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Sample records for broad antifungal activity

  1. 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

  2. In Vitro Activity of a Novel Broad-Spectrum Antifungal, E1210, Tested against Aspergillus spp. Determined by CLSI and EUCAST Broth Microdilution Methods ▿

    Science.gov (United States)

    Pfaller, Michael A.; Duncanson, Frederick; Messer, Shawn A.; Moet, Gary J.; Jones, Ronald N.; Castanheira, Mariana

    2011-01-01

    E1210 is a first-in-class broad-spectrum antifungal that suppresses hyphal growth by inhibiting fungal glycophosphatidylinositol (GPI) biosynthesis. In the present study, we extend these findings by examining the activity of E1210 and comparator antifungal agents against Aspergillus spp. by using the methods of the Clinical and Laboratory Standards Institute (CLSI) and the European Committee for Antimicrobial Susceptibility Testing (EUCAST) to test wild-type (WT) as well as amphotericin B (AMB)-resistant (-R) and azole-R strains (as determined by CLSI methods). Seventy-eight clinical isolates of Aspergillus were tested including 20 isolates of Aspergillus flavus species complex (SC), 22 of A. fumigatus SC, 13 of A. niger SC, and 23 of A. terreus SC. The collection included 15 AMB-R (MIC, ≥2 μg/ml) isolates of A. terreus SC and 10 itraconazole-R (MIC, ≥4 μg/ml) isolates of A. fumigatus SC (7 isolates), A. niger SC (2 isolates), and A. terreus SC (1 isolate). Comparator antifungal agents included anidulafungin, caspofungin, amphotericin B, itraconazole, posaconzole, and voriconazole. Both CLSI and EUCAST methods were highly concordant for E1210 and all comparators. The essential agreement (EA; ±2 log2 dilution steps) was 100% for all comparisons with the exception of posaconazole versus A. terreus SC (EA = 91.3%). The minimum effective concentration (MEC)/MIC90 values (μg/ml) for E1210, anidulafungin, caspofungin, itraconazole, posaconazole, and voriconazole, respectively, were as follows for each species: for A. flavus SC, 0.03, ≤0.008, 0.12, 1, 1, and 1; for A. fumigatus SC, 0.06, 0.015, 0.12, >8, 1, and 4; for A. niger SC, 0.015, 0.03, 0.12, 4, 1, and 2; and for A. terreus SC, 0.06, 0.015, 0.12, 1, 0.5, and 1. E1210 was very active against AMB-R strains of A. terreus SC (MEC range, 0.015 to 0.06 μg/ml) and itraconazole-R strains of A. fumigatus SC (MEC range, 0.03 to 0.12 μg/ml), A. niger SC (MEC, 0.008 μg/ml), and A. terreus SC (MEC, 0.015

  3. 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.

  4. Antifungal activity of five species of Polygala

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    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.

  5. 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.

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

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    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.

  7. 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.

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

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    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.

  9. 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.

  10. 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.

  11. 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.

  12. Synthesis and antifungal activity of derivatives of 2- and 3-benzofurancarboxylic acids.

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    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).

  13. 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.

  14. 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.

  15. 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.

  16. Antifungal activity of Terminalia superba (combretaceae

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    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.

  17. Design, synthesis of novel antifungal triazole derivatives with high activities against Aspergillus fumigatus

    Institute of Scientific and Technical Information of China (English)

    Qiu Qin He; Chao Mei Liu; Ke Li; Yong Bing Cao

    2007-01-01

    Based on the active site of Aspergillusfumigatus lanosterol 14α-demethylase (AF-CYP51), novel triazole compounds were designed. Their chemical synthesis and the antifungal activities were reported. The results showed that all the target compounds exhibited excellent activities with broad spectrum; in which compounds 4, 12 and 15 showed comparable activities against A.fumigatus to the control drug itraconazole.

  18. 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 ...

  19. 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.

  20. 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.

  1. 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).

  2. Antifungal membranolytic activity of the tyrocidines against filamentous plant fungi.

    Science.gov (United States)

    Rautenbach, Marina; Troskie, Anscha M; Vosloo, Johan A; Dathe, Margitta E

    2016-11-01

    The tyrocidines and analogues are cyclic decapeptides produced by Brevibacillus parabrevis with a conserved sequence of cyclo(D-Phe(1)-Pro(2)-X(3)-x(4)-Asn(5)-Gln(6)-X(7)-Val(8)-X(9)-Leu(10)) with Trp(3,4)/Phe(3,4) in the aromatic dipeptide unit, Lys(9)/Orn(9) as their cationic residue and Tyr (tyrocidines), Trp (tryptocidines) or Phe (phenicidines) in position 7. Previous studies indicated they have a broad antifungal spectrum with the peptides containing a Tyr residue in position 7 being more active than those with a Phe or Trp residue in this position. Detailed analysis of antifungal inhibition parameters revealed that Phe(3)-D-Phe(4) in the aromatic dipeptide unit lead to more consistent activity against the three filamentous fungi in this study. These peptides exhibited high membrane activity and fast leakage kinetics against model membranes emulating fungal membranes, with selectivity towards ergosterol containing membranes. More fluid membranes and doping of liposomes with the sphingolipid, glucosylceramide, led to a decreased permeabilising activity. Peptide-induced uptake of membrane impermeable dyes was observed in hyphae of both Fusarium solani and Botrytis cinerea, with uptake more pronounced at the hyphal growth tips that are known to contain ergosterol-sphigolipid rich lipid rafts. Tyrocidine interaction with these rafts may lead to the previously observed fungal hyperbranching. However, the leakage of model membranes and Bot. cinerea did not correlate directly with the antifungal inhibition parameters, indicating another target or mode of action. Proteinase K treatment of target fungi had a minimal influence or even improved the tyrocidine activity, ruling out a mannoprotein target in the fungal cell wall. β-glucanase treatment of Bot. cinerea did not significantly affect the tyrocidine activity, but there was a significant loss in activity towards the β-glucanase treated F. solani. This study showed the tyrocidine antifungal membrane activity is

  3. 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.

  4. 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 ...

  5. 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.

  6. 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.

  7. 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.

  8. 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.

  9. 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.

  10. 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.

  11. 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...

  12. 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.  ...

  13. 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.

  14. 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.

  15. 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.

  16. 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.

  17. 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.

  18. 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.

  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. 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

  1. 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.

  2. 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)

  3. 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.

  4. 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.

  5. 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].

  6. 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...

  7. 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..

  8. 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

  9. Fungal Root Microbiome from Healthy and Brittle Leaf Diseased Date Palm Trees (Phoenix dactylifera L.) Reveals a Hidden Untapped Arsenal of Antibacterial and Broad Spectrum Antifungal Secondary Metabolites.

    Science.gov (United States)

    Mefteh, Fedia B; Daoud, Amal; Chenari Bouket, Ali; Alenezi, Faizah N; Luptakova, Lenka; Rateb, Mostafa E; Kadri, Adel; Gharsallah, Neji; Belbahri, Lassaad

    2017-01-01

    In this study, we aimed to explore and compare the composition, metabolic diversity and antimicrobial potential of endophytic fungi colonizing internal tissues of healthy and brittle leaf diseased (BLD) date palm trees (Phoenix dactylifera L.) widely cultivated in arid zones of Tunisia. A total of 52 endophytic fungi were isolated from healthy and BLD roots of date palm trees, identified based on internal transcribed spacer-rDNA sequence analysis and shown to represent 13 species belonging to five genera. About 36.8% of isolates were shared between healthy and diseased root fungal microbiomes, whereas 18.4 and 44.7% of isolates were specific to healthy and BLD root fungal microbiomes, respectively. All isolates were able to produce at least two of the screened enzymes including amylase, cellulase, chitinase, pectinase, protease, laccase and lipase. A preliminary screening of the isolates using disk diffusion method for antibacterial activity against four Gram-positive and three Gram-negative bacteria and antifungal activities against three phytopathogenic fungi indicated that healthy and BLD root fungal microbiomes displayed interesting bioactivities against examined bacteria and broad spectrum bioactivity against fungal pathogens. Some of these endophytic fungi (17 isolates) were fermented and their extracts were evaluated for antimicrobial potential against bacterial and fungal isolates. Results revealed that fungal extracts exhibited antibacterial activities and were responsible for approximately half of antifungal activities against living fungi. These results suggest a strong link between fungal bioactivities and their secondary metabolite arsenal. EtOAc extracts of Geotrichum candidum and Thielaviopsis punctulata originating from BLD microbiome gave best results against Micrococcus luteus and Bacillus subtilis with minimum inhibitory concentration (MIC, 0.78 mg/mL) and minimum bactericidal concentration (6.25 mg/mL). G. candidum gave the best result against

  10. Fungal Root Microbiome from Healthy and Brittle Leaf Diseased Date Palm Trees (Phoenix dactylifera L.) Reveals a Hidden Untapped Arsenal of Antibacterial and Broad Spectrum Antifungal Secondary Metabolites

    Science.gov (United States)

    Mefteh, Fedia B.; Daoud, Amal; Chenari Bouket, Ali; Alenezi, Faizah N.; Luptakova, Lenka; Rateb, Mostafa E.; Kadri, Adel; Gharsallah, Neji; Belbahri, Lassaad

    2017-01-01

    In this study, we aimed to explore and compare the composition, metabolic diversity and antimicrobial potential of endophytic fungi colonizing internal tissues of healthy and brittle leaf diseased (BLD) date palm trees (Phoenix dactylifera L.) widely cultivated in arid zones of Tunisia. A total of 52 endophytic fungi were isolated from healthy and BLD roots of date palm trees, identified based on internal transcribed spacer-rDNA sequence analysis and shown to represent 13 species belonging to five genera. About 36.8% of isolates were shared between healthy and diseased root fungal microbiomes, whereas 18.4 and 44.7% of isolates were specific to healthy and BLD root fungal microbiomes, respectively. All isolates were able to produce at least two of the screened enzymes including amylase, cellulase, chitinase, pectinase, protease, laccase and lipase. A preliminary screening of the isolates using disk diffusion method for antibacterial activity against four Gram-positive and three Gram-negative bacteria and antifungal activities against three phytopathogenic fungi indicated that healthy and BLD root fungal microbiomes displayed interesting bioactivities against examined bacteria and broad spectrum bioactivity against fungal pathogens. Some of these endophytic fungi (17 isolates) were fermented and their extracts were evaluated for antimicrobial potential against bacterial and fungal isolates. Results revealed that fungal extracts exhibited antibacterial activities and were responsible for approximately half of antifungal activities against living fungi. These results suggest a strong link between fungal bioactivities and their secondary metabolite arsenal. EtOAc extracts of Geotrichum candidum and Thielaviopsis punctulata originating from BLD microbiome gave best results against Micrococcus luteus and Bacillus subtilis with minimum inhibitory concentration (MIC, 0.78 mg/mL) and minimum bactericidal concentration (6.25 mg/mL). G. candidum gave the best result against

  11. 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.

  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. In vitro production and antifungal activity of peptide ABP-dHC-cecropin A.

    Science.gov (United States)

    Zhang, Jiaxin; Movahedi, Ali; Xu, Junjie; Wang, Mengyang; Wu, Xiaolong; Xu, Chen; Yin, Tongming; Zhuge, Qiang

    2015-04-10

    The antimicrobial peptide ABP-dHC-cecropin A is a small cationic peptide with potent activity against a wide range of bacterial species. Evidence of antifungal activity has also been suggested; however, testing of this peptide has been limited due to the low expression of cecropin proteins in Escherichia coli. To improve expression of this peptide in E. coli, ABP-dHC-cecropin A was cloned into a pSUMO vector and transformed into E. coli, resulting in the production of a pSUMO-ABP-dHC-cecropin A fusion protein. The soluble form of this protein was then purified by Ni-IDA chromatography, yielding a total of 496-mg protein per liter of fermentation culture. The SUMO-ABP-dHC-cecropin A fusion protein was then cleaved using a SUMO protease and re-purified by Ni-IDA chromatography, yielding a total of 158-mg recombinant ABP-dHC-cecropin A per liter of fermentation culture at a purity of ≥94%, the highest yield reported to date. Antifungal activity assays performed using this purified recombinant peptide revealed strong antifungal activity against both Candida albicans and Neurospora crassa, as well as Rhizopus, Fusarium, Alternaria, and Mucor species. Combined with previous analyses demonstrating strong antibacterial activity against a number of important bacterial pathogens, these results confirm the use of ABP-dHC-cecropin A as a broad-spectrum antimicrobial peptide, with significant therapeutic potential.

  14. 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.

  15. Antifungal activity of diketopiperazines and stilbenes against plant pathogenic fungi in vitro.

    Science.gov (United States)

    Kumar, S Nishanth; Nambisan, Bala

    2014-01-01

    The present study aimed to investigate antifungal activity of a stilbene and diketopiperazine compounds against plant pathogenic fungi, including Phytophthora capsici, P. colocasiae, Botrytis cinerea and Colletotrichum gloeosporioides. Minimal inhibition concentrations (MIC) and minimal fungicidal concentrations (MFC) of stilbenes and diketopiperazines for each fungus were determined using microplate method. Best activity was recorded by stilbenes against P. capsici and P. colocasiae. All four test compounds were effective in inhibiting different stages of the life cycle of test fungi. Stilbenes were more effective than diketopiperazines in inhibiting mycelial growth and inhibiting different stages of the life cycle of P. capsici and P. colocasiae. Rupture of released zoospores induced by stilbenes was reduced by addition of 100 mM glucose. The effects of stilbenes on mycelial growth and zoospore release, but not zoospore rupture, were reduced largely when pH value was above 7. In addition, stilbenes were investigated for its antifungal stability against Phytophthora sp. The results showed that stilbenes maintained strong fungistatic activity over a wide pH range (pH 4–9) and temperature range (70–120 °C). The compound stilbenes exhibited strong and stable broad-spectrum antifungal activity, and had a significant fungicidal effect on fungal cells. Results from prebiocontrol evaluations performed to date are probably useful in the search for alternative approaches to controlling serious plant pathogens.

  16. Antifungal Activity of 14-Helical β-Peptides against Planktonic Cells and Biofilms of Candida Species

    Directory of Open Access Journals (Sweden)

    Namrata Raman

    2015-08-01

    Full Text Available Candida albicans is the most prevalent cause of fungal infections and treatment is further complicated by the formation of drug resistant biofilms, often on the surfaces of implanted medical devices. In recent years, the incidence of fungal infections by other pathogenic Candida species such as C. glabrata, C. parapsilosis and C. tropicalis has increased. Amphiphilic, helical β-peptide structural mimetics of natural antimicrobial α-peptides have been shown to exhibit specific planktonic antifungal and anti-biofilm formation activity against C. albicans in vitro. Here, we demonstrate that β-peptides are also active against clinically isolated and drug resistant strains of C. albicans and against other opportunistic Candida spp. Different Candida species were susceptible to β-peptides to varying degrees, with C. tropicalis being the most and C. glabrata being the least susceptible. β-peptide hydrophobicity directly correlated with antifungal activity against all the Candida clinical strains and species tested. While β-peptides were largely ineffective at disrupting existing Candida biofilms, hydrophobic β-peptides were able to prevent the formation of C. albicans, C. glabrata, C. parapsilosis and C. tropicalis biofilms. The broad-spectrum antifungal activity of β-peptides against planktonic cells and in preventing biofilm formation suggests the promise of this class of molecules as therapeutics.

  17. Antifungal activity of methanol and n-hexane extracts of three Chenopodium species against Macrophomina phaseolina.

    Science.gov (United States)

    Javaid, Arshad; Amin, Muhammad

    2009-01-01

    Antifungal activity of methanol and n-hexane leaf, stem, root and inflorescence extracts (1, 2, 3 and 4% w/v) of three Chenopodium species (family Chenopodiaceae) namely Chenopodium album L., Chenopodium murale L. and Chenopodium ambrosioides L. was investigated against Macrophomina phaseolina (Tassi) G. Goid., a soil-borne fungal plant pathogen that has a broad host range and wide geographical distribution. All the extracts of the three Chenopodium species significantly suppressed the test fungal growth. However, there was marked variation among the various extract treatments. Methanol inflorescence extract of C. album exhibited highest antifungal activity resulting in up to 96% reduction in fungal biomass production. By contrast, methanol leaf extract of the same species exhibited least antifungal activity where 21-44% reduction in fungal biomass was recorded due to various employed extract concentrations. The various methanol extracts of C. murale and C. ambrosioides decreased fungal biomass by 62-90 and 50-84%, respectively. Similarly, various n-hexane extracts of C. album, C. murale and C. ambrosioides reduced fungal biomass by 60-94, 43-90 and 49-86%, respectively.

  18. 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.

  19. Enhanced Antifungal Activity by Ab-Modified Amphotericin B-Loaded Nanoparticles Using a pH-Responsive Block Copolymer

    Science.gov (United States)

    Tang, Xiaolong; Dai, Jingjing; Xie, Jun; Zhu, Yongqiang; Zhu, Ming; Wang, Zhi; Xie, Chunmei; Yao, Aixia; Liu, Tingting; Wang, Xiaoyu; Chen, Li; Jiang, Qinglin; Wang, Shulei; Liang, Yong; Xu, Congjing

    2015-06-01

    Fungal infections are an important cause of morbidity and mortality in immunocompromised patients. Amphotericin B (AMB), with broad-spectrum antifungal activity, has long been recognized as a powerful fungicidal drug, but its clinical toxicities mainly nephrotoxicity and poor solubility limit its wide application in clinical practice. The fungal metabolism along with the host immune response usually generates acidity at sites of infection, resulting in loss of AMB activity in a pH-dependent manner. Herein, we developed pH-responsive AMB-loaded and surface charge-switching poly( d, l-lactic- co-glycolic acid)- b-poly( l-histidine)- b-poly(ethylene glycol) (PLGA-PLH-PEG) nanoparticles for resolving the localized acidity problem and enhance the antifungal efficacy of AMB. Moreover, we modified AMB-encapsulated PLGA-PLH-PEG nanoparticles with anti- Candida albicans antibody (CDA) (CDA-AMB-NPs) to increase the targetability. Then, CDA-AMB-NPs were characterized in terms of physical characteristics, in vitro drug release, stability, drug encapsulation efficiency, and toxicity. Finally, the targetability and antifungal activity of CDA-AMB-NPs were investigated in vitro /in vivo. The result demonstrated that CDA-AMB-NPs significantly improve the targetability and bioavailability of AMB and thus improve its antifungal activity and reduce its toxicity. These NPs may become a good drug carrier for antifungal treatment.

  20. Antifungal activity of natural and synthetic amides from Piper species

    Energy Technology Data Exchange (ETDEWEB)

    Marques, Joaquim V.; Oliveira, Alberto de; Kato, Massuo J., E-mail: majokato@iq.usp.b [Universidade de Sao Paulo (IQ/USP), SP (Brazil). Inst. de Quimica; Raggi, Ludmila; Young, Maria C. [Instituto de Botanica, Sao Paulo, SP (Brazil). Secao de Fisiologia e Bioquimica de Plantas

    2010-07-01

    The antifungal leaves extract from Piper scutifolium was submitted to bioactivity-guided chromatographic separation against Cladosporium cladosporioides and C. sphaerospermum yielding piperine, piperlonguminine and corcovadine as the active principles which displayed a detection limit of 1 {mu}g. Structure-activity relationships were investigated with the preparation of twelve analogs having differences in the number of unsaturations, aromatic ring substituents and in the amide moiety. Analogs having a single double-bond and no substituent in the aromatic ring displayed higher activity, while N,N,-diethyl analogs displayed higher dose-dependent activity. (author)

  1. New constitutive latex osmotin-like proteins lacking antifungal activity.

    Science.gov (United States)

    Freitas, Cleverson D T; Silva, Maria Z R; Bruno-Moreno, Frederico; Monteiro-Moreira, Ana C O; Moreira, Renato A; Ramos, Márcio V

    2015-11-01

    Proteins that share similar primary sequences to the protein originally described in salt-stressed tobacco cells have been named osmotins. So far, only two osmotin-like proteins were purified and characterized of latex fluids. Osmotin from Carica papaya latex is an inducible protein lacking antifungal activity, whereas the Calotropis procera latex osmotin is a constitutive antifungal protein. To get additional insights into this subject, we investigated osmotins in latex fluids of five species. Two potential osmotin-like proteins in Cryptostegia grandiflora and Plumeria rubra latex were detected by immunological cross-reactivity with polyclonal antibodies produced against the C. procera latex osmotin (CpOsm) by ELISA, Dot Blot and Western Blot assays. Osmotin-like proteins were not detected in the latex of Thevetia peruviana, Himatanthus drasticus and healthy Carica papaya fruits. Later, the two new osmotin-like proteins were purified through immunoaffinity chromatography with anti-CpOsm immobilized antibodies. Worth noting the chromatographic efficiency allowed for the purification of the osmotin-like protein belonging to H. drasticus latex, which was not detectable by immunoassays. The identification of the purified proteins was confirmed after MS/MS analyses of their tryptic digests. It is concluded that the constitutive osmotin-like proteins reported here share structural similarities to CpOsm. However, unlike CpOsm, they did not exhibit antifungal activity against Fusarium solani and Colletotrichum gloeosporioides. These results suggest that osmotins of different latex sources may be involved in distinct physiological or defensive events.

  2. 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.

  3. Antibacterial and antifungal activities of some Mexican medicinal plants.

    Science.gov (United States)

    Ruiz-Bustos, E; Velazquez, C; Garibay-Escobar, A; García, Z; Plascencia-Jatomea, M; Cortez-Rocha, M O; Hernandez-Martínez, J; Robles-Zepeda, R E

    2009-12-01

    In Mexico about 4,000 plant species have some medicinal use. The aim of this work was to evaluate the antimicrobial activity of six Mexican medicinal plants against fungi and Gram-positive and Gram-negative bacteria. Methanolic extracts were prepared from the Mexican medicinal plants Amphypteringium adstrigens, Castella tortuosa, Coutarea latiflora, Ibervillea sonorae, Jatropha cuneata, and Selaginella lepidophylla. The antibacterial and antifungal activities of the plants were determined by the broth microdilution method and the radial growth inhibition assay, respectively. All Mexican plants tested showed antimicrobial activity. Among the six plant extracts analyzed, J. cuneata showed the highest growth-inhibitory activity against fungi, Gram-positive and Gram-negative bacteria (J. cuneata > A. adstrigens > C. latiflora > C. tortuosa > I. sonorae approximately S. lepidophylla). Shigella flexneri and Staphylococcus aureus were the most susceptible bacteria to plant extracts. Complete inhibition of S. flexneri growth was observed with J. cuneata methanolic extract at 90 microg/mL. This plant extract also showed the strongest antifungal activity against Fusarium verticillioides and Aspergillus niger. Our data suggest that the medicinal plants tested have important antimicrobial properties. This is the first report describing the antimicrobial activities of several of the Mexican medicinal plants used in this study.

  4. Antifungal activity of plant-based tinctures on Candida

    Directory of Open Access Journals (Sweden)

    Andreia Medeiros Rodrigues Cardoso

    2012-01-01

    Full Text Available Objective: To evaluate through determination of minimum inhibitory concentration (MIC the antifungal activity of Salvia officinalis (sage, Anacardium occidentale (cashew and Malva sylvestris (mallow tinctures on Candida albicans (ATCC 40227, C. tropicalis (ATCC 13803 and C. krusei (ATCC 40147. Material and methods: In 96-well microplates, 100 μl of Sabouraud-Dextrose broth doubly concentrated, 100 μl of the tested tinctures and 10 μl of fungal inoculums (1.5 x 106 organisms/ml were inserted. The products were diluted from initial concentration of 100 mg/ml until 0.78 mg/ml. MIC corresponded to the lowest dilution at which there was no visible fungal growth. Nystatin (100,000 UI/ml was used as control. Statistical analysis was performed by Kruskal-Wallis and Dunn tests (p < 0.05. Results: S. officinalis tincture did not inhibit the growth of C. albicans and C. tropicalis; MIC was 100 mg/ml for C. krusei. For A. occidentale, MIC was 100 mg/ml for C. albicans and C. krusei, and for C. tropicalis, there was no fungal inhibition. M. sylvestris tincture presented MIC at 25 mg/ml for C. krusei and 100 mg/ml for C. albicans and C. tropicalis. The best antifungal activity was showed by M. sylvestris tincture (p < 0.05. Conclusion: M. sylvestris tincture exhibited antifungal activity against all the tested strains at lower concentrations. S. officinalis tincture inhibited the action of C. krusei and A. occidentale tincture showed activity against C. albicans and C. tropicalis.

  5. 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.

  6. Antifungal activity ofOcimum sanctum Linn. (Lamiaceae) on clinically isolated dermatophytic fungi

    Institute of Scientific and Technical Information of China (English)

    Balakumar S; Rajan S; Thirunalasundari T; Jeeva S

    2011-01-01

    Objective:To assess antifungal activity ofOcimum sanctum leaves against dermatophytic fungi. Methods: Antifungal activity ofOcimum sanctum leaves was measured by38 A NCCLS method. Minimum inhibitory concentration(MIC) and minimum fungicidal concentration(MFC) of various extracts and fractions ofOcimum sanctum leaves were also determined.Results:Ocimum sanctum leaves possessed antifungal activity against clinically isolated dermatophytes at the concentration of200μg/mL.MICandMFC were high with water fraction (200 μg/mL) against dermatophytic fungi used.Conclusions:Ocimum sanctum has antifungal activity, and the leaf extracts may be a useful source for dermatophytic infections.

  7. ANTIFUNGAL ACTIVITY OF SOME PLANT EXTRACT S AGAINST FUSARIUM SOLANI

    Directory of Open Access Journals (Sweden)

    S.K. BHARADWAJ

    2007-01-01

    Full Text Available The aqueous extracts of twenty plants were screened for their antifungal activity Fusarium solani, causal organism if Sudden Death Syndrome (SDS of Soybean (Glycine max wilt diseases, soft rot of potato. The maximum inhibitory effect was shown by leaf extracts of Camellia sinensis (67.17%, root extracts of Asparagus racemosus (54.43%. Some of the other plants showed moderate to intermediate inhibition against the mycelium growth of test fungi whcih varied in the following range Callistemon lanceolatus> Agegle marmelos> Azadirachta> Acacia catechu> Aloevera.

  8. 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...

  9. A technique for detecting antifungal activity of proteins separated by polyacrylamide gel electrophoresis.

    Science.gov (United States)

    De Bolle, M F; Goderis, I J; Terras, F R; Cammue, B P; Broekaert, W F

    1991-06-01

    A technique was developed for the detection of antifungal activity of proteins after discontinuous polyacrylamide gel electrophoresis under native conditions. The antifungal activity is detected as growth inhibition zones in a homogeneous fungal lawn, grown in an agar layer spread on top of the polyacrylamide gel. The position of proteins with antifungal activity can be determined on a diffusion blot prepared from the same gel. The technique is illustrated for three antifungal plant proteins, i.e. alpha-purothionin, Urtica dioica agglutinin, and tobacco chitinase.

  10. Synthesis of Azole-containing Piperazine Derivatives and Evaluation of their Antibacterial, Antifungal and Cytotoxic Activities

    Energy Technology Data Exchange (ETDEWEB)

    Gan, Lin Ling; Fang, Bo; Zhou, Cheng He [Southwest University, Chongqing (China)

    2010-12-15

    A series of azole-containing piperazine derivatives have been designed and synthesized. The obtained compounds were investigated in vitro for their antibacterial, antifungal and cytotoxic activities. The preliminary results showed that most compounds exhibited moderate to significant antibacterial and antifungal activities in vitro. 1-(4-((4-chlorophenyl) (phenyl)methyl)piperazin-1-yl)-2-(1H-imidazol-1-yl)ethanone and 1-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1- yl)-2-(2-phenyl-1H-imidazol-1-yl)ethanone gave remarkable and broad-spectrum antimicrobial efficacy against all tested strains with MIC values ranging from 3.1 to 25 μg/mL, and exhibited comparable activities to the standard drugs chloramphenicol and fluconazole in clinic. Moreover, 2-((4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)methyl)- 1H-benzo[d]imidazole was found to be the most effective in vitro against the PC-3 cell line, reaching growth inhibition values (36.4, 60.1 and 76.5%) for each tested concentration: 25 μM, 50 μM and 100 μM in dose-dependent manner. The results also showed that the azole ring had noticeable effect on their antimicrobial and cytotoxic activities, and imidazole and benzimidazole moiety were much more favourable to biological activity than 1,2,4-triazole.

  11. Chemical Composition, Antifungal and Insecticidal Activities of Hedychium Essential Oils

    Directory of Open Access Journals (Sweden)

    Kanniah Rajasekaran

    2013-04-01

    Full Text Available The antimicrobial properties of essential oils have been documented, and their use as “biocides” is gaining popularity. The aims of this study were to analyze the chemical composition and assess the biological activities of Hedychium essential oils. Oils from 19 Hedychium species and cultivars were analyzed by gas chromatography (GC and gas chromatography-mass spectrometry (GC-MS techniques. The antifungal and insecticidal activities of these oils were tested against Colletotrichum acutatum, C. fragariae, and C. gloeosporioides, and three insects, the azalea lace bug (Stephanitis pyrioides, the yellow fever mosquito (Aedes aegypti, and the red imported fire ant (Solenopsis invicta. Hedychium oils were rich in monoterpenes and sesquiterpenes, especially 1,8-cineole (0.1%–42%, linalool (<0.1%–56%, a-pinene (3%–17%, b-pinene (4%–31%, and (E-nerolidol (0.1%–20%. Hedychium oils had no antifungal effect on C. gloeosporioides, C. fragariae, and C. acutatum, but most Hedychium oils effectively killed azalea lace bugs. The oils also show promise as an adult mosquito repellent, but they would make rather poor larvicides or adulticides for mosquito control. Hedychium oils acted either as a fire ant repellent or attractant, depending on plant genotype and oil concentration.

  12. Screening of Azotobacter isolates for PGP properties and antifungal activity

    Directory of Open Access Journals (Sweden)

    Bjelić Dragana Đ.

    2015-01-01

    Full Text Available Аmong 50 bacterial isolates obtained from maize rhizospherе, 13 isolates belonged to the genus Azotobacter. Isolates were biochemically characterized and estimated for pH and halo tolerance ability and antibiotic resistance. According to characterization, the six representative isolates were selected and further screened in vitro for plant growth promoting properties: production of indole-3-acetic acid (IAA, siderophores, hydrogen cyanide (HCN, exopolysaccharides, phosphate solubilization and antifungal activity (vs. Helminthosporium sp., Macrophomina sp., Fusarium sp.. Beside HCN production, PGP properties were detected for all isolates except Azt7. All isolates produced IAA in the medium without L-tryptophan and the amount of produced IAA increased with concentration of precursor in medium. The highest amount of IAA was produced by isolates Azt4 (37.69 and 45.86 μg ml-1 and Azt5 (29.44 and 50.38 μg ml-1 in the medium with addition of L-tryptophan (2.5 and 5 mM. The isolates showed the highest antifungal activity against Helminthosporium sp. and the smallest antagonistic effect on Macrophomina sp. Radial Growth Inhibition (RGI obtained by the confrontation of isolates with tested phytopathogenic fungi, ranged from 10 to 48%. [Projekat Ministarstva nauke Republike Srbije, br. TR 31073

  13. Methylxanthine Inhibit Fungal Chitinases and Exhibit Antifungal Activity

    Science.gov (United States)

    Tsirilakis, Kalliope; Kim, Christy; Vicencio, Alfin G.; Andrade, Christopher; Casadevall, Arturo; Goldman, David L.

    2015-01-01

    Chitinases are necessary for fungal cell wall remodeling and cell replication. Methylxanthines have been shown to competitively inhibit family 18 chitinases in vitro. We sought to determine the effects of methylxanthines on fungal chitinases. Fungi demonstrated variable chitinase activity and incubation with methylxanthines (0.5–10 mM) resulted in a dose-dependent decrease in this activity. All fungi tested, except for Candida spp., demonstrated growth inhibition in the presence of methylxanthines at a concentration of 10 mM. India ink staining demonstrated impaired budding and decreased cell size for methylxanthine-treated Cryptococcus neoformans. C. neoformans and Aspergillus fumigatus treated with pentoxifylline also exhibited abnormal cell morphology. In addition, pentoxifylline-treated C. neoformans exhibited increased susceptibility to calcofluor and a leaky melanin phenotype consistent with defective cell wall function. Our data suggest that a variety of fungi express chitinases and that methylxanthines have antifungal properties related to their inhibition of fungal chitinases. Our results highlight the potential utility of targeting chitinases in the development of novel antifungal therapies. PMID:21968902

  14. Secretive Expression of Insect Antifungal Peptide-Encoded Genes in Pichia pastoris and Activity Assay of the Products

    Institute of Scientific and Technical Information of China (English)

    SANG Yan-xia; DENG Xiao-juan; YANG Wan-ying; WANG Wen-xian; WEN Shuo-yang; LIU Wen-quan; HUANG Ya-dong; CAO Yang

    2007-01-01

    The antifungal peptides, drosomycin (Drs) and its isoform drosomycin-like C (Drs-lC) from Drosophila melanogaster and Thanatin from Podisus maculiventris, have potent activity with broad spectrum against filamentous fungi. Secretive expression of these genes in yeasts makes it possible to utilize the supernatants of yeast culture as protective reagents on fruit, vegetable, food and other agricultural products. So the study of effective secretion by yeast expression system is of great importance. Three genes, Drs, Drs-lC, and Thanatin, were cloned into pPICZαA and the recombinant vectors,pPICZαA-Drs, pPICZαA-Drs-IC, and pPICZαA-Thanatin were transformed into Pichia pastoris by the electric transfer method. The recombinant P. pastoris, which was screened by phenotype selection and PCR amplification, wasinduced to express antifungal peptide by methanol. The expressive products of the three recombinants showed antifungal activity against 5 out of 6 test fungi strains, and the products of Thanatin also had strong activity against the tested bacteria. The three antifungal peptide genes, Drs, Drs-lC, and Thanatin, were constructed into yeast P. pastoris. The expressed peptides were successfully secreted into the culture medium and exhibited potent activities against the test strains.

  15. Antifungal Activity of Eugenol against Penicillium, Aspergillus, and Fusarium Species.

    Science.gov (United States)

    Campaniello, Daniela; Corbo, Maria Rosaria; Sinigaglia, Milena

    2010-06-01

    The antifungal activity of eugenol in a model system against aspergilli (Aspergillus niger, Aspergillus terreus, and Emericella nidulans), penicilli (Penicillium expansum, Penicillium glabrum, and Penicillium italicum), and fusaria (Fusarium oxysporum and Fusarium avenaceum) was investigated. Minimum detection time (time to attain a colony diameter of 1 cm) and the kinetic parameters were evaluated. The effectiveness of the active compound seemed to be strain or genus dependent; 100 mg/liter represented a critical value for P. expansum, P. glabrum, P. italicum, A. niger, and E. nidulans because a further increase of eugenol resulted in fungistatic activity. The radial growth of A. terreus and F. avenaceum was inhibited at 140 mg/liter, and growth of F. oxysporum was completely inhibited at 150 mg/liter.

  16. The chitin-binding capability of Cy-AMP1 from cycad is essential to antifungal activity.

    Science.gov (United States)

    Yokoyama, Seiya; Iida, Yuto; Kawasaki, Yousuke; Minami, Yuji; Watanabe, Keiichi; Yagi, Fumio

    2009-07-01

    Antimicrobial peptides are important components of the host innate immune responses by exerting broad-spectrum microbicidal activity against pathogenic microbes. Cy-AMP1 found in the cycad (Cycas revoluta) seeds has chitin-binding ability, and the chitin-binding domain was conserved in knottin-type and hevein-type antimicrobial peptides. The recombinant Cy-AMP1 was expressed in Escherichia coli and purified to study the role of chitin-binding domain. The mutants of Cy-AMP1 lost chitin-binding ability completely, and its antifungal activity was markedly decreased in comparison with native Cy-AMP1. However, the antimicrobial activities of the mutant peptides are nearly identical to that of native one. It was suggested that the chitin-binding domain plays an essential role in antifungal, but not antimicrobial, activity of Cy-AMP1.

  17. Synthesis, Structure-Activity Relationships (SAR and in Silico Studies of Coumarin Derivatives with Antifungal Activity

    Directory of Open Access Journals (Sweden)

    José M. Barbosa-Filho

    2013-01-01

    Full Text Available The increased incidence of opportunistic fungal infections, associated with greater resistance to the antifungal drugs currently in use has highlighted the need for new solutions. In this study twenty four coumarin derivatives were screened in vitro for antifungal activity against strains of Aspergillus. Some of the compounds exhibited significant antifungal activity with MICs values ranging between 16 and 32 µg/mL. The structure-activity relationships (SAR study demonstrated that O-substitutions are essential for antifungal activity. It also showed that the presence of a short aliphatic chain and/or electron withdrawing groups (NO2 and/or acetate favor activity. These findings were confirmed using density functional theory (DFT, when calculating the LUMO density. In Principal Component Analysis (PCA, two significant principal components (PCs explained more than 60% of the total variance. The best Partial Least Squares Regression (PLS model showed an r2 of 0.86 and q2cv of 0.64 corroborating the SAR observations as well as demonstrating a greater probe N1 interaction for active compounds. Descriptors generated by TIP correlogram demonstrated the importance of the molecular shape for antifungal activity.

  18. Synthesis of quarternary ammonium salts with dithiocarbamate moiety and their antifungal activities against Helminthosporium oryzae

    Indian Academy of Sciences (India)

    Mandeep Singh; Anita Garg; Anjali Sidhu; Vineet Kumar

    2013-05-01

    Quaternary ammonium salts containing dithiocarbamate moiety were synthesized and evaluated for their antifungal activities against Helminthosporium oryzae. All the synthesized compounds showed moderate to promising fungitoxicity against the test. Some of the synthesized compounds inflicted antifungal activity greater than the standard fungicide.

  19. Antifungal compounds from turmeric and nutmeg with activity against plant pathogens

    Science.gov (United States)

    The antifungal activity of twenty-two common spices was evaluated against plant pathogens using direct-bioautography coupled Colletotrichum bioassays. Turmeric, nutmeg, ginger, clove, oregano, cinnamon, anise, fennel, basil, black cumin, and black pepper showed antifungal activity against the plant ...

  20. [Research on antifungal activity of flowers and leaves of Inula viscosa (Asteraceae)].

    Science.gov (United States)

    Cafarchia, C; De Laurentis, N; Milillo, M A; Losacco, V; Puccini, V

    1999-12-01

    The authors carried out a preliminary screening about the in vitro antifungal activity of some extracts of flowers and leaves of Inula viscosa obtained with different solvents. All extracts showed antifungal activity against dermatophytes and Candida species. The best results were obtained with Inula viscosa flowers extracts. These results may be ascribed to the different flavonoids and different flavonoid concentrations in our samples.

  1. Antifungal activities of the leaves of three Pistacia species grown in Turkey.

    Science.gov (United States)

    Kordali, S; Cakir, A; Zengin, H; Duru, M E

    2003-02-01

    The crude extracts obtained from the leaves of Pistacia vera, Pistacia terebinthus and Pistacia lentiscus were tested for antifungal activities against three pathogenic agricultural fungi, Phythium ultimum, Rhizoctania solani and Fusarium sambucinum. The extracts significantly inhibited the growth of P. ultimum and R. solani. However, the antifungal activity was not observed against F. sambucinum.

  2. 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.

  3. 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.

  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. Antifungal activity of essential oils from leaves and flowers of Inula viscosa (Asteraceae) by Apulian region.

    Science.gov (United States)

    Cafarchia, C; De Laurentis, N; Milillo, M A; Losacco, V; Puccini, V

    2002-12-01

    Some essential oils from several plants (Artemisia verlotorum, Lavandula augustifolia, Ocimum gratissimum) have proved to have acaricidal, antifungal and antibacterial activity. Inula viscosa Ait. (Asteraceae), a plant growing spontaneously in the Mediterranean area, is currently used by popular medicine for its therapeutic effects. Flavonoids, azulenes, sesquiterpenes, and essential oils have been isolated and identified from its leaves. This paper reports the results of the composition and antifungal activity in vitro against dermatophytes and Candida spp. of the four essential oils obtained by steam distillation of the leaves, flowers, whole plant and whole plants without flower extracts of I. viscosa. All the extracts proved to have a significant antifungal activity against dermatophytes even at low concentrations (0.01 mg/ml). The leaf extracts exhibited the greatest antifungal efficacy. The high concentration of the sesquiterpene (carboxyeudesmadiene), occurring in the leaf extracts, may explain its greater antifungal activity.

  6. 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

  7. 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

  8. 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.

  9. Antifungal activity of amphotericin B conjugated to carbon nanotubes.

    Science.gov (United States)

    Benincasa, Monica; Pacor, Sabrina; Wu, Wei; Prato, Maurizio; Bianco, Alberto; Gennaro, Renato

    2011-01-25

    Amphotericin B (AMB) has long been considered the most effective drug in the treatment of serious invasive fungal infections. There are, however, major limitations to its use, due to several adverse effects, including acute infusional reactions and, most relevant, a dose-dependent nephrotoxicity. At least some of these effects are attributed to the aggregation of AMB as a result of its poor water solubility. To overcome this problem, reformulated versions of the drug have been developed, including a micellar dispersion of AMB with sodium deoxycholate (AMBD), its encapsulation into liposomes, or its incorporation into lipidic complexes. The development of nanobiotechnologies provides novel potential drug delivery systems that make use of nanomaterials such as functionalized carbon nanotubes (f-CNTs), which are emerging as an innovative and efficient tool for the transport and cellular translocation of therapeutic molecules. In this study, we prepared two conjugates between f-CNTs and AMB. The antifungal activity of these conjugates was tested against a collection of reference and clinical fungal strains, in comparison to that of AMB alone or AMBD. Measured minimum inhibition concentration (MIC) values for f-CNT-AMB conjugates were either comparable to or better than those displayed by AMB and AMBD. Furthermore, AMBD-resistant Candida strains were found to be susceptible to f-CNT-AMB 1. Additional studies, aimed at understanding the mechanism of action of the conjugates, suggest a nonlytic mechanism, since the compounds show a major permeabilizing effect on the tested fungal strains only after extended incubation. Interestingly, the f-CNT-AMB 1 does not show any significant toxic effect on Jurkat cells at antifungal concentrations.

  10. Eupatorium Capillifolium Essential Oil: Chemical Composition, Antifungal Activity, and Insecticidal Activity

    Science.gov (United States)

    2010-01-01

    Matrix, one-dimensional protocols on silica gel TLC plates along with Colletotrichum spp. as the test organisms were used to identify the antifungal...activity of the antirheumatic herbal drug, gravel root (Eupatorium purpureum): Further biological activities and constituents. Phytotherapy Research

  11. Antifungal activities of three different Lactobacillus species and their production of antifungal carboxylic acids in wheat sourdough.

    Science.gov (United States)

    Axel, Claudia; Brosnan, Brid; Zannini, Emanuele; Peyer, Lorenzo C; Furey, Ambrose; Coffey, Aidan; Arendt, Elke K

    2016-02-01

    This study was undertaken to assess the antifungal performance of three different Lactobacillus species.Experiments were conducted in vitro and in situ to extend the shelf life of wheat bread. Standard sourdough analyses were performed characterising acidity and carbohydrate levels. Overall, the strains showed good inhibition in vitro against the indicator mould Fusarium culmorum TMW4.2043. Sourdough bread fermented with Lactobacillus amylovorus DSM19280 performed best in the in situ shelf life experiment. An average shelf life extension of six more mould-free days was reached when compared to the non-acidified control bread. A range of antifungal-active acids like 3-phenyllactic acid, 4-hydroxyphenyllactic acid and 2-hydroxyisocaproic acid in quantities between 0.1 and 360 mg/kg were present in the freeze-dried sourdoughs. Their concentration differed greatly amongst the species.However, a higher concentration of these compounds could not completely justify the growth inhibition of environmental moulds. In particular, although Lb. reuteri R29 produced the highest total concentration of these active compounds in the sourdough, its addition to bread did not result in a longest shelf life. Nevertheless, when the artificial compounds were spiked into a chemically acidified dough, it succeeded in a longer shelf life (+25 %) than achieved only by acidifying the dough. This provides evidence of their contribution to the antifungal activity and their synergy in concentration levels far below their single minimal inhibition concentrations under acidic conditions.

  12. 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

  13. 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.

  14. IN VITRO ANTIFUNGAL ACTIVITY OF ESSENTIAL OILS ON GROWTH OF PHYTOPATHOGENIC FUNGI

    Directory of Open Access Journals (Sweden)

    Jasenka Ćosić

    2010-12-01

    Full Text Available Eleven essential oils (clove, rosemary, cinnamon leaf, sage, scots pine, neroli, peppermint, aniseed, caraway, lavander, common thyme were tested for in vitro antifungal activity on twelve plant pathogenic fungi (Fusarium graminearum, F. verticillioides, F. subglutinans, F. oxysporum, F. avenaceum, Diaporthe helianthi, Diaporthe phaseolorum var. caulivora, Phomopsis longicolla, P. viticola, Helminthosporium sativum, Colletotrichum coccodes, Thanatephorus cucumeris. The results indicated that all oils except scots pine and neroli had antifungal activity against some or all tested fungi. The best antifungal activity had common thyme, cinnamon leaf, clove and aniseed oils. When compared to control, scots pine, neroli and sage oils stimulated mycelium growth of some investigated fungi.

  15. ANTIFUNGAL ACTIVITY OF NEEM (Azadirachta indica: MELIACEAE EXTRACTS AGAINST DERMATOPHYTES

    Directory of Open Access Journals (Sweden)

    Daniel Iván OSPINA SALAZAR

    2015-07-01

    Full Text Available In order to assess the antifungal activity of methanolic extracts from neem tree (Azadirachta indica A. Juss., several bioassays were conducted following M38-A2 broth microdilution method on 14 isolates of the dermatophytes Trichophyton mentagrophytes, Trichophyton rubrum, Microsporum canis and Epidermophyton floccosum. Neem extracts were obtained through methanol-hexane partitioning of mature green leaves and seed oil. Furthermore, high performance liquid chromatography (HPLC analyses were carried out to relate the chemical profile with their content of terpenoids, of widely known antifungal activity. The antimycotic Terbinafine served as a positive control. Results showed that there was total growth inhibition of the dermatophytes isolates at minimal inhibitory concentrations (MIC between 50 μg/mL and 200 μg/mL for leaves extract, and between 625 μg/mL and 2500 μg/mL for seed oil extract. The MIC of positive control (Terbinafine ranged between 0.0019 μg/mL and 0.0313 μg/mL. Both neem leaves and seed oil methanol extracts exhibited different chromatographic profiles by HPLC, which could explain the differences observed in their antifungal activity. This analysis revealed the possible presence of terpenoids in both extracts, which are known to have biological activity. The results of this research are a new report on the therapeutic potential of neem to the control of dermatophytosis. Actividad antifúngica de extractos de neem (Azadirachta indica: Meliaceae sobre hongos dermatofitosSe determinó la actividad antifúngica de extractos metanólicos de la especie Azadirachta indica A. Juss. (Meliaceae, conocida comúnmente como neem, empleando el método de microdilución en caldo M38-A2 de referencia para hongos filamentosos y dermatofitos. Se evaluaron 14 aislamientos de los dermatofitos Trichophyton mentagrophytes, Trichophyton rubrum, Microsporum canis y Epidermophyton floccosum. Los extractos de neem fueron obtenidos mediante partici

  16. 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.

  17. Vv-AMP1, a ripening induced peptide from Vitis vinifera shows strong antifungal activity

    Directory of Open Access Journals (Sweden)

    Vivier Melané A

    2008-07-01

    Full Text Available Abstract Background Latest research shows that small antimicrobial peptides play a role in the innate defense system of plants. These peptides typically contribute to preformed defense by developing protective barriers around germinating seeds or between different tissue layers within plant organs. The encoding genes could also be upregulated by abiotic and biotic stimuli during active defense processes. The peptides display a broad spectrum of antimicrobial activities. Their potent anti-pathogenic characteristics have ensured that they are promising targets in the medical and agricultural biotechnology sectors. Results A berry specific cDNA sequence designated Vv-AMP1, Vitis vinifera antimicrobial peptide 1, was isolated from Vitis vinifera. Vv-AMP1 encodes for a 77 amino acid peptide that shows sequence homology to the family of plant defensins. Vv-AMP1 is expressed in a tissue specific, developmentally regulated manner, being only expressed in berry tissue at the onset of berry ripening and onwards. Treatment of leaf and berry tissue with biotic or abiotic factors did not lead to increased expression of Vv-AMP1 under the conditions tested. The predicted signal peptide of Vv-AMP1, fused to the green fluorescent protein (GFP, showed that the signal peptide allowed accumulation of its product in the apoplast. Vv-AMP1 peptide, produced in Escherichia coli, had a molecular mass of 5.495 kDa as determined by mass spectrometry. Recombinant Vv-AMP1 was extremely heat-stable and showed strong antifungal activity against a broad spectrum of plant pathogenic fungi, with very high levels of activity against the wilting disease causing pathogens Fusarium oxysporum and Verticillium dahliae. The Vv-AMP1 peptide did not induce morphological changes on the treated fungal hyphae, but instead strongly inhibited hyphal elongation. A propidium iodide uptake assay suggested that the inhibitory activity of Vv-AMP1 might be associated with altering the membrane

  18. Eupatorium capillifolium essential oil: chemical composition antifungal activity and insecticidal activity

    Science.gov (United States)

    Natural plant extracts often contain compounds that are useful in pest management applications. The essential oil of Eupatorium capillifolium (dog-fennel) was investigated for antifungal and insecticidal activities. Essential oil obtained by hydrodistillation of aerial parts was analyzed by gas chro...

  19. 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.

  20. Antifungal activity of some marine organisms from India, against food spoilage Aspergillus strains

    Digital Repository Service at National Institute of Oceanography (India)

    Bhosale, S.H.; Jagtap, T.G.; Naik, C.G.

    ), Sinularia leptocladus (soft coral), Elysia grandifolia (Mollusks), Gorgonian sp. 2 and Haliclona sp. exhibited significant (inhibition zone of 3-5 mm) antifungal activity against one or the other strains. However, extracts of A. ilicifolius, Amphiroa sp...

  1. Comparative study of the recommended methodologies by CLSI and EUCAST for activity evaluation antifungal

    OpenAIRE

    2009-01-01

    The international organizations CLSI and EUCAST developed reference methodologies for activity evaluation antifungal. The aim of this work was to compare the recommended methodologies by the CLSI and EUCAST in the antifungal activity evaluation of crude extracts of Azadirachta indica and green propolis. The results showed that the MIC values determined by the EUCAST methodology were smaller than that determined by the CLSI. Nevertheless, both methodologies were satisfactory to detect and eval...

  2. Antifungal activity and gene expression of lipopeptide antibiotics in strains of genus Bacillus

    OpenAIRE

    Grabova A. Yu.; Dragovoz I. V.; Zelena L. B.; Tkachuk D. M.; Avdeeva L. V.

    2016-01-01

    Aim. To research the antifungal activity and gene expression of lipopeptide antibiotics in strains of genus Bacillus. Methods. Deferred antagonism method, PCR, qRT-PCR, MALDI-TOF mass spectrometry. Results. It was revealed that Bacillus sp. strains C6 and Lg37s out of five tested strains had the highest antifungal activity. Based on the molecular genetic methods, it was shown that the expression of genes of lipopeptide antibiotics, related to the fengycin family, occurred in all these strains...

  3. Antifungal activity of 4-substituted crotonic acid esters.

    Science.gov (United States)

    Gershon, H; Shanks, L; Gawiak, D E

    1976-08-01

    Twenty-three 4-substituted crotonic acid esters were tested for antifungal activity against Candida albicans, Aspergillus niger, Mucor mucedo, and Trichophyton mentagrophytes. For the analogues of the methyl ester containing substituents in the 4 position, the following order of fungitoxicity was observed: I greater than Br greater than Cl greater than CH3S greater than CH3O greater than F=H. Of the homologues of the esters of the 4-iodo and 4-bromo compounds which included methyl, ethyl, n-propyl, n-butyl, n-pentyl, and n-hexyl, ethyl 4-iodocrotonate was most toxic to the four fungi at pH 7.0 in the presence of 10% beef serum (C. albicans, 18mug/ml, A. niger, 40 mug/ml, M. mucedo, 5 mug/ml, T. mentagrophytes, 4 mug/ml). It is believed that the mechanism of fungitoxicity is due, in part, to a nucleophilic reaction involving SH-containing compounds. This is based on the correlation of fungitoxicity with the order of leaving groups in the nucleophilic reaction and the protection against the toxicity of the test compounds to the fungi by cysteine and glutathione.

  4. 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.

  5. Antifungal activity of two Lactobacillus strains with potential probiotic properties.

    Science.gov (United States)

    Gerbaldo, Gisela A; Barberis, Carla; Pascual, Liliana; Dalcero, Ana; Barberis, Lucila

    2012-07-01

    Aflatoxin (highly toxic and carcinogenic secondary metabolites produced by fungi) contamination is a serious problem worldwide. Modern agriculture and animal production systems need to use high-quality and mycotoxin-free feedstuffs. The use of microorganisms to preserve food has gained importance in recent years due to the demand for reduced use of chemical preservatives by consumers. Lactic acid bacteria are known to produce various antimicrobial compounds that are considered to be important in the biopreservation of food and feed. Lactobacillus rhamnosus L60 and Lactobacillus fermentum L23 are producers of secondary metabolites, such as organic acids, bacteriocins and, in the case of L60, hydrogen peroxide. The antifungal activity of lactobacilli strains was determined by coculture with Aspergillus section Flavi strains by two qualitative and one quantitative methods. Both L23 and L60 completely inhibited the fungal growth of all aflatoxicogenic strains assayed. Aflatoxin B (1) production was reduced 95.7-99.8% with L60 and 27.5-100% with L23. Statistical analysis of the data revealed the influence of L60 and L23 on growth parameters and aflatoxin B (1) production. These results are important given that these aflatoxicogenic fungi are natural contaminants of feed used for animal production, and could be effectively controlled by Lactobacillus L60 and L23 strains with probiotic properties.

  6. 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.

  7. Antifungal activity of mango peel and seed extracts against clinically pathogenic and food spoilage yeasts.

    Science.gov (United States)

    Dorta, E; González, M; Lobo, M G; Laich, F

    2015-11-26

    The antioxidant and antifungal (antiyeast) properties of mango (Mangifera indica) peel and seed by-products were investigated. Nine extracts were obtained using three cultivars and two extraction methods. Significant differences between cultivars and extraction methods were detected in their bioactive compounds and antioxidant activity. The antifungal property was determined using agar diffusion and broth micro-dilution assays against 18 yeast species of the genera Candida, Dekkera, Hanseniaspora, Lodderomyces, Metschnikowia, Pichia, Schizosaccharomyces, Saccharomycodes and Zygosaccharomyces. All mango extracts showed antifungal activity. The minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) values were lower for seed than for peel extracts. MICs and MFCs ranged from values 30 mgGAE/mL, respectively. The multivariate analysis showed a relationship between antifungal activity, the capacity to inhibit lipid peroxidation and total phenol content. These properties were associated with high levels of proanthocyanidins, gallates and gallotannins in the extracts.

  8. Anti-fungal activity of Morinda citrifolia (noni extracts against Candida albicans: An in vitro study

    Directory of Open Access Journals (Sweden)

    K Barani

    2014-01-01

    Full Text Available Aim: The aim of this study was to investigate the anti-fungal activity of Morinda citrifolia fruit extract on Candida albicans. Materials and Methods: Juice extract from M. citrifolia fruit was lyophilized and used in anti-fungal testing. Anti-fungal activity of M. citrifolia fruit extract against C. albicans was tested in vitro at various concentrations. The inhibitory effect of M. citrifolia extract on C. albicans was determined by agar culture and applied broth dilution test. Results: M. citrifolia extract at 1000 μg/ml concentration effectively inhibited the growth of C. albicans (16.6 ± 0.3 compared with the positive control - amphotericin B (20.6 ± 0.6. It was found to be a dose-dependent reaction. Conclusion: M. citrifolia fruit extract had an anti-fungal effect on C. albicans and the inhibitory effect varied with concentration.

  9. 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

  10. 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 ...

  11. Synthesis, antibacterial and antifungal activity of some derivatives of 2-phenyl-chromen-4-one

    Indian Academy of Sciences (India)

    Sayed Alam

    2004-11-01

    Some derivatives of 2-phenyl-chromen-4-one (flavone ring) have been synthesized and tested for antibacterial and antifungal activities along with their chalcone precursors against four human pathogenic bacteria and five plant mould fungi. The structures of the synthesized compounds were elucidated by UV, IR and 1H NMR spectroscopic techniques, and elemental analysis. The antibacterial and antifungal screens of the synthesized compounds were performed in vitro by the filter paper disc diffusion method and the poisoned food technique.

  12. 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...

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

    Science.gov (United States)

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

    2011-10-01

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

  14. 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

  15. Antifungal activity of fluid extract and essential oil from anise fruits (Pimpinella anisum L., Apiaceae).

    Science.gov (United States)

    Kosalec, Ivan; Pepeljnjak, Stjepan; Kustrak, Danica

    2005-12-01

    Antifungal activities of fluid extract and essential oil obtained from anise fruits Pimpinella anisum L. (Apiaceae) were tested in vitro on clinical isolates of seven species of yeasts and four species of dermatophytes. Diffusion method with cylinders and the broth dilution method were used for antifungal activity testing. Anise fluid extract showed antimycotic activity against Candida albicans, C. parapsilosis, C. tropicalis, C. pseudotropicalis and C. krusei with MIC values between 17 and 20% (v/v). No activity was noticed against C. glabrata, and anis fruits extracts showed growth promotion activity on Geotrichum spp. Anise fruits extract inhibited the growth of dermatophyte species (Trichophyton rubrum, T. mentagrophytes, Microsporum canis and M. gypseum) with MIC values between 1.5 and 9.0% (V/V). Anise essential oil showed strong antifungal activity against yeasts with MIC lower than 1.56% (V/V) and dermatophytes with MIC lower than 0.78% (V/V). Significant differences in antifungal activities were found between anise fluid extract and anise essential oil (p<0.01). Anise essential oil exhibited stronger antifungal activities against yeasts and dermatophytes with MIC values between 0.10 and 1.56% (V/V), respectively.

  16. Fumigant antifungal activity of Myrtaceae essential oils and constituents from Leptospermum petersonii against three Aspergillus species.

    Science.gov (United States)

    Kim, Eunae; Park, Il-Kwon

    2012-09-03

    Commercial plant essential oils obtained from 11 Myrtaceae plant species were tested for their fumigant antifungal activity against Aspergillus ochraceus, A. flavus, and A. niger. Essential oils extracted from Leptospermum petersonii at air concentrations of 56 × 10(-3) mg/mL and 28 × 10(-3) mg/mL completely inhibited the growth of the three Aspergillus species. However, at an air concentration of 14 × 10(-3) mg/mL, inhibition rates of L. petersonii essential oils were reduced to 20.2% and 18.8% in the case of A. flavus and A. niger, respectively. The other Myrtaceae essential oils (56 × 10(-3) mg/mL) only weakly inhibited the fungi or had no detectable affect. Gas chromatography-mass spectrometry analysis identified 16 compounds in L. petersonii essential oil. The antifungal activity of the identified compounds was tested individually by using standard or synthesized compounds. Of these, neral and geranial inhibited growth by 100%, at an air concentration of 56 × 10(-3) mg/mL, whereas the activity of citronellol was somewhat lover (80%). The other compounds exhibited only moderate or weak antifungal activity. The antifungal activities of blends of constituents identified in L. petersonii oil indicated that neral and geranial were the major contributors to the fumigant and antifungal activities.

  17. Antioxidant and antifungal activities of two spices of mangrove plant extract

    Institute of Scientific and Technical Information of China (English)

    Somayeh Rastegar; Mohsen Gozari

    2016-01-01

    Objective:To evaluate the antifungal and the radical scavenging capacity related to antioxidant potential of ethanol and water extracts of leaves of Rhizophora mucronata (R. mucronata) and Avicennia marina (A. marina) mangrove plant species against five postharvest pathogenic bacteria. Methods:In vitro assessment of antioxidant and antifungal activities was evaluated in this present study for both aqueous and ethanol extracts prepared from leaves of A. marina and R. mucronata. The antioxidant activities of these mangroves were evaluated by using reducing power and 1,1-diphenyl-2-picrylhydrazyl assays with butylated hydroxytoluene and L-(+)-ascorbic acid as standards. Results:The result showed that the antioxidant activities of all extracts increased with increasing concentration of extracts. However, the ethanol extracts of both species showed the highest antioxidant activities. Antimicrobial tests were then carried out by the disk diffusion method. The ethanol extracts of both species showed antifungal activities on Penicillium purpurogenum, Penicillium chrysogenum, Penicillium notatum, Aspergillus niger, Alternaria alternata and Penicillium italicum. However, none of the water extracts exhibited antifungal activity on the studied fungi. Among all the pathogens, tested Aspergillus flavus was the most resistant fungi. Different concentrations of extracts from A. marina and R. mucronata showed different amounts of control against tested fungal strains. Conclusions:This study indicated that mangrove species has natural antioxidant and antifungal properties.

  18. Antioxidant and antifungal activities of two spices of mangrove plant extract

    Directory of Open Access Journals (Sweden)

    Somayeh Rastegar

    2016-10-01

    Full Text Available Objective: To evaluate the antifungal and the radical scavenging capacity related to antioxidant potential of ethanol and water extracts of leaves of Rhizophora mucronata (R. mucronata and Avicennia marina (A. marina mangrove plant species against five postharvest pathogenic bacteria. Methods: In vitro assessment of antioxidant and antifungal activities was evaluated in this present study for both aqueous and ethanol extracts prepared from leaves of A. marina and R. mucronata. The antioxidant activities of these mangroves were evaluated by using reducing power and 1,1-diphenyl-2-picrylhydrazyl assays with butylated hydroxytoluene and L-(+- ascorbic acid as standards. Results: The result showed that the antioxidant activities of all extracts increased with increasing concentration of extracts. However, the ethanol extracts of both species showed the highest antioxidant activities. Antimicrobial tests were then carried out by the disk diffusion method. The ethanol extracts of both species showed antifungal activities on Penicillium purpurogenum, Penicillium chrysogenum, Penicillium notatum, Aspergillus niger, Alternaria alternata and Penicillium italicum. However, none of the water extracts exhibited antifungal activity on the studied fungi. Among all the pathogens, tested Aspergillus flavus was the most resistant fungi. Different concentrations of extracts from A. marina and R. mucronata showed different amounts of control against tested fungal strains. Conclusions: This study indicated that mangrove species has natural antioxidant and antifungal properties.

  19. Correlation between the lipophilicity and antifungal activity of some benzoxazole derivatives

    Directory of Open Access Journals (Sweden)

    Podunavac-Kuzmanović Sanja O.

    2010-01-01

    Full Text Available In the present work, a quantitative relationship between the lipophilicity and antifungal activity of some benzoxazole derivatives against Candida albicans was investigated by using QSAR (quantitative structure-activity relationship analyses. The descriptors which describe numerically the lipophilicity, logP, were calculated using Chem-Office Software version 7.0. The linear correlation between the minimal inhibitory concentration (log1/cMIC and lipophilicity descriptors was investigated. The best QSAR model predicting the antifungal activity of the investigated series of benzoxazole was developed. The results are discussed on the basis of statistical data. High agreement between theoretical and experimental inhibitory values was obtained. The results of this study indicate that the lipophilicity parameter has a significant effect on antifungal activity of this class of compounds, which can be very useful in the design of new biologically active molecules.

  20. Preliminary phytochemical analysis, antibacterial, antifungal and anticandidal activities of successive extracts of Crossandra infundibuliformis

    Institute of Scientific and Technical Information of China (English)

    MadhumithaG; SaralAM

    2011-01-01

    Objective:To investigate the phytochemical, antibacterial, antifungal and anticandidal activity of successive extracts of Crossandra infundibuliformis (Acanthaceae) leaves. Methods:Preliminary screening on the presence of alkaloids, saponins, phytosterols, phenolic compounds, flavanoids, tannins, carbohydrates, terpenoids, oils and fats were carried out by phytochemical analysis. The antibacterial, antifungal and anticandidal activities were done by agar well diffusion technique. Results:The successive extracts have an array of chemical constituents and the MIC values of antibacterial activity ranges from 0.007 8 to 0.015 0μg/mL. In case of antifungal and anticandidal activities the MIC values were between 0.125 and 0.250μg/mL. Conclusions:These findings demonstrate that the leaf extracts of C. infundibuliformis presents excellent antimicrobial activities and thus have great potential as a source for natural health care products.

  1. 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.

  2. 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

  3. 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

  4. Interaction of gelatin with polyenes modulates antifungal activity and biocompatibility of electrospun fiber mats.

    Science.gov (United States)

    Lakshminarayanan, Rajamani; Sridhar, Radhakrishnan; Loh, Xian Jun; Nandhakumar, Muruganantham; Barathi, Veluchamy Amutha; Kalaipriya, Madhaiyan; Kwan, Jia Lin; Liu, Shou Ping; Beuerman, Roger Wilmer; Ramakrishna, Seeram

    2014-01-01

    Topical application of antifungals does not have predictable or well-controlled release characteristics and requires reapplication to achieve therapeutic local concentration in a reasonable time period. In this article, the efficacy of five different US Food and Drug Administration-approved antifungal-loaded (amphotericin B, natamycin, terbinafine, fluconazole, and itraconazole) electrospun gelatin fiber mats were compared. Morphological studies show that incorporation of polyenes resulted in a two-fold increase in fiber diameter and the mats inhibit the growth of yeasts and filamentous fungal pathogens. Terbinafine-loaded mats were effective against three filamentous fungal species. Among the two azole antifungals compared, the itraconazole-loaded mat was potent against Aspergillus strains. However, activity loss was observed for fluconazole-loaded mats against all of the test organisms. The polyene-loaded mats displayed rapid candidacidal activities as well. Biophysical and rheological measurements indicate strong interactions between polyene antifungals and gelatin matrix. As a result, the polyenes stabilized the triple helical conformation of gelatin and the presence of gelatin decreased the hemolytic activity of polyenes. The polyene-loaded fiber mats were noncytotoxic to primary human corneal and sclera fibroblasts. The reduction of toxicity with complete retention of activity of the polyene antifungal-loaded gelatin fiber mats can provide new opportunities in the management of superficial skin infections.

  5. 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.

  6. The antifungal activity of corona treated polyamide and polyester fabrics loaded with silver nanoparticles

    Science.gov (United States)

    Saponjic, Z.; Ilic, V.; Vodnik, V.; Mihailovic, D.; Jovancic, P.; Nedeljkovic, J.; Radetic, M.

    2008-07-01

    This study is aimed to highlight the possibility of using the corona treatment for fiber surface activation that can facilitate the loading of silver nanoparticles from colloids onto the polyester and polyamide fabrics and thus enhance their antifungal activity against Candida albicans. Additionally, the laundering durability of achieved effects was studied. Corona activated polyamide and polyester fabrics loaded with silver nanoparticles showed better antifungal properties compared to untreated fabrics. The positive effect of corona treatment became even more prominent after 5 washing cycles, especially for polyester fabrics.

  7. Antifungal activity of some metabolites of higher fungi (Basidiomycetes - an overview

    Directory of Open Access Journals (Sweden)

    Teresa Florianowicz

    2014-01-01

    Full Text Available A series of compounds of different chemical structures showing antifungal activity were isolated from higher fungi (Basidiomycetes fruit bodies. Among the microflora against which the examined metabolites showed effective activity, there are pathogenic organisms for people as well as for animals: Candida albicans, Candida tropicalis, Rhodotorula rubra, Aspergillus fumigatus and pathogens attacking plants: Penicillium chrysogenum, Botrytis cinerea, Alternaria solani, Fusarium culmorum, Trichoderma lignorum and Verticillium dahlae. Searching for fungal metabolites having antifungal activity creates possibilities of using them against a range of fungal pathogens of clinical, agronomic and environmental significance.

  8. 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.

  9. Natural products as sources of new fungicides (III): Antifungal activity of 2,4-dihydroxy-5-methylacetophenone derivatives.

    Science.gov (United States)

    Shi, Wei; Dan, Wen-Jia; Tang, Jiang-Jiang; Zhang, Yan; Nandinsuren, Tseden; Zhang, An-Ling; Gao, Jin-Ming

    2016-05-01

    A series of new 2,4-dihydroxy-5-methylacetophenone 2 derivatives were synthesized, and characterized by (1)H, (13)C NMR and ESI-MS. Their antifungal activities were evaluated in vitro against five important plant fungal pathogens including Cytospora sp., Glomerella cingulate, Pyricularia oryzaecar, Botrytis cinerea and Alternaria solani by the mycelial growth inhibitory rate assay. Compounds 2b-d, 2g and 2h displayed a broad-spectrum activity. The logP value of these active compounds is ranging from 1.71 to 2.54. Especially, isopropyl ketone 2g (logP 2.27) was found to be the most active to the tested organisms with IC50 values of 17.28-32.32 μg/mL. The results suggest that compound 2g might be a promising candidate in the development of new agrochemical antifungal agents. Preliminary structure-activity relationship (SAR) studies of the acetophenone derivatives are also discussed.

  10. Antifungal Activity of Two Root Canal Sealers against Different Strains of Candida

    Science.gov (United States)

    Jafari, Farnaz; Jafari, Sanaz; Samadi Kafil, Hossein; Momeni, Tahereh; Jamloo, Helen

    2017-01-01

    Introduction: Microorganisms and microbial products are the main etiologic factors in pulp and periapical diseases. The present study aimed to compare the antifungal activity of two different sealers, AH-26 and MTA Fillapex against three strains of Candida, 24, 48, 72 h and 7 days after mixing. Methods and Materials: The microorganisms used in this study were Candidia albicans (ATCC 10231), Candidia glabrata (ATCC 90030) and Candidia krusei (DSM 70079). This test was based on growth of microorganisms and turbidity measurement technique using a spectrophotometer. The direct contact test was conducted by direct and indirect methods. Multiple comparisons were carried out using analysis of variances (ANOVA) with repeated measures followed by Tukey’s tests. Results: The antifungal activity of both sealers was similar in the indirect method. The antifungal activity of both sealers in the direct method was similar against Candida albicans and higher for AH-26 sealer against Candida krusei and Candida glabrata. Conclusion: The total antifungal effect of MTA Fillapex sealer was significantly less than AH-26 sealer in direct method. The antifungal effect of both sealers was similar in indirect method. PMID:28179934

  11. Chemical composition of essential oils of Thymus and Mentha species and their antifungal activities.

    Science.gov (United States)

    Soković, Marina D; Vukojević, Jelena; Marin, Petar D; Brkić, Dejan D; Vajs, Vlatka; van Griensven, Leo J L D

    2009-01-07

    The potential antifungal effects of Thymus vulgaris L., Thymus tosevii L., Mentha spicata L., and Mentha piperita L. (Labiatae) essential oils and their components against 17 micromycetal food poisoning, plant, animal and human pathogens are presented. The essential oils were obtained by hydrodestillation of dried plant material. Their composition was determined by GC-MS. Identification of individual constituents was made by comparison with analytical standards, and by computer matching mass spectral data with those of the Wiley/NBS Library of Mass Spectra. MIC's and MFC's of the oils and their components were determined by dilution assays. Thymol (48.9%) and p-cymene (19.0%) were the main components of T. vulgaris, while carvacrol (12.8%), a-terpinyl acetate (12.3%), cis-myrtanol (11.2%) and thymol (10.4%) were dominant in T. tosevii. Both Thymus species showed very strong antifungal activities. In M. piperita oil menthol (37.4%), menthyl acetate (17.4%) and menthone (12.7%) were the main components, whereas those of M. spicata oil were carvone (69.5%) and menthone (21.9%). Mentha sp. showed strong antifungal activities, however lower than Thymus sp. The commercial fungicide, bifonazole, used as a control, had much lower antifungal activity than the oils and components investigated. It is concluded that essential oils of Thymus and Mentha species possess great antifungal potential and could be used as natural preservatives and fungicides.

  12. Antifungal activity of essential oil from fruits of Indian Cuminum cyminum.

    Science.gov (United States)

    Romagnoli, Carlo; Andreotti, Elisa; Maietti, Silvia; Mahendra, Rai; Mares, Donatella

    2010-07-01

    The essential oil of fruits of Cuminum cyminum L. (Apiaceae), from India, was analyzed by GC and GC-MS, and its antifungal activity was tested on dermatophytes and phytopathogens, fungi, yeasts and some new Aspergilli. The most abundant components were cumin aldehyde, pinenes, and p-cymene, and a fraction of oxygenate compounds such as alcohol and epoxides. Because of the large amount of the highly volatile components in the cumin extract, we used a modified recent technique to evaluate the antifungal activity only of the volatile parts at doses from 5 to 20 microL of pure essential oil. Antifungal testing showed that Cuminum cyminum is active in general on all fungi but in particular on the dermatophytes, where Trichophyton rubrum was the most inhibited fungus also at the lowest dose of 5 microL. Less sensitive to treatment were the phytopathogens.

  13. 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.

  14. Design, synthesis, and antifungal activities of novel triazole derivatives containing the benzyl group

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    Xu K

    2015-03-01

    Full Text Available Kehan Xu,1,* Lei Huang,1,* Zheng Xu,2 Yanwei Wang,1,3 Guojing Bai,1 Qiuye Wu,1 Xiaoyan Wang,1 Shichong Yu,1 Yuanying Jiang1 1School of Pharmacy, Second Military Medical University, Shanghai, 2Shanghai Changzheng Hospital, Second Military Medical University, Shanghai, 3Number 422 Hospital of PLA, Zhanjiang, People’s Republic of China *These authors contributed equally to this work Abstract: In previous studies undertaken by our group, a series of 1-(1H-1,2,4-triazole-1-yl-2-(2,4-difluorophenyl-3-substituted-2-propanols (1a–r, which were analogs of fluconazole, was designed and synthesized by click chemistry. In the study reported here, the in vitro antifungal activities of all the target compounds were evaluated against eight human pathogenic fungi. Compounds 1a, 1q, and 1r showed the more antifungal activity than the others. Keywords: triazole, synthesis, antifungal activity, CYP51

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

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    F. Nouri

    2016-07-01

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

  16. Antifungal Activity of Essential Oils from Some Medicinal Plants of Iran against Alternaria alternate

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    I. Hadizadeh

    2009-01-01

    Full Text Available Problem statement: Increasing public concern over the level of pesticide residues in food especially fresh produce has built up adequate pressure for scientists to look for less hazardous and environmentally safer compounds for controlling post harvest diseases. Essential oils as registered food grade materials have the potential to be applied as alternative anti-fungal treatments for fresh fruits and vegetables. Approach: We present in this study, the identification of the essential oils with antifungal activity from some medicinal plants of Iran (nettle (Urtica dioica L., thyme (Thymus vulgaris L., eucalyptus (Eucalyptus spp., Rue (Ruta graveolens L. and common yarrow (Achillea millefolium L., and their potential application as "generally regarded as safe" antifungal compounds against Alternaria alternate on tomato as a model pathosystem. Results: Both the nettle and the thyme oils exhibited antifungal activity against A. alternata. The thyme oil exhibited a lower degree of inhibition 68.5 and 74.8% at 1500 and 2000 ppm, respectively. Spore germination and germ tube elongation of the pathogens in potato dextrose broth was strongly reduced in the presence of 1500 ppm of the nettle oil. The same concentration of this oil reduced the percentage of decayed tomatoes. The experiments on reducing the development of natural tomato rot gave similar results. Conclusions: Application of essential oils for postharvest disease control of fresh produce, as a novel emerging alternative to hazardous anti-fungal treatments will allow a safer and environmentally more acceptable management of postharvest diseases.

  17. Synthesis and antifungal activities of glycosylated derivatives of the cyclic peptide fungicide caspofungin.

    Science.gov (United States)

    Guo, Junxiang; Hu, Honggang; Zhao, Qingjie; Wang, Ting; Zou, Yan; Yu, Shichong; Wu, Qiuye; Guo, Zhongwu

    2012-08-01

    Diseases caused by systemic fungal infections have become a significant clinical problem in recent decades. A series of glycosyl derivatives of the approved cyclic peptide antifungal drug caspofungin conjugated with β-D-glucopyranose, β-D-galactopyranose, β-D-xylopyranose, β-L-rhamnopyranose, β-maltose and β-lactose units were designed, synthesized, and evaluated as new potential antifungal drugs. The compounds were obtained by coupling the corresponding glycosyl amines to the free primary amino groups of caspofungin through a bifunctional glutaryl linker. In contrast to caspofungin, these glycosylated derivatives are soluble in water, but are not hygroscopic and moreover, are more stable than caspofungin under high humidity and temperature. CD studies showed that glycosylation has very little impact on the conformation of the cyclic peptide of caspofungin. In vitro antifungal tests against seven human pathogenic fungi revealed that the caspofungin-monosaccharide conjugates, but not the disaccharide conjugates, have increased antifungal activities against the majority of tested fungus species relative to caspofungin. The β-D-glucopyranosyl derivative 2 a showed the strongest and broadest antifungal activity, providing a lead for further studies.

  18. Design, synthesis, and antifungal activities of novel triazole derivatives containing the benzyl group.

    Science.gov (United States)

    Xu, Kehan; Huang, Lei; Xu, Zheng; Wang, Yanwei; Bai, Guojing; Wu, Qiuye; Wang, Xiaoyan; Yu, Shichong; Jiang, Yuanying

    2015-01-01

    In previous studies undertaken by our group, a series of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols (1a-r), which were analogs of fluconazole, was designed and synthesized by click chemistry. In the study reported here, the in vitro antifungal activities of all the target compounds were evaluated against eight human pathogenic fungi. Compounds 1a, 1q, and 1r showed the more antifungal activity than the others.

  19. Antifungal activity of Lactobacillus paracasei ssp. tolerans isolated from a sourdough bread culture.

    Science.gov (United States)

    Hassan, Yousef I; Bullerman, Lloyd B

    2008-01-15

    Lactic acid bacteria were isolated from four different sourdough bread cultures previously investigated for antifungal activity. A total of 116 isolates were obtained and screened for antifungal activity against a battery of molds. The most inhibitory isolate obtained was identified by API 50 CHL and 16s ribosomal RNA genotyping and found to be Lactobacillus paracasei ssp. tolerans. This isolate completely inhibited the growth of Fusarium proliferatum M 5689, M 5991 and Fusarium graminearum R 4053 compared to controls in a dual agar plate assay.

  20. Essential oil composition and antifungal activity of Foeniculum vulgare Mill obtained by different distillation conditions.

    Science.gov (United States)

    Mimica-Dukić, N; Kujundzić, S; Soković, M; Couladis, M

    2003-04-01

    The influence of different hydrodistillation conditions was evaluated from the standpoint of essential oil yield, chemical composition and antifungal activity from seeds of Foeniculum vulgare Mill. Three hydrodistillation conditions were considered. The main constituents of the oils were: (E)-anethole (72.27%-74.18%), fenchone (11.32%-16.35%) and methyl chavicol (3.78%-5.29%). The method of distillation significantly effected the essential oil yield and quantitative composition, although the antifungal activity of the oils against some fungi was only slightly altered.

  1. Marine-derived Penicillium in Korea: diversity, enzyme activity, and antifungal properties.

    Science.gov (United States)

    Park, Myung Soo; Fong, Jonathan J; Oh, Seung-Yoon; Kwon, Kae Kyoung; Sohn, Jae Hak; Lim, Young Woon

    2014-08-01

    The diversity of marine-derived Penicillium from Korea was investigated using morphological and multigene phylogenetic approaches, analyzing sequences of the internal transcribed spacer region, β-tubulin gene, and RNA polymerase subunit II gene. In addition, the biological activity of all isolated strains was evaluated. We tested for the extracellular enzyme activity of alginase, endoglucanase, and β-glucosidase, and antifungal activity against two plant pathogens (Colletotrichum acutatum and Fusarium oxysporum). A total of 184 strains of 36 Penicillium species were isolated, with 27 species being identified. The most common species were Penicillium polonicum (19.6 %), P. rubens (11.4 %), P. chrysogenum (11.4 %), and P. crustosum (10.9 %). The diversity of Penicillium strains isolated from soil (foreshore soil and sand) and marine macroorganisms was higher than the diversity of strains isolated from seawater. While many of the isolated strains showed alginase and β-glucosidase activity, no endoglucanase activity was found. More than half the strains (50.5 %) showed antifungal activity against at least one of the plant pathogens tested. Compared with other strains in this study, P. citrinum (strain SFC20140101-M662) showed high antifungal activity against both plant pathogens. The results reported here expand our knowledge of marine-derived Penicillium diversity. The relatively high proportion of strains that showed antifungal and enzyme activity demonstrates that marine-derived Penicillium have great potential to be used in the production of natural bioactive products for pharmaceutical and/or industrial use.

  2. Antifungal Activity of Coumarin Mammeisin Isolated from Species of the Kielmeyera Genre (Family: Clusiaceae or Guttiferae

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    Helcio Cassemiro Marcondes

    2015-01-01

    Full Text Available Coumarin mammeisin isolated from Kielmeyera elata was evaluated for its toxicity and antifungal activities. The toxicity of mammeisin was investigated by utilizing the Artemia salina methodology to determine its LD50 value. The minimum inhibitory concentration (MIC of fungi Candida sp. was assessed for mammeisin, presenting equivalent activity to ketoconazole but displaying better results than fluconazole.

  3. Antifungal Activity of Clove Essential Oil and its Volatile Vapour Against Dermatophytic Fungi

    OpenAIRE

    2007-01-01

    Antifungal activities of clove essential oil and its volatile vapour against dermatophytic fungi including Candida albicans, Epidermophyton floccosum. Microsporum audouinii, Trichophyton mentagrophytes, and Trichophyton rubrum were investigated. Both clove essential oil and its volatile vapour strongly inhibit spore germination and mycelial growth of the dermatophytic fungi tested. The volatile vapour of clove essential oil showed fungistatic activity whereas direct application of clove essen...

  4. In-vitro antibacterial, antifungal and cytotoxic activities of some coumarins and their metal complexes.

    Science.gov (United States)

    Rehman, Saeed U; Chohan, Zahid H; Gulnaz, Farzana; Supuran, Claudiu T

    2005-08-01

    A series of new antibacterial and antifungal coumarin-derived compounds and their transition metal complexes [cobalt (II), copper (II), nickel (II) and zinc (II)] have been synthesized, characterized and screened for their in vitro antibacterial activity against Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Salmonella typhi, Shigella dysenteriae, Bacillus cereus, Corynebacterium diphtheriae, Staphylococcus aureus and Streptococcus pyogenes bacterial strains and for in vitro antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, Candida glaberata. The results of these studies show the metal complexes to be more antibacterial and antifungal as compared to the uncomplexed coumarins. The brine shrimp bioassay was also carried out to study their in vitro cytotoxic properties.

  5. Synthesis, antifungal activity and structure-activity relationships of vanillin oxime-N-O-alkanoates.

    Science.gov (United States)

    Ahluwalia, Vivek; Garg, Nandini; Kumar, Birendra; Walia, Suresh; Sati, Om P

    2012-12-01

    Vanillin oxime-N-O-alkanoates were synthesized following reaction of vanillin with hydroxylamine hydrochloride, followed by reaction of the resultant oxime with acyl chlorides. The structures of the compounds were confirmed by IR, 1H, 13C NMR and mass spectral data. The test compounds were evaluated for their in vitro antifungal activity against three phytopathogenic fungi Macrophomina phaseolina, Rhizoctonia solani and Sclerotium rolfsii by the poisoned food technique. The moderate antifungal activity of vanillin was slightly increased following its conversion to vanillin oxime, but significantly increased after conversion of the oxime to oxime-N-O-alkanoates. While vanillin oxime-N-O-dodecanoate with an EC50 value 73.1 microg/mL was most active against M. phaseolina, vanillin oxime-N-O-nonanoate with EC50 of value 66.7 microg/mL was most active against R. solani. The activity increased with increases in the acyl chain length and was maximal with an acyl chain length of nine carbons.

  6. Study of the Cytotoxic and Antifungal Activities of Neolignans 8.O.4´ and Structurally Related Compounds

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    P. Matyus

    2000-03-01

    Full Text Available In the present work we report the antifungal and cytotoxic activities of a neolignan 8.O.4´series. The most active antifungal compounds show a significant cytotoxic effect which might be related.

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

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    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.

  8. Antimicrobial and antifungal activities of Cordia dichotoma (Forster F.) bark extracts.

    Science.gov (United States)

    Nariya, Pankaj B; Bhalodia, Nayan R; Shukla, V J; Acharya, R N

    2011-10-01

    Cordia dichotoma Forst.f. bark, identified as botanical source of Shlesmataka in Ayurvedic pharmacopoeias. Present study was carried out with an objective to investigate the antibacterial and antifungal potentials of Cordia dichotoma bark. Antibacterial activity of methanol and butanol extracts of the bark was carried out against two gram negative bacteria (Escherichia coli, and Pseudomonas aeruginosa) and two Gram positive bacteria (St. pyogenes and Staphylococcus aureus). The antifungal activity of the extracts was carried out against three common pathogenic fungi (Aspergillus niger, A.clavatus, and Candida albicans). Zone of inhibition of extracts was compared with that of different standards like Amplicilline, Ciprofloxacin, Norfloxacin and Chloramphenicol for antibacterial activity and Nystain and Greseofulvin for antifungal activity. The extracts showed remarkable inhibition of zone of bacterial growth and fungal growth and the results obtained were comparable with that of standards drugs against the organisms tested. The activity of extracts increased linearly with increase in concentration of extract (mg/ml). The results showed the antibacterial and antifungal activity against the organisms tested.

  9. Synthesis and characterization of dithiocarbamate chitosan derivatives with enhanced antifungal activity.

    Science.gov (United States)

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

    2012-06-20

    In this study, ammonium dithiocarbamate chitosan (ADTCCS) and triethylene diamine dithiocarbamate chitosan (TEDADTCCS) derivatives were obtained respectively by mixing chitosan with carbon disulfide and ammonia (triethylenediamine). Their structures were confirmed by FT-IR, 1H NMR, XRD, DSC, SEM, and elemental analysis. Antifungal properties of them against the plant pathogenic fungi Fusarium oxysporum and Alternaria porri were investigated at concentrations ranged from 31.25 to 500 mg/L. The dithiocarbamate chitosan derivatives had enhanced antifungal activity compared with chitosan. Particularly, they showed obvious inhibitory effect on Fusarium oxysporum. At 500 mg/L, TEDADTCCS inhibited growth of F. oxysporum at 60.4%, stronger than polyoxin and triadimefon whose antifungal indexes were found to be 25.3% and 37.7%. The chitosan derivatives described here deserve further study for use in crop protection.

  10. Production of peptide antifungal antibiotic and biocontrol activity of Bacillus subtilis.

    Science.gov (United States)

    Kumar, Ajay; Saini, Pragati; Shrivastava, J N

    2009-01-01

    Among different bacterial cultures, a potent Bacillus subtilis MTCC-8114 was isolated from garden soil samples which showed 16 and 14 mm inhibition zones by spot inoculation method and 24 and 22 mm inhibition zones by well agar diffusion method against test fungi i.e. Microsporum fulvum and Trichophyton species. Among four media tested, the maximum growth and antibiotic production was found in trypticase soya broth (TSB) medium at 37 degrees C, pH-7 and 48 h of incubation. The Rf value (0.64) by Thin Layer Chromatography (TLC) technique and UV and FTIR spectral data of the active antifungal compound, indicated that the isolated compound belongs to peptide antifungal antibiotic group. MIC value of antifungal antibiotic was 135 and 145 microg/ml.

  11. AN OVERVIEW OF AZOLE ANTIFUNGALS

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    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.

  12. Anti-fungal and anti-bacterial activities of ethanol extracts of selected traditional Chinese medicinal herbs

    Institute of Scientific and Technical Information of China (English)

    Lin Zhang; ngeles Melguizo; Ester Jimnez; Francisca Vicente; Anjaneya S Ravipati; Sundar R Koyyalamudi; Sang Chul Jeong; Narsimha Reddy; John Bartlett; Paul T Smith; Mercedes de la Cruz; Maria Cndida Monteiro

    2013-01-01

    Objective:To evaluate in vitro antimicrobial activities of selected 58 ethno-medicinal plant extracts with a view to assess their therapeutic potential. Methods:A total of 58 traditional Chinese medicinal plants were carefully selected based on the literature review and their traditional use. The antimicrobial activities of ethanol extracts of these medicinal plants were tested against fungi (Aspergillus fumigatus), yeast (Candida albicans), gram-negative (Acinetobacter baumannii and Pseudomonas aeruginosa) and gram-positive bacteria (Staphylococcus aureus). The activities were tested at three different concentrations of 1.00, 0.10 and 0.01 mg/mL. The data was analysed using Gene data Screener program. Results: The measured antimicrobial activities indicated that out of the 58 plant extracts, 15 extracts showed anti-fungal activity and 23 extracts exhibited anti-bacterial activity. Eight plant extracts have exhibited both anti-bacterial and anti-fungal activities. For instance, Eucommia ulmoides, Polygonum cuspidatum, Poria cocos and Uncaria rhyncophylla showed activity against both bacterial and fungal strains, indicating their broad spectrum of activity. Conclusions: The results revealed that the ethanol extracts of 30 plants out of the selected 58 possess significant antimicrobial activities. It is interesting to note that the findings from the current study are consistent with the traditional use. A clear correlation has also been found between the antimicrobial activity and the flavonoid content of the plant extracts which is in agreement with the literature. Hence, the results presented here can be used to guide the selection of potential plant species for the isolation and structure elucidation of novel antimicrobial compounds in order to establish the structure-activity relationship. This in turn is expected to lead the way to the discovery of novel antimicrobial agents for therapeutic use.

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

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    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.

  14. Active Internalization of the Penicillium chrysogenum Antifungal Protein PAF in Sensitive Aspergilli

    OpenAIRE

    Oberparleiter, Christoph; Kaiserer, Lydia; Haas, Hubertus; Ladurner, Peter; Andratsch, Manfred; Marx, Florentine

    2003-01-01

    The Penicillium chrysogenum antifungal protein PAF inhibits the growth of various filamentous fungi. In this study, PAF was found to localize to the cytoplasm of sensitive aspergilli by indirect immunofluorescence staining. The internalization process required active metabolism and ATP and was prevented by latrunculin B, suggesting an endocytotic mechanism.

  15. Antifungal activity of some Tanzanian plants used traditionally for the treatment of fungal infections.

    NARCIS (Netherlands)

    Hamza, O.; Beukel, C. van den; Matee, M.I.N.; Moshi, M.J.; Mikx, F.H.M.; Selemani, H.O.; Mbwambo, Z.H.; Ven, A.J.A.M. van der; Verweij, P.E.

    2006-01-01

    Using the ethnobotanical approach, some Tanzanian plants reported to be used by traditional healers for the treatment of oral candidiasis and fungal infections of the skin were collected and screened for their antifungal activity against Candida albicans, Candida glabrata, Candida tropicalis, Candid

  16. Development of buccal adhesive tablet with prolonged antifungal activity: Optimization and ex vivo deposition studies

    Directory of Open Access Journals (Sweden)

    Madgulkar A

    2009-01-01

    Full Text Available The purpose of the present work was to prepare buccal adhesive tablets of miconazole nitrate. The simplex centroid experimental design was used to arrive at optimum ratio of carbopol 934P, hydroxypropylmethylcellulose K4M and polyvinylpyrollidone, which will provide desired drug release and mucoadhesion. Swelling index, mucoadhesive strength and in vitro drug release of the prepared tablet was determined. The drug release and bioadhesion was dependent on type and relative amounts of the polymers. The optimized combination was subjected to in vitro antifungal activity, transmucosal permeation, drug deposition in mucosa, residence time and bioadhesion studies. IR spectroscopy was used to investigate any interaction between drug and excipients. Dissolution of miconazole from tablets was sustained for 6 h. based on the results obtained, it can be concluded that the prepared slow release buccoadhesive tablets of miconazole would markedly prolong the duration of antifungal activity. Comparison of in vitro antifungal activity of tablet with marketed gel showed that drug concentrations above the minimum inhibitory concentration were achieved immediately from both formulations but release from tablet was sustained up to 6 h, while the gel showed initially fast drug release, which did not sustain later. Drug permeation across buccal mucosa was minimum from the tablet as well as marketed gel; the deposition of drug in mucosa was higher in case of tablet. In vitro residence time and bioadhesive strength of tablet was higher than gel. Thus the buccoadhesive tablet of miconazole nitrate may offer better control of antifungal activity as compared to the gel formulation.

  17. Antibacterial, antifungal and antiviral activity of propolis of different geographic origin.

    Science.gov (United States)

    Kujumgiev, A; Tsvetkova, I; Serkedjieva, Y; Bankova, V; Christov, R; Popov, S

    1999-03-01

    Propolis samples from different geographic origins were investigated for their antibacterial (against Staphylococcus aureus and Escherichia coli), antifungal (against Candida albicans) and antiviral (against Avian influenza virus) activities. All samples were active against the fungal and Gram-positive bacterial test strains, and most showed antiviral activity. The activities of all samples were similar in spite of the differences in their chemical composition. In samples from the temperate zone, flavonoids and esters of phenolic acids are known to be responsible for the above mentioned activities of bee glue; tropical samples did not contain such substances but showed similar activities. Obviously, in different samples, different substance combinations are essential for the biological activity of the bee glue. It seems that propolis has general pharmacological value as a natural mixture and not as a source of new powerful antimicrobial, antifungal and antiviral compounds.

  18. Evolution of Broad-line Emission from Active Galactic Nuclei

    CERN Document Server

    Elitzur, Moshe; Trump, Jonathan R

    2013-01-01

    Apart from viewing-dependent obscuration, intrinsic broad-line emission from active galactic nuclei (AGNs) follows an evolutionary sequence: Type $1 \\to 1.2/1.5 \\to 1.8/1.9 \\to 2$ as the accretion rate onto the central black hole is decreasing. This spectral evolution is controlled, at least in part, by the parameter $L_{\\rm bol}/M^{2/3}$, where $L_{\\rm bol}$ is the AGN bolometric luminosity and $M$ is the black hole mass. Both this dependence and the double-peaked profiles that emerge along the sequence arise naturally in the disk-wind scenario for the AGN broad-line region.

  19. 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.

  20. Antifungal activity improved by coproduction of cyclodextrins and anabaenolysins in Cyanobacteria.

    Science.gov (United States)

    Shishido, Tania K; Jokela, Jouni; Kolehmainen, Clara-Theresia; Fewer, David P; Wahlsten, Matti; Wang, Hao; Rouhiainen, Leo; Rizzi, Ermanno; De Bellis, Gianluca; Permi, Perttu; Sivonen, Kaarina

    2015-11-03

    Cyclodextrins are cyclic oligosaccharides widely used in the pharmaceutical industry to improve drug delivery and to increase the solubility of hydrophobic compounds. Anabaenolysins are lipopeptides produced by cyanobacteria with potent lytic activity in cholesterol-containing membranes. Here, we identified the 23- to 24-kb gene clusters responsible for the production of the lipopeptide anabaenolysin. The hybrid nonribosomal peptide synthetase and polyketide synthase biosynthetic gene cluster is encoded in the genomes of three anabaenolysin-producing strains of Anabaena. We detected previously unidentified strains producing known anabaenolysins A and B and discovered the production of new variants of anabaenolysins C and D. Bioassays demonstrated that anabaenolysins have weak antifungal activity against Candida albicans. Surprisingly, addition of the hydrophilic fraction of the whole-cell extracts increased the antifungal activity of the hydrophobic anabaenolysins. The fraction contained compounds identified by NMR as α-, β-, and γ-cyclodextrins, which undergo acetylation. Cyclodextrins have been used for decades to improve the solubility and bioavailability of many drugs including antifungal compounds. This study shows a natural example of cyclodextrins improving the solubility and efficacy of an antifungal compound in an ancient lineage of photosynthetic bacteria.

  1. Crystal Structures and Antifungal Activities of Fluorine-Containing Thioureido Complexes with Nickel(II

    Directory of Open Access Journals (Sweden)

    Chun Li

    2013-12-01

    Full Text Available Ni(II complexes with N-2-fluorobenzoylpiperidine-1-carbothioimidate (L2−, N-4-fluorobenzoylpiperidine-1-carbothioimidate (L3−, N-2-fluorobenzoylmorpholine- 1-carbothioimidate (L5− and N-4-fluorobenzoylmorpholine-1-carbothioimidate (L6−  have been synthesized and characterized by elemental analysis, FTIR and 1H-NMR. The crystal structures of three ligands (HL2, HL3 and HL6 and the corresponding Ni(II complexes ([Ni(L22], [Ni(L32] and [Ni(L62] have been determined by X-ray diffraction. The antifungal activities of the Ni(II complexes together and the corresponding ligands against the fungi Botrytis cinerea, Trichoderma spp., Myrothecium and Verticillium spp. have been investigated. The experimental results showed that the ligands and their complexes have antifungal abilities. When the fluorine was substituted on the para-benzoyl moiety, the antifungal activity of the ligands was obviously increased. Moreover, the ligands were stronger than their complexes in inhibiting fungal activities. The antifungal ability of HL6 is especially strong, and similar to that of the commercial fungicide fluconazole.

  2. Antibacterial, antifungal and cytotoxic activity of terrestrial cyanobacterial strains from Serbia

    Institute of Scientific and Technical Information of China (English)

    Zorica SVIRCEV; Dragana CETOJEVIC-SIMIN; Jelica SIMEUNOVIC; Maja KARAMAN; Dejan STOJANOVIC

    2008-01-01

    Cyanobacteria are known to be a rich source of biologically active compounds some of which can have pharmaceutical importance. In this work we present the screening results of cyanobacterial strains for their antibacterial, antifungal, and cytotoxic activity. Cyanobacterial strains were isolated from various soil types in province of Vojvodina and Central Serbia, Republic of Serbia. The screening included 9 strains of Anabaena and 9 strains of Nostoc. Both, extracellular products (from the culture liquid) and cellular crude Iipophilic extracts were tested against 13 bacterial strains and 8 fungal strains. Cytotoxic activity was tested against three human cell lines. Methanol extracts were prepared according to φstensvik. Antibacterial and antifungal activities were determined measuring inhibition zone, 48 h after inoculation. The cytotoxic activity was determined by suIforhodamine B (SRB) colorimetric assay. Of all cyanobacterial strains tested, 52% showed some antifungal and 41% antibacterial activity. Two out of six tested strains possessed cytotoxic activity. The cytotoxic activity of Anabaena strain S12 was found both in culture liquid and crude cell extract. It occurred specifically between the 21st and 42nd day of cultivation against HeLa and MCF7 cells, but had no activity against cell line derived from a healthy tissue. A high percentage of the active strains among the tested strains justify the effort of screening cyanobacteria that are isolated from terrestrial environments. The most promising strains for the fur-ther study are Anabaena strain S12 which showed strong cytotoxic and antibacterial activity and Ana-baena strain S20 which produces a potent antifungal compound. The future work, besides further screening and chemical identification of the active compounds, should also include the development of culture techniques that would lead to more efficient production of biologically active compounds.

  3. Antibacterial, antifungal and cytotoxic activity of terrestrial cyanobacterial strains from Serbia

    Institute of Scientific and Technical Information of China (English)

    Zorica; SVIRCEV; Dragana; CETOJEVIC-SIMIN; Jelica; SIMEUNOVIC; Maja; KARAMAN; Dejan; STOJANOVIC

    2008-01-01

    Cyanobacteria are known to be a rich source of biologically active compounds some of which can have pharmaceutical importance. In this work we present the screening results of cyanobacterial strains for their antibacterial, antifungal, and cytotoxic activity. Cyanobacterial strains were isolated from various soil types in province of Vojvodina and Central Serbia, Republic of Serbia. The screening included 9 strains of Anabaena and 9 strains of Nostoc. Both, extracellular products (from the culture liquid) and cellular crude lipophilic extracts were tested against 13 bacterial strains and 8 fungal strains. Cytotoxic activity was tested against three human cell lines. Methanol extracts were prepared according to ?stensvik. Antibacterial and antifungal activities were determined measuring inhibition zone, 48 h after inoculation. The cytotoxic activity was determined by sulforhodamine B (SRB) colorimetric assay. Of all cyanobacterial strains tested, 52% showed some antifungal and 41% antibacterial activity. Two out of six tested strains possessed cytotoxic activity. The cytotoxic activity of Anabaena strain S12 was found both in culture liquid and crude cell extract. It occurred specifically between the 21st and 42nd day of cultivation against HeLa and MCF7 cells, but had no activity against cell line derived from a healthy tissue. A high percentage of the active strains among the tested strains justify the effort of screening cyanobacteria that are isolated from terrestrial environments. The most promising strains for the fur- ther study are Anabaena strain S12 which showed strong cytotoxic and antibacterial activity and Ana- baena strain S20 which produces a potent antifungal compound. The future work, besides further screening and chemical identification of the active compounds, should also include the development of culture techniques that would lead to more efficient production of biologically active compounds.

  4. [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.

  5. Antifungal activity of essential oils on Aspergillus parasiticus isolated from peanuts

    Directory of Open Access Journals (Sweden)

    Yooussef Mina M.

    2016-04-01

    Full Text Available Aspergillus parasiticus is one of the most common fungi which contaminates peanuts by destroying peanut shells before they are harvested and the fungus produces aflatoxins. The aim of this study was to evaluate the antifungal activities of seventeen essential oils on the growth of the aflatoxigenic form of A. parasiticus in contaminated peanuts from commercial outlets in Georgia. The agar dilution method was used to test the antifungal activity of essential oils against this form of A. parasiticus at various concentrations: 500; 1,000; 1,500; 2,000; 2,500 ppm. Among the seventeen essential oils tested, the antifungal effect of cinnamon, lemongrass, clove and thyme resulted in complete inhibition of mycelial growth. Cinnamon oil inhibited mycelial growth at ≥ 1,000 ppm, lemongrass and clove oils at ≥ 1,500 ppm and thyme at 2,500 ppm. However, cedar wood, citronella, cumin and peppermint oils showed partial inhibition of mycelial growth. Eucalyptus oil, on the other hand, had less antifungal properties against growth of A. parasiticus, irrespective of its concentration. Our results indicate that the aflatoxigenic form of A. parasiticus is sensitive to selected essential oils, especially cinnamon. These findings clearly indicate that essential oils may find a practical application in controlling the growth of A. parasiticus in stored peanuts.

  6. 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.

  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. 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.

  9. 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.

  10. Characterization of anticancer, DNase and antifungal activity of pumpkin 2S albumin.

    Science.gov (United States)

    Tomar, Prabhat Pratap Singh; Nikhil, Kumar; Singh, Anamika; Selvakumar, Purushotham; Roy, Partha; Sharma, Ashwani Kumar

    2014-06-13

    The plant 2S albumins exhibit a spectrum of biotechnologically exploitable functions. Among them, pumpkin 2S albumin has been shown to possess RNase and cell-free translational inhibitory activities. The present study investigated the anticancer, DNase and antifungal activities of pumpkin 2S albumin. The protein exhibited a strong anticancer activity toward breast cancer (MCF-7), ovarian teratocarcinoma (PA-1), prostate cancer (PC-3 and DU-145) and hepatocellular carcinoma (HepG2) cell lines. Acridine orange staining and DNA fragmentation studies indicated that cytotoxic effect of pumpkin 2S albumin is mediated through induction of apoptosis. Pumpkin 2S albumin showed DNase activity against both supercoiled and linear DNA and exerted antifungal activity against Fusarium oxysporum. Secondary structure analysis by CD showed that protein is highly stable up to 90°C and retains its alpha helical structure. These results demonstrated that pumpkin 2S albumin is a multifunctional protein with host of potential biotechnology applications.

  11. Antibacterial and antifungal activities from leaf extracts of Cassia fistula l.: An ethnomedicinal plant

    Directory of Open Access Journals (Sweden)

    Nayan R Bhalodia

    2011-01-01

    Full Text Available This study was carried out with an objective to investigate the antibacterial and antifungal potentials of leaves of Cassia fistula Linn. The aim of the study is to assess the antimicrobial activity and to determine the zone of inhibition of extracts on some bacterial and fungal strains. In the present study, the microbial activity of hydroalcohol extracts of leaves of Cassia fistula Linn. (an ethnomedicinal plant was evaluated for potential antimicrobial activity against medically important bacterial and fungal strains. The antimicrobial activity was determined in the extracts using agar disc diffusion method. The antibacterial and antifungal activities of extracts (5, 25, 50, 100, 250 ΅g/ml of Cassia fistula were tested against two Gram-positive--Staphylococcus aureus, Streptococcus pyogenes; two Gram-negative--Escherichia coli, Pseudomonas aeruginosa human pathogenic bacteria; and three fungal strains--Aspergillus niger, Aspergillus clavatus, Candida albicans. Zone of inhibition of extracts were compared with that of different standards like ampicillin, ciprofloxacin, norfloxacin, and chloramphenicol for antibacterial activity and nystatin and griseofulvin for antifungal activity. The results showed that the remarkable inhibition of the bacterial growth was shown against the tested organisms. The phytochemical analyses of the plants were carried out. The microbial activity of the Cassia fistula was due to the presence of various secondary metabolites. Hence, these plants can be used to discover bioactive natural products that may serve as leads in the development of new pharmaceuticals research activities.

  12. 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.

  13. 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.

  14. Chemical Composition of Essential Oilsof Thymus and Mentha Speciesand Their Antifungal Activities

    Directory of Open Access Journals (Sweden)

    Leo J. L. D. van Griensven

    2009-01-01

    Full Text Available The potential antifungal effects of Thymus vulgaris L., Thymus tosevii L., Mentha spicata L., and Mentha piperita L. (Labiatae essential oils and their components against 17 micromycetal food poisoning, plant, animal and human pathogens are presented. The essential oils were obtained by hydrodestillation of dried plant material. Their composition was determined by GC-MS. Identification of individual constituents was made by comparison with analytical standards, and by computer matching mass spectral data with those of the Wiley/NBS Library of Mass Spectra. MIC’s and MFC’s of the oils and their components were determined by dilution assays. Thymol (48.9% and p-cymene (19.0% were the main components of T. vulgaris, while carvacrol (12.8%, a-terpinyl acetate (12.3%, cis-myrtanol (11.2% and thymol (10.4% were dominant in T. tosevii. Both Thymus species showed very strong antifungal activities. In M. piperita oil menthol (37.4%, menthyl acetate (17.4% and menthone (12.7% were the main components, whereas those of M. spicata oil were carvone (69.5% and menthone (21.9%. Mentha sp. showed strong antifungal activities, however lower than Thymus sp. The commercial fungicide, bifonazole, used as a control, had much lower antifungal activity than the oils and components investigated. It is concluded that essential oils of Thymus and Mentha species possess great antifungal potential and could be used as natural preservatives and fungicides.

  15. 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

  16. Antioxidant, antifungal and antiviral activities of chitosan from the larvae of housefly, Musca domestica L.

    Science.gov (United States)

    Ai, Hui; Wang, Furong; Xia, Yuqian; Chen, Xiaomin; Lei, Chaoliang

    2012-05-01

    Antioxidant activity of the chitosan from the larvae of Musca domestica L. was evaluated in two different reactive oxygen species assays, and inhibitory effects against seven fungi were also tested. The results showed that the chitosan had scavenging activity for hydroxyl and superoxide radicals which were similar to that of ascorbic acid. Also the chitosan exhibited excellent antifungal activity, especially in the low concentration, it could significantly inhibit the growth of Rhizopus stolonifer. Besides, antiviral results demonstrated that the chitosan could effectively inhibit the infection of AcMNPV and BmNPV. These results suggested that the chitosan from the larvae of housefly could be effectively used as a natural antioxidant to protect the human body from free radicals and retard the progress of many chronic diseases. Furthermore, the chitosan with antiviral and antifungal activity might provide useful information for antiviral breeding technology of economic insect and development of plant pathological control.

  17. Synthesis of -aryl--lactones and relationship: Structure – antifeedant and antifungal activity

    Indian Academy of Sciences (India)

    Andrzej Skrobiszewski; Witold Gładkowski; Paulina Walczak; Anna Gliszczyńska; Gabriela Maciejewska; Tomasz Klejdysz; Jan Nawrot; Czesław Wawrzeńczyk

    2015-04-01

    Eighteen racemic -aryl--lactones derived from simple aromatic aldehydes have been obtained in the chemical synthesis. Iodolactones (5c and 6c) were synthesized from ()-4-(benzo[][1′,3′]-dioxol-5′-yl)- but-3-en-2-one (1). Reductive dehalogenation of iodolactones 5a–c and 6a–c afforded -ethyl--lactones (7a–c, 8a–c) whereas the unsaturated lactones (9a–c, 10a–c) were obtained by dehydrohalogenation of iodolactones. All synthesized lactones were fully characterized by spectroscopic data (NMR, IR, HRMS) and subjected to the tests on the antifeedant activity towards Tribolium confusum, Trogoderma granarium and Sitophilus granaries as well to the tests on the antifungal activity towards four Fusarium species. The biological tests allowed to find some relationships between the structure and biological activity of the compounds studied. -Ethyl--lactones 7a–c, 8a–c and unsaturated lactones 9a–c, 10a-c were usually stronger antifeedants than their parent iodolactones 5a–c and 6a–c. trans-Iodolactones 6a–c were more active than cis isomers 5a-c both in antifeedant and antifungal assays. The structure of aromatic substituent was the key factor in antifungal activity. The lactones with benzo [][1,3]dioxole ring (5c, 6c, 7c, 8c, 9c) were the most active whereas those with unsubstituted benzene ring exhibited almost no 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. Impact of brief exposure to antifungal agents on the post-antifungal effect and hemolysin activity of oral Candida albicans

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    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.

  20. Antifungal Activity of Selected Lactic Acid Bacteria and Propionic Acid Bacteria against Dairy-Associated Spoilage Fungi

    DEFF Research Database (Denmark)

    Aunsbjerg, Stina Dissing

    Bacterial cultures of lactic and propionic acid bacteria are widely used in fermented products including dairy products. Spoilage fungi may constitute a quality and safety issue in these products. The antifungal properties of some lactic and propionic acid bacteria make them potential candidates...... diacetyl and lactic acid, 6 antifungal hydroxy acids were identified. Of these, 3 have previously been reported from antifungal lactic acid bacteria, whereas the other 3 hydroxy acids have not previously been reported produced by antifungal lactic acid bacteria....... factors thereby facilitating development of new protective cultures. The aim of the current thesis was to determine and study metabolites involved in antifungal activity of protective Lactobacillus paracasei and Propionibacterium freudenreichii subsp. shermanii. This involved development of a suitable...

  1. Antibacterial, anti-fungal and phytotoxic activities of Ferula narthex Boiss.

    Science.gov (United States)

    Bashir, Shumaila; Alam, Mahboob; Ahmad, Bashir; Aman, Akhtar

    2014-11-01

    Crude methanolic extract of roots, aerial parts and its subsequent fractions of Ferula narthex Boiss were tested for antibacterial, anti-fungal and phytotoxic activities. Crude methanolic extract of roots and its fractions showed significant antibacterial effect against P.aeruginosa (86.95%, 73.91, 69.59, 78.26 & 73.91%) represented by percent inhibition except ethyl acetate (EtoAc) fraction. The EtoAc fraction of roots and aerial parts showed significant activity against E. coli (80%), S. typhi (81.2 & 81.25%) and S. pneumoniae (80%). The n-hexane, chloroform and aqueous fractions of aerial parts showed significant activity against P. aeruginosa (78.26, 69.56 & 73.91%). Following fungal strains (T. longifusus, C. albicans, A. flavus, M. canis, F. solani, C. glabrata) were also used for anti-fungal activity. Among tested samples only crude methanol extract of roots, n-hexane and chloroform fraction showed moderate anti-fungal activity against M. canis (40, 35 & 30%) represented by percent inhibition. The remaining fractions showed no effect on tested fungi. Different oils fractions were also tested against above fungal strains. Fraction I, II & V showed mild to moderate activity against M. canis (40, 40 & 25%). Phytotoxic effect of tested samples of roots, aerial part and its fractions showed concentration dependent growth inhibition. Maximum phytotoxic effect was noted for n-hexane and aqueous fraction (50% growth inhibition). The remaining tested samples showed mild effect on growth of Lemna minor plant.

  2. Broad activation of latent HIV-1 in vivo

    DEFF Research Database (Denmark)

    Barton, Kirston; Hiener, Bonnie; Winckelmann, Anni;

    2016-01-01

    The 'shock and kill' approach to cure human immunodeficiency virus (HIV) includes transcriptional induction of latent HIV-1 proviruses using latency-reversing agents (LRAs) with targeted immunotherapy to purge infected cells. The administration of LRAs (panobinostat or vorinostat) to HIV-1-infected...... individuals on antiretroviral therapy induces a significant increase in cell-associated unspliced (CA-US) HIV-1 RNA from CD4(+) T cells. However, it is important to discern whether the increases in CA-US HIV-1 RNA are due to limited or broad activation of HIV-1 proviruses. Here we use single-genome sequencing...... to find that the RNA transcripts observed following LRA administration are genetically diverse, indicating activation of transcription from an extensive range of proviruses. Defective sequences are more frequently found in CA HIV-1 RNA than in HIV-1 DNA, which has implications for developing an accurate...

  3. A new furoquinoline alkaloid with antifungal activity from the leaves of Ruta chalepensis L.

    Science.gov (United States)

    Emam, A; Eweis, M; Elbadry, M

    2010-12-01

    Bioassay-guided separation with an eye toward antifungal activity led to the isolation of the new alkaloid 5-(1̀,1̀-dimethylallyl)-8-hydroxyfuro[2-3-b] quinoline (1) and the known biscoumarin daphnoretin (2) as the active constituents of the chloroform extract obtained from the leaves of Ruta chalepensis. The structures of the metabolites were elucidated on the basis of their spectral characteristics (NMR, UV, and MS) and were compared with the literature. The antifungal activity of the isolated compounds was evaluated against the phytopathogenic fungi Rhizoctonia solani, Sclerotium rolfsii, and Fusarium solani, which cause root-rot and wilt diseases in several economically important food crops such as potato, sugar beet, and tomato.

  4. Synthesis and Antifungal Activities of New Type β-Methoxyacrylate-Based StrobUurin Analogues

    Institute of Scientific and Technical Information of China (English)

    张翔; 刘慧君; 高永鑫; 王会利; 郭宝元; 李建中

    2012-01-01

    Strobilurins have become one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel fl-methoxyacrylate analogues were designed and synthesized by integrating substituted pyrimidine with a strobilurin pharmacophore. The compounds were confirmed and characterized by infrared, 1H nuclear magnetic resonance, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds 1 exhibited potent antifungal activity against Colletotrichum orbiculare, Botrytis cinerea Pers and Phytophthora capsici Leonian at the concentration of 50 μg/mL. Exhilaratingly, compound 1 a (R= methyl) showed better antifungal activity against all the tested fungi than the commercial strobilurin fungicide azoxystrobin.

  5. Antifungal activity of Oleoresins used in meat industry on some toxigenic Aspergillus spp.

    Directory of Open Access Journals (Sweden)

    Šošo Vladislava M.

    2013-01-01

    Full Text Available Different spice oleoresins are widely used in meat industry. They contribute to the specific aroma and flavor of the end products, but they have also been reported to have strong antimicrobial activity. These properties open a plenty of possibilities to be used for defining the specific sensory profile of the product but also as natural food preservatives. This paper focuses on the antifungal activity of four oleoresins against different foodborne toxigenic Aspergillus species. Oleoresins used in the experiments were cayenne pepper, black pepper, garlic and rosemary oleoresins, and they were tested against following Aspergillus species: A. clavatus, A. flavus, A. fumigatus, A. niger, A. ochraceus and A. versicolor. Antifungal activity was tested using microtitre-plate-based assay incorporating resazurin as an indicator of cell growth and broth microdilution-method. [Projekat Ministarstva nauke Republike Srbije, br. III46009

  6. Design, synthesis and antifungal activities of novel strobilurin derivatives containing pyrimidine moieties

    Energy Technology Data Exchange (ETDEWEB)

    Zhang, Xiang; Geo, Yongxin; Liu, Huijun; Guo, Baoyuan; Wang, Huili [Research Center for Eco-Environmental Sciences/Chinese Academy of Sciences, Beijing (China)

    2012-04-15

    Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel β-methoxy acrylate analogues were designed and synthesized by integrating substituted pyrimidine with a strobilurin pharmacophore. The compounds were confirmed and characterized by infrared, {sup 1}H nuclear magnetic resonance, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds (1a-1h) exhibited potent antifungal activities against Colletotrichum orbicular, Botrytis cinerea Pers and Protoporphyria caps ici Leon ian at the concentration of 50 μg/mL. Exhilaratingly, compound 1d (R=3-trifluoromethylphenyl) showed better antifungal activity against all the tested fungi than the commercial stilbenetriol fungicide azoxystrobin.

  7. Antifungal Activity of Coumarin from Ageratum conyzoides L. Leaves on Candida albicans cells

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    Gunawan Pamudji Widodo

    2012-07-01

    Full Text Available The aim of this study was to identify the antifungal activity of coumarin isolated from Ageratum conyzoides L. leaves and to observe its influence on Candida albicans cells by scanning electron microscope (SEM and transmission electron microscope (TEM. Antifungal activity testing by disk diffusion method showed coumarin was active toward pathogenic fungus, Candida albicans with the MIC value of coumarin of 125 g mL-1. The influence of this substance on C. albicans cells was observed by scanning and transmission electron microscopies. The result showed that this compound damaged the cell by pores formation on the cell wall. The death of cells occurred due to leakage and necrotic of cytoplasmic content.

  8. Phylogenetic Diversity and Antifungal Activity of Endophytic Fungi Associated with Tephrosia purpurea.

    Science.gov (United States)

    Luo, Ze-Ping; Lin, Hai-Yan; Ding, Wen-Bing; He, Hua-Liang; Li, You-Zhi

    2015-12-01

    Sixty-one endophytic fungus strains with different colony morphologies were isolated from the leaves, stems and roots of Tephrosia purpurea with colonization rates of 66.95%, 37.50%, and 26.92%, respectively. Based on internal transcribed spacer sequence analysis, 61 isolates were classified into 16 genera belonging to 3 classes under the phylum Ascomycota. Of the 61 isolates, 6 (9.84%) exhibited antifungal activity against one or more indicator plant pathogenic fungi according to the dual culture test. Isolate TPL25 had the broadest antifungal spectrum of activity, and isolate TPL35 was active against 5 plant pathogenic fungi. Furthermore, culture filtrates of TPL25 and TPL35 exhibited greater than 80% growth inhibition against Sclerotinia sclerotiorum. We conclude that the endophytic fungal strains TPL25 and TPL35 are promising sources of bioactive compounds.

  9. SYNTHESIS OF SILVER NANOPARTICLES BY CHEMICAL REDUCTION METHOD AND THEIR ANTIFUNGAL ACTIVITY

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    Shenava Aashritha

    2013-10-01

    Full Text Available The aim of this study was to evaluate the antimicrobial activity of silvercolloidal nanoparticles which were synthesised by chemical reduction. Silver nanoparticles were synthesized by reduction of silver nitrate with sodium citrate. The presence of silver nanoparticles was detected by atomic absorption spectroscopy. Antifungal activity of silver nanoparticles was detected by the zone of inhibition. Silver nanoparticles exhibited a characteristic surface plasmon resonance band that is measured by UV-Vis spectroscopy, showing a typical absorbance peak for nanoparticles centred at 430 nm. The antifungal activity of silver nanoparticles was measured by the zones of inhibition by Kirby Bauer sensitivity testing which were measured after 24 h of incubation at 370C of Candida albicans growth on sabouraud dextrose agar. This study, integrates nanotechnology leading to possible advances in the formulation of new types of fungicide.

  10. New aminoporphyrins bearing urea derivative substituents: synthesis, characterization, antibacterial and antifungal activity

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    Gholamreza Karimipour

    2015-06-01

    Full Text Available This work studied the synthesis of 5,10,15-tris(4-aminophenyl-20-(N,N-dialkyl/diaryl-N-phenylurea porphyrins (P1-P4 with alkyl or aryl groups of Ph, iPr, Et and Me, respectively and also the preparation of their manganese (III and cobalt (II complexes (MnP and CoP. The P1-P4 ligands were characterized by different spectroscopic techniques (1H NMR, FTIR, UV-Vis and elemental analysis, and metalated with Mn and Co acetate salts. The antibacterial and antifungal activities of these compounds in vitro were investigated by agar-disc diffusion method against Escherichia coli (-, Pseudomonas aeruginosa (-, Staphylococcus aureus(+, Bacillus subtilis (+ and Aspergillus oryzae and Candida albicans. Results showed that antibacterial and antifungal activity of the test samples increased with increase of their concentrations and the highest activity was obtained when the concentration of porphyrin compounds was 100 µg/mL. The activity for the porphyrin ligands depended on the nature of the urea derivative substituents and increased in the order P1 > P2 > P3 >P4, which was consistent with the order of their liposolubility. MnP and CoP complexes exhibited much higher antibacterial and antifungal activity than P1-P4ligands. Further, the growth inhibitory effects of these compounds was generally in the order CoP complexes > MnP complexes > P1-P4 ligands. Among these porphyrin compounds, CoP1displayed the highest antibacterial and antifungal activity, especially with a concentration of 100 µg/mL, against all the four tested bacteria and two fungi, and therefore it could be potential to be used as drug.

  11. Antifungal compounds from turmeric and nutmeg with activity against plant pathogens.

    Science.gov (United States)

    Radwan, Mohamed M; Tabanca, Nurhayat; Wedge, David E; Tarawneh, Amer H; Cutler, Stephen J

    2014-12-01

    The antifungal activity of twenty-two common spices was evaluated against plant pathogens using direct-bioautography coupled Colletotrichum bioassays. Turmeric, nutmeg, ginger, clove, oregano, cinnamon, anise, fennel, basil, black cumin, and black pepper showed antifungal activity against the plant pathogens Colletotrichum acutatum, Colletotrichum fragariae, and Colletotrichum gloeosporioides. Among the active extracts, turmeric and nutmeg were the most active and were chosen for further investigation. The bioassay-guided fractionation led to the isolation of three compounds from turmeric (1-3) and three compounds from nutmeg (4-6). Their chemical structures were elucidated by spectroscopic analysis including HR-MS, 1D, and 2D NMR as curcumin (1), demethoxycurcumin (2) and bisdemethoxy-curcumin (3), erythro-(7R,8R)-Δ(8')-4,7-dihydroxy-3,3',5'-trimethoxy-8-O-4'-neolignan (4), erythro-(7R,8R)-Δ8'-7-acetoxy-3,4,3',5'-tetra-methoxy-8-O-4'-neolignan (5), and 5-hydroxy-eugenol (6). The isolated compounds were subsequently evaluated using a 96-well microbioassay against plant pathogens. At 30 μM, compounds 2 and 3 possessed the most antifungal activity against Phomopsis obscurans and Phomopsis viticola, respectively.

  12. [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.

  13. Interaction of gelatin with polyenes modulates antifungal activity and biocompatibility of electrospun fiber mats

    Directory of Open Access Journals (Sweden)

    Lakshminarayanan R

    2014-05-01

    Full Text Available Rajamani Lakshminarayanan,1,2 Radhakrishnan Sridhar,3,4 Xian Jun Loh,5 Muruganantham Nandhakumar,1 Veluchamy Amutha Barathi,1,6 Madhaiyan Kalaipriya,3,4 Jia Lin Kwan,1 Shou Ping Liu,1,2 Roger Wilmer Beuerman,1,2 Seeram Ramakrishna3,4,7 1Singapore Eye Research Institute, 2Signature Research Program in Neuroscience and Behavioral Disorders, Duke-NUS Graduate Medical School, 3Department of Mechanical Engineering, National University of Singapore, 4Center for Nanofibers and Nanotechnology, National University of Singapore, 5Institute of Materials Research and Engineering, A*STAR (Agency for Science, Technology and Research, 3 Research Link, Singapore, 6Department of Ophthalmology, Yong Loo Lin School of Medicine, National University of Singapore, 7NUS Nanoscience and Nanotechnology Initiative, Singapore Abstract: Topical application of antifungals does not have predictable or well-controlled release characteristics and requires reapplication to achieve therapeutic local concentration in a reasonable time period. In this article, the efficacy of five different US Food and Drug Administration-approved antifungal-loaded (amphotericin B, natamycin, terbinafine, fluconazole, and itraconazole electrospun gelatin fiber mats were compared. Morphological studies show that incorporation of polyenes resulted in a two-fold increase in fiber diameter and the mats inhibit the growth of yeasts and filamentous fungal pathogens. Terbinafine-loaded mats were effective against three filamentous fungal species. Among the two azole antifungals compared, the itraconazole-loaded mat was potent against Aspergillus strains. However, activity loss was observed for fluconazole-loaded mats against all of the test organisms. The polyene-loaded mats displayed rapid candidacidal activities as well. Biophysical and rheological measurements indicate strong interactions between polyene antifungals and gelatin matrix. As a result, the polyenes stabilized the triple helical

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

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    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.

  15. Antifungal Activity of Lactic Acid Bacteria Strains Isolated from Natural Honey against Pathogenic Candida Species

    Science.gov (United States)

    Bulgasem, Bulgasem Y.; Lani, Mohd Nizam; Wan Yusoff, Wan Mohtar; Fnaish, Sumaya G.

    2016-01-01

    The role of lactic acid bacteria (LAB) in honey as antifungal activity has received little attention and their mechanism of inhibitory of fungi is not fully understood. In this study, LAB were isolated from honey samples from Malaysia, Libya, Saudi Arabia, and Yemen. Twenty-five isolates were confirmed LAB by catalase test and Gram staining, and were screened for antifungal activity. Four LAB showed inhibitory activity against Candida spp. using the dual agar overlay method. And they were identified as Lactobacillus plantarum HS isolated from Al-Seder honey, Lactobacillus curvatus HH isolated from Al-Hanon honey, Pediococcus acidilactici HC isolated from Tualang honey and Pediococcus pentosaceus HM isolated from Al-Maray honey by the 16S rDNA sequence. The growth of Candida glabrata ATCC 2001 was strongly inhibited (>15.0 mm) and (10~15 mm) by the isolates of L. curvatus HH and P. pentosaceus HM, respectively. The antifungal activity of the crude supernatant (cell free supernatant, CFS) was evaluated using well diffusion method. The CFS showed high antifungal activity against Candida spp. especially The CFS of L. curvatus HH was significantly (p < 0.05) inhibited growth of C. glabrata ATCC 2001, C. parapsilosis ATCC 2201, and C. tropicalis ATCC 750 with inhibitory zone 22.0, 15.6, and 14.7 mm, respectively. While CFS of P. pentosaceus HM was significantly (p < 0.05) effective against C. krusei, C. glabrata, and C. albicans with inhibition zone 17.2, 16.0, and 13.3 mm, respectively. The results indicated that LAB isolated from honey produced compounds which can be used to inhibit the growth of the pathogenic Candida species. PMID:28154488

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

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    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

  17. Light-induced antifungal activity of TiO{sub 2} nanoparticles/ZnO nanowires

    Energy Technology Data Exchange (ETDEWEB)

    Haghighi, N. [Nano-Physics Research Lab., Department of Physics, University of Tehran, Tehran (Iran, Islamic Republic of); Abdi, Y., E-mail: y.abdi@ut.ac.ir [Nano-Physics Research Lab., Department of Physics, University of Tehran, Tehran (Iran, Islamic Republic of); Haghighi, F. [Department of Medical Mycology, School of Medical sciences, Tarbiat Modares University, Tehran (Iran, Islamic Republic of)

    2011-09-15

    Antifungal activity of TiO{sub 2}/ZnO nanostructures under visible light irradiation was investigated. A simple chemical method was used to synthesize ZnO nanowires. Zinc acetate dihydrate, Polyvinyl Pyrrolidone and deionized water were used as precursor, capping and solvent, respectively. TiO{sub 2} nanoparticles were deposited on ZnO nanowires using an atmospheric pressure chemical vapor deposition system. X-ray diffraction pattern of TiO{sub 2}/ZnO nano-composite has represented the diffraction peaks relating to the crystal planes of the TiO{sub 2} (anatase and rutile) and ZnO. TiO{sub 2}/ZnO nanostructure antifungal effect on Candida albicans biofilms was studied and compared with the activity of TiO{sub 2} nanoparticles and ZnO nanowires. The high efficiency photocatalytic activity of TiO{sub 2} nanoparticles leads to increased antifungal activity of ZnO nanowires. Scanning electron microscope was utilized to study the morphology of the as prepared nanostructures and the degradation of the yeast.

  18. Antifungal Activity of the Volatiles of High Potency Cannabis sativa L. Against Cryptococcus neoformans

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    Amira S. Wanas

    2016-03-01

    Full Text Available The n-hexane extracted volatile fraction of high potency Cannabis sativa L (Cannabaceae . was assessed in vitro for antifungal, antibacterial and antileishmanial activities. The oil exhibited selective albeit modest, antifungal activity against Cryptococcus neoformans with an IC 50 value of 33.1 µg/mL. Biologically-guided fractionation of the volatile fraction resulted in the isolation of three major compounds (1-3 using various chromatographic techniques. The chemical structures of the isolated compounds were identified as α-humulene (1, b -caryophyllene (2 and caryophyllene oxide (3 using GC/FID, GC/MS, 1D- and 2D-NMR analyses, respectively. Compound 1 showed potent and selective antifungal activity against Cryptococcus neoformans with IC 50 and MIC values of 1.18 m g/mL and 5.0 m g/mL respectively. Whereas compound 2 showed weak activity (IC 50 19.4 µg/mL, while compound 3 was inactive against C. neoformans.

  19. Phytochemical Composition, Antifungal and Antioxidant Activity of Duguetia furfuracea A. St.-Hill

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    Francisca Valéria Soares de Araújo Pinho

    2016-01-01

    Full Text Available Background. Duguetia furfuracea is popular plant used in popular medicine. Hypothesis/Purpose. This claim evaluated the phytochemical composition of the hydroethanolic extract (HEDF, fractions of Duguetia furfuracea, and antioxidant and antifungal activity. Methods. The chemical profile was carried out by HPLC-DAD. The total phenolic contents and flavonoid components were determined by Folin-Ciocalteu and aluminium chloride reaction. The antioxidant activity was measured by scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH free radical and ferric reducing ability of plasma (FRAP methods. The antifungal activity was determined by microdilution assay. Results. HPLC analysis revealed caffeic acid and rutin as major compounds (HEDF, caffeic acid and quercitrin (Mt-OH fraction, and quercitrin and isoquercitrin (Ac-OEt fraction. The highest levels of phenols and total flavonoids were found for Ac-OEt fraction, and the crude extract showed higher in vitro antioxidant potential. The antifungal activity showed synergic effect with fluconazole and EHDF against C. krusei, fluconazole and Mt-OH against C. krusei and C. tropicalis, and Ac-OE and fluconazole against C. albicans. Conclusion. The highest levels of phenols and total flavonoids were marked with antioxidant effect. This is the first report of bioactivity of the synergic effect of HEDF and fractions. More studies would be required to better clarify its mechanism of synergic action.

  20. Phytochemical Composition, Antifungal and Antioxidant Activity of Duguetia furfuracea A. St.-Hill

    Science.gov (United States)

    Pinho, Francisca Valéria Soares de Araújo; da Cruz, Litiele Cezar; Rodrigues, Nathane Rosa; Waczuk, Emily Pansera; Souza, Celestina Elba Sobral; da Costa, José Galberto Martins; Athayde, Margareth Linde; de Menezes, Irwin Rose Alencar

    2016-01-01

    Background. Duguetia furfuracea is popular plant used in popular medicine. Hypothesis/Purpose. This claim evaluated the phytochemical composition of the hydroethanolic extract (HEDF), fractions of Duguetia furfuracea, and antioxidant and antifungal activity. Methods. The chemical profile was carried out by HPLC-DAD. The total phenolic contents and flavonoid components were determined by Folin-Ciocalteu and aluminium chloride reaction. The antioxidant activity was measured by scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical and ferric reducing ability of plasma (FRAP) methods. The antifungal activity was determined by microdilution assay. Results. HPLC analysis revealed caffeic acid and rutin as major compounds (HEDF), caffeic acid and quercitrin (Mt-OH fraction), and quercitrin and isoquercitrin (Ac-OEt fraction). The highest levels of phenols and total flavonoids were found for Ac-OEt fraction, and the crude extract showed higher in vitro antioxidant potential. The antifungal activity showed synergic effect with fluconazole and EHDF against C. krusei, fluconazole and Mt-OH against C. krusei and C. tropicalis, and Ac-OE and fluconazole against C. albicans. Conclusion. The highest levels of phenols and total flavonoids were marked with antioxidant effect. This is the first report of bioactivity of the synergic effect of HEDF and fractions. More studies would be required to better clarify its mechanism of synergic action. PMID:27127550

  1. Antifungal activity, toxicity and chemical composition of the essential oil of Coriandrum sativum L. fruits.

    Science.gov (United States)

    Soares, Bruna V; Morais, Selene M; dos Santos Fontenelle, Raquel Oliveira; Queiroz, Vanessa A; Vila-Nova, Nadja S; Pereira, Christiana M C; Brito, Edy S; Neto, Manoel A S; Brito, Erika H S; Cavalcante, Carolina S P; Castelo-Branco, Débora S C M; Rocha, Marcos F G

    2012-07-11

    The aims of this study were to test the antifungal activity, toxicity and chemical composition of essential oil from C. sativum L. fruits. The essential oil, obtained by hydro-distillation, was analyzed by gas chromatography/mass spectroscopy. Linalool was the main constituent (58.22%). The oil was considered bioactive, showing an LC₅₀ value of 23 μg/mL in the Artemia salina lethality test. The antifungal activity was evaluated against Microsporum canis and Candida spp. by the agar-well diffusion method and the minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) were established by the broth microdilution method. The essential oil induced growth inhibition zones of 28 ± 5.42 and 9.25 ± 0.5 for M. canis and Candida spp. respectively. The MICs and MFCs for M. canis strains ranged from 78 to 620 and 150 to 1,250 μg/mL, and the MICs and MFCs for Candida spp strains ranged from 310 to 620 and 620 to 1,250 μg/mL, respectively. C. sativum essential oil is active in vitro against M. canis and Candida spp. demonstrating good antifungal activity.

  2. Endophytic fungi diversity of aquatic/riparian plants and their antifungal activity in vitro.

    Science.gov (United States)

    Li, Hai-Yan; Zhao, Chun-An; Liu, Chen-Jian; Xu, Xiao-Fei

    2010-02-01

    Two hundred and fourteen endophytic fungi were isolated from 500 segments of aquatic/riparian plants Ottelia acuminata, Myriophyllum verticillatum, Equisetum arvense, Cardamine multijuga, and Impatiens chinensis. They were identified to 31 taxa in which Cladosporium, Fusarium, and Geotrichum were the dominant genera. Among all isolates, 169 (79%) were anamorphic fungi, 1 (0.5%) was an teleomorphic ascomycete and 44 (21%) were sterile mycelia. There were significant differences in the colonization frequency of endophytes between the five plant species (X~2=51.128, P<0.001, Chi-square test). The riparian plants harboured more endophytes than the submerged plants. The antifungal activity of these isolates against Fusarium solani and Phytophthora nicotianae in vitro were tested and 28 (13.1%) isolates showed antifungal activities with more than 30% growth inhibition rate against the two pathogens.

  3. Prenylated flavonoids from the roots of Desmodium caudatum and evaluation of their antifungal activity.

    Science.gov (United States)

    Sasaki, Hisako; Kashiwada, Yoshiki; Shibatav, Hirofumi; Takaishi, Yoshihisa

    2012-11-01

    Two new prenylated flavonoids (1, 4) and two new prenylated C-methyl-flavonoids (6, 7), together with four known flavonoids (2, 3, 5, 8), were isolated from the roots of Desmodium caudatum. The structures of the new compounds were elucidated by extensive spectroscopic analyses including 1D-, 2D-NMR and MS. The antifungal activities of five compounds (1, 2, 4, 6, 8) as well as nine flavonoids (9-17) previously isolated from this plant against Aspergillus niger, Penicillium sp., Rhizopus sp., and Trichophyton sp. were evaluated. Compound 6 showed potent antifungal activity against Trichophyton sp. with a minimum inhibitory concentration (MIC) value of 1.95 µg/mL.

  4. Antifungal activity of Boerhavia diffusa against some dermatophytic species of Microsporum.

    Science.gov (United States)

    Agrawal, Anurag; Srivastava, Shalini; Srivastava, M M

    Various extracts petroleum ether, chloroform, ethyl acetate and ethyl alcohol) of aerial and root parts of Boerhavia diffusa was sereened for Antitungal activity (Inhibition in sporulation) against dermatophytic fungi Microsporum gypseum, M. fulvum and M. canis by using broth dilution method. Extracts of aerial part not show any noticeable antifungal activity. Ethyl acetate extract of root part of the plant was found to be most effective of against target fungal species. The maximum inhibition of mycelial growth was observed for M. gypseum (78.83%) followed by M. fulvum (62.33%) and M. canis (42.30%) of ethyl acetate in the test concentration of 1000 microg/ml 24 hours of incubation. The sporulation of target fungal species decreases with increasing supplementation of phytoextract, confirms the presence of some antifungal phytochemical moiety in roots of the plant.

  5. In vitro evaluation of antifungal activity of the seed extract of embelia ribes

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    A Sabitha Rani

    2011-01-01

    Full Text Available Antifungal activity of Embelia ribes was evaluated on eight different fungal species by employing various concentrations of seed extract (0.5-2.0 mg. All the concentrations of seed extract inhibited the fungal growth, whereas maximum activity was observed at 2.0 mg concentration of seed extract. Among different doses, the diameter of inhibition zones ranged from 9 to 18 mm in various fungal species and increased with the increase in the concentration of test solution. Among all the fungi, high inhibition zones were observed in Colletotricum crassipes (18 mm. This was followed by Cladosporium (17.5 mm, Armillaria mellea (17 mm, Colletotricum capsici (17 mm, Aspergillus niger (16.5 mm, Rhizopus oryzae (16.5 mm, respectively. Aspergillus terreus and Candida albicans showed less inhibition zones (15.5 and 16.0 mm compared to other organisms. The present study clearly demonstrated the antifungal properties of Embelia ribes.

  6. In vitro antioxidant, antifungal and cytotoxic activity of methanolic extract of Calligonum polygonoides

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    Arif Khan

    2015-06-01

    Full Text Available Present study is aimed at the pharmacological characterization of methanol extract of Calligonum polygonoides from District Bannu. Dried plant was grounded and extracted with methanol to prepare methanol crud extract. In vitro biological assays were conducted using this methanolic extract according to standard protocol. Cytotoxic activity of plant methanolic extract against brine shrimps while antifungal activity was also measured. Eighty percent death rate of brine shrimp was observed at 1,000 μg/mL of plant extract. 70 ± 0.0% growth inhibition of Aspergillus niger was measured during the present study. Significant scavenging results were observed during scavenging of free radicles viz; 78.1% against DPPH, 83.1% to ABTS and 36% against superoxide at 500 μg/mL were obtained. The results obtained in this study indicate that C. polygonoides possess significant antioxidant, antifungal and cytotoxic bioactive compounds.

  7. Synthesis and Antifungal Activity of Novel Sulfone Derivatives Containing 1,3,4-Oxadiazole Moieties

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    Maoguo Tong

    2011-11-01

    Full Text Available A series of new sulfone compounds containing 1,3,4-oxadiazole moieties were synthesized. The structures of these compounds were confirmed by spectroscopic data (IR, 1H- and 13C-NMR and elemental analyses. Antifungal tests indicated that all the title compounds exhibited good antifungal activities against eight kinds of plant pathogenic fungi, and some showed superiority over the commercial fungicide hymexazol. Among them, compounds 5d, 5e, 5f, and 5i showed prominent activity against B. cinerea, with determined EC50 values of 5.21 μg/mL, 8.25 µg/mL, 8.03 µg/mL, and 21.00 µg/mL, respectively. The present work demonstrates that sulfone derivatives such as 5d containing a 1,3,4-oxadiazole moiety can be used as possible lead compounds for the development of potential agrochemicals.

  8. PRELIMIARY PHYTOCHEMICAL ANALYSIS AND ANTIFUNGAL ACTIVITIES OF CRUDE EXTRACTS OF ZALEYA PENTANDRA AND CORCHORUS DEPRESSUS LINN.

    Science.gov (United States)

    Afzal, Samina; Chaudhary, Bashir Ahmad; Ahmad, Ashfaq; Afzali, Khurram

    2015-01-01

    Zaleya pentandra (Zp) and Cochoms depressus Linn. (Cd) have been considered as herbs with potential therapeutic benefits. Zp and Cd belong to the important family Aizoaceae and Tiliaceae, respectively. The extractions were carried out successively with methanol and dichloromethane at room temperature for 24 h. Preliminary phytochemical screening of Zp and Cd revealed the presence of steroids, alkaloids, saponins, and anthraquinones. The methanolic and dichloromethane extracts of selected plants were subjected to examination of antifungal activity by using agar tube dilution. The extracts were tested against different fungi such as A. nigeir, A. flavus, F. solani, A. funigatis and Mucor. The dichloromethane extract of aerial parts of Cd showed high antifungal activity against A. niger as compared to all other tested extracts.

  9. Synthesis and antifungal activity of the derivatives of novel pyrazole carboxamide and isoxazolol pyrazole carboxylate.

    Science.gov (United States)

    Sun, Jialong; Zhou, Yuanming

    2015-03-09

    A series of pyrazole carboxamide and isoxazolol pyrazole carboxylate derivatives were designed and synthesized in this study. The structures of the compounds were elucidated based on spectral data (infrared, proton nuclear magnetic resonance and mass spectroscopy). Then, all of the compounds were bioassayed in vitro against four types of phytopathogenic fungi (Alternaria porri, Marssonina coronaria, Cercospora petroselini and Rhizoctonia solani) using the mycelium growth inhibition method. The results showed that some of the synthesized pyrazole carboxamides displayed notable antifungal activity. The isoxazole pyrazole carboxylate 7ai exhibited significant antifungal activity against R. solani, with an EC50 value of 0.37 μg/mL. Nonetheless, this value was lower than that of the commercial fungicide, carbendazol.

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

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    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.

  11. Phyto chemical Screening, Antibacterial, Antifungal and Anthelmintic Activity of Morinda citrifolia stem

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    Dr. D. Gopala Krishna

    2013-05-01

    Full Text Available In the present study, the Petroleum Ether and Alcoholic extract of Morinda citrifolia L. (Noni stem were subjected to preliminary screening for Antimicrobial and Aanthelmintic activity. The alcoholic extract exhibited significant Anti bacterial, Antifungal activity, comparable to the standard drug Tetracycline. The Petroleum Ether and Alcoholic extract were evaluated for Anthelmintic activity on adult Indian Earthworms, ‘Pheretima posithuma’. The Alcoholic extract produced more significant Anthelmintic activity than Petroleum ether extract and the activities are comparable with the reference drug Piperazine citrate

  12. Antifungal activity of plant extracts with potential to control plant pathogens in pineapple

    Institute of Scientific and Technical Information of China (English)

    Maria Diana Cerqueira Sales; Helber Barcellos Costa; Jose Aires Ventura; Debora Dummer Meira

    2016-01-01

    Objective: To evaluate the in vitro antifungal activity of extracts, resins, oils and mother tinctures from plants against the filamentous fungi Fusarium guttiforme (F. guttiforme) and Chalara paradoxa, and to evaluate the control of the pineapple fusariosis in situ using mother tinctures. Methods: The screening of the antifungal potential of 131 extract forms from 63 plant species was performed in vitro by using plate-hole method. To control pineapple fusar-iosis in situ, preventive and post-infection treatments were performed on detached pineapple leaves of cv. P´erola (susceptible). Results: The quantitative study indicated that among the 49 mother tincture samples analyzed, 46% were effective against F. guttiforme and 29% for the Chalara paradoxa. The natural plant extracts, mother tincture of Glycyrrhiza glabra (MTGG1), mother tincture of Myroxylon balsamum (MTBT2), mother tincture of Aloe vera (MTAV3), mother tincture of Allium sativum (MTAS4), resin of Protium heptaphyllum (RESAM5) and crude extracts of Rhizophora mangle (CEMV6), exhibited an antifungal activity against F. guttiforme. In the preventive treatment against pineapple fusariosis, MTAV3, MTAS4 and MTGG1 were statistically similar to the treatment with tebuconazol fungicide. The curative treatments with MTAV3, MTAS4, MTGG1 and MTBT2 presented similar activity to fungicide (P Conclusions: The findings of the present study concluded that mother tinctures can effectively control phytopathogens. The mother tincture extract of Myroxylon balsamum showed antifungal activity and was used here for the first time for inhibition of phyto-pathogenic fungi. This study paves the way for the development of bioactive natural products with phytosanitary applications, with the added benefits of an environmentally safe and economically viable product.

  13. Antifungal activity of plant extracts with potential to control plant pathogens in pineapple

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    Maria Diana Cerqueira Sales

    2016-01-01

    Conclusions: The findings of the present study concluded that mother tinctures can effectively control phytopathogens. The mother tincture extract of Myroxylon balsamum showed antifungal activity and was used here for the first time for inhibition of phytopathogenic fungi. This study paves the way for the development of bioactive natural products with phytosanitary applications, with the added benefits of an environmentally safe and economically viable product.

  14. Antifungal activity of Malaysian honey and propolis extracts against pathogens implicated in denture stomatitis

    Science.gov (United States)

    Yusoff, Nik Yusliyana Nik; Mohamad, Suharni; Abdullah, Haswati@Nurhayati; Rahman, Nurhayu Ab

    2016-12-01

    Malaysian honey and propolis extracts were investigated for their antifungal properties against pathogens implicated in denture stomatitis. Each of the honey and aqueous extracts propolis at net preparation, 1:1 and 1:2 dilutions was evaluated by using agar well diffusion assay and further investigated by minimum inhibitory concentration (MIC) within the range of 500 mg/mL to 62.5 mg/mL against oral fungi. The findings indicated that there was no effect of propolis on Candida spp for both types of propolis based on no inhibition zones was recorded. Meanwhile, for antifungal activity of honey, only honey from Trigona spp has shown activity at net preparation against C. albicans (10.47 ± 0.23 mm), C. tropicalis (12.29 ± 0.23 mm) and C. glabrata (8.69 ± 0.53 mm). For minimum inhibitory concentration, the data indicates that both propolis have shown inhibitory effect at 500 mg/mL. As for honey, Trigona spp was the effective honey that give MIC value at 250 mg/mL against Candida spp. Apis dorsata honey has shown MIC value at 500 mg/mL while Apis mellifera honey had inhibited C.albicans and C.glabrata at 500 mg/mL except for C.tropicalis at 250 mg/mL. It can be concluded that both propolis has shown weaker antifungal activity against oral fungi while only honey produced from Trigona spp had strong antifungal activity compare to other honey against oral fungi implicated in denture stomatitis.

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

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    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.

  16. Antifungal activity of plant extracts with potential to control plant pathogens in pineapple

    Institute of Scientific and Technical Information of China (English)

    Maria Diana Cerqueira Sales; Helber Barcellos Costa; Patrícia Machado Bueno Fernandes; José Aires Ventura; Debora Dummer Meira

    2016-01-01

    Objective:To evaluate the in vitro antifungal activity of extracts,resins,oils and mother tinctures from plants against the filamentous fungi Fusarium guttiforme(F.guttiforme)and Chalara paradoxa,and to evaluate the control of the pineapple fusariosis in situ using mother tinctures.Methods:The screening of the antifungal potential of 131 extract forms from 63 plant species was performed in vitro by using plate-hole method.To control pineapple fusariosis in situ,preventive and post-infection treatments were performed on detached pineapple leaves of cv.Perola(susceptible).Results:The quantitative study indicated that among the 49 mother tincture samples analyzed,46% were effective against F.guttiforme and 29% for the Chalara paradoxa.The natural plant extracts,mother tincture of Glycyrrhiza glabra(MTGG1),mother tincture of Myroxylon balsamum(MTBT2),mother tincture of Aloe vera(MTAV3),mother tincture of Allium sativum(MTAS4),resin of Protium heptaphyllum(RESAM5) and crude extracts of Rhizophora mangle(CEMV6),exhibited an antifungal activity against F.guttiforme.In the preventive treatment against pineapple fusariosis,MTAV3,MTAS4 and MTGG1 were statistically similar to the treatment with tebuconazol fungicide.The curative treatments with MTAV3,MTAS4,MTGG1 and MTBT2 presented similar activity to fungicide(P < 0.05).Conclusions:The findings of the present study concluded that mother tinctures can effectively control phytopathogens.The mother tincture extract of Myroxylon balsamum showed antifungal activity and was used here for the first time for inhibition of phytopathogenic fungi.This study paves the way for the development of bioactive natural products with phytosanitary applications,with the added benefits of an environmentally safe and economically viable product.

  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. Antifungal activity of extracts from endophytic fungi associated with Smallanthus maintained in vitro as autotrophic cultures and as pot plants in the greenhouse.

    Science.gov (United States)

    Rosa, Luiz H; Tabanca, Nurhayat; Techen, Natascha; Pan, Zhiqiang; Wedge, David E; Moraes, Rita M

    2012-10-01

    The endophytic fungal assemblages associated with Smallanthus sonchifolius (Poepp.) H. Rob. and Smallanthus uvedalius (L.) Mack. ex Small growing in vitro autotrophic cultures and in the greenhouse were identified and evaluated for their ability to produce bioactive compounds. A total of 25 isolates were recovered that were genetically closely related to species of the genera Bionectria , Cladosporium , Colletotrichum , Fusarium , Gibberella , Hypocrea , Lecythophora , Nigrospora , Plectosphaerella , and Trichoderma . The endophytic assemblages of S. sonchifolius presented a greater diversity than the group isolated from S. uvedalius and demonstrated the presence of dominant generalist fungi. Extracts of all fungi were screened against the fungal plant pathogens. Ten extracts (41.6%) displayed antifungal activities; some of them had a broad antifungal activity. The phylotypes Lecythophora sp. 1, Lecythophora sp. 2, and Fusarium oxysporum were isolated from in vitro autotrophic cultures and displayed antifungal activity. The presence of bioactive endophytic fungi within S. sonchifolius and S. uvedalius suggests an ecological advantage against pathogenic attacks. This study revealed reduced numbers of endophytes in association with both Smallanthus species in controlled cultivation conditions compared with the endophytic communities of hosts collected in the wild environments. Even as reduced endophytic communities, these fungi continue to provide chemical protection for the host.

  19. Microwave-Assisted Synthesis and Antifungal Activity of Some Novel Thioethers Containing 1,2,4-Triazole Moiety

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    Li-Jing Min

    2015-11-01

    Full Text Available A series of novel thioether derivatives containing 1,2,4-triazole moiety were designed and synthesized from 4-chlorophenol and ethyl 2-chloroacetate as starting materials by multi-step reactions under microwave irradiation, and their structures were characterized by 1H-NMR, MS and elemental analysis. The antifungal activity of title compounds was determined. The results indicated that some of title compounds exhibited moderate antifungal activity.

  20. Antifungal activity of selected Malaysian honeys: a comparison with Manuka honey

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    Siti Aisyah Sayadi

    2015-07-01

    Full Text Available Objective: To evaluate four selected Malaysian honey samples from different floral sources (Gelam, Tualang, Nenas and Acacia for their ability to inhibit the growth of fungi and yeast strains (Candida albicans, Aspergillus niger, Epidermophyton floccosum, Microsporum gypseum, Trichophyton rubrum and Trichophyton mentagrophytes. Methods: The broth microdilution method was used to assess the antifungal activity of honey against yeasts at different concentrations ranging from 0.01% to 70% (v/v. Minimum inhibitory concentration (MIC of the honeys were determined by visual inspection and spectrophotometric assay. Minimum fungicidal concentration test was performed by further sub-culturing from the plates which showed no visible growth in the MIC assay onto Sabroud dextrose agar. Results: All tested Malaysian honeys except Gelam showed antifungal activity against all species analysed, with the MIC ranging from 25% (v/v to 50% (v/v while MIC of Manuka honey ranged between 21% to 53% (v/v. Candida albicans was more susceptible to honey than other species tested. Conclusions: Locally produced honeys exhibited antifungal activity which is less than or equal to that of Manuka honey. Our data showed evidence in support of the therapeutic uses of Malaysian honeys.

  1. Antifungal Activity of Amphotericin B Conjugated to Nanosized Magnetite in the Treatment of Paracoccidioidomycosis.

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    Camila Arruda Saldanha

    2016-06-01

    Full Text Available This study reports on in vitro and in vivo tests that sought to assess the antifungal activity of a newly developed magnetic carrier system comprising amphotericin B loaded onto the surface of pre-coated (with a double-layer of lauric acid magnetite nanoparticles. The in vitro tests compared two drugs; i.e., this newly developed form and free amphotericin B. We found that this nanocomplex exhibited antifungal activity without cytotoxicity to human urinary cells and with low cytotoxicity to peritoneal macrophages. We also evaluated the efficacy of the nanocomplex in experimental paracoccidioidomycosis. BALB/c mice were intratracheally infected with Paracoccidioides brasiliensis and treated with the compound for 30 or 60 days beginning the day after infection. The newly developed amphotericin B coupled with magnetic nanoparticles was effective against experimental paracoccidioidomycosis, and it did not induce clinical, biochemical or histopathological alterations. The nanocomplex also did not induce genotoxic effects in bone marrow cells. Therefore, it is reasonable to believe that amphotericin B coupled to magnetic nanoparticles and stabilized with bilayer lauric acid is a promising nanotool for the treatment of the experimental paracoccidioidomycosis because it exhibited antifungal activity that was similar to that of free amphotericin B, did not induce adverse effects in therapeutic doses and allowed for a reduction in the number of applications.

  2. Antifungal activity of selected Malaysian honeys:a comparison with Manuka honey

    Institute of Scientific and Technical Information of China (English)

    Siti Aisyah Sayadi; Rozaini Mohd Zohdi; Nur Salme Suhana Shamshuddin; Muna Syairah Khairy; Nur Ashikin Hasan; Ahmad Syamil Yasin; Kalavathy Ramasamy

    2015-01-01

    Objective:To evaluate four selected Malaysian honey samples from different floral sources (Gelam,Tualang,Nenas and Acacia) for their ability to inhibit the growth of fungi and yeast strains (Candida albicans, Aspergillus niger, Epidermophyton floccosum, Microsporum gypseum, Trichophyton rubrum andTrichophyton mentagrophytes). Methods: The broth microdilution method was used to assess the antifungal activity of honey against yeasts at different concentrations ranging from 0.01% to 70% (v/v). Minimum inhibitory concentration (MIC) of the honeys were determined by visual inspection and spectrophotometric assay. Minimum fungicidal concentration test was performed by further sub-culturing from the plates which showed no visible growth in theMICassay onto Sabroud dextrose agar. Results: All tested Malaysian honeys except Gelam showed antifungal activity against all species analysed, with theMIC ranging from 25% (v/v) to 50% (v/v) whileMIC of Manuka honey ranged between 21% to 53%(v/v).Candida albicans was more susceptible to honey than other species tested. Conclusions: Locally produced honeys exhibited antifungal activity which is less than or equal to that of Manuka honey. Our data showed evidence in support of the therapeutic uses of Malaysian honeys.

  3. Purification, characterization, and antifungal activity of chitinases from pineapple (Ananas comosus) leaf.

    Science.gov (United States)

    Taira, Toki; Toma, Noriko; Ishihara, Masanobu

    2005-01-01

    Three chitinases, designated pineapple leaf chitinase (PL Chi)-A, -B, and -C were purified from the leaves of pineapple (Ananas comosus) using chitin affinity column chromatography followed by several column chromatographies. PL Chi-A is a class III chitinase having a molecular mass of 25 kDa and an isoelectric point of 4.4. PL Chi-B and -C are class I chitinases having molecular masses of 33 kDa and 39 kDa and isoelectric points of 7.9 and 4.6 respectively. PL Chi-C is a glycoprotein and the others are simple proteins. The optimum pHs of PL Chi-A, -B, and -C toward glycolchitin are pH 3, 4, and 9 respectively. The chitin-binding ability of PL Chi-C is higher than that of PL Chi-B, and PL Chi-A has lower chitin-binding ability than the others. At low ionic strength, PL Chi-B exhibits strong antifungal activity toward Trichoderma viride but the others do not. At high ionic strength, PL Chi-B and -C exhibit strong and weak antifungal activity respectively. PL Chi-A does not have antifungal activity.

  4. Chemical Composition, Antifungal and Antibiofilm Activities of the Essential Oil of Mentha piperita L.

    Science.gov (United States)

    Saharkhiz, Mohammad Jamal; Motamedi, Marjan; Zomorodian, Kamiar; Pakshir, Keyvan; Miri, Ramin; Hemyari, Kimia

    2012-01-01

    Variations in quantity and quality of essential oil (EO) from the aerial parts of cultivated Mentha piperita were determined. The EO of air-dried sample was obtained by a hydrodistillation method and analyzed by a gas chromatography/mass spectrometry (GC/MS). The antifungal activity of the EO was investigated by broth microdilution methods as recommended by Clinical and Laboratory Standards Institute. A biofilm formation inhibition was measured by using an XTT reduction assay. Menthol (53.28%) was the major compound of the EO followed by Menthyl acetate (15.1%) and Menthofuran (11.18%). The EO exhibited strong antifungal activities against the examined fungi at concentrations ranging from 0.12 to 8.0 μL/mL. In addition, the EO inhibited the biofilm formation of Candida albicans and C. dubliniensis at concentrations up to 2 μL/mL. Considering the wide range of the antifungal activities of the examined EO, it might be potentially used in the management of fungal infections or in the extension of the shelf life of food products.

  5. Antifungal activity of zinc oxide nanoparticles against Botrytis cinerea and Penicillium expansum.

    Science.gov (United States)

    He, Lili; Liu, Yang; Mustapha, Azlin; Lin, Mengshi

    2011-03-20

    Antifungal activities of zinc oxide nanoparticles (ZnO NPs) and their mode of action against two postharvest pathogenic fungi (Botrytis cinerea and Penicillium expansum) were investigated in this study. ZnO NPs with sizes of 70 ± 15 nm and concentrations of 0, 3, 6 and 12 mmol l(-1) were used. Traditional microbiological plating, scanning electron microscopy (SEM), and Raman spectroscopy were used to study antifungal activities of ZnO NPs and to characterize the changes in morphology and cellular compositions of fungal hyphae treated with ZnO NPs. Results show that ZnO NPs at concentrations greater than 3 mmol l(-1) can significantly inhibit the growth of B. cinerea and P. expansum. P. expansum was more sensitive to the treatment with ZnO NPs than B. cinerea. SEM images and Raman spectra indicate two different antifungal activities of ZnO NPs against B. cinerea and P. expansum. ZnO NPs inhibited the growth of B. cinerea by affecting cellular functions, which caused deformation in fungal hyphae. In comparison, ZnO NPs prevented the development of conidiophores and conidia of P. expansum, which eventually led to the death of fungal hyphae. These results suggest that ZnO NPs could be used as an effective fungicide in agricultural and food safety applications.

  6. In Vitro Antifungal Activity of Burkholderia gladioli pv. agaricicola against Some Phytopathogenic Fungi

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    Hazem S. Elshafie

    2012-12-01

    Full Text Available The trend to search novel microbial natural biocides has recently been increasing in order to avoid the environmental pollution from use of synthetic pesticides. Among these novel natural biocides are the bioactive secondary metabolites of Burkholderia gladioli pv. agaricicola (Bga. The aim of this study is to determine antifungal activity of Bga strains against some phytopathogenic fungi. The fungicidal tests were carried out using cultures and cell-free culture filtrates against Botrytis cinerea, Aspergillus flavus, Aspergillus niger, Penicillium digitatum, Penicillium expansum, Sclerotinia sclerotiorum and Phytophthora cactorum. Results demonstrated that all tested strains exert antifungal activity against all studied fungi by producing diffusible metabolites which are correlated with their ability to produce extracellular hydrolytic enzymes. All strains significantly reduced the growth of studied fungi and the bacterial cells were more bioactive than bacterial filtrates. All tested Bulkholderia strains produced volatile organic compounds (VOCs, which inhibited the fungal growth and reduced the growth rate of Fusarium oxysporum and Rhizoctonia solani. GC/MS analysis of VOCs emitted by strain Bga 11096 indicated the presence of a compound that was identified as 1-methyl-4-(1-methylethenyl-cyclohexene, a liquid hydrocarbon classified as cyclic terpene. This compound could be responsible for the antifungal activity, which is also in agreement with the work of other authors.

  7. Antifungal Activity of Amphotericin B Conjugated to Nanosized Magnetite in the Treatment of Paracoccidioidomycosis

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    Saldanha, Camila Arruda; Garcia, Mônica Pereira; Iocca, Diego Cesar; Rebelo, Luciana Guilherme; Souza, Ana Camila Oliveira; Bocca, Anamélia Lorenzetti; Almeida Santos, Maria de Fátima Menezes; Morais, Paulo Cesar; Azevedo, Ricardo Bentes

    2016-01-01

    This study reports on in vitro and in vivo tests that sought to assess the antifungal activity of a newly developed magnetic carrier system comprising amphotericin B loaded onto the surface of pre-coated (with a double-layer of lauric acid) magnetite nanoparticles. The in vitro tests compared two drugs; i.e., this newly developed form and free amphotericin B. We found that this nanocomplex exhibited antifungal activity without cytotoxicity to human urinary cells and with low cytotoxicity to peritoneal macrophages. We also evaluated the efficacy of the nanocomplex in experimental paracoccidioidomycosis. BALB/c mice were intratracheally infected with Paracoccidioides brasiliensis and treated with the compound for 30 or 60 days beginning the day after infection. The newly developed amphotericin B coupled with magnetic nanoparticles was effective against experimental paracoccidioidomycosis, and it did not induce clinical, biochemical or histopathological alterations. The nanocomplex also did not induce genotoxic effects in bone marrow cells. Therefore, it is reasonable to believe that amphotericin B coupled to magnetic nanoparticles and stabilized with bilayer lauric acid is a promising nanotool for the treatment of the experimental paracoccidioidomycosis because it exhibited antifungal activity that was similar to that of free amphotericin B, did not induce adverse effects in therapeutic doses and allowed for a reduction in the number of applications. PMID:27303789

  8. Antifungal activity and gene expression of lipopeptide antibiotics in strains of genus Bacillus

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    Grabova A. Yu.

    2016-02-01

    Full Text Available Aim. To research the antifungal activity and gene expression of lipopeptide antibiotics in strains of genus Bacillus. Methods. Deferred antagonism method, PCR, qRT-PCR, MALDI-TOF mass spectrometry. Results. It was revealed that Bacillus sp. strains C6 and Lg37s out of five tested strains had the highest antifungal activity. Based on the molecular genetic methods, it was shown that the expression of genes of lipopeptide antibiotics, related to the fengycin family, occurred in all these strains. At the same time, the gene expression of cyclolipopeptide iturin was found in the Bacillus sp. strains C6 and Lg37s. It was determined that Bacillus sp. C6 strain had the highest level of expression of the fengycin operon`s genes, whereas the lowest level was observed in Bacillus sp. C10 strain. By means of MALDI-TOF mass spectrometry, the presence of fengycins in the cell-free cultural fluid of Bacillus sp. C6 strain was detected. Conclusion. The direct correlation between the level of antifungal activity and the fengycin synthetases expression has not been disclosed. A higher level of antagonism detected for two Bacillus strains is more likely associated with the expression and subsequent synthesis of fengycin and iturin.

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

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    Neveen Helmy Abou El-Soud

    2015-07-01

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

  10. Antifungal Activity of Selected Indigenous Pseudomonas and Bacillus from the Soybean Rhizosphere

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    A. F. García

    2009-01-01

    Full Text Available The purpose of this study was to isolate and select indigenous soil Pseudomonas and Bacillus bacteria capable of developing multiple mechanisms of action related to the biocontrol of phytopathogenic fungi affecting soybean crops. The screening procedure consisted of antagonism tests against a panel of phytopathogenic fungi, taxonomic identification, detection by PCR of several genes related to antifungal activity, in vitro detection of the antifungal products, and root colonization assays. Two isolates, identified and designated as Pseudomonas fluorescens BNM296 and Bacillus amyloliquefaciens BNM340, were selected for further studies. These isolates protected plants against the damping-off caused by Pythium ultimum and were able to increase the seedling emergence rate after inoculation of soybean seeds with each bacterium. Also, the shoot nitrogen content was higher in plants when seeds were inoculated with BNM296. The polyphasic approach of this work allowed us to select two indigenous bacterial strains that promoted the early development of soybean plants.

  11. Anti-fungal activities of constituents from Uvaria scheffleri and Artabotrys brachypetalus

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    Odebode A.C.

    2006-01-01

    Full Text Available The anti-fungal activity of schefflone, a mixture of dimmer, 3,5 dimethoxy carvacrol and annonaceous acetogenin, extracted from stem-bark and root of Uvaria scheffleri and Artabotrys bruchypetalus against Fusarium solani, Botryodiplodia theobromae, Asperillus niger and Aspergillus flavus was determined. An in-vitro bioassay showed that the minimum inhibitory effect of the compounds to the fungal pathogens occurred at 200 ppm in both radial growth and mycelia dry weight measurements. Acetogenin from A brachypetalus had a very strong anti-fungal effect on all the test fungi. The effects of the compounds were more pronounced on F solani than on the other. The bioassay methods also play a significant role in the sensitivity of the samples on the pathogens. .

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

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    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.

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

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    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.

  14. Antifungal activity of selected indigenous pseudomonas and bacillus from the soybean rhizosphere.

    Science.gov (United States)

    León, M; Yaryura, P M; Montecchia, M S; Hernández, A I; Correa, O S; Pucheu, N L; Kerber, N L; García, A F

    2009-01-01

    The purpose of this study was to isolate and select indigenous soil Pseudomonas and Bacillus bacteria capable of developing multiple mechanisms of action related to the biocontrol of phytopathogenic fungi affecting soybean crops. The screening procedure consisted of antagonism tests against a panel of phytopathogenic fungi, taxonomic identification, detection by PCR of several genes related to antifungal activity, in vitro detection of the antifungal products, and root colonization assays. Two isolates, identified and designated as Pseudomonas fluorescens BNM296 and Bacillus amyloliquefaciens BNM340, were selected for further studies. These isolates protected plants against the damping-off caused by Pythium ultimum and were able to increase the seedling emergence rate after inoculation of soybean seeds with each bacterium. Also, the shoot nitrogen content was higher in plants when seeds were inoculated with BNM296. The polyphasic approach of this work allowed us to select two indigenous bacterial strains that promoted the early development of soybean plants.

  15. Synthesis of Oxylipin Mimics and Their Antifungal Activity against the Citrus Postharvest Pathogens

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    Jimei Ma

    2016-02-01

    Full Text Available Nine oxylipin mimics were designed and synthesized starting from d-mannose. Their antifungal activity against three citrus postharvest pathogens was evaluated by spore germination assay. The results indicated that all the compounds significantly inhibited the growth of Penicillium digitatum, Penicillium italicum and Aspergillus niger. The compound (3Z,6Z,8S,9R,10R-octadeca-3,6-diene-8,9,10-triol (3 exhibited excellent inhibitory effect on both Penicillium digitatum (IC50 = 34 ppm and Penicillium italicum (IC50 = 94 ppm. Their in vivo antifungal activities against citrus postharvest blue mold were tested with fruit inoculated with the pathogen Penicillium italicum. The compound (3R,4S-methyl 3,4-dihydroxy-5-octyltetrahydrofuran-2-carboxylate (9 demonstrated significant efficacy by reducing the disease severity to 60%. The antifungal mechanism of these oxylipin mimics was postulated in which both inhibition of pathogenic mycelium and stimuli of the host oxylipin-mediated defense response played important roles.

  16. Evaluation of Antifungal Activity and Mechanism of Action of Citral against Candida albicans

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    Maria Clerya Alvino Leite

    2014-01-01

    Full Text Available Candida albicans is a yeast that commensally inhabits the human body and can cause opportunistic or pathogenic infections. Objective. To investigate the antifungal activity of citral against C. albicans. Methodology. The minimum inhibitory concentration (MIC and the minimum fungicidal concentration (MFC were determined by the broth microdilution techniques. We also investigated possible citral action on cell walls (0.8 M sorbitol, cell membranes (citral to ergosterol binding, the time-kill curve, and biological activity on the yeast’s morphology. Results. The MIC and MFC of citral were, respectively, 64 µg/mL and 256 µg/mL. Involvement with the cell wall and ergosterol binding were excluded as possible mechanisms of action. In the morphological interference assay, it was observed that the product inhibited pseudohyphae and chlamydoconidia formation. The MIC and the MFC of citral required only 4 hours of exposure to effectively kill 99.9% of the inoculum. Conclusion. Citral showed in vitro antifungal potential against strains of C. albicans. Citral’s mechanism of action does not involve the cell wall or ergosterol, and further study is needed to completely describe its effects before being used in the future as a component of new antifungals.

  17. New imidazolidineiminothione derivatives: Synthesis, spectral characterization and evaluation of antitumor, antiviral, antibacterial and antifungal activities.

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    Moussa, Ziad; El-Sharief, Marwa A M Sh; Abbas, Samir Y

    2016-10-21

    A series of new imidazolidineiminothione derivatives with various halogenated and alkylated aromatic substituents at N-(1) and at N-(3) was synthesized through the reaction of N-arylcyanothioformamides with arylisocyanate derivatives. Structure of imidazolidineiminothione derivatives were established based on spectroscopic IR, (1)H NMR, (13)C NMR, (1)H,(1)H-COSY, HSQC, (19)F NMR, MS and elemental analyses data. Evaluation of antitumor, antiviral, antibacterial and antifungal activities for the synthesized compounds were carried out to probe their activities. Most of the synthesized compounds displayed antitumor activity. The presence of 3,5-dichlorophenyl moiety at N-(1) and trichlorophenyl moiety on N-(3) (2f) resulted the highest cytotoxic activity. The presence of 9H-fluorenyl moiety on N-(3) resulted in the lowest cytotoxic activity. The antiviral screening displayed that 2d and 2f were markedly active against one or two viral strains. Compound 2d (3,5-dichlorophenyl moiety at N-(1) and 4-chlorophenyl moiety on N-(3)) showed 100% antiviral effect toward HAV. Compound 2f showed 96.7% antiviral effect toward HSV1 and 80.3% antiviral effect toward HAV. The antimicrobial activity suggested that all of the imidazolidineiminothione derivatives possess significant antimicrobial activity against most of the test organisms. Some imidazolidineiminothione derivatives showed MIC values of antibacterial and antifungal activities ranged from 0.78 to 6.25 μg/ml.

  18. Molecular Design, Structural Analysis and Antifungal Activity of Derivatives of Peptide CGA-N46.

    Science.gov (United States)

    Li, Rui-Fang; Lu, Zhi-Fang; Sun, Ya-Nan; Chen, Shi-Hua; Yi, Yan-Jie; Zhang, Hui-Ru; Yang, Shuo-Ye; Yu, Guang-Hai; Huang, Liang; Li, Chao-Nan

    2016-09-01

    Chromogranin A (CGA)-N46, a derived peptide of human chromogranin A, has antifungal activity. To further research the active domain of CGA-N46, a series of derivatives were designed by successively deleting amino acid from both terminus of CGA-N46, and the amino acid sequence of each derivative was analyzed by bioinformatic software. Based on the predicted physicochemical properties of the peptides, including half-life time in mammalian reticulocytes (in vitro), yeast (in vivo) and E. coli (in vivo), instability index, aliphatic index and grand average of hydropathicity (GRAVY), the secondary structure, net charge, the distribution of hydrophobic residues and hydrophilic residues, the final derivatives CGA-N15, CGA-N16, CGA-N12 and CGA-N8 were synthesized by solid-phase peptide synthesis. The results of bioinformatic analysis showed that CGA-N46 and its derivatives were α-helix, neutral or weak positive charge, hydrophilic, and CGA-N12 and CGA-N8 were more stable than the other derivatives. The results of circular dichroism confirmed that CGA-N46 and its derived peptides displayed α-helical structure in an aqueous solution and 30 mM sodium dodecylsulfate, but α-helical contents decreased in hydrophobic lipid vesicles. CGA-N15, CGA-N16, CGA-N12 and CGA-N8 had higher antifungal activities than their mother peptide CGA-N46. Among of the derived peptides, CGA-N12 showed the least hemolytic activity. In conclusion, we have successfully identified the active domain of CGA-N46 with strong antifungal activity and weak hemolytic activity, which provides the possibility to develop a new class of antibiotics.

  19. A Review on Antibacterial, Antiviral, and Antifungal Activity of Curcumin

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    Soheil Zorofchian Moghadamtousi

    2014-01-01

    Full Text Available Curcuma longa L. (Zingiberaceae family and its polyphenolic compound curcumin have been subjected to a variety of antimicrobial investigations due to extensive traditional uses and low side effects. Antimicrobial activities for curcumin and rhizome extract of C. longa against different bacteria, viruses, fungi, and parasites have been reported. The promising results for antimicrobial activity of curcumin made it a good candidate to enhance the inhibitory effect of existing antimicrobial agents through synergism. Indeed, different investigations have been done to increase the antimicrobial activity of curcumin, including synthesis of different chemical derivatives to increase its water solubility as well ass cell up take of curcumin. This review aims to summarize previous antimicrobial studies of curcumin towards its application in the future studies as a natural antimicrobial agent.

  20. HAMLET - A protein-lipid complex with broad tumoricidal activity.

    Science.gov (United States)

    Ho, James C S; Nadeem, Aftab; Svanborg, Catharina

    2017-01-15

    HAMLET (Human Alpha-lactalbumin Made LEthal to Tumor cells) is a tumoricidal protein-lipid complex with broad effects against cancer cells of different origin. The therapeutic potential is emphasized by a high degree of specificity for tumor tissue. Here we review early studies of HAMLET, in collaboration with the Orrenius laboratory, and some key features of the subsequent development of the HAMLET project. The early studies focused on the apoptotic response that accompanies death in HAMLET treated tumor cells and the role of mitochondria in this process. In subsequent studies, we have identified a sequence of interactions that starts with the membrane integration of HAMLET and the activation of ion fluxes followed by HAMLET internalization, progressive inhibition of MAPK kinases and GTPases and sorting of HAMLET to different cellular compartments, including the nuclei. Therapeutic efficacy of HAMLET has been demonstrated in animal models of glioblastoma, bladder cancer and intestinal cancer. In clinical studies, HAMLET has been shown to target skin papillomas and bladder cancers. The findings identify HAMLET as a new drug candidate with promising selectivity for cancer cells and a strong therapeutic potential.

  1. Antimicrobial and Antifungal Activity of Pelargonium roseum Essential Oils

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    Gâlea Carmen

    2014-12-01

    Conclusion: The volatile oils exhibited considerable inhibitory effects against all the organisms under test, in some cases comparable with those of the reference antibiotics. There were no considerable differences between the antimicrobial activities of the oil obtained by distillation and commercially available Pelargonium oils.

  2. Evaluation of antibacterial and antifungal activities of olive (Olea europaea essential oil

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    R K Upadhyay

    2014-01-01

    Full Text Available Context: Essential oil Olea europaea was investigated for its antibacterial and antifungal activities. Aim: To evaluate antimicrobial activity of O. europaea essential oil against infectious microbial pathogens. Settings and Design: Seeds of O. europaea were grounded by using domestic mixer and powdered material was hydro-distilled in Clevenger apparatus continuously for 5 hrs to yield essential oil. Essential oil was analysed on Gas-Chromatography-Mass spectrometry (GC-MS from which 24 components were identified, representing total 99.98% of the oil. Extracted oil was evaluated for their antibacterial and antifungal activities. Materials and Methods: Paper disc diffusion and serial micro-dilution assays were performed for the determination of inhibition zone diameters and minimal inhibitory concentration, respectively. Results: The O. europaea essential oil showed the diameter of inhibition zone (DIZ ranging from 19.4 ± 0.07-26.4 ± 0.09 mm at a concentration level of 28 μg/disc (W/V separately in all the ten strains tested. The minimum inhibitory concentration of essential oil against bacterial strains was obtained in a range of 7.0-56.0 μg/ml while in and fungal strains it was in a range of 7.0-28 μg/ml. Statistical analysis: All statistical calculations are expressed as mean ± SE of three replicates. Data were analyzed by one-way Analysis of Variance (ANOVA to locate significant variations in oil activity in various bacterial and fungal strains followed by the Duncan′s multiple range tests. Conclusions: Antibacterial and antifungal activities of O. europaea essential oil are due to the presence of certain secondary plant metabolites such as terpenoids, steroids and flavonoids, esters, and acids, which were identified in the essential oil. The oil components can be further investigated for their biological activities and study to overcome the problem of drug resistance in microbes.

  3. Synthesis, antifungal activity, and QSAR studies of 1,6-dihydropyrimidine derivatives

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    Chirag Rami

    2013-01-01

    Full Text Available Introduction: A practical synthesis of pyrimidinone would be very helpful for chemists because pyrimidinone is found in many bioactive natural products and exhibits a wide range of biological properties. The biological significance of pyrimidine derivatives has led us to the synthesis of substituted pyrimidine. Materials and Methods: With the aim of developing potential antimicrobials, new series of 5-cyano-6-oxo-1,6-dihydro-pyrimidine derivatives namely 2-(5-cyano-6-oxo-4-substituted (aryl-1,6-dihydropyrimidin-2-ylthio-N-substituted (phenyl acetamide (C1-C41 were synthesized and characterized by Fourier transform infrared spectroscopy (FTIR, mass analysis, and proton nuclear magnetic resonance ( 1 H NMR. All the compounds were screened for their antifungal activity against Candida albicans (MTCC, 227. Results and Discussion: Quantitative structure activity relationship (QSAR studies of a series of 1,6-dihydro-pyrimidine were carried out to study various structural requirements for fungal inhibition. Various lipophilic, electronic, geometric, and spatial descriptors were correlated with antifungal activity using genetic function approximation. Developed models were found predictive as indicated by their square of predictive regression values (r 2pred and their internal and external cross-validation. Study reveals that CHI_3_C, Molecular_SurfaceArea, and Jurs_DPSA_1 contributed significantly to the activity along with some electronic, geometric, and quantum mechanical descriptors. Conclusion: A careful analysis of the antifungal activity data of synthesized compounds revealed that electron withdrawing substitution on N-phenyl acetamide ring of 1,6-dihydropyrimidine moiety possess good activity.

  4. ANTIFUNGAL ACTIVITY OF ROSEMARY ESSENTIAL OIL AGAINST FOODSTUFFS FUNGI

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    L. Vallone

    2009-06-01

    Full Text Available The essential oils are well known for their antibacteric, antomycotic and insecticide effects. In this research the antomycotic activity of Rosemary essential oil has been tested in vitro versus different moulds, common contaminants of food and feed, as Aspergillus flavus, Aspergillus ochraceus, Aspergillus niger, Aspergillus ustus, Penicillium expansum, Penicillium aurantio-griseum, Fusarium moniliforme. The Rosemary essential oil tested (produced in Sardegna, Italy shows a different efficacy against various moulds and his activity seems to be produced by borneol, α-pinene, eucalyptol, camphor and limonene. Aspergillus and Penicillium are the genus showing an important inhibition of their development in vitro. Rosemary essential oil for these natural properties can be used as antimycotic additive to extended shelf-life of many foodstuffs.

  5. Differential antifungal activity of isomeric forms of nystatin.

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    Ostrosky-Zeichner, L; Bazemore, S; Paetznick, V L; Rodriguez, J R; Chen, E; Wallace, T; Cossum, P; Rex, J H

    2001-10-01

    When nystatin is placed in RPMI and other biological fluids, there is loss of pure nystatin, with the development of two distinguishable chromatographic peaks, 1 and 2. Peak 1 appears identical to commercially prepared nystatin. By nuclear magnetic resonance (NMR) and mass spectral analysis, peak 2 appears to be an isomer of peak 1. The isomers are quantitatively and fully interconvertible. Formation of peak 2 is accelerated at a pH of >7.0 and ultimately reaches a near 55:45 (peak 1/peak 2 ratio) mixture. We sought to determine the relative activities of peaks 1 and 2 against Candida spp. Peak 2 consistently showed higher MICs when it was the predominant form during the experiment. Time-kill analyses showed that peak 2 required > or =8 x the concentration of peak 1 to produce a modest and delayed killing effect, which was never of the same magnitude as that produced by peak 1. In both types of assays, the activity of peak 2 corresponded with intra-assay formation of peak 1. Both MIC measurements and time-kill analysis suggest that peak 2 has considerably less activity, if any at all, against Candida spp. Peak 2 may serve as a reservoir for peak 1.

  6. Antifungal and antibacterial activities of Mexican tarragon (Tagetes lucida).

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    Céspedes, Carlos L; Avila, J Guillermo; Martínez, Andrés; Serrato, Blanca; Calderón-Mugica, José C; Salgado-Garciglia, Rafael

    2006-05-17

    Mexican tarragon (Tagetes lucida Cv. Asteraceae: Campanulatae) is an important, nutritious plant and an effective herbal medicine. Seven coumarins, 7,8-dihydroxycoumarin (4), umbelliferone (7-hydroxycoumarin) (5), scoparone (6,7-dimethoxycoumarin) (7), esculetin (6,7-dihydroxycoumarin) (11), 6-hydroxy-7-methoxycoumarin (12), herniarin (7-methoxycoumarin) (13), and scopoletin (6-methoxy-7-hydroxycoumarin) (14), and three flavonoids, patuletin (18), quercetin (19), and quercetagetin (20), were isolated from CH2Cl2 and MeOH extracts from aerial parts of T. lucida. In addition, 6,7-diacetoxy coumarin (15), 6-methoxy-7-acetylcoumarin (16), and 6-acetoxy-7-methoxycoumarin (17) derivatives were synthesized. 8-Methoxypsoralen (1), 8-acetyl-7-hydroxycoumarin (2), 7,8-dihydroxy-6-meth-oxycoumarin (3), 6,7-dimethoxy-4-methylcoumarin (6), 5,7-dihydroxy-4-methylcoumarin (8), 4-hydroxycoumarin (9), 4-hydroxy-6,7-dimethylcoumarin (10), naringenin (21), glycoside-7-rhamnonaringin (22), and rutin (23) were commercially obtained (Sigma-Aldrich). All of these compounds and extracts (M1 and M2) were assayed against bacteria and fungi. The antibacterial activity was determined on Bacillus subtilis, Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, Salmonella typhi, Salmonella sp., Shigella boydii, Shigella sp., Enterobacter aerogenes, Enterobacter agglomerans, Sarcina lutea, Staphylococcus epidermidis, Staphylococcus aureus, Yersinia enterolitica, Vibrio cholerae (three El Tor strains, CDC-V12, clinic case, and INDRE-206, were obtained from contaminated water), and V. cholerae (NO-O1). The evaluated fungi were Aspergillus niger, Penicillium notatum, Fusarium moniliforme, Fusarium sporotrichum, Rhizoctonia solani, and Trichophyton mentagrophytes. The most active compounds against Gram-positive and -negative bacteria were the dihydroxylated coumarins 3 and 4. In addition, 2-4, 6, 7, and 11 showed an interesting activity against V. cholerae, a key bacterium in the contaminated

  7. Berberine Antifungal Activity in Fluconazole-Resistant Pathogenic Yeasts: Action Mechanism Evaluated by Flow Cytometry and Biofilm Growth Inhibition in Candida spp.

    Science.gov (United States)

    da Silva, Anderson Ramos; de Andrade Neto, João Batista; da Silva, Cecília Rocha; Campos, Rosana de Sousa; Costa Silva, Rose Anny; Freitas, Daniel Domingues; do Nascimento, Francisca Bruna Stefany Aires; de Andrade, Larissa Nara Dantas; Sampaio, Letícia Serpa; Grangeiro, Thalles Barbosa; Magalhães, Hemerson Iury Ferreira; Cavalcanti, Bruno Coêlho; de Moraes, Manoel Odorico; Nobre Júnior, Hélio Vitoriano

    2016-06-01

    The incidence of fungal infections and, in particular, the incidence of fungal antibiotic resistance, which is associated with biofilm formation, have significantly increased, contributing to morbidity and mortality. Thus, new therapeutic strategies need to be developed. In this context, natural products have emerged as a major source of possible antifungal agents. Berberine is a protoberberine-type isoquinoline alkaloid isolated from the roots, rhizomes, and stem bark of natural herbs, such as Berberis aquifolium, Berberis vulgaris, Berberis aristata, and Hydrastis canadensis, and of Phellodendron amurense Berberine has been proven to have broad antibacterial and antifungal activity. In the present study, the potential antifungal effect of berberine against fluconazole-resistant Candida and Cryptococcus neoformans strains, as well as against the biofilm form of Candida spp., was assessed. The antifungal effect of berberine was determined by a broth microdilution method (the M27-A3 method of the Clinical and Laboratory Standards Institute) and flow cytometry techniques, in which the probable mechanism of action of the compound was also assessed. For biofilm assessment, a colorimetric 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was used to determine the susceptibility of sessile cells. The isolates used in the study belonged to the Laboratory of Bioprospection and Experiments in Yeast (LABEL) of the Federal University of Ceará. After 24 and 72 h, fluconazole-resistant Candida and Cryptococcus neoformans strains showed berberine MICs equal to 8 μg/ml and 16 μg/ml, respectively. Cytometric analysis showed that treatment with berberine caused alterations to the integrity of the plasma and mitochondrial membranes and DNA damage, which led to cell death, probably by apoptosis. Assessment of biofilm-forming isolates after treatment showed statistically significant reductions in biofilm cell activity (P < 0.001).

  8. Characterization of a New Sesquiterpene and Antifungal Activities of Chemical Constituents from Dryopteris fragrans (L. Schott

    Directory of Open Access Journals (Sweden)

    Yu-Hong Huang

    2014-01-01

    Full Text Available One new sesquiterpene and six known compounds were isolated from Dryopteris fragrans (L. Schot. They were identified as 3-O-β-D-glucopyranosylalbicanol- 11-O-β-D-glucopyranoside (1, dihydroconiferylalcohol (2, (E-3-(4-hydroxyphenylacrylic acid (3, esculetin (4, 5,7-dihydroxy-2-hydroxymethylchromone (5, eriodictyol (6 and isoorientin (7 by UV, MS, 1D-NMR and 2D-NMR spectroscopy. The antifungal activities of the seven isolated compounds were screened. Compounds 2, 3, 4 and 5 showed obvious activities against Microsporum canis and Epidermophyton floccosum.

  9. Antibacterial and antifungal activity of a soda-lime glass containing copper nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Esteban-Tejeda, L; Pecharroman, C; Moya, J S [Instituto de Ciencia de Materiales de Madrid, CSIC, Sor Juana Ines de la Cruz 3, Cantoblanco, Madrid 28049 (Spain); Malpartida, F [Centro Nacional de Biotecnologia, CSIC, Darwin 3, Cantoblanco, Madrid 28049 (Spain); Esteban-Cubillo, A, E-mail: jsmoya@icmm.csic.es [Tolsa S A R and D Department, Camino de Vallecas-Mejorada del Campo Km 1.6, 28031 Madrid (Spain)

    2009-12-16

    A low melting point soda-lime glass powder containing copper nanoparticles with high antibacterial (against gram-positive and gram-negative bacteria) and antifungal activity has been obtained. Sepiolite fibres containing monodispersed copper nanoparticles (d{sub 50}{approx}30 {+-} 5 nm) were used as the source of the copper nanoparticles. The observed high activity of the obtained glass powder, particularly against yeast, has been explained by considering the inhibitory synergistic effect of the Ca{sup 2+} lixiviated from the glass on the growth of the colonies.

  10. Synthesis and antifungal activity of new bis-{gamma}-lactones analogous to avenaciolide

    Energy Technology Data Exchange (ETDEWEB)

    Magaton, Andreia da Silva; Rubinger, Mayura M. M.; Macedo Junior, Fernando C. de [Vicosa Univ., MG (Brazil). Dept. de Quimica]. E-mail: mayura@ufv.br; Zambolim, Laercio [Vicosa Univ., MG (Brazil). Dept. de Fitopatologia

    2007-03-15

    In a study of the antifungal activity of selected compounds as potentials agrochemicals, we have prepared and characterized by elemental analyses, infrared and NMR spectroscopies three new bis-{gamma}-lactones analogous to avenaciolide, where the octyl group of this natural product was replaced by heptyl, hexyl and pentyl groups. The effects on the mycelia development and conidia germination of Colletotrichum gloesporioides of these compounds and their synthetic precursors were evaluated in vitro. The title compounds were active in the tested conditions, while all the synthetic precursors were inactive. The preparation and characterization of 15 new synthetic intermediates are also described. (author)

  11. Antifungal activity of acetone extracts from Punica granatum L., Quercus suber L. and Vicia faba L.

    Science.gov (United States)

    Akroum, S

    2017-03-01

    Human and animal mycoses become more frequent and more resistant to traditional treatments. In this work, we tested the in vitro antifungal activity of acetonic extracts of Punica granatum L., Quercus suber L. and Vicia faba L. against seven pathogen fungi and the in vivo antifungal activity against Candida albicans and Trichophyton mentagrophytes. The phytochemical screening was also carried out and showed that the extracts contained mainly proanthocyanidins. Other polyphenols were also present but in low quantity. The acetone extract of V. faba L. gave a good in vitro inhibition of yeasts and was the most active for treating candidiasis in mice. It decreased the percentage of mortality with only 20μg. But the in vivo antifungal activity of this extract on T. mentagrophytes was low. It only showed a small diminution of crusting and erythema after the administration of 100μg. On the contrary, the acetone extracts of P. granatum L. had a poor activity against yeasts and a better one against moulds. It gave the best in vivo antifungal activity against T. mentagrophytes by healing animals with 40μg. The extract of P. granatum L. gave also an interesting in vivo antifungal activity against T. mentagrophytes with an active dose of 80μg.

  12. Antifungal activity of eugenol analogues. Influence of different substituents and studies on mechanism of action.

    Science.gov (United States)

    Carrasco, Héctor; Raimondi, Marcela; Svetaz, Laura; Di Liberto, Melina; Rodriguez, María V; Espinoza, Luis; Madrid, Alejandro; Zacchino, Susana

    2012-01-19

    Twenty one phenylpropanoids (including eugenol and safrole) and synthetic analogues, thirteen of them new compounds, were evaluated for antifungal properties, first with non-targeted assays against a panel of human opportunistic pathogenic fungi. Some structure-activity relationships could be observed, mainly related to the influence of an allyl substituent at C-4, an OH group at C-1 and an OCH(3) at C-2 or the presence of one or two NO(2) groups in different positions of the benzene ring. All active compounds were tested in a second panel of clinical isolates of C. albicans and non-albicans Candida spp., Cryptococcus neoformans and dermatophytes. The eugenol derivative 4-allyl-2-methoxy-5-nitrophenol (2) was the most active structure against all strains tested, and therefore it was submitted to targeted assays. These studies showed that the antifungal activity of 2 was not reversed in the presence of an osmotic support such as sorbitol, suggesting that it does not act by inhibiting the fungal cell wall synthesis or assembly. On the other hand, the Ergosterol Assay showed that 2 did not bind to the main sterol of the fungal membrane up to 250 µg mL-1. In contrast, a 22% of fungal membrane damage was observed at concentrations = 1 × MIC and 71% at 4× MIC, when 2 was tested in the Cellular Leakage assay. The comparison of log P and MICs for all compounds revealed that the antifungal activity of the eugenol analogues would not to be related to lipophilicity.

  13. Antifungal Activity of Eugenol Analogues. Influence of Different Substituents and Studies on Mechanism of Action

    Directory of Open Access Journals (Sweden)

    Melina Di Liberto

    2012-01-01

    Full Text Available Twenty one phenylpropanoids (including eugenol and safrole and synthetic analogues, thirteen of them new compounds, were evaluated for antifungal properties, first with non-targeted assays against a panel of human opportunistic pathogenic fungi. Some structure-activity relationships could be observed, mainly related to the influence of an allyl substituent at C-4, an OH group at C-1 and an OCH3 at C-2 or the presence of one or two NO2 groups in different positions of the benzene ring. All active compounds were tested in a second panel of clinical isolates of C. albicans and non-albicans Candida spp., Cryptococcus neoformans and dermatophytes. The eugenol derivative 4-allyl-2-methoxy-5-nitrophenol (2 was the most active structure against all strains tested, and therefore it was submitted to targeted assays. These studies showed that the antifungal activity of 2 was not reversed in the presence of an osmotic support such as sorbitol, suggesting that it does not act by inhibiting the fungal cell wall synthesis or assembly. On the other hand, the Ergosterol Assay showed that 2 did not bind to the main sterol of the fungal membrane up to 250 µg mL−1. In contrast, a 22% of fungal membrane damage was observed at concentrations = 1 × MIC and 71% at 4× MIC, when 2 was tested in the Cellular Leakage assay. The comparison of log P and MICs for all compounds revealed that the antifungal activity of the eugenol analogues would not to be related to lipophilicity.

  14. Antibacterial and Antifungal Activity of ZnO Containing Glasses.

    Science.gov (United States)

    Esteban-Tejeda, Leticia; Prado, Catuxa; Cabal, Belén; Sanz, Jesús; Torrecillas, Ramón; Moya, José Serafín

    2015-01-01

    A new family of non-toxic biocides based on low melting point (1250°C) transparent glasses with high content of ZnO (15-40wt%) belonging to the miscibility region of the B2O3-SiO2-Na2O-ZnO system has been developed. These glasses have shown an excellent biocide activity (logarithmic reduction >3) against Gram- (E. coli), Gram+ (S. aureus) and yeast (C. krusei); they are chemically stable in different media (distilled water, sea-like water, LB and DMEN media) as well as biocompatible. The cytotoxicity was evaluated by the Neutral Red Uptake using NIH-3T3 (mouse embryonic fibroblast cells) and the cell viability was >80%. These new glasses can be considered in several and important applications in the field of inorganic non-toxic biocide agents such as medical implants, surgical equipment, protective apparels in hospitals, water purifications systems, food packaging, food storages or textiles.

  15. Mutational analysis of a plant defensin from radish (Raphanus sativus L.) reveals two adjacent sites important for antifungal activity.

    Science.gov (United States)

    De Samblanx, G W; Goderis, I J; Thevissen, K; Raemaekers, R; Fant, F; Borremans, F; Acland, D P; Osborn, R W; Patel, S; Broekaert, W F

    1997-01-10

    Mutational analysis of Rs-AFP2, a radish antifungal peptide belonging to a family of peptides referred to as plant defensins, was performed using polymerase chain reaction-based site-directed mutagenesis and yeast as a system for heterologous expression. The strategy followed to select candidate amino acid residues for substitution was based on sequence comparison of Rs-AFP2 with other plant defensins exhibiting differential antifungal properties. Several mutations giving rise to peptide variants with reduced antifungal activity against Fusarium culmorum were identified. In parallel, an attempt was made to construct variants with enhanced antifungal activity by substituting single amino acids by arginine. Two arginine substitution variants were found to be more active than wild-type Rs-AFP2 in media with high ionic strength. Our data suggest that Rs-AFP2 possesses two adjacent sites that appear to be important for antifungal activity, namely the region around the type VI beta-turn connecting beta-strands 2 and 3, on the one hand, and the region formed by residues on the loop connecting beta-strand 1 and the alpha-helix and contiguous residues on the alpha-helix and beta-strand 3, on the other hand. When added to F. culmorum in a high ionic strength medium, Rs-AFP2 stimulated Ca2+ uptake by up to 20-fold. An arginine substitution variant with enhanced antifungal activity caused increased Ca2+ uptake by up to 50-fold, whereas a variant that was virtually devoid of antifungal activity did not stimulate Ca2+ uptake.

  16. Study of the antibacterial and antifungal activities of synthetic benzyl bromides, ketones, and corresponding chalcone derivatives

    Science.gov (United States)

    Shakhatreh, Muhamad Ali K; Al-Smadi, Mousa L; Khabour, Omar F; Shuaibu, Fatima A; Hussein, Emad I; Alzoubi, Karem H

    2016-01-01

    Several applications of chalcones and their derivatives encouraged researchers to increase their synthesis as an alternative for the treatment of pathogenic bacterial and fungal infections. In the present study, chalcone derivatives were synthesized through cross aldol condensation reaction between 4-(N,N-dimethylamino)benzaldehyde and multiarm aromatic ketones. The multiarm aromatic ketones were synthesized through nucleophilic substitution reaction between 4-hydroxy acetophenone and benzyl bromides. The benzyl bromides, multiarm aromatic ketones, and corresponding chalcone derivatives were evaluated for their activities against eleven clinical pathogenic Gram-positive, Gram-negative bacteria, and three pathogenic fungi by the disk diffusion method. The minimum inhibitory concentration was determined by the microbroth dilution technique. The results of the present study demonstrated that benzyl bromide derivatives have strong antibacterial and antifungal properties as compared to synthetic chalcone derivatives and ketones. Benzyl bromides (1a and 1c) showed high ester activity against Gram-positive bacteria and fungi but moderate activity against Gram-negative bacteria. Therefore, these compounds may be considered as good antibacterial and antifungal drug discovery. However, substituted ketones (2a–b) as well as chalcone derivatives (3a–c) showed no activity against all the tested strains except for ketone (2c), which showed moderate activity against Candida albicans. PMID:27877017

  17. Sulfonylureas have antifungal activity and are potent inhibitors of Candida albicans acetohydroxyacid synthase.

    Science.gov (United States)

    Lee, Yu-Ting; Cui, Chang-Jun; Chow, Eve W L; Pue, Nason; Lonhienne, Thierry; Wang, Jian-Guo; Fraser, James A; Guddat, Luke W

    2013-01-10

    The sulfonylurea herbicides exert their activity by inhibiting plant acetohydroxyacid synthase (AHAS), the first enzyme in the branched-chain amino acid biosynthesis pathway. It has previously been shown that if the gene for AHAS is deleted in Candida albicans , attenuation of virulence is achieved, suggesting AHAS as an antifungal drug target. Herein, we have cloned, expressed, and purified C. albicans AHAS and shown that several sulfonylureas are inhibitors of this enzyme and possess antifungal activity. The most potent of these compounds is ethyl 2-(N-((4-iodo-6-methoxypyrimidin-2-yl)carbamoyl)sulfamoyl)benzoate (10c), which has a K(i) value of 3.8 nM for C. albicans AHAS and an MIC₉₀ of 0.7 μg/mL for this fungus in cell-based assays. For the sulfonylureas tested there was a strong correlation between inhibitory activity toward C. albicans AHAS and fungicidal activity, supporting the hypothesis that AHAS is the target for their inhibitory activity within the cell.

  18. The study of anticancer and antifungal activities of Pistacia integerrima extract In vitro

    Directory of Open Access Journals (Sweden)

    Y Bibi

    2012-01-01

    Full Text Available Pistacia integerrima Stew. ex Brand (Anacardiaceae is an ethanobotanically important plant species traditionally used in the treatment of chronic wounds, jaundice, dysentery, etc. The crude extract from Pistacia integerrima and its fractions were tested for cytotoxic activity against Michigan Cancer Foundation-7 human breast cancer cell line. We have also investigated that crude stem extract of this plant also exhibits the antitumour as well as antifungal potential activities. Moreover, we have also studied that the crude extract inhibited Michigan Cancer Foundation-7 cell viability in a dose-dependent manner; the poor toxicity (1.6% at 10 μg/ml to moderate toxicity (55.4% at 100 μg/ml. The IC 50 values calculated were 90.9 μg/ml. The ethyl acetate and chloroform fractions at a concentration of 200 μg/ml showed ~100 and 97.4% inhibition against Michigan Cancer Foundation-7 cell line, respectively. The crude methanol extract also showed good antitumour (IC 50 125 ppm activity, but weak antifungal activity. These findings reveal that the ethyl acetate and chloroform fractions of Pistacia integerrima are potent cytotoxic fractions, and could be an alternate candidate for the development of novel biologically active compounds.

  19. Antitumor and antifungal activities of organic extracts of seacucumber Holothuria atra from the southeast coast of India

    Science.gov (United States)

    Dhinakaran, Devaraj Isaac; Lipton, Aaron Premnath

    2015-02-01

    In phylum Echinodermata, the family Holothuridae is distinguished by its capacity of bioactive compounds. Sea cucumber Holothuria atra is commonly known as the lollyfish. The antifungal activity was detected using agar well diffusion method against the various fungal strains such as Trichoderma viride, Aspergillus niger, Aspergillus flavis, Candida albicans and Penicillium chrysogenum. Relatively high antifungal activity was seen against Candida albicans at 100 μL-1 concentration of extracts. Zone of inhibition was measured at 18 mm of diameter. The anti-tumor activities were detected against the Vero and Hep2 cell lines using MTT assay. The cells were treated with H. atra extract at concentrations 0.078-10mg mL-1. The extract showed high proliferative activity against the Hep2 cells. The body wall extracts of sea cucumber ( H. atra) showed effective antifungal and antitumor activities. All these findings suggest that the extracts could be used for the development of drugs.

  20. 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.

  1. 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

  2. Synthesis and in vitro assessment of antifungal activity of oximes, oxime ethers and isoxazoles.

    OpenAIRE

    Diaz-Velandia, John; Laboratorio de síntesis orgánica, Departamento de Química. Facultad de Ciencias, Pontificia Universidad Javeriana, Bogotá, D.C., Colombia.; Durán-Díaz, Natalia; Laboratorio de síntesis orgánica, Departamento de Química. Facultad de Ciencias, Pontificia Universidad Javeriana, Bogotá, D.C., Colombia.; Robles-Camargo, Jorge; Laboratorio de síntesis orgánica, Departamento de Química. Facultad de Ciencias, Pontificia Universidad Javeriana, Bogotá, D.C., Colombia.; Loaiza, Alix Elena; Laboratorio de síntesis orgánica, Departamento de Química. Facultad de Ciencias, Pontificia Universidad Javeriana, Bogotá, D.C., Colombia

    2011-01-01

    Objective. To synthesize and carry out a preliminary evaluation of the in vitro antifungal activity of oximes, oxime ethers and isoxazoles. Materials and methods. Oximes were synthesized from aldehydes or ketones with NH2OH.HCl and K2CO3. Oxime ethers were prepared by alkylation of oximes with propargyl bromide or 2-bromobenzyl bromide, using NaOH as base and acetone as solvent. The isoxazoles were obtained by 1,3-dipolar cycloadditions using ceric ammonium nitrate (CAN), chloramine T (CA...

  3. Antifungal activity of the essential oil of Thymus vulgaris L. and thymol on experimentally induced dermatomycoses.

    Science.gov (United States)

    Soković, M; Glamoclija, J; Cirić, A; Kataranovski, D; Marin, P D; Vukojević, J; Brkić, D

    2008-12-01

    The in vivo evaluation of the toxicological and antifungal activity of the essential oil of Thymus vulgaris L. and its main component thymol was made on 2-month-old male Wistar rats. We examined the therapeutic potency against experimentally induced dermatomycoses in rats, using the most frequent dermatomycetes, Trichophyton mentagrophytes, T. rubrum, and T. tonsurans. The therapeutic efficacy of a 1% solution of the essential oil of Thymus vulgaris and thymol as well as the commercial preparation bifonazole was evaluated. During the 37-day observation period the oil-treated animals were cured.

  4. In vitro activities of eight antifungal drugs against 106 waterborne and cutaneous exophiala species.

    Science.gov (United States)

    Najafzadeh, M J; Saradeghi Keisari, M; Vicente, V A; Feng, P; Shamsian, S A A; Rezaei-Matehkolaei, A; de Hoog, G S; Curfs-Breuker, I; Meis, J F

    2013-12-01

    The in vitro activities of eight antifungal drugs against 106 clinical and environmental isolates of waterborne and cutaneous Exophiala species were tested. The MICs and minimum effective concentrations for 90% of the strains tested (n = 106) were, in increasing order, as follows: posaconazole, 0.063 μg/ml; itraconazole, 0.25 μg/ml; micafungin, 1 μg/ml; voriconazole, 2 μg/ml; isavuconazole, 4 μg/ml; caspofungin, 8 μg/ml; amphotericin B, 16 μg/ml; fluconazole, 64 μg/ml.

  5. STEROIDAL GLYCOSIDES FROM THE SEEDS OF HYOSCYAMUS NIGER L. AND THEIR ANTIFUNGAL ACTIVITY

    Directory of Open Access Journals (Sweden)

    Irina Lunga

    2007-06-01

    Full Text Available Phytochemical analysis of the seeds of Hyocyamus niger L. (Solonaceae resulted in the isolation of six steroidal glycosides, two furostanol (1, 2 and four spirostanol saponins (3, 4, 5, 6, which were found in this plant for the first time. The structures of these compounds were determined by detailed analysis of their spectral data, including two-dimensional NMR spectroscopy and MS spectroscopy. The antifungal activity of a crude steroidal glycoside extract, fractions of spirostanoles and individual glicosides was investigated in vitro against a panel of human pathogenic fungi, yeasts as well as dermatophytes and filamentous species.

  6. Synthesis and antifungal activity of novel (1-aryl-2-heterocyclyl)ethylideneaminooxymethyl-substituted dioxolanes

    Energy Technology Data Exchange (ETDEWEB)

    Baji, H.; Flammang, M.; Kimny, T.; Gasquez, F.; Compagnon, P.L.; Delcourt, A. [Dijon Univ., 21 (France)

    1995-12-31

    A novel series of (1-aryl-2-heterocyclyl)ethylideneaminooxymethyl -substituted dioxolanes IIIa-n were synthesized by condensation of substituted 1,3-dioxolan-4-ylmethyl p-toluenesulfonates 4 with 1-(hydroxyimino)-1-aryl-2-heterocyclylethanes 5. Compounds IIIa-n were found to have effective in vitro antifungal activity when evaluated against the pathogenic fungi Candida albicans, Aspergillus flavus and Fusarium solani with MIC (minimum inhibitory concentration) values of 10 {mu}g-ml{sup -1} for IIIa-I and 5 {mu}g-ml{sup -1} for IIIm,n. (authors). 24 refs., 4 figs., 5 tabs.

  7. Synthesis, antimicrobial and antifungal activities of novel 1H-1,4-diazepines containing pyrazolopyrimidinone moiety

    Indian Academy of Sciences (India)

    Rajesh Kumar; Yogesh Chandra Joshi

    2009-07-01

    Acylation of 5-(2-ethoxyphenyl)-1-methyl-3-propyl-1,6-dihydro-7-pyrazolo [4,3-d) pyrimidin-7-one 1 with chloroacetylchloride in the presence of anyhydrous aluminium chloride affords 5-[(5-chloroacetyl-2-ethoxy)phenyl]-1-methyl-3-propyl-1,6-dihydro-7H-pyrazolo [4,3-d] pyrimidin-7-one 2. The compound 2 condensed with various -diketones/-ketoesters compound, to obtain new -diketones/-ketoesters 4a-i treated with ethylenediamine (EDA) gives 1H-1,4-diazepines. The compounds 5a-i has been screened for antimicrobial, antifungal and anthelmintic activities.

  8. 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

  9. 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

  10. Composition and antifungal activity of the essential oil from the rhizome and roots of Ferula hermonis.

    Science.gov (United States)

    Al-Ja'fari, Abdel-Hadi; Vila, Roser; Freixa, Blanca; Tomi, Felix; Casanova, Joseph; Costa, Joan; Cañigueral, Salvador

    2011-08-01

    The analysis of the essential oil from rhizome and roots of Ferula hermonis Boiss. (Apiaceae) by GC-FID, GC-MS and ¹³C NMR allowed the identification of 79 constituents, more than 90% of the oil, the major one being α-pinene (43.3%), followed by α-bisabolol (11.1%) and the unusual acetylenic compound 3,5-nonadiyne (4.4%). The antifungal activity of the essential oil before and after fractionation was assayed against several yeasts and filamentous fungi. Purification of the active fractions afforded 3,5-nonadiyne, α-bisabolol, jaeschkeanadiol angelate, α-bisabolol oxide B and trans-verbenol, as well as two purified fractions, one of them (JB73) with 73% of jaeschkeanadiol benzoate and the other with 50% of spathulenol. Determination of MIC and MFC values of all these products evidenced strong antifungal activities for JB73 and 3,5-nonadiyne. Particularly, against the dermatophyte Tricophyton mentagrophytes, MIC and MFC values were 0.25 μg/ml for JB73, and 8 μg/ml for 3,5-nonadiyne, the former being more active than amphotericin B and nystatin.

  11. Functional properties and antifungal activity of films based on gliadins containing cinnamaldehyde and natamycin.

    Science.gov (United States)

    Balaguer, Mari Pau; Fajardo, Paula; Gartner, Hunter; Gomez-Estaca, Joaquin; Gavara, Rafael; Almenar, Eva; Hernandez-Munoz, Pilar

    2014-03-03

    Gliadin films cross-linked with cinnamaldehyde (1.5, 3, and 5%) and incorporated with natamycin (0.5%) were prepared by casting, and their antifungal activity, water resistance, and barrier properties were characterized. Incorporation of natamycin gave rise to films with greater water uptake, weight loss and diameter gain, and higher water vapor and oxygen permeabilities. These results may be associated to a looser packing of the protein chains as a consequence of the presence of natamycin. The different cross-linking degree of the matrices influenced the natamycin migration to the agar test media, increasing from 13.3 to 23.7 (μg/g of film) as the percentage of cinnamaldehyde was reduced from 5% to 1.5%. Antifungal activity of films was assayed against common food spoilage fungi (Penicillium species, Alternaria solani, Colletotrichum acutatum). The greatest effectiveness was obtained for films containing natamycin and treated with 5% of cinnamaldehyde. The level of cinnamaldehyde reached in the head-space of the test assay showed a diminishing trend as a function of time, which was in agreement with fungal growth and cinnamaldehyde metabolization. Developed active films were used in the packaging of cheese slices showing promising results for their application in active packaging against food spoilage.

  12. Known and novel terpenes from Buddleja globosa displaying selective antifungal activity against dermatophytes.

    Science.gov (United States)

    Mensah, A Y; Houghton, P J; Bloomfield, S; Vlietinck, A; Vanden Berghe, D

    2000-09-01

    Lipophilic extracts of the stembark of Buddleja globosa were found to have antifungal activity at 125 microg/mL against three dermatophytic fungal species but had no activity at 1000 microg/mL against four other fungal species or two yeast species. Bioassay-guided fractionation of Si gel column eluates using the sensitive fungal species resulted in active fractions from which were isolated five compounds that were characterized by spectroscopic methods as one novel and four known compounds. The known compounds were the diterpene buddlejone (1), the bisditerpene maytenone, and the two sesquiterpenes buddledin A and buddledin B, while the novel compound was characterized as the diterpene deoxybuddlejone (2). The minimum inhibitory concentration of all the compounds was determined against all the microorganisms under test, and buddledins A and B were shown to exhibit the greatest antifungal activity, with values of 43 microM and 51 microM, respectively, against the sensitive fungi Trichophyton rubrum, Tricophyton interdigitale, and Epidermophyton floccosum.

  13. Antifungal, antioxidant and anti-inflammatory activities of Oenanthe crocata L. essential oil.

    Science.gov (United States)

    Valente, J; Zuzarte, M; Gonçalves, M J; Lopes, M C; Cavaleiro, C; Salgueiro, L; Cruz, M T

    2013-12-01

    The present study reports the chemical composition, antifungal, antioxidant and anti-inflammatory properties as well as the cytotoxicity of Oenanthe crocata essential oil and one of its main compounds. The essential oil was obtained from the aerial parts of the plant by hydrodistillation and analysed by GC and GC/MS. The oil was predominantly composed of monoterpene hydrocarbons (85.8%), being the main compounds trans-β-ocimene (31.3%), sabinene (29.0%) and cis-β-ocimene (12.3%). For the antifungal activity, the minimal inhibitory and minimal lethal concentrations (MICs and MLCs) were determined. The oil was particularly active against dermatophytes and Cryptococcus neoformans, with MIC values ranging from 0.08 to 0.16 μL/mL. Regarding the anti-inflammatory activity, both the oil and sabinene demonstrated strong anti-inflammatory activity through nitric oxide (NO) production inhibition in lipopolysaccharide (LPS) plus interferon gamma (IFN-γ)-triggered macrophages. Furthermore, the essential oil showed a potent NO scavenging effect and inhibited inducible NO synthase expression. Interestingly, and although we detected a cytotoxic effect in macrophages and keratinocytes for the highest concentrations tested of the oil and sabinene, we also disclosed bioactive and safe concentrations to be further explored for therapeutic proposes. Taking together, these results support the use of the oil and sabinene for the management of dermatophytosis and/or inflammatory-related diseases.

  14. Identification and antifungal activity of an actinomycete strain against Alternaria spp.

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    Fen Gao

    2014-10-01

    Full Text Available Alternaria alternata (Fries Keissler is a phytopathogenic fungus responsible for tobacco brown spot disease. This study aims to evaluate the antifungal activity of strain 163 against A. alternata and clarify its taxonomic status. The evaluation of the antifungal activity of strain 163 and its bacteria-free filtrate of fermentation broth was done through measuring the diameters of inhibition zones, and testing the antimicrobial spectrum and the inhibition effect on mycelial growth in vitro. The biocontrol activity of the bacteria-free filtrate in vivo was evaluated by using detached tobacco leaves method and assaying the inhibition rate to disease incidence in growth chamber. A polyphasic approach was taken in the identification of strain 163. The bacterial strain 163 showed inhibitory effect in vitro against A. alternata. The bacteria-free filtrate of the strain 163 fermentation broth showed a 56.7% inhibition rate in a detached leaf assay. In growth chamber conditions, it showed greater biocontrol activity when applied before plants being inoculated with A. alternata than after, the inhibition rate being 46.05%. Investigations into the morphological, cultural, physiological and biochemical properties of strain 163 found it to be most similar to Streptomyces microflavus. Its classification into cell wall type I and sugar type C further confirmed its Streptomyces characteristics. Construction of a phylogenetic tree based on 16S rDNA verified that strain 163 was most closely related to Streptomyces microflavus. From polyphasic taxonomical analysis, strain 163 was found to be identical to S. microflavus.

  15. Antifungal activity of components used for decontamination of dental prostheses on the growth of Candida albicans

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    Cíntia Lima Gouveia

    Full Text Available Introduction: The effectiveness of antimicrobial solutions employed in dental prosthesis decontamination is still uncertain. Aim: To evaluate the antifungal activity of cleaners used in the decontamination of dental prostheses on the growth of Candida albicans. Material and method: The evaluated products were: Corega Tabs(r (S1, Sodium Hypochlorite 1% (S2, Sodium Bicarbonate 1% (S3, Hydrogen Peroxide 1% (S4, Chlorhexidine Digluconate 0.12% - Periogard (r (S5, Mouthrinse based on essential oils - Listerine(r (S6, essential oil from Rosmarinus officinalis (rosemary at concentrations of 1% (S7 and 2% (S8. The antifungal activity of the products was evaluated by agar diffusion technique and the determination of microbial death curve of samples of C. albicans (ATCC 90028 in concentration 1.5 × 106 CFU/mL. The tests were performed in triplicate and statistical analysis was made by ANOVA Two-Way and Tukey tests, with the confidence level of 95%. Result: The average of the zones of inhibition growth, in millimeters, obtained for the products were: 0.0 (S1, 44.7 (S2, 0.0 (S3, 21.6 (S4, 10.0 (S5, 6.1 (S6, 0.0 (S7 and 2.4 (S8. Considering the determination of microbial death curve, all products showed a statistical difference (p<0.01 from control (0.85% sodium chloride and S3 groups. Fungal growth less than 2×104 CFU/mL and an accentuation of the microbial death curve were observed after 30 minutes, with exception for S3 and control groups. Conclusion: The studied compounds, with the exception of Sodium Bicarbonate, have antifungal effect against C. albicans, which contribute for dental prostheses hygiene.

  16. 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.

  17. 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

  18. Production and characterization of antifungal compounds produced by Lactobacillus plantarum IMAU10014.

    Directory of Open Access Journals (Sweden)

    HaiKuan Wang

    Full Text Available Lactobacillus plantarum IMAU10014 was isolated from koumiss that produces a broad spectrum of antifungal compounds, all of which were active against plant pathogenic fungi in an agar plate assay. Two major antifungal compounds were extracted from the cell-free supernatant broth of L. plantarum IMAU10014. 3-phenyllactic acid and Benzeneacetic acid, 2-propenyl ester were carried out by HPLC, LC-MS, GC-MS, NMR analysis. It is the first report that lactic acid bacteria produce antifungal Benzeneacetic acid, 2-propenyl ester. Of these, the antifungal products also have a broad spectrum of antifungal activity, namely against Botrytis cinerea, Glomerella cingulate, Phytophthora drechsleri Tucker, Penicillium citrinum, Penicillium digitatum and Fusarium oxysporum, which was identified by the overlay and well-diffusion assay. F. oxysporum, P. citrinum and P. drechsleri Tucker were the most sensitive among molds.

  19. In Vitro Antifungal Activity of Sertraline and Synergistic Effects in Combination with Antifungal Drugs against Planktonic Forms and Biofilms of Clinical Trichosporon asahii Isolates

    Science.gov (United States)

    Cong, Lin; Liao, Yong; Yang, Suteng

    2016-01-01

    Trichosporon asahii (T. asahii) is the major pathogen of invasive trichosporonosis which occurred mostly in immunocompromised patients. The biofilms formation ability of T. asahii may account for resistance to antifungal drugs and results a high mortality rate. Sertraline, a commonly prescribed antidepressant, has been demonstrated to show in vitro and in vivo antifungal activities against many kinds of pathogenic fungi, especially Cryptococcus species. In the present study, the in vitro activities of sertraline alone or combined with fluconazole, voriconazole, itraconazole, caspofungin and amphotericin B against planktonic forms and biofilms of 21 clinical T. asahii isolates were evaluated using broth microdilution checkerboard method and XTT reduction assay, respectively. The fractional inhibitory concentration index (FICI) was used to interpret drug interactions. Sertraline alone exhibited antifungal activities against both T. asahii planktonic cells (MICs, 4–8 μg/ml) and T. asahii biofilms (SMICs, 16–32 μg/ml). Furthermore, SRT exhibited synergistic effects against T. asahii planktonic cells in combination with amphotericin B, caspofungin or fluconazole (FICI≤0.5) and exhibited synergistic effects against T. asahii biofilms in combination with amphotericin B (FICI≤0.5). SRT exhibited mostly indifferent interactions against T. asahii biofilms in combination with three azoles in this study. Sertraline-amphotericin B combination showed the highest percentage of synergistic effects against both T. asahii planktonic cells (90.5%) and T. asahii biofilms (81.0%). No antagonistic interaction was observed. Our study suggests the therapeutic potential of sertraline against invasive T. asahii infection, especially catheter-related T. asahii infection. Further in vivo studies are needed to validate our findings. PMID:27930704

  20. 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.

  1. Antifungal activity of propolis extract against yeasts isolated from onychomycosis lesions

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    Ana Carla Pozzi Oliveira

    2006-08-01

    Full Text Available The aim of this study was to determine the in vitro activity of propolis extract against 67 yeasts isolated from onychomycosis in patients attending at the Teaching and Research Laboratory of Clinical Analysis of the State University of Maringá. The method used was an adaptation made from the protocol approved by the National Committee for Clinical Laboratory Standards. The yeasts tested were: Candida parapsilosis 35%, C. tropicalis 23%, C. albicans 13%, and other species 29%. The propolis extract showed excellent performance regarding its antifungal activity: the concentration capable of inhibiting the all of the yeasts was 5 × 10-2 mg/ml of flavonoids and 2 × 10-2 mg/ml of flavonoids stimulated their cellular death. Trichosporon sp. were the most sensitive species, showing MIC50 and MIC90 of 1.25 × 10-2 mg/ml of flavonoids, and C. tropicalis was the most resistant, with CFM50 of 5 × 10-2 mg/ml of flavonoids and MFC90 of 10 × 10-2 mg/ml. In view of the fact that propolis is a natural, low cost, non-toxic product with proven antifungal activity, it should be considered as another option in the onychomycosis treatment.

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

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    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.

  3. Phytochemical analysis and antifungal activity of selected seaweeds from Okha coast, Gujarat, India

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    Isaiah Nirmal Kumar

    2015-07-01

    Full Text Available Objective: To deal with the assessment of the chemical composition of carbohydrate, protein, phenol, flavanoid, chlorophyll, and carotenoid and antifungal activity of various marine seaweeds collected from Okha coast, Gujarat during September, 2013. Methods: Biochemical compounds of selected seaweeds were quantified and antifungal activity of these species belonging to red, green, and brown seaweeds was explored and the seaweeds were extracted in acetone, ethanol and chloroform. Results: The carbohydrate content was highest in Cystoseira indica Mairh, protein was highest in Gracilaria corticata J. Agardh and phenol content was highest in Padina boergesenii; flavanoid content was found greater in Cystoseira indica, chlorophyll content was found greater in Monostroma latissimum Wittrock and carotenoid content was more in Dictyopteris acrostichoides Bornet. The highest inhibiting effect was noted for Sargassum tenerrimum J. Agardh and Turbinaria ornata J. Agardh belonging to brown algae, against Aspergillus niger and Penicillium janthinellum in chloroform extracts and ethanolic extracts, which caused opportunistic infection of HIV-infected person, lung disease, aspergillosis, and otomycosis (fungal ear infections. Conclusions: The study reveals that the seaweeds contain high amount of biochemical constituents. Besides, the crude extracts of the seaweeds showed promising activity against the tested fungal pathogens. Therefore, seaweeds collected from Okha coast, Gujarat region are biochemical compounds with potential capacity which make them useful for screening natural products for pharmaceutical industry.

  4. Phytochemical analysis and antifungal activity of selected seaweeds from Okha coast, Gujarat, India

    Institute of Scientific and Technical Information of China (English)

    Isaiah Nirmal Kumar; Megha Barot; Rita Kumar

    2015-01-01

    Objective:To deal with the assessment of the chemical composition of carbohydrate, protein, phenol, flavanoid, chlorophyll, and carotenoid and antifungal activity of various marine seaweeds collected from Okha coast, Gujarat during September, 2013. Methods:Biochemical compounds of selected seaweeds were quantified and antifungal activity of these species belonging to red, green, and brown seaweeds was explored and the seaweeds were extracted in acetone, ethanol and chloroform. Results:The carbohydrate content was highest inCystoseira indica Mairh, protein was highest inGracilaria corticataJ. Agardh and phenol content was highest inPadina boergesenii; flavanoid content was found greater inCystoseira indica, chlorophyll content was found greater inMonostroma latissimum Wittrock and carotenoid content was more inDictyopteris acrostichoides Bornet. The highest inhibiting effect was noted forSargassum tenerrimum J. Agardh andTurbinaria ornata J. Agardh belonging to brown algae, againstAspergillus niger andPenicillium janthinellum in chloroform extracts and ethanolic extracts, which caused opportunistic infection ofHIV-infected person, lung disease, aspergillosis, and otomycosis (fungal ear infections). Conclusions:The study reveals that the seaweeds contain high amount of biochemical constituents. Besides, the crude extracts of the seaweeds showed promising activity against the tested fungal pathogens. Therefore, seaweeds collected from Okha coast, Gujarat region are biochemical compounds with potential capacity which make them useful for screening natural products for pharmaceutical industry.

  5. Antifungal activity of different neem leaf extracts and the nimonol against some important human pathogens

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    D.A Mahmoud

    2011-09-01

    Full Text Available This study was conducted to evaluate the effect of aqueous, ethanolic and ethyl acetate extracts from neem leaves on growth of some human pathogens (Aspergillus flavus, Aspergillus fumigatus, Aspergillus niger, Aspergillus terreus, Candida albicans and Microsporum gypseum in vitro. Different concentrations (5, 10, 15 and 20% prepared from these extracts inhibited the growth of the test pathogens and the effect gradually increased with concentration. The 20% ethyl acetate extract gave the strongest inhibition compared with the activity obtained by the same concentration of the other extracts. High Performance Liquid Chromatography (HPLC analysis of ethyl acetate extract showed the presence of a main component (nimonol which was purified and chemically confirmed by Nuclear Magnetic Resonance (NMR spectroscopic analysis. The 20% ethyl acetate extract lost a part of its antifungal effect after pooling out the nimonol and this loss in activity was variable on test pathogens. The purified nimonol as a separate compound did not show any antifungal activity when assayed against all the six fungal pathogens.

  6. Synthesis, Antimycobacterial, Antifungal and Photosynthesis-Inhibiting Activity of Chlorinated N-phenylpyrazine-2-carboxamides †

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    Katarina Kralova

    2010-11-01

    Full Text Available A series of sixteen pyrazinamide analogues with the -CONH- linker connecting the pyrazine and benzene rings was synthesized by the condensation of chlorides of substituted pyrazinecarboxylic acids with ring-substituted (chlorine anilines. The prepared compounds were characterized and evaluated for their antimycobacterial and antifungal activity, and for their ability to inhibit photosynthetic electron transport (PET. 6-Chloro-N-(4-chlorophenylpyrazine-2-carboxamide manifested the highest activity against Mycobacterium tuberculosis strain H37Rv (65% inhibition at 6.25 μg/mL. The highest antifungal effect against Trichophyton mentagrophytes, the most susceptible fungal strain tested, was found for 6-chloro-5-tert-butyl-N-(3,4-dichlorophenylpyrazine-2-carboxamide (MIC = 62.5 μmol/L. 6-Chloro-5-tert-butyl-N-(4-chlorophenylpyrazine-2-carboxamide showed the highest PET inhibition in spinach chloroplasts (Spinacia oleracea L. chloroplasts (IC50 = 43.0 μmol/L. For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds as well as their structure-activity relationships are discussed.

  7. Probiotic Potential of Lactobacillus Strains with Antifungal Activity Isolated from Animal Manure

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    Soundharrajan Ilavenil

    2015-01-01

    Full Text Available The aim of the study was to isolate and characterize the lactic acid bacteria (LAB from animal manure. Among the thirty LAB strains, four strains, namely, KCC-25, KCC-26, KCC-27, and KCC-28, showed good cell growth and antifungal activity and were selected for further characterization. Biochemical and physiology properties of strains confirmed that the strains are related to the Lactobacillus sp.; further, the 16S rRNA sequencing confirmed 99.99% sequence similarity towards Lactobacillus plantarum. The strains exhibited susceptibility against commonly used antibiotics with negative hemolytic property. Strains KCC-25, KCC-26, KCC-27, and KCC-28 showed strong antifungal activity against Aspergillus fumigatus, Penicillium chrysogenum, Penicillium roqueforti, Botrytis elliptica, and Fusarium oxysporum, respectively. Fermentation studies noted that the strains were able to produce significant amount of lactic, acetic, and succinic acids. Further, the production of extracellular proteolytic and glycolytic enzymes, survival under low pH, bile salts, and gastric juice together with positive bile salt hydrolase (Bsh activity, cholesterol lowering, cell surface hydrophobicity, and aggregation properties were the strains advantages. Thus, KCC-25, KCC-26, KCC-27, and KCC-28 could have the survival ability in the harsh condition of the digestive system in the gastrointestinal tract. In conclusion, novel L. plantarum KCC-25, KCC-26, KCC-27, and KCC-28 could be considered as potential antimicrobial probiotic strains.

  8. Assessment of antifungal activity of herbal and conventional toothpastes against clinical isolates of Candida albicans

    Institute of Scientific and Technical Information of China (English)

    Ghaleb Adwan; Yousef Salameh; Kamel Adwan; Ali Barakat

    2012-01-01

    Objective: To detect the anticandidal activity of nine toothpastes containing sodium fluoride, sodium monofluorophosphate and herbal extracts as an active ingredients against 45 oral and non oral Candida albicans (C. albicans) isolates. Methods: The antifungal activity of these toothpaste formulations was determined using a standard agar well diffusion method. Statistical analysis was performed using a statistical package, SPSS windows version 15, by applying mean values using one-way ANOVA with post-hoc least square differences (LSD) method. A P value of less than 0.05 was considered significant. Results: All toothpastes studied in our experiments were effective in inhibiting the growth of all C. albicans isolates. The highest anticandidal activity was obtained from toothpaste that containing both herbal extracts and sodium fluoride as active ingredients, while the lowest activity was obtained from toothpaste containing sodium monofluorophosphate as an active ingredient. Antifungal activity of Parodontax toothpaste showed a significant difference (P< 0.001) against C. albicans isolates compared to toothpastes containing sodium fluoride or herbal products. Conclusions: In the present study, it has been demonstrated that toothpaste containing both herbal extracts and sodium fluoride as active ingredients are more effective in control of C. albicans, while toothpaste that containing monofluorophosphate as an active ingredient is less effective against C. albicans. Some herbal toothpaste formulations studied in our experiments, appear to be equally effective as the fluoride dental formulations and it can be used as an alternative to conventional formulations for individuals who have an interest in naturally-based products. Our results may provide invaluable information for dental professionals.

  9. 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.

  10. The Antifungal Activity of Lactoferrin and Its Derived Peptides: Mechanisms of Action and Synergy with Drugs against Fungal Pathogens

    Science.gov (United States)

    Fernandes, Kenya E.; Carter, Dee A.

    2017-01-01

    Lactoferrin is a multifunctional iron-binding glycoprotein belonging to the transferrin family. It is found abundantly in milk and is present as a major protein in human exocrine secretions where it plays a role in the innate immune response. Various antifungal functions of lactoferrin have been reported including a wide spectrum of activity across yeasts and molds and synergy with other antifungal drugs in combination therapy, and various modes of action have been proposed. Bioactive peptides derived from lactoferrin can also exhibit strong antifungal activity, with some surpassing the potency of the whole protein. This paper reviews current knowledge of the spectrum of activity, proposed mechanisms of action, and capacity for synergy of lactoferrin and its peptides, including the three most studied derivatives: lactoferricin, lactoferrampin, and Lf(1–11), as well as some lactoferrin-derived variants and modified peptides. PMID:28149293

  11. Antifungal activity of four honeys of different types from Algeria against pathogenic yeast:Candida albicans and Rhodotorula sp.

    Institute of Scientific and Technical Information of China (English)

    Ahmed Moussa; Djebli Noureddine; Aissat Saad; Meslem Abdelmelek; Benhalima Abdelkader

    2012-01-01

    Objective: To evaluate the antifungal activity of four honeys of different types from Algeria against pathogenic yeast i.e. Candida albicans (C. albicans) and Rhodotorula sp. Methods:Four Algeria honeys of different botanical origin were analyzed to test antifungal effect against C. albicans, and Rhodotorula sp. Different concentrations (undiluted, 10%, 30%, 50%and 70%w/v) of honey were studied in vitro for their antifugal activity using C. albicans and Rhodotorula sp. as fungal strains. Results:The range of the diameter of zone of inhibition of various concentrations of tested honeys was (7-23 mm) for Rhodotorula sp., while C. albicans showed clearly resistance towards all concentrations used. The MICs of tested honey concentrations against C. albicans and Rhodotorula sp. were (70.09-93.48)%and (4.90-99.70)%v/v, respectively. Conclusions:This study demonstrates that, in vitro, these natural products have clearly an antifungal activity against Rhodotorula sp. and C. albicans.

  12. Bombyx mori cecropin A has a high antifungal activity to entomopathogenic fungus Beauveria bassiana.

    Science.gov (United States)

    Lu, Dingding; Geng, Tao; Hou, Chengxiang; Huang, Yuxia; Qin, Guangxing; Guo, Xijie

    2016-05-25

    A cDNA encoding cecropin A (CecA) was cloned from the larvae of silkworm, Bombyx mori, using RT-PCR. It encodes a protein of 63 amino acids, containing a 22 amino acid signal peptide and a 37 amino acid mat peptide of functional domain. The CecA secondary structure contains two typical amphiphilic α-helices. Real-time qPCR analysis revealed that CecA was expressed in all the tissues tested, including cuticle, fat body, hemocytes, Malpighian tubule, midgut and silk gland in the silkworm larvae with the highest expression in the fat body and hemocytes. The gene expression of B. mori CecA was rapidly induced by Beauveria bassiana challenge and reached maximum levels at 36h after inoculation in third instar larvae. In the fifth instar larvae infected with B. bassiana, the relative expression level of CecA was upregulated in fat body and hemocytes, but not in cuticle, Malpighian tubule, midgut and silk gland. The cDNA segment of the CecA was inserted into the expression plasmid pET-30a(+) to construct a recombinant expression plasmid. Western blot results revealed that his-tagged fusion protein was successfully expressed and purified. Then the mat peptide of CecA was chemically synthesized with C-terminus amidation for in vivo antifungal assay and purity achieved 93.7%. Mass spectrometry and SDS-PAGE showed its molecular weight to be 4046.95Da. Antifungal assays indicated that the B. mori CecA had a high antifungal activity to entomopathogenic fungus B. bassiana both in vitro and in vivo in the silkworm larvae. This is the first report that the CecA is effective to inhibit B. bassiana inside the body of silkworm.

  13. 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.

  14. Antibacterial and antifungal activities of different parts of Tribulus terrestris L. growing in Iraq.

    Science.gov (United States)

    Al-Bayati, Firas A; Al-Mola, Hassan F

    2008-02-01

    Antimicrobial activity of organic and aqueous extracts from fruits, leaves and roots of Tribulus terrestris L., an Iraqi medicinal plant used as urinary anti-infective in folk medicine, was examined against 11 species of pathogenic and non-pathogenic microorganisms: Staphylococcus aureus, Bacillus subtilis, Bacillus cereus, Corynebacterium diphtheriae, Escherichia coli, Proteus vulgaris, Serratia marcescens, Salmonella typhimurium, Klebsiella pneumoniae, Pseudomonas aeruginosa and Candida albicans using microdilution method in 96 multiwell microtiter plates. All the extracts from the different parts of the plant showed antimicrobial activity against most tested microorganisms. The most active extract against both Gram-negative and Gram-positive bacteria was ethanol extract from the fruits with a minimal inhibitory concentration (MIC) value of 0.15 mg/ml against B. subtilis, B. cereus, P. vulgaris and C. diphtheriae. In addition, the same extract from the same plant part demonstrated the strongest antifungal activity against C. albicans with an MIC value of 0.15 mg/ml.

  15. Isolation of a new Mexican strain of Bacillus subtilis with antifungal and antibacterial activities.

    Science.gov (United States)

    Basurto-Cadena, M G L; Vázquez-Arista, M; García-Jiménez, J; Salcedo-Hernández, R; Bideshi, D K; Barboza-Corona, J E

    2012-01-01

    Although several strains of B. subtilis with antifungal activity have been isolated worldwide, to date there are no published reports regarding the isolation of a native B. subtilis strain from strawberry plants in Mexico. A native bacterium (Bacillus subtilis 21) demonstrated in vitro antagonistic activity against different plant pathogenic fungi. Under greenhouse conditions, it was shown that plants infected with Rhizoctonia solani and Fusarium verticillioides and treated with B. subtilis 21 produced augment in the number of leaves per plant and an increment in the length of healthy leaves in comparison with untreated plants. In addition, B. subtilis 21 showed activity against pathogenic bacteria. Secreted proteins by B. subtilis 21 were studied, detecting the presence of proteases and bacteriocin-like inhibitor substances that could be implicated in its antagonistic activity. Chitinases and zwittermicin production could not be detected. Then, B. subtilis 21 could potentially be used to control phytopathogenic fungi that infect strawberry plants.

  16. Isolation of a New Mexican Strain of Bacillus subtilis with Antifungal and Antibacterial Activities

    Directory of Open Access Journals (Sweden)

    M. G. L. Basurto-Cadena

    2012-01-01

    Full Text Available Although several strains of B. subtilis with antifungal activity have been isolated worldwide, to date there are no published reports regarding the isolation of a native B. subtilis strain from strawberry plants in Mexico. A native bacterium (Bacillus subtilis 21 demonstrated in vitro antagonistic activity against different plant pathogenic fungi. Under greenhouse conditions, it was shown that plants infected with Rhizoctonia solani and Fusarium verticillioides and treated with B. subtilis 21 produced augment in the number of leaves per plant and an increment in the length of healthy leaves in comparison with untreated plants. In addition, B. subtilis 21 showed activity against pathogenic bacteria. Secreted proteins by B. subtilis 21 were studied, detecting the presence of proteases and bacteriocin-like inhibitor substances that could be implicated in its antagonistic activity. Chitinases and zwittermicin production could not be detected. Then, B. subtilis 21 could potentially be used to control phytopathogenic fungi that infect strawberry plants.

  17. Antifungal activity of six plant essential oils from Serbia against Trichoderma aggressivum f. europaeum

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    Rada Đurović-Pejčev

    2014-12-01

    Full Text Available Six essential oils (EOs extracted from plants originating in Serbia were assayed for inhibitory and fungicidal activity against a major fungal pathogen of button mushroom causing green mould disease, Trichoderma agressivum f. europaeum. The strongest activity was demonstrated by the oils of basil (Ocimum basilicum L. and peppermint (Mentha piperita L.. Medium antifungal activity of St. John's wort (Hypericum perforatum L. and walnut [Juglans regia (F] oils was also recorded. Oils extracted from yarrow (Achillea millepholium L. and juniper (Juniperus communis L. exhibited the lowest activity. Peppermint oil showed fungicidal effect on the pathogen, having a minimum fungicidal concentration of 0.64 μl ml-1. The main components of peppermint essential oil were menthone (37.02%, menthol (29.57% and isomenthone (9.06%.

  18. Synthesis, characterization, and antifungal activity of novel inulin derivatives with chlorinated benzene.

    Science.gov (United States)

    Guo, Zhanyong; Li, Qing; Wang, Gang; Dong, Fang; Zhou, Haoyuan; Zhang, Jing

    2014-01-01

    A group of novel inulin derivatives containing benzene or chlorinated benzene were synthesized by reaction of chloracetyl inulin (CAIL) with the Schiff bases of 4-amino-pyridine, including (2-pyridyl)acetyl inulin chloride (PAIL), 2-[4-(2-chlorobenzylideneamino)-pyridyl]acetyl inulin chloride (2CPAIL), 2-[4-(4-chlorobenzylideneamino)-pyridyl]acetyl inulin chloride (4CPAIL), and 2-[4-(2,4-dichlorobenzylideneamino)-pyridyl]acetyl inulin chloride (2,4DCPAIL). Their antifungal activity against three kinds of phytopathogens was estimated by hypha measurement in vitro. Of all the synthesized chitosan derivatives, 2,4DCPAIL inhibited the growth of the tested phytopathogens with inhibitory indices of 67%, 47%, and 43% against Colletotrichum lagenarium (Pass) Ell.et halst, Phomopsis asparagi (Sacc.) Bubak and Fusarium oxysporum (schl.) F.sp. niveum (F. oxysporum) respectively at 1.0 mg/mL. The results indicate that all the inulin derivatives have better antifungal activity than inulin, and the inhibitory index is affected by the chlorine atom grafted to the inulin derivatives.

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

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    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.

  20. In vitro antifungal activity of the essential oil and the methanolic extract of Ruta chalepensis.

    Science.gov (United States)

    Aouadhi, Ch; Ghazghazi, H; Hamrouni, S; Hasnaoui, B; Maaroufi, A

    2013-01-01

    Ruta chalepensis L. (Rutaceae), is an ancient aromatic medicinal plant still used in the traditional medicine of many countries as a laxative, antiinflammatory, analgesic, antispasmodic, abortifacient, antiepileptic, emmenagogue and for dermatopathy treatment. Regarding increasing prevalence of mycotoxins and inefficiency of methods used to decrease them, it is possible to use plants metabolites to decrease mycotoxins. This study was carried out to evaluate chemical composition, antifungal and anticandidal activities of R. chalepensis extracts. The chemical composition of its essential oil was analyzed by gas chromatography coupled with mass spectrometry (GCMS). The major components of R. chalepensis essential oil were menthol (49.92%), linalool (31.1%) and 2-hexanal (5.2%). The antifungal and anticandidal effects of the essential oil and methanolic extract of R. chalepensis leaves were studied by disc diffusion assay and broth dilution method. The obtained results showed that R. chalepensis extracts had a significant fungicidal effect against Aspergillus niger, Aspergillus flavus and Candida albicans. The inhibition zones diameters and the minimum inhibitory concentration values for tested microorganisms were in the range of 11-17 mm and 3.25-6.25% (v/v), respectively. The methanolic extract showed much better antimicrobial activity than the essential oil against three tested micro-organisms

  1. Antifungal activity evaluation of Aloe arborescens dry extract against trichosporon genus yeasts

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    João Ricardo Bueno de Morais Borba

    2014-10-01

    Full Text Available The objective of this study was to investigate the antifungal activity of Aloe arborescens dry extract against Trichosporon genus yeast species. Extraction was carried out by means of a longitudinal incision in fresh leaves, which were collected on a vat, and the total volume was frozen and subsequently lyophilized. Then, 40 mg of the dry extract was dissolved in DMSO by gentle inversion in order to obtain a solution whose concentration was 4000 µg mL-1. This solution became limpid and slightly yellowish because the pigment of the latex was attenuated. It was performed serial dilutions from 2,000 to 15.625 µg mL-1 with RPMI-1640 broth. There was already no pigment in the first dilution of 2000 μg mL-1. It was analyzed fifteen strains of Trichosporon spp., and Candida albicans ATCC 10231 was used as control strain. We carried out the reading of microplates in the ELISA reader device at a wavelength of 530 nm, after incubation for 24 and 48 hours, and it was determinated the Minimum Inhibitory Concentration (MIC. The MIC50 value obtained for all Trichosporon species and for C. albicans was 500 µg mL-1. As a result, we concluded that Aloe arborescens dry extract has antifungal activity against Trichosporon yeasts.

  2. Antifungal activity of Rubus chingii extract combined with fluconazole against fluconazole-resistant Candida albicans.

    Science.gov (United States)

    Han, Bing; Chen, Jia; Yu, Yi-qun; Cao, Yong-bing; Jiang, Yuan-ying

    2016-02-01

    This study aimed to investigate the antifungal activity of Rubus chingii extract in combination with fluconazole (FLC) against FLC-resistant Candida albicans 100 in vitro. A R. chingii extract and FLC-resistant C. albicans fungus suspension were prepared. The minimum inhibitory concentration and fractional inhibitory concentration index of R. chingii extract combined with FLC against C. albicans were determined, after which growth curves for C. albicans treated with R. chingii extract, FLC alone and a combination of these preparations were constructed. Additionally, the mechanisms of drug combination against C. albicans were explored by flow cytometry, gas chromatographic mass spectrometry and drug efflux pump function detection. R. chingii extract combined with FLC showed significant synergy. Flow cytometry suggested that C. albicans cells mainly arrest in G1 and S phases when they have been treated with the drug combination. The drug combination resulted in a marked decrease in the ergosterol content of the cell membrane. Additionally, efflux of Rhodamine 6G decreased with increasing concentrations of R. chingii extract. R. chingii extract combined with FLC has antifungal activity against FLC-resistant C. albicans.

  3. Metal based new triazoles: their synthesis, characterization and antibacterial/antifungal activities.

    Science.gov (United States)

    Sumrra, Sajjad H; Chohan, Zahid H

    2012-12-01

    A series of new triazoles and their oxovanadium(IV) complexes have been synthesized, characterized and evaluated for antibacterial/antifungal properties. The new Schiff bases ligands (L(1))-(L(5)) were prepared by the condensation reaction of 3,5-diamino-1,2,4-triazole with 2-hydroxy-1-naphthaldehyde, pyrrole-2-carboxaldehyde, pyridine-2-carboxaldehyde, 2-acetyl pyridine and 2-methoxy benzaldehyde. The structures of the ligands have been established on the basis of their physical, spectral (IR, (1)H and (13)C NMR and mass spectrometry) and elemental analytical data. The prepared ligands were used to synthesize their oxovanadium(IV) complexes (1)-(5) which were also characterized by their physical, spectral and analytical data and proposed to have a square pyramidal geometry. The ligands and their complexes were screened for in vitro antibacterial activity against six bacterial species such as, Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa, Salmonella typhi, Staphylococcus aureus, and Bacillus subtilis and for in vitro antifungal activity against six fungal strains, Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, and Candida glabrata. Cytotoxic nature of the compounds was also reported using brine shrimp bioassay method against Artemia salina.

  4. Metal based new triazoles: Their synthesis, characterization and antibacterial/antifungal activities

    Science.gov (United States)

    Sumrra, Sajjad H.; Chohan, Zahid H.

    2012-12-01

    A series of new triazoles and their oxovanadium(IV) complexes have been synthesized, characterized and evaluated for antibacterial/antifungal properties. The new Schiff bases ligands (L1)-(L5) were prepared by the condensation reaction of 3,5-diamino-1,2,4-triazole with 2-hydroxy-1-naphthaldehyde, pyrrole-2-carboxaldehyde, pyridine-2-carboxaldehyde, 2-acetyl pyridine and 2-methoxy benzaldehyde. The structures of the ligands have been established on the basis of their physical, spectral (IR, 1H and 13C NMR and mass spectrometry) and elemental analytical data. The prepared ligands were used to synthesize their oxovanadium(IV) complexes (1)-(5) which were also characterized by their physical, spectral and analytical data and proposed to have a square pyramidal geometry. The ligands and their complexes were screened for in vitro antibacterial activity against six bacterial species such as, Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa, Salmonella typhi, Staphylococcus aureus, and Bacillus subtilis and for in vitro antifungal activity against six fungal strains, Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, and Candida glabrata. Cytotoxic nature of the compounds was also reported using brine shrimp bioassay method against Artemia salina.

  5. Screening for antifungal activities of extracts of the brazilian seaweed genus Laurencia (Ceramiales, Rhodophyta

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    Erika M. Stein

    2011-04-01

    Full Text Available The resistance of pathogens to commonly used antibiotics has enhanced morbidity and mortality and has triggered the search for new drugs. Several species of the red alga genus Laurencia are very interesting candidates as potential sources of natural products with pharmaceutical activity because they are known to produce a wide range of chemically interesting halogenated secondary metabolites. This is an initial report of the antifungal activities of the secondary metabolites of five species of Laurencia, collected in the state of Espírito Santo, against three strains of pathogenic fungi: Candida albicans (CA, Candida parapsilosis (CP, and Cryptococcus neoformans (CN. Minimum inhibitory concentrations (MIC of the algal extracts were determined by serial dilution method in RPMI 1640 Medium in 96-well plates according to the NCCLS and microbial growth was determined by absorbance at 492nm. A result showing maintenance or reduction of the inoculum was defined as fungistatic, while fungicidal action was no observed growth in the 10 µL fungistatic samples subcultured in Sabouraud Agar. Our results indicate that apolar extracts of Laurencia species possess antifungal properties and encourage continued research to find new drugs for therapy of infectious diseases in these algae.

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

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    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.

  7. Antifungal Activity of Essential Oil of Eucalyptus camaldulensis Dehnh. against Selected Fusarium spp.

    Science.gov (United States)

    Maina, Angeline W.; Wagacha, John M.

    2017-01-01

    The objective of this study was to evaluate the antifungal activity of essential oil (EO) of Eucalyptus camaldulensis Dehnh. against five Fusarium spp. commonly associated with maize. The essential oil had been extracted by steam distillation in a modified Clevenger-type apparatus from leaves of E. camaldulensis and their chemical composition characterized by gas chromatography mass spectrometry. Poisoned food technique was used to determine the percentage inhibition of mycelial growth, minimum inhibitory concentration, and minimum fungicidal concentration of the EO on the test pathogens. Antifungal activity of different concentrations of the EO was evaluated using disc diffusion method. The most abundant compounds identified in the EO were 1,8-cineole (16.2%), α-pinene (15.6%), α-phellandrene (10.0%), and p-cymene (8.1%). The EO produced complete mycelial growth inhibition in all the test pathogens at a concentration of 7-8 μL/mL after five days of incubation. The minimum inhibitory concentration and minimum fungicidal concentration of the EO on the test fungi were in the range of 7-8 μL/mL and 8–10 μL/mL, respectively. These findings confirm the fungicidal properties of E. camaldulensis essential oils and their potential use in the management of economically important Fusarium spp. and as possible alternatives to synthetic fungicides. PMID:28127308

  8. Antifungal activity of oregano extract against A. Versicolor, E. Nidulans and Eurotium spp.: Producers of sterigmatocystin

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    Kocić-Tanackov Sunčica D.

    2011-01-01

    Full Text Available The paper presents the influence of oregano extract (Origanum vulgare L. on growth of Aspergillus versicolor, Emericella nidulans, Eurotium herbariorum, E. amstelodami, E. chevalieri and E. rubrum - producers of sterigmatocystin (STC isolated from salads. Antifungal tests were performed by agar plates method. The composition of the active component of extract was determined by GC-MS method and the major components were: carvacrol (34.20%, triacetin (22.91%, carvone (18.05%, p-cymene (8.05% and thymol (3.74%. The examined extract showed the ability to reduce mold growth at all applied concentrations. Minimum inhibitory concentrations (MIC for E. nidulans, E. chevalieri and E. amstelodami were 2.5% (v/v and over 2.5% (v/v for A. versicolor. At 1.5% (v/v concentration the extract completely inhibited the growth of E. rubrum, whereas higher dose of 2.5% (v/v was fungicidal against E. herbariorum. Besides its sensory role in food products, the examined oregano extract also exhibits antifungal activities against producers of STC.

  9. 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

  10. A cultured endophyte community is associated with the plant Clerodendrum inerme and antifungal activity.

    Science.gov (United States)

    Gong, B; Yao, X H; Zhang, Y Q; Fang, H Y; Pang, T C; Dong, Q L

    2015-06-10

    Fungal endophytes live in the inner tissues of Clerodendrum inerme and may be significant resources for new chemicals in drug discovery. A total of 242 endophytic fungi were recovered from 602 sample segments of C. inerme; 66 were purified. The 66 fungi belonging to 16 taxa and 11 genera (Alternaria, Nigrospora, Bartalinia, Pestalotiopsis, Fusarium, Mycoleptodiscus, Trichoderma, Phomopsis, Diaporthe, Lasiodiplodia, and Curvularia) were identified by morphological characteristics and fungal internal transcribed spacer sequences. The most abundant genera were Alternaria and Lasiodiplodia. Some of the endophytes exhibited tissue specificity. The colonization frequencies of endophytes in the stems were evidently higher than those in the roots and leaves. The crude ethyl acetate extracts were tested against 6 endophytes isolated from C. inerme. Three of 10 (33.3%) endophytes, which were identified as Phomopsis sp, Curvularia sp, and Mycoleptodiscus sp, displayed distinct antifungal activity against ≥3 tested fungi. To our knowledge, this is the first report of an endophytic community associated with C. inerme in China and its antifungal activity in vitro.

  11. Antifungal Activity of Brazilian Propolis Microparticles against Yeasts Isolated from Vulvovaginal Candidiasis

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    Kelen Fátima Dalben Dota

    2011-01-01

    Full Text Available Propolis, a resinous compound produced by Apis mellifera L. bees, is known to possess a variety of biological activities and is applied in the therapy of various infectious diseases. The aim of this study was to evaluate the in vitro antifungal activity of propolis ethanol extract (PE and propolis microparticles (PMs obtained from a sample of Brazilian propolis against clinical yeast isolates of importance in the vulvovaginal candidiasis (VVC. PE was used to prepare the microparticles. Yeast isolates (n=89, obtained from vaginal exudates of patients with VVC, were exposed to the PE and the PMs. Moreover, the main antifungal drugs used in the treatment of VVC (Fluconazole, Voriconazole, Itraconazole, Ketoconazole, Miconazole and Amphotericin B were also tested. Minimum inhibitory concentration (MIC was determined according to the standard broth microdilution method. Some Candida albicans isolates showed resistance or dose-dependent susceptibility for the azolic drugs and Amphotericin B. Non-C. albicans isolates showed more resistance and dose-dependent susceptibility for the azolic drugs than C. albicans. However, all of them were sensitive or dose-dependent susceptible for Amphotericin B. All yeasts were inhibited by PE and PMs, with small variation, independent of the species of yeast. The overall results provided important information for the potential application of PMs in the therapy of VVC and the possible prevention of the occurrence of new symptomatic episodes.

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

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    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.

  13. Antibacterial and antifungal activities of crude plant extracts from Colombian biodiversity.

    Science.gov (United States)

    Niño, Jaime; Mosquera, Oscar M; Correa, Yaned M

    2012-12-01

    On a global scale, people have used plants to treat diseases and infections, and this has raised interest on the plant biodiversity potencial in the search of antimicrobial principles. In this work, 75 crude n-hexanes, dichloromethane and methanol extracts from the aerial parts of 25 plants belonging to four botanical families (Asteraceae, Euphorbiaceae, Rubiaceae and Solanaceae), collected at the Natural Regional Park Ucumari (Risaralda, Colombia), were evaluated for their antibacterial and antifungal activities by the agar well diffusion method. The antibacterial activities were assayed against two Gram-positive bacteria Staphylococcus aureus and Bacillus subtilis, and three Gram-negative ones named, Klebsiella pneumoniae, Escherichia coli and Pseudomonas aeruginosa. In addition, the same plant extracts were tested against the yeast Candida albicans and the fungi Aspergillus fumigatus and Fusarium solani. Overall, the plant extracts examined displayed better bactericide rather than fungicide activities. In general, the best antibacterial activity was showed by the plant extracts from the Rubiaceae family, followed in order by the extracts from the Euphorbiaceae and Solanaceae ones. It is important to emphasize the great activity displayed by the methanol extract of Alchornea coelophylla (Euphorbiaceae) that inhibited four out of five bacteria tested (B. Subtilis, P. aeruginosa, S. aureus and E. coli). Furthermore, the best Minimal Inhibitory Concentration for the extracts with antifungal activities were displayed by the dichloromethane extracts from Acalypha diversifolia and Euphorbia sp (Euphorbiaceae). The most susceptible fungus evaluated was F. Solani since 60% and 20% of the dichloromethane and methanol extracts evaluated inhibited the growth of this phytopathogenic fungus. The antimicrobial activity of the different plant extracts examined in this work could be related to the secondary metabolites contents and their interaction and susceptibility of

  14. Characteristic spectral studies and in vitro antifungal activity of some Schiff bases and their organotin (Ⅳ) complexes

    Institute of Scientific and Technical Information of China (English)

    Wajid Rehman; Musa Kaleem Baloch; Bakhtiar Muhammad; Amin Badshah; Khalid M. Khan

    2004-01-01

    The synthesis and in vitro antifungal activity of some Schiff bases and their Sn (Ⅳ) complexes has been tested against plant pathogenic fungi and it is found that they possess excellent fungicidal activity. On the basis of 1H-, 13C-, 119Sn NMR-, 119Sn Mossbauer, IR and Elemental analysis the tetrahedral geometry is proposed for the synthesized compounds.

  15. The Drosophila PRR GNBP3 assembles effector complexes involved in antifungal defenses independently of its Toll-pathway activation function.

    NARCIS (Netherlands)

    Matskevich, A.A.; Quintin, J.; Ferrandon, D.

    2010-01-01

    The Drosophila Toll-signaling pathway controls the systemic antifungal host response. Gram-negative binding protein 3 (GNBP3), a member of the beta-glucan recognition protein family senses fungal infections and activates this pathway. A second detection system perceives the activity of proteolytic f

  16. Thermal solvent-free synthesis of chromonyl chalcones, pyrazolines and their in vitro antibacterial, antifungal activities.

    Science.gov (United States)

    Siddiqui, Zeba N; Praveen, Shagufta; Musthafa, T N Mohammed; Ahmad, Anis; Khan, Asad U

    2012-02-01

    A facile and ecofriendly synthesis of new chromonyl chalcones 3a-b from 3-formylchromone 1 and active methyl compounds 2a-b is reported under thermal solvent-free heating condition in good yields. The chromonyl chalcones 3a-b were used as intermediates under green condition for the synthesis of new bioactive pyrazoline derivatives 4a-f. The compounds were tested for antimicrobial activity by disk diffusion assay with slight modifications against Gram-positive, Gram-negative strains of bacteria as well as fungal strains. The investigation of antimicrobial screening revealed that compounds 3a-b and 4a-f showed antibacterial and antifungal activities.

  17. ANTIFUNGAL AND CYTOTOXIC ACTIVITIES OF FIVE TRADITIONALLY USED INDIAN MEDICINAL PLANTS

    Directory of Open Access Journals (Sweden)

    Adhikarimayum Haripyaree

    2013-02-01

    Full Text Available Hexane, Methanol and Distilled water extracts of five Indian Medicinal plants viz., Mimosa pudica L, Vitex trifolia Linn, Leucas aspera Spreng, Centella asiatica (L Urban and Plantago major Linn belonging to different families were subjected to preliminary antimicrobial screening against six standard organisms viz., Ceratocystis paradoxa, Aspergillus niger, Penicillium citrinum, Macrophomina phaseoli, Trichoderma viride and Rhizopus nigricans. To evaluate antifungal activity agar well diffusion method was used. In addition LD50 of the same plant extracts were determined by using Range test on Mus musculus for cytotoxic activity. Methanolic extract of M. pudica showed the highest and significant inhibitory effect against some fungal species. Again, methanolic extract of M. pudica displayed the greatest cytotoxic activity.

  18. Antifungal activity of different natural dyes against traditional products affected fungal pathogens

    Institute of Scientific and Technical Information of China (English)

    R Mari selvam; AJA Ranjit Singh; K Kalirajan

    2012-01-01

    Objective: In the present study to evaluate the anti fungal activity of natural dyes against traditional products affected fungal pathogens. Methods: Many traditional craft products affected fungal pathogens were isolated using potato dextrose agar medium. The isolated fungus were identified by morphological and microscopically characterization using Alexopolus manual. 50μl of Turmeric, Terminalli, Guava and Henna natural dyes were poured into the wells of the culture plates. If antifungal activity was present on the plates, it was indicated by an inhibition zone surrounding the well containing the natural dye. Result: At a dose level of 50μl of terminalli dye was able to inhibit the growth of all the fungi tested. The absorbance rate of natural dyes analyzed by UV Spectrophotometer. The absorbance rate is high in terminalli (2.266) and turmeric (2.255). Conclusions: Natural dyes were bound with traditional products to give good colour and good antimicrobial activity against isolated fungal pathogens.

  19. Antifungal activity of Aegle marmelos (L.) Correa (Rutaceae) leaf extract on dermatophytes

    Institute of Scientific and Technical Information of China (English)

    Balakumar S; Rajan S; Thirunalasundari T; Jeeva S

    2011-01-01

    Objective: To evaluate the in vitro antifungal activity of Aegle marmelos leaf extracts and fractions on the clinical isolates of dermatophytic fungi like Trichophyton mentagrophytes,Trichophyton rubrum, Microsporum canis, Microsporum gypseum and Epidermophyton floccosum. Methods: The minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) of various extracts and fractions of the leaves of Aegle marmelos were measured using method of National Committee for Clinical Laboratory Standards (NCCLS). Results: Aegle marmelos leaf extracts and fractions were found to have fungicidal activity against various clinical isolates of dermatophytic fungi. The MIC and MFC was found to be high in water and ethyl alcohol extracts and methanol fractions (200μg/mL) against dermatophytic fungi studied. Conclusions:Aegle marmelos leaf extracts significantly inhibites the growth of all dermatophytic fungi studied. If this activity is confirmed by in vivo studies and if the compound is isolated and identified, it could be a remedy for dermatophytosis.

  20. 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.

  1. Antiviral, antifungal, and antiparasitic activities of fluoroquinolones optimized for treatment of bacterial infections: a puzzling paradox or a logical consequence of their mode of action?

    Science.gov (United States)

    Dalhoff, A

    2015-04-01

    This review summarizes evidence that commercially available fluoroquinolones used for the treatment of bacterial infections are active against other non-bacterial infectious agents as well. Any of these fluoroquinolones exerts, in parallel to its antibacterial action, antiviral, antifungal, and antiparasitic actions at clinically achievable concentrations. This broad range of anti-infective activities is due to one common mode of action, i.e., the inhibition of type II topoisomerases or inhibition of viral helicases, thus maintaining the selective toxicity of fluoroquinolones inhibiting microbial topoisomerases at low concentrations but mammalian topoisomerases at much higher concentrations. Evidence suggests that standard doses of the fluoroquinolones studied are clinically effective against viral and parasitic infections, whereas higher doses administered topically were active against Candida spp. causing ophthalmological infections. Well-designed clinical studies should be performed to substantiate these findings.

  2. [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.

  3. 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.

  4. Evaluation of antifungal activity of essential oils against potentially mycotoxigenic Aspergillus flavus and Aspergillus parasiticus

    Directory of Open Access Journals (Sweden)

    Fernanda C. da Silva

    2012-10-01

    Full Text Available The antifungal activity of essential oils of fennel (Foeniculum vulgare Mill., Apiaceae, ginger (Zingiber officinale Roscoe, Zingiberaceae, mint (Mentha piperita L., Lamiaceae and thyme (Thymus vulgaris L., Lamiaceae was evaluated against mycotoxin producers Aspergillus flavus and A. parasiticus. High Resolution Gas Chromatography was applied to analyze chemical constituents of essential oils. The effect of different concentrations of essential oils was determined by solid medium diffusion assay. Mycelial growth and sporulation were determined for each essential oil at the concentrations established by solid medium diffusion assay. At the fifth, seventh and ninth days the mycelial diameter (Ø mm and spore production were also determined. FUN-1 staining was performed to assess cell viability after broth macrodilution assay. Trans-anethole, zingiberene, menthol and thymol are the major component of essential oils of fennel, ginger, mint and thyme, respectively. The effective concentrations for fennel, ginger, mint and thyme were 50, 80, 50 and 50% (oil/DMSO; v/v, respectively. The four essential oils analysed in this study showed antifungal effect. Additionally, FUN-1 staining showed to be a suitable method to evaluate cell viability of potential mycotoxigenic fungi A. flavus and A. parasiticus after treatment with essential oils.

  5. Antifungal activity of nanocapsule suspensions containing tea tree oil on the growth of Trichophyton rubrum.

    Science.gov (United States)

    Flores, F C; de Lima, J A; Ribeiro, R F; Alves, S H; Rolim, C M B; Beck, R C R; da Silva, Cristiane Bona

    2013-04-01

    The aim of this study was to evaluate, for the first time, the antifungal efficacy of nanocapsules and nanoemulsions containing Melaleuca alternifolia essential oil (tea tree oil) in an onychomycosis model. The antifungal activity of nanostructured formulations was evaluated against Trichophyton rubrum in two different in vitro models of dermatophyte nail infection. First, nail powder was infected with T. rubrum in a 96-well plate and then treated with the formulations. After 7 and 14 days, cell viability was verified. The plate counts for the samples were 2.37, 1.45 and 1.0 log CFU mL(-1) (emulsion, nanoemulsion containing tea tree oil and nanocapsules containing tea tree oil, respectively). A second model employed nails fragments which were infected with the microorganism and treated with the formulations. The diameter of fungal colony was measured. The areas obtained were 2.88 ± 2.08 mm(2), 14.59 ± 2.01 mm(2), 40.98 ± 2.76 mm(2) and 38.72 ± 1.22 mm(2) for the nanocapsules containing tea tree oil, nanoemulsion containing tea tree oil, emulsion and untreated nail, respectively. Nail infection models demonstrated the ability of the formulations to reduce T. rubrum growth, with the inclusion of oil in nanocapsules being most efficient.

  6. 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.

  7. An antifungal peptide with antiproliferative activity toward tumor cells from red kidney beans.

    Science.gov (United States)

    Li, Miao; Wang, Hexiang; Ng, Tzi Bun

    2011-06-01

    A 7.3-kDa antifungal peptide was purified from dried red kidney beans. The purification procedure entailed ion exchange chromatography on DEAE-cellulose, affinity chromatography on Affi-gel blue gel, ion exchange chromatography on CM-cellulose, followed by fast protein liquid chromatography-gel filtration on Superdex 75. The peptide was unadsorbed on DEAE-cellulose but adsorbed on Affi-gel blue gel and CM-cellulose. It exhibited a molecular mass of 7.3 kDa in gel filtration and also in SDS-polyacrylamide gel electrophoresis, indicating that it is a single-chained protein. The N-terminal sequence of the peptide was DGVCFGGLANGDRT. The peptide exerted an antifungal action on Fusarium oxysporum with an IC₅₀ of 3.8±0.4 µM (mean±SD, n=3). It also inhibited mycelial growth in Mycosphaerella arachidicola. It suppressed growth of lymphoma MBL2 cells and leukemia L1210 cells with an IC₅₀ of 5.2±0.4 µM and 7.6±0.6 µM, respectively. HIV-1 reverse transcriptase was inhibited with an IC₅₀ of 40±3.2 µM. However, no activity was demonstrated toward other viral enzymes.

  8. Posaconazole/hydroxypropyl-β-cyclodextrin host-guest system: Improving dissolution while maintaining antifungal activity.

    Science.gov (United States)

    Tang, Peixiao; Ma, Xiaoli; Wu, Di; Li, Shanshan; Xu, Kailin; Tang, Bin; Li, Hui

    2016-05-20

    This study aimed to prepare and characterize the inclusion complex between posaconazole (POS) and hydroxypropyl-β-cyclodextrin (HP-β-CD). Phase solubility study was conducted to investigate the drug/CD interaction in solution, including the stoichiometry and apparent stability constant. The solid complex (HP-β-CD-POS) obtained was characterized through Fourier transform infrared spectroscopy, powder X-ray diffraction, (1)H and ROESY 2D nuclear magnetic resonance, differential scanning calorimetry, and scanning electron microscopy. These approaches confirmed the formation of the inclusion complex. The HP-β-CD-POS inclusion complex exhibited better water solubility and higher dissolution rate than the free POS did; the water solubility of POS was increased by 82 times and almost 90% of the loaded drug dissolved after 10 min in the dissolution media. In addition, preliminary in vitro antifungal susceptibility testing revealed that HP-β-CD-POS maintains a high level of antifungal activities. Therefore, the HP-β-CD complex may be useful in the delivery of posaconazole.

  9. Design and Synthesis of Some New 1,3,4-Thiadiazines with Coumarin Moieties and Their Antioxidative and Antifungal Activity

    Directory of Open Access Journals (Sweden)

    Milan Čačić

    2014-01-01

    Full Text Available A series of newly disubstituted (compounds 4a,b and trisubstituted 1,3,4-thiadiazines 5a–l with various substituents was prepared utilizing different thiosemicarbazides and 3-α-bromoacetylcoumarins as starting compounds. The structures of the synthesized 1,3,4-thiadiazines are elucidated and confirmed utilizing the corresponding analytical and spectroscopic data. All of the new thiadiazine derivatives were tested for their antioxidant activity, employing different antioxidant assays (DPPH scavenging activity, iron chelating activity, power reducing activity. Compounds 5b, 5f, 5j and 4b were proven to be the best DPPH radical scavengers, while compounds 5h and 5j have shown the best iron chelating activity. Thiadiazine derivatives were also tested on their antifungal activity against four mycotoxicogenic fungi, Aspergillus flavus, A. ochraceus, Fusarium graminearum and F. verticillioides. The best antifungal against A. flavus was proven to be compound 5e, while compounds 4a and 5c were the best antifungals on A. ochraceus, and compound 5g showed the best antifungal activity on F. verticillioides.

  10. Radiation-induced enhancement of antifungal activity of chitosan on fruit-spoiling fungi during postharvest storage

    Energy Technology Data Exchange (ETDEWEB)

    Diep, Tran Bang; Lam, Nguyen Duy; Quynh, Tran Minh [Institute for Nuclear Science and Technique-VAEC, Hanoi (Viet Nam); Kume, Tamikazu [Japan Atomic Energy Research Inst., Takasaki, Gunma (Japan). Takasaki Radiation Chemistry Research Establishment

    2001-03-01

    Experiment conducted four fruit-spoiling fungal strains that were isolated from spoilt fruits (mango and dragon fruit) and were identified as follows: Fusarium dimerum Penzig, Aspergillus nidulans Wint, Aspergillus fumigatus Fresenius and Aspergillus japonicus Saito. Chitosan samples with various deacetylation degree (70-99%) were irradiated at doses ranging from 20 to 200kGy, then were supplemented to liquid medium for growth of fungi. We have found that chitosan possesses not only well known antibacterial activity but also the antifungal one on fruit-spoiling fungi. Method of fungal cultivation using liquid medium showed that it has higher sensitivity compared with the cultivation on agar plate, so we recommend this method should be used for evaluation of antimicrobial activity of chitosan. Our study also indicated that deacetylation degree of chitosan clearly affects its antifungal activity, the higher the deacetylation of chitosan, stronger antifungal activity can be observed. This finding recommends the use of chitosan with higher deacetylation for fruit coating and other pharmacology utilization. Results from the minimal inhibitory concentrations (MIC) on fungal growth showed that radiation treatment increased antifungal activity of chitosan and dose of 60kGy gave highest activity. (author)

  11. Antifungal activity and isomerization of octadecyl p-coumarates from Ipomoea carnea subsp. fistulosa.

    Science.gov (United States)

    Nidiry, Eugene Sebastian J; Ganeshan, Girija; Lokesha, Ankanahalli N

    2011-12-01

    Bioassay monitored HPLC assisted isolation and purification of the chief antifungal fraction of the leaves of Ipomoea carnea subsp. fistulosa (Convulvulaceae) were achieved using Colletotrichum gloeosporioides and Cladosporium cucumerinum as test organisms. The activity of the purified fraction was further confirmed by the dose dependent inhibition of the spore germination of Alternaria alternata and A. porri. The active fraction was identified as a mixture of (E)-octadecyl p-coumarate and (Z)-octadecyl p-coumarate. The two isomers were detected on an HPLC column with substantially different retention times, but once eluted from the column, one form was partly converted to the other in daylight. Conclusive evidence for the structures and their isomerization were obtained from the HPLC behavior, IR, UV, HRESIMS, CIMS and and NMR spectral data. Important 1H NMR and 13C NMR signals could be separately assigned for the isomers using 2D NMR techniques.

  12. ANTIFUNGAL ACTIVITY OF Cymbopogon nardus (L. Rendle (CITRONELLA AGAINST Microsporum canis FROM ANIMALS AND HOME ENVIRONMENT

    Directory of Open Access Journals (Sweden)

    Isis Regina Grenier CAPOCI

    2015-12-01

    Full Text Available Dermatophytosis is a common zoonosis in urban centers. Dogs and cats have played an important role as its disseminators. Environmental decontamination is essential for the prevention of its propagation to humans and animals. However, sanitizers or disinfectants with antifungal activity, currently available, have high toxicity. The present study evaluated the in vitro effects of an extract of citronella (Cymbopogon nardus on 31 Microsporum canis isolates from animals and home environments. Susceptibility tests were performed based on document M38-A2 (2008 of the Clinical and Laboratory Standards Institute with modifications for natural products. Although susceptibility variation was observed between the fungus tested, the concentrations that inhibited the growth of 50 and 90% of the microorganisms were low (19.5 and 78 µg/mL, respectively. Thus, this citronella extract showed potent fungistatic and fungicide activities against M. canis isolated from animals and home environments. Therefore, it could be an alternative for dermatophytosis prophylaxis in the home environment.

  13. ANTIFUNGAL ACTIVITY OF Cymbopogon nardus (L.) Rendle (CITRONELLA) AGAINST Microsporum canis FROM ANIMALS AND HOME ENVIRONMENT.

    Science.gov (United States)

    Capoci, Isis Regina Grenier; Cunha, Michele Milano da; Bonfim-Mendonça, Patricia de Souza; Ghiraldi-Lopes, Luciana Dias; Baeza, Lilian Cristiane; Kioshima, Erika Seki; Svidzinski, Terezinha Inez Estivalet

    2015-12-01

    Dermatophytosis is a common zoonosis in urban centers. Dogs and cats have played an important role as its disseminators. Environmental decontamination is essential for the prevention of its propagation to humans and animals. However, sanitizers or disinfectants with antifungal activity, currently available, have high toxicity. The present study evaluated the in vitro effects of an extract of citronella (Cymbopogon nardus) on 31 Microsporum canis isolates from animals and home environments. Susceptibility tests were performed based on document M38-A2 (2008) of the Clinical and Laboratory Standards Institute with modifications for natural products. Although susceptibility variation was observed between the fungus tested, the concentrations that inhibited the growth of 50 and 90% of the microorganisms were low (19.5 and 78 µg/mL, respectively). Thus, this citronella extract showed potent fungistatic and fungicide activities against M. canis isolated from animals and home environments. Therefore, it could be an alternative for dermatophytosis prophylaxis in the home environment.

  14. Syntheses, characterization and antifungal activity of novel dimethylbis(N-R-sulfonyldithiocarbimato)stannate(IV) complexes

    Science.gov (United States)

    Bomfim Filho, Lucius F. O.; Oliveira, Marcelo R. L.; Miranda, Liany D. L.; Vidigal, Antonio E. C.; Guilardi, Silvana; Souza, Rafael A. C.; Ellena, Javier; Ardisson, José D.; Zambolim, Laércio; Rubinger, Mayura M. M.

    2017-02-01

    Four new complexes of the general formula: (Ph4P)2[Sn(CH3)2(RSO2Ndbnd CS2)2], where Ph4P = tetraphenylphosphonium cation and R = CH3, (1), CH3CH2 (2), C6H5 (3), 4-FC6H4 (4), were prepared by the reaction of the appropriate potassium N-R-sulfonyldithiocarbimates, K2(RSO2Ndbnd CS2), and tetraphenylphosphonium chloride with dimethyltin dichloride. The compounds 1-4 were characterized by 1H, 13C and 119Sn NMR, 119Sn Mössbauer, vibrational spectroscopy and by elemental analyses of C, H, N and Sn. The crystal structure of 1 was determined by X-ray diffraction techniques. The in vitro antifungal activity of the tin(IV) complexes were evaluated against the fungi Rhizoctonia solani and Botrytis cinerea by the Poisoned food test. The new compounds showed comparable activities to the fungicides manzate and ziram.

  15. A new aurone glycoside with antifungal activity from marine-derived fungus Penicillium sp. FJ-1.

    Science.gov (United States)

    Song, Yan-xia; Ma, Qiang; Li, Jie

    2015-03-01

    Endophytic fungi which reside in the tissue of mangrove plants seem to play an important role in the discovery of new biologically active substances. During the course of screening for the antimicrobial metabolites from the endophytic fugus Penicillium sp. FJ-1 of mangrove plant Avicennia marina, a new aurone glycoside (1) was isolated by repeated column chromatography on silica gel and recrystallization methods. The structure of 1 was elucidated as (Z)-7,4'-dimethoxy-6-hydroxy-aurone-4-O-β-glucopyranoside, on the basis of spectroscopic analysis. Compound 1 exhibited antifungal activity against Candida sp., with the potency comparable to amphotericin B and much better than fluconazole. Compound 1 can also inhibit extracellular phospholipase secretion in a concentration-dependent manner.

  16. Synthesis and Antifungal Activity of Benzamidine Derivatives Carrying 1,2,3-Triazole Moieties

    Directory of Open Access Journals (Sweden)

    Guangyou Chen

    2014-05-01

    Full Text Available Eighteen novel benzamidine derivatives containing 1,2,3-triazole moieties were synthesized. The in vitro and in vivo fungicidal acitivities of the title compounds and the arylamidine intermediates against Colletotrichum lagenarium and Botrytis cinerea were tested. The synthesized benzamidines exhibited weak antifungal activities in vitro against the tested fungi, but some of the compounds showed excellent activities in vivo to the same strains. Among the compounds tested, 9b showed 79% efficacy in vivo against C. lagenarium at a concentration of 200 μg/mL, and the efficacy of compound 16d (90% toward the same strain was even superior than that of the commercial fungicide carbendazim (85%.

  17. Characterization and antifungal activity of gazyumaru (Ficus microcarpa) latex chitinases: both the chitin-binding and the antifungal activities of class I chitinase are reinforced with increasing ionic strength.

    Science.gov (United States)

    Taira, Toki; Ohdomari, Atsuko; Nakama, Naoya; Shimoji, Makiko; Ishihara, Masanobu

    2005-04-01

    Three chitinases, designated gazyumaru latex chitinase (GLx Chi)-A, -B, and -C, were purified from the latex of gazyumaru (Ficus microcarpa). GLx Chi-A,-B, and -C are an acidic class III (33 kDa, pI 4.0), a basic class I (32 kDa, pI 9.3), and a basic class II chitinase (27 kDa, pI > 10) respectively. GLx Chi-A did not exhibit any antifungal activity. At low ionic strength, GLx Chi-C exhibited strong antifungal activity, to a similar extent as GLx Chi-B. The antifungal activity of GLx Chi-C became weaker with increasing ionic strength, whereas that of GLx Chi-B became slightly stronger. GLx Chi-B and -C bound to the fungal cell-walls at low ionic strength, and then GLx Chi-C was dissociated from them by an escalation of ionic strength, but this was not the case for GLx Chi-B. The chitin-binding activity of GLx Chi-B was enhanced by increasing ionic strength. These results suggest that the chitin-binding domain of basic class I chitinase binds to the chitin in fungal cell walls by hydrophobic interaction and assists the antifungal action of the chitinase.

  18. Synthesis, antifungal activity and docking study of 2-amino-4H-benzochromene-3-carbonitrile derivatives

    Science.gov (United States)

    Mirjalili, BiBi Fatemeh; Zamani, Leila; Zomorodian, Kamiar; Khabnadideh, Soghra; Haghighijoo, Zahra; Malakotikhah, Zahra; Ayatollahi Mousavi, Seyyed Amin; Khojasteh, Shaghayegh

    2016-07-01

    Pathogenic fungi are associated with diseases ranging from simple dermatosis to life-threatening infections, particularly in immunocompromised patients. During the past two decades, resistance to established antifungal drugs has increased dramatically and has made it crucial to identify novel antimicrobial compounds. Here, we selected 12 new compounds of 2-amino-4H-benzochromene-3-carbonitrile drivetives (C1-C12) for synthesis by using nano-TiCl4.SiO2 as efficient and green catalyst, then nine of synthetic compounds were evaluated against different species of fungi, positive gram and negative gram of bacteria. Standard and clinical strains of antibiotics sensitive and resistant fungi and bacteria were cultured in appropriate media. Biological activity of the 2-amino-4H-benzochromene-3-carbonitrile derivatives against fungi and bacteries were estimated by the broth micro-dilution method as recommended by clinical and laboratory standard institute (CLSI). In addition minimal fangicidal and bactericial concenteration of the compounds were also determined. Considering our results showed that compound 2-amino-4-(4-methyl benzoate)-4H-benzo[f]chromen-3-carbonitrile (C9) had the most antifungal activity against Aspergillus clavatus, Candida glabarata, Candida dubliniensis, Candida albicans and Candida tropicalis at concentrations ranging from 8 to ≤128 μg/mL. Also compounds 2-amino-4-(3,4-dimethoxyphenyl)-4H-benzo[f]chromen-3-carbonitrile (C4) and 2-amino-4-(4-isopropylphenyl)-4H-benzo[f]chromen-3-carbonitrile (C3) had significant inhibitory activities against Epidermophyton floccosum following 2-amino-4-(4-methylbenzoate)-4H-benzo[f]chromen-3-carbonitrile (C9), respectively. Docking simulation was performed to insert compounds C3, C4 and C9 in to CYP51 active site to determine the probable binding model.

  19. Antifungal activity of essential oil isolated from Ocimum gratissimum L. (eugenol chemotype against phytopathogenic fungi

    Directory of Open Access Journals (Sweden)

    Terezinha de Jesus Faria

    2006-11-01

    Full Text Available An investigation of antifungal activity of the essential oil obtained by steam-distillation (1.1% w/w of the aerial parts of Ocimum gratissimum and of an ethanolic extract from the steam-distillation residue was carried out using the agar diffusion method. The results revealed that the essential oil inhibited the growth of all fungi tested, including the phytopathogens, Botryosphaeria rhodina, Rhizoctonia sp. and two strains of Alternaria sp., while the extract from the residue was inactive. The essential oil was subjected to TLC bioautography used to detect fungitoxic constituents. The compound that showed antifungal activity was isolated and identified as eugenol. GC/MS analysis showed that eugenol was the main constituent of the essential oil studied. The antifungal activity of eugenol was evaluated against a species of Alternaria isolated from tomato (A1 and Penicillium chrysogenum. The minimal inhibitory concentrations of eugenol were 0.16 and 0.31 mg/disc for Alternaria sp. (A1 and P. chrysogenum, respectively.O óleo essencial resultante da destilação por arraste a vapor das partes aéreas de Ocimum gratissimum e o extrato etanólico obtido do resíduo da destilação foram avaliados quanto à atividade antifúngica, utilizando-se o método de difusão em agar. O óleo essencial inibiu o crescimento de todos os fungos testados, incluindo os fitopatogênicos Botryosphaeria rhodina e duas espécies de Alternaria sp, enquanto que o extrato do resíduo da destilação não apresentou atividade. O óleo essencial foi, então, submetido ao método de bioautografia em TLC para detecção do composto ativo. O componente ativo foi isolado e identificado através da análise por cromatografia gasosa acoplada à espectrometria de massas como o eugenol, constituinte majoritário do óleo estudado. Ensaios de atividade antifúngica revelaram a atividade do eugenol contra Alternaria isolada de tomate (A1 e Penicillium chrysogenum. As concentra

  20. General Toxicity and Antifungal Activity of a New Dental Gel with Essential Oil from Abies Sibirica L

    Science.gov (United States)

    Noreikaitė, Aurelija; Ayupova, Rizvangul; Satbayeva, Elmira; Seitaliyeva, Aida; Amirkulova, Marzhan; Pichkhadze, Guram; Datkhayev, Ubaidilla; Stankeviandccaron;ius, Edgaras

    2017-01-01

    Background The aim of this study was to analyze the antifungal activity and the general toxicity of a new dental gel containing essential oil from the tree Abies sibirica L., which grows in the Republic of Kazakhstan. Material/Methods The essential oil from Abies sibirica L. was obtained by microwave heating method using the STARTE Microwave Extraction System. Adjutants used to prepare the oil were carbomer 974P, glycerin, polysorbate 80, xylitol, triethanolamine, and purified water, all allowed for medical usage. The antifungal activity of the essential oil was assessed by monitoring the optical density of Candida albicans in a microplate reader. The safety was determined by analyzing the acute and subacute toxicity. Results The essential oil obtained by the microwave heating method revealed a higher antifungal activity in comparison with the essential oil obtained by the steam distillation method. No obvious changes were detected in guinea pigs following cutaneous application of the gel. Enteral administration of the essential oil caused minimal functional and histological changes in mice after 4 weeks. The new harmless dental gel containing pine oil from Abies sibirica L. was provided for the purposes of this particular clinical research. Conclusions The high antifungal activity of the gel is the basis for more in-depth studies on its safety and pharmacological activity. PMID:28132065

  1. General Toxicity and Antifungal Activity of a New Dental Gel with Essential Oil from Abies Sibirica L.

    Science.gov (United States)

    Noreikaitė, Aurelija; Ayupova, Rizvangul; Satbayeva, Elmira; Seitaliyeva, Aida; Amirkulova, Marzhan; Pichkhadze, Guram; Datkhayev, Ubaidilla; Stankevičius, Edgaras

    2017-01-29

    BACKGROUND The aim of this study was to analyze the antifungal activity and the general toxicity of a new dental gel containing essential oil from the tree Abies sibirica L., which grows in the Republic of Kazakhstan. MATERIAL AND METHODS The essential oil from Abies sibirica L. was obtained by microwave heating method using the STARTE Microwave Extraction System. Adjutants used to prepare the oil were carbomer 974P, glycerin, polysorbate 80, xylitol, triethanolamine, and purified water, all allowed for medical usage. The antifungal activity of the essential oil was assessed by monitoring the optical density of Candida albicans in a microplate reader. The safety was determined by analyzing the acute and subacute toxicity. RESULTS The essential oil obtained by the microwave heating method revealed a higher antifungal activity in comparison with the essential oil obtained by the steam distillation method. No obvious changes were detected in guinea pigs following cutaneous application of the gel. Enteral administration of the essential oil caused minimal functional and histological changes in mice after 4 weeks. The new harmless dental gel containing pine oil from Abies sibirica L. was provided for the purposes of this particular clinical research. CONCLUSIONS The high antifungal activity of the gel is the basis for more in-depth studies on its safety and pharmacological activity.

  2. Antifungal Production of a Strain of Actinomycetes spp Isolated from the Rhizosphere of Cajuput Plant: Selection and Detection of Exhibiting Activity Against Tested Fungi

    Directory of Open Access Journals (Sweden)

    Alimuddin A

    2015-11-01

    Full Text Available Actinomycetes are bacteria known to constitute a large part of the rhizosphere microbiota. Their isolation is an important step for screening of new bioactive compounds. Culturable actinomycetes populations from cajuput plant rhizosphere soils in Wanagama I Forest UGM Yogyakarta were collected to study about their antifungal activity. Among 17 of a total 43 isolates that showed activity were screened for producing antifungi substances. Screening for antifungal activity of isolates were performed with dual culture bioassay in vitro. One isolate that was designated as Streptomyces sp.GMR-22 was the strongest against all tested fungi and appeared promising for a sources of antifungal. Culture’s supernatant and mycelia were extracted with chloroform, ethyl acetate and methanol, respectively. Antifungal activity of crude extracts was tested by diffusion method against tested fungi. The result indicates that isolates of actinomycetes from cajuput plant rhizosphere could be an interesting sources of antifungal bioactive substances.

  3. Chemical composition and antifungal activities of essential oils of Satureja thymbra L. and Salvia pomifera ssp. calycina (Sm.) Hayek

    NARCIS (Netherlands)

    Glamoclija, J.; Sokovic, M.; Vukojevic, J.; Milenkovic, I.; Griensven, van L.J.L.D.

    2006-01-01

    This work covers the chemical composition and antifungal activities of essential oils isolated from savory (Satureja thymbra) and sage (Salvia pomifera ssp. calycina) analyzed using GC/MS. The main components of S. thymbra oil were gamma-terpinene (23.2%) and carvacrol (48.5%). The main components i

  4. 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.

  5. Psc-AFP, an antifungal protein with trypsin inhibitor activity from Psoralea corylifolia seeds.

    Science.gov (United States)

    Yang, Xingyong; Li, Jun; Wang, Xiaowen; Fang, Weiguo; Bidochka, Michael J; She, Rong; Xiao, Yuehua; Pei, Yan

    2006-07-01

    An antifungal protein designated as Psc-AFP, with an apparent molecular mass of 18kDa, was isolated from a traditional Chinese herb, malaytea scurfpea (Psoralea corylifolia L.). The isolation procedure entailed extraction, cation exchange chromatography on CM FF, gel filtration chromatography on Superdex 75 and reversed-phase high performance liquid chromatography on SOURCE 5RPC column. Automated Edman degradation determined the partial N-terminal sequence of Psc-AFP to be NH2-EWEPVQNGGSSYYMVPRIWA, which displayed homology with plant trypsin inhibitors. The protease inhibitor activity of Psc-AFP was then confirmed by the inhibition on trypsin. Psc-AFP at 10 microM inhibited the mycelial growth of Alternari brassicae, Aspergillus niger, Fusarium oxysporum and Rhizoctonia cerealis, suggesting that Psc-AFP has a role in the defense against pathogens.

  6. Antifungal activity of extracts of Rosmarinus officinalis and Thymus vulgaris against Aspergillus flavus and A. ochraceus.

    Science.gov (United States)

    Centeno, S; Calvo, M A; Adelantado, C; Figueroa, S

    2010-05-01

    The antifungal activity of ethanolic extracts of Rosmarinus officinalis and Thymus vulgaris were tested against strains of Aspergillus flavus and A. ochraceus, since these two species are common contaminants of cereals and grains and are able to produce and accumulate mycotoxins. The methodology used is based on measuring the inhibition halos produced by discs impregnated with the extracts and establishing their Minimum Inhibitory Concentration (MIC) as well as the Minimum Fungicide Concentration (MFC). The results obtained suggest that the assayed extracts affect the proper development of A. flavus and A. ochraceus; leading to a lower MIC (1200 ppm) and MFC (2400 ppm) for T. vulgaris extract against A. ochraceus than against A. flavus. The results show, that the extracts of Rosmarinus officinalis and Thymus vulgaris used at low concentrations could have significant potential for the biological control of fungi in foodstuffs.

  7. Evaluation of the antifungal activities of various extracts from Pistacia atlantica Desf

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    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.

  8. Composition of Cassia fistula oil and its antifungal activity by disrupting ergosterol biosynthesis.

    Science.gov (United States)

    Irshad, Md; Ahmad, Aijaz; Zafaryab, Md; Ahmad, Farah; Manzoor, Nikhat; Singh, Man; Rizvi, M Moshahid A

    2013-02-01

    Cassia fistula oil was investigated for antifungal activities against standard and clinical isolates of Candida species. Gas chromatography coupled with mass spectrometric (GC-MS) analysis of C. fistula oil revealed the presence of antimicrobial compounds like beta-sitosterol, stigmasterol, ergosterol, betulinic acid, lupeol, fucosterol, alpha-amyrin and friedelin. The minimum inhibitory concentration (MIC) of the pulp and seed oils ranged between 250-300 and 350-500 microg/mL respectively. Both oils also inhibited by > or = 63.8% ergosterol bio-synthesis in Candida cell wall {fluconazole (standard) > or = 89.1%)}. The MICs were significantly correlated with the ergosterol content decrease in the cell wall (Student's t test p Cassia fistula oil that primarily target ergosterol biosynthesis in Candida cell wall.

  9. Synthesis, Larvicidal Activities and Antifungal Activities of Novel Chlorantraniliprole Derivatives and Their Target in the Ryanodine Receptor

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    Qichao Chen

    2015-03-01

    Full Text Available In order to identify novel chlorantraniliprole derivatives as potential insecticides or fungicides, 25 analogues of chlorantraniliprole were synthesized. The insecticidal activities against oriental armyworm and the antifungal activities against five typical fungi of these derivatives were tested. Compounds 2u, 2x and 2y exhibited good activities against oriental armyworm, especially compounds 2u and 2x which showed higher larvicidal activities than indoxacarb. Moreover, all of the tested compounds exhibited activities against five typical fungi. The Ki values of all synthesized compounds were calculated using AutoDock4. The relationship between the Ki values and the results of insecticidal activities against oriental armyworm further indicated that the membrane-spanning domain protein of the ryanodine receptor might contain chlorantraniliprole binding sites.

  10. 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

  11. Extraction, Chemical Composition, and Antifungal Activity of Essential Oil of Bitter Almond.

    Science.gov (United States)

    Geng, Huiling; Yu, Xinchi; Lu, Ailin; Cao, Haoqiang; Zhou, Bohang; Zhou, Le; Zhao, Zhong

    2016-08-29

    The essential oil from the powder residual of dried bitter almond, a novel and environmentally-friendly fungicide, was successfully extracted in a 0.7% yield by hydro-distillation under optimized conditions. The chemical composition of bitter almond essential oil (BAEO) was analyzed by gas chromatography-mass spectrometry (GC-MS). Twenty-one different components representing 99.90% of the total essential oil were identified, of which benzaldehyde (62.52%), benzoic acid (14.80%), and hexadecane (3.97%) were the most abundant components. Furthermore, the in vitro and in vivo antifungal activities of BAEO against common plant pathogenic fungi were evaluated by the mycelium linear growth rate method and pot test, respectively. It was documented that 1 mg/mL of BAEO could variously inhibit all tested pathogenic fungi with the inhibition rates of 44.8%~100%. Among the tested 19 strains of fungi, the median effective concentration (EC50) values of BAEO against Alternaria brassicae and Alternaria solani were only 50.2 and 103.2 μg/mL, respectively, which were higher than those of other fungi. The in vivo antifungal activity of BAEO against Gloeosporium orbiculare was much higher than Blumeria graminis. The protective efficacy for the former was up to 98.07% at 10 mg/mL and the treatment efficacy was 93.41% at 12 mg/mL. The above results indicated that BAEO has the great potential to be developed as a botanical and agricultural fungicide.

  12. Extraction, Chemical Composition, and Antifungal Activity of Essential Oil of Bitter Almond

    Science.gov (United States)

    Geng, Huiling; Yu, Xinchi; Lu, Ailin; Cao, Haoqiang; Zhou, Bohang; Zhou, Le; Zhao, Zhong

    2016-01-01

    The essential oil from the powder residual of dried bitter almond, a novel and environmentally-friendly fungicide, was successfully extracted in a 0.7% yield by hydro-distillation under optimized conditions. The chemical composition of bitter almond essential oil (BAEO) was analyzed by gas chromatography–mass spectrometry (GC–MS). Twenty-one different components representing 99.90% of the total essential oil were identified, of which benzaldehyde (62.52%), benzoic acid (14.80%), and hexadecane (3.97%) were the most abundant components. Furthermore, the in vitro and in vivo antifungal activities of BAEO against common plant pathogenic fungi were evaluated by the mycelium linear growth rate method and pot test, respectively. It was documented that 1 mg/mL of BAEO could variously inhibit all tested pathogenic fungi with the inhibition rates of 44.8%~100%. Among the tested 19 strains of fungi, the median effective concentration (EC50) values of BAEO against Alternaria brassicae and Alternaria solani were only 50.2 and 103.2 μg/mL, respectively, which were higher than those of other fungi. The in vivo antifungal activity of BAEO against Gloeosporium orbiculare was much higher than Blumeria graminis. The protective efficacy for the former was up to 98.07% at 10 mg/mL and the treatment efficacy was 93.41% at 12 mg/mL. The above results indicated that BAEO has the great potential to be developed as a botanical and agricultural fungicide. PMID:27589723

  13. Extraction, Chemical Composition, and Antifungal Activity of Essential Oil of Bitter Almond

    Directory of Open Access Journals (Sweden)

    Huiling Geng

    2016-08-01

    Full Text Available The essential oil from the powder residual of dried bitter almond, a novel and environmentally-friendly fungicide, was successfully extracted in a 0.7% yield by hydro-distillation under optimized conditions. The chemical composition of bitter almond essential oil (BAEO was analyzed by gas chromatography–mass spectrometry (GC–MS. Twenty-one different components representing 99.90% of the total essential oil were identified, of which benzaldehyde (62.52%, benzoic acid (14.80%, and hexadecane (3.97% were the most abundant components. Furthermore, the in vitro and in vivo antifungal activities of BAEO against common plant pathogenic fungi were evaluated by the mycelium linear growth rate method and pot test, respectively. It was documented that 1 mg/mL of BAEO could variously inhibit all tested pathogenic fungi with the inhibition rates of 44.8%~100%. Among the tested 19 strains of fungi, the median effective concentration (EC50 values of BAEO against Alternaria brassicae and Alternaria solani were only 50.2 and 103.2 μg/mL, respectively, which were higher than those of other fungi. The in vivo antifungal activity of BAEO against Gloeosporium orbiculare was much higher than Blumeria graminis. The protective efficacy for the former was up to 98.07% at 10 mg/mL and the treatment efficacy was 93.41% at 12 mg/mL. The above results indicated that BAEO has the great potential to be developed as a botanical and agricultural fungicide.

  14. Investigating the antifungal activity of TiO{sub 2} nanoparticles deposited on branched carbon nanotube arrays

    Energy Technology Data Exchange (ETDEWEB)

    Darbari, S; Abdi, Y; Haghighi, N [Nano-Physics Research Laboratory, Department of Physics, University of Tehran, Tehran (Iran, Islamic Republic of); Haghighi, F [Department of Medical Mycology, School of Medical Sciences, Tarbiat Modares University, Tehran (Iran, Islamic Republic of); Mohajerzadeh, S, E-mail: y.abdi@ut.ac.ir [Thin Film Laboratory, ECE Department, University of Tehran, Tehran (Iran, Islamic Republic of)

    2011-06-22

    Branched carbon nanotube (CNT) arrays were synthesized by plasma-enhanced chemical vapour deposition on a silicon substrate. Ni was used as the catalyst and played an important role in the realization of branches in vertically aligned nanotubes. TiO{sub 2} nanoparticles on the branched CNTs were produced by atmospheric pressure chemical vapour deposition followed by a 500 {sup 0}C annealing step. Transmission and scanning electron microscopic techniques were used to study the morphology of the TiO{sub 2}/branched CNT structures while x-ray diffraction and Raman spectroscopy were used to verify the characteristics of the prepared nanostructures. Their antifungal effect on Candida albicans biofilms under visible light was investigated and compared with the activity of TiO{sub 2}/CNT arrays and thin films of TiO{sub 2}. The TiO{sub 2}/branched CNTs showed a highly improved photocatalytic antifungal activity in comparison with the TiO{sub 2}/CNTs and TiO{sub 2} film. The excellent visible light-induced photocatalytic antifungal activity of the TiO{sub 2}/branched CNTs was attributed to the generation of electron-hole pairs by visible light excitation with a low recombination rate, in addition to the high surface area provided for the interaction between the cells and the nanostructures. Scanning electron microscopy was used to observe the resulting morphological changes in the cell body of the biofilms existing on the antifungal samples.

  15. In Vitro Investigation of Antifungal Activities of Actinomycetes against Microsporum gypseum

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    Naser Keikha

    2013-02-01

    Conclusion: The findings of the present research show that terrigenous actinomycetes have an antifungal effect upon Microsporum gypseum. So, one hopes that-in future-rather than administering antifungal chemicals that have side-effects, dermatophytic infections can be cured by applying these actinomycetes.

  16. Virilization of the Broad Line Region in Active Galactic Nuclei - connection between shifts and widths of broad emission lines

    CERN Document Server

    Jonic, Sanja; Ilic, Dragana; Popovic, Luka C

    2016-01-01

    We investigate the virilization of the emission lines Hbeta and Mg II in the sample of 287 Type 1 Active Galactic Nuclei taken from the Sloan Digital Sky Survey database. We explore the connections between the intrinsic line shifts and full widths at different levels of maximal intensity. We found that: (i) Hbeta seems to be a good virial estimator of black hole masses, and an intrinsic redshift of Hbeta is dominantly caused by the gravitational effect, (ii) there is an anti-correlation between the redshift and width of the wings of the Mg II line, (iii) the broad Mg II line can be used as virial estimator only at 50% of the maximal intensity, while the widths and intrinsic shifts of the line wings can not be used for this purpose.

  17. Antistaphylococcal activity of ceftobiprole, a new broad-spectrum cephalosporin.

    Science.gov (United States)

    Bogdanovich, Tatiana; Ednie, Lois M; Shapiro, Stuart; Appelbaum, Peter C

    2005-10-01

    Ceftobiprole (formerly BAL9141), the active component of the prodrug BAL5788 (ceftobiprole medocaril), is a novel cephalosporin with expanded activity against gram-positive bacteria. Among 152 Staphylococcus aureus isolates, including 5 vancomycin-intermediate and 2 vancomycin-resistant strains, MIC(50) and MIC(90) values for ceftobiprole were each 0.5 microg/ml against methicillin-susceptible strains and 2 mug/ml against methicillin-resistant strains. Against 151 coagulase-negative staphylococci (including 4 vancomycin-intermediate strains), MIC(50) and MIC(90) values were, respectively, 0.125 microg/ml and 1 microg/ml against methicillin-susceptible and 1 microg/ml and 2 microg/ml against methicillin-resistant strains. Teicoplanin was less active than vancomycin against coagulase-negative strains. Linezolid, quinupristin-dalfopristin, and daptomycin were active against all strains, whereas increased MICs for amoxicillin-clavulanate, cefazolin, minocycline, gentamicin, trimethoprim-sulfamethoxazole, levofloxacin, rifampin, mupirocin, fusidic acid, and fosfomycin were sometimes observed. At 2x MIC, ceftobiprole was bactericidal against 11 of 12 test strains by 24 h. Prolonged serial passage in the presence of subinhibitory concentrations of ceftobiprole failed to select for clones with MICs >4 times those of the parents; the maximum MIC achieved for ceftobiprole after 50 passages (in 1 of 10 strains) was 8 mug/ml. Single-passage selections showed very low frequencies of resistance to ceftobiprole irrespective of genotype or phenotype; the maximal ceftobiprole MIC of recovered clones was 8 mug/ml.

  18. 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.

  19. 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.

  20. Evaluation of antifungal, antimycobacterial and larvicide activity of the Duroia macrophylla and D. saccifera

    Directory of Open Access Journals (Sweden)

    Ana Júlia Reis

    2016-10-01

    Full Text Available Bachground and objective: The wide Amazonian biodiversity has been identified as a source of natural product candidates to various pharmacological activities, particularly in combating infectious diseases. Some species, such as the genus Duroia, belonging to the Rubiaceae family, has been characterized by the production of secondary metabolites with important biological properties, but there are few studies with species of this genus. Thus, the objective of this study was to evaluate the antimycobacterial, antifungal and antiparasitic activity of D. macrophylla and D. saccifera extracts by determining the minimum inhibitory concentration and minimum larvicide concentration. Methods: Were collected plant materials of the D. macrophylla and D. saccifera in Forest Reserve A. Ducke in Manaus AM, from which were prepared dichloromethane, methanol and aqueous extracts and determined the minimum inhibitory concentration and larvicidal concentration. Results: With regard to D. saccifera¸ extracts the dichloromethane extract of the branches was the most active against the fungal species and mycobacterial strains evaluated. On the other hand, the methanol and dichloromethane extract of the D. macrophylla leaves, were most active against Candida sp. and Mycobacterium tuberculosis, respectively, but none of the six evaluated extracts showed antiparasitic activity against Toxocara canis. Conclusion: These results demonstrate the antimicrobial properties of these Amazonian plants for the development of new therapies in the treatment of infectious diseases such as tuberculosis and candidiasis.

  1. 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

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    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.

  2. 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.

  3. Antianaerobe activity of ceftobiprole, a new broad-spectrum cephalosporin.

    Science.gov (United States)

    Ednie, Lois; Shapiro, Stuart; Appelbaum, Peter C

    2007-05-01

    Agar dilution testing of 463 anaerobes showed most Gram-positive beta-lactamase-negative strains (other than some Clostridium difficile and Peptostreptococcus anaerobius), as well as both beta-lactamase-positive and beta-lactamase-negative strains of Fusobacterium nucleatum, to have ceftobiprole MIC values of Ceftobiprole was less active against beta-lactamase-positive Gram-negative bacilli, especially the members of the Bacteroides fragilis group. Like ceftobiprole, piperacillin was active mainly against beta-lactamase-negative strains, though MIC values for piperacillin were often 1 to 2 dilutions higher than for ceftobiprole. Carbapenems had MIC values < or =4 microg/L against all except some C. difficile and 2 strains of B. fragilis. All strains were susceptible to metronidazole, and all bacteria, except C. difficile and a single Bacteroides distasonis strain, were susceptible to chloramphenicol. Clindamycin resistance was seen in most anaerobe groups, whereas high moxifloxacin MICs were found mainly among the B. fragilis and Prevotella groups, and a few C. difficile and F. nucleatum strains.

  4. Improved antifungal activity of itraconazole-loaded PEG/PLA nanoparticles.

    Science.gov (United States)

    Essa, Sherief; Louhichi, Fatiha; Raymond, Martine; Hildgen, Patrice

    2013-01-01

    Poly(ethylene glycol)/polylactic acid (PEG/PLA) nanoparticles (NPs) containing the hydrophobic antifungal itraconazole (ITZ) were developed to provide a controlled release pattern of ITZ as well as to improve its aqueous dispersibility and hence enhance its antifungal action. Two PEG/PLA copolymers (PEGylated PLA polymers) were used in this study; branched PEGylated polymer in which PEG was grafted on PLA backbone at 7% (mol/mol of lactic acid monomer), PEG7%-g-PLA, and multiblock copolymer of PLA and PEG, (PLA-PEG-PLA)n with nearly similar PEG insertion ratio and similar PEG chain length. ITZ-loaded PLA NPs were also prepared and included in this study as a control. ITZ-NPs were prepared from a 1 : 1 w/w blend of PLA and each PEGylated polymer either PEG7%-g-PLA or (PLA-PEG-PLA)n using an oil-in-water emulsion evaporation method. The NPs morphology, size and size distribution, zeta potential, loading efficiency, release profile and antifungal activity were characterized. All ITZ-NPs were nearly spherical with smooth surface and showed less aggregating tendency with a size range of 185-285 nm. All ITZ-NPs measured nearly neutral zeta potential values close to 0 mV. The % LE of ITZ was ∼94% for PEG7%-g-PLA NPs and ∼83% for (PLA-PEG-PLA)n at 15.3% w/w theoretical loading. PEG/PLA NPs were stable over time regarding size and size distribution and % ITZ loading efficiency (% LE). ITZ release showed an initial burst followed by a gradual release profile for ITZ-NPs over 5 days. (PLA-PEG-PLA)n NPs exhibited faster release rates than PEG7%-g-PLA NPs particularly at the last 2 days. Differential scanning calorimetry and powder X-ray diffractometry data confirmed that ITZ exists in an amorphous state or a solid solution state into the NPs matrix. Fourier transform infrared revealed the possibility of chemical interaction between ITZ and the NPs matrix polymer indicating the successful entrapment of ITZ inside the particles. In haemolysis test, ITZ-NPs caused

  5. 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.

  6. Antibacterial and antifungal activities of different parts of Tribulus terrestris L. growing in Iraq

    Institute of Scientific and Technical Information of China (English)

    Firas A. AL-BAYATI; Hassan F. AL-MOLA

    2008-01-01

    Antimicrobial activity of organic and aqueous extracts from fruits, leaves and roots of Tribulus terrestris L., an Iraqi medicinal plant used as urinary anti-infective in folk medicine, was examined against 11 species of pathogenic and non-pathogenic microorganisms: Staphylococcus aureus, Bacillus subtilis, Bacillus cereus, Corynebacterium diphtheriae, Escherichia coli,Proteus vulgaris, Serratia marcescens, Salmonella typhimurium, Klebsiella pneumoniae, Pseudomonas aeruginosa and Candida albicans using microdilution method in 96 multiwell microtiter plates. All the extracts from the different parts of the plant showed antimicrobial activity against most tested microorganisms. The most active extract against both Gram-negative and Gram-positive bacteria was ethanol extract from the fruits with a minimal inhibitory concentration (MIC) value of 0.15 mg/ml against B. subtilis,B. cereus, P. vulgaris and C. diphtheriae. In addition, the same extract from the same plant part demonstrated the strongest antifungal activity against C. albicans with an MIC value of 0.15 mg/ml.

  7. Antifungal Activity and Biochemical Response of Cuminic Acid against Phytophthora capsici Leonian

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    Yong Wang

    2016-06-01

    Full Text Available Phytophthora blight of pepper caused by Phytophthora capsici Leonian is a destructive disease throughout the world. Cuminic acid, extracted from the seed of Cuminum cyminum L., belongs to the benzoic acid chemical class. In this study, the sensitivity and biochemical response of P. capsici to cuminic acid was determined. The mean EC50 (50% effective concentration values for cuminic acid in inhibiting mycelial growth and zoospore germination of the 54 studied P. capsici isolates were 14.54 ± 5.23 μg/mL and 6.97 ± 2.82 μg/mL, respectively. After treatment with cuminic acid, mycelial morphology, sporangium formation and mycelial respiration were significantly influenced; cell membrane permeability and DNA content increased markedly, but pyruvic acid content, adenosine triphosphate (ATP content, and ATPase activity decreased compared with the untreated control. In pot experiments, cuminic acid exhibited both protective and curative activity. Importantly, POD and PAL activity of the pepper leaves increased after being treated with cuminic acid. These indicated that cuminic acid not only showed antifungal activity, but also could improve the defense capacity of the plants. All the results suggested that cuminic acid exhibits the potential to be developed as a new phytochemical fungicide, and this information increases our understanding of the mechanism of action of cuminic acid against Phytophthora capsici.

  8. Antiproliferative, Antibacterial and Antifungal Activity of the Lichen Xanthoria parietina and Its Secondary Metabolite Parietin

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    Adriana Basile

    2015-04-01

    Full Text Available Lichens are valuable natural resources used for centuries throughout the world as medicine, food, fodder, perfume, spices and dyes, as well as for other miscellaneous purposes. This study investigates the antiproliferative, antibacterial and antifungal activity of the acetone extract of the lichen Xanthoria parietina (Linnaeus Theodor Fries and its major secondary metabolite, parietin. The extract and parietin were tested for antimicrobial activity against nine American Type Culture Collection standard and clinically isolated bacterial strains, and three fungal strains. Both showed strong antibacterial activity against all bacterial strains and matched clinical isolates, particularly against Staphylococcus aureus from standard and clinical sources. Among the fungi tested, Rhizoctonia solani was the most sensitive. The antiproliferative effects of the extract and parietin were also investigated in human breast cancer cells. The extract inhibited proliferation and induced apoptosis, both effects being accompanied by modulation of expression of cell cycle regulating genes such as p16, p27, cyclin D1 and cyclin A. It also mediated apoptosis by activating extrinsic and intrinsic cell death pathways, modulating Tumor Necrosis Factor-related apoptosis-inducing ligand (TRAIL and B-cell lymphoma 2 (Bcl-2, and inducing Bcl-2-associated agonist of cell death (BAD phosphorylation. Our results indicate that Xanthoria parietina is a major potential source of antimicrobial and anticancer substances.

  9. Antifungal activity of some 2,2':5',2"-terthiophene derivatives.

    Science.gov (United States)

    Mares, D; Romagnoli, C; Rossi, R; Carpita, A; Ciofalo, M; Bruni, A

    1994-01-01

    The dermatophyte Microsporum cookei Ajello was treated with nine new natural and synthetic 2,2':5',2"-terthiophenes to determine their possible antifungal activity. In the dark the thiophenes were inactive, while when photoactivated with UV-A they induced a remarkable reduction in the growth rate of the fungus. The only exception was (E)-N-(2-methylpropyl)-3-(2,2':5',2"-terthien-5-yl)-propenamide , which was not fungistatic even at the highest dose tested (24 microM). The more active compounds were 3'-methoxy-2,2':5',2"-terthiophene and 3'-methylthio-2,2':5',2"-terthiophene, whose activity seems to be related to the presence of a substituent in the 3' position of the central ring of thiophenes. Transmission electron microscopic observations demonstrated the photoactive nature of the synthetic molecules to be similar to that of alpha-terthienyl, a natural thiophene present in some Asteraceae. The dark treatment caused only the accumulation of the compound in vacuoles, without other evident alterations. After UV-A irradiation the activated thiophene causes severe modifications to the endomembrane system, probably via oxygen-dependent mechanism.

  10. Antibacterial and Antifungal Activity of Biopolymers Modified with Ionic Liquid and Laponite.

    Science.gov (United States)

    Sharma, Anshu; Prakash, Prem; Rawat, Kamla; Solanki, Pratima R; Bohidar, H B

    2015-09-01

    In the present study, the antimicrobial properties of modified biopolymers such as gelatin and agar have been investigated. These biopolymers (agar and gelatin) are modified by dissolving in ionic liquid (IL) [1-ethyl-3-methylimidazolium chloride ([C2mim][Cl]) and 1-octyl-3-methyl imidazolium chloride ([C8mim][Cl])] solutions. It was noticed that agar-ionogel (Ag-IL), gelatin-ionogel (GB-IL), and gelatin organogel (gelatin-glycerol solution along with laponite, nanoclay) nanocomposite (GA-NC) formed are highly stable, optically clear, and transparent without any air bubbles. The antimicrobial activity of these (Ag-IL), (GB-IL), and GA-NC were analyzed for both gram-negative (Escherichia coli, Klebsiella pneumoniae) and gram-positive bacterial strains (Staphylococcus aureus and Staphylococcus pyogenes) and fungus A. niger, C. albicans. Antibacterial and antifungal activity studies were carried out at different dilutions such as 100, 99, and 90 % (v/v). It was found that Ag-IL, GB-IL, and individual IL ([C8mim][Cl]) exhibited superior antimicrobial activities, indicating that longer IL chain enhance the cell membrane permeability of S. aureus, S. pyogenes, and E. coli cells. However, GA-NC nanocomposite and [C2mim][Cl]-based composites does not exhibit any bacterial inhibition activity for all bacterial strains.

  11. Isolation and characterization of a novel lectin with antifungal and antiproliferative activities from Sophora alopecuroides seeds

    Institute of Scientific and Technical Information of China (English)

    Tinging Li; Xiaoli Yin; Dongliang Liu; Xiaojin Ma; Hui Lv; Surong Sun

    2012-01-01

    Sophora alopecuroides lectin (SAL),a novel lectin from the seeds of Sophora alopecuroides,was purified by ionexchange chromatography on diethylaminoethyl (DEAE)-and carboxymethyl (CM)-Sepharose columns,followed by gel filtration on a Sephadex 75 10/300 GL column.SAL was found to be a monomer of 39916.3 Da,as determined by tricine-sodium dodecyl sulphate-polyacrylamide gel electrophoresis and high-performance liquid chromato-graphy (HPLC).The N-terminal 10-amino acid sequence of SAL,KPWALSFSFG,resembles those of other legume lectins.SAL exhibits hemagglutinating activity against rabbit erythrocytes at 11.9 μg/ml.Its hemagglutinating activity is stable in the pH range 7-11 and in the temperature range 30-90℃,and is stimulated by Mn2+.The hemagglutinating activity of SAL is most potently inhibited by 50-mM D-galactose.SAL suppresses mycelial growth in Penicillium digitatum and Alternaria alternata;the IC50 of the antifungal activity toward P.digitatum and A.alternata were found to be 3.125 and 3.338 μM,respectively.SAL suppresses the proliferation of human cervical cancer cells (HeLa) at an ICso of 6.25 μM (P< 0.05).But it has no inhibiting effect on bacteria.This is the first report of a lectin from seeds of S.alopecuroides.

  12. The behavior of active bactericidal and antifungal coating under visible light irradiation

    Energy Technology Data Exchange (ETDEWEB)

    Xiao, Gang; Zhang, Xiaodong; Zhao, Yan; Su, Haijia, E-mail: suhj@mail.buct.edu.cn; Tan, Tianwei

    2014-02-15

    In the present paper, the novel active bactericidal and antifungal coatings (ABAC) have been prepared through the immobilization of Fe-doped TiO{sub 2} (anatase) with chitosan. The characterization of ABAC using optical microscope imaging, SEM, AFM and FTIR shows that the Fe doped TiO{sub 2} is embedded into the chitosan coating with favorable dispersion through the hydrogen bonds interaction between chitosan molecules and TiO{sub 2}. The contact angle measurement demonstrated the hydrophilicity of ABAC (θ = 34.5 ± 4.1°). The bactericidal activity of ABAC has been evaluated by inactivating three different test strains: Escherichia coli, Candida albicans and Aspergillus niger which illustrates the apparently higher bactericidal ability than chitosan, Fe-TiO{sub 2} and chitosan/TiO{sub 2} (pure) under visible light irradiation and its bactericidal activity is lasting for at least 24 h. ABAC showed rapid and efficient antibacterial ability for the three tested strains and its antibacterial ratio in 2 h for E. coli, C. albicans and A. niger was 99.9%, 97.0% and 95.0%, respectively. The prepared chitosan/TiO{sub 2} composite emulsion shows favorable storage stability and can be stored up to 1 year without losing its bactericidal activity. ABAC is a low-cost and eco-friendly antibacterial coating products and promising for domestic, medical and industrial applications.

  13. Antioxidant, antifungal and anticancer activities of se-enriched Pleurotus spp. mycelium extracts

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    Milovanović Ivan

    2014-01-01

    Full Text Available The goal of this study was the evaluation of antifungal, antioxidant and anticancer potentials of Pleurotus eryngii, P. ostreatus and P. pulmonarius mycelial extracts, and the influence of mycelium enrichment with selenium on these activities. Both Se-amended and non-amended extracts showed the same or similar minimal inhibitory concentration for 14 studied micromycetes, while a fungicidal effect was not noted, contrary to ketoconazole, which had inhibitory and fungicidal effects at very low concentrations. Se-non-amended extracts exhibited antioxidant activity, especially at higher concentrations. Selenium enrichment influenced activity, its effects decreasing in P. eryngii and P. pulmonarius, while in P. ostreatus no effect was noted. The DPPH• radical scavenging capacity of the extracts was in direct correlation with their phenol and flavonoid contents. Cytotoxic activity against both HeLa and LS174 cell lines was very low compared with cis-DDP. These features suggest that mycelium should be an object of intensive studies. [Projekat Ministarstva nauke Republike Srbije, br. 173032

  14. Peptides from the scorpion Vaejovis punctatus with broad antimicrobial activity.

    Science.gov (United States)

    Ramírez-Carreto, Santos; Jiménez-Vargas, Juana María; Rivas-Santiago, Bruno; Corzo, Gerardo; Possani, Lourival D; Becerril, Baltazar; Ortiz, Ernesto

    2015-11-01

    The antimicrobial potential of two new non-disulfide bound peptides, named VpAmp1.0 (LPFFLLSLIPSAISAIKKI, amidated) and VpAmp2.0 (FWGFLGKLAMKAVPSLIGGNKSSSK) is here reported. These are 19- and 25-aminoacid-long peptides with +2 and +4 net charges, respectively. Their sequences correspond to the predicted mature regions from longer precursors, putatively encoded by cDNAs derived from the venom glands of the Mexican scorpion Vaejovis punctatus. Both peptides were chemically synthesized and assayed against a variety of microorganisms, including pathogenic strains from clinical isolates and strains resistant to conventional antibiotics. Two shorter variants, named VpAmp1.1 (FFLLSLIPSAISAIKKI, amidated) and VpAmp2.1 (FWGFLGKLAMKAVPSLIGGNKK), were also synthesized and tested. The antimicrobial assays revealed that the four synthetic peptides effectively inhibit the growth of both Gram-positive (Staphylococcus aureus and Streptococcus agalactiaea) and Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacteria, with MICs in the range of 2.5-24.0 μM; yeasts (Candida albicans and Candida glabrata) with MICs of 3.1-50.0 μM; and two clinically isolated strains of Mycobacterium tuberculosis-including a multi-drug resistant one- with MICs in the range of 4.8-30.5 μM. A comparison between the activities of the original peptides and their derivatives gives insight into the structural/functional role of their distinctive residues.

  15. Antipneumococcal activity of ceftobiprole, a novel broad-spectrum cephalosporin.

    Science.gov (United States)

    Kosowska, Klaudia; Hoellman, Dianne B; Lin, Gengrong; Clark, Catherine; Credito, Kim; McGhee, Pamela; Dewasse, Bonifacio; Bozdogan, Bülent; Shapiro, Stuart; Appelbaum, Peter C

    2005-05-01

    Ceftobiprole (previously known as BAL9141), an anti-methicillin-resistant Staphylococcus aureus cephalosporin, was very highly active against a panel of 299 drug-susceptible and -resistant pneumococci, with MIC(50) and MIC(90) values (microg/ml) of 0.016 and 0.016 (penicillin susceptible), 0.06 and 0.5 (penicillin intermediate), and 0.5 and 1.0 (penicillin resistant). Ceftobiprole, imipenem, and ertapenem had lower MICs against all pneumococcal strains than amoxicillin, cefepime, ceftriaxone, cefotaxime, cefuroxime, or cefdinir. Macrolide and penicillin G MICs generally varied in parallel, whereas fluoroquinolone MICs did not correlate with penicillin or macrolide susceptibility or resistance. All strains were susceptible to linezolid, quinupristin-dalfopristin, daptomycin, vancomycin, and teicoplanin. Time-kill analyses showed that at 1x and 2x the MIC, ceftobiprole was bactericidal against 10/12 and 11/12 strains, respectively. Levofloxacin, moxifloxacin, vancomycin, and teicoplanin were each bactericidal against 10 to 12 strains at 2x the MIC. Azithromycin and clarithromycin were slowly bactericidal, and telithromycin was bactericidal against only 5/12 strains at 2x the MIC. Linezolid was mainly bacteriostatic, whereas quinupristin-dalfopristin and daptomycin showed marked killing at early time periods. Prolonged serial passage in the presence of subinhibitory concentrations of ceftobiprole failed to yield mutants with high MICs towards this cephalosporin, and single-passage selection showed very low frequencies of spontaneous mutants with breakthrough MICs towards ceftobiprole.

  16. 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.

  17. Optically active antifungal azoles. V. Synthesis and antifungal activity of stereoisomers of 3-azolyl-2-(substituted phenyl)-1-(1H-1,2,4-triazol-1-yl)-2- butanols.

    Science.gov (United States)

    Tasaka, A; Tsuchimori, N; Kitazaki, T; Hiroe, K; Hayashi, R; Okonogi, K; Itoh, K

    1995-03-01

    The (2S,3S)-, (2R,3S)- and (2S,3R)-stereoisomers of (2R,3R)-3-azolyl-2-(substituted phenyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanols [(2R,3R)-1a--d] were prepared and evaluated for antifungal activity against Candida albicans in vitro and in vivo to clarify the relationships between stereochemistry and biological activities. The results revealed that the in vitro antifungal activity in each set of the four stereoisomers [(2R,3R)-, (2S,3S)-, (2R,3S)- and (2S,3R)-1a--d] definitely paralleled the in vivo antifungal activity against candidosis in mice, and the order of potency was (2R,3R) > (2R,3S) > or = (2S,3S) > or = (2S,3R). In addition, the four stereoisomers in each set were assessed for sterol biosynthesis-inhibitory activities in C. albicans and rat liver. The (2R,3R)-isomer was found to exert a strong and selective inhibitory effect on the sterol synthesis in C. albicans as compared with that in rat liver.

  18. Antifungal and proteolytic activities of endophytic fungi isolated from Piper hispidum Sw.

    Science.gov (United States)

    Orlandelli, Ravely Casarotti; de Almeida, Tiago Tognolli; Alberto, Raiani Nascimento; Polonio, Julio Cesar; Azevedo, João Lúcio; Pamphile, João Alencar

    2015-06-01

    Endophytes are being considered for use in biological control, and the enzymes they secrete might facilitate their initial colonization of internal plant tissues and direct interactions with microbial pathogens. Microbial proteases are also biotechnologically important products employed in bioremediation processes, cosmetics, and the pharmaceutical, photographic and food industries. In the present study, we evaluated antagonism and competitive interactions between 98 fungal endophytes and Alternaria alternata, Colletotrichum sp., Phyllosticta citricarpa and Moniliophthora perniciosa. We also examined the proteolytic activities of endophytes grown in liquid medium and conducted cup plate assays. The results showed that certain strains in the assemblage of P. hispidum endophytes are important sources of antifungal properties, primarily Lasiodiplodia theobromae JF766989, which reduced phytopathogen growth by approximately 54 to 65%. We detected 28 endophytes producing enzymatic halos of up to 16.40 mm in diameter. The results obtained in the present study highlight the proteolytic activity of the endophytes Phoma herbarum JF766995 and Schizophyllum commune JF766994, which presented the highest enzymatic halo diameters under at least one culture condition tested. The increased activities of certain isolates in the presence of rice or soy flour as a substrate (with halos up to 17.67 mm in diameter) suggests that these endophytes have the potential to produce enzymes using agricultural wastes.

  19. Antifungal and Antioxidant Activities of the Essential Oil from Angelica koreana Nakai.

    Science.gov (United States)

    Roh, Junghyun; Shin, Seungwon

    2014-01-01

    Purpose. The purpose of this study is to determine the antifungal and antioxidant activities of the essential oil from Angelica koreana. Methods. Essential oil was obtained from the dried roots of A. koreana by steam distillation, and its composition was identified by gas chromatography and mass spectrometry (GC-MS). The minimal inhibitory concentrations (MICs) of the oil fraction and its main components were determined by broth dilution assay using common pathogenic Aspergillus and Trichophyton species. The combined effects of the oils with itraconazole were evaluated using a checkerboard titer test. In addition, 1,1-diphenyl-2-picryl-hydrazil (DPPH) free radical scavenging, nitrite inhibition, and reducing power were determined to assess the antioxidant activity of this oil. Results. The essential oil fraction and its main components showed inhibitory activity against all of the tested fungi, with minimal inhibitory concentrations (MICs) of 250-1000 μg/mL. Furthermore, this oil exhibited synergism when combined with itraconazole. Conclusion. In the treatment of infections caused by Aspergillus and Trichophyton species, combining itraconazole with either A. koreana essential oil or its main components may reduce the minimum effective dose of itraconazole required and, thus, minimize its side effects. In addition, this oil is a promising source of natural antioxidant agents.

  20. Antifungal activity of extracts from three species of lichens in Cuba.

    Directory of Open Access Journals (Sweden)

    Daymara Idonay Vaillant-Flores

    2015-06-01

    Full Text Available The objective of this work was to evaluate the antifungal activity of the three lichens extracts. Extracts from Leptogium cyanescens, Physcia americana and Pyxine aff. cocoes were collected from the lichens thallus in 2009 in areas fromo the Cienfuegos Botanic Garden, Cuba. The fungicide activity was evaluated against phytopathogens fungi of potato: Rhizoctonia solani and Phytophthora nicotianae var parasitica. The study was conducted from 2009 to 2011. The compounds were extracted with acetone, concentrated by rotoevaporation, and evaluated at concentrations of 0,01 and 0,07% in potato dextrose agar (PDA culture medium; stock solution was made of 5% dimethilsufoxide. These extracts were classified by their toxicity as: toxic, slight and moderately toxic and harmless. The extracts from P. americana of 0,07% inhibited P. nicotianae 100%, and it showed values over 50% for R. solani. L. cyanescens only showed fungicide activity in both phytopathogens at the maximum concentration studied; similar results were obtained with the extract from P. aff. cocoes. The lichens extracts were classified as lightly toxic at the maximum concentration, and harmless at the minimum concentration.

  1. Antifungal and proteolytic activities of endophytic fungi isolated from Piper hispidum Sw

    Directory of Open Access Journals (Sweden)

    Ravely Casarotti Orlandelli

    2015-06-01

    Full Text Available Endophytes are being considered for use in biological control, and the enzymes they secrete might facilitate their initial colonization of internal plant tissues and direct interactions with microbial pathogens. Microbial proteases are also biotechnologically important products employed in bioremediation processes, cosmetics, and the pharmaceutical, photographic and food industries. In the present study, we evaluated antagonism and competitive interactions between 98 fungal endophytes and Alternaria alternata, Colletotrichum sp., Phyllosticta citricarpa and Moniliophthora perniciosa. We also examined the proteolytic activities of endophytes grown in liquid medium and conducted cup plate assays. The results showed that certain strains in the assemblage of P. hispidum endophytes are important sources of antifungal properties, primarily Lasiodiplodia theobromae JF766989, which reduced phytopathogen growth by approximately 54 to 65%. We detected 28 endophytes producing enzymatic halos of up to 16.40 mm in diameter. The results obtained in the present study highlight the proteolytic activity of the endophytes Phoma herbarum JF766995 and Schizophyllum commune JF766994, which presented the highest enzymatic halo diameters under at least one culture condition tested. The increased activities of certain isolates in the presence of rice or soy flour as a substrate (with halos up to 17.67 mm in diameter suggests that these endophytes have the potential to produce enzymes using agricultural wastes.

  2. 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.

  3. Antifungal activity of Helichrysum italicum (Roth G. Don (Asteraceae essential oil against fungi isolated from cultural heritage objects

    Directory of Open Access Journals (Sweden)

    Stupar Miloš

    2014-01-01

    Full Text Available There is considerable interest in the use of essential oils as alternative methods to control micromycetes from cultural heritage objects. We investigated the chemical composition and antifungal activity of the essential oil of Helichrysum italicum. The main components of the oil were γ-curcumene (22.45%, α-pinene (15.91 % and neryl acetate (7.85 %. H. italicum essential oil showed moderate antifungal activity against fungi isolated from cultural heritage objects. The most susceptible fungi to oil treatment were Epicoccum nigrum and Penicillium sp., while the most resistant was Trichoderma viride. The H. italicum essential oil showed demelanizing activity against Aspergillus niger. [Projekat Ministarstva nauke Republike Srbije, br. 173032

  4. 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

  5. Characterization of inhibitory mechanism and antifungal activity between group-1 and group-2 phytocystatins from taro (Colocasia esculenta).

    Science.gov (United States)

    Wang, Ke-Ming; Kumar, Senthil; Cheng, Yi-Sheng; Venkatagiri, Shripathi; Yang, Ai-Hwa; Yeh, Kai-Wun

    2008-10-01

    Tarocystatin from Colocasia esculenta, a group-2 phytocystatin, is a defense protein against phytopathogenic nematodes and fungi. It is composed of a highly conserved N-terminal region, which is homological to group-1 cystatin, and a repetitive peptide at the C-terminus. The purified recombinant proteins of tarocystatin, such as full-length (FL), N-terminus (Nt) and C-terminus (Ct) peptides, were produced and their inhibitory activities against papain as well as their antifungal effects were investigated. Kinetic analysis revealed that FL peptide exhibited mixed type inhibition (K(ia) = 0.098 microM and K(ib) = 0.252 microM) and Nt peptide showed competitive inhibition (K(i) = 0.057 microM), whereas Ct peptide possessed weak papain activation properties. A shift in the inhibitory pattern from competitive inhibition of Nt peptide alone to mixed type inhibition of FL peptide implied that the Ct peptide has an regulatory effect on the function of FL peptide. Based on the inhibitory kinetics of FL (group-2) and Nt (group-1) peptides on papain activity, an inhibitory mechanism of group-2 phytocystatins and a regulatory mechanism of extended Ct peptide have each been proposed. By contrast, the antifungal activity of Nt peptide appeared to be greater than that of FL peptide, and the Ct peptide showed no effect on antifungal activity, indicating that the antifungal effect is not related to proteinase inhibitory activity. The results are valid for most phytocystatins with respect to the inhibitory mechanism against cysteine proteinase.

  6. Synthesis, characterisation and antifungal activity of chemically and fungal-produced silver nanoparticles against Trichophyton rubrum

    OpenAIRE

    Pereira, Leonel; Dias, Nicolina; Carvalho,Juliana de; Fernandes, Sara; Santos, Cledir; Lima, Nelson

    2014-01-01

    Aims To characterise and explore the potential in extracellular biosynthesis of silver nanoparticles (AgNPs) by Penicillium chrysogenum and Aspergillus oryzae and to investigate the antifungal effect of chemically vs. biologically synthesised AgNPs comparing with conventional antifungal drugs against Trichophyton rubrum. Methods and Results Chemically synthesised AgNPs (Chem-AgNPs) coated with polyvinylpyrrolidone (PVP) were synthesised by chemical reduction method with glucose in PV...

  7. Antitumor and Antifungal Activities of Organic Extracts of SeacucumberHolothuria atra from the Southeast Coast of India

    Institute of Scientific and Technical Information of China (English)

    Devaraj Isaac DHINAKARAN; Aaron Premnath LIPTON

    2015-01-01

    In phylum Echinodermata, the family Holothuridae is distinguished by its capacity of bioactive compounds. Sea cu-cumberHolothuria atra is commonly known as the lollyfish. The antifungal activity was detected using agar well diffusion method against the various fungal strains such asTrichoderma viride, Aspergillus niger,Aspergillus flavis,Candida albicansandPenicillium chrysogenum. Relatively high antifungal activity was seen againstCandida albicans at 100µL−1 concentration of extracts. Zone of inhibition was measured at 18mm of diameter. The anti-tumor activities were detected against the Vero and Hep2 cell lines using MTT assay. The cells were treated withH. atra extract at concentrations 0.078−10mgmL−1. The extract showed high proliferative activity against the Hep2 cells. The body wall extracts of sea cucumber (H. atra)showed effective antifungal and antitumor activities. All these findings suggest that the extracts could be used for the development of drugs.

  8. In vitro evaluation of dill seed essential oil antifungal activities to control Zymoseptoria tritici.

    Science.gov (United States)

    Deweer, C; Yaguiyan, A; Muchembled, J; Sahmer, K; Dermont, C; Halama, P

    2013-01-01

    Zymoseptoria tritici (teleomorph: Mycosphaerella graminicola) is the causal agent of Septoria Leaf Blotch of wheat (up to 40% yield loss). The study aims to evaluate the antifungal activities of dill seed Essential Oil (EO) on this pathogen to investigate an alternative solution to decrease the use of synthetic fungicides in the context of sustainable agriculture. Thus, two strains of Zymoseptoria tritici in relation to their sensitivity to DOMIs were tested in microplates (S6, sensitive strain; R1187, resistant strain). The essays were repeatedly carried out with dill seed EO crude, with Tween 80 (5% v/v) or with DMSO (1% v/v). A range of nine EO dilutions were tried out in comparison to two fungicides: a DMI (metconazole) and a SDHI (Boscalid). A Gas Chromatography - Mass Spectrometry (GC-MS) analysis reveals that dill seed EO is mostly composed of Carvone (45%) and Limonene (25%). Consequently, D-Carvone/L-Carvone and D-Limonene/L-Limonene were tested as well to determine the origins of the EO effectiveness observed. The IC50 (half maximal inhibitory concentration) are calculated and then statistically analysed to find significant differences between each product tested. The comparison of the IC50 shows that S6 is more sensitive to metconazole than R1187 but they both have the same sensitivity to Boscalid. Dill seed EO, D-Carvone/L-Carvone have the same effectiveness on S6 whatever the preparation tested. D-Limonene/L-Limonene are less efficient unless they are supplemented with Tween 80. On R1187, Dill seed EO is more efficient when it is prepared with Tween 80. This efficiency is also observed for D-Carvone/L-Carvone whatever the preparation tested. D-Limonene/L-Limonene are generally less efficient than Carvone even if L-limonene is as efficient as L-Carvone when these products are prepared with Tween 80. Dill seed EO used crude or with DMSO is more efficient on S6 (350 mg/L) than on R1187 (1000 mg/L) but with Tween 80, the EO effectiveness is the same on

  9. [Induction, purification and antifungal activity of beta-1, 3-glucanase from wheat leaves].

    Science.gov (United States)

    Sun, Bin; Li, Duo-Chuan; Ci, Xiao-Yan; Guo, Run-Fang; Wang, Ying

    2004-08-01

    Treatment with mercuric chloride (0.01%), salicylic acid (10.0 mg/mL) or riboflavin (1 mmol/L) induced the beta-1, 3-glucanase activity in all the three wheat varieties i.e. 331, Kangdao 680 and Lumai 23 tested, with the strongest inductive effect on variety 331 by treatment with mercuric chloride (0.01%) for 24 h. From leaves of variety 331 treated with mercuric chloride (0.01%) for 24 h, a kind of beta-1, 3-glucanase was purified by fractional precipitation with ammonium sulphate, Phenyl-Sepharose chromatography (Phenyl-Sepharose Fast Flow), ion-exchange chromatography (DEAE-Sepharose Fast Flow) and gel-filtration chromatography (Sephacryl S-100). Through SDS-PAGE and gel filtration, the molecular weight of the purified beta-1, 3-glucanase was determined to be about 52.0-53.6 kD. The purified beta-1, 3-glucanase showed antifungal activity against both Alternaria longipes and Rhizoctonia cerealis on tested plates, and inhibited the germ tube elongation and spore germination of Verticillium dahliae and Fusarium omysporum f.sp cucumerinum.

  10. 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.

  11. Syntheses, crystal structure, spectroscopic characterization and antifungal activity of new N-R-sulfonyldithiocarbimate metal complexes.

    Science.gov (United States)

    Alves, Leandro C; Rubinger, Mayura M M; Lindemann, Renata H; Perpétuo, Genivaldo J; Janczak, Jan; Miranda, Liany D L; Zambolim, Laércio; Oliveira, Marcelo R L

    2009-07-01

    Five new compounds with the general formula of (Bu(4)N)(2)[M(RSO(2)NCS(2))(2)], where Bu(4)N=tetrabutylammonium cation, (M=Ni, R=4-FC(6)H(4)) (1), (M=Zn, R=4-FC(6)H(4), 4-ClC(6)H(4), 4-BrC(6)H(4), 4-IC(6)H(4)), (2), (3), (4) and (5), respectively, were obtained by the reaction of the appropriate potassium N-R-sulfonyldithiocarbimate (RSO(2)N=CS(2)K(2)) with nickel(II) chloride hexahydrate or zinc(II) acetate dihydrate in metanol:water 1:1. The elemental analyses and the IR data are consistent with the formation of the expected bis(dithiocarbimato)metal(II) complexes. The (1)H and (13)C NMR spectra showed the signals for the tetrabutylammonium cation and the dithiocarbimate moieties. The compounds 1, 2 and 5 were also characterized by X-ray diffraction techniques. The nickel(II) is coordinated by two N-4-fluorophenylsulphonyldithiocarbimato(2-) ligands forming a planar coordination. The zinc(II) exhibits distorted tetrahedral configuration in compounds 2 and 5 due to the chelation effect of two sulfur atoms of the N-R-sulfonyldithiocarbimate ligands. The antifungal activities of the compounds were tested in vitro against Colletotrichum gloeosporioides, an important fungus that causes the plant disease known as anthracnose in fruit trees. All the complexes were active.

  12. Design, synthesis, antifungal, and antioxidant activities of (E)-6-((2-phenylhydrazono)methyl)quinoxaline derivatives.

    Science.gov (United States)

    Zhang, Mao; Dai, Zhi-Cheng; Qian, Shao-Song; Liu, Jun-Yan; Xiao, Yu; Lu, Ai-Min; Zhu, Hai-Liang; Wang, Jian-Xin; Ye, Yong-Hao

    2014-10-01

    Different substituted phenylhydrazone groups were linked to the quinoxaline scaffold to provide 26 compounds (6a-6z). Their structures were confirmed by (1)H and (13)C NMR, MS, elemental analysis, and X-ray single-crystal diffraction. The antifungal activities of these compounds against Rhizoctonia solani were evaluated in vitro. Compound 6p is the most promising one among all the tested compounds with an EC50 of 0.16 μg·mL(-1), more potent than the coassayed positive control fungicide carbendazim (EC50: 1.42 μg·mL(-1)). In addition, these compounds were subjected to antioxidant assay by employing diphenylpicrylhydrazyl (DPPH) and mice microsome lipid peroxidation (LPO) methods. Most of these compounds are potent antioxidants. The strongest compounds are 6e (EC50: 7.60 μg·mL(-1), DPPH) and 6a (EC50: 0.96 μg·mL(-1), LPO), comparative to or more potent than the positive control Trolox [EC50: 5.90 μg·mL(-1) (DPPH) and 18.23 μg·mL(-1) (LPO)]. The structure and activity relationships were also discussed.

  13. Antifungal Activity and Aflatoxin Degradation of Bifidobacterium Bifidum and Lactobacillus Fermentum Against Toxigenic Aspergillus Parasiticus

    Science.gov (United States)

    Ghazvini, Roshanak Daie; Kouhsari, Ebrahim; Zibafar, Ensieh; Hashemi, Seyed Jamal; Amini, Abolfazl; Niknejad, Farhad

    2016-01-01

    Food and feedstuff contamination with aflatoxins (AFTs) is a serious health problem for humans and animals, especially in developing countries. The present study evaluated antifungal activities of two lactic acid bacteria (LAB) against growth and aflatoxin production of toxigenic Aspergillus parasiticus. The mycelial growth inhibition rate of A. parasiticus PTCC 5286 was investigated in the presence of Bifidobacterium bifidum PTCC 1644 and Lactobacillus fermentum PTCC 1744 by the pour plate method. After seven days incubation in yeast extract sucrose broth at 30°C, the mycelial mass was weighed after drying. The inhibitory activity of LAB metabolites against aflatoxin production by A. parasiticus was evaluated using HPLC method. B. bifidum and L. fermentum significantly reduced aflatoxin production and growth rate of A. parasiticus in comparison with the controls (p≤0.05). LAB reduced total aflatoxins and B1, B2, G1 and G2 fractions by more than 99%. Moreover, LAB metabolites reduced the level of standard AFB1, B2, G1 and G2 from 88.8% to 99.8% (p≤0.05). Based on these findings, B. bifidum and L. fermentum are recommended as suitable biocontrol agents against the growth and aflatoxin production by aflatoxigenic Aspergillus species. PMID:28077976

  14. Antifungal activity of resveratrol against Botrytis cinerea is improved using 2-furyl derivatives.

    Directory of Open Access Journals (Sweden)

    Francesco Caruso

    Full Text Available The antifungal effect of three furyl compounds closely related to resveratrol, (E-3,4,5-trimethoxy-β-(2-furyl-styrene (1, (E-4-methoxy-β-(2-furyl-styrene (2 and (E-3,5-dimethoxy-β-(2-furyl-styrene (3 against Botrytis cinerea was analyzed. The inhibitory effect, at 100 µg ml(-1 of compounds 1, 2, 3 and resveratrol on conidia germination, was determined to be about 70%, while at the same concentration pterostilbene (a dimethoxyl derivative of resveratrol produced complete inhibition. The title compounds were more fungitoxic towards in vitro mycelial growth than resveratrol and pterostilbene. Compound 3 was the most active and a potential explanation of this feature is given using density functional theory (DFT calculations on the demethoxylation/demethylation process. Compound 3 was further evaluated for its effects on laccase production, oxygen consumption and membrane integrity of B. cinerea. An increase of the laccase activity was observed in the presence of compound 3 and, using Sytox Green nucleic acid stain, it was demonstrated that this compound altered B. cinerea membrane. Finally, compound 3 partially affected conidia respiration.

  15. Impurities contained in antifungal drug ketoconazole are potent activators of human aryl hydrocarbon receptor.

    Science.gov (United States)

    Grycová, Aneta; Dořičáková, Aneta; Dvořák, Zdeněk

    2015-12-03

    Antifungal drug ketoconazole is a mixture of (+)/(-) cis-enantiomers, which also contains several impurities. Ketoconazole was identified as an activator of aryl hydrocarbon receptor AhR by three independent research teams. In the current paper we demonstrate that impurities contained in ketoconazole preparations are strong activators of human AhR and inducers of CYP1A1. Impurity IMP-C had similar potency (EC50), but 10-15 times higher efficacy (magnitude of induction) towards AhR, comparing to (+)-ketoconazole, as revealed by gene reporter assay in AZ-AHR stably transfected cells. Impurities IMP-B and IMP-C, and in lesser extent IMP-E, induced a formation of AhR-DNA complex, as demonstrated by electromobility shift assay EMSA. Impurities IMP-C and IMP-E dose-dependently induced CYP1A1 mRNA after 24 h, and their effects were comparable to those by (+)-ketoconazole. The level of CYP1A1 protein in HepG2 cells was strongly increased by IMP-C after 48h. In conclusion, our data further elucidated molecular effects of ketoconazole towards AhR signaling pathway, with possible implications in ketoconazole role in skin chemoprevention and/or damage, involving AhR.

  16. 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.

  17. Neural network modelling of antifungal activity of a series of oxazole derivatives based on in silico pharmacokinetic parameters

    Directory of Open Access Journals (Sweden)

    Kovačević Strahinja Z.

    2013-01-01

    Full Text Available In the present paper, the antifungal activity of a series of benzoxazole and oxazolo[ 4,5-b]pyridine derivatives was evaluated against Candida albicans by using quantitative structure-activity relationships chemometric methodology with artificial neural network (ANN regression approach. In vitro antifungal activity of the tested compounds was presented by minimum inhibitory concentration expressed as log(1/cMIC. In silico pharmacokinetic parameters related to absorption, distribution, metabolism and excretion (ADME were calculated for all studied compounds by using PreADMET software. A feedforward back-propagation ANN with gradient descent learning algorithm was applied for modelling of the relationship between ADME descriptors (blood-brain barrier penetration, plasma protein binding, Madin-Darby cell permeability and Caco-2 cell permeability and experimental log(1/cMIC values. A 4-6-1 ANN was developed with the optimum momentum and learning rates of 0.3 and 0.05, respectively. An excellent correlation between experimental antifungal activity and values predicted by the ANN was obtained with a correlation coefficient of 0.9536. [Projekat Ministarstva nauke Republike Srbije, br. 172012 i br. 172014

  18. ORIGINAL ARTICLE: Antifungal Activity of Some Natural Essential Oils against Candida Species Isolated from Blood Stream Infection

    Directory of Open Access Journals (Sweden)

    Amit Kumar

    2012-01-01

    Full Text Available Background: Candida is a part of normal microflora of human body and exists as an opportunistic pathogen as it attacks immunocompromised patients. Aims and Objectives: Candida is the most commonly isolated organism from blood stream infections. Fluconazole is the major antifungal drug used for treatment of Candida. Resistance to fluconazole has been increasing in recent years so there should be search of some other alternative. To find out these alternatives, anti candidial activity of some natural essential oils was studied. Materials and Methods: In the present study nine Candida strains isolated from blood stream infections were collected from National Culture Collection of Pathogenic Fungi (N.C.C.P.F. P.G.I.M.E.R Chandigarh India and the antifungal activity of some natural essential oils such as lemongrass oil, coconut oil, almond oil and clove oil was checked by using agar diffusion method. Result: All oils have shown a significantly anti-candidal activity. However, the antifungal activity was maximum in lemongrass oil. Conclusion: Our study may help to design new chemotherapeutic strategies against Candidal infections.

  19. Antifungal activity of Coriandrum sativum essential oil, its mode of action against Candida species and potential synergism with amphotericin B.

    Science.gov (United States)

    Silva, Filomena; Ferreira, Susana; Duarte, Andreia; Mendonça, Dina I; Domingues, Fernanda C

    2011-12-15

    The increasing incidence of drug-resistant pathogens and toxicity of existing antifungal compounds has drawn attention towards the antimicrobial activity of natural products. The aim of the present study was to evaluate the antifungal activity of coriander essential oil according to classical bacteriological techniques, as well as with flow cytometry. The effect of the essential oil upon germ tube formation, seen as an important virulence factor, and potential synergism with amphotericin B were also studied. Coriander essential oil has a fungicidal activity against the Candida strains tested with MLC values equal to the MIC value and ranging from 0.05 to 0.4% (v/v). Flow cytometric evaluation of BOX, PI and DRAQ5 staining indicates that the fungicidal effect is a result of cytoplasmic membrane damage and subsequent leakage of intracellular components such as DNA. Also, concentrations bellow the MIC value caused a marked reduction in the percentage of germ tube formation for C. albicans strains. A synergetic effect between coriander oil and amphotericin B was also obtained for C. albicans strains, while for C. tropicalis strain only an additive effect was observed. This study describes the antifungal activity of coriander essential oil on Candida spp., which could be useful in designing new formulations for candidosis treatment.

  20. Antifungal Activity, Toxicity and Chemical Composition of the Essential Oil of Coriandrum sativum L. Fruits

    Directory of Open Access Journals (Sweden)

    Erika H. S. Brito

    2012-07-01

    Full Text Available The aims of this study were to test the antifungal activity, toxicity and chemical composition of essential oil from C. sativum L. fruits. The essential oil, obtained by hydro-distillation, was analyzed by gas chromatography/mass spectroscopy. Linalool was the main constituent (58.22%. The oil was considered bioactive, showing an LC50 value of 23 µg/mL in the Artemia salina lethality test. The antifungal activity was evaluated against Microsporum canis and Candida spp. by the agar-well diffusion method and the minimum inhibitory concentration (MIC and the minimum fungicidal concentration (MFC were established by the broth microdilution method. The essential oil induced growth inhibition zones of 28 ± 5.42 and 9.25 ± 0.5 for M. canis and Candida spp. respectively. The MICs and MFCs for M. canis strains ranged from 78 to 620 and 150 to 1,250 µg/mL, and the MICs and MFCs for Candida spp strains ranged from 310 to 620 and 620 to 1,250 µg/mL, respectively. C. sativum essential oil is active in vitro against M. canis and Candida spp. demonstrating good antifungal activity.

  1. Antifungal activity of storage 2S albumins from seeds of the invasive weed dandelion Taraxacum officinale Wigg.

    Science.gov (United States)

    Odintsova, T I; Rogozhin, E A; Sklyar, I V; Musolyamov, A K; Kudryavtsev, A M; Pukhalsky, V A; Smirnov, A N; Grishin, E V; Egorov, T A

    2010-04-01

    In this work, we isolated and characterized novel antifungal proteins from seeds of dandelion (Taraxacum officinale Wigg.). We showed that they are represented by five isoforms, each consisting of two disulphide-bonded large and small subunits. One of them, To-A1 was studied in detail, including N-terminal amino acid sequencing of both subunits, and shown to display sequence homology with the sunflower 2S albumin. Using different assays we demonstrated that dandelion 2S albumins possess inhibitory activity against phytopathogenic fungi and the oomycete Phytophtora infestans at micromolar concentrations with various isoforms differing in their antifungal activity. Thus, 2S albumins of dandelion seeds represent a novel example of storage proteins with defense functions.

  2. 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.

  3. Essential oil composition, phytotoxic and antifungal activities of Ruta chalepensis L. leaves from High Atlas Mountains (Morocco).

    Science.gov (United States)

    Bouajaj, Sana; Romane, Abderrahmane; Benyamna, Abdennaji; Amri, Ismail; Hanana, Mohsen; Hamrouni, Lamia; Romdhane, Mehrez

    2014-01-01

    This study aimed at the determination of chemical composition of essential oil obtained by hydrodistillation, and to evaluate their phytotoxic and antifungal activities. Leaves of Ruta chalepensis L. were collected from the region of Tensift Al Haouz (High Atlas Mountains) Marrakech, Morocco. The essential oil (oil yield is 0.56%) was analysed by GC-FID and GC/MS. Twenty-two compounds were identified and accounted for 92.4% of the total oil composition. The major components were undecan-2-one (49.08%), nonan-2-one (33.15%), limonene (4.19%) and decanone (2.71%). Antifungal ability of essential oils was tested by disc agar diffusion against five plant pathogenic fungi: Fusarium proliferatum, Fusarium pseudograminearum, Fusarium culmorum, Fusarium graminearum and Fusarium polyphialidicum. The oils were also tested in vitro for herbicidal activity by determining their influence on the germination and the shoot and root growth of two weed species, Triticum durum and Phalaris canariensis L.

  4. Aaptamine Derivatives with Antifungal and Anti-HIV-1 Activities from the South China Sea Sponge Aaptos aaptos

    Directory of Open Access Journals (Sweden)

    Hao-Bing Yu

    2014-12-01

    Full Text Available Five new alkaloids of aaptamine family, compounds (1–5 and three known derivatives (6–8, have been isolated from the South China Sea sponge Aaptos aaptos. The structures of all compounds were unambiguously elucidated by spectroscopic analyses, as well as by comparison with the literature data. Compounds 1–2 are characterized with triazapyrene lactam skeleton, whereas compounds 4–5 share an imidazole-fused aaptamine moiety. These compounds were evaluated in antifungal and anti-HIV-1 assays. Compounds 3, 7, and 8 showed antifungal activity against six fungi, with MIC values in the range of 4 to 64 μg/mL. Compounds 7–8 exhibited anti-HIV-1 activity, with inhibitory rates of 88.0% and 72.3%, respectively, at a concentration of 10 μM.

  5. Antibacterial and antifungal activity of streptomycetes isolated from Portonova coastal environment. Papers presented in the symposium held at Cochin, India, 16-17 September 1993

    Digital Repository Service at National Institute of Oceanography (India)

    Lakshmanaperumalsamy, P.; Chandramohan, D.; Natarajan, R.

    The antibacterial and antifungal activities of 518 streptomycetes strains were tested against Bacillus circulans, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Saccharomyces cerevisiae and Fusarium oxysporum. 27.03% of the strains...

  6. A comparative in vitro study on antifungal and antioxidant activities of Nervilia aragoana and Atlantia monophylla.

    Science.gov (United States)

    Reddy, K Himakar; Sharma, P V G K; Reddy, O V S

    2010-05-01

    Ethyl acetate extract of the whole plant of Nervilia aragoana Gaud. (Orchidaceae) and ethanol extract of the leaves of Atlantia monophylla Linn. (Rutaceae) were evaluated for antifungal and antioxidant activities. At 5 mg/mL concentration of the extracts, the former exhibited more inhibitory activity than the latter against fungi. The order of MIC values for Nervilia aragoana were Saccharomyces cerevisiae (1.4 mg/mL) > Aspergillus niger (1.2 mg/mL) > Aspergillus fumigatus (0.95 mg/mL) > Cryptococcus neoformans (0.75 mg/mL). In the case of Atlantia monophylla values were Cryptococcus neoformans (1 mg/mL) > Candida albicans (0.95 mg/mL) > Aspergillus niger (0.65 mg/mL). TLC-DPPH method assay was carried out to evaluate the antioxidant potential. Further DPPH radical, superoxide, nitric oxide, H(2)O(2) scavenging, and reducing power activities were carried out. N. aragoana (85%) extract exhibited more scavenging activity than that of A. monophylla (66%) by DPPH free radical scavenging method. A. monophylla extract exhibited more superoxide, nitric oxide, H(2)O(2) scavenging activities than that of N. aragoana. The acute toxicity studies of both extracts have shown no mortality rate even up to 3 g/kg body weight in albino rats. Screening for secondary metabolites showed the presence of carbohydrates in both extracts. Flavonoids were found only in the ethyl acetate extract of N. aragoana. Tannins, alkaloids, triterpenoids and steroids were present in A. monophylla. Total phenols present in N. aragoana and A. monophylla were 340 and 560 mg/g extract of gallic acid equivalents, respectively.

  7. Antifungal Activity of Isolated Bacillus amyloliquefaciens SYBC H47 for the Biocontrol of Peach Gummosis.

    Science.gov (United States)

    Li, Xunhang; Zhang, Yanzhou; Wei, Zhiwen; Guan, Zhengbing; Cai, Yujie; Liao, Xiangru

    2016-01-01

    The gummosis disease is caused by Botryosphaeria dothidea (Moug. ex. Fr) Ces. et de Not., and it is one of the most important diseases of stone fruits worldwide. The use of biocontrol as an alternative approach to synthetic chemical fungicides has aroused general concern about how to control plant diseases that are caused by phytopathogens. The aim of this study is to isolate Bacillus strains from raw honeys with the capacity to inhibit B. dothidea and to explore the mechanisms by which they could be used in the biocontrol of peach gummosis. Bacillus amyloliquefaciens SYBC H47 was isolated and identified on the basis of its physiological and biochemical characteristics and its 16S rRNA and gyrB gene sequences. The cell suspension and the cell-free supernatant of its culture showed significant antifungal activity against Aspergillus niger, Mucor racemosus, Fusarium oxysporum, Penicillium citrinum, and Candida albicans by agar-diffusion assays. The primary antifungal substances were bacillomycin L, fengycin, and surfactin, which were analyzed by HPLC LC/ESI-MS/MS. Bacillomycin L showed the best inhibitory effect against conidial germination of B. dothidea, followed by fengycin and surfactin. Surfactin had limited effects on mycelial growth, contrary to those of bacillomycin L and fengycin. However, a mixture of the three lipopeptides had a synergistic effect that disrupted the structure of the conidia and mycelia. In order to reduce the production cost, the use of waste frying peanut oil and soy oil as the sole carbon source increased the lipopeptide yield levels by approximately 17% (2.42 g/L) and 110% (4.35 g/L), respectively. In a field trial, the decreases in the infected gummosis rate (IGR) and the disease severity index (DSI) through cell suspension treatments were 20% and 57.5% (in 2014), respectively, and 40% and 57.5% (in 2015), respectively, in comparison with the control. In conclusion, B. amyloliquefaciens SYBC H47 could inhibit the germination of conidia

  8. Antifungal Activity of Isolated Bacillus amyloliquefaciens SYBC H47 for the Biocontrol of Peach Gummosis

    Science.gov (United States)

    Zhang, Yanzhou; Wei, Zhiwen; Guan, Zhengbing; Cai, Yujie; Liao, Xiangru

    2016-01-01

    The gummosis disease is caused by Botryosphaeria dothidea (Moug. ex. Fr) Ces. et de Not., and it is one of the most important diseases of stone fruits worldwide. The use of biocontrol as an alternative approach to synthetic chemical fungicides has aroused general concern about how to control plant diseases that are caused by phytopathogens. The aim of this study is to isolate Bacillus strains from raw honeys with the capacity to inhibit B. dothidea and to explore the mechanisms by which they could be used in the biocontrol of peach gummosis. Bacillus amyloliquefaciens SYBC H47 was isolated and identified on the basis of its physiological and biochemical characteristics and its 16S rRNA and gyrB gene sequences. The cell suspension and the cell-free supernatant of its culture showed significant antifungal activity against Aspergillus niger, Mucor racemosus, Fusarium oxysporum, Penicillium citrinum, and Candida albicans by agar-diffusion assays. The primary antifungal substances were bacillomycin L, fengycin, and surfactin, which were analyzed by HPLC LC/ESI-MS/MS. Bacillomycin L showed the best inhibitory effect against conidial germination of B. dothidea, followed by fengycin and surfactin. Surfactin had limited effects on mycelial growth, contrary to those of bacillomycin L and fengycin. However, a mixture of the three lipopeptides had a synergistic effect that disrupted the structure of the conidia and mycelia. In order to reduce the production cost, the use of waste frying peanut oil and soy oil as the sole carbon source increased the lipopeptide yield levels by approximately 17% (2.42 g/L) and 110% (4.35 g/L), respectively. In a field trial, the decreases in the infected gummosis rate (IGR) and the disease severity index (DSI) through cell suspension treatments were 20% and 57.5% (in 2014), respectively, and 40% and 57.5% (in 2015), respectively, in comparison with the control. In conclusion, B. amyloliquefaciens SYBC H47 could inhibit the germination of conidia

  9. In Vitro Antifungal Activity and Mode of Action of 2',4'-Dihydroxychalcone against Aspergillus fumigatus.

    Science.gov (United States)

    Seo, Young Ho; Kim, Sung-Su; Shin, Kwang-Soo

    2015-06-01

    2',4'-Dihydroxychalcone (2',4'-DHC) was identified from a heat shock protein 90 (Hsp90)-targeting library as a compound with Hsp90 inhibitory and antifungal effects. In the presence of 2',4'-DHC (8 µg/mL), radial growth of Aspergillus fumigatus was inhibited 20% compared to the control, and green pigmentation was completely blocked. The expression of the conidiation-associated genes abaA, brlA, and wetA was significantly decreased (approximately 3- to 5-fold) by treatment with 2',4'-DHC. The expression of calcineurin signaling components, cnaA and crzA, was also significantly reduced. The inhibitory effects of 2',4'-DHC on metabolic activity and mycelial growth were significantly enhanced by combination treatment with itraconazole and caspofungin. Docking studies indicated that 2',4'-DHC bind to the ATPase domain of Hsp90. These results suggest that 2',4'-DHC act as an Hsp90-calcinurin pathway inhibitor.

  10. In Vitro Antifungal Activity against Oral Candida Species Using a Denture Base Coated with Silver Nanoparticles

    Directory of Open Access Journals (Sweden)

    Yoshiaki Kamikawa

    2014-01-01

    Full Text Available Although oral Candida easily adheres to denture base materials, many denture detergents are effective only against bacteria but not against Candida. Silver nanoparticles (AgNPs, which are known to have potent antibacterial and antifungal activity, have been used in the prevention of oral candidiasis (OC. We evaluated the adherence of Candida albicans and Candida glabrata on a heat-cured Acron resin piece supported by AgNPs by low-vacuum scanning electron microscopy (SEM and measuring colony-forming units. C. albicans and C. glabrata increasingly adhered to the resin surface of the control piece over time, but the adhesion AgNP of both Candida species to the AgNP-coated surface was significantly inhibited (P<0.001. Low-vacuum SEM revealed that C. albicans and C. glabrata on the resin surface of control pieces appeared as oval colonies, with a major axis of 3-4 μm and a smooth cell wall, but those on the AgNP-coated resin surface were less abundant than the control and showed swollen yeast features, with a major axis of more than 5 μm and a corrugated cell wall. Our results suggest a way to prevent denture-associated OC by using denture base materials processed by AgNPs.

  11. SYNTHESIS AND ANTIFUNGAL ACTIVITY OF PALMITIC ACID-BASED NEOGLYCOLIPIDS RELATED TO PAPULACANDIN D

    Directory of Open Access Journals (Sweden)

    Thiago Belarmino de Souza

    2015-12-01

    Full Text Available A series of six new palmitic acid-based neoglycolipids related to Papulacandin D were synthesized in five steps, resulting in good yields, and they were evaluated against Candida spp. All twelve synthetic intermediates were also evaluated. The synthesis involved the initial glycosylation of two phenols (4-hydroxy-3-methoxybenzaldehyde and 3-hydroxybenzaldehyde via their reaction with peracetylated glucosyl bromide. This was followed by deacetylation with potassium methoxide/metanol solution and the protection of two hydroxyls (C4 and C6 positions of the saccharide unit as benzilidene acetals (10-11. The next step involved the acylation of the acetal derivatives with palmitic acid, thereby affording a mixture of two isomers mono-acylated at the C2 and C3 positions and a di-acylated product (12-17. After being isolated, each compound was subjected to the removal of the acetal protecting group to yield the papulacandin D analogues 18-23. Three compounds showed low antifungal activity against two species: C. albicans (compounds 7 and 23 and C. tropicalis (compound 17 at 200 µg mL−1.

  12. Combination of CuO nanoparticles and fluconazole: preparation, characterization, and antifungal activity against Candida albicans

    Science.gov (United States)

    Weitz, Iris S.; Maoz, Michal; Panitz, Daniel; Eichler, Sigal; Segal, Ester

    2015-08-01

    Combination therapy becomes an important strategy in the management of invasive fungal infections and emergence of resistant fungi mutants. In this work, we examine the combination of copper oxide (CuO) nanoparticles (NPs) with fluconazole as potential treatment against the pathogenic fungi, Candida albicans. CuO NPs ( 7 nm in size) were synthesized with acetate ligands assembled on their surface, as shown by both thermal gravimetric analysis and FTIR spectroscopy. Unlike the commercial CuO (both bulk and 50 nm particles), that are poorly dispersed in water, the interaction with water allows the fine dispersion of the coated CuO NPs and their excellent colloidal stability. The addition of fluconazole to the aqueous CuO dispersion induced spontaneous self-assembly of the NPs into linear pearl-like chains network, shown by cryogenic transmission electron microscopy (cryo-TEM). The antifungal activity of the CuO NPs and their combination with fluconazole (fluconazole-CuO NPs) was studied against C. albicans. The best MIC values were obtained at concentrations as low as 0.2 and 0.3 mg/mL, respectively. The results suggest that fluconazole-CuO NPs can provide a potential alternative treatment for C. albicans infections.

  13. Antifungal activity of commercial ethanolic and aqueous extracts of Brazilian propolis against Candida spp.

    Directory of Open Access Journals (Sweden)

    S. M.D. Dias

    2009-01-01

    Full Text Available

    Fourteen commercial ethanolic extracts (EEP and five aqueous extracts (AEP of Brazilian propolis were tested for antifungal activity in vitro by employing the agar diffusion assay to determine the susceptibility of Candida spp. Nystatin (100 IU, sterile distilled water and ethanol 93.2ºGL were used as positive, negative and solvent controls. Except for one sample, all EEP tested inhibited the in vitro growth of Candida spp., while the AEP extracts were only weakly inhibitory to the growth of these microorganisms. Four EEP products exhibited inhibition zones similar to those induced by nystatin. It was concluded that the commercial EEP extracts were more effective against Candida spp. than the aqueous extracts. This suggests that EEP could be used as an alternative medicine for the treatment of fungal infections of the oral cavity, such as oral candidosis (thrush or denture stomatitis. Keywords: ethanolic extract; aqueous extract; Brazilian propolis; Candida spp.

  14. Antifungal Activity of Chitosan on Fusarium sulphureum in Relation to Dry Rot of Potato Tuber

    Institute of Scientific and Technical Information of China (English)

    LI Yong-cai; SUN Xiao-juan; BI Yang; GE Yong-hong; WANG Yi

    2009-01-01

    The antifungal activity of chitosan on Fusarium sulphureum in relation to the inhibitory effect on dry rot of potato tuber was investigated.The results showed spore germination and mycelial growth of F.sulphureura were inhibited by ehitosan treatment and the inhibitory effect was highly correlated with ehitosan concentration used in this study.Morphological changes such as intertwisting hyphal,distortion,and swelling with excessive branching were observed by scanning electron microscopy (SEM) observation.Transmission electron microscopy (TEM) observation further indicated the ultrastructural alterations of hyphae.These changes included abnormal distribution of eytoplasma,non-membraneous inclusion bodies assembling in cytoplasm,considerable thickening of the hyphal cellular walls,and very frequent septation with malformed septa.Application of chitosan at higher concentration caused serious damage to fungal hyphae,including cellular membrane disorganisation,cell wall disruption,and breaking of inner cytoplast.New hyphae (daughter hyphae) inside the collapsed hyphal cells was often detected in the cytoplasm of ehitosan-treated hyphae.In vivo tests showed that chitosan treatment at 0.5 or 1% effectively controlled the dry rot of potato tuber inoculated with a spore suspension ofF.sulphureum.However,the chitosan treatment at 1% caused phytotoxicity to potato tuber.This study suggests that the use of ehitosan could be a promising handling as a natural fungicide to partially substitute for the synthetic fungicides in potato tuber.

  15. Combination of CuO nanoparticles and fluconazole: preparation, characterization, and antifungal activity against Candida albicans

    Energy Technology Data Exchange (ETDEWEB)

    Weitz, Iris S., E-mail: irisweitz@braude.ac.il; Maoz, Michal; Panitz, Daniel [ORT Braude College, Department of Biotechnology Engineering (Israel); Eichler, Sigal; Segal, Ester [Technion – Israel Institute of Technology, Department of Biotechnology and Food Engineering (Israel)

    2015-08-15

    Combination therapy becomes an important strategy in the management of invasive fungal infections and emergence of resistant fungi mutants. In this work, we examine the combination of copper oxide (CuO) nanoparticles (NPs) with fluconazole as potential treatment against the pathogenic fungi, Candidaalbicans. CuO NPs (∼7 nm in size) were synthesized with acetate ligands assembled on their surface, as shown by both thermal gravimetric analysis and FTIR spectroscopy. Unlike the commercial CuO (both bulk and 50 nm particles), that are poorly dispersed in water, the interaction with water allows the fine dispersion of the coated CuO NPs and their excellent colloidal stability. The addition of fluconazole to the aqueous CuO dispersion induced spontaneous self-assembly of the NPs into linear pearl-like chains network, shown by cryogenic transmission electron microscopy (cryo-TEM). The antifungal activity of the CuO NPs and their combination with fluconazole (fluconazole–CuO NPs) was studied against C. albicans. The best MIC values were obtained at concentrations as low as 0.2 and 0.3 mg/mL, respectively. The results suggest that fluconazole–CuO NPs can provide a potential alternative treatment for C. albicans infections.

  16. Streptomyces gamaensis sp. nov., a novel actinomycete with antifungal activity isolated from soil in Gama, Chad.

    Science.gov (United States)

    Zhao, Shanshan; Ye, Lan; Liu, Chongxi; Abagana, Adam Yacoub; Zheng, Weiwei; Sun, Pengyu; Li, Jiansong; Xiang, Wensheng; Wang, Xiangjing

    2016-12-22

    During an investigation exploring potential sources of novel species and natural products, a novel actinomycete with antifungal activity, designated strain NEAU-Gz11(T), was isolated from a soil sample, which was collected from Gama, Chad. The isolate was found to have morphological and chemotaxonomic characteristics typical of members of the genus Streptomyces. 16S rRNA gene sequence similarity studies showed that strain NEAU-Gz11(T) belongs to the genus Streptomyces with high sequence similarity to Streptomyces hiroshimensis JCM 4098(T) (98.0 %). Similarities to other type strains of the genus Streptomyces were lower than 98.0 %. However, the physiological and biochemical characteristics and low levels of DNA-DNA relatedness could differentiate the isolate genotypically and phenotypically from S. hiroshimensis JCM 4098(T). Therefore, the strain is concluded to represent a novel species of the genus Streptomyces, for which the name Streptomyces gamaensis sp. nov. is proposed. The type strain is NEAU-Gz11(T) (=CGMCC 4.7304(T)=DSM 101531(T)).

  17. Antifungal activity against plant pathogens of metabolites from the endophytic fungus Cladosporium cladosporioides.

    Science.gov (United States)

    Wang, Xiaoning; Radwan, Mohamed M; Taráwneh, Amer H; Gao, Jiangtao; Wedge, David E; Rosa, Luiz H; Cutler, Horace G; Cutler, Stephen J

    2013-05-15

    Bioassay-guided fractionation of Cladosporium cladosporioides (Fresen.) de Vries extracts led to the isolation of four compounds, including cladosporin, 1; isocladosporin, 2; 5'-hydroxyasperentin, 3; and cladosporin-8-methyl ether, 4. An additional compound, 5',6-diacetylcladosporin, 5, was synthesized by acetylation of compound 3. Compounds 1-5 were evaluated for antifungal activity against plant pathogens. Phomopsis viticola was the most sensitive fungus to the tested compounds. At 30 μM, compound 1 exhibited 92.7, 90.1, 95.4, and 79.9% growth inhibition against Colletotrichum acutatum , Colletotrichum fragariae , Colletotrichum gloeosporioides , and P. viticola, respectively. Compound 2 showed 50.4, 60.2, and 83.0% growth inhibition at 30 μM against Co. fragariae, Co. gloeosporioides, and P. viticola, respectively. Compounds 3 and 4 were isolated for the first time from Cl. cladosporioides. Moreover, the identification of essential structural features of the cladosporin nuclei has also been evaluated. These structures provide new templates for the potential treatment and management of plant diseases.

  18. Chemical composition and antifungal activity of essential oil from Cicuta virosa L. var. latisecta Celak.

    Science.gov (United States)

    Tian, Jun; Ban, Xiaoquan; Zeng, Hong; He, Jingsheng; Huang, Bo; Wang, Youwei

    2011-02-28

    The essential oil extracted from the fruits of Cicuta virosa L. var. latisecta Celak was tested in vitro and in vivo against four foodborne fungi, Aspergillus flavus, Aspergillus oryzae, Aspergillus niger, and Alternaria alternata. Forty-five different components accounting for 98.4% of the total oil composition were identified by gas chromatography-mass spectrometry. The major components were γ-terpinene (40.92%), p-cymene (27.93%), and cumin aldehyde (21.20%). Antifungal activity was tested by the poisoned food technique against the four fungi. Minimum inhibitory concentration against the fungi was 5 μL/mL and percentage inhibition of mycelial growth was determined at day 9. The essential oil had a strong inhibitory effect on spore production and germination in all tested fungi proportional to concentration. The oil exhibited noticeable inhibition on dry mycelium weight and synthesis of aflatoxin B₁ (AFB₁) by A. flavus, completely inhibiting AFB(1) production at 4 μL/mL. The effect of the essential oil on inhibition of decay development in cherry tomatoes was tested in vivo by exposing inoculated and control fruit to essential oil vapor at a concentration of 200 μL/mL. Results indicated that the essential oil from C. virosa var. latisecta (CVEO) has potential as a preservative to control food spoilage.

  19. Design, synthesis and antifungal activity of novel triazole derivatives%新型三唑类化合物的设计、合成和抗真菌活性研究

    Institute of Scientific and Technical Information of China (English)

    李洋洋; 刘华; 刘宏; 张永强; 张万年; 盛春泉

    2013-01-01

    目的 基于唑类药物合理优化的分子设计模型,设计新型三唑类化合物,并测试其对常见致病真菌的抑制活性.方法 采用环氧化物开环法合成目标化合物,通过1H NMR和MS确证其化学结构,经微量液基豨释法测试体外抗真菌活性.结果 合成了2个含三唑酮侧链的新型唑类化合物,它们均显示了优秀的广谱抗真菌活性.结论 目标化合物对白色念珠菌的活性优于对照药氟康唑和酮康唑,值得进一步深入构效关系研究.%Objective To design the novel triazole derivatives and test their in vitro antifungal activities on the basis of the molecular design model for rational optimization of azole drugs. Methods Ring-open reaction of the oxiranes was used to synthesize the target compounds, whose chemical structures were confirmed by 'H NMR and MS. Serial dilution method was used to determine the in vitro antifungal activities. Results Two novel azole compounds containing trizaolone side chains were synthesized which showed excellent and broad-spectrum antifungal activity. Conclusion The targeted compounds showed better antifungal activity against Candida al-bicans than the positive drugs fluconazole and ketoconazole, which was worth to further investigate the structure-activity relationship.

  20. Hydrophobic Effect of Amphiphilic Derivatives of Chitosan on the Antifungal Activity against Aspergillus flavus and Aspergillus parasiticus

    Directory of Open Access Journals (Sweden)

    Vera Ap. de Oliveira Tiera

    2013-04-01

    Full Text Available Low molecular weight amphiphilic derivatives of chitosan were synthesized, characterized and their antifungal activities against Aspergillus flavus and Aspergillus parasiticus were tested. The derivatives were synthesized using as starting material a deacetylated chitosan sample in a two step process: the reaction with propyltrimethyl-ammonium bromide (Pr, followed by reductive amination with dodecyl aldehyde. Aiming to evaluate the effect of the hydrophobic modification of the derivatives on the antifungal activity against the pathogens, the degree of substitution (DS1 by Pr groups was kept constant and the proportion of dodecyl (Dod groups was varied from 7 to 29% (DS2. The derivatives were characterized by 1H-NMR and FTIR and their antifungal activities against the pathogens were tested by the radial growth of the colony and minimum inhibitory concentration (MIC methods. The derivatives substituted with only Pr groups exhibited modest inhibition against A. flavus and A. parasiticus, like that obtained with deacetylated chitosan. Results revealed that the amphiphilic derivatives grafted with Dod groups exhibited increasing inhibition indexes, depending on polymer concentration and hydrophobic content. At 0.6 g/L, all amphiphilic derivatives having from 7.0 to 29% of Dod groups completely inhibited fungal growth and the MIC values were found to decrease from 4.0 g/L for deacetylated chitosan to 0.25–0.50 g/L for the derivatives. These new derivatives open up the possibility of new applications and avenues to develop effective biofungicides based on chitosan.

  1. 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.

  2. Purification and characterization of a CkTLP protein from Cynanchum komarovii seeds that confers antifungal activity.

    Directory of Open Access Journals (Sweden)

    Qinghua Wang

    Full Text Available BACKGROUND: Cynanchum komarovii Al Iljinski is a desert plant that has been used as analgesic, anthelminthic and antidiarrheal, but also as a herbal medicine to treat cholecystitis in people. We have found that the protein extractions from C. komarovii seeds have strong antifungal activity. There is strong interest to develop protein medication and antifungal pesticides from C. komarovii for pharmacological or other uses. METHODOLOGY/PRINCIPAL FINDINGS: An antifungal protein with sequence homology to thaumatin-like proteins (TLPs was isolated from C. komarovii seeds and named CkTLP. The three-dimensional structure prediction of CkTLP indicated the protein has an acid cleft and a hydrophobic patch. The protein showed antifungal activity against fungal growth of Verticillium dahliae, Fusarium oxysporum, Rhizoctonia solani, Botrytis cinerea and Valsa mali. The full-length cDNA was cloned by RT-PCR and RACE-PCR according to the partial protein sequences obtained by nanoESI-MS/MS. The real-time PCR showed the transcription level of CkTLP had a significant increase under the stress of abscisic acid (ABA, salicylic acid (SA, methyl jasmonate (MeJA, NaCl and drought, which indicates that CkTLP may play an important role in response to abiotic stresses. Histochemical staining showed GUS activity in almost the whole plant, especially in cotyledons, trichomes and vascular tissues of primary root and inflorescences. The CkTLP protein was located in the extracellular space/cell wall by CkTLP::GFP fusion protein in transgenic Arabidopsis. Furthermore, over-expression of CkTLP significantly enhanced the resistance of Arabidopsis against V. dahliae. CONCLUSIONS/SIGNIFICANCE: The results suggest that the CkTLP is a good candidate protein or gene for contributing to the development of disease-resistant crops.

  3. Tin(IV) complexes of pyrrolidinedithiocarbamate: synthesis, characterisation and antifungal activity.

    Science.gov (United States)

    Menezes, D C; Vieira, F T; de Lima, G M; Porto, A O; Cortés, M E; Ardisson, J D; Albrecht-Schmitt, T E

    2005-12-01

    The reaction of ammonium pyrrolidinedithiocarbamate, [NH4{S2CN(CH2)4}], with SnCl2, [Sn(C6H5)2Cl2], [Sn(C6H5)3Cl], [Sn(C4H9)2Cl2] and [Sn(C6H11)3Cl] produced in good yield the compounds [Sn{S2CN(CH2)4}2Cl2] (1), [Sn{S2CN(CH2)4}2Ph2] (2), [Sn{S2CN(CH2)4}Ph3] (3), [Sn{S2CN(CH2)4}2 n-Bu2] (4) and [Sn{S2CN(CH2)4}Cy3] (5). The complexes were characterised by infrared, multinuclear NMR (1H, 13C{1H} and 119Sn{1H}) and 119Sn Mössbauer spectroscopies. In addition, the crystal structure of 4 was determined by X-ray crystallography. The in vitro antifungal activity of the tin(IV) complexes as well of the ligand was performed on human pathogenic fungi, Candida albicans, in concentrations of 0.025; 0.050; 0.100; 0.200; 0.400; 0.800; 1.600 and 3.200 mM. The microorganism presented resistance to the dithiocarbamate ligand and all tin(IV) complexes tested were actives. The highest activity was found for compounds 1 and 4.

  4. 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.

  5. Synthesis, characterization, thermal behavior, and antifungal activity of La(III) complexes with cinnamates and 4-methoxyphenylacetate

    Institute of Scientific and Technical Information of China (English)

    Alberto Aragón-Muriel; Dorian Polo-Cerón

    2013-01-01

    In this study a series of trivalent lanthanum complexes with 4-(R)-cinnamate (4-Rcinn, R=H(1), MeO(2), Cl(3)) and 4-methoxyphenylacetate ligands (4) were prepared and their antifungal activity against Candida albicans, Aspergillus niger and Trichophyton mentagrophytes were examined. Compounds 1-4 were synthesized by a metathesis reaction and fully characterized by elemental analysis, IR, 1H and 13C NMR spectroscopy, fluorescence spectra, thermogravimetry (TG), derivative thermogravimetry (DTG), differential scanning calorimetry (DSC) and X-ray diffraction powder patterns. In emission studies, it was observed that lu-minescence intensity was enhanced in the presence of lanthanide ion. The results of X-ray diffraction patterns indicated that all com-plexes studied exhibited crystalline structure. Thermal behavior by TG, DTG, and DSC studies permitted to estimating the hydration degree of the compounds and showed the formation of decomposition products like lanthanum oxide. Determined by antifungal stud-ies, lanthanum complexes 1-4 demonstrated antifungal activity toward all pathogenic fungal strains tested. Compounds 2 and 4 showed significant growth inhibition for A. niger and C. albicans, respectively.

  6. Microwave-Assisted Synthesis of Novel Pyrazolo[3,4-g][1,8]naphthyridin-5-amine with Potential Antifungal and Antitumor Activity

    Directory of Open Access Journals (Sweden)

    Paola Acosta

    2015-05-01

    Full Text Available The microwave assisted reaction between heterocyclic o-aminonitriles 1 and cyclic ketones 2 catalyzed by zinc chloride led to new series of pyrazolo[3,4-b] [1,8]naphthyridin-5-amines 3 in good yields. This procedure provides several advantages such as being environmentally friendly, high yields, simple work-up procedure, broad scope of applicability and the protocol provides an alternative for the synthesis of pyrazolonaphthyridines. The whole series showed antifungal activities against Candida albicans and Cryptococcus neoformans standardized strains, being compounds with a 4-p-tolyl substituent of the naphthyridin scheleton (3a, 3d and 3g, the most active ones mainly against C. albicans, which appear to be related to their comparative hydrophobicity. Among them, 3d, containing a cyclohexyl fused ring, showed the best activity. The anti-Candida activity was corroborated by testing the three most active compounds against clinical isolates of albicans and non-albicans Candida strains. These compounds were also screened by the US National Cancer Institute (NCI for their ability to inhibit 60 different human tumor cell lines. Compounds 3a and 3e showed remarkable antitumor activity against cancer cell lines, with the most important GI50 values ranging from 0.62 to 2.18 μM

  7. 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

  8. A peptide with potent antifungal and antiproliferative activities from Nepalese large red beans.

    Science.gov (United States)

    Ma, D Z; Wang, H X; Ng, T B

    2009-12-01

    An antifungal defensin-like peptide with a molecular mass of 7.1kDa was isolated from dried Nepalese large red beans (Phaseolus angularis). The purification protocol employed included ion exchange chromatography on DEAE-cellulose, affinity chromatography on Affi-gel blue gel, ion exchange chromatography on SP-Sepharose, and gel filtration by fast protein liquid chromatography on Superdex 75. The antifungal peptide was unadsorbed on DEAE-cellulose, and adsorbed on Affi-gel blue gel and SP-Sepharose. The antifungal peptide inhibited mycelial growth in Fusarium oxysporum and Mycosphaerella arachidicola with an IC(50) value of 1.4 and 1.8 microM, respectively. It did not inhibit HIV-1 reverse transcriptase when tested up to 200 microM. It exerted an antiproliferative action on L1210 leukemia cells and MBL2 lymphoma cells with an IC(50) of 15 and 60 microM, respectively.

  9. Chemical composition, toxicity and larvicidal and antifungal activities of Persea americana (avocado) seed extracts.

    Science.gov (United States)

    Leite, João Jaime Giffoni; Brito, Erika Helena Salles; Cordeiro, Rossana Aguiar; Brilhante, Raimunda Sâmia Nogueira; Sidrim, José Júlio Costa; Bertini, Luciana Medeiros; Morais, Selene Maia de; Rocha, Marcos Fábio Gadelha

    2009-01-01

    The present study had the aim of testing the hexane and methanol extracts of avocado seeds, in order to determine their toxicity towards Artemia salina, evaluate their larvicidal activity towards Aedes aegypti and investigate their in vitro antifungal potential against strains of Candida spp, Cryptococcus neoformans and Malassezia pachydermatis through the microdilution technique. In toxicity tests on Artemia salina, the hexane and methanol extracts from avocado seeds showed LC50 values of 2.37 and 24.13 mg mL-1 respectively. Against Aedes aegypti larvae, the LC50 results obtained were 16.7 mg mL-1 for hexane extract and 8.87 mg mL-1 for methanol extract from avocado seeds. The extracts tested were also active against all the yeast strains tested in vitro, with differing results such that the minimum inhibitory concentration of the hexane extract ranged from 0.625 to 1.25mg L-(1), from 0.312 to 0.625 mg mL-1 and from 0.031 to 0.625 mg mL-1, for the strains of Candida spp, Cryptococcus neoformans and Malassezia pachydermatis, respectively. The minimal inhibitory concentration for the methanol extract ranged from 0.125 to 0.625 mg mL-1, from 0.08 to 0.156 mg mL-1 and from 0.312 to 0.625 mg mL-1, for the strains of Candida spp., Cryptococcus neoformans and Malassezia pachydermatis, respectively.

  10. Antifungal activity of saponins originated from Medicago hybrida against some ornamental plant pathogens

    Directory of Open Access Journals (Sweden)

    Alicja Saniewska

    2012-12-01

    Full Text Available Antifungal activity of total saponins originated from roots of Medicago hybrida (Pourret Trautv. were evaluated in vitro against six pathogenic fungi and eight individual major saponin glycosides were tested against one of the most susceptible fungi. The total saponins showed fungitoxic effect at all investigated concentrations (0.01%, 0.05% and 0.1% but their potency was different for individual fungi. The highest saponin concentration (0.1% was the most effective and the inhibition of Fusarium oxysporum f. sp. callistephi, Botrytis cinerea, Botrytis tulipae, Phoma narcissi, Fusarium oxysporum f. sp. narcissi was 84.4%, 69.9%, 68.6%, 57.2%, 55.0%, respectively. While Fusarium oxysporum Schlecht., a pathogen of Muscari armeniacum, was inhibited by 9.5% only. Eight major saponin glycosides isolated from the total saponins of M. hybrida roots were tested against the mycelium growth of Botrytis tulipae. The mycelium growth of the pathogen was greatly inhibited by hederagenin 3-O-β-D-glucopyranoside and medicagenic acid 3-O-β-D-glucopyranoside. Medicagenic acid 3-O-β-D-glucuronopyranosyl-28-O-β-D-glucopyranoside and oleanolic acid 3-O-[β-D-glucuronopyranosyl(1→2-α-L-galactopyranosyl]-28-O-β-D-glucopyranoside showed low fungitoxic activity. Medicagenic acid 3-O-a-D-glucopyranosyl- 28-O-β-D-glucopyranoside, hederagenin 3-O-[α-L- hamnopyranosyl(1→2-β-D-glucopyranosyl(1→2-β-D-glucopyranosyl]- 28-O-α-D-glucopyranoside and hederagenin 3-O-β-D-glucuronopyranosyl-28-O-β-D- lucopyranoside did not limit or only slightly inhibited growth of the tested pathogen. While 2β, 3β-dihydroxyolean-12 ene-23-al-28-oic acid 3-O-β-D-glucuronopyranosyl-28-O-β-D-glucopyranoside slightly stimulated mycelium growth of B. tulipae.

  11. A novel antifungal is active against Candida albicans biofilms and inhibits mutagenic acetaldehyde production in vitro.

    Directory of Open Access Journals (Sweden)

    Mikko T Nieminen

    Full Text Available The ability of C. albicans to form biofilms is a major virulence factor and a challenge for management. This is evident in biofilm-associated chronic oral-oesophageal candidosis, which has been shown to be potentially carcinogenic in vivo. We have previously shown that most Candida spp. can produce significant levels of mutagenic acetaldehyde (ACH. ACH is also an important mediator of candidal biofilm formation. We have also reported that D,L-2-hydroxyisocaproic acid (HICA significantly inhibits planktonic growth of C. albicans. The aim of the present study was to investigate the effect of HICA on C. albicans biofilm formation and ACH production in vitro. Inhibition of biofilm formation by HICA, analogous control compounds or caspofungin was measured using XTT to measure biofilm metabolic activity and PicoGreen as a marker of biomass. Biofilms were visualised by scanning electron microscopy (SEM. ACH levels were measured by gas chromatography. Transcriptional changes in the genes involved in ACH metabolism were measured using RT-qPCR. The mean metabolic activity and biomass of all pre-grown (4, 24, 48 h biofilms were significantly reduced after exposure to HICA (p40 µM of ACH were detected in 24 and 48 h biofilms at both pHs. Interestingly, no ACH production was detected from D-glucose in the presence of HICA at acidic pH (p<0.05. Expression of genes responsible for ACH catabolism was up-regulated by HICA but down-regulated by caspofungin. SEM showed aberrant hyphae and collapsed hyphal structures during incubation with HICA at acidic pH. We conclude that HICA has potential as an antifungal agent with ability to inhibit C. albicans cell growth and biofilm formation. HICA also significantly reduces the mutagenic potential of C. albicans biofilms, which may be important when treating bacterial-fungal biofilm infections.

  12. 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.

  13. Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity

    Directory of Open Access Journals (Sweden)

    Alba Montoya

    2016-07-01

    Full Text Available Twenty-four new hybrid analogues (15–38 containing 7-chloro-4-aminoquinoline and 2-pyrazoline N-heterocyclic fragments were synthesized. Twelve of the new compounds were evaluated against 58 human cancer cell lines by the U.S. National Cancer Institute (NCI. Compounds 25, 30, 31, 36, and 37 showed significant cytostatic activity, with the most outstanding GI50 values ranging from 0.05 to 0.95 µM. The hybrid compounds (15–38 were also evaluated for antifungal activity against Candida albicans and Cryptococcus neoformans. From the obtained results some structure–activity relationships were outlined.

  14. Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity.

    Science.gov (United States)

    Montoya, Alba; Quiroga, Jairo; Abonia, Rodrigo; Derita, Marcos; Sortino, Maximiliano; Ornelas, Alfredo; Zacchino, Susana; Insuasty, Braulio

    2016-07-27

    Twenty-four new hybrid analogues (15-38) containing 7-chloro-4-aminoquinoline and 2-pyrazoline N-heterocyclic fragments were synthesized. Twelve of the new compounds were evaluated against 58 human cancer cell lines by the U.S. National Cancer Institute (NCI). Compounds 25, 30, 31, 36, and 37 showed significant cytostatic activity, with the most outstanding GI50 values ranging from 0.05 to 0.95 µM. The hybrid compounds (15-38) were also evaluated for antifungal activity against Candida albicans and Cryptococcus neoformans. From the obtained results some structure-activity relationships were outlined.

  15. 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.

  16. In vitro antifungal activity against Candida species of Sri Lankan orthodox black tea (Camellia sinensis L. belonging to different agro-climatic elevations

    Directory of Open Access Journals (Sweden)

    Wanigasekara Daya Ratnasooriya

    2017-02-01

    Full Text Available Objective: To investigate the antifungal potential of different grades of Sri Lankan orthodox black tea [orange pekoe, broken orange pekoe fannings (BOPF and Dust No. 1] belonging to the three agro-climatic elevations (low, mid and high. Methods: Antifungal activity was assessed in vitro using methanolic extracts (300 µg/disc and agar disc diffusion bioassay technique against three Candida species, Candida albicans (C. albicans, Candida glabrata (C. glabrata, and Candida tropicalis. ketoconazole and itraconazole mixture was used as positive control (10 µg/disc and methanol was used as the negative control. The minimum inhibitory concentrations were also determined using standard protocols. Results: None of the extracts were effective against Candida tropicalis. Furthermore, orange pekoe grade tea belonging to all agro-climatic elevations did not induce any antifungal activity against C. albicans and C. glabrata as well. Conversely, Dust No. 1 belonging to all three agro-climatic elevations and low-grown BOPF showed moderate antifungal activity against C. albicans and C. glabrata. Interestingly, the severity of the antifungal effect varied with agroclimatic elevations. The minimum inhibitory concentrations ranged from 64.00–128.00 µg/mL against C. glabrata and 128.00-256.00 µg/mL against C. albicans. Conclusions: Sri Lankan Dust No. 1 and BOPF have marked antifungal activity in vitro and offer promise to be used as a supplementary beverage in prophylaxis and during drug treatment in candidiasis.

  17. Agp2p, the Plasma Membrane Transregulator of Polyamine Uptake, Regulates the Antifungal Activities of the Plant Defensin NaD1 and Other Cationic Peptides

    OpenAIRE

    Bleackley, Mark R.; Wiltshire, Jennifer L.; Perrine-Walker, Francine; Vasa, Shaily; Burns, Rhiannon L.; van der Weerden, Nicole L.; Anderson, Marilyn A.

    2014-01-01

    Cationic antifungal peptides (AFPs) act through a variety of mechanisms but share the common feature of interacting with the fungal cell surface. NaD1, a defensin from Nicotiana alata, has potent antifungal activity against a variety of fungi of both hyphal and yeast morphologies. The mechanism of action of NaD1 occurs via three steps: binding to the fungal cell surface, permeabilization of the plasma membrane, and internalization and interaction with intracellular targets to induce fungal ce...

  18. 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.

  19. 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.

  20. Bacillus isolates from the spermosphere of peas and dwarf French beans with antifungal activity against Botrytis cinerea and Pythium species.

    Science.gov (United States)

    Walker, R; Powell, A A; Seddon, B

    1998-05-01

    A range of isolation procedures including washing, sonication and incubation in nutrient broth were used separately and in combination to obtain potential bacterial antagonists to Botrytis cinerea and Pythium mamillatum from the testae and cotyledons of peas and dwarf French beans. Heat treatment was also used to bias this selection towards spore-forming bacteria. Ninety-two bacterial isolates were obtained, 72 of which were provisionally characterized as species of Bacillus. Four of these Bacillus isolates (B3, C1, D4 and J7) displayed distinct antagonism in vitro against Botrytis cinerea and P. mamillatum when screened using dual culture analysis. Further characterization of these antagonists using API 50CHB biochemical profiling identified isolate D4 as Bacillus polymyxa and isolates B3, C1 and J7 as strains of B. subtilis. In vitro screening techniques, using cell-free and heat-killed extracts of liquid cultures against Botrytis cinerea, demonstrated the production of antifungal compounds by these four Bacillus antagonists. With each isolate the antifungal activity was found not to be either exclusively spore-bound nor released entirely into the medium but present in both fractions. The antifungal compounds produced by these isolates were shown to be heat-stable. Their identification, production and release require further study for exploitation as biocontrol systems.

  1. 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

  2. Activation of toll-like receptors and dendritic cells by a broad range of bacterial molecules

    NARCIS (Netherlands)

    Boele, L.C.L.; Bajramovic, J.J.; Vries, A.M.M.B.C. de; Voskamp-Visser, I.A.I.; Kaman, W.E.; Kleij, D. van der

    2009-01-01

    Activation of pattern recognition receptors such as Toll-like receptors (TLRs) by pathogens leads to activation and maturation of dendritic cells (DC), which orchestrate the development of the adaptive immune response. To create an overview of the effects of a broad range of pathogenic bacteria, the

  3. In vitro activity of the antifungal azoles itraconazole and posaconazole against Leishmania amazonensis.

    Science.gov (United States)

    de Macedo-Silva, Sara Teixeira; Urbina, Julio A; de Souza, Wanderley; Rodrigues, Juliany Cola Fernandes

    2013-01-01

    Leishmaniasis, caused by protozoan parasites of the Leishmania genus, is one of the most prevalent neglected tropical diseases. It is endemic in 98 countries, causing considerable morbidity and mortality. Pentavalent antimonials are the first line of treatment for leishmaniasis except in India. In resistant cases, miltefosine, amphotericin B and pentamidine are used. These treatments are unsatisfactory due to toxicity, limited efficacy, high cost and difficult administration. Thus, there is an urgent need to develop drugs that are efficacious, safe, and more accessible to patients. Trypanosomatids, including Leishmania spp. and Trypanosoma cruzi, have an essential requirement for ergosterol and other 24-alkyl sterols, which are absent in mammalian cells. Inhibition of ergosterol biosynthesis is increasingly recognized as a promising target for the development of new chemotherapeutic agents. The aim of this work was to investigate the antiproliferative, physiological and ultrastructural effects against Leishmania amazonensis of itraconazole (ITZ) and posaconazole (POSA), two azole antifungal agents that inhibit sterol C14α-demethylase (CYP51). Antiproliferative studies demonstrated potent activity of POSA and ITZ: for promastigotes, the IC50 values were 2.74 µM and 0.44 µM for POSA and ITZ, respectively, and for intracellular amastigotes, the corresponding values were 1.63 µM and 0.08 µM, for both stages after 72 h of treatment. Physiological studies revealed that both inhibitors induced a collapse of the mitochondrial membrane potential (ΔΨm), which was consistent with ultrastructural alterations in the mitochondrion. Intense mitochondrial swelling, disorganization and rupture of mitochondrial membranes were observed by transmission electron microscopy. In addition, accumulation of lipid bodies, appearance of autophagosome-like structures and alterations in the kinetoplast were also observed. In conclusion, our results indicate that ITZ and POSA are potent

  4. In vitro activity of the antifungal azoles itraconazole and posaconazole against Leishmania amazonensis.

    Directory of Open Access Journals (Sweden)

    Sara Teixeira de Macedo-Silva

    Full Text Available Leishmaniasis, caused by protozoan parasites of the Leishmania genus, is one of the most prevalent neglected tropical diseases. It is endemic in 98 countries, causing considerable morbidity and mortality. Pentavalent antimonials are the first line of treatment for leishmaniasis except in India. In resistant cases, miltefosine, amphotericin B and pentamidine are used. These treatments are unsatisfactory due to toxicity, limited efficacy, high cost and difficult administration. Thus, there is an urgent need to develop drugs that are efficacious, safe, and more accessible to patients. Trypanosomatids, including Leishmania spp. and Trypanosoma cruzi, have an essential requirement for ergosterol and other 24-alkyl sterols, which are absent in mammalian cells. Inhibition of ergosterol biosynthesis is increasingly recognized as a promising target for the development of new chemotherapeutic agents. The aim of this work was to investigate the antiproliferative, physiological and ultrastructural effects against Leishmania amazonensis of itraconazole (ITZ and posaconazole (POSA, two azole antifungal agents that inhibit sterol C14α-demethylase (CYP51. Antiproliferative studies demonstrated potent activity of POSA and ITZ: for promastigotes, the IC50 values were 2.74 µM and 0.44 µM for POSA and ITZ, respectively, and for intracellular amastigotes, the corresponding values were 1.63 µM and 0.08 µM, for both stages after 72 h of treatment. Physiological studies revealed that both inhibitors induced a collapse of the mitochondrial membrane potential (ΔΨm, which was consistent with ultrastructural alterations in the mitochondrion. Intense mitochondrial swelling, disorganization and rupture of mitochondrial membranes were observed by transmission electron microscopy. In addition, accumulation of lipid bodies, appearance of autophagosome-like structures and alterations in the kinetoplast were also observed. In conclusion, our results indicate that ITZ and

  5. In Vitro Activity of the Antifungal Azoles Itraconazole and Posaconazole against Leishmania amazonensis

    Science.gov (United States)

    de Macedo-Silva, Sara Teixeira; Urbina, Julio A.; de Souza, Wanderley; Rodrigues, Juliany Cola Fernandes

    2013-01-01

    Leishmaniasis, caused by protozoan parasites of the Leishmania genus, is one of the most prevalent neglected tropical diseases. It is endemic in 98 countries, causing considerable morbidity and mortality. Pentavalent antimonials are the first line of treatment for leishmaniasis except in India. In resistant cases, miltefosine, amphotericin B and pentamidine are used. These treatments are unsatisfactory due to toxicity, limited efficacy, high cost and difficult administration. Thus, there is an urgent need to develop drugs that are efficacious, safe, and more accessible to patients. Trypanosomatids, including Leishmania spp. and Trypanosoma cruzi, have an essential requirement for ergosterol and other 24-alkyl sterols, which are absent in mammalian cells. Inhibition of ergosterol biosynthesis is increasingly recognized as a promising target for the development of new chemotherapeutic agents. The aim of this work was to investigate the antiproliferative, physiological and ultrastructural effects against Leishmania amazonensis of itraconazole (ITZ) and posaconazole (POSA), two azole antifungal agents that inhibit sterol C14α-demethylase (CYP51). Antiproliferative studies demonstrated potent activity of POSA and ITZ: for promastigotes, the IC50 values were 2.74 µM and 0.44 µM for POSA and ITZ, respectively, and for intracellular amastigotes, the corresponding values were 1.63 µM and 0.08 µM, for both stages after 72 h of treatment. Physiological studies revealed that both inhibitors induced a collapse of the mitochondrial membrane potential (ΔΨm), which was consistent with ultrastructural alterations in the mitochondrion. Intense mitochondrial swelling, disorganization and rupture of mitochondrial membranes were observed by transmission electron microscopy. In addition, accumulation of lipid bodies, appearance of autophagosome-like structures and alterations in the kinetoplast were also observed. In conclusion, our results indicate that ITZ and POSA are potent

  6. Composition and antifungal activity of the essential oil of the Brazilian Chenopodium ambrosioides L.

    Science.gov (United States)

    Jardim, Carolina Marangon; Jham, Gulab Newandram; Dhingra, Onkar Dev; Freire, Marcelo Moreira

    2008-09-01

    The antifungal activity of essential oil (EO) from the Brazilian epazote (Chenopodium ambrosioides L.) was evaluated by the poison food assay at concentrations of 0.3%, 0.1%, and 0.05% with eight postharvest deteriorating fungi (Aspergillus flavus, Aspergillus glaucus, Aspergillus niger, Aspergillus ochraceous, Colletotrichum gloesporioides, Colletotrichum musae, Fusarium oxysporum, and Fusarium semitectum). EO components were tentatively identified by Kováts retention indices (RIs) using gas chromatography and gas chromatography combined with mass spectrometry (GC-MS). Growth of all fungi was completely inhibited at 0.3% concentration, and by 90% to 100% at 0.1% concentration. The following 13 tentatively identified compounds (relative percent) accounted for 90.4% of the total volatile oil: alpha-terpinene (0.9), p-cymene (2.0), benzyl alcohol (0.3), p-cresol (0.3), p-mentha-1,3,8-triene (0.2), p-cimen-8-ol (0.6), alpha-terpineol (0.5), (Z)-ascaridole (61.4), piperitone (0.9), carvacrol (3.9), (E)-ascaridole (18.6), (E)-piperitol acetate (0.5), and (Z)-carvyl acetate (0.3). Autobiographic thin layer chromatography of the EO to separate the principal fungitoxic fraction yielded only one fraction that completely inhibited the growth of all test fungi at a concentration of 0.1%. This fraction was characterized by RIs and GC-MS presenting a composition (%) of p-cymene (25.4), (Z)-ascaridole (44.4), and (E)-ascaridole (30.2). The results suggest ascaridoles were the principal fungitoxic components of the EO.

  7. [Derivatization of berberine based on its synergistic antifungal activity with fluconazole against fluconazole-resistant Candida albicans].

    Science.gov (United States)

    Tian, Shu-Juan; Gao, Yue; Zang, Cheng-Xu; Cai, Zhan; Ni, Ting-jun-hong; Tan, Shan-Lun; Cao, Yong-Bing; Jiang, Yuan-Ying; Zhang, Da-Zhi

    2014-11-01

    Abstract: Our previous work revealed berberine can significantly enhance the susceptibility of fluconazole against fluconazole-resistant Candida albicans, which suggested that berberine has synergistic antifungal activity with fluconazole. Preliminary SAR of berberine needs to be studied for the possibility of investigating its target and SAR, improving its drug-likeness, and exploring new scaffold. In this work, 13-substitutited benzyl berberine derivatives and N-benzyl isoquinoline analogues were synthesized and characterized by 1H NMR and MS. Their synergetic activity with fluconazole against fluconazole-resistant Candida albicans was evaluated in vitro. The 13-substitutited benzyl berberine derivatives 1a-1e exhibited comparable activity to berberine, which suggested that the introduction of functional groups to C-13 can maintain its activity. The N-benzyl isoquinolines, which were designed as analogues of berberine with its D ring opened, exhibited lower activity than berberine. However, compound 2b, 2c, and 4b showed moderate activity, which indicated that berberine may be deconstructed to new scaffold with synergistic antifungal activity with fluconazole. The results of our research may be helpful to the SAR studies on its other biological activities.

  8. Chemical composition of essential oils of Thymus and Mentha species and their antifungal activities.

    NARCIS (Netherlands)

    Sokovic, M.D.; Vukojevic, J.; Marin, P.D.; Brkic, D.D.; Vajs, V.; Griensven, van L.J.L.D.

    2009-01-01

    The potential antifungal effects of Thymus vulgaris L., Thymus tosevii L., Mentha spicata L., and Mentha piperita L. (Labiatae) essential oils and their components against 17 micromycetal food poisoning, plant, animal and human pathogens are presented. The essential oils were obtained by hydrodestil

  9. 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

  10. Enhanced activity of antifungal drugs using natural phenolics against yeast strains of Candida and Cryptococcus

    Science.gov (United States)

    Candidiasis and cryptococcosis are diseases of widening global incidence as a result of increasing immunosuppressive disorders, such as AIDS. An enduring problem for treatment of these mycoses is recurrent development of resistance to introduced antifungal drugs. We examined the potential for enhan...

  11. 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

  12. 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.

  13. 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.

  14. Radiation application for upgrading of bioresources - Development of antifungal and/or nitrogen fixative microbes

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Ki Sung; Ko, Dong Kyu; Han, Gab Jin [Paichai University, Taejon (Korea)

    2000-04-01

    (1) In this study, the antifungal bacteria six strains were isolated from various environment located in Chung-cheong area, Korea. These isolates were identified the genera Bacillus sp, Pseudomonas sp. through morphological, physiological and biochemical analysis. Strains KL3362 and KL3397 were identified as Pseudomonas aurantiaca and Alcaligenes faecalis, respectively. Considering antifungal(AF) spectrum, strain KL3303, 3334, and 3341 show the broad range, KL3362 and KL3397 the narrow range of AF activity on a number of pathogenic fungi. Therefore, strains KL3341 and KL3362 were selected as the strong candidate of antifungal bacteria on every purpose and usage related with our research goal. (2) KL3341 producing-antifungal substances were consisted of five different kinds of low molecular weight polypeptides (3) Optimal conditions for the production of antifungal substances were analyzed under various environmental conditions. Growth rates were different according to carbon and nitrogen source, antifungal substance production yields were not different, however. Product of antifungal substances according t phosphate is proportional to the concentration. And productivity of antifungal substances was generally high in the range 30 {approx} 37 deg. C at pH 7. In case of adding vitamin B1 or lysine to medium, the antifungal activity was enhanced. (4) Mutants with enhanced antifungal activities were constructed by radiation of {gamma}-ray. (5) AF strains were screened and selected from this research can be used in the microbial biocides as well as multifunctional bio-controllers in order to remove plant pathogenic fungi and to clarify the polluted environment. Due to their excellent degradation capability for agricultural and/or organic substances, they also can be used to improve soil quality, to ferment compost and to clean up the environment. 35 refs., 17 figs., 15 tabs. (Author)

  15. The Drosophila PRR GNBP3 assembles effector complexes involved in antifungal defenses independently of its Toll-pathway activation function.

    Science.gov (United States)

    Matskevich, Alexey A; Quintin, Jessica; Ferrandon, Dominique

    2010-05-01

    The Drosophila Toll-signaling pathway controls the systemic antifungal host response. Gram-negative binding protein 3 (GNBP3), a member of the beta-glucan recognition protein family senses fungal infections and activates this pathway. A second detection system perceives the activity of proteolytic fungal virulence factors and redundantly activates Toll. GNBP3(hades) mutant flies succumb more rapidly to Candida albicans and to entomopathogenic fungal infections than WT flies, despite normal triggering of the Toll pathway via the virulence detection system. These observations suggest that GNBP3 triggers antifungal defenses that are not dependent on activation of the Toll pathway. Here, we show that GNBP3 agglutinates fungal cells. Furthermore, it can activate melanization in a Toll-independent manner. Melanization is likely to be an essential defense against some fungal infections given that the entomopathogenic fungus Beauveria bassiana inhibits the activity of the main melanization enzymes, the phenol oxidases. Finally, we show that GNBP3 assembles "attack complexes", which comprise phenoloxidase and the necrotic serpin. We propose that Drosophila GNBP3 targets fungi immediately at the inception of the infection by bringing effector molecules in direct contact with the invading microorganisms.

  16. Isolation of flavonoids from Anemopaegma arvense (Vell Stellf. ex de Souza and their antifungal activity against Trichophyton rubrum

    Directory of Open Access Journals (Sweden)

    Camila Di Giovane Costanzo

    2013-09-01

    Full Text Available Anemopaegma arvense (Vell Stellf. ex de Souza belongs to the family Bignoniaceae, and is popularly known as catuaba. To evaluate the cytotoxic and antimicrobial activity of A. arvense, fraction F3 and flavonoids 1 (quercetin 3-O-α-L-rhamnopyranosyl-(1→6-β-D-glucopyranoside (rutin and flavonoid 2 (quercetin 3-O-α-L-rhamnopyranosyl-(1→6-β-D-galactopyranoside were isolated from the leaves of this plant. Fraction F3 and flavonoids 1 and 2 exhibited no antibacterial activity. Furthermore, no cytotoxic activity of fraction 3 or flavonoids 1 and 2 was observed against the tumor cells tested. However, analysis of the antifungal activity of flavonoids 1 and 2 revealed minimum inhibitory concentrations of 0.5 and 0.25 mg/mL, respectively, against the Trichophyton rubrum strains tested (wild type and mutant. This study demonstrates for the first time the antifungal activity of isolated flavonoids, validating the same activity for A. arvense.

  17. Antifungal activity of Glycyrrhiza glabra extracts and its active constituent glabridin.

    Science.gov (United States)

    Fatima, Atiya; Gupta, Vivek K; Luqman, Suaib; Negi, Arvind S; Kumar, J K; Shanker, Karuna; Saikia, Dharmendra; Srivastava, Suchita; Darokar, M P; Khanuja, Suman P S

    2009-08-01

    Glabridin, an active constituent of Glycyrrhiza glabra roots, was found to be active against both yeast and filamentous fungi. Glabridin also showed resistance modifying activity against drug resistant mutants of Candida albicans at a minimum inhibitory concentration of 31.25-250 microg/mL. Although the compound was reported earlier to be active against Candida albicans, but this is the first report of its activity against drug resistant mutants.

  18. Comparative pharmacokinetics of antifungal drugs in domestic turkeys, red-tailed hawks, broad-winged hawks, and great-horned owls.

    Science.gov (United States)

    Redig, P T; Duke, G E

    1985-01-01

    The present research was to test in vitro activity of thiabendazole, 5-fluorocytosine, and amphotericin B against 11 isolates of Aspergillus fumigatus from avian species. Additionally, the plasma concentrations of these drugs were determined in four avian species given a range of dosages by oral, intravenous, and intratracheal routes. Thiabendazole inhibited most isolates in vitro at concentrations between 25 and 50 micrograms/ml; however, there were no detectable inhibitory concentrations in the plasma of any species at any of the doses. The arithmetic mean minimum inhibitory in vitro concentration for 5-fluorocytosine against the 11 Aspergillus isolates was 2.73 micrograms/ml. Inhibitory concentrations of 5-fluorocytosine were found 2 and 6 hours post-administration in all species when given oral doses of 30 or 60 mg/kg as a single dose or when given three divided doses a day totaling 120 mg/kg. No inhibitory concentrations were found 24 hours post-administration. Inhibitory concentrations of amphotericin B were found only 2 and 6 hours post-administration in birds receiving three doses of 1.5 mg/kg at 2-hour intervals. The arithmetic mean minimum inhibitory in vitro concentration for amphotericin B against 11 isolates of A. fumigatus was 0.81 micrograms/ml.

  19. 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.

  20. In vitro antileukemia, antibacterial and antifungal activities of some 3d metal complexes: chemical synthesis and structure - activity relationships.

    Science.gov (United States)

    Gulea, Aurelian; Poirier, Donald; Roy, Jenny; Stavila, Vitalie; Bulimestru, Ion; Tapcov, Victor; Birca, Maria; Popovschi, Lilia

    2008-12-01

    The present paper describes the synthesis, characterization and in vitro biological evaluation screening of different classes (ammoniacates, dioximates, carboxylates, semi- and thiosemicarbazidates) of Co(II), Co(III), Cu(II), Ni(II), Mn(II), Zn(II) and Fe(III) complexes. Schiff bases were obtained from the reaction of some salicyl aldehydes with, respectively, furoylhydrazine, benzoylhydrazine, semicarbazide, thiosemicarbazide and S-methylthiosemicarbazide to give tridentate ligands containing ONO, ONS or ONN as donor atoms. The synthetic metal complexes are of various geometrical and electronic structures, thermodynamic and thermal stabilities, and magnetic and conductance properties. All complexes, except those of Cu, are octahedral. Some Cu, Co and Mn compounds have a dimeric or a polymeric structure. The composition and structure of complexes were analysed by elemental analysis, IR and (1)H NMR and (13)C NMR spectroscopies, and magnetochemical, thermoanalytical and molar conductance measurements. All ligands and metal complexes were tested as inhibitors of human leukemia (HL-60) cells growth, and the most potent, the Cu(II) complexes, have been also tested for their in vitro antibacterial and antifungal activities. Structure-activity relationships were carried out.

  1. Vegetable Peel Waste for the Production of ZnO Nanoparticles and its Toxicological Efficiency, Antifungal, Hemolytic, and Antibacterial Activities.

    Science.gov (United States)

    Surendra, T V; Roopan, Selvaraj Mohana; Al-Dhabi, Naif Abdullah; Arasu, Mariadhas Valan; Sarkar, Gargi; Suthindhiran, K

    2016-12-01

    Zinc oxide (ZnO) nanoparticles (NPs) are important materials when making different products like sun screens, textiles, and paints. In the current study, the photocatalytic effect of prepared ZnO NPs from Moringa oleifera (M. oleifera) was evaluated on degradation of crystal violet (CV) dye, which is largely released from textile industries and is harmful to the environment. Preliminarily, ZnO NP formation was confirmed using a double beam ultraviolet visible (UV-Vis) spectrophotometer; further, the NP size was estimated using XRD analysis and the functional group analysis was determined using Fourier transform infrared (FT-IR) spectroscopy. The morphology of the synthesized NPs was found to be a hexagonal shape using SEM and TEM analysis and elemental screening was analyzed using EDX. ZnO NPs were shown sized 40-45 nm and spherical in shape. The degradation percentage of ZnO NPs was calculated as 94% at 70 min and the rate of the reaction -k = 0.0282. The synthesized ZnO NPs were determined for effectiveness on biological activities such as antifungal, hemolytic, and antibacterial activity. ZnO NPs showed good antifungal activity against Alternaria saloni and Sclerrotium rolfii strains. Further, we have determined the hemolytic and antibacterial activity of ZnO NPs and we got successive results in antibacterial and hemolytic activities.

  2. Vegetable Peel Waste for the Production of ZnO Nanoparticles and its Toxicological Efficiency, Antifungal, Hemolytic, and Antibacterial Activities

    Science.gov (United States)

    Surendra, T. V.; Roopan, Selvaraj Mohana; Al-Dhabi, Naif Abdullah; Arasu, Mariadhas Valan; Sarkar, Gargi; Suthindhiran, K.

    2016-12-01

    Zinc oxide (ZnO) nanoparticles (NPs) are important materials when making different products like sun screens, textiles, and paints. In the current study, the photocatalytic effect of prepared ZnO NPs from Moringa oleifera ( M. oleifera) was evaluated on degradation of crystal violet (CV) dye, which is largely released from textile industries and is harmful to the environment. Preliminarily, ZnO NP formation was confirmed using a double beam ultraviolet visible (UV-Vis) spectrophotometer; further, the NP size was estimated using XRD analysis and the functional group analysis was determined using Fourier transform infrared (FT-IR) spectroscopy. The morphology of the synthesized NPs was found to be a hexagonal shape using SEM and TEM analysis and elemental screening was analyzed using EDX. ZnO NPs were shown sized 40-45 nm and spherical in shape. The degradation percentage of ZnO NPs was calculated as 94% at 70 min and the rate of the reaction -k = 0.0282. The synthesized ZnO NPs were determined for effectiveness on biological activities such as antifungal, hemolytic, and antibacterial activity. ZnO NPs showed good antifungal activity against Alternaria saloni and Sclerrotium rolfii strains. Further, we have determined the hemolytic and antibacterial activity of ZnO NPs and we got successive results in antibacterial and hemolytic activities.

  3. In vitro cytotoxic, antibacterial, antifungal and urease inhibitory activities of some N4- substituted isatin-3-thiosemicarbazones.

    Science.gov (United States)

    Pervez, Humayun; Iqbal, Mohammad S; Tahir, Muhammad Younas; Nasim, Faiz-ul-Hassan; Choudhary, Muhammad Iqbal; Khan, Khalid Mohammed

    2008-12-01

    A series of 15 previously reported N(4)-substituted isatin-3-thiosemicarbazones 3a-o has been screened for cytotoxic, antibacterial, antifungal and urease inhibitory activities. Compounds 3b, 3e and 3n proved to be active in cytotoxicity assay; 3e exhibited a high degree of cytotoxic activity (LD(50) = 1.10 x 10(-5) M). Compound 3h exhibited significant antibacterial activity against B. subtilis, whereas compounds 3a, 3k and 3l displayed significant antifungal activity against one or more fungal strains i.e. T. longifusus, A. flavus and M. canis. In human urease enzyme inhibition assay, compounds 3g, 3k and 3m proved to be the most potent inhibitors, exhibiting relatively pronounced inhibition of the enzyme. These compounds, being non-toxic, could be potential candidates for orally effective therapeutic agents to treat certain clinical conditions induced by bacterial ureases like H. pylori urease. This study presents the first example of inhibition of urease by isatin-thiosemicarbazones and as such provides a solid basis for further research on such compounds to develop more potent inhibitors.

  4. MDGC-MS analysis of essential oils from Protium heptaphyllum (Aubl. and their antifungal activity against Candida specie

    Directory of Open Access Journals (Sweden)

    M. MOBIN

    Full Text Available ABSTRACT Protium heptaphyllum is found in the Amazon region, and in various Brazilian states and South American countries. Also Known as almecega, it produces an oil resin used in traditional medicine as analgesic, anti-inflammatory, cicatrizant and expectorant, it is rich in pentacyclic triterpenes and essential oil. The main objective of this study was to analyze the chemical composition of P. heptaphyllumresin (OEPh over different extraction times and to evaluate their antifungal activity against Candida species, obtained from gardeners with onychomycosis, using the disk diffusion method. The OEPh was obtained by hydrodistillation and analyzed by Multidimensional Gas Chromatography coupled with Mass Spectrometry (MDGC / MS. Candida species were obtained from lesions on the nails of horticulturist from a community garden in the city of Teresina, Piauí, Brazil. The antifungal activity in concentrations of 1000 µg/L, 500 µg/L and 250 µg/L, PROTOCOL M44-A2 (CLSI 2009 OEPh was tested. The main constituents identified were: l-limonene, α-terpineol, p-cineol, o-cymene and α-phellandrene, however, its composition varies significantly with extraction time. All species, except C. rugosa, were inhibited with halo (≥ 14 mm at 1000 μg / L. C. krusei is naturally resistant to the drug fluconazole, but when tested with OEPh the clinical species (case 9 demonstrated sensitivity in three dilutions (halo ≤ 10 ≥ 14 and the standard strain was inhibited at concentration of 1000 μg/Lg / L (halo 14mm. A similar situation also occurred with the standard strain of C. parapsilosis (halo ≥ 11mm. OEPh has considerable antifungal activity, which merits further investigation for alternative clinical applications, since this species is widely distributed in our community, and it presents good yields, and also has important therapeutic applications.

  5. 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.

  6. Antifungal activity of TiO2 photocatalysis against Penicillium expansum in vitro and in fruit tests.

    Science.gov (United States)

    Maneerat, Chamorn; Hayata, Yasuyoshi

    2006-03-15

    The antifungal activity of TiO2 photocatalytic reaction in the form of TiO2 powder and TiO2 coated on a plastic film against Penicillium expansum was investigated in vitro and in fruit tests. The mixture of P. expansum conidial suspension and TiO2 powder was added to potato dextrose agar (PDA) plates for vitro test. The TiO2 photocatalytic reaction reduced conidial germination of the fungal pathogen. It was found that the ability of the TiO2 photocatalytic reaction to suppress P. expansum growth correlated to the amount of TiO2 added. Lower numbers of viable colonies of P. expansum were observed with increasing amount of TiO2. Regardless of the kind of selected fruit inoculated with P. expansum, both TiO2 powder and TiO2-coated film exhibited antifungal activity to control fruit rot. Development of Penicillium rot in apple was significantly (P = 0.05) retarded by the TiO2 photocatalytic reaction. Similarly the TiO2 photocatalytic reaction was the only treatment where no tomato fruit rot was noticeable after 1 week of storage. TiO2-coated film also decreased brown lesions and Penicillium rot infection in lemons. The mean severity fruit rot scores (browning and softening flesh) were 3.2 and 1.9 for uncoated and TiO2-coated film, respectively. Our findings suggest that "TiO2 photocatalytic reaction" shows antifungal activity against P. expansum which may have potential for postharvest disease control.

  7. Observation of electro-activated localized structures in broad area VCSELs

    CERN Document Server

    Parravicini, J; Columbo, L; Prati, F; Rizza, C; Tissoni, G; Agranat, A J; DelRe, E

    2014-01-01

    We demonstrate experimentally the electro-activation of a localized optical structure in a coherently driven broad-area vertical-cavity surface-emitting laser (VCSEL) operated below threshold. Control is achieved by electro-optically steering a writing beam through a pre-programmable switch based on a photorefractive funnel waveguide.

  8. Asialoerythropoietin is a nonerythropoietic cytokine with broad neuroprotective activity in vivo

    DEFF Research Database (Denmark)

    Erbayraktar, Serhat; Grasso, Giovanni; Sfacteria, Alessandra;

    2003-01-01

    importantly, asialoEPO exhibits a broad spectrum of neuroprotective activities, as demonstrated in models of cerebral ischemia, spinal cord compression, and sciatic nerve crush. These data suggest that nonerythropoietic variants of rhEPO can cross the blood-brain barrier and provide neuroprotection....

  9. Bioactive compounds and antifungal activity of three different seaweed speciesUlva lactuca,Sargassum tenerrimum andLaurencia obtusa collected from Okha coast, Western India

    Institute of Scientific and Technical Information of China (English)

    Megha Barot; Nirmal Kumar J.I.; Rita N. Kumar

    2016-01-01

    Objective:To evaluate bioactive compounds responsible for antifungal activity from seaweeds of Okha coast, Western India. Methods: Each species were extracted with different solvents with increasing polarity: hexane, ethyl acetate, chloroform and methanol using Soxhlet apparatus. The antifungal activity was determined by agar diffusion plate method by using fluconazole, ketoconazole and amphotericin B as standards. Gas chromatography-mass spectrometer analysis was done for identification of bioactive compounds present in crude extract. Results: The gas chromatography-mass spectrometer analysis of all the extracts revealed the presence of steroids, fatty acids and esters compounds. Among the three species, the maximum crude extract yield (53.46%) and the largest inhibition zone (36 mm) were recorded in methanol extract ofUlva lactuca, whereas the minimum crude extract yield and inhibition zone were recorded in chloroform extract of the same species as 0.5% and 10 mm, respectively. Methanol and ethyl acetate extract showed the maximum antifungal activity and the major important compounds like steroids, fatty acids and esters were detected with higher amount in all the extracts. Conclusions: The present study revealed that the different seaweed extracts showed moderate to significant antifungal activity against the strains tested as compared with the standard fungicides, and polar solvents methanol and ethyl acetate were comparatively efficient for extraction of different metabolites that are responsible for antifungal activity.

  10. Chemical variability, antioxidant and antifungal activities of essential oils and hydrosol extract of Calendula arvensis L. from western Algeria.

    Science.gov (United States)

    Belabbes, Rania; Dib, Mohammed El Amine; Djabou, Nassim; Ilias, Faiza; Tabti, Boufeldja; Costa, Jean; Muselli, Alain

    2017-01-21

    The chemical composition of the essential oils and hydrosol extract from aerial parts of Calendula arvensis L. was investigated using GC-FID and GC/MS. Intra-species variations of the chemical compositions of essential oils from 18 Algerian sample locations were investigated using statistical analysis. Chemical analysis allowed the identification of fifty-three compounds amounting to 92.3-98.5% with yields varied of 0.09-0.36% and the main compounds were zingiberenol 1 (8.7-29.8%), eremoligenol (4.2-12.5%), β-curcumene (2.1-12.5%), zingiberenol 2 (4.6-19.8%) and (E,Z)-farnesol (3.5-23.4%). The study of the chemical variability of essential oils allowed the discrimination of two main clusters confirming that there is a relation between the essential oil compositions and the harvest locations. Different concentrations of essential oil and hydrosol extract were prepared and their antioxidant activity were assessed using three methods (DPPH, FRAP and β-carotene). The results showed that hydrosol extract presented an interesting antioxidant activity. The in vitro antifungal activity of hydrosol extract produced the best antifungal inhibition against Penicillium expansum and Aspergillus niger, while, essential oil was inhibitory at relatively higher concentrations. Results showed that the treatments of pear fruits with essential oil and hydrosol extract presented a very interesting protective activity on disease severity of pears caused by P. expansum. This article is protected by copyright. All rights reserved.

  11. Antifungal Activity of Amphotericin B Cochleates against Candida albicans Infection in a Mouse Model

    OpenAIRE

    Zarif, Leila; Graybill, John R.; Perlin, David; Najvar, Laura; Bocanegra, Rosie; Mannino, Raphael J.

    2000-01-01

    Cochleates are lipid-based supramolecular assemblies composed of natural products, negatively charged phospholipid, and a divalent cation. Cochleates can encapsulate amphotericin B (AmB), an important antifungal drug. AmB cochleates (CAMB) have a unique shape and the ability to target AmB to fungi. The minimal inhibitory concentration and the minimum lethal concentration against Candida albicans are similar to that for desoxycholate AmB (DAMB; Fungizone). In vitro, CAMB induced no hemolysis o...

  12. Chemical Composition of Essential Oilsof Thymus and Mentha Speciesand Their Antifungal Activities

    OpenAIRE

    Leo J. L. D. van Griensven; Vlatka Vajs; Dejan D. Brkić; Marin, Petar D.; Jelena Vukojević; Marina D. Soković

    2009-01-01

    The potential antifungal effects of Thymus vulgaris L., Thymus tosevii L., Mentha spicata L., and Mentha piperita L. (Labiatae) essential oils and their components against 17 micromycetal food poisoning, plant, animal and human pathogens are presented. The essential oils were obtained by hydrodestillation of dried plant material. Their composition was determined by GC-MS. Identification of individual constituents was made by comparison with analytical standards, and by computer matching mass ...

  13. Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds

    Directory of Open Access Journals (Sweden)

    Da-Jun Zhang

    2014-01-01

    Full Text Available A series of novel unsaturated five-membered benzo-heterocyclic amine derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that most of our synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compounds 3f (IC50 = 3.21–5.06 μM and 3g (IC50 = 0.71–34.87 μM showed potent activity towards both RNA viruses (influenza A, HCV and Cox B3 virus and a DNA virus (HBV at low micromolar concentrations. An SAR study showed that electron-withdrawing substituents located on the aromatic or heteroaromatic ring favored antiviral activity towards RNA viruses.

  14. Activation of stress signalling pathways enhances tolerance of fungi to chemical fungicides and antifungal proteins.

    Science.gov (United States)

    Hayes, Brigitte M E; Anderson, Marilyn A; Traven, Ana; van der Weerden, Nicole L; Bleackley, Mark R

    2014-07-01

    Fungal disease is an increasing problem in both agriculture and human health. Treatment of human fungal disease involves the use of chemical fungicides, which generally target the integrity of the fungal plasma membrane or cell wall. Chemical fungicides used for the treatment of plant disease, have more diverse mechanisms of action including inhibition of sterol biosynthesis, microtubule assembly and the mitochondrial respiratory chain. However, these treatments have limitations, including toxicity and the emergence of resistance. This has led to increased interest in the use of antimicrobial peptides for the treatment of fungal disease in both plants and humans. Antimicrobial peptides are a diverse group of molecules with differing mechanisms of action, many of which remain poorly understood. Furthermore, it is becoming increasingly apparent that stress response pathways are involved in the tolerance of fungi to both chemical fungicides and antimicrobial peptides. These signalling pathways such as the cell wall integrity and high-osmolarity glycerol pathway are triggered by stimuli, such as cell wall instability, changes in osmolarity and production of reactive oxygen species. Here we review stress signalling induced by treatment of fungi with chemical fungicides and antifungal peptides. Study of these pathways gives insight into how these molecules exert their antifungal effect and also into the mechanisms used by fungi to tolerate sub-lethal treatment by these molecules. Inactivation of stress response pathways represents a potential method of increasing the efficacy of antifungal molecules.

  15. Antibacterial, antifungal and cytotoxic activities exhibited by endophytic fungi from the Brazilian marine red alga Bostrychia tenella (Ceramiales

    Directory of Open Access Journals (Sweden)

    Rafael de Felício

    2015-12-01

    Full Text Available Abstract Marine environment is one of the most important sources regarding natural products research. Besides, marine microorganisms have been denominated as a talented natural source for discovery of new leads. Although the association of macroalgae and fungi has been described regarding ecological issues, there is a lack of studies about marine seaweed endophytic fungi. In this context, the goal of this study was to evaluate cytotoxic, antifungal and antibacterial activities of endophytic fungi isolated from the Brazilian marine seaweed Bostrychia tenella (J.V. Lamouroux J. Agardh (Ceramiales, Rhodophyta. Forty-five endophytic microorganism strains were isolated from B. tenella. Crude extracts and organic fractions of ten selected strains were obtained after growth in rice medium. Samples were evaluated for cytotoxicity, antifungal and antibacterial assays. Penicillium strains showed positive results in a diversity of assays, and other five strains were active in at least one test. In addition, cytochalasin D was isolated from Xylaria sp. This alga is composed of a microbiological potential, since its endophytic strains exhibited remarkable biological properties. Moreover, cytochalasin D isolation has confirmed chemical potential of marine endophytic strains. This is the first study in which cultured fungi isolates from the Brazilian macroalga B. tenella were evaluated concerning biological properties. Results corroborated that this species could be a pharmaceutical source from marine environment. Furthermore, Acremonium implicatum is being firstly described as marine endophyte and Xylaria sp., Trichoderma atroviride and Nigrospora oryzae as marine seaweed endophytes. Thus, this work reports the first study relating detailed isolation, cultivation and biological evaluation (cytotoxic, antifungal and antibacterial of endophytes Penicillium decaturense and P. waksmanii from the Brazilian marine red alga B. tenella. We are also reporting the

  16. Design, Synthesis, Antifungal Activities and 3D-QSAR of New N,N'-Diacylhydrazines Containing 2,4-Dichlorophenoxy Moiety

    Directory of Open Access Journals (Sweden)

    Bao-Ju Li

    2013-11-01

    Full Text Available A series of new N,N'-diacylhydrazine derivatives were designed and synthesized. Their structures were verified by 1H-NMR, mass spectra (MS and elemental analysis. The antifungal activities of these N,N'-diacylhydrazines were evaluated. The bioassay results showed that most of these N,N'-diacylhydrazines showed excellent antifungal activities against Cladosporium cucumerinum, Corynespora cassiicola, Sclerotinia sclerotiorum, Erysiphe cichoracearum, and Colletotrichum orbiculare in vivo. The half maximal effective concentration (EC50 of one of the compounds was also determined, and found to be comparable with a commercial drug. To further investigate the structure–activity relationship, comparative molecular field analysis (CoMFA was performed on the basis of antifungal activity data. Both the steric and electronic field distributions of CoMFA are in good agreement in this study.

  17. 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.

  18. Antifungal Activity of Salvia miltiorrhiza Against Candida albicans Is Associated with the Alteration of Membrane Permeability and (1,3)-β-D-Glucan Synthase Activity.

    Science.gov (United States)

    Lee, Heung-Shick; Kim, Younhee

    2016-03-01

    Candidiasis has posed a serious health risk to immunocompromised patients owing to the increase in resistant yeasts, and Candida albicans is the prominent pathogen of fungal infections. Therefore, there is a critical need for the discovery and characterization of novel antifungals to treat infections caused by C. albicans. In the present study, we report on the antifungal activity of the ethanol extract from Salvia miltiorrhiza against C. albicans and the possible mode of action against C. albicans. The increase in the membrane permeability was evidenced by changes in diphenylhexatriene binding and release of both 260-nm-absorbing intracellular materials and protein. In addition, inhibition of cell wall synthesis was demonstrated by the enhanced minimal inhibitory concentration in the presence of sorbitol and reduced (1,3)-β-D-glucan synthase activity. The above evidence supports the notion that S. miltiorrhiza has antifungal activity against C. albicans by the synergistic activity of targeting the cell membrane and cell wall. These findings indicate that S. miltiorrhiza displays effective activity against C. albicans in vitro and merits further investigation to treat C. albicans-associated infections.

  19. Solid lipid nanoparticles containing copaiba oil and allantoin: development and role of nanoencapsulation on the antifungal activity.

    Science.gov (United States)

    Svetlichny, G; Külkamp-Guerreiro, I C; Cunha, S L; Silva, F E K; Bueno, K; Pohlmann, A R; Fuentefria, A M; Guterres, S S

    2015-03-01

    The aim of this work was to develop solid lipid nanoparticles (SLN) containing copaiba oil with and without allantoin (NCOA, NCO, respectively) and to evaluate their antifungal activity. Nanoparticle suspensions were prepared using a high homogenisation technique and characterised by dynamic light scattering, laser diffraction, nanoparticle tracking analysis, multiple light scattering analysis, high-pressure liquid chromatography, pH and rheology. The antifungal activities of the formulations were tested in vitro against the emergent yeasts Candida krusei and Candida parapsilosis, and the fungal pathogens of human skin Trichophyton rubrum and Microsporum canis. The dynamic light scattering analysis showed z-average diameters (intensity) between 118.63 ± 8.89 nm for the nanoparticles with both copaiba oil and allantoin and 126.06 ± 9.84nm for the nanoparticles with just copaiba oil. The D[4,3] determined by laser diffraction showed similar results of 123 ± 1.73 nm for the nanoparticles with copaiba oil and allantoin and 130 ± 3.6 nm for the nanoparticles with copaiba oil alone. Nanoparticle tracking analysis demonstrated that both suspensions had monomodal profiles and consequently, the nanoparticle populations were homogeneous. This analysis also corroborated the results of dynamic light scattering and laser diffraction, exhibiting a smaller mean diameter for the nanoparticles with copaiba oil and allantoin (143 nm) than for the nanoparticles with copaiba oil (204 nm). The physicochemical properties indicated that the dispersions were stable overtime. Rheology evidenced Newtonian behaviour for both suspensions. Antifungal susceptibility showed a MIC90 of 125 μg/mL (nanoparticles with copaiba oil) and 7.8 μg/mL (nanoparticles with copaiba oil and allantoin) against C. parapsilosis. The nanoparticles with copaiba oil and the nanoparticles with copaiba oil and allantoin presented a MIC90 of 500 μg/mL and 250 μg/mL, respectively, against C. krusei. The MIC90

  20. The Fundamental Plane of the Broad-line Region in Active Galactic Nuclei

    CERN Document Server

    Du, Pu; Hu, Chen; Ho, Luis C; Li, Yan-Rong; Bai, Jin-Ming

    2016-01-01

    Broad emission lines in active galactic nuclei (AGNs) mainly arise from gas photoionized by continuum radiation from an accretion disk around a central black hole. The shape of the broad-line profile, described by ${\\cal D}_{_{\\rm H\\beta}}={\\rm FWHM}/\\sigma_{_{\\rm H\\beta}}$, the ratio of full width at half maximum to the dispersion of broad H$\\beta$, reflects the dynamics of the broad-line region (BLR) and correlates with the dimensionless accretion rate ($\\dot{\\mathscr{M}}$) or Eddington ratio ($L_{\\rm bol}/L_{\\rm Edd}$). At the same time, $\\dot{\\mathscr{M}}$ and $L_{\\rm bol}/L_{\\rm Edd}$ correlate with ${\\cal R}_{\\rm Fe}$, the ratio of optical Fe II to H$\\beta$ line flux emission. Assembling all AGNs with reverberation mapping measurements of broad H$\\beta$, both from the literature and from new observations reported here, we find a strong bivariate correlation of the form $\\log(\\dot{\\mathscr{M}},L_{\\rm bol}/L_{\\rm Edd})=\\alpha+\\beta{\\cal D}_{_{\\rm H\\beta}}+\\gamma{\\cal R}_{\\rm Fe},$ where $\\alpha=(2.47,0.31...

  1. Constraints on the outer radius of the broad emission line region of active galactic nuclei

    CERN Document Server

    Landt, Hermine; Elvis, Martin; Karovska, Margarita

    2014-01-01

    Here we present observational evidence that the broad emission line region (BELR) of active galactic nuclei (AGN) generally has an outer boundary. This was already clear for sources with an obvious transition between the broad and narrow components of their emission lines. We show that the narrow component of the higher-order Paschen lines is absent in all sources, revealing a broad emission line profile with a broad, flat top. This indicates that the BELR is kinematically separate from the narrow emission line region. We use the virial theorem to estimate the BELR outer radius from the flat top width of the unblended profiles of the strongest Paschen lines, Pa alpha and Pa beta, and find that it scales with the ionising continuum luminosity roughly as expected from photoionisation theory. The value of the incident continuum photon flux resulting from this relationship corresponds to that required for dust sublimation. A flat-topped broad emission line profile is produced by both a spherical gas distribution ...

  2. Expression and functional analysis of two osmotin (PR5) isoforms with differential antifungal activity from Piper colubrinum: prediction of structure-function relationship by bioinformatics approach.

    Science.gov (United States)

    Mani, Tomson; Sivakumar, K C; Manjula, S

    2012-11-01

    Osmotin, a pathogenesis-related antifungal protein, is relevant in induced plant immunity and belongs to the thaumatin-like group of proteins (TLPs). This article describes comparative structural and functional analysis of the two osmotin isoforms cloned from Phytophthora-resistant wild Piper colubrinum. The two isoforms differ mainly by an internal deletion of 50 amino acid residues which separates them into two size categories (16.4 kDa-PcOSM1 and 21.5 kDa-PcOSM2) with pI values 5.6 and 8.3, respectively. Recombinant proteins were expressed in E. coli and antifungal activity assays of the purified proteins demonstrated significant inhibitory activity of the larger osmotin isoform (PcOSM2) on Phytophthora capsici and Fusarium oxysporum, and a markedly reduced antifungal potential of the smaller isoform (PcOSM1). Homology modelling of the proteins indicated structural alterations in their three-dimensional architecture. Tertiary structure of PcOSM2 conformed to the known structure of osmotin, with domain I comprising of 12 β-sheets, an α-helical domain II and a domain III composed of 2 β-sheets. PcOSM1 (smaller isoform) exhibited a distorted, indistinguishable domain III and loss of 4 β-sheets in domain I. Interestingly, an interdomain acidic cleft between domains I and II, containing an optimally placed endoglucanase catalytic pair composed of Glu-Asp residues, which is characteristic of antifungal PR5 proteins, was present in both isoforms. It is well accepted that the presence of an acidic cleft correlates with antifungal activity due to the presence of endoglucanase catalytic property, and hence the present observation of significantly reduced antifungal capacity of PcOSM1 despite the presence of a strong acidic cleft, is suggestive of the possible roles played by other structural features like domain I or/and III, in deciding the antifungal potential of osmotin.

  3. SCREENING FOR ANTIBACTERIAL AND ANTIFUNGAL ACTIVITIES IN SOME MARINE ALGAE FROM THE FUJIAN COAST OF CHINA WITH THREE DIFFERENT SOLVENTS

    Institute of Scientific and Technical Information of China (English)

    郑怡; 陈寅山; 卢海声

    2001-01-01

    Three different solvents viz ethanol, acetone and methanol-toluene (3:1) were used to extract antibiotics from 23 species of marine algae belonging to the Chlorophyta, Phaeophyta and Rhodophyta. Their crude extracts were tested for antibacterial and antifungal activities. Among them, the ethanol extract showed the strongest activity against the bacteria and fungi tested. Four species of the Rhodophyta (Laurencia okamurai, Dasya scoparia, Grateloupia filicina and plocamium telfairiae ) showed a wide spectrum of antibacterial activity. Every solvent extract from the four species was active against all the bacteria tested. The test bacterium Pseudomonas solancearum and the fungus Penicilium citrinum were most sensitive to the extracts of marine algae. In general, the extracts of seaweeds inhibited bacteria more strongly than fungi and species of the Rhodophyta showed the greatest activity against the bacteria and fungi tested.

  4. SCREENING FOR ANTIBACTERIAL AND ANTIFUNGAL ACTIVITIES IN SOME MARINE ALGAE FROM THE FUJIAN COAST OF CHINA WITH THREE DIFFERENT SOLVENTS

    Institute of Scientific and Technical Information of China (English)

    郑怡; 陈寅山; 卢海声

    2001-01-01

    Three different solvents viz ethanol, acetone and methanol-toluene (3:1) were used to extract antibiotics from 23 species of marine algae belonging to the Chlomphyta, Phaeophyta and Rhodophyta. Their crude extracts were tested for antibacterial and antifungal activities. Among them, the ethanol extract showed the strongest activity against the bacteria and fungi tested. Four species of the Rhodophyta (Laurenc/a okamurai, Dasya scoparia, Grateloupia filicina and plocamium telfairiae ) showed a wide spectrum of antibacterial activity. Every solvent extract from the four species was active against all the bacteria tested. The test bacterium Pseudomonas solancearum and the fungus Penicilium citrinum were most sensitive to the extracts of marine algae. In general, the extracts of seaweeds inhibited bacteria more strongly than fungi and species of the Rhodophyta showed the greatest activity against the bacteria and fungi tested.

  5. Silver nanoparticle production by the fungus Fusarium oxysporum: nanoparticle characterisation and analysis of antifungal activity against pathogenic yeasts

    Science.gov (United States)

    Ishida, Kelly; Cipriano, Talita Ferreira; Rocha, Gustavo Miranda; Weissmüller, Gilberto; Gomes, Fabio; Miranda, Kildare; Rozental, Sonia

    2013-01-01

    The microbial synthesis of nanoparticles is a green chemistry approach that combines nanotechnology and microbial biotechnology. The aim of this study was to obtain silver nanoparticles (SNPs) using aqueous extract from the filamentous fungus Fusarium oxysporum as an alternative to chemical procedures and to evaluate its antifungal activity. SNPs production increased in a concentration-dependent way up to 1 mM silver nitrate until 30 days of reaction. Monodispersed and spherical SNPs were predominantly produced. After 60 days, it was possible to observe degenerated SNPs with in additional needle morphology. The SNPs showed a high antifungal activity against Candida and Cryptococcus , with minimum inhibitory concentration values ≤ 1.68 µg/mL for both genera. Morphological alterations of Cryptococcus neoformans treated with SNPs were observed such as disruption of the cell wall and cytoplasmic membrane and lost of the cytoplasm content. This work revealed that SNPs can be easily produced by F. oxysporum aqueous extracts and may be a feasible, low-cost, environmentally friendly method for generating stable and uniformly sized SNPs. Finally, we have demonstrated that these SNPs are active against pathogenic fungi, such as Candida and Cryptococcus . PMID:24714966

  6. Development and Application of a High-Throughput Screening Method to Evaluate Antifungal Activity against Trichophyton tonsurans.

    Science.gov (United States)

    Preuett, Barry; Leeder, J Steven; Abdel-Rahman, Susan

    2015-10-01

    There exist relatively few drug classes on the market to treat dermatophyte infections. This investigation was designed to develop and validate high-throughput methodology for screening and confirmation of chemicals for activity against Trichophyton tonsurans. Growth characteristics were examined on two platforms (96- and 384-well) in three media at eight spore concentrations over a period of up to 120 h. Microspectrophotometry was used to automate plate reads. The 384-well platform was used to screen more than 7000 compounds from six chemical libraries. Z-scores for optical density relative to positive growth controls were used to flag compounds of interest and activity confirmed in separate assays. The final conditions selected for both screening and confirmation with minimum inhibitory concentration (MIC) determination were growth for 48 h at 32 °C in SabDex with 1 × 10(4) spores per reaction. Sensitivity and specificity averaged 99.2% (range, 95.2%-100%) and 99.8% (range, 99.1%-100%), respectively. MICs for known antifungals were similar to those reported by others using Clinical and Laboratory Standards Institute methods. Several novel compound classes were identified to have activity against T. tonsurans with potency comparable to known antifungals. A robust, reproducible assay is described that permits high-throughput screening in T. tonsurans.

  7. Antifungal Activity of Phenyl Derivative of Pyranocoumarin from Psoralea corylifolia L. Seeds by Inhibition of Acetylation Activity of Trichothecene 3-O-Acetyltransferase (Tri101

    Directory of Open Access Journals (Sweden)

    Sangeetha Srinivasan

    2012-01-01

    Full Text Available Antifungal activity of petroleum ether extract of Psoralea corylifolia L. seed, tested against Fusarium sp. namely, Fusarium oxysporum, Fusarium moniliforme, and Fusarium graminearum, was evaluated by agar well diffusion assay. The chromatographic fractionation of the extract yielded a new phenyl derivative of pyranocoumarin (PDP. The structure of the PDP was confirmed using spectroscopic characterization (GC-MS, IR, and NMR, and a molecular mass of m/z 414 [M-2H]+ with molecular formula C27H28O4 was obtained. The PDP had a potent antifungal activity with a minimum inhibitory concentration of 1 mg/mL against Fusarium sp. Molecular docking using Grid-Based Ligand Docking with Energetics (GLIDE, Schrodinger was carried out with the Tri101, trichothecene 3-O-acetyltransferase, as target protein to propose a mechanism for the antifungal activity. The ligand PDP showed bifurcated hydrogen bond interaction with active site residues at TYR 413 and a single hydrogen bond interaction at ARG 402 with a docking score −7.19 and glide energy of −45.78 kcal/mol. This indicated a strong binding of the ligand with the trichothecene 3-O-acetyltransferase, preventing as a result the acetylation of the trichothecene mycotoxin and destruction of the “self-defense mechanism” of the Fusarium sp.

  8. Oat (Avena sativa) seed extract as an antifungal food preservative through the catalytic activity of a highly abundant class I chitinase

    DEFF Research Database (Denmark)

    Sørensen, Hans Peter; Madsen, Lone Søvad; Petersen, Jørgen;

    2010-01-01

    to prevent the formation of P. roqueforti colonies. Proteins in the oat seed extracts were fractionated by column chromatography and proteins in fractions containing antifungal activity were identified by liquid chromatography-tandem mass spectrometry (LC-MS/MS) and database searches. Identified antifungal......Extracts from different higher plants were screened for the ability to inhibit the growth of Penicillium roqueforti, a major contaminating species in industrial food processing. Oat (Avena sativa) seed extracts exhibited a high degree of antifungal activity and could be used directly on rye bread...... candidates included thaumatin-like proteins, 1,3-beta-glucanase, permatin precursor, pathogenesis-related protein type 1, and chitinases of class I and II. Class I chitinase could be specifically removed from the extracts and was found to be indispensable for 50% of the P. roqueforti inhibiting activity...

  9. Antifungal activity of the basil (Ocimmum basilicum L. extract on Penicillium aurantiogriseum, P. glabrum, P. chrysogenum, and P. brevicompactum

    Directory of Open Access Journals (Sweden)

    Kocić-Tanackov Sunčica D.

    2012-01-01

    Full Text Available This study was aimed at investigating the antifungal potential of basil (Ocimmum basilicum L. extract against toxin-producing Penicillium spp. (P. aurantiogriseum, P. glabrum, P. chrysogenum, and P. brevicompactum isolated from food. The basil extract composition was determined by the GC-MS method. The major component identified in the extract was estragole (86.72%. The determination of the antifungal activity of basil extract on Penicillium spp. was performed using the agar plate method. Basil extract reduced the growth of Penicillium spp. at all applied concentration levels (0.16, 0.35, 0.70, and 1.50 mL/100mL with the colony growth inhibition from 3.6 (for P. glabrum to 100% (for P. chrysogenum. The highest sensitivity showed P. chrysogenum, where the growth was completely inhibited at the basil extract concentration of 1.50 mL/100mL. The growth of other Penicillium spp. was partially inhibited with the colony growth inhibition of 63.4 % (P. brevicompactum, 67.5% (P. aurantiogriseum, and 71.7% (P. glabrum. Higher concentrations (0.70 and 1.50 mL/100mL reduced the growth of the aerial mycelium of all tested Penicillium species. In addition,