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Last update: November 12, 2013.


EPA Science Inventory

Conazoles used in agriculture and pharmaceutical products comprise a class of chemicals which inhibit ergosterol biosynthesis to act as fungicides. Both propiconazole and triadimefon are hepatotoxic and hepatotumorigenic in mice, while myclobutanil is not a mouse liver tumorigen....



EPA Science Inventory

Conazoles are a class of azole based fungicides used in agriculture and as pharmaceutical products. They have a common mode of antifungal action through inhibition of ergosterol biosynthesis. Some members of this class have been shown to be hepatotoxic and will induce mouse hepa...


Inhibition of Rat and Human Steroidogenesis by Triazole Antifungals  

EPA Science Inventory

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



EPA Science Inventory

Conazoles comprise a class of fungicides used in agriculture and as pharmaceutical products. The fungicidal properties of conazoles are due to their inhibition of ergosterol biosynthesis. Certain conazoles are tumorigenic in rodents; both propiconazole and triadimefon are hepatot...



EPA Science Inventory

1. This study was undertaken to examine the inductive effects of two triazole antifungal agents, myclobutanil and triadimefon on the expression of hepatic cytochrome P450 (CYP) genes and on the activities of CYP enzymes in male Sprague-Dawley rats. Rats were dosed by gavage for 1...


Dissipation and residue of myclobutanil in lychee.  


The dissipation and residue of myclobutanil in lychee under field conditions were studied. To determine myclobutanil residue in samples, an analytical method with a florisil column clean-up and detected by gas chromatography-electron capture detector (GC-ECD) was developed. Recoveries were found in the range of 83.24 %-89.00 % with relative standard deviations of 2.67 %-9.88 %. This method was successfully applied to analyze the dissipation and residue of myclobutanil in lychee in Guangdong and Guangxi Province, China. The half lives in lychee were from 2.2 to 3.4 days. The residues of myclobutanil in lychee flesh were all below the limit of quantification (LOQ) value (0.01 mg/kg), and most of the residues were concentrated in the peel. The terminal residues of myclobutanil were all bellow the maximum residue limit (MRL) value set by European Union (EU) (0.02 mg/kg). Hence it was safe for the use of this pesticide and the results also could give a reference for MRL setting of myclobutanil in lychee in China. PMID:22526985

Liu, Yanping; Sun, Haibin; Liu, Fengmao; Wang, Siwei



77 FR 75039 - Propiconazole; Pesticide Tolerances  

Federal Register 2010, 2011, 2012, 2013

...susceptibility of the offspring to the toxic doses of propiconazole. Propiconazole was negative for mutagenicity in the in vitro BALB/ 3T3 cell transformation assay, bacterial reverse mutation assay, Chinese hamster bone marrow chromosomal aberration...



77 FR 38199 - Propiconazole; Pesticide Tolerances  

Federal Register 2010, 2011, 2012, 2013

...the offspring to the toxic doses of propiconazole in this study. Propiconazole was negative for mutagenicity in the in vitro BALB/C 3T3 cell transformation assay, bacterial reverse mutation assay, Chinese hamster bone marrow chromosomal aberration...



76 FR 27261 - Propiconazole; Pesticide Tolerances  

Federal Register 2010, 2011, 2012, 2013

...the offspring to the toxic doses of propiconazole in this study. Propiconazole was negative for mutagenicity in the in vitro BALB/C 3T3 cell transformation assay, bacterial reverse mutation assay, Chinese hamster bone marrow chromosomal aberration...



78 FR 23497 - Propiconazole; Pesticide Tolerances  

Federal Register 2010, 2011, 2012, 2013

...toxicity occurred at a higher dose than the parental toxic dose. Propiconazole was negative for mutagenicity in the in vitro BALB/3T3 cell transformation assay, bacterial reverse mutation assay, Chinese hamster bone marrow chromosomal aberration...




EPA Science Inventory

Toxicogenomic analysis of five environmental contaminants was performed to investigate the ability of genomics to categorize chemicals and elucidate mechanisms of toxicity. Three triazole antifungals (myclobutanil, propiconazole and triadimefon) and two perfluorinated compounds (...



EPA Science Inventory

Toxicogenomic analysis of five environmental chemicals was performed to investigate the ability of genomics to predict toxicity, categorize chemicals, and elucidate mechanisms of toxicity. Three triazole antifungals (myclobutanil, propiconazole, and triadimefon) and two perfluori...


Raman microscopy for the quantitation of propiconazole in white spruce  

Microsoft Academic Search

The Raman signature of propiconazole at 647–693 cm?1 was used to determine the propiconazole distribution in white spruce (Picea glauca). Samples treated with propiconazole were milled at ~1.5 mm intervals and analysed by methanol extraction and GC-MS to obtain\\u000a a depth profile in the longitudinal direction. The concentration of propiconazole in the milled wood layers ranged from 0.5\\u000a to 7.3 mg\\/g (dry mass

Erlet Kurti; D. V. Heyd; R. Stephen Wylie



Toxicogenomic effects common to triazole antifungals and conserved between rats and humans  

SciTech Connect

The triazole antifungals myclobutanil, propiconazole and triadimefon cause varying degrees of hepatic toxicity and disrupt steroid hormone homeostasis in rodent in vivo models. To identify biological pathways consistently modulated across multiple timepoints and various study designs, gene expression profiling was conducted on rat livers from three separate studies with triazole treatment groups ranging from 6 h after a single oral gavage exposure, to prenatal to adult exposures via feed. To explore conservation of responses across species, gene expression from the rat liver studies were compared to in vitro data from rat and human primary hepatocytes exposed to the triazoles. Toxicogenomic data on triazoles from 33 different treatment groups and 135 samples (microarrays) identified thousands of probe sets and dozens of pathways differentially expressed across time, dose, and species - many of these were common to all three triazoles, or conserved between rodents and humans. Common and conserved pathways included androgen and estrogen metabolism, xenobiotic metabolism signaling through CAR and PXR, and CYP mediated metabolism. Differentially expressed genes included the Phase I xenobiotic, fatty acid, sterol and steroid metabolism genes Cyp2b2 and CYP2B6, Cyp3a1 and CYP3A4, and Cyp4a22 and CYP4A11; Phase II conjugation enzyme genes Ugt1a1 and UGT1A1; and Phase III ABC transporter genes Abcb1 and ABCB1. Gene expression changes caused by all three triazoles in liver and hepatocytes were concentrated in biological pathways regulating lipid, sterol and steroid homeostasis, identifying a potential common mode of action conserved between rodents and humans. Modulation of hepatic sterol and steroid metabolism is a plausible mode of action for changes in serum testosterone and adverse reproductive outcomes observed in rat studies, and may be relevant to human risk assessment.

Goetz, Amber K. [National Center for Computational Toxicology, Office of Research and Development, U.S. Environmental Protection Agency, Research Triangle Park, North Carolina 27711 (United States); Department of Environmental and Molecular Toxicology, North Carolina State University, Raleigh, North Carolina 27695 (United States); Dix, David J. [National Center for Computational Toxicology, Office of Research and Development, U.S. Environmental Protection Agency, Research Triangle Park, North Carolina 27711 (United States)], E-mail:




EPA Science Inventory

The mode of action of conazole fungicides is to inhibit cytochrome P450 (CYP) 51 activity and thus the biosynthesis of ergosterol by fungi. Conazoles can also modulate other CYP activities in vertebrate species including humans. Myclobutanil (MCL) and triadimefon (TRD) are ag...


Influence of lysozyme, yeast, azoxystrobin, and myclobutanil on fungal diseases of cucumbers grown hydroponically  

Microsoft Academic Search

The influence of hen egg white lysozyme (HEWL) on root rot caused by Pythium aphanidermatum, and of HEWL, yeast, azoxystrobin, and myclobutanil on stem canker caused by Botrytis cinerea and gummy stem blight caused by Didymella bryoniae in cucumber grown under near-commercial greenhouse conditions was studied. HEWL treatments applied as a root drench at 5g\\/l every 3 weeks gave a

R. Utkhede; C. Bogdanoff



Antifungal polypeptides  


The invention relates to antifungal compositions and methods for protecting a plant from a fungal pathogen. Compositions including antifungal polypeptides isolated from a fungal fermentation broth are provided.

Altier, Daniel J. (Waukee, IA); Ellanskaya, Irina (Kyiv, UA); Ellanskaya, legal representative, Natalia (Kyiv, UA); Gilliam, Jacob T. (Norwalk, IA); Hunter-Cevera, Jennie (Elliott City, MD); Presnail, James K. (Avondale, PA); Schepers, Eric (Port Deposit, MD); Simmons, Carl R. (Des Moines, IA); Torok, Tamas (Richmond, CA); Yalpani, Nasser (Johnston, IA)



Occurrence of azoxystrobin, propiconazole, and selected other fungicides in US streams, 2005-2006  

USGS Publications Warehouse

Fungicides are used to prevent foliar diseases on a wide range of vegetable, field, fruit, and ornamental crops. They are generally more effective as protective rather than curative treatments, and hence tend to be applied before infections take place. Less than 1% of US soybeans were treated with a fungicide in 2002 but by 2006, 4% were treated. Like other pesticides, fungicides can move-off of fields after application and subsequently contaminate surface water, groundwater, and associated sediments. Due to the constant pressure from fungal diseases such as the recent Asian soybean rust outbreak, and the always-present desire to increase crop yields, there is the potential for a significant increase in the amount of fungicides used on US farms. Increased fungicide use could lead to increased environmental concentrations of these compounds. This study documents the occurrence of fungicides in select US streams soon after the first documentation of soybean rust in the US and prior to the corresponding increase in fungicide use to treat this problem. Water samples were collected from 29 streams in 13 states in 2005 and/or 2006, and analyzed for 12 target fungicides. Nine of the 12 fungicides were detected in at least one stream sample and at least one fungicide was detected in 20 of 29 streams. At least one fungicide was detected in 56% of the 103 samples, as many as five fungicides were detected in an individual sample, and mixtures of fungicides were common. Azoxystrobin was detected most frequently (45% of 103 samples) followed by metalaxyl (27%), propiconazole (17%), myclobutanil (9%), and tebuconazole (6%). Fungicide detections ranged from 0.002 to 1.15 ?/L. There was indication of a seasonal pattern to fungicide occurrence, with detections more common and concentrations higher in late summer and early fall than in spring. At a few sites, fungicides were detected in all samples collected suggesting the potential for season-long occurrence in some streams. Fungicide occurrence appears to be related to fungicide use in the associated drainage basins; however, current use information is generally lacking and more detailed occurrence data are needed to accurately quantify such a relation. Maximum concentrations of fungicides were typically one or more orders of magnitude less than current toxicity estimates for freshwater aquatic organisms or humans; however, gaps in current toxicological understandings of the effects of fungicides in the environment limit these interpretations.

Battaglin, William A.; Sandstrom, Mark W.; Kuivila, Kathryn M.; Kolpin, Dana W.; Meyer, Michael T.



40 CFR 180.434 - Propiconazole; tolerances for residues.  

Code of Federal Regulations, 2013 CFR

...equivalent of propiconazole, in or on the commodity in the table below: Commodity Parts per million Almond, hulls 7.0 Banana 0.2 Barley, bran 6.0 Barley, grain 3.0 Barley, hay 30 Barley, straw 20 Bean, dry seed...



Combined effects of the fungicide propiconazole and agricultural runoff sediments on the aquatic bryophyte Vesicularia dubyana.  


Pesticides, firmly attached to the topsoil, might enter nearby watercourses at periods with high erosive loss of sediments. Therefore, exposure of aquatic organisms to these low mobility pesticides, in many cases, will coincide with a high sediment concentration. In this study, both individual and combined effects of propiconazole and runoff sediment on the aquatic model bryophyte Vesicularia dubyana are studied. Individual exposure to propiconazole induced responses in V. dubyana at rather low concentration levels (approximately 1 microg/L), showing that harmful effects of propiconazole potentially may occur in watercourses draining propiconazole-treated fields. Individual exposure to the sediment size fractions S1 (0.16-2 microm) and S2 (0.03-0.16 microm) caused plant stress at a concentration of 100 mg/L. The coarser fraction S1 showed strong inhibition effects on photosynthesis, probably due to light attenuation. Compared to S1, the suspension with the finer fraction S2 showed lower turbidity, higher nutrient content, and a higher proportion of sediment-bound propiconazole. The combined effects of propiconazole and suspended sediment are dependent on concentrations of sediment and propiconazole. At low sediment concentration (e.g., 100 mg/L), neither S1 nor S2 reduce the toxicity of propiconazole, as only 2% of propiconazole are bound to particles. An increase in sediment concentration decreases the bioavailable concentration of propiconazole; however, at the same time, this increases the turbidity, thereby inhibiting plant photosynthesis. PMID:16193757

Wu, Qinglan; Riise, Gunnhild; Pflugmacher, Stephan; Greulich, K; Steinberg, Christian E W



Toxicogenomic Study of Triazole Fungicides and Perfluoroalkyl Acids in Rat Livers Predicts Toxicity and Categorizes Chemicals Based on Mechanisms of Toxicity  

Microsoft Academic Search

Toxicogenomic analysis of five environmental chemicals was performed to investigate the ability of genomics to predict toxicity, categorize chemicals, and elucidate mechanisms of toxicity. Three triazole antifungals (myclobutanil, propiconazole, and triadime- fon) and two perfluorinated chemicals (perfluorooctanoic acid (PFOA) and perfluorooctane sulfonate (PFOS)) were administered daily via oral gavage for one, three, or five consecutive days to male Sprague-Dawley rats

Matthew T. Martin; Richard J. Brennan; Wenyue Hu; Eser Ayanoglu; Christopher Lau; Hongzu Ren; Carmen R. Wood; J. Christopher Corton; Robert J. Kavlock; David J. Dix



Cytotoxic effects of propiconazole and its metabolites in mouse and human hepatoma cells and primary mouse hepatocytes  

EPA Science Inventory

Abstract: Propiconazole is a triazole-containing fungicide that is used agriculturally on grasses, fruits, grains, seeds, hardwoods, and conifers. Propiconazole is a mouse liver hepatotoxicant and a hepatocarcinogen and has adverse reproductive and developmental toxicities in exp...


Cytotoxic effects of propiconazole and its metabolites in mouse and human hepatoma cells and primary mouse hepatocytes  

Microsoft Academic Search

Propiconazole is a triazole-containing fungicide that is used agriculturally on grasses, fruits, grains, seeds, hardwoods, and conifers. Propiconazole is a mouse liver hepatotoxicant and a hepatocarcinogen that has adverse reproductive and developmental toxicities in experimental animals. The goal of this study was to investigate the cytotoxic responses of propiconazole and its metabolites to determine if metabolism of this agent differentially

Pei-Jen Chen; Tanya Moore; Stephen Nesnow



Altered microRNA expression induced by tumorigenic conazoles in mouse liver.  

EPA Science Inventory

Triadimefon, propiconazole, and myclobutanil are conazoles, an important class of agricultural and therapeutic fungicides. Triadimefon and propiconazole are mouse liver tumorigens, while myclobutanil is not. As part of a coordinated study to understand the molecular determinants ...



EPA Science Inventory

Triadimefon, propiconazole, and myclobutanil are conazoles, an important class of agricultural and therapeutic fungicides. Triadimefon and propiconazole are mouse liver tumorigens, while myclobutanil is not. All three conazoles are generally inactive in short-term genotoxicity t...


In vivo mutagenicity of conazole fungicides correlates with tumorigenicity  

EPA Science Inventory

Triadimefon, propiconazole, and myclobutanil are conazoles, an important class of agricultural and therapeutic fungicides. Triadimefon and propiconazole are mouse liver tumorigens, while myclobutanil is not. All three conazoles are generally inactive in short-term genotoxicity te...


Propiconazole inhibits steroidogenesis and reproduction in the fathead minnow (Pimephales promelas)  

EPA Science Inventory

This study assessed effects of the conazole-fungicide propiconazole on endocrine function and reproductive success of the fathead minnow, using an experimental approach based on previously defined adverse outcome pathways (AOPs) for chemicals that inhibit steroidogenesis in fish...


Antifungal hydrogels  

PubMed Central

Fungi are increasingly identified as major pathogens in bloodstream infections, often involving indwelling devices. Materials with antifungal properties may provide an important deterrent to these infections. Here we describe amphogel, a dextran-based hydrogel into which amphotericin B is adsorbed. Amphogel kills fungi within 2 h of contact and can be reused for at least 53 days without losing its effectiveness against Candida albicans. The antifungal material is biocompatible in vivo and does not cause hemolysis in human blood. Amphogel inoculated with C. albicans and implanted in mice prevents fungal infection. Amphogel also mitigates fungal biofilm formation. An antifungal matrix with these properties could be used to coat a variety of medical devices such as catheters as well as industrial surfaces.

Zumbuehl, Andreas; Ferreira, Lino; Kuhn, Duncan; Astashkina, Anna; Long, Lisa; Yeo, Yoon; Iaconis, Tiffany; Ghannoum, Mahmoud; Fink, Gerald R.; Langer, Robert; Kohane, Daniel S.



Propiconazole increases reactive oxygen species levels in mouse hepatic cells in culture and in mouse liver by a cytochrome P450 enzyme mediated process  

EPA Science Inventory

Propiconazole induces hepatocarcinomas and hepatoadenomas in mice and is a rat liver tumor promoter. Transcriptional, proteomic, metabolomic and biochemical studies of hepatic tissues from mice treated with propiconazole under the conditions of the chronic bioassay indicate that ...


Propiconazole inhibits steroidogenesis and reproduction in the fathead minnow (Pimephales promelas).  


Conazoles are designed to inhibit cytochrome P450 (CYP) 14?-demethylase, an enzyme key to fungal cell wall formation. In vertebrates, conazoles may inhibit other CYPs, potentially disrupting processes like sex steroid synthesis. Propiconazole is a current-use pesticide that is among the first chemicals being tested in the U.S. Environmental Protection Agency endocrine disruptor screening program. Fathead minnows (Pimephales promelas) were exposed to 0, 5, 50, 500, or 1000 µg propiconazole/l in a 21-day study that evaluated apical reproductive endpoints (fecundity, fertility, hatch); measures of endocrine function and steroid synthesis, such as cholesterol, vitellogenin (VTG), and sex steroid (testosterone [T], 17?-estradiol [E2]) concentrations in the plasma; and changes in gonadal expression of steroidogenic genes. Plasma E2 and VTG concentrations in females were reduced by exposure to propiconazole, and egg production was decreased in the 500 and 1000 µg/l treatment groups. These in vivo effects coincided with inhibition of E2 synthesis by ovary explants exposed to propiconazole in vitro. We also observed a compensatory response in females exposed to propiconazole, manifested as increased gonad weight and upregulation of genes coding for key steriodogenic proteins, including CYP19 (aromatase), CYP17 (hydroxylase/lyase), CYP11A (cholesterol side-chain-cleavage), and steroidogenic acute regulatory protein. Other than an increase in relative testis weight, effects on endocrine function in males were less pronounced than in females. This study provides important data relative to the potential endocrine activity of propiconazole in fish and, more generally, to the further delineation of pathways for the reproductive effects of steroid synthesis inhibitors in fish. PMID:23339182

Skolness, Sarah Y; Blanksma, Chad A; Cavallin, Jenna E; Churchill, Jessica J; Durhan, Elizabeth J; Jensen, Kathleen M; Johnson, Rodney D; Kahl, Michael D; Makynen, Elizabeth A; Villeneuve, Daniel L; Ankley, Gerald T



Proteomic analysis of propiconazole responses in mouse liver: comparison of genomic and proteomic profiles  

EPA Science Inventory

We have performed for the first time a comprehensive profiling of changes in protein expression of soluble proteins in livers from mice treated with the mouse liver tumorigen, propiconazole, to uncover the pathways and networks altered by this fungicide. Utilizing twodimensional ...


Proteomic Analysis of Propiconazole Responses in Mouse Liver-Comparison of Genomic and Proteomic Profiles  

EPA Science Inventory

We have performed for the first time a comprehensive profiling of changes in protein expression of soluble proteins in livers from mice treated with the mouse liver tumorigen, propiconazole, to uncover the pathways and networks altered by this commonly used fungicide. Utilizing t...


Defining Adverse Outcome Pathways for Effects of the Fungicide Propiconazole of Fish Reproduction  

EPA Science Inventory

Adverse outcome pathways (AOPs) are used to describe the linkage of chemical interactions in terms of molecular initiating events to whole organism responses suitable for risk assessment. This study was conducted to develop AOPs for the model fungicide propiconazole relative to r...


Use of Adverse Outcome Pathways for Assessing Effects of the Fungicide Propiconazole on Fish Reproduction  

EPA Science Inventory

Adverse outcome pathways (AOP) are used to describe the linkage of biological events from a molecular initiating point, to individual-level-endpoints relevant to risk assessment. This study was done to assess toxicity outcomes for the conazole fungicide propiconazole based on a p...


Effects of propiconazole on extra-cellular enzymes involved in nutrient mobilization during Trametes versicolor wood colonization  

Microsoft Academic Search

The effects of propiconazole on extra-cellular enzyme levels in Trametes versicolor have been investigated during wood colonization and degradation. The working hypothesis was that the biocide could alter\\u000a metabolic pathways, which could lead to an alteration of extra-cellular enzyme production. In the presence of a propiconazole\\u000a sub-lethal concentration, the wood degradation rate decrease concomitantly with the lag phase of fungal

Serge Lekounougou; Jean-Pierre Jacquot; Philippe Gérardin; Eric Gelhaye



Effect of turfgrass cover and irrigation on soil mobility and dissipation of mefenoxam and propiconazole.  


Irrigation effects on pesticide mobility have been studied, but few direct comparisons of pesticide mobility or persistence have been conducted on turfgrass versus bare soil. The interaction of irrigation practices and the presence of turfgrass on the mobility and dissipation of mefenoxam [N-(2,6-dimethylphenyl)-N-(methoxyacetyl)-D-alanine methyl ester] and propiconazole (1-[[2-(2,4-dichlorophenyl)-4-propyl-1,3-dioxolan-2-yl]methyl]-1H-1,2,4-triazole) was studied. Sampling cylinders (20-cm diam.) were placed in either creeping bentgrass [Agrostis stolonifera L. var. palustris (Huds.) Farw.] or bare soil. Mefenoxam was applied at 770 g a.i. ha(-1) and propiconazole was applied at 1540 g a.i. ha(-1) on 14 June 1999. Sampling cylinders were removed 2 h after treatment and 4,8,16, 32, and 64 days after treatment (DAT) and the cores were sectioned by depth. Dissipation of mefenoxam was rapid, regardless of the amount of surface organic matter or irrigation. The half-life (t1/2) of mefenoxam was 5 to 6 d in turf and 7 to 8 d in bare soil. Most mefenoxam residues found in soil under turfgrass were in the 0- to 1-cm section at 0, 4, and 8 DAT. Residues were found in the 15- to 30-cm section at 4, 8, 16, 32, and 64 DAT, regardless of turf cover or irrigation. The t1/2 of propiconazole was 12 to 15 d in turfgrass and 29 d in bare soil. Little movement of propiconazole was observed in either bare soil or turf. PMID:11577867

Gardner, D S; Branham, B E


Molecular impact of propiconazole on Daphnia magna using a reproduction-related cDNA array  

Microsoft Academic Search

We have developed a first version cDNA microarray of the cladoceran Daphnia magna. Through Suppression Subtractive Hybridisation PCR (SSH–PCR) 855 life stage-specific cDNAs were collected and used to document the toxicological mode of action of the pesticide propiconazole. DNA sequencing analysis revealed gene fragments related to important functional classes such as embryo development, energy metabolism, molting and cell cycle. Major

Anneleen Soetaert; Lotte N. Moens; Karlijn Van der Ven; Koen Van Leemput; Bart Naudts; Ronny Blust; Wim M. De Coen



Propiconazole enhanced hepatic cell proliferation is associated with dysregulation of the cholesterol biosynthesis pathway leading to activation of Erk1/2 through Ras famesylation  

EPA Science Inventory

Propiconazole is a mouse hepatotumorigenic fungicide designed to inhibit CYP51, a key enzyme in the biosynthesis of ergosterol in fungi and is widely used in agriculture to prevent fungal growth. Metabolomic studies in mice revealed that propiconazole increased levels of hepatic ...


Introduction to Antifungal Drugs  

Microsoft Academic Search

In the United States, only 10 antifungal drugs are currently approved by the Food and Drug Administration (FDA) for the therapy of systemic fungal infections. As shown in table 1, these drugs belong to 3 principal classes: polyenes, pyrimidines, and azoles. Drugs that belong to other classes are also approved as topical antifungal drugs, but will not be considered further

William E. Dismukes



Propiconazole-enhanced hepatic cell proliferation is associated with dysregulation of the cholesterol biosynthesis pathway leading to activation of Erk1/2 through Ras farnesylation.  


Propiconazole is a mouse hepatotumorigenic fungicide designed to inhibit CYP51, a key enzyme in the biosynthesis of ergosterol in fungi and is widely used in agriculture to prevent fungal growth. Metabolomic studies in mice revealed that propiconazole increased levels of hepatic cholesterol metabolites and bile acids, and transcriptomic studies revealed that genes within the cholesterol biosynthesis, cholesterol metabolism and bile acid biosyntheses pathways were up-regulated. Hepatic cell proliferation was also increased by propiconazole. AML12 immortalized hepatocytes were used to study propiconazole's effects on cell proliferation focusing on the dysregulation of cholesterol biosynthesis and resulting effects on Ras farnesylation and Erk1/2 activation as a primary pathway. Mevalonate, a key intermediate in the cholesterol biosynthesis pathway, increases cell proliferation in several cancer cell lines and tumors in vivo and serves as the precursor for isoprenoids (e.g. farnesyl pyrophosphate) which are crucial in the farnesylation of the Ras protein by farnesyl transferase. Farnesylation targets Ras to the cell membrane where it is involved in signal transduction, including the mitogen-activated protein kinase (MAPK) pathway. In our studies, mevalonic acid lactone (MVAL), a source of mevalonic acid, increased cell proliferation in AML12 cells which was reduced by farnesyl transferase inhibitors (L-744,832 or manumycin) or simvastatin, an HMG-CoA reductase inhibitor, indicating that this cell system responded to alterations in the cholesterol biosynthesis pathway. Cell proliferation in AML12 cells was increased by propiconazole which was reversed by co-incubation with L-744,832 or simvastatin. Increasing concentrations of exogenous cholesterol muted the proliferative effects of propiconazole and the inhibitory effects of L-733,832, results ascribed to reduced stimulation of the endogenous cholesterol biosynthesis pathway. Western blot analysis of subcellular fractions from control, MVAL or propiconazole-treated cells revealed increased Ras protein in the cytoplasmic fraction of L-744,832-treated cells, while propiconazole or MVAL reversed these effects. Western blot analysis indicated that phosphorylation of Erk1/2, a protein downstream of Ras, was increased by propiconazole. These data indicate that propiconazole increases cell proliferation by increasing the levels of cholesterol biosynthesis intermediates presumably through a negative feedback mechanism within the pathway, a result of CYP51 inhibition. This feedback mechanism increases Erk1/2 signaling through mevalonate-mediated Ras activation. These results provide an explanation for the observed effects of propiconazole on hepatic cholesterol pathways and on the increased hepatic cell proliferation induced by propiconazole in mice. PMID:22361350

Murphy, Lynea A; Moore, Tanya; Nesnow, Stephen



Antifungal activity of wogonin.  


The antifungal activity of the wogonin isolated from Holmskioldia sanguinea Retz was determined on four different fungal organisms. The pure compound wogonin significantly inhibited the growth of Aspergillus niger, Penicillium frequentance, P. notatum and Botrytis cinerea, in a concentration dependent fashion, when tested by turbidity and spore germination methods. The effects produced by the compound were compared with the standard antifungal agent griseofulvin. PMID:14669259

Pal, Mahesh; Joshi, Harsha; Kapoor, V P; Pushpangadan, P; Chaurasia, Leena



Antifungal activity of nontraditional antifungal agents  

Microsoft Academic Search

Invasive fungal infections are becoming increasingly important in the management of critically ill and immunocompromised patients.\\u000a As organ and stem cell transplantation becomes more prominent and immune therapies are employed for diseases such as rheumatoid\\u000a arthritis and plaque psoriasis, the population of patients at risk continues to grow. Many invasive fungal infections are\\u000a associated with extremely high mortality rates. Antifungal

William R. Judd; Craig A. Martin



Propiconazole Is a Specific and Accessible Brassinosteroid (BR) Biosynthesis Inhibitor for Arabidopsis and Maize  

PubMed Central

Brassinosteroids (BRs) are steroidal hormones that play pivotal roles during plant development. In addition to the characterization of BR deficient mutants, specific BR biosynthesis inhibitors played an essential role in the elucidation of BR function in plants. However, high costs and limited availability of common BR biosynthetic inhibitors constrain their key advantage as a species-independent tool to investigate BR function. We studied propiconazole (Pcz) as an alternative to the BR inhibitor brassinazole (Brz). Arabidopsis seedlings treated with Pcz phenocopied BR biosynthetic mutants. The steady state mRNA levels of BR, but not gibberellic acid (GA), regulated genes increased proportional to the concentrations of Pcz. Moreover, root inhibition and Pcz-induced expression of BR biosynthetic genes were rescued by 24epi-brassinolide, but not by GA3 co-applications. Maize seedlings treated with Pcz showed impaired mesocotyl, coleoptile, and true leaf elongation. Interestingly, the genetic background strongly impacted the tissue specific sensitivity towards Pcz. Based on these findings we conclude that Pcz is a potent and specific inhibitor of BR biosynthesis and an alternative to Brz. The reduced cost and increased availability of Pcz, compared to Brz, opens new possibilities to study BR function in larger crop species.

Best, Norman B.; Budka, Joshua S.; Zhu, Jia-Ying; Choe, Sunghwa; Schulz, Burkhard




EPA Science Inventory

Conazoles are N-substituted azole antifungal agents used as both pesticides and drugs. Some of these compounds are hepatocarcinogenic in mice and some can induce thyroid tumors in rats. Many of these compounds are able to induce and/or inhibit mammalian hepatic cytochrome P450s t...


Antifungal susceptibility testing.  


Unlike antibacterial susceptibility testing, reliable antifungal susceptibility testing is still largely in its infancy. Many methods have been described, but they produce widely discrepant results unless such factors as pH, inoculum size, medium formulation, incubation time, and incubation temperature are carefully controlled. Even when laboratories agree upon a common method, interlaboratory agreement may be poor. As a result of numerous collaborative projects carried out both independently and under the aegis of the Subcommittee on Antifungal Susceptibility Testing of the National Committee for Clinical Laboratory Standards, the effects of varying these factors have been extensively studied and a standard method which minimizes interlaboratory variability during the testing of Candida spp. and Cryptococcus neoformans has been proposed. This review summarizes this work, reviews the strengths and weaknesses of the proposed susceptibility testing standard, and identifies directions for future work. PMID:8269392

Rex, J H; Pfaller, M A; Rinaldi, M G; Polak, A; Galgiani, J N



Antifungal flavonoids from Hildegardia barteri.  


A new isoflavan, (3R)-6,2'-dihydroxy-7-methoxy-4',5'-methylenedioxyisoflavan, hildegardiol (1), and two known flavonoids, 2-hydroxymaackiain (2) and farrerol (3), were isolated from the antifungal root extract of Hildegardia barteri. The pterocarpan 2 was largely responsible for the observed antifungal activity. PMID:16378378

Meragelman, Tamara L; Tucker, Kenneth D; McCloud, Thomas G; Cardellina, John H; Shoemaker, Robert H



Antifungal agents: mechanisms of action  

Microsoft Academic Search

Clinical needs for novel antifungal agents have altered steadily with the rise and fall of AIDS-related mycoses, and the change in spectrum of fatal disseminated fungal infections that has accompanied changes in therapeutic immunosuppressive therapies. The search for new molecular targets for antifungals has generated considerable research using modern genomic approaches, so far without generating new agents for clinical use.

Frank C. Odds; Alistair J. P. Brown; Neil A. R. Gow



Antifungal treatment and chronic rhinosinusitis.  


Chronic rhinosinusitis (CRS) is an inflammatory disease with a multifactorial etiology. Antifungal therapy is not routinely used to treat it. However, evidence implicating fungi in some forms of CRS recently has been published. Controversy exists as to whether fungi identified in sinonasal cultures are always pathogenic. Immunologic evidence supporting the role of fungi in the pathogenesis of CRS is also debated. Topical antifungal therapy is more widely used than oral therapy, with amphotericin B irrigation being the most common. Although some studies show benefit from this irrigation, others refute the efficacy. Although oral antifungal agents are used uncommonly, itraconazole is the most commonly used drug. The efficacy of oral itraconazole in CRS has never been assessed in a clinical trial. Given the current evidence, the use of antifungals to treat CRS is controversial and has limited indications. PMID:19348723

Lal, Devyani; Stankiewicz, James A



Antibody Peptide Based Antifungal Immunotherapy  

PubMed Central

Fungal infections still represent relevant human illnesses worldwide and some are accompanied by unacceptably high mortality rates. The limited current availability of effective and safe antifungal agents makes the development of new drugs and approaches of antifungal vaccination/immunotherapy every day more needed. Among them, small antibody(Ab)-derived peptides are arousing great expectations as new potential antifungal agents. In this topic, the search path from the study of the yeast killer phenomenon to the production of Ab-derived peptides characterized by in vitro and in vivo fungicidal activity will be focused. In particular, Abs that mimic the antimicrobial activity of a killer toxin (“antibiobodies”) and antifungal peptides derived from antibiobodies (killer peptide) and other unrelated Abs [complementarity determining regions (CDR)-based and constant region (Fc)-based synthetic peptides] are described. Mycological implications in terms of reevaluation of the yeast killer phenomenon, roles of antibiobodies in antifungal immunity, of ?-glucans as antifungal targets and vaccines, and of Abs as sources of an unlimited number of sequences potentially active as new immunotherapeutic tools against fungal agents and related mycoses, are discussed.

Magliani, Walter; Conti, Stefania; Giovati, Laura; Zanello, Pier Paolo; Sperinde, Martina; Ciociola, Tecla; Polonelli, Luciano



Antifungal therapy with an emphasis on biofilms.  


Fungal infections are on the rise as advances in modern medicine prolong the lives of severely ill patients. Fungi are eukaryotic organisms and there are a limited number of targets for antifungal drug development; as a result the antifungal arsenal is exceedingly limited. Azoles, polyenes and echinocandins constitute the mainstay of antifungal therapy for patients with life-threatening mycoses. One of the main factors complicating antifungal therapy is the formation of fungal biofilms, microbial communities displaying resistance to most antifungal agents. A better understanding of fungal biofilms provides for new opportunities for the development of urgently needed novel antifungal agents and strategies. PMID:24011516

Pierce, Christopher G; Srinivasan, Anand; Uppuluri, Priya; Ramasubramanian, Anand K; López-Ribot, José L



Haloprogin: a Topical Antifungal Agent  

PubMed Central

Haloprogin was shown to be a highly effective agent for the treatment of experimentally induced topical mycotic infections in guinea pigs. Its in vitro spectrum of activity also includes yeasts, yeastlike fungi (Candida species), and certain gram-positive bacteria. The in vitro and in vivo antifungal activity of haloprogin against dermatophytes was equal to that observed with tolnaftate. The striking differences between the two agents were the marked antimonilial and selective antibacterial activities shown by haloprogin, contrasted with the negligible activities found with tolnaftate. Addition of serum decreased the in vitro antifungal activity of haloprogin to a greater extent than that of tolnaftate; however, diminished antifungal activity was not observed when haloprogin was applied topically to experimental dermatophytic infections. Based on its broad spectrum of antimicrobial activity, haloprogin may prove to be a superior topical agent in the treatment of dermatophytic and monilial infections in man.

Harrison, E. F.; Zwadyk, P.; Bequette, R. J.; Hamlow, E. E.; Tavormina, P. A.; Zygmunt, W. A.



Haloprogin: a topical antifungal agent.  


Haloprogin was shown to be a highly effective agent for the treatment of experimentally induced topical mycotic infections in guinea pigs. Its in vitro spectrum of activity also includes yeasts, yeastlike fungi (Candida species), and certain gram-positive bacteria. The in vitro and in vivo antifungal activity of haloprogin against dermatophytes was equal to that observed with tolnaftate. The striking differences between the two agents were the marked antimonilial and selective antibacterial activities shown by haloprogin, contrasted with the negligible activities found with tolnaftate. Addition of serum decreased the in vitro antifungal activity of haloprogin to a greater extent than that of tolnaftate; however, diminished antifungal activity was not observed when haloprogin was applied topically to experimental dermatophytic infections. Based on its broad spectrum of antimicrobial activity, haloprogin may prove to be a superior topical agent in the treatment of dermatophytic and monilial infections in man. PMID:5422306

Harrison, E F; Zwadyk, P; Bequette, R J; Hamlow, E E; Tavormina, P A; Zygmunt, W A



Alternative approaches to antifungal therapies  

PubMed Central

The expansive use of immunosuppressive medications in fields such as transplantational medicine and oncology, the higher frequency of invasive procedures in an aging population and the HIV/AIDS pandemic have increased the frequency of systemic fungal infections. At the same time, increased resistance of pathogenic fungi to classical antifungal agents has led to sustained research efforts targeting alternative antifungal strategies. In this review, we focus on two promising approaches: cationic peptides and the targeting of fungal virulence factors. Cationic peptides are small, predominantly positively charged protein fragments which exert direct and indirect antifungal activities, one mechanism of action being the permeabilization of the fungal membrane. They include lysozyme, defensins, and cathelicidins, as well as novel synthetic peptides. Amongst fungal virulence factors, the targeting of candidal secreted aspartic proteinases seems to be a particularly promising approach.

Mehra, T; Koberle, M; Braunsdorf, C; Mailander-Sanchez, D; Borelli, C; Schaller, M



Comparison of echinocandin antifungals  

PubMed Central

The incidence of invasive fungal infections, especially those due to Aspergillus spp. and Candida spp., continues to increase. Despite advances in medical practice, the associated mortality from these infections continues to be substantial. The echinocandin antifungals provide clinicians with another treatment option for serious fungal infections. These agents possess a completely novel mechanism of action, are relatively well-tolerated, and have a low potential for serious drug–drug interactions. At the present time, the echinocandins are an option for the treatment of infections due Candida spp (such as esophageal candidiasis, invasive candidiasis, and candidemia). In addition, caspofungin is a viable option for the treatment of refractory aspergillosis. Although micafungin is not Food and Drug Administration-approved for this indication, recent data suggests that it may also be effective. Finally, caspofungin- or micafungin-containing combination therapy should be a consideration for the treatment of severe infections due to Aspergillus spp. Although the echinocandins share many common properties, data regarding their differences are emerging at a rapid pace. Anidulafungin exhibits a unique pharmacokinetic profile, and limited cases have shown a potential far activity in isolates with increased minimum inhibitory concentrations to caspofungin and micafungin. Caspofungin appears to have a slightly higher incidence of side effects and potential for drug–drug interactions. This, combined with some evidence of decreasing susceptibility among some strains of Candida, may lessen its future utility. However, one must take these findings in the context of substantially more data and use with caspofungin compared with the other agents. Micafungin appears to be very similar to caspofungin, with very few obvious differences between the two agents.

Eschenauer, Gregory; DePestel, Daryl D; Carver, Peggy L



Side effects of propiconazole (tilt 250 EC TM ) on non-target soil fungi in a field trial compared with natural stress effects  

Microsoft Academic Search

The present study was performed as a dose-response field experiment using a trade marked formulation of the ergosterol biosynthesis\\u000a inhibiting fungicide, propiconazole, applied at the recommended and ten times the recommended application rates. The soil\\u000a dilution plate method was used to isolate fungi from 0–1 and 1–2 cm soil depth. Soil samples were taken 10 times during the\\u000a period from

Susanne Elmholt




EPA Science Inventory

Conazoles are fungicides used in crop protection and as pharmaceuticals. Triadimefon and propiconazole are hepatotumorigenic in mice, while myclobutanil is not. Previous toxicogenomic studies suggest that alteration of the retinoic acid metabolism pathway may involve in conazole-...



EPA Science Inventory

Conazoles comprise a chemical class of fungicides used as agricultural and pham-taceutical products. Both propiconazole and triadimefon are hepatotoxic and hepatotumorigenic in mice, while myclobutanil is not a mouse liver tumorigen. The tumorigenic activities of these conazoles ...



EPA Science Inventory

Four triazole fungicides were studied using toxicogenomic techniques to identify potential mechanisms of action. Adult male Sprague-Dawley rats were dosed for 14 days by gavage with fluconazole, myclobutanil, propiconazole, or triadimefon. Following exposure, serum was collected ...


Gene Expression Profiling in Liver and Testis of Rats to Characterize the Toxicity of Triazole Fungicides  

EPA Science Inventory

Four triazole fungicides were studied using toxicogenomic techniques to identify potential mechanisms of action. Adult male Sprague-Dawley rats were dosed for 14 days by gavage with fluconazole, myclobutanil, propiconazole, or triadimefon. Following exposure, serum was collected ...



EPA Science Inventory

Conazoles arc a class of fungicides used as pharmaceutical and agricultural products. In chronic bioassays, triadimefon was hepatotoxic and induced transitional cell adenomas in the thyroid gland. Both propiconazole and myclobutanil were hepatotoxic but had no effect on the thyro...



EPA Science Inventory

Normal Raman spectroscopy was evaluated as a metabolomic tool for assessing the impacts of exposure to environmental contaminants, using rat urine collected during the course of a toxicological study. Specifically, one of three triazole fungicides, myclobutanil, propiconazole or ...


A Prototype Antifungal Contact Lens  

PubMed Central

Purpose. To design a contact lens to treat and prevent fungal ocular infections. Methods. Curved contact lenses were created by encapsulating econazole-impregnated poly(lactic-co-glycolic) acid (PLGA) films in poly(hydroxyethyl methacrylate) (pHEMA) by ultraviolet photopolymerization. Release studies were conducted in phosphate-buffered saline at 37°C with continuous shaking. The contact lenses and their release media were tested in an antifungal assay against Candida albicans. Cross sections of the pre- and postrelease contact lenses were characterized by scanning electron microscopy and by Raman spectroscopy. Results. Econazole-eluting contact lenses provided extended antifungal activity against Candida albicans fungi. Fungicidal activity varied in duration and effectiveness depending on the mass of the econazole-PLGA film encapsulated in the contact lens. Conclusions. An econazole-eluting contact lens could be used as a treatment for fungal ocular infections.

Ciolino, Joseph B.; Hudson, Sarah P.; Mobbs, Ashley N.; Hoare, Todd R.; Iwata, Naomi G.; Fink, Gerald R.



Antifungal Resistance Mechanisms in Dermatophytes  

Microsoft Academic Search

Although fungi do not cause outbreaks or pandemics, the incidence of severe systemic fungal infections has increased significantly,\\u000a mainly because of the explosive growth in the number of patients with compromised immune system. Thus, drug resistance in\\u000a pathogenic fungi, including dermatophytes, is gaining importance. The molecular aspects involved in the resistance of dermatophytes\\u000a to marketed antifungals and other cytotoxic drugs,

Nilce M. Martinez-Rossi; Nalu T. A. Peres; Antonio Rossi



Caspofungin: An echinocandin antifungal agent  

Microsoft Academic Search

Background: The mainstays of treatment for nosocomial fungal infections have been amphotericin B and azole derivatives. Caspofungin acetate is a new echinocandin antifungal agent with a mechanism of action that targets a structural component of the fungal cell wall.Objective: This article describes the pharmacologic properties and potential clinical usefulness of caspofungin.Methods: Relevant information was identified through searches of MEDLINE (1966–September

Elizabeth A. Stone; Horatio B. Fung; Harold L. Kirschenbaum



Synthesis, antifungal and antimicrobial activity of alkylphospholipids.  


The antifungal, antibacterial and haemolytic activity of a series of alkylphosphocholines (e.g., miltefosine) and alkylglycerophosphocholines (e.g., edelfosine) has been investigated. These compound classes exhibit significant antifungal and moderate antibacterial activities. Several new alkylphosphocholine derivatives with amide or ester bonds in the alkyl chain have been synthesised. These compounds show much lower haemolytic activity than miltefosine. Alkylphosphocholines and alkylglycerophosphocholines show significant promise as novel orally available antifungal and antibacterial therapeutics. PMID:17532639

Obando, Daniel; Widmer, Fred; Wright, Lesley C; Sorrell, Tania C; Jolliffe, Katrina A



Screening antifungal activities of selected medicinal plants  

Microsoft Academic Search

Plants synthesise a vast array of secondary metabolites that are gaining importance for their biotechnological applications. The antifungal activity of the ethanolic extracts of ten Argentinean plants used in native medicine is reported. Antifungal assays included radial growth inhibition, disk and well diffusion assays and growth inhibition by broth dilution tests. The chosen test fungi were yeasts, microfungi and wood-rot

Emma Nelly Quiroga; Antonio Rodolfo Sampietro; Marta Amelia Vattuone



The search for new triazole antifungal agents  

Microsoft Academic Search

The first generation antifungal agent triazoles, fluconazole and itraconazole, have revolutionised the treatment of serious fungal infections such as mucosal and invasive candidiasis and cryptococcal meningitis. However, the treatment of some fungal infections, particularly aspergillosis, is still far from satisfactory and thus there is an important requirement for new broad-spectrum antifungal agents. The new second generation triazoles voriconazole and SCH-56592

Yigal Koltin; Christopher A Hitchcock



Photodynamic antifungal therapy against chromoblastomycosis.  


Photodynamic therapy (PDT) is a minimally invasive approach, in which a photosensitizer compound is activated by exposure to light. The activation of the sensitizer drug results in several chemical reactions, such as the production of reactive oxygen species and other reactive molecules, which presence in the biological site leads to the damage of target cells. Although PDT has been primarily developed to combat cancerous lesions, this therapy can be employed for the treatment of several conditions, including infectious diseases. A wide range of microorganisms, including Gram-positive and Gram-negative bacteria, viruses, protozoa, and fungi, have demonstrated susceptibility to antimicrobial PDT. This treatment might consist in an alternative for the management of fungal infections. Antifungal photodynamic therapy has been successfully employed against Candida species, dermatophytes, and Aspergillus niger. Chromoblastomycosis is an infection that involves skin and subcutaneous tissues caused by the traumatic inoculation of dematiaceous fungi species, being that the most prevalent are Fonsecaea pedrosoi and Claphialophora carrionii. In the present work, the clinical applications of PDT for the treatment of chromoblastomycosis are evaluated. We have employed methylene blue as photosensitizer and a LED (Light Emitting Diode) device as light source. The results of this treatment are positive, denoting the efficacy of PDT against chromoblastomycosis. Considering that great part of the published works are focused on in vitro trials, these clinical tests can be considered a relevant source of information about antifungal PDT, since its results have demonstrated to be promising. The perspectives of this kind of treatment are analyzed in agreement with the recent literature involving antifungal PDT. PMID:21643843

Lyon, Juliana Pereira; Pedroso e Silva Azevedo, Conceição de Maria; Moreira, Leonardo Marmo; de Lima, Carlos José; de Resende, Maria Aparecida



Antifungal Activity of C-27 Steroidal Saponins  

PubMed Central

As part of our search for new antifungal agents from natural resources, 22 C-27 steroidal saponins and 6 steroidal sapogenins isolated from several monocotyledonous plants were tested for their antifungal activity against the opportunistic pathogens Candida albicans, Candida glabrata, Candida krusei, Cryptococcus neoformans, and Aspergillus fumigatus. The results showed that the antifungal activity of the steroidal saponins was associated with their aglycone moieties and the number and structure of monosaccharide units in their sugar chains. Within the 10 active saponins, four tigogenin saponins (compounds 1 to 4) with a sugar moiety of four or five monosaccharide units exhibited significant activity against C. neoformans and A. fumigatus, comparable to the positive control amphotericin B. The antifungal potency of these compounds was not associated with cytotoxicity to mammalian cells. This suggests that the C-27 steroidal saponins may be considered potential antifungal leads for further preclinical study.

Yang, Chong-Ren; Zhang, Ying; Jacob, Melissa R.; Khan, Shabana I.; Zhang, Ying-Jun; Li, Xing-Cong



Antifungal peptides homologous to the Penicillium chrysogenum antifungal protein (PAF) are widespread among Fusaria.  


Putative antifungal peptide encoding genes containing Penicillium chrysogenum antifungal protein (PAF) characteristic amino acid motifs were identified in 15 Fusarium isolates, representing 10 species. Based on the predicted sequences of mature peptides, discrepancy in one, two or three amino acids was observed between them. Phylogenetic investigations revealed that they show high amino acid sequence similarity to PAF and they belong to the group of fungal derived antifungal peptides with PAF-cluster. Ten from the 15 partially purified <10 kDa peptide fraction of Fusarium ferment broths showed antifungal activity. The presence of approximately 6.3 kDa molecular weight peptides was detected in all of the antifungally active ferment broths, and this peptide was isolated and purified from Fusarium polyphilaidicum. The minimal inhibitiory concentrations of F. polyphilaidicum antifungal protein (FPAP) were determined against different filamentous fungi, yeasts and bacteria. Filamentous fungal species were the most susceptible to FPAF, but some yeasts were also slightly sensitive. PMID:23174348

Galgóczy, László; Virágh, Máté; Kovács, Laura; Tóth, Beáta; Papp, Tamás; Vágvölgyi, Csaba



Antifungal Drug Resistance: Clinical Relevance and Impact of Antifungal Drug Use  

Microsoft Academic Search

Antifungal drug resistance significantly impacts treatment outcomes in patients with invasive fungal infections (IFIs). Although\\u000a primary (intrinsic) resistance may occur independent of previous therapy, prior concomitant antifungal exposure increases\\u000a the risk for secondary (acquired) resistance and subsequent colonization or infection with less-susceptible pathogens. Among\\u000a various pathogen-antifungal combinations, this effect has been best studied clinically with azole exposure and the risk

Richard H. Drew; Mary L. Townsend



Antifungal sesquiterpenes from Cedrus deodara.  


Two new sesquiterpenes, (E)-(2S,3S,6R)-atlantone-2,3-diol (1) and (E)-(2S,3S,6S)-atlantone-2,3,6-triol (2), along with two known sesquiterpenes, atlantolone (3) and (E)-?-atlantone (4), were isolated from Cedrus deodara Loud. The structures of the new compounds were elucidated on the basis of UV, IR, NMR, HR?ESI-QTOF?MS, and EI mass spectral studies. The n-hexane and chloroformextracts of sawdust and compounds 3 and 4 from the plant exhibited antifungal activity against Aspergillus flavus, A. niger, A. ochracoeus, A. parasiticus, and A. sydowii. A weak activity was also recorded against A. parasiticus and A. sydowii for compound 1, while Trichophyton rubrum was inhibited by compound 2 and the extracts. PMID:21979930

Chaudhary, Abha; Sood, Swati; Kaur, Pushpinder; Kumar, Neeraj; Thakur, Archana; Gulati, Arvind; Singh, Bikram



Antifungal susceptibility of Malassezia pachydermatis biofilm.  


Abstract Antifungal resistance has been associated with biofilm formation in many microorganisms, but not yet in Malassezia pachydermatis. This saprophytic yeast can cause otitis and dermatitis in dogs and has emerged as an important human pathogen, responsible for systemic infections in neonates in intensive care units. This study aims to evaluate the in vitro antifungal susceptibility of M. pachydermatis strains, in both their planktonic and sessile forms, to fluconazole, miconazole, ketoconazole, itraconazole, posaconazole, terbinafine and voriconazole using the XTT assay and Clinical and Laboratory Standards Institute (CLSI) microdilution method. The minimum inhibitory concentration (MIC) values recorded for each drug were significantly higher for sessile cells relative to planktonic cells to the extent that ? 90% of M. pachydermatis strains in their sessile form were classified as resistant to all antifungal agents tested. Data suggest that M. pachydermatis biofilm formation is associated with antifungal resistance, paving the way towards investigating drug resistance mechanisms in Malassezia spp. PMID:23834283

Figueredo, Luciana A; Cafarchia, Claudia; Otranto, Domenico



Rechargeable Infection-responsive Antifungal Denture Materials  

Microsoft Academic Search

Candida-associated denture stomatitis (CADS) is a significant clinical concern. We developed rechargeable infection-responsive antifungal denture materials for potentially managing the disease. Polymethacrylic acid (PMAA) was covalently bound onto diurethane dimethacrylate denture resins in the curing step. The PMAA resins bound cationic antifungal drugs such as miconazole and chlorhexidine digluconate (CG) through ionic interactions. The anticandidal activities of the drug-containing PMAA-resin

Z. Cao; X. Sun; C.-K. Yeh; Y. Sun



Antifungal agents in current pediatric practice.  


Invasive fungal infections are an important cause of morbidity and mortality in immunocompromised children. Increases in the incidence of systemic mycoses have been observed during the last 2 decades. Treatment of invasive fungal infections has improved through a better knowledge and application of current treatment strategies and through the development of new antifungal compounds. The purpose of this review is to provide antifungal treatment recommendations for pediatric patients that can help clinicians find the most suitable treatment for each specific case. PMID:23616182

Valerio, Cecinati; Perillo, Teresa; Brescia, Letizia; Russo, Fabio Giovanni



The antifungal action of dandruff shampoos  

Microsoft Academic Search

The disease commonly known as “dandruff” is caused by numerous host factors in conjunction with the normal flora yeast Malassezia furfur (Pityrosporumovale). Indeed, clinical studies have shown that administration of antifungal agents correlates with an improved clinical condition.\\u000a Almost all commercially available hair shampoos publicize that they contain some form of antifungal agent(s). However, few\\u000a studies have been published in

Amelia C. Bulmer; Glenn S. Bulmer



An antifungal protein from ginger rhizomes  

Microsoft Academic Search

There are very few reports on antifungal proteins from rhizomes and there is none from the family of Zingiberaceae. An antifungal protein with a novel N-terminal sequence was isolated from ginger rhizomes utilizing a protocol that involved ion exchange chromatography on DEAE–cellulose, affinity chromatography on Affi-gel blue gel, and fast protein liquid chromatography on Superdex 75. The protein was unadsorbed

Hexiang Wang; Tzi Bun Ng



Antifungal Resistance and New Strategies to Control Fungal Infections  

PubMed Central

Despite improvement of antifungal therapies over the last 30 years, the phenomenon of antifungal resistance is still of major concern in clinical practice. In the last 10 years the molecular mechanisms underlying this phenomenon were extensively unraveled. In this paper, after a brief overview of currently available antifungals, molecular mechanisms of antifungal resistance will be detailed. It appears that major mechanisms of resistance are essential due to the deregulation of antifungal resistance effector genes. This deregulation is a consequence of point mutations occurring in transcriptional regulators of these effector genes. Resistance can also follow the emergence of point mutations directly in the genes coding antifungal targets. In addition we further describe new strategies currently undertaken to discover alternative therapy targets and antifungals. Identification of new antifungals is essentially achieved by the screening of natural or synthetic chemical compound collections. Discovery of new putative antifungal targets is performed through genome-wide approaches for a better understanding of the human pathogenic fungi biology.

Vandeputte, Patrick; Ferrari, Selene; Coste, Alix T.



Antifungal activity of limonoids from Khaya ivorensis.  


Chemical investigation of the diethyl ether extract of the stem bark of Khaya ivorensis A Chev (Meliaceae) afforded ten limonoids of angolensates, ring D-opened limonoids and mexicanolides. The structures of the limonoids isolated were determined by comparison of their (1)H and (13)C NMR data with those reported in the literature. These compounds were evaluated for their antifungal activity against the plant pathogenic fungus Botrytis cinerea Pers. Methyl 6-hydroxyangolensate and 3,7-dideacetylkhivorin were also tested for their antifungal and antibacterial activities on several fungal and bacterial species. Methyl angolensate and 1,3,7-trideacetylkhivorin displayed the highest antifungal activity against B. cinerea, with respectively 62.8 and 64.0% mycelial growth inhibition at 1000 mg litre(-1), and 73.3 and 68.6% mycelial growth inhibition at 1500 mg litre(-1). 3,7-Dideacetylkhivorin showed stronger antifungal and antibacterial activities than methyl 6-hydroxyangolensate against all of the test fungi and bacteria except Penicillium expansum Link. This is the first report on the antifungal and antibacterial effects of these limonoids. Structure-antifungal activity relationships of the limonoids isolated are discussed. PMID:15619711

Abdelgaleil, Samir A M; Hashinaga, Fumio; Nakatani, Munehiro



Antifungal activity of five species of Polygala  

PubMed Central

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 ?g/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 ?g/mL and 250 ?g/mL, respectively) and C. gattii (both with MICs of 250 ?g/mL). Rutin and aurapten isolated from P. paniculata showed antifungal activity against C. gattii with MIC values of 60 and 250 ?g/mL, respectively. In the antifungal screening, few of the isolated compounds showed good antifungal inhibition. The compound ?-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.

Johann, Susana; Mendes, Beatriz G.; Missau, Fabiana C.; de Resende, Maria A.; Pizzolatti, Moacir G.



Immunomodulating activity of antifungal drugs.  


1. The immunomodulating activity of antifungal drugs was reviewed. Although results are conflicting, all azole drugs tend to be immunosuppressive, except for fluconazole, which has no immunologic effect. In contrast, the polyene antibiotic amphotericin B (AMPH) is immunostimulatory. 2. AMPH induced host resistance to Pseudomonas aeruginosa infection in mice, whereas no azole drugs did so. 3. Polymorphonuclear leukocytes are activated by AMPH, but not by any azole drugs, in terms of the level of their adherence. 4. No azole drugs induce in vitro tumor necrosis factor alpha (TNF) production by macrophages, whereas AMPH slightly but substantially does so. 5. AMPH potently primes macrophages in vitro and in vivo so that they produce large amounts of TNF after the secondary stimulation (triggering) by bacterial lipopolysaccharides or a streptococcal preparation used for antitumor immunotherapy, OK432. 6. Viable or heat-killed Candida albicans cells are capable of inducing in vitro TNF production by macrophages. This activity of the fungal cells is enhanced by AMPH. PMID:8363252

Yamaguchi, H; Abe, S; Tokuda, Y



Hospital use of systemic antifungal drugs  

PubMed Central

Background Sales data indicate a major increase in the prescription of antifungal drugs in the last two decades. Many new agents for systemic use that only recently have become available are likely to be prescribed intensively in acute care hospitals. Sales data do not adequately describe the developments of drug use density. Given the concerns about the potential emergence of antifungal drug resistance, data on drug use density, however, may be valuable and are needed for analyses of the relationship between drug use and antifungal resistance. Methods Hospital pharmacy records for the years 2001 to 2003 were evaluated, and the number of prescribed daily doses (PDD, defined according to locally used doses) per 100 patient days were calculated to compare systemic antifungal drug use density in different medical and surgical service areas between five state university hospitals. Results The 3-year averages in recent antifungal drug use for the five hospitals ranged between 8.6 and 29.3 PDD/100 patient days in the medical services (including subspecialties and intensive care), and between 1.1 and 4.0 PDD/100 patient days in the surgical services, respectively. In all five hospitals, systemic antifungal drug use was higher in the hematology-oncology service areas (mean, 48.4, range, 24 to 101 PDD/100 patient days, data for the year 2003) than in the medical intensive care units (mean, 18.3, range, 10 to 33 PDD/100) or in the surgical intensive care units (mean, 10.7, range, 6 to 18 PDD/100). Fluconazole was the most prescribed antifungal drug in all areas. In 2003, amphotericin B consumption had declined to 3 PDD/100 in the hematology-oncology areas while voriconazole use had increased to 10 PDD/100 in 2003. Conclusion Hematology-oncology services are intense antifungal drug prescribing areas. Fluconazole and other azol antifungal drugs are the most prescribed drugs in all patient care areas while amphotericin B use has considerably decreased. The data may be useful as a benchmark for focused interventions to improve prescribing quality.

de With, Katja; Steib-Bauert, Michaela; Knoth, Holger; Dorje, Frank; Strehl, Egid; Rothe, Ulrich; Maier, Ludwig; Kern, Winfried V



21 CFR 333.210 - Antifungal active ingredients.  

Code of Federal Regulations, 2013 CFR




Synthesis and antifungal activity of coumarins and angular furanocoumarins  

Microsoft Academic Search

Angelicin, a naturally occurring furanocoumarin, that showed antifungal activity, was considered as a lead structure for a group of synthetic coumarins. Antifungal activities of the synthesized coumarins and angelicin derivatives were reported against Candida albicans, Cryptococcus neoformans, Saccharomyces cerevisiae and Aspergillus niger. Human cell line cytotoxicity of several coumarins was evaluated against KB cells. Angelicin and several potent antifungals showed

Soroush Sardari; Yoki Mori; Kiyoshi Horita; Ronald G Micetich; Sansei Nishibe; Mohsen Daneshtalab



Antifungal therapy in children: an update.  


Invasive fungal infections are a common problem in children affected by primary or secondary immunodeficiencies. Thanks to an increased knowledge about their mechanisms of action and their pharmacokinetic and toxicity profiles, the use of these drugs in common and uncommon invasive infections in immunocompromised children has improved over the last decades. Choosing the most appropriate antifungal drug is a serious challenge for any clinician, also considering that, in most cases, therapy has to be started before cultures are available, the choice being driven by clinical symptoms and statistical criteria only. In this study, we performed a systematic review of literature, providing antifungal treatment recommendations for paediatric patients which can help clinicians find the most suitable treatment for each specific case. Principal antifungal drugs-ranging from first-generation antimycotics to the latest molecules-are classified according to their targets, and of each group, the pharmacokinetic profile, clinical indications and side effects are extensively described. PMID:22652706

Cecinati, Valerio; Guastadisegni, Chiara; Russo, Fabio Giovanni; Brescia, Letizia Pomponia



Rechargeable Infection-responsive Antifungal Denture Materials  

PubMed Central

Candida-associated denture stomatitis (CADS) is a significant clinical concern. We developed rechargeable infection-responsive antifungal denture materials for potentially managing the disease. Polymethacrylic acid (PMAA) was covalently bound onto diurethane dimethacrylate denture resins in the curing step. The PMAA resins bound cationic antifungal drugs such as miconazole and chlorhexidine digluconate (CG) through ionic interactions. The anticandidal activities of the drug-containing PMAA-resin discs were sustained for a prolonged period of time (weeks and months). Drug release was much faster at acidic conditions (pH 5) than at pH 7. Drugs bound to the denture materials could be “washed out” by treatment with EDTA, and the drug-depleted resins could be recharged with the same or a different class of anticandidal drugs. These results suggest clinical potential of the newly developed antifungal denture materials in the management of CADS and other infectious conditions.

Cao, Z.; Sun, X.; Yeh, C.-K.; Sun, Y.



Antifungal and antibacterial activities of diarylamidine derivatives.  

PubMed Central

The antifungal and antibacterial properties of a series of 70 diarylamidine derivatives were evaluated. Several of these compounds exhibited considerable antimicrobial potency. A survey of the structure-activity relationship demonstrated that minor structural variations resulted in significant changes of antimicrobial activity. In general, the structural features required for antifungal activity coincided with those required for antibacterial activity. Both the antifungal and the antibacterial properties of the diarylamidines depended on the presence and the positions, of both amidino groups, on the nature of the central bridge connecting the two aryl moieties, and on the nature of these aryl residues (preferably indole). The most active compound was evaluated for its activity against Candida albicans infection in mice.

Anne, J; De Clercq, E; Eyssen, H; Dann, O



Imidazoles as potential antifungal agents: a review.  


Imidazoles are one of the most promising and vigorously pursued areas of contemporary antifungal chemotherapy depicting broad spectrum and potent activity. They have relatively simple molecular nucleus, which is amenable to many structural modifications. These agents have several favorable properties such as excellent bioavailability, good tissue penetrability and permeability and a relatively low incidence of adverse and toxic effects. They have been found effective in the treatment of various infectious diseases. This paper is an attempt to review the therapeutic potential of imidazoles as antifungal with an updated account on their development. PMID:23815583

Rani, Nidhi; Sharma, Ajay; Gupta, Girish Kumar; Singh, Randhir



Resveratrol lacks antifungal activity against Candida albicans.  


The putative candicidal activity of resveratrol is currently a matter of controversy. Here, the antifungal activity as well as the antioxidant response of resveratrol against Candida albicans, have been tested in a set of strains with a well-established genetic background At the doses usually employed in antifungal tests (10-40 ?g/ml), resveratrol has no effect on the exponential growth of the C. albicans CAI.4 strain, a tenfold increase (400 ?g/ml) was required in order to record a certain degree of cell killing, which was negligible in comparison with the strong antifungal effect caused by the addition of amphotericin B (5 ?g/ml). An identical pattern was recorded in the prototrophic strains of C. albicans SC5314 and RM-100, whereas the oxidative sensitive trehalose-deficient mutant (tps1/tps1 strain) was totally refractory to the presence of resveratrol. In turn, the serum-induced yeast-to-hypha transition remained unaffected upon addition of different concentrations of resveratrol. Determination of endogenous trehalose and catalase activity, two antioxidant markers in C. albicans; revealed no significant changes in their basal contents induced by resveratrol. Collectively, our results seem to dismiss a main antifungal role as well as the therapeutic application of resveratrol against the infections caused by C. albicans. PMID:22806119

Collado-González, Mar; Guirao-Abad, José P; Sánchez-Fresneda, Ruth; Belchí-Navarro, Sarai; Argüelles, Juan-Carlos



Antifungal properties of chitinolytic dune soil bacteria  

Microsoft Academic Search

Anti-fungal properties of chitinolytic soil bacteria may enable them to compete successfully for chitin with fungi. Additionally, the production of chitinase may be part of a lytic system that enables the bacteria to use living hyphae rather than chitin as the actual growth substrate, since chitin is an important constituent of most fungal cell walls. Lysis of living fungal hyphae

Wietse De Boer; Paulien J. A. Klein Gunnewiek; Petra Lafeber; Jaap D. Janse; Bendien E. Spit; Jan W. Woldendorp



Antifungal activity of Cynara scolymus L. extracts  

Microsoft Academic Search

Chloroform, ethanol and ethyl acetate extracts of Cynara scolymus L. leaves, heads and stems were tested for their antifungal activity using the agar-well diffusion assay technique. The leaves extracts and the ethanol fractions were found to be the most effective extract against all the tested organisms.

X. F. Zhu; H. X. Zhang; R. Lo



Efflux-Mediated Antifungal Drug Resistance†  

PubMed Central

Summary: Fungi cause serious infections in the immunocompromised and debilitated, and the incidence of invasive mycoses has increased significantly over the last 3 decades. Slow diagnosis and the relatively few classes of antifungal drugs result in high attributable mortality for systemic fungal infections. Azole antifungals are commonly used for fungal infections, but azole resistance can be a problem for some patient groups. High-level, clinically significant azole resistance usually involves overexpression of plasma membrane efflux pumps belonging to the ATP-binding cassette (ABC) or the major facilitator superfamily class of transporters. The heterologous expression of efflux pumps in model systems, such Saccharomyces cerevisiae, has enabled the functional analysis of efflux pumps from a variety of fungi. Phylogenetic analysis of the ABC pleiotropic drug resistance family has provided a new view of the evolution of this important class of efflux pumps. There are several ways in which the clinical significance of efflux-mediated antifungal drug resistance can be mitigated. Alternative antifungal drugs, such as the echinocandins, that are not efflux pump substrates provide one option. Potential therapeutic approaches that could overcome azole resistance include targeting efflux pump transcriptional regulators and fungal stress response pathways, blockade of energy supply, and direct inhibition of efflux pumps.

Cannon, Richard D.; Lamping, Erwin; Holmes, Ann R.; Niimi, Kyoko; Baret, Philippe V.; Keniya, Mikhail V.; Tanabe, Koichi; Niimi, Masakazu; Goffeau, Andre; Monk, Brian C.



Mutation Spectrum Induced by Conazole Fungicides in LacI Transgenic C57BL/6 Mouse Liver.  

EPA Science Inventory

Conazoles are antifungal agents used in both agricultural and pharmaceutical settings. Some conazoles, including propiconazole and triadimefon, induce hepatocellular tumors in mice, while other conazoles do not. We reported in a previous study that both propiconazole and triadime...


[Antifungal therapy update: new drugs and medical uses].  


Increases in the rates of fungal infections, as well as their associated morbidity and mortality has led to a need for additional antifungal agents. The most common serious fungal agents in immunosuppressed and critically ill patients are Candida spp. and Aspergillus spp., although other emerging fungi must be considered. Rational, early systemic antifungal treatment should be based on diagnostic imaging techniques and conventional mycological and non-culture-based procedures. While the availability of new therapeutic options is an important advance, antifungal therapy has become increasingly complex. In addition to the available antifungal armamentarium, recent research has resulted in the introduction of three new antifungal agents: micafungin, anidulafungin, and posaconazole. This article provides an update, based on the latest scientific evidence, of the clinical efficacy, pharmacokinetics, safety and dosing of antifungal drugs administered in the management of Candida spp., Aspergillus spp., Cryptococcus spp., Zygomycetes, Scedosporium spp. and Fusarium spp. PMID:22305668

Fortún, Jesús



Antifungal activity of thiophenes from Echinops ritro.  


Extracts from 30 plants of the Greek flora were evaluated for their antifungal activity using direct bioautography assays with three Colletotrichum species. Among the bioactive extracts, the dichloromethane extract of the radix of Echinops ritro (Asteraceae) was the most potent. Bioassay-guided fractionation of this extract led to the isolation of eight thiophenes. Antifungal activities of isolated compounds together with a previously isolated thiophene from Echinops transiliensis were first evaluated by bioautography and subsequently evaluated in greater detail using a broth microdilution assay against plant pathogens Colletotrichum acutatum, Colletotrichum fragariae, Colletotrichum gloeosporioides, Botrytis cinerea, Fusarium oxysporum, Phomopsis viticola, and Phomopsis obscurans. 5'-(3-Buten-1-ynyl)-2,2'-bithiophen (1), alpha-terthienyl (2), and 2-[pent-1,3-diynyl]-5-[4-hydroxybut-1-ynyl]thiophene (5) at 3 and 30 microM were active against all three Colletotrichum species, F. oxysporum, P. viticola, and P. obscurans. PMID:16506815

Fokialakis, Nikolas; Cantrell, Charles L; Duke, Stephen O; Skaltsounis, Alexios L; Wedge, David E



Antifungal Activity of 10 Guadeloupean Plants.  


Screening of the antifungal activities of ten Guadeloupean plants was undertaken to find new extracts and formulations against superficial mycoses such as onychomycosis, athlete's foot, Pityriasis versicolor, as well as the deep fungal infection Pneumocystis pneumonia. For the first time, the CMI of these plant extracts [cyclohexane, ethanol and ethanol/water (1:1, v/v)] was determined against five dermatophytes, five Candida species, Scytalidium dimidiatum, a Malassezia sp. strain and Pneumocystis carinii. Cytotoxicity tests of the most active extracts were also performed on an HaCat keratinocyte cell line. Results suggest that the extracts of Bursera simaruba, Cedrela odorata, Enterolobium cyclocarpum and Pluchea carolinensis have interesting activities and could be good candidates for developing antifungal formulations. Copyright © 2012 John Wiley & Sons, Ltd. PMID:23280633

Biabiany, Murielle; Roumy, Vincent; Hennebelle, Thierry; François, Nadine; Sendid, Boualem; Pottier, Muriel; Aliouat, El Moukhtar; Rouaud, Isabelle; Lohézic-Le Dévéhat, Françoise; Joseph, Henry; Bourgeois, Paul; Sahpaz, Sevser; Bailleul, François



Natural Killer Cells and Antifungal Host Response  

PubMed Central

As a result of improved experimental methodologies and a better understanding of the immune system, there is increasing insight into the antifungal activity of natural killer (NK) cells. Murine and human NK cells are able to damage fungi of different genera and species in vitro, and they exert both direct and indirect antifungal activity through cytotoxic molecules such as perforin and through cytokines and interferons, respectively. On the other hand, recent data suggest that fungi exhibit immunosuppressive effects on NK cells. Whereas clear in vivo data are lacking in humans, the importance of NK cells in the host response against fungi has been demonstrated in animal models. Further knowledge of the interaction of NK cells with fungi might help to better understand the pathogenesis of invasive fungal infections and to improve treatment strategies.

Schmidt, Stanislaw; Zimmermann, Stefanie-Yvonne; Tramsen, Lars; Koehl, Ulrike



From memory to antifungal vaccine design.  


Fungal infections and related diseases have a high morbidity and mortality rate. Human antifungal vaccines are therefore of great interest, however, their development is challenging. Major hurdles include fungal species-specific differences in pathogenic mechanisms and strategies to escape immune surveillance, as well as the fact that individuals susceptible to infection do not necessarily share the same risk factors. Progress in antifungal vaccines demands the integration of immunology with systems biology, immunogenetics and bioinformatics in the arena of both fungal and host biology. Bridging the fields of basic immunology and vaccine research is needed to create individualized host immune profiles that will direct the rational development of customized adjuvants and vaccines with a predicted efficacy in each target population. PMID:22647597

Iannitti, Rossana G; Carvalho, Agostinho; Romani, Luigina



[Choice and use of antifungal drugs].  


During the last decade the incidence of deep mycotic infections has continued to increase dramatically. This new epidemiological feature is mostly due to the expanding population of at risk subjects submitted to intensive and protracted immunosupression. Amphotericin B has a broad spectrum and has remained the drug of choice for these life threatening invasive fungal infections. However adverse events, particularly renal insufficiency, are limiting factors in achieving an effective dose. Since the 1990s the number of oral and parenteral antifungal agents has significantly increased. The use of phospholipid carriers for amphotericin B or cyclodextrine for triazoles improved safety profil and/or pharmacokinetics. New families of drugs with a new target in the fungal cell are under clinical investigation and should be soon available. Comparative studies, consensus on diagnosis criteria and practice guidelines for the treatment of fungal infections will contribute to a better management of the patients and optimize the use of antifungal agents. PMID:11387672

Dupont, B



Rechargeable Antibacterial and Antifungal Polymeric Silver Sulfadiazines  

Microsoft Academic Search

Poly(methyl methacrylate) (PMMA)-based rechargeable antibacterial and antifungal polymeric silver sulfadiazines were prepared by copolymerizing acryloyl sulfadiazine with methyl methacrylate and sequentially treating the copolymers with dilute silver nitrate aqueous solutions. The chemical structures of the samples were characterized by FT-IR, 1H-NMR, XPS, and TGA analyses. On contact, the PMMA-based polymeric silver sulfadiazines provided 100% inactivation of 108—109 CFU\\/mL of Escherichia

Zhengbing Cao; Xinbo Sun; Yuyu Sun; Hao Fong



Xanthone and antifungal constituents from Monnina obtusifolia.  


Three biphenyls and four xanthones have been isolated from the aerial parts of Monnina obtusifolia. The structures were established on the basis of their spectral data and that of some derivatives. The biphenyls have been isolated previously from the same genus. 1,3,6-Trihydroxy-2,5-dimethoxyxanthone is a new natural product, whereas the other xanthones have been described in other species. The antifungal activity of the isolated compounds has been determined. PMID:7765695

Pinto, D C; Fuzzati, N; Pazmino, X C; Hostettmann, K



Chemical modification of antifungal polyene macrolide antibiotics  

Microsoft Academic Search

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

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



An antifungal peptide from baby lima bean  

Microsoft Academic Search

A 6-kDa antifungal peptide with inhibitory activity on mycelial growth in Fusarium oxysporum, Mycosphaerella arachidicola, and Physalospora piricola was isolated from baby lima beans. The peptide suppressed growth in M. arachidicola with an IC50 of 0.87 ?M and inhibited activity of HIV-1 reverse transcriptase with an IC50 of 4 ?M. The peptide exhibited an N-terminal amino acid sequence similar to those of

H. X. Wang; T. B. Ng



Antifungal activity of lauric acid derivatives against Aspergillus niger  

Microsoft Academic Search

The antifungal effects of lauric acid and four lauric acid derivatives (monolauroylglycerol, D-laurate A, T-laurate A, 6-O-lauroysucrose) were tested on the spore germination and the growth rate of Aspergillus niger DMF 0801. The results showed that the tested substances varied in their antifungal activity and they also confirmed the relation of the structure of tested substances and their antifungal effects.

Zde?ka ?iháková; Milada Plocková; Vladimír Filip; Jan Šmidrkal



Antifungal activity of some coleus species growing in nilgiris.  


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. PMID:22557230

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




PubMed Central

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 against the selected organisms.

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



In vitro antifungal activity of posaconazole against various pathogenic fungi  

Microsoft Academic Search

The antifungal activity of posaconazole (SCH56592), a new triazole antifungal, against stock cultures and fresh clinical isolates of a wide range of pathogenic fungi was compared with that of itraconazole, fluconazole and amphotericin B. Posaconazole inhibited growth of all the fungal species tested except Fusarium spp. at 1 mg\\/l or lower concentrations, showing a broad-spectrum antifungal activity. The activities of

Katsuhisa Uchida; Nobuko Yokota; Hideyo Yamaguchi



Ergosterol biosynthesis in Aspergillus fumigatus: its relevance as an antifungal target and role in antifungal drug resistance  

PubMed Central

Ergosterol, the major sterol of fungal membranes, is essential for developmental growth and the main target of antifungals that are currently used to treat fatal fungal infections. Emergence of resistance to existing antifungals is a current problem and several secondary resistance mechanisms have been described in Aspergillus fumigatus clinical isolates. A full understanding of ergosterol biosynthetic control therefore appears to be essential for improvement of antifungal efficacy and to prevent antifungal resistance. An ergosterol biosynthesis pathway in A. fumigatus has been proposed with 14 sterol intermediates resulting in ergosterol and another secondary final compound C-24 ethyl sterol. Transcriptomic analysis of the A. fumigatus response to host-imposed stresses or antifungal agents is expanding our understanding of both sterol biosynthesis and the modes of action of antifungal drugs. Ultimately, the identification of new targets for novel drug design, or the study of combinatorial effects of targeting sterol biosynthesis together with other metabolic pathways, is warranted.

Alcazar-Fuoli, Laura; Mellado, Emilia



Antifungal activity of rhodium, iridium, and ruthenium tripodal phosphine complexes.  


Twenty-eight rhodium, iridium or ruthenium complexes were evaluated for their in vitro antifungal activities against Candida albicans and Candida tropicalis. Fourteen compounds showed an antifungal activity against C. albicans and C. tropicalis with a range of the minimum inhibitor concentrations (MICs) between 16 and 250 micrograms/mL. PMID:10946408

Sülü, M; Küçükbay, H; Durmaz, R; Günal, S



Antifungal activity of extracellular metabolites produced by Sporothrix flocculosa  

Microsoft Academic Search

The antifungal properties of extracellular compounds produced by the epiphytic fungus Sporothrix flocculosa were bioassayed against phytopathogenie fungi on the basis of inhibition of spore germination, and mycelial growth and induction of cellular leakage. Following incubation in stationary culture, S. flocculosa released antifungal metabolites into the culture medium which were extractable with méthylene chloride. When separated by thin layer chromatography,

M. R. Hajlaou; J. A. Traquair; W. R. Jarvis; R. R. Belanger




Microsoft Academic Search

The development of lipid formulations of antifungal drugs has been a remarkable progress in the systemic antifungal arena. The lipid-based amphotericin B formulations; amphotericin B lipid complex (ABLC), amphotericin B colloidal dispersion (ABCD), and liposomal amphotericin B (L- AMB) have been in clinical use since the 1990s. They are significantly less nephrotoxic than the parent compound and can be safely



Antifungal Activity of Endemic Salvia tigrina in Turkey  

Microsoft Academic Search

Purpose: The ethanol extracts obtained from the leaves, rootstock and the combined formulation of endemic Salvia tigrina Hedge & Hub.-Mor. (Labiatea) have been investigated for their antifungal activities. Method: The antifungal activity of the extract was tested against Candida species (C. albicans ATCC 10231, C. tropicalis ATCC 13803 and C. guilliermondii ATCC 6260 and Cryptococcus species (C. neoformans ATCC 90112

B Dulger; N Hacioglu


A New Antifungal Macrolide, Eushearilide, Isolated from Eupenicillium shearii  

Microsoft Academic Search

In screening for antifungal substances, a new macrolide, eushearilide (1), was isolated from Eupenicillium shearii IFM54447. The structure of 1 was established to be 24-membered macrolide having a non-conjugated diene and a choline phosphate ester moetiy on the basis of detailed investigation of NMR, UV, IR and MS spectral data. Compound 1 showed antifungal activity against various fungi and yeasts,

Tomoo Hosoe; Kazutaka Fukushima; Kayoko Takizawa; Takeshi Itabashi; Nobuo Kawahara; Valerio Vidotto; Ken-ichi Kawai



Antifungal effect of essential oils on southern yellow pine  

Microsoft Academic Search

Moisture management remains the most critical factor for controlling mold growth on wood and wood products during storage, construction, and while in service. When moisture management practices fail to adequately control moisture, plant extracts demonstrating antifungal properties may provide protection for these applications. The objective of this study was to evaluate the antifungal properties of natural plant extracts, such as

Vina W. Yang; Carol A. Clausen



Antifungal activity of a human antiglucuronoxylomannan antibody.  


The human immunoglobulin M (IgM) monoclonal antibody (MAb) 2E9 binds the glucuronoxylomannan (GXM) of Cryptococcus neoformans serotypes A, B, and D. This study was undertaken to determine the opsonic efficacy of 2E9 and its ability to promote the antifungal activity of human polymorphonuclear neutrophils (PMNs) against C. neoformans. We incubated purified PMNs with fluorescein isothiocyanate-labeled C. neoformans cells that were treated with the GXM IgM 2E9, IgM antibodies that do not bind GXM, and rabbit and human factor-B-deficient serum as complement sources. PMN-associated C. neoformans cells fluoresced and were detected with a fluorescence-activated cell sorter. The amount of phagocytosis was defined as the percent fluorescing PMNs, which was 37% for yeast cells opsonized with 2E9 plus rabbit serum and 57% for yeast cells opsonized with 2E9 plus factor-B-deficient serum. Phagocytosis was significantly greater for yeast cells that were treated with 2E9 plus a complement source than for yeast cells treated with the complement sources alone or treated with the control IgMs alone or with the complement sources. Fluorescence quenching and light and electron microscopy of the phagocytosis mixtures revealed that 2E9-opsonized yeast cells were internalized by PMNs. Maximal inhibition of C. neoformans growth occurred when PMNs were cocultured with yeast cells that were opsonized with 2E9 plus a complement source. Our data demonstrate that the human GXM IgM 2E9 can mediate PMN phagocytosis and C. neoformans growth inhibition in vitro. These findings strongly suggest that antibody-mediated deposition of complement components on the cryptococcal capsule can augment PMN complement receptor-mediated antifungal activity. Antibody activation of complement-mediated effector cell antifungal mechanisms may play a role in host defense against cryptococcosis and represents a goal for the use of MAbs to treat or prevent human C. neoformans infections. PMID:9455881

Zhong, Z; Pirofski, L A



Advances in synthetic approach to and antifungal activity of triazoles  

PubMed Central

Summary 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.

Kumar, Nitin; Drabu, Sushma; Sharma, Pramod Kumar



The antifungal activity of graphene oxide-silver nanocomposites.  


Graphene oxide (GO)-based nanocomposites' antibacteria activity exhibits great potential in clinical application. Herein we reported for the first time the preparation and enhanced antifungal activity of carbon nanoscrolls (CNSs) filled with silver nanoparticles (AgNPs). The nanoscrolls filled with silver nanoparticles were prepared by sonication, TEM picture showed AgNPs filled and wrapped inside prepared nanocomposites, the antifungal test showed that CNSs-AgNPs exhibited ideal lengthened activities against Candida albicans and Candida tropical compared with the GO-AgNPs nanocomposites based on silver nanoparticles directly deposited on the surface of grapheme oxides, which is caused by CNS-AgNPs' controlled durative slow-releasing of silver ion. It is also observed that graphene oxides exhibited no antifungal activity. In conclusion, the carbon nanoscrolls composed of graphene oxides and silver nanoparticles own enhanced and lengthened antifungal activity, and have great potential in applications such as clinical nosocomial infections and local antifungal therapy. PMID:23465487

Li, Chao; Wang, Xiansong; Chen, Feng; Zhang, Chunlei; Zhi, Xiao; Wang, Kan; Cui, Daxiang



Antifungal amide from leaves of Piper hispidum.  


Bioactivity-guided fractionation of a CH2Cl2 extract from leaves of Piper hispidum (Piperaceae) yielded a new pyrrolidine amide, N-[7-(3',4'-methylenedioxyphenyl)-2(Z),4(Z)-heptadienoyl] pyrrolidine 1, in addition to two known amides N-[5-(3', 4'-methylenedioxyphenyl)-2(E)-pentadienoyl] pyrrolidine and N-[2-(3', 4'-methylenedioxy-6'-methoxyphenyl)-2(Z)-propenoyl]pyrrolidine. The structure of compound 1 was elucidated by interpretation of spectral data, including ES-MS. Compound 1 showed antifungal activity against Cladosporium sphaerospermum. PMID:9599264

Alécio, A C; da Silva Bolzani, V; Young, M C; Kato, M J; Furlan, M



Antifungal activity of the systemic fungicide imazalil  

Microsoft Academic Search

The antifungal activity of imazalil against spores of Penicillium italicum and several other fungi was found to be pH-dependent.\\u000a The fungicide was much less effective at pH 5.2 than at pH 7.0. However, related members of the imidazole class of fungicides\\u000a (miconazole and clotrimazole) did not show this pH dependency. Fungitoxicity of imazalil and miconazole at different pH’s\\u000a was correlated

M. R. Siegel; A. Kerkenaar; A. Kaars Sijpesteijn



Echinocandins: A promising new antifungal group Echinocandins: A promising new antifungal group Echinocandins: A promising new antifungal group Echinocandins: A promising new antifungal group Echinocandins: A promising new antifungal group  

Microsoft Academic Search

Echinocandins are a new option for fungal infections. They are fungicidal and less toxic to the host by virtue of their novel mechanism of action. They are ?-1, 3-glucan synthase inhibitors. FDA, USA has approved caspofungin for treatment of invasive aspergillosis in patients who fail to respond or are unable to tolerate other antifungals. Two other agents are in phase

G. K. Randhawa; G. Sharma



Colorimetric broth microdilution method for the antifungal screening of plant extracts against yeasts  

Microsoft Academic Search

Screening plant extracts for antifungal activity is increasing due to demand for new antifungal agents, but the testing methods present many challenges. Standard broth microdilution methods for antifungal susceptibility testing of available antifungal agents are available now, but these methods are optimised for single compounds instead of crude plant extracts. In this study we evaluated the standard NCCLS method as

Manjuan Liu; Veronique Seidel; David R. Katerere; Alexander I. Gray



Novel antifungal peptides from Ceylon spinach seeds.  


Two novel antifungal peptides, designated alpha- and beta-basrubrins, respectively, were isolated from seeds of the Ceylon spinach Basella rubra. The purification procedure involved saline extraction, (NH(4))(2)SO(4) precipitation, ion exchange chromatography on DEAE-cellulose, affinity chromatography on Affi-gel blue gel, ion exchange chromatography on CM-cellulose and FPLC-gel filtration on Superdex peptide column. alpha- and beta-basrubrins exhibited a molecular weight of 4.3 and 5 kDa, respectively. They inhibited translation in a rabbit reticulocyte system with an IC(50) value of 400 and 100 nM, respectively. alpha- and beta-basrubrin inhibited HIV-1 reverse transcriptase by (79.4 +/- 7.8)% and (54.6 +/- 3.6)%, respectively, at a concentration of 400 microM, and (10.56 +/- 0.92)% and (2.12 +/- 0.81)%, respectively, at a concentration of 40 microM. Both alpha- and beta-basrubrins exerted potent antifungal activity toward Botrytis cinerea, Mycosphaerella arachidicola, and Fusarium oxysporum. PMID:11688973

Wang, H; Ng, T B



Potentiation of azole antifungals by 2-adamantanamine.  


Azoles are among the most successful classes of antifungals. They act by inhibiting ?-14 lanosterol demethylase in the ergosterol biosynthesis pathway. Oropharyngeal candidiasis (OPC) occurs in about 90% of HIV-infected individuals, and 4 to 5% are refractory to current therapies, including azoles, due to the formation of resistant biofilms produced in the course of OPC. We reasoned that compounds affecting a different target may potentiate azoles to produce increased killing and an antibiofilm therapeutic. 2-Adamantanamine (AC17) was identified in a screen for compounds potentiating the action of miconazole against biofilms of Candida albicans. AC17, a close structural analog to the antiviral amantadine, did not affect the viability of C. albicans but caused the normally fungistatic azoles to become fungicidal. Transcriptome analysis of cells treated with AC17 revealed that the ergosterol and filamentation pathways were affected. Indeed, cells exposed to AC17 had decreased ergosterol contents and were unable to invade agar. In vivo, the combination of AC17 and fluconazole produced a significant reduction in fungal tissue burden in a guinea pig model of cutaneous candidiasis, while each treatment alone did not have a significant effect. The combination of fluconazole and AC17 also showed improved efficacy (P value of 0.018) compared to fluconazole alone when fungal lesions were evaluated. AC17 is a promising lead in the search for more effective antifungal therapeutics. PMID:23689724

Lafleur, Michael D; Sun, Lingmei; Lister, Ida; Keating, John; Nantel, Andre; Long, Lisa; Ghannoum, Mahmoud; North, Jeffrey; Lee, Richard E; Coleman, Ken; Dahl, Thomas; Lewis, Kim



Identification of antifungal compounds produced by Lactobacillus casei AST18.  


Lactobacillus casei AST18 was screened as an antifungal lactic acid bacteria which we have reported before. In this research, the antifungal properties of cell-free culture filtrate (CCF) from L. casei AST18 were detected, and the antifungal compounds of CCF were prepared by ultrafiltration, and semi-preparative HPLC, and then determined by GC-MS. CCF was sensitive to pH and heat treatment but it was not affected by the treatment of trypsin and pepsin. Through the treatment of ultrafiltration and semi-preparative HPLC there were two parts of CCF which showed antifungal activities: part 1 and part 4. Lactic acid was identified as the main antifungal compound in part 1. In part 4, three small molecular substances were detected with GC-MS. The three potential antifungal substances were cyclo-(Leu-Pro), 2,6-diphenyl-piperidine, and 5,10-diethoxy-2,3,7,8-tetrahydro-1H,6H-dipyrrolo[1,2-a;1',2'-d]pyrazine. The antifungal activity of L. casei AST18 was a synergistic effect of lactic acid and cyclopeptides. PMID:22580887

Li, Hongjuan; Liu, Lu; Zhang, Shuwen; Cui, Wenming; Lv, Jiaping



Antifungal Activity of Antifungal Drugs, as Well as Drug Combinations Against Exophiala dermatitidis  

Microsoft Academic Search

To evaluate the in vitro efficacy of common antifungal drugs, as well as the interactions of caspofungin with voriconazole,\\u000a 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,\\u000a and caspofungin against 16 strains of E. dermatitidis were determined by using CLSI broth microdilution method (M38-A2).

Yi Sun; Wei Liu; Zhe Wan; Xiaohong Wang; Ruoyu Li



Has the era of individualised medicine arrived for antifungals? A review of antifungal pharmacogenomics.  


Treatment or prophylaxis of invasive fungal infection in recipients of haemopoietic SCT (HSCT) may require management of coexistent malnutrition, organ dysfunction and GVHD, all of which create added potential for inter- and intra-patient variations in drug metabolism as well as drug interactions. Polymorphism is common in genes encoding pathway components of antifungal drug metabolism such as enzymes (cytochrome P450 (CYP450), glutathione S-transferase, N-acetyltransferase and uridine 5'-diphospho-glucuronosyltransferase), uptake transporters (organic cationic transporter, novel organic cationic transporter, organic anion transporter protein (OATP), organic anion transport (OAT), and peptide tranporter) and efflux transporters (breast cancer resistance protein, bile sale export pump (BSEP), multidrug and toxin extrusion type transporter, multidrug resistance protein (MRP), OAT, permeability glycoprotein (P-gp), and urate transporter). Specific polymorphisms may be generalised throughout a population or largely confined to ethnic groups. CYP450 enzymes, especially 2C9 and 2C19, exhibit extensive polymorphism and are central to the metabolism of azole antifungals and their interactions with other drugs including calcineurin inhibitors, cytotoxics and benzodiazepines. Polymorphism may ultimately affect drug efficacy: CYP2C19 variation leads to a fivefold variation in voriconazole levels between individuals. Anticipated routine provision of pharmacogenomic data in the future for new drugs, together with accumulating knowledge about established agents, challenge physicians to assimilate and apply that information to drug prescribing. Increasing availability of pharmacogenomic data may strengthen demand for rapid turn-around therapeutic drug monitoring of antifungal agents in HSCT recipients. PMID:21785468

Ashbee, H R; Gilleece, M H



Candicidin and other polyenic antifungal antibiotics  

PubMed Central

About 50 polyenic antifungal antibiotics produced by actinomycetes have been isolated and described. Among these are the most effective antimonilial agents so far known. These polyenes can be classified into four broad groups depending on the number of conjugated carbon-to-carbon double bonds that are present in their chromophores. Only some of the tetraenes (four conjugated double bonds), such as nystatin and pimaricin, and a few heptaenes (seven conjugated double bonds), such as amphotericin B, Trichomycin candicidin and hamycin, have found practical application in the treatment of infectious diseases caused by fungi. Nystatin and pimaricin show the least in vitro activity against fungi, while trichomycin and candicidin are the most active. Recent clinical investigations carried out in the USA have shown that candicidin is very effective in the treatment of vaginal monilial infections.

Waksman, Selman A.; Lechevalier, Hubert A.; Schaffner, Carl P.



Update in antifungal therapy of dermatophytosis.  


Treatment of dermatophyte infection involves primarily oral and/or topical formulations of azoles or allylamines, particularly itraconazole and terbinafine. Topical medications applied once or twice daily are the primary treatment indicated for tinea corporis/cruris, and tinea pedis/manuum. Use of oral antifungals may be practical where the tinea involvement is extensive or chronic, or where application of a topical is not feasible. For tinea unguium (onychomycosis) and tinea capitis, oral therapies are the primary treatments provided. Recently, topical amorolfine and ciclopirox formulations have been approved for use in milder onychomycosis cases, and their role in the treatment of the different clinical forms of onychomycosis is currently being defined. Relapse of infection remains a problem, particularly with tinea pedis/unguium. Appropriate follow-up duration and education of patients on proper foot hygiene are also important components in providing effective therapy. PMID:18478357

Gupta, Aditya K; Cooper, Elizabeth A



Ophiocordin, an antifungal antibiotic of Cordyceps ophioglossoides.  


An unknown antibiotic, ophiocordin, C21H22N2O8, MW: 430, was isolated from submerged cultures of Cordyceps ophioglossoides, strain TU 276, grown in a glycerol soybean meal medium at 27 degrees C. The antibiotic was extracted from acidified culture fluids with n-butanol and purified by subsequent column chromatography on DEAE-Sephadex and cellulose. Studies including nuclear magnetic resonance and mass spectrometry resulted in proposals of partial structures of the molecule. Inhibition by ophiocordin could be demonstrated for a small number of fungi belonging to different taxonomic groups. Bacteria were not inhibited. The antifungal effect was antagonized by ammonia and nitrate ions and by certain amino acids. PMID:560831

Kneifel, H; König, W A; Loeffler, W; Müller, R



An antifungal peptide from baby lima bean.  


A 6-kDa antifungal peptide with inhibitory activity on mycelial growth in Fusarium oxysporum, Mycosphaerella arachidicola, and Physalospora piricola was isolated from baby lima beans. The peptide suppressed growth in M. arachidicola with an IC(50) of 0.87 muM and inhibited activity of HIV-1 reverse transcriptase with an IC(50) of 4 muM. The peptide exhibited an N-terminal amino acid sequence similar to those of leguminous defensins. The isolation procedure comprised ion exchange chromatography on diethylaminoethyl (DEAE)-cellulose, affinity chromatography on Affi-gel blue gel, ion exchange chromatography on carboxymethyl (CM)-cellulose, and gel filtration by fast protein liquid chromatography on Superdex 75. The peptide was unadsorbed on DEAE-cellulose and Affi-gel blue gel but was adsorbed on CM-cellulose. PMID:16850300

Wang, H X; Ng, T B



21 CFR 333.250 - Labeling of antifungal drug products.  

Code of Federal Regulations, 2013 CFR




Synthesis and Antifungal Activity of Musa Phytoalexins and Structural Analogs  

Microsoft Academic Search

Several perinaphthenone\\/phenylphenalenone compounds were synthesized to e s- tablish a relationship between structure and antifungal activity against Mycosphaerella fijien- sis. Substitutions on the unsaturated carbonyl system or addition of a phenyl group reduced antibiotic activity.

Winston Quiñones; Gustavo Escobar; Fernando Echeverri; Fernando Torres; Yoni Rosero; Victor Arango; Gloria Cardona; Adriana Gallego



Antifungal effect of essential oils on southern yellow pine  


The objective of this study was to evaluate the antifungal properties of natural ... of Aspergillus niger, Trichoderma viride, and Penicillium chrysogenum on ... pine (SYP) stakes that were either dip treated or exposed to vapors of the test oils.


Antifungal activity of anthraquinone derivatives from Rheum emodi  

Microsoft Academic Search

Rhein, physcion, aloe-emodin and chrysophanol isolated from Rheum emodi rhizomes exhibited antifungal activity against Candida albicans, Cryptococcus neoformans, Trichophyton mentagrophytes and Aspergillus fumigatus (MIC 25–250 ?g\\/ml).

S. K Agarwal; Sudhir S Singh; Sushma Verma; Sushil Kumar



Research to Identify Effective Antifungal Agents, 1991 Annual Report.  

SciTech Connect

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

Schreck, Carl



Research to Identify Effective Antifungal Agents, 1993 Annual Report.  

SciTech Connect

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

Schreck, Carl



Chemosensitization as a means to augment commercial antifungal agents.  


Antimycotic chemosensitization and its mode of action are of growing interest. Currently, use of antifungal agents in agriculture and medicine has a number of obstacles. Foremost of these is development of resistance or cross-resistance to one or more antifungal agents. The generally high expense and negative impact, or side effects, associated with antifungal agents are two further issues of concern. Collectively, these problems are exacerbated by efforts to control resistant strains, which can evolve into a treadmill of higher dosages for longer periods. This cycle in turn, inflates cost of treatment, dramatically. A further problem is stagnation in development of new and effective antifungal agents, especially for treatment of human mycoses. Efforts to overcome some of these issues have involved using combinations of available antimycotics (e.g., combination therapy for invasive mycoses). However, this approach has had inconsistent success and is often associated with a marked increase in negative side effects. Chemosensitization by natural compounds to increase effectiveness of commercial antimycotics is a somewhat new approach to dealing with the aforementioned problems. The potential for safe natural products to improve antifungal activity has been observed for over three decades. Chemosensitizing agents possess antifungal activity, but at insufficient levels to serve as antimycotics, alone. Their main function is to disrupt fungal stress response, destabilize the structural integrity of cellular and vacuolar membranes or stimulate production of reactive oxygen species, augmenting oxidative stress and apoptosis. Use of safe chemosensitizing agents has potential benefit to both agriculture and medicine. When co-applied with a commercial antifungal agent, an additive or synergistic interaction may occur, augmenting antifungal efficacy. This augmentation, in turn, lowers effective dosages, costs, negative side effects and, in some cases, countermands resistance. PMID:22393330

Campbell, Bruce C; Chan, Kathleen L; Kim, Jong H



Actinomycetes of Moroccan habitats: Isolation and screening for antifungal activities  

Microsoft Academic Search

During a search for non-polyenic antifungal antibiotics, 320 actinomycete strains were isolated from several Moroccan habitats. Antibiotic productions of the isolates have been tested at various temperatures and production media. Thirty-two isolates showed strong activity against yeast, moulds and bacteria. The production of non-polyenic antifungal metabolites by active isolates was investigated using some of their biological activities: antibacterial activity, spheroplast regeneration

Yedir Ouhdouch; Mustapha Barakate



Growth medium effect on the antifungal activity of LY 303366  

Microsoft Academic Search

The impact of growth medium selection on antifungal susceptibility testing has been well documented. Previously we described the antifungal characteristics of LY 303366 via time-kill curve methods using RPMI 1640 buffered with 0.165 M morpholinepropane-sulfonic acid as growth medium. The purpose of the current study was to compare the previously reported kill curve results with results obtained using antibiotic medium

Michael E. Klepser; Erika J. Ernst; Michael E. Ernst; Michael A. Pfaller



Antifungal activity of polymer-based copper nanocomposite coatings  

NASA Astrophysics Data System (ADS)

Eukaryotes, such as fungi, can be harmful pathogen agents, and the control of their bioactivity is critical as humans are eukaryote organisms, too. Here, copper/polymer nanocomposites are proposed as antifungal spinnable coatings with controlled copper-releasing properties. The tests of the bioactivity show that fungal growth is inhibited on the nanocomposite-coated plates, and the antifungal activity can be modulated by controlling the Cu nanoparticle loading.

Cioffi, Nicola; Torsi, Luisa; Ditaranto, Nicoletta; Sabbatini, Luigia; Zambonin, Pier Giorgio; Tantillo, Giuseppina; Ghibelli, Lina; D'Alessio, Maria; Bleve-Zacheo, Teresa; Traversa, Enrico



Synthesis and antifungal activity of benzimidazole, benzotriazole and aminothiazole derivatives.  


In recent years, the use of antifungal drugs in human medicine has increased, especially with the advent of AIDS epidemic. Efforts have focused on the development of new, less toxic and more efficacious antifungal drugs with novel mechanism of action. The purpose of this study was to synthesize of some new benzimidazole, benzotriazole and aminothiazole derivatives and to evaluate their activity against some species of Candida, Aspergillus and dermatophytes. The desired compounds were synthesized by the reaction of benzimidazole and benzotriazole with bromoalkanes and also by the reaction of an amide derivative of aminothiazole with 2-piperazino-1-ethanol in an efficient solvent in the presence of tetraethyl ammounim bromide or triethylamine) as catalyst. Chemical structures of all the new compounds were confirmed by spectrophotometric methods. Antifungal activities of the new compounds were evaluated by broth micro dilution method as recommended by CLSI. Among the tested compounds, 1-nonyl-1H-benzo[d]imidazole and 1-decyl-1H-benzo[d]imidazole exhibited the best antifungal activities. Of the examined synthetic compounds in different categories, benzimidazole derivatives established better antifungal activities than benzotriazole derivatives, and the piperazine analogue had no significant antifungal effect. PMID:23181082

Khabnadideh, S; Rezaei, Z; Pakshir, K; Zomorodian, K; Ghafari, N



Hydrogel of ketoconazole and PAMAM dendrimers: formulation and antifungal activity.  


Ketoconazole (KET), an imidazole derivative with well-known antifungal properties, is lipophilic and practically insoluble in water, therefore its clinical use has some practical disadvantages. The aim of the present study was to investigate the influence of PAMAM-NH(2) and PAMAM-OH dendrimers generation 2 and generation 3 on the solubility and antifungal activity of KET and to design and evaluate KET hydrogel with PAMAM dendrimers. It was shown that the surface charge of PAMAM dendrimers strongly affects their influence on the improvement of solubility and antifungal activity of KET. The MIC and MFC values obtained by broth dilution method indicate that PAMAM-NH(2) dendrimers significantly (up to 16-fold) increased the antifungal activity of KET against Candida strains (e.g., in culture Candida albicans 1103059/11 MIC value was 0.008 ?g/mL and 0.064 ?g/mL, and MFC was 2 ?g/mL and 32 ?g/mL for KET in 10 mg/mL solution of PAMAM-NH(2) G2 and pure KET, respectively). Antifungal activity of designed KET hydrogel with PAMAM-NH(2) dendrimers measured by the plate diffusion method was definitely higher than pure KET hydrogel and than commercial available product. It was shown that the improvement of solubility and in the consequence the higher KET release from hydrogels seems to be a very significant factor affecting antifungal activity of KET in hydrogels containing PAMAM dendrimers. PMID:22513487

Winnicka, Katarzyna; Wroblewska, Magdalena; Wieczorek, Piotr; Sacha, Pawel Tomasz; Tryniszewska, Elzbieta



Influence of antifungal pre-treatment in preparing test mycelium on MIC values of several antifungal agents against Aspergillus niger  

Microsoft Academic Search

Antifungal activity of two imidazoles (miconazole and ketoconazole) and one polyene (amphotericin B) was evaluated using an\\u000a automatic growth analysis system. Spores ofAspergillus niger were inoculated on the polylysine-coated glass bottom of a culture vessel. A colony formed in liquid medium was exposed to\\u000a an antifungal agent and subsequently washed. Based on the dynamic growth rate of a test hypha

Jong-Chul Parkll; Kosuke Takatori; Hun-Jun Lee; Hideaki Matsuoka; Hiroshi Kurata



Nationwide Study of Candidemia, Antifungal Use, and Antifungal Drug Resistance in Iceland, 2000 to 2011  

PubMed Central

Candidemia is often a life-threatening infection, with highly variable incidence among countries. We conducted a nationwide study of candidemia in Iceland from 2000 to 2011, in order to determine recent trends in incidence rates, fungal species distribution, antifungal susceptibility patterns, and concurrent antifungal consumption. A total of 208 infection episodes in 199 patients were identified. The average incidence during the 12 years was 5.7 cases/100,000 population/year, which was significantly higher than that from 1990 to 1999 (4.3/100,000/year; P = 0.02). A significant reduction in the use of blood cultures was noted in the last 3 years of the study, coinciding with the economic crisis in the country (P < 0.001). Age-specific incidence rates were highest among patients at the extremes of age, 20.7/100,000 for <1 year of age and 18.1/100,000 for >60 years, and varied by gender. Age-specific incidence among males >80 years old was 28.6/100,000/year, and it was 8.3/100,000/year for females in this age group (P = 0.028). The 30-day survival rate among adult patients remained unchanged compared to that from 1990 to 1999 (70.4% versus 69.5%, P = 0.97). Candida albicans was the predominant species (56%), followed by C. glabrata (16%) and C. tropicalis (13%). The species distribution remained stable compared to that from previous decades. Fluconazole use increased 2.4-fold from 2000 to 2011, with no increase in resistance. In summary, the incidence of candidemia in Iceland has continued to increase but may have reached a steady state, and no increase in antifungal drug resistance has been noted. Decreased use of blood cultures toward the end of the study may have influenced detection rates.

Asmundsdottir, Lena Ros; Erlendsdottir, Helga



Extension of the bioautograph technique for multiresidue determination of fungicide residues in plants and water  

Microsoft Academic Search

The inhibition effect of 17 fungicides on spores germination of different species of fungi on thin layer Chromatographie (TLC) plates has been studied in order to extend the applicability of bioautography and to increase the sensitivity of the detection. Minimum detectable amounts on TLC plates of vinclozolin, iprodione, procymidone, captan, imazalil, triadimefon, triadimenol, fenarimol, propiconazole, myclobutanil, flutriafol, flusilazole, hexaconazole, tebuconazole,

Anna Balinova



High-performance chiral separation of fourteen triazole fungicides by sulfated ?-cyclodextrin-mediated capillary electrophoresis  

Microsoft Academic Search

In this paper, sulfated ?-cyclodextrin-mediated capillary electrophoresis (CE) is evaluated as a new approach for the chiral separation of triazole-type fungicides. The 14 fungicides investigated were bitertanol, cyproconazole, difenoconazole, diniconazole, flutriafol, hexaconazole, myclobutanil, paclobutrazol, penconazole, propiconazole, tebuconazole, tetraconazole, triadimefon and triadimenol. Under the optimal conditions, excellent enantioseparation was achieved for all the 14 fungicides, including those fungicides containing two chiral

Y. S. Wu; H. K. Lee; S. F. Y. Li



Antibacterial and antifungal properties of essential oils.  


In recent years there has been an increasing interest in the use of natural substances, and some questions concerning the safety of synthetic compounds have encouraged more detailed studies of plant resources. Essential oils, odorous and volatile products of plant secondary metabolism, have a wide application in folk medicine, food flavouring and preservation as well as in fragrance industries. The antimicrobial properties of essential oils have been known for many centuries. In recent years (1987-2001), a large number of essential oils and their constituents have been investigated for their antimicrobial properties against some bacteria and fungi in more than 500 reports. This paper reviews the classical methods commonly used for the evaluation of essential oils antibacterial and antifungal activities. The agar diffusion method (paper disc and well) and the dilution method (agar and liquid broth) as well as turbidimetric and impedimetric monitoring of microorganism growth in the presence of tested essential oils are described. Factors influencing the in vitro antimicrobial activity of essential oils and the mechanisms of essential oils action on microorganisms are reported. This paper gives an overview on the susceptibility of human and food-borne bacteria and fungi towards different essential oils and their constituents. Essential oils of spices and herbs (thyme, origanum, mint, cinnamon, salvia and clove) were found to possess the strongest antimicrobial properties among many tested. PMID:12678685

Kalemba, D; Kunicka, A



Antifungal activity of plant extracts against dermatophytes.  


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 < 0.05) between test plants. Extracts of Capparis spinosa and Juglans regia completely prevented growth of M. canis and T. violaceum. The most active extracts (90-100% inhibition) were those of Anagallis arvensis, C. spinosa, J. regia, Pistacia lentiscus and Ruta chalapensis against M. canis; 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. PMID:10680445

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



Antifungal Hydroxy Fatty Acids Produced during Sourdough Fermentation: Microbial and Enzymatic Pathways, and Antifungal Activity in Bread  

PubMed Central

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 C18:1 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 C18:1 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.

Black, Brenna A.; Zannini, Emanuele; Curtis, Jonathan M.



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


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. PMID:23315734

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



[The antifungal activity of fibrous materials containing chemically bound antimicrobial substances].  


Studies of the antifungal characteristics of modified cellulose and polycaproamide materials containing chemically bound antibacterial agents, hexachlorophene or catamine AB, have shown antifungal activity of these materials towards the major fungi inducing mycoses of the feet. PMID:2773582

Stepanova, Zh V; Skokova, I F; Penenzhik, M A; Iaglom, D L



Exploring the molecular basis of antifungal synergies using genome-wide approaches  

Technology Transfer Automated Retrieval System (TEKTRAN)

This is a review article summarizing genomic profiling strategies for determining the mechanism of action of antifungal synergies, and highlighting the potential applications of these technologies. Given the limitations of currently available antifungal agents and the development of drug resistance...


Treatment of endogenous fungal endophthalmitis: focus on new antifungal agents.  


Endogenous fungal endophthalmitis, involving only the chorioretinal structures or extending to involve the vitreous (vitritis), is a sight-threatening infection requiring early appropriate therapy. Endophthalmitis is a relatively frequent complication of candidemia and less commonly occurs in patients who have invasive aspergillosis. Because the eye is a protected compartment, penetration of systemically administered antifungal agents is highly variable. In the posterior segment of the eye, amphotericin B (AmB) achieves very poor concentrations, but fluconazole concentrations are high. Among newer antifungal agents, voriconazole shows the most promise, because therapeutic concentrations for most Candida and Aspergillus species are achieved in the vitreous, and its antifungal activity is broad. In contrast, neither posaconazole nor the 3 echinocandins achieve adequate therapeutic concentrations in the vitreous. For sight-threatening macular involvement and vitritis, intravitreal injection of either AmB or voriconazole is helpful to achieve high local antifungal activity as quickly as possible. We review the available evidence regarding the most appropriate use of antifungal agents for endogenous fungal endophthalmitis, with the emphasis on treatment of infections due to Candida species. PMID:21239843

Riddell, James; Comer, Grant M; Kauffman, Carol A



Fungal endophytes: a potential source of antifungal compounds.  


The prevalence of invasive fungal infections has increased significantly during organ transplantation, cancer chemotherapy and allogeneic bone marrow transplantation. However, only a limited number of antifungal agents are currently available for the treatment of life-threatening fungal infections. Although new antifungal agents have been introduced in the market, the development of resistance to antifungal drugs has become increasingly apparent, especially in patients with long term treatment. Microbial natural products have always been an alternative natural source for the isolation of novel molecules for various therapeutic applications. Endophytes are the microorganisms that colonize internal tissues of all plant species and represent an abundant and dependable source of bioactive and chemically novel compounds with potential for exploitation in a wide variety of medical, agricultural and industrial arenas. In the present review several metabolites obtained from endophytic fungi with a potential as antifungal agents are mentioned with bioactivity including volatile organic compounds. The compounds reported here with a diverse scaffold can be a potential starting point for new antifungal agents either as such or after chemical modification. PMID:22202019

Deshmukh, Sunil Kumar; Verekar, Shilpa Amit



Poly(amidoamine) dendrimers increase antifungal activity of clotrimazole.  


Clotrimazole (CLO) is a local imidazolic antifungal agent. A major problem associated with the successful formulation of effective dosage forms containing CLO is its poor aqueous solubility, which presents a hindrance for the local availability of CLO and limits the effective antifungal therapy. In the present study, the effects of various concentrations of poly(amidoamine) (PAMAM) dendrimers generation 2 (G2) and generation 3 (G3) with amine (PAMAM-NH(2)) or hydroxyl surface groups (PAMAM-OH) on aqueous solubility and antifungal activity of CLO were studied. The obtained results showed that all tested PAMAM dendrimers improved the solubility of CLO and the more potent were PAMAM-NH(2) dendrimers. The increase in solubility of CLO was highest at dendrimer concentration of 10 mg/ml. Microbiology studies indicated that only PAMAM-NH(2) dendrimers significantly increased the antifungal activity of CLO (a 4-32-fold increase in the antifungal activity compared to pure CLO) and the most potent was dendrimer PAMAM-NH(2) G2. These observations indicate that PAMAM dendrimers might be considered as potential carriers of CLO and provide further impetus to evaluate these polymers for use in basic drug delivery studies and to design semisolid dosage forms based on dendrimers with antimicrobial drugs, like CLO. PMID:21720026

Winnicka, Katarzyna; Sosnowska, Katarzyna; Wieczorek, Piotr; Sacha, Pawel Tomasz; Tryniszewska, Elzbieta



In Search of the Holy Grail of Antifungal Therapy  

PubMed Central

The ideal antifungal agent remains an elusive goal for treatment of life-threatening systemic fungal infections. Such an agent would have broad antifungal activity, low rates of resistance, flexible routes of administration, few associated adverse events, and limited drug-drug interactions. Only three of the seven classes of antifungal agents currently available are suitable for treatment of systemic infection: the polyenes, the azoles, and the echinocandins. None match all the characteristics of an ideal agent, the Holy Grail of antifungal therapy. Academia and industry need to collaborate in the search for new lead antifungal compounds using traditional screening methods as well as the new pharmacogenomics methods. Enhancing efficacy and reducing toxicity of the currently available therapeutic agents is also another important avenue of study. As an example, the Mycosis Research Center at the University of Mississippi Medical Center has identified pyogenic polyenes in commercial preparations of amphotericin B deoxycholate which correlate with infusion related toxicities. A highly purified formulation of amphotericin B appears promising, with a better therapeutic index compared to its parent compound as evidenced by results of in vitro and in vivo studies reviewed in this presentation.

Chapman, Stanley W.; Sullivan, Donna C.; Cleary, John D.



Cadinene sesquiterpenes from Eupatorium adenophorum and their antifungal activity.  


Bioactive constituents of Eupatorium adenophorum were investigated for antifungal activity. A structure-antifungal activity relationship of cadinene sesquiterpenes was predicted by evaluating individual derivatives. Cadinene derivatives were extracted from leaves of Eupatorium adenophorum using ethyl acetate. Five cadinene sesquiterpenes were isolated by column chromatography and Preparative Thin Layer Chromatography. Bioactivity of these cadinene sesquiterpenes were evaluated in vitro against four phytopathogenic fungi using poison food technique. Purified sesquiterpenes were spectroscopically elucidated as cadinan-3-ene-2,7-dione (1), 7-hydroxycadinan-3-ene-2-one (2), 5,6-dihydroxycadinan-3-ene-2,7-dione (3), cadinan-3,6-diene-2,7-dione (4) and 2-acetyl-cadinan-3,6-diene-7-one (5). Antifungal evaluation of these compounds against pathogenic fungi was found to be selective. Compound 1 was highly inhibitory towards S. rolfsii (ED50 181.60 ± 0.58 ?gmL(-1)) and R. solani (ED50 189.74 ± 1.03 ?gmL(-1)). Availability of plant material and significant antifungal activity makes the plant a potential source of antifungal agent and that can be exploited for the development of a natural fungicide. PMID:23452218

Kundu, Aditi; Saha, Supradip; Walia, Suresh; Shakil, Najam A; Kumar, Jitendra; Annapurna, Kannepalli



How to select an antifungal agent in critically ill patients.  


Fungal infections are common in critically ill patients and are associated with increased morbidity and mortality. Candida spp are the most commonly isolated fungal pathogens. The last 2 decades have seen an increased incidence of fungal infections in critical illness and the emergence of new pathogenic fungal species and also the development of more effective (better bioavailability) and safer (less toxicity, fewer drug interactions) drugs. The distinction between colonization and infection can be difficult, and problems diagnosing infection may delay initiation of antifungal treatment. A number of factors have been identified that can help to distinguish patients at high risk for fungal infection. The antifungal agents that are most frequently used in the intensive care unit are the first- and second-generation azoles and the echinocandins; amphotericin B derivatives (mainly the liposomal agents) are less widely used because of adverse effects. The choice of antifungal agent in critically ill patients will depend on the aim of therapy (prophylaxis, pre-emptive, empiric, definitive), as well as on local epidemiology and specific properties of the drug (antifungal spectrum, efficacy, toxicity, pharmacokinetic/pharmacodynamic properties, cost). In this article we will review all these aspects and propose an algorithm to guide selection of antifungal agents in critically ill patients. PMID:24018296

Dimopoulos, George; Antonopoulou, Anastasia; Armaganidis, Apostolos; Vincent, Jean-Louis



Systemic antifungals to treat onychomycosis in children: a systematic review.  


Because of the low prevalence of onychomycosis in children, little is known about the efficacy and safety of systemic antifungals in this population. PubMed and Embase databases and the references of related publications were searched in March 2012 for clinical trials (CTs), retrospective analyses (RAs), and case reports (CRs) on the use of systemic antifungals for onychomycosis in children (<18 years). Twenty-six studies (5 CTs, 3 RAs, and 18 CRs) were published between 1976 and 2011. Most of these studies reported the use of systemic terbinafine and itraconazole for the treatment of onychomycosis in children. Therapy with systemic antifungals alone in children ages 1 to 17 years resulted in a complete cure rate of 70.8% (n = 151), whereas combined systemic and topical antifungal therapy in one infant and 19 children age 8 and older resulted in a complete cure rate of 80.0% (n = 20). The efficacy and safety profiles of terbinafine, itraconazole, griseofulvin, and fluconazole in children were similar to those previously reported for adults. In conclusion, based on the little information available on onychomycosis in children, systemic antifungal therapies in children are safe and cure rates are similar to the rates achieved in adults. PMID:23278514

Gupta, Aditya K; Paquet, Maryse



Chloroquine sensitizes biofilms of Candida albicans to antifungal azoles.  


Biofilms formed by Candida albicans, a human pathogen, are known to be resistant to different antifungal agents. Novel strategies to combat the biofilm associated Candida infections like multiple drug therapy are being explored. In this study, potential of chloroquine to be a partner drug in combination with four antifungal agents, namely fluconazole, voriconazole, amphotericin B, and caspofungin, was explored against biofilms of C. albicans. Activity of various concentrations of chloroquine in combination with a particular antifungal drug was analyzed in a checkerboard format. Growth of biofilm in presence of drugs was analyzed by XTT-assay, in terms of relative metabolic activity compared to that of drug free control. Results obtained by XTT-metabolic assay were confirmed by scanning electron microscopy. The interactions between chloroquine and four antifungal drugs were determined by calculating fractional inhibitory concentration indices. Azole resistance in biofilms was reverted significantly (p<0.05) in presence of 250?g/mL of chloroquine, which resulted in inhibition of biofilms at very low concentrations of antifungal drugs. No significant alteration in the sensitivity of biofilms to caspofungin and amphotericin B was evident in combination with chloroquine. This study for the first time indicates that chloroquine potentiates anti-biofilm activity of fluconazole and voriconazole. PMID:23602464

Shinde, Ravikumar Bapurao; Raut, Jayant Shankar; Chauhan, Nitin Mahendra; Karuppayil, Sankunny Mohan



Antifungal activity of cinnamaldehyde and eugenol congeners against wood-rot fungi  

Microsoft Academic Search

In this study, the antifungal activities of cinnamaldehyde and eugenol congeners against white-rot fungus Lenzites betulina and brown-rot fungus Laetiporus sulphureus were evaluated and the relationships between the antifungal activity and the chemical structures were also examined. Results from antifungal tests revealed that cinnamaldehyde, ?-methyl cinnamaldehyde, (E)-2-methylcinnamic acid, eugenol and isoeugenol exhibited strong antifungal activity against all fungi tested. Results

Sen-Sung Cheng; Ju-Yun Liu; Ed-Haun Chang; Shang-Tzen Chang



Antifungal mechanism of the Aspergillus giganteus AFP against the rice blast fungus Magnaporthe grisea  

Microsoft Academic Search

The mold Aspergillus giganteus produces a basic, low molecular weight protein showing antifungal properties against economically important plant pathogens, the AFP (Antifungal Protein). In this study, we investigated the mechanisms by which AFP exerts its antifungal activity against Magnaporthe grisea. M. grisea is the causal agent of rice blast, one of the most devastating diseases of cultivated rice worldwide. AFP

Ana Beatriz Moreno; Blanca San Segundo


A Chemically Modified Tetracycline (CMT3) Is a New Antifungal Agent  

Microsoft Academic Search

Several chemically modified tetracycline analogs (CMTs), which were chemically modified to eliminate their antibacterial efficacy, were unexpectedly found to have antifungal properties. Of 10 CMTs screened in vitro, all exhibited antifungal activities, although their efficacies varied. Among these compounds, CMT-315, -3, and -308 were found to be the most potent as antifungal agents. The MICs of CMT-3 against 47 strains

Yu Liu; Maria E. Ryan; Hsi-Ming Lee; Sanford Simon; George Tortora; Carol Lauzon; Michael K. Leung; Lorne M. Golub



Antifungal activity of sakurasosaponin from the root extract of Jacquinia flammea  

Microsoft Academic Search

The methanolic crude extract from the roots of Jacquinia flammea showed moderate antifungal activity against dermatophytes and very strong antifungal activity against Colletotrichum gloeosporioides. The bioassay-guided purification of the extract, using a combination of vacuum-liquid chromatography and high performance liquid chromatography, allowed the identification of sakurasosaponin (1) as the main metabolite responsible for the antifungal activity.

K. García-Sosa; A. Sánchez-Medina; Sandra L. Álvarez; S. Zacchino; N. C. Veitch; P. Simá-Polanco; L. M. Peña-Rodriguez



Determination of Antifungal MICs by a Rapid Susceptibility Assay  

PubMed Central

A novel microtiter assay for antifungal susceptibility testing was developed. This method has several potential advantages over the M27-A assay of the National Committee for Clinical Laboratory Standards. These include provision of MIC results within 6 to 19 h, graphical display of data, and the availability of objective quantitative endpoints. We refer to the method as the rapid susceptibility assay (RSA). RSA is based on substrate utilization by fungi in the presence of antifungal drugs. Substrate uptake is determined by a colorimetric method, which can be scored by analysis of data obtained from a microplate reader. Variables evaluated in the development of the RSA included inoculum size, incubation period, and efficacy with different classes of antifungal drugs and different yeast isolates. With the rapidly available and quantitative endpoints of the RSA, correlation of MICs and therapeutic drug doses can be evaluated more successfully than they can be evaluated by existing assays.

Riesselman, Marcia H.; Hazen, Kevin C.; Cutler, Jim E.



Enhancement of Commercial Antifungal Agents by Kojic Acid  

PubMed Central

Natural compounds that pose no significant medical or environmental side effects are potential sources of antifungal agents, either in their nascent form or as structural backbones for more effective derivatives. Kojic acid (KA) is one such compound. It is a natural by-product of fungal fermentation commonly employed by food and cosmetic industries. We show that KA greatly lowers minimum inhibitory (MIC) or fungicidal (MFC) concentrations of commercial medicinal and agricultural antifungal agents, amphotericin B (AMB) and strobilurin, respectively, against pathogenic yeasts and filamentous fungi. Assays using two mitogen-activated protein kinase (MAPK) mutants, i.e., sakA?, mpkC?, of Aspergillus fumigatus, an agent for human invasive aspergillosis, with hydrogen peroxide (H2O2) or AMB indicate such chemosensitizing activity of KA is most conceivably through disruption of fungal antioxidation systems. KA could be developed as a chemosensitizer to enhance efficacy of certain conventional antifungal drugs or fungicides.

Kim, Jong H.; Chang, Perng-Kuang; Chan, Kathleen L.; Faria, Natalia C. G.; Mahoney, Noreen; Kim, Young K.; Martins, Maria de L.; Campbell, Bruce C.



Antifungal Chemical Compounds Identified Using a C. elegans Pathogenicity Assay  

PubMed Central

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

Breger, Julia; Fuchs, Beth Burgwyn; Aperis, George; Moy, Terence I; Ausubel, Frederick M; Mylonakis, Eleftherios



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


There is an urgent need for the development of new antifungal agents. A facile in vivo model that evaluates libraries of chemical compounds could solve some of the main obstacles in current antifungal discovery. We show that Candida albicans, as well as other Candida species, are ingested by Caenorhabditis elegans and establish a persistent lethal infection in the C. elegans intestinal track. Importantly, key components of Candida pathogenesis in mammals, such as filament formation, are also involved in nematode killing. We devised a Candida-mediated C. elegans assay that allows high-throughput in vivo screening of chemical libraries for antifungal activities, while synchronously screening against toxic compounds. The assay is performed in liquid media using standard 96-well plate technology and allows the study of C. albicans in non-planktonic form. A screen of 1,266 compounds with known pharmaceutical activities identified 15 (approximately 1.2%) that prolonged survival of C. albicans-infected nematodes and inhibited in vivo filamentation of C. albicans. Two compounds identified in the screen, caffeic acid phenethyl ester, a major active component of honeybee propolis, and the fluoroquinolone agent enoxacin exhibited antifungal activity in a murine model of candidiasis. The whole-animal C. elegans assay may help to study the molecular basis of C. albicans pathogenesis and identify antifungal compounds that most likely would not be identified by in vitro screens that target fungal growth. Compounds identified in the screen that affect the virulence of Candida in vivo can potentially be used as "probe compounds" and may have antifungal activity against other fungi. PMID:17274686

Breger, Julia; Fuchs, Beth Burgwyn; Aperis, George; Moy, Terence I; Ausubel, Frederick M; Mylonakis, Eleftherios



Antifungal activity of Mexican oregano (Lippia berlandieri Shauer).  


Antifungal and sensorial properties of spices have been recognized for years. The antifungal compounds are products of the plant's secondary metabolism, and the action of those compounds could be used to inhibit the growth of spoilage and pathogenic microorganisms in food. Mexican oregano (Lippia berlandieri) grows wildly in the desert zone of Mexico and is usually added to regional foods. The goal of this study was to evaluate the antifungal activity of Mexican oregano versus food-contaminant fungi. Fungi were isolated from spoiled fruit and vegetables and identified according to morphological characteristics. The antifungal activity of oregano was evaluated by radial growth measurement on potato dextrose agar added with dried oregano (0.25 to 4.0%). The essential oil antifungal activity of oregano was also evaluated by the diffusion well test. Twenty-one fungal strains were isolated, which included Penicillium, Geotrichum, Aspergillus, and Bipolaris. In seven of the 21 strains, no inhibitory effect was observed at either concentration of oregano. An increase in growth at the lower or higher concentrations of oregano, when compared to the control, was observed in two fungal strains; in 12 strains, a strong inhibitory effect of oregano was evident. The oregano essential oil was inhibitory to all fungal strains, but there were differences in the extent of the effect. Although the antifungal effect of oregano is strongly established, there was a differential effect with the fungal strains studied. Besides pathogenic fungi and bacteria, microbial spoilage flora should be considered when the addition of spices for food preservation is proposed. PMID:16355848

Portillo-Ruiz, Martha Cristina; Viramontes-Ramos, Sabina; Muñoz-Castellanos, Laila Nayzzel; Gastélum-Franco, María Guadalupe; Nevárez-Moorillón, Guadalupe Virginia



Use of Antifungal Combination Therapy: Agents, Order, and Timing  

PubMed Central

Given the substantial morbidity and mortality related to invasive fungal infections, treatment with a combination of antifungal agents is often considered. A growing body of literature from in vitro studies, animal models, and clinical experience provides data evaluating this approach. This review describes combination antifungal strategies for the management of cryptococcal meningitis, invasive candidiasis, invasive aspergillosis, and rare mold infections. The potential effects that sequencing and timing have on the efficacy of such approaches are discussed, with a focus on recent clinical data in this arena.

Perfect, John R.



Fungal virulence genes as targets for antifungal chemotherapy.  

PubMed Central

Fungal virulence genes have now met the age of molecular pathogenesis. The definition of virulence genes needs to be broad so that it encompasses the focus on molecular antifungal targets and vaccine epitopes. However, in the broad but simple definition of a virulence gene, there will be many complex genetic and host interactions which investigators will need to carefully define. Nevertheless, with the increasing numbers of serious fungal infections produced by old and newly reported organisms, the paucity of present antifungal drugs, and the likelihood of increasing drug resistance, the need for investigations into understanding fungal virulence at the molecular level has never been more important.

Perfect, J R



Antibacterial and antifungal metal based triazole Schiff bases.  


A new series of four biologically active triazole derived Schiff base ligands (L(1)-L(4)) and their cobalt(II), nickel(II), copper(II) and zinc(II) complexes (1-16) have been synthesized and characterized. The ligands were prepared by the condensation reaction of 3-amino-5-methylthio-1H-1,2,4-triazole with chloro-, bromo- and nitro-substituted 2-hydroxybenzaldehyde in an equimolar ratio. The antibacterial and antifungal bioactivity data showed the metal(II) complexes to be more potent antibacterial and antifungal than the parent Schiff bases against one or more bacterial and fungal species. PMID:22803673

Chohan, Zahid H; Hanif, Muhammad



Novel antifungal defensins from Nigella sativa L. seeds.  


From seeds of Nigella sativa L. (Ranunculaceae), an endemic plant of Uzbekistan, two novel defensins named Ns-D1 and Ns-D2, were isolated and sequenced. The peptides differ by a single amino acid residue and show high sequence similarity to Raphanus sativus L. defensins Rs-AFP1 and Rs-AFP2. The Ns-D1 and Ns-D2 defensins display strong although divergent antifungal activity towards a number of phytopathogenic fungi. High antifungal activity of N. sativa defensins makes them promising candidates for engineering pathogen-resistant plants. PMID:21144761

Rogozhin, Eugene A; Oshchepkova, Yulia I; Odintsova, Tatyiana I; Khadeeva, Natalia V; Veshkurova, Olga N; Egorov, Tsezi A; Grishin, Eugene V; Salikhov, Shavkat I



[Research of antifungal substances secreted by higher fungi in culture].  


A screening in vitro of antifungic activity of 24 strains of Basidiomycetes was realized with their culture filtrate. Lycoperdon perlatum Pers. = Pers., Oudemansiella platyphylla (Pers. ex Fr.) Mos., Agrocybe dura (Bolt) Singer have shown an activity against Candida albicans, Candida tropicalis and Aspergillus fumigatus; Pholiota spumosa (Fr.) Singer towards Botrytis cinerea and Lycoperdon perlatum Pers. = Pers. towards Alternaria solani, Botrytis cinerea and Verticillium dahliae. More extensive studies of the kinetics of antifungic substances production from Lycoperdon perlatum Pers. = Pers. were effectued with 2 different media and 2 different seeding technics on the strains which were sensible to the inhibitory character of this Gasteromycete. PMID:2082797

Pujol, V; Seux, V; Villard, J



In Vitro Antifungal Activity of Isavuconazole against Madurella mycetomatis  

PubMed Central

Currently, therapy of black-grain mycetoma caused by Madurella mycetomatis consists of extensive debridement of the infected tissue combined with prolonged antifungal therapy with ketoconazole or itraconazole. In the present study, the in vitro activity of the new triazole isavuconazole toward M. mycetomatis was evaluated. Isavuconazole appeared to have high activity against M. mycetomatis, with MICs ranging from ?0.016 to 0.125 ?g/ml. Due to its favorable pharmacokinetics, isavuconazole could be a promising antifungal agent in the treatment of mycetoma.

Meis, Jacques F.; Curfs-Breuker, Ilse; Fahal, Ahmed H.



In vitro antifungal activity of isavuconazole against Madurella mycetomatis.  


Currently, therapy of black-grain mycetoma caused by Madurella mycetomatis consists of extensive debridement of the infected tissue combined with prolonged antifungal therapy with ketoconazole or itraconazole. In the present study, the in vitro activity of the new triazole isavuconazole toward M. mycetomatis was evaluated. Isavuconazole appeared to have high activity against M. mycetomatis, with MICs ranging from ?0.016 to 0.125 ?g/ml. Due to its favorable pharmacokinetics, isavuconazole could be a promising antifungal agent in the treatment of mycetoma. PMID:22964246

Kloezen, Wendy; Meis, Jacques F; Curfs-Breuker, Ilse; Fahal, Ahmed H; van de Sande, Wendy W J



A review of clinical experience with newer antifungals in children.  


Fungal infections are a significant cause of morbidity and mortality in immunocompromised children. Since the beginning of the 21st century, many new antifungals including the echinocandins (i.e., caspofungin, micafungin, anidulafungin) and the newer generation triazoles (i.e., voriconazole and posaconazole) have received Food and Drug Administration approval. Unfortunately, despite making great strides in the adult arena, these agents are not currently approved in the pediatric population. However, pharmacokinetic data and clinical experiences with these agents in infants, children, and adolescents are mounting. As such, this review will discuss key concepts in pediatric pharmacology and clinical use of these newer antifungal agents. PMID:23055874

Fallon, Renee M; Girotto, Jennifer E



A Review of Clinical Experience with Newer Antifungals in Children  

PubMed Central

Fungal infections are a significant cause of morbidity and mortality in immunocompromised children. Since the beginning of the 21st century, many new antifungals including the echinocandins (i.e., caspofungin, micafungin, anidulafungin) and the newer generation triazoles (i.e., voriconazole and posaconazole) have received Food and Drug Administration approval. Unfortunately, despite making great strides in the adult arena, these agents are not currently approved in the pediatric population. However, pharmacokinetic data and clinical experiences with these agents in infants, children, and adolescents are mounting. As such, this review will discuss key concepts in pediatric pharmacology and clinical use of these newer antifungal agents.

Fallon, Renee M.; Girotto, Jennifer E.



Orally administered antifungal therapy for experimental keratomycosis.  

PubMed Central

Fluconazole, an experimental azole antifungal agent with good tissue penetration following oral administration, offers the possibility of a new approach to the treatment of keratomycosis. Its efficacy as an orally administered agent was investigated in two models of experimental fungal infection in Dutch-belted rabbits. The study proceeded in three stages. In the first, a model of keratitis due to Aspergillus fumigatus was developed, the suitability of quantitative isolate recovery techniques for the evaluation of the disease caused by this organism was confirmed, and the correlation between the severity of clinical disease scored nonparametrically and the isolate recovery rate was established. The model was found to be most useful for study during the first 5 days of infection. The natural course of experimental Candida alibcans keratitis was evaluated and, on the basis of quantitative isolate recovery techniques, this model was found to be appropriate for studies lasting up to 1 week. In the second stage, corneal uptake following oral administration of fluconazole was studied in Dutch-belted rabbits. The drug was found to readily penetrate the cornea in amounts that correlated with serum levels (R = 0.89). Eight hours following a single 20 mg/kg dose, the corneal level was 7.4 mg/gm, almost double the amount when a 10 mg/kg dose was administered. When given in a twice daily divided dose, fluconazole accumulated steadily in the corneas over a period of 5 days. The presence of inflammation induced by fungal infection did not influence corneal uptake. In the final stage, the efficacy of orally administered fluconazole in the treatment of keratomycosis was evaluated. Overall, a significant therapeutic effect was observed with both infections. Treatment of the animals with oral fluconazole for 1 day prior to inoculation with Candida albicans led to a significant decrease in isolate recovery 1 day later (P = 0.01). However, when treatment was continued for 5 days following inoculation, no additive effect of pretreatment was noted. Pretreatment for 1 day followed by 5 days postinoculation treatment led to a significant decrease in clinical disease (P less than 0.05) and isolate recovery (P = 0.05). A beneficial effect of pretreatment compared to treatment begun 1 day postinoculation, as measured by a reduction in clinical severity and isolate recovery, was also noted. On the basis of these short-term therapeutic studies and the excellent corneal penetration of fluconazole, further investigation of oral therapy of keratomycosis appears warranted. Images FIGURE 1 FIGURE 2 FIGURE 3 FIGURE 4 FIGURE 5

O'Day, D M



Identification and Biological Activity of Antifungal Saponins from Shallot ( Allium cepa L. Aggregatum Group).  


The n-butanol extract of shallot basal plates and roots showed antifungal activity against plant pathogenic fungi. The purified compounds from the extract were examined for antifungal activity to determine the predominant antifungal compounds in the extract. Two major antifungal compounds purified were determined to be alliospiroside A (ALA) and alliospiroside B. ALA had prominent antifungal activity against a wide range of fungi. The products of acid hydrolysis of ALA showed a reduced antifungal activity, suggesting that the compound's sugar chain is essential for its antifungal activity. Fungal cells treated with ALA showed rapid production of reactive oxygen species. The fungicidal action of ALA was partially inhibited by a superoxide scavenger, Tiron, suggesting that superoxide anion generation in the fungal cells may be related to the compound's action. Inoculation experiments showed that ALA protected strawberry plants against Colletotrichum gloeosporioides , indicating that ALA has the potential to control anthracnose of the plant. PMID:24138065

Teshima, Yoshiki; Ikeda, Tsuyoshi; Imada, Kiyoshi; Sasaki, Kazunori; El-Sayed, Magdi A; Shigyo, Masayoshi; Tanaka, Shuhei; Ito, Shin-Ichi



Antifungal amides from Piper hispidum and Piper tuberculatum.  


Piper hispidum and Piper tuberculatum accumulate amides bearing isobutyl, pyrrolidine, dihydropyridone and piperidine moieties. The isolation and characterization of several representatives including two hitherto unreported amides were performed by chromatographic techniques and by analysis of spectroscopic data. The antifungal activity of each amide was determined by direct bioautography against Cladosporium sphaerospermum. PMID:11130674

Navickiene, H M; Alécio, A C; Kato, M J; Bolzani, V D; Young, M C; Cavalheiro, A J; Furlan, M



Antifungal amides from Piper hispidum and Piper tuberculatum  

Microsoft Academic Search

Piper hispidum and Piper tuberculatum accumulate amides bearing isobutyl, pyrrolidine, dihydropyridone and piperidine moieties. The isolation and characterization of several representatives including two hitherto unreported amides were performed by chromatographic techniques and by analysis of spectroscopic data. The antifungal activity of each amide was determined by direct bioautography against Cladosporium sphaerospermum.

Hosana Maria D. Navickiene; Alberto Camilo Alécio; Massuo Jorge Kato; Vanderlan da S. Bolzani; Maria Claudia M. Young; Alberto José Cavalheiro; Maysa Furlan



American Fisheries Society Evaluation of Antifungal Agents for Fish Culture  

Microsoft Academic Search

The antifungal activities of 21 chemicals against species of Saprolegnia, a ubiquitous genus of aquatic fungi frequently found in fish hatcheries, were evaluated with pure fungal culture and with Saprolegnia-infected eggs of rainbow trout (Oncorhynchus mykiss). Fourteen compounds were ineffective for control of fungus on rainbow trout eggs or were toxic to the eggs. The seven compounds that effectively controlled

L. L. Marking; J. J. Rach; T. M. Schreier




Microsoft Academic Search

Fungicides are expensive, dangerous, and can be harmful to the environment, but they are often necessary for profitable farming operations. New technologies may soon allow farmers to replace these chemicals with genetically engineered plants producing antifungal enzymes that degrade fungal cell walls. To explore this option, a Paenbacillus chitosanase gene was cloned, sequenced, and modified for plant expression. The modified

Bill L. Hendrix


Antifungal Activity of Intraocularly Used Liquids against Aspergillus  

Microsoft Academic Search

The antifungal effectiveness of liquids used as intraocular tamponading agents in vitrectomy was tested against a strain of Aspergillus niger. This microorganism is a frequent causative factor of endophthalmitis. The strain belonged to the ATCC collection (A. niger ATCC 16404). The samples tested were: (a) perfluorocarbons: perfluorodecalin and perfluoroctane, (b) silicone oils: Siloil 1,000 and Siloil 5,000, and (c) balanced

Calliope Economou-Stamatelopoulou; George P. Roussopoulos; John C. Prouskas; Michael Apostolopoulos



Properties and mechanisms of action of naturally occurring antifungal peptides.  


Antimicrobial peptides are a vital component of the innate immune system of all eukaryotic organisms and many of these peptides have potent antifungal activity. They have potential application in the control of fungal pathogens that are a serious threat to both human health and food security. Development of antifungal peptides as therapeutics requires an understanding of their mechanism of action on fungal cells. To date, most research on antimicrobial peptides has focused on their activity against bacteria. Several antimicrobial peptides specifically target fungal cells and are not active against bacteria. Others with broader specificity often have different mechanisms of action against bacteria and fungi. This review focuses on the mechanism of action of naturally occurring antifungal peptides from a diverse range of sources including plants, mammals, amphibians, insects, crabs, spiders, and fungi. While antimicrobial peptides were originally proposed to act via membrane permeabilization, the mechanism of antifungal activity for these peptides is generally more complex and often involves entry of the peptide into the cell. PMID:23381653

van der Weerden, Nicole L; Bleackley, Mark R; Anderson, Marilyn A



Antifungal activity of a thiophene polyine from Leuzea carthamoides.  


The thiophene polyine (E)-2-[5-(hept-5-en-1,3-diynyl)-thien-2-yl]-ethan-1,2-diol was isolated from an ethanolic extract of underground parts of Leuzea carthamoides. The thiophene polyine demonstrated significant antifungal activity against all tested species. PMID:12727496

Chobot, V; Buchta, V; Jahodárová, H; Pour, M; Opletal, L; Jahodár, L; Harant, P



Using chemical ecology to locate new antifungal natural products  

Microsoft Academic Search

The quest for new antifungal drugs is critical for several reasons. Immune suppression causes susceptibility to fungal infections. The number of immune-suppressed individuals continues to rise as society is faced with an aging population, an increase in AIDS infected patients, and medical advances. Most drugs used to treat mycological infections have low bioavailability or are too toxic for prolonged use.

Stephanie J. Eckerman; Kate J. Graham



Research to identify effective antifungal agents. Annual report 1993.  

National Technical Information Service (NTIS)

Use of malachite green as a fungicide in fish culture was terminated by the Food and Drug Administration (FDA) on August 27,1991. Formalin has been the replacement antifungal agent, but the present registration restricts its use only to eggs of salmonids ...

C. B. Schreck M. S. Fitzpatric R. L. Chitwood L. L. Marking J. J. Rach



In vitro antifungal drug susceptibilities of Penicillium marneffei from China.  


Penicillium marneffei infections in immunocompromised patients are often fatal, but early treatment with appropriate antifungal agents may have a good prognosis. To select drugs for treating P. marneffei infection in Southern China, the susceptibilities of antifungal agents against P. marneffei isolates were evaluated. Twenty-five strains of P. marneffei were isolated from patients from 2008 to 2010 in Guangxi Province of China, and 14 strains were isolated from bamboo rats. The activity of voriconazole, fluconazole, itraconazole, terbinafine, and amphotericin B on the isolates was assessed by MIC analysis. Voriconazole MIC against strains of P. marneffei ranged from 0.004 to 0.25 mg/l, and it had the lowest MIC (geometric mean values, 0.04 mg/l) in comparison to the other antifungal agents. The MICs of other antifungal agents, in order of lowest to highest, were as follows: itraconazole, terbinafine, amphotericin B, and fluconazole. The results show voriconazole and itraconazole are active against P. marneffei isolates in vitro, and terbinafine may have unrealized usefulness in the treatment of infections caused by this yeast form. PMID:23104584

Liu, Donghua; Liang, Ling; Chen, Jimin



Antifungal activity of Bacillus sp. isolated from compost.  


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. PMID:11501422

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



Antifungal effect of dairy propionibacteria—contribution of organic acids  

Microsoft Academic Search

Large amounts of food and feed are lost every year due to spoilage by moulds and yeasts. Biopreservation, i.e. the use of microorganisms as preservatives instead of chemicals, has gained increased interest. Lactic acid bacteria and propionibacteria might be particularly useful due to their important role in many food fermentations. Knowledge of the antifungal effects of the organic acids produced

Helena Lind; Hans Jonsson; Johan Schnürer



Screening of selected West Bengal plants for antifungal activity  

Microsoft Academic Search

A systematic screening of 170 different West Bengal plants was carried out to find antifungal antibiotics, usingAspergillus niger andTrichophyton rubrum as test organisms. From them, four plant species, viz.Curcuma zedoaria, C. aromatica, C. amada, and aBrassica sp. have been found to contain active antibiotic principles with strong inhibitory effects against both test organisms.

S. K. Gupta; A. B. Banerjee



Antifungal metabolites from fungal endophytes of Pinus strobus  

Microsoft Academic Search

The extracts of five foliar fungal endophytes isolated from Pinus strobus (eastern white pine) that showed antifungal activity in disc diffusion assays were selected for further study. From these strains, the aliphatic polyketide compound 1 and three related sesquiterpenes 2–4 were isolated and characterized. Compound 2 is reported for the first time as a natural product and the E\\/Z conformational

Mark W. Sumarah; Julie R. Kesting; Dan Sørensen; J. David Miller



Synthesis, antifungal, and antiviral activity of hydrophosphoryl derivatives of mycoheptin  

Microsoft Academic Search

Reactions of the polyene macrolide antibiotic mycoheptin with aldehydes and hypophosphorous acid yielded its hydrophosphoryl\\u000a derivatives. The physicochemical and biological properties the resulting mycoheptin derivatives were studied. Biological investigations\\u000a showed that hydrophosphoryl derivatives of mycoheptin were less toxic than the initial antibiotic and had antifungal and antiviral\\u000a activity.

V. V. Belakhov; Yu. L. Shenin



Synthesis of novel chiral macrolides and their antifungal activity  

Microsoft Academic Search

Nineteen chiral macrocyclic diamide–diester ligands were synthesized using a three step reaction. The synthesis utilized the condensation of dicarbonyl dichlorides with chiral 2-aminoethanol derivatives. The reaction was catalyzed in a dual catalyst system. Some of the compounds were found to display antifungal activity.

Ming Zhang Gao; Jian Gao; Zun Le Xu; Ralph A. Zingaro



Antibacterial and Antifungal Activities of Nitroxoline Mannich Bases  

Microsoft Academic Search

The in vitro activity of nitroxoline and its Mannich bases against bacteria and fungi was investigated. Nitroxoline and its derivative with diisopropylamine as an amino component, exhibited the highest antimicrobial activity. The optimum hydro\\/lipophilic properties (log P), both for antibacterial and antifungal activity, are about log P values of 2. The least effective compound was this nitroxoline Mannich base which

D. Maysinger; M. Movrin



[In vitro antifungal activity of nitroxoline. Preliminary clinical results].  


Nitroxoline is an oxyquinoline derivative with a large antifungical activity. The fungistatic activity of nitroxoline is greater against Candida albicans than against Torulopsis glabrata, Candida tropicalis and Candida krusei. The MIC are compatible with urinary concentrations of nitroxoline. These preliminary clinical results favor the use of nitroxoline in the management of fungal urinary tract infections. PMID:3309833

Cancet, B; Amgar, A



Antibacterial and antifungal activity of Syzygium jambolanum seeds  

Microsoft Academic Search

The water and methanolic extracts of Syzygium jambolanum seeds were examined for antibacterial and antifungal activity in vitro using the disc diffusion method, minimum inhibitory concentration, minimum bactericidal concentration and minimum fungicidal concentration. Activity against gram positive bacteria (Bacillus subtilis, Staphylococcus aureus), gram negative bacteria (Salmonella typhimurium, Pseudomonas aeruginosa, Klebsiella pneumoniae and Escherichia coli) and fungal strains (Candida albicans, Cryptococcus

M Chandrasekaran; V Venkatesalu



Effect of Antifungal Compounds on Aspergillosis in Hatching Chick Embryos  

PubMed Central

Aspergillosis was induced experimentally in hatching chick embryos by dipping them in water containing spores of Aspergillus fumigatus or A. flavus. The addition to the dip water of antifungal compounds prevented the development of this syndrome. Of the compounds studied, amphotericin B was most effective, followed by pimaricin and nystatin. Sorbic acid was without effect.

Huhtanen, C. N.; Pensack, J. M.



Invasive fungal infection — laboratory diagnosis and antifungal treatment  

Microsoft Academic Search

Invasive fungal infections (IFIs) have become increasingly prevalent in the recent decade along with the increasing populations of immunocompromised patients and widespread use of the broad-spectrum antibiotics. The morbidity and the mortality of IFIs remain high while the diagnosis and treatment of IFIs are highly challenging. Recent advances in diagnostic methods and antifungal agents provide the potential to improve the

Pei-Lan Shao; Li-Min Huang; Po-Ren Hsueh



In Vitro Interactions between Antifungals and Immunosuppressive Drugs against Zygomycetes  

Microsoft Academic Search

The in vitro interaction of antifungals with immunosuppressive drugs was evaluated against zygomycetes. The combination of amphotericin B with cyclosporine, rapamycin, or tacrolimus was synergistic for 90%, 70%, and 30% of the isolates, respectively. For posaconazole, itraconazole, and ravuconazole, synergy was more frequently observed with cyclosporine than with rapamycin or tacrolimus and antagonistic interactions were rarely noted. In summary, calcineurin

Eric Dannaoui; Patrick Schwarz; Olivier Lortholary



Topical medications: A focus on antifungals and topical steroids  

Microsoft Academic Search

Because skin disease is accessible, it can be treated with locally applied medication, which offers great advantages-exposure to a drug is limited to the affected skin and systemic effects of potentially toxic drugs are minimized. Ointments, creams, antifungals, and antibiotics all have their place in treating various skin diseases. Topical steroids, the largest group of topical medications, are effective but

Guy F. Webster



10 Non-conventional yeasts in antifungal application  

Microsoft Academic Search

The antimicrobial, and hence antifungal effects of yeast-produced ethanol has been recognised for centuries. Application of yeasts for biocontrol of fungi in agriculture, postharvest technology, forest industry, and food science presents a new area of biotechnology. Biocontrol environments are complex; consequently, there is an enormous diversity among the organisms involved in biocontrol and of inhibition mechanisms. Current genetic approaches focus

Volkmar Passoth; Johan Schnürer


Posaconazole: An extended-spectrum triazole antifungal agent  

Microsoft Academic Search

Background: The incidence of invasive fungal infections (IFIs) caused by opportunistic filamentous molds is increasing, along with emerging fungal resistance. Posaconazole, a structural analogue of itraconazole that was approved for marketing in the United States in 2006, appears to be a promising antifungal agent.Objective: This article provides an overview of the pharmacology, efficacy, and tolerability of posaconazole when used for

Daryl S. Schiller; Horatio B. Fung



Laccase Protects Cryptococcus neoformans from Antifungal Activity of Alveolar Macrophages  

Microsoft Academic Search

While laccase of Cryptococcus neoformans is implicated in the virulence of the organism, our recent studies showing absence of melanin in the infected mouse brain has led us to a search for alternative roles for laccase in cryptococcosis. We investigated the role of laccase in protection of C. neoformans against murine alveolar macrophage (AM)-mediated antifungal activity by using a pair




Antifungal activities of origanum oil against Candida albicans  

Microsoft Academic Search

The antimicrobial properties of volatile aromatic oils from medicinal as well as other edible plants has been recognized since antiquity. Origanum oil, which is used as a food flavoring agent, possesses a broad spectrum of in vitro antimicrobial activities attributed to the high content of phenolic derivatives such as carvacrol and thymol. In the present study, antifungal properties of origanum

Vijaya Manohar; Cass Ingram; Judy Gray; Nadeem A. Talpur; Bobby W. Echard; Debasis Bagchi; Harry G. Preuss



Antifungal activity of Paraguayan plants used in traditional medicine  

Microsoft Academic Search

The antifungal activity of aqueous, dichloromethane and methanol extracts from 14 Paraguayan plants used in traditional medicine for the treatment of skin diseases was assayed in vitro by the agar disk diffusion method against 11 fungal strains comprising several filamentous fungi and yeasts. Among them, the dichloromethane extracts of Acanthospermum australe, Calycophyllum multiflorum, Geophila repens and Tabebuia avellanedae, as well

Aida Portillo; Roser Vila; Blanca Freixa; Tomás Adzet; Salvador Cañigueral



Antibacterial and antifungal activity of pinosylvin, a constituent of pine  

Microsoft Academic Search

The antibacterial and antifungal activities of pinosylvin (3,5-dihydroxy-trans-stilbene), a constituent of pine, were studied and compared with those of resveratrol (3,5,4?-trihydroxy-trans-stilbene). Pinosylvin exhibited more potent growth inhibitory activity against Candida albicans and Saccharomyces cerevisiae.

S. K. Lee; H. J. Lee; H. Y. Min; E. J. Park; K. M. Lee; Y. H. Ahn; Y. J. Cho; J. H. Pyee



Antifungal defenses of seagrasses from the Indian River Lagoon, Florida  

Microsoft Academic Search

We investigated the antifungal chemical defenses and physiological responses of five seagrasses collected from nearshore seagrass beds from the Indian River Lagoon, Florida, against a panel of co-occurring marine fungi isolated from nearby coastal communities. Whole plant tissues from Thalassia testudinum, Halodule wrightii and Syringodium filiforme prevented overgrowth by three of the seven fungi used in this study. Organic extracts

Cliff Ross; Melany P. Puglisi; Valerie J. Paul



Research to Identify Effective Antifungal Agents, 1992 Annual Report.  

SciTech Connect

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

Schreck, Carl



Enhancement of commercial antifungal agents by kojic acid  

Technology Transfer Automated Retrieval System (TEKTRAN)

Kojic acid (KA), a natural by-product of fungal fermentation, is a commonly used food and cosmetic additive. We show that KA increases activity of amphotericin B and strobilurin, medical and agricultural antifungal agents, respectively, possibly targeting the fungal antioxidative system. KA shows pr...


Human Salivary Histatins: Promising AntiFungal Therapeutic Agents  

Microsoft Academic Search

Histatins constitute a group of small, cationic multifunctional proteins present in the saliva of human and some nonhuman primates. The most significant function of histatins may be their anti-fungal activity against Candida albicans and Cryptococcus neoformans. Histatins have been extensively studied at both the protein and gene levels. The structure-function relationship of histatins with respect to their candidacidal activity has

H. Tsai; L. A. Bobek



Antifungal Synergy of Theaflavin and Epicatechin Combinations Against Candida albicans.  


New antifungal agents are required to compensate for the increase in resistance to standard antifungal agents of Candida albicans, which is an important opportunistic fungal pathogen that causes minor infections in many individuals but very serious infections in those who are immune-compromised. In this study, combinations of theaflavin and epicatechin are investigated as potential antifungal agents and also to establish whether antifungal synergy exists between these two readily accessible and cost-effective polyphenols isolated from black and green tea. The results of disc diffusion assays showed stronger antibacterial activity of theaflavin:epicatechin combinations against C. albicans NCTC 3255 and NCTC 3179, than that of theaflavin alone. Minimum inhibitory concentrations (MICs) of 1,024 ?g/ml with theaflavin and 128-256 ?g/ml with theaflavin:epicatechin combinations were found. The fractional inhibitory concentration indexes were calculated, and the synergy between theaflavin and epicatechin against both isolates of C. albicans was confirmed. Theaflavin:epicatechin combinations show real potential for future use as a treatment for infections caused by C. albicans. PMID:23711519

Betts, Jonathan W; Wareham, David W; Haswell, Stephen J; Kelly, Stephen M



Antifungal activity of sodium acetate and Lactobacillus rhamnosus.  


The inhibition of molds by sodium acetate in deMan Rogosa Sharpe (MRS) medium, along with the antifungal activity of Lactobacillus rhamnosus VT1, was studied by the slope agar plate method. MRS agar prepared with and without sodium acetate was used as the agar substrate. A total of 42 strains of Aspergillus, Penicillium, Fusarium, Alternaria, Cladosporium, and Rhizopus were used to compare sensitivities to the inhibitory activity of sodium acetate and L. rhamnosus VT1. It was found that sodium acetate in MRS medium affected the growth of 33 of the 42 mold strains tested to various degrees. The highest sensitivity to sodium acetate was shown by strains of Fusarium, followed by strains of Penicillium, Aspergillus, and Rhizopus. L. rhamnosus VT1 also inhibited mold growth. A significant finding was that sodium acetate and L. rhamnosus VT1 in combination exhibited a possible synergistic action. Thirty-nine of the 42 mold strains tested were completely inhibited by the presence of both antifungal agents. This finding confirms that sodium acetate, a basic component of commercial MRS medium, has strong antifungal properties, and this must be taken into consideration when evaluating the antifungal activity of Lactobacillus cultures grown in MRS broth. PMID:12117257

Stiles, J; Penkar, S; Plocková, M; Chumchalová, J; Bullerman, L B



Characterization of peptidyl-nucleoside antifungal antibiotics from fermentation broth  

Microsoft Academic Search

Summary Characterization of sinefungin related antifungal antibiotics from fermentation broth was accomplished by coupling photodiode array (PDA) detection to high performance liquid chromatography (HPLC). From the combined HPLC-PDA evaluation of broth filtrate, we detected five sinefungin related components. Fast atom bombardment (FAB) mass spectroscopic evaluations, mass-analysed ion kinetic energy spectra (MIKES) and collision activated (CA) MIKES of these components confirmed

Raymond Cooper; Pradip Das; Claire Federbush; Ronald Mierzwa; Mahesh Patel; Birendra Pramanik; Imbi Truumees



Standardization of Antifungal Susceptibility Variables for a Semiautomated Methodology  

Microsoft Academic Search

Recently, the methodology that will serve as a basis of the standard for antifungal susceptibility testing of fermentative yeasts of the European Committee on Antibiotic Susceptibility Testing has been described. This procedure employs a spectrophotometric method for both inoculum adjustment and endpoint determination. However, the utilization of a spectrophotometer requires studies for standardization. The present work analyzes the following parameters:




Evaluation of the antifungal activity and modulation between Cajanus cajan (L.) Millsp. leaves and roots ethanolic extracts and conventional antifungals  

PubMed Central

Background: The use and investigation of natural products with antimicrobial activity from vegeral source have been reported by several researchers. Cajanus cajan (Fabaceae) is a multiple use specie mainly as human food. In popular medicine, diverse parts of the plant are used as sedative and to treat cough, hepatitis, and diabetes. Materials and Methods: This study shows the characterization of secondary metabolites present in ehtanolic extracts from leaves and roots of Cajanus cajan by phytochemical prospection. The evaluation of the antifungal activity was performed by the microdilution method, and from the subinhibitory concentrations (MIC 1/8) the modulatory activity of antifungical (fluconazole and ketoconazole) was analyzed by the direct contact assay against C. albicans ATCC40006, Candida krusei ATCC 6538 and Candida tropicalis ATCC 40042. Results: The results showed the presence of tannins, flavonoids, and alkaloids in both extracts as the clinically relevant antifungal activity. The modulatory potential is presented by the antifungal tested against yeasts. Conclusion: The extracts studied here have demonstrated to be a new therapeutic source to treat these microorganism-associated diseases.

Brito, Samara A.; Rodrigues, Fabiola F. G.; Campos, Adriana R.; da Costa, Jose G. M.



40 CFR 180.443 - Myclobutanil; tolerances for residues.  

Code of Federal Regulations, 2013 CFR

...following food commodities: Commodity Parts per million Almond 0.1 Almond, hulls 2.0 Apple 0.5 Apple, dry pomace 5.0 Apple, wet pomace 5.0 Artichoke, globe 0.90 Asparagus 0.02 Banana, postharvest...



40 CFR 180.443 - Myclobutanil; tolerances for residues.  

Code of Federal Regulations, 2011 CFR

...following food commodities: Commodity Parts per million Almond 0.1 Almond, hulls 2.0 Apple 0.5 Apple, dry pomace 5.0 Apple, wet pomace 5.0 Artichoke, globe 0.90 Asparagus 0.02 Banana, postharvest...



40 CFR 180.443 - Myclobutanil; tolerances for residues.  

Code of Federal Regulations, 2012 CFR

...following food commodities: Commodity Parts per million Almond 0.1 Almond, hulls 2.0 Apple 0.5 Apple, dry pomace 5.0 Apple, wet pomace 5.0 Artichoke, globe 0.90 Asparagus 0.02 Banana, postharvest...



Antifungal effects of citronella oil against Aspergillus niger ATCC 16404.  


Essential oils are aromatic oily liquids obtained from some aromatic plant materials. Certain essential oils such as citronella oil contain antifungal activity, but the antifungal effect is still unknown. In this study, we explored the antifungal effect of citronella oil with Aspergillus niger ATCC 16404. The antifungal activity of citronella oil on conidia of A. niger was determined by poisoned food technique, broth dilution method, and disc volatility method. Experimental results indicated that the citronella oil has strong antifungal activity: 0.125 (v/v) and 0.25 % (v/v) citronella oil inhibited the growth of 5?×?10? spore/ml conidia separately for 7 and 28 days while 0.5 % (v/v) citronella oil could completely kill the conidia of 5?×?10? spore/ml. Moreover, the fungicidal kinetic curves revealed that more than 90 % conidia (initial concentration is 5?×?10? spore/ml) were killed in all the treatments with 0.125 to 2 % citronella oil after 24 h. Furthermore, with increase of citronella oil concentration and treatment time, the antifungal activity was increased correspondingly. The 0.5 % (v/v) concentration of citronella oil was a threshold to kill the conidia thoroughly. The surviving conidia treated with 0.5 to 2 % citronella oil decreased by an order of magnitude every day, and no fungus survived after 10 days. With light microscope, scanning electron microscope, and transmission electron microscope, we found that citronella oil could lead to irreversible alteration of the hyphae and conidia. Based on our observation, we hypothesized that the citronella oil destroyed the cell wall of the A. niger hyphae, passed through the cell membrane, penetrated into the cytoplasm, and acted on the main organelles. Subsequently, the hyphae was collapsed and squashed due to large cytoplasm loss, and the organelles were severely destroyed. Similarly, citronella oil could lead to the rupture of hard cell wall and then act on the sporoplasm to kill the conidia. Nevertheless, the citronella oil provides a potential of being a safe and environmentally friendly fungicide in the future. PMID:23081773

Li, Wen-Ru; Shi, Qing-Shan; Ouyang, You-Sheng; Chen, Yi-Ben; Duan, Shun-Shan



Conventional and alternative antifungal therapies to oral candidiasis  

PubMed Central

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

Anibal, Paula Cristina; de Cassia Orlandi Sardi, Janaina; Peixoto, Iza Teixeira Alves; de Carvalho Moraes, Julianna Joanna; Hofling, Jose Francisco



Screening for Antibacterial, Antifungal, and Anti quorum Sensing Activity.  


The plate-hole diffusion assay is an invaluable screening tool to evaluate the antibacterial potential of natural products. It relies on the diffusion of test material from pre-cut wells through agar seeded with bacteria. Samples that are capable of inhibiting bacterial growth will produce a clear zone surrounding their well. For the evaluation of antifungal activity of natural products, we describe the broth microdilution method. This assay is performed using a 96 well microtiter tray containing fungal inoculum, test medium and natural product material. Samples demonstrating antifungal activity will prevent any discernible growth as detected visually. A disk diffusion assay, utilizing the pigmented indicator strain Chromobacterium violaceum, is described here for the screening of natural products for anti quorum sensing activity. Inhibition of quorum sensing results in growth of non-pigmented bacteria. PMID:23963914

Hayhoe, Elisa J; Palombo, Enzo A



Antifungal metabolites from fungal endophytes of Pinus strobus.  


The extracts of five foliar fungal endophytes isolated from Pinus strobus (eastern white pine) that showed antifungal activity in disc diffusion assays were selected for further study. From these strains, the aliphatic polyketide compound 1 and three related sesquiterpenes 2-4 were isolated and characterized. Compound 2 is reported for the first time as a natural product and the E/Z conformational isomers 3 and 4 were hitherto unknown. Additionally, the three known macrolides; pyrenophorol (5), dihydropyrenophorin (6), and pyrenophorin (7) were isolated and identified. Their structures were elucidated by spectroscopic analyses including 2D NMR, HRMS and by comparison to literature data where available. The isolated compounds 1, 2, and 5 were antifungal against both the rust Microbotryum violaceum and Saccharomyces cerevisae. PMID:21632082

Sumarah, Mark W; Kesting, Julie R; Sørensen, Dan; Miller, J David



Antifungal activity of biflavones from Taxus baccata and Ginkgo biloba.  


Bilobetin and 4'''-O-methylamentoflavone were isolated and identified in the needles of Taxus baccata, for the first time in this species. The antifungal activity of biflavones from T. baccata and Ginkgo biloba, namely amentoflavone, 7-O-methylamentoflavone, bilobetin, ginkgetin, sciadopitysin and 2,3-dihydrosciadopitysin towards the fungi Alternaria alternata, Fusarium culmorum, Cladosporium oxysporum was determined employing computer-aided image analysis couplet to a microscope. Bilobetin exhibited a significant antifungal activity with values of ED50 14, 11 and 17 microM respectively. This compound completely inhibited the growth of germinating tubes of Cladosporium oxysporum and Fusarium culmorum at a concentration 100 microM. Activity of ginkgetin and 7-O-methylamentoflavone towards Alternaria alternata was stronger than that of bilobetin. Moreover, slight structural changes in the cell wall of Alternaria alternata exposed to ginkgetin at concentration of 200 microM were observed. PMID:12622229

Krauze-Baranowska, Miros?awa; Wiwart, Marian


C-type lectin receptors orchestrate antifungal immunity.  


Fungal infections are an emerging threat for human health. A coordinated host immune response is fundamental for successful elimination of an invading fungal microbe. A panel of C-type lectin receptors expressed on antigen-presenting dendritic cells enable innate recognition of fungal cell wall carbohydrates and tailors adaptive responses via the instruction of CD4? T helper cell fates. Well-balanced T helper cell type 1 and IL-17-producing T helper cell responses are crucial in antifungal immunity and facilitate phagocytic clearance of fungal encounters. Strikingly, different classes of fungi trigger distinct sets of C-type lectin receptors to evoke a pathogen-specific T helper response. In this review, we outline the key roles of several C-type lectin receptors during the generation of protective antifungal immunity, with particular emphasis on the distinct signaling pathways and transcriptional programs triggered by these receptors, which collaborate to orchestrate polarization of the T helper response. PMID:23841632

Wevers, Brigitte A; Geijtenbeek, Teunis B H; Gringhuis, Sonja I



Antifungal activities of crude extracts of Mitracarpus villosus (Rubiaceae).  


Extracts of Mitracarpus villosus leaves and inflorescences were investigated individually for in vitro antifungal activities by agar-diffusion and tube-dilution techniques. Ethanolic extracts produced definite antifungal activities against Trichophyton rubrum, Microsporum gypseum, Candida albicans, Aspergillus niger and Fusarium solani. The aqueous extracts and the glycerol vehicle control did not inhibit any of the fungi tested. The zones of inhibition produced by the ethanol extracts ranged from 10 to 20.5 mm while ketoconazole control ranged from 9 to 19 mm. The minimum inhibitory concentration of the extracts ranged from 0.50 to 4.0 mg/ml while their minimum fungicidal concentration values ranged from 1 to 8 mg/ml. These results indicate that the extracts were fungistatic at lower concentrations and fungicidal at higher concentrations. PMID:8133654

Irobi, O N; Daramola, S O



Antifungal activity of Paraguayan plants used in traditional medicine.  


The antifungal activity of aqueous, dichloromethane and methanol extracts from 14 Paraguayan plants used in traditional medicine for the treatment of skin diseases was assayed in vitro by the agar disk diffusion method against 11 fungal strains comprising several filamentous fungi and yeasts. Among them, the dichloromethane extracts of Acanthospermum australe, Calycophyllum multiflorum, Geophila repens and Tabebuia avellanedae, as well as the aqueous and methanol extracts of the latter, showed the highest activity. PMID:11378288

Portillo, A; Vila, R; Freixa, B; Adzet, T; Cañigueral, S



Experimental evaluation of antifungal and antiseptic agents against Rhodotorula spp.  


We studied the susceptibility of 21 strains of Rhodotorula rubra and nine strains of R. glutinis to eight antifungals and tested eight antiseptic agents on one strain of R. rubra. The tested strains were susceptible to ketoconazole, 5-fluorocytosine, amphotericin B, and nystatin, intermediate to econazole and resistant to fluconazole, itraconazole and miconazole. After 5-min contact, six of the eight antiseptic agents tested showed a fungicidal activity on the tested R. rubra strain. PMID:14641623

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



First total synthesis of the antifungal antibiotic thiobutacin  

Microsoft Academic Search

The first total synthesis of thiobutacin, a butanoic acid with antifungal activity recently isolated from the culture broth of a soil actinomycete, Lechevalieria aerocolonigenes strain VK-A9, is described. The five-step procedure involves readily available and cheap starting materials and can easily be transposed to the large scale. Fungal growth inhibition of thiobutacin is mediated by the pH of the growth

Narayan Chakor; Sabrina Dallavalle; Loana Musso; Maddalena Moretti



Antifungal Textiles Formed Using Silver Deposition in Supercritical Carbon Dioxide  

Microsoft Academic Search

The antifungal properties of two silver-coated natural cotton fiber structures prepared using a supercritical carbon dioxide (scCO2) solvent were examined. Scanning electron microscopy confirmed that the scCO2 process may be used to produce cotton fiber textiles with uniform silver nanoparticle coatings. A version of the Kirby-Bauer disk diffusion test was used to assess the ability of these textiles to inhibit

Shaun D. Gittard; Daisuke Hojo; G. Kevin Hyde; Giovanna Scarel; Roger J. Narayan; Gregory N. Parsons



Antifungal Textiles Formed Using Silver Deposition in Supercritical Carbon Dioxide  

Microsoft Academic Search

The antifungal properties of two silver-coated natural cotton fiber structures prepared using a supercritical carbon dioxide\\u000a (scCO2) solvent were examined. Scanning electron microscopy confirmed that the scCO2 process may be used to produce cotton fiber textiles with uniform silver nanoparticle coatings. A version of the Kirby-Bauer\\u000a disk diffusion test was used to assess the ability of these textiles to inhibit

Shaun D. Gittard; Daisuke Hojo; G. Kevin Hyde; Giovanna Scarel; Roger J. Narayan; Gregory N. Parsons



Antifungal activity of tuberose absolute and some of its constituents.  


The antifungal activity of the absolute of tuberose (Polianthes tuberosa ) and some of its constituents were evaluated against the mycelial growth of Colletotrichum gloeosporioides on potato-dextrose-agar medium. Tuberose absolute showed only mild activity at a concentration of 500 mg/L. However, three constituents present in the absolute, namely geraniol, indole and methyl anthranilate exhibited significant activity showing total inhibition of the mycelial growth at this concentration. PMID:16106389

Nidiry, Eugene Sebastian J; Babu, C S Bujji



Synthesis and antifungal activity of organofluorine derivatives of levorin  

Microsoft Academic Search

Reactions of the polyene macrolide antibiotic levorin with organofluorine alcohols lead to the formation of organofluorine\\u000a esters. Two organofluorine derivatives of levorin have been synthesized and their physicochemical and biological properties\\u000a have been studied. These derivatives show high antifungal activity against a large number of test cultures. The acute toxicity\\u000a (LD50) of levorin derivatives was about half that of the

V. V. Belakhov; Yu. D. Shenin; R. A. Araviisky



Screening of terrestrial and freshwater halotolerant cyanobacteria for antifungal activities  

Microsoft Academic Search

Cyanobacterial cultures tolerating 200 mmol l?1 sodium chloride isolated from terrestrial and freshwater habitats of North Maharashtra region of India were evaluated for\\u000a antifungal activity. Aqueous, methanol, n-propanol, and petroleum ether extracts of 40 cyanobacterial isolates belonging to nine genera were examined for inhibitory\\u000a activity against five fungal pathogens. Eighteen isolates belonging to genus Oscillatoria dominated the population of halotolerant cyanobacterial cultures.

Sunil T. Pawar; Pravin R. Puranik



Capillary zone electrophoretic separation and determination of imidazolic antifungal drugs  

Microsoft Academic Search

Capillary zone electrophoresis (CZE) was adapted to the simultaneous determination of a mixture of three imidazolic antifungal drugs. Separation was achieved by using a fused-silica capillary column with an acetic acid–Tris buffer at pH 5.18 and UV detection at 196 nm. Several electrophoretic parameters were investigated: pH and buffer concentration, applied voltage, temperature and injection conditions. The optimized CZE method

Adela Arranz; Camilo Echevarr??a; Jose Mar??a Moreda; Adolfo Cid; Juan Francisco Arranz



Antibacterial and antifungal activities of nitroxoline Mannich bases.  


The in vitro activity of nitroxoline and its Mannich bases against bacteria and fungi was investigated. Nitroxoline and its derivative with diisopropylamine as an amino component, exhibited the highest antimicrobial activity. The optimum hydro/lipophilic properties (log P), both for antibacterial and antifungal activity, are about log P values of 2. The least effective compound was this nitroxoline Mannich base which has diethanolamine as an amino component. PMID:6771105

Medi?-Sari?, M; Maysinger, D; Movrin, M; Dvorzak, I



Colorimetric Assay for Antifungal Susceptibility Testing of Aspergillus Species  

Microsoft Academic Search

A colorimetric assay for antifungal susceptibility testing of Aspergillus species (Aspergillus fumigatus, Asper- gillus flavus, Aspergillus terreus, Aspergillus nidulans, and Aspergillus ustus) is described based on the reduction of the tetrazolium salt 2,3-bis(2-methoxy-4-nitro-5-((sulphenylamino)carbonyl)-2H-tetrazolium-hydroxide (XTT) in the presence of menadione as an electron-coupling agent. The combination of 200 g of XTT\\/ml with 25 M menadione resulted in a high production of




Antifungal drug resistance in molds: Clinical and microbiological factors  

Microsoft Academic Search

The incidence of fungal infections has increased over the past decade. In addition to classical pathogens, such as Aspergillus spp, new fungal species are increasingly reported. Despite the availability of new antifungals, mortality of invasive fungal\\u000a infections remains very high. The host immune status is the main factor for survival. However, most of these pathogens have\\u000a high minimum inhibitory concentrations

Laura Alcazar-Fuoli; Juan L. Rodríguez-Tudela; Emilia Mellado



Antifungal activity of cucumber ?-1,3-glucanase and chitinase  

Microsoft Academic Search

An acidic ?-1,3-glucanase and three isoforms of chitinase (A, B, C) were isolated and purified from cucumber (Cucumis sativusL.) leaves inoculated with a necrogenic fungus,Colletotrichum lagenarium. Tests of antifungal activity toC. lagenarium in vitrowere conducted with the purified ?-1,3-glucanase, the three purified isoforms of chitinase and with intercellular wash fluids (ICF) from cucumber leaves above those inoculated withC. lagenariumor those

C. Ji; J. Ku?



Persistence of histoplasma in adrenals 7 years after antifungal therapy.  


Adrenal histoplasmosis is an uncommon cause for adrenal insufficiency. The duration of treatment for adrenal histoplasmosis is not clear. Existing treatment regimens advocate antifungals given for periods ranging from 6 months to 2 years. We report here a rare case who showed persistence of histoplasma in adrenal biopsy 7 years after being initially treated with itraconazole for 9 months. This calls for a prolonged therapy with regular review of adrenal morphology and histology in these patients. PMID:23869317

Kothari, Deepak; Chopra, Shweta; Bhardwaj, Minakshi; Ajmani, Ajay K; Kulshreshtha, Bindu



Persistence of histoplasma in adrenals 7 years after antifungal therapy  

PubMed Central

Adrenal histoplasmosis is an uncommon cause for adrenal insufficiency. The duration of treatment for adrenal histoplasmosis is not clear. Existing treatment regimens advocate antifungals given for periods ranging from 6 months to 2 years. We report here a rare case who showed persistence of histoplasma in adrenal biopsy 7 years after being initially treated with itraconazole for 9 months. This calls for a prolonged therapy with regular review of adrenal morphology and histology in these patients.

Kothari, Deepak; Chopra, Shweta; Bhardwaj, Minakshi; Ajmani, Ajay K.; Kulshreshtha, Bindu



Antioxidant and Antifungal Activity of Verbena officinalis L. Leaves  

Microsoft Academic Search

The scavenging activity against DPPH (1,1-diphenil-2-picrylhydrazyl) radical and the antifungal effect against chloroform,\\u000a ethyl acetate and 50% methanolic extracts of Verbena officinalis leaves were investigated. The activity of different fractions of 50% methanolic extract and some isolated compounds were\\u000a also investigated. The results suggest that 50% methanolic extract and caffeoyl derivatives could potentially be considered\\u000a as excellent and readily available

E. Casanova; J. M. García-Mina; M. I. Calvo



Interaction of Common Azole Antifungals with P Glycoprotein  

Microsoft Academic Search

Both eucaryotic and procaryotic cells are resistant to a large number of antibiotics because of the activities of export transporters. The most studied transporter in the mammalian ATP-binding cassette transporter superfamily, P glycoprotein (P-gp), ejects many structurally unrelated amphiphilic and lipophilic xenobiotics. Observed clinical interactions and some in vitro studies suggest that azole antifungals may interact with P-gp. Such an

Er-jia Wang; Karen Lew; Christopher N. Casciano; Robert P. Clement; William W. Johnson



Antifungal constituents isolated from the seeds of Aegle marmelos.  


Antifungal constituents, 2-isopropenyl-4-methyl-1-oxa-cyclopenta[b]anthracene-5,10-dione and (+)-4-(2'-hydroxy-3'-methylbut-3'-enyloxy)-8H-[1,3]dioxolo[4,5-h]chromen-8-one in addition to known compounds imperatorin, beta-sitosterol, plumbagin, 1-methyl-2-(3'-methyl-but-2'-enyloxy)-anthraquinone, beta-sitosterol glucoside, stigmasterol, vanillin and salicin were isolated during phytochemical investigation on seeds of Aegle marmelos Correa. PMID:19913858

Mishra, Bhuwan B; Singh, Desh D; Kishore, Navneet; Tiwari, Vinod K; Tripathi, Vyasji



2-Aminobenzothiazole derivatives: search for new antifungal agents.  


A new series of 6-substituted 2-aminobenzothiazole derivatives were synthesized and screened in vitro as potential antimicrobials. Almost all the compounds showed antifungal activity. In particular, compounds 1n,o, designed on the basis of molecular modeling studies, were the best of the series, showing MIC values of 4-8 ?g/mL against Candida albicans, Candida parapsilosis and Candida tropicalis. None of the two compounds did show any cytotoxicity effect on human THP-1 cells. PMID:23644218

Catalano, Alessia; Carocci, Alessia; Defrenza, Ivana; Muraglia, Marilena; Carrieri, Antonio; Van Bambeke, Françoise; Rosato, Antonio; Corbo, Filomena; Franchini, Carlo



Antifungal activities of actinomycete strains associated with high-altitude sagebrush rhizosphere  

Microsoft Academic Search

The antifungal-producing potential of actinomycete populations from the rhizosphere of low-altitude sagebrush, Artemisia tridentata, has been examined. In a continued investigation of new sources of antifungal-producing microorganisms, this study examined\\u000a the antifungal-producing potential of actinomycetes from the rhizosphere of high-altitude A. tridentata. With high-altitude sagebrush, rhizosphere soil actinomycete numbers were one to four orders of magnitude higher than those\\u000a found

A. E. Jiménez-Esquilín; T. M. Roane



The Role of Preformed Antifungal Substances in the Resistance of Fruits to Postharvest Pathogens  

Microsoft Academic Search

\\u000a Plants contain secondary metabolites with antifungal properties. In fruits they are mostly concentrated in the peel at immature\\u000a stage and decline during ripening in coincidence with fungal rot development. The information on antifungal systems in immature\\u000a avocado and mango, reviewed here, suggests that they play a role in natural disease resistance. Immature mangoes have evolved\\u000a a formidable antifungal system comprising

Nimal Adikaram; Chathurika Karunanayake; Charmalie Abayasekara


Isolation and biochemical characterization of a novel leguminous defense peptide with antifungal and antiproliferative potency  

Microsoft Academic Search

Leguminous plants have formed a popular subject of research owing to the abundance of proteins and peptides with important\\u000a biological activities that they produce. The antifungal proteins and peptides have been purified from a number of leguminous\\u000a species. However, research continues to discover novel antifungal plant-produced peptides and proteins are being needed, specially\\u000a those novel ones with both antifungal activity

Shaoyun Wang; Pingfan Rao; Xiuyun Ye



Antifungal activity of itraconazole and terbinafine in human stratum corneum: A comparative study  

Microsoft Academic Search

Background: The evaluation of antifungal agents by in vitro and animal experiments cannot predict clinical efficacy with certainty. New models are needed to assess and compare antifungal activity.Objective: We compared on human stratum corneum ex vivo the antifungal activity and lingering effect of 200 mg itraconazole daily and twice daily, and 250 mg\\/day terbinafine.Methods: Three groups of 10 healthy volunteers

G. E Piérard; J. E Arrese; P De Doncker



Synthesis and antifungal activity of thiadiazole-functionalized chitosan derivatives.  


A groups of novel water soluble chitosan derivatives containing 1,3,4-thiadiazole group were synthesized including 1,3,4-thiadiazole (TPCTS), 2-methyl-1,3,4-thiadiazole (MTPCTS), and 2-phenyl-1,3,4-thiadiazole (PTPCTS). Their antifungal activity against three kinds of phytopathogens was estimated by hypha measurement in vitro, and the fungicidal assessment shows that the synthesized chitosan derivatives have excellent activity against tested fungi. Of all the synthesized chitosan derivatives, MTPCTS inhibited the growth of the tested phytopathogens most effectively with inhibitory indices of 75.3%, 82.5%, and 65.8% against Colletotrichum lagenarium (Pass) halst, Phomopsis asparagi (Sacc.) Bubak, and Monilinia fructicola (Wint.) Honey respectively at 1.0 mg/mL. These indices are higher than those of chitosan. These data also demonstrate that the hydrophobic moiety (alkyl and phenyl) and the length of alkyl substituent in thiadiazole tend to affect the antifungal activity of chitosan derivatives. It is hypothesized that thiadiazole groups enable the synthesized chitosan to possess obviously better antifungal activity and good solubility in water. PMID:23624516

Li, Qing; Ren, Jianming; Dong, Fang; Feng, Yan; Gu, Guodong; Guo, Zhanyong



Synthesis, in vitro antifungal evaluation and in silico study of 3-azolyl-4-chromanone phenylhydrazones  

PubMed Central

Background The currently available antifungal drugs suffer from toxicity, greatest potential drug interactions with other drugs, insufficient pharmacokinetics properties, and development of resistance. Thus, development of new antifungal agents with optimum pharmacokinetics and less toxicity is urgent task. In the search for new azole antifungals, we have been previously described azolylchromanone oxime ethers as rigid analogs of oxiconazole. In continuation of our work, we incorporated phenylhydrazone moiety instead of oxime ether fragment in azolylchromanone derivatives. Methods The 3-azolyl-4-chromanone phenylhydrazones were synthesized via ring closure of 2-azolyl-2'-hydroxyacetophenones and subsequent reaction with phenylhydrazine. The biological activity of title compounds was evaluated against different pathogenic fungi including Candida albicans, Saccharomyces cerevisiae, Aspergillus niger, and Microsporum gypseum. Docking study, in silico toxicity risks and drug-likeness predictions were used to better define of title compounds as antifungal agents. Results The in vitro antifungal activity of compounds based on MIC values revealed that all compounds showed good antifungal activity against C. albicans, S. cerevisiae and M. gypseum at concentrations less than 16 ?g/mL. Among the test compounds, 2-methyl-3-imidazolyl derivative 3b showed the highest values of drug-likeness and drug-score. Conclusion The 3-azolyl-4-chromanone phenylhydrazones considered as analogs of 3-azolyl-4-chromanone oxime ethers basically designed as antifungal agents. The antifungal activity of title compounds was comparable to that of standard drug fluconazole. The drug-likeness data of synthesized compounds make them promising leads for future development of antifungal agents.



A case of fungal keratitis caused by Scopulariopsis brevicaulis: treatment with antifungal agents and penetrating keratoplasty.  

PubMed Central

A case of fungal keratitis caused by Scopulariopsis brevicaulis following a penetrating eye injury is described. Treatment with antifungal agents and keratoplasty resulted in a favourable outcome. Images

Ragge, N K; Hart, J C; Easty, D L; Tyers, A G



Antifungal therapy in European hospitals: data from the ESAC point-prevalence surveys 2008 and 2009.  


The study aimed to identify targets for quality improvement in antifungal use in European hospitals and determine the variability of such prescribing. Hospitals that participated in the European Surveillance of Antimicrobial Consumption Point Prevalence Surveys (ESAC-PPS) were included. The WHO Anatomical Therapeutic Chemical (ATC) classification for 'antimycotics for systemic use' (J02) 2009 version was used. Demographic data and information about indications and diagnoses were collected in 2008 and 2009. From 99,053 patients, 29,324 (29.6%) received antimicrobials. Antifungals represented 1529 of 40,878 (3.7%) antimicrobials. Antifungals were mainly (54.2%) administered orally. Hospital-acquired infections represented 44.5% of indications for antifungals followed by medical prophylaxis at 31.2%. The site of infection was not defined in 36.0% of cases but the most commonly targeted sites were respiratory (19.2%) and gastrointestinal (18.8%). The most used antifungal was fluconazole (60.5%) followed by caspofungin (10.5%). Antifungal-antibacterial combinations were frequently used (77.5%). The predominance of fluconazole use in participating hospitals could result in an increase in prevalence of inherently resistant fungi, increasing the need for newer antifungals. Although acknowledging that antifungal prophylaxis in the immunocompromised host needs further exploration, repetitive surveys using ESAC-PPS methodology may help to monitor the effects of interventions set to regulate antifungal use. PMID:22827696

Zarb, P; Amadeo, B; Muller, A; Drapier, N; Vankerckhoven, V; Davey, P; Goossens, H



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

PubMed Central

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

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



Antifungal activities of Hedychium essential oils and plant extracts against mycotoxigenic fungi  

Technology Transfer Automated Retrieval System (TEKTRAN)

Plant-derived antifungal compounds are preferred to chemicals to reduce the risk of toxic effects on humans, livestock and the environment. Essential oil extracted from rhizomes and plant extracts of ornamental ginger lily (Hedychium spp.) were evaluated for their antifungal activity against two fu...


Stability of amphotericin B and nystatin in antifungal mouthrinses containing sodium hydrogen carbonate  

Microsoft Academic Search

Amphotericin B and nystatin are two polyene antibiotics that are potent antifungal agents. These drugs are active against most pathogenic fungi like Aspergillus and Candida. Mouthrinses containing these drugs are used for preventive and curative treatment of fungal infections like oral candidiasis, which can cause multiple diseases in cancer patients. Because there were no marketed antifungal mouthrinses available, their preparations

J. Groeschke; I. Solassol; F. Bressolle; F. Pinguet



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

Microsoft Academic Search

Invasive fungal infections are increasing in incidence and are associated with substantial mortality. Improved diagnostics and the availability of new antifungals have revolutionized the field of medical mycology in the past decades. This Review focuses on recent developments in the antifungal pipeline, concentrating on promising candidates such as new azoles, polyenes and echinocandins, as well as agents such as nikkomycin

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



Properties of the chitinase of the antifungal biocontrol agent Streptomyces lydicus WYEC108  

Microsoft Academic Search

An extracellular chitinase from culture filtrates of Streptomyces lydicus WYEC108, a broad spectrum antifungal biocontrol agent, was characterized and purified. Its role in the antifungal activity of this actinomycete was studied. Low constitutive levels of the enzyme were observed when cultures were grown with both simple and complex carbon substrates. The optimal temperature and substrate concentration for maximal chitinase production

Brinda Mahadevan; Don L. Crawford



Control of Preharvest Aflatoxin Contamination in Cotton - Update on New Antifungal Pepetides and Chloroplast Expression  

Technology Transfer Automated Retrieval System (TEKTRAN)

In order to combat the problem of preharvest aflatoxin contamination, we have made many advances using transgenic approaches in our lab. Most notably, we have demonstrated the antifungal activities of transgenic tobacco or cotton plants expressing the antifungal peptide D4E1 or the chloroperoxidase...


In Vitro Antifungal and Fungicidal Spectra of a New Pradimicin Derivative, BMS-181184  

Microsoft Academic Search

A new pradimicin derivative, BMS-181184, was compared with amphotericin B andfluconazole against 249 strains from 35 fungal species to determine its antifungal spectrum. Antifungal testing was performed by the broth macrodilution reference method recommended by the National Committee for Clinical Laboratory Standards (document M27-P, 1992). BMS-181184 MICs for 97% of the 167 strains of Candida spp., Crypto- coccus neoformans, Torulopsis




Isolation and partial characterization of antifungal protein from Bacillus polymyxa strain VLB16  

Microsoft Academic Search

An antifungal protein produced by Bacillus polymyxa strain VLB16 has been purified to homogeneity by ammonium sulfate precipitation and Sephadex-G-200 column chromatography. The purified protein inhibited the growth of Pyricularia grisea and Rhizoctonia solani, the causative agents of rice blast and sheath blight diseases, respectively. Microscopy studies revealed that the antifungal protein caused severe alterations in cell morphogenesis that gave

Saravanakumar Kavitha; Sivanesan Senthilkumar; Samuel Gnanamanickam; Mohammed Inayathullah; Rajadas Jayakumar



Some Antifungal Properties of Sorbic Acid Extracted from Berries of Rowan (Sorbus Aucuparia).  

ERIC Educational Resources Information Center

|The food preservative sorbic acid can be extracted from Eurasian mountain ash berries (commercially available) and used to show antifungal properties in microbiological investigations. Techniques for extraction, purification, ultraviolet analysis, and experiments displaying antifungal activity are described. A systematic search for similar…

Brunner, Ulrich



Antifungal activity of plant extracts against Arthrinium sacchari and Chaetomium funicola  

Microsoft Academic Search

Various plant extracts were examined for antifungal activity with the objective of improving the commercial sterility of aseptically filled tea beverage products in PET bottles. When the hot water extract and the methanol extract of 29 samples were measured for their antifungal activity against Arthrinium sacchari M001 and Chaetomium funicola M002 strains, five samples, Acer nikoense, Glycyrrhiza glabra, Lagerstroemia speciosa,

Jun Sato; Keiichi Goto; Fumio Nanjo; Shigeyuki Kawai; Kousaku Murata



The Antifungal Protein AFP from Aspergillus giganteus Inhibits Chitin Synthesis in Sensitive Fungi  

Microsoft Academic Search

The antifungal protein AFP from Aspergillus giganteus is highly effective in restricting the growth of major human- and plant-pathogenic filamentous fungi. However, a fundamental prerequisite for the use of AFP as an antifungal drug is a complete understanding of its mode of action. In this study, we performed several analyses focusing on the assumption that the chitin biosynthesis of sensitive

Silke Hagen; Florentine Marx; Arthur F. Ram; Vera Meyer



Efficacy and safety of topical antifungals in the treatment of dermatomycosis: a systematic review.  


The analysis of comparative efficacy and safety of topical antifungals in the literature is restricted to the treatment of tinea pedis and onychomycosis. Therefore our objective was to evaluate and compare the efficacy and safety of topical antifungals used in the treatment of dermatomycosis, we performed a comprehensive search for randomized controlled trials (RCTs) in the following databases: Medline, Cochrane Central Register of Controlled Trials, EMBASE, Lilacs and International Pharmaceutical Abstracts, we identified studies that compared the use of topical antifungals with other antifungals or with placebo published up to July 2010 in English, Spanish or Portuguese. The quality of reporting was assessed according to the Jadad scale; only studies with a score of 3 or more were included. The outcomes evaluated were mycological cure at the end of treatment, sustained cure, occurrence of adverse events and tolerability, including withdrawals due to adverse events. A total of 104 RCTs satisfied the inclusion criteria, containing a total of 135 comparisons, with 55 out of 120 possible comparisons among the 16 drugs evaluated. Pooled data on efficacy showed that all the antifungals were better than placebo. There were no significant differences among antifungal classes. No differences were found in safety or tolerability in any direct comparison. Sensitivity analysis indicated the robustness of the findings. Our results indicate the clear superiority of topical antifungals over placebo but that there is no consistent difference among classes. Mixed treatment comparisons are necessary to rank antifungals, as direct comparisons among many of them are lacking. PMID:22233283

Rotta, I; Sanchez, A; Gonçalves, P R; Otuki, M F; Correr, C J



Selection of antifungal protein-producing molds from dry-cured meat products  

Microsoft Academic Search

To control unwanted molds in dry-cured meats it is necessary to allow the fungal development essential for the desired characteristics of the final product. Molds producing antifungal proteins could be useful to prevent hazards due to the growth of mycotoxigenic molds. The objective has been to select Penicillium spp. that produce antifungal proteins against toxigenic molds. To obtain strains adapted

Raquel Acosta; Andrea Rodríguez-Martín; Alberto Martín; Félix Núñez; Miguel A. Asensio



Antifungal activity of the essential oil from Calendula officinalis L. (asteraceae) growing in Brazil  

PubMed Central

This study tested in vitro activity of the essential oil from flowers of Calendula officinalis using disk-diffusion techniques. The antifungal assay results showed for the first time that the essential oil has good potential antifungal activity: it was effective against all 23 clinical fungi strains tested.

Gazim, Zilda Cristiane; Rezende, Claudia Moraes; Fraga, Sandra Regina; Svidzinski, Terezinha Inez Estivaleti; Cortez, Diogenes Aparicio Garcia



Characteristics and antifungal activity of a chitin binding protein from Ginkgo biloba  

Microsoft Academic Search

An antifungal peptide from leaves of Ginkgo biloba, designated GAFP, has been isolated. Its molecular mass of 4244.0 Da was determined by mass spectrometry. The complete amino acid sequence was obtained from automated Edman degradation. GAFP exhibited antifungal activity towards Pellicularia sasakii Ito, Alternaria alternata (Fries) Keissler, Fusarium graminearum Schw. and Fusarium moniliforme. Its activities differed among various fungi. GAFP

Xu Huang; Wei-jun Xie; Zhen-zhen Gong



Broad and complex antifungal activity among environmental isolates of lactic acid bacteria  

Microsoft Academic Search

More than 1200 isolates of lactic acid bacteria isolated from different environments were screened for antifungal activity in a dual-culture agar plate assay. Approximately 10% of the isolates showed inhibitory activity and 4% showed strong activity against the indicator mould Aspergillus fumigatus. The antifungal spectra for 37 isolates with strong activity and five isolates with low or no activity were

Jesper Magnusson; Katrin Ström; Stefan Roos; Jörgen Sjögren; Johan Schnürer



Activity of the Triazole Antifungal R126638 as Assessed by Corneofungimetry  

Microsoft Academic Search

Background: R126638 is a novel triazole exhibiting potent in vitro and in vivo antifungal activity against fungal pathogens including dermatophytes and yeasts. Objective: To determine the antifungal activity in time in the stratum corneum of healthy volunteers after oral intake of R126638 at a daily dose of 100 or 200 mg for 1 week. Method: Sixteen male volunteers were randomly

C. Piérard-Franchimont; J. Ausma; L. Wouters; V. Vroome; L. Vandeplassche; M. Borgers; G. Cauwenbergh; G. E. Piérard



Production of antifungal substance by Lactococcus lactis subsp. lactis CHD28.3  

Microsoft Academic Search

Six of the 2100 colonies of lactic acid bacteria isolated from 4 month old Cheddar cheese and raw buffalo milk showed antifungal activity against Aspergillus flavus IARI when tested by the well agar diffusion assay on Potato Dextrose Agar containing 0.1% Triton X-100. Out of these, the most promising isolate having a broad spectrum of antifungal activity including Aspergillus flavus

Utpal Roy; V. K. Batish; S. Grover; S. Neelakantan



Antifungal Activities of Natural and Synthetic Iron Chelators Alone and in Combination with Azole and Polyene Antibiotics against Aspergillus fumigatus  

Microsoft Academic Search

Antifungal effects of iron chelators (lactoferrin, deferoxamine, deferiprone, and ciclopirox) were tested alone and in combination with antifungal drugs against Aspergillus fumigatus B5233 conidia. Lactoferrin, ciclopirox, and deferiprone inhibited whereas deferoxamine enhanced fungal growth. Antifungal synergy against conidia was observed for combinations of ketoconazole with ciclopirox or deferiprone, lactoferrin with amphotericin B, and fluconazole with deferiprone. Iron chelation alone or

Kol A. Zarember; Anna R. Cruz; Chiung-Yu Huang; John I. Gallin



Actinomycetes Antagonizing Plant and Human Pathogenic Fungi. II. Factors Affecting Antifungal Production and Chemical Characterization of the Active Components  

Microsoft Academic Search

A study was carried out to investigate the factors affecting the antifungal production of four actinomycetes species i.e. Streptomyces lydicus, S. ederensis, S. erumpens and S. antimycoticus. Glycerol was the best carbon source for antifungal production by the selected species followed by starch. Glutamic acid was found to be the best nitrogen source for antifungal production by S. lydicus and



Production and Characterization of Antifungal Compounds Produced by Lactobacillus plantarum IMAU10014  

PubMed Central

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.

Wang, HaiKuan; Yan, YanHua; Wang, JiaMing; Zhang, HePing; Qi, Wei



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


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. PMID:12701377

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



Correlation of antifungal susceptibility and molecular type within the Cryptococcus neoformans/C. gattii species complex.  


Members of the Cryptococcus neoformans/C. gattii species complex are grouped into eight molecular types, differing in their epidemiology, disease severity and geographic range. Recent in vitro antifungal susceptibility studies of isolates of the complex revealed contradictory results. The objective of the present study was to assess if this variation is random or correlates with different molecular types by testing the in vitro antifungal susceptibility of 18 C. neoformans (VNI), 11 C. gattii (VGI) and 38 C. gattii (VGII) strains from Brazil to eight antifungal drugs using the CLSI microdilution method. We herein report that the molecular type VGII is the least susceptible genotype, followed by VGI and VNI. This indicates a clear correlation between antifungal susceptibilities and genotypes of the causative cryptococcosis agents, emphasizing the importance of determining the molecular type as part of the clinical diagnostic process to enable an informed decision as to the most appropriate antifungal treatment. PMID:21859388

Trilles, Luciana; Meyer, Wieland; Wanke, Bodo; Guarro, Josep; Lazéra, Marcia



Antifungal limonoids from the fruits of Khaya senegalensis.  


Investigation of the fruits of Khaya senegalensis resulted in the isolation of three new mexicanolide limonoids containing a rare conjugated diene lactone system named seneganolide A (1), 2-hydroxyseneganolide A (2) and 2-acetoxyseneganolide A (3). Two known limonoids, 3-deacetyl-7-deacetoxy-7-oxokhivorin (4) and methyl 6-hydroxyangolensate (5), were also found. The structures of the new compounds were elucidated on the basis of spectral methods. The antifungal activity of compounds 1, 3 and 5 was tested against the fungus Botrytis cinerea. PMID:15351110

Abdelgaleil, Samir A M; Iwagawa, Tetsuo; Doe, Matsumi; Nakatani, Munehiro



Mechanism of action of efinaconazole, a novel triazole antifungal agent.  


The mechanism of action of efinaconazole, a new triazole antifungal, was investigated with Trichophyton mentagrophytes and Candida albicans. Efinaconazole dose-dependently decreased ergosterol production and accumulated 4,4-dimethylsterols and 4?-methylsterols at concentrations below its MICs. Efinaconazole induced morphological and ultrastructural changes in T. mentagrophytes hyphae that became more prominent with increasing drug concentrations. In conclusion, the primary mechanism of action of efinaconazole is blockage of ergosterol biosynthesis, presumably through sterol 14?-demethylase inhibition, leading to secondary degenerative changes. PMID:23459486

Tatsumi, Yoshiyuki; Nagashima, Maria; Shibanushi, Toshiyuki; Iwata, Atsushi; Kangawa, Yumi; Inui, Fumie; Siu, William J Jo; Pillai, Radhakrishnan; Nishiyama, Yayoi



Local anaesthetic, antibacterial and antifungal properties of sesquiterpenes from myrrh.  


We extracted, purified and characterized 8 sesquiterpene fractions from Commyphora molmol. In particular, we focused our attention on a mixture of furanodiene-6-one and methoxyfuranoguaia-9-ene-8-one, which showed antibacterial and antifungal activity against standard pathogenic strains of Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Candida albicans, with minimum inhibitory concentrations ranging from 0.18 to 2.8 micrograms/ml. These compounds also had local anaesthetic activity, blocking the inward sodium current of excitable mammalian membranes. PMID:10865454

Dolara, P; Corte, B; Ghelardini, C; Pugliese, A M; Cerbai, E; Menichetti, S; Lo Nostro, A



Antifungal and Antioxidant Activities of Pyrrolidone Thiosemicarbazone Complexes  

PubMed Central

Metal complexes of (Z)-2-(pyrrolidin-2-ylidene)hydrazinecarbothioamide (L) with Cu(II), Co(II), and Ni(II) chlorides were tested against selected types of fungi and were found to have significant antifungal activities. The free-radical-scavenging ability of the metal complexes was determined by their interaction with the stable free radical 2,2??-diphenyl-1-picrylhydrazyl, and all the compounds showed encouraging antioxidant activities. DFT calculations of the Cu complex were performed using molecular structures with optimized geometries. Molecular orbital calculations provide a detailed description of the orbitals, including spatial characteristics, nodal patterns, and the contributions of individual atoms.

Al-Amiery, Ahmed A.; Kadhum, Abdul Amir H.; Mohamad, Abu Bakar



Antifungal activity of fenticonazole in experimental dermatomycosis and candidiasis.  


The antifungal activity of alpha-(2,4-dichlorophenyl)-beta,N-imidazolylethyl 4-phenylthiobenzyl ether nitrate (fenticonazole, Rec 15/1476) in experimental dermatomycosis and candidiasis in guinea pigs was studied. Fenticonazole proved to be a very active drug with a healing capacity generally higher than that of the reference compounds. The adequate range of activity was from 1% to 3%, giving complete healing without relapses in 100% of cases treated. Fenticonazole is presently undergoing further experimental studies and on the basis of our results a clinical trial would therefore seem to be essential. PMID:7199314

Veronese, M; Barzaghi, D; Bertoncini, A



New Polyene Antifungal Antibiotic Produced by a Species of Actinoplanes  

PubMed Central

A new species of Actinoplanes, which has been deposited with the designation NRRL 5325 at the Northern Utilization Research and Development Division of the U. S. Department of Agriculture, produces a polyene antifungal complex designated as Sch 16656. The complex, consisting of one major and three minor components, is isolated from the fermentation broth by a solvent extraction procedure and purified by precipitation methods. The major component is a heptaene and is highly active in vitro and in vivo against Candida albicans. It is active also against strains of Torulopsis and is significantly more potent orally than candicidin in mice against Candida infections. Images

Wagman, G. H.; Testa, R. T.; Patel, M.; Marquez, J. A.; Oden, E. M.; Waitz, J. A.; Weinstein, M. J.



Evaluation of the antifungal potential of Brazilian Cerrado medicinal plants.  


Therapeutic limitations, development of fungal drug resistance, drug-related toxicity, drug interactions and insufficient bioavailability of the currently available antifungal drugs have made the development of drugs necessary that would be able to treat the emerging fungal infections. The Cerrado is the second greater biome of Brazil and it was identified as one of the most distinguished biomes of South America, becoming an important source of innovative vegetal molecules to treat several conditions. Thus, the objective of this study was to evaluate the antifungal potential of Cerrado plants, mainly those used to treat infections and wounds. A total of 57 extracts were screened by the agar-well diffusion technique against Candida albicans and Trichophyton rubrum. The most promising extracts were tested in smaller concentrations and their minimal inhibitory concentrations (MIC) were determined by microdilution method. Results were analysed statistically by anova tests. Extracts of Kielmeyera coriacea, Renealmia alpinia, Stryphnodendron adstringens and Tabebuia caraiba were very active against T. rubrum, presented geometric means of the MIC values between 170.39 and 23.23 microg ml(-1). Extracts of Cerrado plants are of particular interest as source of new agents for the treatment of dermatophytic infections. PMID:19207849

Melo e Silva, Fernanda; de Paula, José Elias; Espindola, Laila Salmen



Structural Basis of Human CYP51 Inhibition by Antifungal Azoles  

SciTech Connect

The obligatory step in sterol biosynthesis in eukaryotes is demethylation of sterol precursors at the C14-position, which is catalyzed by CYP51 (sterol 14-alpha demethylase) in three sequential reactions. In mammals, the final product of the pathway is cholesterol, while important intermediates, meiosis-activating sterols, are produced by CYP51. Three crystal structures of human CYP51, ligand-free and complexed with antifungal drugs ketoconazole and econazole, were determined, allowing analysis of the molecular basis for functional conservation within the CYP51 family. Azole binding occurs mostly through hydrophobic interactions with conservative residues of the active site. The substantial conformational changes in the B{prime} helix and F-G loop regions are induced upon ligand binding, consistent with the membrane nature of the protein and its substrate. The access channel is typical for mammalian sterol-metabolizing P450 enzymes, but is different from that observed in Mycobacterium tuberculosis CYP51. Comparison of the azole-bound structures provides insight into the relative binding affinities of human and bacterial P450 enzymes to ketoconazole and fluconazole, which can be useful for the rational design of antifungal compounds and specific modulators of human CYP51.

Strushkevich, Natallia; Usanov, Sergey A.; Park, Hee-Won (Toronto); (IBC-Belarus)



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


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 activity of chimaphilin was evaluated using the microdilution method with Saccharomyces cerevisiae (0.05mg/mL) and the dandruff-associated fungi Malassezia globosa (0.39mg/mL) and Malassezia restricta (0.55mg/mL). Pronounced antioxidant activity of C. umbellata crude extract was also identified using the DPPH (2,2-diphenyl-1-picrylhydrazyl) assay, suggesting this phytomedicine has an antioxidant function in wound healing. A chemical-genetic profile was completed with chimaphilin using approximately 4700 S. cerevisiae gene deletion mutants. Cellular roles of deleted genes in the most susceptible mutants and secondary assays indicate that the targets for chimaphilin include pathways involved in cell wall biogenesis and transcription. PMID:17950387

Galván, Imelda J; Mir-Rashed, Nadereh; Jessulat, Matthew; Atanya, Monica; Golshani, Ashkan; Durst, Tony; Petit, Philippe; Amiguet, Virginie Treyvaud; Boekhout, Teun; Summerbell, Richard; Cruz, Isabel; Arnason, John T; Smith, Myron L



Lipidome analysis reveals antifungal polyphenol curcumin affects membrane lipid homeostasis  

PubMed Central

This study shows that antifungal curcumin (CUR), significantly depletes ergosterol levels in Candida albicans. CUR while displaying synergy with fluconazole (FLC) lowers ergosterol. However, CUR alone at its synergistic concentration (lower than MIC50), could not affect ergosterol contents. For deeper insight of CUR effects on lipids, we performed high throughput mass spectroscopy (MS) based lipid profiling of C. albicans cells. The lipidome analysis revealed that there were no major changes in PGLs composition following CUR treatment of Candida, however, significant differences in molecular species of PGLs were detected. Among major SPLs, CUR treatment resulted in the reduction of ceramide and accumulation of IPCs levels. The lipidome of CUR treated cells confirmed a dramatic drop in the ergosterol levels with a simultaneous accumulation of its biosynthetic precursors. This was further supported by the fact that the mutants defective in ergosterol biosynthesis (ERG2 and ERG11) and those lacking the transcription factor regulating ergosterol biosynthesis, UPC2, were highly susceptible to CUR. Our study first time shows that CUR, for its antifungal activity, targets and down regulates ?5, 6 desaturase (ERG3) resulting in depletion of ergosterol. This results in parallel accumulation of ergosterol biosynthetic precursors, generation of ROS and cell death.

Sharma, Monika; Dhamgaye, Sanjiveeni; Singh, Ashutosh; Prasad, Rajendra



Antifungal properties of Canavalia ensiformis urease and derived peptides.  


Ureases (EC are metalloenzymes that hydrolyze urea into ammonia and CO(2). These proteins have insecticidal and fungicidal effects not related to their enzymatic activity. The insecticidal activity of urease is mostly dependent on the release of internal peptides after hydrolysis by insect digestive cathepsins. Jaburetox is a recombinant version of one of these peptides, expressed in Escherichia coli. The antifungal activity of ureases in filamentous fungi occurs at submicromolar doses, with damage to the cell membranes. Here we evaluated the toxic effect of Canavalia ensiformis urease (JBU) on different yeast species and carried out studies aiming to identify antifungal domain(s) of JBU. Data showed that toxicity of JBU varied according to the genus and species of yeasts, causing inhibition of proliferation, induction of morphological alterations with formation of pseudohyphae, changes in the transport of H(+) and carbohydrate metabolism, and permeabilization of membranes, which eventually lead to cell death. Hydrolysis of JBU with papain resulted in fungitoxic peptides (~10 kDa), which analyzed by mass spectrometry, revealed the presence of a fragment containing the N-terminal sequence of the entomotoxic peptide Jaburetox. Tests with Jaburetox on yeasts and filamentous fungi indicated a fungitoxic activity similar to ureases. Plant ureases, such as JBU, and its derived peptides, may represent a new alternative to control medically important mycoses as well as phytopathogenic fungi, especially considering their potent activity in the range of 10(-6)-10(-7)M. PMID:22922160

Postal, Melissa; Martinelli, Anne H S; Becker-Ritt, Arlete B; Ligabue-Braun, Rodrigo; Demartini, Diogo R; Ribeiro, Suzanna F F; Pasquali, Giancarlo; Gomes, Valdirene M; Carlini, Celia R



Thymol antifungal mode of action involves telomerase inhibition.  


Abstract The antifungal mode of action of thymol was investigated by a chemical-genetic profile analysis. Growth of each of ˜ 4700 haploid Saccharomyces cerevisiae gene deletion mutants was monitored on medium with a subinhibitory concentration (50 ?g/ml) of thymol and compared to growth on non-thymol control medium. This analysis revealed that, of the 76 deletion mutants with the greatest degree of susceptibility to thymol, 29% had deletions in genes involved in telomere length maintenance. A telomere restriction fragment (TRF) length assay showed that yeast exposed to a subinhibitory concentration of thymol for 15 days had telomere size reductions of 13-20% compared to non-thymol controls. By accelerating telomere shortening, thymol may increase the rate of cell senescence and apoptosis. Furthermore, real-time RT-PCR analysis revealed approximately two-fold reductions in EST2 mRNA but no change in TLC1 RNA in thymol-treated S. cerevisiae relative to untreated cells. EST2 encodes the essential reverse transcriptase subunit of telomerase that uses TLC1 RNA as a template during addition of TG(1-3) repeats to maintain telomere ends. This study provides compelling evidence that a primary mode of thymol antifungal activity is through inhibition of transcription of EST2 and thus telomerase activity. PMID:23718894

Darvishi, Emad; Omidi, Mansoor; Bushehri, Ali Akbar; Golshani, Ashkan; Smith, Myron L



Antifungal prophylaxis in hematopoietic stem cell transplant recipients.  


Efforts at preventing and treating fungal infection in hematopoietic stem cell transplant (HSCT) recipients must take into account the types of infections likely to be encountered during the different risk periods in hosts with different underlying risks. Given the emergence of molds as prevalent pathogens and the long duration of risk in allogeneic HSCT recipients, optimal antifungal prophylaxis would consist of treatment that can be given over a prolonged period and that would provide both anti-Candida and anti-Aspergillus activity. Optimal empiric therapy would consist of a broad-spectrum agent in the absence of more sensitive and specific methods for microbial diagnosis. Fluconazole (Diflucan) is currently the standard prophylactic agent for candidiasis, although mold-active agents and alternative strategies for polyene administration are being investigated. The gold standardfor empiric therapy is currently a polyene antifungal, yet an increased appreciation for amphotericin B-resistant yeasts and molds, and less toxic mold-active alternatives, might lead to the use of other compounds in the future. The recent development of multiple alternatives emphasizes our need to establish treatment algorithms that consider both the likely pathogens and potential toxicities. PMID:11757846

Marr, K A



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


A great number of fungal infections are related to biofilm formation on inert or biological surfaces, which are recalcitrant to most treatments and cause human mortality. Cryptococcus laurentii has been diagnosed as the aetiological pathogen able to cause human infections mainly in immunosuppressed patients and the spectrum of clinical manifestations ranges from skin lesions to fungaemia. The effect of temperature, pH and surface preconditioning on C. laurentii biofilm formation was determined by 2, 3-bis (2-methoxy-4-nitro-5-sulfophenyl)-5-[(phenylamino) carbonyl]-2H-tetrazolium hydroxide (XTT) reduction assay. Scanning electron microscopic (SEM) analysis of C. laurentii biofilms demonstrated surface topographies of profuse growth and dense colonization with extensive polymeric substances around the cells. In this study, we determined the activity of amphotericin B, itraconazole and fluconazole against C. laurentii free-living cells and biofilms. The activity of antifungals tested was greater against free-living cells, but sessile cells fell into the resistant range for these antifungal agents. Extracellular polymeric substances (EPS), comprising the matrix of C. laurentii biofilms, were isolated by ultrasonication. Fourier transform infrared spectroscopy (FT-IR) was performed with ethanol-precipitated and dried samples. Also, the multielement analysis of the EPS was performed by inductively coupled plasma optical emission spectroscopy (ICP-OES). PMID:22936102

Ajesh, K; Sreejith, K



Characterization of the Escherichia coli Antifungal Protein PPEBL21  

PubMed Central

An antifungal protein isolated from Escherichia coli BL21 (PPEBL21) and predicted to be alcohol dehydrogenase (ADH) was subjected to biological characterization. The PPEBL21, indeed, demonstrated propionaldehyde-specific ADH activity. The Km and Vmax of PPEBL21 were found to be 644.8 ?M and 1.2?U/mg, respectively. In-gel activity assay also showed that PPEBL21 was a propionaldehyde-specific ADH. The pI of PPEBL21 was observed to be 7.8. PPEBL21 was found to be stable up to a temperature of 40°C with optimum activity at pH 7.5. The decrease in pH decreased the activity of PPEBL21. These results suggested that PPEBL21 having alcohol dehydrogenase activity and stability at significantly high temperature might be an important lead antifungal molecule. Experiments were performed to identify the possible target of PPEBL21 in the pathogen A. fumigatus. Results revealed that PPEBL21 inhibited completely the expression of a 16?kDa protein in A. fumigatus. The?16 kDa protein of A. fumigatus targeted by PPEBL21 was identified as a hypothetical protein by peptide mass fingerprinting. It is thus hypothesized that a 16?kDa factor is essentially required by A. fumigatus for survival and its impaired synthesis due to treatment with PPEBL21 may lead to the death of pathogen.

Yadav, V.; Mandhan, R.; Kumar, M.; Gupta, J.; Sharma, G. L.



Pr-1, a novel antifungal protein from pumpkin rinds.  


A novel antifungal protein, M(r) = ca. 40 kDa, was isolated from pumpkin rind and designated Pr-1. When purified by anion exchange chromatography and HPLC, it inhibited growth of several fungi including Botrytis cinerea, Fusarium oxysporum, Fusarium solani and Rhizoctonia solani, as well as the yeast, Candida albicans, at 10-20 microM. It did not inhibit growth of Escherichia coli or Staphylococcus aureus even at 200 microM. Laser scanning microscopy of fungal cells exposed to rhodamine-labeled Pr-1 revealed that the protein accumulated and was localized on the cell surface. Uptake of the vital stain, SYTOX Green, was enhanced when fungal conidia were treated with Pr-1 suggesting that the protein has membrane permeabilization activity. Pr-1 was thermostable at 70 degrees C and did not lyse human red blood cells at 128 microM suggesting that the protein may be useful as an antifungal agent with little, if any human cytotoxicity. PMID:19760117

Park, Seong-Cheol; Lee, Jung Ro; Kim, Jin-Young; Hwang, Indeok; Nah, Jae-Woon; Cheong, Hyeonsook; Park, Yoonkyung; Hahm, Kyung-Soo



Antifungal activity of lectins against yeast of vaginal secretion  

PubMed Central

Lectins are carbohydrate-binding proteins of non-imune origin. This group of proteins is distributed widely in nature and they have been found in viruses, microorganisms, plants and animals. Lectins of plants have been isolated and characterized according to their chemical, physical-chemical, structural and biological properties. Among their biological activities, we can stress its fungicidal action. It has been previously described the effect of the lectins Dviol, DRL, ConBr and LSL obtained from the seeds of leguminous plants on the growth of yeasts isolated from vaginal secretions. In the present work the experiments were carried out in microtiter plates and the results interpreted by both methods: visual observations and a microplate reader at 530nm. The lectin concentrations varied from 0.5 to 256?g/mL, and the inoculum was established between 65-70% of trammitance. All yeast samples isolated from vaginal secretion were evaluated taxonomically, where were observed macroscopic and microscopic characteristics to each species. The LSL lectin did not demonstrate any antifungal activity to any isolate studied. The other lectins DRL, ConBr and DvioL, showed antifungal potential against yeast isolated from vaginal secretion. These findings offering offer a promising field of investigation to develop new therapeutic strategies against vaginal yeast infections, collaborating to improve women's health.

Gomes, Bruno Severo; Siqueira, Ana Beatriz Sotero; de Cassia Carvalho Maia, Rita; Giampaoli, Viviana; Teixeira, Edson Holanda; Arruda, Francisco Vassiliepe Sousa; do Nascimento, Kyria Santiago; de Lima, Adriana Nunes; Souza-Motta, Cristina Maria; Cavada, Benildo Sousa; Porto, Ana Lucia Figueiredo



Antifungal Susceptibility Profiles of 1698 Yeast Reference Strains Revealing Potential Emerging Human Pathogens  

PubMed Central

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

Desnos-Ollivier, Marie; Robert, Vincent; Raoux-Barbot, Dorothee; Groenewald, Marizeth; Dromer, Francoise



Antifungal activity of gallic acid purified from Terminalia nigrovenulosa bark against Fusarium solani.  


The antifungal activities of methanolic extracts from Terminalia nigrovenulosa bark (TNB) was investigated for effects on the initial growth of mycelia against Fusarium solani. The ethyl acetate fraction separated from TNB demonstrated the highest antifungal activity against F. solani. The antifungal compound was isolated from TNB using silica gel column and Sephadex LH-20 chromatography combined with thin-layer chromatography and high performance liquid chromatography. Structural identification of the antifungal compound was conducted using (1)H NMR, (13)C NMR, and liquid chromatography-tandem mass spectrometry. The purified antifungal compound was gallic acid (GA) or 3,4,5-trihydroxy benzoic acid. Purified-GA possesses the high antifungal activity against F. solani, and that antifungal activity was dosage-dependent. The hyphae became collapsed and shrunken after 24 h incubation with GA (500 ppm). In pot experiments, the application of TNB crude extract was found to be effective in controlling the cucumber Fusarium root rot disease by enhancing activities of chitinase, peroxidase thereby promoting the growth of plants. The applied TNB extract significantly suppressed root rot disease compared to control. It resulted in 33, 75 and 81% disease suppression with 100, 500 and 1000 ppm of TNB crude extract, respectively. The study effectively demonstrated biological activities of the TNB extract, therefore suggesting the application of TNB for the control of soil-borne diseases of cucumber plants. PMID:23333407

Nguyen, Dang-Minh-Chanh; Seo, Dong-Jun; Lee, Hyang-Burm; Kim, In-Seon; Kim, Kil-Yong; Park, Ro-Dong; Jung, Woo-Jin



Correlation between Antifungal Susceptibilities of Coccidioides immitis In Vitro and Antifungal Treatment with Caspofungin in a Mouse Model  

PubMed Central

Caspofungin (Merck Pharmaceuticals) was tested in vitro against 25 clinical isolates of Coccidoides immitis. In vitro susceptibility testing was performed in accordance with the National Committee for Clinical Laboratory Standards document M38-P guidelines. Two C. immitis isolates for which the caspofungin MICs were different were selected for determination of the minimum effective concentration (MEC), and these same strains were used for animal studies. Survival and tissue burdens of the spleens, livers, and lungs were used as antifungal response markers. Mice infected with strain 98-449 (48-h MIC, 8 ?g/ml; 48-h MEC, 0.125 ?g/ml) showed 100% survival to day 50 when treated with caspofungin at ?1 mg/kg. Mice infected with strain 98-571 (48-h MIC, 64 ?g/ml; 48-h MEC, 0.125 ?g/ml) displayed ?80% survival when the treatment was caspofungin at ?5 mg/kg. Treatment with caspofungin at 0.5, 1, 5, or 10 mg/kg was effective in reducing the tissue fungal burdens of mice infected with either isolate. When tissue fungal burden study results were compared between strains, caspofungin showed no statistically significant difference in efficacy in the organs of the mice treated with both strains. A better in vitro-in vivo correlation was noted when we used the MEC instead of the MIC as the endpoint for antifungal susceptibility testing. Caspofungin may have a role in the treatment of coccidioidomycosis.

Gonzalez, Gloria M.; Tijerina, Rolando; Najvar, Laura K.; Bocanegra, Rosie; Luther, Michael; Rinaldi, Michael G.; Graybill, John R.



Anti-fungal activity of SiO2/Ag2S nanocomposites against Aspergillus niger.  


Submicron particles of amorphous SiO(2) have been used to grow Ag(2)S nanophases at their surfaces. SEM and TEM analysis showed morphological well-defined nanocomposite particles consisting of Ag(2)S nanocrystals dispersed over the silica surfaces. These SiO(2)/Ag(2)S nanocomposites were investigated as anti-fungal agents against Aspergillus niger in different experimental conditions, including as nanofillers in cellulosic fibres. The anti-fungal activity in these composite systems is suggested to result from a synergistic effect due to Ag(2)S anti-fungal centres and the SiO(2) surfaces in promoting the adsorption of the fungus. PMID:19709863

Fateixa, Sara; Neves, Márcia C; Almeida, Adelaide; Oliveira, João; Trindade, Tito



Synthesis, antifungal and haemolytic activity of a series of bis(pyridinium)alkanes.  


A series of bis(pyridinium)alkanes have been prepared and their antifungal activity, haemolytic activity and ability to inhibit fungal phospholipase B1 have been investigated, together with those of the commercially available antiseptics octenidine and dequalinium. Removal of the amino substituents from the pyridinium rings resulted in a significant decrease in antifungal activity. However, shortening or removing the alkyl chains attached to the amino groups had little effect on antifungal activity and significantly reduced haemolytic activity. Only octenidine was a strong inhibitor of fungal phospholipase B1. PMID:17383187

Ng, Clarissa K L; Singhal, Vatsala; Widmer, Fred; Wright, Lesley C; Sorrell, Tania C; Jolliffe, Katrina A



Antifungal activity and mode of action of silver nano-particles on Candida albicans  

Microsoft Academic Search

In this study, the antifungal effects of silver nano-particles (nano-Ag) and their mode of action were investigated. Nano-Ag\\u000a showed antifungal effects on fungi tested with low hemolytic effects against human erythrocytes. To elucidate the antifungal\\u000a mode of action of nano-Ag, flow cytometry analysis, a glucose-release test, transmission electron microscopy (TEM) and the\\u000a change in membrane dynamics using 1,6-diphenyl-1,3,5-hexatriene (DPH), as

Keuk-Jun Kim; Woo Sang Sung; Bo Kyoung Suh; Seok-Ki Moon; Jong-Soo Choi; Jong Guk Kim; Dong Gun Lee



Three conazoles increase hepatic microsomal retinoic acid metabolism and decrease mouse hepatic retinoic acid levels in vivo  

SciTech Connect

Conazoles are fungicides used in agriculture and as pharmaceuticals. In a previous toxicogenomic study of triazole-containing conazoles we found gene expression changes consistent with the alteration of the metabolism of all trans-retinoic acid (atRA), a vitamin A metabolite with cancer-preventative properties (Ward et al., Toxicol. Pathol. 2006; 34:863-78). The goals of this study were to examine effects of propiconazole, triadimefon, and myclobutanil, three triazole-containing conazoles, on the microsomal metabolism of atRA, the associated hepatic cytochrome P450 (P450) enzyme(s) involved in atRA metabolism, and their effects on hepatic atRA levels in vivo. The in vitro metabolism of atRA was quantitatively measured in liver microsomes from male CD-1 mice following four daily intraperitoneal injections of propiconazole (210 mg/kg/d), triadimefon (257 mg/kg/d) or myclobutanil (270 mg/kg/d). The formation of both 4-hydroxy-atRA and 4-oxo-atRA were significantly increased by all three conazoles. Propiconazole-induced microsomes possessed slightly greater metabolizing activities compared to myclobutanil-induced microsomes. Both propiconazole and triadimefon treatment induced greater formation of 4-hydroxy-atRA compared to myclobutanil treatment. Chemical and immuno-inhibition metabolism studies suggested that Cyp26a1, Cyp2b, and Cyp3a, but not Cyp1a1 proteins were involved in atRA metabolism. Cyp2b10/20 and Cyp3a11 genes were significantly over-expressed in the livers of both triadimefon- and propiconazole-treated mice while Cyp26a1, Cyp2c65 and Cyp1a2 genes were over-expressed in the livers of either triadimefon- or propiconazole-treated mice, and Cyp2b10/20 and Cyp3a13 genes were over-expressed in the livers of myclobutanil-treated mice. Western blot analyses indicated conazole induced-increases in Cyp2b and Cyp3a proteins. All three conazoles decreased hepatic atRA tissue levels ranging from 45-67%. The possible implications of these changes in hepatic atRA levels on cell proliferation in the mouse tumorigenesis process are discussed.

Chen, P.-J. [Department of Agricultural Chemistry, National Taiwan University, Taipei, Taiwan (China); Environmental Carcinogenesis Division, National Health and Environmental Effects Research Laboratory, U.S. Environmental Protection Agency, B143-06, 109 T.W. Alexander Drive, Research Triangle Park, NC 27711 (United States); Padgett, William T.; Moore, Tanya; Winnik, Witold; Lambert, Guy R.; Thai, Sheau-Fung; Hester, Susan D. [Environmental Carcinogenesis Division, National Health and Environmental Effects Research Laboratory, U.S. Environmental Protection Agency, B143-06, 109 T.W. Alexander Drive, Research Triangle Park, NC 27711 (United States); Nesnow, Stephen [Environmental Carcinogenesis Division, National Health and Environmental Effects Research Laboratory, U.S. Environmental Protection Agency, B143-06, 109 T.W. Alexander Drive, Research Triangle Park, NC 27711 (United States)], E-mail:



Design, synthesis and antifungal activities of novel pyrrole alkaloid analogs.  


A series of novel analogs of pyrrole alkaloid were designed and synthesized by a facile method and their structures were characterized by 1H NMR, 13C NMR and high-resolution mass spectrometry (HRMS). The structure of compound 2a was identified by 2D NMR including heteronuclear multiple-quantum coherence (HMQC), heteronuclear multiple-bond correlation (HMBC) and H-H correlation spectrometry (H-H COSY) spectra. Their antifungal activities against five fungi were evaluated, and the results indicated that some of the title compounds showed moderate fungicidal activities in vitro against Alternaria solani, Cercospora arachidicola, Fusarium omysporum, Gibberella zeae and Physalospora piricola at the dosage of 50 ?g mL(-1). Compound 2a and 3a exhibited good activities against P. piricola at low dosage. PMID:21356570

Wang, Ming-Zhong; Xu, Han; Liu, Tuan-Wei; Feng, Qi; Yu, Shu-Jing; Wang, Su-Hua; Li, Zheng-Ming



Partial identification of antifungal compounds from Punica granatum peel extracts.  


Aqueous extracts of pomegranate peels were assayed in vitro for their antifungal activity against six rot fungi that cause fruit and vegetable decay during storage. The growth rates of Alternaria alternata , Stemphylium botryosum , and Fusarium spp. were significantly inhibited by the extracts. The growth rates were negatively correlated with the levels of total polyphenolic compounds in the extract and particularly with punicalagins, the major ellagitannins in pomegranate peels. Ellagitannins were also found to be the main compounds in the bioactive fractions using bioautograms, and punicalagins were identified as the main bioactive compounds using chromatographic separation. These results suggest that ellagitannins, and more specifically punicalagins, which are the dominant compounds in pomegranate peels, may be used as a control agent of storage diseases and to reduce the use of synthetic fungicides. PMID:22533815

Glazer, Ira; Masaphy, Segula; Marciano, Prosper; Bar-Ilan, Igal; Holland, Doron; Kerem, Zohar; Amir, Rachel



The antifungal constituents from the seeds of Itoa orientalis.  


Three new phenolic constituents, itolide A (1), itolide B (2), itoside P (3), and 1D-3-deoxy-3-hydroxymethyl-myo-inositol (4), which is described herein for the first time as a natural product, were isolated along with four other known compounds (5 to 8) from the methanol extract of the seeds of Itoa orientalis Hemsl by the activity-guided fractionation. Their structures were determined by spectroscopic means. Compounds 1 to 8 exhibited antifungal activities against Sclerotium rolfsii with IC?? values ranging from 60.12 to 240.00 ?M and against Rhizoctonia solani with IC?? values ranging from 45.34 to 233.14 ?M, respectively, and compounds 1, 2, 5 exhibited cytotoxic activity against Tn5B1-4 insect cell line with EC?? values of 203.68, 93.41 and 40.37 ?M, respectively. PMID:22233862

Tang, WenWei; Xu, HanHong; Zeng, DongQiang; Yu, LiJia



Acetoxychavicol Acetate, an Antifungal Component of Alpinia galanga1.  


The essential oils from fresh and dried rhizomes of ALPINIA GALANGA showed an antimicrobial activity against gram-positive bacteria, a yeast and some dermatophytes, using the agar overlay technique. The main components of the oils were also tested and terpinen-4-ol was found most active. An N-pentane/diethyl ether extract of dried rhizomes was active against TRICHOPHYTON MENTAGROPHYTES. 1'-Acetoxychavicol acetate, 1'-acetoxyeugenol acetate and 1'-hydroxychavicol acetate identified by MS and NMR were found in the antifungally active fractions obtained by LSC. Acetoxychavicol acetate was active against the seven fungi tested and its MIC value for dermatophytes ranged from 50 to 250 microg/ml. Dried sliced rhizomes contained 1.5% of this compound. The compound was not found in rhizomes of ALPINIA OFFICINARUM, ZINGIBER OFFICINALE and KAEMPFERIA GALANGA. PMID:17345272

Janssen, A M; Scheffer, J J



Toxicity of six novel fungicides and sulphur to Galendromus occidentalis (Acari: Phytoseiidae).  


A laboratory evaluation of fenbuconazole, myclobutanil propiconazole, boscalid, fenhexamid and pyraclostrobin revealed these fungicides to be harmless to adult Galendromus occidentalis. None of these fungicides affected adversely fecundity and egg viability. Elemental sulphur also had no effect on adults and fecundity. However, 72.4% of the young larvae perished after hatching. The six novel fungicides are safer alternatives to sulphur in perennial crops in British Columbia. PMID:18792796

Bostanian, Noubar J; Thistlewood, Howard M A; Hardman, John M; Racette, Gaétan



Candida biofilms: antifungal resistance and emerging therapeutic options.  


Intravascular catheter infections are a major cause of morbidity and mortality in hospitalized patients, accounting for the majority of the 200,000 nosocomial bloodstream infections occurring in the US annually. Of the intravenous lines that are culture-positive for Candida, 40% actually represent fungemia, which generally necessitates systemic treatment and line removal to affect cure. Until recently, the reason for the need for device removal was unclear. However, our research group and others have demonstrated a near-total resistance to antifungals by biofilm-associated Candida. Similar to bacterial species, Candida biofilm formation proceeds through early, intermediate and maturation phases. This process is associated with the generation of a polysaccharide extracellular matrix (ECM). Mature C. albicans biofilms have a heterogeneous architecture, in terms of distribution of fungal cells and ECM, and exhibit broad antimicrobial resistance. The mechanisms causing such profound antifungal resistance are beginning to be understood. Recent data indicate that resistance is phase-specific and multifactorial, involving efflux pumps and sterol synthesis (at early and mature biofilm phases, respectively). Neither metabolic quiescence nor the ECM appear to contribute substantially. Susceptibility testing and confocal scanning laser microscopy demonstrated that azoles failed to exert activity against mature Candida biofilms. However, sub-inhibitory concentrations of voriconazole impaired biofilm formation and caused cell morphological aberrations. In contrast, lipid-formulation amphotericins and the echinocandins uniquely exhibited activity against mature biofilms. The mechanisms underlying this ability are unknown. The role of other pharmacological (eg, catheter coatings, antimicrobial peptides and antibiotic locks) and non-pharmacological methods in the prevention and treatment of device-related biofilms is discussed in this review. PMID:15043393

Kuhn, Duncan M; Ghannoum, Mahmoud A



Transcriptional Analyses of Antifungal Drug Resistance in Candida albicans  

PubMed Central

Oral infections with the pathogenic yeast Candida albicans are one of the most frequent and earliest opportunistic infections in human immunodeficiency virus-infected patients. The widespread use of azole antifungal drugs has led to the development of drug-resistant isolates. Several molecular mechanisms that contribute to drug resistance have been identified, including increased mRNA levels for two types of efflux pump genes: the ATP binding cassette transporter CDRs (CDR1 and CDR2) and the major facilitator MDR1. Using Northern blot analyses, the expression patterns of these genes have been determined during logarithmic and stationary phases of cell growth and during growth in different carbon sources in a set of matched susceptible and fluconazole-resistant isolates that have been characterized previously. MDR1, CDR1, and CDR2 are expressed early during logarithmic growth, CDR4 is expressed late during logarithmic growth, and CDR1 is preferentially expressed in stationary-phase cells. There is a small decrease in expression of these genes when the cells are grown in carbon sources other than glucose. While increased mRNA levels of efflux pump genes are commonly associated with azole resistance, the causes of increased mRNA levels have not yet been resolved. Southern blot analysis demonstrates that the increased mRNA levels in these isolates are not the result of gene amplification. Nuclear run-on assays show that MDR1 and CDR mRNAs are transcriptionally overexpressed in the resistant isolate, suggesting that the antifungal drug resistance in this series is associated with the promoter and trans-acting factors of the CDR1, CDR2, and MDR1 genes.

Lyons, Chris N.; White, Theodore C.



Pharmacodynamics and pharmacokinetics of antifungals for treatment of invasive aspergillosis.  


Amphotericin B has been the only therapeutic option for invasive aspergillosis over decades. It acts by binding to membrane ergosterol, lipid peroxidation and proton-ATPase inhibition. Amphotericin B is eliminated unchanged via urine and feces. It displays a considerable toxicity, particularly infusion-related adverse events and renal damage. Continuous infusion and administration of lipidformulations of amphotericin B are strategies to improve its tolerability. Amphotericin B has a post-antifungal effect (PAFE), and its peak concentration is probably crucial for its fungicidal efficacy. The amphotericin B lipid-formulations display largely different pharmacokinetics. Kinetics of amphotericin B which is liberated from its lipid encapsulation in the plasma is similar for all three available lipid formulations. Azoles inhibit the synthesis of fungal cell membrane ergosterol. The triazoles itraconazole, voriconazole and posaconazole are active against Aspergilli. Voriconazole is the drug of choice for therapy of invasive aspergillosis. It is metabolized in the liver and metabolites are excreted via the kidneys. Posaconazole is licensed for antifungal prophylaxis in hematological high-risk patients and for salvage therapy of invasive aspergillosis. A variety of drug-drug interactions have to be considered with all azoles. The ratio between the area under the time-concentration profile (AUC) and the minimal inhibitory concentration (MIC) is the relevant pharmacokinetic/ pharmacodynamic parameter for azoles. Caspofungin the only echinocandin licensed for second line therapy of invasive aspergillosis is fungistatic to Aspergilli displaying a paradoxical pharmacodynamic effect. Caspofungin elimination is independent from renal function. Although it is metabolized in the liver its potential for drug interactions is moderate. PMID:23278532

Bellmann, Romuald



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

PubMed Central

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

Malik, Maqsood Ahmad; Al-Thabaiti, Shaeel Ahmed; Malik, Manzoor A.



Correlation of antifungal activity with fungal phospholipase inhibition using a series of bisquaternary ammonium salts.  


A series of bisquaternary ammonium salts with a 12-carbon spacer between the positive charges were synthesized, and their antifungal activity has been investigated. Compounds with butyl, pentyl, and isopentyl headgroups were the most potent antifungal agents with MICs in the range of 2.2-5.5 microM against both Cryptococcus neoformans and Candida albicans. The antifungal activity of these compounds correlated with their inhibition of cryptococcal phospholipase B1 (PLB1), a newly identified virulence factor. This indicates that the mode of action of these compounds may be inhibition of the fungal PLB1 enzyme, further validating this enzyme as a target for the development of novel antifungal therapies. PMID:16420066

Ng, Clarissa K L; Obando, Daniel; Widmer, Fred; Wright, Lesley C; Sorrell, Tania C; Jolliffe, Katrina A



Enhanced susceptibility to antifungal oligopeptides in yeast strains overexpressing ABC multidrug efflux pumps.  


The susceptibility to several oligopeptide and amino acid antifungals of a Saccharomyces cerevisiae strain carrying multiple deletions in yeast multidrug resistance genes was compared to transformants containing the CDR1, CDR2, or MDR1 genes that encode the major Candida albicans drug efflux pumps. Recombinant yeast strains overexpressing Cdr1p and Cdr2p showed enhanced susceptibilities to all tested oligopeptide antifungals. The enhanced susceptibilities of multidrug-resistant yeast strains to oligopeptide antifungals corresponded to higher rates of oligopeptide uptake. Yeast cells overexpressing Cdr1p or Cdr2p effluxed protons at higher rates than the reference cells lacking these ABC transporters. An increased plasma membrane electrochemical gradient caused by the functional overexpression of Cdr1p or Cdr2p appeared to increase cellular susceptibility to oligopeptide antifungals by stimulating their uptake via oligopeptide permeases. PMID:18794383

Wakiec, Roland; Gabriel, Iwona; Prasad, Rajendra; Becker, Jeffrey M; Payne, John W; Milewski, Slawomir



In vitro antifungal activity of dihydroxyacetone against causative agents of dermatomycosis.  


Dihydroxyacetone (DHA), a three-carbon sugar, is the browning ingredient in commercial sunless tanning formulations. DHA preparations have been used for more than 50 years and are currently highly popular for producing temporary pigmentation resembling an ultraviolet-induced tan. In this work, the in vitro antifungal activity of dihydroxyacetone was tested against causative agents of dermatomycosis, more specifically against dermatophytes and Candida spp. The antifungal activity was determined by the broth microdilution method according to the Clinical and Laboratory Standards Institute guidelines for yeasts and filamentous fungi. The data obtained show that the fungicidal activity varied from 1.6 to 50 mg ml(-1). DHA seems to be a promising substance for the treatment of dermatomycosis because it has antifungal properties at the same concentration used in artificial suntan lotions. Therefore, it is a potential low-toxicity antifungal agent that may be used topically because of its penetration into the corneal layers of the skin. PMID:20936361

Stopiglia, Cheila Denise Ottonelli; Vieira, Fabiane Jamono; Mondadori, Andressa Grazziotin; Oppe, Tércio Paschke; Scroferneker, Maria Lúcia



Biochemically Vulnerable Sites for Antifungal Intercession in the Control of Fungal Growth.  

National Technical Information Service (NTIS)

Virtually every antifungal agent in use intercedes some aspect of sterol synthesis or function. Ergosterol is the principal sterol in fungi, while cholesterol is the most abundant sterol in vertebrates. Research in our laboratory has shown that the struct...

L. W. Parks



Duration of Antifungal Treatment and Development of Delayed Complications in Patients with Candidaemia  

Microsoft Academic Search

  \\u000a The optimal duration of antifungal treatment of candidaemia is unknown. Prolonged treatment has been advocated to prevent\\u000a late-onset complications caused by metastatic infectious foci. To evaluate the relationship between duration of antifungal\\u000a therapy and the development of delayed complications in patients with candidaemia, a retrospective descriptive study was performed\\u000a in a tertiary care centre. The study included 180 consecutive

A. M. L. Oude Lashof; J. P. Donnelly; J. F. G. M. Meis; J. W. M. van der Meer; B. J. Kullberg



AHL-deficient mutants of Burkholderia ambifaria BC-F have decreased antifungal activity.  


Burkholderia ambifaria BC-F, a biocontrol strain reported previously to exhibit broad-spectrum antifungal activity, was highly active in formation of N-acyl homoserine lactones (AHLs). We constructed AHL-deficient derivatives of strain BC-F in which the genes specifying AHL synthase (bafI) and AHL-binding transcriptional activator (bafR) were inactivated by allelic exchange. The resulting AHL-deficient mutants had decreased antifungal activity. PMID:14570265

Zhou, Hongwei; Yao, Fude; Roberts, Daniel P; Lessie, Thomas G



Production and Characterization of Antifungal Compounds Produced by Lactobacillus plantarum IMAU10014  

Microsoft Academic Search

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.

HaiKuan Wang; YanHua Yan; JiaMing Wang; HePing Zhang; Wei Qi



Antifungal agents from Pseudallescheria boydii SNB-CN73 isolated from a Nasutitermes sp. termite.  


Defense mutualisms between social insects and microorganisms have been described in the literature. The present article describes the discovery of a Pseudallescheria boydii strain isolated from Nasutitermes sp. The microbial symbiont produces two antifungal metabolites: tyroscherin and N-methyltyroscherin, a compound not previously described in the literature. Methylation of tyroscherin has confirmed the structure of N-methyltyroscherin. Both compounds are effective antifungal agents with favorable selectivity indices for Candida albicans and Trichophyton rubrum. PMID:23627396

Nirma, Charlotte; Eparvier, Véronique; Stien, Didier



A non-polyene antifungal antibiotic from Streptomyces albidoflavus PU 23  

Microsoft Academic Search

In all 312 actinomycete strains were isolated from water and soil samples from different regions. All these isolates were\\u000a purified and screened for their antifungal activity against pathogenic fungi. Out of these, 22% of the isolates exhibited\\u000a activity against fungi. One promising strain,Streptomyces albidoflavus PU 23 with strong antifungal activity against pathogenic fungi was selected for further studies. Antibiotic was

S. K. Augustine; S. P. Bhavsar; B. P. Kapadnis



Incidence and possibilities of screening antifungal non-polyene antibiotics in actinomycetes  

Microsoft Academic Search

The author studied 114 strains of actinomycetes recovered from different geographical localities with different vegetation.\\u000a Under submerse cultivation conditions 57% of the strains displayed antibiotic activity—48% antibacterial, 56% antifungal.\\u000a As distinct from intracellular antibiotics, production of extracellular antibiotics was manifestly influenced by the composition\\u000a of the fermentation medium. The commonest antifungal antibiotics were polyenes and non-polyenes, in the ratio 2?1

Z. ?ehá?ek



A Novel Antifungal Furanone from Pseudomonas aureofaciens, a Biocontrol Agent of Fungal Plant Pathogens  

Microsoft Academic Search

Pseudomonas aureofaciens (= P. chlororaphis) strain 63-28 is a biocontrol agent active against many soil-borne fungal plant pathogens and shows antifungal activity in culture assays. 3-(1-Hexenyl)-5-methyl-2-(5H)furanone was isolated from culture filtrates of this bacterium. The purified furanone showed antifungal activity against Pythium ultimum, Fusarium solani, Fusarium oxysporum, and Thielaviopsis basicola. The ED50S for spore germination of these fungi were 45,

Timothy Paulitz; Brian Nowak-Thompson; Pascale Gamard; Evelyn Tsang; Joyce Loper



Silver nanoparticles stabilized by tannin grafted collagen fiber: synthesis, characterization and antifungal activity  

Microsoft Academic Search

A novel antifungal nano-silver agent (BT-CF-AgNPs) was synthesized by using bayberry tannin (BT) grafted collagen fiber (CF)\\u000a as support, and the antifungal behaviors of the nano-silver were investigated by using Saccharomyces cerevisiae as a typical fungus. Bayberry tannin (BT), a kind of natural polyphenol, was grafted onto the CF surface to improve the loading\\u000a capacity and control the size of

Li He; Hao Wu; Siying Gao; Xuepin Liao; Qiang He; Bi Shi


Production and Characterization of an Antifungal Compound (3-Phenyllactic Acid) Produced by Lactobacillus plantarum Strain  

Microsoft Academic Search

The Lactobacillus plantarum strain was isolated from grass silage that produces a broad spectrum of antifungal compound, active against food and feed-borne\\u000a filamentous fungi in agar plate assay. Aspergillus fumigatus and Rhizopus stolonifer were the most sensitive among molds. No inhibitory activity could be detected against mold Penicillium roqueforti. Enhanced antifungal activity was observed at 30 °C in pH 6.5. Minimum inhibitory

P. Prema; D. Smila; A. Palavesam; G. Immanuel



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


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. PMID:10870565

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



Synthesis and antifungal activity of some s-mercaptotriazolobenzothiazolyl amino acid derivatives.  


A series of s-triazolobenzothiazolylthioacetyl/propionyl amino acid derivatives were synthesized with the aim of evaluating their antifungal activity. Their chemical structures were confirmed by (1)H, (13)C NMR, IR, mass spectrometry and elemental analyses. The synthesized derivatives were screened for their antifungal activity against Aspergillus flavus and Candida albicans. Five compounds (3, 5, 7c, 8 and 17) were found to possess high activity comparable to fluconazole at 100 ?g/mL against C. albicans. PMID:23376218

Aboelmagd, A; Ali, Ibrahim A I; Salem, Ezzeldin M S; Abdel-Razik, M



Facilitated diffusion of glucosamine-6-phosphate synthase inhibitors enhances their antifungal activity  

Microsoft Academic Search

N3-(4-Methoxyfumaroyl)-L-2,3-diaminopropanoic acid (FMDP) and 2-amino-2- deoxy-D-glucitol-6-phosphate (ADGP) are strong inhibitors of the essential fungal en- zyme, glucosamine-6-phosphate synthase, but their antifungal activity is poor, due to slow penetration of these agents through the cytoplasmic membrane. In the present studies we have exploited the possibility of enhancement of ADGP and FMDP antifungal activity by improving their transport properties. It has been

Agnieszka Janiak; Barbara Cybulska; Joanna Szlinder-Richert; Edward Borowski



Proteins with antifungal properties and other medicinal applications from plants and mushrooms  

Microsoft Academic Search

Living organisms produce a myriad of molecules to protect themselves from fungal pathogens. This review focuses on antifungal\\u000a proteins from plants and mushrooms, many of which are components of the human diet or have medicinal value. Plant antifungal\\u000a proteins can be classified into different groups comprising chitinases and chitinase-like proteins, chitin-binding proteins,\\u000a cyclophilin-like proteins, defensins and defensin-like proteins, deoxyribonucleases, embryo-abundant

Jack H. Wong; T. B. Ng; Randy C. F. Cheung; X. J. Ye; H. X. Wang; S. K. Lam; P. Lin; Y. S. Chan; Evandro F. Fang; Patrick H. K. Ngai; L. X. Xia; X. Y. Ye; Y. Jiang; F. Liu



In vitro antifungal susceptibility of clinically relevant species belonging to Aspergillus section Flavi.  


The in vitro antifungal susceptibility of 77 isolates belonging to different clinically relevant species of Aspergillus section Flavi, including those of different phylogenetic clades of A. flavus, was tested for nine antifungal agents using a microdilution reference method (CLSI, M38-A2). Terbinafine and the echinocandins demonstrated lower MICs/MECs for all species evaluated, followed by posaconazole. Amphotericin B showed MICs ? 2 ?g/ml for 38 (49.4%) of the 77 isolates tested. PMID:23335742

Gonçalves, Sarah S; Stchigel, Alberto M; Cano, Josep; Guarro, Josep; Colombo, Arnaldo L



Evaluation of Antifungal Susceptibility Testing with Microdilution and Etest Methods of Candida Blood Isolates  

Microsoft Academic Search

Candida species that show an increasing number of clinical and\\/or microbiological resistance to several antifungals and are the most\\u000a common agents of invasive fungal infections. The aim of this study was to investigate the in vitro susceptibility of Candida blood isolates to antifungal agents (amphotericin B, fluconazole, itraconazole, and voriconazole) by comparative use of the\\u000a CLSI reference microdilution method and

Dilek Yesim Metin; Suleyha Hilmioglu-Polat; Pinar Samlioglu; Biray Doganay-Oflazoglu; Ramazan Inci; Emel Tumbay


In Vitro Antifungal Susceptibility of Clinically Relevant Species Belonging to Aspergillus Section Flavi  

PubMed Central

The in vitro antifungal susceptibility of 77 isolates belonging to different clinically relevant species of Aspergillus section Flavi, including those of different phylogenetic clades of A. flavus, was tested for nine antifungal agents using a microdilution reference method (CLSI, M38-A2). Terbinafine and the echinocandins demonstrated lower MICs/MECs for all species evaluated, followed by posaconazole. Amphotericin B showed MICs ? 2 ?g/ml for 38 (49.4%) of the 77 isolates tested.

Goncalves, Sarah S.; Stchigel, Alberto M.; Cano, Josep; Guarro, Josep



First isolation of a novel thermostable antifungal peptide secreted by Aspergillus clavatus  

Microsoft Academic Search

A novel antifungal peptide produced by an indigenous fungal strain (VR) of Aspergillus clavatus was purified. The antifungal peptide was enriched in the supernatant after heat treatment at 70°C. The thermostable character was exploited in the first purification step, as purified peptide was obtained after ultrafiltration and reverse phase-HPLC on C18 column application. The purified peptide named “AcAFP” for A.

Houda Skouri-Gargouri; Ali Gargouri



Antifungal 3-Hydroxy Fatty Acids from Lactobacillus plantarum MiLAB 14  

PubMed Central

We report the identification and chemical characterization of four antifungal substances, 3-(R)-hydroxydecanoic acid, 3-hydroxy-5-cis-dodecenoic acid, 3-(R)-hydroxydodecanoic acid and 3-(R)-hydroxytetradecanoic acid, from Lactobacillus plantarum MiLAB 14. The concentrations of the 3-hydroxy fatty acids in the supernatant followed the bacterial growth. Racemic mixtures of the saturated 3-hydroxy fatty acids showed antifungal activity against different molds and yeasts with MICs between 10 and 100 ?g ml?1.

Sjogren, Jorgen; Magnusson, Jesper; Broberg, Anders; Schnurer, Johan; Kenne, Lennart



An imidazole derivative (econazole) as an antifungal agent in cell culture systems  

Microsoft Academic Search

Summary  Econazole, an imidazole derivative, was tested as an antifungal agent in different cell culture systems. In comparison with\\u000a Fungizone, Econazole has the following advantageous properties: higher stability, higher solubility, better antifungal activity\\u000a against contaminants of cell cultures and a wider range between minimal inhibitory to cytotoxic concentration withAspergillus fumigatus, Candida albicans andPenicillium sp., activity against gram-positive bacteria and lower price.

R. Wyler; A. Murbach; H. Möhl



Stilbene derivatives with antifungal and radical scavenging properties from the Stem Bark of artocarpus nobilis  

Microsoft Academic Search

Antifungal activity-guided fractionation of the n-butanol extract from the methanol extract of the stem bark of Artocarpus nobilis furnished two stilbene derivatives (E)-4-isopentenyl-3,5,2?,4?-tetrahydroxystilbene and (E)-4-(3-methyl-E-but-1-enyl)-3,5,2?,4?-tetrahydroxystilbene. Both compounds showed strong antifungal activity against Cladosporium cladosporioides and high radical scavenging activity towards the DPPH radical in TLC bio-autography method.

U. L. B. Jayasinghe; S. Puvanendran; N. Hara; Y. Fujimoto



Postantifungal Effects of Echinocandin, Azole, and Polyene Antifungal Agents against Candida albicans and Cryptococcus neoformans  

Microsoft Academic Search

The postantifungal effect (PAFE) of fluconazole, MK-0991, LY303366, and amphotericin B was determined against isolates of Candida albicans and Cryptococcus neoformans. Concentrations ranging from 0.125 to 4 times the MIC were tested following exposure to the antifungal for 0.25 to 1 h. Combinations of azole and echino- candin antifungals (MK-0991 and LY303366) were tested against C. neoformans. Fluconazole displayed no




Candida albicans Mutations in the Ergosterol Biosynthetic Pathway and Resistance to Several Antifungal Agents  

Microsoft Academic Search

The role of sterol mutations in the resistance of Candida albicans to antifungal agents has not been thoroughly investigated. Previous work reported that clinical C. albicans strains resistant to both azole antifungals and amphotericin B were defective in ERG3, a gene encoding sterol 5,6 -desaturase. It is also believed that a deletion of the lanosterol 14-demethylase gene, ERG11, is possible

Dominique Sanglard; Francoise Ischer; Tania Parkinson; Derek Falconer; Jacques Bille



Risk of Oral Anti-fungal Agent-Induced Liver Injury in Taiwanese.  


AIM: Oral anti-fungal agent-induced liver injury is a common safety concern that may lead to patients' hesitation in treating fungal infections such as onychomycosis. This study evaluated risk of drug-induced liver injury (DILI) caused by oral anti-fungal agents in Taiwanese populations. METHODS: A population-based study was conducted by analyzing Taiwan National Health Insurance Database who used oral anti-fungal agents from 2002 to 2008. A comparison control group was randomly extracted from the remainder of the original cohort. RESULTS: Of the 90,847 oral anti-fungal agents users, 52 patients had DILI. Twenty-eight DILI cases used ketoconazole, 12 fluconazole, 8 griseofulvin, 3 itraconazole, and 2 terbinafine. The incidence rates (IR) of DILI per 10000 persons were 31.6, 4.9, 4.3, 3.6 and 1.6 for fluconazole, ketoconazole, griseofulvin, itraconazole, and terbinafine, respectively. Longer exposure duration increased risk of DILI, with IR for exposure duration ? 60 defined daily dose (DDD) of 170.9, 62.5, and 36.1 per 10000 persons for ketoconazole, itraconazole, and terbinafine, respectively. Patients taking anti-fungal agents had higher incidences of developing DILI compared to those in the control group after adjusting for age, gender, and co-morbidities (relative risk: 2.38; P < 0.001). All of the 6 patients with fatal DILI used fluconazole. Old age and fluconazole increased the risk of oral anti-fungal induced fatal DILI. CONCLUSIONS: Oral anti-fungal agents are associated with low incidence of acute liver injury, but which may be fatal, especially for the elderly. Longer treatment duration may increase the risk of anti-fungal agent-induced liver injury, especially ketoconazole. PMID:23750489

Kao, Wei-Yu; Su, Chien-Wei; Huang, Yi-Shin; Chou, Yueh-Ching; Chen, Yi-Chih; Chung, Wen-Hung; Hou, Ming-Chih; Lin, Han-Chieh; Lee, Fa-Yauh; Wu, Jaw-Ching



Role of Matrix ?-1,3 Glucan in Antifungal Resistance of Non-albicans Candida Biofilms  

PubMed Central

Candida biofilm infections pose an increasing threat in the health care setting due to the drug resistance associated with this lifestyle. Several mechanisms underlie the resistance phenomenon. In Candida albicans, one mechanism involves drug impedance by the biofilm matrix linked to ?-1,3 glucan. Here, we show this is important for other Candida spp. We identified ?-1,3 glucan in the matrix, found that the matrix sequesters antifungal drug, and enhanced antifungal susceptibility with matrix ?-1,3 glucan hydrolysis.

Mitchell, K. F.; Taff, H. T.; Cuevas, M. A.; Reinicke, E. L.; Sanchez, H.



Toxicogenomic study of triazole fungicides and perfluoroalkyl acids in rat livers predicts toxicity and categorizes chemicals based on mechanisms of toxicity.  


Toxicogenomic analysis of five environmental chemicals was performed to investigate the ability of genomics to predict toxicity, categorize chemicals, and elucidate mechanisms of toxicity. Three triazole antifungals (myclobutanil, propiconazole, and triadimefon) and two perfluorinated chemicals [perfluorooctanoic acid (PFOA) and perfluorooctane sulfonate (PFOS)] were administered daily via oral gavage for one, three, or five consecutive days to male Sprague-Dawley rats at single doses of 300, 300, 175, 20, or 10 mg/kg/day, respectively. Clinical chemistry, hematology, and histopathology were measured at all time points. Gene expression profiling of livers from three rats per treatment group at all time points was performed on the CodeLink Uniset Rat I Expression array. Data were analyzed in the context of a large reference toxicogenomic database containing gene expression profiles for over 630 chemicals. Genomic signatures predicting hepatomegaly and hepatic injury preceded those results for all five chemicals, and further analysis segregated chemicals into two distinct classes. The triazoles caused similar gene expression changes as other azole antifungals, particularly the induction of pregnane X receptor (PXR)-regulated xenobiotic metabolism and oxidative stress genes. In contrast, PFOA and PFOS exhibited peroxisome proliferator-activated receptor alpha agonist-like effects on genes associated with fatty acid homeostasis. PFOA and PFOS also resulted in downregulation of cholesterol biosynthesis genes, matching an in vivo decrease in serum cholesterol, and perturbation of thyroid hormone metabolism genes matched by serum thyroid hormone depletion in vivo. The concordance of in vivo observations and gene expression findings demonstrated the ability of genomics to accurately categorize chemicals, identify toxic mechanisms of action, and predict subsequent pathological responses. PMID:17383973

Martin, Matthew T; Brennan, Richard J; Hu, Wenyue; Ayanoglu, Eser; Lau, Christopher; Ren, Hongzu; Wood, Carmen R; Corton, J Christopher; Kavlock, Robert J; Dix, David J



Isolation of lysozyme and an antifungal peptide from sea lamprey (Petromyzon marinus) plasma.  


The sea lamprey (Petromyzon marinus) belongs to the most primitive class of fish and has only innate immunity. The innate immune factors, lysozyme and an antifungal peptide, were isolated from sea lamprey plasma. Sea lamprey plasma (40.1mg protein/ml) was assayed for lysozyme activity by gel diffusion assay. Using hen egg white lysozyme standards, plasma concentration of lamprey lysozyme was 5microg lysozyme/mg total protein. The presence of lysozyme in such high concentration in lamprey plasma could be important in their innate immunity and resistance to infection. Lysozyme and the antifungal peptide were isolated by low molecular weight gel filtration chromatography from sea lamprey plasma. Gel filtration chromatography yielded two peak tubes containing lysozyme (1microg/211microg total protein) and antifungal peptide (1microg/66microg total protein). Lysozyme and antifungal activity of each fraction were determined by well diffusion assay using Gram-negative bacteria, Gram-positive bacteria and two fungal species. The molecular weight of lamprey lysozyme was 14.3kDa. The sea lamprey lysozyme was effective against Gram-positive bacteria but not against Gram-negative bacteria or fungi. Molecular weight of the antifungal peptide was approximately 3000Da. Antifungal plasma activity was seen against Penicillium notatum and Aspergillus flavus. No plasma antibacterial peptide was found. PMID:19552965

Rose, Wendy M; Ourth, Donald D



Adhesion of oral Candida albicans isolates to denture acrylic following limited exposure to antifungal agents.  


Candidal adherence to denture acrylic surfaces is implicated as the first step in the pathogenesis of Candida-associated denture stomatitis, the most prevalent form of oral candidosis in the West. This condition is treated by topically administered antifungal agents, mainly belonging to the polyenes and azoles. As the intraoral concentrations of antifungals fluctuate considerably due to the dynamics of the oral environment, the effect of short exposure to sublethal concentrations of antifungals on the adhesion of Candida albicans to denture acrylic surfaces was investigated. Seven oral C. albicans isolates were exposed to four-eight times minimum inhibitory concentrations (MIC) of five antifungal drugs, nystatin, amphotericin B, 5-fluorocytosine, ketoconazole and fluconazole, for 1 h. After removing the drug (by repeated washing) the adhesion of these isolates to acrylic strips was assessed by an in vitro adhesion assay. Exposure to antifungal agents significantly reduced the adherence of all seven C. albicans isolates to denture acrylic. The mean percentage reductions of adhesion after limited exposure to nystatin, amphotericin B, 5-fluorocytosine, ketoconazole and fluconazole were 86.48, 90.85, 66.72, 65.88 and 47.42%, respectively. These findings indicate that subtherapeutic doses of antifungals may modulate oral candidal colonization. Further, these results may have an important bearing on dosage regimens currently employed in treating oral candidosis. PMID:9877331

Ellepola, A N; Samaranayake, L P



Exploring the Molecular Basis of Antifungal Synergies Using Genome-Wide Approaches  

PubMed Central

Drug resistance poses a significant challenge in antifungal therapy since resistance has been found for all known classes of antifungal drugs. The discovery of compounds that can act synergistically with antifungal drugs is an important strategy to overcome resistance. For such combination therapies to be effective, it is critical to understand the molecular basis for the synergism by examining the cellular effects exerted by the combined drugs. Genomic profiling technologies developed in the model yeast Saccharomyces cerevisiae have been successfully used to investigate antifungal combinations. This review discusses how these technologies have been used not only to identify synergistic mechanisms but also to predict drug synergies. It also discusses how genome-wide genetic interaction studies have been combined with drug–target information to differentiate between antifungal drug synergies that are target-specific versus those that are non-specific. The investigation of the mechanism of action of antifungal synergies will undoubtedly advance the development of optimal and safe combination therapies for the treatment of drug-resistant fungal infections.

Agarwal, Ameeta K.; Tripathi, Siddharth K.; Xu, Tao; Jacob, Melissa R.; Li, Xing-Cong; Clark, Alice M.



Candida tropicalis antifungal cross-resistance is related to different azole target (Erg11p) modifications.  


Candida tropicalis ranks between third and fourth among Candida species most commonly isolated from clinical specimens. Invasive candidiasis and candidemia are treated with amphotericin B or echinocandins as first-line therapy, with extended-spectrum triazoles as acceptable alternatives. Candida tropicalis is usually susceptible to all antifungal agents, although several azole drug-resistant clinical isolates are being reported. However, C. tropicalis resistant to amphotericin B is uncommon, and only a few strains have reliably demonstrated a high level of resistance to this agent. The resistance mechanisms operating in C. tropicalis strains isolated from clinical samples showing resistance to azole drugs alone or with amphotericin B cross-resistance were elucidated. Antifungal drug resistance was related to mutations of the azole target (Erg11p) with or without alterations of the ergosterol biosynthesis pathway. The antifungal drug resistance shown in vitro correlated very well with the results obtained in vivo using the model host Galleria mellonella. Using this panel of strains, the G. mellonella model system was validated as a simple, nonmammalian minihost model that can be used to study in vitro-in vivo correlation of antifungals in C. tropicalis. The development in C. tropicalis of antifungal drug resistance with different mechanisms during antifungal treatment has potential clinical impact and deserves specific prospective studies. PMID:23877676

Forastiero, A; Mesa-Arango, A C; Alastruey-Izquierdo, A; Alcazar-Fuoli, L; Bernal-Martinez, L; Pelaez, T; Lopez, J F; Grimalt, J O; Gomez-Lopez, A; Cuesta, I; Zaragoza, O; Mellado, E



Passiflin, a novel dimeric antifungal protein from seeds of the passion fruit.  


The intent was to isolate an antifungal protein from seeds of the passion fruit (Passiflora edulis) and to compare its characteristics with other antifungal proteins and bovine beta-lactoglobulin in view of its N-terminal amino acid sequence similarity to beta-lactoglobulin. The isolation procedure entailed ion-exchange chromatography on Q-Sepharose, hydrophobic interaction chromatography on Phenyl-Sepharose, ion-exchange chromatography on DEAE-cellulose, and FPLC-gel filtration on Superdex 75. The isolated 67-kDa protein, designated as passiflin, exhibited an N-terminal amino acid sequence closely resembling that of bovine beta-lactoglobulin. It is the first antifungal protein found to have a beta-lactoglobulin-like N-terminal sequence. Its dimeric nature is rarely found in antifungal proteins. It impeded mycelial growth in Rhizotonia solani with an IC(50) of 16 microM and potently inhibited proliferation of MCF-7 breast cancer cells with an IC(50) of 15 microM. There was no cross-reactivity of passiflin with anti-beta-lactoglobulin antiserum. Intact beta-lactoglobulin lacks antifungal and antiproliferative activities and is much smaller in molecular size than passiflin. However, it has been reported that hydrolyzed beta-lactoglobulin shows antifungal activity. The data suggest that passiflin is distinct from beta-lactoglobulin. PMID:19200704

Lam, S K; Ng, T B



In vitro antifungal activities of Bay n 7133 and Bay L 9139, two new orally absorbed antifungal imidazole derivatives, against pathogenic yeasts  

Microsoft Academic Search

Bay n 7133 and Bay L 9139 (Bayer AG, Wuppertal, Fed. Rep. Germany) are new, orally absorbable, antifungal imidazole derivatives. In vitro, Bay n 7133 was comparable to ketoconazole and miconazole when tested against isolates of Candida albicans and Cryptococcus neoformans. Bay L 9139 also was active against these organisms but to a lesser degree than the other imidazoles. LY

R. A. Fromtling; H. P. Yu; S. Shadomy



Geographic and Temporal Trends in Isolation and Antifungal Susceptibility of Candida parapsilosis: a Global Assessment from the ARTEMIS DISK Antifungal Surveillance Program, 2001 to 2005  

Microsoft Academic Search

We examined data from the ARTEMIS DISK Antifungal Surveillance Program to describe geographic and temporal trends in the isolation of Candida parapsilosis from clinical specimens and the in vitro susceptibilities of 9,371 isolates to fluconazole and voriconazole. We also report the in vitro susceptibility of bloodstream infection (BSI) isolates of C. parapsilosis to the echinocandins, anidulafungin, caspofungin, and micafungin. C.

M. A. Pfaller; D. J. Diekema; D. L. Gibbs; V. A. Newell; K. P. Ng; A. Colombo; J. Finquelievich; R. Barnes; J. Wadula



Antifungal activity of two Lactobacillus strains with potential probiotic properties.  


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. PMID:22497448

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



Azospirillum brasilense siderophores with antifungal activity against Colletotrichum acutatum.  


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. PMID:21234749

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



Biosynthesis and pathway engineering of antifungal polyene macrolides in actinomycetes.  


Polyene macrolides are a large family of natural products typically produced by soil actinomycetes. Polyene macrolides are usually biosynthesized by modular and large type I polyketide synthases (PKSs), followed by several steps of sequential post-PKS modifications such as region-specific oxidations and glycosylations. Although known as powerful antibiotics containing potent antifungal activities (along with additional activities against parasites, enveloped viruses and prion diseases), their high toxicity toward mammalian cells and poor distribution in tissues have led to the continuous identification and structural modification of polyene macrolides to expand their general uses. Advances in in-depth investigations of the biosynthetic mechanism of polyene macrolides and the genetic manipulations of the polyene biosynthetic pathways provide great opportunities to generate new analogues. Recently, a novel class of polyene antibiotics was discovered (a disaccharide-containing NPP) that displays better pharmacological properties such as improved water-solubility and reduced hemolysis. In this review, we summarize the recent advances in the biosynthesis, pathway engineering, and regulation of polyene antibiotics in actinomycetes. PMID:23515854

Kong, Dekun; Lee, Mi-Jin; Lin, Shuangjun; Kim, Eung-Soo



Comparison of In Vitro Antifungal Activities of Efinaconazole and Currently Available Antifungal Agents against a Variety of Pathogenic Fungi Associated with Onychomycosis  

PubMed Central

Onychomycosis is a common fungal nail infection in adults that is difficult to treat. The in vitro antifungal activity of efinaconazole, a novel triazole antifungal, was evaluated in recent clinical isolates of Trichophyton rubrum, Trichophyton mentagrophytes, and Candida albicans, common causative onychomycosis pathogens. In a comprehensive survey of 1,493 isolates, efinaconazole MICs against T. rubrum and T. mentagrophytes ranged from ?0.002 to 0.06 ?g/ml, with 90% of isolates inhibited (MIC90) at 0.008 and 0.015 ?g/ml, respectively. Efinaconazole MICs against 105 C. albicans isolates ranged from ?0.0005 to >0.25 ?g/ml, with 50% of isolates inhibited (MIC50) by 0.001 and 0.004 ?g/ml at 24 and 48 h, respectively. Efinaconazole potency against these organisms was similar to or greater than those of antifungal drugs currently used in onychomycosis, including amorolfine, ciclopirox, itraconazole, and terbinafine. In 13 T. rubrum toenail isolates from onychomycosis patients who were treated daily with topical efinaconazole for 48 weeks, there were no apparent increases in susceptibility, suggesting low potential for dermatophytes to develop resistance to efinaconazole. The activity of efinaconazole was further evaluated in another 8 dermatophyte, 15 nondermatophyte, and 10 yeast species (a total of 109 isolates from research repositories). Efinaconazole was active against Trichophyton, Microsporum, Epidermophyton, Acremonium, Fusarium, Paecilomyces, Pseudallescheria, Scopulariopsis, Aspergillus, Cryptococcus, Trichosporon, and Candida and compared favorably to other antifungal drugs. In conclusion, efinaconazole is a potent antifungal with a broad spectrum of activity that may have clinical applications in onychomycosis and other mycoses.

Tatsumi, Yoshiyuki; Senda, Hisato; Pillai, Radhakrishnan; Nakamura, Takashi; Sone, Daisuke; Fothergill, Annette



Antifungal activity of redox-active benzaldehydes that target cellular antioxidation  

PubMed Central

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 (sod1?, sod2?, glr1?) and two mitogen-activated protein kinase (MAPK) mutants of A. fumigatus (sakA?, mpkC?), 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) concentrations. Effective inhibition of fungal growth can also be achieved using combinations of these benzaldehydes. Conclusions Natural benzaldehydes targeting cellular antioxidation components of fungi, such as superoxide dismutases, glutathione reductase, etc., effectively inhibit fungal growth. They possess antifungal or chemosensitizing capacity to enhance efficacy of conventional antifungal agents. Chemosensitization can reduce costs, abate resistance, and alleviate negative side effects associated with current antifungal treatments.



Purification and molecular identification of an antifungal peptide from the hemolymph of Musca domestica (housefly).  


Antibacterial and antifungal peptides found in houseflies (Musca domestica) in large number are indispensable components of its immune defense mechanism. In this study the anterior tip of the larvae of housefly was cut off with a pair of fine scissors and hemolymph was collected and exuded in an ice-cold test tube. From the hemolymph an antifungal substance was isolated by solid-phase extraction combined with reverse phase-high performance liquid chromotography (RP-HPLC) and named as Musca domestica antifungal peptide-1 (MAF-1). Sodium dodecyl sulphate-polyacrylamide gel electrophoresis (SDS-PAGE) showed its molecular weight was 17 kDa. UV absorption spectra revealed that this antifungal substance possessed the characteristics of protein peptides. Analysis by fingerprint-identification and tandem mass spectrometry suggested MAF-1 was an unknown protein. Edman degradation identified the sequence of 30 amino acids of its N-terminal which matched no peptide in the MASCOT search database, indicating MAF-1 was a novel insect antifungal peptide. Mass spectrometry showed the precise molecular weight of MAF-1 was 17203.384 Da. Its isoelectric point was acidic. PMID:19728925

Fu, Ping; Wu, Jianwei; Guo, Guo



Isolation and biochemical characterization of a novel leguminous defense peptide with antifungal and antiproliferative potency.  


Leguminous plants have formed a popular subject of research owing to the abundance of proteins and peptides with important biological activities that they produce. The antifungal proteins and peptides have been purified from a number of leguminous species. However, research continues to discover novel antifungal plant-produced peptides and proteins are being needed, specially those novel ones with both antifungal activity and other significant bioactivities. The objective of this study was to isolate a novel peptide from Phaseolus limensis. A 6.8 kDa peptide designated Limyin, with both antifungal and antiproliferative activity, was isolated from the large lima bean (P. limensis) legumes. The isolation procedure consisted of extraction, precipitation, affinity chromatography on Affi-gel blue gel, ion chromatography on SP-Toyopearl, and gel filtration on Superdex 75. Its N-terminal sequence was determined to be KTCENLATYYRGPCF, showing high homology to defensin and defensin precursors from plants. It potently suppressed mycelial growth in Alternaria alternata, Fusarium solani, and Botrytis cinerea. Its antifungal activity was stable up to 80 degrees C. It showed antiproliferative activity towards tumor cells including human liver hepatoma cells Bel-7402 and neuroblastoma cells SHSY5Y. However, it had no effect on bacteria Staphylococcus aureus and Salmonella. The present findings make a significant addition of the research on leguminous plants. PMID:18841359

Wang, Shaoyun; Rao, Pingfan; Ye, Xiuyun



Antifungal activity of borrelidin produced by a Streptomyces strain isolated from soybean.  


In this study, an endophytic Streptomyces sp. neau-D50 with strong antifungal activity against Phytophthora sojae was isolated from healthy soybean root, using an in vitro screening technique. A bioactivity-guided approach was then employed to isolate and determine the chemical identity of bioactive constituents with antifungal activity from strain neau-D50. The structure of the antifungal metabolite was elucidated as borrelidin on the basis of spectral analysis. To our knowledge, this is the first report that borrelidin has strong antifungal activity against dominant race 1 of P. sojae with EC(50) and EC(95) of 0.0056 and 0.026 mg/L, respectively. The values were respectively 62.5- and 262.3-fold lower than those of the commercial fungicide metalaxyl, which has been used to treat soybean seed for the control of P. sojae . The in situ bioassays demonstrated that borrelidin at 10 mg/L reduced P. sojae race 1 lesions on soybean seedlings by 94.72% without affecting root growth. Thus, borrelidin might be a promising candidate for new antifungal agents against P. sojae. PMID:22242825

Liu, Chong-Xi; Zhang, Ji; Wang, Xiang-Jing; Qian, Ping-Ting; Wang, Ji-Dong; Gao, Ya-Mei; Yan, Yi-Jun; Zhang, Shu-Zhen; Xu, Peng-Fei; Li, Wen-Bin; Xiang, Wen-Sheng



Antifungal potential of extracellular metabolites produced by Streptomyces hygroscopicus against phytopathogenic fungi.  


Indigenous actinomycetes isolated from rhizosphere soils were assessed for in vitro antagonism against Colletotrichum gloeosporioides and Sclerotium rolfsii. A potent antagonist against both plant pathogenic fungi, designated SRA14, was selected and identified as Streptomyces hygroscopicus. The strain SRA14 highly produced extracellular chitinase and beta-1,3-glucanase during the exponential and late exponential phases, respectively. Culture filtrates collected from the exponential and stationary phases inhibited the growth of both the fungi tested, indicating that growth suppression was due to extracellular antifungal metabolites present in culture filtrates. The percentage of growth inhibition by the stationary culture filtrate was significantly higher than that of exponential culture filtrate. Morphological changes such as hyphal swelling and abnormal shapes were observed in fungi grown on potato dextrose agar that contained the culture filtrates. However, the antifungal activity of exponential culture filtrates against both the experimental fungi was significantly reduced after boiling or treatment with proteinase K. There was no significant decrease in the percentage of fungal growth inhibition by the stationary culture filtrate that was treated as above. These data indicated that the antifungal potential of the exponential culture filtrate was mainly due to the presence of extracellular chitinase enzyme, whereas the antifungal activity of the stationary culture filtrate involved the action of unknown thermostable antifungal compound(s). PMID:18825279

Prapagdee, Benjaphorn; Kuekulvong, Chutima; Mongkolsuk, Skorn



Isolation and identification of antifungal peptides from Bacillus BH072, a novel bacterium isolated from honey.  


A bacterial strain BH072 isolated from a honey sample showed antifungal activity against mold. Based on morphological, biochemical, physiological tests, and analysis of 16S rDNA sequence, the strain was identified to be a new subspecies of Bacillus sp. It had a broad spectrum of antifungal activity against various mold, such as Aspergillus niger, Pythium, and Botrytis cinerea. Six pairs of antifungal genes primers were designed and synthesized, and ituA, hag, tasA genes were detected by PCR analysis. The remarkable antifungal activity could be associated with the co-production of these three peptides. One of them was purified by 30-40% ammonium sulfate precipitation, Sephadex G-75 gel filtration and anion exchange chromatography on D201 resin. The purified peptide was estimated to be 35.615 kDa and identified to be flagellin by micrOTOF-Q II. By using methanol extraction, another substance was isolated from fermentation liquor, and determined to be iturin with liquid chromatography-mass spectrometry (LC-MS) method. The third possible peptide encoded by tasA was not isolated in this study. The culture liquor displayed antifungal activity in a wide pH range (5.0-9.0) and at 40-100°C. The result of the present work suggested that Bacillus BH072 might be a bio-control bacterium of research value. PMID:23545354

Zhao, Xin; Zhou, Zhi-jiang; Han, Ye; Wang, Zhan-zhong; Fan, Jie; Xiao, Hua-zhi



Injectable in situ cross-linking hydrogels for local antifungal therapy.  


Invasive fungal infections can be devastating, particularly in immunocompromised patients, and difficult to treat with systemic drugs. Furthermore, systemic administration of those medications can have severe side effects. We have developed an injectable local antifungal treatment for direct administration into existing or potential sites of fungal infection. Amphotericin B (AmB), a hydrophobic, potent, and broad-spectrum antifungal agent, was rendered water-soluble by conjugation to a dextran-aldehyde polymer. The dextran-aldehyde-AmB conjugate retained antifungal efficacy against Candida albicans. Mixing carboxymethylcellulose-hydrazide with dextran-aldehyde formed a gel that cross-linked in situ by formation of hydrazone bonds. The gel provided in vitro release of antifungal activity for 11 days, and contact with the gel killed Candida for three weeks. There was no apparent tissue toxicity in the murine peritoneum and the gel caused no adhesions. Gels produced by entrapment of a suspension of AmB in CMC-dextran without conjugation of drug to polymers did not release fungicidal activity, but did kill on contact. Injectable systems of these types, containing soluble or insoluble drug formulations, could be useful for treatment of local antifungal infections, with or without concurrent systemic therapy. PMID:19942285

Hudson, Sarah P; Langer, Robert; Fink, Gerald R; Kohane, Daniel S



Concentration of Antifungal Agents within Host Cell Membranes: a New Paradigm Governing the Efficacy of Prophylaxis ? †  

PubMed Central

Posaconazole prophylaxis has proven highly effective in preventing invasive fungal infections, despite relatively low serum concentrations. However, high tissue levels of this agent have been reported in treated patients. We therefore hypothesized that the intracellular levels of antifungal agents are an important factor in determining the success of fungal prophylaxis. To examine the effect of host cell-associated antifungals on the growth of medically important molds, we exposed cells to antifungal agents and removed the extracellular drug prior to infection. Epithelial cells loaded with posaconazole and its parent molecule itraconazole, but not other antifungals, were able to inhibit fungal growth for at least 48 h and were protected from damage caused by infection. Cell-associated posaconazole levels were 40- to 50-fold higher than extracellular levels, and the drug was predominantly detected in cellular membranes. Fungistatic levels of posaconazole persisted within epithelial cells for up to 48 h. Therefore, the concentration of posaconazole in mammalian host cell membranes mediates its efficacy in prophylactic regimens and likely explains the observed discrepancy between serum antifungal levels and efficacy.

Campoli, P.; Al Abdallah, Q.; Robitaille, R.; Solis, N. V.; Fielhaber, J. A.; Kristof, A. S.; Laverdiere, M.; Filler, S. G.; Sheppard, D. C.



4-Methyl-7-hydroxycoumarin antifungal and antioxidant activity enhancement by substitution with thiosemicarbazide and thiazolidinone moieties.  


According to literature data, thiosemicarbazide and thiazolidinone moieties should enhance biological properties of coumarin. Antioxidant, metal-chelating and antifungal activities of all compounds were investigated and compared to the activity of the starting material, 7-hydroxy-4-methylcoumarin, and were proven to possess potent antioxidant and antifungal activity. In general, thiosemicarbazides showed higher scavenging activity towards DPPH and galvinoxyl radicals than did 4-thiazolidinones and some of them had the same or even better activity than had ascorbic acid itself, depending on the free radical used. In antifungal activity tests towards four foodborne mycotoxigenic fungi, Aspergillus flavus, Aspergillus ochraceus. Fusarium graminearum and Fusarium verticillioides, coumarin derivatives were proven to possess a very high activity in terms of growth inhibition, depending on the fungi investigated. In general, 4-thiazolidinones showed better antifungal activity than did thiosemicarbazides. F. graminearum was the most susceptible to the compounds investigated and F. verticillioides was proven to be the most resistant. Two compounds, both coumarinyl thiosemicarbazides, were found to possess both antifungal and antioxidant activity which could be useful for applications in medicine, food industry and agriculture. PMID:23561135

Šarkanj, Bojan; Molnar, Maja; ?a?i?, Milan; Gille, Lars



Purification and modes of antifungal action by Vicia faba cv. Egypt trypsin inhibitor.  


A new 15 kDa Bowman-Birk type trypsin inhibitor (termed VFTI-E1) from fava beans (Vicia faba cv. Egypt 1) was isolated using liquid chromatography. Though it exhibited substantial homology in N-terminal amino acid sequence to other protease inhibitors, VFTI-E1 showed antiproteolytic activity against trypsin (K(i) 11.9 × 10(-9) M) but hardly any activity against chymotrypsin. It demonstrated antifungal activity toward the filamentous fungus Valsa mali with an IC(50) of 20 ?M. The mechanism of its antifungal action toward V. mali included (1) induction of alteration of hyphal morphology, (2) growth inhibition by chitin deposition at hyphal tips, and (3) permeabilization of fungal membrane. The antifungal activity of VFTI-E1 was dependent on the ambient ionic strength as increasing concentrations of NaCl, CaCl(2), and MgCl(2) diminished the activity. The membranolytic action of VFTI-E1 was confined to fungus, but not exerted on human and rabbit erythrocytes. This study sheds light on the mode of hyphal growth inhibitory activity of protease inhibitors with antifungal activity. The antifungal activity of VFTI-E1 amplifies the scope of its potential applications. PMID:20836498

Fang, Evandro Fei; Hassanien, Abdallah Abd Elazeem; Wong, Jack Ho; Bah, Clara Shui Fern; Soliman, Saeed Saad; Ng, Tzi Bun



Antifungal and peroxidative activities of nonheme chloroperoxidase in relation to transgenic plant protection.  


Nonheme chloroperoxidase (CPO-P) of Pseudomonas pyrrocinia catalyzes the oxidation of alkyl acids to peracids by hydrogen peroxide. Alkyl peracids possess potent antifungal activity as found with peracetate: 50% killing (LD(50)) of Aspergillus flavus occurred at 25 microM compared to 3.0 mM for the hydrogen peroxide substrate. To evaluate whether CPO-P could protect plants from fungal infection, tobacco was transformed with a gene for CPO-P from P. pyrrocinia and assayed for antifungal activity. Leaf extracts from transformed plants inhibited growth of A. flavus by up to 100%, and levels of inhibition were quantitatively correlated to the amounts of CPO-P activity expressed in leaves. To clarify if the peroxidative activity of CPO-P could be the basis for the increased resistance, the antifungal activity of the purified enzyme was investigated. The LD(50) of hydrogen peroxide combined with CPO-P occurred at 2.0 mM against A. flavus. Because this value was too small to account for the enhanced antifungal activity of transgenic plants, the kinetics of the enzyme reaction was examined and it was found that the concentration of hydrogen peroxide needed for enzyme saturation (K(m) = 5.9 mM) was already lethal. Thus, the peroxidative activity of CPO-P is not the basis for antifungal activity or enhanced resistance in transgenic plants expressing the gene. PMID:11052700

Jacks, T J; De Lucca, A J; Rajasekaran, K; Stromberg, K; van Pée, K



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

PubMed Central

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

Al-Attas, Safia A.; Amro, Soliman O.



Antifungal property of hibicuslide C and its membrane-active mechanism in Candida albicans.  


In this study, the antifungal activity and mode of action(s) of hibicuslide C derived from Abutilon theophrasti were investigated. Antifungal susceptibility testing showed that hibicuslide C possessed potent activities toward various fungal strains and less hemolytic activity than amphotericin B. To understand the antifungal mechanism(s) of hibicuslide C in Candida albicans, flow cytometric analysis with propidium iodide was done. The results showed that hibicuslide C perturbed the plasma membrane of the C. albicans. The analysis of the transmembrane electrical potential with 3,3'-dipropylthiacarbocyanine iodide [DiSC3(5)] indicated that hibicuslide C induced membrane depolarization. Furthermore, model membrane studies were performed with calcein encapsulating large unilamellar vesicles (LUVs) and FITC-dextran (FD) loaded LUVs. These results demonstrated that the antifungal effects of hibicuslide C on the fungal plasma membrane were through the formation of pores with radii between 2.3 nm and 3.3 nm. Finally, in three dimensional flow cytometric contour plots, a reduced cell sizes by the pore-forming action of hibicuslide C were observed. Therefore, the present study suggests that hibicuslide C exerts its antifungal effect by membrane-active mechanism. PMID:23816874

Hwang, Ji Hong; Jin, Qinglong; Woo, Eun-Rhan; Lee, Dong Gun



Antifungal activities of essential oils and their constituents from indigenous cinnamon ( Cinnamomum osmophloeum) leaves against wood decay fungi  

Microsoft Academic Search

Cinnamomum osmophloeum Kaneh is one of the hardwood species indigenous to Taiwan that possesses significant antifungal activity. To examine the antifungal activity of leaf essential oils and dominant constituents from C. osmophloeum, the essential oils of leaves from three clones (A, B, and C) collected from Haw-Lin experimental forest were extracted and their components analyzed by gas chromatography. Results from

Sheng-Yang Wang; Pin-Fun Chen; Shang-Tzen Chang



Botryorhodines A–D, antifungal and cytotoxic depsidones from Botryosphaeria rhodina, an endophyte of the medicinal plant Bidens pilosa  

Microsoft Academic Search

An endophytic fungus (Botryosphaeria rhodina) was isolated from the stems of the medicinal plant Bidens pilosa (Asteraceae) that is known for its anti-inflammatory, antiseptic and antifungal effects. The ethyl acetate extract of the fungal isolate exhibits significant antifungal activity as well as potent cytotoxic and antiproliferative effects against several cancer cell lines. Activity-guided fractionation resulted in the isolation of a

Randa Abdou; Kirstin Scherlach; Hans-Martin Dahse; Isabel Sattler; Christian Hertweck



Augmenting the activity of antifungal agents against aspergilli using structural analogues of benzoic acid as chemosensitizing agents  

Microsoft Academic Search

A number of benzoic acid analogues showed antifungal activity against strains of Aspergillus flavus, Aspergillus fumigatus and Aspergillus terreus, causative agents of human aspergillosis, in in vitro bioassays. Structure–activity analysis revealed that antifungal activities of benzoic and gallic acids were increased by addition of a methyl, methoxyl or chloro group at position 4 of the aromatic ring, or by esterification

Jong H. Kim; Bruce C. Campbell; Noreen Mahoney; Kathleen L. Chan; Russell J. Molyneux; Arunmozhi Balajee



The use of sourdough fermented by antifungal LAB to reduce the amount of calcium propionate in bread  

Microsoft Academic Search

Addition of sourdough is a common practice in the bakery industry to improve, among other quality parameters, the shelf life of bread. In this study, sourdough fermented by antifungal Lactobacillus plantarum strains was investigated for the ability to inhibit growth of common bread spoilage fungi. In both in vitro and sourdough wheat bread system, the antifungal sourdoughs significantly affected the

L. A. M. Ryan; F. Dal Bello; E. K. Arendt



Augmenting the activity of antifungal agents against aspergilli using structural analogues of benzoic acid as chemosensitizing agents  

Technology Transfer Automated Retrieval System (TEKTRAN)

Several benzoic acid analogs showed antifungal activity against strains of Aspergillus flavus, A. fumigatus and A. terreus, causative agents of human aspergillosis. Structure-activity analysis revealed that antifungal activities of benzoic and gallic acids increased by addition of a methyl, methoxyl...


HA1-92, A new antifungal antibiotic produced by Streptomyces CDRIL-312: Fermentation, isolation, purification and biological activity  

Microsoft Academic Search

A new antifungal antibiotic, HA-1-92, was isolated from the biomass of Streptomyces CDRIL-312, by extracting in butanol and further purified by silica gel column chromatography followed by preparative TLC. The antibiotic is presumed to be an oxohexaene macrolide and showed promising antifungal activity against yeasts and filamentous fungi including human and plant pathogens. It was found to be less toxic

J. Harindran; T. E. Gupte; S. R. Naik



Implementation of Practice Guidelines for Antifungal Therapy in a Surgical Intensive Care Unit and Its Impact on Use and Costs  

Microsoft Academic Search

Background: Considering the complexity of diagnosis, high costs of therapy and high morbidity and mortality of systemic fungal infections, antifungal therapy of intensive care patients should follow clearly defined guidelines. We outline the impact of a standardised practice of antifungal treatment in an interdisciplinary surgical intensive care unit of a university hospital. Methods: Therapy was intended to be optimised by

Stefanie Swoboda; Christoph Lichtenstern; Michael Christoff Ober; Lenka Alexandra Taylor; Dominic Störzinger; André Michel; Angelika Brobeil; Markus Mieth; Stefan Hofer; Hans-Günther Sonntag; Torsten Hoppe-Tichy; Markus Alexander Weigand



Oxygen accessibility and iron levels are critical factors for the antifungal action of ciclopirox against Candida albicans  

Microsoft Academic Search

Objectives: Ciclopirox is a topical antifungal agent of the hydroxypyridone class whose mode of action is poorly understood. In order to elucidate the mechanism of action of ciclopirox, we analysed the growth, cellular integrity, biochemical properties, viability and transcriptional profile of the poly- morphic yeast Candida albicans following exposure to this antifungal agent. Methods: Multiple biochemical assays served to identify

Hans-Christian Sigle; Sascha Thewes; Markus Niewerth; Hans Christian Korting; Monika Schafer-Korting; Bernhard Hube


Correlation between In Vitro and In Vivo Antifungal Activities in Experimental Fluconazole-Resistant Oropharyngeal and Esophageal Candidiasis  

Microsoft Academic Search

Oropharyngeal and esophageal candidiasis (OPEC) is a frequent opportunistic mycosis in immunocompro- mised patients. Azole-resistant OPEC is a refractory form of this infection occurring particularly in human immunodeficiency virus (HIV)-infected patients. The procedures developed by the Antifungal Subcommittee of the National Committee for Clinical Laboratory Standards (NCCLS) are an important advance in standard- ization of in vitro antifungal susceptibility methodology.




Genome-Wide Expression Profiling of the Response to Azole, Polyene, Echinocandin, and Pyrimidine Antifungal Agents in Candida albicans  

Microsoft Academic Search

Antifungal agents exert their activity through a variety of mechanisms, some of which are poorly understood. We examined changes in the gene expression profile of Candida albicans following exposure to representatives of the four currently available classes of antifungal agents used in the treatment of systemic fungal infections. Ketoconazole exposure increased expression of genes involved in lipid, fatty acid, and

Teresa T. Liu; Robin E. B. Lee; Katherine S. Barker; Richard E. Lee; Lai Wei; Ramin Homayouni; P. David Rogers



Antitumor and antifungal activities in endophytic fungi isolated from pharmaceutical plants Taxus mairei, Cephalataxus fortunei and Torreya grandis  

Microsoft Academic Search

The purpose of this work was to screen the endophytic fungi having antitumor or antifungal activity, which were isolated from the inner barks of three kinds of pharmaceutical plants, Taxus mairei, Cephalataxus fortunei and Torreya grandis, collected from Fujian province, China. Antitumor activity was studied by the MTT assay and antifungal activity was determined by observing fungal growth inhibition. 13.4%

Yaojian Huang; Jianfeng Wang; Guiling Li; Zhonghui Zheng; Wenjin Su



Synthesis and antifungal activity of 6-arylamino-phthalazine-5,8-diones and 6,7-bis(arylthio)-phthalazine-5,8-diones.  


6-Arylamino-phthalazine-5,8-diones and 6,7-bis(arylthio)-phthalazine-5,8-diones were synthesized and tested for in vitro antifungal activity against two pathogenic strains of fungi. Among those tested, many compounds showed good antifungal activity. The results suggest that phthalazine-5,8-diones would be potent antifungal agents. PMID:17320386

Ryu, Chung-Kyu; Park, Rae-Eun; Ma, Mi-Young; Nho, Ji-Hee



Synthesis and antifungal activity of 2-hydroxy-4,5-methylenedioxyaryl ketones as analogues of kakuol.  


In a study aiming to determine the structural elements essential to the antifungal activity of kakuol, we synthesized a series of 2-hydroxy-4,5-methylenedioxyaryl ketones, and we assayed their in vitro antifungal activity. The most sensitive target organisms to the action of these class of compounds were Phytophthora infestans, Phytium ultimum, Cercospora beticola, Cladosporium cucumerinum, and Rhizoctonia solani. Most of the analogs showed a remarkable in vitro activity, and some of them appeared significantly more effective than the natural product. The biological activity was mainly affected by introducing structural modification on the carbonyl moiety of the natural-product molecule. In particular, compound 5a, bearing a C=C bond conjugated to the C=O group, was found active with a MIC value of 10 microg ml(-1) against Cladosporium cucumerinum. The results suggest that 2-hydroxy-4,5-methylenedioxyaryl ketones can be considered promising candidates in the development of new antifungal compounds. PMID:20397224

Musso, Loana; Dallavalle, Sabrina; Merlini, Lucio; Farina, Gandolfina



Discrimination of Modes of Action of Antifungal Substances by Use of Metabolic Footprinting  

PubMed Central

Diploid cells of Saccharomyces cerevisiae were grown under controlled conditions with a Bioscreen instrument, which permitted the essentially continuous registration of their growth via optical density measurements. Some cultures were exposed to concentrations of a number of antifungal substances with different targets or modes of action (sterol biosynthesis, respiratory chain, amino acid synthesis, and the uncoupler). Culture supernatants were taken and analyzed for their “metabolic footprints” by using direct-injection mass spectrometry. Discriminant function analysis and hierarchical cluster analysis allowed these antifungal compounds to be distinguished and classified according to their modes of action. Genetic programming, a rule-evolving machine learning strategy, allowed respiratory inhibitors to be discriminated from others by using just two masses. Metabolic footprinting thus represents a rapid, convenient, and information-rich method for classifying the modes of action of antifungal substances.

Allen, Jess; Davey, Hazel M.; Broadhurst, David; Rowland, Jem J.; Oliver, Stephen G.; Kell, Douglas B.



Antifungal activity of Leuconostoc citreum and Weissella confusa in rice cakes.  


The antifungal activity of organic acids greatly improves the shelf life of bread and bakery products. However, little is known about the effect of lactic acid fermentation on fungal contamination in rice cakes. Here, we show that lactic acid fermentation in rice dough can greatly retard the growth of three fungal species when present in rice cakes, namely Cladosporium sp. YS1, Neurospora sp. YS3, and Penicillium crustosum YS2. The antifungal activity of the lactic acid bacteria against these fungi was much better than that of 0.3% calcium propionate. We found that organic acids including lactic and acetic acid, which are byproducts of lactic fermentation or can be artificially added, were the main antifungal substances. We also found that some Leuconostoc citreum and Weissella confusa strains could be good starter species for rice dough fermentation. These results imply that these lactic acid bacteria can be applicable to improve the preservation of rice cakes. PMID:23124754

Baek, Eunjong; Kim, Hyojin; Choi, Hyejung; Yoon, Sun; Kim, Jeongho



Flufuran, an antifungal 3,5-disubstituted furan produced by Aspergillus flavus link.  


A 3,5-disubstituted furan, named flufuran, was isolated from a culture filtrate of a strain of Aspergillus flavus obtained from a chestnut compost created in the same orchard. Flufuran was identified by spectroscopic methods, and its structure was confirmed through the preparation of some key derivatives, also used to test the antifungal activity. At a concentration of 0.2 mg/ml, assayed against three Phytophthora species, pathogenic of some forest and agrarian plants, flufuran and especially its acetyl derivative showed significant antifungal activity. Although flufuran appears to be identical to a fungal metabolite isolated previously from some Polyporus spp., its interesting antifungal activity has never been reported before. PMID:19319868

Evidente, Antonio; Cristinzio, Gennaro; Punzo, Biancavaleria; Andolfi, Anna; Testa, Antonino; Melck, Dominique



Antifungal activity of crude extracts of gladiolus dalenii van geel (iridaceae).  


Bulb extracts of Gladiolus dalenii reportedly used in the treatment of fungal infections in HIV/AIDS patients in the Lake Victoria region were tested for antifungal activity using the disc diffusion assay technique. Commercially used antifungal drugs, Ketaconazole and Griseofulvin (Cosmos Pharmaceuticals) were used as standards. Dichloromethane (CH?CL?)/Methanol (MeOH) in the ratio 1:1. Soluble extracts showed antifungal activity against Aspergillus niger. Direct bioautography on silica gel Thin Layer Chromatography (TLC) and appropriate spraying agents were used to identify the active component in the extract. The activities of both the extracts were higher than that of Griseofulvin. CH?CL? soluble extract in addition showed ability to delay sporulation in A.niger. The active group of compounds in the extracts was identified as alkaloids, which offer immense potential for development of new and valuable pharmaceutical products. PMID:21304613

Odhiambo, Judith Agot; Siboe, George Muyala; Lukhoba, Catherine Wanjiru; Dossaji, Saiffudin Fidahussein



Isolation and characterization of a novel antifungal peptide from Aspergillus niger.  


A novel antifungal peptide (termed as Anafp) was isolated from the culture supernatant of the filamentous fungi, Aspergillus niger. The whole amino acid sequence of Anafp was determined and the peptide was found to be composed of a single polypeptide chain with 58 amino acids including six cysteine residues. The peptide shows some degree of sequence homology to a cysteine-rich antifungal peptides reported from the seeds of Sinapis alba and Arabidopsis thaliana or the extracellular media of Aspergillus giganteus and Penicillium chrysogenumsome. Cysteine-spacing pattern of Anafp was similar to that of the antifungal peptide from Penicillium chrysogenum. The Anafp exhibited potent growth inhibitory activities against yeast strains as well as filamentous fungi at a range from 4 to 15 microM. In contrast, Anafp did not show antibacterial activity against Escherichia coli and Bacillus subtilis even at 50 microM. PMID:10512732

Gun Lee, D; Shin, S Y; Maeng, C Y; Jin, Z Z; Kim, K L; Hahm, K S



Antibacterial, antifungal and cytotoxic activities of two flavonoids from Retama raetam flowers.  


We have investigated the antibacterial, antifungal and cytotoxic activities of two flavonoids isolated from Retama raetam flowers using the disc diffusion and micro-dilution broth methods. The cytotoxic activity was tested against Hep-2 cells using the MTT assay. The compounds licoflavone C (1) and derrone (2) were active against Pseudomonas aeruginosa and Escherichia coli (7.81-15.62 ?g/mL) and showed important antifungal activity. Strong antifungal activity against Candida species (7.81 ?g/mL) was for example found with compound 2. The tested compounds also showed strong cytotoxicity against Hep-2 cells. These two compounds may be interesting antimicrobial agents to be used against infectious diseases caused by many pathogens. PMID:22695233

Edziri, Hayet; Mastouri, Maha; Mahjoub, Mohamed Ali; Mighri, Zine; Mahjoub, Aouni; Verschaeve, Luc



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


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. PMID:19056546

Tomczykowa, Monika; Tomczyk, Micha?; Jakoniuk, Piotr; Tryniszewska, Elzbieta



Analysis Of Volatile Fingerprints: A Rapid Screening Method For Antifungal Agents For Efficacy Against Dermatophytes  

NASA Astrophysics Data System (ADS)

The potential of using an electronic nose (E. nose) for rapid screening dermatophytes to antifungal agents was studied. In vitro, the 50 and 90% effective concentration (EC) values of five antifungal agents for T. rubrum and T. mentagrophytes were obtained by mycelial growth assays. Then, the qualitative volatile production patterns of the growth responses of these fungi to these values were incorporated into solid medium were analysed after 96-120 hrs incubation at 25° C using headspace analyses. Overall, results, using PCA and CA demonstrated that it is possible to differentiate between various treatments within 96-120 hrs. This study showed that potential exists for using qualitative volatile patterns as a rapid screening method for antifungal agents for microorganism. This approach could also facilitate the monitoring of antimicrobial drug activities and infection control programmes and perhaps drug resistance build up in microbial species.

Naraghi, Kamran; Sahgal, Natasha; Adriaans, Beverley; Barr, Hugh; Magan, Naresh



Alocasin, an anti-fungal protein from rhizomes of the giant taro Alocasia macrorrhiza.  


An anti-fungal protein designated alocasin was isolated from the rhizomes of the giant taro Alocasia macrorrhiza. The isolation protocol involved ion exchange chromatography on diethylaminoethyl (DEAE)-cellulose, ion exchange chromatography on sulfopropyl (SP)-Sepharose, and gel filtration on Superdex 75. Alocasin, which was unadsorbed on DEAE-cellulose and SP-Sepharose, possessed the N-terminal sequence APEGEV, which exhibited some similarity to that of the miraculin-like anti-fungal protein from Pisum sativum legumes. It demonstrated a molecular mass of 11kDa in sodium dodecyl sulfate-polyacrylamide gel electrophoresis and gel filtration, and displayed anti-fungal activity against Botrytis cinerea. Alocasin reduced the activity of HIV-1 reverse transcriptase. It exhibited weak hemagglutinating activity, only at a concentration of 1mg/ml. PMID:12651101

Wang, H X; Ng, T B



The antifungal, cytotoxic, antitermite and insecticidal activities of Zizyphus jujube.  


Plants are very useful, self-generating machines, producing a variety of useful bioactive products. Keeping in view this idea, the crude methanolic extract and various fractions of Zizyphus jujuba were screened for antifungal, cytotoxic, antitermite and insecticidal activities. Low activity was shown by the crude methanolic extract (12%), n-hexane (9%), chloroform (20%) and ethyl acetate (14%) fraction against Penicillium notatum. Low activity was shown by the n-hexane fraction against Aspergillus niger (10%) and Trichoderma harzianum (13%) and inactive against Aspergillus flavus, Fusarium oxysporum and Rhizopus stolonifer. The CHCl(3) fraction exhibited low activity of 10% against F. oxysporum while showing no activity against the rest of the test fungi. All the test samples were inactive against Rhizopus stolonifer. The crude methanolic extract was highly cytotoxic (73.33%) at the concentration of 1000 (µg/ml) while the rest of the test samples were low in toxicity at the same concentration. The crude methanolic extract of Zizyphus jujuba showed significant antitermite activity against Heterotermes indicola, among the test samples. Against Tribolium castaneum, Rhizopertha dominica and Callosbruchus analis the insecticidal activity was determined. All the test samples except n-hexane showed low activity (20%) against T. castaneum. The n-hexane fraction showed low activity (20%) against R. dominica while the rest of the fractions were inactive against it. Low activity of 40% and 20% was shown by the chloroform and n-hexane fraction respectively against C. analis. The results of the present study revealed that the plant could be as potent source of cytotoxic drugs. PMID:21959810

Ahmad, Bashir; Khan, Ibrar; Bashir, Shumaila; Azam, Sadiq; Ali, Niaz



Primary antifungal prophylaxis in adult hematopoietic stem cell transplant recipients: current therapeutic concepts.  


In recipients of hematopoietic stem cell transplants (HSCTs), the mortality associated with invasive fungal infections (IFIs) remains high, despite the introduction of broad-spectrum antifungal agents over the past 2 decades. Preventing exposure to fungal pathogens in this population is impossible; therefore, clinicians have focused on prophylactic use of antifungal agents to prevent IFIs in high-risk HSCT recipients. It is important to target antifungal prophylaxis by type of HSCT (autologous or allogeneic), local epidemiology, and risk factors for IFIs so that patients can receive the most appropriate agent while balancing costs and the risks of toxicity, and minimizing the development of resistance. To assist clinicians in weighing the pros and cons of currently available antifungal agents when choosing a suitable prophylactic regimen, we provide a review of several key prospective randomized trials that evaluated various antifungal agents for primary prophylaxis in adult HSCT recipients. In addition, we describe the epidemiology of and risk factors for IFIs in HSCT recipients, the difficulties in diagnosing IFIs, antifungal agents used for prophylaxis, and the goals of primary prophylaxis. Fluconazole remains the gold standard for primary prophylaxis in autologous HSCT recipients. For allogeneic HSCT recipients, the agent chosen for prophylaxis must be based on the patient's risk factors for IFIs. In low-risk patients, fluconazole is an appropriate agent to use for primary prophylaxis immediately after transplantation. However, in allogeneic HSCT recipients who develop complications, such as graft failure, graft-versus-host disease, or cytomegalovirus infection, prophylaxis with a mould-active agent should be used. PMID:19857148

McCoy, Dorothy; Depestel, Daryl D; Carver, Peggy L



Impact of First-Line Antifungal Agents on the Outcomes and Costs of Candidemia  

PubMed Central

Candida species are the leading causes of invasive fungal infection among hospitalized patients and are responsible for major economic burdens. The goals of this study were to estimate the costs directly associated with the treatment of candidemia and factors associated with increased costs, as well as the impact of first-line antifungal agents on the outcomes and costs. A retrospective study was conducted in a sample of 199 patients from four university-affiliated tertiary care hospitals in Korea over 1 year. Only costs attributable to the treatment of candidemia were estimated by reviewing resource utilization during treatment. Risk factors for increased costs, treatment outcome, and hospital length of stay (LOS) were analyzed. Approximately 65% of the patients were treated with fluconazole, and 28% were treated with conventional amphotericin B. The overall treatment success rate was 52.8%, and the 30-day mortality rate was 47.9%. Hematologic malignancy, need for mechanical ventilation, and treatment failure of first-line antifungal agents were independent risk factors for mortality. The mean total cost for the treatment of candidemia was $4,743 per patient. Intensive care unit stay at candidemia onset and antifungal switch to second-line agents were independent risk factors for increased costs. The LOS was also significantly longer in patients who switched antifungal agents to second-line drugs. Antifungal switch to second-line agents for any reasons was the only modifiable risk factor of increased costs and LOS. Choosing an appropriate first-line antifungal agent is crucial for better outcomes and reduced hospital costs of candidemia.

Ha, Young Eun; Joo, Eun-Jeong; Kim, Shin Woo; Jung, Sook-In; Chang, Hyun Ha; Park, Kyong Hwa; Han, Sang Hoon



New lignan esters from Alyxia schlechteri and antifungal activity against Pythium insidiosum.  


Three new lignan esters, alyterinates A-C (1-3), as well as 10 known compounds were isolated from the roots of Alyxia schlechteri. Antifungal activity against Pythium insidiosum of all lignan derivatives was evaluated using disk diffusion assay. P. insidiosum is not a true fungus since its cell walls do not contain ergosterol as usual fungi, so the antifungals available now are not effective. From activity testing, it was found that compounds 3, 4 and 5 could inhibit the mycelia growth of P. insidiosum. PMID:23994626

Sriphana, Uraiwan; Thongsri, Yordhathai; Ardwichai, Pispong; Poopasit, Kitisak; Prariyachatigul, Chularut; Simasathiansophon, Sontaya; Yenjai, Chavi



Mycotic Keratitis Due to Curvularia senegalensis and In Vitro Antifungal Susceptibilities of Curvularia spp.  

PubMed Central

A case of mycotic keratitis due to Curvularia senegalensis is reported. This case represents the third known reported infection caused by this rare species. Fungal hyphae were detected in corneal scrapings, and repeated cultures were positive for this fungi. The patient was presumed cured after a corneal transplant and treatment with itraconazole, but the infection recurred and the patient is waiting for a keratoplasty. The in vitro antifungal susceptibilities of the case strain and another 24 strains belonging to seven species of Curvularia were tested for six antifungal agents. With the exception of flucytosine, and occasionally fluconazole, the other drugs assayed (amphotericin B, miconazole, itraconazole, and ketoconazole) were highly effective in vitro.

Guarro, Josep; Akiti, Tiyomi; Horta, Roberto Almada-; Morizot Leite-Filho, L. A.; Gene, Josepa; Ferreira-Gomes, Sueli; Aguilar, Carme; Ortoneda, Montserrat



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


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. PMID:18077044

Hassan, Yousef I; Bullerman, Lloyd B



Designing and Synthesis of Antifungal Active Macrocyclic Ligand and Its Complexes Derived from Diethylphthalate and Benzidine  

PubMed Central

Three novel complexes of Cu(II), Co(II) and Zn(II) using a macrocyclic ligand derived by the condensation of diethylphthalate and benzidine have been designed,synthesized and characterized by UV-Vis.,IR,Mass and Elemental analyses data in order to find out their antifungal activities. The stoichiometry of the complexes has been found to be 1 : 1 (Metal : Ligand). The analytical data indicate that the complexes exhibit square-planar geometry. The antifungal activity of the macrocyclic ligand and its metal complexes has been screened in vitro against fungi such as Aspergillus niger, A. flavus, Trichoderma harizanum, T. viridae and Rhizoctonia solani.

Parameswari, S.



Antifungal activity in human urine and serum after ingestion of garlic (Allium sativum).  

PubMed Central

A fresh extract of garlic (Allium sativum) was administered orally to human volunteers. At intervals, serum and urine were collected and assayed for antifungal activity. The maximum tolerable dose was determined to be 25 ml of garlic extract. Larger amounts caused severe burning sensations in the esophagus and the stomach and vomiting. After oral ingestion of 25 ml of the extract, anticandidal and anticryptococcal activities were detected in undiluted serum 0.5 and 1 h after ingestion. No detectable antifungal activity was found in the excreted urine at any time after oral ingestion. Oral garlic is of limited value in the therapy of human fungal infections.

Caporaso, N; Smith, S M; Eng, R H



Antifungal activity of statins and their interaction with amphotericin B against clinically important Zygomycetes.  


The in vitro antifungal activity of different statins and the combinations of the two most effective ones (fluvastatin and rosuvastatin) with amphotericin B were investigated in this study on 6 fungal isolates representing 4 clinically important genera, namely Absidia, Rhizomucor, Rhizopus and Syncephalastrum . The antifungal effects of statins revealed substantial differences. The synthetic statins proved to be more effective than the fungal metabolites. All investigated strains proved to be sensitive to fluvastatin. Fluvastatin and rosuvastatin acted synergistically and additively with amphotericin B in inhibiting the fungal growth in clinically available concentration ranges. Results suggest that statins combined with amphotericin B have a therapeutic potential against fungal infections caused by Zygomycetes species. PMID:20724281

Galgóczy, L; Lukács, Gyöngyi; Nyilasi, Ildikó; Papp, T; Vágvölgyi, Cs



Synthesis, antifungal, haemolytic and cytotoxic activities of a series of bis(alkylpyridinium)alkanes.  


A series of bis(alkylpyridinium)alkanes with a twelve carbon spacer between the positive charges was synthesised and their antifungal activity has been investigated. Compounds with 2-pentyl, 4-pentyl, 4-hexyl, 4-octyl, 4-propylbenzene, 3,4-dipentyl, 4-(5'-nonyl) and 3-methyl,4-pentyl head groups were the most potent antifungal agents with MICs in the range of 1.4-2.7 microM against reference strains of both Cryptococcus neoformans and Candida albicans. PMID:19665385

Obando, Daniel; Pantarat, Namfon; Handke, Rosemary; Koda, Yasuko; Widmer, Fred; Djordjevic, Julianne T; Ellis, David H; Sorrell, Tania C; Jolliffe, Katrina A



Antifungal susceptibility of invasive yeast isolates in Italy: the GISIA3 study in critically ill patients  

Microsoft Academic Search

Background  Yeasts are a common cause of invasive fungal infections in critically ill patients. Antifungal susceptibility testing results\\u000a of clinically significant fungal strains are of interest to physicians, enabling them to adopt appropriate strategies for\\u000a empiric and prophylactic therapies. We investigated the antifungal susceptibility of yeasts isolated over a 2-year period\\u000a from hospitalised patients with invasive yeast infections.\\u000a \\u000a \\u000a \\u000a \\u000a Methods  638 yeasts were

Giulia Morace; Elisa Borghi; Roberta Iatta; Gerardino Amato; Stefano Andreoni; Gioconda Brigante; Claudio Farina; Giuliana Lo Cascio; Gianluigi Lombardi; Ester Manso; Michele Mussap; Patrizia Pecile; Roberto Rigoli; Elisabetta Tangorra; Maria Valmarin; Maria Teresa Montagna



First Simultaneous Isolation of a Ribosome Inactivating Protein and an Antifungal Protein from a Mushroom ( Lyophyllum shimeji) Together with Evidence for Synergism of their Antifungal Effects  

Microsoft Academic Search

From the fruiting bodies of the mushroom Lyophyllum shimeji, a novel ribosome inactivating protein with a molecular weight of 20 kDa and exhibiting antifungal activity against Physalospora piricola (IC50 = 2.5 ?M) and Coprinus comatus was isolated. The protein, designated lyophyllin, was purified by ion exchange chromatography on CM–cellulose, affinity chromatography on Affi-gel Blue Gel, and then ion exchange chromatography

S. K. Lam; T. B. Ng



Interlaboratory Evaluation of Etest Method for Testing Antifungal Susceptibilities of Pathogenic Yeasts to Five Antifungal Agents by Using Casitone Agar and Solidified RPMI 1640 Medium with 2% Glucose  

Microsoft Academic Search

An interlaboratory evaluation (two centers) of the Etest method was conducted for testing the antifungal susceptibilities of yeasts. The MICs of amphotericin B,fluconazole,flucytosine, itraconazole, and ketoconazole were determined for 83 isolates ofCandidaspp.,Cryptococcus neoformans, andTorulopsis glabrata. Two buffered (phosphate buffer) culture media were evaluated: solidified RPMI 1640 medium with 2% glucose and Casitone agar. MIC endpoints were determined after both 24




Novel micelle formulations to increase cutaneous bioavailability of azole antifungals.  


Efficient topical drug administration for the treatment of superficial fungal infections would deliver the therapeutic agent to the target compartment and reduce the risk of systemic side effects. However, the physicochemical properties of the commonly used azole antifungals make their formulation a considerable challenge. The objective of the present investigation was to develop aqueous micelle solutions of clotrimazole (CLZ), econazole nitrate (ECZ) and fluconazole (FLZ) using novel amphiphilic methoxy-poly(ethylene glycol)-hexyl substituted polylactide (MPEG-hexPLA) block copolymers. The CLZ, ECZ and FLZ formulations were characterized with respect to drug loading and micelle size. The optimal drug formulation was selected for skin transport studies that were performed using full thickness porcine and human skin. Penetration pathways and micellar distribution in the skin were visualized using fluorescein loaded micelles and confocal laser scanning microscopy. The hydrodynamic diameters of the azole loaded micelles were between 70 and 165nm and the corresponding number weighted diameters (d(n)) were 30 to 40nm. Somewhat surprisingly, the lowest loading efficiency (<20%) was observed for CLZ (the most hydrophobic of the three azoles tested); in contrast, under the same conditions, ECZ was incorporated with an efficiency of 98.3% in MPEG-dihexPLA micelles. Based on the characterization data and preliminary transport experiments, ECZ loaded MPEG-dihexPLA micelles (concentration 1.3mg/mL; d(n)<40nm) were selected for further study. ECZ delivery was compared to that from Pevaryl® cream (1% w/w ECZ), a marketed liposomal formulation for topical application. ECZ deposition in porcine skin following 6h application using the MPEG-dihexPLA micelles was >13-fold higher than that from Pevaryl® cream (22.8±3.8 and 1.7±0.6?g/cm(2), respectively). A significant enhancement was also observed with human skin; the amounts of ECZ deposited were 11.3±1.6 and 1.5±0.4?g/cm(2), respectively (i.e., a 7.5-fold improvement in delivery). Confocal laser scanning microscopy images supported the hypothesis that the higher delivery observed in porcine skin was due to a larger contribution of the follicular penetration pathway. In conclusion, the significant increase in ECZ skin deposition achieved using the MPEG-dihexPLA micelles demonstrates their ability to improve cutaneous drug bioavailability; this may translate into improved clinical efficacy in vivo. Moreover, these micelle systems may also enable targeting of the hair follicle and this will be investigated in future studies. PMID:21397643

Bachhav, Y G; Mondon, K; Kalia, Y N; Gurny, R; Möller, M



Candida albicans Biofilms Produce Antifungal-Tolerant Persister Cells?  

PubMed Central

Fungal pathogens form biofilms that are highly recalcitrant to antimicrobial therapy. The expression of multidrug resistance pumps in young biofilms has been linked to increased resistance to azoles, but this mechanism does not seem to underlie the resistance of mature biofilms that is a model of in vivo infection. The mechanism of drug resistance of mature biofilms remains largely unknown. We report that biofilms formed by the major human pathogen Candida albicans exhibited a strikingly biphasic killing pattern in response to two microbicidal agents, amphotericin B, a polyene antifungal, and chlorhexidine, an antiseptic, indicating that a subpopulation of highly tolerant cells, termed persisters, existed. The extent of killing with a combination of amphotericin B and chlorhexidine was similar to that observed with individually added antimicrobials. Thus, surviving persisters form a multidrug-tolerant subpopulation. Interestingly, surviving C. albicans persisters were detected only in biofilms and not in exponentially growing or stationary-phase planktonic populations. Reinoculation of cells that survived killing of the biofilm by amphotericin B produced a new biofilm with a new subpopulation of persisters. This suggests that C. albicans persisters are not mutants but phenotypic variants of the wild type. Using a stain for dead cells, rare dark cells were visible in a biofilm after amphotericin B treatment, and a bright and a dim population were physically sorted from this biofilm. Only the dim cells produced colonies, showing that this method allows the isolation of yeast persisters. Given that persisters formed only in biofilms, mutants defective in biofilm formation were examined for tolerance of amphotericin B. All of the known mutants affected in biofilm formation were able to produce normal levels of persisters. This finding indicates that attachment rather than formation of a complex biofilm architecture initiates persister formation. Bacteria produce multidrug-tolerant persister cells in both planktonic and biofilm populations, and it appears that yeasts and bacteria have evolved analogous strategies that assign the function of survival to a small part of the population. In bacteria, persisters are dormant cells. It remains to be seen whether attachment initiates dormancy that leads to the formation of fungal persisters. This study suggests that persisters may be largely responsible for the multidrug tolerance of fungal biofilms.

LaFleur, Michael D.; Kumamoto, Carol A.; Lewis, Kim



Identification of antifungal natural products via Saccharomyces cerevisiae bioassay: insights into macrotetrolide drug spectrum, potency and mode of action  

PubMed Central

Since current antifungal drugs have not kept pace with the escalating medical demands of fungal infections, new, effective medications are required. However, antifungal drug discovery is hindered by the evolutionary similarity of mammalian and fungal cells, which results in fungal drug targets having human homologs and drug non-selectivity. The group III hybrid histidine kinases (HHKs) are an attractive drug target since they are conserved in fungi and absent in mammals. We used a Saccharomyces cerevisiae reporter strain that conditionally expresses HHK to establish a high-throughput bioassay to screen microbial extracts natural products for antifungals. We identified macrotetrolides, a group of related ionophores thought to exhibit restricted antifungal activity. In addition to confirming the use of this bioassay for the discovery of antifungal natural products, we demonstrated broader, more potent fungistatic activity of the macrotetrolides against multiple Candida spp., Cryptococcus spp., and Candida albicans in biofilms. Macrotetrolides were also active in an animal model of C. albicans biofilm, but were found to have inconsistent activity against fluconazole-resistant C. albicans, with most isolates resistant to this natural product. The macrotetrolides do not directly target HHKs, but their selective activity against S. cerevisiae grown in galactose (regardless of Drk1 expression) revealed potential new insight into the role of ion transport in the mode of action of these promising antifungal compounds. Thus, this simple, high-throughput bioassay permitted us to screen microbial extracts, identify natural products as antifungal drugs, and expand our understanding of the activity of macrotetrolides.

Tebbets, Brad; Yu, Zhiguo; Stewart, Douglas; Zhao, Li-Xing; Jiang, Yi; Xu, Li-Hua; Andes, David; Shen, Ben; Klein, Bruce



Ketoconazole, an oral antifungal: laboratory and clinical assessment of imidazole drugs  

Microsoft Academic Search

Miconazole, a parenterally administered imidazole antifungal agent has been shown to produce responses in systemic fungal infections in man. Ketoconazole, an analogue, can be given by mouth. It is inhibitory in vitro at low concentrations to most fungi. Blood levels after oral administration to animals and man greatly exceed these inhibitory concentrations for several hours. The efficacy of this drug

D. Borelli; J. L. Bran; J. Fuentes; R. Legendre; E. Leiderman; H. B. Levine; A. Restrepo; D. A. Stevens



Antifungal susceptibilities of Cryptococcus neoformans cerebrospinal fluid isolates from AIDS patients in Kenya.  


Poor susceptibility of Cryptococcus neoformans to fluconazole (FLC) is a matter of concern among clinicians in Africa. The emergence of resistance to FLC was recently reported in Kenya, but it is not known whether it is widespread. Thus, there is need for more antifungal drug susceptibility studies in Kenya. The aim of this study was to measure the in vitro antifungal drug susceptibilities of incident C. neoformans isolates from acquired immunodeficiency syndrome patients in Kenya. Antifungal susceptibility testing was performed in 67 C. neoformans isolates by broth microdilution method as outlined in the Clinical and Laboratory Standards Institute document M27-A3 using FLC, amphotericin B (AMB), voriconazole (VOR), ravuconazole (RAV) and flucytosine (5-FC). Isolates were grown on l-canavanine glycine bromothymol blue medium for serotype identification. Six per cent of the isolates were identified as C. neoformans var. gattii serotype B or C and 94% as C. neoformans var. neoformans. All isolates tested were susceptible to AMB, VOR and RAV (100%), and high susceptibilities were seen to FLC (97%), and 5-FC (90%). Only 3% and 10% of the isolates' susceptibility to FLC and 5-FC, respectively, was dose-dependent or intermediate. These results demonstrate high susceptibilities of incident C. neoformans isolates to FLC and AMB, antifungals used for treatment of cryptococcal meningitis in Kenya. PMID:21535451

Mdodo, Rennatus; Moser, Stephen A; Jaoko, Walter; Baddley, John; Pappas, Peter; Kempf, Mirjam-Colette; Aban, Inmaculada; Odera, Susan; Jolly, Pauline



Antifungal effect of different methyl and propyl paraben mixtures on the treatment of paper biodeterioration  

Microsoft Academic Search

With many important artistic works and documents made of paper, and thus susceptible to biodeterioration by fungi, research is required in an effort to replace toxic chemical products with other more benign ones. In this work the antifungal effect of methyl and propyl paraben mixtures at different concentrations was evaluated. The fungi used in the experiments were a Cladosporium species

Eva Raquel Neves; Stephan Schäfer; Alan Phillips; João Canejo; Maria Filomena Macedo



Aspergillus tanneri sp. nov, a new pathogenic Aspergillus that causes invasive disease refractory to antifungal therapy  

Technology Transfer Automated Retrieval System (TEKTRAN)

This is the first report documenting fatal invasive aspergillosis caused by a new pathogenic Aspergillus species that is inherently resistant to antifungal drugs. Phenotypic characteristics of A. tanneri combined with the molecular approach enabled diagnosis of this new pathogen. This study undersco...


Argentinean propolis from Zuccagnia punctata Cav. (Caesalpinieae) exudates: phytochemical characterization and antifungal activity.  


This paper reports the in vitro antifungal activity of propolis extracts from the province of Tucuman (Argentina) as well as the identification of their main antifungal compounds and botanical origin. The antifungal activity was determined by the microdilution technique, using reference microorganisms and clinical isolates. All dermatophytes and yeasts tested were strongly inhibited by different propolis extracts (MICs between 16 and 125 microg mL(-1)). The most susceptible species were Microsporum gypseum, Trichophyton mentagrophytes, and Trichophyton rubrum. The main bioactive compounds were 2',4'-dihydroxy-3'-methoxychalcone 2 and 2',4'-dihydroxychalcone 3. Both displayed strong activity against clinical isolates of T. rubrum and T. mentagrophytes (MICs and MFCs between 1.9 and 2.9 microg mL(-1)). Additionally, galangin 5, pinocembrin 6, and 7-hydroxy-8-methoxyflavanone 9 were isolated from propolis samples and Zuccagnia punctata exudates, showing moderate antifungal activity. This is the first study matching the chemical profile of Z. punctata Cav. exudates with their corresponding propolis, giving strong evidence on the botanical origin of the studied propolis. PMID:19916546

Agüero, María Belén; Gonzalez, Mariela; Lima, Beatriz; Svetaz, Laura; Sánchez, Marianela; Zacchino, Susana; Feresin, Gabriela Egly; Schmeda-Hirschmann, Guillermo; Palermo, Jorge; Wunderlin, Daniel; Tapia, Alejandro



The Petasis Reaction: Microscale Synthesis of a Tertiary Amine Antifungal Analog  

ERIC Educational Resources Information Center

|Students prepare a tertiary amine antifungal analog in an upper-level undergraduate organic laboratory. A microscale Petasis reaction is performed to generate a liquid compound readily characterized via IR and proton NMR spectroscopy. The biological relevance of the product is highlighted, with the tertiary amine scaffold being an important…

Koroluk, Katherine J.; Jackson, Derek A.; Dicks, Andrew P.



Limitations of antifungal agents in the treatment of Candida vaginitis: future challenges  

Microsoft Academic Search

The availability of several potent antifungal agents, systemic or topical, over the counter or prescription would suggest that therapeutic needs for Candida vaginitis are minimal or absent. Unfortunately, unmet needs still exist. Moreover, the pharmaceutical industry has abandoned Candida vaginitis and no new agents or studies are imminent. Perhaps the most important advance in the last decade has been the

Jack D. Sobel



Rhizocticin A, an antifungal phosphono-oligopeptide of Bacillus subtilis ATCC 6633: biological properties  

Microsoft Academic Search

Rhizocticin A, the main component of the antifungal, hydrophilic phosphono-oligopeptides of Bacillus subtilis ATCC 6633, was used for sensitivity testing and experiments into the molecular mechanism of the antibiotic action. Budding and filamentous fungi as well as the cultivated nematode Caenorhabditis elegans were found to be sensitive, whereas bacteria and the protozoon Paramecium caudatum were insensitive. Rhizoctonia solani was inhibited

Martin Kugler; Wolfgang Loeffler; Claudius Rapp; Armin Kern; Giinther Jung



Multilaboratory Testing of Antifungal Combinations against a Quality Control Isolate of Candida krusei  

Microsoft Academic Search

Several new antifungal agents (caspofungin (CSP), posacon- azole (PSC), and voriconazole (VRC)) have recently become available for the treatment of deeply invasive fungal infections. These drugs are reported to vary in terms of efficacy, bioavail- ability, and tissue penetration in infections caused by patho- genic molds and yeasts (6, 17). They have been tested in the laboratory against a wide

Vishnu Chaturvedi; Rama Ramani; Mahmoud A. Ghannoum; Scott B. Killian; Nicole Holliday; Cindy Knapp; Luis Ostrosky-Zeichner; Shawn A. Messer; Michael A. Pfaller; Naureen J. Iqbal; Beth A. Arthington-Skaggs; Jose A. Vazquez; Tin Sein; John H. Rex; Thomas J. Walsh



In Vitro Activities of the New Antifungal Triazole SCH 56592 against Common and Emerging Yeast Pathogens  

Microsoft Academic Search

A broth microdilution method performed in accordance with the National Committee for Clinical Labora- tory Standards guidelines was used to compare the in vitro activity of the new antifungal triazole SCH 56592 (SCH) to that of fluconazole (FLC), itraconazole (ITC), and ketoconazole (KETO) against 257 clinical yeast isolates. They included 220 isolates belonging to 12 different species of Candida, 15




Genetic analysis of the antifungal activity of a soilborne Pseudomonas aureofaciens strain.  

PubMed Central

Pseudomonas aureofaciens Q2-87 produces the antibiotic 2,4-diacetophloroglucinol (Phl), which inhibits Gaeumannomyces graminis var. tritici and other fungi in vitro. Strain Q2-87 also provides biological control of take-all, a root disease of wheat caused by this fungus. To assess the role of Phl in the antifungal activity of strain Q2-87, a genetic analysis of antibiotic production was conducted. Two mutants of Q2-87 with altered antifungal activity were isolated by site-directed mutagenesis with Tn5. One mutant, Q2-87::Tn5-1, did not inhibit G. graminis var. tritici in vitro and did not produce Phl. Two cosmids were isolated from a genomic library of the wild-type strain by probing with the mutant genomic fragment. Antifungal activity and Phl production were coordinately restored in Q2-87::Tn5-1 by complementation with either cosmid. Mobilization of one of these cosmids into two heterologous Pseudomonas strains conferred the ability to synthesize Phl and increased their activity against G. graminis var. tritici, Pythium ultimum, and Rhizoctonia solani in vitro. Subcloning and deletion analysis of these cosmids identified a 4.8-kb region which was necessary for Phl synthesis and antifungal activity. Images

Vincent, M N; Harrison, L A; Brackin, J M; Kovacevich, P A; Mukerji, P; Weller, D M; Pierson, E A



Investigating the antifungal activity of TiO2 nanoparticles deposited on branched carbon nanotube arrays  

NASA Astrophysics Data System (ADS)

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. TiO2 nanoparticles on the branched CNTs were produced by atmospheric pressure chemical vapour deposition followed by a 500 °C annealing step. Transmission and scanning electron microscopic techniques were used to study the morphology of the TiO2/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 TiO2/CNT arrays and thin films of TiO2. The TiO2/branched CNTs showed a highly improved photocatalytic antifungal activity in comparison with the TiO2/CNTs and TiO2 film. The excellent visible light-induced photocatalytic antifungal activity of the TiO2/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.

Darbari, S.; Abdi, Y.; Haghighi, F.; Mohajerzadeh, S.; Haghighi, N.



Imaging mass spectrometry and genome mining reveal highly antifungal virulence factor of mushroom soft rot pathogen.  


Caught in the act: imaging mass spectrometry of a button mushroom infected with the soft rot pathogen Janthinobacterium agaricidamnosum in conjunction with genome mining revealed jagaricin as a highly antifungal virulence factor that is not produced under standard cultivation conditions. The structure of jagaricin was rigorously elucidated by a combination of physicochemical analyses, chemical derivatization, and bioinformatics. PMID:23161559

Graupner, Katharina; Scherlach, Kirstin; Bretschneider, Tom; Lackner, Gerald; Roth, Martin; Gross, Harald; Hertweck, Christian



Maclafungin, a new antifungal macrocyclic lactone from Actinomycete sp. Y-8521050  

Microsoft Academic Search

A new antifungal macrocyclic lactone maclafungin, belonging to the oligomycin class has been isolated from an actinomycete sp. Y-8521050. The antibiotic, having a molecular formula of C46H80O12, is active against several fungal species. Its structure was elucidated by analysis of 2D NMR experiments.

H.-W. Fehlhaber; H. Kogler



An Antifungal Agent Produced by Streptomyces olivaceiscleroticus, AZ-SH514  

Microsoft Academic Search

This work was carried out in the course of a screening program for specific the bioactive substances that demonstrated inhibitory affects against pathogenic fungi from actinomycetes strains. Forty five Streptomyces strains were isolated from soil sample collected from El-Sharkia governorate, Egypt. All these strains were screened for their antifungal activity against pathogenic fungi. Among the forty five Streptomyces, the broad

Houssam M. Atta


Isolating antifungals from fungus-growing ant symbionts using a genome-guided chemistry approach.  


We describe methods used to isolate and identify antifungal compounds from actinomycete strains associated with the leaf-cutter ant Acromyrmex octospinosus. These ants use antibiotics produced by symbiotic actinomycete bacteria to protect themselves and their fungal cultivar against bacterial and fungal infections. The fungal cultivar serves as the sole food source for the ant colony, which can number up to tens of thousands of individuals. We describe how we isolate bacteria from leaf-cutter ants collected in Trinidad and analyze the antifungal compounds made by two of these strains (Pseudonocardia and Streptomyces spp.), using a combination of genome analysis, mutagenesis, and chemical isolation. These methods should be generalizable to a wide variety of insect-symbiont situations. Although more time consuming than traditional activity-guided fractionation methods, this approach provides a powerful technique for unlocking the complete biosynthetic potential of individual strains and for avoiding the problems of rediscovery of known compounds. We describe the discovery of a novel nystatin compound, named nystatin P1, and identification of the biosynthetic pathway for antimycins, compounds that were first described more than 60 years ago. We also report that disruption of two known antifungal pathways in a single Streptomyces strain has revealed a third, and likely novel, antifungal plus four more pathways with unknown products. This validates our approach, which clearly has the potential to identify numerous new compounds, even from well-characterized actinomycete strains. PMID:23084933

Seipke, Ryan F; Grüschow, Sabine; Goss, Rebecca J M; Hutchings, Matthew I



Microbial hydroxylation of rustmicin (galbonolide A) and galbonolide B, two antifungal products produced by Micromonospora sp  

Microsoft Academic Search

In order to synthesize derivatives of galbonolide A and B with improved chemical stability and antifungal activity profiles, a panel of microorganisms consisting of various species of actinomycetes and fungi were screened. As a result, an organism, Streptomyces halstedii, was identified, which catalyzed the formation of two polar compounds, one from each of the galbonolides. The synthesis and the relative

A Shafiee; G Harris; H Motamedi; M Rosenbach; T Chen; D Zink; B Heimbuch



Voriconazole versus itraconazole for antifungal prophylaxis following allogeneic haematopoietic stem-cell transplantation  

PubMed Central

Antifungal prophylaxis for allogeneic haematopoietic stem-cell transplant (alloHCT) recipients should prevent invasive mould and yeast infections (IFIs) and be well tolerated. This prospective, randomized, open-label, multicentre study compared the efficacy and safety of voriconazole (234 patients) versus itraconazole (255 patients) in alloHCT recipients. The primary composite endpoint, success of prophylaxis, incorporated ability to tolerate study drug for ?100 d (with ?14 d interruption) with survival to day 180 without proven/probable IFI. Success of prophylaxis was significantly higher with voriconazole than itraconazole (48·7% vs. 33·2%, P <0·01); more voriconazole patients tolerated prophylaxis for 100 d (53·6% vs. 39·0%, P<0·01; median total duration 96 vs. 68 d). The most common (>10%) treatment-related adverse events were vomiting (16·6%), nausea (15·8%) and diarrhoea (10·4%) for itraconazole, and hepatotoxicity/liver function abnormality (12·9%) for voriconazole. More itraconazole patients received other systemic antifungals (41·9% vs. 29·9%, P<0·01). There was no difference in incidence of proven/probable IFI (1·3% vs. 2·1%) or survival to day 180 (81·9% vs. 80·9%) for voriconazole and itraconazole respectively. Voriconazole was superior to itraconazole as antifungal prophylaxis after alloHCT, based on differences in the primary composite endpoint. Voriconazole could be given for significantly longer durations, with less need for other systemic antifungals.

Marks, David I; Pagliuca, Antonio; Kibbler, Christopher C; Glasmacher, Axel; Heussel, Claus-Peter; Kantecki, Michal; Miller, Paul JS; Ribaud, Patricia; Schlamm, Haran T; Solano, Carlos; Cook, Gordon



Clinical, Cellular, and Molecular Factors That Contribute to Antifungal Drug Resistance  

PubMed Central

In the past decade, the frequency of diagnosed fungal infections has risen sharply due to several factors, including the increase in the number of immunosuppressed patients resulting from the AIDS epidemic and treatments during and after organ and bone marrow transplants. Linked with the increase in fungal infections is a recent increase in the frequency with which these infections are recalcitrant to standard antifungal therapy. This review summarizes the factors that contribute to antifungal drug resistance on three levels: (i) clinical factors that result in the inability to successfully treat refractory disease; (ii) cellular factors associated with a resistant fungal strain; and (iii) molecular factors that are ultimately responsible for the resistance phenotype in the cell. Many of the clinical factors that contribute to resistance are associated with the immune status of the patient, with the pharmacology of the drugs, or with the degree or type of fungal infection present. At a cellular level, antifungal drug resistance can be the result of replacement of a susceptible strain with a more resistant strain or species or the alteration of an endogenous strain (by mutation or gene expression) to a resistant phenotype. The molecular mechanisms of resistance that have been identified to date in Candida albicans include overexpression of two types of efflux pumps, overexpression or mutation of the target enzyme, and alteration of other enzymes in the same biosynthetic pathway as the target enzyme. Since the study of antifungal drug resistance is relatively new, other factors that may also contribute to resistance are discussed.

White, Theodore C.; Marr, Kieren A.; Bowden, Raleigh A.



Antifungal susceptibilities of Cryptococcus neoformans cerebrospinal fluid isolates from AIDS patients in Kenya  

PubMed Central

Background Poor susceptibility of Cryptococcus neoformans to fluconazole (FLC) is a matter of concern among clinicians in Africa. The emergence of resistance to FLC was recently reported in Kenya but it is not known if it is widespread. Thus, there is need for more antifungal drug susceptibility studies in Kenya. Objective To measure the in vitro antifungal drug susceptibilities of incident C. neoformans isolates from acquired immunodeficiency syndrome patients in Kenya. Methods Antifungal susceptibility testing was performed on 67 C. neoformans isolates by broth microdilution method as outlined in the Clinical and Laboratory Standards Institute document M27-A3 using FLC, amphotericin B (AMB), voriconazole (VOR), ravuconazole (RAV), and flucytosine (5-FC). Isolates were grown on L-canavanine glycine bromothymol blue medium for serotype identification. Results Six percent of the isolates were identified as C. neoformans var. gattii serotype B or C and 94% as C. neoformans var. neoformans. All isolates tested were susceptible to AMB, VOR and RAV (100%), and high susceptibilities were seen to FLC (97%), and 5-FC (90%). Only 3% and 10% of the isolates’ susceptibility to FLC and 5-FC respectively, was dose dependent or intermediate. Conclusions These results demonstrate high susceptibilities of incident C. neoformans isolates to FLC and AMB, antifungals used for treatment of cryptococcal meningitis in Kenya.

Mdodo, Rennatus; Moser, Stephen A.; Jaoko, Walter; Baddley, John; Pappas, Peter; Kempf, Mirjam-Colette; Aban, Inmaculada; Odera, Susan; Jolly, Pauline



Antimycobacterial, antibacterial and antifungal activities of the methanol extract and compounds from Thecacoris annobonae (Euphorbiaceae)  

Microsoft Academic Search

This study was designed to evaluate the antimycobacterial, antibacterial and antifungal activities of the methanol extract from the stem bark of Thecacoris annobonae Pax & K. Hoffm, that of aristolochic acid I (1) and other isolated compounds. The microplate alamar blue assay (MABA) and the broth microdilution method were used to determine the minimal inhibitory concentration (MIC) and minimal microbicidal

V. Kuete; H. M. Poumale Poumale; A. N. Guedem; Y. Shiono; R. Randrianasolo; B. T. Ngadjui



Antifungal activities of anise oil, lime oil, and tangerine oil against molds on rubberwood ( Hevea brasiliensis)  

Microsoft Academic Search

The antifungal activities of anise oil, lime oil, and tangerine oil against molds identified from rubberwood surfaces (Aspergillus niger, Penicillium chrysogenum, and Penicillium sp.) were investigated. The broth dilution method was employed to determine the minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) using the concentration of essential oils between 20 and 200?lml?1. Inhibitory effects of the essential oils

Narumol Matan; Nirundorn Matan



Isolation, identification and antifungal susceptibility of lemon pathogenic and non pathogenic fungi  

Microsoft Academic Search

Numerous species of filamentous fungi were isolated from lemon on different plantations in the province of Tucuman, Argentina. The techniques suggested by the Subcommittee of Antifungal Susceptibility of the National Committee for Clinical Laboratory Standards, (USA) were adapted. The effect of three different concentrations of the fungicides imazalil, guazatine, SOPP and thiabendazole on the fungi Fusarium oxysporum, Fusarium moniliforme, Aspergillus

María Cristina Maldonado; Rosa Santa Runco; Antonio Roberto Navarro


Molecular structure of terrecyclodiol: a derivative of the antifungal metabolite terrecyclic acid A from Aspergillus terreus.  


A strain of Aspergillus terreus, which was isolated from organic mulch and inhibited the growth of the plant pathogen Phytophthora cinnamomi, produces an antifungal metabolite when grown in liquid culture. This metabolite was isolated by bioassay-guided fractionation and identified as terrecyclic acid A (1). X-ray diffraction studies and spectroscopic details of the derived terrecyclodiol (2) are described. PMID:8984154

Almassi, F; Ghisalberti, E L; Skelton, B W; White, A H



Antifungal Activity of Aqueous Extracts of the Leaves of Cowparsnip and Comfrey  

Microsoft Academic Search

We found that extracts from the leaves of medicinal comfrey and cowparsnip strongly inhibit the germination of Erysiphe graminisconidia and uredospores of Puccinia graminis. Spraying wheat seedlings with these extracts, in contrast to the irrigation of soil, markedly diminished infection in plants with powdery mildew. Antifungal activity in vitroand protective activity (when plants were sprayed) correlated with the level of

V. A. Karavaev; M. K. Solntsev; T. P. Yurina; E. V. Yurina; I. B. Polyakova; A. M. Kuznetsov



Lipid Formulations of Polyene Antifungal Drugs and Attenuation of Associated Nephrotoxicity  

Microsoft Academic Search

Amphotericin B is an effective broad-spectrum antifungal agent, but various side effects, especially nephrotoxicity, have restricted its use. Recently, lipid formulations of amphotericin B have been developed in order to reduce its toxic side effects. Clinical trials, although in the early stages, suggest promising results, and that some of these lipid formulations are potent and less toxic, even at higher

M. S. Razzaque; M. A. Hossain; N. Ahsan; T. Taguchi



Synthesis of hydrophospohoryl derivatives of the antifungal antibiotic pimaricin by the Kabachnik-Fields reaction  

Microsoft Academic Search

Reactions of the polyene macrolide antibiotic pimaricin with aromatic aldehydes and hypophosphorous acid are shown to afford\\u000a pimaricin hydrophosphoryl derivatives. Physicochemical and biological properties of these compounds are explored. Biological\\u000a studies indicated that the pimaricin hydrophosphoryl derivatives are low toxic agents possessing a high antifungal activity.

V. V. Belakhov; Yu. D. Shenin; B. I. Ionin



Identification of Novel Pharmacological Activities of an Antifungal Agent, Nystatin, to Promote Dendritic Cell Maturation  

Microsoft Academic Search

As an unbiased functional screen to identify agents activating dendritic cells (DCs), we recently developed a DC-based biosensor system, in which a stable murine DC line XS106 was engineered to express the yellow fluorescent protein (YFP) gene under the control of the IL-1? promoter. Here we report that nystatin (NYT), an antifungal drug of the family of polyene macrolide antibiotics,

Yasushi Ogawa; Norikatsu Mizumoto; Hiroaki Tanaka; Hironori Matsushima; Akira Takashima



A first convergent synthesis of the polyolic fragment of the antifungal pentaene macrolide strevertene A  

Microsoft Academic Search

The C(4–14) polyolic segment of antifungal macrolide strevertenes has been synthesized for the first time in protected form, incorporating four stereogenic centers. The synthetic strategy developed is based on the connection of two subunits prepared starting from the same chiral building block.

Carlo Bonini; Lucia Chiummiento; Maria Funicello; Paolo Lupattelli; Valeria Videtta



New advances in fatty acids as antimalarial, antimycobacterial and antifungal agents  

Microsoft Academic Search

This review deals with the most recent findings on the antimalarial, antimycobacterial, and antifungal properties of fatty acids, with particular emphasis on novel marine fatty acids. The first section deals with the most recent and some background literature on what has been the latest developments with respect to fatty acids as antimalarial agents and the importance of enzyme inhibition, in

N. M. Carballeira



Antifungal compounds from Melia azedarach leaves for management of Ascochyta rabiei, the cause of chickpea blight  

Microsoft Academic Search

The antifungal activity of Melia azedarach L. leaves was investigated against Ascochyta rabiei (Pass.) Lab., the cause of destructive blight disease of chickpea (Cicer arietinum L.). Bioassay guided fractionation revealed that the chloroform fraction of the methanolic extract of M. azedarach leaves was highly effective against A. rabiei. Six compounds, namely ?-sitosterol (1), ?-amyrin (2), ursolic acid (3), benzoic acid

Khajista Jabeen; Arshad Javaid; Ejaz Ahmad; Makshoof Athar



Antifungal Activity of Chitosan Nanoparticles and Correlation with Their Physical Properties  

PubMed Central

The need of natural antimicrobials is paramount to avoid harmful synthetic chemicals. The study aimed to determine the antifungal activity of natural compound chitosan and its nanoparticles forms against Candida albicans, Fusarium solani and Aspergillus niger. Chitosan nanoparticles were prepared from low (LMW), high molecular weight (HMW) chitosan and its derivative, trimethyl chitosan (TMC). Particle size was increased when chitosan/TMC concentration was increased from 1 to 3 mg/mL. Their zeta potential ranged from +22 to +55?mV. Chitosan nanoparticles prepared from different concentrations of LMW and HMW were also found to serve a better inhibitory activity against C. albicans (MICLMW = 0.25–0.86?mg/mL and MICHMW = 0.6–1.0?mg/mL) and F. solani (MICLMW = 0.86–1.2?mg/mL and MICHMW = 0.5–1.2?mg/mL) compared to the solution form (MIC = 3?mg/mL for both MWs and species). This inhibitory effect was also influenced by particle size and zeta potential of chitosan nanoparticles. Besides, Aspergillus niger was found to be resistant to chitosan nanoparticles except for nanoparticles prepared from higher concentrations of HMW. Antifungal activity of nanoparticles prepared from TMC was negligible. The parent compound therefore could be formulated and applied as a natural antifungal agent into nanoparticles form to enhance its antifungal activity.

Ing, Ling Yien; Zin, Noraziah Mohamad; Sarwar, Atif; Katas, Haliza



Medicinal plants from Riau Province, Sumatra, Indonesia. Part 2: antibacterial and antifungal activity  

Microsoft Academic Search

Antibacterial assays of 114 species listed in Part 1 showed that 82% of the extracts tested were active against Staphylococcus aureus, while 35% were active against Escherichia coli. Antifungal activity was less dramatic: 19% of the extracts inhibited Saccharomyces cerevisiae, while 20% inhibited Fusarium oxysporum. Our survey of relevant literature indicates that less than 30% of these Angiosperm species have

Paul W. Grosvenor; Agus Supriono; David O. Gray



The Petasis Reaction: Microscale Synthesis of a Tertiary Amine Antifungal Analog  

ERIC Educational Resources Information Center

Students prepare a tertiary amine antifungal analog in an upper-level undergraduate organic laboratory. A microscale Petasis reaction is performed to generate a liquid compound readily characterized via IR and proton NMR spectroscopy. The biological relevance of the product is highlighted, with the tertiary amine scaffold being an important…

Koroluk, Katherine J.; Jackson, Derek A.; Dicks, Andrew P.



Purification and characterization of a novel antifungal protein secreted by Penicillium chrysogenum from an Arctic sediment.  


A fungal strain, Penicillium chrysogenum A096, was isolated from an Arctic sediment sample. Its culture supernatant inhibited mycelial growth of some plant pathogenic fungi. After saturation of P. chrysogenum A096 culture supernatant with ammonium sulfate and ion exchange chromatography, a novel antifungal protein (Pc-Arctin) was purified and identified by matrix assisted laser desorption ionization-time of flight-time of flight-mass spectrometry (MALDI-TOF-TOF-MS). The gene encoding for Pc-Arctin consisting of 195 nucleotides was cloned from P. chrysogenum A096 to confirm the mass spectrometry result. Pc-Arctin displays antifungal activity against Paecilomyces variotii, Alternaria longipes, and Trichoderma viride at minimum inhibitory concentrations (MIC) of 24, 48, and 192 ng/disc, respectively. Pc-Arctin was most sensitive to proteinase K and then to trypsin but insensitive to papain. Pc-Arctin possesses high thermostability and cannot be antagonized by common surfactants, except for sodium dodecyl sulfate (SDS). Divalent ions, such as Mn(2+), Mg(2+), and Zn(2+), inhibited the antifungal activity of Pc-Arctin. Hemagglutination assays showed that Pc-Arctin had no hemagglutinating or hemolytic activity against red blood cells (RBC) from rabbits, rats, and guinea pigs. Therefore, Pc-Arctin from Arctic P. chrysogenum may represent a novel antifungal protein with potential for application in controlling plant pathogenic fungal infection. PMID:23474616

Chen, Zhiteng; Ao, Jingqun; Yang, Wenchuan; Jiao, Liping; Zheng, Tianling; Chen, Xinhua



Application of antifungal CFB to increase the durability of cement mortar.  


Antifungal cement mortar or microbiological calcium carbonate precipitation on cement surface has been investigated as functional concrete research. However, these research concepts have never been fused with each other. In this study, we introduced the antifungal calciteforming bacteria (CFB) Bacillus aryabhattai KNUC205, isolated from an urban tunnel (Daegu, South Korea). The major fungal deteriogens in urban tunnel, Cladosporium sphaerospermum KNUC253, was used as a sensitive fungal strain. B. aryabhattai KNUC205 showed CaCO3 precipitation on B4 medium. Cracked cement mortar pastes were made and neutralized by modified methods. Subsequently, the mixture of B. aryabhattai KNUC205, conidiospore of C. sphaerospermum KNUC253, and B4 agar was applied to cement cracks and incubated at 18 degrees C for 16 days. B. aryabhattai KNUC205 showed fungal growth inhibition against C. sphaerospermum. Furthermore, B. aryabhattai KNUC205 showed crack remediation ability and water permeability reduction of cement mortar pastes. Taken together, these results suggest that the CaCO3 precipitation and antifungal properties of B. aryabhattai KNUC205 could be used as an effective sealing or coating material that can also prevent deteriorative fungal growth. This study is the first application and evaluation research that incorporates calcite formation with antifungal capabilities of microorganisms for an environment-friendly and more effective protection of cement materials. In this research, the conception of microbial construction materials was expanded. PMID:22580322

Park, Jong-Myong; Park, Sung-Jin; Kim, Wha-Jung; Ghim, Sa-Youl



Antibiotics from basidiomycetes. IX. Oudemansin, an antifungal antibiotic from Oudemansiella mucida (Schrader ex Fr.) Hoehnel (Agaricales).  


From mycelial cultures of Oudemansiella mucida a crystalline optically active antibiotic, oudemansin (2), has been isolated; its structure is closely related to strobilurin A (1). The relative configuration of oudemansin have been determined by X-ray analysis. The antibiotic exhibits strong antifungal properties and inhibits respiration in fungi, cells of the ascitic form of EHRLICH carcinoma, and rat liver mitochondria. PMID:528381

Anke, T; Hecht, H J; Schramm, G; Steglich, W



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

Technology Transfer Automated Retrieval System (TEKTRAN)

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...


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


With an aim to discover novel chitosan derivatives with significant activities against crop-threatening fungi, (1,2,3-triazol-4-yl)methyl nicotinate chitosan (TAMNCS) was prepared via azide-alkyne click reaction. Its structure was characterized by FT-IR, (1)H NMR, elemental analysis, DSC, and SEM. In vitro antifungal properties of TAMNCS against Rhizoctonia solani Kühn (R. solani), Stemphylium solani weber (S. solani), and Alternaria porri (A. porri) were studied at the concentrations ranged from 0.25mg/mL to 1.0mg/mL. Experiments conducted displayed the derivative had obviously enhanced antifungal activity after chemical modification compared with original chitosan. Moreover, it was shown that TAMNCS can 94.2% inhibit growth of A. porri at 1.0mg/mL, while dose at which the fungicide triadimefon had lower inhibitory index (62.2%). The primary antifungal results described here indicate this derivative may be a promising candidate as an antifungal agent. PMID:23732332

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



Identification and use of potential bacterial organic antifungal volatiles in biocontrol  

Microsoft Academic Search

Bacteria, isolated from canola and soybean plants, produced antifungal organic volatile compounds. These compounds inhibited sclerotia and ascospore germination, and mycelial growth of Sclerotinia sclerotiorum, in vitro and in soil tests. Ascospore germination in cavity slides was inhibited 54–90% by the volatile producers. When mycelial plugs or the sclerotia, exposed to these volatiles, were transferred to fresh agar plates, the

W. G. Dilantha Fernando; Rajesh Ramarathnam; Akkanas S. Krishnamoorthy; Sarah C. Savchuk



Experimental Models in Predicting Topical Antifungal Efficacy: Practical Aspects and Challenges  

Microsoft Academic Search

What are efficient screening models for improved topical antifungals? The use of minimum inhibitory concentrations (MICs) as one such parameter is discussed; we focus on the use of animal membranes for in vitro testing while highlighting the pros and cons of each model, exploring alternatives and discussing the importance of data transferability to humans and the influence of penetration kinetics

J. Lai; H. I. Maibach



Reliability of the WIDERYST Susceptibility Testing System for Detection of In Vitro Antifungal Resistance in Yeasts  

Microsoft Academic Search

This study evaluated the WIDERYST system, a commercially available computer-assisted image-processing device for the antifungal susceptibility testing of yeasts. A collection of 90 clinical isolates selected to represent ranges of susceptibilities in vitro as broad as possible was tested. An evaluation compared the results obtained by the new system with those achieved by both the Clinical and Laboratory Standards Institute

Manuel Cuenca-Estrella; Alicia Gomez-Lopez; M. Olga Gutierrez; M. Jose Buitrago; Juan L. Rodriguez-Tudela



Effect of Neutropenia and Treatment Delay on the Response to Antifungal Agents in Experimental Disseminated Candidiasis  

Microsoft Academic Search

Disseminated candidiasis is associated with a high rate of morbidity and mortality. The presence of neutrophils and the timely administration of antifungal agents are likely to be critical factors for a favorable therapeutic outcome of this syndrome. The effect of neutropenia on the temporal profile of the burden of Candida albicans in untreated mice and those treated with amphotericin B

William W. Hope; George L. Drusano; Caroline B. Moore; Andrew Sharp; Arnold Louie; Thomas J. Walsh; David W. Denning; Peter A. Warn



Antifungal Agents: In Vitro Susceptibility Testing, Pharmacodynamics, and Prospects for Combination Therapy  

Microsoft Academic Search

As invasive fungal infections in immunocompromised patients become increasingly important, the field of antifungal chemotherapy continues to evolve rapidly. New agents have entered the clinical arena, providing physicians with a variety of choices for treatment of most infections. Standardized methods for testing the in vitro susceptibility of fungi have become available, and concentration-effect relationships are increasingly explored. Finally, the availability

A. H. Groll; H. Kolve



The Determination of Antibacterial and Antifungal Activities of Polygonum hydropiper (L.) Root Extract  

Microsoft Academic Search

A study was conducted to determine the antibacterial and antifungal activities of Polygonum hydropiper (L.) root extract on chloroform against both bacteria and fungi using the disc diffusion method. The extract showed significant antibacterial activities against four gram-positive (Bacillus subtilis, Bacillus megaterium, Stapphylococcus aureus and Enterobacter aerogenes) and four gram-negative (Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi and Shigella sonnei) bacteria.

M. F. Hasan; Alam Khan; M. S. Hossain; M. Rahman


Antifungal activity of films and solutions based on chitosan against typical seed fungi  

Microsoft Academic Search

The use of eco-freindly polymers as antimicrobial materials is in growth due to the need to reduce the negative impact of conventional treatments on the environment and the human health. The purpose of the present study was to assess the antifungal properties of films and solutions based on chitosan with different molecular weight at different concentrations. Surfactants were added to

Khalid Ziani; Idoya Fernández-Pan; Maite Royo; Juan. I. Maté



Variations in DNA subtype, antifungal susceptibility, and slime production among clinical isolates of Candida parapsilosis  

Microsoft Academic Search

Candida parapsilosis is an important nosocomial pathogen that can proliferate in high concentrations of glucose and form biofilms on prosthetic materials. We investigated the genotypic diversity, slime production, and antifungal susceptibility among 60 isolates of C. parapsilosis from 44 patients and 10 patient care providers from five different medical centers. Molecular typing was performed using macrorestriction digest profiles with BssHII

Michael A. Pfaller; S. A. Messer; Richard J. Hollis



Successful use of combination antifungal therapy in the treatment of coccidioides meningitis.  

PubMed Central

Coccidioidal meningitis is a highly lethal condition with a high morbidity and relapse rate caused by Coccidioides immitis. This case report highlights the difficulty in diagnosing and treating coccidioidal meningitis, and discusses a novel combination antifungal therapy (voriconazole and liposomal amphotericin B), which was used to treat this patient. Images Figure 1 Figure 2

Antony, Suresh J.; Jurczyk, Peter; Brumble, Lisa



Anticancer and antifungal compounds from Aspergillus, penicillium and other filamentous fungi.  


This review covers important anticancer and antifungal compounds reported from filamentous fungi and in particular from Aspergillus, Penicillium and Talaromyces. The taxonomy of these fungi is not trivial, so a focus of this review has been to report the correct identity of the producing organisms based on substantial previous in-house chemotaxonomic studies. PMID:24064454

Bladt, Tanja Thorskov; Frisvad, Jens Christian; Knudsen, Peter Boldsen; Larsen, Thomas Ostenfeld



Antibacterial, antifungal and cytotoxic activities of amblyone isolated from Amorphophallus campanulatus  

PubMed Central

Objective: To assess the in vitro antibacterial, antifungal and cytotoxic activities of amblyone, a triterpenoid isolated from Amorphophallus campanulatus (Roxb). Methods: Disc diffusion technique was used for in vitro antibacterial and antifungal screening. Cytotoxicity was determined against brine shrimp nauplii. In addition, minimum inhibitory concentration (MIC) was determined using serial dilution technique to determine the antibacterial potency. Results: Large zones of inhibition were observed in disc diffusion antibacterial screening against four Gram-positive bacteria (Bacillus subtilis, Bacillus megaterium, Staphylococcus aureus and Streptococcus pyogenes) and six Gram-negative bacteria (Escherichia coli, Shigella dysenteriae, Shigella sonnei, Shigella flexneri, Pseudomonas aeruginosa and Salmonella typhi). The MIC values against these bacteria ranged from 8 to 64 ?g/ml. In antifungal screening, the compound showed small zones of inhibition against Aspergillus flavus, Aspergillus niger and Rhizopus aryzae. Candida albicans was resistant against the compound. In the cytotoxicity determination, LC50 of the compound against brine shrimp nauplii was 13.25 ?g/ml. Conclusions: These results suggest that the compound has good antibacterial activity against the tested bacteria, moderate cytotoxicity against brine shrimp nauplii and insignificant antifungal activity against the tested fungi.

Khan, Alam; Rahman, Moizur; Islam, M.S.



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


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, Candida parapsilosis, Candida krusei and Cryptococcus neoformans. A total of 65 crude methanol extracts belonging to 56 plant species and 38 families were screened using the broth microdilution method, according to the guidelines of the Clinical and Laboratory Standard Institute (CLSI) (formerly, National Committee for Clinical and Laboratory Standards) [National Committee for Clinical Laboratory Standards, 2002. Reference Method for Broth Dilution Antifungal Susceptibility Testing of Yeasts. Approved Standard-2nd Edition M27-A2, National Committee for Clinical Laboratory Standards, Wayne, PA, USA]. Among the tested plant species, 45% (25 species) showed antifungal activity against one or more of the test fungi. The most susceptible yeasts were Cryptococcus neoformans, followed by Candida krusei, Candida tropicalis, and Candida parapsilosis. The least susceptible were Candida albicans and Candida glabrata. Strong antifungal activity was exhibited by extracts of Clausena anisata Oliv., Sclerocariya birrea Sond, Turraea holstii Gurk, Sterculia africana (Lour) Fiori, Acacia robusta subsp. Usambarensis (Taub) Brenan, Cyphosterma hildebrandti (Gilg), Desc, Elaeodendron buchannanii (Lows), Acacia nilotica (L.) Wild ex Del, Jatropha multifida L., and Pteridium aquilinum (L.) Kuhn. PMID:16829001

Hamza, Omar J M; van den Bout-van den Beukel, Carolien J P; Matee, Mecky I N; Moshi, Mainen J; Mikx, Frans H M; Selemani, Haji O; Mbwambo, Zakaria H; Van der Ven, André J A M; Verweij, Paul E



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

Microsoft Academic Search

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, Candida parapsilosis, Candida krusei and Cryptococcus neoformans.A total of 65 crude methanol extracts belonging to 56 plant species and

Omar J. M. Hamza; Carolien J. P. van den Bout-van den Beukel; Mecky I. N. Matee; Mainen J. Moshi; Frans H. M. Mikx; Haji O. Selemani; Zakaria H. Mbwambo; André J. A. M. Van der Ven; Paul E. Verweij



Rabbit Model of Candida albicans Biofilm Infection: Liposomal Amphotericin B Antifungal Lock Therapy  

Microsoft Academic Search

Catheter-related infections due to Candida albicans biofilms are a leading cause of fungal nosocomial bloodstream infection. In this paper, we describe the development of a model of catheter-associated infection with C. albicans biofilms and show that antifungal lock therapy with liposomal amphotericin B is an effective treatment strategy for these infections. Silicone catheters surgically placed in New Zealand White rabbits

Matthew K. Schinabeck; Lisa A. Long; Mohammad A. Hossain; Jyotsna Chandra; Pranab K. Mukherjee; Sotohy Mohamed; Mahmoud A. Ghannoum



Synthesis and antifungal activity of natural product-based 6-alkyl-2 3 4 5-tetrahydropyridines  

Technology Transfer Automated Retrieval System (TEKTRAN)

Seven 6-alkyl-2,3,4,5-tetrahydropyridines (5a–5g) that mimic the natural products piperideines that were recently identified in the fire ant venom have been synthesized. Compounds 5c–5g with the C-6 alkyl chain lengths from C14 to C18 showed varying degrees of antifungal activities, with 5e (6-hexa...


[Identification of actinomycetes with antifungal activity which do not affect Rhizobium meliloti].  


Thirteen isolates of actinomycetes that have broad antifungal activity and do not affect two efficient strains of Rhizobium meliloti were identified as: Nocardia autotrophica, Streptomyces antimycoticus, S. anulatus, S. capoamus, S. lydicus, S. murinus, S. roseo-luteus, and S. thermotolerans. PMID:709436

Antoun, H; Bordeleau, L M; Gagnon, C; Lachance, R A



In vitro antifungal activity of hydroxychavicol isolated from Piper betle L  

Microsoft Academic Search

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

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



Optimization for the Production of Surfactin with a New Synergistic Antifungal Activity  

Microsoft Academic Search

BackgroundTwo of our long term efforts are to discover compounds with synergistic antifungal activity from metabolites of marine derived microbes and to optimize the production of the interesting compounds produced by microorganisms. In this respect, new applications or mechanisms of already known compounds with a high production yield could be continually identified. Surfactin is a well-known lipopeptide biosurfactant with a

Xiangyang Liu; Biao Ren; Hong Gao; Mei Liu; Huanqin Dai; Fuhang Song; Zhenyan Yu; Shujin Wang; Jiangchun Hu; Chandrakant R. Kokare; Lixin Zhang



Antifungal activity of chitosan nanoparticles and correlation with their physical properties.  


The need of natural antimicrobials is paramount to avoid harmful synthetic chemicals. The study aimed to determine the antifungal activity of natural compound chitosan and its nanoparticles forms against Candida albicans, Fusarium solani and Aspergillus niger. Chitosan nanoparticles were prepared from low (LMW), high molecular weight (HMW) chitosan and its derivative, trimethyl chitosan (TMC). Particle size was increased when chitosan/TMC concentration was increased from 1 to 3 mg/mL. Their zeta potential ranged from +22 to +55?mV. Chitosan nanoparticles prepared from different concentrations of LMW and HMW were also found to serve a better inhibitory activity against C. albicans (MIC(LMW) = 0.25-0.86?mg/mL and MIC(HMW) = 0.6-1.0?mg/mL) and F. solani (MIC(LMW) = 0.86-1.2?mg/mL and MIC(HMW) = 0.5-1.2?mg/mL) compared to the solution form (MIC = 3?mg/mL for both MWs and species). This inhibitory effect was also influenced by particle size and zeta potential of chitosan nanoparticles. Besides, Aspergillus niger was found to be resistant to chitosan nanoparticles except for nanoparticles prepared from higher concentrations of HMW. Antifungal activity of nanoparticles prepared from TMC was negligible. The parent compound therefore could be formulated and applied as a natural antifungal agent into nanoparticles form to enhance its antifungal activity. PMID:22829829

Ing, Ling Yien; Zin, Noraziah Mohamad; Sarwar, Atif; Katas, Haliza



Effectiveness of antifungal treatments during artificial incubation of the signal crayfish eggs ( Pacifastacus leniusculus Dana. Astacidae)  

Microsoft Academic Search

In artificial incubation of astacid crayfish eggs, the use of effective antifungal treatments is advisable for controlling the spread of fungi from dead to healthy eggs and increasing final efficiency rates. The aim of this study was to evaluate the effectiveness of formaldehyde, malachite green, hydrogen peroxide, isopropyl alcohol, copper sulfate, potassium permanganate and iodine (as polyvidone iodine) on signal

P. M. Melendre; J. D. Celada; J. M. Carral; M. Sáez-Royuela; A. Aguilera



Antifungal activity of crude extracts and essential oil of Moringa oleifera Lam  

Microsoft Academic Search

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

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



Relationships between Respiration and Susceptibility to Azole Antifungals in Candida glabrata  

Microsoft Academic Search

Over the past two decades, the incidence of infections due to Candida glabrata, a yeast with intrinsic low susceptibility to azole antifungals, has increased markedly. Respiratory deficiency due to mutations in mito- chondrial DNA (mtDNA) associated with resistance to azoles frequently occurs in vitro in this species. In order to specify the relationships between respiration and azole susceptibility, the effects

Sophie Brun; Christophe Aubry; Osana Lima; Robert Filmon; Thierry Berges; Dominique Chabasse; Jean-Philippe Bouchara



Emulsions of ?-cyclodextrins grafted to silicone for the transport of antifungal drugs  

Microsoft Academic Search

The transport of pharmaceutical or cosmetic active substances that are not soluble in water requires their solubilisation or encapsulation in a suitable dosage form. A material combining the solubilising properties of ?-cyclodextrins and the biocompatibility of silicone has been prepared as an aqueous emulsion and used for the encapsulation of an antifungal molecule.?-cyclodextrins have been chemically grafted to the poly(methylhydrosiloxane)

Ahlem Noomen; Souhaira Hbaieb; Hélène Parrot-Lopez; Rafik Kalfat; Hatem Fessi; Noureddine Amdouni; Yves Chevalier



Bir yýl içerisinde kan kültürlerinden izole edilen candida türlerinin daðýlýmý ve antifungal duyarlýlýklarý  

Microsoft Academic Search

Purpose: In intensive care units, 10-20% of nosocomial bloodstream infections are composed of Candida species. Candida species of normal flora omits the skin barrier by the way of invasive catheter application or endothracheal intubation and cause infections. In this study, we aimed to determine the distribution and the antifungal susceptibilities of Candida species isolated from blood cultures. Material Methods: Amphotericin

Çiðdem Kuzucu; Gülay Yetkin; Ahmet Çalýþkan



Combinations of Antifungal and Antineoplastic Drugs with Interactive Effects on Inhibition of Yeast Growth  

Microsoft Academic Search

Interactive effects among antifungal and antineoplastic drugs contributed to toxicities when combinations of these drugs were used to inhibit the growth of five Candida spp. Drug interactions were measured by growth inhibition in both liquid and solid media, by viable cell counts and by examination using scanning electron microscopy. Large cooperative effects on toxicity were demonstrated between some antineoplastic and

Mahmoud A. Ghannoum; Khaled H. Abu-Elteen; Mohamed S. Motawy; Moeen A. Abu-Hatab; Ashraf S. Ibrahim; Richard S. Criddle



Cysteine Protease Inhibitor from Pearl Millet: A New Class of Antifungal Protein  

Microsoft Academic Search

A Cysteine protease inhibitor exhibiting antifungal activity from pearl millet seeds has been purified to homogeneity by ammonium sulphate precipitation and chromatographic procedures involving CM- sephadex and SP- sepharose cation exchange columns. The molecular characterization has revealed its molecular mass as 24 kD and isoelectric point 9.8. The amino acid composition data shows presence of high content of serine and

Bimba N. Joshi; Mohini N. Sainani; Kulbhushan B. Bastawade; Vidya S. Gupta; Prabhakar K. Ranjekar



Lactobacillus coryniformis subsp. coryniformis Strain Si3 Produces a Broad-Spectrum Proteinaceous Antifungal Compound  

Microsoft Academic Search

The antifungal activity spectrum of Lactobacillus coryniformis subsp. coryniformis strain Si3 was investigated. The strain had strong inhibitory activity in dual-culture agar plate assays against the molds Aspergillus fumigatus, A. nidulans, Penicillium roqueforti, Mucor hiemalis, Talaromyces flavus, Fusarium poae, F. graminearum, F. culmorum, and F. sporotrichoides. A weaker activity was observed against the yeasts Debaryomyces hansenii, Kluyveromyces marxianus, and Saccharomyces




Antifungal activity of the components of Melaleuca alternifolia (tea tree) oil  

Microsoft Academic Search

K. A. H A M M E R , C. F. C A R S O N A N D T. V. R I L E Y. 2003. Aims: To investigate the in vitro antifungal activity of the components of Melaleuca alternifolia (tea tree) oil. Methods and Results: Activity was investigated by broth microdilution and macrodilution, and time kill methods.

K. A. Hammer; C. F. Carson; T. V. Riley



Antifungal activity and kinetics of inhibition by essential oil isolated from leaves of Aegle marmelos  

Microsoft Academic Search

The antifungal activity of essential oil isolated from the leaves of bael (Aegle marmelos (L.) Correa ex Roxb., Rutaceae) has been evaluated using spore germination assay. The oil exhibited variable efficacy against different fungal isolates and 100% inhibition of spore germination of all the fungi tested was observed at 500 ppm. However, the most resistant fungus, Fusarium udum was inhibited

B. K. Rana; U. P. Singh; V. Taneja



Need for Early Antifungal Treatment Confirmed in Experimental Disseminated Candida albicans Infection  

Microsoft Academic Search

Guidelines for treatment of disseminated Candida infections have always emphasized the need for early implementation of antifungal therapy (12, 14). Amphotericin B, fluconazole, and caspofungin are first-line treatment choices, but their impact is reduced by the difficulties of accurate diagnosis of the disease (5, 8, 16). In practice, many, if not most, Candida infections are treated either empirically, when infection

Donna M. MacCallum; Frank C. Odds



Relapses of Onychomycosis after Successful Treatment with Systemic Antifungals: A Three-Year Follow-Up  

Microsoft Academic Search

Background: Data about relapses of onychomycosis after treatment with the new systemic antifungals vary among the different studies, with figures ranging from 3 to 20% for terbinafine and from 21 to 27% for itraconazole, depending on the follow-up duration. Objective: To determine the prevalence of relapses of onychomycosis cured by terbinafine compared with that of onychomycosis cured by itraconazole. Methods:

A. Tosti; B. M. Piraccini; C. Stinchi; M. D. Colombo



Effect of Growth Rate on Resistance of Candida albicans Biofilms to Antifungal Agents  

Microsoft Academic Search

A perfused biofilm fermentor, which allows growth-rate control of adherent microbial populations, was used to assess whether the susceptibility of Candida albicans biofilms to antifungal agents is dependent on growth rate. Biofilms were generated under conditions of glucose limitation and were perfused with drugs at a high concentration (20 times the MIC). Amphotericin B produced a greater reduction in the




Chemical Composition and Antifungal Activity of Angelica sinensis Essential Oil Against Three Colletotrichum Species  

Technology Transfer Automated Retrieval System (TEKTRAN)

Chemical fungicides are an important component in disease management for most crops. As part of a program to discover natural product-based fungicides, several sensitive assay systems have been developed for the evaluation of naturally occurring antifungal agents. In this study, we focused on the di...


Efficacy of UK109496, a New Azole Antifungal Agent, in an Experimental Model of Invasive Aspergillosis  

Microsoft Academic Search

The efficacy of UK-109496, a new azole antifungal agent, was evaluated in an immunosuppressed, tempo- rarily leukopenic rabbit model of invasive aspergillosis. Oral therapy with UK-109496 at a dosage of 10 or 15 mg\\/kg of body weight every 8 h was begun 24 h after a lethal or sublethal challenge, and results were compared with those for amphotericin B therapy




Allylamine Derivatives: New Class of Synthetic Antifungal Agents Inhibiting Fungal Squalene Epoxidase  

Microsoft Academic Search

A new class of synthetic antifungal agents, the allylamines, has been developed by modification of naftifine, a topical antimycotic. SF 86-327, the most effective of these compounds so far, is highly active in vitro against a wide range of fungi and exceeds clinical standards in the oral and topical treatment of guinea pig dermatophytoses. SF 86-327 is a powerful specific

Gabor Petranyi; Neil S. Ryder; Anton Stutz