对各药出库数量和金额数据进行统计排序.采用世界卫生组织推荐的限定日剂量(DDD)作为药物利用研究的测定单位,调查解放军第三○九医院2010-2012年抗真菌药销售金额、销售量,采用金额分析法、用药频度(DDDs)分析法对抗真菌药的销售金额、年DDDs和日均费用等进行统计分析.结果 2010-2012年本院抗真菌药物的年销售总金额呈明显下降趋势,2011年销售总金额(11 381 151元)较2010年销售总金额(13 756 650元)下降17.3%,2012年销售总金额(11 349 923元)较2010年销售总金额(13 756 650元)下降17.5%,DDDs同步性较好.临床使用占主导地位的是三唑类及棘白菌素类抗真菌药,2010-2012年销售总金额位列前3位的是注射用米卡芬净钠、氟康唑注射液及注射用伏立康唑;用药频度位列前3位的是伊曲康唑胶囊、氟康唑注射液及氟康唑胶囊.结论 本院抗真菌药物应用合理、管理完善,疗效确定、价格适中的抗真菌药具有良好的发展趋势.%Objective To evaluate the application of the antifungal agents from 2010 to 2012; to provide the references for clinical management and rational use of drugs.Methods The utilization data such as consumption sum and quantity of Antifungal agents in our hospital from 2010 to 2012 were statistically analyzd from the consumption sum,annual defined daily dose statistic(DDDs) and defined daily cost(DDC) by methods of consumption analysis and DDDs analysis.Results The consumption sum of antifungal agents markedly reduced year by year,the consumption sum of the year 2011 (11 381 151 yuan) decreased 17.3% compared with the year 2010 (13 756 650 yuan),the consumption sum of the year 2012 (11 349 923 yuan) decreased 17.5% compared with the year 2010(13 756 650 yuan),and the DDDs showed good synchronism.triazole antifungal agents and echinocandins were the dominant

  8. Search for antibacterial and antifungal agents from selected Indian medicinal plants.

    Science.gov (United States)

    Kumar, V Prashanth; Chauhan, Neelam S; Padh, Harish; Rajani, M

    2006-09-19

    A series of 61 Indian medicinal plants belonging to 33 different families used in various infectious disorders, were screened for their antimicrobial properties. Screening was carried out at 1000 and 500 microg/ml concentrations by agar dilution method against Bacillus cereus var mycoides, Bacillus pumilus, Bacillus subtilis, Bordetella bronchiseptica, Micrococcus luteus, Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Streptococcus faecalis, Candida albicans, Aspergillus niger and Saccharomyces cerevisiae. Twenty-eight plant extracts showed activity against at least one of the test organisms used in the screening. On the basis of the results obtained, we conclude that the crude extracts of Dorema ammoniacum, Sphaeranthus indicus, Dracaena cinnabari, Mallotus philippinensis, Jatropha gossypifolia, Aristolochia indica, Lantana camara, Nardostachys jatamansi, Randia dumetorum and Cassia fistula exhibited significant antimicrobial activity and properties that support folkloric use in the treatment of some diseases as broad-spectrum antimicrobial agents. This probably explains the use of these plants by the indigenous people against a number of infections.

  9. 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.

  10. 五种新型唑类抗真菌药物%Five novel azole antifungal agents

    Institute of Scientific and Technical Information of China (English)

    王乐; 刘维达

    2011-01-01

    Azoles are a primary treatment choice for superficial and deep fungal infections. They can be divided into two groups, i.e., imidazoles and triazoles, according to chemical structure. Three new imidazoles including luliconazole, lanoconazole and flutrimazole have been on the medical market abroad and shown notable efficacy with no obvious local side effects in the treatment of superficial fungal infection including dermatophytosis. Two triazoles including pramiconazole and ravuconazole are still in clinical trials, although they have proved to be safe and effective in the treatment of superficial and deep fungal infection, and have shown some potential as new antifungal agents.%唑类药物是目前治疗浅部和深部真菌感染的一线用药.按照其结构的不同,该药可以分为咪唑类和三唑类.3种咪唑类新药卢立康唑、拉诺康唑和氟曲乌唑已在国外上市,外用治疗皮肤癣菌等浅部真菌病疗效明显且局部无明显不良反应.2种三唑类新药普拉康唑和雷夫康唑则仍在临床试验阶段,但从目前研究来看,两者用于治疗浅部和深部真菌感染亦较安全有效,有望作为新型抗真菌药应用于临床.

  11. Triazole antifungals: a review.

    Science.gov (United States)

    Peyton, L R; Gallagher, S; Hashemzadeh, M

    2015-12-01

    Invasive fungal infections and systemic mycosis, whether from nosocomial infection or immunodeficiency, have been on an upward trend for numerous years. Despite advancements in antifungal medication, treatment in certain patients can still be difficult for reasons such as impaired organ function, limited administration routes or poor safety profiles of the available antifungal medications. The growing number of invasive fungal species becoming resistant to current antifungal medications is of appreciable concern. Triazole compounds containing one or more 1,2,4-triazole rings have been shown to contain some of the most potent antifungal properties. Itracon-azole and fluconazole were some of the first triazoles synthesized, but had limitations associated with their use. Second-generation triazoles such as voriconazole, posa-conazole, albaconazole, efinaconazole, ravuconazole and isavuconazole are all derivatives of either itraconazole or fluconazole, and designed to overcome the deficiencies of their parent drugs. The goal of this manuscript is to review antifungal agents derived from triazole.

  12. Isavuconazole, micafungin, and 8 comparator antifungal agents' susceptibility profiles for common and uncommon opportunistic fungi collected in 2013: temporal analysis of antifungal drug resistance using CLSI species-specific clinical breakpoints and proposed epidemiological cutoff values.

    Science.gov (United States)

    Pfaller, M A; Rhomberg, P R; Messer, S A; Jones, R N; Castanheira, M

    2015-08-01

    The in vitro activities of isavuconazole, micafungin, and 8 comparator antifungal agents were determined for 1613 clinical isolates of fungi (1320 isolates of Candida spp., 155 of Aspergillus spp., 103 of non-Candida yeasts, and 35 non-Aspergillus molds) collected during a global survey conducted in 2013. The vast majority of the isolates of the 21 different species of Candida, with the exception of Candida glabrata (MIC90, 2 μg/mL), Candida krusei (MIC90, 1 μg/mL), and Candida guilliermondii (MIC90, 8 μg/mL), were inhibited by ≤0.25 μg/mL of isavuconazole. C. glabrata and C. krusei were largely inhibited by ≤1 μg/mL of isavuconazole. Resistance to fluconazole was seen in 0.5% of Candida albicans isolates, 11.1% of C. glabrata isolates, 2.5% of Candida parapsilosis isolates, 4.5% of Candida tropicalis isolates, and 20.0% of C. guilliermondii isolates. Resistance to the echinocandins was restricted to C. glabrata (1.3-2.1%) and C. tropicalis (0.9-1.8%). All agents except for the echinocandins were active against 69 Cryptococcus neoformans isolates, and the triazoles, including isavuconazole, were active against the other yeasts. Both the mold active triazoles as well as the echinocandins were active against 155 Aspergillus spp. isolates belonging to 10 species/species complex. In general, there was low resistance levels to the available systemically active antifungal agents in a large, contemporary (2013), global collection of molecularly characterized yeasts and molds. Resistance to azoles and echinocandins was most prominent among isolates of C. glabrata, C. tropicalis, and C. guilliermondii.

  13. 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)

  14. 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.

  15. Antifungal agents. 5. Chemical modification of antibiotics from Polyangium cellulosum var. fulvum. Alcohol, ketone, aldehyde, and oxime analogues of ambruticin.

    Science.gov (United States)

    Connor, D T; von Strandtmann, M

    1979-09-01

    Alcohol, ketone, aldehyde, and oxime analogues of ambruticin (1) were prepared. The analogues were tested against Histoplasma capsulatum, Microsporum fulvum, Candida albicans, and Streptococcus pyogenes. Structure-activity relationships are described. Increasing the bulk of substituent at C1 and C5 reduces antifungal activity.

  16. The novel antifungal agent PLD-118 is neither metabolized by liver microsomes nor inhibits cytochrome P450 in vitro

    NARCIS (Netherlands)

    Parnham, M.J.; Bogaards, J.J.P.; Schrander, F.; Schut, M.W.; Orešković, K.; Mildner, B.

    2005-01-01

    PLD-118 is a novel, oral antifungal drug, under development for the treatment of Candida infections. Possible metabolism of PLD-118 by rat, dog and human S9 liver homogenates and inhibition of human cytochrome P450 (CYP) enzymes were investigated. PLD-118 (10 and 100 μm) incubated for 0-60 min with

  17. Microwave-Assisted Synthesis and Biological Evaluation of Dihydropyrimidinone Derivatives as Anti-Inflammatory, Antibacterial, and Antifungal Agents

    Directory of Open Access Journals (Sweden)

    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.

  18. Comparison of EUCAST and CLSI broth microdilution methods for the susceptibility testing of 10 systemically active antifungal agents when tested against Candida spp.

    Science.gov (United States)

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

    2014-06-01

    The antifungal broth microdilution (BMD) method of the European Committee on Antimicrobial Susceptibility Testing (EUCAST) was compared with Clinical and Laboratory Standards Institute (CLSI) BMD method M27-A3 for amphotericin B, flucytosine, anidulafungin, caspofungin, micafungin, fluconazole, isavuconazole, itraconazole, posaconazole, and voriconazole susceptibility testing of 357 isolates of Candida. The isolates were selected from global surveillance collections to represent both wild-type (WT) and non-WT MIC results for the azoles (12% of fluconazole and voriconazole results were non-WT) and the echinocandins (6% of anidulafungin and micafungin results were non-WT). The study collection included 114 isolates of Candida albicans, 73 of C. glabrata, 76 of C. parapsilosis, 60 of C. tropicalis, and 34 of C. krusei. The overall essential agreement (EA) between EUCAST and CLSI results ranged from 78.9% (posaconazole) to 99.6% (flucytosine). The categorical agreement (CA) between methods and species of Candida was assessed using previously determined CLSI epidemiological cutoff values. The overall CA between methods was 95.0% with 2.5% very major (VM) and major (M) discrepancies. The CA was >93% for all antifungal agents with the exception of caspofungin (84.6%), where 10% of the results were categorized as non-WT by the EUCAST method and WT by the CLSI method. Problem areas with low EA or CA include testing of amphotericin B, anidulafungin, and isavuconazole against C. glabrata, itraconazole, and posaconazole against most species, and caspofungin against C. parapsilosis, C. tropicalis, and C. krusei. We confirm high level EA and CA (>90%) between the 2 methods for testing fluconazole, voriconazole, and micafungin against all 5 species. The results indicate that the EUCAST and CLSI methods produce comparable results for testing the systemically active antifungal agents against the 5 most common species of Candida; however, there are several areas where additional

  19. In Vitro Activity of Seven Systemically Active Antifungal Agents against a Large Global Collection of Rare Candida Species as Determined by CLSI Broth Microdilution Methods ▿

    Science.gov (United States)

    Diekema, D. J.; Messer, S. A.; Boyken, L. B.; Hollis, R. J.; Kroeger, J.; Tendolkar, S.; Pfaller, M. A.

    2009-01-01

    Five Candida species (C. albicans, C. glabrata, C. tropicalis, C. parapsilosis, and C. krusei) account for over 95% of invasive candidiasis cases. Some less common Candida species have emerged as causes of nosocomial candidiasis, but there is little information about their in vitro susceptibilities to antifungals. We determined the in vitro activities of fluconazole, voriconazole, posaconazole, amphotericin B, anidulafungin, caspofungin, and micafungin against invasive, unique patient isolates of Candida collected from 100 centers worldwide between January 2001 and December 2007. Antifungal susceptibility testing was performed by the CLSI M27-A3 method. CLSI breakpoints for susceptibility were used for fluconazole, voriconazole, anidulafungin, caspofungin, and micafungin, while a provisional susceptibility breakpoint of ≤1 μg/ml was used for amphotericin and posaconazole. Of 14,007 Candida isolates tested, 658 (4.7%) were among the less common species. Against all 658 isolates combined, the activity of each agent, expressed as the MIC50/MIC90 ratio (and the percentage of susceptible isolates) was as follows: fluconazole, 1/4 (94.8%); voriconazole, 0.03/0.12 (98.6%); posaconazole, 0.12/0.5 (95.9%); amphotericin, 0.5/2 (88.3%); anidulafungin, 0.5/2 (97.4%); caspofungin, 0.12/0.5 (98.0%); and micafungin, 0.25/1 (99.2%). Among the isolates not susceptible to one or more of the echinocandins, most (68%) were C. guilliermondii. All isolates of the less common species within the C. parapsilosis complex (C. orthopsilosis and C. metapsilosis) were susceptible to voriconazole, posaconazole, anidulafungin, caspofungin, and micafungin. Over 95% of clinical isolates of the rare Candida species were susceptible to the available antifungals. However, activity did vary by drug-species combination, with some species (e.g., C. rugosa and C. guilliermondii) demonstrating reduced susceptibilities to commonly used agents such as fluconazole and echinocandins. PMID:19710283

  20. Comparative biorelease study of fluticasone in combination with antibacterial (Neomycin and or antifungal (coltrimazol, miconazole agents by histamine percutaneous reaction method in healthy volunteers

    Directory of Open Access Journals (Sweden)

    Shahani S

    1997-01-01

    Full Text Available Fluticasone propionate is a novel, potent and topically active synthetic corticosteroid preparation with a much reduced potential, in relation to its anti-inflammatory potency, for unwanted systemic side effects. It is indicated for the treatment of eczema, dermatitis etc. The objective of the present study was to evaluate and compare the biorelease of fluticassone with placebo (base formulation; its combination with antifungal (miconazole, clotrimazole and / or antibacterial agents based on the attenuation of histamine induced wheal and flare reaction and flare intensity (on visual analouge scale by McNemar test. In the present study, fluticasone alone and in combination with clotrimazole, miconazole and neomycin significantly reduced the wheal and flare response of histamine prick test. The flare intensity response was also significantly inhibited by these treatments. Furthermore, there was no difference in the anti-inflammatory activity of various treatment groups. It may, therefore, be concluded that antibacterial (neomycin and / or antifungal (miconazole, clotrimazole agents in combination with steroid (fluticasone do not alter the pharmacodynamic response of the latter.

  1. Activity of a Long-Acting Echinocandin (CD101) and Seven Comparator Antifungal Agents Tested against a Global Collection of Contemporary Invasive Fungal Isolates in the SENTRY 2014 Antifungal Surveillance Program

    Science.gov (United States)

    Pfaller, Michael A.; Messer, Shawn A.; Rhomberg, Paul R.

    2017-01-01

    ABSTRACT The activity of CD101 and comparator antifungal agents against 606 invasive fungal isolates collected worldwide during 2014 was evaluated using the Clinical and Laboratory Standards Institute (CLSI) method. All Candida albicans (n = 251), Candida tropicalis (n = 51), Candida krusei (n = 16), and Candida dubliniensis (n = 11) isolates were inhibited by ≤0.12 μg/ml of CD101 and were susceptible or showed wild-type susceptibility to the other echinocandins tested. Five C. glabrata isolates (n = 100) displayed CD101 MIC values of 1 to 4 μg/ml, had elevated MICs of caspofungin (2 to >8 μg/ml), anidulafungin (2 to 4 μg/ml), and micafungin (2 to 4 μg/ml), and carried mutations on fks1 and fks2. Candida parapsilosis (n = 92) and Candida orthopsilosis (n = 10) displayed higher CD101 MIC values (ranges, 0.5 to 4 μg/ml and 0.12 to 2 μg/ml, respectively), and similar results were observed for the other echinocandins tested. Fluconazole resistance was noted among 11.0% of Candida glabrata isolates, 4.3% of C. parapsilosis isolates, and 2.0% of C. albicans and C. tropicalis isolates. The activity of CD101 against Aspergillus fumigatus (n = 56) was similar to that of micafungin and 2-fold greater than that of caspofungin but less than that of anidulafungin. These isolates had wild-type susceptibility to itraconazole, voriconazole, and posaconazole. The echinocandins had limited activity against Cryptococcus neoformans (n = 19). CD101 was as active as the other echinocandins against common fungal organisms recovered from patients with invasive fungal infections. The long half-life profile is very desirable for the prevention and treatment of serious fungal infections, especially in patients who can then be discharged from the hospital to complete antifungal therapy on an outpatient basis. PMID:28052853

  2. Fluconazole exposure rather than clonal spreading is correlated with the emergence of Candida glabrata with cross-resistance to triazole antifungal agents.

    Science.gov (United States)

    Chen, Tun-Chieh; Chen, Yen-Hsu; Chen, Yee-Chun; Lu, Po-Liang

    2012-06-01

    The emergence of antifungal resistance in Candida species has raised concern in recent years, especially resistance toward triazole. Several newer triazole antifungal agents have been introduced which have a broader spectrum for fungal infections, such as voriconazole. However, cross-resistance among triazoles is a major concern with regard to their clinical application. Antifungal susceptibility was performed using E-test for 166 clinical isolates (29 blood and 137 nonblood isolates) in 2003 and 2004. We applied pulsed-field gel electrophoresis for genotyping. Ninety isolates of C. albicans, 47 isolates of C. tropicalis, 27 isolates of C. glabrata, and two isolates of C. krusei were included. All isolates were susceptible to amphotericin B. Eleven (40.7%) of the 27 C. glabrata had intermediate resistance to caspofungin. Forty-seven (28.3%) of the 166 isolates were not susceptible to fluconazole, including two C. albicans, 16 C. tropicalis, 27 C. glabrata, and two C. krusei isolates. All except seven of the C. glabrata isolates were susceptible to voriconazole. All the triazole drugs had a positive correlation among their minimum inhibitory concentrations (MICs). Fluconazole MIC was a good predictor for susceptibility to voriconazole, as determined using a receiver operating characteristic curve. Furthermore, a high diversity of pulsotypes for the 27 clinical isolates of C. glabrata was observed. Previous fluconazole exposure within 3 months was associated with reduced triazole susceptibility for C. glabrata. We demonstrated a significant positive correlation of MIC values among the four tested triazole drugs. No amphotericin B and caspofungin resistant isolates were found in this study. The cross-resistance to triazole among C. glabrata isolates was associated with previous fluconazole exposure as opposed to clonal spreading. Selection pressure due to fluconazole use may play a major role in triazole cross-resistance.

  3. Special Issue: Novel Antifungal Drug Discovery

    Directory of Open Access Journals (Sweden)

    Maurizio Del Poeta

    2016-12-01

    Full Text Available This Special Issue is designed to highlight the latest research and development on new antifungal compounds with mechanisms of action different from the ones of polyenes, azoles, and echinocandins. The papers presented here highlight new pathways and targets that could be exploited for the future development of new antifungal agents to be used alone or in combination with existing antifungals. A computational model for better predicting antifungal drug resistance is also presented.

  4. Selected Essential Oils as Antifungal Agents Against Antibiotic-Resistant Candida spp.: In Vitro Study on Clinical and Food-Borne Isolates.

    Science.gov (United States)

    Rajkowska, Katarzyna; Kunicka-Styczyńska, Alina; Maroszyńska, Marta

    2017-01-01

    Candida spp. cause significant health problems, inducing various types of superficial and deep-seated mycoses in humans. As a result of the increasing antibiotic resistance among pathogenic yeasts, the interest in alternative agents of antifungal activity is growing. This study evaluated the antimicrobial activity of selected essential oils (EOs) against Candida clinical and food-borne strains, including antibiotic-resistant isolates, in relation to yeast cell surface hydrophobicity (CSH). Candida strains showed different range of susceptibility to tea tree, thyme, peppermint, and clove oils, and peppermint oil demonstrated the lowest anticandidal activity with minimal inhibitory concentrations (MICs) of 0.03-8.0% v/v. MIC values for thyme and clove oils ranged from 0.03% to 0.25% v/v, and for tea tree oil-from 0.12% to 2.0% v/v. The exception was Candida tropicalis food-borne strain, the growth of which was inhibited after application of EOs at concentration of 8% v/v. Due to diverse yeast susceptibility to EOs, isolates were divided into five clusters in a principal component analysis model, each containing both clinical and food-borne strains. Hydrophobic properties of yeast were also diversified, and 37% of clinical and 50% of food-borne strains exhibited high hydrophobicity. The study indicates high homology of clinical and food-borne Candida isolates in relation to their susceptibility to anticandidal agents and hydrophobic properties. The susceptibility of yeasts to EOs could be partially related to their CSH. High antifungal activity of examined EOs, also against antibiotic-resistant isolates, indicates their usefulness as agents preventing the development of Candida strains of different origin.

  5. In Vitro Interactions between Non-Steroidal Anti-Inflammatory Drugs and Antifungal Agents against Planktonic and Biofilm Forms of Trichosporon asahii.

    Directory of Open Access Journals (Sweden)

    Suteng Yang

    Full Text Available Increasing drug resistance has brought enormous challenges to the management of Trichosporon spp. infections. The in vitro antifungal activities of non-steroidal anti-inflammatory drugs (NSAIDs against Candida spp. and Cryptococcus spp. were recently discovered. In the present study, the in vitro interactions between three NSAIDs (aspirin, ibuprofen and diclofenac sodium and commonly used antifungal agents (fluconazole, itraconazole, voriconazole, caspofungin and amphotericin B against planktonic and biofilm cells of T. asahii were evaluated using the checkerboard microdilution method. The spectrophotometric method and the XTT reduction assay were used to generate data on biofilm cells. The fractional inhibitory concentration index (FICI and the ΔE model were compared to interpret drug interactions. Using the FICI, the highest percentages of synergistic effects against planktonic cells (86.67% and biofilm cells (73.33% were found for amphotericin B/ibuprofen, and caspofungin/ibuprofen showed appreciable percentages (73.33% for planktonic form and 60.00% for biofilm as well. We did not observe antagonism. The ΔE model gave consistent results with FICI (86.67%. Our findings suggest that amphotericin B/ibuprofen and caspofungin/ibuprofen combinations have potential effects against T. asahii. Further in vivo and animal studies to investigate associated mechanisms need to be conducted.

  6. Structure-activity relationships of 1,3-benzoxazole-4-carbonitriles as novel antifungal agents with potent in vivo efficacy.

    Science.gov (United States)

    Kuroyanagi, Jun-ichi; Kanai, Kazuo; Horiuchi, Takao; Takeshita, Hiroshi; Kobayashi, Shozo; Achiwa, Issei; Yoshida, Kumi; Nakamura, Koichi; Kawakami, Katsuhiro

    2011-01-01

    A series of 1,3-benzoxazole-4-carbonitriles was synthesized and evaluated for its antifungal activity, solubility, and metabolic stability. Among those compounds, 4-cyano-N,N,5-trimethyl-7-[(3S)-3-methyl-3-(methylamino)pyrrolidin-1-yl]-6-phenyl-1,3-benzoxazole-2-carboxamide (16b) exhibited potent in vitro activity against Candida species, higher water solubility, and improved metabolic stability compared to lead compound 1. Compound 16b showed potent in vivo efficacy against mice Candida infection models and good bioavailability in rats.

  7. Amphotericin B-copper(II) complex as a potential agent with higher antifungal activity against Candida albicans.

    Science.gov (United States)

    Chudzik, Barbara; Tracz, Izabela B; Czernel, Grzegorz; Fiołka, Marta J; Borsuk, Grzegorz; Gagoś, Mariusz

    2013-08-16

    Amphotericin B (AmB) is a polyene antibiotic produced by Streptomyces nodosus used for more than 50 years in the treatment of acute systemic fungal infections. It exhibits a broad spectrum of activity against fungal and protozoan pathogens with relatively rare resistance. The aim of this study was to prepare and evaluate the utility of the AmB-Cu(2+) complex as a potential compound with a high fungicidal activity at lower concentrations, compared with conventional AmB. It was hypothesized that insertion of copper ions into fungal cell membranes, together with the AmB-Cu(2+) complex bypassing the natural homeostatic mechanisms of this element, may contribute to the increased fungicidal activity of AmB. The analysis of results indicates the increased antifungal activity of the AmB-Cu(2+) complex against Candida albicans in comparison with the pure AmB and Fungizone. Additionally, it was stated that the increased antifungal activity of the AmB-Cu(2+) complex is not the sum of the toxic effects of AmB and Cu(2+) ions, but is a result of the unique structure of this compound.

  8. In vitro and in vivo antifungal activities of the essential oils of various plants against tomato grey mould disease agent Botrytis cinerea.

    Science.gov (United States)

    Soylu, Emine Mine; Kurt, Sener; Soylu, Soner

    2010-10-15

    The aim of this study was to find an alternative to synthetic fungicides currently used in the control of devastating fungal pathogen Botrytis cinerea, the causal agent of grey mould disease of tomato. Antifungal activities of essential oils obtained from aerial parts of aromatic plants, which belong to the Lamiacea family such as origanum (Origanum syriacum L. var. bevanii), lavender (Lavandula stoechas L. var. stoechas) and rosemary (Rosmarinus officinalis L.), were investigated against B. cinerea. Contact and volatile phase effects of different concentrations of the essential oils were found to inhibit the growth of B. cinerea in a dose-dependent manner. Volatile phase effects of essential oils were consistently found to be more effective on fungal growth than contact phase effect. A volatile vapour of origanum oil at 0.2 μg/ml air was found to completely inhibit the growth of B. cinerea. Complete growth inhibition of pathogen by essential oil of lavender and rosemary was, however, observed at 1.6 μg/ml air concentrations. For the determination of the contact phase effects of the tested essential oils, origanum oil at 12.8 μg/ml was found to inhibit the growth of B. cinerea completely. Essential oils of rosemary and lavender were inhibitory at relatively higher concentrations (25.6 μg/ml). Spore germination and germ tube elongation were also inhibited by the essential oils tested. Light and scanning electron microscopic (SEM) observations revealed that the essential oils cause considerable morphological degenerations of the fungal hyphae such as cytoplasmic coagulation, vacuolations, hyphal shrivelling and protoplast leakage and loss of conidiation. In vivo assays with the origanum essential oil, being the most efficient essential oil, under greenhouse conditions using susceptible tomato plants resulted in good protection against grey mould severity especially as a curative treatment. This study has demonstrated that the essential oils are potential and

  9. Effect of voriconazole and other azole antifungal agents on CYP3A activity and metabolism of tacrolimus in human liver microsomes.

    Science.gov (United States)

    Zhang, Shimin; Pillai, Venkateswaran C; Mada, Sripal Reddy; Strom, Steve; Venkataramanan, Raman

    2012-05-01

    Azole antifungal agents are known to inhibit cytochrome P450 3A (CYP3A) enzymes. Limited information is available regarding the effect of voriconazole on CYP3A activity. We examined the effect of voriconazole on CYP3A activity in human liver microsomes as measured by the formation of 6β-hydroxytestosterone from testosterone. We also evaluated the interaction between voriconazole and tacrolimus, an immunosuppressive drug, using human liver microsomes. The effect of voriconazole on CYP3A activity and tacrolimus metabolism was compared to that of other azole antifungal agents. CYP3A4 activity and the metabolism of tacrolimus were measured in the absence and in the presence of various concentrations of voriconazole (0-1.43 mM), fluconazole (0-1.63 mM), itraconazole (0-14 µM) and ketoconazole (0-0.19 µM). At a concentration of 21.2 ± 15.4 µM and 29.8 ± 12.3 µM, voriconazole inhibited the formation of 6β-hydroxytestosterone from testosterone and the metabolism of tacrolimus by 50%, respectively. The rank order of inhibition of 6β-hydroxytestosterone formation from testosterone and the metabolism of tacrolimus, is ketoconazole > itraconazole > voriconazole > fluconazole. Our observations suggest that voriconazole at clinically relevant concentrations will inhibit the hepatic metabolism of tacrolimus and increase the concentration of tacrolimus more than two-fold. Close monitoring of the blood concentrations and adjustment in the dose of tacrolimus are warranted when transplant patients receiving tacrolimus are treated with voriconazole.

  10. In vivo toxicity of a new antifungal agent 2,4-dithiophenoxy-1-iodo-4-bromo benzene: a follow up on our in vitro study.

    Science.gov (United States)

    Kılıç Süloğlu, Aysun; Koçkaya, Evrim; Karacaoğlu, Elif; Selmanoğlu, Güldeniz; Loğoğlu, Elif

    2015-03-01

    Triazole fungicide fluconazole has become the most widely used antifungal agent in the world, mainly because of its ability to penetrate well into body fluids and tissues. However, it has been reported to interact with many drugs and because of its common use, the risk of resistance to fluconazole increases. This calls for new anti-fungal drugs that would be able to replace it. In 2006, a new thialo benzene derivative - 2,4-dithiophenoxy-1-iodo-4-bromo benzene (C18H12S2IBr) - was synthesised with a carbon backbone similar to fluconazole, and, according to the early in vitro tests, much greater efficiency. Followed an in vitro test of its cytotoxicity, in which the new drug showed promising results as an alternative to fluconazole. The aim of this study was take the next step and test C18H12S2IBr toxicity in vivo. We opted for a four-week test on Wistar rats, in which the new antifungal agent was orally applied at doses two and a half and five times lower than those of fluconazole. There were no changes in daily food and water consumption, but weight gain in female rats and relative organ weights changed in the treated groups, pointing to sex-related differences in drug metabolism and effects. Fluconazole significantly increased leukocytes and lowered neutrophils whereas C18H12S2IBr did not, while other haematological changes in respect to the vehicle control were similar between the treated groups. Differences in cytochrome c in the liver and kidney suggested greater apoptotic effect of the new drug, but interpretation remains inconclusive, considering that other key indicators (biochemistry and histopathology) do not support greater toxicity. Considering that C18H12S2IBr is more active at lower concentrations and has comparable toxic effects to fluconazole in rats, this new compound shows some promise in the treatment of fungal infections. Future, more detailed animal studies are needed, that will include drug interactions and molecular toxicity pathways. If the

  11. Molecular and biochemical approaches for characterization of antifungal trait of a potent biocontrol agent Bacillus subtilis RP24.

    Science.gov (United States)

    Grover, Minakshi; Nain, Lata; Singh, Shashi Bala; Saxena, Anil Kumar

    2010-02-01

    Bacillus subtilis strain RP24, isolated from rhizoplane of field grown pigeon pea, exhibited in vitro antagonism against a wide range of phytopathogenic fungi. An attempt was made to partially purify and characterize the diffusible antifungal metabolite/s produced by the strain RP24 and its negative mutant (NM) in potato dextrose medium. High performance liquid chromatography (HPLC) of partially purified extract of RP24 showed the presence of lipopeptide antibiotic iturin as a major peak that was comparable to that of standard iturin A (5.230 min) from Sigma-Aldrich whereas the corresponding peak was absent in extract of NM. The structure was further confirmed by liquid chromatographic mass spectrometric (LCMS) analysis as iturin A. LCMS analysis also showed the presence of surfactin and fengycin besides iturin A. Amplification of the lpa-14 (encodes the 4'-phosphopantetheinyl transferase required for the maturation of template enzyme of iturin A) and ituD (encodes a putative malonyl coenzyme A transacylase, whose disruption results in a specific deficiency in iturin A production) genes of iturin operon of strain RP24 was carried out and the sequences obtained were compared with the existing database of NCBI. The sequences of lpa-14 and ituD gene of RP24 showed 98% and 97% homology with lpa-14 and ituD genes of B. subtilis in the existing database. The results indicated that strain RP24 harbors iturin operon in its genome and a chemical mutation in this operon might have resulted in loss of antifungal activity in the negative mutant.

  12. Antifungal pharmacokinetics and pharmacodynamics.

    Science.gov (United States)

    Lepak, Alexander J; Andes, David R

    2014-11-10

    Successful treatment of infectious diseases requires choice of the most suitable antimicrobial agent, comprising consideration of drug pharmacokinetics (PK), including penetration into infection site, pathogen susceptibility, optimal route of drug administration, drug dose, frequency of administration, duration of therapy, and drug toxicity. Antimicrobial pharmacokinetic/pharmacodynamic (PK/PD) studies consider these variables and have been useful in drug development, optimizing dosing regimens, determining susceptibility breakpoints, and limiting toxicity of antifungal therapy. Here the concepts of antifungal PK/PD studies are reviewed, with emphasis on methodology and application. The initial sections of this review focus on principles and methodology. Then the pharmacodynamics of each major antifungal drug class (polyenes, flucytosine, azoles, and echinocandins) is discussed. Finally, the review discusses novel areas of pharmacodynamic investigation in the study and application of combination therapy.

  13. AN OVERVIEW ON ANTIFUNGAL THERAPY

    OpenAIRE

    Karki, Nirmal K.; Ahmed, Azhar; Charde, Rita; Charde, Manoj; Gandhare, Bhushan

    2011-01-01

    The number of fungi causing systemic disease is growing and the number of systemic diseases caused by fungi is increasing. The currently available antifungal agents for the treatment of systemic mycoses include polyene antibiotics (Amphotericin B), fluoropyrimidine (Flu cytosine), and Nystatin andazole group of drugs (Ketoconazole, Fluconazole, and Itraconazole). Novel drug delivery systems for antifungal therapy, based on the type of formulation are classified as Liposomes Nanocochleates, Na...

  14. Controlled nail delivery of a novel lipophilic antifungal agent using various modern drug carrier systems as well as in vitro and ex vivo model systems.

    Science.gov (United States)

    Naumann, Sandy; Meyer, Jean-Philippe; Kiesow, Andreas; Mrestani, Yahya; Wohlrab, Johannes; Neubert, Reinhard H H

    2014-04-28

    The penetration behavior into human nails and animal hoof membranes of a novel antifungal agent (EV-086K) for the treatment of onychomycosis was investigated in this study. The new drug provides a high lipophilicity which is adverse for penetration into nails. Therefore, four different formulations were developed, with particular focus on a colloidal carrier system (CCS) due to its penetration enhancing properties. On the one hand, ex vivo penetration experiments on human nails were performed. Afterwards the human nail plates were cut by cryomicrotome in order to quantify the drug concentration in the dorsal, intermediate and ventral nail layer using high-performance liquid chromatography (HPLC) with UV detection. On the other hand, equine and bovine hoof membranes were used to determine the in vitro penetration of the drug into the acceptor compartment of an online diffusion cell coupled with Fourier transform infrared attenuated total reflectance (FTIR-ATR) spectroscopy. In combination, both results should exhibit a correlation between the EV-086K penetration behavior in human nail plates and animal hoof membranes. The investigations showed that the developed CCS could increase drug delivery through the human nail most compared to other formulations (nail lacquer, solution and hydrogel). Using animal hooves in the online diffusion cell, we were able to calculate pharmacokinetic data of the penetration process, especially diffusion and permeability coefficients. Finally, a qualitative correlation between the penetration results of human nails and equine hooves was established.

  15. Treating chromoblastomycosis with systemic antifungals.

    Science.gov (United States)

    Bonifaz, Alexandro; Paredes-Solís, Vanessa; Saúl, Amado

    2004-02-01

    Chromoblastomycosis is a subcutaneous mycosis for which there is no treatment of choice but rather, several treatment options, with low cure rates and many relapses. The choice of treatment should consider several conditions, such as the causal agent (the most common one being Fonsecaea pedrosoi ), extension of the lesions, clinical topography and health status of the patient. Most oral and systemic antifungals have been used; the best results have been obtained with itraconazole and terbinafine at high doses, for a mean of 6 - 12 months. In extensive and refractory cases, chemotherapy with oral antifungals may be associated with thermotherapy (local heat and/or cryosurgery). Limited or early cases may be managed with surgical methods, always associated with oral antifungal agents. It is important to determine the in vitro sensitivity of the major causal agents to the various drugs, by estimating the minimum inhibitory concentration, as well as drug tolerability and drug interactions.

  16. Novel approaches to antifungal prophylaxis.

    Science.gov (United States)

    Ostrosky-Zeichner, Luis

    2004-06-01

    Antifungal prophylaxis represents a significant advance in the management of patients at risk from fungal infections in a variety of settings. Identification of patients at the highest risk and the utilisation of safe and effective drugs maximises the benefits of prophylaxis. Situations in which antifungal prophylaxis has been shown to be useful are bone marrow transplantation, liver and lung transplantation, surgical and neonatal intensive care units, secondary prophylaxis of fungal infections associated with HIV and neutropenia associated haematological malignancies and their treatment. New antifungal agents, such as the echinocandins and the new azoles, are available and have a potential role in antifungal prophylaxis. Future studies should evaluate which strategy is more useful; prophylaxis or pre-emptive therapy.

  17. Fenton reagent and titanium dioxide nanoparticles as antifungal agents to control leaf spot of sugar beet under field conditions

    Directory of Open Access Journals (Sweden)

    Hamza Amany

    2016-07-01

    Full Text Available In this study, foliar sprays of Fenton solutions (Fenton reaction, Fenton-like reaction and Fenton complex, titanium dioxide (TiO2 and the recommended fungicide (chlorothalonil were estimated in the control of sugar beet leaf spot caused by Cercospora beticola under field conditions in two growing seasons. In addition, the impacts of these treatments on some crop characters (leaf dry weight, root fresh weight, soluble solid content, sucrose content and purity of sugar were examined. Biochemical and histological changes in the livers and kidneys of treated rats compared to an untreated control were utilized to assess the toxicity of the examined curative agents. Overall, chlorothalonil and Fenton complex were the most effective treatments for disease suppression in both tested seasons followed by Fenton-like reagent, Fenton’s reagent and TiO2, respectively. Growth and yield characters of treated sugar beet significantly increased in comparison to an untreated control. There were mild or no (biochemical and histological changes in the livers and kidneys of treated rats compared to the control. Fenton solutions and TiO2 may offer a new alternative for leaf spot control in sugar beet.

  18. AN OVERVIEW OF AZOLE ANTIFUNGALS

    Directory of Open Access Journals (Sweden)

    Pratibha Shivaji Gavarkar*, Rahul Shivaji Adnaik, and Shrinivas Krishna Mohite

    2013-11-01

    Full Text Available Fungal infections in critically ill or immunosuppressed patients were increasing in incidence in the human population over the last 1-2 decades. There were few advances in antifungal therapy and, until recently, there were few choices from which to select a treatment for systemic mycoses. However, in the past decade, there have been several developments in this area. Antifungal agents are sufficiently diverse in activity, toxicity, and drug interaction potential. Azoles are synthetic and semi-synthetic compounds. They have a broad spectrum of activity. Triazole antifungals are active to treat an array of fungal pathogens, whereas imidazoles are used almost exclusively in the treatment of superficial mycoses and vaginal candidiasis. Despite the advances, serious fungal infections remain difficult to treat, and resistance to the available drugs is emerging. Use of the currently available azoles in combination with other antifungal agents with different mechanisms of action is likely to provide enhanced efficacy. The present review aims to explore the pharmacology, pharmacokinetics, spectrum of activity, safety, toxicity and potential for drug–drug interactions of the azole antifungal agents.

  19. Antifungal Susceptibility of Candida Biofilms: Unique Efficacy of Amphotericin B Lipid Formulations and Echinocandins

    OpenAIRE

    Kuhn, D M; T. George; CHANDRA, J; P. K. Mukherjee; Ghannoum, M A

    2002-01-01

    Biofilms, likely the predominant mode of device-related microbial infection, exhibit resistance to antimicrobial agents. Evidence suggests that Candida biofilms have dramatically reduced susceptibility to antifungal drugs. We examined antifungal susceptibilities of Candida albicans and Candida parapsilosis biofilms grown on a bioprosthetic model. In addition to conventional agents, we determined if new antifungal agents (triazoles, amphotericin B lipid formulations, and echinocandins) have ac...

  20. Azide-enolate 1,3-dipolar cycloaddition in the synthesis of novel triazole-based miconazole analogues as promising antifungal agents.

    Science.gov (United States)

    González-Calderón, Davir; Mejía-Dionicio, María G; Morales-Reza, Marco A; Ramírez-Villalva, Alejandra; Morales-Rodríguez, Macario; Jauregui-Rodríguez, Bertha; Díaz-Torres, Eduardo; González-Romero, Carlos; Fuentes-Benítes, Aydeé

    2016-04-13

    Seven miconazole analogs involving 1,4,5-tri and 1,5-disubstituted triazole moieties were synthesized by azide-enolate 1,3-dipolar cycloaddition. The antifungal activity of these compounds was evaluated in vitro against four filamentous fungi, including Aspergillus fumigatus, Trichosporon cutaneum, Rhizopus oryzae, and Mucor hiemalis as well as three species of Candida spp. as yeast specimens. These pre-clinical studies suggest that compounds 4b, 4d and 7b can be considered as drug candidates for future complementary biological studies due to their good/excellent antifungal activities.

  1. Appropriate use of antifungal agents

    Directory of Open Access Journals (Sweden)

    Elio Castagnola

    2013-07-01

    Full Text Available As knowledge increases faster and faster, authorizations for drug use often don’t report the most recent evidence. In addition, trials on pediatric populations are rare: as a consequence, a lot of drugs in pediatrics are prescribed out of their indications. This is called off-label use, if the drug isn’t approved for the treatment of a specific disease, or unauthorized use, if, for example, a dose isn’t written in the summary of product characteristics. These uses aren’t illegal, but physicians should take some steps in order to protect their liability: for example, the hospital should write documents based on shared scientific evidence, where the reasons supporting a choice are explained. Informed consent should be obtained, after an exhaustive explanation, from the parents. There is also the exceptional use, i.e. the use in desperate cases, where no other treatments are possible, but, for example, a study in an animal model has resulted in good outcomes. Even in this case, similar measures should be taken by the physician.http://dx.doi.org/10.7175/rhc.v4i1S.861

  2. 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.

  3. ANTIFUNGAL PROPHYLAXIS IN IMMUNOCOMPROMISED PATIENTS

    Directory of Open Access Journals (Sweden)

    Lourdes Vazquez

    2016-09-01

    Full Text Available Invasive fungal infections (IFIs represent significant complications in patients with hematological malignancies. Chemoprevention of IFIs may be important in this setting, but most antifungal drugs have demonstrated poor efficacy, particularly in the prevention of invasive aspergillosis. Antifungal prophylaxis in hematological patients is currently regarded as the gold standard in situations with a high risk of infection, such as acute leukemia, myelodysplastic syndromes, and autologous or allogeneic hematopoietic stem cell transplantation. Over the years, various scientific societies have established a series of recommendations for antifungal prophylaxis based on prospective studies performed with different drugs. However, the prescription of each agent must be personalized, adapting its administration to the characteristics of individual patients and taking into account possible interactions with concomitant medication.

  4. 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

  5. Antifungal testing and high-throughput screening of compound library against Geomyces destructans, the etiologic agent of geomycosis (WNS in bats.

    Directory of Open Access Journals (Sweden)

    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.

  6. Antifungal drug resistance to azoles and polyenes.

    Science.gov (United States)

    Masiá Canuto, Mar; Gutiérrez Rodero, Félix

    2002-09-01

    There is an increased awareness of the morbidity and mortality associated with fungal infections caused by resistant fungi in various groups of patients. Epidemiological studies have identified risk factors associated with antifungal drug resistance. Selection pressure due to the continuous exposure to azoles seems to have an essential role in developing resistance to fluconazole in Candida species. Haematological malignancies, especially acute leukaemia with severe and prolonged neutropenia, seem to be the main risk factors for acquiring deep-seated mycosis caused by resistant filamentous fungi, such us Fusarium species, Scedosporium prolificans, and Aspergillus terreus. The still unacceptably high mortality rate associated with some resistant mycosis indicates that alternatives to existing therapeutic options are needed. Potential measures to overcome antifungal resistance ranges from the development of new drugs with better antifungal activity to improving current therapeutic strategies with the present antifungal agents. Among the new antifungal drugs, inhibitors of beta glucan synthesis and second-generation azole and triazole derivatives have characteristics that render them potentially suitable agents against some resistant fungi. Other strategies including the use of high doses of lipid formulations of amphotericin B, combination therapy, and adjunctive immune therapy with cytokines are under investigation. In addition, antifungal control programmes to prevent extensive and inappropriate use of antifungals may be needed.

  7. The Impact of Antibacterial Agents on Dynamic Antifungal Effects of Fluconazole and Biofilm Penetration%抗菌药物对氟康唑动态抗真菌作用及透过生物膜的影响

    Institute of Scientific and Technical Information of China (English)

    杨久丽; 孙素梅; 刘书源; 孙淑娟

    2014-01-01

    Objective:To determine the combined dynamic antifungal effects of fluconazole and the tested antibacterial agents and evaluate the impact of the tested antibacterial agents on fluconazole penetration through biofilm. Methods:The dynamic killing curve was obtained based on the combined drugs against Candida albicans using viable bacterial counting method. The biofilm penetration test was evaluated by “sandwich” experimental method. Results:Synergistic effects on fluconazole were showed by using the tested antibacterial agents. The penetrating ability of fluconazole through biofilm by the drug resistant Candida albicans varied by different tested antibacterial drugs ,of which minocycline and rifampicin shown strongest impact on it but also on the synergistic effects of dynamic antifungal action. Levofloxacin ,azithromycin and others had a lower impact. Conclusion:The tested antibacterial agents can promote the fluconazole penetration of Candida albican ’ s biofilm and increase fluconazole’s dynamic antifungal effect.%目的:测定试验用抗菌药物与氟康唑联合的动态抗真菌作用,并评价试验用抗菌药物对氟康唑透过生物膜的影响。方法:采用活菌计数法描绘联合用药对白色念珠菌的动态杀菌曲线,以“三明治”透膜实验法评价试验用抗菌药物对氟康唑透过生物膜的影响。结果:试验抗菌药物对氟康唑有不同程度的增效作用,其中米诺环素和利福平对氟康唑透过耐药白色念珠菌生物膜的作用及其对氟康唑动态抗真菌的增效作用最强,氧氟沙星、阿奇霉素等次之。结论:试验用抗菌药物能促进氟康唑透过白色念珠菌生物膜,增强氟康唑的动态抗真菌作用。

  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. 抗真菌药物治疗外阴阴道念珠菌病敏感性的临床研究%Clinical Research of Susceptibility to Antifungal Agents in the Treatment of Vulvovaginal Candidiasis

    Institute of Scientific and Technical Information of China (English)

    郭爱芹

    2012-01-01

    目的 探讨外阴阴道念珠菌病(VVC)的临床特征及抗真菌药物治疗VVC的敏感性.方法 对我院自2008年1月至2011年8月收治的1000例妇科门诊患者的VVC发病情况进行回顾性分析,观察念珠菌对抗真菌药物的敏感性.结果 通过分离1000株念珠菌,白念珠菌为610例(61%),非白念珠菌为390例(39%).白念珠菌及非白念珠菌对氟康唑和伊曲康唑的敏感度比较差异有统计学意义(P<0.05);对酮康唑和两性霉素B的敏感度比较,差异无统计学意义(P>0.05).结论 白念珠菌是VVC的主要致病菌,非白念珠菌的药物敏感性较白念珠菌低,白念珠菌对抗真菌药物的耐药性不常见.%Objective To discuss the clinical features of vulvovaginal candidiasis( VVC )and the susceptibility to antifungal agents in the treatment. Methods Retrospective analysis of VVC incidence of 1000 gynecological outpatients of our hospital from January 2008 to August 2011 was done, Candida albicans sensitivity to antifungal agents was observed. Results Among the 1000 cases,610 patients( 61% )had Candida albicans,and 390 patients( 39% )had non-Candida albicans. Sensitivity of Candida albicans and non-Candida albicans to fluconazole and itraconazole werestatistically significantly different^ P 0. 05 ). Conclusion The main pathogen of VCC is Candida albicans, non-Candida albicans drug sensitivity is lower than Candida albicans, antifungal drug resistance is not common in Candida albicans.

  10. Synthesis of 2-(3-methyl-2-oxoquinoxalin-1(2)-yl)acetamide-based azetidinone derivatives as potent antibacterial and antifungal agents

    Indian Academy of Sciences (India)

    Shiv Kumar; Nitin Kumar; Sushma Drabu; Md Akram Minhaj

    2013-01-01

    Twelve compounds belonging to series N-[3-chloro-2-oxo-4-(substituted)phenylazetidin-1-yl]-2-(3-methyl-2-oxoquinoxalin-1(2)-yl)acetamide (5a-l) were synthesized. These compounds were evaluated for their in vitro antibacterial against E. coli, S. aureus, K. pneumoniae, P. aeruginosa and antifungal activity against C. albicans, A. niger and A. flavus by cup-plate method. Structures of all the newly synthesized compounds were confirmed by their spectral data interpretation. Compound 5g having -dimethylaminophenyl group on 4-position of azetidinone ring attached to N-atom of acetamido group on 1-position of 3-methyl-1-quinoxaline-2-one, was found to be active against all the bacterial and fungal strains under investigation.

  11. 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.

  12. Some O,O',O'',O'''-di/tetra aryldithioimidophonate transition metal complexes derived from catechol and bisphenol-A as antibacterial and antifungal agents.

    Science.gov (United States)

    Kumar, Vikrant; Ahamad, Tansir; Nishat, N

    2009-02-01

    Two new substituted-thioimidophonate derivatives H1L1 (O,O',O'',O'''-diaryldithioimidophonates) and H1L2 (O,O',O'',O'''-tetra aryldithioimidophonates) were synthesized. These thioimidophonates are potential ligands towards transition metal ions. The reaction of M(II) acetates (M(II)=Mn(II), Co(II), Ni(II), Cu(II), and Zn(II)) with H1L1 and H1L2 resulted in the formation of solid complexes with the composition (L1/L2)(2)M(II). These compounds were characterized through elemental analysis, electrical conductance, infrared, electronic spectra, nmr, magnetic susceptibilities etc. Vibrational mode assignments of nu(PN), nu(PS), nu(MS), phenyl and methyl group bands are made. Structural and bonding changes are correlated with these vibrational frequencies. All the compounds were screened for their antibacterial and antifungal properties and have exhibited potential activities with MIC (0.09-1.50 microg/ml).

  13. Green Route for Efficient Synthesis of Novel Amino Acid Schiff Bases as Potent Antibacterial and Antifungal Agents and Evaluation of Cytotoxic Effects

    Directory of Open Access Journals (Sweden)

    Harshita Sachdeva

    2014-01-01

    Full Text Available Green chemical one-pot multicomponent condensation reaction of substituted 1H-indole-2,3-diones (1, various amino acids (2, and thiosemicarbazide (3 is found to be catalyzed by lemon juice as natural acid using water as a green solvent to give the corresponding Schiff bases (4 in good to excellent yields. This method is experimentally simple, clean, high yielding, and green, with reduced reaction times. The product is purified by simple filtration followed by washing with water and drying process. The synthesized compounds are characterized by FT-IR, 13CNMR, and 1HNMR spectroscopy and are screened for their antifungal activity against Aspergillus niger, Penicillium notatum, Fusarium oxysporum, Alternaria brassicicola, Chaetomium orium, and Lycopodium sp. and antibacterial activity against Gram-positive bacteria, Bacillus licheniformis, Staphylococcus aureus, and Micrococcus luteus, and Gram-negative bacteria, Pseudomonas aeruginosa and Escherichia coli. Compounds have also been evaluated for cytotoxic effects against human colon cancer cell line Colo205.

  14. 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.

  15. 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.

  16. 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.

  17. In vitro evaluation of antifungal activity of monolaurin against Candida albicans biofilms

    OpenAIRE

    Seleem, Dalia; Chen, Emily; Benso, Bruna; Pardi, Vanessa; Murata, Ramiro M.

    2016-01-01

    Monolaurin (also known as glycerol monolaurate) is a natural compound found in coconut oil and is known for its protective biological activities as an antimicrobial agent. The nature of oral candidiasis and the increased antifungal resistance demand the search for novel antifungal therapeutic agents. In this study, we examine the antifungal activity of monolaurin against Candida albicans biofilms (strain ATCC:SC5314/MYA2876) in vitro and investigate whether monolaurin can alter gene expressio...

  18. Advances in synthetic approach to and antifungal activity of triazoles

    Directory of Open Access Journals (Sweden)

    Pramod Kumar Sharma

    2011-05-01

    Full Text Available Several five membered ring systems, e.g., triazole, oxadiazole dithiazole and thiadiazole with three heteroatoms at symmetrical or asymmetrical positions have been studied because of their interesting pharmacological properties. In this article our emphasis is on synthetic development and pharmacological activity of the triazole moiety which exhibit a broad spectrum of pharmacological activity such as antifungal, antibacterial, anti-inflammatory and anticancer etc. Triazoles have increased our ability to treat many fungal infections, for example, candidiasis, cryptococcal meningitis, aspergillosis etc. However, mortality due to these infections even with antifungal therapy is still unacceptably high. Therefore, the development of new antifungal agents targeting specific fungal structures or functions is being actively pursued. Rapid developments in molecular mycology have led to a concentrated search for more target antifungals. Although we are entering a new era of antifungal therapy in which we will continue to be challenged by systemic fungal diseases, the options for treatment will have greatly expanded.

  19. 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.

  20. Antifungal activity of traditional medicinal plants from Tamil Nadu, India

    Institute of Scientific and Technical Information of China (English)

    Duraipandiyan V; Ignacimuthu S

    2011-01-01

    Objective:To assess the antifungal activity of hexane, ethyl acetate and methanol extracts of 45 medicinal plants and to determine the minimum inhibitory concentration for each extract against human pathogenic fungi. Methods:A total of 45 medicinal plants were collected from different places of Tamil Nadu and identified. Hexane, ethyl acetate and methanol extracts of 45 medicinal plants were assessed for antifungal susceptibility using broth microdilution method. Two known antifungal agents were used as positive controls. Results: Most of the extracts inhibited more than four fungal strains. From the evaluation we found that ethyl acetate extracts inhibited large number of fungal growth. Hexane extracts also nearly showed the same level of inhibition against fungal growth. Methanol extracts showed the minimum antifungal activity. Among the 45 plants tested, broad spectrum antifungal activity was detected in Albizzia procera (A. procera), Atalantia monophylla, Asclepias curassavica, Azima tetracantha, Cassia fistula (C. fistula), Cinnomomum verum, Costus speciosus (C. speciosus), Nymphaea stellata, Osbeckia chinensis, Piper argyrophyllum, Punica granatum, Tinospora cordifolia and Toddalia asiatica (T. asiatica). Promising antifungal activity was seen in A. procera, C. speciosus, C. fistula and T. asiatica. Conclusions:It can be concluded that the plant species assayed possess antifungal properties. Further phytochemical research is needed to identify the active principles responsible for the antifungal effects of some of these medicinal plants.

  1. Azole Antifungal Agents To Treat the Human Pathogens Acanthamoeba castellanii and Acanthamoeba polyphaga through Inhibition of Sterol 14α-Demethylase (CYP51).

    Science.gov (United States)

    Lamb, David C; Warrilow, Andrew G S; Rolley, Nicola J; Parker, Josie E; Nes, W David; Smith, Stephen N; Kelly, Diane E; Kelly, Steven L

    2015-08-01

    In this study, we investigate the amebicidal activities of the pharmaceutical triazole CYP51 inhibitors fluconazole, itraconazole, and voriconazole against Acanthamoeba castellanii and Acanthamoeba polyphaga and assess their potential as therapeutic agents against Acanthamoeba infections in humans. Amebicidal activities of the triazoles were assessed by in vitro minimum inhibition concentration (MIC) determinations using trophozoites of A. castellanii and A. polyphaga. In addition, triazole effectiveness was assessed by ligand binding studies and inhibition of CYP51 activity of purified A. castellanii CYP51 (AcCYP51) that was heterologously expressed in Escherichia coli. Itraconazole and voriconazole bound tightly to AcCYP51 (dissociation constant [Kd] of 10 and 13 nM), whereas fluconazole bound weakly (Kd of 2,137 nM). Both itraconazole and voriconazole were confirmed to be strong inhibitors of AcCYP51 activity (50% inhibitory concentrations [IC50] of 0.23 and 0.39 μM), whereas inhibition by fluconazole was weak (IC50, 30 μM). However, itraconazole was 8- to 16-fold less effective (MIC, 16 mg/liter) at inhibiting A. polyphaga and A. castellanii cell proliferation than voriconazole (MIC, 1 to 2 mg/liter), while fluconazole did not inhibit Acanthamoeba cell division (MIC, >64 mg/liter) in vitro. Voriconazole was an effective inhibitor of trophozoite proliferation for A. castellanii and A. polyphaga; therefore, it should be evaluated in trials versus itraconazole for controlling Acanthamoeba infections.

  2. Soluble material secreted from Penicillium chrysogenum isolate exhibits antifungal activity against Cryphonectria parasitica- the causative agent of the American Chestnut Blight

    Science.gov (United States)

    Florjanczyk, Aleksandr; Barnes, Rebecca; Kenney, Adam; Horzempa, Joseph

    2016-01-01

    The American chestnut (Castanea dentata) was once the dominant canopy tree along the eastern region of the United States. Cryphonectria parasitica, the causative agent of chestnut blight, was introduced from Asia in the early 1900's, and obliterated the chestnut population within 50 years. We sought to identify environmental microbes capable of producing factors that were fungicidal or inhibited growth of C. parasitica in the hopes developing a biological control of chestnut blight. We isolated a filamentous fungus that significantly inhibited the growth of C. parasitica upon co-cultivation. Extracellular fractions of this fungal isolate prevented C. parasitica growth, indicating that a potential fungicide was produced by the novel isolate. Sequence analysis of 18S rRNA identified this inhibitory fungus as Penicillium chrysogenum. Furthermore, these extracellular fractions were tested as treatments for blight in vivo using chestnut saplings. Scarred saplings that were treated with the P. chrysogenum extracellular fractions healed subjectively better than those without treatment when inoculated with C. parasitica. These data suggest that material secreted by P. chrysogenum could be used as a treatment for the American chestnut blight. This work may assist the reclamation of the American chestnut in association with breeding programs and blight attenuation. Specifically, treatment of small groves under the right conditions may allow them to remain blight free. Future work will explore the mechanism of action and specific target of the extracellular fraction. PMID:27274909

  3. Production and characterization of Iturinic lipopeptides as antifungal agents and biosurfactants produced by a marine pinctada martensii-derived Bacillus mojavensis B0621A.

    Science.gov (United States)

    Ma, Zongwang; Hu, Jiangchun

    2014-06-01

    Bacillus mojavensis B0621A was isolated from a pearl oyster Pinctada martensii collected from South China Sea. While screening for cyclic lipopeptides potentially useful as lead compounds for biological control against soil-bone fungal plant pathogens, three lipopeptides were isolated and purified from the fermentation broth of B. mojavensis B0621A via vacuum flash chromatography coupled with reversed-phase high performance liquid chromatography (RP-HPLC). The structural characterization and identification of these cyclic lipopeptides were performed by tandem mass spectrometry (MS/MS) combined with gas chromatography-mass spectrometry (GC-MS) analysis as well as chemical degradation. These lipopeptides were finally characterized as homologues of mojavensins, which contained identical amino acids back bones of asparagine1, tyrosine2, asparagine3, glutamine4, proline5, asparagine6, and asparagine7 and differed from each other by their saturated β-amino fatty acid chain residues, namely, iso-C14 mojavensin, iso-C16 mojavensin, and anteiso-C17 mojavensin, respectively. All lipopeptide isomers, especially iso-C16 mojavensin and anteiso-C17 mojavensin, displayed moderate antagonism and dose-dependent activity against several formae speciales of Fusarium oxysporum and presented surface tension activities. These properties demonstrated that the lipopeptides produced by B. mojavensis B0621A may be useful as biological control agent to fungal plant pathogens.

  4. 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.

  5. Can agricultural fungicides accelerate the discovery of human antifungal drugs?

    Science.gov (United States)

    Myung, Kyung; Klittich, Carla J R

    2015-01-01

    Twelve drugs from four chemical classes are currently available for treatment of systemic fungal infections in humans. By contrast, more than 100 structurally distinct compounds from over 30 chemical classes have been developed as agricultural fungicides, and these fungicides target many modes of action not represented among human antifungal drugs. In this article we introduce the diverse aspects of agricultural fungicides and compare them with human antifungal drugs. We propose that the information gained from the development of agricultural fungicides can be applied to the discovery of new mechanisms of action and new antifungal agents for the management of human fungal infections.

  6. 7-Chloroquinolin-4-yl Arylhydrazone Derivatives: Synthesis and Antifungal Activity

    Directory of Open Access Journals (Sweden)

    Auri R. Duval

    2011-01-01

    Full Text Available Fifteen 7-chloro-4-arylhydrazonequinolines have been evaluated for their in vitro antifungal activity against eight oral fungi: Candida albicans, C. parapsilosis, C. lipolytica, C. tropicalis, C. famata, C. glabrata, Rhodutorula mucilaginosa, and R. glutinis. Several compounds exhibited minimum inhibitory concentration (MIC and minimum fungicidal concentration (MFC activities comparable with the first-line drug fluconazole. These results could be considered as an important starting point for the rational design of new antifungal agents.

  7. Antifungal Drug Resistance - Concerns for Veterinarians

    Directory of Open Access Journals (Sweden)

    Bharat B. Bhanderi

    2009-10-01

    Full Text Available In the 1990s, there were increased incidences of fungal infectious diseases in human population which might be due to increase in immunosuppressive diseases. But the major concern was increase in prevalence of resistance to antifungal drugs which were reported both in the fungal isolates of human beings and that of animal origin. In both animals and human beings, resistance to antimicrobial agents has important implications for morbidity, mortality and health care costs, because resistant strains are responsible for bulk of infection in animals and human beings, and large number of antimicrobial classes offers more diverse range of resistance mechanisms to study and resistance determinants move into standard well-characterized strains that facilitates the detailed study of molecular mechanisms of resistance in microorganisms. Studies on resistance to antifungal agents has been lagging behind that of antibacterial resistance for several reasons, the foremost reason might be fungal agents were not recognized as important animal and human pathogens, until relatively in recent past. But the initial studies of antifungal drug resistance in the early 1980s, have accumulated a wealth of knowledge concerning the clinical, biochemical, and genetic aspects of this phenomenon. Presently, exploration of the molecular aspects for antifungal drug resistance has been undertaken. Recently, the focus was on several points like developing a more detailed understanding of the mechanisms of antimicrobial resistance, improved methods to detect resistance when it occurs, methods to prevent the emergence and spread of resistance and new antimicrobial options for the treatment of infections caused by resistant organisms. [Vet. World 2009; 2(5.000: 204-207

  8. Design, synthesis, and biological evaluation of 1,2,3-trisubstituted-1,4-dihydrobenzo[g]quinoxaline-5,10-diones and related compounds as antifungal and antibacterial agents.

    Science.gov (United States)

    Tandon, Vishnu K; Yadav, Dharmendra B; Maurya, Hardesh K; Chaturvedi, Ashok K; Shukla, Praveen K

    2006-09-01

    A series of (S)-N-(3-chloro-1,4-naphthoquinon-2-yl)-alpha-amino acid ethyl esters 3 and 1,2,3-trisubstituted-1,4-dihydrobenzo[g]quinoxaline-5,10-diones 6-23 were synthesized and evaluated for antifungal and antibacterial activities. The structure-activity relationship of these compounds was studied and the results show that the compounds 3a and 3b exhibited in vitro antifungal activity against Candida albicans, Cryptococcus neoformans, and Sporothrix schenckii whereas compounds 12 and 22 showed in vitro antibacterial activity against Klebsiella pneumoniae and Escherichia coli.

  9. Traditional Chinese Medicine Combined with Antifungal Agents for Treating Fungal Keratitis in 53 Cases%中药联合抗真菌药物治疗真菌性角膜炎53例

    Institute of Scientific and Technical Information of China (English)

    邓显峰

    2015-01-01

    Objective To observe the clinical effect of traditional Chinese medicine combined with antifungal agents in treating fungal keratitis. Methods Totally 106 patients with fungal keratitis in the hospital were selected and divided into the experimental group and the control group,53 cases each. The control group adopted 5% Natamycin Eye Drops and 0. 2% Fluconazole Eye Drops for treatment, while on this basis the experimental group adopted oral Yupingfeng Powder and Yinhuatufuling Decoction,and traditional Chinese medicine fumigation eye treatment. The curative effect,vision,adverse reactions and cure time after 15 d treatment were evaluat-ed. Results The experimental group was significantly better than the control group in the curative effect,visual acuity and cure time ( P ﹤ 0. 05);the adverse reactions had no statistically significant difference between the two groups. Conclusion The integrated tradi-tional Chinese and Western medicine for treating fungal keratitis can obtain better curative effect,shorten the cure time and deserves to be promoted in clinic.%目的:观察中药联合抗真菌药物治疗真菌性角膜炎的临床疗效。方法选取医院诊治的真菌性角膜炎患者106例,按就诊先后顺序将其分为试验组和对照组,各53例。对照组患者采用5%那他霉素滴眼液和0.2%氟康唑滴眼液滴眼治疗,试验组患者在对照组基础上采用玉屏风散合银花土茯苓汤内服和中药熏蒸患眼治疗。治疗15 d后进行疗效、视力、不良反应、痊愈时间等评估。结果试验组的疗效、视力和痊愈时间均明显优于对照组( P﹤0.05),两组患者不良反应发生情况无显著性差异。结论中西医结合治疗真菌性角膜炎可取得较好疗效,能缩短痊愈时间,值得临床推广。

  10. 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.

  11. Antifungal effect of (+)-pinoresinol isolated from Sambucus williamsii.

    Science.gov (United States)

    Hwang, Bomi; Lee, Juneyoung; Liu, Qing-He; Woo, Eun-Rhan; Lee, Dong Gun

    2010-05-14

    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.

  12. Antifungal activity of diethyldithiocarbamate.

    Science.gov (United States)

    Allerberger, F; Reisinger, E C; Söldner, B; Dierich, M P

    1989-10-01

    Sodium diethyldithiocarbamate (DTC) was evaluated for its ability to combat four different species of fungi in vitro. Using a microtiter-broth-dilution method we were able to demonstrate an antifungal activity against Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus and Mucor mucedo in doses achievable by intravenous administration in man.

  13. Antifungal susceptibilities of bloodstream isolates of Candida species from nine hospitals in Korea: application of new antifungal breakpoints and relationship to antifungal usage.

    Directory of Open Access Journals (Sweden)

    Eun Jeong Won

    Full Text Available We applied the new clinical breakpoints (CBPs of the Clinical and Laboratory Standards Institute (CLSI to a multicenter study to determine the antifungal susceptibility of bloodstream infection (BSI isolates of Candida species in Korea, and determined the relationship between the frequency of antifungal-resistant Candida BSI isolates and antifungal use at hospitals. Four hundred and fifty BSI isolates of Candida species were collected over a 1-year period in 2011 from nine hospitals. The susceptibilities of the isolates to four antifungal agents were determined using the CLSI M27 broth microdilution method. By applying the species-specific CBPs, non-susceptibility to fluconazole was found in 16.4% (70/428 of isolates, comprising 2.6% resistant and 13.8% susceptible-dose dependent isolates. However, non-susceptibility to voriconazole, caspofungin, or micafungin was found in 0% (0/370, 0% (0/437, or 0.5% (2/437 of the Candida BSI isolates, respectively. Of the 450 isolates, 72 (16.0% showed decreased susceptibility to fluconazole [minimum inhibitory concentration (MIC ≥4 μg/ml]. The total usage of systemic antifungals varied considerably among the hospitals, ranging from 190.0 to 7.7 defined daily dose per 1,000 patient days, and fluconazole was the most commonly prescribed agent (46.3%. By Spearman's correlation analysis, fluconazole usage did not show a significant correlation with the percentage of fluconazole resistant isolates at hospitals. However, fluconazole usage was significantly correlated with the percentage of fluconazole non-susceptible isolates (r = 0.733; P = 0.025 or the percentage of isolates with decreased susceptibility to fluconazole (MIC ≥4 μg/ml (r = 0.700; P = 0.036 at hospitals. Our work represents the first South Korean multicenter study demonstrating an association between antifungal use and antifungal resistance among BSI isolates of Candida at hospitals using the new CBPs of the CLSI.

  14. In vitro antifungal activity and mechanism of essential oil from fennel (Foeniculum vulgare L.) on dermatophyte species.

    Science.gov (United States)

    Zeng, Hong; Chen, Xinping; Liang, Jingnan

    2015-01-01

    Fennel seed essential oil (FSEO) is a plant-derived natural therapeutic against dermatophytes. In this study, the antifungal effects of FSEO were investigated from varied aspects, such as MIC and minimum fungicidal concentration, mycelia growth, spore germination and biomass. The results indicated that FSEO had potent antifungal activities on Trichophyton rubrum ATCC 40051, Trichophyton tonsurans 10-0400, Microsporum gypseum 44693-1 and Trichophyton mentagrophytes 10-0060, which is better than the commonly used antifungal agents fluconazole and amphotericin B. Flow cytometry and transmission electron microscopy experiments suggested that the antifungal mechanism of FSEO was to damage the plasma membrane and intracellular organelles. Further study revealed that it could also inhibit the mitochondrial enzyme activities, such as succinate dehydrogenase, malate dehydrogenase and ATPase. With better antifungal activity than the commonly used antifungal agents and less possibility of inducing drug resistance, FSEO could be used as a potential antidermatophytic agent.

  15. 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

  16. New targets and delivery systems for antifungal therapy.

    Science.gov (United States)

    Walsh, T J; Viviani, M A; Arathoon, E; Chiou, C; Ghannoum, M; Groll, A H; Odds, F C

    2000-01-01

    Development of new approaches for treatment of invasive fungal infections encompasses new delivery systems for approved and investigational compounds, as well as exploiting the cell membrane, cell wall and virulence factors as putative antifungal targets. Novel delivery systems consisting of cyclodextrins, cochleates, nanoparticles/nanospheres and long circulating ('stealth') liposomes, substantially modulate the pharmacokinetics of existing compounds, and may also be useful to enhance the delivery of antifungal agents to sites of infection. Further insights into the structure-activity relationship of the antifungal triazoles that target the biosynthesis of ergosterol in the fungal cell membrane have led to the development of highly potent broad spectrum agents, including posaconazole, ravuconazole and voriconazole. Similarly, a novel generation of cell-wall active semisynthetic echinocandin 1,3 beta-glucan inhibitors (caspofungin, FK463, and VER-002) has entered clinical development. These agents have potent and broad-spectrum activity against Candida spp, and potentially useful activity against Aspergillus spp. and Pneumocystis carinii. The ongoing convergence of the fields of molecular pathogenesis, antifungal pharmacology and vaccine development will afford the opportunity to develop novel targets to complement the existing antifungal armamentarium.

  17. 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

  18. Susceptibility to heat and antifungal agents of Cryptococcus neoformans var. neoformans (serotype D isolated from Eucalyptus spp in Rio Grande do Sul, Brazil Susceptibilidade de Cryptococcus neoformans var. neoformans (sorotipo D isolados de Eucalyptus spp., no Rio Grande do Sul (Brasil, frente ao calor e a agentes antifúngicos

    Directory of Open Access Journals (Sweden)

    Jorge A Horta

    2005-03-01

    Full Text Available In this work we studied the susceptibility to heat and antifungal agents of the first strains of environmental Cryptococcus neoformans var neoformans (serotype D isolated in the state of Rio Grande do Sul, Brazil. In order to achieve a rigorous analysis, we employed the methodology recommended by NCCLS, Yeast Nitrogen Base (YNB proposed by Ghannoum et al (YNB-1, Antibiotic medium 3 (AM3 indicated by others, YNB adjusted to the NCCLS methodology (YNB-2 and Etest. Our results indicate that all strains were susceptible to amphotericin B (0.0625-0.5 µg/mL, fluconazole (0.125-8.0 µg/mL, itraconazole (0.031-0.25 µg/mL and flucytosine (0.125-4.0 µg/mL. The C. neoformans serotype D strains were more susceptible to heat (47ºC/30 min than C. neoformans serotype A.Este estudo foi realizado com os primeiros isolados ambientais de C. neoformans sorotipo D, obtidos no Rio Grande do Sul. Objetivando-se avaliar a susceptibilidade a agentes antifúngicos de forma mais rigorosa, utilizou-se a técnica de referência proposta pelo NCCLS, Caldo Yeast Nitrogen Base (YNB proposto por Ghannoum et al., Antibiotic medium 3, caldo YNB adequado à metodologia do NCCLS e o E-test. Os resultados indicaram que todos os isolados foram sensíveis à anfotericina B (0,0625-0,5 µg/mL, fluconazol (0,125-4,0 µg/mL, itraconazol (0,031-0,25 µg/ml e fluorocitosina (0,125-4,0 µg/mL através das técnicas empregadas. Nos testes de termotolerância (47ºC/30 min, observou-se que as culturas de C. neoformans sorotipo D são mais sensíveis do que as de C. neoformans sorotipo A.

  19. In Vitro Screening of 10 Edible Thai Plants for Potential Antifungal Properties

    Directory of Open Access Journals (Sweden)

    Supattra Suwanmanee

    2014-01-01

    Full Text Available Growing rates of fungal infections and increasing resistance against standard antifungal drugs can cause serious health problems. There is, therefore, increasing interest in the potential use of medicinal plants as novel antifungal agents. This study investigates the antifungal properties of crude plant extracts from ten medicinal plant species. Crude samples were extracted using the hot water extraction process. The minimum inhibitory concentrations (MIC and diameter zone of inhibition were determined in each extract against ten fungal strains, and fluconazole was used as a positive control. The cytotoxicity of crude extracts on in vitro human skin fibroblast (HSF cell models was determined by MTT assay. Of the ten crude extracts, Psidium guajava L. exhibited the highest antifungal activity, diameter zone of inhibition, and percentage HSF cell viability. Although all extracts exhibited antifungal activity, Psidium guajava L. had the greatest potential for developing antifungal treatments.

  20. Antifungal Therapy: New Advances in the Understanding and Treatment of Mycosis

    Science.gov (United States)

    Scorzoni, Liliana; de Paula e Silva, Ana C. A.; Marcos, Caroline M.; Assato, Patrícia A.; de Melo, Wanessa C. M. A.; de Oliveira, Haroldo C.; Costa-Orlandi, Caroline B.; Mendes-Giannini, Maria J. S.; Fusco-Almeida, Ana M.

    2017-01-01

    The high rates of morbidity and mortality caused by fungal infections are associated with the current limited antifungal arsenal and the high toxicity of the compounds. Additionally, identifying novel drug targets is challenging because there are many similarities between fungal and human cells. The most common antifungal targets include fungal RNA synthesis and cell wall and membrane components, though new antifungal targets are being investigated. Nonetheless, fungi have developed resistance mechanisms, such as overexpression of efflux pump proteins and biofilm formation, emphasizing the importance of understanding these mechanisms. To address these problems, different approaches to preventing and treating fungal diseases are described in this review, with a focus on the resistance mechanisms of fungi, with the goal of developing efficient strategies to overcoming and preventing resistance as well as new advances in antifungal therapy. Due to the limited antifungal arsenal, researchers have sought to improve treatment via different approaches, and the synergistic effect obtained by the combination of antifungals contributes to reducing toxicity and could be an alternative for treatment. Another important issue is the development of new formulations for antifungal agents, and interest in nanoparticles as new types of carriers of antifungal drugs has increased. In addition, modifications to the chemical structures of traditional antifungals have improved their activity and pharmacokinetic parameters. Moreover, a different approach to preventing and treating fungal diseases is immunotherapy, which involves different mechanisms, such as vaccines, activation of the immune response and inducing the production of host antimicrobial molecules. Finally, the use of a mini-host has been encouraging for in vivo testing because these animal models demonstrate a good correlation with the mammalian model; they also increase the speediness of as well as facilitate the

  1. Antifungal Therapy: New Advances in the Understanding and Treatment of Mycosis.

    Science.gov (United States)

    Scorzoni, Liliana; de Paula E Silva, Ana C A; Marcos, Caroline M; Assato, Patrícia A; de Melo, Wanessa C M A; de Oliveira, Haroldo C; Costa-Orlandi, Caroline B; Mendes-Giannini, Maria J S; Fusco-Almeida, Ana M

    2017-01-01

    The high rates of morbidity and mortality caused by fungal infections are associated with the current limited antifungal arsenal and the high toxicity of the compounds. Additionally, identifying novel drug targets is challenging because there are many similarities between fungal and human cells. The most common antifungal targets include fungal RNA synthesis and cell wall and membrane components, though new antifungal targets are being investigated. Nonetheless, fungi have developed resistance mechanisms, such as overexpression of efflux pump proteins and biofilm formation, emphasizing the importance of understanding these mechanisms. To address these problems, different approaches to preventing and treating fungal diseases are described in this review, with a focus on the resistance mechanisms of fungi, with the goal of developing efficient strategies to overcoming and preventing resistance as well as new advances in antifungal therapy. Due to the limited antifungal arsenal, researchers have sought to improve treatment via different approaches, and the synergistic effect obtained by the combination of antifungals contributes to reducing toxicity and could be an alternative for treatment. Another important issue is the development of new formulations for antifungal agents, and interest in nanoparticles as new types of carriers of antifungal drugs has increased. In addition, modifications to the chemical structures of traditional antifungals have improved their activity and pharmacokinetic parameters. Moreover, a different approach to preventing and treating fungal diseases is immunotherapy, which involves different mechanisms, such as vaccines, activation of the immune response and inducing the production of host antimicrobial molecules. Finally, the use of a mini-host has been encouraging for in vivo testing because these animal models demonstrate a good correlation with the mammalian model; they also increase the speediness of as well as facilitate the

  2. 我院2009-2011年老年真菌感染菌种分布及其对抗真菌药敏感性分析%Analysis of Species Distribution and Drug Susceptibility to Antifungal Agents in the Aged with Fungal Infection of Our Hospital during 2009-2011

    Institute of Scientific and Technical Information of China (English)

    张慧儿; 裘莉佩

    2013-01-01

    目的:探讨临床老年患者标本中所分离的假丝酵母菌属的菌种分布及其对临床常用抗真菌药的敏感性,为老年人使用抗真菌药提供参考.方法:对我院2009-2011年从老年体内分离的213例假丝酵母菌进行回顾性分析,分析其菌种分布情况以及对5种抗真菌药的敏感性.结果:在213株假丝酵母菌中,白假丝酵母菌占42.3%(90/213),非白假丝酵母菌占57.7% (123/213);5-氟胞嘧啶、两性霉素B、氟康唑、伊曲康唑和伏立康唑的总敏感率分别为87.8%、100%、93.2%、85.9%和95.9%;90株白假丝酵母菌对上述5种抗真菌药的敏感率分别为93.3%、100%、95.4%、92.2%和96.3%,123株非白假丝酵母菌分别为83.7%、100%、91.6%、81.3%和95.6%.结论:在老年感染假丝酵母菌中最常见的菌种仍是白假丝酵母菌,但其比例较已报道的非老年感染者比例有所下降;白假丝酵母菌对常用抗真菌药仍有较高的敏感性,非白假丝酵母菌的耐药性则高于白假丝酵母菌.%OBJECTIVE: To discuss the species distribution and drug susceptibility to antifungal agent of isolated Candida, and to provide reference for the use of antifungal agent in the aged. METHODS: A total of 213 isolates were collected from our hospital during 2009 — 2011 were analyzed statistically, and the species distribution of Candida and drug resistance to 5 commonly used antifungal agents were analyzed. RESULTS: Among 213 Candida, Candida albicans accounted for 42.3% (90/213) and non-Candida albicans accounted for 57.7% (123/213). The overall percentage of strains susceptible to 5-flucytosine, amphotericin B, flucytosine, itraconazole and voriconazole were 87.8% , 100% , 93.2% , 85.9% and 95.9% , respectively. About 93.3% , 100%, 95.4% , 92.2% and 96.3% of 90 strains of Candida albicans were susceptible to these 5 antifungal agents. The susceptibility rates of 123 non-Candida albicans isolates were 83.7%, 100

  3. IPC synthase as a useful target for antifungal drugs.

    Science.gov (United States)

    Sugimoto, Yuichi; Sakoh, Hiroki; Yamada, Koji

    2004-12-01

    Inositol phosphorylceramide (IPC) synthase is a common and essential enzyme in fungi and plants, which catalyzes the transfer of phosphoinositol to the C-1 hydroxy of ceramide to produce IPC. This reaction is a key step in fungal sphingolipid biosynthesis, therefore the enzyme is a potential target for the development of nontoxic therapeutic antifungal agents. Natural products with a desired biological activity, aureobasidin A (AbA), khafrefungin, and galbonolide A, have been reported. AbA, a cyclic depsipeptide containing 8 amino acids and a hydroxyl acid, is a broad spectrum antifungal with strong activity against many pathogenic fungi such as Candida spp., Cryptococcus neoformans, and some Aspergillus spp. Khafrefungin, an aldonic acid ester with a C22 long alkyl chain, has antifungal activity against C. albicans, Cr. Neoformans, and Saccharomyces cerevisiae. Galbonolide A is a 14-membered macrolide with fungicidal activity against clinically important strains, and is especially potent against Cr. neoformans. These classes of natural products are potent and specific antifungal agents. We review current progress in the development of IPC synthase inhibitors with antifungal activities, and present structure-activity relationships (SAR), physicochemical and structural properties, and synthetic methodology for chemical modification.

  4. Chloroquine sensitizes biofilms of Candida albicans to antifungal azoles

    Directory of Open Access Journals (Sweden)

    Ravikumar Bapurao Shinde

    2013-08-01

    Full Text Available Biofilms formed by Candida albicans, a human pathogen, are known to be resistant to different antifungal agents. Novel strategies to combat the biofilm associated Candida infections like multiple drug therapy are being explored. In this study, potential of chloroquine to be a partner drug in combination with four antifungal agents, namely fluconazole, voriconazole, amphotericin B, and caspofungin, was explored against biofilms of C. albicans. Activity of various concentrations of chloroquine in combination with a particular antifungal drug was analyzed in a checkerboard format. Growth of biofilm in presence of drugs was analyzed by XTT-assay, in terms of relative metabolic activity compared to that of drug free control. Results obtained by XTT-metabolic assay were confirmed by scanning electron microscopy. The interactions between chloroquine and four antifungal drugs were determined by calculating fractional inhibitory concentration indices. Azole resistance in biofilms was reverted significantly (p < 0.05 in presence of 250 µg/mL of chloroquine, which resulted in inhibition of biofilms at very low concentrations of antifungal drugs. No significant alteration in the sensitivity of biofilms to caspofungin and amphotericin B was evident in combination with chloroquine. This study for the first time indicates that chloroquine potentiates anti-biofilm activity of fluconazole and voriconazole.

  5. New small-size peptides possessing antifungal activity

    NARCIS (Netherlands)

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

    2010-01-01

    The synthesis, in vitro evaluation, and conformational study of a new series of small-size peptides acting as antifungal agents are reported. In a first step of our study we performed a conformational analysis using Molecular Mechanics calculations. The electronic study was carried out using Molecul

  6. 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.

  7. Antifungal ellagitannin isolated from Euphorbia antisyphilitica Zucc

    Institute of Scientific and Technical Information of China (English)

    Juan; Ascacio-Valdés; Edgardo; Burboa; Antonio; F; Aguilera-Carbo; Mario; Aparicio; Ramón; Pérez-Schmidt; Raúl; Rodríguez; Cristóbal; N; Aguilar

    2013-01-01

    Objective:To study antifungal activity of a new ellagitannin isolated from the plant residues of Euphorbia antisyphilitica(E.antisyphilitica)Zucc in the wax extraction process.Methods:An extract was prepared from dehydrated and pulverized residues and fractionated by liquid chromatography on Amberilte XAD-16,until obtained an ellagitannin-rich ethanolic fraction which was treated by rotaevaporation to recover the ellagitannin as fine powder.An aqueous solution was prepared and treated through ionic exchange liquid chromatography(Q XL)and gel permeation chromatography(G 25).The ellagitannin-rich fraction was thermogravimetrically evaluated(TGA and DTA)to test the thermo-stability of ellagic acid(monomeric unit).Then ellagitannin powder was analyzed by infrared spectrospcopy to determinate the functional groups and.also mass spectroscopy was used to determine the molecular ion.Results:The principal functional groups of ellagitannin were determined,the molecular weight was 860.7 g/mol;and an effective antifungal activity against phytopathogenic fungi was demonstrated.Conclusions:It can be concluded that the new ellagitannin(860.7 g/mol)isolated from E.antisyphilitica Zucc is an effective antifungal agent against Alternaria alternata,Fusarium oxyzporum,Colletotrichum gloeosporoides and Rhizoctnia solani.

  8. Antifungal ellagitannin isolated from Euphorbia antisyphilitica Zucc

    Institute of Scientific and Technical Information of China (English)

    Juan Ascacio-Valds; Edgardo Burboa; Antonio F Aguilera-Carbo; Mario Aparicio; Ramn Prez-Schmidt; Ral Rodrguez; Cristbal N Aguilar

    2013-01-01

    Objective: To study antifungal activity of a new ellagitannin isolated from the plant residues of Euphorbia antisyphilitica (E. antisyphilitica) Zucc in the wax extraction process. Methods:An extract was prepared from dehydrated and pulverized residues and fractionated by liquid chromatography on Amberilte XAD-16, until obtained an ellagitannin-rich ethanolic fraction which was treated by rotaevaporation to recover the ellagitannin as fine powder. An aqueous solution was prepared and treated through ionic exchange liquid chromatography (Q XL) and gel permeation chromatography (G 25). The ellagitannin-rich fraction was thermogravimetrically evaluated (TGA and DTA) to test the thermo-stability of ellagic acid (monomeric unit). Then ellagitannin powder was analyzed by infrared spectrospcopy to determinate the functional groups and, also mass spectroscopy was used to determine the molecular ion. Results: The principal functional groups of ellagitannin were determined, the molecular weight was 860.7 g/mol; and an effective antifungal activity against phytopathogenic fungi was demonstrated. Conclusions: It can be concluded that the new ellagitannin (860.7 g/mol) isolated from E. antisyphilitica Zucc is an effective antifungal agent against Alternaria alternata, Fusarium oxyzporum, Colletotrichum gloeosporoides and Rhizoctnia solani.

  9. Antifungal adjuvants: Preserving and extending the antifungal arsenal.

    Science.gov (United States)

    Butts, Arielle; Palmer, Glen E; Rogers, P David

    2017-02-17

    As the rates of systemic fungal infections continue to rise and antifungal drug resistance becomes more prevalent, there is an urgent need for new therapeutic options. This issue is exacerbated by the limited number of systemic antifungal drug classes. However, the discovery, development, and approval of novel antifungals is an extensive process that often takes decades. For this reason, there is growing interest and research into the possibility of combining existing therapies with various adjuvants that either enhance activity or overcome existing mechanisms of resistance. Reports of antifungal adjuvants range from plant extracts to repurposed compounds, to synthetic peptides. This approach would potentially prolong the utility of currently approved antifungals and mitigate the ongoing development of resistance.

  10. Progress in antibacterial and antifungal chemotherapy.

    Science.gov (United States)

    Fromtling, R A

    2000-08-01

    The European Society of Clinical Microbiology and Infectious Diseases sponsored the 10th European Congress on Clinical Microbiology and Infectious Diseases in Stockholm, Sweden, May 28-31, 2000. At the ECMID, well-attended sessions were held which focused on the pathogenesis and therapy of viral, bacterial and fungal diseases. This report focuses on new information on resistance to antibacterial agents, including data from recent surveillance studies, and the in vitro and investigational clinical activity of new antibacterial (moxifloxacin, telithromycin) and antifungal (fluconazole, itraconazole, voriconazole, amphotericin B, liposomal formulations of amphotericin B, terbinafine and the candins) drugs.

  11. Chemical modification of antifungal polyene macrolide antibiotics

    Science.gov (United States)

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

    2011-02-01

    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.

  12. Chemical modification of antifungal polyene macrolide antibiotics

    Energy Technology Data Exchange (ETDEWEB)

    Solovieva, S E; Olsufyeva, E N; Preobrazhenskaya, M N [G.F.Gause Institute of New Antibiotics, Russian Academy of Medical Sciences (Russian Federation)

    2011-02-28

    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.

  13. Antifungal therapy in European hospitals

    DEFF Research Database (Denmark)

    Zarb, P; Amadeo, B; Muller, A;

    2012-01-01

    respiratory (19.2%) and gastrointestinal (18.8%). The most used antifungal was fluconazole (60.5%) followed by caspofungin (10.5%). Antifungal-antibacterial combinations were frequently used (77.5%). The predominance of fluconazole use in participating hospitals could result in an increase in prevalence...

  14. Antifungal susceptibility profile of cryptic species of Aspergillus.

    Science.gov (United States)

    Alastruey-Izquierdo, Ana; Alcazar-Fuoli, Laura; Cuenca-Estrella, Manuel

    2014-12-01

    The use of molecular tools has led to the description of new cryptic species among different Aspergillus species complexes. Their frequency in the clinical setting has been reported to be between 10 and 15%. The susceptibility to azoles and amphotericin B of many of these species is low, and some of them, such as Aspergillus calidoustus or Aspergillus lentulus, are considered multi-resistant. The changing epidemiology, the frequency of cryptic species, and the different susceptibility profiles make antifungal susceptibility testing an important tool to identify the optimal antifungal agent to treat the infections caused by these species.

  15. 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-ylpropylidene]-hydroxylamine: A New Potential Antifungal Agent Precursor

    Directory of Open Access Journals (Sweden)

    Reem I. Al-Wabli

    2017-02-01

    Full Text Available 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, C13H13N3O3·C3H8O, crystallizes in the monoclinic space group P21with a = 9.0963(3 Å, b = 14.7244(6 Å, c = 10.7035(4 Å, β = 94.298 (3°, V = 1429.57(9 Å3, 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.

  16. Fungus-Elicited Metabolites from Plants as an Enriched Source for New Leishmanicidal Agents: Antifungal Phenyl-Phenalenone Phytoalexins from the Banana Plant (Musa acuminata) Target Mitochondria of Leishmania donovani Promastigotes

    Science.gov (United States)

    Luque-Ortega, Juan Román; Martínez, Silvia; Saugar, José María; Izquierdo, Laura R.; Abad, Teresa; Luis, Javier G.; Piñero, José; Valladares, Basilio; Rivas, Luis

    2004-01-01

    Two antifungal phenyl-phenalenone phytoalexins isolated from the banana plant (Musa acuminata) elicited with the fungus Fusarium oxysporum, together with a methoxy derivative of one of them and two epoxide precursors of their chemical synthesis, were tested for leishmanicidal activity on Leishmania donovani promastigotes and L. infantum amastigotes. Drugs inhibited proliferation of both forms of the parasite with a 50% lethal concentration range between 10.3 and 68.7 μg/ml. Their lethal mechanism was found linked to the respiratory chain by a systematic approach, including electron microscopy, measurement of the oxygen consumption rate on digitonin-permeabilized promastigotes, and enzymatic assays on a mitochondrial enriched fraction. Whereas the whole set of compounds inhibited the activity of fumarate reductase in the mitochondrial fraction (50% effective concentration [EC50] between 33.3 and 78.8 μg/ml) and on purified enzyme (EC50 = 53.3 to 115 μg/ml), inhibition for succinate dehydrogenase was only observed for the two phytoalexins with the highest leishmanicidal activity: anigorufone and its natural analogue 2-methoxy-9-phenyl-phenalen-1-one (EC50 = 33.5 and 59.6 μg/ml, respectively). These results provided a new structural motif, phenyl-phenalenone, as a new lead for leishmanicidal activity, and support the use of plant extracts enriched in antifungal phytoalexins, synthesized under fungal challenge, as a more rational and effective strategy to screen for new plant leishmanicidal drugs. PMID:15105102

  17. Antifungal Constituents from the Roots of Piper dilatatum Rich.

    Directory of Open Access Journals (Sweden)

    Ruilan Alves dos Santos

    2013-01-01

    Full Text Available The compounds (+-(7S,8R-epoxy-5,6-didehydrokavain (1, flavokavain B (2, β-sitosterol (3, and stigmasterol (4 are reported here as chemical constituents of Piper dilatatum Rich. (Piperaceae. Their structures were determined on the basis of their spectroscopic data (1H and 13C NMR, MS, and IR. The antifungal activities of pyrone 1 (1 μg and chalcone 2 (100 μg were determined by means of direct bioautography against Cladosporium cladosporioides and C. sphaerospermum. Results indicate P. dilatatum as a candidate for the development of novel antifungal phytotherapic products as well as point out pyrone 1 as a promising hit compound in the quest for novel antifungal agents.

  18. 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.

  19. 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.

  20. Metal-Based Antibacterial and Antifungal Agents: Synthesis, Characterization, and In Vitro Biological Evaluation of Co(II, Cu(II, Ni(II, and Zn(II Complexes with Amino Acid-Derived Compounds

    Directory of Open Access Journals (Sweden)

    Zahid H. Chohan

    2006-01-01

    Full Text Available A series of antibacterial and antifungal amino acid-derived compounds and their cobalt(II, copper(II, nickel(II, and zinc(II metal complexes have been synthesized and characterized by their elemental analyses, molar conductances, magnetic moments, and IR, and electronic spectral measurements. Ligands (L1–(L5 were derived by condensation of β-diketones with glycine, phenylalanine, valine, and histidine and act as bidentate towards metal ions (cobalt, copper, nickel, and zinc via the azomethine-N and deprotonated-O of the respective amino acid. The stoichiometric reaction between the metal(II ion and synthesized ligands in molar ratio of M: L (1: 1 resulted in the formation of the metal complexes of type [M(L(H2O4]Cl (where M = Co(II, Cu(II, and Zn(II and of M: L (1: 2 of type [M(L2(H2O2] (where M = Co(II, Cu(II, Ni(II, and Zn(II. The magnetic moment data suggested for the complexes to have an octahedral geometry around the central metal atom. The electronic spectral data also supported the same octahedral geometry of the complexes. Elemental analyses and NMR spectral data of the ligands and their metal(II complexes agree with their proposed structures. The synthesized ligands, along with their metal(II complexes, were screened for their in vitro antibacterial activity against four Gram-negative (Escherichia coli, Shigella flexeneri, Pseudomonas aeruginosa, and Salmonella typhi and two Gram-positive (Bacillus subtilis and Staphylococcus aureus bacterial strains and for in vitro antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, and Candida glaberata. The results of these studies show the metal(II complexes to be more antibacterial/antifungal against one or more species as compared to the uncomplexed ligands. The brine shrimp bioassay was also carried out to study their in vitro cytotoxic properties. Five compounds, (3, (7, (10, (11, and (22, displayed potent cytotoxic

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

    Directory of Open Access Journals (Sweden)

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

    Directory of Open Access Journals (Sweden)

    Cristiane de Bona da Silva

    2008-02-01

    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.

  3. 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.

    2013-01-01

    Abstract 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. PMID:23819641

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

    OpenAIRE

    Neveen Helmy Abou El-Soud; Mohamed Deabes; Lamia Abou El-Kassem; Mona Khalil

    2015-01-01

    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 anal...

  5. The effectiveness of corneal ulcer debridement and antifungal agents in the treatment of patients with fungal keratitis%角膜溃疡清创术与抗真菌药物联用治疗真菌性角膜炎的有效性评价

    Institute of Scientific and Technical Information of China (English)

    廖敏

    2016-01-01

    目的探究角膜溃疡清创术与抗真菌药物联用治疗真菌性角膜炎的有效性。方法选取从2011年7月至2015年7月进行治疗的真菌性角膜炎患者184例。对照组88例患者进行角膜溃疡清创术治疗,观察组96例患者进行角膜溃疡清创术与抗真菌药物联用治疗。治疗结束后对两组患者的治疗效果进行对比分析。结果在治疗结束后,观察组患者总有效率为92例(95.8%),对照组患者总有效率为60例(68.2%)。观察组患者视力>0.5比率为54.2%,明显高于对照组患者0.5比率36.62%,差异有统计学意义( P <0.05)。观察组患者的愈合时间、眼前指数、手动-光感、手术次数均优于对照组,差异有统计学意义( P <0.05)。结论在治疗真菌性角膜炎时,采用角膜溃疡清创术与抗真菌药物联用的方法效果良好,能明显改善患者视力,值得临床推广使用。%Objective To explore the effectiveness of corneal ulcer debridement combined with antifungal agents in the treatment of pa-tients with fungal keratitis. Methods Select 184 patients with fungal keratitis treatment in our hospital from July 2011 to July 2015,the 88 cases of control group with treatment of corneal ulcer debridement,the 96 cases of observation group with treatment of corneal ulcer debridement and an-tifungal agents. The clinical parameters and effect of 2 groupspatients were compared. Results After treatment,the total effective rate in the ob-servation group was 95. 8% ,and the total effective rate was 68. 2% in the control group. The observation group of patients with visual > 0. 5 ratio was 54. 2% ,significantly higher than the control group(36. 62% ),the difference was statistically significant( P < 0. 05). The observation group,the healing time,immediate index,manual light perception,and number of operations were superior to the control group,the difference was statistically significant( P < 0. 05). Conclusion

  6. 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.

  7. Antifungal property of quaternized chitosan and its derivatives.

    Science.gov (United States)

    Sajomsang, Warayuth; Gonil, Pattarapond; Saesoo, Somsak; Ovatlarnporn, Chitchamai

    2012-01-01

    Five water-soluble chitosan derivatives were carried out by quaternizing either iodomethane or N-(3-chloro-2-hydroxypropyl) trimethylammonium chloride (Quat188) as a quaternizing agent under basic condition. The degree of quaternization (DQ) ranged between 28±2% and 90±2%. The antifungal activity was evaluated by using disc diffusion method, minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) methods against Trichophyton rubrum (T. rubrum), Trichophyton mentagrophyte (T. mentagrophyte), and Microsporum gypseum (M. gypseum) at pH 7.2. All quaternized chitosans and its derivatives showed more effective against T. rubrum than M. gypseum and T. mentagrophyte. The MIC and MFC values were found to range between 125-1000 μg/mL and 500-4000 μg/mL, respectively against all fungi. Our results indicated that the quaternized N-(4-N,N-dimethylaminocinnamyl) chitosan chloride showed highest antifungal activity against T. rubrum and M. gypseum compared to other quaternized chitosan derivatives. The antifungal activity tended to increase with an increase in molecular weight, degree of quaternization and hydrophobic moiety against T. rubrum. However, the antifungal activity was depended on type of fungal as well as chemical structure of the quaternized chitosan derivatives.

  8. 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.

  9. 阴道白假丝酵母菌的耐药性和ERG11基因突变关系研究%Research on the relationship between the mutations of ERG11 gene and the resistance of pyrrolic antifungal agents in vaginal candida albicans

    Institute of Scientific and Technical Information of China (English)

    谭皓妍; 李倩珺; 冯浩华; 何艳屏

    2014-01-01

    目的 探讨ERG11基因突变与白假丝酵母菌对吡咯类药物敏感性下降的关系.方法 收集VVC患者的白假丝酵母菌60株,用科玛嘉念珠菌显色培养基作菌种鉴定,纸片扩散法进行药敏试验,选取所有中度敏感株和耐药株用聚合酶链反应扩增(PCR)ERG11基因,将PCR产物进行测序分析和比对分析.结果 60株白假丝酵母菌对咪康唑、酮康唑和氟康唑敏感率分别为36.7%、56.1%和80%;将38株中度敏感株和耐药株进行ERG11基因分析后共发现29个有义突变和25个同义突变,其中,有义突变中发现多个新突变位点.结论 有些新发现的突变位点可能与耐药相关;多位点有义突变可能降低菌株对药物的敏感性.%Objective To invesigate the relationship between mutation of ERG11 gene and the decreased sensitivity to pyrrolic antifungal agents in vaginal Candida albicans.Methods sixty strains of Candida albicans from VVC patients were collected and identified by CHROM agar.The drug resistance was detected by disk diffusion method.The ERG11 gene of the moderately susceptible and resistant strains was amplified by PCR.The PCR products were analyzed by DNA sequencing.Results The sensitive rates of sixty strains of Candida albicans strains to miconazole,ketoconazole and fluconazole were 36.7%,56.1% and 80%,respectively.After comparison of ERG11 gene DNA sequences alignment,we found 29 missense mutations and 25 silent mutations in 38 strains of moderately susceptible and resistant strains.Several new mutations were found in ERG11 genein the missense mutations.Conclusion Some new mutations were found in ERG11 gene which might be associated with drug resistance.Multiple amino acid substitutions in Erg11 of vaginal Candida albicans may reduce the sensitivity to pyrrolic antifungal agents.

  10. 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.

  11. 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.

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

    Directory of Open Access Journals (Sweden)

    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

  13. Biochemical approaches to selective antifungal activity. Focus on azole antifungals.

    Science.gov (United States)

    Vanden Bossche, H; Marichal, P; Gorrens, J; Coene, M C; Willemsens, G; Bellens, D; Roels, I; Moereels, H; Janssen, P A

    1989-01-01

    Azole antifungals (e.g. the imidazoles: miconazole, clotrimazole, bifonazole, imazalil, ketoconazole, and the triazoles: diniconazole, triadimenol, propiconazole, fluconazole and itraconazole) inhibit in fungal cells the 14 alpha-demethylation of lanosterol or 24-methylenedihydrolanosterol. The consequent inhibition of ergosterol synthesis originates from binding of the unsubstituted nitrogen (N-3 or N-4) of their imidazole or triazole moiety to the heme iron and from binding of their N-1 substituent to the apoprotein of a cytochrome P-450 (P-450(14)DM) of the endoplasmic reticulum. Great differences in both potency and selectivity are found between the different azole antifungals. For example, after 16h of growth of Candida albicans in medium supplemented with [14C]-acetate and increasing concentrations of itraconazole, 100% inhibition of ergosterol synthesis is achieved at 3 x 10(-8) M. Complete inhibition of this synthesis by fluconazole is obtained at 10(-5) M only. The agrochemical imidazole derivative, imazalil, shows high selectivity, it has almost 80 and 98 times more affinity for the Candida P-450(s) than for those of the piglet testes microsomes and bovine adrenal mitochondria, respectively. However, the topically active imidazole antifungal, bifonazole, has the highest affinity for P-450(s) of the testicular microsomes. The triazole antifungal itraconazole inhibits at 10(-5) M the P-450-dependent aromatase by 17.9, whereas 50% inhibition of this enzyme is obtained at about 7.5 x 10(-6)M of the bistriazole derivative fluconazole. The overall results show that both the affinity for the fungal P-450(14)DM and the selectivity are determined by the nitrogen heterocycle and the hydrophobic N-1 substituent of the azole antifungals. The latter has certainly a greater impact. The presence of a triazole and a long hypdrophobic nonligating portion form the basis for itraconazole's potency and selectivity.

  14. Current recommendations and importance of antifungal stewardship for the management of invasive candidiasis.

    Science.gov (United States)

    Miyazaki, Taiga; Kohno, Shigeru

    2015-01-01

    Invasive candidiasis can have a major effect on patient prognosis and medical economics. Quickly eliminating the focus of the infection and administering appropriate antifungal therapy are important. Clinical guidelines for invasive candidiasis have been issued in the USA, Europe and recently in Japan. The purpose of this review is to summarize the current recommendations on how to diagnose and treat invasive candidiasis based on the evidence gathered to date and by referencing guidelines from various countries. Echinocandin antifungals play a central role in the prevention and treatment of invasive candidiasis although a recent increase in echinocandin-resistant Candida glabrata is seen as problematic. In the future, promoting the appropriate use of antifungal agents by antifungal stewardship teams will be necessary to suppress adverse effects, appearance of resistant strains and unnecessary medical expenses, as well as improve positive clinical outcomes and prognoses.

  15. Antifungal constituents of Melicope borbonica

    DEFF Research Database (Denmark)

    Simonsen, Henrik Toft; Adsersen, Anne; Bremner, Paul

    2004-01-01

    , as the major constituents. All three compounds exhibited moderate antifungal activity against Candida albicans and Penicillium expansum, in accordance with the traditional use of the plant. Moreover, 2,4,6-trimethoxyacetophenone (methylxanthoxylin), three other coumarins [7-(3-methyl-2-butenyloxy)-6...

  16. An insight into the antifungal pipeline: selected new molecules and beyond.

    Science.gov (United States)

    Ostrosky-Zeichner, Luis; Casadevall, Arturo; Galgiani, John N; Odds, Frank C; Rex, John H

    2010-09-01

    Invasive fungal infections are increasing in incidence and are associated with substantial mortality. Improved diagnostics and the availability of new antifungals have revolutionized the field of medical mycology in the past decades. This Review focuses on recent developments in the antifungal pipeline, concentrating on promising candidates such as new azoles, polyenes and echinocandins, as well as agents such as nikkomycin Z and the sordarins. Developments in vaccines and antibody-based immunotherapy are also discussed. Few therapeutic products are currently in active development, and progression of therapeutic agents with fungus-specific mechanisms of action is of key importance.

  17. Sporothrix schenckii complex in Iran: Molecular identification and antifungal susceptibility.

    Science.gov (United States)

    Mahmoudi, Shahram; Zaini, Farideh; Kordbacheh, Parivash; Safara, Mahin; Heidari, Mansour

    2016-08-01

    Sporotrichosis is a global subcutaneous fungal infection caused by the Sporothrix schenckii complex. Sporotrichosis is an uncommon infection in Iran, and there have been no phenotypic, molecular typing or antifungal susceptibility studies of Sporothrix species. This study aimed to identify nine Iranian isolates of the S. schenckii complex to the species level using colony morphology, carbohydrate assimilation tests, and PCR-sequencing of the calmodulin gene. The antifungal susceptibilities of these Sporothrix isolates to five antifungal agents (amphotericin B (AMB), voriconazole (VRC), itraconazole (ITC), fluconazole (FLC), and terbinafine (TRB)) were also evaluated according to the M27-A3 and M38-A2 protocols of the Clinical and Laboratory Standards Institute for yeast and mycelial phases, respectively. Five of seven clinical isolates were identified as S. schenckii, and two clinical and two environmental isolates were identified as S. globosa. This is the first report of S. globosa in Iran. There was significant agreement (73%) between the results of the phenotypic and genotypic identification methods. TRB and ITC were the most effective antifungals against the Sporothrix isolates. The minimum inhibitory concentration (MIC) values of TRB for the yeast and mycelial phases of S. schenckii differed significantly. There was also a significant difference in the minimum fungicidal concentration (MFC) values of AMB and TRB for the two phases. Considering the low efficacy of VRC and FLC and the wide MIC ranges of AMB (1-16 μg/ml and 1-8 μg/ml for yeast and mycelial forms, respectively) observed in the present study, in vitro antifungal susceptibility testing should be performed to determine appropriate therapeutic regimens.

  18. The use of the antifungal agent miconazole as an inhibitor of Blastocystis hominis growth in Entamoeba histolytica/E. dispar cultures Uso do antifúngico miconazol como inibidor do crescimento de Blastocystis hominis em culturas de Entamoeba histolytica/E. dispar

    Directory of Open Access Journals (Sweden)

    Alessandra Queiroga Gonçalves

    2007-06-01

    Full Text Available In regions with high prevalence, Blastocystis hominis is frequently found in association with Entamoeba histolytica/E. dispar in xenic cultures. Its exacerbated growth is often superimposed on the growth of amebas, thus impeding the continuation of the amebas in the culture, within a few generations. The present study reports on the excellent efficacy (100% of the antifungal agent miconazole in eliminating B. hominis from cultures of E. histolytica/E. dispar, thereby maintaining the integrity of the trophozoites of the amebas. Nystatin presented low efficacy (33.3%.Em regiões de alta prevalência, Blastocystis hominis é freqüentemente encontrado em associação com Entamoeba histolytica/E. dispar em cultivos xênicos. Seu crescimento exacerbado se sobrepõe muitas vezes ao das amebas, impedindo a manutenção destas em cultura, dentro de poucas gerações. O presente estudo relata a excelente eficácia (100% do antifúngico miconazol na eliminação de B. hominis dos cultivos de E. histolytica/E. dispar, mantendo-se a integridade dos trofozoítos das amebas. A nistatina apresentou eficácia baixa (33,3%.

  19. In vitro antifungal activity of 2-(2'-hydroxy-5'-aminophenyl)benzoxazole in Candida spp. strains.

    Science.gov (United States)

    Daboit, Tatiane Caroline; Stopiglia, Cheila Denise Ottonelli; Carissimi, Mariana; Corbellini, Valeriano Antonio; Stefani, Valter; Scroferneker, Maria Lúcia

    2009-11-01

    The development of azole antifungals has allowed for the treatment of several fungal infections. However, the use of these compounds is restricted because of their hepatotoxicity or because they need to be administered together with other drugs in order to prevent resistance to monotherapy. Benzoxazole derivatives are among the most thriving molecular prototypes for the development of antifungal agents. 2-(2'-hydroxyphenyl) benzoxazoles are versatile molecules that emit fluorescence and have antibacterial, antiviral and antifungal properties. 2-(2'-hydroxy-5'-aminophenyl) benzoxazole (HAMBO) was tested against Candida yeast. The inhibition provided by HAMBO was lower than that of fluconazole, showing low antifungal activity against Candida spp., but equivalent to that of benzoxazoles tested in similar studies. HAMBO showed fungistatic activity against all analysed strains. This class of novel benzoxazole compounds may be used as template to produce better antifungal drugs.

  20. Conventional and alternative antifungal therapies to oral candidiasis.

    Science.gov (United States)

    Anibal, Paula Cristina; de Cássia Orlandi Sardi, Janaina; Peixoto, Iza Teixeira Alves; de Carvalho Moraes, Julianna Joanna; Höfling, José Francisco

    2010-10-01

    Candida-associated denture stomatitis is the most common form of oral candidal infection, with Candida albicans being the principal etiological agent. Candida adheres directly or via an intermediary layer of plaque-forming bacteria to denture acrylic. Despite antifungal therapy to treat denture stomatitis, infection is reestablished soon after the treatment ceases. In addition, many predisposing factors have been identified as important in the development of oral candidiasis, including malnourishment, common endocrine disorders, such as diabetis mellitus, antibacterial drug therapy, corticosteroids, radiotherapy and other immunocompromised conditions, such as acquired immunodeficiency syndrome (AIDS). These often results in increased tolerance to the most commonly used antifungals. So this review suggests new therapies to oral candidiasis.

  1. Conventional and alternative antifungal therapies to oral candidiasis

    Directory of Open Access Journals (Sweden)

    Paula Cristina Anibal

    2010-12-01

    Full Text Available Candida-associated denture stomatitis is the most common form of oral candidal infection, with Candida albicans being the principal etiological agent. Candida adheres directly or via an intermediary layer of plaque-forming bacteria to denture acrylic. Despite antifungal therapy to treat denture stomatitis, infection is reestablished soon after the treatment ceases. In addition, many predisposing factors have been identified as important in the development of oral candidiasis, including malnourishment, common endocrine disorders, such as diabetis mellitus, antibacterial drug therapy, corticosteroids, radiotherapy and other immunocompromised conditions, such as acquired immunodeficiency syndrome (AIDS. These often results in increased tolerance to the most commonly used antifungals. So this review suggests new therapies to oral candidiasis.

  2. Potential Use of Alginate-Based Carriers As Antifungal Delivery System

    Science.gov (United States)

    Spadari, Cristina de Castro; Lopes, Luciana B.; Ishida, Kelly

    2017-01-01

    Fungal infections have become a major public health problem, growing in number and severity in recent decades due to an increase of immunocompromised patients. The use of therapeutic agents available to treat these fungal infections is limited by their toxicity, low bioavailability, antifungal resistance, and high cost of treatment. Thus, it becomes extremely important to search for new therapeutic options. The use of polymeric systems as drug carriers has emerged as a promising alternative to conventional formulations for antifungals. Alginate is a natural polymer that has been explored in the last decade for development of drug delivery systems due to its non-toxicity, biodegradability, biocompatibility, low cost, mucoadhesive, and non-immunogenic properties. Several antifungal agents have been incorporated in alginate-based delivery systems, including micro and nanoparticles, with great success, displaying promising in vitro and in vivo results for antifungal activities, reduction in the toxicity and the total drug dose used in the treatment, and improved bioavailability. This review aims at discussing the potential use and benefits of alginate-based nanocarriers and other delivery systems containing antifungal agents in the therapy of fungal infections. PMID:28194145

  3. Antifungal activity of benzalkonium chloride, dettol , and chlorhexidine on opportunistic isolated fungi from the environment and operating rooms in private clinics of Tehran in 2011

    Directory of Open Access Journals (Sweden)

    Hossein Nowrozi

    2013-11-01

    Conclusion: Benzalkonium chloride and Dettol had a complete antifungal activity, but chlorhexidine was found to be the least effective agent.. Therefore, the tested concentrations give out their most fungicidal activity as disinfectants, if their durability is taken into account.

  4. Repurposing Approach Identifies Auranofin with Broad Spectrum Antifungal Activity That Targets Mia40-Erv1 Pathway

    Science.gov (United States)

    Thangamani, Shankar; Maland, Matthew; Mohammad, Haroon; Pascuzzi, Pete E.; Avramova, Larisa; Koehler, Carla M.; Hazbun, Tony R.; Seleem, Mohamed N.

    2017-01-01

    Current antifungal therapies have limited effectiveness in treating invasive fungal infections. Furthermore, the development of new antifungal is currently unable to keep pace with the urgent demand for safe and effective new drugs. Auranofin, an FDA-approved drug for the treatment of rheumatoid arthritis, inhibits growth of a diverse array of clinical isolates of fungi and represents a new antifungal agent with a previously unexploited mechanism of action. In addition to auranofin's potent antifungal activity against planktonic fungi, this drug significantly reduces the metabolic activity of Candida cells encased in a biofilm. Unbiased chemogenomic profiling, using heterozygous S. cerevisiae deletion strains, combined with growth assays revealed three probable targets for auranofin's antifungal activity—mia40, acn9, and coa4. Mia40 is of particular interest given its essential role in oxidation of cysteine rich proteins imported into the mitochondria. Biochemical analysis confirmed auranofin targets the Mia40-Erv1 pathway as the drug inhibited Mia40 from interacting with its substrate, Cmc1, in a dose-dependent manner similar to the control, MB-7. Furthermore, yeast mitochondria overexpressing Erv1 were shown to exhibit resistance to auranofin as an increase in Cmc1 import was observed compared to wild-type yeast. Further in vivo antifungal activity of auranofin was examined in a Caenorhabditis elegans animal model of Cryptococcus neoformans infection. Auranofin significantly reduced the fungal load in infected C. elegans. Collectively, the present study provides valuable evidence that auranofin has significant promise to be repurposed as a novel antifungal agent and may offer a safe, effective, and quick supplement to current approaches for treating fungal infections. PMID:28149831

  5. The antifungal activity of Natamycin : a novel mode of action of the polyene antibiotics

    NARCIS (Netherlands)

    te Welscher, Y.M.

    2010-01-01

    Fungal infections have recently become a growing threat to human health, especially in persons whose immune systems are compromised (for example transplant recipients or patients with HIV or cancer). Only a few effective antifungal agents are currently in use and a major problem is the increase of d

  6. Polyglycolic acid microneedles modified with inkjet-deposited antifungal coatings.

    Science.gov (United States)

    Boehm, Ryan D; Daniels, Justin; Stafslien, Shane; Nasir, Adnan; Lefebvre, Joe; Narayan, Roger J

    2015-03-02

    In this study, the authors examined use of piezoelectric inkjet printing to apply an antifungal agent, voriconazole, to the surfaces of biodegradable polyglycolic acid microneedles. Polyglycolic acid microneedles with sharp tips (average tip radius = 25 ± 3 μm) were prepared using a combination of injection molding and drawing lithography. The elastic modulus (9.9 ± 0.3 GPa) and hardness (588.2 ± 33.8 MPa) values of the polyglycolic acid material were determined using nanoindentation and were found to be suitable for use in transdermal drug delivery devices. Voriconazole was deposited onto the polyglycolic acid microneedles by means of piezoelectric inkjet printing. It should be noted that voriconazole has poor solubility in water; however, it is readily soluble in many organic solvents. Optical imaging, scanning electron microscopy, energy dispersive x-ray spectrometry, and Fourier transform infrared spectroscopy were utilized to examine the microneedle geometries and inkjet-deposited surface coatings. Furthermore, an in vitro agar plating study was performed on the unmodified, vehicle-modified, and voriconazole-modified microneedles. Unlike the unmodified and vehicle-modified microneedles, the voriconazole-modified microneedles showed antifungal activity against Candida albicans. The unmodified, vehicle-modified, and voriconazole-modified microneedles did not show activity against Escherichia coli, Pseudomonas aeruginosa, or Staphylococcus aureus. The results indicate that piezoelectric inkjet printing may be useful for loading transdermal drug delivery devices such as polyglycolic acid microneedles with antifungal pharmacologic agents and other pharmacologic agents with poor solubility in aqueous solutions.

  7. 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.

  8. 对唑类药物交叉耐药的烟曲霉临床分离株耐药机制的初步探讨%Molecular mechanisms of cross-resistance to azole antifungal agents in a clinical isolate of Aspergillus fumigatus: a preliminary study

    Institute of Scientific and Technical Information of China (English)

    孙毅; 刘伟; 陈伟; 万喆; 李若瑜

    2011-01-01

    Objective To investigate the molecular mechanisms of cross-resistance to azoles in a clinical isolate of Aspergillus fumigatus. Methods A. fumigatus was isolated from a patient with invasive aspergillosis.Clinical Laboratory Standard Institute M38-A2 broth microdilution method and E-test method were used to determine the minimum inhibitory concentrations (MICs) or minimum effective concentration (MEC) of itraconazole, voriconazole, amphotericin B, posaconazole and caspofungin for the A. fumigatus isolate. DNA was extracted from the isolate and subjected to the amplification of cyp51A gene encoding the target enzyme of azole antifungal agents followed by sequence analysis. Results The broth microdilution test showed that the MEC of caspofungin was 0.5 mg/L, and MICs of itraconazole, voriconazole and amphotericin B were ≥ 16 mg/L,8 mg/L and 1 mg/L, respectively, for this isolate; while E-test assay revealed that the MICs of caspofungin,itraconazole, voriconazole, amphotericin B and posaconazole were 0.047 mg/L, ≥32 mg/L,≥32 mg/L, 12 mg/L and ≥32 mg/L, respectively. Sequence analysis showed an insertion of a 34-bp tandem sequence in the promoter region of the cyp51A gene as well as a T364A point mutation causing the substitution of leucine 98 (L98H). In addition, there were some other mutations in the cyp51A gene of this isolate, such as A137T,G585A, C814A, G836C, T991C and A1350G, which could result in corresponding amino acid substitutions.Conclusions An A. fumigatus strain with cross-resistance to azole antifungal agents is isolated. There is an insertion of a 34-bp tandem sequence into the promoter region as well as a T364A point mutation in the cyp51A gene, which contribute to the cross resistance to azole antifungal agents including itraconazole, voriconazole,and posaconazole. In addition, other mutations causing amino acid substitutions have also been detected in the cyp51 A gene of this isolate.%目的 研究对唑类药物交叉耐药的烟曲霉临

  9. [Recommendations of antifungal treatment in patients with low grade immunosuppression].

    Science.gov (United States)

    Barberán, J; Mensa, J; Fariñas, C; Llinares, P; Serrano, R; Menéndez, R; Agustí, C; Gobernado, M; Azanza, J R; García Rodríguez, J A

    2008-06-01

    Because of the relevance that the systemic mycoses has acquired in non-highly immunocompromised patients, the treatment difficulties they have due to the increase of the non-albicans Candida species and the need to have a better and more rational use of the new antifungal agents (voriconazole, posaconazole, caspofungin, anidulafungin and micafungin), an experts' panel on infectious diseases in representation of the Spanish Society of Chemotherapy, Spanish Society of Internal Medicine, and Spanish Society of Pneumology and Thoracic Surgery has met in order to make a few recommendations based on the scientific evidence in an effort to improve their efficiency.

  10. The Influence of 3 Anti-fungal Agents on the Growth of Metarhizium and 6 Non-target Fungis%3种真菌抗生素对绿僵菌和6种非目标真菌的生长影响分析

    Institute of Scientific and Technical Information of China (English)

    杨华; 徐金柱; 秦长生; 揭育泽

    2014-01-01

    文章比较了两性霉素、伊曲康唑和放线菌酮对土壤内金龟子绿僵菌(Metarhizium anisopliae)、黄绿绿僵菌(M.flavoviride)和6种非目标真菌生长的影响。结果表明,伊曲康唑对毛霉(Mucor racemosus)和黑曲霉(Aspergillus niger)的抑菌效果较差,浓度达200μg/mL时对毛霉的抑制率仅达54.84%,且对绿僵菌生长的抑制作用显著大于两性霉素和放线菌酮(P<0.01),不适宜用于土壤绿僵菌的分离。两性霉素和放线菌酮在浓度为100μg/mL时,对6种非目标真菌抑制率达69%以上,可作为绿僵菌分离的真菌抗生素。%The effects of 3 anti- fungal agents on the growth of Metarhizium anisopliae,M.flavoviride strains and 6 non-target fungis were studied.The results showed that itraconazole did not have good inhibitory effects on Mucor racemosus and Aspergillus niger,the rate of M.racemosus controlling was 54.84%,but the inhibi-tory effects on the growth of Metarhizium were significantly higher than that of amphotericin and cycloheximide (P<0.01),suggesting it was not suitable for Metarhizium isolation from soil.Amphotericin and cycloheximide of 100μg/mL could inhibit over 69%of 6 non-target fungis,and were the most suitable anti-fungal agents for Metarhizium isolation.

  11. Candida Infections: An Update on Host Immune Defenses and Anti-Fungal Drugs

    Directory of Open Access Journals (Sweden)

    Ning Gao

    2016-04-01

    Full Text Available Infections by fungal pathogens such as Candida albicans and non-albicans Candida species are becoming increasing prevalent in the human population. Such pathogens cause life-threatening diseases with high mortality, particularly in immunocompromised patients. Host defenses against fungal infections are provided by an exquisite interplay between innate and adaptive immune responses. However, effective anti-fungal agents for Candida infections are limited, and fungal drug resistance is a significant treatment challenge. In this review, we summarize the current understanding of host–fungal interactions, discuss the modes action of anti-fungal drugs, explore host defense mechanisms, and define the new challenges for treating Candida infections.

  12. Active packaging with antifungal activities.

    Science.gov (United States)

    Nguyen Van Long, N; Joly, Catherine; Dantigny, Philippe

    2016-03-01

    There have been many reviews concerned with antimicrobial food packaging, and with the use of antifungal compounds, but none provided an exhaustive picture of the applications of active packaging to control fungal spoilage. Very recently, many studies have been done in these fields, therefore it is timely to review this topic. This article examines the effects of essential oils, preservatives, natural products, chemical fungicides, nanoparticles coated to different films, and chitosan in vitro on the growth of moulds, but also in vivo on the mould free shelf-life of bread, cheese, and fresh fruits and vegetables. A short section is also dedicated to yeasts. All the applications are described from a microbiological point of view, and these were sorted depending on the name of the species. Methods and results obtained are discussed. Essential oils and preservatives were ranked by increased efficacy on mould growth. For all the tested molecules, Penicillium species were shown more sensitive than Aspergillus species. However, comparison between the results was difficult because it appeared that the efficiency of active packaging depended greatly on the environmental factors of food such as water activity, pH, temperature, NaCl concentration, the nature, the size, and the mode of application of the films, in addition to the fact that the amount of released antifungal compounds was not constant with time.

  13. Antifungal susceptibility of Candida biofilms: unique efficacy of amphotericin B lipid formulations and echinocandins.

    Science.gov (United States)

    Kuhn, D M; George, T; Chandra, J; Mukherjee, P K; Ghannoum, M A

    2002-06-01

    Biofilms, likely the predominant mode of device-related microbial infection, exhibit resistance to antimicrobial agents. Evidence suggests that Candida biofilms have dramatically reduced susceptibility to antifungal drugs. We examined antifungal susceptibilities of Candida albicans and Candida parapsilosis biofilms grown on a bioprosthetic model. In addition to conventional agents, we determined if new antifungal agents (triazoles, amphotericin B lipid formulations, and echinocandins) have activities against Candida biofilms. We also explored effects of preincubation of C. albicans cells with subinhibitory concentrations (sub-MICs) of drugs to see if they could modify subsequent biofilm formation. Finally, we used confocal scanning laser microscopy (CSLM) to image planktonic- and biofilm-exposed blastospores to examine drug effects on cell structure. Candida biofilms were formed on silicone elastomer and quantified by tetrazolium and dry weight (DW) assays. Susceptibility testing of fluconazole, nystatin, chlorhexidine, terbenafine, amphotericin B (AMB), and the triazoles voriconazole (VRC) and ravuconazole revealed resistance in all Candida isolates examined when grown as biofilms, compared to planktonic forms. In contrast, lipid formulations of AMB (liposomal AMB and AMB lipid complex [ABLC]) and echinocandins (caspofungin [Casp] and micafungin) showed activity against Candida biofilms. Preincubation of C. albicans cells with sub-MIC levels of antifungals decreased the ability of cells to subsequently form biofilm (measured by DW; P formulations.

  14. Antifungal effect of cumin essential oil alone and in combination with antifungal drugs

    Directory of Open Access Journals (Sweden)

    SAHADEO PATIL

    2015-05-01

    Full Text Available Abstract. Patil S, Maknikar P, Wankhade S, Ukesh C, Rai M. 2015. Antifungal effect of cumin essential oil alone and in combination with antifungal drugs. Nusantara Bioscience 7: 55-59. We report evaluation of antifungal activity of cumin seed oil and its pharmacological interactions when used in combination with some of the widely used conventional antifungal drugs using CLSI broth microdilution, agar disc diffusion and checkerboard microtitre assay against Candida. The essential oil was obtained from cumin seeds using hydrodistillation technique and was later evaluated for the presence of major chemical constituents present in it using gas chromatography and mass spectrometry (GC-MS assay. The GC-MS assay revealed the abundance of γ-terpinene (35.42% followed by p-cymene (30.72%. The agar disc diffusion assay demonstrated highly potent antifungal effect against Candida species. Moreover, the combination of cumin essential oil (CEO with conventional antifungal drugs was found to reduce the individual MIC of antifungal drug suggesting the occurrence of synergistic interactions. Therefore, the therapy involving combinations of CEO and conventional antifungal drugs can be used for reducing the toxicity induced by antifungal drugs and at the same time enhancing their antifungal efficacy in controlling the infections caused due to Candida species.

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

    Science.gov (United States)

    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.

  16. 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.

  17. Evaluation of Benzophenone-N-ethyl Morpholine Ethers as Antibacterial and Antifungal Activities

    Directory of Open Access Journals (Sweden)

    A. Bushra Begum

    2014-01-01

    Full Text Available Microorganisms are closely associated with the health and welfare of human beings. Whereas some microorganisms are beneficial, others are detrimental. Bacterial infections often produce inflammation and pains and in some instances, infections result in high mortality. Any subtle change in the drug molecule, which may not be detected by chemical methods, can be revealed by a change in the antimicrobial activity and hence microbiological assays are very useful. A series of substituted hydroxy benzophenones and benzophenone-N-ethyl morpholine ethers were screened for their antibacterial and antifungal activities. Antibacterial activity against S. aureus, E. aerogenes, M. luteus, K. pneumonia, and S. typhimurium, S. paratyphi-B and P. vulgaris bacterial strains and antifungal activity against C. albicans, B. cinerea, M. pachydermatis, C. krusei fungal strains were carried out. The bioassays indicated that most of the synthesized compounds showed potential antibacterial and antifungal agents.

  18. A chemometric approach for prediction of antifungal activity of some benzoxazole derivatives against Candida albicans

    Directory of Open Access Journals (Sweden)

    Podunavac-Kuzmanović Sanja O.

    2012-01-01

    Full Text Available The purpose of the article is to promote and facilitate prediction of antifungal activity of the investigated series of benzoxazoles against Candida albicans. The clinical importance of this investigation is to simplify design of new antifungal agents against the fungi which can cause serious illnesses in humans. Quantitative structure activity relationship analysis was applied on nineteen benzoxazole derivatives. A multiple linear regression (MLR procedure was used to model the relationships between the molecular descriptors and the antifungal activity of benzoxazole derivatives. Two mathematical models have been developed as a calibration models for predicting the inhibitory activity of this class of compounds against Candida albicans. The quality of the models was validated by the leave-one-out technique, as well as by the calculation of statistical parameters for the established model. [Projekat Ministarstva nauke Republike Srbije, br. 172012 i br. 172014

  19. Silver and gold nanostructures: antifungal property of different shapes of these nanostructures on Candida species.

    Science.gov (United States)

    Jebali, Ali; Hajjar, Farzaneh Haji Esmaeil; Pourdanesh, Fereydoun; Hekmatimoghaddam, Seyedhossein; Kazemi, Bahram; Masoudi, Alireza; Daliri, Karim; Sedighi, Najme

    2014-01-01

    The shape of nanoparticles is an important determinant of their physical and chemical properties, possibly including the little-explored area of their use as antifungal agents. Therefore, we evaluated the in vitro antifungal activities of three different shapes of silver and gold nanostructures, including nanocubes, nanospheres, and nanowires, on Candida albicans, C. glabrata and C. tropicalis, using the microdilution and disk diffusion methods as per the guidelines of the Clinical and Laboratory Standards Institute. We found that silver and gold nanocubes had higher antifungal properties against the test species than nanospheres and nanowires. While some isolates were resistant to silver and gold nanospheres and nanowires, none of the isolates were resistant to silver and gold nanocubes. The occurrence of resistance is a new finding which should be further explored.

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

    Directory of Open Access Journals (Sweden)

    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.

  1. Novel, Synergistic Antifungal Combinations that Target Translation Fidelity

    Science.gov (United States)

    Moreno-Martinez, Elena; Vallieres, Cindy; Holland, Sara L.; Avery, Simon V.

    2015-01-01

    There is an unmet need for new antifungal or fungicide treatments, as resistance to existing treatments grows. Combination treatments help to combat resistance. Here we develop a novel, effective target for combination antifungal therapy. Different aminoglycoside antibiotics combined with different sulphate-transport inhibitors produced strong, synergistic growth-inhibition of several fungi. Combinations decreased the respective MICs by ≥8-fold. Synergy was suppressed in yeast mutants resistant to effects of sulphate-mimetics (like chromate or molybdate) on sulphate transport. By different mechanisms, aminoglycosides and inhibition of sulphate transport cause errors in mRNA translation. The mistranslation rate was stimulated up to 10-fold when the agents were used in combination, consistent with this being the mode of synergistic action. A range of undesirable fungi were susceptible to synergistic inhibition by the combinations, including the human pathogens Candida albicans, C. glabrata and Cryptococcus neoformans, the food spoilage organism Zygosaccharomyces bailii and the phytopathogens Rhizoctonia solani and Zymoseptoria tritici. There was some specificity as certain fungi were unaffected. There was no synergy against bacterial or mammalian cells. The results indicate that translation fidelity is a promising new target for combinatorial treatment of undesirable fungi, the combinations requiring substantially decreased doses of active components compared to each agent alone. PMID:26573415

  2. Evaluation of antifungal potential of selected medicinal plants against human pathogenic fungi

    Directory of Open Access Journals (Sweden)

    Hayat Sakander

    2015-01-01

    Full Text Available Context: Evaluation of medicinal plants used in traditional medicine lead to novel bioactive compounds with antifungal activity that could be exploited as therapeutic agents. Aims: The aim was to screen selected medicinal plants for antifungal activity against three important human pathogenic fungi and to identify the broad group of phytochemicals responsible for the activity. Materials and Methods: A total of 8 medicinal plants were screened for antifungal activity against three human pathogenic fungi. Aqueous and the solvent extracts of the plant materials were prepared by polarity based solvent extraction. Antifungal activity was tested by well and disc diffusion methods. Minimum inhibitory concentration (MIC of the active extract was determined by micro-broth dilution technique. Phytochemical analysis of the active extract was done. Statistical Analysis Used: The results were statistically analysed by One-Way analysis of variance with Post-hoc Tukey′s B test at P < 0.05 using the  Software SPSS version 20 (IBM Corp. Armonk, NY Released 2011. Results: Significant antifungal activity was observed in the aqueous extracts of the fruits of Terminalia chebula (47.75 mm against Microsporum gypseum and the mesocarp of Persea americana (40.5 mm against Microsporum canis. Candida albicans was inhibited by the ethyl acetate (20 mm and aqueous extracts (16 mm of T. chebula fruits and aqueous extract of the seeds of Syzygium jambos (16 mm. The aqueous extract of mesocarp of P. americana showed lowest MIC value (312.5 μg/ml against M. canis and M. gypseum. Phytochemical analysis of the active extracts revealed the presence of phenols, tannins, alkaloids and flavonoids. Conclusions: The study validates the use of the plants in the treatment of fungal infections and has provided important leads for the discovery of new plant-based antifungal agents.

  3. Allergic Fungal Rhinosinusitis and the Unified Airway: the Role of Antifungal Therapy in AFRS.

    Science.gov (United States)

    Ryan, Matthew W; Clark, Christopher M

    2015-12-01

    Allergic fungal sinusitis (AFS) or rhinosinusitis (AFRS) is a form of polypoid chronic rhinosinusitis that is believed to be due to hypersensitivity to fungal antigens. The disease is characterized by type 1 hypersensitivity to fungal allergens, dramatically elevated total serum IgE, accumulation of thick eosinophil-laden mucin with non-invasive fungal hyphae within the paranasal sinuses, nasal polyposis, and sinus bony remodeling. Because of many clinicopathologic similarities to allergic bronchopulmonary aspergillosis (ABPA), these conditions can be considered analogous examples of disease in the unified airway. However, these conditions rarely occur together and their treatment differs. The treatment of AFRS relies upon surgical removal of fungal hyphae in eosinophilic mucin, while antifungal therapy is used to clear fungi from the airways in ABPA. Several uncontrolled studies suggest there may be some benefit to antifungal agents in AFRS, but randomized trials of topical and systemic antifungal therapies have not shown beneficial results in chronic rhinosinusitis (CRS). Antifungal treatment within the sinonasal cavities does not appear to be an effective approach for most chronic sinusitis, and antifungal therapy for AFRS is unproven.

  4. Comparative Antifungal Effect of Lactic Acid Bacteria Strains on Penicillium digitatum

    Directory of Open Access Journals (Sweden)

    Adrian Matei

    2015-11-01

    Full Text Available Lactic acid bacteria (LAB are natural alternative to chemical preservatives for fruits. The aim of the research was to select LAB strains with high antifungal activity against Penicillium digitatum for the biopreservation of fruits. The antifungal activity of eight lactic acid bacteria strains has been evaluated against Penicilliuum digitatum isolated from orange, by overlay assay method and by optical microscope examination. The reversion of inhibition zone after 96 h was recorded as a fungistatic effect while those with inhibition zone for at least 7 days were recorded as fungicidal. The antifungal effect of efficient LAB strains was assessed by comparing inhibition of fungal biofilm formation in liquid media. The strains Lpl, Lpa, LAB 13, LAB 15, LAB 43 and LAB 58 presented intense antifungal activity with clear inhibition zones diameter over 20 mm. The microscopy evidenced atypical hyphae and delaying of conidial chain formation. The strains Lpa, LAB 13, LAB 15 fully inhibited the mycelia growth, strains LAB 43 and LAB 58 partly with delaying of biofilm formation on the surface of culture medium. The results of comparative antifungal activity of LAB strains evidenced the highest inhibition of fungal biofilm formation and structural damages of hyphae and spores caused by the strains Lpa, LAB 13 and LAB 15. These strains could be efficient biocontrol agents of Penicillium digitatum in fruits.

  5. An antifungal protein from ginger rhizomes.

    Science.gov (United States)

    Wang, Hexiang; Ng, Tzi Bun

    2005-10-14

    There are very few reports on antifungal proteins from rhizomes and there is none from the family of Zingiberaceae. An antifungal protein with a novel N-terminal sequence was isolated from ginger rhizomes utilizing a protocol that involved ion exchange chromatography on DEAE-cellulose, affinity chromatography on Affi-gel blue gel, and fast protein liquid chromatography on Superdex 75. The protein was unadsorbed on DEAE-cellulose and adsorbed on Affi-gel blue gel. It exhibited an apparent molecular mass of 32kDa and exerted antifungal activity toward various fungi including Botrytis cinerea, Fusarium oxysporum, Mycosphaerella arachidicola, and Physalospora piricola.

  6. Isavuconazole: A New Broad-Spectrum Triazole Antifungal Agent.

    Science.gov (United States)

    Miceli, Marisa H; Kauffman, Carol A

    2015-11-15

    Isavuconazole is a new extended-spectrum triazole with activity against yeasts, molds, and dimorphic fungi. It is approved for the treatment of invasive aspergillosis and mucormycosis. Advantages of this triazole include the availability of a water-soluble intravenous formulation, excellent bioavailability of the oral formulation, and predictable pharmacokinetics in adults. A randomized, double-blind comparison clinical trial for treatment of invasive aspergillosis found that the efficacy of isavuconazole was noninferior to that of voriconazole. An open-label trial that studied primary as well as salvage therapy of invasive mucormycosis showed efficacy with isavuconazole that was similar to that reported for amphotericin B and posaconazole. In patients in these studies, as well as in normal volunteers, isavuconazole was well tolerated, appeared to have few serious adverse effects, and had fewer drug-drug interactions than those noted with voriconazole. As clinical experience increases, the role of this new triazole in the treatment of invasive fungal infections will be better defined.

  7. Genetic diversity and antifungal susceptibility profiles in agents of sporotrichosis

    NARCIS (Netherlands)

    A. Messias Rodrigues; G.S. de Hoog; D. de Cássia Pires; R.S. Nogueira Brihante; J.J. da Costa Sidrim; M.F. Gadelha; A. Lopes Colombo; Z. Pires de Camargo

    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 c

  8. Concise synthesis of a novel antifungal agent 4-methoxydecanoic acid

    Directory of Open Access Journals (Sweden)

    Pagudala Narsimha

    2013-12-01

    Full Text Available 4-Methoxy decanoic acid is belongs to a fatty acid family and has a novel anti- fungal activity. The aliphatic molecule has been synthesized in seven steps with an overall yield 41%. The synthesis was started from a commercially available epichloro hydrin and all the reactions were very clean.

  9. Antifungal properties of halofumarate esters.

    Science.gov (United States)

    Gershon, H; Shanks, L

    1978-04-01

    Alkyl esters (C1--C4) of the four halofumaric acids were tested for antifungal activity against Candida albicans, Aspergillus niger, Mucor mucedo, and Trichophyton mentagrophytes at pH 5.6 and 7.0 in the absence and presence of 10% beef serum in Sabouraud dextrose agar. The most toxic compound to each organism was: C. albicans, ethyl iodofumarate (0.054 mmole/liter); A. niger, methyl bromofumarate (0.090 mmole/liter); M. mucedo, methyl fluorofumarate (0.037 mmole/liter); and T. mentagrophytes, ethyl iodofumarate (0.020 mmole/liter). The order of overall activity of the six most toxic compounds was: ethyl iodofumarate greater than ethyl chlorofumarate greater than methyl iodofumarate = methyl bromofumarate greater than methyl chlorofumarate greater than bromofumarate.

  10. Early State Research on Antifungal Natural Products

    Directory of Open Access Journals (Sweden)

    Melyssa Negri

    2014-03-01

    Full Text Available Nosocomial infections caused by fungi have increased greatly in recent years, mainly due to the rising number of immunocompromised patients. However, the available antifungal therapeutic arsenal is limited, and the development of new drugs has been slow. Therefore, the search for alternative drugs with low resistance rates and fewer side effects remains a major challenge. Plants produce a variety of medicinal components that can inhibit pathogen growth. Studies of plant species have been conducted to evaluate the characteristics of natural drug products, including their sustainability, affordability, and antimicrobial activity. A considerable number of studies of medicinal plants and alternative compounds, such as secondary metabolites, phenolic compounds, essential oils and extracts, have been performed. Thus, this review discusses the history of the antifungal arsenal, surveys natural products with potential antifungal activity, discusses strategies to develop derivatives of natural products, and presents perspectives on the development of novel antifungal drug candidates.

  11. Investigation on mechanism of antifungal activity of eugenol against Trichophyton rubrum.

    Science.gov (United States)

    de Oliveira Pereira, Fillipe; Mendes, Juliana Moura; de Oliveira Lima, Edeltrudes

    2013-07-01

    Trichophyton rubrum is a worldwide agent responsible for chronic cases of dermatophytosis which have high rates of resistance to antifungal drugs. Attention has been drawn to the antimicrobial activity of aromatic compounds because of their promising biological properties. Therefore, we investigated the antifungal activity of eugenol against 14 strains of T. rubrum which involved determining its minimum inhibitory concentration (MIC) and effects on mycelial growth (dry weight), conidial germination and morphogenesis. The effects of eugenol on the cell wall (sorbitol protect effect) and the cell membrane (release of intracellular material, complex with ergosterol, ergosterol synthesis) were investigated. Eugenol inhibited the growth of 50% of T. rubrum strains employed in this study at an MIC = 256 μg/ml, as well as mycelial growth and conidia germination. It also caused abnormalities in the morphology of the dermatophyte in that we found wide, short, twisted hyphae and decreased conidiogenesis. The results of these studies on the mechanisms of action suggested that eugenol exerts antifungal effects on the cell wall and cell membrane of T. rubrum. Eugenol act on cell membrane by a mechanism that seems to involve the inhibition of ergosterol biosynthesis. The lower ergosterol content interferes with the integrity and functionality of the cell membrane. Finally, our studies support the potential use of the eugenol as an antifungal agent against T. rubrum.

  12. 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.

  13. IDENTIFICATION OF CANDIDA SPECIES FROM CLINICAL SAMPLES AND THEIR ANTIFUNGAL SUSCEPTIBILITY PATTERNS

    Directory of Open Access Journals (Sweden)

    Bhaskar

    2015-09-01

    Full Text Available OBJECTIVE AND BACKGROUND : The incidence of Candida infections has increased dramatically over the past few decades due to increase in the number of population susceptible to fungal infections. With multiple antifungal ag ents that are available and recovery of clinical isolates that exhibit inherent or developed resistance to commonly used antifungal agents, it has become imperative to do susceptibility testing routinely. The study was done to determine the predisposing fa ctors, species incidence and susceptibility pattern of Candida isolates to commonly use d antifungal agents. METHODS: A total of 108 Candida species were recovered from symptomatic clinical cases. Candida isolates were speciated by germ tube test, chlamydospore formation on corn meal agar and color produced on chromogenic media. Antifungal susceptibility test was done by disk diffusion method for nystatin, fluconazole, itraconazole, voriconazole and amphotericin - B. RESULTS: Candida albicans is the m ost frequently isolated species. However, non - albicans Candida species, taken as a group has predominated in clinical samples. Chromogenic agar medium showed good correlation in species identification in comparison with conventional germ tube test and chla mydospore formation on corn meal agar. C. albicans (41, C. tropicalis (33, C. krusei (30 and C. glabrata (04 were isolated. Candida species showed 95.4% susceptibility to amphotericin - B, 77.8% to voriconazol e, 69.4% to nystatin, 64.1% to f luconazole an d 63.9% to itraconazole. CONCLUSION : Increasing incidence of non - albicans species infection. Chromogenic medium can be used for species identification. Increasing resistance of Candida species to commonly used antifungal agents.

  14. 皮炎外瓶霉临床和环境分离株对6种常用抗真菌药物的敏感性测定%In vitro susceptibility testing of 16 strains of Exophiala dermatitidis to 6 commonly used antifungal agents

    Institute of Scientific and Technical Information of China (English)

    孙毅; 刘伟; 万喆; 陈伟; 李若瑜

    2010-01-01

    Objective To investigate the in vitro susceptibility of 16 strains of Exophiala dermatitidis to 6 commonly used antifungal agents. Methods The Glinical and Laboratory Standards Institute (CLSI)M27-A2 protocol was carried out to determine the MIGs of terbinafine (TRB), itraconazole (ITC), amphotericin B (AMB), fluconazole (FLC), voriconazole (VRC), and caspofungin (GAS) to 16 strains of E. dermatitidis, and E-test was performed to determine those of VRG, ITC and AMB. Besides, the minimal fungicidal concentrations (MFGs) of the above antifungal agents to the 16 strains of E. dermatitidis were further assessed.The activity of TRB in combination with ITC and VRG against E. dermatitidis was also estimated. Results The MIC ranges of TRB, VRC, ITC, AMB, FLC, and CAS were 0.125 - 0.25 mg/L, 0.25 - 0.5 mg/L, 2.0 mg/L,2.0 mg/L, 16 - 32 mg/L and 16 - 64 mg/L respectively as shown by M27-A2 microdilution assay, while the MIC ranges of VRG, ITG and AMB, as determined by E-test, were 0.032 - 0.094 mg/L, 0.047 - 0.5 mg/L and 0.125 - 3.0 mg/L, respectively. The MFC ranges of TRB, VRC, ITG, AMB and FLG were 0.125 - 0.5 mg/L,0.25 - 0.5 mg/L, 2.0 - 4.0 mg/L, 2.0 - 4.0 mg/L and 16 - 64 mg/L, respectively. No synergism in the acitivity against E. dermatitidis was observed for the combination of TBR with ITC or VRC. Conclusion E. dermatitidis is susceptible to TRB, ITC, AMB, and VRC, but less sensitive to both FLC and GAS.%目的 探讨临床分离的皮炎外瓶霉对6种常用抗真菌药物的敏感性.方法 参考美国临床实验室标准化研究所M27-A2方案测定特比萘芬(TRB)、伊曲康唑(ITC)、两性霉素B(AMB)、氟康唑(FLC)、伏立康唑(VRC)及卡泊芬净(CAS)对16株皮炎外瓶霉的最低抑菌浓度(MIC),同时以E-test法测定VRC、ITC和AMB对16株皮炎外瓶霉的MIC,并进一步测定每种药物的最低杀菌浓度(MFC).在此基础上,观察TRB与ITC及vRC联合应用时对皮炎外瓶霉的抗菌作用.结果 微量液基稀释法测得TRB

  15. Antifungal susceptibilities of non-Aspergillus filamentous fungi causing invasive infection in Australia: support for current antifungal guideline recommendations.

    Science.gov (United States)

    Halliday, Catriona L; Chen, Sharon C-A; Kidd, Sarah E; van Hal, Sebastian; Chapman, Belinda; Heath, Christopher H; Lee, Andie; Kennedy, Karina J; Daveson, Kathryn; Sorrell, Tania C; Morrissey, C Orla; Marriott, Deborah J; Slavin, Monica A

    2016-10-01

    Antifungal susceptibilities of non-Aspergillus filamentous fungal pathogens cannot always be inferred from their identification. Here we determined, using the Sensititre(®) YeastOne(®) YO10 panel, the in vitro activities of nine antifungal agents against 52 clinical isolates of emergent non-Aspergillus moulds representing 17 fungal groups in Australia. Isolates comprised Mucorales (n = 14), Scedosporium/Lomentospora spp. (n = 18) and a range of hyaline hyphomycetes (n = 9) and other dematiaceous fungi (n = 11). Excluding Verruconis gallopava, echinocandins demonstrated poor activity (MICs generally >8 mg/L) against these moulds. Lomentospora prolificans (n = 4) and Fusarium spp. (n = 6) demonstrated raised MICs to all antifungal drugs tested, with the lowest being to voriconazole and amphotericin B (AmB), respectively (geometric mean MICs of 3.4 mg/L and 2.2 mg/L, respectively). All Scedosporium apiospermum complex isolates (n = 14) were inhibited by voriconazole concentrations of ≤0.25 mg/L, followed by posaconazole and itraconazole at ≤1 mg/L. Posaconazole and AmB were the most active agents against the Mucorales, with MIC90 values of 1 mg/L and 2 mg/L, respectively, for Rhizopus spp. For dematiaceous fungi, all isolates were inhibited by itraconazole and posaconazole concentrations of ≤0.5 mg/L (MIC90, 0.12 mg/L and 0.25 mg/L, respectively), but voriconazole and AmB also had in vitro activity (MIC90, 0.5 mg/L and 1 mg/L, respectively). Differences in antifungal susceptibility within species and between species within genera support the need for testing individual patient isolates to guide therapy. The Sensititre(®) YeastOne(®) offers a practical alternative to the reference methodology for susceptibility testing of moulds.

  16. Antifungal activity of five species of Polygala

    Directory of Open Access Journals (Sweden)

    Susana Johann

    2011-09-01

    Full Text Available Crude extracts and fractions of five species of Polygala - P. campestris, P. cyparissias, P. paniculata, P. pulchella and P. sabulosa - were investigated for their in vitro antifungal activity against opportunistic Candida species, Cryptococcus gattii and Sporothrix schenckii with bioautographic and microdilution assays. In the bioautographic assays, the major extracts were active against the fungi tested. In the minimal concentration inhibitory (MIC assay, the hexane extract of P. paniculata and EtOAc fraction of P. sabulosa showed the best antifungal activity, with MIC values of 60 and 30 µg/mL, respectively, against C. tropicalis, C. gattii and S. schenckii. The compounds isolated from P. sabulosa prenyloxycoumarin and 1,2,3,4,5,6-hexanehexol displayed antifungal activity against S. schenckii (with MICs of 125 µg/mL and 250 µg/mL, respectively and C. gattii (both with MICs of 250 µg/mL. Rutin and aurapten isolated from P. paniculata showed antifungal activity against C. gattii with MIC values of 60 and 250 µg/mL, respectively. In the antifungal screening, few of the isolated compounds showed good antifungal inhibition. The compound α-spinasterol showed broad activity against the species tested, while rutin had the best activity with the lowest MIC values for the microorganisms tested. These two compounds may be chemically modified by the introduction of a substitute group that would alter several physico-chemical properties of the molecule, such as hydrophobicity, electronic density and steric strain.

  17. Design, synthesis and antifungal activity of novel triazole derivatives containing substituted 1,2,3-triazole-piperdine side chains.

    Science.gov (United States)

    Jiang, Zhigan; Gu, Julin; Wang, Chen; Wang, Shengzheng; Liu, Na; Jiang, Yan; Dong, Guoqiang; Wang, Yan; Liu, Yang; Yao, Jianzhong; Miao, Zhenyuan; Zhang, Wannian; Sheng, Chunquan

    2014-07-23

    Due to increasing incidence of invasive fungal infections and severe drug resistance to triazole antifungal agents, a series of novel antifungal triazoles with substituted triazole-piperidine side chains were designed and synthesized. Most of the target compounds showed good inhibitory activity against a variety of clinically important fungal pathogens. In particular, compounds 8t and 8v were highly active against Candida albicans and Cryptococcus neoformans with MIC values in the range of 0.125 μg/mL to 0.0125 μg/mL. They represent promising leads for the development of new generation of triazole antifungal agents. Molecular docking studies revealed that the target compounds interacted with CACYP51 mainly through hydrophobic and Van der Waals interactions.

  18. Antifungal, Cytotoxic, and Immunomodulatory Properties of Tea Tree Oil and Its Derivative Components: Potential Role in Management of Oral Candidosis in Cancer Patients

    OpenAIRE

    Ramage, Gordon; Milligan, Steven; Lappin, David F; Sherry, Leighann; Sweeney, Petrina; Williams, Craig; Bagg, Jeremy; Culshaw, Shauna

    2012-01-01

    Candida albicans forms oral biofilms that cause disease and are difficult to treat with conventional antifungal agents. Tea tree oil (TTO) is a natural compound with reported antimicrobial and immunomodulatory activities. The aims of the study were to evaluate the antifungal efficacy of TTO and key derivatives against C. albicans biofilms, to assess the toxicological effects of TTO on a clinically relevant oral cell line, and to investigate its impact on inflammation. TTO and its derivatives ...

  19. Antifungal, cytotoxic and immunomodulatory properties of tea tree oil and its derivative components: potential role in management of oral candidosis in cancer patients

    OpenAIRE

    Gordon eRamage; Steven eMilligan; Lappin, David F; Leighann eSherry; Petrina eSweeney; Craig eWilliams; Jeremy eBagg; Shauna eCulshaw

    2012-01-01

    Candida albicans forms oral biofilms that cause disease and are difficult to treat with conventional antifungal agents. Tea tree oil (TTO) is a natural compound with reported antimicrobial and immunomodulatory activities. The aims of the study were to evaluate the antifungal efficacy of TTO and key derivatives against C. albicans biofilms, to assess the toxicological effects of TTO on a clinically relevant oral cell line, and to investigate its impact on inflammation. TTO and its derivatives ...

  20. Scedosporium apiospermum infections and the role of combination antifungal therapy and GM-CSF: A case report and review of the literature

    Directory of Open Access Journals (Sweden)

    Chloe Goldman

    2016-03-01

    Full Text Available Scedosporium apiospermum, a ubiquitous environmental mold, is increasingly reported as causing invasive fungal disease in immunocompromised hosts. It poses a therapeutic challenge due to its intrinsic resistance to traditional antifungals and ability to recur despite demonstrating susceptibility. We present an immunocompromised patient with a cutaneous S. apiospermum infection that disseminated despite treatment with voriconazole, the drug of choice. Adding echinocandins and GM-CSF provided partial recovery, indicating a potential synergistic role of dual-antifungal and immunotherapeutic agents.

  1. Calcium signaling mediates antifungal activity of triazole drugs in the Aspergilli.

    Science.gov (United States)

    Liu, Fei-fei; Pu, Li; Zheng, Qing-qing; Zhang, Yuan-wei; Gao, Rong-sui; Xu, Xu-shi; Zhang, Shi-zhu; Lu, Ling

    2015-08-01

    Azoles are widely applied and largely effective as antifungals; however, the increasing prevalence of clinically resistant isolates has yet to be matched by approaches to improve the efficacy of antimicrobial therapy. In this study, using the model fungus Aspergillus nidulans and one of the most common human pathogen Aspergillus fumigatus as research materials, we present the evidence that calcium signaling is involved in the azole-antifungals-induced stress-response reactions. In normal media, antifungal-itraconazole (ITZ) is able to induce the [Ca(2+)]c increased sharply but the addition of calcium chelator-EGTA or BAPTA almost blocks the calcium influx responses, resulted in the dramatically decreasing of [Ca(2+)]c transient. Real-time PCR analysis verified that six-tested Ca(2+)-inducible genes-two calcium channels (cchA/midA), a calmodulin-dependent phosphatase-calcineurin (cnaA), a transcription factor-crzA, and two calcium transporters (pmrA/pmcA)-could be transiently up-regulated by adding ITZ, indicating these components are involved in the azole stress-response reaction. Defect of cnaA or crzA caused more susceptibility to azole antifungals than did single mutants or double deletions of midA and cchA. Notably, EGTA may influence Rh123 accumulation as an azole-mimicking substrate through the process of the drug absorption. In vivo studies of a Galleria mellonella model identified that the calcium chelator works as an adjunct antifungal agent with azoles for invasive aspergillosis. Most importantly, combination of ITZ and EGTA or ITZ with calcium signaling inhibitor-FK506 greatly enhances the ITZ efficacy. Thus, our study provides potential clues that specific inhibitors of calcium signaling could be clinically useful adjuncts to conventional azole antifungals in the Aspergilli.

  2. In Vitro Antifungal Susceptibility of Oral Candida Species from Iranian HIV Infected Patients

    Directory of Open Access Journals (Sweden)

    A A Khaksar

    2012-05-01

    Full Text Available Background: Oropharyngeal candidiasis and antifungal drug resistance are major problems in HIV positive patients. The increased reports of antifungal resistance and expanding therapeutic options prompted the determination of antifungal susceptibility profile of Candida species isolates in Iranian patients living with HIV/AIDS (PLWHA in the present study. Methods: One hundred fifty oral samples from Iranian HIV positive patients were obtained and cultured on CHROMagar and Sabourauds dextrose agar. All isolates were identified according to assimilation profile, germ tube, colony color and other conventional methods. Disk diffusion testing and Broth Microdilution of six antifungal agents were performed according to the methods described in CLSI. 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.

  3. Distribution and antifungal susceptibility of Candida species causing nosocomial candiduria.

    Science.gov (United States)

    Ozhak-Baysan, Betil; Ogunc, Dilara; Colak, Dilek; Ongut, Gozde; Donmez, Levent; Vural, Tumer; Gunseren, Filiz

    2012-07-01

    The aim of the study was to investigate the distribution of Candida species isolated from urine specimens of hospitalized patients in Akdeniz University Hospital, Antalya, Turkey, as well as their susceptibilities to antifungal agents. A total of 100 patients who had nosocomial candiduria between March 2003 and May 2004 at the facility were included in the study. Organisms were identified by conventional methods and the use of API ID 32C strips. Susceptibilities of the isolates to amphotericin B were determined by Etest, whereas the minimum inhibitory concentration (MIC) values of these same strains to fluconazole, voriconazole and caspofungin were assessed using the broth microdilution method. The most common species recovered was C. albicans 44% of all yeasts, followed by C. tropicalis (20%), C. glabrata (18%), C. krusei (6%), C. famata (5%), C. parapsilosis (4%), C. kefyr (2%) and C. guilliermondii (1%). A total of nine (9%) of the isolates, including five C. krusei and four C. glabrata isolates were susceptible dose-dependent (SDD) to fluconazole. In constrast, only two C. glabrata and one C. krusei isolates were resistant to this antifungal. The voriconazole MICs for all Candida isolates were ≤0.5 μg/ml, except for one C. glabrata isolate with a MIC value of 2 μg/ml. Among all isolates, 94% were susceptible to amphotericin B with MIC values of Candida urinary tract infections.

  4. Onychomycosis: Potential of Nail Lacquers in Transungual Delivery of Antifungals

    Directory of Open Access Journals (Sweden)

    Nida Akhtar

    2016-01-01

    Full Text Available Onychomycosis constitutes the most common fungal infection of the nail (skin beneath the nail bed that affects the finger as well as toe nails. It is an infection that is initiated by yeasts, dermatophytes, and nondermatophyte molds. Nail lacquers are topical solutions intended only for use on fingernails as well as toenails and have been found to be useful in the treatment of onychomycosis. Thus, in the present review an attempt has been made to focus on the treatment aspects of onychomycosis and the ungual delivery of antifungals via nail lacquer. Several patents issued on nail lacquer till date have also been discussed. Penetration efficiency was assessed by several researchers across the human nail plate to investigate the potentiality of nail lacquer based formulations. Various clinical trials have also been conducted in order to evaluate the safety and efficacy of nail lacquers in delivering antifungal agents. Thus, it can be concluded that nail lacquer based preparations are efficacious and stable formulations. These possess tremendous potential for clinical topical application to the nail bed in the treatment of onychomycosis.

  5. Cryptococcus laurentii biofilms: structure, development and antifungal drug resistance.

    Science.gov (United States)

    Ajesh, K; Sreejith, K

    2012-12-01

    A great number of fungal infections are related to biofilm formation on inert or biological surfaces, which are recalcitrant to most treatments and cause human mortality. Cryptococcus laurentii has been diagnosed as the aetiological pathogen able to cause human infections mainly in immunosuppressed patients and the spectrum of clinical manifestations ranges from skin lesions to fungaemia. The effect of temperature, pH and surface preconditioning on C. laurentii biofilm formation was determined by 2, 3-bis (2-methoxy-4-nitro-5-sulfophenyl)-5-[(phenylamino) carbonyl]-2H-tetrazolium hydroxide (XTT) reduction assay. Scanning electron microscopic (SEM) analysis of C. laurentii biofilms demonstrated surface topographies of profuse growth and dense colonization with extensive polymeric substances around the cells. In this study, we determined the activity of amphotericin B, itraconazole and fluconazole against C. laurentii free-living cells and biofilms. The activity of antifungals tested was greater against free-living cells, but sessile cells fell into the resistant range for these antifungal agents. Extracellular polymeric substances (EPS), comprising the matrix of C. laurentii biofilms, were isolated by ultrasonication. Fourier transform infrared spectroscopy (FT-IR) was performed with ethanol-precipitated and dried samples. Also, the multielement analysis of the EPS was performed by inductively coupled plasma optical emission spectroscopy (ICP-OES).

  6. 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

  7. Conditions influencing the in vitro antifungal activity of lactoferrin combined with antimycotics against clinical isolates of Candida - Impact on the development of buccal preparations of lactoferrin

    NARCIS (Netherlands)

    Kuipers, ME; Beljaars, L; Van Beek, N; De Vries, HG; Heegsma, J; Van Den Berg, JJM; Meijer, DKF; Swart, PJ

    2002-01-01

    Lactoferrin, an iron-binding glycoprotein, is a potential agent for the treatment of oropharyngeal Candidiasis. The aim of the present study was to test the capability of lactoferrin, combined or not combined with conventional antifungal agents, to inhibit the growth of different Candida species und

  8. In vitro antifungal susceptibility profiles of Cryptococcus species isolated from HIV-associated cryptococcal meningitis patients in Zimbabwe.

    Science.gov (United States)

    Nyazika, Tinashe K; Herkert, Patricia F; Hagen, Ferry; Mateveke, Kudzanai; Robertson, Valerie J; Meis, Jacques F

    2016-11-01

    Cryptococcus neoformans is the leading cause of cryptococcosis in HIV-infected subjects worldwide. Treatment of cryptococcosis is based on amphotericin B, flucytosine, and fluconazole. In Zimbabwe, little is known about antifungal susceptibility of Cryptococcus. Sixty-eight genotyped Cryptococcus isolates were tested for antifungal profiles. Amphotericin B, isavuconazole, and voriconazole showed higher activity than other triazoles. Fluconazole and flucytosine were less effective, with geometric mean MICs of 2.24 and 2.67mg/L for C. neoformans AFLP1/VNI, 1.38 and 1.53mg/L for C. neoformans AFLP1A/VNB/VNII and AFLP1B/VNII, and 1.85 and 0.68mg/L for Cryptococcus tetragattii, respectively. A significant difference between flucytosine geometric mean MICs of C. neoformans and C. tetragattii was observed (P=0.0002). The majority of isolates (n=66/68; 97.1%) had a wild-type MIC phenotype of all antifungal agents. This study demonstrates a favorable situation with respect to the tested antifungals agents. Continued surveillance of antifungal susceptibility profiles is important due to the high burden of cryptococcosis in Africa.

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

    Directory of Open Access Journals (Sweden)

    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.

  10. Antifungal efficacy of three medicinal plants Glycyrrhiza glabra, Ficus religiosa, and Plantago major against oral Candida albicans: A comparative analysis

    Directory of Open Access Journals (Sweden)

    Hunny Sharma

    2016-01-01

    Conclusion: G. glabra, F. religiosa, and P. major showed acceptable potency against C. albicans (ATCC 66027 comparable to that of synthetic antifungal agents. However, further studies should be undertaken to affirm the same and test their efficacy in different concentrations and clinical utility.

  11. In vitro resistance of clinical Fusarium species to amphotericin B and voriconazole using the EUCAST antifungal susceptibility method

    NARCIS (Netherlands)

    Taj-Aldeen, Saad J; Salah, Husam; Al-Hatmi, Abdullah M S; Hamed, Manal; Theelen, Bart; van Diepeningen, Anne D; Boekhout, Teun; Lass-Flörl, Cornelia

    2016-01-01

    Susceptibility testing using the EUCAST-AFST method against 39 clinical Fusarium strains consecutively collected from local and invasive infections during the last 10years assessed the in vitro activities of amphotericin B (AmB) and triazole antifungal agents. In addition, the susceptibility pattern

  12. Topical antifungal-corticosteroid combination therapy for the treatment of superficial mycoses: conclusions of an expert panel meeting.

    Science.gov (United States)

    Schaller, Martin; Friedrich, Markus; Papini, Manuela; Pujol, Ramon M; Veraldi, Stefano

    2016-06-01

    Superficial fungal infections affect 20-25% of people worldwide and can cause considerable morbidity, particularly if an inflammatory component is present. As superficial fungal infections can be diverse, the treatment should be tailored to the individual needs of the patient and several factors should be taken into account when deciding on the most appropriate treatment option. These include the type, location and surface area of the infection, patient age, degree of inflammation and underlying comorbidities. Although several meta-analyses have shown that there are no significant differences between the numerous available topical antifungal agents with regard to mycological cure, agents differ in their specific intrinsic properties, which can affect their clinical use. The addition of a corticosteroid to an antifungal agent at the initiation of treatment can attenuate the inflammatory symptoms of the infection and is thought to increase patient compliance, reduce the risk of bacterial superinfection and enhance the efficacy of the antifungal agent. However, incorrect use of antifungal-corticosteroid therapy may be associated with treatment failure and adverse effects. This review summarises available treatment options for superficial fungal infections and provides general treatment recommendations based on the consensus outcomes of an Expert Panel meeting on the topical treatment of superficial mycoses.

  13. In vitro evaluation of antifungal activity of monolaurin against Candida albicans biofilms.

    Science.gov (United States)

    Seleem, Dalia; Chen, Emily; Benso, Bruna; Pardi, Vanessa; Murata, Ramiro M

    2016-01-01

    Monolaurin (also known as glycerol monolaurate) is a natural compound found in coconut oil and is known for its protective biological activities as an antimicrobial agent. The nature of oral candidiasis and the increased antifungal resistance demand the search for novel antifungal therapeutic agents. In this study, we examine the antifungal activity of monolaurin against Candida albicans biofilms (strain ATCC:SC5314/MYA2876) in vitro and investigate whether monolaurin can alter gene expression of host inflammatory cytokines, IL-1α and IL-1β. In a co-culture model, oral fibroblast cells were cultured simultaneously with C. albicans for 24 hrs followed by the exposure to treatments of monolaurin (3.9-2,500 µM), positive control fluconazole (32.2 µM), and vehicle control group (1% ethanol), which was a model used to evaluate the cytotoxicity of monolaurin on fibroblasts as well as to analyze morphological characteristics of biofilms through fluorescence microscopy. In addition, the co-culture model was used for RNA extraction of oral fibroblasts to assess gene expression of host inflammatory cytokines, using quantitative real-time PCR. Our results showed the MIC and MFC of monolaurin were in the range 62.5-125 µM and 125-250 µM, respectively. Biofilm antifungal assay showed significant reduction in Log (CFU/ml) of biofilms treated with 1,250 and 2,500 µM of 1-monolaurin when compared to the control groups . There was also a significant down-regulation of IL-1α and IL-1β in the co-culture treated with monolaurin. It can be concluded that monolaurin has a potential antifungal activity against C. albicans and can modulate the pro-inflammatory response of the host.

  14. In vitro evaluation of antifungal activity of monolaurin against Candida albicans biofilms

    Directory of Open Access Journals (Sweden)

    Dalia Seleem

    2016-06-01

    Full Text Available Monolaurin (also known as glycerol monolaurate is a natural compound found in coconut oil and is known for its protective biological activities as an antimicrobial agent. The nature of oral candidiasis and the increased antifungal resistance demand the search for novel antifungal therapeutic agents. In this study, we examine the antifungal activity of monolaurin against Candida albicans biofilms (strain ATCC:SC5314/MYA2876 in vitro and investigate whether monolaurin can alter gene expression of host inflammatory cytokines, IL-1α and IL-1β. In a co-culture model, oral fibroblast cells were cultured simultaneously with C. albicans for 24 hrs followed by the exposure to treatments of monolaurin (3.9–2,500 µM, positive control fluconazole (32.2 µM, and vehicle control group (1% ethanol, which was a model used to evaluate the cytotoxicity of monolaurin on fibroblasts as well as to analyze morphological characteristics of biofilms through fluorescence microscopy. In addition, the co-culture model was used for RNA extraction of oral fibroblasts to assess gene expression of host inflammatory cytokines, using quantitative real-time PCR. Our results showed the MIC and MFC of monolaurin were in the range 62.5–125 µM and 125–250 µM, respectively. Biofilm antifungal assay showed significant reduction in Log (CFU/ml of biofilms treated with 1,250 and 2,500 µM of 1-monolaurin when compared to the control groups . There was also a significant down-regulation of IL-1α and IL-1β in the co-culture treated with monolaurin. It can be concluded that monolaurin has a potential antifungal activity against C. albicans and can modulate the pro-inflammatory response of the host.

  15. In Vitro and In Vivo Antifungal Activity of Lichochalcone-A against Candida albicans Biofilms

    Science.gov (United States)

    Seleem, Dalia; Benso, Bruna; Noguti, Juliana; Pardi, Vanessa; Murata, Ramiro Mendonça

    2016-01-01

    Oral candidiasis (OC) is an opportunistic fungal infection with high prevalence among immunocompromised patients. Candida albicans is the most common fungal pathogen responsible for OC, often manifested in denture stomatitis and oral thrush. Virulence factors, such as biofilms formation and secretion of proteolytic enzymes, are key components in the pathogenicity of C. albicans. Given the limited number of available antifungal therapies and the increase in antifungal resistance, demand the search for new safe and effective antifungal treatments. Lichochalcone-A is a polyphenol natural compound, known for its broad protective activities, as an antimicrobial agent. In this study, we investigated the antifungal activity of lichochalcone-A against C. albicans biofilms both in vitro and in vivo. Lichochalcone-A (625 μM; equivalent to 10x MIC) significantly reduced C. albicans (MYA 2876) biofilm growth compared to the vehicle control group (1% ethanol), as indicated by the reduction in the colony formation unit (CFU)/ml/g of biofilm dry weight. Furthermore, proteolytic enzymatic activities of proteinases and phospholipases, secreted by C. albicans were significantly decreased in the lichochalcone-A treated biofilms. In vivo model utilized longitudinal imaging of OC fungal load using a bioluminescent-engineered C. albicans (SKCa23-ActgLUC) and coelenterazine substrate. Mice treated with lichochalcone-A topical treatments exhibited a significant reduction in total photon flux over 4 and 5 days post-infection. Similarly, ex vivo analysis of tongue samples, showed a significant decrease in CFU/ml/mg in tongue tissue sample of lichochalcone-A treated group, which suggest the potential of lichochalcone-A as a novel antifungal agent for future clinical use. PMID:27284694

  16. In vitro evaluation of antifungal activity of monolaurin against Candida albicans biofilms

    Science.gov (United States)

    Benso, Bruna; Pardi, Vanessa

    2016-01-01

    Monolaurin (also known as glycerol monolaurate) is a natural compound found in coconut oil and is known for its protective biological activities as an antimicrobial agent. The nature of oral candidiasis and the increased antifungal resistance demand the search for novel antifungal therapeutic agents. In this study, we examine the antifungal activity of monolaurin against Candida albicans biofilms (strain ATCC:SC5314/MYA2876) in vitro and investigate whether monolaurin can alter gene expression of host inflammatory cytokines, IL-1α and IL-1β. In a co-culture model, oral fibroblast cells were cultured simultaneously with C. albicans for 24 hrs followed by the exposure to treatments of monolaurin (3.9–2,500 µM), positive control fluconazole (32.2 µM), and vehicle control group (1% ethanol), which was a model used to evaluate the cytotoxicity of monolaurin on fibroblasts as well as to analyze morphological characteristics of biofilms through fluorescence microscopy. In addition, the co-culture model was used for RNA extraction of oral fibroblasts to assess gene expression of host inflammatory cytokines, using quantitative real-time PCR. Our results showed the MIC and MFC of monolaurin were in the range 62.5–125 µM and 125–250 µM, respectively. Biofilm antifungal assay showed significant reduction in Log (CFU/ml) of biofilms treated with 1,250 and 2,500 µM of 1-monolaurin when compared to the control groups . There was also a significant down-regulation of IL-1α and IL-1β in the co-culture treated with monolaurin. It can be concluded that monolaurin has a potential antifungal activity against C. albicans and can modulate the pro-inflammatory response of the host. PMID:27366648

  17. Anti-fungal activity of crude extracts and essential oil of Moringa oleifera Lam.

    Science.gov (United States)

    Chuang, Ping-Hsien; Lee, Chi-Wei; Chou, Jia-Ying; Murugan, M; Shieh, Bor-Jinn; Chen, Hueih-Min

    2007-01-01

    Investigations were carried out to evaluate the therapeutic properties of the seeds and leaves of Moringa oleifera Lam as herbal medicines. Ethanol extracts showed anti-fungal activities in vitro against dermatophytes such as Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis. GC-MS analysis of the chemical composition of the essential oil from leaves showed a total of 44 compounds. Isolated extracts could be of use for the future development of anti-skin disease agents.

  18. Candida species isolated from urine specimens and antifungal susceptibility in hospitalized patients

    Directory of Open Access Journals (Sweden)

    Mustafa Altay Atalay

    2014-01-01

    [¤]CONCLUSION[|] In our hospital, C. albicans was the most frequently isolated Candida species from urine cultures, however, C. glabrata was found as the second most frequent species. As a result, in parallel to the increase of patient population who are at risk for Candida infections, the necessity of doing epidemiological studies for identification of species and susceptibility tests including new antifungal agents was concluded.[¤

  19. Antifungal susceptibility analysis of berberine, baicalin, eugenol and curcumin on Candida albicans

    Institute of Scientific and Technical Information of China (English)

    Wu Jianhua; Wen Hai

    2009-01-01

    Objective: To analyze the antifungal effects of Chinese herb monomers, i.e. berberine, baicalin, eugenol and curcumin, on Candida albicans. Methods: After Candida albicans strain Y01-09 was incubated for 48 h in YEPD broth which contained different concentrations of Chinese herb components, the cell cycle, fluorescent intensity and the size of cell volume were detected by flow cytometry. Results: The 4 Chinese herb monomers could affect the cell cycle of Candida albicans in different ranges. The ratio of cells in S-G2-M period decreased as the agents concentration increased, indicating that the cell division was inhibited. The fluorescent intensity of Candida albicans cells became weaker after being incubated, which reflected the loss of DNA fragments. The higher the concentration was, the weaker the fluorescent intensity became. The cell size, cell diopter and particle size changed much as the agents concentration increased. Conclusion: Chinese herb monomers play the antifungal role in inhibiting cell division. FCM could be used to determine the susceptibility of antifungal agents.

  20. Rapid identification of antifungal compounds against Exserohilum rostratum using high throughput drug repurposing screens.

    Directory of Open Access Journals (Sweden)

    Wei Sun

    Full Text Available A recent large outbreak of fungal infections by Exserohilum rostratum from contaminated compounding solutions has highlighted the need to rapidly screen available pharmaceuticals that could be useful in therapy. The present study utilized two newly-developed high throughput assays to screen approved drugs and pharmaceutically active compounds for identification of potential antifungal agents. Several known drugs were found that have potent effects against E. rostratum including the triazole antifungal posaconazole. Posaconazole is likely to be effective against infections involving septic joints and may provide an alternative for refractory central nervous system infections. The anti-E. rostratum activities of several other drugs including bithionol (an anti-parasitic drug, tacrolimus (an immunosuppressive agent and floxuridine (an antimetabolite were also identified from the drug repurposing screens. In addition, activities of other potential antifungal agents against E. rostratum were excluded, which may avoid unnecessary therapeutic trials and reveals the limited therapeutic alternatives for this outbreak. In summary, this study has demonstrated that drug repurposing screens can be quickly conducted within a useful time-frame. This would allow clinical implementation of identified alternative therapeutics and should be considered as part of the initial public health response to new outbreaks or rapidly-emerging microbial pathogens.

  1. In vitro antifungal susceptibility of Malassezia pachydermatis strains isolated from dogs with chronic and acute otitis externa.

    Science.gov (United States)

    Chiavassa, E; Tizzani, P; Peano, A

    2014-10-01

    Malassezia pachydermatis is a yeast that is frequently involved as a secondary/perpetuating factor in canine otitis externa. Topical therapies with different antifungal agents, mainly azole compounds, are generally successful in controlling the yeast overgrowth, but treatment failure and rapid recurrences are common. This study compared the in vitro antifungal susceptibility of M. pachydermatis isolates obtained from chronic and acute cases of otitis externa. The aim was to assess the possible onset of resistance mechanisms in isolates involved in long-lasting episodes with poor response to treatment. We evaluated the in vitro susceptibility to miconazole (MCZ) and clotrimazole (CTZ) of 42 isolates of M. pachydermatis obtained from dogs with chronic (group A, n = 25) and acute otitis (group B, n = 17), using a modified CLSI M27-A3 microdilution method. All isolates were inhibited by the antifungal agents employed, but Malassezia isolates from group A were significantly associated with higher minimum inhibitory concentration (MIC) values for both agents (Median MIC values: MCZ group A 2 µg/ml, group B 1 µg/ml; CTZ group A 8 µg/ml, group B 4 µg/ml). These findings prove that these isolates had a reduced in vitro susceptibility to the antifungal agents tested. However, it is unlikely that this could have any influence on the outcome of a topical treatment. Indeed, marketed products include concentrations of the tested agents that largely exceed even the highest MICs found in this study (in most cases at least 1,000 × the MIC, or greater). In conclusion, this study suggests that isolates of M. pachydermatis involved in chronic cases of canine external otitis and exposed to repeated antifungal treatments are unlikely to develop mechanisms of resistance of clinical relevance.

  2. Antibacterial and antifungal activities of the endemic species Glaucium vitellinum Boiss. and Buhse

    Directory of Open Access Journals (Sweden)

    Mina Mehrara

    2014-12-01

    Full Text Available Objectives: Belonging to Papaveraceae family, Glaucium vitellinum is one of the Persian endemic plants which has not been investigated biologically. The present paper focused on the assessment of the antibacterial and antifungal activities of the total methanol extract and alkaloid sub-fraction of the flowering aerial parts of G. vitellinum. Materials and Methods: The antibacterial and antifungal activities were investigated using cup plate method and disc diffusion assay, respectively. The MIC values of the active samples were determined using micro plate dilution method. Results: The crude extract and alkaloid sub-fraction of G. vitellinum had significant inhibition activity on the growth of S. aureus and S. typhi. From antifungal assay, it is concluded that only the yeast C. albicans, showed a high sensitivity to the extract and especially to the related alkaloid sub-fraction. Conclusions: Regarding the results, G. vitellinum could be employed as a natural antibacterial and antifungal agent against S. aureus, S. typhi, and C. albicans, respectively. Moreover, based on the results of this study, further in vivo and ex vivo confirmatory tests for total methanol extract and alkaloid sub-fraction are recommended.

  3. Antifungal Susceptibility Analysis of Clinical Isolates of Candida parapsilosis in Iran

    Directory of Open Access Journals (Sweden)

    Ensieh LOTFALI

    2016-03-01

    Full Text Available Background: Candida parapsilosis is an emergent agent of invasive fungal infections. This yeast is one of the five most widespread yeasts concerned in invasive candidiasis.C. parapsilosis stands out as the second most common yeast species isolated from patients with bloodstream infections especially in neonates with catheter.Recently several reports suggested that its reduced susceptibility to azoles and polyene might become a cause for clinical concern, although C. parapsilosis is not believed to be intensely prone to the development of antifungal resistance.Methods: In the present report, One hundred and twenty clinical isolates of C. parapsilosis complex were identified and differentiated by using PCR-RFLP analysis. The isolates were then analyzed to determine their susceptibility profile to fluconazole (FLU, itraconazole (ITC and amphotericin B. The minimum inhibitory concentration (MIC results were analyzed according to the standard CLSI guide.Results: All of isolates were identified as C. parapsilosis. No C. metapsilosis and C. orthopsilosis strains were found. Evaluation of the antifungal susceptibility profile showed that only three (2.5% C. parapsilosis were resistant to fluconazole, three (2.5% C. parapsilosis were resistant to itraconazole and two (1.7% C. parapsilosis were amphotericin B resistant.Conclusion: Profiles in clinical isolates of C. parapsilosis can provide important information for the control of antifungal resistance as well as distribution and susceptibility profiles in populations. Keywords: Candida parapsilosis, Antifungal susceptibility, Resistant, Iran

  4. Endophytic fungus strain 28 isolated from Houttuynia cordata possesses wide-spectrum antifungal activity

    Directory of Open Access Journals (Sweden)

    Feng Pan

    2016-06-01

    Full Text Available Abstract The aim of this paper is to identify and investigate an endophytic fungus (strain 28 that was isolated from Houttuynia cordata Thunb, a famous and widely-used Traditional Chinese Medicine. Based on morphological methods and a phylogenetic analysis of ITS sequences, this strain was identified as Chaetomium globosum. An antifungal activity bioassay demonstrated that the crude ethyl acetate (EtOAc extracts of strain 28 had a wide antifungal spectrum and strong antimicrobial activity, particularly against Exserohilum turcicum (Pass. Leonard et Suggs, Botrytis cinerea persoon and Botrytis cinerea Pers. ex Fr. Furthermore, the fermentation conditions, extraction method and the heat stability of antifungal substances from strain 28 were also studied. The results showed that optimal antifungal activity can be obtained with the following parameters: using potato dextrose broth (PDB as the base culture medium, fermentation for 4–8 d (initial pH: 7.5, followed by extraction with EtOAc. The extract was stable at temperatures up to 80 °C. This is the first report on the isolation of endophytic C. globosum from H. cordata to identify potential alternative biocontrol agents that could provide new opportunities for practical applications involving H. cordata.

  5. [In vitro activities of antifungal drugs against clinical isolates of Trichophyton tonsurans].

    Science.gov (United States)

    Koga, Hiroyasu; Nanjoh, Yasuko; Inoue, Kazuyoshi; Makimura, Koichi; Tsuboi, Ryoji

    2006-01-01

    To determine drug susceptibility of Trichophyton tonsurans endemic in Japan, in vitro MICs of antifungal drugs against a total of 10 clinical isolates of T. tonsurans collected from dermatophytosis patients were measured by the agar dilution method and the broth microdilution method. The agar dilution method was not appropriate as the growth of T. tonsurans on the agar medium was too slow to determine drug activity, while the broth microdilution method was thought to be an appropriate method for this study. The MIC90 values determined by the broth microdilution method for terbinafine, itraconazole, miconazole and ketoconazole were 0.013, 0.1, 0.8 and 0.4 microg/ml, respectively. Meanwhile, the MIC90 values of lanoconazole and luliconazole, known to be antifungal drugs potent against dermatomycosis, were 0.00078 and 0.00039 microg/ ml, respectively. The drug susceptibility of these T. tonsurans isolates to the aforementioned antifungal drugs was found to be on a similar level with that of T. mentagrophytes and T. rubrum, major causative agents of dermatomycosis. The results also demonstrated the strong antifungal activity of lanoconazole and luliconazole against T. tonsurans.

  6. Radiation-induced mutagenesis of antifungal metabolite producing bacillus sp. HKA-17

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Young Keun; Senthilkumar, M. [Korea Atomic Energy Research Institute, Jeongeup (Korea, Republic of)

    2009-09-15

    Bacillus sp. Strain HKA-17, isolated from the surface sterilized root nodule of Glycine max, inhibited several fungal plant pathogens. It produced a diffusible extracellular antifungal metabolite that was extracted with n-butanol. The crude extract was purified through Superdex{sup TM} 75 10/300 GL FPLC column. FT-IR spectrum of the FPLC purified-antifungal metabolite confirmed the presence of peptide and glycosidic bonds in its structure. Gamma induced mutagenesis of HKA-17 was carried out at an LD{sub 99} dose (8.46 kGy) to generate a mutant library. By screening the mutant library through a duel plate assay with Alternaria alternata, we selected one mutant with enhanced biocontrol activity (HKA-17e1) and two defective mutants (HKA-17d1 and HKA-17d2). Overproducing mutant recorded the largest inhibition zone (16.25 {+-} 0.86 mm) compared to any other mutant clone as well as wild type, and could be used as a potential biocontrol agent for plant disease suppression. The effect of HKA-17 antifungal metabolite on hyphal morphology was clearly demonstrated through scanning electron microscopy. The crude extract of defective mutant HKA-17 d1 did not induce any changes in hyphal morphology of A. alternata. However, antifungal metabolites of HKA-17 induced abnormal hyphal structures such as hyphal shrivelling, the bulging and swelling of intercalary cells, fragmentation, and cell lysis.

  7. Antifungal activity of natural compounds against Candida species isolated from HIV-positive patients

    Institute of Scientific and Technical Information of China (English)

    Dbora Oro; Andria Heissler; Eliandra Mirlei Rossi; Diane Scapin; Patrcia da Silva Malheiros; Everton Boff

    2015-01-01

    To evaluate the antifungal effect of Cinnamomum zeylanicum (C. zeylanicum) and Melaleuca alternifolia essential oils and honey against strains of Candida sp. from HIV-positive patients in order to subsidize new therapeutic strategies for candidiasis. Methods: The study evaluated the antifungal effect of natural antimicrobials against 30 strains of Candida sp. isolated from oral cavities in HIV-infected patients. Then, they were compared to the action of fluconazole and amphotericin B. Antifungal susceptibility was evaluated by the broth macrodilution technique and the minimum inhibitory concentration and the minimum fungicidal concentration were determined. Results: Among all antifungals evaluated in this study, amphotericin B was the one showing the best results; however, all compounds studied here showed inhibitory activities against isolates of Candida sp. Honey (0.031 3 to 64 μg/mL) demonstrated fungistatic activity inhibiting 70% of the isolates. C. zeylanicum essential oil (0.0313 to 64 μg/mL) inhibited 93.3% of the Candida strains and Melaleuca alternifolia essential oil (0.0313 to 64 μg/mL) was able to inhibit 73.3% of them. Conclusions: Therefore, all natural compounds evaluated in this study, especially C. zeylanicum essential oil, may become promising agents for oral candidiasis therapy including in HIV-positive patients.

  8. OTYPIC CHARACTERIZATION AND ANTIFUNGAL SUSCEPTIBILITY PATTERN OF CANDIDA SP ISOLATED FROM A TERTIARY CARE CENTER

    Directory of Open Access Journals (Sweden)

    Rudramurthy

    2014-02-01

    Full Text Available ACT: Candida , a yeast like ubiquitous fungus , is an endogenous species which produces commonest fungal infection; Candidiasis. Resistance to antifungal agents is an alarming sign for the emerging common nosocomial candidiasis. MATERIALS AND METHODS: Various types of specimens we re collected from the c linically suspected cases of candidiasis. Isolation and characterization of candida sp . was done by standard procedures. Antifungal susceptibility was done by disc diffusion method. RESULT: The candida was isolated from various clinical specimens , vaginal swab (24.66% , skin scraping (13.33% oral swabs (12.66% , ear swabs ( 11.33% , nail scraping (10% , and pus from diabetes foot ulcer and post - operative wound infection ( 8% , sputum ( 6% , urine (4.66% , stool ( 4% , blood ( 2.66% , and eye swabs ( 2.66%. Amon g different species of candida isolated C.albicans was the predominant species (79.33% followed by C tropicalis (19.33% and C.Guilliermondii (1.33%. Antifungal resistance of different species of candida was higher to fluconazole . The least resistance wa s seen with amphotericin - B (1.33%. CONCLUSION: The increased isolation of candida species and development of resistance to commonly used antifungal drugs requires careful interpretation and the in vitro susceptibility testing. This facilitates better pat ient care.

  9. In Vitro Antifungal Activity of Sanguinarine and Chelerythrine Derivatives against Phytopathogenic Fungi

    Directory of Open Access Journals (Sweden)

    Yan-Ni Ma

    2012-11-01

    Full Text Available In order to understand the antifungal activity of some derivatives of sanguinarine (S and chelerythrine (C and their structure-activity relationships, sixteen derivatives of S and C were prepared and evaluated for in vitro antifungal activity against seven phytopathogenic fungi by the mycelial growth rate method. The results showed that S, C and their 6-alkoxy dihydro derivatives S1–S4, C1–C4 and 6-cyanodihydro derivatives S5, C5 showed significant antifungal activity at 100 µg/mL against all the tested fungi. For most tested fungi, the median effective concentrations of S, S1, C and C1 were in a range of 14–50 µg/mL. The structure-activity relationship showed that the C=N+ moiety was the determinant for the antifungal activity of S and C. S1–S5 and C1–C5 could be considered as the precursors of S and C, respectively. Thus, the present results strongly suggested that S and C or their derivatives S1–S5 and C1–C5 should be considered as good lead compounds or model molecules to develop new anti-phytopathogenic fungal agents.

  10. Antifungal activity of natural compounds against Candida species isolated from HIV-positive patients

    Institute of Scientific and Technical Information of China (English)

    Débora; Oro; Andréia; Heissler; Eliandra; Mirlei; Rossi; Diane; Scapin; Patrícia; da; Silva; Malheiros; Everton; Boff

    2015-01-01

    Objective: To evaluate the antifungal effect of Cinnamomum zeylanicum(C. zeylanicum) and Melaleuca alternifolia essential oils and honey against strains of Candida sp. from HIV-positive patients in order to subsidize new therapeutic strategies for candidiasis.Methods: The study evaluated the antifungal effect of natural antimicrobials against 30 strains of Candida sp. isolated from oral cavities in HIV-infected patients. Then, they were compared to the action of fl uconazole and amphotericin B. Antifungal susceptibility was evaluated by the broth macrodilution technique and the minimum inhibitory concentration and the minimum fungicidal concentration were determined.Results: Among all antifungals evaluated in this study, amphotericin B was the one showing the best results; however, all compounds studied here showed inhibitory activities against isolates of Candida sp. Honey(0.031 3 to 64 μg/m L) demonstrated fungistatic activity inhibiting 70% of the isolates. C. zeylanicum essential oil(0.031 3 to 64 μg/m L) inhibited 93.3% of the Candida strains and Melaleuca alternifolia essential oil(0.031 3 to 64 μg/m L) was able to inhibit 73.3% of them.Conclusions: Therefore, all natural compounds evaluated in this study, especially C. zeylanicum essential oil, may become promising agents for oral candidiasis therapy including in HIV-positive patients.

  11. Characterization of three antifungal calcite-forming bacteria, Arthrobacter nicotianae KNUC2100, Bacillus thuringiensis KNUC2103, and Stenotrophomonas maltophilia KNUC2106, derived from the Korean islands, Dokdo and their application on mortar.

    Science.gov (United States)

    Park, Jong-Myong; Park, Sung-Jin; Ghim, Sa-Youl

    2013-09-28

    Crack remediation on the surface of cement mortar using microbiological calcium carbonate (CaCO3) precipitation (MICP) has been investigated as a microbial sealing agent on construction materials. However, MICP research has never acknowledged the antifungal properties of calcite-forming bacteria (CFB). Since fungal colonization on concrete surfaces can trigger biodeterioration processes, fungi on concrete buildings have to be prevented. Therefore, to develop a microbial sealing agent that has antifungal properties to remediate cement cracks without deteriorative fungal colonization, we introduced an antifungal CFB isolated from oceanic islands (Dokdo islands, territory of South Korea, located at the edge of the East Sea in Korea.). The isolation of CFB was done using B4 or urea-CaCl2 media. Furthermore, antifungal assays were done using the pairing culture and disk diffusion methods. Five isolated CFB showed CaCO3 precipitation and antifungal activities against deteriorative fungal strains. Subsequently, five candidate bacteria were identified using 16S rDNA sequence analysis. Crack remediation, fungi growth inhibition, and water permeability reduction of antifungal CFB-treated cement surfaces were tested. All antifungal CFB showed crack remediation abilities, but only three strains (KNUC2100, 2103, and 2106) reduced the water permeability. Furthermore, these three strains showed fungi growth inhibition. This paper is the first application research of CFB that have antifungal activity, for an eco-friendly improvement of construction materials.

  12. DFT vibrational assignments, in vitro antifungal activity, genotoxic and acute toxicity determinations of the [Zn(phen)2(cnge)(H2O)](NO3)2·H2O complex

    Science.gov (United States)

    Martínez Medina, Juan J.; Torres, Carola A.; Alegre, Walter S.; Franca, Carlos A.; López Tévez, Libertad L.; Ferrer, Evelina G.; Okulik, Nora B.; Williams, Patricia A. M.

    2015-11-01

    Calculations based on density functional methods were carried out for the [Zn(phen)2(cnge)(H2O)](NO3)2·H2O complex taking into account the presence of two different conformers for the cyanoguanidine ligand. The calculated geometrical parameters and the vibrational IR and Raman spectra were in agreement with the experimental data. On the other hand, the activities of the complex, the ligands and the metal against fungal strains have been measured. The complexation increased the antifungal activity of the metal and the ligand cyanoguanidine, and slightly decreased the antifungal activity of the ligand 1,10-phenanthroline against Candida albicans, C. albicans ATCC 10231 and Candida krusei (not against the others strains of Candida). The ligand 1,10-phenanthroline and the zinc complex showed in some cases higher activity than the common antifungal drug fluconazole. The complexation also increased the post-antifungal effect in the tested strains, except for Candida parapsilosis, even with a better efficiency than those of some conventional antifungal agents. Antifungal studies were coupled with safety evaluations using the Artemia salina and the Ames tests. The zinc complex behaved as a non-mutagenic and non-toxic compound at the tested concentrations. Moreover, the zinc complex could be safer than the ligand when used as an antifungal agent. Therefore, the interaction of zinc(II) with N-containing ligands may provide a promising strategy for the development of novel and more secure drugs with antifungal activity.

  13. Design,Synthesis and Antifungal Activity of Novel Triazole Derivatives

    Institute of Scientific and Technical Information of China (English)

    Chun Quan SHENG; Wan Nian ZHANG; Hai Tao JI; Yun Long SONG; Min ZHANG; You Jun ZHOU; Jia Guo LU; Jü ZHU

    2004-01-01

    Twenty-one 1-(1H-1,2,4-triazolyl)-2-(2,4-diflurophenyl)-3-(4-substituted-1- piperazinyl)-2-propanol derivatives were designed and synthesized,on the basis of the active site of lanosterol 14(-demethylase.In vitro antifungal activities showed that some of the target compounds had higher antifungal activity and broader antifungal spectrum than fluconazole.

  14. Human mycoses and advances in antifungal therapy.

    Science.gov (United States)

    Fromtling, R A

    2001-04-01

    The 11th Focus on Fungal Infections meeting was held in Washington, D.C., U.S.A., March 1416, 2001. At the conference, there were well-attended sessions that focused on the pathogenesis and therapy of fungal disease. This report focuses on new information on fungal incidence and pathogenesis as well as on the in vitro and clinical experience of established antifungal drugs (fluconazole, itraconazole, amphotericin B, liposomal formulations of amphotericin B, terbinafine) and the newer antifungal compounds approved for use (e.g., caspofungin) and in development (the new-generation azoles: voriconazole, posaconazole, ravuconazole, and the candins, micafungin and anidulafungin).

  15. Microscopic Evaluation, Molecular Identification, Antifungal Susceptibility, and Clinical Outcomes in Fusarium, Aspergillus and, Dematiaceous Keratitis

    Directory of Open Access Journals (Sweden)

    Devarshi U. Gajjar

    2013-01-01

    Full Text Available Purpose. Fusarium, Aspergillus, and Dematiaceous are the most common fungal species causing keratitis in tropical countries. Herein we report a prospective study on fungal keratitis caused by these three fungal species. Methodology. A prospective investigation was undertaken to evaluate eyes with presumed fungal keratitis. All the fungal isolates (n=73 obtained from keratitis infections were identified using morphological and microscopic characters. Molecular identification using sequencing of the ITS region and antifungal susceptibility tests using microdilution method were done. The final clinical outcome was evaluated in terms of the time taken for resolution of keratitis and the final visual outcome. The results were analyzed after segregating the cases into three groups, namely, Fusarium, Aspergillus, and Dematiaceous keratitis. Results. Diagnosis of fungal keratitis was established in 73 (35.9% cases out of 208 cases. The spectra of fungi isolated were Fusarium spp. (26.6%, Aspergillus spp. (21.6%, and Dematiaceous fungi (11.6%. The sequence of the ITS region could identify the Fusarium and Aspergillus species at the species complex level, and the Dematiaceous isolates were accurately identified. Using antifungal agents such as fluconazole, natamycin, amphotericin B, and itraconazole, the minimum inhibitory concentrations (MICs for Fusarium spp. were >32 μg/mL, 4–8 μg/mL, 0.5–1 μg/mL, and >32 μg/mL, respectively. Antifungal susceptibility data showed that Curvularia spp. was highly resistant to all the antifungal agents. Overall, natamycin and amphotericin B were found to be the most effective antifungal agents. The comparative clinical outcomes in all cases showed that the healing response in terms of visual acuity of the Dematiaceous group was significantly good when compared with the Fusarium and Aspergillus groups (P<0.05. The time required for healing in the Fusarium group was statistically significantly less when

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

    Directory of Open Access Journals (Sweden)

    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.

  17. Antifungal activity of extracts from Atacama Desert fungi againstParacoccidioides brasiliensis and identification ofAspergillus felis as a promising source of natural bioactive compounds

    Directory of Open Access Journals (Sweden)

    Graziele Mendes

    2016-03-01

    Full Text Available Fungi of the genus Paracoccidioides are responsible for paracoccidioidomycosis. The occurrence of drug toxicity and relapse in this disease justify the development of new antifungal agents. Compounds extracted from fungal extract have showing antifungal activity. Extracts of 78 fungi isolated from rocks of the Atacama Desert were tested in a microdilution assay against Paracoccidioides brasiliensis Pb18. Approximately 18% (5 of the extracts showed minimum inhibitory concentration (MIC values≤ 125.0 µg/mL. Among these, extract from the fungus UFMGCB 8030 demonstrated the best results, with an MIC of 15.6 µg/mL. This isolate was identified as Aspergillus felis (by macro and micromorphologies, and internal transcribed spacer, β-tubulin, and ribosomal polymerase II gene analyses and was grown in five different culture media and extracted with various solvents to optimise its antifungal activity. Potato dextrose agar culture and dichloromethane extraction resulted in an MIC of 1.9 µg/mL against P. brasiliensis and did not show cytotoxicity at the concentrations tested in normal mammalian cell (Vero. This extract was subjected to bioassay-guided fractionation using analytical C18RP-high-performance liquid chromatography (HPLC and an antifungal assay using P. brasiliensis. Analysis of the active fractions by HPLC-high resolution mass spectrometry allowed us to identify the antifungal agents present in the A. felis extracts cytochalasins. These results reveal the potential of A. felis as a producer of bioactive compounds with antifungal activity.

  18. 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

  19. PHYTOCHEMICAL SCREENING AND IN-VITRO ANTIFUNGAL INVESTIGATION OF PARTHENIUM HYSTEROPHORUS EXTRACTS AGAINST ALTERNARIA ALTERNATA

    Directory of Open Access Journals (Sweden)

    Singh Padma

    2013-07-01

    Full Text Available The extensive use of fungicides are polluting the environment and giving rise to undesirable biological effects on animal and human beings. Therefore use of plant extracts as biological control agents is being popularized in recent years. Alternaria alternata is reported for causing foliage disease in several important vegetables and crops. In an approach towards the development of eco friendly antifungal compound for controlling plant diseases caused by Alternaria alternata different extracts of Parthenium hysterophorus were tested for their antifungal potential. Parthenium hysterophorus is considered as an obnoxious weed, growing on waste land. The four different solvent extracts viz., aqueous, methanol, acetone and ethanol extracts of leaves of Parthenium hysterophorus was evaluated from antifungal potential against four different isolates of Alternaria alternata isolated from potato (Solanum tuberosum, onion (Allium cepa, tomato (Lycopersicon esculentum and mustard (Brassica compestris by food poison technique. The ethanolic extract showed complete inhibition against the four isolates i.e. 100 % followed by acetone and methanol extracts which was approximately 96 % and 76 % respectively, while aqueous extract do not showed any antifungal activity. Thus the result showed that the ethanolic extract was the best extract to be used. The phytochemical analysis revealed the presence of alkaloid, glycoside, steroid, saponin in varying concentration in different extracts which might be the cause of antifungal potential. The present study supports the use of leaf extract of Parthenium hysterophorus as biofungicides for the disease caused by Alternaria alternata. This will help to save the environment from chemical hazards as most of the synthetic fungicide constitute mercury, zinc etc which are toxic for nature.

  20. The research process of the synergistic antifungal effect of plant compositions%植物成分协同抗真菌作用的研究进展

    Institute of Scientific and Technical Information of China (English)

    申玲; 姜远英; 曹永兵

    2013-01-01

    The incidence of systemic fungal infections have increased dramatically in recent years, but now clinically available antifungal drugs are limited, and the research and development of new drugs are difficult. So combination therapy is expected to become the ideal choice for antifungal therapy. Plant compositions can play a synergistic antifungal effect with the antifungal agents in the form of a monomer or mixture. Such research is more extensive and thorough in vitro , but further study on the antifungal effects in vivo , mechanisms and clinical trials is still needed. This review focuses on the antifungal synergism of plant compositions combined with antifungal agents, so as to provide a reference for the study of the novel antifungal drugs.%近年来深部真菌感染的发病率显著上升,而目前临床可用的抗真菌药有限,新药研发难度大,因此联合用药有望成为抗真菌治疗的理想选择.植物成分以单体或混合物的形式与抗真菌药物协同发挥抗真菌的作用,已在体外实验中有比较广泛和深入的研究,但体内抗真菌实验、机制研究和临床试验有待进一步探究.该文就植物成分协同抗真菌作用及其机制的研究进展进行了综述,旨在为新型抗真菌药物的研究提供参考.

  1. Two new cyclopeptides from the co-culture broth of two marine mangrove fungi and their antifungal activity

    Science.gov (United States)

    Huang, Song; Ding, Weijia; Li, Chunyuan; Cox, Daniel G.

    2014-01-01

    Background: The strategy that co-cultivation two microorganisms in a single confined environment were recently developed to generate new active natural products. In the study, two new cyclic tetrapeptides, cyclo (D-Pro-L-Tyr-L-Pro-L-Tyr) (1) and cyclo (Gly-L-Phe-L-Pro-L-Tyr) (2) were isolated from the co-culture broth of two mangrove fungi Phomopsis sp. K38 and Alternaria sp. E33. Their antifungal activity against Candida albicans, Gaeumannomyces graminis, Rhzioctonia cerealis, Helminthosporium sativum and Fusarium graminearum was evaluated. Materials and Methods: Different column chromatographic techniques with different solvent systems were used to separate the constituents of the n-butyl alcohol extract of the culture broth. The structures of compounds 1 and 2 were identified by analysis of spectroscopic data (one-dimensional, two-dimensional - nuclear magnetic resonance, mass spectrometry) and Marfey's analytic method. Dilution method was used for the evaluation of antifungal activity. Results: Compounds 1 and 2 were identified as cyclo (D-Pro-L-Tyr-L-Pro-L-Tyr) and cyclo (Gly-L-Phe-L-Pro-L-Tyr), respectively. Compounds 1 and 2 showed moderate to high antifungal activities as compared with the positive control. Conclusions: Compounds 1 and 2 are new cyclopeptides with moderate antifungal activity being worthy of consideration for the development and research of antifungal agents. PMID:25422539

  2. Antifungal New Oxepine-Containing Alkaloids and Xanthones from the Deep-Sea-Derived Fungus Aspergillus versicolor SCSIO 05879.

    Science.gov (United States)

    Wang, Junfeng; He, Weijun; Huang, Xiaolong; Tian, Xinpeng; Liao, Shengrong; Yang, Bin; Wang, Fazuo; Zhou, Xiaojiang; Liu, Yonghong

    2016-04-13

    Phytopathogenic fungi remain a continuous and huge threat in the agricultural fields. The agrochemical industry has made great development of the use of microbial natural products, which has been regarded as an effective strategy against phytopathogenic fungi. Antifungal bioassay-directed fractionation was used to isolate two new oxepine-containing alkaloids (1 and 2), two new 4-aryl-quinolin-2-one alkaloids (3 and 4), and four new prenylated xanthones (5-8) from the deep-sea-derived fungus Aspergillus versicolor SCSIO 05879. Extensive NMR spectroscopic analysis, quantum mechanical calculations, and X-ray single-crystal diffraction were used to elucidate their structures, including their absolute configurations. Versicoloids A and B, versicone A, and cottoquinazoline A showed antifungal activities against three phytopathogenic fungi. The antifungal activities of these bioactive compounds strongly depend on the fungal species. Especially versicoloids A and B showed strong fungicidal effect (MIC of 1.6 μg/mL) against Colletotrichum acutatum, compared with that of the positive control cycloheximide (MIC of 6.4 μg/mL). The results of antifungal experiments indicated that versicoloids A and B may be regarded as candidate agents of antifungal agrochemicals.

  3. Biogenic ZnO nanoparticles synthesized using L. aculeata leaf extract and their antifungal activity against plant fungal pathogens

    Indian Academy of Sciences (India)

    S Narendhran; Rajeshwari Sivaraj

    2016-02-01

    In this study, Zinc oxide (ZnO) nanoparticles were synthesized using aqueous extract of Lantana aculeata Linn. leaf and assessed their effects on antifungal activity against the plant fungal pathogens. Synthesized nanoparticles were confirmed by ultraviolet–visible spectroscopy, Fourier transform infrared spectrometer, energy-dispersive X-ray spectrometer, X-ray diffractometer, Field-emission scanning electron microscopy, high-resolution transmission electron microscopy. The antifungal activity of ZnO nanoparticles were determined using the well diffusion method. All the characterization analyses revealed that nanoparticles were highly stable and crystalline in nature. L. aculeata-mediated ZnO nanoparticles were spherical in shape with an average particle size of 12 ± 3 nm. Antifungal studies concluded that the maximum zone of inhibition was observed in Aspergillus flavus (21 ± 1.0 mm) and Fusarium oxysporum (19 ± 1.0 mm) at 100 g ml-1 concentration. These results clearly indicated the benefits of using ZnO nanoparticles synthesized using biological methods and shown to have antifungal activities and also that it can be effectively used as antifungal agent in environmental aspect of agricultural development.

  4. Additive potential of ginger starch on antifungal potency of honey against Candida albicans

    Institute of Scientific and Technical Information of China (English)

    Ahmed Moussa; Djebli Noureddine; Hammoudi SM; Aissat Saad; Akila Bourabeh; Hemida Houari

    2012-01-01

    Objective: To evaluate the additive action of ginger starch on the antifungal activity of honey against Candida albicans (C. albicans). Methods: C. albicans was used to determine the minimum inhibitory concentration (MIC) of four varieties of Algerian honey. Lower concentrations of honey than the MIC were incubated with a set of concentrations of starch and then added to media to determine the minimum additive inhibitory concentration (MAIC). Results: The MIC for the four varieties of honey without starch against C. albicans ranged between 38% and 42% (v/v). When starch was incubated with honey and then added to media, a MIC drop was noticed with each variety. MAIC of the four varieties ranged between 32% honey (v/v) with 4% starch and 36% honey (v/v) with 2% starch. Conclusions: The use of ginger starch allows honey benefit and will constitute an alternative way against the resistance to antifungal agents.

  5. The "in vitro" antifungal activity evaluation of propolis G12 ethanol extract on Cryptococcus neoformans.

    Science.gov (United States)

    Fernandes, Fabrício Freitas; Dias, Amanda Latercia Tranches; Ramos, Cíntia Lacerda; Ikegaki, Masaharu; de Siqueira, Antonio Martins; Franco, Marília Caixeta

    2007-01-01

    Cryptococcosis is a worldwide disease caused by the etiological agent Cryptococcus neoformans. It affects mainly immunocompromised humans. It is relatively rare in animals only affecting those that have received prolonged antibiotic therapy. The propolis is a resin that can present several biological properties, including antibacterial, antifungal and antiviral activities. The standard strain C. neoformans ATTC 90112 was used to the antifungal evaluation. The tests were realized with propolis ethanol extract (PEE) G12 in concentrations from 0.1 to 1.6 mg mL-1. The evaluation of MIC and MFC were done according to DUARTE (2002)5. The inhibitory effect of PEE G12 on the fungal growing was seen at the concentration of 0.2 mg mL-1 and 1.6 mg mL-1 was considered a fungicidal one.

  6. Antifungal activity of essential oil Hyssopus officinalis L. against micopathogen Mycogone perniciosa (Mang

    Directory of Open Access Journals (Sweden)

    Glamočlija Jasmina M.

    2005-01-01

    Full Text Available The most commonly cultivated mushroom species is the Agaricus bisporus Lange (Imb. One of the major pathogenic diseases of the cultivated mushroom in Serbia is Mycogone perniciosa (Mang. Biological control systems are not much used in mushroom cultivation. Medical and aromatic plants have been placed in the focus of intense studies. Pure culture of the M. perniciosa was isolated from infected A. bisporus. The essential oil of Hyssopus officinalis L. is used as a potential antifungal agent. The most abundant components in oil are isopinocamphone (43.29%, pinocamphone (16.79% and b-pinene (16.31%. Antifungal activity of Hyssop was investigated by the modified microatmosphere method. The minimal inhibitory quantity was 5 μL/mL and a minimal fungicidal quantity was 15-20 μL/mL. There is no report on the use of Hyssop essential oil in mushroom disease.

  7. Sentinel surveillance of invasive candidiasis in Spain: epidemiology and antifungal susceptibility.

    Science.gov (United States)

    Nieto, M C; Tellería, O; Cisterna, R

    2015-01-01

    In order to know the epidemiology and the changes of antifungal resistance in invasive candidiasis (IC) we carried out this prospective study of Candida strains belonging to patients admitted to 26 Spanish hospitals from June 2011 to June 2012 diagnosed with IC. Clinical information and the identity of the Candida species were collected and antifungal susceptibility was tested using broth microdilution in five agents: amphotericin B, fluconazole, voriconazole, caspofungin and anidulafungin. A total of 705 cases-isolates were documented. Most of the patients suffered from candidemia and several underlying diseases and more than half of them were neutropenic or under immunosuppressive therapy, factors associated with higher mortality. Thirty percent of global mortality was documented. C. albicans was the most frequently isolated species, although an increase of non-C. albicans species was observed. Resistance to fluconazole was of 3.4%, lower than in previous years (6.3%). C. parapsilosis presented a higher MIC90 of echinocandins compared to other species.

  8. Antifungal activity of Thymus vulgaris L. essential oil and its constituent phytochemicals against Rhizopus oryzae: interaction with ergosterol.

    Science.gov (United States)

    de Lira Mota, Kelly Samara; de Oliveira Pereira, Fillipe; de Oliveira, Wylly Araújo; Lima, Igara Oliveira; de Oliveira Lima, Edeltrudes

    2012-12-05

    Mucormycoses are emerging infections that have high rates of morbidity and mortality. They show high resistance to antifungal agents, and there is a limited therapeutic arsenal currently available, therefore, there is a great need to give priority to testing therapeutic agents for the treatment of mucormycosis. Along this line, the use of essential oils and phytoconstituents has been emphasized as a new therapeutic approach. The objective of this work was to investigate the antifungal activity of the essential oil (EO) of Thymus vulgaris, and its constituents thymol and p-cymene against Rhizopus oryzae, through microbiological screening, determination of minimal inhibitory concentration (MICs) and minimal fungicidal concentration (MFCs), effects on mycelial growth and germination of sporangiospores and interaction with ergosterol. The MIC of EO and thymol varied 128-512 µg/mL, but the MFC of EO and thymol varied 512-1024 µg/mL and 128-1024 µg/mL, respectively. The results also showed that EO and thymol significantly inhibited mycelial development and germination of sporangiospores. Investigation of the mechanism of antifungal action showed that EO and thymol interact with ergosterol. These data indicate that EO of T. vulgaris and thymol possess strong antifungal activity, which can be related to their interaction with ergosterol, supporting the possible use of these products in the treatment of mucormycosis.

  9. Antifungal and antibacterial activities of Petroselinum crispum essential oil.

    Science.gov (United States)

    Linde, G A; Gazim, Z C; Cardoso, B K; Jorge, L F; Tešević, V; Glamoćlija, J; Soković, M; Colauto, N B

    2016-07-29

    Parsley [Petroselinum crispum (Mill.) Fuss] is regarded as an aromatic, culinary, and medicinal plant and is used in the cosmetic, food, and pharmaceutical industries. However, few studies with conflicting results have been conducted on the antimicrobial activity of parsley essential oil. In addition, there have been no reports of essential oil obtained from parsley aerial parts, except seeds, as an alternative natural antimicrobial agent. Also, microorganism resistance is still a challenge for health and food production. Based on the demand for natural products to control microorganisms, and the re-evaluation of potential medicinal plants for controlling diseases, the objective of this study was to determine the chemical composition and antibacterial and antifungal activities of parsley essential oil against foodborne diseases and opportunistic pathogens. Seven bacteria and eight fungi were tested. The essential oil major compounds were apiol, myristicin, and b-phellandrene. Parsley essential oil had bacteriostatic activity against all tested bacteria, mainly Staphylococcus aureus, Listeria monocytogenes, and Salmonella enterica, at similar or lower concentrations than at least one of the controls, and bactericidal activity against all tested bacteria, mainly S. aureus, at similar or lower concentrations than at least one of the controls. This essential oil also had fungistatic activity against all tested fungi, mainly, Penicillium ochrochloron and Trichoderma viride, at lower concentrations than the ketoconazole control and fungicidal activity against all tested fungi at higher concentrations than the controls. Parsley is used in cooking and medicine, and its essential oil is an effective antimicrobial agent.

  10. Azospirillum brasilense siderophores with antifungal activity against Colletotrichum acutatum.

    Science.gov (United States)

    Tortora, María L; Díaz-Ricci, Juan C; Pedraza, Raúl O

    2011-04-01

    Anthracnose, caused by the fungus Colletotrichum acutatum is one of the most important diseases in strawberry crop. Due to environmental pollution and resistance produced by chemical fungicides, nowadays biological control is considered a good alternative for crop protection. Among biocontrol agents, there are plant growth-promoting bacteria, such as members of the genus Azospirillum. In this work, we demonstrate that under iron limiting conditions different strains of A. brasilense produce siderophores, exhibiting different yields and rates of production according to their origin. Chemical assays revealed that strains REC2 and REC3 secrete catechol type siderophores, including salicylic acid, detected by thin layer chromatography coupled with fluorescence spectroscopy and gas chromatography-mass spectrometry analysis. Siderophores produced by them showed in vitro antifungal activity against C. acutatum M11. Furthermore, this latter coincided with results obtained from phytopathological tests performed in planta, where a reduction of anthracnose symptoms on strawberry plants previously inoculated with A. brasilense was observed. These outcomes suggest that some strains of A. brasilense could act as biocontrol agent preventing anthracnose disease in strawberry.

  11. An antifungal peptide from the coconut.

    Science.gov (United States)

    Wang, H X; Ng, T B

    2005-12-01

    A chromatographic procedure consisting of ion exchange chromatography on DEAE-cellulose, affinity chromatography on Affi-gel blue gel, ion exchange chromatography on CM-cellulose, and gel filtration by fast performance liquid chromatography on Supedex 75 was utilized to isolate a 10 kDa antifungal peptide from coconut flesh. The peptide was unadsorbed on DEAE-cellulose, but adsorbed on Affi-gel blue gel and CM-cellulose. It displayed antifungal activity against Fusarium oxysporum, Mycosphaerella arachidicola and Physalospora piricola. The IC50 values of its inhibitory activities on mycelial growth in M. arachidicola and HIV-1 reverse transcriptase activity were respectively 1.2 and 52.5 microM.

  12. Antifungal Efficacy of Myrtus communis Linn

    OpenAIRE

    Sadeghi Nejad; Erfani Nejad; Yusef Naanaie; Zarrin

    2014-01-01

    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 g...

  13. Candida albicans biofilm chip (CaBChip) for high-throughput antifungal drug screening.

    Science.gov (United States)

    Srinivasan, Anand; Lopez-Ribot, Jose L; Ramasubramanian, Anand K

    2012-07-18

    Candida albicans remains the main etiological agent of candidiasis, which currently represents the fourth most common nosocomial bloodstream infection in US hospitals. These opportunistic infections pose a growing threat for an increasing number of compromised individuals, and carry unacceptably high mortality rates. This is in part due to the limited arsenal of antifungal drugs, but also to the emergence of resistance against the most commonly used antifungal agents. Further complicating treatment is the fact that a majority of manifestations of candidiasis are associated with the formation of biofilms, and cells within these biofilms show increased levels of resistance to most clinically-used antifungal agents. Here we describe the development of a high-density microarray that consists of C. albicans nano-biofilms, which we have named CaBChip. Briefly, a robotic microarrayer is used to print yeast cells of C. albicans onto a solid substrate. During printing, the yeast cells are enclosed in a three dimensional matrix using a volume as low as 50 nL and immobilized on a glass substrate with a suitable coating. After initial printing, the slides are incubated at 37 °C for 24 hours to allow for biofilm development. During this period the spots grow into fully developed "nano-biofilms" that display typical structural and phenotypic characteristics associated with mature C. albicans biofilms (i.e. morphological complexity, three dimensional architecture and drug resistance). Overall, the CaBChip is composed of ~750 equivalent and spatially distinct biofilms; with the additional advantage that multiple chips can be printed and processed simultaneously. Cell viability is estimated by measuring the fluorescent intensity of FUN1 metabolic stain using a microarray scanner. This fungal chip is ideally suited for use in true high-throughput screening for antifungal drug discovery. Compared to current standards (i.e. the 96-well microtiter plate model of biofilm formation

  14. Econazole imprinted textiles with antifungal activity.

    Science.gov (United States)

    Hossain, Mirza Akram; Lalloz, Augustine; Benhaddou, Aicha; Pagniez, Fabrice; Raymond, Martine; Le Pape, Patrice; Simard, Pierre; Théberge, Karine; Leblond, Jeanne

    2016-04-01

    In this work, we propose pharmaceutical textiles imprinted with lipid microparticles of Econazole nitrate (ECN) as a mean to improve patient compliance while maintaining drug activity. Lipid microparticles were prepared and characterized by laser diffraction (3.5±0.1 μm). Using an optimized screen-printing method, microparticles were deposited on textiles, as observed by scanning electron microscopy. The drug content of textiles (97±3 μg/cm(2)) was reproducible and stable up to 4 months storage at 25 °C/65% Relative Humidity. Imprinted textiles exhibited a thermosensitive behavior, as witnessed by a fusion temperature of 34.8 °C, which enabled a larger drug release at 32 °C (temperature of the skin) than at room temperature. In vitro antifungal activity of ECN textiles was compared to commercial 1% (wt/wt) ECN cream Pevaryl®. ECN textiles maintained their antifungal activity against a broad range of Candida species as well as major dermatophyte species. In vivo, ECN textiles also preserved the antifungal efficacy of ECN on cutaneous candidiasis infection in mice. Ex vivo percutaneous absorption studies demonstrated that ECN released from pharmaceutical textiles concentrated more in the upper skin layers, where the fungal infections develop, as compared to dermal absorption of Pevaryl®. Overall, these results showed that this technology is promising to develop pharmaceutical garments textiles for the treatment of superficial fungal infections.

  15. Antifungal activity of Terminalia superba (combretaceae

    Directory of Open Access Journals (Sweden)

    SIAKA Sohro

    2015-04-01

    Full Text Available The aim of the present study was to optimize the anticandidosic activities of Terminalia superba (TEKAM4 and the identification of major compounds present in the most active chromatographic fraction. The hydroethanolic extract TEKAM4-X0 was prepared by homogenization employing a blender. Two derivatives extracts of TEKAM4-X0 (X1-1 and X1-2 were obtained by a liquid/liquid partition of TEKAM4-X0 in a mixture of hexane and water (v/v. Three chromatographic fractions (F1, F2 and F3 from X1-2 were separated by means of Sephadex-LH20 gel filtration chromatography. All the extracts were incorporated to Sabouraud according to the agar slanted double dilution method. Ketoconazole was used as standards for antifungal assay. The entire fractions were tested on the previously prepared medium culture containing 1000 cells of C. albicans. Antifungal activity was determined by evaluating antifungal parameters values (MFC and IC50. Lastly, the structures of 2 isolated compounds were elucidated by combination of Flash chromatography and spectroscopic methods, including MS, and multiple stage RMN experiments.

  16. ANTIFUNGAL ACTIVITY OF SOME COLEUS SPECIES GROWING IN NILGIRIS

    OpenAIRE

    Nilani, P.; Duraisamy, B.; Dhanabal, P.S.; khan, Saleemullah; Suresh, B.; Shankar, V.; Kavitha, K.Y.; Syamala, G.

    2006-01-01

    The in vitro antifungal activity of solvent extracts of Coleus forskohlii, Coleus blumei and Coleus barbatus were compared by testing against some pathogenic fungi like Aspergillus niger, Aspergillus fumigatus, Aspergillus ruantii, Proteus vulgaris and Candida albicans. The petroleum ether extract of Coleus forskohlii and Coleus barbatus exhibited significant antifungal activity against all the selected organisms. The extracts of Coleus blumei did not show any significant antifungal activity ...

  17. Antifungal activity of some coleus species growing in nilgiris.

    Science.gov (United States)

    Nilani, P; Duraisamy, B; Dhanabal, P S; Khan, Saleemullah; Suresh, B; Shankar, V; Kavitha, K Y; Syamala, G

    2006-07-01

    The in vitro antifungal activity of solvent extracts of Coleus forskohlii, Coleus blumei and Coleus barbatus were compared by testing against some pathogenic fungi like Aspergillus niger, Aspergillusfumigatus, Aspergillus ruantii, Proteus vulgaris and Candida albicans. The petroleum ether extract of Coleus forskohlii and Coleus barbatus exhibited significant antifungal activity against all the selected organisms. The extracts of Coleus blumei did not show any significant antifungal activity against the selected organisms.

  18. Design, synthesis and antifungal activity of novel triazole derivatives

    Institute of Scientific and Technical Information of China (English)

    Qing lie Zhao; Yan Song; Hong Gang Hu; Shi Chong Yu; Qiu Ye Wu

    2007-01-01

    Twenty-three 1 -(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-cycloproyl-N-substituted-amino)-2-propanols were designed and synthesized on the basis of the active site of lanosterol 14α-demethylase.In vitro antifungal activities showed that some of the title compounds had higher antifungal activity and broader antifungal spectrum than fluconazole.

  19. 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.

  20. [Expression of N domain of chromogranin A in Bacillus subtilis and its antifungal activity].

    Science.gov (United States)

    Li, Rui-Fang; Lou, Jin-Xian; Zhang, Tian-Yuan

    2004-03-01

    Chromogranin A (CGA) is a soluble protein existed in most secreted cells and neurons. It was recently found that the bovine CGA N terminal region has vasoinhibitory, antibacterial and antifungal activities. Since the need for effective antifungal agents increases in parallel with the expanding number of immunocompromised patients at risk for fungal infections, it becomes imperative to find antifungal compounds with low toxicity toward mammalian cells. To study the antifungal activity of CGA N terminal region, the DNA fragment encoding for the N terminal 1-76 amino acid sequence (CGA1-76) of human CGA was amplified by PCR technique. After DNA sequence analysis, the amplified DNA fragment was cloned into the Bacillus subtilis inducible and expression vector pSBPTQ constructed in this study and the resultant plasmid pSVTQ was then transformed into triple-protease deficient Bacillus subtilis strain DB403 competent cells. The transformants was screened on LB plates containing 10 microg/mL kanamycin. The positive transformant DB403 (pSVTQ) was grown on kanmycin containing 2 x MSR medium and sucrose was added to 2% final concentration for induction after 2h cultivation. The culture supernatant was used to run SDS-PAGE. The result of SDS-PAGE showed that the CGA1-76 was expressed by sucrose induction and the expressed product secreted into the medium with a yield of 5 mg/L. The expressed product reacts specifically with mouse anti CGA47-68 monoclonal antibody. The antifungal activity of the expressed product was examined by adding the culture supernatant to the fungal spore or Candida albican suspensions at appropriate proportion and found that the recombinant human CGA1-76 produced in Bacillus subtilis inhibits the growth of Fusarium sp. Alternaria sp. and Candida albican at the concerntration of 4 micromol/L. These results demonstrate that human CGA1-76 has expressed in Bacillus subtilis and the expressed product is immunogenic and has the antifungal activity.

  1. Antifungal Susceptibility Analysis of Clinical Isolates of Candida parapsilosis in Iran

    Science.gov (United States)

    LOTFALI, Ensieh; KORDBACHEH, Parivash; MIRHENDI, Hossein; ZAINI, Farideh; GHAJARI, Ali; MOHAMMADI, Rasoul; NOORBAKHSH, Fatemeh; MOAZENI, Maryam; FALLAHI, Aliakbar; REZAIE, Sassan

    2016-01-01

    Background: Candida parapsilosis is an emergent agent of invasive fungal infections. This yeast is one of the five most widespread yeasts concerned in invasive candidiasis. C. parapsilosis stands out as the second most common yeast species isolated from patients with bloodstream infections especially in neonates with catheter. Recently several reports suggested that its reduced susceptibility to azoles and polyene might become a cause for clinical concern, although C. parapsilosis is not believed to be intensely prone to the development of antifungal resistance. Methods: In the present report, One hundred and twenty clinical isolates of C. parapsilosis complex were identified and differentiated by using PCR-RFLP analysis. The isolates were then analyzed to determine their susceptibility profile to fluconazole (FLU), itraconazole (ITC) and amphotericin B. The minimum inhibitory concentration (MIC) results were analyzed according to the standard CLSI guide. Results: All of isolates were identified as C. parapsilosis. No C. metapsilosis and C. orthopsilosis strains were found. Evaluation of the antifungal susceptibility profile showed that only three (2.5%) C. parapsilosis were resistant to fluconazole, three (2.5%) C. parapsilosis were resistant to itraconazole and two (1.7%) C. parapsilosis were amphotericin B resistant. Conclusion: Profiles in clinical isolates of C. parapsilosis can provide important information for the control of antifungal resistance as well as distribution and susceptibility profiles in populations. PMID:27141494

  2. Candida vaginitis during contraceptive use: the influence of methods, antifungal susceptibility and virulence patterns.

    Science.gov (United States)

    Güzel, A B; Küçükgöz-Güleç, U; Aydin, M; Gümral, R; Kalkanci, A; Ilkit, M

    2013-11-01

    No consensus exists about whether contraceptives cause an increased risk of vaginitis, including vulvovaginal candidosis (VVC). We investigated 495 women (252 who used contraceptives; 243 who did not) for the presence of VVC. Antifungal susceptibility testing was performed for five antifungal agents and for boric acid, and three virulence factors were also examined. We recovered 129 (26.1%) monofungal populations from vaginal samples of women with acute VVC (AVVC, n = 18), symptomatic recurrent VVC (RVVC, n = 22) and asymptomatic RVVC (n = 28), as well as of other contraceptive users who carried Candida in their vaginas (n = 61). It is important to note that the women who had VVC used the same contraceptive methods (p > 0.05). Candida albicans was the most common species isolated (45%), followed by C. glabrata (40.3%). Most of the vaginal yeast isolates exhibited low minimum inhibitory concentration levels for the five antifungals tested. However, this was not the case for boric acid. In addition, the yeast fungi that was derived from the AVVC and RVVC patients showed higher amounts of haemolytic activity than the yeast fungi found among the controls (p contraception does not predispose women to VVC (p > 0.05). Also, both host- and organism-related factors were required to achieve optimal clinical treatment for VVC.

  3. Cytotoxic and Antifungal Constituents Isolated from the Metabolites of Endophytic Fungus DO14 from Dendrobium officinale

    Directory of Open Access Journals (Sweden)

    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.

  4. In vitro antifungal activities of Actinomyces species isolated from soil samples against Trichophyton mentagrophytes

    Directory of Open Access Journals (Sweden)

    Nasser Keikha

    2015-09-01

    Full Text Available Background and Purpose: Cutaneous infections arise from a homogeneous group of keratinophilic fungi, known as dermatophytes. Since these pathogenic dermatophytes are eukaryotes in nature, use of chemical antifungal agents for treatment may affect the host tissue cells. In this study, we aimed to evaluate the antifungal activity of Actinomyces species against Trichophyton mentagrophytes (abbreviated as T. mentagrophytes. The isolates were obtained from soil samples and identified by polymerase chain reaction (PCR technique. Material and Methods: In total, 100 strains of Actinomyces species were isolated from soil samples in order to determine their antagonistic activities against T. mentagrophytes in Kerman, Iran. The electron microscopic study of these isolates was performed, based on the physiological properties of these antagonists (e.g., lipase, amylase, protease and chitinase, using relevant protocols. The isolates were identified using gene 16S rDNA via PCR technique. Results: Streptomyces flavogriseus, Streptomyces zaomyceticus strain xsd08149 and Streptomyces rochei were isolated and exhibited the most significant antagonistic activities against T. mentagrophytes. Images were obtained by an electron microscope and some spores, mycelia and morphology of spore chains were identified. Molecular, morphological and biochemical characteristics of these isolates were studied, using the internal 16S rDNA gene. Active isolates of Streptomyces sequence were compared to GenBank sequences. According to nucleotide analysis, isolate D5 had maximum similarity to Streptomyces flavogriseus (99%. Conclusion: The findings of this study showed that Streptomyces isolates from soil samples could exert antifungal effects on T. mentagrophytes

  5. Molecular typing and antifungal susceptibility of Exophiala isolates from patients with cystic fibrosis.

    Science.gov (United States)

    Packeu, Ann; Lebecque, Patrick; Rodriguez-Villalobos, Hector; Boeras, Anca; Hendrickx, Marijke; Bouchara, Jean-Philippe; Symoens, Françoise

    2012-09-01

    The black yeast Exophiala dermatitidis is a frequent agent of colonization of the lungs of patients with cystic fibrosis (CF). A total of 71 clinical isolates of Exophiala from 13 patients were identified at the species level by sequencing the internal transcribed spacer (ITS) regions 1 and 2 of the rDNA genes and typed by random amplification of polymorphic DNA (RAPD), using two different primers, BG-2 and ERIC-1. In vitro susceptibility of these isolates to some systemic antifungal drugs was investigated using the CLSI method. Almost all the isolates were identified as E. dermatitidis, but long-term colonization with the closely related species E. phaeomuriformis was observed in one patient. No clustering was found according to the geographical origin of the isolates, the isolation date or the antifungal susceptibility. Variations were seen in the susceptibility of studied isolates to antifungals but most of them exhibited low susceptibility to amphotericin B and although some patients were successively colonized by two distinct genotypes, most of the isolates were distributed in patient-specific clusters. This phenomenon may be due to genomic variations of E. dermatitidis in the lung environment of CF patients. These results are typical of colonization of the airways of patients by a poorly distributed environmental fungus, which occupies particular reservoirs that need to be defined.

  6. Synthesis, Antifungal Evaluation and In Silico Study of N-(4-Halobenzylamides

    Directory of Open Access Journals (Sweden)

    Ricardo Carneiro Montes

    2016-12-01

    Full Text Available A collection of 32 structurally related N-(4-halobenzylamides were synthesized from cinnamic and benzoic acids through coupling reactions with 4-halobenzylamines, using (benzotriazol-1-yloxytris(dimethylaminophosphonium hexafluorophosphate (BOP as a coupling agent. The compounds were identified by spectroscopic methods such as infrared, 1H- and 13C- 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.

  7. Discovery and development of first in class antifungal caspofungin (CANCIDAS®)--a case study.

    Science.gov (United States)

    Balkovec, James M; Hughes, David L; Masurekar, Prakash S; Sable, Carole A; Schwartz, Robert E; Singh, Sheo B

    2014-01-01

    Covering: 1985 to 2001.This paper describes a fifteen year journey from concept to clinical discovery and development of the first in class caspofungin acetate (CANCIDAS®) a parenteral antifungal agent. Caspofungin is a semisynthetic derivative of pneumocandin B0, a naturally occurring, lipophilic cyclic peptide isolated from the fungus, Glarea lozoyensis. While the echinocandins had been previously studied for antifungal activity by several organizations, the class was dropped for a variety of reasons. Merck subsequently initiated a research program leading to the discovery and development of caspofungin. The multitude of challenges that ensued during the discovery and development process and which were successfully resolved by multi-disciplinary teams constitute the content of this article. The article consists of five sections that describe the discovery and development of caspofungin in chronological order: (i) discovery of the natural product pneumocandin B0 from fungal fermentations, (ii) fermentation development to improve the titer of pneumocandin B0 to make it commercially viable, (iii) semisynthetic modification by medicinal chemistry to successfully improve the properties of pneumocandin B0 leading to the discovery of caspofungin, (iv) development of commercial semisynthesis and purification and formulation development to improve stability and (v) clinical development and approval of CANCIDAS® as an antifungal drug which subsequently saved thousands of lives.

  8. 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

  9. Clinicomycological Profile and Antifungal Sensitivity Pattern of Commonly Used Azoles in Dermatophytosis

    Directory of Open Access Journals (Sweden)

    Mahesh Mathur

    2015-06-01

    Conclusions: This study highlighted the increasing resistance of the antifungals, which is responsible for the treatment failure in dermatophye infections. Keywords: antifungal resistance; dermatophyte; epidemiology.

  10. Bacterial and fungal keratitis in Upper Egypt: In vitro screening of enzymes, toxins and antifungal activity

    Directory of Open Access Journals (Sweden)

    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.

  11. Enhanced antifungal efficacy of tebuconazole using gated pH-driven mesoporous nanoparticles

    Science.gov (United States)

    Mas, Núria; Galiana, Irene; Hurtado, Silvia; Mondragón, Laura; Bernardos, Andrea; Sancenón, Félix; Marcos, María D; Amorós, Pedro; Abril-Utrillas, Nuria; Martínez-Máñez, Ramón; Murguía, José Ramón

    2014-01-01

    pH-sensitive gated mesoporous silica nanoparticles have been synthesized. Increased extracellular pH and internalization into living yeast cells triggered molecular gate aperture and cargo release. Proper performance of the system was demonstrated with nanodevices loaded with fluorescein or with the antifungal agent tebuconazole. Interestingly, nanodevices loaded with tebuconazole significantly enhanced tebuconazole cytotoxicity. As alterations of acidic external pH are a key parameter in the onset of fungal vaginitis, this nanodevice could improve the treatment for vaginal mycoses. PMID:24920897

  12. Determination of antibacterial, antifungal activity and chemical composition of essential oil portion of unani formulation kulzam

    Directory of Open Access Journals (Sweden)

    K Ashok Kumar

    2011-01-01

    Full Text Available Kulzam is a popular unani, liquid formulation; indicated for several minor ailments like cough, cold, running nose, sore throat, insect bites, earache, tooth ache, etc. by the manufacturer. However, this over the counter formulation has not been scientifically evaluated for its claimed uses. Hence in the present study an attempt has been to check the chemical composition, antibacterial and antifungal activity as most of the above-mentioned conditions are underpinned by microbial activity. The antibacterial and antifungal activity of the formulation was carried out on human pathogenic bacteria Pseudomonas aerogenousa, Escherichia coli, Staphylococcus aureus, Corynebacterium and fungi Candida albicans, Aspergillus fumigates and was compared with standards ciprofloxacin and clotrimazole. Kulzam exhibited strong in vitro inhibition of growth against all the test micro-organisms at both 100 and 150 μl levels of undiluted formulation (test sample and more than that of standard at 150 μl level. The chemical composition of essential oil of the formulation was determined by gas chromatography−mass spectroscopy (GC-MS analysis. Thirteen compounds constituting about 93.56% of the essential oil were identified. The main components were Camphor, menthol, thymol, 2-propenal 3-phenyl-, eugenol, trans-caryophyllene, p-allylanisole, linalool, eucalyptol, l-limonene, 1-methyl-2-isopropylbenzene, and 1S-alpha-pinene. The outcome of this study shows that kulzam contain terpenes and their oxygenated derivatives, which are believed to be highly effective antibacterial, antifungal, analgesic, anti-inflammatory, antioxidant, spasmolytic and immunomodulatory agents. The formulation has been found to possess strong antibacterial and antifungal properties, and it becomes very difficult to pin point the specific compound responsible for studied activities. However, the study positively motivates the use of kulzam for common ailments.

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

    Directory of Open Access Journals (Sweden)

    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.

  14. Optimization of Antifungal Extracts from Ficus hirta Fruits Using Response Surface Methodology and Antifungal Activity Tests

    Directory of Open Access Journals (Sweden)

    Chuying Chen

    2015-10-01

    Full Text Available The fruits of Ficus hirta (FH display strong antifungal activity against Penicillium italicum and Penicillium digitatum. In order to optimize the extraction conditions of antifungal extracts from FH fruit, various extraction parameters, such as ethanol concentration, extraction time, solvent to solid ratio and temperature, were chosen to identify their effects on the diameters of inhibition zones (DIZs against these two Penicillium molds. Response surface methodology (RSM was applied to obtain the optimal combination of these parameters. Results showed that the optimal extraction parameters for maximum antifungal activity were: 90% (v/v ethanol concentration, 65 min extraction time, 31 mL/g solvent to solid ratio and 51 °C temperature. Under the abovementioned extraction conditions, the experimental DIZs values obtained experimentally were 57.17 ± 0.75 and 39.33 ± 0.82 mm, which were very close to the values of 57.26 and 39.29 mm predicted by the model. Further, nine kinds of phytopathogens were tested in vitro to explore the antifungal activity of the FH extracts. It was found for the first time that the FH extracts showed significant inhibition on the growth of P. italicum, A. citri, P. vexans, P. cytosporella and P. digitatum.

  15. Antifungal and antiviral products of marine organisms.

    Science.gov (United States)

    Cheung, Randy Chi Fai; Wong, Jack Ho; Pan, Wen Liang; Chan, Yau Sang; Yin, Cui Ming; Dan, Xiu Li; Wang, He Xiang; Fang, Evandro Fei; Lam, Sze Kwan; Ngai, Patrick Hung Kui; Xia, Li Xin; Liu, Fang; Ye, Xiu Yun; Zhang, Guo Qing; Liu, Qing Hong; Sha, Ou; Lin, Peng; Ki, Chan; Bekhit, Adnan A; Bekhit, Alaa El-Din; Wan, David Chi Cheong; Ye, Xiu Juan; Xia, Jiang; Ng, Tzi Bun

    2014-04-01

    Marine organisms including bacteria, fungi, algae, sponges, echinoderms, mollusks, and cephalochordates produce a variety of products with antifungal activity including bacterial chitinases, lipopeptides, and lactones; fungal (-)-sclerotiorin and peptaibols, purpurides B and C, berkedrimane B and purpuride; algal gambieric acids A and B, phlorotannins; 3,5-dibromo-2-(3,5-dibromo-2-methoxyphenoxy)phenol, spongistatin 1, eurysterols A and B, nortetillapyrone, bromotyrosine alkaloids, bis-indole alkaloid, ageloxime B and (-)-ageloxime D, haliscosamine, hamigeran G, hippolachnin A from sponges; echinoderm triterpene glycosides and alkene sulfates; molluscan kahalalide F and a 1485-Da peptide with a sequence SRSELIVHQR; and cepalochordate chitotriosidase and a 5026.9-Da antifungal peptide. The antiviral compounds from marine organisms include bacterial polysaccharide and furan-2-yl acetate; fungal macrolide, purpurester A, purpurquinone B, isoindolone derivatives, alterporriol Q, tetrahydroaltersolanol C and asperterrestide A, algal diterpenes, xylogalactofucan, alginic acid, glycolipid sulfoquinovosyldiacylglycerol, sulfated polysaccharide p-KG03, meroditerpenoids, methyl ester derivative of vatomaric acid, lectins, polysaccharides, tannins, cnidarian zoanthoxanthin alkaloids, norditerpenoid and capilloquinol; crustacean antilipopolysaccharide factors, molluscan hemocyanin; echinoderm triterpenoid glycosides; tunicate didemnin B, tamandarins A and B and; tilapia hepcidin 1-5 (TH 1-5), seabream SauMx1, SauMx2, and SauMx3, and orange-spotted grouper β-defensin. Although the mechanisms of antifungal and antiviral activities of only some of the aforementioned compounds have been elucidated, the possibility to use those known to have distinctly different mechanisms, good bioavailability, and minimal toxicity in combination therapy remains to be investigated. It is also worthwhile to test the marine antimicrobials for possible synergism with existing drugs. The prospects of

  16. Nylon-3 polymers with selective antifungal activity.

    Science.gov (United States)

    Liu, Runhui; Chen, Xinyu; Hayouka, Zvi; Chakraborty, Saswata; Falk, Shaun P; Weisblum, Bernard; Masters, Kristyn S; Gellman, Samuel H

    2013-04-10

    Host-defense peptides inhibit bacterial growth but show little toxicity toward mammalian cells. A variety of synthetic polymers have been reported to mimic this antibacterial selectivity; however, achieving comparable selectivity for fungi is more difficult because these pathogens are eukaryotes. Here we report nylon-3 polymers based on a novel subunit that display potent antifungal activity (MIC = 3.1 μg/mL for Candida albicans ) and favorable selectivity (IC10 > 400 μg/mL for 3T3 fibroblast toxicity; HC10 > 400 μg/mL for hemolysis).

  17. Synthesis of Novel Antifungal Triazole Compounds

    Institute of Scientific and Technical Information of China (English)

    Yong CHU; Ming Xia XU; Ding LU

    2004-01-01

    Based on our previous studies of 3D-QSAR, 38 novel objective compounds belonging to 4 series were designed and successfully synthesized directed by the idea of reconstructing the structure of non-pharmacophores while reserving essential ones in triazoles. In vitro pilot studies on their antifungal activities showed that most compounds have inhibitory effects on C.albicans and some inhibit S.cerevisiae also. The effects on C.albicans of 5 compounds are more potent than or equal to that of fluconazole or itraconazole.

  18. Antifungal and antioxidant activities of the phytomedicine pipsissewa, Chimaphila umbellata.

    NARCIS (Netherlands)

    Galván, I.; Mir-Rashed, N.; Jessulat, M.; Atanya, M.; Golshani, A.; Boekhout, T.; Durst, T.; Petit, P.; Amiguet, V.T.; Summerbell, R.C.; Cruz, I.; Arnason, J.T.; Smith, M.L.

    2008-01-01

    Bioassay-guided fractionation of Chimaphila umbellata (L.) W. Bart (Pyrolaceae) ethanol extracts led to the identification of 2,7-dimethyl-1,4-naphthoquinone (chimaphilin) as the principal antifungal component. The structure of chimaphilin was confirmed by 1H and 13C NMR spectroscopy. The antifungal

  19. 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...

  20. OUTCOME OF ANTIFUNGAL COMBINATION THERAPY FOR INVASIVE MOLD INFECTIONS IN HEMATOLOGICAL PATIENTS IS INDEPENDENT OF THE CHOSEN COMBINATION

    Directory of Open Access Journals (Sweden)

    Rafael Rojas

    2012-02-01

    Full Text Available Invasive mold infection (IMI remains a major cause of mortality in high-risk hematological patients. The aim of this multicenter retrospective, observational study was to evaluate antifungal combination therapy for proven and probable IMI in hematological patients. We analyzed 61 consecutive cases of proven (n=25 and probable (n=36 IMI treated with antifungal combination therapy (ACT collected from eight Spanish hospitals from January 2005 to December 2009. Causal pathogens were: Aspergillus spp (n=49, Zygomycetes (n=6, Fusarium spp (n=3, and Scedosporium spp (n=3. Patients were classified in three groups according to the antifungal combination employed: Group A, liposomal amphotericin B (L-Amb plus caspofungin (n=20; Group B, L-Amb plus a triazole (n=20, and Group C, voriconazole plus a candin (n=21. ACT was well tolerated with minimal adverse effects. Thirty-eight patients (62.3% achieved a favorable response (35 complete. End of treatment and 12-week survival rates were 62.3% and 57.4% respectively, without statistical differences among groups. Granulocyte recovery was significantly related to favorable responses and survival (p<0.001 in multivariate analysis. Our results suggest that comparable outcomes can be achieved with ACT in high risk hematological patients with proven or probable IMI, whatever the combination of antifungal agents used.

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

    Directory of Open Access Journals (Sweden)

    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.

  2. 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.

  3. Selective sweeps in Cryptocercus woodroach antifungal proteins.

    Science.gov (United States)

    Velenovsky, Joseph F; Kalisch, Jessica; Bulmer, Mark S

    2016-10-01

    We identified the antifungal gene termicin in three species of Cryptocercus woodroaches. Cryptocercus represents the closest living cockroach lineage of termites, which suggests that the antifungal role of termicin evolved prior to the divergence of termites from other cockroaches. An analysis of Cryptocercus termicin and two β-1,3-glucanase genes (GNBP1 and GNBP2), which appear to work synergistically with termicin in termites, revealed evidence of selection in these proteins. We identified the signature of past selective sweeps within GNBP2 from Cryptocercus punctulatus and Cryptocercus wrighti. The signature of past selective sweeps was also found within termicin from Cryptocercus punctulatus and Cryptocercus darwini. Our analysis further suggests a phenotypically identical variant of GNBP2 was maintained within Cryptocercus punctulatus, Cryptocercus wrighti, and Cryptocercus darwini while synonymous sites diverged. Cryptocercus termicin and GNBP2 appear to have experienced similar selective pressure to that of their termite orthologues in Reticulitermes. This selective pressure may be a result of ubiquitous entomopathogenic fungal pathogens such as Metarhizium. This study further reveals the similarities between Cryptocercus woodroaches and termites.

  4. Bibliometric analysis of literature on antifungal triazole resistance: 1980 – 2015

    Science.gov (United States)

    Sweileh, Waleed M.; Sawalha, Ansam F.; Al-Jabi, Samah; Zyoud, Sa’ed H.

    2017-01-01

    Background Triazole antifungal agents play an important role in the treatment of a wide range of fungal infections. Little is known about antifungal triazole drug resistance when compared to antibiotic resistance. Therefore, this study was carried out to give a bibliometric overview of literature on triazole antifungal drug resistance. Methods Keywords related to triazole drug class and resistance were used in a search query in the Scopus search engine. The time span was set from 1980 to 2015. Data pertaining to growth of publications, the most active countries and institutions, the most cited articles, and mapping of molecular mechanisms of resistance were analyzed. Results A total of 1648 journal articles were retrieved with an average of 20.46 citations per article. Annual growth of triazole resistance showed an increasing pattern during the study period. The United States of America (n=446; 27.06%) ranked first in productivity followed by the United Kingdom (UK) (n=176; 10.68%), and China (n=133; 8.07%). Radboud University Nijmegen Medical Centre (n=69, 4.19%) in the Netherlands ranked first in productivity, while the journal Antimicrobial Agents and Chemotherapy ranked first (n=255; 15.47%) in publishing articles on triazole resistance. Mapping mechanisms of resistance showed that efflux pump and mutations in target enzyme are major mechanisms described in resistance to triazoles. Conclusion There was a growth of publications on triazole resistance in the past two decades with the bulk of publications on triazole resistance in Candida species. The data presented here will serve as baseline information for future comparative purposes. PMID:28331838

  5. Candiduria in adults and children: prevalence and antifungal susceptibility in outpatient of Jataí-GO

    Directory of Open Access Journals (Sweden)

    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.

  6. Dermatophyte susceptibilities to antifungal azole agents tested in vitro by broth macro and microdilution methods Suscetibilidade in vitro de dermatófitos a azóis pelos métodos macro e microdiluição em caldo

    Directory of Open Access Journals (Sweden)

    Emerson Roberto Siqueira

    2008-02-01

    Full Text Available The in vitro susceptibility of dermatophytes to the azole antifungals itraconazole, fluconazole and ketoconazole was evaluated by broth macro and microdilution methods, according to recommendations of the CLSI, with some adaptations. Twenty nail and skin clinical isolates, four of Trichophyton mentagrophytes and 16 of T. rubrum were selected for the tests. Itraconazole minimal inhibitory concentrations (MIC varied from Foi avaliada a suscetibilidade in vitro de dermatófitos aos antifúngicos itraconazol, fluconazol e cetoconazol, pelos métodos macro e microdiluição em caldo, de acordo com as recomendações do CLSI, com algumas modificações. Foram estudados 20 isolados clínicos de lesões de unha e pele, sendo quatro Trichophyton mentagrophytes e 16 T. rubrum. A concentração inibitória mínima (CIM para itraconazol variou de < 0,03 a 0,25 µg/mL pelo método da macrodiluição, e de < 0,03 a 0,5 µg/mL pela microdiluição em caldo; de 0,5 a 64 µg/mL e de 0,125 a 16 µg/mL para fluconazol, respectivamente, pela macro e microdiluição; e de < 0,03 a 0,5 µg/mL por ambos os métodos para cetoconazol. A concordância entre os dois métodos (considerando ± uma diluição foi de 70% para itraconazol, 45% para fluconazol e 85% para cetoconazol. Conclui-se que os isolados estudados foram inibidos por concentrações relativamente baixas dos antifúngicos testados, e os dois métodos apresentam boa concordância, especialmente para itraconazol e cetoconazol.

  7. Isolation and identification of N-butyl-tetrahydro-5-oxofuran-2-carboxamide produced by Bacillus sp. L60 and its antifungal activity.

    Science.gov (United States)

    Lee, Yong-Seong; Cho, Jeong-Yong; Moon, Jae-Hak; Kim, Kil-Yong

    2017-03-01

    Rhizoctonia solani is the cause of substantial economic loss in many crops. The aim of this study is to investigate biocontrol potential of Bacillus sp. L60 against R. solani and to purify an antifungal compound. In this study, Bacillus sp. L60 demonstrated significant antagonism toward R. solani with the dual culture assay. The antifungal compound was extracted from Bacillus sp. L60 culture supernatant with n-butanol, and identified as N-butyl-tetrahydro-5-oxofuran-2-carboxamide (BT-5O-2C) having molecular weights of 185.1052 Da with the formula C9 H15 NO3 using NMR and HR-ESI-MS analysis. The minimum inhibitory concentration (MIC) value of the antifungal compound was 256 µg ml(-1) against R. solani. Therefore, our results clearly demonstrated BT-5O-2C as well as Bacillus sp. L60 as potential biological control agents for the management of R. solani.

  8. 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.

  9. Requirement for ergosterol in V-ATPase function underlies antifungal activity of azole drugs.

    Directory of Open Access Journals (Sweden)

    Yong-Qiang Zhang

    Full Text Available Ergosterol is an important constituent of fungal membranes. Azoles inhibit ergosterol biosynthesis, although the cellular basis for their antifungal activity is not understood. We used multiple approaches to demonstrate a critical requirement for ergosterol in vacuolar H(+-ATPase function, which is known to be essential for fungal virulence. Ergosterol biosynthesis mutants of S. cerevisiae failed to acidify the vacuole and exhibited multiple vma(- phenotypes. Extraction of ergosterol from vacuolar membranes also inactivated V-ATPase without disrupting membrane association of its subdomains. In both S. cerevisiae and the fungal pathogen C. albicans, fluconazole impaired vacuolar acidification, whereas concomitant ergosterol feeding restored V-ATPase function and cell growth. Furthermore, fluconazole exacerbated cytosolic Ca(2+ and H(+ surges triggered by the antimicrobial agent amiodarone, and impaired Ca(2+ sequestration in purified vacuolar vesicles. These findings provide a mechanistic basis for the synergy between azoles and amiodarone observed in vitro. Moreover, we show the clinical potential of this synergy in treatment of systemic fungal infections using a murine model of Candidiasis. In summary, we demonstrate a new regulatory component in fungal V-ATPase function, a novel role for ergosterol in vacuolar ion homeostasis, a plausible cellular mechanism for azole toxicity in fungi, and preliminary in vivo evidence for synergism between two antifungal agents. New insights into the cellular basis of azole toxicity in fungi may broaden therapeutic regimens for patient populations afflicted with systemic fungal infections.

  10. Purification and characterization of a potential antifungal protein from Bacillus subtilis E1R-J against Valsa mali.

    Science.gov (United States)

    Wang, N N; Yan, X; Gao, X N; Niu, H J; Kang, Z S; Huang, L L

    2016-04-01

    In order to identify the antagonistic substances produced by Bacillus subtilis E1R-J as candidate of biocontrol agents for controlling Apple Valsa Canker, hydrochloric acid precipitation, reverse phase chromatography, gel filtration, and ion exchange chromatography were used. The purified fraction EP-2 showed a single band in native-polyacrylamide gel electrophoresis (native-PAGE) and sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE). Fraction EP-2 was eluted from native-PAGE and showed a clear inhibition zone against V. mali 03-8. These results prove that EP-2 is one of the most important antifungal substances produced by B. subtilis E1R-J in fermentation broth. SDS-PAGE and Nano-LC-ESI-MS/MS analysis results demonstrated that EP-2 was likely an antifungal peptide (trA0A086WXP9), with a relative molecular mass of 12.44 kDa and isoelectric point of 9.94. The examination of antagonistic mechanism under SEM and TEM showed that EP-2 appeared to inhibit Valsa mali 03-8 by causing hyphal swelling, distortion, abnormality and protoplasts extravasation. Inhibition spectrum results showed that antifungal protein EP-2 had significantly inhibition on sixteen kinds of plant pathogenic fungi. The stability test results showed that protein EP-2 was stable with antifungal activity at temperatures as high as 100 °C for 30 min and in pH values ranging from 1.0 to 8.0, or incubated with each 5 mM Cu(2+), Zn(2+), Mg(2+), or K(+). However, the antifungal activity was negatively affected by Proteinase K treatment.

  11. Antifungal susceptibility and distribution of Candida spp. isolates from the University Hospital in the municipality of Dourados, State of Mato Grosso do Sul, Brazil

    Directory of Open Access Journals (Sweden)

    Adriana Araujo de Almeida

    2013-06-01

    Full Text Available Introduction Hospital infections caused by Candida spp. are a leading cause of morbidity and mortality in hospitalized patients, particularly those that are critically ill or immunocompromised. In this study, the distribution of Candida species in isolates from the University Hospital of the Federal University at Grande Dourados and their in vitro susceptibility to antifungal drugs were analyzed. Methods Yeasts were phenotypically identified using classical methodologies. Antifungal susceptibility tests to amphotericin B and fluconazole were performed using the broth microdilution technique. Results A total of 50 Candida isolates were obtained from hospitalized patients during the study period. We analyzed yeast isolates from urine (n=31; 62%, blood (n=12; 24%, and tracheal secretions (n=7; 14%. The following Candida species were identified: C. tropicalis (n=21; 42%, C. albicans (n=18; 36%, C. glabrata (n=10; 20%, and C. krusei (n=1; 2%. Antifungal susceptibility tests demonstrated that C. albicans was susceptible to both antifungal agents. However, 31.2% of the non-C. albicans Candida isolates displayed dose-dependent susceptibility to fluconazole, and 3.1% were resistant to amphotericin B. Conclusions In contrast to previous reports, our results indicated that C. tropicalis was the most commonly isolated yeast species among the hospital patients. The predominance of non-C. albicans Candida infections confirms the importance of species-level identification for implementing appropriate antifungal therapies.

  12. Effects of UV-accelerated weathering and natural weathering conditions on anti-fungal efficacy of wood/PVC composites doped with propylene glycol-based HPQM

    Directory of Open Access Journals (Sweden)

    P. Srimalanon

    2016-04-01

    Full Text Available This work studied the mechanical, physical and weathering properties and anti-fungal efficacy of polyvinyl chloride(PVC and wood flour/polyvinyl chloride composites(WPVC. 2-hydroxypropyl-3-piperazinyl-quinoline carboxylic acid methacrylate (HPQM in propylene glycol was used as an anti-fungal agent. Propylene glycol-based HPQM was doped in neat PVC and in WPVC containing 50 and 100 pph wood (WPVC-50 and WPVC-100. The flexural properties of PVC decreased when propylene glycol-based HPQM was added. However, adding this component did not affect the flexural properties of WPVC. Fungal growth inhibition test and dry weight technique were used for evaluation of anti-fungal effectiveness. Aspergillus niger was used as a testing fungus. Adding propylene glycol-based HPQM to WPVC-100 led to the most effective anti-fungal performance. Wood flour acted as an anti-fungal promoter for the WPVC composites. The optimal dosages of propylene glycol-based HPQM in PVC, WPVC-50, and WPVC-100 were 50000, 15000, and 10000 ppm, respectively. UV-accelerated weathering aging and natural weathering conditions were found to affect the flexural properties of PVC and WPVC. The change in the anti-microbial performance of WPVC under natural weathering were slower than those under UV-accelerated weathering aging. The anti-microbial evaluation indicated that the samples doped with less than 20000 ppm propylene glycol-based HPQM had a more pronounced effect than the ones doped with higher dosages.

  13. 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.

  14. Screening of Iranian plants for antifungal activity: Part 2

    Directory of Open Access Journals (Sweden)

    "Amin Gh.R

    2002-08-01

    Full Text Available In this study, 278 species from 37 families of native Iranian plants were screened for in vitro antifungal activity against 19 fungal strains. Initially, the crude extracts in concentration of 100 μg/ml were tested. Among 278 plant extracts, 201(71.27% of them showed antifungal activity against at least one fungal strain. A wide range of total extracts of different species were shown to have potentially noticeable antifungal effects. The outstanding species were: Mentha longifolia, Saliva multicaulis, Thymus transcaspicus, Zataria multiflora, Glycyrrhiza glabra, Hulthemia persica, Heracleum persicum, Pimpinella anisum, Pragnos ferulacea, Pragnos uloptera, and Viola odorata.

  15. Metabolic footprinting for investigation of antifungal properties of Lactobacillus paracasei

    DEFF Research Database (Denmark)

    Honoré, Anders Hans; Aunsbjerg, Stina Dissing; Ebrahimi, Parvaneh

    2016-01-01

    Lactic acid bacteria with antifungal properties are applied for biopreservation of food. In order to further our understanding of their antifungal mechanism, there is an ongoing search for bioactive molecules. With a focus on the metabolites formed, bioassay-guided fractionation and comprehensive....... The antifungal properties were assessed by measuring mold growth of two Penicillium strains on cell-free ferments of three strains of Lactobacillus paracasei pre-fermented in a chemically defined medium. Exometabolomic profiling was performed by reversed-phase liquid chromatography in combination with mass...

  16. Antifungal Treatment in Stem Cell Transplantation Centers in Turkey.

    Science.gov (United States)

    Akan, Hamdi; Atilla, Erden

    2016-03-05

    Despite the development of various guidelines, the approach to antifungal treatment in stem cell transplantation centers differs according to country or even between centers. This led to the development of another survey that aims to understand the antifungal treatment policies of Turkish stem cell transplantation centers. Although there has been an increasing trend towards the use of diagnostic-based treatments in Turkey in the last few years, empirical treatment is still the main approach. The practices of the stem cell transplantation centers reflect the general trends and controversies in this area, while there is a considerable use of antifungal combination therapy.

  17. Caerulomycin A- An antifungal compound isolated from marine actinomycetes.

    Digital Repository Service at National Institute of Oceanography (India)

    Ambavane, V.; Tokdar, P.; Parab, R.; Sreekumar, E.S.; Mahajan, G.B.; Mishra, P.D.; DeSouza, L.; Ranadive, P.

    krusei GO3FlucR 0.78 - 1.56 0.313 - 0.625 64 NT: Not Tested. 4. Discussion The global antifungal market was estimated at $9.4 billion in 2010 and is expected to grow at a rate of 1.9% during 2010-2017. The major class of antifungal compound includes... Genetics Analysis Using Maximum Likelihood, Evolutionary Distance and Maximum Parsimony Methods. Molecular Biology and Evolution, 28, 2731-2739. http://dx.doi.org/10.1093/molbev/msr121 [24] Antifungals Market to 2017—Generic Erosion of Major Polyenes...

  18. An antifungal peptide from baby lima bean.

    Science.gov (United States)

    Wang, H X; Ng, T B

    2006-12-01

    A 6-kDa antifungal peptide with inhibitory activity on mycelial growth in Fusarium oxysporum, Mycosphaerella arachidicola, and Physalospora piricola was isolated from baby lima beans. The peptide suppressed growth in M. arachidicola with an IC(50) of 0.87 muM and inhibited activity of HIV-1 reverse transcriptase with an IC(50) of 4 muM. The peptide exhibited an N-terminal amino acid sequence similar to those of leguminous defensins. The isolation procedure comprised ion exchange chromatography on diethylaminoethyl (DEAE)-cellulose, affinity chromatography on Affi-gel blue gel, ion exchange chromatography on carboxymethyl (CM)-cellulose, and gel filtration by fast protein liquid chromatography on Superdex 75. The peptide was unadsorbed on DEAE-cellulose and Affi-gel blue gel but was adsorbed on CM-cellulose.

  19. Pomegranin, an antifungal peptide from pomegranate peels.

    Science.gov (United States)

    Guo, Guang; Wang, He Xiang; Ng, Tzi Bun

    2009-01-01

    A new antifungal peptide designated as pomegranin, with an N-terminal sequence resembling that of rice disease resistance NB-S-LRR-like protein, was isolated from fresh pomegranate peels by ion exchange chromatography on DEAE-cellulose, affinity chromatography on Affi-gel blue gel, and gel filtration by fast protein liquid chromatography on Superdex 75. Pomegranin was unadsorbed on DEAE-cellulose but adsorbed on Affi-gel blue gel. It exhibited a molecular mass of 11 kDa in both gel filtration and sodium dodecyl sulfate-polyacrylamide gel electrophoresis. It inhibited mycelial growth in the fungi Botrytis cinerea and Fusarium oxysporum with an IC(50) of 2 microM and 6.1 microM, respectively. It was devoid of hemagglutinating, ribonuclease, deoxyribonuclease and protease inhibitory activities.

  20. 硝酸银与三种抗真菌药物体外抗眼部致病真菌活性的对比实验研究%Comparison of the activities of silver nitrate with those of three antifungal agents against ocular pathogenic fungi in vitro

    Institute of Scientific and Technical Information of China (English)

    徐岩; 庞广仁; 高传文; 赵东卿; 王丙亮; 周路坦; 孙声桃; 杜连心; 陈祖基

    2009-01-01

    Objective To investigate antifungal activity of silver nitrate compared with fluconazole,ketoconazole and amphotericin B against ocular pathogenic fungi in vitro.Methods It was an experimental study.Susceptibility tests were performed against 260 isolates(15 genera and 29 species)of ocular pathogenic fungi by broth dilution antifungal susceptibility testing of filamentous fungi(M38-A)approved by National Committee for Clinical Laboratory Standards(NCCLS).Final concentrations ranged from 0.031 to 16.000 mg/L for silver nitrate,ketoconazole and amphotericin B,from 0.5-256.0 mg/L for fluconazole.Minimum inhibitory concentration (MIC) was defined as the lowest drug concentration that showed absence of growth or complete growth inhibition(100%).The end points were determined as 100% growth inhibition for silver nitrate and amphotericin B.and≥75%growth inhibition for ketoconazole and fluconazole.Results The MICs at which 90% of isolates were inhibited(MIC90) of silver nitrat,ketoconazole,amphotericin B and flueonazole were 2.000,512.000,32.000 and 2.000 mg/L for Fusarium species,respectively;1.000,256.000,2.000 and 2.000 ms/L for Aspergillus species,respectively;2.000.128.000.4.000 and 2.000 mg/L for Alternaria altemat,respectively;2.000,4.000,0.125 and 0.500 mg/L for Curvularia lunata,respectively;and 1.000,256.000,1.000 and 1.000 mg/L for unusual ocular pathogens,respectively.Silver nitrate WaS highly active against Aspergilus species(92.9%susceptible at a MIC of ≤1.0 mg/L)and Fusarium species(96.3% susceptibie at a MIC of ≤2.0 mg/L).95.6%of Fusarium species and 90.8%of Aspergillus species exhibited resistance to flueonazole.44.1% of Fusarium species and 42.9%of Aspergillus species exhibited resistance to amphotericin B.66.2% of Fusarium species exhibited resistance to ketoconazole.The activity of silver nitrate against the flueonazole resistant,ketoconazole-resistant and amphotericin B-resistant strains was high.Conclusion Silver nitrate has promising activity

  1. Chemical composition and antifungal activity of the essential oil of Douglas fir (Pseudosuga menziesii Mirb. Franco from Serbia

    Directory of Open Access Journals (Sweden)

    VELE TEŠEVIĆ

    2009-09-01

    Full Text Available The chemical composition of the essential oil of fresh young needles with twigs of Douglas fir (Pseudosuga menziesii Mirb. Franco obtained by hydrodistillation were analyzed by gas chromatography (GC and gas chromatography–mass spectrometry (GC–MS. Ten compounds, accounting for 94.26 % of the oil, were identified. The main compounds found were bornyl acetate (34.65 %, camphene (29.82 %, a-pinene (11.65 % and santene (5.45 %. The antifungal activity of the essential oil was tested against various fungal species. The minimum inhibitory concentration of Douglas fir essential oil ranged from 1.5 to 4 µg mL-1. The fungi most sensitive to the tested oil were Phomopsis helianthi, while Penicillium species, along with Microsporum canis, were the most resistant. Compared to the commercial fungicidal agent bifonazole, the studied essential oil demonstrated higher antifungal activity.

  2. Synthesis and characterization of Eichhornia-mediated copper oxide nanoparticles and assessing their antifungal activity against plant pathogens

    Indian Academy of Sciences (India)

    P VANATHI; P RAJIV; RAJESHWARI SIVARAJ

    2016-09-01

    In this paper, we report the biosynthesis and characterization of copper oxide nanoparticles from an aquatic noxious weed, Eichhornia crassipes by green chemistry approach. The aim of this work is to synthesize copper oxide nanoparticles by simple, cost-effective and ecofriendly method as an alternative to other available techniques. The synthesized copper oxide nanoparticles were characterized by UV–visible spectroscopy, Fourier transform infrared spectroscopy (FTIR), Field emission scanning electron microscopy (FESEM) and Energy dispersive X-ray spectroscopy (EDX) analyses. The synthesized particles were highly stable, spherical in shape with an average diameter of $28\\pm 4$ nm. The synthesized nanoparticles were then explored to antifungal activity against plant pathogens. Highest zone of inhibition were observed in 100 $\\mu$g ml$^{−1}$ of Eichhornia-mediated copper oxide nanoparticle against Fusarium culmorum and Aspergillus niger. This Eichhornia-mediated copper oxide nanoparticles wereproved to be good antifungal agents against plant fungal pathogens.

  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. Alginate Oligosaccharides Inhibit Fungal Cell Growth and Potentiate the Activity of Antifungals against Candida and Aspergillus spp

    Science.gov (United States)

    Tøndervik, Anne; Sletta, Håvard; Klinkenberg, Geir; Emanuel, Charlotte; Powell, Lydia C.; Pritchard, Manon F.; Khan, Saira; Craine, Kieron M.; Onsøyen, Edvar; Rye, Phil D.; Wright, Chris; Thomas, David W.; Hill, Katja E.

    2014-01-01

    The oligosaccharide OligoG, an alginate derived from seaweed, has been shown to have anti-bacterial and anti-biofilm properties and potentiates the activity of selected antibiotics against multi-drug resistant bacteria. The ability of OligoG to perturb fungal growth and potentiate conventional antifungal agents was evaluated using a range of pathogenic fungal strains. Candida (n = 11) and Aspergillus (n = 3) spp. were tested using germ tube assays, LIVE/DEAD staining, scanning electron microscopy (SEM), atomic force microscopy (AFM) and high-throughput minimum inhibition concentration assays (MICs). In general, the strains tested showed a significant dose-dependent reduction in cell growth at ≥6% OligoG as measured by optical density (OD600; P0.5%) also showed a significant inhibitory effect on hyphal growth in germ tube assays, although strain-dependent variations in efficacy were observed (P<0.05). SEM and AFM both showed that OligoG (≥2%) markedly disrupted fungal biofilm formation, both alone, and in combination with fluconazole. Cell surface roughness was also significantly increased by the combination treatment (P<0.001). High-throughput robotic MIC screening demonstrated the potentiating effects of OligoG (2, 6, 10%) with nystatin, amphotericin B, fluconazole, miconazole, voriconazole or terbinafine with the test strains. Potentiating effects were observed for the Aspergillus strains with all six antifungal agents, with an up to 16-fold (nystatin) reduction in MIC. Similarly, all the Candida spp. showed potentiation with nystatin (up to 16-fold) and fluconazole (up to 8-fold). These findings demonstrate the antifungal properties of OligoG and suggest a potential role in the management of fungal infections and possible reduction of antifungal toxicity. PMID:25409186

  5. Inhibition of Rat and Human Steroidogenesis by Triazole Antifungals

    Science.gov (United States)

    Environmental chemicals that alter steroid production could interfere with male reproductive development and function. Three agricultural antifungal triazoles (myclobutanil, propiconazole and triadimefon) that are known to modulate expression of cytochrome P450 (CYP) genes and e...

  6. Antifungal activity of fruit pulp extract from Bromelia pinguin.

    Science.gov (United States)

    Camacho-Hernández, I L; Chávez-Velázquez, J A; Uribe-Beltrán, M J; Ríos-Morgan, A; Delgado-Vargas, F

    2002-08-01

    The methanol extract of the fruit pulp of Bromelia pinguin was evaluated for its antifungal activity. The extract showed a significant activity against some Trichophyton strains, although Candida strains were generally insensitive.

  7. Antifungal activity of Bacillus sp. isolated from compost.

    Science.gov (United States)

    Czaczyk, K; Stachowiak, B; Trojanowska, K; Gulewicz, K

    2000-01-01

    Four strains of Bacillus isolated from lupine compost exhibited an antifungal activity against six plant fungal pathogens (Rhizoctonia solani, Bipolaris sorokiniana, Sclerotinia sclerotiorum, Trichothecium roseum, Fusarium solani, Fusarium oxysporum). It was significantly influenced by the composition of the cultivation media.

  8. 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.

  9. Taxonomy and antifungal susceptibility of clinically important Rasamsonia species

    DEFF Research Database (Denmark)

    Houbraken, J.; Giraud, S.; Meijer, M.

    2013-01-01

    In recent years, Geosmithia argillacea has been increasingly reported in humans and animals and can be considered an emerging pathogen. The taxonomy of Geosmithia was recently studied, and Geosmithia argillacea and related species were transferred to the new genus Rasamsonia. The diversity among...... a set of Rasamsonia argillacea strains, including 28 clinical strains, was studied, and antifungal susceptibility profiles were generated. Data obtained from morphological studies and from phylogenetic analyses of internal transcribed spacer (ITS) and partial _-tubulin and calmodulin sequences revealed...... was the least active of the antifungals tested. The phenotypically similar species R. brevistipitata and R. cylindrospora had different antifungal susceptibility profiles, and this indicates that correct species identification is important to help guide appropriate antifungal therapy....

  10. Solubility, photostability and antifungal activity of phenylpropanoids encapsulated in cyclodextrins.

    Science.gov (United States)

    Kfoury, Miriana; Lounès-Hadj Sahraoui, Anissa; Bourdon, Natacha; Laruelle, Frédéric; Fontaine, Joël; Auezova, Lizette; Greige-Gerges, Hélène; Fourmentin, Sophie

    2016-04-01

    Effects of the encapsulation in cyclodextrins (CDs) on the solubility, photostability and antifungal activities of some phenylpropanoids (PPs) were investigated. Solubility experiments were carried out to evaluate the effect of CDs on PPs aqueous solubility. Loading capacities and encapsulation efficiencies of freeze-dried inclusion complexes were determined. Moreover, photostability assays for both inclusion complexes in solution and solid state were performed. Finally, two of the most widespread phytopathogenic fungi, Fusarium oxysporum and Botrytis cinerea, were chosen to examine the antifungal activity of free and encapsulated PPs. Results showed that encapsulation in CDs significantly increased the solubility and photostability of studied PPs (by 2 to 17-fold and 2 to 44-fold, respectively). Free PPs revealed remarkable antifungal properties with isoeugenol showing the lowest half-maximal inhibitory concentration (IC50) values of mycelium growth and spore germination inhibition. Encapsulated PPs, despite their reduced antifungal activity, could be helpful to solve drawbacks such as solubility and stability.

  11. Combination antifungal therapy: a critical review of the evidence.

    Science.gov (United States)

    Ostrosky-Zeichner, L

    2008-05-01

    Invasive fungal infections have extremely high rates of morbidity and mortality, particularly in immunocompromised hosts. Combination antifungal therapy is conceptually attractive as a life-saving measure. However, in-vitro and in-vivo evidence is often conflicting and clinical trials in this area are limited. Most clinical studies show similar outcomes for combination antifungal therapy when compared to monotherapy, although secondary endpoints and sub-analyses often show advantages for the combinations in endpoints such as culture sterilisation. The logistics of large clinical trials of combination therapy are highly complex. Combination of antifungals with immune modulators is an exciting new research area. Until more data are available, clinicians should approach combination antifungal therapy with caution.

  12. THE ANTIFUNGAL AND ANTIBACTERIAL ACTIVITY OF TWO PLANTS FROM ASTEMCEAE

    OpenAIRE

    2015-01-01

    In this study, we have found that, Chlysanthemum coronarium has shownantifungal and antibacterial activity, but Inula viscosa didn't show any antifungalor antibacterial activity.Key words: Chrysanthemum coronarium; Inula viscosa; antifungal andantibacterial activities.

  13. 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.  ...

  14. Antileishmanial, antimicrobial and antifungal activities of some new aryl azomethines.

    Science.gov (United States)

    Al-Kahraman, Yasser M S A; Madkour, Hassan M F; Ali, Dildar; Yasinzai, Masoom

    2010-01-28

    A series of eighteen azomethines has been synthesized by the reaction of appropriate primary aromatic amines with aryl and/or heteroaryl carboxaldehydes. The synthesized azomethines have been evaluated for their in vitro antileishmanial, antibacterial and antifungal activities. The results revealed some antifungal activity of most of the synthesized compounds, whereas the antileishmaniasis activity results highlighted that all synthesized azomethines inhibited parasite growth and most of them showed highly potent action towards Leishmania major promastigotes. No remarkable bactericidal activities were observed.

  15. The role of the multidisciplinary team in antifungal stewardship.

    Science.gov (United States)

    Agrawal, Samir; Barnes, Rosemary; Brüggemann, Roger J; Rautemaa-Richardson, Riina; Warris, Adilia

    2016-11-01

    There are a variety of challenges faced in the management of invasive fungal diseases (IFD), including high case-fatality rates, high cost of antifungal drugs and development of antifungal resistance. The diagnostic challenges and poor outcomes associated with IFD have resulted in excessive empirical use of antifungals in various hospital settings, exposing many patients without IFD to potential drug toxicities as well as causing spiralling antifungal drug costs. Further complexity arises as different patient groups show marked variation in their risk for IFD, fungal epidemiology, sensitivity and specificity of diagnostic tests and the pharmacokinetics and pharmacodynamics of antifungal drugs. To address these issues and to ensure optimal management of IFD, specialist knowledge and experience from a range of backgrounds is required, which extends beyond the remit of most antibiotic stewardship programmes. The first step in the development of any antifungal stewardship (AFS) programme is to build a multidisciplinary team encompassing the necessary expertise in the management of IFD to develop and implement the AFS programme. The specific roles of the key individuals within the AFS team and the importance of collaboration are discussed in this article.

  16. Potent heterologous antifungal proteins from cheeseweed (Malva parviflora).

    Science.gov (United States)

    Wang, X; Bunkers, G J

    2000-12-20

    Two novel antifungal proteins were purified and characterized from cheeseweed (Malva parviflora). Both proteins, designated CW-1 and CW-2, are composed of two different subunits of 5000 and 3000 Da, respectively. These proteins possess very potent antifungal activities, and more interestingly the inhibition is fungicidal instead of fungistatic. At low salt condition, the IC(50) of CW-1 and CW-2 against Fusarium graminearum (Fg) is 2.5 ppm. At high salt condition which diminishes the antifungal activity of many antifungal proteins, both CW-1 and CW-2 still maintain potent activity against Fg with IC(50) of 10 ppm. The two subunits could be separated by gel filtration in the presence of 6 M urea, but their antifungal activity cannot be recovered after the removal of urea. Amino acid sequence analysis indicates that both subunits of CW-1 show homology to 2S albumin, whereas the two subunits of CW-2 have homology to vicilin protein from cotton. To our knowledge, this is the first report of isolation and characterization of heterologous antifungal proteins from any source.

  17. An antifungal peptide from Phaseolus vulgaris cv. brown kidney bean

    Institute of Scientific and Technical Information of China (English)

    Yau Sang Chan; Jack Ho Wong; Evandro Fei Fang; Wen Liang Pan; Tzi Bun Ng

    2012-01-01

    A 5.4-kDa antifungal peptide,with an N-terminal sequence highly homologous to defensins and inhibitory activity against Mycosphaerella arachidicola (IC5o=3 μM),Setospaeria turcica and Bipolaris maydis,was isolated from the seeds of Phaseolus vulgaris cv.brown kidney bean.The peptide was purified by employing a protocol that entailed adsorption on Affi-gel blue gel and Mono S and finally gel filtration on Superdex 75.The antifungal activity of the peptide against M.arachidicola was stable in the pH range 3-12 and in the temperature range 0℃ to 80℃.There was a slight reduction of the antifungal activity at pH 2 and 13,and the activity was indiscernible at pH 0,1,and 14.The activity at 90℃ and 100℃ was slightly diminished.Deposition of Congo red at the hyphal tips of M.arachidicola was induced by the peptide indicating inhibition of hyphal growth.The lack of antiproliferative activity of brown kidney bean antifungal peptide toward tumor cells,in contrast to the presence of such activity of other antifungal peptides,indicates that different domains are responsible for the antifungal and antiproliferative activities.

  18. An antifungal peptide from Phaseolus vulgaris cv. brown kidney bean.

    Science.gov (United States)

    Chan, Yau Sang; Wong, Jack Ho; Fang, Evandro Fei; Pan, Wen Liang; Ng, Tzi Bun

    2012-04-01

    A 5.4-kDa antifungal peptide, with an N-terminal sequence highly homologous to defensins and inhibitory activity against Mycosphaerella arachidicola (IC(50)= 3 μM), Setospaeria turcica and Bipolaris maydis, was isolated from the seeds of Phaseolus vulgaris cv. brown kidney bean. The peptide was purified by employing a protocol that entailed adsorption on Affi-gel blue gel and Mono S and finally gel filtration on Superdex 75. The antifungal activity of the peptide against M. arachidicola was stable in the pH range 3-12 and in the temperature range 0°C to 80°C. There was a slight reduction of the antifungal activity at pH 2 and 13, and the activity was indiscernible at pH 0, 1, and 14. The activity at 90°C and 100°C was slightly diminished. Deposition of Congo red at the hyphal tips of M. arachidicola was induced by the peptide indicating inhibition of hyphal growth. The lack of antiproliferative activity of brown kidney bean antifungal peptide toward tumor cells, in contrast to the presence of such activity of other antifungal peptides, indicates that different domains are responsible for the antifungal and antiproliferative activities.

  19. Antifungal effect and mechanism of garlic oil on Penicillium funiculosum.

    Science.gov (United States)

    Li, Wen-Ru; Shi, Qing-Shan; Liang, Qing; Huang, Xiao-Mo; Chen, Yi-Ben

    2014-10-01

    Garlic oil is a kind of fungicide, but little is known about its antifungal effects and mechanism. In this study, the chemical constituents, antifungal activity, and effects of garlic oil were studied with Penicillium funiculosum as a model strain. Results showed that the minimum fungicidal concentrations (MFCs, v/v) were 0.125 and 0.0313 % in agar medium and broth medium, respectively, suggesting that the garlic oil had a strong antifungal activity. The main ingredients of garlic oil were identified as sulfides, mainly including disulfides (36 %), trisulfides (32 %) and monosulfides (29 %) by gas chromatograph-mass spectrometer (GC/MS), which were estimated as the dominant antifungal factors. The observation results by transmission electron microscope (TEM) and scanning electron microscope (SEM) indicated that garlic oil could firstly penetrate into hyphae cells and even their organelles, and then destroy the cellular structure, finally leading to the leakage of both cytoplasm and macromolecules. Further proteomic analysis displayed garlic oil was able to induce a stimulated or weakened expression of some key proteins for physiological metabolism. Therefore, our study proved that garlic oil can work multiple sites of the hyphae of P. funiculosum to cause their death. The high antifungal effects of garlic oil makes it a broad application prospect in antifungal industries.

  20. Species Distribution and In Vitro Antifungal Susceptibility of Vulvovaginal Candida Isolates in China

    Science.gov (United States)

    Wang, Feng-Juan; Zhang, Dai; Liu, Zhao-Hui; Wu, Wen-Xiang; Bai, Hui-Hui; Dong, Han-Yu

    2016-01-01

    Background: Vulvovaginal candidiasis (VVC) was a common infection associated with lifelong harassment of woman's social and sexual life. The purpose of this study was to describe the species distribution and in vitro antifungal susceptibility of Candida species (Candida spp.) isolated from patients with VVC over 8 years. Methods: Species which isolated from patients with VVC in Peking University First Hospital were identified using chromogenic culture media. Susceptibility to common antifungal agents was determined using agar diffusion method based on CLSI M44-A2 document. SPSS software (version 14.0, Inc., Chicago, IL, USA) was used for statistical analysis, involving statistical description and Chi-square test. Results: The most common strains were Candida (C.) albicans, 80.5% (n = 1775) followed by C. glabrata, 18.1% (n = 400). Nystatin exhibited excellent activity against all species (<4% resistant [R]). Resistance to azole drugs varied among different species. C. albicans: clotrimazole (3.1% R) < fluconazole (16.6% R) < itraconazole (51.5% R) < miconazole (54.0% R); C. glabrata: miconazole (25.6% R) < clotrimazole (50.5% R) < itraconazole (61.9% R) < fluconazole (73.3% R); Candida krusei: clotrimazole (0 R) < fluconazole (57.7% R) < miconazole (73.1% R) < itraconazole (83.3% R). The susceptibility of fluconazole was noticeably decreasing among all species in the study period. Conclusions: Nystatin was the optimal choice for the treatment of VVC at present. The species distribution and in vitro antifungal susceptibility of Candida spp. isolated from patients with VVC had changed over time. PMID:27174323

  1. Essential Oil from Inula britannica Extraction with SF-CO2 and Its Antifungal Activity

    Institute of Scientific and Technical Information of China (English)

    ZHAO Te; GAO Fei; ZHOU Lin; SONG Tian-you

    2013-01-01

    The aim of this study was to determine the extraction technique of supercritical fluid carbon dioxide (SF-CO2) for the essential oil from Inula britannica flowers and its antifungal activities against plant pathogenic fungi for its potential application as botanical fungicide. The effects of factors, including extraction temperature, extraction pressure, SF-CO2 flow rate, flower powder size, and time on the essential oil yield were studied using the single factor experiment. An orthogonal experiment was conducted to determine the best operating conditions for the maximum extraction oil yield. Adopting the optimum conditions, the maximum yield reached 10.01% at 40°C temperature, 30 MPa pressure, 60 mesh flower powder size, 20 L h-1 SF-CO2 flow rate, and 90 min extraction time. The antifungal activities of I. britannica essential oil using the SF-CO2 against the most important plant pathogenic fungi were also examined through in vitro and in vivo tests. Sixteen plant pathogenic fungi were inhibited to varying degrees at 1 mg mL-1 concentration of the essential oil. The mycelial growth of Gaeumannomyces graminis var. tritici was completely inhibited. The radial growths of Phytophthora capsici and Fusarium monilifome were also inhibited by 83.76 and 64.69%, respectively. In addition, the essential oil can inhibit the spore germination of Fusarium oxysporum f. sp. vasinfectum, Phytophthora capsici, Colletotrichum orbiculare, and Pyricularia grisea, and the corresponding inhibition rates were 98.26, 96.54, 87.89, and 87.35%respectively. The present study has demonstrated that the essential oil of I. britannica flowers extracted through the SF-CO2 technique is one potential and promising antifungal agent that can be used as botanical fungicide to protect crops.

  2. Antifungal activity of low molecular weight chitosan produced from non-traditional marine resources

    Directory of Open Access Journals (Sweden)

    Francisco Pires Avelelas

    2014-06-01

    Full Text Available The four plants pathogens, Botrytis cinerea, Phytophthora cinnamomi, Cryphonectria parasitica and Heterobasidion annosum are responsible for several diseases affecting different plant species in Portugal, such as pines (H. annosum, chestnuts (P. cinnamomi and C. parasitica and eucalyptus (B. cinerea. These pathogens incurs in large economic losses, and ultimately causes the death of these plants. The use of biopolymers as antimicrobial agents, such as chitosan (derived from chitin, is increasing, in order to reduce the negative impact of conventional chemical treatments on the environment, avoiding health risks. Therefore, eco-friendly polymers were produced through (1 N-acetylation with addition of acetic anhydride and (2 hydrogen peroxide of chitosan samples, obtained from two different sources: shrimp (commercial chitosan and swimming crab bycatch specie Polybius henslowii. The chemical structure and molecular weight of the prepared chitosan derivatives, water soluble chitosan (WSC and chitooligosaccharides (COS, was confirmed by Fourier Transform Infrared (FT-IR and Gel Permeation Chromatography (GPC and their antifungal activity evaluated against Botrytis cinerea, Phytophthora cinnamomi, Cryphonectria parasitica and Heterobasidion annosum. The concentration range varied from 0.0125 to 0.1 mg/mL and inhibition percentages were determined by differences in radial growth on the agar plates for all species. Although not all species tested exhibited equal vulnerability towards the concentrations range, antifungal activity of chitosan samples proved to be dependent, increasing the inhibitory capacity with lower concentrations. The results obtained support the use of chitosan fromPolybius henslowii when compared with commercial chitosan with shrimp towards antifungal approaches, suggesting that chitin producers can rely on this crab waste as a raw material for chitin extraction, adding value to this bycatch specie. Financial support was obtained

  3. Posaconazole after previous antifungal therapy with voriconazole for therapy of invasive aspergillus disease, a retrospective analysis.

    Science.gov (United States)

    Heinz, Werner J; Egerer, Gerlinde; Lellek, Heinrich; Boehme, Angelika; Greiner, Jochen

    2013-05-01

    Invasive aspergillosis is an important cause of morbidity and mortality in haematological patients. Current guidelines recommend voriconazole as first-line therapy. A change in class of antifungal agent is generally recommended for salvage therapy. The focus of this analysis was to assess if posaconazole is suitable for salvage therapy following voriconazole treatment. This was a retrospective investigation on patients with sequential antifungal therapy of posaconazole after voriconazole identified at four German hospitals. Response rates at 30 and 60 days following start of posaconazole application and toxicity of azoles by comparing liver enzymes and cholestasis parameters were evaluated. Data were analysed by descriptive statistics. Overall, the success rate was 72.2% [15 of 36 patients showed complete response (41.7%), 11 patients partial response (30.6%) at any time point], eight patients failed treatment and two were not evaluable. Mean laboratory values increased during voriconazole and decreased during posaconazole treatment: aspartate aminotransferase (increase: 31.9 U l(-1) vs. decrease: 19.6 U l(-1) ), alanine aminotransferase (32.4 U l(-1) vs. 19.8 U l(-1) ), gamma-glutamyl transferase (124.2 U l(-1) vs. 152.3 U l(-1) ) and alkaline phosphatase (71.5 U l(-1) vs. 40.3 U l(-1) ) respectively. No patient discontinued posaconazole therapy due to an adverse event. In this analysis posaconazole was a safe and effective antifungal salvage therapy in patients with prior administration of another triazole.

  4. Multilaboratory Evaluation of In Vitro Antifungal Susceptibility Testing of Dermatophytes for ME1111

    Science.gov (United States)

    Chaturvedi, V.; Diekema, D.; Ostrosky-Zeichner, L.; Rennie, R.; Walsh, T.; Wengenack, N.; Fothergill, A.; Wiederhold, N.

    2015-01-01

    ME1111 is a novel small molecule antifungal agent under development for the topical treatment of onychomycosis. Standardization of the susceptibility testing method for this candidate antifungal is needed. Toward this end, 8 independent laboratories determined the interlaboratory reproducibility of ME1111 susceptibility testing. In addition, we subsequently identified 2 strains as quality control (QC) isolates for the method. In the reproducibility study, 5 blinded clinical strains each of Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum were tested, while the QC study tested 6 blinded T. rubrum or T. mentagrophytes ATCC strains. Testing was performed in frozen microtiter panels according to the Clinical and Laboratory Standards Institute (CLSI) M38-A2 methodology. In the reproducibility study, 9 of 15 clinical strains showed interlaboratory agreement of >90% at the 80% inhibition endpoint, with a range of agreement of 76.2% to 100%. In the QC study, 4 of the 6 ATCC strains showed interlaboratory agreement of >90%. ME1111 demonstrated excellent interlaboratory agreement when tested against dermatophytes. Based on this data, the CLSI Subcommittee on Antifungal Susceptibility Tests approved the susceptibility testing of ME1111 against dermatophytes according to M38-A2 methodology, which stipulates RPMI 1640 as the test medium, an inoculum size of 1 to 3 × 103 CFU/ml, and an incubation time and temperature of 96 h at 35°C. The MIC endpoint should be 80% inhibition compared with the growth control. T. rubrum ATCC MYA-4438 and T. mentagrophytes ATCC 28185 were selected as QC isolates, with an acceptable range of 0.12 to 1 μg/ml for the two strains. PMID:26719434

  5. Species Distribution and In Vitro Antifungal Susceptibility of Vulvovaginal Candida Isolates in China

    Institute of Scientific and Technical Information of China (English)

    Feng-Juan Wang; Dai Zhang; Zhao-Hui Liu; Wen-Xiang Wu; Hui-Hui Bai; Han-Yu Dong

    2016-01-01

    Background:Vulvovaginal candidiasis (VVC) was a common infection associated with lifelong harassment of woman's social and sexual life.The purpose of this study was to describe the species distribution and in vitro antifungal susceptibility of Candida species (Candida spp.) isolated from patients with WC over 8 years.Methods:Species which isolated from patients with WC in Peking University First Hospital were identified using chromogenic culture media.Susceptibility to common antifungal agents was determined using agar diffusion method based on CLSI M44-A2 document.SPSS software (version 14.0,Inc.,Chicago,IL,USA) was used for statistical analysis,involving statistical description and Chi-square test.Results:The most common strains were Candida (C.) albicans,80.5% (n =1775) followed by C.glabrata,18.1% (n =400).Nystatin exhibited excellent activity against all species (<4% resistant [R]).Resistance to azole drugs varied among different species.C albicans:clotrimazole (3.1% R) < fluconazole (16.6% R) < itraconazole (51.5% R) < miconazole (54.0% R);C.glabrata:miconazole (25.6% R) < clotrimazole (50.5% R) < itraconazole (61.9% R) < fluconazole (73.3% R);Candida krusei:clotrimazole (0 R) < fluconazole (57.7% R) < miconazole (73.1% R) < itraconazole (83.3% R).The susceptibility offluconazole was noticeably decreasing among all species in the study period.Conclusions:Nystatin was the optimal choice for the treatment of WC at present.The species distribution and in vitro antifungal susceptibility of Candida spp.isolated from patients with VVC had changed over time.

  6. Nationwide study of candidemia, antifungal use, and antifungal drug resistance in Iceland, 2000 to 2011.

    Science.gov (United States)

    Asmundsdottir, Lena Ros; Erlendsdottir, Helga; Gottfredsson, Magnus

    2013-03-01

    Candidemia is often a life-threatening infection, with highly variable incidence among countries. We conducted a nationwide study of candidemia in Iceland from 2000 to 2011, in order to determine recent trends in incidence rates, fungal species distribution, antifungal susceptibility patterns, and concurrent antifungal consumption. A total of 208 infection episodes in 199 patients were identified. The average incidence during the 12 years was 5.7 cases/100,000 population/year, which was significantly higher than that from 1990 to 1999 (4.3/100,000/year; P = 0.02). A significant reduction in the use of blood cultures was noted in the last 3 years of the study, coinciding with the economic crisis in the country (P 60 years, and varied by gender. Age-specific incidence among males >80 years old was 28.6/100,000/year, and it was 8.3/100,000/year for females in this age group (P = 0.028). The 30-day survival rate among adult patients remained unchanged compared to that from 1990 to 1999 (70.4% versus 69.5%, P = 0.97). Candida albicans was the predominant species (56%), followed by C. glabrata (16%) and C. tropicalis (13%). The species distribution remained stable compared to that from previous decades. Fluconazole use increased 2.4-fold from 2000 to 2011, with no increase in resistance. In summary, the incidence of candidemia in Iceland has continued to increase but may have reached a steady state, and no increase in antifungal drug resistance has been noted. Decreased use of blood cultures toward the end of the study may have influenced detection rates.

  7. Functional assignment of YvgO, a novel set of purified and chemically characterized proteinaceous antifungal variants produced by Bacillus thuringiensis SF361.

    Science.gov (United States)

    Manns, David C; Churey, John J; Worobo, Randy W

    2012-04-01

    This study reports a novel class of antifungal protein derived from bacterial origin. Bacillus thuringiensis SF361, the strain also responsible for producing the novel bacteriocin thurincin H, exhibits broad antifungal activity against select members of several fungal genera, including Aspergillus, Byssochlamys, and Penicillium, as well as the pathogenic yeast Candida albicans. Optimal antifungal production and secretion were observed after-log phase growth when incubated at 37°C in a carbohydrate-free growth medium. High-performance liquid chromatography purification was performed after pH-selective ammonium sulfate precipitation and size-exclusion chromatography. Intact mass analysis and peptide mass fingerprinting identified the 13,484-Da protein to be a mass homolog to the YvgO protein construct sequenced from Bacillus cereus AH 1134. Further analysis via amino-terminal sequencing also revealed the existence of four distinct yet equally efficacious YvgO variants differing only within the first four N-terminal residues. YvgO was found to be remarkably stable, maintaining its antifungal activity under a wide pH and temperature range. When assayed against the toxigenic species Byssochlamys fulva H25, the selected primary filamentous fungal indicator, the MIC was estimated to be 1.5 ppm. Candida albicans 3153 was more resistant, exhibiting MICs between 25 and 800 ppm, depending on growth conditions. YvgO is unique among antifungals, showing no known sequential or functional homology to the typical classes of antifungal proteins, including common membrane-acting agents such as cellulases and glucanases. Due to its activity against an array of pathogenic and spoilage fungi, the potentials for clinical, agricultural, and food-processing applications are encouraging.

  8. Macrocyclic trichothecenes as antifungal and anticancer compounds.

    Science.gov (United States)

    de Carvalho, Maira Peres; Weich, Herbert; Abraham, Wolf-Rainer

    2016-01-01

    Trichothecenes are sesquiterpenoid metabolites produced by fungi and species of the plant genus Baccharis, family Asteraceae. They comprise a tricyclic core with an epoxide at C-12 and C-13 and can be grouped into non-macrocyclic and macrocyclic compounds. While many of these compounds are of concern in agriculture, the macrocyclic metabolites have been evaluated as antiviral, anti-cancer, antimalarial and antifungal compounds. Some known cytotoxic responses on eukaryotic cells include inhibition of protein, DNA and RNA syntheses, interference with mitochondrial function, effects on cell division and membranes. These targets however have been elucidated essentially employing non-macrocyclic trichothecenes and only one or two closely related macrocyclic compounds. For several macrocyclic trichothecenes high selectivity against fungal species and against cancer cell lines have been reported suggesting that the macrocycle and its stereochemistry are of crucial importance regarding biological activity and selectivity. This review is focused on compounds belonging to the macrocyclic type, where a cyclic diester or triester ring binds to the trichothecane moiety at C-4 and C- 15 leading to natural products belonging to the groups of satratoxins, verrucarins, roridins, myrotoxins and baccharinoids. Their biological activities, cytotoxic mechanisms and structure-activity relationships (SAR) are discussed. From the reported data it becomes evident that even small changes in the molecules can lead to pronounced effects on biological activity or selectivity against cancer cells lines. Understanding the underlying mechanisms may help to design highly specific drugs for cancer therapy.

  9. Antifungal and molluscicidal saponins from Serjania salzmanniana.

    Science.gov (United States)

    Ekabo, O A; Farnsworth, N R; Henderson, T O; Mao, G; Mukherjee, R

    1996-04-01

    An investigation of Serjania salzmanniana for biologically active substances has led to the isolation of two novel saponins, salzmannianoside A (3-O-[[beta-D- glucopyranosyl-(1-->4)]-[alpha-L-rhamnopyranosyl-(1-->2)]-alpha-L- arabinopyranosyl] gypsogenin) [3] and salzmannianoside B (3-O-[[beta-D-glucopyranosyl-(1-->4)]-[alpha-L- arabinopyranosyl-(1-->3)-alpha-L-rhamnopyranosyl-(1-->2)] -alpha-L-arabinopyranosyl] hederagenin) (4). Two known saponins, pulsatilla saponin D (3-O-[[beta-D- glucopyranosyl-(1-->4)]-[alpha-L-rhamnopyranosyl-(1-->2)]-alpha-L- arabinopyranosyl] hederagenin) (1) and 3-O-[[beta-D-glucopyranosyl-(1-->4)]-[alpha-L-rhamnopyranosyl-(1-->2)]-a lpha-L- arabinopyranosyl] oleanolic acid (2) were also isolated from this plant. The structures of 3 and 4 were elucidated by FABMS and 2D NMR techniques. All these four saponins were mollusicidal, causing 70-100% mortality at 10 ppm against Biomphalaria alexandrina, a vector of Schistosoma mansoni in the Nile Valley. The saponins also showed antifungal activity against Cryptococcus neoformans and Candida albicans at minimal inhibitory concentrations of 8 and 16 micrograms/mL, respectively.

  10. Antifungal activity of plant extracts against dermatophytes.

    Science.gov (United States)

    Ali-Shtayeh, M S; Abu Ghdeib, S I

    1999-01-01

    The aqueous extracts (15 micrograms ml-1 medium) of 22 plants used in folkloric medicine in Palestine were investigated for their antifungal activity and minimum inhibitory concentrations (MICs) against nine isolates of Microsporum canis, Trichophyton mentagrophytes and Trichophyton violaceum. The extract of the different plant species reduced colony growth of the three dermatophytes by 36 to 100% compared with the control treatment. Antimycotic activity of the extract against the three dermatophytes varied significantly (P Inula viscosa, J. regia and P. lentiscus against T. mentagrophytes; and Asphodelus luteus, A. arvensis, C. spinosa, Clematis cirrhosa, I. viscosa, J. regia, P. lentiscus, Plumbago europea, Ruscus aculeatus, Retema raetam and Salvia fruticosa against T. violaceum. The MICs of these most active plants ranged from 0.6 to 40 micrograms ml-1. The three dermatophytes differed significantly with regard to their susceptibility to plant extracts. Trichophyton violaceum was the most susceptible being completely inhibited by 50% of the extracts followed by M. canis and T. mentagrophytes which were completely inhibited by only 23 and 14% of the extracts, respectively.

  11. Antifungal prophylaxis in stem cell transplantation centers in Turkey

    Directory of Open Access Journals (Sweden)

    Hamdi Akan

    2011-12-01

    Full Text Available Objective: This study aimed to determine the current state of antifungal prophylaxis in Turkish stem cell transplantation (SCT centers. Materials and Methods: The were 38 active stem cell transplantation centers in Turkey, 28 of which were registered with the European Group for Blood and Marrow Transplantation (EBMT. Survey questionnaires were sent to the 28 EBMT centers in an effort to collect data on antifungal prophylaxis in different settings. In all, 24 of the centers completed the survey; 1 of the 24 centers was excluded from the study, as it was under construction at the time and was not performing transplantation.Results: In all, 15 (65% of the 23 centers were adult SCT centers, 7 (31% were pediatric SCT centers, and 1 center treated both adult and pediatric patients. All centers (23/23 performed both allogeneic and autologous transplants, 20 centers performed non-myeloablative transplants, 8 performed cord blood transplants, and 7 performed unrelated transplants. Primary antifungal prophylaxis was used at all 23 centers during allogeneic transplants, whereas 18 of the 23 centers used it during every autologous transplant and 2 of the 23 centers used it during autologous transplants on a per case basis. The most common drug used for prophylaxis was fluconazole (F (21/23, followed by itraconazole (I (3/23, amphotericin-B (2/23, and posaconazole (1/23. Among the 23 centers, 3 reported that for allogenic transplants they changed the antifungal prophylactic in cases of graft versus host disease (GVHD, and 12 of the 23 centers reported that they changed the antifungal prophylactic in case of nearby construction. All 23 centers performed secondary prophylaxis. Conclusion: Antifungal prophylaxis for hematopoetic SCT patients was the standard protocol in the 23 centers included in the study, usually with such azoles as F. The introduction of posaconazole in Turkey and the potential approval of voriconazole for antifungal prophylaxis will

  12. [Species distribution and antifungal susceptibility of Candida spp. causing superficial mycosis. Coro, Falcon state, Venezuela].

    Science.gov (United States)

    Saúl-García, Yotsabeth; Humbría-García, Leyla; Hernández-Valles, Rosaura

    2015-09-01

    Candida species other than C. albicans are often described as causative agents of superficial mycosis and are more resistant to treatment with azoles. In order to determine the distribution of species and in vitro antifungal susceptibility of Candida spp., one ambispective study, which analyzed 18 yeast isolates obtained from samples from patients diagnosed with superficial mycosis, was performed. Taxonomic identification was performed by macroscopic visualization of the growth characteristics in chromogenic agar and by conventional methods. The susceptibility to fluconazole and voriconazole was evaluated by the disc diffusion method. Most of the isolates (88.8%), came from nail samples. C. parapsilosis was the most common species, followed by C. tropicalis, C. albicans and C. krusei, which confirmed the prevalence of non-albicans species as a cause of superficial mycoses. The pattern of susceptibility to fluconazole and voriconazole was similar: all isolates of C. parapsilosis and C. albicans were susceptible, while 83.3% of C. tropicalis showed sensitivity to both antifungals. C. krusei, fluconazole-resistant species showed intermediate susceptibility io voriconazole. The use of chromogenic agar allowed to detect mixed infections in nail samples, involving Candida spp. and C. tropicalis in one case, the latter with resistance to both fluconazole and voriconazole. The results demonstrate the importance of species identification and susceptibility testing to avoid therapeutic failures in superficial mycoses.

  13. ArtinM offers new perspectives in the development of antifungal therapy

    Directory of Open Access Journals (Sweden)

    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

  14. "Green preservatives": combating fungi in the food and feed industry by applying antifungal lactic acid bacteria.

    Science.gov (United States)

    Pawlowska, Agata M; Zannini, Emanuele; Coffey, Aidan; Arendt, Elke K

    2012-01-01

    Fungal food spoilage plays a pivotal role in the deterioration of food and feed systems and some of them are also able to produce toxic compounds for humans and animals. The mycotoxins produced by fungi can cause serious health hazards, including cancerogenic, immunotoxic, teratogenic, neurotoxic, nephrotoxic and hepatotoxic effects, and Kashin-Beck disease. In addition to this, fungal spoilage/pathogens are causing losses of marketable quality and hygiene of foodstuffs, resulting in major economic problem throughout the world. Nowadays, food spoilage can be prevented using physical and chemical methods, but no efficient strategy has been proposed so far to reduce the microbial growth ensuring public health. Therefore, lactic acid bacteria (LAB) can play an important role as natural preservatives. The protection of food products using LAB is mainly due to the production of antifungal compounds such as carboxylic acids, fatty acids, ethanol, carbon dioxide, hydrogen peroxide, and bacteriocins. In addition to this, LAB can also positively contribute to the flavor, texture, and nutritional value of food products. This review mainly focuses on the use of LAB for food preservation given their extensive industrial application in a wide range of foods and feeds. The attention points out the several industrial patents concerning the use of antifungal LAB as biocontrol agent against spoilage organisms in different fermented foods and feeds.

  15. Identification of an extracellular antifungal protein from the endophytic fungus Colletotrichum sp. DM06.

    Science.gov (United States)

    Dey, Prabuddha; Kamdar, Maulik R; Mandal, Santi M; Maiti, Mrinal K

    2013-02-01

    An extracellular antifungal protein of 28 kDa (exAFP-C28) was identified from an endophytic fungus Colletotrichum sp. DM-06. After purification, the MIC value of exAFP-C28 against Candida albicans, a well-known human pathogenic fungus was found to be 32 μg/mL that unaffected the human red blood cells. The antifungal activity associated with exAFP-C28 was manifested by the increased membrane permeability of C. albicans cells followed by disruption. Proteomics and bioinformatics analyses revealed that several peptide fragments of exAFP-C28 have identity with the bacterial 50S ribosomal protein L10, and a stretch of 55 amino acids of two peptide fragments corresponding to the Nterminus of L10 protein is capable of forming amphipathic helix required for membrane penetration. Taken together, our results suggest that the exAFP-C28 protein from Colletotrichum sp. DM-06 is a promising therapeutic agent in controlling candidiasis disease in animals including humans.

  16. Antifungal, antibacterial and antimycobacterial activity of Entada abysinnica Steudel ex A. Rich (Fabaceae methanol extract

    Directory of Open Access Journals (Sweden)

    Richard M Mariita

    2010-01-01

    Full Text Available The purpose of the study was to investigate the antifungal, antibacterial and antimycobacterial properties of methanol extract of Entada abysinnica steudel ex. A. Rich (Fabaceae leaves used by herbalists from the Lake Victoria region, Kenya. The extract was tested against four strains of mycobacteria (Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium fortuitum, and Mycobacterium smegmatis using BACTEC Mycobacteria Growth Indicator Tube (MGIT 960 system and the proportional method. Standard procedures were used to determine the zones of inhibition, minimum inhibitory concentrations (MICs and minimum bactericidal/fungicidal concentrations (MBCs/MFCs for Candida albicans, Salmonella typhi, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, and Klebsiella pneumoniae. The extract showed activity against some mycobacteria strains, especially M. tuberculosis. It also showed strong antimicrobial activity (zones of inhibition were between 9.00 and 14.10 mm against C. albicans, Sa. typhi, and St. aureus. The extract gave a better zone of inhibition against C. albicans than fluconazole whose zone of inhibition was 13.00 mm. The MICs and MBCs for C. albicans and Sa. typhi were good. The crude extracts were also analyzed for the presence of phytochemicals. Phytochemical screening indicated that the extract most abundantly contained tannins, saponins, and flavonoids. The data suggest that the methanolic leaves extract of E. abysinnica could be a rich source of antimicrobial agents, especially antifungals. The results further show that there is some merit in the use of the plant in alternative medical practices. However, bioassays of isolated compounds are underway and will be reported during subsequent communications.

  17. Species Distribution, Virulence Factors, and Antifungal Susceptibility Among Candida parapsilosis Complex Isolates Recovered from Clinical Specimens.

    Science.gov (United States)

    da Silva, Beatriz Virgínia; Silva, Larissa Beatriz; de Oliveira, Diego Batista Carneiro; da Silva, Paulo Roberto; Ferreira-Paim, Kennio; Andrade-Silva, Leonardo Euripides; Silva-Vergara, Mario León; Andrade, Anderson Assunção

    2015-12-01

    The Candida parapsilosis complex has emerged as an important fungal pathogen. In spite of this, relatively little is known about its characteristics. Thus, the purposes of this study were (1) to determine by BanI-RFLP-assay the occurrence of C. parapsilosis complex species among 81 clinical isolates primarily identified as C. parapsilosis; (2) to evaluate their in vitro production of virulence factors; and (3) to compare their susceptibility profiles, grown as planktonic cells and biofilms, against amphotericin B, fluconazole, voriconazole, and caspofungin by following the Clinical and Laboratory Standards Institute (CLSI) guidelines. Seventy-seven isolates (95%) were identified as C. parapsilosis sensu stricto, 2 (2.5%) as C. orthopsilosis, and 2 (2.5%) as C. metapsilosis. Protease activity was detected in 29 (37.7%) isolates of C. parapsilosis sensu stricto, whereas only 7 (9.1%) exhibited phospholipase activity. None of the C. metapsilosis or C. orthopsilosis was able to produce protease or phospholipase. Biofilm production was detected in 35 (43.2%) isolates, among which 33 were C. parapsilosis sensu stricto and 2 were C. orthopsilosis. Antifungal resistance was uncommon; only one C. metapsilosis was fluconazole resistant. However, biofilm-producing isolates showed a marked resistance to all antifungal agents tested, particularly to voriconazole. This knowledge could be of clinical relevance for guiding therapeutic decisions.

  18. Antifungal susceptibility of Candida albicans biofilms on titanium discs with different surface roughness.

    Science.gov (United States)

    Tsang, C S P; Ng, H; McMillan, A S

    2007-12-01

    Although it is well known that fungal biofilms have increased resistance to antimicrobial agents, limited information is available on the formation of candidal biofilms on implant surfaces with different surface roughness and their resistance to conventional antifungal therapy. In the current study, the effect of increasing the surface roughness of titanium discs on the susceptibility of Candida albicans biofilms to amphotericin B was determined. Grade I commercially pure titanium discs were sandblasted with 99.6% aluminium oxide of different grit sizes, producing surface roughness of 0.90, 1.88 and 3.82 microm (Groups A, B and C), respectively (P XTT assay. The 50% reduction in metabolic activity (50% RMA) of planktonic C. albicans (0.5 microg/mL) was much lower than those from Groups A, B and C (2, 16, 2 microg/mL, respectively), while the 50% RMA from Group B was three-fold higher than those from Groups A and C. In conclusion, difference in titanium surface roughness was associated with variations in the antifungal resistance of the candidal biofilm. Group C appeared to have an optimum surface roughness for biofilm resistance.

  19. Flow cytometry susceptibility testing for conventional antifungal drugs and Comparison with the NCCLS Broth Macrodilution Test

    Directory of Open Access Journals (Sweden)

    M.J. Najafzadeh

    2009-08-01

    Full Text Available Introduction: During the last decade, the incidence of fungal infection has been increased in many countries. Because of the advent of resistant to antifungal agents, determination of an efficient strategic plan for treatment of fungal disease is an important issue in clinical mycology. Many methods have been introduced and developed for determination of invitro susceptibility tests. During the recent years, flow cytometry has developed to solving the problem and many papers have documented the usefulness of this technique. Materials and methods: As the first step, the invitro susceptibility of standard PTCC (Persian Type of Culture Collection strain and some clinical isolates of Candida consisting of Candida albicans, C. dubliniensis, C. glabrata, C. kefyer and C. parapsilosis were evaluated by macrodilution broth method according to NCCLS (National Committee for Clinical Laboratory Standards guidelines and flow cytometry susceptibility test. Results:  The data indicated that macro dilution broth methods and flow cytometry have the same results in determination of MIC (Minimum Inhibitory Concentration for amphotericin B, clotrimazole, fluconazole, ketoconazole and miconazole in C. albicans PTCC 5027 as well as clinical Candida isolates, such as C.albicans, C.dubliniensis, C.glabrata C.kefyr, and C.parapsilosis. Discussion: Comparing the results obtained by macrodilution broth and flow cytometry methods revealed that flow cytometry was faster. It is suggested that flow cytometry susceptibility test can be used as a powerful tool for determination of MIC and administration of the best antifungal drug in treatment of patients with Candida infections.

  20. Antifungal curcumin promotes chitin accumulation associated with decreased virulence of Sporothrix schenckii.

    Science.gov (United States)

    Huang, Lilin; Zhang, Jing; Song, Tianzhang; Yuan, Liyan; Zhou, Junjie; Yin, Hongling; He, Tailong; Gao, Wenchao; Sun, Yao; Hu, Xuchu; Huang, Huaiqiu

    2016-05-01

    Curcumin, a yellow polyphenol compound, is known to possess antifungal activity for a range of pathogenic fungi. However, the fungicidal mechanism of curcumin (CUR) has not been identified. We have occasionally found that chitin redistributes to the cell wall outer layer of Sporothrix schenckii (S. schenckii) upon sublethal CUR treatment. Whether CUR can affect chitin synthesis via the protein kinase C (PKC) signaling pathway has not been investigated. This study describes a direct fungicidal activity of CUR against S. schenckii demonstrated by the results of a checkerboard microdilution assay and, for the first time, a synergistic effect of CUR with terbinafine (TRB). Furthermore, the results of real-time PCR showed that sublethal CUR upregulated the transcription of PKC, chitin synthase1 (CHS1), and chitin synthase3 (CHS3) in S. schenckii. The fluorescence staining results using wheat germ agglutinin-fluorescein isothiocyanate (WGA-FITC) and calcofluor white (CFW) consistently showed that chitin exposure and total chitin content were increased on the conidial cell wall of S. schenckii by sublethal CUR treatment. A histopathological analysis of mice infected with CUR-treated conidia showed dampened inflammation in the local lesion and a reduced fungal burden. The ELISA results showed proinflammatory cytokine secretion at an early stage from macrophages stimulated by the CUR-treated conidia. The present data led to the conclusion that CUR is a potential antifungal agent and that its fungicidal mechanism may involve chitin accumulation on the cell wall of S. schenckii, which is associated with decreased virulence in infected mice.

  1. Antifungal Susceptibility Patterns of Candida Species Recovered from Endotracheal Tube in an Intensive Care Unit.

    Science.gov (United States)

    Baghdadi, Elham; Khodavaisy, Sadegh; Rezaie, Sassan; Abolghasem, Sara; Kiasat, Neda; Salehi, Zahra; Sharifynia, Somayeh; Aala, Farzad

    2016-01-01

    Aims. Biofilms formed by Candida species which associated with drastically enhanced resistance against most antimicrobial agents. The aim of this study was to identify and determine the antifungal susceptibility pattern of Candida species isolated from endotracheal tubes from ICU patients. Methods. One hundred forty ICU patients with tracheal tubes who were intubated and mechanically ventilated were surveyed for endotracheal tube biofilms. Samples were processed for quantitative microbial culture. Yeast isolates were identified to the species level based on morphological characteristics and their identity was confirmed by PCR-RFLP. Antifungal susceptibility testing was determined according to CLSI document (M27-A3). Results. Ninety-five strains of Candida were obtained from endotracheal tubes of which C. albicans (n = 34; 35.7%) was the most frequently isolated species followed by other species which included C. glabrata (n = 24; 25.2%), C. parapsilosis (n = 16; 16.8%), C. tropicalis (n = 12; 12.6%), and C. krusei (n = 9; 9.4%). The resulting MIC90 for all Candida species were in increasing order as follows: caspofungin (0.5 μg/mL); amphotericin B (2 μg/mL); voriconazole (8.8 μg/mL); itraconazole (16 μg/mL); and fluconazole (64 μg/mL). Conclusion. Candida species recovered from endotracheal tube are the most susceptible to caspofungin.

  2. Microdilution in vitro antifungal susceptibility of Exophiala dermatitidis, a systemic opportunist.

    Science.gov (United States)

    Badali, H; de Hoog, G S; Sudhadham, M; Meis, J F

    2011-11-01

    The in vitro activities of eight antifungal agents were determined against clinical (n = 63 genotype A, n = 3 genotype B) and environmental (n = 2 genotype A, n = 13 genotype B) strains of Exophiala dermatitidis. The resulting MIC(90)s for all strains (N = 81) were, in increasing order, as follows: posaconazole, 0.125 μg/ml; itraconazole, 0.25 μg/ml; voriconazole, 0.5 μg/ml; amphotericin B, 0.5 μg/ml; isavuconazole, 1 μ/ml; caspofungin, 8 μg/ml; anidulafungin, 8 μg/ml and fluconazole, 16 μg/ml. There were no significant differences in the patterns of susceptibility between genotypes A and B, environmental and clinical strains, isolates recovered from cutaneous and deep locations and strains from different geographical areas (P > 0.05). The difference in the MIC(90)s between each of these groups was not more than one dilution. The present study demonstrated that, based on in vitro activity, posaconazole and itraconazole have the highest activity against this fungus. In addition, voriconazole and the experimental broad-spectrum antifungal triazole, isavuconazole, both of which are available as intravenous preparations, have adequate activity against E. dermatitidis. However, in vivo efficacy remains to be determined.

  3. ANTIFUNGAL ACTIVITY OF STILBENES AGAINST CANDIDA ALBICANS BY TIME KILL ASSAY

    Directory of Open Access Journals (Sweden)

    S. Nishanth Kumar*, J. V. Siji, Bala Nambisan and C. Mohandas

    2012-06-01

    Full Text Available Candida albicans is one of the most important fungi associated with oral candidiasis and the treatment of this fungi is a serious problem today because of the resistance of these fungi against conventionally used drugs. So, there is an urgent need of alternative antifungal substances especially from the natural sources. The study was conducted to examine the MFC and time kill activity of two stilbenes [3, 4', 5-trihydroxystilbene (1 and 3,5-dihydroxy-4-isopropylstilbene (2] purified from a bacterium associated with entomopathgenic nematode against C. albicans. The activity was also compared to amphotericin B. The cytotoxicity of stilbenes was also tested against normal human cell lines (L231 lung epithelial and FS normal fibroblast. Results showed that stilbenes was effective against C. albicans with MIC and MFC of 64 and 128 µg/ml for compound 1 and 32 and 64 µg/ml for compound 2. The time kill assay of stilbenes against C. albicans was more effective than amphotericin B. No cytotoxicity was recorded for stilbenes upto 200 µg/ml. The strong antifungal activity and low cytotoxicity of stilbenes make it a promising agent for the treatment of Candida.

  4. 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.

  5. Assessment of in vitro antifungal activity of preparation ''fin Candimis'' against Candida strains

    Directory of Open Access Journals (Sweden)

    Anna Głowacka

    2013-12-01

    Full Text Available The aim of the study was to assess the antifungal activity of preparation „fin Candimis” (oregano essential oil against yeast-like strains belonging to the genus Candida. During the investigation, there were used up nine Candida albicans strains and ten C. glabrata strains isolated from different clinical material, along with one C. albicans demonstration strain ATCC 90028. The oregano essential oil, utilized in the study, was obtained from fresh leaves of Origanum vulgare L. and bore a trade name „fin Candimis”. According to data yielded by its manufacturer, concentration of pure oregano essential oil in preparation „fin Candimis” totals up to 210 mg/ml. The susceptibility of the Candida strains to preparation „fin Candimis” was assessed by means of the disc-diffusion method, upon the Sabouraud solid medium (after a 24-hour incubation of the cultures at temperature of 37 degrees centigrade; the oregano essential oil had been diluted in 1 ml of DMSO, according to the geometrical progression. A measure of the antifungal activity of preparation „fin Candimis” was the minimal inhibitory concentration (MIC, in terms of the fungus growth. Preparation „fin Candimis” is capable of being applied in the prevention and treatment of candidiasis – alone, or as a natural adjunctive agent. The C. albicans strains are more susceptible to preparation „fin Candimis” in comparison to the C. glabrata ones.

  6. 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

  7. Chemical composition and antifungal activity of essential oil from Eucalyptus smithii against dermatophytes

    Directory of Open Access Journals (Sweden)

    Edilene Bolutari Baptista

    2015-12-01

    Full Text Available ABSTRACT INTRODUCTION: In this study, we evaluated the chemical composition of a commercial sample of essential oil from Eucalyptus smithii R.T. Baker and its antifungal activity against Microsporum canis ATCC 32903, Microsporum gypseum ATCC 14683, Trichophyton mentagrophytes ATCC 9533, T. mentagrophytes ATCC 11480, T. mentagrophytes ATCC 11481, and Trichophyton rubrum CCT 5507. METHODS: Morphological changes in these fungi after treatment with the oil were determined by scanning electron microscopy (SEM. The antifungal activity of the oil was determined on the basis of minimum inhibitory concentration (MIC and minimum fungicidal concentration (MFC values. RESULTS: The compound 1,8-cineole was found to be the predominant component (72.2% of the essential oil. The MIC values of the oil ranged from 62.5μg·mL−1 to >1,000μg·mL−1, and the MFC values of the oil ranged from 125μg·mL−1 to >1,000μg·mL−1. SEM analysis showed physical damage and morphological alterations in the fungi exposed to this oil. CONCLUSIONS: We demonstrated the potential of Eucalyptus smithii essential oil as a natural therapeutic agent for the treatment of dermatophytosis.

  8. Antifungal Susceptibility Patterns of Candida Species Recovered from Endotracheal Tube in an Intensive Care Unit

    Directory of Open Access Journals (Sweden)

    Elham Baghdadi

    2016-01-01

    Full Text Available Aims. Biofilms formed by Candida species which associated with drastically enhanced resistance against most antimicrobial agents. The aim of this study was to identify and determine the antifungal susceptibility pattern of Candida species isolated from endotracheal tubes from ICU patients. Methods. One hundred forty ICU patients with tracheal tubes who were intubated and mechanically ventilated were surveyed for endotracheal tube biofilms. Samples were processed for quantitative microbial culture. Yeast isolates were identified to the species level based on morphological characteristics and their identity was confirmed by PCR-RFLP. Antifungal susceptibility testing was determined according to CLSI document (M27-A3. Results. Ninety-five strains of Candida were obtained from endotracheal tubes of which C. albicans (n=34; 35.7% was the most frequently isolated species followed by other species which included C. glabrata (n=24; 25.2%, C. parapsilosis (n=16; 16.8%, C. tropicalis (n=12; 12.6%, and C. krusei (n=9; 9.4%. The resulting MIC90 for all Candida species were in increasing order as follows: caspofungin (0.5 μg/mL; amphotericin B (2 μg/mL; voriconazole (8.8 μg/mL; itraconazole (16 μg/mL; and fluconazole (64 μg/mL. Conclusion. Candida species recovered from endotracheal tube are the most susceptible to caspofungin.

  9. 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.

  10. In vitro antifungal activity of extracts obtained from Hypericum perforatum adventitious roots cultured in a mist bioreactor against planktonic cells and biofilm of Malassezia furfur.

    Science.gov (United States)

    Simonetti, Giovanna; Tocci, Noemi; Valletta, Alessio; Brasili, Elisa; D'Auria, Felicia Diodata; Idoux, Alicia; Pasqua, Gabriella

    2016-01-01

    Xanthone-rich extracts from Hypericum perforatum root cultures grown in a Mist Bioreactor as antifungal agents against Malassezia furfur. Extracts of Hypericum perforatum roots grown in a bioreactor showed activity against planktonic cells and biofilm of Malassezia furfur. Dried biomass, obtained from roots grown under controlled conditions in a ROOTec mist bioreactor, has been extracted with solvents of increasing polarity (i.e. chloroform, ethyl acetate and methanol). The methanolic fraction was the richest in xanthones (2.86 ± 0.43 mg g(-1) DW) as revealed by HPLC. The minimal inhibitory concentration of the methanol extract against M. furfur planktonic cells was 16 μg mL(-1). The inhibition percentage of biofilm formation, at a concentration of 16 μg mL(-1), ranged from 14% to 39%. The results show that H. perforatum root extracts could be used as new antifungal agents in the treatment of Malassezia infections.

  11. Antifungal activity of ibuprofen against aspergillus species and its interaction with common antifungal drugs

    Institute of Scientific and Technical Information of China (English)

    LI Li-juan; CHEN Wei; XU Hui; WAN Zhe; LI Ruo-yu; LIU Wei

    2010-01-01

    Background The incidence of invasive aspergillosis (IA) has increased in frequency in immunocompromised patients with a variety of diseases. The poor prognosis might be due to limited treatment option. This study aimed to evaluate antifungal activity of ibuprofen against clinical isolates of aspergillus species, as well as its interaction with azoles or with amphotericin B or with micafungin.Methods Antifungal activity of ibuprofen against 10 strains of Aspergillus fumigatus, Aspergillus flavus, and Aspergillus terreus were tested with both disk diffusion assay and standard broth microdilution method. To determine whether ibuprofen combined with itraconazole, voriconazole, amphotericin B, or micafungin had interactive effects on aspergillus spp., we used both disk diffusion assay and Chequerboard method.Results As for disk diffusion method, ibuprofen produced a zone of growth inhibition with diameters of (20.1±3.9) mm at 48 hours of incubation. As for broth microdilution method, the minimal inhibitory concentration (MIC) ranges of ibuprofen against aspergillus spp. were 1000-2000 μg/ml, and the minimal fungicidal concentration (MFC) ranges of that was 2000-8000 μg/ml. For 2 of 5 isolates, when ibuprofen combined with itraconazole or voriconazole, the zones of growth inhibition were larger than those of the individual drug. The results of Chequerboard method showed that fractional inhibitory concentration index (FICI) ranges were 1.125-2.500.Conclusions Ibuprofen is active against aspergillus spp.. And ibuprofen does not affect the in vitro activity of itraconazole, voriconazole, amphotericin B or micafungin against aspergillus spp..

  12. Prevalence and antifungal susceptibility of Candida parapsilosis complex isolates collected from oral cavities of HIV-infected individuals.

    Science.gov (United States)

    Moris, D V; Melhem, M S C; Martins, M A; Souza, L R; Kacew, S; Szeszs, M W; Carvalho, L R; Pimenta-Rodrigues, M V; Berghs, H A M; Mendes, R P

    2012-12-01

    At present, few data are available on the prevalence and antifungal susceptibility of Candida parapsilosis complex isolates from HIV-infected individuals. The C. parapsilosis complex comprises three species, C. parapsilosis sensu stricto, C. metapsilosis and C. orthopsilosis. Fifteen of 318 Candida isolates were identified as members of the C. parapsilosis complex by PCR and restriction fragment length polymorphism (RFLP). The prevalence of C. parapsilosis complex isolates was 4.7 %, 2.2 % being identified as C. parapsilosis sensu stricto and 2.5 % as C. metapsilosis, while no C. orthopsilosis was isolated. This is believed to be the first study that has identified isolates of C. metapsilosis obtained from the oral cavity of HIV-infected individuals. Antifungal susceptibility tests indicated that all the isolates were susceptible to amphotericin B (AMB), fluconazole (FLC), ketoconazole (KTC), itraconazole (ITC), voriconazole (VRC) and caspofungin (CASPO). Although isolates of C. parapsilosis sensu stricto and C. metapsilosis were susceptible to FLC, isolates of C. metapsilosis showed a tendency for higher MICs (≥1.0 µg ml(-1)). Based upon the frequency of candidiasis and the fact that certain isolates of the C. parapsilosis complex respond differently to FLC therapy, our data may be of therapeutic relevance with respect to susceptibility and potential resistance to specific antifungal agents. Our data suggest that C. metapsilosis can be a human commensal; its importance as a pathogen has yet to be confirmed.

  13. 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.

  14. Synthesis, Antiproliferative and Antifungal Activities of 1,2,3-Triazole-Substituted Carnosic Acid and Carnosol Derivatives

    Directory of Open Access Journals (Sweden)

    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.

  15. Antifungal activity of wide band gap Thioglycolic acid capped ZnS:Mn semiconductor nanoparticles against some pathogenic fungi.

    Science.gov (United States)

    Ibrahim, Isam M; Ali, Iftikhar M; Dheeb, Batol Imran; Abas, Qayes A; Asmeit Ramizy; Eisa, M H; Aljameel, A I

    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 ~2.73nm 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.

  16. Antifungal and Zearalenone Inhibitory Activity of Pediococcus pentosaceus Isolated from Dairy Products on Fusarium graminearum.

    Science.gov (United States)

    Sellamani, Muthulakshmi; Kalagatur, Naveen K; Siddaiah, Chandranayaka; Mudili, Venkataramana; Krishna, Kadirvelu; Natarajan, Gopalan; Rao Putcha, Venkata L

    2016-01-01

    The present study was aimed to evaluate the bio-control efficacy of Pediococcus pentosaceus isolated from traditional fermented dairy products originated from India, against the growth and zearalenone (ZEA) production of Fusarium graminearum. The cell-free supernatants of P. pentosaceus (PPCS) were prepared and chemical profiling was carried out by GC-MS and MALDI-TOF analysis. Chemical profiling of PPCS evidenced that, the presence of phenolic antioxidants, which are responsible for the antifungal activity. Another hand, MALDI-TOF analysis also indicated the presence of antimicrobial peptides. To know the antioxidant potential of PPCS, DPPH free radical scavenging assay was carried out and IC50 value was determined as 32 ± 1.89 μL/mL. The antifungal activity of P. pentosaceus was determined by dual culture overlay technique and zone of inhibition was recorded as 47 ± 2.81%, and antifungal activity of PPCS on F. graminearum was determined by micro-well dilution and scanning electron microscopic techniques. The minimum inhibitory concentration (MIC) of PPCS was determined as 66 ± 2.18 μL/mL in the present study. Also a clear variation in the micromorphology of mycelia treated with MIC value of PPCS compared to untreated control was documented. Further, the mechanism of growth inhibition was revealed by ergosterol analysis and determination of reactive oxygen species (ROS) in PPCS treated samples. The effects of PPCS on mycelial biomass and ZEA production were observed in a dose-dependent manner. The mechanism behind the suppression of ZEA production was studied by reverse transcriptase qPCR analysis of ZEA metabolic pathway genes (PKS4 and PKS13), and results showed that there is a dose dependent down-regulation of target gene expression in PPCS treated samples. The results of the present study were collectively proved that, the antifungal and ZEA inhibitory activity of PPCS against F. graminearum and it may find a potential application in agriculture and food

  17. Antifungal and Zearalenone Inhibitory Activity of Pediococcus pentosaceus Isolated from Dairy Products on Fusarium graminearum

    Science.gov (United States)

    Sellamani, Muthulakshmi; Kalagatur, Naveen K.; Siddaiah, Chandranayaka; Mudili, Venkataramana; Krishna, Kadirvelu; Natarajan, Gopalan; Rao Putcha, Venkata L.

    2016-01-01

    The present study was aimed to evaluate the bio-control efficacy of Pediococcus pentosaceus isolated from traditional fermented dairy products originated from India, against the growth and zearalenone (ZEA) production of Fusarium graminearum. The cell-free supernatants of P. pentosaceus (PPCS) were prepared and chemical profiling was carried out by GC-MS and MALDI-TOF analysis. Chemical profiling of PPCS evidenced that, the presence of phenolic antioxidants, which are responsible for the antifungal activity. Another hand, MALDI-TOF analysis also indicated the presence of antimicrobial peptides. To know the antioxidant potential of PPCS, DPPH free radical scavenging assay was carried out and IC50 value was determined as 32 ± 1.89 μL/mL. The antifungal activity of P. pentosaceus was determined by dual culture overlay technique and zone of inhibition was recorded as 47 ± 2.81%, and antifungal activity of PPCS on F. graminearum was determined by micro-well dilution and scanning electron microscopic techniques. The minimum inhibitory concentration (MIC) of PPCS was determined as 66 ± 2.18 μL/mL in the present study. Also a clear variation in the micromorphology of mycelia treated with MIC value of PPCS compared to untreated control was documented. Further, the mechanism of growth inhibition was revealed by ergosterol analysis and determination of reactive oxygen species (ROS) in PPCS treated samples. The effects of PPCS on mycelial biomass and ZEA production were observed in a dose-dependent manner. The mechanism behind the suppression of ZEA production was studied by reverse transcriptase qPCR analysis of ZEA metabolic pathway genes (PKS4 and PKS13), and results showed that there is a dose dependent down-regulation of target gene expression in PPCS treated samples. The results of the present study were collectively proved that, the antifungal and ZEA inhibitory activity of PPCS against F. graminearum and it may find a potential application in agriculture and food

  18. Isavuconazole and nine comparator antifungal susceptibility profiles for common and uncommon Candida species collected in 2012: application of new CLSI clinical breakpoints and epidemiological cutoff values.

    Science.gov (United States)

    Castanheira, Mariana; Messer, Shawn A; Rhomberg, Paul R; Dietrich, Rachel R; Jones, Ronald N; Pfaller, Michael A

    2014-08-01

    The in vitro activity of isavuconazole and nine antifungal comparator agents was assessed using reference broth microdilution methods against 1,421 common and uncommon species of Candida from a 2012 global survey. Isolates were identified using CHROMagar, biochemical methods and sequencing of ITS and/or 28S regions. Candida spp. were classified as either susceptible or resistant and as wild type (WT) or non-WT using CLSI clinical breakpoints or epidemiological cutoff values, respectively, for the antifungal agents. Isolates included 1,421 organisms from 21 different species of Candida. Among Candida spp., resistance to all 10 tested antifungal agents was low (0.0-7.9 %). The vast majority of each species of Candida, with the exception of Candida glabrata, Candida krusei, and Candida guilliermondii (modal MICs of 0.5 µg/ml), were inhibited by ≤0.12 µg/ml of isavuconazole (99.0 %; range 94.3 % [Candida tropicalis] to 100.0 % [Candida lusitaniae and Candida dubliniensis]). C. glabrata, C. krusei, and C. guilliermondii were largely inhibited by ≤1 µg/ml of isavuconazole (89.7, 96.9 and 92.8 %, respectively). Decreased susceptibility to isavuconazole was most prominent with C. glabrata where the modal MIC for isavuconazole was 0.5 µg/ml for those strains that were SDD to fluconazole or WT to voriconazole, and was 4 µg/ml for those that were either resistant or non-WT to fluconazole or voriconazole, respectively. In conclusion, these data document the activity of isavuconazole and generally the low resistance levels to the available antifungal agents in a large, contemporary (2012), global collection of molecularly characterized species of Candida.

  19. Antifungal hydroxy fatty acids produced during sourdough fermentation: microbial and enzymatic pathways, and antifungal activity in bread.

    Science.gov (United States)

    Black, Brenna A; Zannini, Emanuele; Curtis, Jonathan M; Gänzle, Michael G

    2013-03-01

    Lactobacilli convert linoleic acid to hydroxy fatty acids; however, this conversion has not been demonstrated in food fermentations and it remains unknown whether hydroxy fatty acids produced by lactobacilli have antifungal activity. This study aimed to determine whether lactobacilli convert linoleic acid to metabolites with antifungal activity and to assess whether this conversion can be employed to delay fungal growth on bread. Aqueous and organic extracts from seven strains of lactobacilli grown in modified De Man Rogosa Sharpe medium or sourdough were assayed for antifungal activity. Lactobacillus hammesii exhibited increased antifungal activity upon the addition of linoleic acid as a substrate. Bioassay-guided fractionation attributed the antifungal activity of L. hammesii to a monohydroxy C(18:1) fatty acid. Comparison of its antifungal activity to those of other hydroxy fatty acids revealed that the monohydroxy fraction from L. hammesii and coriolic (13-hydroxy-9,11-octadecadienoic) acid were the most active, with MICs of 0.1 to 0.7 g liter(-1). Ricinoleic (12-hydroxy-9-octadecenoic) acid was active at a MIC of 2.4 g liter(-1). L. hammesii accumulated the monohydroxy C(18:1) fatty acid in sourdough to a concentration of 0.73 ± 0.03 g liter(-1) (mean ± standard deviation). Generation of hydroxy fatty acids in sourdough also occurred through enzymatic oxidation of linoleic acid to coriolic acid. The use of 20% sourdough fermented with L. hammesii or the use of 0.15% coriolic acid in bread making increased the mold-free shelf life by 2 to 3 days or from 2 to more than 6 days, respectively. In conclusion, L. hammesii converts linoleic acid in sourdough and the resulting monohydroxy octadecenoic acid exerts antifungal activity in bread.

  20. [Uricosuric agent].

    Science.gov (United States)

    Ohno, Iwao

    2008-04-01

    Urate lowering treatment is indicated in patients with recurrent acute attacks, tophi, gouty arthropathy, radiographic changes of gout, multiple joint involvement, or associated uric acid nephrolithiasis. Uricosuric agents like benzbromarone and probenecid are very useful to treat hyperuricemia as well as allopurinol (xanthine oxidase inhibitor). Uricosuric agents act the urate lowering effect through blocking the URAT1, an urate transporter, in brush border of renal proximal tubular cells. In order to avoid the nephrotoxicity and urolithiasis due to increasing of urinary urate excretion by using uricosuric agents, the proper urinary tract management (enough urine volume and correction of aciduria) should be performed.

  1. Antifungal activity of essential oils against selected terverticillate penicillia.

    Science.gov (United States)

    Felšöciová, Soňa; Kačániová, Miroslava; Horská, Elena; Vukovič, Nenad; Hleba, Lukáš; Petrová, Jana; Rovná, Katarina; Stričík, Michal; Hajduová, Zuzana

    2015-01-01

    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.

  2. Antifungal susceptibilities of Candida species isolated from urine culture.

    Science.gov (United States)

    Toka Özer, Türkan; Durmaz, Süleyman; Yula, Erkan

    2016-09-01

    Candida spp. are the most common opportunistic mycosis worldwide. Although Candida albicans is the most common cause of urinary tract infections, the frequency of non-albicans Candida species is increasing with common use of antifungal in the prophylaxis and treatment. This may lead to difficulties in treatment. Antifungal tests should be applied with identification of species for effective treatment. In this study, identification of Candida species isolated from urine culture and investigation of susceptibility of these strains to amphotericin B, flucytosine, fluconazole, voriconazole was aimed. In this study, 58 Candida strains isolated from urine cultures at Osmaniye State Hospital between January 2012 and April 2013 were included. Urine culture and antifungal susceptibility tests were applied. Incidence rate of Candida spp. was determined as C. albicans (56.9%), Candida glabrata (20.6%), Candida tropicalis (10.3%), Candida parapsilosis (7%), Candida krusei (3.4%), Candida kefyr (1.8%). Most of the isolates were susceptible to amphotericin B, flucytosine, fluconazole, voriconazole. Twenty three (39.7%) Candida strains were isolated from internal medical branches and Intensive Care Unit and 12 (20.6%) from the Surgical Medical Branches. C. albicans and C. glabrata species were isolated most frequently as a candiduria factor in this hospital between January 2012 and April 2013. The analysis of antifungal susceptibility profile shows no significant resistance to antifungals.

  3. Antimycobacterial and Antifungal Activities of Selected Four Salvia Species

    Directory of Open Access Journals (Sweden)

    Nur Tan

    2016-03-01

    Full Text Available The content of essential oils of endemic Salvia cilicica was analyzed by GC-FID and GC-MS techniques. Spathulenol (23.8 %, caryophyllene oxide (14.9 % and hexadecanoic acid (10.3 % were identified as the major components in the oil of Salvia cilicica. Additionally, in this study ethanol extracts of the aerial parts and essential oils of four Salvia species ( S. cilicica, S. officinalis, S. fruticosa, S. tomentosa , as well as the roots of S. cilicica were investigated their antimycobacterial and antifungal activities including infectious diseases. The antimycobacterial activity was analyzed against three Mycobacterium tuberculosis (sensitive-, resistant-standard strains and multidrug resistance clinical isolate strains and the antifungal activity was compared with two dermotophytes (Microsporum gypseum and Trichophyton mentagrophytes var. erinacei and three Candida species by the broth microdilution method. The essentials oils of the four tested Salvia species showed high antimycobacterial and antifungal activity (MIC between 0.2-12.5 mcg/mL in comparison to the aerial parts and root extracts . The antifungal and antimycobacterial potential of the ethanol extracts and essential oils were introduced to determine whether, Salvia species can be used in phytotherapy against the yeasts, dermatophytes and M. tuberculosis. To the best of our knowledge this is the first study of S. cilicica about their antimycobacterial and antifungal activities and chemical composition of its essential oils.

  4. An antifungal defensin from Phaseolus vulgaris cv. 'Cloud Bean'.

    Science.gov (United States)

    Wu, Xiangli; Sun, Jian; Zhang, Guoqing; Wang, Hexiang; Ng, Tzi Bun

    2011-01-15

    An antifungal peptide with a defensin-like sequence and exhibiting a molecular mass of 7.3kDa was purified from dried seeds of Phaseolus vulgaris 'Cloud Bean'. The isolation procedure entailed anion exchange chromatography on DEAE-cellulose, affinity chromatography an Affi-gel blue gel, cation exchange chromatography on SP-Sepharose, and gel filtration by fast protein liquid chromatography on Superdex 75. Although the antifungal peptide was unadsorbed on DEAE-cellulose, it was adsorbed on both Affi-gel blue gel and SP-Sepharose. The antifungal peptide exerted antifungal activity against Mycosphaerella arachidicola with an IC(50) value of 1.8 μM. It was also active against Fusarium oxysporum with an IC(50) value of 2.2 μM. It had no inhibitory effect on HIV-1 reverse transcriptase when tested up to 100 μM. Proliferation of L1210 mouse leukemia cells and MBL2 lymphoma cells was inhibited by the antifungal peptide with an IC(50) of 10 μM and 40 μM, respectively.

  5. Exploration of Islamic medicine plant extracts as powerful antifungals for the prevention of mycotoxigenic Aspergilli growth in organic silage

    DEFF Research Database (Denmark)

    Tayel, Ahmed A.; Salem, Mohammed F.; El-Tras, Wael F.

    2011-01-01

    Feed contamination with mycotoxins is a major risk factor for animals and humans as several toxins can exist as residues in meat and milk products, giving rise to carry-over to consumers via ingestion of foods of animal origin. The starting point for prevention, in this chain, is to eliminate the...... the growth of mycotoxigenic fungi in the animal forage. Ten plant extracts, recommended in Islamic medicine, were evaluated as antifungal agents against mycotoxigenic Aspergilli, i.e. Aspergillus flavus and A. ochraceus, growth in organic maize silage....

  6. 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

  7. The clinical spectrum of Exophiala jeanselmei, with a case report and in vitro antifungal susceptibility of the species.

    Science.gov (United States)

    Badali, H; Najafzadeh, M J; van Esbroeck, M; van den Enden, E; Tarazooie, B; Meis, J F G M; de Hoog, G S

    2010-03-01

    Exophiala jeanselmei is clinically redefined as a rare agent of subcutaneous lesions of traumatic origin, eventually causing eumycetoma. Mycetoma is a localized, chronic, suppurative subcutaneous infection of tissue and contiguous bone after a traumatic inoculation of the causative organism. In advanced stages of the infection, one finds tumefaction, abscess formation and draining sinuses. The species has been described as being common in the environment, but molecular methods have only confirmed its occurrence in clinical samples. Current diagnostics of E. jeanselmei is based on sequence data of the Internal Transcribed Spacer (ITS) region of ribosomal DNA (rDNA), which sufficiently reflects the taxonomy of this group. The first purpose of this study was the re-identification of all clinical (n=11) and environmental strains (n=6) maintained under the name E. jeanselmei, and to establish clinical preference of the species in its restricted sense. Given the high incidence of eumycetoma in endemic areas, the second goal of this investigation was the evaluation of in vitro susceptibility of E.jeanselmei to eight conventional and new generations of antifungal drugs to improve antifungal therapy in patients. As an example, we describe a case of black grain mycetoma in a 43-year-old Thai male with several draining sinuses involving the left foot. The disease required extensive surgical excision coupled with intense antifungal chemotherapy to achieve cure. In vitro studies demonstrated that posaconazole and itraconazole had the highest antifungal activity against E. jeanselmei and E. oligosperma for which high MICs were found for caspofungin. However, their clinical effectiveness in the treatment of Exophiala infections remains to be determined.

  8. Saccharomyces cerevisiae biofilm tolerance towards systemic antifungals depends on growth phase

    DEFF Research Database (Denmark)

    Bojsen, Rasmus Kenneth; Regenberg, Birgitte; Folkesson, Sven Anders

    2014-01-01

    growing planktonic cells, voriconazole had limited antifungal activity, flucytosine was fungistatic, caspofungin and amphotericin B were fungicidal. In growth-arrested cells, only amphotericin B had antifungal activity. Confocal microscopy and colony count viability assays revealed that the response...

  9. Antibiotic Agents

    Science.gov (United States)

    ... Superbugs and Drugs" Home | Contact Us General Background: Antibiotic Agents What is an antibacterial and how are ... with the growth and reproduction of bacteria. While antibiotics and antibacterials both attack bacteria, these terms have ...

  10. Vasoactive Agents

    OpenAIRE

    Husedzinovic, Ino; Bradic, Nikola; Goranovic, Tanja

    2006-01-01

    This article is a short review of vasoactive drugs which are in use in todays clinical practice. In the past century, development of vasoactive drugs went through several phases. All of these drugs are today divided into several groups, depending on their place of action, pharmacological pathways and/or effects on target organ or organ system. Hence, many different agents are today in clinical practice, we have shown comparison between them. These agents provide new directions in the treatmen...

  11. Novel triazole alcohol antifungals derived from fluconazole: design, synthesis, and biological activity.

    Science.gov (United States)

    Hashemi, Seyedeh Mahdieh; Badali, Hamid; Faramarzi, Mohammad Ali; Samadi, Nasrin; Afsarian, Mohammad Hosein; Irannejad, Hamid; Emami, Saeed

    2015-02-01

    A series of new triazole alcohol antifungals were designed by replacing one of the triazolyl moiety from fluconazole with a distinct 4-amino-3-mercapto-1,2,4-triazole motif, which is found in some antimicrobial agents. The antimicrobial susceptibility testing of target compounds demonstrated that the direct analogs of fluconazole (difluorophenethyl-triazoles) were less active against fungi, while compound 10h containing dichloro substitutions on both phenyl rings of the molecule had potent activity against yeasts including Candida albicans (four strains) and Cryptococcus neoformans (MICs = 2-8 μg/mL). Also, compound 10h was active against Candida parapsilosis, Epidermophyton floccosum, and Trichophyton mentagrophytes, while it showed no activity against Gram-positive and Gram-negative bacteria. Finally, a molecular docking study suggested that compound 10h interacts suitably with lanosterol 14α-demethylase, which is the key enzyme in ergosterol biosynthesis.

  12. Isolation and characterization of antifungal peptides produced by Bacillus amyloliquefaciens LBM5006.

    Science.gov (United States)

    Benitez, Lisianne Brittes; Velho, Renata Voltolini; Lisboa, Marcia Pagno; Medina, Luis Fernando da Costa; Brandelli, Adriano

    2010-12-01

    Bacillus amyloliquefaciens LBM 5006 produces antagonistic activity against pathogenic bacteria and phytopathogenic fungi, including Aspergillus spp., Fusarium spp., and Bipolaris sorokiniana. PCR analysis revealed the presence of ituD, but not sfp genes, coding for iturin and surfactin, respectively. The antimicrobial substance produced by this strain was isolated by ammonium sulfate precipitation, gel filtration chromatography and 1-butanol extraction. The ultraviolet spectrum was typical of a polypeptide and the infrared spectrum indicates the presence of peptide bonds and acyl group(s). The antimicrobial substance was resistant to proteolytic enzymes and heat treatment, and was reactive with ninhydrin. Mass spectroscopy analysis indicated that B. amyloliquefaciens LBM 5006 produces two antimicrobial peptides, with main peaks at m/z 1,058 Da and 1,464 Da, corresponding to iturin-like and fengycin-like peptides, respectively. B. amyloliquefaciens LBM 5006 showed significant activity against phytopatogenic fungi, showing potential for use as a biocontrol agent or production of antifungal preparations.

  13. Synthesis and Anti-Fungal Activity of Seven Oleanolic Acid Glycosides

    Directory of Open Access Journals (Sweden)

    Daoquan Wang

    2011-01-01

    Full Text Available In order to develop potential anti-fungal agents, seven glycoconjugates composed of a-L-rhamnose, 6-deoxy-a-L-talose, b-D-galactose, a-D-mannose, b-D-xylose-(1®4-6-deoxy-a-L-talose, b-D-galactose-(1®4-a-L-rhamnose, b-D-galactose-(1®3-b-D-xylose-(1®4-6-deoxy-a-L-talose as the glycone and oleanolic acid as the aglycone were synthesized in an efficient and practical way using glycosyl trichloroacetimidates as donors. The structures of the new compounds were confirmed by MS, 1H-NMR and 13C- NMR. Preliminary studies based on means of mycelium growth rate, indicated that all the compounds possess certain fungicidal activity against Sclerotinia sclerotiorum (Lib. de Bary, Rhizoctonia solani Kuhn, Botrytis cinerea Pers and Phytophthora parasitica Dast.

  14. Chemical composition, cytotoxicity, antimicrobial and antifungal activity of several essential oils.

    Science.gov (United States)

    Cannas, Sara; Usai, Donatella; Tardugno, Roberta; Benvenuti, Stefania; Pellati, Federica; Zanetti, Stefania; Molicotti, Paola

    2016-01-01

    Essential oils (EOs) are known and used for their biological, antibacterial, antifungal and antioxidant properties. Numerous studies have shown that EOs exhibit a large spectrum of biological activities in vitro. The incidence of drug-resistant pathogens and the toxicity of antibiotics have drawn attention to the antimicrobial activity of natural products, encouraging the development of alternative treatments. The aim of this study was to analyse the phytochemical and the cytotoxic characteristic of 36 EOs; we then evaluated the antimicrobial activity of the less-toxic EOs on Gram-positive, Gram-negative and fungi strains. The results showed low cytotoxicity in seven EOs and good activity against Gram-negative and Candida spp. strains. Based on our results, EOs could be proposed as a novel group of therapeutic agents. Further experiments are necessary to confirm their pharmacological effectiveness, and to determine potential toxic effects and the mechanism of their activity in in vivo models.

  15. Evaluation of the antifungal activities of various extracts from Pistacia atlantica Desf

    Directory of Open Access Journals (Sweden)

    Mehraban Falahati

    2015-09-01

    Results: Based on GC/MS analysis, the main constituents of P. atlantica fruit extracts were &beta-myrcene (41.4%, &alpha-pinene (32.48% and limonene (4.66%, respectively, whereas the major constituents of P. atlantica leaf extracts were trans-caryophyllene (15.18%, &alpha-amorphene (8.1% and neo-allo-ocimene (6.21%, respectively. As the findings indicated, all the constituents exhibited both fungistatic and fungicidal activities, with MICs ranging from 6.66 to 26.66 mg/mL and MFCs ranging from 13.3 to 37.3 mg/mL, respectively. Among the evaluated extracts, the methanolic fresh fruit extract of P. atlantica was significantly more effective than other extracts (P<0.05. Conclusion: Based on the findings of the present study, novel antifungal agents need to be developed, and use of P. atlantica should be promoted in the traditional treatment of Candida infections.

  16. Antifungal compounds from the rhizome and roots of Ferula hermonis.

    Science.gov (United States)

    Al-Ja'fari, Abdel-Hadi; Vila, Roser; Freixa, Blanca; Costa, Joan; Cañigueral, Salvador

    2013-06-01

    The antifungal activity of hexane, dichloromethane, methanol and aqueous extracts from the rhizome and root of Ferula hermonis was assayed in vitro by the agar disk diffusion method against a panel of human opportunistic and pathogenic fungi. Among them, the hexane and dichloromethane extracts showed the highest activity particularly against the dermatophytes Microsporum gypseum and Tricophyton mentagrophytes as well as the yeast Candida lactis-condensi. Activity-guided fractionation of both extracts using an agar overlay bioautographic method led to the isolation of two antifungal compounds which were identified as the daucane aryl esters jaeschkeanadiol p-hydroxybenzoate (ferutinin) and jaeschkeanadiol benzoate (teferidin). Determination of minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) values of both compounds evidenced a stronger antifungal activity for ferutinin than for teferidin. Particularly, T. mentagrophytes was the most sensitive strain with MIC and MFC values ranging from 8 to 256 µg/mL.

  17. Mechanisms of antifungal drug resistance in Candida dubliniensis.

    LENUS (Irish Health Repository)

    Coleman, David C

    2010-06-01

    Candida dubliniensis was first described in 1995 and is the most closely related species to the predominant human fungal pathogen Candida albicans. C. dubliniensis is significantly less prevalent and less pathogenic than C. albicans and is primarily associated with infections in HIV-infected individuals and other immunocompromised cohorts. The population structure of C. dubliniensis consists of three well-defined major clades and is significantly less diverse than C. albicans. The majority of C. dubliniensis isolates are susceptible to antifungal drugs commonly used to treat Candida infections. To date only two major patterns of antifungal drug resistance have been identified and the molecular mechanisms of these are very similar to the resistance mechanisms that have been described previously in C. albicans. However, significant differences are evident in the predominant antifungal drug mechanisms employed by C. dubliniensis, differences that reflect its more clonal nature, its lower prevalence and characteristics of its genome, the complete sequence of which has only recently been determined.

  18. Targeting efflux pumps to overcome antifungal drug resistance.

    Science.gov (United States)

    Holmes, Ann R; Cardno, Tony S; Strouse, J Jacob; Ivnitski-Steele, Irena; Keniya, Mikhail V; Lackovic, Kurt; Monk, Brian C; Sklar, Larry A; Cannon, Richard D

    2016-08-01

    Resistance to antifungal drugs is an increasingly significant clinical problem. The most common antifungal resistance encountered is efflux pump-mediated resistance of Candida species to azole drugs. One approach to overcome this resistance is to inhibit the pumps and chemosensitize resistant strains to azole drugs. Drug discovery targeting fungal efflux pumps could thus result in the development of azole-enhancing combination therapy. Heterologous expression of fungal efflux pumps in Saccharomyces cerevisiae provides a versatile system for screening for pump inhibitors. Fungal efflux pumps transport a range of xenobiotics including fluorescent compounds. This enables the use of fluorescence-based detection, as well as growth inhibition assays, in screens to discover compounds targeting efflux-mediated antifungal drug resistance. A variety of medium- and high-throughput screens have been used to identify a number of chemical entities that inhibit fungal efflux pumps.

  19. Antifungal prophylaxis following reduced-intensity stem cell transplantation.

    Science.gov (United States)

    Kami, M; Murashige, N; Tanaka, Y; Narimatsu, H

    2006-12-01

    Reduced-intensity stem cell transplantation (RIST) has been developed to be a novel curative option for advanced hematologic diseases. Its minimal toxicity allows for transplantation in patients with advanced age or with organ dysfunction. Young patients without comorbidity can undergo RIST as outpatients. However, fungal infection remains an important complication in RIST. Given the poor prognosis of fungal infection, prophylaxis is critical in its management. The prophylactic strategy is recently changing with the development of RIST. Hospital equipment is important for fungal prophylaxis; however, the median day for the development of fungal infection is day 100, when most RIST patients are followed as outpatients. The focus of fungal management after RIST needs to shift from in-hospital equipment to oral antifungals. Various antifungals have recently been developed and introduced for clinical use. A major change in antifungal management will probably occur within several years.

  20. Antifungal Applications of Ag-Decorated Hydroxyapatite Nanoparticles

    Directory of Open Access Journals (Sweden)

    C. A. Zamperini

    2013-01-01

    Full Text Available Pure hydroxyapatite (HA and hydroxyapatite decorated with silver (HA@Ag nanoparticles were synthesized and characterized. The antifungal effect of HA@Ag nanoparticles in a distilled water solution was evaluated against Candida albicans. The origin of the antifungal activity of the HA@Ag is also discussed. The results obtained showed that the HA nanorod morphology remained the same with Ag ions decorations on the HA structure which were deposited in the form of nanospheres. Interaction where occurred between the structure and its defect density variation in the interfacial HA@Ag and intrafacial HA region with the fungal medium resulted in antifungal activity. The reaction mechanisms involved oxygen and water adsorption which formed an active complex cluster. The decomposition and desorption of the final products as well as the electron/hole recombination process have an important role in fungicidal effects.

  1. Studies in Phylogeny, Development of Rapid IdentificationMethods, Antifungal Susceptibility, and Growth Rates of Clinical Strains of Sporothrix schenckii Complex in Japan.

    Science.gov (United States)

    Suzuki, Rumi; Yikelamu, Alimu; Tanaka, Reiko; Igawa, Ken; Yokozeki, Hiroo; Yaguchi, Takashi

    2016-01-01

    Sporotrichosis is a fungal infection caused by the Sporothrix species, which have distinct virulence profiles and geographic distributions. We performed a phylogenetic study in strains morphologically identified as Sporothrix schenckii from clinical specimens in Japan, which were preserved at the Medical Mycology Research Center, Chiba University. In addition, we examined the in vitro antifungal susceptibility and growth rate to evaluate their physiological features. Three hundred strains were examined using sequence analysis of the partial calmodulin gene, or polymerase chain reaction(PCR)method using newly designed species-specific primers; 291 strains were Sporothrix globosa and 9 strains were S. schenckii sensu stricto (in narrow sense, s. s.). S. globosa strains were further clustered into two subclades, and S. schenckii s. s. strains were divided into three subclades. In 38 strains of S. globosa for which antifungal profiles were determined, 4 strains (11%) showed high minimal inhibitory concentration (MIC) value for itraconazole. All tested strains of S. schenckii s. s. and S. globosa showed low sensitivity for amphotericin B. These antifungals are used for treatment of sporotrichosis when infection is severe. S. schenckii s. s. grew better than S. globosa; wherein S. globosa showed restricted growth at 35℃ and did not grow at 37℃. Our molecular data showed that S. globosa is the main causal agent of sporotrichosis in Japan. It is important to determine the antifungal profiles of each case, in addition to accurate species-level identification, to strategize the therapy for sporotrichosis.

  2. 2-(Substituted phenyl-3,4-dihydroisoquinolin-2-iums as Novel Antifungal Lead Compounds: Biological Evaluation and Structure-Activity Relationships

    Directory of Open Access Journals (Sweden)

    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.

  3. Synthesis, structure-activity relationships, and in vitro antibacterial and antifungal activity evaluations of novel pyrazole carboxylic and dicarboxylic acid derivatives.

    Science.gov (United States)

    Mert, Samet; Kasımoğulları, Rahmi; İça, Tuba; Çolak, Ferdağ; Altun, Ahmet; Ok, Salim

    2014-05-06

    A series of pyrazole-3-carboxylic acid and pyrazole-3,4-dicarboxylic acid derivatives were synthesized, the structures were confirmed by their NMR ((1)H and (13)C) and FT-IR spectra, and elemental analyses. The antibacterial and antifungal activities of the compounds against five bacterial and five fungal pathogens were screened using modified agar well diffusion assay. Most of the molecules have inhibitory effects on both standard and clinical Candida albicans strains. However, only the molecules 8, 10, 21, and 22 demonstrate some inhibitory effects on Candida parapsilosis, Candida tropicalis, and Candida glabrata strains. The structure-antifungal activity relationships of the compounds on the C. albicans strains were investigated by electron-conformational method. The pharmacophores and antipharmacophores responsible for the inhibition and non-inhibition of the C. albicans strains were obtained by electronic and geometrical characteristics of the reactive fragments of the molecules. These fragments along with the associated parameters can be used in designing the future more potent antifungal agents. It has been shown that both the positions of electronegative atoms like F and O in the pyrazole substituents and the amount of the associated charges on such atoms are crucial in regulating the strength of antifungal activity for the C. albicans strain.

  4. Wide-range antifungal antagonism of Paenibacillus ehimensis IB-X-b and its dependence on chitinase and beta-1,3-glucanase production.

    Science.gov (United States)

    Aktuganov, G; Melentjev, A; Galimzianova, N; Khalikova, E; Korpela, T; Susi, P

    2008-07-01

    Previously, we isolated a strain of Bacillus that had antifungal activity and produced lytic enzymes with fungicidal potential. In the present study, we identified the bacterium as Paenibacillus ehimensis and further explored its antifungal properties. In liquid co-cultivation assays, P. ehimensis IB-X-b decreased biomass production of several pathogenic fungi by 45%-75%. The inhibition was accompanied by degradation of fungal cell walls and alterations in hyphal morphology. Residual medium from cultures of P. ehimensis IB-X-b inhibited fungal growth, indicating the inhibitors were secreted into the medium. Of the 2 major lytic enzymes, chitinases were only induced by chitin-containing substrates, whereas beta-1,3-glucanase showed steady levels in all carbon sources. Both purified chitinase and beta-1,3-glucanase degraded cell walls of macerated fungal mycelia, whereas only the latter also degraded cell walls of intact mycelia. The results indicate synergism between the antifungal action mechanisms of these enzymes in which beta-1,3-glucanase is the initiator of the cell wall hydrolysis, whereas the degradation process is reinforced by chitinases. Paenibacillus ehimensis IB-X-b has pronounced antifungal activity with a wide range of fungi and has potential as a biological control agent against plant pathogenic fungi.

  5. 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.

  6. 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

  7. Phytotoxic, Antifungal and Immunosuppressive Metabolites from Aspergillus terreus QT122 Isolated from the Gut of Dragonfly.

    Science.gov (United States)

    Lu, Yi-Hui; Jin, Li-Ping; Kong, Li-Chun; Zhang, Ying-Lao

    2017-01-01

    Insect gut microbes have been considered as a resource for bioactive metabolites. The aim of this study was to characterize the compounds of a fungus Aspergillus terreus QT122 associated with the gut of dragonfly. Five main phytotoxic, antifungal, and immunosuppressive substances were isolated from the fungus QT122. The structures of such compounds were identified as emodin (1), 1-methyl emodin (2), terrein (3), methyl 6-acetyl-4-methoxy-7,8-dihydroxynaphthalene-2-carboxylate (4), and dihydrogeodin (5) on the basis of spectroscopic analysis and by comparison of the corresponding data to those reported in the literature previously. The compound 3 exhibited the best phytotoxic activity against the radicle growth of A. retroflexus L. and E. crusgalli L. with their IC50 values of 11.2 and 3.1 μg/mL, which were comparable to that of the positive control of 2,4-dichlorophenoxyacetic acid (2,4-D) with the IC50 values of 8.1 and 1.6 μg/mL, respectively. The compounds 2-3 showed potent antifungal activity in the growth of Alternaria solani with the IC50 value of less than 0.1 μg/mL and the compound 2 also had great inhibitory effect against the growth of Fusarium oxysporum f. sp. cucumerinum (IC50 < 0.1 μg/mL), which was comparable to that of referenced cycloheximide with IC50 value of below 0.1 μg/mL. The compounds 3-5 exhibited strong immunosuppressive activities against the T cell viability with the inhibition rates of more than 99%, which were comparable to positive cyclosporin A under the concentration of 20 μM. These results suggest that the compounds 2-5 have the potential to be used as bio-control agents in agriculture or immunosuppressive agents.

  8. Antifungal activity by vapor contact of essential oils added to amaranth, chitosan, or starch edible films.

    Science.gov (United States)

    Avila-Sosa, Raúl; Palou, Enrique; Jiménez Munguía, María Teresa; Nevárez-Moorillón, Guadalupe Virginia; Navarro Cruz, Addí Rhode; López-Malo, Aurelio

    2012-02-01

    Antimicrobial agents can be incorporated into edible films to provide microbiological stability, since films can be used as carriers of a variety of additives to extend product shelf life and reduce the risk of microbial growth on food surfaces. Addition of antimicrobial agents to edible films offers advantages such as the use of small antimicrobial concentrations and low diffusion rates. The aim of this study was to evaluate inhibition by vapor contact of Aspergillus niger and Penicillium digitatum by selected concentrations of Mexican oregano (Lippia berlandieri Schauer), cinnamon (Cinnamomum verum) or lemongrass (Cymbopogon citratus) essential oils (EOs) added to amaranth, chitosan, or starch edible films. Essential oils were characterized by gas chromatography-mass spectrometry (GC/MS) analysis. Amaranth, chitosan and starch edible films were formulated with essential oil concentrations of 0.00, 0.25, 0.50, 0.75, 1.00, 2.00, or 4.00%. Antifungal activity was evaluated by determining the mold radial growth on agar media inoculated with A. niger and P. digitatum after exposure to vapors arising from essential oils added to amaranth, chitosan or starch films using the inverted lid technique. The modified Gompertz model adequately described mold growth curves (mean coefficient of determination 0.991 ± 0.05). Chitosan films exhibited better antifungal effectiveness (inhibition of A. niger with 0.25% of Mexican oregano and cinnamon EO; inhibition of P. digitatum with 0.50% EOs) than amaranth films (2.00 and 4.00% of cinnamon and Mexican oregano EO were needed to inhibit the studied molds, respectively). For chitosan and amaranth films a significant increase (pfilm concentrations while a significant decrease (pedible films incorporating Mexican oregano or cinnamon essential oil could improve the quality of foods by the action of the volatile compounds on surface growth of molds.

  9. DMPD: C-type lectin receptors in antifungal immunity. [Dynamic Macrophage Pathway CSML Database

    Lifescience Database Archive (English)

    Full Text Available 18160296 C-type lectin receptors in antifungal immunity. Willment JA, Brown GD. Tre...nds Microbiol. 2008 Jan;16(1):27-32. Epub 2007 Dec 21. (.png) (.svg) (.html) (.csml) Show C-type lectin receptors in anti...fungal immunity. PubmedID 18160296 Title C-type lectin receptors in antifungal immunity. Author

  10. [Inotropic agents].

    Science.gov (United States)

    Sasayama, Shigetake

    2003-05-01

    Depression of myocardial contractility plays an important role in the development of heart failure and many inotropic agents were developed to improve the contractile function of the failing heart. Agents that increase cyclic AMP, either by increasing its synthesis or reducing its degradation, exerted dramatic short-term hemodynamic benefits, but these acute effects were not extrapolated into long-term improvement of the clinical outcome of heart failure patients. Administration of these agents to an energy starved failing heart would be expected to increase myocardial energy use and could accelerate disease progression. The role of digitalis in the management of heart failure has been controversial, however, the recent large scale clinical trial has ironically proved that digoxin reduced the rate of hospitalization both overall and for worsening heart failure. More recently, attention was paid to other inotropic agents that have a complex and diversified mechanism. These agents have some phosphodiesterase-inhibitory action but also possess additional effects, including cytokine inhibitors, immunomodulators, or calcium sensitizers. In the Western Societies these agents were again shown to increase mortality of patients with severe heart failure in a dose dependent manner with the long-term administration. However, it may not be the case in the Japanese population in whom mortality is relatively low. Chronic treatment with inotropic agent may be justified in Japanese, as it allows optimal care in the context of relief of symptoms and an improved quality of life. Therefore, each racial group should obtain specific evidence aimed at developing its own guidelines for therapy rather than translating major guidelines developed for other populations.

  11. 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

  12. Antibacterial and antifungal metal based triazole Schiff bases.

    Science.gov (United States)

    Chohan, Zahid H; Hanif, Muhammad

    2013-10-01

    A new series of four biologically active triazole derived Schiff base ligands (L(1)-L(4)) and their cobalt(II), nickel(II), copper(II) and zinc(II) complexes (1-16) have been synthesized and characterized. The ligands were prepared by the condensation reaction of 3-amino-5-methylthio-1H-1,2,4-triazole with chloro-, bromo- and nitro-substituted 2-hydroxybenzaldehyde in an equimolar ratio. The antibacterial and antifungal bioactivity data showed the metal(II) complexes to be more potent antibacterial and antifungal than the parent Schiff bases against one or more bacterial and fungal species.

  13. Plant antifungal proteins and their applications in agriculture.

    Science.gov (United States)

    Yan, Juan; Yuan, Su-Su; Jiang, Luan-Luan; Ye, Xiu-Juan; Ng, Tzi Bun; Wu, Zu-Jian

    2015-06-01

    Fungi are far more complex organisms than viruses or bacteria and can develop numerous diseases in plants that cause loss of a substantial portion of the crop every year. Plants have developed various mechanisms to defend themselves against these fungi which include the production of low-molecular-weight secondary metabolites and proteins and peptides with antifungal activity. In this review, families of plant antifungal proteins (AFPs) including defensins, lectins, and several others will be summarized. Moreover, the application of AFPs in agriculture will also be analyzed.

  14. Antifungal activity against postharvest fungi by extracts from Colombian propolis

    Directory of Open Access Journals (Sweden)

    Erick A. Meneses

    2009-01-01

    Full Text Available The aims of the present study were to evaluate the antifungal properties of Colombian propolis extracts against Colletotrichum gloeosporioides and Botryodiplodia theobromae, and to isolate and identify the main constituents from the active extracts. Therefore, propolis samples were thoroughly extracted with n-hexane/methanol (EPEM, dichloromethane, ethyl acetate, and methanol. Experimental results indicated that mycelial growth of all selected microorganisms was reduced in culture media containing EPEM and dichloromethane fractions. Furthermore, through antifungal bioassay-guided fractionation, three known labdane-type diterpenes: isocupressic acid (1, (+-agathadiol (2 and epi-13-torulosol (3 were isolated as the main constituents from the active fractions.

  15. Antifungal activity against postharvest fungi by extracts from Colombian propolis

    Energy Technology Data Exchange (ETDEWEB)

    Meneses, Erick A.; Durango, Diego L.; Garcia, Carlos M. [Universidad Nacional de Colombia, Medellin (Colombia). Facultad de Ciencias. Escuela de Quimica], e-mail: cmgarcia@unal.edu.co

    2009-07-01

    The aims of the present study were to evaluate the antifungal properties of Colombian propolis extracts against Colletotrichum gloeosporioides and Botryodiplodia theobromae, and to isolate and identify the main constituents from the active extracts. Therefore, propolis samples were thoroughly extracted with n-hexane/methanol (EPEM), dichloromethane, ethyl acetate, and methanol. Experimental results indicated that mycelial growth of all selected microorganisms was reduced in culture media containing EPEM and dichloromethane fractions. Furthermore, through antifungal bioassay-guided fractionation, three known labdane-type diterpenes: isocupressic acid (1), (+)-agathadiol (2) and epi-13-torulosol (3) were isolated as the main constituents from the active fractions. (author)

  16. ANTIFUNGAL ACTIVITY OF HYBANTHUS ENNEASPERMUS ON WET CLOTHES

    Directory of Open Access Journals (Sweden)

    Arumugam Napoleon

    2011-04-01

    Full Text Available During rainy season, when clothes are not properly dried they develop spots. In clothes the spots appear as black or greenish black in color and these spots or mildews were cultured and microscopically examined. It was identified as fungi, viz. Aspergillus niger, Aspergillus flavus and Aspergillus fumigatus. Antifungal activities of different extracts of Hybanthus enneaspermus were screened. The antifungal activity was graded, based on the zone of inhibition. Among the three extracts used for the present studies, methanolic extract exhibited the maximum growth inhibition, followed by chloroform and petroleum ether extract.

  17. Antileishmanial, Antimicrobial and Antifungal Activities of Some New Aryl Azomethines

    Directory of Open Access Journals (Sweden)

    Masoom Yasinzai

    2010-01-01

    Full Text Available A series of eighteen azomethines has been synthesized by the reaction of appropriate primary aromatic amines with aryl and/or heteroaryl carboxaldehydes. The synthesized azomethines have been evaluated for their in vitro antileishmanial, antibacterial and antifungal activities. The results revealed some antifungal activity of most of the synthesized compounds, whereas the antileishmaniasis activity results highlighted that all synthesized azomethines inhibited parasite growth and most of them showed highly potent action towards Leishmania major promastigotes. No remarkable bactericidal activities were observed.

  18. In Vitro antifungal potency of plant extracts against five phytopathogens

    Directory of Open Access Journals (Sweden)

    Ashwani Tapwal

    2011-12-01

    Full Text Available The antifungal activity of aqueous extract of Cannabis sativa, Parthenium hysterophorus, Urtica dioeca, Polystichum squarrosum and Adiantum venustum was investigated against Alternaria solani, Alternaria zinniae, Curvularia lunata, Rhizoctonia solani and Fusarium oxysporum at different concentrations (5, 10, 15 and 20%. At 20%, maximum antifungal potential was observed with the extracts of C. sativa, which recorded excellent inhibitory activity against C. lunata (100%, A. zinniae (59.68%, followed by leaf extract of P. hysterophorus (50% against A. solani. The application of botanical extracts for disease management could be less expensive, easily available, non-polluting and eco-friendly.

  19. Antifungal activity of three mouth rinses--in vitro study.

    Science.gov (United States)

    Abirami, C P; Venugopal, Pankajalakshmi V

    2005-01-01

    Mouthrinses are nowadays routinely included in the home care oral hygiene maintenance besides dentifrice/tooth paste. Mouthrinses prevent bacterial attachment and prevent or slow down bacterial proliferation. Fungal organisms have now gained more importance due to increased incidence of AIDS/HIV. This has necessitated for mouthrinses to possess antifungal activity also. The mouthrinses used were Povidone iodine ( Wokadine), Thymol with Eucalyptol and Benzoic acid (Listerine) and fluoride with Triclosan (Colgate Plax), which were tested against oral isolates of different species of Candida. The agar diffusion test was used to evaluate the inhibitory activity of the mouthrinses and all of them exhibited antifungal activity especially against Candida albicans.

  20. Chemo-sensitization of fungal pathogens to antimicrobial agents using benzaldehyde analogs

    Science.gov (United States)

    Activity of conventional antifungal agents, fludioxonil, strobilurin and antimycinA, which target the oxidative and osmotic stress response systems, was elevated by co-application of certain analogs of benzaldehyde. Fungal tolerance to 2,3-dihydroxybenzaldehyde or 2,3-dihydroxybenzoic acid was foun...

  1. Sunscreening Agents

    Science.gov (United States)

    Martis, Jacintha; Shobha, V; Sham Shinde, Rutuja; Bangera, Sudhakar; Krishnankutty, Binny; Bellary, Shantala; Varughese, Sunoj; Rao, Prabhakar; Naveen Kumar, B.R.

    2013-01-01

    The increasing incidence of skin cancers and photodamaging effects caused by ultraviolet radiation has increased the use of sunscreening agents, which have shown beneficial effects in reducing the symptoms and reoccurrence of these problems. Many sunscreen compounds are in use, but their safety and efficacy are still in question. Efficacy is measured through indices, such as sun protection factor, persistent pigment darkening protection factor, and COLIPA guidelines. The United States Food and Drug Administration and European Union have incorporated changes in their guidelines to help consumers select products based on their sun protection factor and protection against ultraviolet radiation, whereas the Indian regulatory agency has not yet issued any special guidance on sunscreening agents, as they are classified under cosmetics. In this article, the authors discuss the pharmacological actions of sunscreening agents as well as the available formulations, their benefits, possible health hazards, safety, challenges, and proper application technique. New technologies and scope for the development of sunscreening agents are also discussed as well as the role of the physician in patient education about the use of these agents. PMID:23320122

  2. Yeasts acquire resistance secondary to antifungal drug treatment by adaptive mutagenesis.

    Directory of Open Access Journals (Sweden)

    David Quinto-Alemany

    Full Text Available Acquisition of resistance secondary to treatment both by microorganisms and by tumor cells is a major public health concern. Several species of bacteria acquire resistance to various antibiotics through stress-induced responses that have an adaptive mutagenesis effect. So far, adaptive mutagenesis in yeast has only been described when the stress is nutrient deprivation. Here, we hypothesized that adaptive mutagenesis in yeast (Saccharomyces cerevisiae and Candida albicans as model organisms would also take place in response to antifungal agents (5-fluorocytosine or flucytosine, 5-FC, and caspofungin, CSP, giving rise to resistance secondary to treatment with these agents. We have developed a clinically relevant model where both yeasts acquire resistance when exposed to these agents. Stressful lifestyle associated mutation (SLAM experiments show that the adaptive mutation frequencies are 20 (S. cerevisiae -5-FC, 600 (C. albicans -5-FC or 1000 (S. cerevisiae--CSP fold higher than the spontaneous mutation frequency, the experimental data for C. albicans -5-FC being in agreement with the clinical data of acquisition of resistance secondary to treatment. The spectrum of mutations in the S. cerevisiae -5-FC model differs between spontaneous and acquired, indicating that the molecular mechanisms that generate them are different. Remarkably, in the acquired mutations, an ectopic intrachromosomal recombination with an 87% homologous gene takes place with a high frequency. In conclusion, we present here a clinically relevant adaptive mutation model that fulfils the conditions reported previously.

  3. Mobile Agents

    Science.gov (United States)

    Satoh, Ichiro

    Mobile agents are autonomous programs that can travel from computer to computer in a network, at times and to places of their own choosing. The state of the running program is saved, by being transmitted to the destination. The program is resumed at the destination continuing its processing with the saved state. They can provide a convenient, efficient, and robust framework for implementing distributed applications and smart environments for several reasons, including improvements to the latency and bandwidth of client-server applications and reducing vulnerability to network disconnection. In fact, mobile agents have several advantages in the development of various services in smart environments in addition to distributed applications.

  4. Biocontrol of Aspergillus species on peanut kernels by antifungal diketopiperazine producing Bacillus cereus associated with entomopathogenic nematode.

    Science.gov (United States)

    Kumar, Sasidharan Nishanth; Sreekala, Sreerag Ravikumar; Chandrasekaran, Dileep; Nambisan, Bala; Anto, Ruby John

    2014-01-01

    The rhabditid entomopathogenic nematode associated Bacillus cereus and the antifungal compounds produced by this bacterium were evaluated for their activity in reducing postharvest decay of peanut kernels caused by Aspergillus species in in vitro and in vivo tests. The results showed that B. cereus had a significant effect on biocontrol effectiveness in in vitro and in vivo conditions. The antifungal compounds produced by the B. cereus were purified using silica gel column chromatography and their structure was elucidated using extensive spectral analyses. The compounds were identified as diketopiperazines (DKPs) [cyclo-(L-Pro-Gly), cyclo(L-Tyr-L-Tyr), cyclo-(L-Phe-Gly) and cyclo(4-hydroxy-L-Pro-L-Trp)]. The antifungal activities of diketopiperazines were studied against five Aspergillus species and best MIC of 2 µg/ml was recorded against A. flavus by cyclo(4-hydroxy-L-Pro-L-Trp). To investigate the potential application of cyclo(4-hydroxy-L-Pro-L-Trp) to eliminate fungal spoilage in food and feed, peanut kernels was used as a food model system. White mycelia and dark/pale green spores of Aspergillus species were observed in the control peanut kernels after 2 days incubation. However the fungal growth was not observed in peanut kernels treated with cyclo(4-hydroxy-L-Pro-L-Trp). The cyclo(4-hydroxy-L-Pro-L-Trp) was nontoxic to two normal cell lines [fore skin (FS) normal fibroblast and African green monkey kidney (VERO)] up to 200 µg/ml in MTT assay. Thus the cyclo(4-hydroxy-L-Pro-L-Trp) identified in this study may be a promising alternative to chemical preservatives as a potential biopreservative agent which prevent fungal growth in food and feed. To the best of our knowledge, this is the first report demonstrating that the entomopathogenic nematode associated B. cereus and cyclo(4-hydroxy-L-Pro-L-Trp) could be used as a biocontrol agents against postharvest fungal disease caused by Aspergillus species.

  5. [Yeasts in domestic animals: species identification and susceptibility to antifungals].

    Science.gov (United States)

    Hamal, Petr; Koukalová, Dagmar

    2010-02-01

    Yeasts frequently colonize various kinds of domestic animals, but may also cause serious diseases. The aim of this study was to identify yeast isolates collected from dogs, cows and pigs, and to determine their in vitro antifungal susceptibility. Fifty-six yeast isolates from dogs (n = 24), cows (n = 20), and pigs (n = 12) were investigated. Appearance of colonies grown on Sabouraud agar, micromorphology on rice agar, as well as assimilation and fermentation of various carbon and nitrogen sources were evaluated. Susceptibility to six antifungals (flucytosine, amphotericin B, miconazole, ketoconazole, itraconazole and fluconazole) was determined semiquantitatively using the commercially available Fungitest kit (Bio-Rad Laboratories). Ten yeast species were identified in dogs with relatively even distribution. On the other hand, cow and pig were clearly dominated by Candida krusei (from 7 species) and Candida rugosa (from 5 species), respectively. Further, most of yeast isolates exhibited good susceptibility to the antifungals tested particularly to amphotericin B, ketoconazole and itraconazole. Based on results, it can be concluded that significant differences in the species spectrum and distribution were documented between groups of yeasts from dogs, cows and pigs. This is probably due to different environmental conditions and the endogenous origin of the yeast isolates. Mostly good susceptibility to systemic antifungals should positively influence the therapy of diseases caused by yeasts in veterinary medicine.

  6. Fusarielin E, a new antifungal antibiotic from Fusarium sp.

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    A new antifungal antibiotic, fusarielin E, was isolated from the marine-derived fungus Fusarium sp. Its structure was established on the basis of various NMR spectroscopic analyses and HR-FAB-MS. Fusarielin E displayed significant biological activity against Pyricularia oryzae.

  7. Successful management of renal mucormycosis with antifungal therapy and drainage

    Directory of Open Access Journals (Sweden)

    Sudheer K Devana

    2016-01-01

    Full Text Available We report a case of isolated extensive renal mucormycosis in an immunocompetent adult, who was successfully managed conservatively without surgical debridement. To the best of our knowledge, this is the first case where antifungal therapy alone was sufficient even with such an extensive involvement.

  8. Therapeutic potential of antifungal plant and insect defensins

    NARCIS (Netherlands)

    Thevissen, K.; Kristensen, H.H.; Thomma, B.P.H.J.; Cammue, B.P.A.; François, I.E.J.A.

    2007-01-01

    To defend themselves against invading fungal pathogens, plants and insects largely depend on the production of a wide array of antifungal molecules, including antimicrobial peptides such as defensins. Interestingly, plant and insect defensins display antimicrobial activity not only against plant and

  9. Echinocandins: A ray of hope in antifungal drug therapy

    Directory of Open Access Journals (Sweden)

    Grover Neeta

    2010-01-01

    Full Text Available Invasive fungal infections are on the rise. Amphotericin B and azole antifungals have been the mainstay of antifungal therapy so far. The high incidence of infusion related toxicity and nephrotoxicity with amphotericin B and the emergence of fluconazole resistant strains of Candida glabrata egged on the search for alternatives. Echinocandins are a new class of antifungal drugs that act by inhibition of β (1, 3-D- glucan synthase, a key enzyme necessary for integrity of the fungal cell wall. Caspofungin was the first drug in this class to be approved. It is indicated for esophageal candidiasis, candidemia, invasive candidiasis, empirical therapy in febrile neutropenia and invasive aspergillosis. Response rates are comparable to those of amphotericin B and fluconazole. Micafungin is presently approved for esophageal candidiasis, for prophylaxis of candida infections in patients undergoing hematopoietic stem cell transplant (HSCT and in disseminated candidiasis and candidemia. The currently approved indications for anidulafungin are esophageal candidiasis, candidemia and invasive candidiasis. The incidence of infusion related adverse effects and nephrotoxicity is much lower than with amphotericin B. The main adverse effect is hepatotoxicity and derangement of serum transaminases. Liver function may need to be monitored. They are, however, safer in renal impairment. Even though a better pharmacoeconomical choice than amphotericin B, the higher cost of these drugs in comparison to azole antifungals is likely to limit their use to azole resistant cases of candidial infections and as salvage therapy in invasive aspergillosis rather than as first line drugs.

  10. [New developments in antifungal therapy: fluconazole, itraconazole, voriconazole, caspofungin

    NARCIS (Netherlands)

    Wout, J.W. van 't; Kuijper, E.J.; Verweij, P.E.; Kullberg, B.J.

    2004-01-01

    The azole antifungal voriconazole and the echinocandin caspofungin have recently become available for the treatment of invasive mycoses. Fluconazole remains the drug of choice for candidemia, except for infections with one of the resistent species such as Candida krusei and some strains of Candida g

  11. Septic arthritis and osteomyelitis due to the chromoblastomycosis agent Fonsecaea pedrosoi.

    Science.gov (United States)

    De Guzman, Leonidiz; Perlman, David C; Hubbard, Christopher E

    2012-07-01

    Fonsecaea pedrosoi is the most common agent of chromoblastomycosis, a chronic localized fungal infection of the skin and subcutaneous tissues mainly involving the lower extremities. We report a rare case of septic arthritis and osteomyelitis due to the chromoblastomycosis agent F pedrosoi, which was successfully treated with arthrotomy and debridement, followed by a long course of oral antifungal therapy. To our knowledge, this is the second case of F pedrosoi osteomyelitis treated successfully to be ever reported.

  12. A novel assay of biofilm antifungal activity reveals that amphotericin B and caspofungin lyse Candida albicans cells in biofilms.

    Science.gov (United States)

    DiDone, Louis; Oga, Duana; Krysan, Damian J

    2011-08-01

    The ability of Candida albicans to form drug-resistant biofilms is an important factor in its contribution to human disease. Assays to identify and characterize molecules with activity against fungal biofilms are crucial for the development of drugs with improved anti-biofilm activity. Here we report the application of an adenylate kinase (AK)-based cytotoxicity assay of fungal cell lysis to the characterization of agents active against C. albicans biofilms. We have developed three protocols for the AK assay. The first measures AK activity in the supernatants of biofilms treated with antifungal drugs and can be performed in parallel with a standard 2,3-bis-(2-methoxy-4-nitro-5-sulphophenyl)-2H-tetrazolium-5-caboxanilide-based biofilm susceptibility assay; a second, more sensitive protocol measures the AK activity present within the biofilm matrix; and a third procedure allows the direct visualization of lytic activity toward biofilms formed on catheter material. Amphotericin B and caspofungin, the two most effective anti-biofilm drugs currently used to treat fungal infections, both directly lyse planktonic C. albicans cells in vitro, leading to the release of AK into the culture medium. These studies serve to validate the AK-based lysis assay as a useful addition to the methods for the characterization of antifungal agents active toward biofilms and provide insights into the mode of action of amphotericin B and caspofungin against C. albicans biofilms.

  13. New insights into the structure and mode of action of Mo-CBP3, an antifungal chitin-binding protein of Moringa oleifera seeds.

    Directory of Open Access Journals (Sweden)

    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.

  14. New insights into the structure and mode of action of Mo-CBP3, an antifungal chitin-binding protein of Moringa oleifera seeds.

    Science.gov (United States)

    Batista, Adelina B; Oliveira, José T A; Gifoni, Juliana M; Pereira, Mirella L; Almeida, Marina G G; Gomes, Valdirene M; Da Cunha, Maura; Ribeiro, Suzanna F F; Dias, Germana B; Beltramini, Leila M; Lopes, José Luiz S; Grangeiro, Thalles B; Vasconcelos, Ilka M

    2014-01-01

    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.

  15. Economic considerations of antifungal prophylaxis in patients undergoing surgical procedures

    Directory of Open Access Journals (Sweden)

    Maria Adriana Cataldo

    2011-01-01

    Full Text Available Maria Adriana Cataldo, Nicola PetrosilloSecond Infectious Diseases Division, National Institute for Infectious Diseases, “Lazzaro Spallanzani”, Rome, ItalyAbstract: Fungi are a frequent cause of nosocomial infections, with an incidence that has increased significantly in recent years, especially among critically ill patients who require intensive care unit (ICU admission. Among ICU patients, postsurgical patients have a higher risk of Candida infections in the bloodstream. In consideration of the high incidence of fungal infections in these patients, their strong impact on mortality rate, and of the difficulties in Candida diagnosis, some experts suggest the use of antifungal prophylaxis in critically ill surgical patients. A clinical benefit from this strategy has been demonstrated, but the economic impact of the use of antifungal prophylaxis in surgical patients has not been systematically evaluated, and its cost–benefit ratio has not been defined. Whereas the costs associated with treating fungal infections are very high, the cost of antifungal drugs varies from affordable (ie, the older azoles to expensive (ie, echinocandins, polyenes, and the newer azoles. Adverse drug-related effects and the possibly increased incidence of fluconazole resistance and of isolates other than Candida albicans must also be taken into account. From the published studies of antifungal prophylaxis in surgical patients, a likely economic benefit of this strategy could be inferred, but its usefulness and cost–benefits should be evaluated in light of local data, because the available evidence does not permit general recommendations.Keywords: antifungal prophylaxis, cost-effectiveness, economics, surgery, fungal infection 

  16. 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. [i]Lavandula angustifolia[/i], [i]Carum carvi[/i], [i]Pinus mungo var. pulmilio[/i], [i]Mentha piperita[/i], [i]Chamomilla recutita[/i] L.,[i] Pinus sylvestris[/i], [i]Satureia hortensis[/i] L., [i]Origanum vulgare[/i] L., [i]Pimpinella anisum[/i], [i]Rosmarinus officinali[/i]s L., [i]Salvia officinalis[/i] L., [i]Abietis albia etheroleum[/i], [i]Chamomilla recutita[/i] L. [i]Rausch[/i], [i]Thymus vulgaris[/i] L., [i]Origanum vulgare[/i] L. for antifungal activity against five [i]Penicillium[/i] species: [i]Penicillium brevicompactum[/i], [i]Penicillium citrinum[/i], [i]Penicillium crustosum[/i], [i]Penicillium expansum[/i] and [i]Penicillium griseofulvum[/i]. The method used for screening included the disc diffusion method. The study points out the wide spectrum of antifungal activity of essential oils against [i]Penicillium[/i] fungi. There were five essential oils of the 15 mentioned above which showed a hopeful antifungal activity: [i]Pimpinella anisum[/i], [i]Chamomilla recutita[/i] L., [i]Thymus vulgaris[/i], [i]Origanum vulgare[/i] L. The most hopeful antifungal activity and killing effect against all tested penicillia was found to be [i]Origanum vulgare[/i] L. and [i]Pimpinella anisum[/i]. The lowest level of antifungal activity was demonstrated by the oils [i]Pinus mungo var. pulmilio[/i], [i]Salvia officinalis[/i] L., [i]Abietis albia etheroleum[/i], [i]Chamomilla recutita[/i] L.[i] Rausch[/i], [i]Rosmarinus officinalis[/i].

  17. Intermolecular interaction of voriconazole analogues with model membrane by DSC and NMR, and their antifungal activity using NMR based metabolic profiling.

    Science.gov (United States)

    Kalamkar, Vaibhav; Joshi, Mamata; Borkar, Varsha; Srivastava, Sudha; Kanyalkar, Meena

    2013-11-01

    The development of novel antifungal agents with high susceptibility and increased potency can be achieved by increasing their overall lipophilicity. To enhance the lipophilicity of voriconazole, a second generation azole antifungal agent, we have synthesized its carboxylic acid ester analogues, namely p-methoxybenzoate (Vpmb), toluate (Vtol), benzoate (Vbz) and p-nitrobenzoate (Vpnb). The intermolecular interactions of these analogues with model membrane have been investigated using nuclear magnetic resonance (NMR) and differential scanning calorimetric (DSC) techniques. The results indicate varying degree of changes in the membrane bilayer's structural architecture and physico-chemical characteristics which possibly can be correlated with the antifungal effects via fungal membrane. Rapid metabolite profiling of chemical entities using cell preparations is one of the most important steps in drug discovery. We have evaluated the effect of synthesized analogues on Candida albicans. The method involves real time (1)H NMR measurement of intact cells monitoring NMR signals from fungal metabolites which gives Metabolic End Point (MEP). This is then compared with Minimum Inhibitory Concentration (MIC) determined using conventional methods. Results indicate that one of the synthesized analogues, Vpmb shows reasonably good activity.

  18. Design, Synthesis and in Vivo Evaluation of Novel Glycosylated Sulfonylureas as Antihyperglycemic Agents.

    Science.gov (United States)

    Suaifan, Ghadeer A R Y; Shehadeh, Mayadah B; Darwish, Rula M; Al-Ijel, Hebah; Abbate, Vincenzo

    2015-11-06

    Sulphonylurea compounds have versatile activities such as antidiabetic, diuretic, herbicide, oncolytic, antimalarial, antifungal and anticancer. The present study describes the design, synthesis and in vivo testing of novel glycosylated aryl sulfonylurea compounds as antihyperglycaemic agents in streptozocine-induced diabetic mice. The rational for the introduction of the glucosamine moiety is to enhance selective drug uptake by pancreatic β-cells in order to decrease the cardiotoxic side effect commonly associated with sulfonylurea agents. 2-Deoxy-2-(4-chlorophenylsulfonylurea)-D-glucopyranose was found to be the most potent antihyperglycaemic agents among the synthesized compounds in diabetic mice. This investigation indicates the importance of this novel class as potential antihyperglycaemic agents.

  19. Radioprotective Agents

    Science.gov (United States)

    1982-01-01

    claimed to be effective are gallic acid derivatives, eg, sodium gallate 12053-21-61 (295-297) and propyl gallate 1121-79-91 (298). p...inhibition of a-adrenergic receptors can be achieved through the use of the antiradiation agents 2-(5-aminopentylamino)ethanephos- phorothioic acid ...tissue was ap- preciated immediately as a potential medical set, and they were put to use en- thusiastically. Early workers did notice an erythematous

  20. Structure-activity relationships among antifungal nylon-3 polymers: identification of materials active against drug-resistant strains of Candida albicans.

    Science.gov (United States)

    Liu, Runhui; Chen, Xinyu; Falk, Shaun P; Mowery, Brendan P; Karlsson, Amy J; Weisblum, Bernard; Palecek, Sean P; Masters, Kristyn S; Gellman, Samuel H

    2014-03-19

    Fungal infections are a major challenge to human health that is heightened by pathogen resistance to current therapeutic agents. Previously, we were inspired by host-defense peptides to develop nylon-3 polymers (poly-β-peptides) that are toxic toward the fungal pathogen Candida albicans but exert little effect on mammalian cells. Based on subsequent analysis of structure-activity relationships among antifungal nylon-3 polymers, we have now identified readily prepared cationic homopolymers active against strains of C. albicans that are resistant to the antifungal drugs fluconazole and amphotericin B. These nylon-3 polymers are nonhemolytic. In addition, we have identified cationic-hydrophobic copolymers that are highly active against a second fungal pathogen, Cryptococcus neoformans, and moderately active against a third pathogen, Aspergillus fumigatus.

  1. Analysis of Antifungal Components in the Galls of Melaphis chinensis and Their Effects on Control of Anthracnose Disease of Chinese Cabbage Caused by Colletotrichum higginsianum

    Directory of Open Access Journals (Sweden)

    Ping-Chung Kuo

    2015-01-01

    Full Text Available Fungal pathogens caused various diseases which resulted in heavy yield and quality losses on plants of commercial interests such as fruits, vegetables, and flowers. In our preliminary experimental results, the methanol extracts of four species of medicinal plants Melaphis chinensis, Eugenia caryophyllata, Polygonum cuspidatum, and Rheum officinale possessed antifungal activity to causal agent of cabbage anthracnose, Colletotrichum higginsianum. Thus it was conducted to identify and quantify the chemical constituents in these herbs and to assess the antifungal effects of these compounds. Among the tested principles, the indicator compound methyl gallate from M. chinensis was the most effective one against the conidial germination. In addition, it exhibited significant effects of controlling anthracnose disease of Chinese cabbage caused by C. higginsianum PA-01 in growth chamber. These results indicate that M. chinensis may be potential for further development of plant-derived pesticides for control of anthracnose of cabbage and other cruciferous crops.

  2. Empirical antifungal therapy in patients with neutropenia and persistent or recurrent fever of unknown origin.

    Science.gov (United States)

    Martino, Rodrigo; Viscoli, Claudio

    2006-01-01

    Persistent or recurrent fever of unexplained origin (PFUO) in neutropenic patients receiving antibiotic therapy is commonly treated with empirical antifungal therapy (EAFT). EAFT was established as an adequate management of PFUO around 20 years ago with conventional amphotericin B deoxycholate (c-AmB), despite its high rate of infusional and systemic toxicities. In recent years, EAFT trials for PFUO have used less toxic agents, such as the lipid formulations of AmB, the new azoles, and the echinocandin, caspofungin. In clinical trials, the lipid formulations of AmB [especially liposomal AmB (L-AmB)] provided similar efficacy with lower toxicity but at a much higher cost. Although rarely used in clinical practice, fluconazole is equivalent to c-AmB, provided patients at high risk of Aspergillus infections are excluded. Intravenous itraconazole was shown to be equivalent to c-AmB, with a lower toxicity. Voriconazole did not meet non-inferiority criteria when compared with L-AmB. Caspofungin was shown to be non-inferior to L-AmB and more effective in treating baseline invasive fungal infections. To date, alternatives to AmB have shown less toxicity, but improved efficacy is less clear. This is probably because of the weakness of the indication and to the consequent difficulty in establishing objective and reproducible endpoints for comparisons. The new challenge for physicians in this field is probably presumptive antifungal therapy, an approach based on patient risk-group stratification for developing invasive candidiasis or aspergillosis and/or the use of new diagnostic techniques to identify patients at a very early stage of infection.

  3. Antifungal Activity of Condensed Tannins from Stryphnodendron adstringens: Effect on Candida tropicalis Growth and Adhesion Properties.

    Science.gov (United States)

    Morey, Alexandre T; de Souza, Felipe C; Santos, Jussevania P; Pereira, Caibe A; Cardoso, Juscelio D; de Almeida, Ricardo S C; Costa, Marco A; de Mello, João C P; Nakamura, Celso V; Pinge-Filho, Phileno; Yamauchi, Lucy M; Yamada-Ogatta, Sueli F

    2016-01-01

    Candida species are some of the most common causes of fungal infection worldwide. The limited efficacy of clinically available antifungals warrants the search for new compounds for treating candidiasis. This study evaluated the effect of condensed tannin-rich fraction (F2 fraction) of Stryphnodendron adstringens on in vitro and in vivo growth of Candida tropicalis, and on yeast adhesion properties. F2 exhibited a fungistatic effect with the minimum inhibitory concentration ranging from 0.5 to 8.0 μg/mL. A significant reduction in biofilm mass was observed after either pretreatment of planktonic cells for 2 h (mean reduction of 46.31±8.17%) or incubation during biofilm formation (mean reduction of 28.44±13.38%) with 4x MIC of F2. Prior exposure of planktonic cells to this F2 concentration also significantly decreased yeast adherence on HEp-2 cells (mean reduction of 43.13±14.29%), cell surface hydrophobicity (mean reduction of 25.89±10.49%) and mRNA levels of the genes ALST1-3 (2.9-, 1.8- and 1.8-fold decrease, respectively). Tenebrio molitor larvae, which are susceptible to C. tropicalis infection, were used for in vivo testing. Treatment with 128 and 256 μg/mL F2 significantly increased the survival of infected larvae. These results indicate a combined effect of F2 on inhibition of yeast growth and interference in yeast adhesion, which may contribute to the suppression of infection caused by C. tropicalis, thus reinforcing the potential of the condensed tannins from S. adstringens for the development of novel antifungal agents.

  4. Design and synthesis of novel complexes containing N-phenyl-1H-pyrazole moiety: Ni complex as potential antifungal and antiproliferative compound

    Science.gov (United States)

    El-Gamel, Nadia E. A.; Farghaly, Thoraya A.

    2013-11-01

    Cu(II) (1), Ni(II) (2), Cr(III) (3) and Fe(III) (4) complexes with 3-acetyl-4-benzoyl-1-phenyl-1H-pyrazole (L1) were prepared and structurally characterized. Usual coordination of L1 was achieved through nitrogen of pyrazole moiety and carbonyl acetyl group. Electronic spectra of the complexes indicate that the geometry of the metal center was six coordinate octahedral. In vitro antimicrobial activity of the ligand and complex compounds was screened in terms of antibacterial effect on Staphylococcus aureus (Gram-positive), Escherichia coli (Gram-negative) and antifungal effect on the fungi Aspergillus flavus and candida albicans using the modified Kirby-Bauer disc diffusion and minimum inhibitory concentrations (MIC) methods. Ni(II) complex (2) exhibited remarkable antifungal inhibition against Candida albicans equal to the standard antifungal agent. To continue our study some structural modifications are formed by adding 4-fluoro-benzoyl moiety to L1 in different forms to produce different ligands, 3-acetyl-4-(4-flourobenzoyl)-1-phenyl-1H-pyrazole (L2) and 3-[(3-acetyl-1-phenyl-1H-4-pyrazolyl)carbonyl]-1-phenyl-4-(4-flourobenzoyl)-1H-pyrazole (L3), Ni complexes (5 and 6) are prepared and comparable in vitro antimicrobial study is evaluated. In vitro cytotoxicity of the Ni(II) complex (2) is studied using MTT assay. The analysis of the cell test showed that (2) displayed quite small cytotoxic response at the higher concentration level which indeed would further enable us for more opportunities in therapeutic and biomedical challenges. Both of the capability as a potent in vitro antifungal agent and the cell test analysis show Ni(II) complex (2) as a promising material in the translation of observed in vitro biological phenomenon into clinical therapies settings.

  5. Synthesis and antifungal activity of derivatives of 2- and 3-benzofurancarboxylic acids.

    Science.gov (United States)

    Hejchman, Elzbieta; Ostrowska, Kinga; Maciejewska, Dorota; Kossakowski, Jerzy; Courchesne, William E

    2012-11-01

    We found that amiodarone has potent antifungal activity against a broad range of fungi, potentially defining a new class of antimycotics. Investigations into its molecular mechanisms showed amiodarone mobilized intracellular Ca2+, which is thought to be an important antifungal characteristic of its fungicidal activity. Amiodarone is a synthetic drug based on the benzofuran ring system, which is contained in numerous compounds that are both synthetic and isolated from natural sources with antifungal activity. To define the structural components responsible for antifungal activity, we synthesized a series of benzofuran derivatives and tested them for the inhibition of growth of two pathogenic fungi, Cryptococcus neoformans and Aspergillus fumigatus, to find new compounds with antifungal activity. We found several derivatives that inhibited fungal growth, two of which had significant antifungal activity. We were surprised to find that calcium fluxes in cells treated with these derivatives did not correlate directly with their antifungal effects; however, the derivatives did augment the amiodarone-elicited calcium flux into the cytoplasm. We conclude that antifungal activity of these new compounds includes changes in cytoplasmic calcium concentration. Analyses of these benzofuran derivatives suggest that certain structural features are important for antifungal activity. Antifungal activity drastically increased on converting methyl 7-acetyl-6-hydroxy-3-methyl-2-benzofurancarboxylate (2b) into its dibromo derivative, methyl 7-acetyl-5-bromo-6-hydroxy-3-bromomethyl-2-benzofurancarboxylate (4).

  6. In vitro antifungal action of different substances over microwaved-cured acrylic resins

    Directory of Open Access Journals (Sweden)

    Henrique Montagner

    2009-10-01

    Full Text Available OBJECTIVE: The presence of Candida albicans on the surfaces of denture-base acrylic resins is strongly related to the development of oral stomatitis. This study evaluated the antifungal action of different agents over microwave-cured acrylic resin without polishing specimens previously contaminated with Candida albicans. MATERIAL AND METHODS: Sixty specimens were immersed in BHI broth previously inoculated with the yeast and stored for 3 h at 37ºC. They were divided into 5 experimental groups (n=10: G1: 2% chlorhexidine solution (10 min; G2: 0.5% sodium hypochlorite (10 min; G3: modified sodium hypochlorite (10 min; G4: effervescent agent (5 min; G5: hydrogen peroxide 10v (30 min. The specimens of the control group 1 (C1 were not disinfected. Ten additional specimens of the control group 2 (C2 were not infected with the yeast, aiming to check the asepsis during the experiment. The disinfection agents were neutralized and the acrylic resin specimens were immersed in BHI Broth for 24 h. Culture media turbidity was evaluated spectrophotometrically according to the transmittance degree, i.e. the higher the transmittance the stronger the antimicrobial action. Statistical analysis was performed (Kruskal-Wallis Test, p<0.05. RESULTS: The results, represented by the medians, were: G1 = 40; G2 = 100; G3 = 100; G4 = 90; G5 = 100; C1 = 40; C2 = 100. CONCLUSIONS: This in vitro study suggested that sodium hypochlorite-based substances and hydrogen peroxide are more efficient disinfectants against C. albicans than 2% chlorhexidine solution and the effervescent agent.

  7. Antifungal activity using medicinal plant extracts against pathogens of coffee tree

    Directory of Open Access Journals (Sweden)

    J.L. Silva

    2014-09-01

    Full Text Available Generally, the medicinal plants have antifungal substances that can be used for the plant protection against phytopathogens. The objective of this study was to know the efficiency of aqueous extracts from medicinal plants against the major etiological agents of coffee tree. The aqueous extracts used were extracted from bulbs of Allium sativum, leaves of Vernonia polysphaera, Cymbopogon citratus, Cymbopogon nardus, Cordia verbenacea, Eucalyptus citriodora, Ricinus communis, Azadirachta indica, Piper hispidinervum and flower buds of Syzygium aromaticum. The etiological agents considered for this study were Cercospora coffeicola, Colletotrichum gloeosporioides, Fusarium oxysporum, Phoma tarda, Rhizoctonia solani and Hemileia vastatrix. The screening for harmful extracts was done based on mycelial growth and conidial germination inhibition. All experiments performed were in vitro conditions. The inhibition of mycelial growth was performed mixing the extracts with the PDA. This mixture was poured in Petri dishes. On the center of the dishes was added one PDA disc with mycelium. It was incubated in a chamber set to 25ºC. The evaluation was done daily by measuring the mycelial growth. The germination assessment was also performed with Petri dishes containing agar-water medium at 2%. These were incubated at 25ºC for 24 hours. After this period the interruption of germination was performed using lactoglycerol. The experiments were conducted in a completely randomized design. The most effective plant extracts against the micelial growth and conidial germination were V. polysphaera, S. aromaticum and A. sativum.

  8. Chemical composition and antifungal activity of Salvia sclarea (Lamiaceae essential oil

    Directory of Open Access Journals (Sweden)

    Džamić Ana

    2008-01-01

    Full Text Available Clary sage (Salvia sclarea L. is native to Southern Europe and is cultivated worldwide. The essential oil of clary sage was analyzed as a potential antifungal agent. The main compounds in the oil were linalyl acetate (52.83% and linalool (18.18%. Food poisoning agents, spoilage fungi, and plant and animal pathogens were among the tested fungal species. The microdilution method was used to establish minimal inhibitory concentrations (MIC and minimal fungicidal concentrations (MFC. The commercial antimycotic bifonazole was used as a control. A concentration of 25 μl/ml showed fungicidal activity against Aspergillus, Penicillium, and Fusarium species and Trichoderma viride. For the species Mucor mucedo and Aspergillus viride, the MFC was 15μl/ml; for Candida albicans, it was 10 μl/ml, as in the case of bifonazole. Fungistatic and fungicidal activities of the oil against Cladosporium cladosporioides and Trichophyton menthagrophytes were recorded at concentrations of 2.5 μl/ml and 5 μl/ml. The most sensitive micromycetes were Cladosporium fulvum, Alternaria alternata, Phomopsis helianthi, and Phoma macdonaldii, where a concentration of 2.5 μl/ml was lethal.

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

    Directory of Open Access Journals (Sweden)

    N. Chami

    2004-06-01

    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.

  10. In vitro and in vivo antifungal activity of natural inhibitors against Penicillium expansum

    Directory of Open Access Journals (Sweden)

    Claudia Fieira

    2013-02-01

    Full Text Available Penicillium expansum is the causative agent of apple blue mold. The inhibitory effects of the capsaicin derived from Capsicum spp. fruits and yeast Hansenula wingei against P. expansum were evaluated in an in vitro and in in vivo assay using Fuji apples. The minimum inhibitory concentration of capsaicin determined using the broth micro-dilution method was 122.16 µg mL-1. Capsaicin did not reduce blue mold incidence in apples. However, it was able to delay fungal growth in the first 14 days of the in vivo assay. The in vivo effect of the yeast Hansenula wingei AM2(-2, alone and combined with thiabendazole at low dosage (40 µg mL-1, on the incidence of apple diseases caused by P. expansum was also described. H. wingei AM2(-2 combined with a low fungicide dosage (10% of the dosage recommended by the manufacturer showed the best efficacy (100% up to 7 days of storage at 21 ºC, later showing a non-statistically different decrease (p > 0.05 after 14 (80.45% and 21 days (72.13%, respectively. These results contribute providing new options for using antifungal agents against Penicillium expansum.

  11. In vitro susceptibility of Paracoccidioides brasiliensis yeast form to antifungal agents

    Directory of Open Access Journals (Sweden)

    Angela Restrepo

    1984-12-01

    Full Text Available A study was conducted to determine the susceptibility of P. brasiliensis yeast form to amphotericin B (A, ketoconazole (K, 5-fluorocytosine (5-FC and rifampin (R. The three isolates tested produced minimal inhibitory concentrations (MICs (mcg/ml in the following range: A: 0.09-0.18; K: 0.001-0.007; 5-FC: 62.5-250 and R: 40-80. The minimal fungicidal concentrations (MFC were several times higher than the corresponding MICs. Precise MFC for 5-FC were not obtained (> 500 mcg/ml. Combination of K plus A proved synergic, with the fractional inhibitory concentration (FIC indices revealing synergy when the drugs were combined at the 1 to 1 and 1 to 5 MIC ratios. R (40 mcg/ml appeared to antagonize K. These results indicate promise for the combined use of K plus A as a therapeutical regimen.

  12. Exopolysaccharide matrix of developed candida albicans biofilms after exposure to antifungal agents

    OpenAIRE

    2012-01-01

    This study aimed to evaluate the effects of fluconazole or nystatin exposure on developed Candida albicans biofilms regarding their exopolysaccharide matrix. The minimal inhibitory concentration (MIC) against fluconazole or nystatin was determined for C. albicans reference strain (ATCC 90028). Poly(methlymethacrylate) resin (PMMA) specimens were fabricated according to the manufacturer's instructions and had their surface roughness measured. Biofilms were developed on specimens surfaces for 4...

  13. Sporothrix schenckii COMPLEX:SUSCEPTIBILITIES TO COMBINED ANTIFUNGAL AGENTS AND CHARACTERIZATION OF ENZYMATIC PROFILES.

    Science.gov (United States)

    Oliveira, Daniele Carvalho; de Loreto, Érico Silva; Mario, Débora Alves Nunes; Lopes, Paulo G Markus; Neves, Louise Vignolles; da Rocha, Marta Pires; Santurio, Janio Morais; Alves, Sydney Hartz

    2015-01-01

    Sporothrix schenckii was reclassified as a complex encompassing six cryptic species, which calls for the reassessment of clinical and epidemiological data of these new species. We evaluated the susceptibility of Sporothrix albicans(n = 1) , S. brasiliensis(n = 6) , S. globosa(n = 1), S. mexicana(n = 1) and S. schenckii(n = 36) to terbinafine (TRB) alone and in combination with itraconazole (ITZ), ketoconazole (KTZ), and voriconazole (VRZ) by a checkerboard microdilution method and determined the enzymatic profile of these species with the API-ZYM kit. Most interactions were additive (27.5%, 32.5% and 5%) or indifferent (70%, 50% and 52.5%) for TRB+KTZ, TRB+ITZ and TRB+VRZ, respectively. Antagonisms were observed in 42.5% of isolates for the TRB+VRZ combination. Based on enzymatic profiling, the Sporothrix schenckii strains were categorized into 14 biotypes. Leucine arylamidase (LA) activity was observed only for S. albicans and S. mexicana. The species S. globosa and S. Mexicana were the only species without β-glucosidase (GS) activity. Our results may contribute to a better understanding of virulence and resistance among species of the genus Sporothrix in further studies.

  14. Construction and screening of 2-aryl benzimidazole library identifies a new antifouling and antifungal agent.

    Digital Repository Service at National Institute of Oceanography (India)

    Majik, M.S.; Tilvi, S.; Mascarenhas, S.; Kumar, Vikash.; Chatterjee, Amrita; Banerjee, Mainak.

    compound with maximum antifouling properties and hence was selected for further studies. The dose response studies were performed on compound 4j against 10 strains of Gram positive and Gram negative fouling bacteria with concentration ranging from 25...-fouling capacity of the compounds: Gram positive bacteria (Planococcus donghaensis) & Gram negative bacteria (Alcanivorax spp, Aeromonas hydrophila subsp hydrophila ATCC 7966, Aeromonas hydrophila subsp. salmonicida A449, Erythrobacter litoralis, Pseudomonas...

  15. Sporothrix schenckii COMPLEX: SUSCEPTIBILITIES TO COMBINED ANTIFUNGAL AGENTS AND CHARACTERIZATION OF ENZYMATIC PROFILES

    Directory of Open Access Journals (Sweden)

    Daniele Carvalho OLIVEIRA

    2015-08-01

    Full Text Available SUMMARY Sporothrix schenckiiwas reclassified as a complex encompassing six cryptic species, which calls for the reassessment of clinical and epidemiological data of these new species. We evaluated the susceptibility of Sporothrix albicans (n = 1 , S. brasiliensis (n = 6 , S. globosa (n = 1, S. mexicana(n = 1 and S. schenckii(n = 36 to terbinafine (TRB alone and in combination with itraconazole (ITZ, ketoconazole (KTZ, and voriconazole (VRZ by a checkerboard microdilution method and determined the enzymatic profile of these species with the API-ZYM kit. Most interactions were additive (27.5%, 32.5% and 5% or indifferent (70%, 50% and 52.5% for TRB+KTZ, TRB+ITZ and TRB+VRZ, respectively. Antagonisms were observed in 42.5% of isolates for the TRB+VRZ combination. Based on enzymatic profiling, the Sporothrix schenckii strains were categorized into 14 biotypes. Leucine arylamidase (LA activity was observed only for S. albicans and S. mexicana. The species S. globosaand S. mexicanawere the only species without β-glucosidase (GS activity. Our results may contribute to a better understanding of virulence and resistance among species of the genus Sporothrixin further studies.

  16. Sporothrix schenckii COMPLEX: SUSCEPTIBILITIES TO COMBINED ANTIFUNGAL AGENTS AND CHARACTERIZATION OF ENZYMATIC PROFILES

    Science.gov (United States)

    OLIVEIRA, Daniele Carvalho; de LORETO, Érico Silva; MARIO, Débora Alves Nunes; LOPES, Paulo G. Markus; NEVES, Louise Vignolles; da ROCHA, Marta Pires; SANTURIO, Janio Morais; ALVES, Sydney Hartz

    2015-01-01

    SUMMARY Sporothrix schenckiiwas reclassified as a complex encompassing six cryptic species, which calls for the reassessment of clinical and epidemiological data of these new species. We evaluated the susceptibility of Sporothrix albicans (n = 1) , S. brasiliensis (n = 6) , S. globosa (n = 1), S. mexicana(n = 1) and S. schenckii(n = 36) to terbinafine (TRB) alone and in combination with itraconazole (ITZ), ketoconazole (KTZ), and voriconazole (VRZ) by a checkerboard microdilution method and determined the enzymatic profile of these species with the API-ZYM kit. Most interactions were additive (27.5%, 32.5% and 5%) or indifferent (70%, 50% and 52.5%) for TRB+KTZ, TRB+ITZ and TRB+VRZ, respectively. Antagonisms were observed in 42.5% of isolates for the TRB+VRZ combination. Based on enzymatic profiling, the Sporothrix schenckii strains were categorized into 14 biotypes. Leucine arylamidase (LA) activity was observed only for S. albicans and S. mexicana. The species S. globosaand S. mexicanawere the only species without β-glucosidase (GS) activity. Our results may contribute to a better understanding of virulence and resistance among species of the genus Sporothrixin further studies. PMID:26422151

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

    NARCIS (Netherlands)

    Rodrigues, Anderson Messias; de Hoog, G Sybren; de Cássia Pires, Débora; Brihante, Raimunda Sâmia Nogueira; Sidrim, José Júlio da Costa; Gadelha, Marcos Fabio; Colombo, Arnaldo Lopes; de Camargo, Zoilo Pires

    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 c

  18. A new antifungal agent,Caspofungin%抗真菌新药--卡泊芬净

    Institute of Scientific and Technical Information of China (English)

    陈轶坚; 吴菊芳

    2004-01-01

    @@ 随着免疫缺陷患者的增多以及新的操作技术的开展,深部真菌感染的发病率逐年增加.据报道,深部真菌感染列美国医院感染第4位.是侵袭性真菌感染病死率上升的重要原因.卡泊芬净(caspofungin)是一类全新的抗真菌药--棘白菌素(echinocandins)的第1个上市品种(商品名Cancidas,Merk 公司).本品对包括曲霉和念珠菌属在内的真菌均有良好的抗菌作用,已有的临床资料显示本品用于治疗侵袭性曲霉病和念珠菌感染等真菌感染可获得较满意的疗效.以下就卡泊芬净的抗真菌作用、药动学、临床应用和安全性等方面分别综述如下.

  19. A new class of antifungal agent: caspofungin%新型抗真菌药物caspofungin

    Institute of Scientific and Technical Information of China (English)

    安富荣; 戈升荣

    2003-01-01

    caspofungin是新型葡聚糖合成酶抑制剂类抗真菌药物中第1个上市的药物,它能有效抑制β-(1,3)-D-葡聚糖的合成,从而干扰真菌细胞壁的合成.caspofungin在体内、外具有广泛的抗真菌活性,包括曲菌和念珠菌.多中心试验表明,caspofungin治疗难治性或不能耐受其他治疗的侵袭性曲菌感染病人的临床有效率为40.7%.2个随机双盲试验表明,caspofungin能有效治疗咽或食道念珠菌感染.侵袭性曲菌病人对caspofungin的耐受性较好.本文综述了caspofungin的药效学、药动学特性、临床疗效和不良反应等.

  20. New α-Methylene-γ-Butyrolactone Derivatives as Potential Fungicidal Agents: Design, Synthesis and Antifungal Activities

    Directory of Open Access Journals (Sweden)

    Yongling Wu

    2016-01-01

    Full Text Available In consideration of the fact that the α-methylene-γ-butyrolactone moiety is a major bio-functional group in the structure of carabrone and possesses some agricultural biological activity, forty-six new ester and six new ether derivatives containing α-methylene-γ-butyrolactone moieties were synthesized, and their fungicidal activities against Colletotrichum lagenarium and Botrytis cinerea were investigated. Most of the synthesized compounds showed moderate to significant fungicidal activity. Among them, halogen atom-containing derivatives showed better activity than others, especially compounds 6a,d which exhibited excellent fungicidal activity against C. lagenarium, with IC50 values of 7.68 and 8.17 μM. The structure-activity relationship (SAR analysis indicated that ester derivatives with electron-withdrawing groups on the benzene ring showed better fungicidal activity than those with electron-donating groups. A quantitative structure-activity relationship (QSAR model (R2 = 0.9824, F = 203.01, S2 = 0.0083 was obtained through the heuristic method. The built model revealed a strong correlation of fungicidal activity against C. lagenarium with the molecular structures of these compounds. These results are expected to prove helpful in the design and exploration of low toxicity and high efficiency α-methylene-γ-butyrolactone-based fungicides.

  1. Eucalyptus globulus L. extract as an antifungal agent against Candida species

    OpenAIRE

    Martins, Natália; FERREIRA, ISABEL C.F.R.; Barros, Lillian; Henriques, Mariana; Silva, Sónia

    2014-01-01

    Hundreds of botanical preparations have been prepared and used for a wide variety of conditions. Different studies have been carried out towards to confirm the effective multitude of health benefits provided by medicinal plants [I]. In parallel with these studies, in the last years, high rates of opportunistic fungal infections have been observed, namely involving Candida species. Candida albicans is the most common but, currently, other non-Candida albicans Candida (NCAC) species have also b...

  2. 抗真菌药物的研究进展%Advances in antifungal agents

    Institute of Scientific and Technical Information of China (English)

    刘正印; 王爱霞

    2006-01-01

    近20多年来,随着大量广谱抗生素的应用、骨髓和脏器的移植、皮质激素及免疫抑制剂的应用、艾滋病发病率的增加、各种导管的介入和真菌检测技术的提高,念珠菌血症和系统性曲霉感染逐渐增多.北京协和医院报道在四个不同年代败血症血培养的结果显示,1994~1995年真菌发生率为8.1%;2000年为6.7%.20年149例真菌感染的分析显示,真菌感染呈逐年上升的趋势.临床上已有耐氟康唑的念珠菌和耐两性霉素B的曲霉存在.因此需要新的抗真菌药物.目前即将推出和已上市的新药有:多烯类的制霉菌素脂质体、两性霉素B脂质体剂型AmBisome、两性霉素B脂质体复合物Abelect、两性霉素B胶样分散体Amphotec、伊曲康唑口服液和注射剂、伏立康唑注射剂和口服片剂以及卡泊芬净注射剂.各种新药均有其特点与不良反应,但总的是新药的开发和临床应用,将会对侵性真菌感染提供有力的治疗措施,真菌感染的治疗前景将会有进一步的改观.

  3. Trading Agents

    CERN Document Server

    Wellman, Michael

    2011-01-01

    Automated trading in electronic markets is one of the most common and consequential applications of autonomous software agents. Design of effective trading strategies requires thorough understanding of how market mechanisms operate, and appreciation of strategic issues that commonly manifest in trading scenarios. Drawing on research in auction theory and artificial intelligence, this book presents core principles of strategic reasoning that apply to market situations. The author illustrates trading strategy choices through examples of concrete market environments, such as eBay, as well as abst

  4. Posaconazole: A New Agent for the Prevention and Management of Severe, Refractory or Invasive Fungal Infections

    Directory of Open Access Journals (Sweden)

    Andrea V Page

    2008-01-01

    Full Text Available Posaconazole is the newest antifungal agent to be approved for use in Canada. With excellent in vitro activity against a broad spectrum of yeasts and filamentous fungi, as well as having a well-tolerated oral formulation, posaconazole offers many potential advantages. Of particular interest are its seemingly lower potential for cross-resistance with other azoles and its activity (unique among oral antifungal agents against the zygomycetes. As the incidence of both common and uncommon fungal infections increases commensurate with the growing population of immunocompromised individuals, posaconazole may ultimately become an important therapeutic option. The present article reviews the in vitro and in vivo data describing its activity, and focuses on both the proven and the potential clinical applications of this new triazole agent.

  5. Purification of castamollin, a novel antifungal protein from Chinese chestnuts.

    Science.gov (United States)

    Wang, H X; Ng, T B

    2003-11-01

    A novel antifungal protein, designated castamollin, was isolated from Chinese chestnut (Castanea mollisima) seeds with a procedure involving ion exchange chromatography on DEAE-cellulose, affinity chromatography on Affi-gel blue gel, ion exchange chromatography on CM-Sepharose and FPLC-gel filtration on Superdex 75. Castamollin possessed a novel N-terminal sequence demonstrating little similarity to N-terminal sequences of Castanea sativa chitinase. Castamollin exhibited a molecular mass of 37kDa in gel filtration and SDS-PAGE. It inhibited the activity of human immunodeficiency virus-1 reverse transcriptase with an IC(50) of 7microM and translation in a cell-free rabbit reticulocyte lysate system with an IC(50) of 2.7microM. Castamollin displayed antifungal activity against Botrytis cinerea, Mycosphaerella arachidicola, Physalospora piricola, and Coprinus comatus but was devoid of lectin activity.

  6. THE IMPACT OF ANTIFUNGALS ON TOLL-LIKE RECEPTORS

    Directory of Open Access Journals (Sweden)

    Mircea Radu Mihu

    2014-03-01

    Full Text Available Fungi are increasingly recognized as major pathogens in immunocompromised individuals. The most common invasive fungal infections are caused by Candida spp., Aspergillus spp. and Cryptococcus spp. Amphotericin B has remained the cornerstone of therapy against many fulminant fungal infections but its use is limited by its multitude of side effects. Echinocandins are a newer class of antifungal drugs with activity against Candida spp. and Aspergillus spp. and constitutes an alternative to amphotericin B due to superior patient tolerability and fewer side effects. Due to their excellent bioavailability and oral availability, azoles continue to be heavily used for simple, such as fluconazole for candidal vaginitis, and complex diseases, such as voriconazole for aspergilloisis. The objective of this paper is to present current knowledge regarding the multiple interactions between the broad spectrum antifungals and the innate immune response, primarily focusing on the toll-like receptors.

  7. A Novel Infrared Radiant Glaze Exhibiting Antibacterialand Antifungal Functions

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    Infrared radiant powder was synthesized by conventional ceramic processing techniques by using Fe2O3, MnO2, CuO, Co2O3 and kaolin as raw materials. A novel infrared radiant glaze was developed by introducing the infrared radiant powder into glazing as a functional additive. Infrared radiant characteristics of the powder and the glaze were investigated. The optimum content of infrared radiant powder in glazing was ascertained to be 5%. The infrared radiant glaze exhibits significant antibacterial and antifungal functions due to the thermal effect of infrared radiation. Antibacterial percentages of the glaze reach 91%-100% when Escherichia coli, Staphylococcus aureus and Bacillus subtilis are used as model bacterium respectively, while antifungal percentage of the glaze exceeds 95% when Penicillum citrinum is used as model fungus.

  8. Persistence of histoplasma in adrenals 7 years after antifungal therapy

    Directory of Open Access Journals (Sweden)

    Deepak Kothari

    2013-01-01

    Full Text Available Adrenal histoplasmosis is an uncommon cause for adrenal insufficiency. The duration of treatment for adrenal histoplasmosis is not clear. Existing treatment regimens advocate antifungals given for periods ranging from 6 months to 2 years. We report here a rare case who showed persistence of histoplasma in adrenal biopsy 7 years after being initially treated with itraconazole for 9 months. This calls for a prolonged therapy with regular review of adrenal morphology and histology in these patients.

  9. Antibacterial and antifungal activities of benzimidazole and benzoxazole derivatives.

    OpenAIRE

    Elnima, E I; Zubair, M U; Al-Badr, A A

    1981-01-01

    The in vitro antibacterial and antifungal activities of six benzimidazole and benzoxazole derivatives were tested against standard strains and 59 clinical isolates. Of the six compounds, only compounds II and III (both benzoxazoles) were active, whereas the rest were devoid of any activity. Considerable growth inhibition of all of the standard strains, including fungi and gram-positive and gram-negative bacteria, resulted when they were treated with these compounds. Fifty-nine clinical isolat...

  10. SUSCEPTIBILITY OF CANDIDA SPECIES TO ANTIFUNGAL DRUGS IN WESTERN INDIA

    Directory of Open Access Journals (Sweden)

    Geeta M Vaghela

    2015-06-01

    Full Text Available Introduction: The increase in candidaemia is associated with high mortality. A shift has been observed in the relative frequency of each Candida spp. isolated from blood. Options of the antifungal drugs available for treatment of systemic and invasive candidiasis are restricted to polyenes, allylamines, azoles and recently developed echinocandin class of molecules. A rise in the incidence of antifungal resistance to Candida spp. has also been reported over the past decade. Studies on prevalence of infections and antifungal susceptibility testing are useful in deciding clinical strategies. Aims: To do species level identification and detect resistance, if any, among Indian clinical isolates of C. albicans. Methodology: From total 135 patients from a tertiary care hospital of Gujarat, Candida species were isolated from different clinical specimens. The growth of Candida on Sabouraud's dextrose agar was confirmed by Gram staining in which gram positive budding fungal cells were observed. Then its growth was examined for colony morphology on Sabouraud's dextrose agar and chlamydospore production on Corn meal tween 80 agar. Germ tube tests and other biochemical tests like sugar fermentation, sugar assimilation and urease test were performed to identify the species of Candida. Antifungal susceptibility testing was performed by NCCLS M44-A Disc diffusion method. Results: Out of total 135 samples, C. Albicans were isolated from 52 (38.5%. Among Non Albican Candid (NAC, Candida glabrata was 36 (26.7% followed by Candida tropicalis 25(18.5%. C. albicans was found resistant to Fluconazole, Itraconazole and Amphotericine B in 3.8%, 3.8% and 1.9% cases respectively. For NAC, resistance of Fluconazole, Itraconazole and Amphotericine B was found in 4.8%, 3.6% and 2.4% cases respectively. [Natl J Med Res 2015; 5(2.000: 122-126

  11. Peptide-based Antifungal Therapies against Emerging Infections

    OpenAIRE

    Matejuk, A.; Leng, Q.; Begum, M.D.; Woodle, M.C.; Scaria, P.; Chou, S-T; Mixson, A. J.

    2010-01-01

    Acquired drug resistance to mycotic infections is rapidly emerging as a major medical problem. Opportunistic fungal infections create therapeutic challenges, particularly in high risk immunocompromised patients with AIDS, cancer, and those undergoing transplantation. Higher mortality and/or morbidity rates due to invasive mycosis have been increasing over the last 20 years, and in light of growing resistance to commonly used antibiotics, novel antifungal drugs and approaches are required. Cur...

  12. Antifungal and anthelmintic activities of Cleistopholis patens (Annonaceae).

    Science.gov (United States)

    Akendengué, Blandine; Champy, Pierre; Nzamba, Joseph; Roblot, François; Loiseau, Philippe M; Bories, Christian

    2009-08-01

    Basic CH2Cl2 extract of the trunk bark of Cleistopholis patens (Annonaceae) exhibited antifungal activities against Candida albicans, C. parapsilosis, and C. glabrata using an agar well-diffusion assay method. Bioassay-guided fractionation of the extract led to the isolation of 8-hydroxysampangine. The methanolic extract displayed anthelmintic activity against Rhabditis pseudoelongata. Purification of the neutral CH2Cl2 extract yielded bornyl-p-transcoumarate and bornyl-p-cis-coumarate.

  13. Antifungal amphiphilic aminoglycoside K20: bioactivities and mechanism of action

    Directory of Open Access Journals (Sweden)

    Sanjib K. Shrestha

    2014-12-01

    Full Text Available K20 is a novel amphiphilic antifungal aminoglycoside that is synthetically derived from the antibiotic kanamycin A. Reported here are investigations of K20’s antimicrobial activities, cytotoxicity, and fungicidal mechanism of action. In vitro growth inhibitory activities against a variety of human and plant pathogenic yeasts, filamentous fungi, and bacteria were determined using microbroth dilution assays and time-kill curve analyses, and hemolytic and animal cell cytotoxic activities were determined. Effects on Cryptococcus neoformans H-99 infectivity were determined with a preventive murine lung infection model. The antifungal mechanism of action was studied using intact fungal cells, yeast lipid mutants, and small unilamellar lipid vesicles. K20 exhibited broad-spectrum in vitro antifungal activities but not antibacterial activities. Pulmonary, single dose-administration of K20 reduced C. neoformans lung infection rates 4-fold compared to controls. Hemolysis and half-maximal cytotoxicities of mammalian cells occurred at concentrations that were 10 to 32-fold higher than fungicidal MICs. With fluorescein isothiocyanate, 20 to 25 mg/L K20 caused staining of >95% of C. neoformans and Fusarium graminearum cells and at 31.3 mg/L caused rapid leakage (30 to 80% in 15 min of calcein from preloaded small unilamellar lipid vesicles. K20 appears to be a broad-spectrum fungicide, capable of reducing the infectivity of C. neoformans, and exhibits low hemolytic activity and mammalian cell toxicity. It perturbs the plasma membrane by mechanisms that are lipid modulated. K20 is a novel amphiphilic aminoglycoside amenable to scalable production and a potential lead antifungal for therapeutic and crop protection applications.

  14. Trichoharzianol, a new antifungal from Trichoderma harzianum F031.

    Science.gov (United States)

    Jeerapong, Chotika; Phupong, Worrapong; Bangrak, Phuwadol; Intana, Warin; Tuchinda, Patoomratana

    2015-04-15

    A new decalin derivative, trichoharzianol (1), together with three known compounds, eujavanicol A (2), 5-hydroxy-3-hydroxymethyl-2-methyl-7-methoxychromone (3), and 4,6-dihydroxy-5-methylphthalide (4), were isolated from Trichoderma harzianum F031. For the first time, compounds 2-4 were reported from the Trichoderma species. Their structures were characterized by spectroscopic methods. Trichoharzianol (1) showed the highest antifungal activity against Colletotrichum gloeosporioides, with a minimum inhibitory concentration (MIC) of 128 μg/mL.

  15. Antifungal activity of antifungal drugs, as well as drug combinations against Exophiala dermatitidis.

    Science.gov (United States)

    Sun, Yi; Liu, Wei; Wan, Zhe; Wang, Xiaohong; Li, Ruoyu

    2011-02-01

    To evaluate the in vitro efficacy of common antifungal drugs, as well as the interactions of caspofungin with voriconazole, amphotericin B, or itraconazole against the pathogenic black yeast Exophiala dermatitidis from China, the minimal inhibitory concentrations (MICs) of terbinafine, voriconazole, itraconazole, amphotericin B, fluconazole, and caspofungin against 16 strains of E. dermatitidis were determined by using CLSI broth microdilution method (M38-A2). The minimal fungicidal concentrations (MFCs) were also determined. Additionally, the interactions of caspofungin with voriconazole, amphotericin B, itraconazole or fluconazole, that of terbinafine with itraconazole, or that of fluconazole with amphotericin B were assessed by using the checkerboard technique. The fractional inhibitory concentration index (FICI) was used to categorize drug interactions as following, synergy, FICI ≤ 0.5; indifference, FICI > 0.5 and ≤4.0; or antagonism, FICI > 4.0. The MIC ranges of terbinafine, voriconazole, itraconazole, amphotericin B, fluconazole, and caspofungin against E. dermatitidis were 0.06-0.125 mg/l, 0.25-1.0 mg/l, 1.0-2.0 mg/l, 1.0-2.0 mg/l, 16-64 mg/l, and 32-64 mg/l, respectively. The in vitro interactions of caspofungin with voriconazole, amphotericin B, and itraconazole showed synergic effect against 10/16(62.5%), 15/16(93.75%), and 16/16(100%) isolates, while that of caspofungin with fluconazole showed indifference. Besides, the interaction of terbinafine with itraconazole as well as that of fluconazole with amphotericin B showed indifference. Terbinafine, voriconazole, itraconazole, and amphotericin B have good activity against E. dermatitidis. The combinations of caspofungin with voriconazole, amphotericin B or itraconazole present synergic activity against E. dermatitidis. These results provide the basis for novel options in treating various E. dermatitidis infections.

  16. Antifungal activity of essential oil of Ziziphora clinopodioides and the inhibition of aflatoxin B1 production in maize grain.

    Science.gov (United States)

    Moghadam, Hediyeh Davoudi; Sani, Ali Mohamadi; Sangatash, Masoomeh Mehraban

    2016-03-01

    The aim of this study was to determine the antifungal effect of the essential oil obtained from Ziziphora clinopodioides L on two fungi species including Aspergillus flavus and Aspergillus parasiticus using microdilution method. The minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) were determined for the essential oil at 10 different concentrations (i.e. 25,000, 12,500, 6250, 3125, 1562.5, 781.25, 390.625, 195.31, 97.65, and 48.82 µg/ml). Finally, the effect of the essential oil at six levels (6250, 3125, 1600, 800, 400, and 196 µg/ml) was investigated on the growth and activity of A. flavus and A. parasiticus, and also toxin production of these species in maize at 0.97 aw and 25°C after 29 days. Aflatoxin B1 (AFB1) content was assayed by enzyme linked immuno-sorbent assay technique. Results showed that essential oil of Z. clinopodioides was found more effective on A. parasiticus than A. flavus in both in vitro and in vivo conditions. Z. clinopodioides oil exhibited the same MIC value in the liquid medium against all fungal strains (48.82 µg/ml), while it showed different activity against A. flavus and A. parasiticus with MFC values of 781.25 and 390.625 µg/ml respectively. Under storage condition in maize, AFB1 production was significantly (p essential oil of Z. clinopodioides had significant antifungal activity (p < 0.05); therefore, it can be used as an antifungal agent in the food and medicinal industries.

  17. In vitro antifungal susceptibility patterns of Candida albicans from HIV and AIDS patients attending the Nylon Health District Hospital in Douala, Cameroon

    Directory of Open Access Journals (Sweden)

    Anna L. Njunda

    2012-05-01

    Full Text Available HIV and AIDS are major public health problems in Cameroon where the HIV prevalence is 5.5%. Candidiasis is the leading opportunistic mycosis in HIV and AIDS patients. The objective of this study was to determine the in vitro antifungal susceptibility pattern of Candida albicans in HIV and AIDS patients to eight antifungal agents in the Nylon Health District of Douala in Cameroon. Three hundred and four HIV and AIDS patients were recruited between March and August 2007 to participate in a cross-sectional study. All subjects who fulfilled the inclusion criteria were enrolled. Informed consent was obtained from all subjects before samples were collected. Three samples comprising oral swabs, vagina/urethra swabs and a mid-stream urine were collected from each subject. Specimens were cultured on sabouraud dextrose agar and C. albicans isolates were identified using the germ tube technique. The disk diffusion method was used for antifungal susceptibility testing using eight antifungal agents. The prevalence of candidiasis in the study population was 67.8% (95% CI: 62.5-73.1% and that of C. albicans was 42.8% (95% CI: 37.2-48.4%. Oral swabs had the highest prevalence of C. albicans followed by vaginal/urethral samples (52.6% vs. 29.7% respectively. Forty (30.8% subjects had C. albicans infection at more than one collection site. There was a statistically significant difference in the infectivity of C. albicans with age, sex and site of infection (P<0.05. C. albicans isolates were most sensitive to ketoconazole (80% followed by econazole (64.6% while fluconazole and 5-flurocytosin recorded the poorest sensitivities (22.9% vs 24.6%, respectively. There was a statistically significant difference in the sensitivity pattern of antifungal agents with respect to the site of isolation of the organism (P<0.05. Ketoconazole is the drug of choice for the treatment of C. albicans infection in HIV and AIDS patients in the Nylon Health District of Douala, Cameroon.

  18. Antifungal Properties of Chenopodium ambrosioides Essential Oil Against Candida Species

    Directory of Open Access Journals (Sweden)

    Gerard Vilarem

    2010-09-01

    Full Text Available The essential oil of the aerial part (leaves, flowers and stem of Chenopodium ambrosioides was obtained by hydrodistillation and its chemical composition analyzed by GC and GC/MS, which permitted the identification of 14 components, representing 98.8% of the total oil. Major components were α-terpinene (51.3%, p-cymene (23.4% and p-mentha-1,8-diène (15.3%. The antifungal properties of this essential oil were investigated in vitro by the well diffusion and broth microdilution methods. The in vitro antifungal activity was concentration dependent and minimum inhibitory concentration values varied from 0.25 to 2 mg/mL. The in vivo antifungal activity was evaluated on an induced vaginal candidiasis rat model. The in vivo activity of the oil on mice vaginal candidiasis was not dose-dependent. Indeed, all the three tested doses; 0.1%, 1% and 10% led to the recovery of mice from the induced infection after 12 days of treatment. The effect of the essential oil on C. albicans ATCC 1663 fatty acid profile was studied. This oil has a relatively important dose-dependent effect on the fatty acids profile.

  19. Antifungal and Antibacterial Metabolites from a French Poplar Type Propolis

    Science.gov (United States)

    Boisard, Séverine; Le Ray, Anne-Marie; Landreau, Anne; Kempf, Marie; Cassisa, Viviane; Flurin, Catherine; Richomme, Pascal

    2015-01-01

    During this study, the in vitro antifungal and antibacterial activities of different extracts (aqueous and organic) obtained from a French propolis batch were evaluated. Antifungal activity was evaluated by broth microdilution on three pathogenic strains: Candida albicans, C. glabrata, and Aspergillus fumigatus. Antibacterial activity was assayed using agar dilution method on 36 Gram-negative and Gram-positive strains including Staphylococcus aureus. Organic extracts showed a significant antifungal activity against C. albicans and C. glabrata (MIC80 between 16 and 31 µg/mL) but only a weak activity towards A. fumigatus (MIC80 = 250 µg/mL). DCM based extracts exhibited a selective Gram-positive antibacterial activity, especially against S. aureus (SA) and several of its methicillin-resistant (MRSA) and methicillin-susceptible (MSSA) strains (MIC100 30–97 µg/mL). A new and active derivative of catechin was also identified whereas a synergistic antimicrobial effect was noticed during this study. PMID:25873978

  20. An overview of antifungal peptides derived from insect.

    Science.gov (United States)

    Faruck, Mohammad Omer; Yusof, Faridah; Chowdhury, Silvia

    2016-06-01

    Fungi are not classified as plants or animals. They resemble plants in many ways but do not produce chlorophyll or make their own food photosynthetically like plants. Fungi are useful for the production of beer, bread, medicine, etc. More complex than viruses or bacteria; fungi can be destructive human pathogens responsible for various diseases in humans. Most people have a strong natural immunity against fungal infection. However, fungi can cause diseases when this immunity breaks down. In the last few years, fungal infection has increased strikingly and has been accompanied by a rise in the number of deaths of cancer patients, transplant recipients, and acquired immunodeficiency syndrome (AIDS) patients owing to fungal infections. The growth rate of fungi is very slow and quite difficult to identify. A series of molecules with antifungal activity against different strains of fungi have been found in insects, which can be of great importance to tackle human diseases