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1

COMPARATIVE LIVER P450 ENZYME ACTIVITY AND HISTOPATHOLOGY IN MICE TREATED WITH THE CONAZOLE FUNGICIDES: MYCLOBUTANIL, PROPICONAZOLE AND TRIADIMETON  

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....

2

TRANSCRIPTIONAL PROFILES IN LIVER FROM RATS TREATED WITH TUMORIGENIC AND NON-TUMORIGENIC TRIAZOLE CONAZOLE FUNGICIDES: PROPICONAZOLE, TRIADIMEFON, AND MYCLOBUTANIL  

EPA Science Inventory

Conazoles are a class of fungicides used as pharmaceutical and agricultural agents. In chronic bioassays in rats, triadimefon was hepatotoxic and induced follicular cell adenomas in the thyroid gland, whereas, propiconazole and myclobutanil were hepatotoxic but had no effect on t...

3

Transcriptional Profiles in Liver from Rats Treated with Tumorigenic and Non-tumorigenic Triazole Conazole Fungicides: Propiconazole, Triadimefon, and Myclobutanil  

Microsoft Academic Search

Conazoles are a class of fungicides used as pharmaceutical and agricultural agents. In chronic bioassays in rats, triadimefon was hepatotoxic and induced follicular cell adenomas in the thyroid gland, whereas, propiconazole and myclobutanil were hepatotoxic but had no effect on the thyroid gland. These conazoles administered in the feed to male Wistar\\/Han rats were found to induce hepatomegaly, induce high

SUSAN D. HESTER; Douglas Wolf; Stephen Nesnow; Sheau-Fung Thai

2006-01-01

4

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...

5

TOXICITY PROFILES IN RATS TREATED WITH TUMORIGENIC AND NONTUMORIGENIC TRIAZOLE CONAZOLE FUNGICIDES: PROPICONAZOLE, TRIADIMEFON, AND MYCLOBUTANIL  

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...

6

METABOLISM OF MYCLOBUTANIL AND TRIADIMEFON BY HUMAN AND RAT CYTOCHROME P450 ENZYMES AND LIVER MICROSOMES.  

EPA Science Inventory

Metabolism of two triazole-containing antifungal azoles was studied using expressed human and rat cytochrome P450s (CYP) and liver microsomes. Substrate depletion methods were used due to the complex array of metabolites produced from myclobutanil and triadimefon. Myclobutanil wa...

7

CAR and PXR-dependent transcriptional changes in the mouse liver after exposure to propiconazole  

EPA Science Inventory

Exposure to the conazoles propiconazole and triadimefon but not myclobutanilled to tumors in mice after 2 years. Transcript profiling studies in the livers ofwild-type mice after short-term exposure to the conazoles revealed signatures indicating the involvement ofthe nuclear rec...

8

INDUCTION OF CYTOCHROME P450 ISOFORMS IN RAT LIVER BY TWO CONAZOLES, TRIADIMEFON AND MYCLOBUTANIL  

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...

9

Stereoselective degradation of chiral fungicide myclobutanil in rat liver microsomes.  

PubMed

Myclobutanil, (RS)-2-(4-chlorophenyl)-2-(1H-1, 2, 4-triazol-1-ylmethyl)hexanenitrile is a broad-spectrum systemic triazole fungicide which consists of a pair of enantiomers. The stereoselective degradation of myclobutanil was investigated in rat liver microsomes. The concentrations of myclobutanil enantiomers were determined by high-performance liquid chromatography (HPLC) with a cellulose-tris-(3,5-dimethyl-phenylcarbamate)-based chiral stationary phase (CDMPC-CSP) under reversed phase condition. The t(1/2) of (+)-myclobutanil is 8.49 min, while the t(1/2) of (-)-myclobutanil is 96.27 min. Such consequences clearly indicated that the degradation of myclobutanil in rat liver microsomes was stereoselective and the degradation rate of (+)-myclobutanil was much faster than (-)-myclobutanil. In addition, significant differences between two enantiomers were also observed in enzyme kinetic parameters. The V(max) of (+)-myclobutanil was about 4-fold of (-)-myclobutanil and the CL(int) of (+)-myclobutanil was three times as much as (-)-myclobutanil after incubation in rat liver microsomes. Corresponding consequences may shed light on the environmental and ecological risk assessment for myclobutanil and may improve human health. PMID:24249205

Yan, Jin; Zhang, Ping; Wang, Xinru; Wang, Yao; Zhou, Zhiqiang; Zhu, Wentao

2014-01-01

10

77 FR 75039 - Propiconazole; Pesticide Tolerances  

Federal Register 2010, 2011, 2012, 2013

...mutagenicity in the in vitro BALB/ 3T3 cell transformation assay, bacterial reverse...mice suggest that propiconazole induces cell proliferation followed by treatment-related...hepatocarcinogenic in mice. Some induce thyroid tumors in rats. Some induce...

2012-12-19

11

77 FR 38199 - Propiconazole; Pesticide Tolerances  

Federal Register 2010, 2011, 2012, 2013

...mutagenicity in the in vitro BALB/C 3T3 cell transformation assay, bacterial reverse...mice suggest that propiconazole induces cell proliferation followed by treatment-related...hepatocarcinogenic in mice. Some induce thyroid tumors in rats. Some induce...

2012-06-27

12

76 FR 27261 - Propiconazole; Pesticide Tolerances  

Federal Register 2010, 2011, 2012, 2013

...mutagenicity in the in vitro BALB/C 3T3 cell transformation assay, bacterial reverse...mice suggest that propiconazole induces cell proliferation followed by treatment-related...hepatocarcinogenic in mice. Some induce thyroid tumors in rats. Some induce...

2011-05-11

13

78 FR 23497 - Propiconazole; Pesticide Tolerances  

Federal Register 2010, 2011, 2012, 2013

...mutagenicity in the in vitro BALB/3T3 cell transformation assay, bacterial reverse...mice suggest that propiconazole induces cell proliferation followed by treatment-related...hepatocarcinogenic in mice. Some induce thyroid tumors in rats. Some induce...

2013-04-19

14

TOXICOGENOMIC STUDY OF TRIAZOLE FUNGICIDES AND PERFLUOROALKYL ACIDS  

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 (...

15

TOXICOGENOMIC STUDY OF TRIAZOLE FUNGICIDES AND PERFLUOROALKYL ACIDS IN RAT LIVERS ACCURATELY CATEGORIZES CHEMICALS AND IDENTIFIES MECHANISMS OF TOXICITY  

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...

16

Propiconazole induces alterations in the hepatic metabolome of mice: relevance to propiconazole-induced hepatocarcinogenesis  

EPA Science Inventory

Propiconazole is a mouse hepatotumorigenic fungicide and has been the subject of recent mechanistic investigations on its carcinogenic mechanism of action. The goals of this study were: 1. To identify metabolomic changes induced in the liver by increasing doses of propiconazole i...

17

Propiconazole induces alterations in the hepatic metabolome of mice: relevance to propiconazole-induced hepatocarcinogenesis  

EPA Science Inventory

Propiconazole is a mouse hepatotumorigenic fungicide and has been the subject of recent investigations into its carcinogenic mechanism of action. The goals of this study were: 1. To identify metabolomic changes induced in the liver by increasing doses of propiconazole in mice; 2...

18

TRANSCRIPTIONAL PROFILES IN LIVER FROM MICE TREATED WITH HEPATOTUMORIGENIC AND NON-HEPATOTUMORIGENIC TRIAZOLE CONAZOLE FUNGICIDES: PROPICONAZOLE, TRIADIMEFON, AND MYCLOBUTANIL  

EPA Science Inventory

Conazoles are environmental and pharmaceutical fungicides. The present study relates the toxicological effects of conazoles to alterations of gene and pathway transcription and identifies potential modes of tumorigenic action. In a companion study (Allen et al. 2006) under...

19

PROPICONAZOLE-INDUCED CARCINOGENESIS: ROLE OF OXIDATIVE STRESS  

EPA Science Inventory

Propiconazole is a systemic foliar fungicide with a broad range of activity. Rodents fed with propiconazole at high dose resulted in diminished body weight, increased liver weight of adults and pups, and eventually liver carcinogenesis. In order to unravel the toxic processes inv...

20

Protein Carbonyl Formation in Response to Propiconazole-Induced Oxidative Stress.  

EPA Science Inventory

Propiconazole, a widely used fungicide, is hepatotoxic and hepatotumorigenic in mice. Previous genomic analysis of liver tissues from propiconazole-treated mice identified genes and pathways involved in oxidative stress, suggesting that oxidative stress may play a role in propico...

21

Acute toxicity, bioactivity, and enantioselective behavior with tissue distribution in rabbits of myclobutanil enantiomers.  

PubMed

The enantioselective bioactivity against pathogens (Cercospora arachidicola, Fulvia fulva, and Phytophthora infestans) and acute toxicity to Daphnia magna of the fungicide myclobutanil enantiomers were studied. The (+)-enantiomer in an antimicrobial activity test was about 1.79-1.96 times more active than the (-)-enantiomer. In the toxicity assay, the calculated 24-h LC50 values of the (-)-form, rac-form and (+)-form were 16.88, 13.17, and 11.91?mg/L, and the 48-h LC50 values were 10.15, 9.24, and 5.48?mg/L, respectively, showing that (+)-myclobutanil was more toxic. Meanwhile, the enantioselective metabolism of myclobutanil enantiomers following a single intravenous (i.v.) administration was investigated in rabbits. Total plasma clearance value (CL) of the (+)-enantiomer was 1.68-fold higher than its antipode. Significant differences in pharmacokinetics parameters between the two enantiomers indicated that the high bioactive (+)-enantiomer was preferentially metabolized and eliminated in plasma. Consistent consequences were found in the tissues (liver, brain, heart, kidney, fat, and muscle), resulting in a relative enrichment of the low-activity (-)-myclobutanil. These systemic assessments of the stereoisomers of myclobutanil cannot be used only to investigate environmental and biological behavior, but also have human health implications because of the long persistence of triazole fungicide and enantiomeric enrichment in mammals and humans. Chirality 26:784-789, 2014. © 2014 Wiley Periodicals, Inc. PMID:25043148

Sun, Mingjing; Liu, Donghui; Qiu, Xinxu; Zhou, Qian; Shen, Zhigang; Wang, Peng; Zhou, Zhiqiang

2014-12-01

22

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.

2011-01-01

23

MYCLOBUTANIL AND TRIADIMEFON METHABOLISM BY RAT CYP ISOFORMS AND LIVER MICROSOMES  

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...

24

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

2003-01-01

25

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...

26

IN VIVO MUTAGENICITY OF CONAZOLE FUNGICIDES CORRELATES WITH TUMORIGENICITY-JOURNAL  

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...

27

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 ...

28

A potential microRNA signature for tumorigenic conazoles in mouse liver  

EPA Science Inventory

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

29

A microRNA signature for 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 o...

30

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...

31

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 ...

32

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

PubMed

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

2013-04-01

33

[Determination of myclobutanil 25% WG degradation dynamics in ginseng root, stem, leaf and soil by HPLC-MS/MS].  

PubMed

A high performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS) method was developed for determining degradation dynamics and final residues of myclobutanil 25% WG in ginseng root, stem, leaf and soil. The samples were extracted with acetonitrile, cleaned-up with primary secondary amine (PSA) solid phase extraction cartridge, separated by Kromasil Eternity-5-C18 (2.1 mm x 150 mm, 5 microm) column with a gradient of acetonitrile and 0.1% formate in water as mobile phases, and analyzed with the multiple reaction monitoring (MRM) in positive ion mode by employing the external standard method. The average recoveries and the relative standard derivations (RSDs) of myclobutanil at the spiked level of 0.01-0.20 mg x kg(-1) were 80.9%-90.7% and 5.54%-9.29%, respectively, and the limit of quantification (LOQ) was 0.005 mg x kg(-1). The method with good reproducible, high precision and low detection limit could meet the requirements of residual analysis on ginseng production. The half-lives of myclobutanil were from 6.25 days to 9.94 days in ginseng root, stem, leaf and soil at spraying dosage of 1 152 g x hm(-2) The final residues were below 0.060 1 mg x kg(-1) in root, below 0.081 7 mg x kg(-1) in stem, 0.006 0-0.102 2 mg x kg(-1) in leaf and below 0.037 6 mg x kg(-1) in soil at spraying dosage range from 576 to 1 152 g x hm(-2). It is recommended that the MRLs of myclobutanil in dried ginseng may be suggested to be 0.10 mg x kg(-1) temporarily, and the preharvest interval was set at 35 days. PMID:25276964

Wang, Yan; Wang, Chun-Wei; Gao, Jie; Cui, Li-Li; Xu, Yun-Cheng

2014-07-01

34

Two azole fungicides (carcinogenic triadimefon and non-carcinogenic myclobutanil) exhibit different hepatic cytochrome P450 activities in medaka fish.  

PubMed

Conazoles are a class of imidazole- or triazole-containing drugs commonly used as fungicides in agriculture and medicine. The broad application of azole drugs has led to the contamination of surface aquifers receiving the effluent of municipal or hospital wastewater or agricultural runoff. Several triazoles are rodent carcinogens; azole pollution is a concern to environmental safety and human health. However, the carcinogenic mechanisms associated with cytochrome P450 enzymes (CYPs) of conazoles remain unclear. We exposed adult medaka fish (Oryzias latipes) to continuous aqueous solutions of carcinogenic triadimefon and non-carcinogenic myclobutanil for 7 to 20 days at sub-lethal or environmentally relevant concentrations and assessed hepatic CYP activity and gene expression associated with CYP-mediated toxicity. Both triadimefon and myclobutanil induced hepatic CYP3A activity, but only triadimefon enhanced CYP1A activity. The gene expression of cyp3a38, cyp3a40, pregnane x receptor (pxr), cyp26b, retinoid acid receptor ?1 (rar?1) and p53 was higher with triadimefon than myclobutanil. As well, yeast-based reporter gene assay revealed that 4 tested conazoles were weak agonists of aryl hydrocarbon receptor (AhR). We reveal differential CYP gene expression with carcinogenic and non-carcinogenic conazoles in a lower vertebrate, medaka fish. Liver CYP-enzyme induction may be a key event in conazole-induced tumorigenesis. This information is essential to evaluate the potential threat of conazoles to human health and fish populations in the aquatic environment. PMID:24962053

Lin, Chun-Hung; Chou, Pei-Hsin; Chen, Pei-Jen

2014-07-30

35

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...

36

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...

37

Short-term effects of propiconazole on hypothalamic-pituitary-gonadal function in the fathead minnows (Pimephales promelas)  

EPA Science Inventory

Propiconazole is an ergosterol inhibitor commonly used in agriculture and has been detected in aquatic environments. Ergosterol inhibitors decrease fungal growth through effects on 14á-demethylase, a cytochrome P450 (CYP), isoform important for ergosterol biosynthesis. In higher ...

38

Soil applied propiconazole alleviates the impact of salinity on Catharanthus roseus by improving antioxidant status  

Microsoft Academic Search

An investigation was carried out to estimate the salt stress ameliorative effect of propiconazole (a triazole group of fungicide cum plant growth regulator) on the NaCl stressed Catharanthus roseus. The experiment was conducted in pots. All the pots were irrigated to the field capacity with ground water up to 30 days after sowing (DAS). The treatments were given as 80mM

C. Abdul Jaleel; R. Gopi; P. Manivannan; M. Gomathinayagam; P. V. Murali; R. Panneerselvam

2008-01-01

39

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

PubMed

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

2001-01-01

40

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 ...

41

Loss of Propiconazole and its Four Stereoisomers from the Water Phase of Two Soil-Water Slurries as Measured by Capillary Electrophoresis  

EPA Science Inventory

Propiconazole is a chiral fungicide used in agriculture for control of many fungal diseases on a variety of crops. This use provides opportunities for pollution of soil and, subsequently, groundwater. The rate of loss of propiconazole from the water phase of two different soil-wa...

42

Pediatric Antifungal Agents  

PubMed Central

Purpose of review In immunocompromised hosts, invasive fungal infections are common and fatal. In the past decade, the antifungal armamentarium against invasive mycoses has expanded greatly. The purpose of this report is to review the most recent literature addressing the use of antifungal agents in children. Recent findings Most studies evaluating the safety and efficacy of antifungal agents are limited to adults. However, important progress has been made in describing the pharmacokinetics and safety of newer antifungal agents in children, including the echinocandins. Summary Dosage guidelines for newer antifungal agents are currently based on adult and limited pediatric data. Because important developmental pharmacology changes occur throughout childhood impacting the pharmacokinetics of these agents, antifungal studies specifically designed for children are necessary. PMID:19741525

Cohen-Wolkowiez, Michael; Moran, Cassandra; Benjamin, Daniel K.; Smith, P Brian

2009-01-01

43

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

PubMed

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

2012-04-15

44

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

SciTech Connect

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. Highlights: ? Propiconazole increases cell proliferation in AML12 mouse hepatocytes. ? Propiconazole increases Ras farnesylation and alters Ras membrane localization. ? Propiconazole increases Erk1/2 phosphorylation. ? Dysregulation of the cholesterol biosynthesis pathway can explain these results. ? These results can explain similar effects induced by propiconazole in mice.

Murphy, Lynea A.; Moore, Tanya; Nesnow, Stephen, E-mail: nesnow.stephen@epa.gov

2012-04-15

45

Organic Compounds in the Environment Laboratory Degradation Studies of Bentazone, Dichlorprop, MCPA, and Propiconazole in Norwegian Soils  

Microsoft Academic Search

sidered minor dissipation pathways (Barnett et al., 1967). Dichlorprop has been reported to degrade com- Laboratory degradation studies were performed in Norwegian soils pletely in soil within 31 d, with a half-life of 6.6 d (Garri- using two commercial formulations (Tilt and Triagran-P) containing either propiconazole alone or a combination of bentazone, dichlor- son et al., 1996). Degradation occurred with

Christian W. Thorstensen; Olav Lode

46

New topical antifungal drugs.  

PubMed

The new antifungal drugs used for topical treatment of superficial, skin and mucosal mycoses are reviewed. Amorolfine and allylamines (naftifine and terbinafine) are promising original molecules with new and different modes of action against fungi. Rilopirox is a new pyridone derivative under study. A great number of azole derivatives, such as oxiconazole, isoconazole, sulconazole, and terconazole, are used as topical antifungals. Three of them are synthesized in Barcelona by pharmaceutical laboratories: sertaconazole, flutrimazole and eberconazole. All of them are now in the register process for commercialization. The combination of antifungals with active products, such as keratoplastics, is used mainly for the treatment of onychomycoses; 40% urea associated with 1% bifonazole has shown high efficacy for this indication. PMID:8118161

Torres-Rodríguez, J M

1993-01-01

47

Impact of Fungicides Chlorothalonil and Propiconazole on Microbial Activities in Groundnut (Arachis hypogaea L.) Soils.  

PubMed

Introduction of agrochemicals (fungicides) into soil may have lasting effects on soil microbial activities and thus affect soil health. In order to determine the changes in microbial activity in a black clay and red sandy loam soils of groundnut (Arachis hypogaea L.) cultivated fields, a case study was conducted with propiconazole and chlorothalonil to evaluate its effects on soil enzymes (cellulase and invertase) throughout 40 days of incubation under laboratory conditions with different concentrations (1.0, 2.5, 5.0, 7.5, and 10.0?kg ha(-1)). Individual application of the two fungicides at 1.0, 2.5, and 5.0?kg ha(-1) to the soil distinctly enhanced the activities of cellulase and invertase but at higher concentrations of 7.5 and 10?kg ha(-1) was toxic or innocuous to both cellulase and invertase activities. In soil samples receiving 2.5-5.0?kg ha(-1) of the fungicides, the accumulation of reducing sugar was pronounced more at 20 days, and the activity of the cellulase and invertase was drastically decreased with increasing period of incubation up to 30 and 40 days. PMID:23724306

Ramudu, A C; Mohiddin, G Jaffer; Srinivasulu, M; Madakka, M; Rangaswamy, V

2011-01-01

48

Impact of Fungicides Chlorothalonil and Propiconazole on Microbial Activities in Groundnut (Arachis hypogaea L.) Soils  

PubMed Central

Introduction of agrochemicals (fungicides) into soil may have lasting effects on soil microbial activities and thus affect soil health. In order to determine the changes in microbial activity in a black clay and red sandy loam soils of groundnut (Arachis hypogaea L.) cultivated fields, a case study was conducted with propiconazole and chlorothalonil to evaluate its effects on soil enzymes (cellulase and invertase) throughout 40 days of incubation under laboratory conditions with different concentrations (1.0, 2.5, 5.0, 7.5, and 10.0?kg ha?1). Individual application of the two fungicides at 1.0, 2.5, and 5.0?kg ha?1 to the soil distinctly enhanced the activities of cellulase and invertase but at higher concentrations of 7.5 and 10?kg ha?1 was toxic or innocuous to both cellulase and invertase activities. In soil samples receiving 2.5–5.0?kg ha?1 of the fungicides, the accumulation of reducing sugar was pronounced more at 20 days, and the activity of the cellulase and invertase was drastically decreased with increasing period of incubation up to 30 and 40 days. PMID:23724306

Ramudu, A. C.; Mohiddin, G. Jaffer; Srinivasulu, M.; Madakka, M.; Rangaswamy, V.

2011-01-01

49

PROPICONAZOLE-INDUCED CYTOCHROME P450 GENE EXPRESSION AND ENZYMATIC ACTIVITIES IN RAT AND MOUSE LIVER  

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...

50

Current and future antifungal therapy: new targets for antifungal therapy.  

PubMed

Invasive fungal infections will continue to cause major complications in immunocompromized patients. At the moment, the expansion of antifungal drug research has occurred because there is a critical need for new antifungal agents to treat these life-threatening invasive fungal infections. The overview of the development of antifungal therapy which is provided here demonstrates the increased interest in this very special area of infectious diseases. Although we now have some newer and less toxic antifungal agents that are currently available for clinical use, their clinical efficacy in some invasive fungal infections, such as aspergillosis and fusariosis, is not very good. Intense efforts in antifungal drug discovery are urgently needed to develop more promising and effective antifungal agents for use in the clinical arena. PMID:11091055

Andriole, V T

2000-11-01

51

New antifungal agents.  

PubMed

Two new antifungal agents, voriconazole and caspofungin, are now available for treatment of systemic fungal infections. Voriconazole is an extended-spectrum triazole that is fungicidal for filamentous fungi, including Aspergillus, Scedosporium, Fusarium, Paecilomyces, and is active against all species of Candida. It has become first-line therapy for invasive aspergillosis. Voriconazole is given either by the oral or the intravenous route. Clinicians must be aware of drug-drug interactions and side effects, including visual disturbances and photosensitivity rash that can occur when voriconazole is used. Caspofungin is the first drug available from a new class of antifungal agents, echinocandins, that act to inhibit fungal cell wall synthesis. Caspofungin is fungicidal for all species of Candida and more slowly kills Aspergillus species. Caspofungin, available only for intravenous administration, has minimal side effects and very few drug interactions. The echinocandins will find most use for Candida infections and as second-line therapy for Aspergillus infections. PMID:16088465

Kauffman, Carol A

2004-04-01

52

Trends in antifungal research  

Microsoft Academic Search

\\u000a With the increasing use of aggressive immunosuppressive therapies in the management of a variety of patient populations, the\\u000a continuing presence of the AIDS pandemic and the therapeutic advances employed in critical care settings, an increasing number\\u000a of serious fungal infections are being encountered by today’s practicing clinicians. Traditionally, antifungal drug therapy\\u000a has been delivered by means of intravenous infusion, oral

Vorapann Mahaguna; Robert O. Williams; Thomas C. Hardin

53

Current Concepts in Antifungal Pharmacology  

PubMed Central

The introduction of new antifungal agents (eg, echinocandins, second-generation triazoles) in the past decade has transformed the management of invasive mycoses to the point that drug toxicity is no longer the major limiting factor in treatment. Yet, many of these newer antifungal agents have important limitations in their spectrum of activity, pharmacokinetics, and unique predisposition for pharmacokinetic drug-drug interactions and unusual toxicities associated with long-term use. This article reviews key pharmacological aspects of systemic antifungal agents as well as evolving strategies, such as pharmacokinetic-pharmacodynamic optimization and therapeutic drug monitoring, to improve the safety and efficacy of systemic antifungal therapy. PMID:21803962

Lewis, Russell E.

2011-01-01

54

Antifungal constituent from Gordonia dassanayakei.  

PubMed

The hexane extract of the stem bark of Gordonia dassanayakei showed high antifungal activity against plant pathogenic fungi Curvularia sp., Colletotrichum gloeosporioides, Rhizoctonia solani, Corynespora cassiicola, and Fusarium sp. A compound responsible for the antifungal activity was isolated and identified as 3-formyl-2,4-dihydroxy-6-methylbenzoic acid 3-hydroxy-4-(methoxycarbonyl)-2,5-dimethylphenyl ester (1). PMID:11429257

Athukoralage, P S; Herath, H M; Deraniyagala, S A; Wijesundera, R L; Weerasinghe, P A

2001-06-01

55

Loss of Propiconazole and Its Four Stereoisomers from the Water Phase of Two Soil-Water Slurries as Measured by Capillary Electrophoresis  

PubMed Central

Propiconazole is a chiral fungicide used in agriculture for control of many fungal diseases on a variety of crops. This use provides opportunities for pollution of soil and, subsequently, groundwater. The rate of loss of propiconazole from the water phase of two different soil-water slurries spiked with the fungicide at 50 mg/L was followed under aerobic conditions over five months; the t1/2 was 45 and 51 days for the two soil slurries. To accurately assess environmental and human risk, it is necessary to analyze the separate stereoisomers of chiral pollutants, because it is known that for most such pollutants, both biotransformation and toxicity are likely to be stereoselective. Micellar electrokinetic chromatography (MEKC), the mode of capillary electrophoresis used for analysis of neutral chemicals, was used for analysis of the four propiconazole stereoisomers with time in the water phase of the slurries. MEKC resulted in baseline separation of all stereoisomers, while GC-MS using a chiral column gave only partial separation. The four stereoisomers of propiconazole were lost from the aqueous phase of the slurries at experimentally equivalent rates, i.e., there was very little, if any, stereoselectivity. No loss of propiconazole was observed from the autoclaved controls of either soil, indicating that the loss from active samples was most likely caused by aerobic biotansformation, with a possible contribution by sorption to the non-autoclaved active soils. MEKC is a powerful tool for separation of stereoisomers and can be used to study the fate and transformation kinetics of chiral pesticides in water and soil. PMID:21909317

Garrison, Arthur W.; Avants, Jimmy K.; Miller, Rebecca D.

2011-01-01

56

Antifungal macrodiolide from Streptomyces sp.  

PubMed Central

Aerobic fermentation cultures of Streptomyces sp. produced an antifungal macrodiolide. This new antibiotic consists of two units of homononactic acid linked to form a cyclic diester. An unknown polypeptide was also isolated in trace quantities. The antibiotic with polypeptide complex showed high levels of antifungal activity compared with that of the macrodiolide alone. The macrodiolide also showed a stimulatory effect on some species of fungi. The production, purification, and characterization of these compounds are reported. PMID:3777909

Jois, H R; Sarkar, A; Gurusiddaiah, S

1986-01-01

57

Echinocandins--new antifungal agents.  

PubMed

Over the past 10-15 years, the number of clinically available antifungal agents has increased substantially, due to rise in the number of invasive fungal infections, which are a real problem for specialists. Echinocandins are the new class of antifungal agents available for clinical use. This class comprises over 20 natural echinocandins and several semisynthetic ones. Natural echinocandins are not of clinical utility due to their toxicity and low water-solubility (which does not allow obtaining parenteral pharmaceutical forms), although they have good antifungal activity against Candida species. Consequently, semisynthetic echinocandins with minimal toxicity, good antifungal activity and high water-solubility were obtained. All echinocandins inhibit beta-1,3-glucan-synthase, an essential component of the fungal cell wall. Echinocandins exhibit potent antifungal activity against key pathogenic fungi, including Candida species, Aspergillus species and Pneumocystis carinii. The available echinocandins lack in vitro activity against Cryptococcus neoformans. The semisynthetic echinocandins have great advantages, among which low toxicity, fast antifungal activity, favorable pharmacokinetics that allow once-daily administration. The echinocandins recently available for clinical use are: caspofungin, micafungin and anidulafungin. PMID:25076727

Stan, C?t?lina Daniela; Tuchilu?, Cristina; Stan, C I

2014-01-01

58

ALTERATIONS IN A11 TRANS RETINOIC ACID METABOLISM IN LIVER MICROSOMES FROM MICE TREATED WITH HEPATOTUMORIGENIC AND NON-HEPATOTUMORIGENIC CONAZOLES  

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 be a key event in co...

59

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 ...

60

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 ...

61

COMPARISON OF HEPATIC GENE EXPRESSION PROFILES FROM MICE EXPOSED TO THREE TOXICOLOGICALLY DIFFERENT CONAZOLES  

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 ...

62

Antifungal prophylaxis in lung transplantation.  

PubMed

Lung transplant (LTx) patients have an increased risk of developing invasive fungal infections (IFIs), particularly invasive aspergillosis. Rapid identification of the causative fungal pathogen, to allow for early administration of appropriate initial antifungal therapy, in LTx patients has been challenging due to the limited sensitivity and specificity of the diagnostic tools. Hence, there is increasing emphasis on antifungal prophylaxis in the LTx setting, given the high mortality rates and substantial cost of treating IFIs. Evidence for the optimal antifungal prophylactic approach in this setting, however, remains scant and inconsistent. This review will briefly discuss the epidemiology, risk factors, timing and clinical manifestations of fungal infections in LTx patients and will focus primarily on the available evidence related to the efficacy, safety and practicality of current prophylactic strategies in LTx recipients as well as challenges and gaps for future research. PMID:25123811

Neoh, Chin Fen; Snell, Greg; Levvey, Bronwyn; Morrissey, C Orla; Stewart, Kay; Kong, David C M

2014-09-01

63

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. PMID:23078400

Mehra, T; Köberle, M; Braunsdorf, C; Mailänder-Sanchez, D; Borelli, C; Schaller, M

2012-01-01

64

Traditional and emerging antifungal therapies.  

PubMed

Invasive mycoses continue to be a major problem in the growing population of immunosuppressed patients. More antifungal agents are now available than ever. The options are many, with more efficacies and less toxicity than in the past. These agents differ in terms of spectrum of activity, pharmacologic properties, and indications. In this article we discuss the three major classes of antifungal agents: the polyens, the triazoles, and the echinocandins. The emphasis is placed on their clinical use, side effects, drug interactions, and other practical issues. PMID:20463252

Arnold, Tamra M; Dotson, Emily; Sarosi, George A; Hage, Chadi A

2010-05-01

65

Antifungal Compounds from Piper Species  

PubMed Central

This review documents chemical structures and antifungal activities of 68 compounds isolated from 22 Piper species of the plant family Piperaceae. These compounds include amides, flavonoids, prenylated benzoic acid derivatives, lignans, phenylpropanoids, butenolides, and cyclopentendiones. Some of them may serve as leads for potential pharmaceutical or agricultural fungicide development. PMID:24307889

Xu, Wen-Hui; Li, Xing-Cong

2013-01-01

66

Antifungal Application of Nonantifungal Drugs  

PubMed Central

Candida species are the cause of 60% of all mycoses in immunosuppressed individuals, leading to ?150,000 deaths annually due to systemic infections, whereas the current antifungal therapies either have toxic side effects or are insufficiently efficient. We performed a screening of two compound libraries, the Enzo and the Institute for Molecular Medicine Finland (FIMM) oncology collection library, for anti-Candida activity based on the European Committee on Antimicrobial Susceptibility Testing (EUCAST) guidelines. From a total of 844 drugs, 26 agents showed activity against Candida albicans. Of those, 12 were standard antifungal drugs (SADs) and 7 were off-target drugs previously reported to be active against Candida spp. The remaining 7 off-target drugs, amonafide, tosedostat, megestrol acetate, melengestrol acetate, stanozolol, trifluperidol, and haloperidol, were identified with this screen. The anti-Candida activities of the new agents were investigated by three individual assays using optical density, ATP levels, and microscopy. The antifungal activities of these drugs were comparable to those of the SADs found in the screen. The aminopeptidase inhibitor tosedostat, which is currently in a clinical trial phase for anticancer therapy, displayed a broad antifungal activity against different Candida spp., including Candida glabrata. Thus, this screen reveals agents that were previously unknown to be anti-Candida agents, which allows for the design of novel therapies against invasive candidiasis. PMID:24277040

Stylianou, Marios; Kulesskiy, Evgeny; Lopes, Jose Pedro; Granlund, Margareta; Wennerberg, Krister

2014-01-01

67

Antifungal chemotherapy: advances and perspectives  

Microsoft Academic Search

Invasive fungal infections have emerged as im- portant causes of morbidity and mortality in im- munocompromised patients. In response to this challenge, the field of antifungal chemotherapy has considerably expanded. Fluconazole and itra- conazole, introduced in the late 1980s, were the first durably useful alternatives to amphotericin B deoxycholate. The clinical development of the lipid formulations of amphotericin B, and,

Andreas H. Groll; Thomas J. Walsh

68

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

2008-01-01

69

Defensins: antifungal lessons from eukaryotes  

PubMed Central

Over the last years, antimicrobial peptides (AMPs) have been the focus of intense research toward the finding of a viable alternative to current antifungal drugs. Defensins are one of the major families of AMPs and the most represented among all eukaryotic groups, providing an important first line of host defense against pathogenic microorganisms. Several of these cysteine-stabilized peptides present a relevant effect against fungi. Defensins are the AMPs with the broader distribution across all eukaryotic kingdoms, namely, Fungi, Plantae, and Animalia, and were recently shown to have an ancestor in a bacterial organism. As a part of the host defense, defensins act as an important vehicle of information between innate and adaptive immune system and have a role in immunomodulation. This multidimensionality represents a powerful host shield, hard for microorganisms to overcome using single approach resistance strategies. Pathogenic fungi resistance to conventional antimycotic drugs is becoming a major problem. Defensins, as other AMPs, have shown to be an effective alternative to the current antimycotic therapies, demonstrating potential as novel therapeutic agents or drug leads. In this review, we summarize the current knowledge on some eukaryotic defensins with antifungal action. An overview of the main targets in the fungal cell and the mechanism of action of these AMPs (namely, the selectivity for some fungal membrane components) are presented. Additionally, recent works on antifungal defensins structure, activity, and cytotoxicity are also reviewed. PMID:24688483

Silva, Patricia M.; Goncalves, Sonia; Santos, Nuno C.

2014-01-01

70

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

1997-01-01

71

Development of Prophylactic Anti-Fungal Preparations.  

National Technical Information Service (NTIS)

In order to develop better topical anti-fungal agents with prophylactic activity against common ringworm infection a chemical assay for sodium pyrithione (a known anti-fungal drug) was developed in stratum corneum and its persistence there determined a do...

S. Riegelman, W. L. Epstein, R. A. Upton

1980-01-01

72

The 1998 Garrod lecture. Current and future antifungal therapy: new targets for antifungal agents.  

PubMed

Invasive fungal infections are a major problem in immunocompromised patients. The recent expansion of antifungal drug research has occurred because there is a critical need for new antifungal agents to treat these life-threatening invasive infections. The overview of the development of antifungal therapy which is provided herein reflects the increased interest in this very special area of infectious diseases. Although we have newer, less toxic, antifungal agents that are available for clinical use, their clinical efficacy in some invasive fungal infections, such as aspergillosis and fusariosis, is not optimal. Thus, intense efforts in antifungal drug discovery are still needed to develop more promising and effective antifungal agents for use in the clinical arena. PMID:10473222

Andriole, V T

1999-08-01

73

Antifungal Activity of Isothiocyanates and Related Compounds  

PubMed Central

Data are presented concerning the antifungal activity of 11 natural isothiocyanates and 27 synthetized analogues in Aspergillus niger, Penicillium cyclopium, and Rhizopus oryzae, as well as in 13 additional saprophytic and parasitic fungi. A remarkable antifungal activity was observed in some analogues of benzylisothiocyanate and ?-phenylethylisothiocyanate. The latter-mentioned compounds have not been described previously. In the group of benzylisothiocyanates, a correlation, which was inversely proportional, was detected between ed100 values for A. niger and R. oryzae and the corresponding molar solubilities of compounds in water. In contradistinction, no relationship was observed between antifungal activity and chemical reactivity of investigated derivatives. PMID:6049294

Drobnica, L.; Zemanova, M.; Nemec, P.; Antos, K.; Kristian, P.; Stullerova, A.; Knoppova, V.; Nemec, P.

1967-01-01

74

Toxicokinetic-toxicodynamic modelling of survival of Gammarus pulex in multiple pulse exposures to propiconazole: model assumptions, calibration data requirements and predictive power.  

PubMed

Toxicokinetic-toxicodynamic (TKTD) models quantify the time-course of internal concentration, which is defined by uptake, elimination and biotransformation (TK), and the processes which lead to the toxic effects (TD). TKTD models show potential in predicting pesticide effects in fluctuating concentrations, but the data requirements and validity of underlying model assumptions are not known. We calibrated TKTD models to predict survival of Gammarus pulex in propiconazole exposure and investigated the data requirements. In order to assess the need of TK in survival models, we included or excluded simulated internal concentrations based on pre-calibrated TK. Adding TK did not improve goodness of fits. Moreover, different types of calibration data could be used to model survival, which might affect model parameterization. We used two types of data for calibration: acute toxicity (standard LC50, 4 d) or pulsed toxicity data (total length 10 d). The calibration data set influenced how well the survival in the other exposure scenario was predicted (acute to pulsed scenario or vice versa). We also tested two contrasting assumptions in ecotoxicology: stochastic death and individual tolerance distribution. Neither assumption fitted to data better than the other. We observed in 10-d toxicity experiments that pulsed treatments killed more organisms than treatments with constant concentration. All treatments received the same dose, i.e. the time-weighted average concentration was equal. We studied mode of toxic action of propiconazole and it likely acts as a baseline toxicant in G. pulex during 10-days of exposure for the endpoint survival. PMID:22562719

Nyman, Anna-Maija; Schirmer, Kristin; Ashauer, Roman

2012-10-01

75

Antifungal stewardship in invasive Candida infections.  

PubMed

Bloodstream and other invasive infections due to Candida species (invasive fungal diseases = IFD) are a major cause of morbidity and mortality in hospitalized adults and children in many countries worldwide. The high infection-related morbidity and mortality associated with invasive Candida infection/candidaemia (IC/C), combined with suboptimal diagnostic tools, have driven the overuse of antifungal drugs. Antifungal stewardship (AFS) may be regarded as subentity of the more general term Anti-infective or Antimicrobial Stewardship Program (AIS/AMS). The high costs and high contribution of antifungal agents to the management of IFDs along with their recognized toxicities have been addressed as the principal justification for antifungal stewardship. AFS programmes should be organized by an interdisciplinary team of clinicians, pharmacists, microbiologists and infection control experts with the lead of an infectious disease specialist preferably in each large hospital/institution dealing with high-risk patients for invasive fungal infections. These programmes should consider various aspects of IC/C including (i) the local fungal epidemiology, (ii) information on antifungal resistance rates, (iii) establishing and application of therapeutic guidelines, (iv) implementation of treatment strategies for empirical, pre-emptive therapy including PK/PD data for antifungal drugs, de-escalation and 'switch and step-down strategies' (from intravenous to oral medication) in defined patient populations, (v) catheter management together with the application of routine diagnostic procedures such as ophthalmological and cardiac evaluations and (vi) the best available diagnostic tests for diagnosing IC and candidaemia. PMID:24661820

Ruhnke, M

2014-06-01

76

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. PMID:24031724

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

2011-01-01

77

Evaluation of solid sorbents for the determination of fenhexamid, metalaxyl-M, pyrimethanil, malathion and myclobutanil residues in air samples: application to monitoring malathion and fenhexamid dissipation in greenhouse air using C-18 or Supelpak-2 for sampling.  

PubMed

A methodology is described for greenhouse air analysis by sampling fenhexamid, pyrimethanil, malathion, metalaxyl-M and myclobutanil in solid sorbents. Pesticides were determined by gas chromatography with NP Detector. The trapping efficiency of XAD-2, XAD-4, Supelpak-2, Florisil and C-18 at different sampling conditions (rate, time and air humidity) and pesticides concentration levels has been evaluated. No breakthrough was observed in the range of concentration studied (0.10-75 microg of each pesticide). In almost all the cases good stability results were obtained. Personal pumps have been used with selected sorbents (Supelpak-2 and C-18) in order to sample malathion and fenhexamid in air of experimental greenhouse after their application in a tomato crop. The dissipation process of the analytes in various time periods after application has been studied. Malathion concentrations varied between 20.1 microg m(-3) just after application and 1.06 microg m(-3) 3 days later. Fenhexamid concentrations, determined by high performance liquid chromatography with UV detection, fall rapidly; after 12 h post-application being below 0.50 microg m(-3). PMID:17723526

Tsiropoulos, Nikolaos G; Bakeas, Evangelos B; Raptis, Vasilios; Batistatou, Stavroula S

2006-07-28

78

Antifungal Drug Resistance: Mechanisms, Epidemiology, and Consequences for Treatment  

Microsoft Academic Search

Antifungal resistance continues to grow and evolve and complicate patient management, despite the introduction of new antifungal agents. In vitro susceptibility testing is often used to select agents with likely activity for a given infection, but perhaps its most important use is in identifying agents that will not work, i.e., to detect resistance. Standardized methods for reliable in vitro antifungal

Michael A. Pfaller

79

Antifungal drug discovery: the process and outcomes.  

PubMed

New data suggest that the global incidence of several types of fungal diseases have traditionally been under-documented. Of these, mortality caused by invasive fungal infections remains disturbingly high, equal to or exceeding deaths caused by drug-resistant tuberculosis and malaria. It is clear that basic research on new antifungal drugs, vaccines and diagnostic tools is needed. In this review, we focus upon antifungal drug discovery including in vitro assays, compound libraries and approaches to target identification. Genome mining has made it possible to identify fungal-specific targets; however, new compounds to these targets are apparently not in the antimicrobial pipeline. We suggest that 'repurposing' compounds (off patent) might be a more immediate starting point. Furthermore, we examine the dogma on antifungal discovery and suggest that a major thrust in technologies such as structural biology, homology modeling and virtual imaging is needed to drive discovery. PMID:25046525

Calderone, Richard; Sun, Nuo; Gay-Andrieu, Francoise; Groutas, William; Weerawarna, Pathum; Prasad, Sridhar; Alex, Deepu; Li, Dongmei

2014-06-01

80

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. PMID:20940361

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

2010-01-01

81

Sertaconazole: pharmacology of a gynecological antifungal agent.  

PubMed

Sertaconazole is a broad spectrum antifungal agent with excellent activity against yeasts, dermatophytes and opportunistic fungi. In addition to this antifungal efficacy, it has a good safety profile, sustained cutaneous retention, and low systemic absorption, all of which make it ideal for topical applications. In this study, the pharmacological properties of sertaconazole related to the treatment of vaginal fungi, in particular vulvovaginal candidiasis, are reviewed. As with all other infectious processes, the interacting components are infectious microorganism, host and drug. The following properties of sertaconazole have been investigated in pre-clinical studies: its in vitro spectrum of activity and potency against causative agents and accompanying factors in vaginal infection; its mechanism of action, whether it acts on the pathogenic properties of the microorganism; if it affects host defense mechanisms and how its antifungal activity is manifested in vivo in experimental candidiasis in the mouse. PMID:11118563

Palacín, C; Tarragó, C; Ortiz, J A

2000-12-01

82

Synthesis, antifungal activities and qualitative structure activity relationship of carabrone hydrazone derivatives as potential antifungal agents.  

PubMed

Aimed at developing novel fungicides for relieving the ever-increasing pressure of agricultural production caused by phytopathogenic fungi, 28 new hydrazone derivatives of carabrone, a natural bioactive sesquisterpene, in three types were designed, synthesized and their antifungal activities against Botrytis cinerea and Colletotrichum lagenarium were evaluated. The result revealed that all the derivatives synthesized exhibited considerable antifungal activities in vitro and in vivo, which led to the improved activities for carabrone and its analogues and further confirmed their potential as antifungal agents. PMID:24619221

Wang, Hao; Ren, Shuang-Xi; He, Ze-Yu; Wang, De-Long; Yan, Xiao-Nan; Feng, Jun-Tao; Zhang, Xing

2014-01-01

83

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

PubMed Central

Aimed at developing novel fungicides for relieving the ever-increasing pressure of agricultural production caused by phytopathogenic fungi, 28 new hydrazone derivatives of carabrone, a natural bioactive sesquisterpene, in three types were designed, synthesized and their antifungal activities against Botrytis cinerea and Colletotrichum lagenarium were evaluated. The result revealed that all the derivatives synthesized exhibited considerable antifungal activities in vitro and in vivo, which led to the improved activities for carabrone and its analogues and further confirmed their potential as antifungal agents. PMID:24619221

Wang, Hao; Ren, Shuang-Xi; He, Ze-Yu; Wang, De-Long; Yan, Xiao-Nan; Feng, Jun-Tao; Zhang, Xing

2014-01-01

84

Antifungal Activity of Isothiocyanates and Related Compounds  

PubMed Central

This paper presents the results of a study on the antifungal activity of isothiocyanates—derivatives of biphenyl (group “A”), of stilbene (“B”), of azobenzene and benzeneazonaphthalene (“C”), of naphthalene (“D”), and of further polycondensed aromatic hydrocarbons (“E”). From a total of 48 investigated compounds, antifungal activity was observed only in A and D group compounds. B, C, and E group derivatives are extremely insoluble in water, and the molecules are very large; as a result, they probably cannot pass into spores or mycelium of fungi. Thus, the —NCS group cannot manifest its reactivity. PMID:5647516

Drobnica, L.; Zemanova, M.; Nemec, P.; Antos, K.; Kristian, P.; Martvon, A.; Zavodska, E.

1968-01-01

85

Molecular basis of resistance to azole antifungals  

Microsoft Academic Search

The increased incidence of invasive mycoses and the emerging problem of antifungal drug resistance has prompted investigations of the underlying molecular mechanisms, particularly for the azole compounds central to current therapy. The target site for the azoles is the ERG11 gene product, the cytochrome P450 lanosterol 14?-demethylase, which is part of the ergosterol biosynthetic pathway. The resulting ergosterol depletion renders

Antonella Lupetti; Romano Danesi; Mario Campa; Mario Del Tacca; Steven Kelly

2002-01-01

86

Antifungal potential of Indian medicinal plants  

Microsoft Academic Search

Fourteen Indian plants, selected based on their use in respiratory and other disorders in traditional systems of medicine, were analyzed for their potential activity against fungi. The antifungal activity was investigated by disc diffusion, microbroth dilution and percent spore germination inhibition tests against pathogenic Aspergilli. Methanolic extracts of Solanum xanthocarpum and Datura metel inhibited the growth of Aspergillus fumigatus, A.

Rajesh Dabur; H. Singh; A. K. Chhillar; M. Ali; G. L. Sharma

2004-01-01

87

Antifungal stress compounds from Vicia cracca  

Microsoft Academic Search

From the leaflets of Vicia cracca two new antifungal stress compounds, 2-methoxy-6-[2-(4-methoxyphenyl)ethenyl]pyran-4-one and 2-methoxy-6-[2-(phenyl)ethenyl]pyran-4-one were isolated. Their structures were elucidated by spectroscopic means.

Mustafa M. Saleh; Karl-Werner Glombitza

1997-01-01

88

Antifungal prophylaxis during neutropenia and immunodeficiency.  

PubMed Central

Fungal infections represent a major source of morbidity and mortality in patients with almost all types of immunodeficiencies. These infections may be nosocomial (aspergillosis) or community acquired (cryptococcosis), or both (candidiasis). Endemic mycoses such as histoplasmosis, coccidioidomycosis, and penicilliosis may infect many immunocompromised hosts in some geographic areas and thereby create major public health problems. With the wide availability of oral azoles, antifungal prophylactic strategies have been extensively developed. However, only a few well-designed studies involving strict criteria have been performed, mostly in patients with hematological malignancies or AIDS. In these situations, the best dose and duration of administration of the antifungal drug often remain to be determined. In high-risk neutropenic or bone marrow transplant patients, fluconazole is effective for the prevention of superficial and/or systemic candidal infections but is not always able to prolong overall survival and potentially selects less susceptible or resistant Candida spp. Primary prophylaxis against aspergillosis remains investigative. At present, no standard general recommendation for primary antifungal prophylaxis can be proposed for AIDS patients or transplant recipients. However, for persistently immunocompromised patients who previously experienced a noncandidal systemic fungal infection, prolonged suppressive antifungal therapy is often indicated to prevent a relapse. Better strategies for controlling immune deficiencies should also help to avoid some potentially life-threatening deep mycoses. When prescribing antifungal prophylaxis, physicians should be aware of the potential emergence of resistant strains, drug-drug interactions, and the cost. Well-designed, randomized, multicenter clinical trials in high-risk immunocompromised hosts are urgently needed to better define how to prevent severe invasive mycoses. PMID:9227863

Lortholary, O; Dupont, B

1997-01-01

89

From antidiabetic to antifungal: discovery of highly potent triazole-thiazolidinedione hybrids as novel antifungal agents.  

PubMed

In an attempt to discover a new generation of triazole antifungal agents, a series of triazole-thiazolidinedione hybrids were designed and synthesized by molecular hybridization of the antifungal agent fluconazole and rosiglitazone (an antidiabetic). Most of the target compounds showed good to excellent inhibitory activity against a variety of clinically important fungal pathogens. In particular, compounds (Z)-5-(2,4-dichlorobenzylidene)-3-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)thiazolidine-2,4-dione) (15?c), (Z)-3-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-5-(furan-3-ylmethylene)thiazolidine-2,4-dione (15?j), and (Z)-3-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-5-(furan-3-ylmethylene)thiazolidine-2,4-dione (15?r) were highly active against Candida albicans, with MIC80 values in the range of 0.03-0.15??M. Moreover, compounds 15?j and 15?r were found to be effective against four fluconazole-resistant clinical isolates; these two compounds are particularly promising antifungal leads for further optimization. Molecular docking studies revealed that the hydrogen bonding interactions between thiazolidinedione and CYP51 from C.?albicans are important for antifungal activity. This study also demonstrates the effectiveness of molecular hybridization in antifungal drug discovery. PMID:25196996

Wu, Shanchao; Zhang, Yongqiang; He, Xiaomeng; Che, Xiaoying; Wang, Shengzheng; Liu, Yang; Jiang, Yan; Liu, Na; Dong, Guoqiang; Yao, Jianzhong; Miao, Zhenyuan; Wang, Yan; Zhang, Wannian; Sheng, Chunquan

2014-12-01

90

Efflux pump proteins in antifungal resistance.  

PubMed

It is now well-known that the enhanced expression of ATP binding cassette (ABC) and major facilitator superfamily (MFS) proteins contribute to the development of tolerance to antifungals in yeasts. For example, the azole resistant clinical isolates of the opportunistic human fungal pathogen Candida albicans show an overexpression of Cdr1p and/or CaMdr1p belonging to ABC and MFS superfamilies, respectively. Hence, azole resistant isolates display reduced accumulation of therapeutic drug due to its rapid extrusion and that facilitates its survival. Considering the importance of major antifungal transporters, the focus of recent research has been to understand the structure and function of these proteins to design inhibitors/modulators to block the pump protein activity so that the drug already in use could again sensitize resistant yeast cells. The review focuses on the structure and function of ABC and MFS transporters of Candida to highlight the recent advancement in the field. PMID:25221515

Prasad, Rajendra; Rawal, Manpreet K

2014-01-01

91

Antifungal activity of 10 Guadeloupean plants.  

PubMed

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. 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

2013-11-01

92

A new antifungal coumarin from Clausena excavata.  

PubMed

A new ?-lactone coumarin, named as excavarin-A, showing antifungal activity was isolated from the leaves of Clausena excavata by bioassay guided fractionation method. The structure was elucidated by spectroscopic data analysis and identified as 7((2E)-4(4,5-dihydro-3-methylene-2-oxo-5-furanyl)-3-methylbut-2-enyloxy) coumarin. Minimum inhibitory concentration (MIC) was determined against fifteen fungal strains pathogenic against plants and human. The least MIC was recorded against the human pathogen, Candida tropicalis and the plant pathogens Rhizoctonia solani and Sclerotinia sclerotiorum. Antifungal activities against the human pathogens, Aspergillus fumigatus and Mucor circinelloides and plant pathogens, Colletotrichum gloeosporioides, Lasiodiplodia theobromae, Fusarium oxysporum and Rhizopus stolonifer were stronger than that of the standard antimicrobials. PMID:22088496

Kumar, Ramashish; Saha, Aniruddha; Saha, Dipanwita

2012-01-01

93

Resistance to echinocandin-class antifungal drugs  

Microsoft Academic Search

Invasive fungal infections cause morbidity and mortality in severely ill patients, and limited drug classes restrict treatment choices. The echinocandin drugs are the first new class of antifungal compounds that target the fungal cell wall by blocking ?-1,3-d-glucan synthase. Elevated MIC values with occasional treatment failure have been reported for strains of Candida. Yet, an uncertain correlation exists between clinical

David S. Perlin

2007-01-01

94

Current and Emerging Azole Antifungal Agents  

PubMed Central

Major developments in research into the azole class of antifungal agents during the 1990s have provided expanded options for the treatment of many opportunistic and endemic fungal infections. Fluconazole and itraconazole have proved to be safer than both amphotericin B and ketoconazole. Despite these advances, serious fungal infections remain difficult to treat, and resistance to the available drugs is emerging. This review describes present and future uses of the currently available azole antifungal agents in the treatment of systemic and superficial fungal infections and provides a brief overview of the current status of in vitro susceptibility testing and the growing problem of clinical resistance to the azoles. Use of the currently available azoles in combination with other antifungal agents with different mechanisms of action is likely to provide enhanced efficacy. Detailed information on some of the second-generation triazoles being developed to provide extended coverage of opportunistic, endemic, and emerging fungal pathogens, as well as those in which resistance to older agents is becoming problematic, is provided. PMID:9880474

Sheehan, Daniel J.; Hitchcock, Christopher A.; Sibley, Carol M.

1999-01-01

95

Antifungal activity of Eugenia umbelliflora against dermatophytes.  

PubMed

Antifungal activities of Eugenia umbelliflora Berg. (Myrtaceae) were tested in vitro against a panel of standard and clinical isolates of human fungal pathogens (dermatophytes and opportunistic saprobes). Methanol extracts of leaves and fruits of E. umbelliflora were separately prepared and partitioned, to yield dichloromethane (DCM), ethyl acetate (EtOAc) and aqueous fractions (Aq). Three compounds (1-3) were obtained from the DCM extract using chromatographic procedures. Antifungal assays were performed using agar dilution techniques. Both extracts (fruits and leaves), their DCM and EtOAc fractions, and compound 2 (betulin and betulinic acid) presented selective antifungal activity against dermatophytes (Epidermophyton floccosum, Microsporum canis, Microsporum gypseum, Trichophyton rubrum, Trichophyton mentagrophytes), with MIC values between 200 and 1000 microg/mL, and interestingly, inhibited 4/5 species with MIC values of < or = 500 microg/mL. The aqueous fractions of fruits and leaves, and compounds 1 (alpha, beta amyrin) and 3 (taraxerol) were inactive up to the maximum concentrations tested (1000 microg/mL). PMID:19831024

Machado, Karina E; Cechinel Filho, Valdir; Cruz, Rosana C B; Meyre-Silva, Christiane; Cruz, Alexandre Bella

2009-09-01

96

Posaconazole (Noxafil): a new triazole antifungal agent  

PubMed Central

Posaconazole is the newest triazole antifungal agent. It is structurally related to itraconazole and has activity against Candida species, Aspergillus species, Cryptococcus neoformans, the zygomycetes, and other filamentous fungi. Randomized, double-blind trials have shown posaconazole to be at least as efficacious as fluconazole for the prevention of invasive fungal infections in immunocompromised patients. It has also shown promising results in the treatment of various fungal infections refractory to other antifungal therapy. The dose of posaconazole is 200 mg orally three times daily for the prevention of invasive fungal infections and 800 mg daily in two to four divided doses for the treatment of invasive fungal infections refractory to other antifungal treatment. All posaconazole doses should be given with food or a nutritional supplement to enhance absorption. The most common adverse effects reported with posaconazole therapy were fever, diarrhea, nausea, vomiting, and headache. Instances of elevated liver enzyme levels, hyperbilirubinemia, and hepatocellular damage were also noted in clinical trials, and these laboratory values should be monitored during treatment with posaconazole. PMID:17431456

2007-01-01

97

Antifungal ellagitannin isolated from Euphorbia antisyphilitica Zucc  

PubMed Central

Objective To study antifungal activity of a new ellagitannin isolated from the plant residues of Euphorbia antisyphilitica (E. antisyphilitica) Zucc in the wax extraction process. Methods An extract was prepared from dehydrated and pulverized residues and fractionated by liquid chromatography on Amberilte XAD-16, until obtained an ellagitannin-rich ethanolic fraction which was treated by rotaevaporation to recover the ellagitannin as fine powder. An aqueous solution was prepared and treated through ionic exchange liquid chromatography (Q XL) and gel permeation chromatography (G 25). The ellagitannin-rich fraction was thermogravimetrically evaluated (TGA and DTA) to test the thermo-stability of ellagic acid (monomeric unit). Then ellagitannin powder was analyzed by infrared spectrospcopy to determinate the functional groups and, also mass spectroscopy was used to determine the molecular ion. Results The principal functional groups of ellagitannin were determined, the molecular weight was 860.7 g/mol; and an effective antifungal activity against phytopathogenic fungi was demonstrated. Conclusions It can be concluded that the new ellagitannin (860.7 g/mol) isolated from E. antisyphilitica Zucc is an effective antifungal agent against Alternaria alternata, Fusarium oxyzporum, Colletotrichum gloeosporoides and Rhizoctnia solani. PMID:23570015

Ascacio-Valdes, Juan; Burboa, Edgardo; Aguilera-Carbo, Antonio F; Aparicio, Mario; Perez-Schmidt, Ramon; Rodriguez, Raul; Aguilar, Cristobal N

2013-01-01

98

Hydroxytyrosol expresses antifungal activity in vitro.  

PubMed

Hydroxytyrosol (HT) is a potent antioxidant found in olive oil and leaves. Using several in vitro approaches, we tested antifungal activity of HT. HT showed broad spectrum of antifungal activity against medically important yeasts and dermatophyte strains with MIC values ranging between 97.6 µgml?¹ and 6.25 mgml?¹. The antimicrobial activity of HT was also tested using the time-kill methodology. Below the MIC value, HT showed potent damage of cell wall of Candida albicans ATCC 10231 using fluorescent dye-exclusion method. At the subinhibitory concentration, HT also influenced dimorphic transition of Candida indicating that HT is inhibitor of germ-tube formation as one of the most important virulence factor of C. albicans. Furthermore, HT showed disturbances in cell surface hydrophobicity (CSH) of C. albicans. The in vitro results indicate that HT caused a significant cell wall damage and changes in CSH as well as inhibition of germ-tube formation as virulence factor of C. albicans. The study indicates that HT has a considerable in vitro antifungal activity against medically important yeasts. PMID:23721186

Zoric, Natasa; Horvat, Igor; Kopjar, Nevenka; Vucemilovic, Ante; Kremer, Dario; Tomic, Sinisa; Kosalec, Ivan

2013-08-01

99

Antifungal Activity of Maytenin and Pristimerin  

PubMed Central

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

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

2012-01-01

100

Antifungal activity against Scedosporium species and novel assays to assess antifungal pharmacodynamics against filamentous fungi.  

PubMed

The saprophytic moulds Scedosporium prolificans and Scedosporium apiospermum/Pseudallescheria boydii are an increasing cause of invasive fungal infections in immunocompromised hosts. The growing importance and high mortality rates of invasive disease caused by these fungi necessitates the search for newer treatment strategies. However, clinically available antifungal agents have modest to minimal activity against these organisms that has been confirmed by suboptimal responses in the clinic. Due to this limited in vitro activity and poor clinical response, antifungal combinations and high-dose regimens are frequently recommended to treat these refractory infections. However, development of a pharmacodynamic basis for antifungal dosing in scedosporiosis has been hampered by the limitations in the application of traditional microbiological techniques and endpoints for Scedosporium species. Newer quantitative and qualitative assays have demonstrated utility for measuring drug lethality in filamentous fungi, including Scedosporium species, and may aid in the development of new treatment strategies to improve patient outcomes PMID:19058049

Wiederhold, Nathan P; Lewis, Russell E

2009-06-01

101

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

2007-01-01

102

Synthesis of novel substituted tetrazoles having antifungal activity  

Microsoft Academic Search

In an effort to find potent antifungal agents, a variety of triazole derivatives with a 5-substituted tetrazole structure 6, 7, 12 and 14 were prepared and evaluated for antifungal activity against Candida spp., Cryptococcus neoformans, and Aspergillus spp. in vitro. The location of the methyl group at the C-3 of compounds 12 and 14 has been demonstrated to be a

Ram Shankar Upadhayaya; Sanjay Jain; Neelima Sinha; Nawal Kishore; Ramesh Chandra; Sudershan K Arora

2004-01-01

103

Cuticular Antifungals in Spiders: Density- and Condition Dependence  

PubMed Central

Animals living in groups face a high risk of disease contagion. In many arthropod species, cuticular antimicrobials constitute the first protective barrier that prevents infections. Here we report that group-living spiders produce cuticular chemicals which inhibit fungal growth. Given that cuticular antifungals may be costly to produce, we explored whether they can be modulated according to the risk of contagion (i.e. under high densities). For this purpose, we quantified cuticular antifungal activity in the subsocial crab spider Diaea ergandros in both natural nests and experimentally manipulated nests of varying density. We quantified the body-condition of spiders to test whether antifungal activity is condition dependent, as well as the effect of spider density on body-condition. We predicted cuticular antifungal activity to increase and body-condition to decrease with high spider densities, and that antifungal activity would be inversely related to body-condition. Contrary to our predictions, antifungal activity was neither density- nor condition-dependent. However, body-condition decreased with density in natural nests, but increased in experimental nests. We suggest that pathogen pressure is so important in nature that it maintains high levels of cuticular antifungal activity in spiders, impacting negatively on individual energetic condition. Future studies should identify the chemical structure of the isolated antifungal compounds in order to understand the physiological basis of a trade-off between disease prevention and energetic condition caused by group living, and its consequences in the evolution of sociality in spiders. PMID:24637563

Gonzalez-Tokman, Daniel; Ruch, Jasmin; Pulpitel, Tamara; Ponton, Fleur

2014-01-01

104

Characterization of the Penicillium chrysogenum antifungal protein PAF  

Microsoft Academic Search

The filamentous fungus Penicillium chrysogenum abundantly secretes the small, highly basic and cysteine-rich protein PAF ( Penicillium antifungal protein). In this study, the antifungal activity of PAF is described. PAF inhibited the growth of a variety of filamentous fungi, including opportunistic human pathogenic and phytopathogenic fungi, whereas bacterial and yeast cells were unaffected. PAF reduced the conidial germination and hyphal

Lydia Kaiserer; Christoph Oberparleiter; Renate Weiler-Görz; Wolfgang Burgstaller; Eva Leiter; Florentine Marx

2003-01-01

105

Antifungal Chemical Compounds Identified Using a C. elegans Pathogenicity Assay  

E-print Network

of the main obstacles in current antifungal discovery. We show that Candida albicans, as well as other Candida of the main obstacles in current antifungal discovery. Here, we show that Candida albicans, as well as other. elegans intestinal track. Importantly, key components of Candida pathogenesis in mammals, such as filament

Ausubel, Frederick M.

106

Cuticular antifungals in spiders: density- and condition dependence.  

PubMed

Animals living in groups face a high risk of disease contagion. In many arthropod species, cuticular antimicrobials constitute the first protective barrier that prevents infections. Here we report that group-living spiders produce cuticular chemicals which inhibit fungal growth. Given that cuticular antifungals may be costly to produce, we explored whether they can be modulated according to the risk of contagion (i.e. under high densities). For this purpose, we quantified cuticular antifungal activity in the subsocial crab spider Diaea ergandros in both natural nests and experimentally manipulated nests of varying density. We quantified the body-condition of spiders to test whether antifungal activity is condition dependent, as well as the effect of spider density on body-condition. We predicted cuticular antifungal activity to increase and body-condition to decrease with high spider densities, and that antifungal activity would be inversely related to body-condition. Contrary to our predictions, antifungal activity was neither density- nor condition-dependent. However, body-condition decreased with density in natural nests, but increased in experimental nests. We suggest that pathogen pressure is so important in nature that it maintains high levels of cuticular antifungal activity in spiders, impacting negatively on individual energetic condition. Future studies should identify the chemical structure of the isolated antifungal compounds in order to understand the physiological basis of a trade-off between disease prevention and energetic condition caused by group living, and its consequences in the evolution of sociality in spiders. PMID:24637563

González-Tokman, Daniel; Ruch, Jasmin; Pulpitel, Tamara; Ponton, Fleur

2014-01-01

107

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. PMID:21804864

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

2011-01-01

108

Antifungal ether diglycosides from Matayba guianensis Aublet.  

PubMed

Since the 1960s, fungal infections have become a major worldwide public health problem. Antifungal treatments have many limitations, such as toxicity and resistance. Matayba guianensis Aublet (Sapindaceae) was chemically investigated as part of our ongoing search for lead molecules against fungi in the Brazilian Cerrado biome. The ethanolic extract of M. guianensis root bark revealed the presence of two previously unreported ether diglycosides: matayoside E (1) and F (2) with anti Candida activity, along with two known compounds: cupanioside (3) and stigmasterol (4). PMID:24485783

de Assis, Polyana A; Theodoro, Phellipe N E T; de Paula, José E; Araújo, Ana J; Costa-Lotufo, Letícia V; Michel, Sylvie; Grougnet, Raphaël; Kritsanida, Marina; Espindola, Laila S

2014-03-01

109

Nylon-3 polymers with selective antifungal activity.  

PubMed

Host-defense peptides inhibit bacterial growth but show little toxicity toward mammalian cells. A variety of synthetic polymers have been reported to mimic this antibacterial selectivity; however, achieving comparable selectivity for fungi is more difficult because these pathogens are eukaryotes. Here we report nylon-3 polymers based on a novel subunit that display potent antifungal activity (MIC = 3.1 ?g/mL for Candida albicans ) and favorable selectivity (IC10 > 400 ?g/mL for 3T3 fibroblast toxicity; HC10 > 400 ?g/mL for hemolysis). PMID:23547967

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

2013-04-10

110

In Vitro Antifungal Susceptibility of Cryptococcus gattii  

PubMed Central

We have determined the in vitro susceptibilities of 57 strains of Cryptococcus gattii to nine antifungal agents and have compared the MICs for these strains with those for C. neoformans. MICs were determined by a microdilution reference method. Albaconazole and ravuconazole (MICs of 0.04 and 0.05 ?g/ml, respectively) showed the best activities. Micafungin showed no activity (MIC of >128 ?g/ml). In general, C. gattii was less susceptible than C. neoformans to all drugs tested, with the exception of amphotericin B and flucytosine. PMID:15472349

Trilles, Luciana; Fernandez-Torres, Belkys; dos Santos Lazera, Marcia; Wanke, Bodo; Guarro, Josep

2004-01-01

111

Resistance to antifungals that target CYP51.  

PubMed

Fungal diseases are an increasing global burden. Fungi are now recognised to kill more people annually than malaria, whilst in agriculture, fungi threaten crop yields and food security. Azole resistance, mediated by several mechanisms including point mutations in the target enzyme (CYP51), is increasing through selection pressure as a result of widespread use of triazole fungicides in agriculture and triazole antifungal drugs in the clinic. Mutations similar to those seen in clinical isolates as long ago as the 1990s in Candida albicans and later in Aspergillus fumigatus have been identified in agriculturally important fungal species and also wider combinations of point mutations. Recently, evidence that mutations originate in the field and now appear in clinical infections has been suggested. This situation is likely to increase in prevalence as triazole fungicide use continues to rise. Here, we review the progress made in understanding azole resistance found amongst clinically and agriculturally important fungal species focussing on resistance mechanisms associated with CYP51. Biochemical characterisation of wild-type and mutant CYP51 enzymes through ligand binding studies and azole IC50 determinations is an important tool for understanding azole susceptibility and can be used in conjunction with microbiological methods (MIC50 values), molecular biological studies (site-directed mutagenesis) and protein modelling studies to inform future antifungal development with increased specificity for the target enzyme over the host homologue. PMID:25320648

Parker, Josie E; Warrilow, Andrew G S; Price, Claire L; Mullins, Jonathan G L; Kelly, Diane E; Kelly, Steven L

2014-10-01

112

Susceptibility of Prototheca Species to Antifungal Agents  

PubMed Central

Twenty isolates of Prototheca filamenta, Prototheca moriformis, Prototheca stagnora, Prototheca wickerhamii, and Prototheca zopfii were tested for in vitro susceptibility to five commonly used antifungal agents: amphotericin B, 5-fluorocytosine, griseofulvin, miconazole, and nystatin. The results revealed resistance to griseofulvin of all the Prototheca isolates tested and an inhibitory effect on P. filamenta by high 5-fluorocytosine concentrations (minimal inhibitory concentration [MIC] = 12.5 to 100 ?g/ml; minimal fungicidal or algacidal concentration [MFC/MAC] = 50 to 100 ?g/ml). P. filamenta isolates were also susceptible to miconazole (MIC = 0.1 to 0.5 ?g/ml, MFC/MAC = 0.5 to 1 ?g/ml); isolates of the other Prototheca species varied in regard to miconazole activity from susceptible to resistant (MIC = 1 ? >100 ?g/ml, MFC/MAC = 5 ? >100 ?g/ml). The Prototheca isolates revealed an in vitro susceptibility to the polyene antifungal agents, amphotericin B, and nystatin (MIC = 0.09 to 3.12 ?g/ml and 0.19 to 12.5 ?g/ml, respectively; MFC/MAC = 0.19 to 25 ?g/ml and 0.75 to 25 ?g/ml, respectively). PMID:984758

Segal, Ester; Padhye, Arvind A.; Ajello, Libero

1976-01-01

113

Potentiation of azole antifungals by 2-adamantanamine.  

PubMed

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

2013-08-01

114

Antifungal Th Immunity: Growing up in Family  

PubMed Central

Fungal diseases represent an important paradigm in immunology since they can result from either the lack of recognition or over-activation of the inflammatory response. Current understanding of the pathophysiology underlying fungal infections and diseases highlights the multiple cell populations and cell-signaling pathways involved in these conditions. A systems biology approach that integrates investigations of immunity at the systems-level is required to generate novel insights into this complexity and to decipher the dynamics of the host–fungus interaction. It is becoming clear that a three-way interaction between the host, microbiota, and fungi dictates the types of host–fungus relationship. Tryptophan metabolism helps support this interaction, being exploited by the mammalian host and commensals to increase fitness in response to fungi via resistance and tolerance mechanisms of antifungal immunity. The cellular and molecular mechanisms that provide immune homeostasis with the fungal biota and its possible rupture in fungal infections and diseases will be discussed within the expanding role of antifungal Th cell responses.

Borghi, Monica; Renga, Giorgia; Puccetti, Matteo; Oikonomou, Vasileios; Palmieri, Melissa; Galosi, Claudia; Bartoli, Andrea; Romani, Luigina

2014-01-01

115

Antifungal Th Immunity: Growing up in Family.  

PubMed

Fungal diseases represent an important paradigm in immunology since they can result from either the lack of recognition or over-activation of the inflammatory response. Current understanding of the pathophysiology underlying fungal infections and diseases highlights the multiple cell populations and cell-signaling pathways involved in these conditions. A systems biology approach that integrates investigations of immunity at the systems-level is required to generate novel insights into this complexity and to decipher the dynamics of the host-fungus interaction. It is becoming clear that a three-way interaction between the host, microbiota, and fungi dictates the types of host-fungus relationship. Tryptophan metabolism helps support this interaction, being exploited by the mammalian host and commensals to increase fitness in response to fungi via resistance and tolerance mechanisms of antifungal immunity. The cellular and molecular mechanisms that provide immune homeostasis with the fungal biota and its possible rupture in fungal infections and diseases will be discussed within the expanding role of antifungal Th cell responses. PMID:25360137

Borghi, Monica; Renga, Giorgia; Puccetti, Matteo; Oikonomou, Vasileios; Palmieri, Melissa; Galosi, Claudia; Bartoli, Andrea; Romani, Luigina

2014-01-01

116

Scaffold hopping of sampangine: discovery of potent antifungal lead compound against Aspergillus fumigatus and Cryptococcus neoformans.  

PubMed

Discovery of novel antifungal agents against Aspergillus fumigatus and Cryptococcus neoformans remains a significant challenge in current antifungal therapy. Herein the antifungal natural product sampangine was used as the lead compound for novel antifungal drug discovery. A series of D-ring scaffold hopping derivatives were designed and synthesized to improve antifungal activity and water solubility. Among them, the thiophene derivative S2 showed broad-spectrum antifungal activity, particularly for Aspergillus fumigatus and Cryptococcus neoformans. Moreover, compound S2 also revealed better water solubility than sampangine, which represents a promising antifungal lead compound for further structural optimization. PMID:25115626

Jiang, Zhigan; Liu, Na; Dong, Guoqiang; Jiang, Yan; Liu, Yang; He, Xiaomeng; Huang, Yahui; He, Shipeng; Chen, Wei; Li, Zhengang; Yao, Jianzhong; Miao, Zhenyuan; Zhang, Wannian; Sheng, Chunquan

2014-09-01

117

Antifungal activities of ethanolic extract from Jatropha curcas seed cake.  

PubMed

Phorbol ester extraction was carried out from Jatropha curcas seed cake, a by-product from the bio-diesel fuel industry. Four repeated extractions from 5 g J. curcas seed cake using 15 ml of 90% (v/v) ethanol and a shaking speed of 150 rev/min gave the highest yield of phosbol esters. The ethanolic extract of J. curcas seed cake showed antifungal activities against important phytofungal pathogens: Fusarium oxysporum, Pythium aphanidermatum, Lasiodiplodia theobromae, Curvularia lunata, Fusarium semitectum, Colletotrichum capsici and Colletotrichum gloeosporiodes. The extract contained phorbol esters mainly responsible for antifungal activities. The extract could therefore be used as an antifungal agent for agricultural applications. PMID:20208435

Saetae, Dolaporn; Suntornsuk, Worapot

2010-02-01

118

Overview of medically important antifungal azole derivatives.  

PubMed Central

Fungal infections are a major burden to the health and welfare of modern humans. They range from simply cosmetic, non-life-threatening skin infections to severe, systemic infections that may lead to significant debilitation or death. The selection of chemotherapeutic agents useful for the treatment of fungal infections is small. In this overview, a major chemical group with antifungal activity, the azole derivatives, is examined. Included are historical and state of the art information on the in vitro activity, experimental in vivo activity, mode of action, pharmacokinetics, clinical studies, and uses and adverse reactions of imidazoles currently marketed (clotrimazole, miconazole, econazole, ketoconazole, bifonazole, butoconazole, croconazole, fenticonazole, isoconazole, oxiconazole, sulconazole, and tioconazole) and under development (aliconazole and omoconazole), as well as triazoles currently marketed (terconazole) and under development (fluconazole, itraconazole, vibunazole, alteconazole, and ICI 195,739). PMID:3069196

Fromtling, R A

1988-01-01

119

Antifungal activity of three spermidine conjugates.  

PubMed

Three tri-substituted spermidines, di-p-coumaroyl-caffeoylspermidine, tri-caffeoylspermidine and tri-p-coumaroylspermidine, isolated from pollen of Quercus alba, were examined for antifungal activity. Both di-p-coumaroyl-caffeoylspermidine and tri-p-coumaroylspermidine reduced mycelial growth of the oat leaf stripe pathogen, Pyrenophora avenae and reduced powdery mildew (Blumeria graminis f. sp. hordei) infection of barley seedlings when applied as a post-inoculation treatment. When used as a pre-inoculation treatment, only di-p-coumaroyl-caffeoylspermidine reduced powdery mildew infection significantly. Growth of P. avenae in the presence of 100 microM di-p-coumaroyl-caffeoylspermidine reduced activity of S-adenosylmethionine decarboxylase (AdoMetDC), and led to a reduction in the incorporation of labelled ornithine into spermidine. The other two spermidine conjugates increased AdoMetDC activity and the flux label from ornithine into spermine in P. avenae significantly. PMID:11470370

Walters, D; Meurer-Grimes, B; Rovira, I

2001-07-24

120

Antifungal combination therapy for invasive aspergillosis.  

PubMed

The outcome of invasive aspergillosis (IA) continues to be associated with significant attributable mortality, especially in patients with hematological malignancies and in hematopoietic stem cell transplant recipients. In this context, antifungal combined therapy (ACT) has become an emerging strategy against IA. In an attempt to evaluate the benefits of ACT, a large number of experimental studies, clinical series, and randomized trials have been performed, with varying results. In addition, several controlled trials have been registered; however, in most cases, their final results have not been made available. In summary, there is an imbalance between the lack of published evidence regarding the benefits of ACT and its extensive and increasing use in current clinical practice, despite its associated cost. Here, we present a critical analysis of the available information regarding ACT for the treatment of IA as well as the authors' opinion with respect to its use. PMID:25048847

Martín-Peña, Almudena; Aguilar-Guisado, Manuela; Espigado, Ildefonso; Cisneros, José Miguel

2014-11-15

121

Role of micafungin in the antifungal armamentarium.  

PubMed

Serious infections caused by opportunistic molds remain a major problem for public health. Immune deficiency following organ transplantation and aggressive cancer treatment has greatly increased the incidence of systemic mycoses, and invasive aspergillosis in patients with AIDS is associated with significant morbidity and mortality. Amphotericin B is the first-line therapy for systemic infection because of its broad-spectrum and fungicidal activity. However, considerable side effects limit its clinical utility. The echinocandins are large lipopeptide molecules that inhibit the synthesis of 1,3-beta-D-glucan, a key component of the fungal cell wall. Three echinocandins have reached the market, and some others are in early clinical development. Caspofungin was the first echinocandin to be licensed for clinical use in most countries. Micafungin is licensed for clinical use in Japan, China, Taiwan, Jordan, Korea, Hong-Kong and the US, and anidulafungin is currently licensed in the US. The novel class of echinocandins represents a milestone in antifungal drug research that has further expanded our therapeutic options. Studies to date have shown that micafungin exhibits extremely potent antifungal activity against clinically important fungi, including Aspergillus and azole-resistant strains of Candida. In animal studies, micafungin is as efficacious as amphotericin B with respect to improvement of survival rate. Micafungin is also characterized by a linear pharmacokinetic profile and substantially fewer toxic effects. Micafungin is a poor substrate for the cytochrome P450 enzymes, and compared to azoles, fewer drug interactions are described. No dose adjustments of the drug are required in the presence of mycophenolate mofetil, cyclosporin, tacrolimus, prednisolone, or sirolimus. Strategies using this new echinocandin agent will benefit a large number of patients with severe immune dysfunction. PMID:17504145

Ikeda, Fumiaki; Tanaka, Shigeki; Ohki, Hidenori; Matsumoto, Satoru; Maki, Katsuyuki; Katashima, Masataka; Barrett, David; Aoki, Yoshiyasu

2007-01-01

122

ALTERATIONS IN mRNA GENE EXPRESSION ASSOCIATED WITH CHOLESTEROL METABOLISM, CELL CYCLE, AND OXIDATIVE STRESS INDUCED BY TRIAZOLE CONTAINING CONAZOLES IN RAT LIVER  

EPA Science Inventory

Conazoles are fungicides used as pharmaceuticals and in agriculture. Triadimefon was hepatotoxic and induced follicular cell adenomas in the thyroid gland. In contrast,propiconazole and myclobutanil were hepatotoxic but had no effect on the thyroid gland. It was proposed that tri...

123

Evaluation of selected fungicides to control mint rust on Scotch spearmint  

Microsoft Academic Search

Mint rust, caused by the fungus Puccinia menthae, is a serious disease limiting the establishment of a viable spearmint oil industry in north east Victoria, Australia. Six fungicide-active ingredients: bitertanol, triadimenol, fluquinconazole, tebuconazole, myclobutanil and propiconazole, were evaluated for control of this disease. Bitertanol gave the most effective control resulting in higher oil yields, followed by tebuconazole. Fluquinconazole was the

J Edwards; F. E Bienvenu

2000-01-01

124

Antifungal activity of fruit pulp extract from Bromelia pinguin.  

PubMed

The methanol extract of the fruit pulp of Bromelia pinguin was evaluated for its antifungal activity. The extract showed a significant activity against some Trichophyton strains, although Candida strains were generally insensitive. PMID:12165338

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

2002-08-01

125

Dendritic Cells in Anti-Fungal Immunity and Vaccine Design  

PubMed Central

Life-threatening fungal infections have increased in recent years while treatment options remain limited. The development of vaccines against fungal pathogens represents a key advance sorely needed to combat the increasing fungal disease threat. Dendritic cells (DC) are uniquely able to shape anti-fungal immunity by initiating and modulating naive T cell responses. Targeting DC may allow for the generation of potent vaccines against fungal pathogens. In the context of anti-fungal vaccine design, we describe the characteristics of the varied DC subsets, how DC recognize fungi, their function in immunity against fungal pathogens, and how DC can be targeted in order to create new anti-fungal vaccines. Ongoing studies continue to highlight the critical role of DC in anti-fungal immunity and will help guide DC-based vaccine strategies. PMID:22607797

Roy, Rene M.; Klein, Bruce S.

2012-01-01

126

An antifungal constituent from the stem bark of Butea monosperma.  

PubMed

The petroleum and ethyl acetate extracts of the stem bark from Butea monosperma displayed antifungal activity against Cladosporium cladosporioides. The active constituent of low polarity was isolated by bioassay-monitored chromatographic fractionation, and identified as (-)-medicarpin by comparison of physical data. The antifungal activity of (-)-medicarpin was found to be greater than that of Benlate, a standard fungicide, while (-)-medicarpin acetate also exhibited significant activity against C. cladosporiodes. PMID:2716344

Bandara, B M; Kumar, N S; Samaranayake, K M

1989-02-01

127

Antibacterial and antifungal activity of Indonesian ethnomedical plants.  

PubMed

Methylene chloride and methanol extracts of 20 Indonesian plants with ethnomedical uses have been assessed for in vitro antibacterial and antifungal properties by disk diffusion method. Extracts of the six plants: Terminalia catappa, Swietenia mahagoni Jacq., Phyllanthus acuminatus, Ipomoea spp., Tylophora asthmatica and Hyptis brevipes demonstrated high activity in this bioassay system. These findings should stimulate the search for novel, natural product such as new antibacterial and antifungal agents. PMID:12946723

Goun, E; Cunningham, G; Chu, D; Nguyen, C; Miles, D

2003-09-01

128

Antifungal constituents in the bark of Magnolia obovata Thunb  

Microsoft Academic Search

The acetone extract of the bark ofMagnolia obovata Thunb. had potent antifungal activity against plant pathogenic and wood destroying fungi. The active principles were isolated\\u000a and identified to be eudesmols (I), magnolol (II) and honokiol (III). Eudesmols, which are main components of the volatile\\u000a bark oil, showed strong antifungal activity against all of the fungi tested, especially basidiomycetes. It completely

M. Mori; M. Aoyama; S. Doi

1997-01-01

129

Antifungal effect and mechanism of garlic oil on Penicillium funiculosum.  

PubMed

Garlic oil is a kind of fungicide, but little is known about its antifungal effects and mechanism. In this study, the chemical constituents, antifungal activity, and effects of garlic oil were studied with Penicillium funiculosum as a model strain. Results showed that the minimum fungicidal concentrations (MFCs, v/v) were 0.125 and 0.0313 % in agar medium and broth medium, respectively, suggesting that the garlic oil had a strong antifungal activity. The main ingredients of garlic oil were identified as sulfides, mainly including disulfides (36 %), trisulfides (32 %) and monosulfides (29 %) by gas chromatograph-mass spectrometer (GC/MS), which were estimated as the dominant antifungal factors. The observation results by transmission electron microscope (TEM) and scanning electron microscope (SEM) indicated that garlic oil could firstly penetrate into hyphae cells and even their organelles, and then destroy the cellular structure, finally leading to the leakage of both cytoplasm and macromolecules. Further proteomic analysis displayed garlic oil was able to induce a stimulated or weakened expression of some key proteins for physiological metabolism. Therefore, our study proved that garlic oil can work multiple sites of the hyphae of P. funiculosum to cause their death. The high antifungal effects of garlic oil makes it a broad application prospect in antifungal industries. PMID:25012787

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

2014-10-01

130

Isolation of Bacillus amyloliquefaciens Strains with Antifungal Activities from Meju  

PubMed Central

Bacilli with fibrinolytic activities were isolated from traditionally-prepared Meju and some of these strains showed strong antifungal activities. One isolate, MJ1-4, showed the strongest antifungal activity. MJ1-4 and other isolates were identified as B. amyloliquefaciens strains by recA gene sequencing and RAPD-PCR results. B. amyloliqufaciens MJ1-4 efficiently inhibited an Aspergillus spp.-producing aflatoxin B1 (AFB1) and a Penicillium spp.-producing ochratoxin (OTA) in addition to other fungi. Antifungal activity of B. amyloliquefaciens MJ1-4 culture reached its maximum (40 AU/mg protein) in LB or TSB medium around 48 hr at 37°C. Antifungal activity of the concentrated culture supernatant was not decreased significantly by protease treatments, implying that the antifungal substance might not be a simple peptide or protein. Considering its antifungal and fibrinolytic activities together, B. amyloliquefaciens MJ1-4 can serve as a starter for fermented soyfoods such as Cheonggukjang and Doenjang. PMID:24471064

Lee, Hwang A; Kim, Jeong Hwan

2012-01-01

131

Antifungal effect of 4-arylthiosemicarbazides against Candida species. Search for molecular basis of antifungal activity of thiosemicarbazide derivatives.  

PubMed

The in vitro antifungal potency of six series of 4-arylthiosemicarbazides was evaluated. Two isoquinoline derivatives with an ortho-methoxy or ortho-methyl group at the phenyl ring were the most potent antifungal agents. Molecular modeling studies and docking of all 4-arylthiosemicarbazides into the active sites of sterol 14?-demethylase (CYP51), topoisomerase II (topo II), L: -glutamine: D: -fructose-6-phosphate amidotransferase (GlcN-6-P), secreted aspartic proteinase (SAP), N-myristoyltransferase (NMT), and UDP-N-acetylmuramoyl-L: -alanine:D: -glutamate ligase (MurD) indicated the importance of both structural and electronic factors in ligand recognition and thus for the antifungal effectiveness of 4-arylthiosemicarbazides. A possible antifungal target was identified (NMT) and isoquinoline-thiosemicarbazides showed more favorable affinity than the native ligand. PMID:22535361

Siwek, Agata; Stefa?ska, Joanna; Dzitko, Katarzyna; Ruszczak, Artur

2012-09-01

132

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

PubMed

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. PMID:23269738

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

2013-03-01

133

Antifungal activity of plant extracts against dermatophytes.  

PubMed

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

1999-01-01

134

Synthesis and antifungal activities of miltefosine analogs  

PubMed Central

Miltefosine is an alkylphosphocholine that shows broad-spectrum in vitro antifungal activities and limited in vivo efficacy in mouse models of cryptococcosis. To further explore the potential of this class of compounds for the treatment of systemic mycoses, nine analogs (3a–3i) were synthesized by modifying the choline structural moiety and the alkyl chain length of miltefosine. In vitro testing of these compounds against the opportunistic fungal pathogens Candida albicans, Candida glabrata, Candida krusei, Aspergillus fumigatus, and Cryptococcus neoformans revealed that N-benzyl-N,N-dimethyl-2-{[(hexadecyloxy)hydroxyphosphinyl]oxy}ethanaminium inner salt (3a), N,N-dimethyl-N-(4-nitrobenzyl)-2-{[(hexadecyloxy)hydroxyphosphinyl]oxy}ethanaminium inner salt (3d), and N-(4-methoxybenzyl)-N,N-dimethyl-2-{[(hexadecyloxy)hydroxyphosphinyl]oxy}ethanaminium inner salt (3e) exhibited minimum inhibitory concentrations (MIC) of 2.5–5.0 ?g/mL against all tested pathogens, when compared to miltefosine with MICs of 2.5–3.3 ?g/mL. Compound 3a showed low in vitro cytotoxicity against three mammalian cell lines similar to miltefosine. In vivo testing of 3a and miltefosine against C. albicans in a mouse model of systemic infection did not demonstrate efficacy. The results of this study indicate that further investigation will be required to determine the potential usefulness of the alkylphosphocholines in the treatment of invasive fungal infections. PMID:23891181

Ravu, Ranga Rao; Chen, Ying-Lien; Jacob, Melissa R.; Pan, Xuewen; Agarwal, Ameeta K.; Khan, Shabana I.; Heitman, Joseph; Clark, Alice M.; Li, Xing-Cong

2013-01-01

135

Antifungal Activity of Isothiocyanates and Related Compounds  

PubMed Central

Antifungal activity on Aspergillus niger, Penicillium cyclopium, and Rhizopus oryzae, as well as on additional saprophytic and parasitic fungi, was determined in 57 substituted derivatives of phenylisothiocyanate. Most of the investigated compounds displayed rather equal activity against the three mentioned fungi, in contradistinction to the analogues of natural benzyl- and ?-phenylethylisothiocyanate with their characteristic low activity against R. oryzae. Differences occurred in the type of activity of compounds in which the —NCS group is directly bound on the aromatic moiety, as compared with those compounds in which this group is bound to the aliphatic radical or to the aromatic moiety indirectly by means of the methyl group or by a longer aliphatic chain. The results obtained confirm the negative influence of ionized substituents on the aromatic moiety, i.e., of —COOH, —CH2— COOH, and —SO3H groups, as well as of substituents which cause an extreme increase in reactivity of the —NCS group resulting in a high instability of the entire isothiocyanate molecule. PMID:6049295

Drobnica, L.; Zemanova, M.; Nemec, P.; Kristian, P.; Antos, K.; Hulka, A.

1967-01-01

136

Resistance to echinocandin-class antifungal drugs.  

PubMed

Invasive fungal infections cause morbidity and mortality in severely ill patients, and limited drug classes restrict treatment choices. The echinocandin drugs are the first new class of antifungal compounds that target the fungal cell wall by blocking beta-1,3-d-glucan synthase. Elevated MIC values with occasional treatment failure have been reported for strains of Candida. Yet, an uncertain correlation exists between clinical failure and elevated MIC values for the echinocandin drugs. Fungi display several adaptive physiological mechanisms that result in elevated MIC values. However, resistance to echinocandin drugs among clinical isolates is associated with amino acid substitutions in two "hot-spot" regions of Fks1, the major subunit of glucan synthase. The mutations, yielding highly elevated MIC values, are genetically dominant and confer cross-resistance to all echinocandin drugs. Prominent Fks1 mutations decrease the sensitivity of glucan synthase for drug by 1000-fold or more, and strains harboring such mutations may require a concomitant increase in drug to reduce fungal organ burdens in animal infection models. The Fks1-mediated resistance mechanism is conserved in a wide variety of Candida spp. and can account for intrinsic reduced susceptibility of certain species. Fks1 mutations confer resistance in both yeasts and moulds suggesting that this mechanism is pervasive in the fungal kingdom. PMID:17569573

Perlin, David S

2007-06-01

137

In vitro antifungal activity of sertaconazole.  

PubMed

The antifungal activity of 7-chloro-3-[1-(2,4-dichlorophenyl)-2-(1H- imidazol-1-yl)ethoxy-methyl]benzo[b]thiophene (sertaconazole, FI-7045, CAS 99592-32-2) versus miconazole has been studied in vitro against yeast-like fungi, dermatophytes and other filamentous fungi. Candida albicans was very sensitive to sertaconazole both in serotype A and serotype B strains (MIC = 0.21 micrograms/ml). Sensitivity of Candida non albicans species (MIC = 0.17 microgram/ml), Torulopsis (MIC = 0.09 microgram/ml) and Trichosporon (MIC = 0.09 microgram/ml) was also remarkable. For dermatophytes, partial inhibitions were observed at concentrations of 0.04 and 0.09 microgram/ml, the 50% inhibition ranging between 0.36 and 12.56 micrograms/ml for most strains. Filamentous opportunistic fungi were less sensitive to azoles, although sertaconazole MICs were lower than those of miconazole. Sertaconazole also proved to possess a remarkable fungicidal activity on all strains of Candida albicans under study. PMID:1627187

Drouhet, E; Dupont, B

1992-05-01

138

Increasing Patient Adherence in Antifungal Infection Treatment  

PubMed Central

Adherence to treatment is an important issue in all areas of clinical medicine, including dermatology. Consequences of poor compliance include reduced treatment benefits, biased assessments of treatment efficacy, increased healthcare costs, and in some cases even death. To date, even the most effective interventions in patients' habits have not led to large improvements in either adherence or treatment outcome. New objective electronic measures permit unbiased reporting of actual adherence to therapy regimens and have revealed that nonadherence is more pervasive than had been suspected, usually occurring when patients omit or delay a dose. In dermatology, adherence to therapy for dermatomycosis is known to decrease with the duration of treatment and the number of applications required each day, particularly once symptoms have disappeared. Simpler dosing regimens are sought for the treatment of cutaneous fungal infections. Sertaconazole, an imidazole antifungal, has pharmacokinetics that are considered favorable for once-daily antimycotic therapy. It is hypothesized that its prolonged dermal retention may translate into the need for less frequent application for successful treatment in clinical practice. PMID:20967180

2009-01-01

139

Antifungal activity of multifunctional Fe 3O 4-Ag nanocolloids  

NASA Astrophysics Data System (ADS)

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

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

2011-05-01

140

Chloroquine sensitizes biofilms of Candida albicans to antifungal azoles.  

PubMed

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

2013-01-01

141

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

PubMed

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

2011-03-01

142

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. PMID:18596853

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

2008-01-01

143

Cadinene sesquiterpenes from Eupatorium adenophorum and their antifungal activity.  

PubMed

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

2013-01-01

144

IPC synthase as a useful target for antifungal drugs.  

PubMed

Inositol phosphorylceramide (IPC) synthase is a common and essential enzyme in fungi and plants, which catalyzes the transfer of phosphoinositol to the C-1 hydroxy of ceramide to produce IPC. This reaction is a key step in fungal sphingolipid biosynthesis, therefore the enzyme is a potential target for the development of nontoxic therapeutic antifungal agents. Natural products with a desired biological activity, aureobasidin A (AbA), khafrefungin, and galbonolide A, have been reported. AbA, a cyclic depsipeptide containing 8 amino acids and a hydroxyl acid, is a broad spectrum antifungal with strong activity against many pathogenic fungi such as Candida spp., Cryptococcus neoformans, and some Aspergillus spp. Khafrefungin, an aldonic acid ester with a C22 long alkyl chain, has antifungal activity against C. albicans, Cr. Neoformans, and Saccharomyces cerevisiae. Galbonolide A is a 14-membered macrolide with fungicidal activity against clinically important strains, and is especially potent against Cr. neoformans. These classes of natural products are potent and specific antifungal agents. We review current progress in the development of IPC synthase inhibitors with antifungal activities, and present structure-activity relationships (SAR), physicochemical and structural properties, and synthetic methodology for chemical modification. PMID:15578972

Sugimoto, Yuichi; Sakoh, Hiroki; Yamada, Koji

2004-12-01

145

Characterization of antifungal glycoprotein in red-light-irradiated broadbean leaflets  

Microsoft Academic Search

Red-light treatment of broadbean leaflets resulted in the production of antifungal substance(s) against Botrytis cinerea. The antifungal substance(s) was positively charged, as the antifungal constituent was removed by the cation exchanger CM\\u000a cellulose. Treatment of infection droplets with glycosidases (?-mannosidase, ?-galactosidase, ?-glucosidase), glycol-specific\\u000a reagent periodate (NaIO4), and proteinase K completely eliminated antifungal activity, suggesting that both protein and carbohydrate are

Sayed Zahirul Islam; Yuichi Honda; Yoshihiro Sawa; Mohammad Babadoost

2002-01-01

146

Reversal of antifungal resistance mediated by ABC efflux pumps from Candida albicans functionally expressed in yeast  

Microsoft Academic Search

The enhanced efflux of antifungal drugs through ATP-binding cassette (ABC) transporters constitutes a major cause of clinical multidrug resistance (MDR). The inhibition of drug efflux pumps by specific compounds is considered to be a feasible strategy to overcome clinical antifungal resistance. Therefore, several blockers of mammalian and yeast ABC drug pumps, including FK506, propafenones, as well as the antifungal drug

Manuela Schuetzer-Muehlbauer; Birgit Willinger; Ralf Egner; Gerhard Ecker; Karl Kuchler

2003-01-01

147

Antifungal effect of TONS504-photodynamic therapy on Malassezia furfur.  

PubMed

Numerous reports indicate therapeutic efficacy of photodynamic therapy (PDT) against skin tumors, acne and for skin rejuvenation. However, few reports exist regarding its efficacy for fungal skin diseases. In order to determine the antifungal effect, PDT was applied on Malassezia furfur. M. furfur was cultured in the presence of a novel cationic photosensitizer, TONS504, and was irradiated with a 670-nm diode laser. TONS504-PDT showed a significant antifungal effect against M. furfur. The effect was irradiation dose- and TONS504 concentration-dependent and the maximal effect was observed at 100 J/cm(2) and 1 ?g/mL, respectively. In conclusion, TONS504-PDT showed antifungal effect against M. furfur in vitro, and may be a new therapeutic modality for M. furfur-related skin disorders. PMID:25226792

Takahashi, Hidetoshi; Nakajima, Susumu; Sakata, Isao; Iizuka, Hajime

2014-10-01

148

In vitro activity of ME1401, a new antifungal agent.  

PubMed Central

The in vitro antifungal activity of ME1401, a potential topical antifungal agent, was compared with that of haloprogin, clotrimazole, miconazole, tolnaftate, and ciclopirox olamine by using an agar dilution procedure. ME1401 showed a broad antifungal spectrum and inhibited all of the 428 strains of 52 species of pathogenic yeasts and filamentous fungi tested at concentrations ranging from 0.01 to 12.5 micrograms/ml. In general, the activity of ME1401 was comparable or superior to that of clotrimazole and was greater than that of haloprogin and the other reference drugs under the conditions used. Only tolnaftate was superior to ME1401 in its activity against clinical isolates of Trichophyton rubrum. ME1401 showed no cross-resistance with any of the reference drugs and exhibited potent fungicidal activity. PMID:3800346

Yamaguchi, H; Uchida, K; Hiratani, T; Hara, T; Fukuyasu, H; Kazuno, Y; Inouye, S

1986-01-01

149

Antifungal screening of medicinal plants of British Columbian native peoples.  

PubMed

One hundred methanolic plant extracts were screened for antifungal activity against 9 fungal species. Eighty-one were found to have some antifungal activity and 30 extracts showed activity against 4 or more of the fungi assayed. The extracts with the greatest fungal inhibition were prepared from Alnus rubra catkins, Artemisia ludoviciana aerial parts, Artemisia tridentata aerial parts, Geum macrophyllum roots, Mahonia aquifolium roots and Moneses uniflora aerial parts. In addition to these, extracts prepared from the following plants also exhibited antifungal activity against all 9 fungi: Asarum caudatum whole plant, Balsamorhiza sagittata roots, Empetrum nigrum branches, Fragaria chiloensis leaves, Gilia aggregata aerial parts and roots, Glehnia littoralis roots, Heracleum lanatum roots, Heuchera cylindrica roots and Rhus glabra branches. PMID:7898123

McCutcheon, A R; Ellis, S M; Hancock, R E; Towers, G H

1994-12-01

150

Antimicrobial and antifungal effects of tissue conditioners containing a photocatalyst.  

PubMed

This study examined the antimicrobial/antifungal ability of a tissue conditioner containing a photocatalyst for Escherichia coli, Streptococcus mutans, Staphylococcus aureus and Candida albicans. The photocatalyst was mixed with tissue conditioners powders at concentrations of 0, 10, 15, and 20 wt%. Tissue conditioners powders containing a photocatalyst were mixed with liquid to make test specimens. Test specimens inoculated by each microorganism were irradiated by ultraviolet light for 0-, 2- and 4 hours. The antimicrobial/antifungal effects were evaluated by the CFU technique. The CFU values of each microorganism for tissue conditioners containing a photocatalyst showed significant decrease following UV-irradiation. The improvement in antimicrobial/antifungal effects was concomitant with the increase of the mixing ratio and the irradiation time. Therefore, the results indicated that tissue conditioners containing a photocatalyst might have photocatalytic ability. PMID:21946490

Uchimaru, Masayuki; Sakai, Takako; Moroi, Ryoji; Shiota, Susumu; Shibata, Yukie; Deguchi, Mikito; Sakai, Hidetaka; Yamashita, Yoshihisa; Terada, Yoshihiro

2011-01-01

151

Biological properties of aureobasidin A, a cyclic depsipeptide antifungal antibiotic.  

PubMed

Aureobasidin A (AbA) is a novel cyclic depsipeptide antifungal antibiotic. The antifungal activity of AbA was studied in vitro and in vivo in comparison with clinically effective antifungal agents, amphotericin B and fluconazole. AbA was highly active in vitro against many pathogenic fungi, including Candida albicans, Cryptococcus neoformans, Blastomyces dermatitidis and Histoplasma capsulatum. The activity was superior to amphotericin B in most cases. AbA exhibited fungicidal action toward growing cultures of C. albicans. It was highly tolerated by mice and showed good efficacy in the treatment of murine systemic candidiasis when given orally or subcutaneously. AbA's fungicidal action in mice with candidiasis was more effective than fluconazole and amphotericin B. PMID:8226319

Takesako, K; Kuroda, H; Inoue, T; Haruna, F; Yoshikawa, Y; Kato, I; Uchida, K; Hiratani, T; Yamaguchi, H

1993-09-01

152

Antifungal susceptibility profile of cryptic species of Aspergillus.  

PubMed

The use of molecular tools has led to the description of new cryptic species among different Aspergillus species complexes. Their frequency in the clinical setting has been reported to be between 10 and 15 %. The susceptibility to azoles and amphotericin B of many of these species is low, and some of them, such as Aspergillus calidoustus or Aspergillus lentulus, are considered multi-resistant. The changing epidemiology, the frequency of cryptic species, and the different susceptibility profiles make antifungal susceptibility testing an important tool to identify the optimal antifungal agent to treat the infections caused by these species. PMID:24972670

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

2014-12-01

153

Antifungal activity of three mouth rinses--in vitro study.  

PubMed

Mouthrinses are nowadays routinely included in the home care oral hygiene maintenance besides dentifrice/tooth paste. Mouthrinses prevent bacterial attachment and prevent or slow down bacterial proliferation. Fungal organisms have now gained more importance due to increased incidence of AIDS/HIV. This has necessitated for mouthrinses to possess antifungal activity also. The mouthrinses used were Povidone iodine ( Wokadine), Thymol with Eucalyptol and Benzoic acid (Listerine) and fluoride with Triclosan (Colgate Plax), which were tested against oral isolates of different species of Candida. The agar diffusion test was used to evaluate the inhibitory activity of the mouthrinses and all of them exhibited antifungal activity especially against Candida albicans. PMID:16758789

Abirami, C P; Venugopal, Pankajalakshmi V

2005-01-01

154

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. PMID:20574543

Perfect, John R.

2010-01-01

155

Antifungal and antioxidant activities of the phytomedicine pipsissewa, Chimaphila umbellata  

Microsoft Academic Search

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

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

2008-01-01

156

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. PMID:22964246

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

2012-01-01

157

Atmospheric pressure cold plasma as an antifungal therapy  

SciTech Connect

A microhollow cathode based, direct-current, atmospheric pressure, He/O{sub 2} (2%) cold plasma microjet was used to inactive antifungal resistants Candida albicans, Candida krusei, and Candida glabrata in air and in water. Effective inactivation (>90%) was achieved in 10 min in air and 1 min in water. Antifungal susceptibility tests showed drastic reduction of the minimum inhibitory concentration after plasma treatment. The inactivation was attributed to the reactive oxygen species generated in plasma or in water. Hydroxyl and singlet molecular oxygen radicals were detected in plasma-water system by electron spin resonance spectroscopy. This approach proposed a promising clinical dermatology therapy.

Sun Peng; Wu Haiyan [College of Engineering, Peking University, Beijing 100871 (China); Sun Yi; Liu Wei; Li Ruoyu [Department of Dermatology and Venereology, Peking Univ. 1st Hospital and Research Center for Medical Mycology, Peking Univ., Beijing 100034 (China); Zhu Weidong; Lopez, Jose L. [Department of Applied Science and Technology and Center for Microplasma Science and Technology, Saint Peter's College, Jersey City, New Jersey 07306 (United States); Zhang Jue; Fang Jing [College of Engineering, Peking University, Beijing 100871 (China); Academy for Advanced Interdisciplinary Studies, Peking University, Beijing 100871 (China)

2011-01-10

158

Combination Antifungal Therapy for Cryptococcal Meningitis  

PubMed Central

BACKGROUND Combination antifungal therapy (amphotericin B deoxycholate and flucytosine) is the recommended treatment for cryptococcal meningitis but has not been shown to reduce mortality, as compared with amphotericin B alone. We performed a randomized, controlled trial to determine whether combining flucytosine or high-dose fluconazole with high-dose amphotericin B improved survival at 14 and 70 days. METHODS We conducted a randomized, three-group, open-label trial of induction therapy for cryptococcal meningitis in patients with human immunodeficiency virus infection. All patients received amphotericin B at a dose of 1 mg per kilogram of body weight per day; patients in group 1 were treated for 4 weeks, and those in groups 2 and 3 for 2 weeks. Patients in group 2 concurrently received flucytosine at a dose of 100 mg per kilogram per day for 2 weeks, and those in group 3 concurrently received fluconazole at a dose of 400 mg twice daily for 2 weeks. RESULTS A total of 299 patients were enrolled. Fewer deaths occurred by days 14 and 70 among patients receiving amphotericin B and flucytosine than among those receiving amphotericin B alone (15 vs. 25 deaths by day 14; hazard ratio, 0.57; 95% confidence interval [CI], 0.30 to 1.08; unadjusted P = 0.08; and 30 vs. 44 deaths by day 70; hazard ratio, 0.61; 95% CI, 0.39 to 0.97; unadjusted P = 0.04). Combination therapy with fluconazole had no significant effect on survival, as compared with monotherapy (hazard ratio for death by 14 days, 0.78; 95% CI, 0.44 to 1.41; P = 0.42; hazard ratio for death by 70 days, 0.71; 95% CI, 0.45 to 1.11; P = 0.13). amphotericin B plus flucytosine was associated with significantly increased rates of yeast clearance from cerebrospinal fluid (?0.42 log10 colony-forming units [CFU] per milliliter per day vs. ?0.31 and ?0.32 log10 CFU per milliliter per day in groups 1 and 3, respectively; P<0.001 for both comparisons). Rates of adverse events were similar in all groups, although neutropenia was more frequent in patients receiving a combination therapy. CONCLUSIONS Amphotericin B plus flucytosine, as compared with amphotericin B alone, is associated with improved survival among patients with cryptococcal meningitis. A survival benefit of amphotericin B plus fluconazole was not found. (Funded by the Wellcome Trust and the British Infection Society; Controlled-Trials.com number, ISRCTN95123928.) PMID:23550668

Day, Jeremy N.; Chau, Tran T.H.; Wolbers, Marcel; Mai, Pham P.; Dung, Nguyen T.; Mai, Nguyen H.; Phu, Nguyen H.; Nghia, Ho D.; Phong, Nguyen D.; Thai, Cao Q.; Thai, Le H.; Chuong, Ly V.; Sinh, Dinh X.; Duong, Van A.; Hoang, Thu N.; Diep, Pham T.; Campbell, James I.; Sieu, Tran P.M.; Baker, Stephen G.; Chau, Nguyen V.V.; Hien, Tran T.

2014-01-01

159

Antifungal activity in seed coat extracts of woodland plants  

Microsoft Academic Search

Aqueous extracts from seeds of four woodland ground flora species (Hyacinthoides non-scripta, Allium ursinum, Digitalis purpurea and Hypericum pulchrum) were tested for antifungal activity using a petriplate technique. Four species of fungi were investigated. The growth of three of these (Trichoderma viride, Rhizoctonia solani and Pythium sp.) was not affected by any of the seed coat extracts. The growth of

Susan J. Warr; Ken Thompson; Martin Kent

1992-01-01

160

Multiple resistance mechanisms to azole antifungals in yeast clinical isolates  

Microsoft Academic Search

The use of antifungal agents, especially the azole class, has increased in parallel with a higher incidence of fungal infections, particularly in immunocompromised patients. This situation has favored the appearance of Candida species, prominent among them C. albicans and C. globrata, with acquired resistance to these agents. This review focuses on the latest developments in investigations of molecular mechanisms contributing

Dominique Sanglard; Françoise Ischer; David Calabrese; Michelle de Micheli; Jacques Bille

1998-01-01

161

Melanization and morphological effects on antifungal susceptibility of Penicillium marneffei.  

PubMed

The biosynthesis of melanin has been linked with virulence in diverse pathogenic fungi. Penicillium marneffei, a dimorphic fungus, is capable of melanization in both mycelial and yeast phases, and the pigment may be produced during infection to protect the fungus from the host immune system. To investigate the impact of yeast morphological transformation on antifungal susceptibility, P. marneffei was cultured on various media including minimal medium, 1 % tryptone, brain heart infusion broth, and malt extract broth by using the standardized susceptibility protocol (the M27-A protocol, RPMI medium) for yeasts. We also investigated whether P. marneffei melanization affected its susceptibility to antifungal drugs by adding L-DOPA into culture broths. There were no differences in the minimum inhibitory concentrations of P. marneffei yeast cells previously grown in various culture broths with or without L-DOPA using the M27A protocol (into which no melanin substrate can be added due to a rapid colour change of the RPMI medium to black) for testing amphotericin B, clotrimazole, fluconazole, itraconazole and ketoconazole. However, both melanized and non-melanized P. marneffei displayed increased resistance to antifungal drugs when L-DOPA was added into a selected assay medium, 0.17 % yeast nitrogen base, 2 % glucose, and 1.5 % agar. Hence, active melanin formation appears to protect P. marneffei by enhancing its resistance to antifungal drugs. PMID:25227777

Kaewmalakul, Jutikul; Nosanchuk, Joshua D; Vanittanakom, Nongnuch; Youngchim, Sirida

2014-11-01

162

Human Pharmacogenomic Variations and Their Implications for Antifungal Efficacy  

PubMed Central

Pharmacogenomics is defined as the study of the impacts of heritable traits on pharmacology and toxicology. Candidate genes with potential pharmacogenomic importance include drug transporters involved in absorption and excretion, phase I enzymes (e.g., cytochrome P450-dependent mixed-function oxidases) and phase II enzymes (e.g., glucuronosyltransferases) contributing to metabolism, and those molecules (e.g., albumin, A1-acid glycoprotein, and lipoproteins) involved in the distribution of antifungal compounds. By using the tools of population genetics to define interindividual differences in drug absorption, distribution, metabolism, and excretion, pharmacogenomic models for genetic variations in antifungal pharmacokinetics can be derived. Pharmacogenomic factors may become especially important in the treatment of immunocompromised patients or those with persistent or refractory mycoses that cannot be explained by elevated MICs and where rational dosage optimization of the antifungal agent may be particularly critical. Pharmacogenomics has the potential to shift the paradigm of therapy and to improve the selection of antifungal compounds and adjustment of dosage based upon individual variations in drug absorption, metabolism, and excretion. PMID:17041143

Meletiadis, Joseph; Chanock, Stephen; Walsh, Thomas J.

2006-01-01

163

Using Aspergillus nidulans to identify antifungal drug resistance mutations.  

PubMed

Systemic fungal infections contribute to at least 10% of deaths in hospital settings. Most antifungal drugs target ergosterol (polyenes) or its biosynthetic pathway (azoles and allylamines), or beta-glucan synthesis (echinocandins). Antifungal drugs that target proteins are prone to the emergence of resistant strains. Identification of genes whose mutations lead to targeted resistance can provide new information on those pathways. We used Aspergillus nidulans as a model system to exploit its tractable sexual cycle and calcofluor white as a model antifungal agent to cross-reference our results with other studies. Within 2 weeks from inoculation on sublethal doses of calcofluor white, we isolated 24 A. nidulans adaptive strains from sectoring colonies. Meiotic analysis showed that these strains had single-gene mutations. In each case, the resistance was specific to calcofluor white, since there was no cross-resistance to caspofungin (echinocandin). Mutation sites were identified in two mutants by next-generation sequencing. These were confirmed by reengineering the mutation in a wild-type strain using a gene replacement strategy. One of these mutated genes was related to cell wall synthesis, and the other one was related to drug metabolism. Our strategy has wide application for many fungal species, for antifungal compounds used in agriculture as well as health care, and potentially during protracted drug therapy once drug resistance arises. We suggest that our strategy will be useful for keeping ahead in the drug resistance arms race. PMID:24363365

He, Xiaoxiao; Li, Shengnan; Kaminskyj, Susan G W

2014-02-01

164

New antifungal agents for the treatment of candidaemia  

Microsoft Academic Search

Suspected or proven invasive candidiasis is an important indication for antifungal drugs and a leading cause of death. Prompt initiation of effective therapy has a marked effect on survival, but the indiscriminate application of different risk-factor-based prediction models is massively increasing the number of patients treated unnecessarily. Fluconazole resistance levels are

Patricia Muñoz; Jesus Guinea; Loreto Rojas; Emilio Bouza

2010-01-01

165

Antifungal Properties of Haem Peroxidase from Acorus calamus  

Microsoft Academic Search

Background and Aims Plants have evolved a number of inducible defence mechanisms against pathogen attack, including synthesis of pathogenesis-related proteins. The aim of the study was to purify and characterize antifungal protein from leaves of Acorus calamus. Methods Leaf proteins from A. calamus were fractionated by cation exchange chromatography and gel filtration and the fraction inhibiting the hyphal extension of

MODHUMITA GHOSH

2006-01-01

166

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

2008-01-01

167

Antifungal properties of Singapore gorgonians: a preliminary study  

Microsoft Academic Search

Gorgonians possess a huge array of secondary metabolites for various functions, many of which are not known. One of these functions is antifungal. This study investigates if gorgonians from reefs in Singapore can defend themselves against the settlement and invasion of fungi. Crude extracts from 10 species of gorgonians from three families, Ellisellidae, Subergorgiidae and Plexauridae, were screened against nine

L. L. Koh; T. K. Tan; L. M. Chou; N. K. C. Goh

2002-01-01

168

Echinocandins: A ray of hope in antifungal drug therapy.  

PubMed

Invasive fungal infections are on the rise. Amphotericin B and azole antifungals have been the mainstay of antifungal therapy so far. The high incidence of infusion related toxicity and nephrotoxicity with amphotericin B and the emergence of fluconazole resistant strains of Candida glabrata egged on the search for alternatives. Echinocandins are a new class of antifungal drugs that act by inhibition of beta (1, 3)-D- glucan synthase, a key enzyme necessary for integrity of the fungal cell wall.Caspofungin was the first drug in this class to be approved. It is indicated for esophageal candidiasis, candidemia, invasive candidiasis, empirical therapy in febrile neutropenia and invasive aspergillosis. Response rates are comparable to those of amphotericin B and fluconazole. Micafungin is presently approved for esophageal candidiasis, for prophylaxis of candida infections in patients undergoing hematopoietic stem cell transplant (HSCT) and in disseminated candidiasis and candidemia. The currently approved indications for anidulafungin are esophageal candidiasis, candidemia and invasive candidiasis.The incidence of infusion related adverse effects and nephrotoxicity is much lower than with amphotericin B. The main adverse effect is hepatotoxicity and derangement of serum transaminases. Liver function may need to be monitored. They are, however, safer in renal impairment. Even though a better pharmacoeconomical choice than amphotericin B, the higher cost of these drugs in comparison to azole antifungals is likely to limit their use to azole resistant cases of candidial infections and as salvage therapy in invasive aspergillosis rather than as first line drugs. PMID:20606829

Grover, Neeta D

2010-02-01

169

Antifungal effects of citronella oil against Aspergillus niger ATCC 16404.  

PubMed

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

2013-08-01

170

Antifungal Textiles Formed Using Silver Deposition in Supercritical Carbon Dioxide  

NASA Astrophysics Data System (ADS)

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 fungal growth. Cotton fabric samples modified with Ag(hepta) and Ag(cod)(hfac) exhibited measurable zones of inhibition. On the other hand, the uncoated fabric had no zone of inhibition. Possible applications of antifungal textiles prepared using scCO2 processing include use in hospital uniforms and wound dressings.

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

2010-04-01

171

Pharmacognostic and antifungal investigations of Elaeocarpus ganitrus (Rudrakasha).  

PubMed

Rudrakasha is the dried bead obtained from the ripe fruit of Elaeocarpus ganitrus Roxb. (Family: Elaeocarpaceae). Microscopic studies revealed the presence of a hard endocarp with lignified isodiametric sclereids, seeds with membranous seed coat, which enclosed a dense cellular endosperm comprising of calcium oxalate druses. Physicochemical parameters showed that total ash was 1.36 times and 1.56 times more than the acid insoluble ash and water-soluble ash, respectively. Further, ethanol had a maximum extractable value of 2.4% and moisture content was found to be 9.7%. Different extracts, petroleum ether, chloroform, ethanol and water were prepared. Chemically the extracts showed the presence of phytosterols, fats, alkaloids, flavonoids, carbohydrates, proteins and tannins. The extracts were evaluated for antifungal activity on different fungal strains. Chlorofom and ethanol extracts have high antifungal activity against Candida albicans. Whereas, chloroform, ethanol and water extracts showed moderate inhibition against Aspergillus niger. PMID:20838538

Singh, B; Chopra, A; Ishar, M P S; Sharma, A; Raj, T

2010-03-01

172

Pharmacognostic and antifungal investigations of Elaeocarpus ganitrus (Rudrakasha)  

PubMed Central

Rudrakasha is the dried bead obtained from the ripe fruit of Elaeocarpus ganitrus Roxb. (Family: Elaeocarpaceae). Microscopic studies revealed the presence of a hard endocarp with lignified isodiametric sclereids, seeds with membranous seed coat, which enclosed a dense cellular endosperm comprising of calcium oxalate druses. Physicochemical parameters showed that total ash was 1.36 times and 1.56 times more than the acid insoluble ash and water-soluble ash, respectively. Further, ethanol had a maximum extractable value of 2.4% and moisture content was found to be 9.7%. Different extracts, petroleum ether, chloroform, ethanol and water were prepared. Chemically the extracts showed the presence of phytosterols, fats, alkaloids, flavonoids, carbohydrates, proteins and tannins. The extracts were evaluated for antifungal activity on different fungal strains. Chlorofom and ethanol extracts have high antifungal activity against Candida albicans. Whereas, chloroform, ethanol and water extracts showed moderate inhibition against Aspergillus niger. PMID:20838538

Singh, B.; Chopra, A.; Ishar, M.P.S.; Sharma, A.; Raj, T.

2010-01-01

173

Isolation, structures, and antifungal activities of new aureobasidins.  

PubMed

Aureobasidins are a group of cyclic depsipeptides with antifungal activity and are produced by Aureobasidium pullulans. Aureobasidins are composed of eight amino acids and one hydroxy acid such as 2-hydroxy-3-methylpentanoic acid (Hmp), and highly lipophilic. Five new aureobasidins, S1, S2a, S2b, S3 and S4, which have higher hydrophilicity in reversed phase HPLC than the known aureobasidins A-R, were discovered in a fermentation broth of A. pullulans R106 by means of on-line liquid chromatography/mass spectrometry with electrospray ionization. We identified the structures of the compounds and studied their antifungal activities. Three of the new aureobasidins, S2b, S3 and S4, which have hydroxylated Hmp as the hydroxy acid, were highly active against Candida spp. and Cryptococcus neoformans. PMID:8226313

Yoshikawa, Y; Ikai, K; Umeda, Y; Ogawa, A; Takesako, K; Kato, I; Naganawa, H

1993-09-01

174

Antifungal cyclic peptides from the marine sponge Microscleroderma herdmani  

PubMed Central

Screening natural product extracts from the National Cancer Institute Open Repository for antifungal discovery afforded hits for bioassay-guided fractionation. Using LC–MS analysis to generate chemical structure information on potentially active compounds, two new cyclic hexapeptides, microsclerodermins J (1) and K (2), were isolated from the deep-water sponge Microscleroderma herdmani, along with microsclerodermins A (3) and B (4), previously isolated from an unidentified Microscleroderma species. The structures of the new compounds were elucidated by spectroscopic analysis and chemical methods. In vitro antifungal testing showed that the four compounds possessed strong activities against the opportunistic fungal pathogens Candida albicans, Candida glabrata, Candida krusei, Cryptococcus neoformans, and Aspergillus fumigatus. PMID:23936761

Zhang, Xiaohui; Jacob, Melissa R; Rao, R Ranga; Wang, Yan-Hong; Agarwal, Ameeta K; Newman, David J; Khan, Ikhlas A; Clark, Alice M; Li, Xing-Cong

2013-01-01

175

Transcriptional Analyses of Antifungal Drug Resistance in Candida albicans  

Microsoft Academic Search

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:

CHRIS N. LYONS; THEODORE C. WHITE

2000-01-01

176

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

2002-01-01

177

Efficacy of some natural compounds as antifungal agents  

PubMed Central

Natural sources have been important for the development of new active molecules for many years. Various small molecules with unique chemical skeleton and potent bioactivities were discovered through various sources like plants, marine products, and microorganisms, etc., which are considered as very important part of the nature. A number of potent antifungals have been originated from various natural sources. This account describes structure and activities of selected agents isolated from various natural sources. PMID:23055634

Vengurlekar, Sudha; Sharma, Rajesh; Trivedi, Piyush

2012-01-01

178

Current evidence of antifungal prophylaxis and therapy in pediatric patients  

PubMed Central

Invasive fungal infections (IFI) are an important complication in pediatric haematological and oncological patients who undergo intensive chemotherapy for leukemia, solid tumour at advanced stage or relapsed, and hematopoietic stem cell transplantation. The incidence of IFI is lower than bacterial infection but mortality rate remains high. This review is designed to help paediatric oncologists in choosing the appropriate anti-fungal strategy and agents for prophylaxis, empirical, pre-emptive and specific therapy on the basis of published evidence. PMID:21647279

Giacchino, Mareva; Milano, Giuseppe Maria; Carraro, Francesca; Bezzio, Stefania; Pegoraro, Anna; Aversa, Franco; Cesaro, Simone

2011-01-01

179

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. PMID:23869317

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

2013-01-01

180

Antifungal agents and therapy for infants and children with invasive fungal infections: a pharmacological perspective  

PubMed Central

Invasive fungal infections, although relatively rare, are life-threatening diseases in premature infants and immunocompromised children. While many advances have been made in antifungal therapeutics in the last two decades, knowledge of the pharmacokinetics and pharmacodynamics of antifungal agents for infants and children remains incomplete. This review summarizes the pharmacology and clinical utility of currently available antifungal agents and discusses the opportunities and challenges for future research. PMID:23126319

Lestner, Jodi M; Smith, P Brian; Cohen-Wolkowiez, Michael; Benjamin, Daniel K; Hope, William W

2013-01-01

181

The Mediterranean red alga Asparagopsis taxiformis has antifungal activity against Aspergillus species.  

PubMed

The red algae Asparagopsis taxiformis collected from the Straits of Messina (Italy) were screened for antifungal activity against Aspergillus species. EUCAST methodology was applied and extracts showed antifungal activity against A. fumigatus, A. terreus and A. flavus. The lowest minimum inhibitory concentrations observed were <0.15 mg ml(-1) and the highest were >5 mg ml(-1) for Aspergillus spp. tested. Agar diffusion assays confirmed antifungal activity of A. taxiformis extracts in Aspergillus species. PMID:23437896

Genovese, Giuseppa; Leitner, Sandra; Minicante, Simona A; Lass-Flörl, Cornelia

2013-09-01

182

Benzofurazan derivatives as antifungal agents against phytopathogenic fungi.  

PubMed

A series of benzofurazan derivatives were prepared and evaluated for their biological activities against four important phytopathogenic fungi, namely, Rhizoctonia solani, Sclerotinia sclerotiorum, Fusarium graminearum and Phytophthora capsici, using the mycelium growth inhibition method. The structures of these compounds were characterized by (1)H NMR, (13)C NMR, and HRMS. N-(3-chloro-4-fluorophenyl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine (A3) displayed the maximum antifungal activity against R. solani (IC50 = 1.91 ?g/mL), which is close to that of the positive control Carbendazim (IC50 = 1.42 ?g/mL). For other benzofurazan derivatives with nitro group at R(4) position (A series), 9 out of 30 compounds exhibited high antifungal effect against strain R. solani, with IC50 values less than 5 ?g/mL. Most of the derivatives with substituents at R(2) and R(3) positions (B series) displayed moderate growth inhibition against S. sclerotiorum (IC50 < 25 ?g/mL). Also, several benzofuran derivatives with nitro group at R(4) position and another conjugated aromatic ring at the R(1) position of the phenyl ring displayed high antifungal capability against strain R. solani. Compounds with substituents at R(2) and R(3) position had moderate efficacy against strain S. sclerotiorum. PMID:24813881

Wang, Lili; Zhang, Ying-Ying; Wang, Lei; Liu, Feng-you; Cao, Ling-Ling; Yang, Jing; Qiao, Chunhua; Ye, Yonghao

2014-06-10

183

Mechanisms of antifungal drug resistance in Candida dubliniensis.  

PubMed

Candida dubliniensis was first described in 1995 and is the most closely related species to the predominant human fungal pathogen Candida albicans. C. dubliniensis is significantly less prevalent and less pathogenic than C. albicans and is primarily associated with infections in HIV-infected individuals and other immunocompromised cohorts. The population structure of C. dubliniensis consists of three well-defined major clades and is significantly less diverse than C. albicans. The majority of C. dubliniensis isolates are susceptible to antifungal drugs commonly used to treat Candida infections. To date only two major patterns of antifungal drug resistance have been identified and the molecular mechanisms of these are very similar to the resistance mechanisms that have been described previously in C. albicans. However, significant differences are evident in the predominant antifungal drug mechanisms employed by C. dubliniensis, differences that reflect its more clonal nature, its lower prevalence and characteristics of its genome, the complete sequence of which has only recently been determined. PMID:20521937

Coleman, David C; Moran, Gary P; McManus, Brenda A; Sullivan, Derek J

2010-06-01

184

Antifungal activity of topical microemulsion containing a thiophene derivative.  

PubMed

Fungal infections have become a major problem of worldwide concern. Yeasts belonging to the Candida genus and the pathogenic fungus Cryptococcus neoformans are responsible for different clinical manifestations, especially in immunocompromised patients. Antifungal therapies are currently based on a few chemotherapeutic agents that have problems related to effectiveness and resistance profiles. Microemulsions are isotropic, thermodynamically stable transparent systems of oil, water and surfactant that can improve the solubilization of lipophilic drugs. Taking into account the need for more effective and less toxic drugs along with the potential of thiophene derivatives as inhibitors of pathogenic fungi growth, this study aimed to evaluate the antifungal activity of a thiophene derivative (5CN05) embedded in a microemulsion (ME). The minimum inhibitory concentration (MIC) was determined using the microdilution method using amphotericin B as a control. The formulations tested (ME- blank and ME-5CN05) showed physico-chemical properties that would allow their use by the topical route. 5CN05 as such exhibited moderate or weak antifungal activity against Candida species (MIC = 270-540 ?g . mL(-1)) and good activity against C. neoformans (MIC = 17 ?g . mL(-1)). Candida species were susceptible to ME-5CN05 (70-140 ?g . mL(-1)), but C. neoformans was much more, presenting a MIC value of 2.2 ?g . mL(-1). The results of this work proved promising for the pharmaceutical industry, because they suggest an alternative therapy against C. neoformans. PMID:25242940

Guimarães, Geovani Pereira; de Freitas Araújo Reis, Mysrayn Yargo; da Silva, Dayanne Tomaz Casimiro; Junior, Francisco Jaime Bezerra Mendonça; Converti, Attílio; Pessoa, Adalberto; de Lima Damasceno, Bolívar Ponciano Goulart; da Silva, José Alexsandro

2014-01-01

185

Cytocompatible antifungal acrylic resin containing silver nanoparticles for dentures  

PubMed Central

Background Inhibition of Candida albicans on denture resins could play a significant role in preventing the development of denture stomatitis. The safety of a new dental material with antifungal properties was analyzed in this work. Methods Poly(methyl methacrylate) [PMMA] discs and PMMA-silver nanoparticle discs were formulated, with the commercial acrylic resin, Nature-CrylTM, used as a control. Silver nanoparticles were synthesized and characterized by ultraviolet-visible spectroscopy, dispersive Raman spectroscopy, and transmission electron microscopy. The antifungal effect was assessed using a luminescent microbial cell viability assay. Biocompatibility tests were carried out using NIH-3T3 mouse embryonic fibroblasts and a Jurkat human lymphocyte cell line. Cells were cultured for 24 or 72 hours in the presence or absence of the polymer formulations and analyzed using three different tests, ie, cellular viability by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and cell proliferation by enzyme-linked immunosorbent assay BrdU, and genomic DNA damage (Comet assay). Finally, the samples were evaluated mechanically, and the polymer-bearing silver nanoparticles were analyzed microscopically to evaluate dispersion of the nanoparticles. Results The results show that PMMA-silver nanoparticle discs significantly reduce adherence of C. albicans and do not affect metabolism or proliferation. They also appear not to cause genotoxic damage to cells. Conclusion The present work has developed a new biocompatible antifungal PMMA denture base material. PMID:22969297

Acosta-Torres, Laura Susana; Mendieta, Irasema; Nunez-Anita, Rosa Elvira; Cajero-Juarez, Marcos; Castano, Victor M

2012-01-01

186

Antifungal activity of topical microemulsion containing a thiophene derivative  

PubMed Central

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

Guimaraes, Geovani Pereira; de Freitas Araujo Reis, Mysrayn Yargo; da Silva, Dayanne Tomaz Casimiro; Junior, Francisco Jaime Bezerra Mendonca; Converti, Attilio; Pessoa, Adalberto; de Lima Damasceno, Bolivar Ponciano Goulart; da Silva, Jose Alexsandro

2014-01-01

187

Antifungal susceptibilities of dermatophytic agents isolated from clinical specimens.  

PubMed

The aim of this study was to investigate the susceptibility to four antifungal agents: ketoconazole, terbinafine, itraconazole and fluconazole, of the different species of dermatophyte strains isolated from clinical specimens. A total of 128 specimens were collected from toe nail, foot, inguinal region, trunk, hands and head. The dermatophytes tested included Trichophyton rubrum 108 (84.4%), Trichophyton mentagrophytes 11 (8.6%), Epidermophyton floccosum 5 (3.9%), Microsporum canis 2 (1.5%) and Trichophyton tonsurans 2 (1.5%). The mean minimum inhibitory concentrations (MIC) for the five species of dermatophytes ranged between 0.09-1.12 microg/mL for ketoconazole, 0.04-0.27 microg/mL for terbinafine, 0.08-0.43 microg/mL for itraconazole and 16.18-24.0 microg/mL for fluconazole. In vitro analysis of antifungal activity of these agents would also allow for the comparison between different systemic antifungals, which in turn may clarify the reasons for the lack of clinical response or serve as an effective therapy for patients with chronic infection. PMID:16048753

Cetinkaya, Zafer; Kiraz, Nuri; Karaca, Semsettin; Kulac, Mustafa; Ciftci, Ihsan H; Aktepe, Orhan C; Altindis, Mustafa; Kiyildi, Nilay; Piyade, Meltem

2005-01-01

188

[Chemical constituents of Hyptis rhomboidea and their antifungal activity].  

PubMed

The present work is to investigate the chemical constitutions of Hyptis rhomboidea and their antifungal activities. The compounds were isolated by Toyopearl HW-40, Sephadex LH-20, MCI-Gel CHP-20, RP-18, PTLC and silica column chromatographic methods and subjected to evaluate some monomers antifungal activity of eight kinds of plant pathogenic bacteria. Eleven compounds were isolated and identified as ethyl caffeate (1), ursolic acid (2), oleanolic acid (3), vanillactic acid (4), methyl rosmarinate (5), kaempferol 3-O-alpha-L-rhamnopyranosyl-(1 --> 6) -beta-D-glucopyranoside (6), kaempferol 3-O-alpha-L-rhamnopyranosyl-(1 --> 6)-beta-D-glucopyranoside (7), ilexgenin A (8), beta-amyrin (9), kaempferol 3-O-beta-D-glucopyranoside (astrgalin, 10) and cholest-5-ene-3beta, 4beta-diol (11). Compound 1 showed the strongest inhibitory effect on Sclerotinia sclerotiorum with the MIC 16.2 mg x L(-1), and compound 5 showed the strongest inhibitory effect on S. minor and Exserohilum turcicum with MIC 16.2, 8.1 mg x L(-1), respectively. All compounds were isolated from the H. rhomboidea for the first time, and compounds 1 and 5 showed antifungal activity. PMID:25244760

Tang, Lu; Li, Xi-Feng; Yang, Sheng-Xiang; Qiu, Yan; Yuan, Ke

2014-06-01

189

Antibacterial and antifungal effects of essential oils from coniferous trees.  

PubMed

Essential oils have potential biological effects, i.e., antibiotic, anticarcinogenic, and sedative effects during stress. In the present study, we investigated the antibacterial and antifungal effects of essential oils extracted from the coniferous species Pinus densiflora, Pinus koraiensis, and Chamaecyparis obtusa, because their biological activities have not been yet elucidated. The essential oils were quantified using gas chromatography and identified in gas chromatography-mass spectrometric analysis. Simultaneously, antibacterial and antifungal assays were performed using the essential oils distilled from the needles of coniferous trees. The major components and the percentage of each essential oil were: 19.33% beta-thujene in P. densiflora; 10.49% alpha-pinene in P. koraiensis; 10.88% bornyl acetate in C. obtusa. The essential oils from P. densiflora and C. obtusa have antibacterial effects, whereas essential oils from P. koraiensis and C. obtusa have antifungal effects. These results indicate that the essential oils from the three coniferous trees, which have mild antimicrobial properties, can inhibit the growth of gram-positive and gram-negative bacteria and fungi. PMID:15187434

Hong, Eui-Ju; Na, Ki-Jeung; Choi, In-Gyu; Choi, Kyung-Chul; Jeung, Eui-Bae

2004-06-01

190

Antifungal activities and chemical composition of some medicinal plants.  

PubMed

The use of and search for drugs and dietary supplements derived from plants have accelerated in recent years. Ethnopharmacologists, botanists, microbiologists and natural-products scientists are combing the earth for phytochemicals and leads, which could be developed for treatment of infectious diseases. The aim of this study was to investigate the antifungal activities of the essential oils of some medicinal plants such as Stachys pubescens, Thymus kotschyanus, Thymus daenensis and Bupleurum falcatum against Fusarium oxysporum, Aspergillus flavus and Alternaria alternata. The essential oils were used to evaluate their MICs and MFCs compared to the amphotricin B as a standard drug. The essential oils were also analyzed by GC/MS. Essential oils isolated from the S. pubescens, T. kotschyanus and B. falcatum showed strong antifungal activities. The essential oil of T. daenensis exhibited a moderate activity against the selected fungi in comparison with the other plants' essential oils. In addition, the results showed that 26, 23, 22 and 15 components were identified from the essential oils of T. kotschyanus, S. pubescens, T. daenensis and B. falcatum, respectively. These oils exhibited a noticeable antifungal activity against the selected fungi. Regarding obtained results and that natural antimicrobial substances are inexpensive and have fewer side effects, they convey potential for implementation in fungal pathogenic systems. PMID:24768063

Mohammadi, A; Nazari, H; Imani, S; Amrollahi, H

2014-06-01

191

Antifungal defensins and their role in plant defense  

PubMed Central

Since the beginning of the 90s lots of cationic plant, cysteine-rich antimicrobial peptides (AMP) have been studied. However, Broekaert et al. (1995) only coined the term “plant defensin,” after comparison of a new class of plant antifungal peptides with known insect defensins. From there, many plant defensins have been reported and studies on this class of peptides encompass its activity toward microorganisms and molecular features of the mechanism of action against bacteria and fungi. Plant defensins also have been tested as biotechnological tools to improve crop production through fungi resistance generation in organisms genetically modified (OGM). Its low effective concentration towards fungi, ranging from 0.1 to 10 ?M and its safety to mammals and birds makes them a better choice, in place of chemicals, to control fungi infection on crop fields. Herein, is a review of the history of plant defensins since their discovery at the beginning of 90s, following the advances on its structure conformation and mechanism of action towards microorganisms is reported. This review also points out some important topics, including: (i) the most studied plant defensins and their fungal targets; (ii) the molecular features of plant defensins and their relation with antifungal activity; (iii) the possibility of using plant defensin(s) genes to generate fungi resistant GM crops and biofungicides; and (iv) a brief discussion about the absence of products in the market containing plant antifungal defensins. PMID:24765086

Lacerda, Ariane F.; Vasconcelos, Erico A. R.; Pelegrini, Patricia Barbosa; Grossi de Sa, Maria F.

2014-01-01

192

Combination antifungal therapy against Candida species: the new frontier--are we there yet?  

PubMed

In the past decade, we have seen a significant increase in the incidence of invasive fungal infections. In addition, opportunistic fungal infections resistant to antifungal agents have become increasingly common and their frequency will more than likely continue to increase. The antifungal armamentarium for the treatment of serious fungal infections remains limited. A possible approach to overcoming antifungal drug resistance and high mortality rates seen in severe fungal infections is to combine two or three classes of antifungals, especially if the drugs have different mechanisms of action. The unique properties of newer antifungals now provide us with the opportunity to investigate antifungal combinations that may become the standard of care for serious fungal infections. Combinations of new agents along with more traditional antifungals have now been shown to possess some synergistic or at least additive activity against Candida in clinical trials. On the other hand, caution is still needed since other antifungal combinations have demonstrated antagonistic activity in vitro. Well-controlled clinical trials are needed to define the most efficacious antifungal regimen. Furthermore, these trials should also evaluate the side effect potential of combination regimens and the pharmacoeconomic impact these regimens may have. Thus, while much optimism exists for combination therapy, there is much yet to be done. PMID:14653512

Vazquez, J A

2003-10-01

193

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

PubMed

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

2012-10-01

194

The role of primary antifungal prophylaxis in patients with haematological malignancies.  

PubMed

Invasive fungal infections (IFIs) represent important complications in patients with haematological malignancies. Chemoprevention of IFIs may play an important role in this setting, but in the past decades the majority of antifungal drugs utilized demonstrated poor efficacy, particularly in the prevention of invasive aspergillosis. The new triazoles are very useful antifungal drugs, more suitable for prophylaxis of IFIs than amphotericin B and echinocandins. In this review, the main clinical data about antifungal prophylaxis with fluconazole, itraconazole, voriconazole and posaconazole are analysed. At present, posaconazole appears to be the most efficacious azole in antifungal prophylaxis, particularly in patients with acute myeloid leukaemia. PMID:24372659

Pagano, L; Caira, M

2014-06-01

195

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

1985-01-01

196

Direct Interaction of Antifungal Azole-Derivatives with Calmodulin: A Possible Mechanism for Their Therapeutic Activity  

Microsoft Academic Search

Azole derivatives, such as ketoconazole and bifonazole, are well-established antifungal drugs. Recently, these compounds have been reported to have therapeutic efficacy also in inflammatory skin disorders. These is increasing evidence that calmodulin is involved in fungal infections as well as in inflammatory skin diseases. Therefore, we investigated the effects of various antifungal drugs on calmodulin activity, using calmodulin-dependent phosphodiesterase as

Lutz Hegemann; Susan M. Toso; Khosrow L Lahijani; Guy F. Webster; Jouni Uitto

1993-01-01

197

Diversity of cutaneous bacteria with antifungal activity isolated from female four-toed salamanders  

Microsoft Academic Search

Among the microbiota of amphibian skin are bacteria that produce antifungal compounds. We isolated cutaneous bacteria from the skins of three populations of the nest-attending plethodontid salamander Hemidactylium scutatum and subsequently tested the bacterial isolates against two different fungi (related to Mariannaea elegans and Rhizomucor variabilis) that were obtained from dead salamander eggs. The culturable antifungal bacteria were phylogenetically characterized

Antje Lauer; Mary Alice Simon; Jenifer L Banning; Brianna A Lam; Reid N Harris

2008-01-01

198

Suppressive Drug Interactions between Antifungals Marjon G.J. de Vos1 and Tobias Bollenbach1,*  

E-print Network

Suppressive Drug Interactions between Antifungals Marjon G.J. de Vos1 and Tobias Bollenbach1,* 1IST a systematic study of drug interactions be- tween antifungal compounds. Suppressive drug interactions occur. When two drugs are combined, they may interact synergistically or antago- nistically; for synergistic

Bulyk, Martha L.

199

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

2000-01-01

200

Evaluation of in vitro Resistance in Patients with Onychomycosis Who Fail Antifungal Therapy  

Microsoft Academic Search

Background: With the increased awareness of onychomycosis and the increasing use of antifungals for this indication, it is prudent to be concerned about the possible emergence of resistant strains. There has been substantial work on the development of standardized methods for testing the in vitro resistance of various fungi and yeasts to the currently available antifungal agents. However, relatively little

Aditya K. Gupta; Yatika Kohli

2003-01-01

201

No Adverse Effect of Genetically Modified Antifungal Wheat on Decomposition Dynamics and the Soil Fauna  

E-print Network

No Adverse Effect of Genetically Modified Antifungal Wheat on Decomposition Dynamics and the Soil and Evolution, University of Bern, Bern, Switzerland Abstract The cultivation of genetically modified (GM: Duc C, Nentwig W, Lindfeld A (2011) No Adverse Effect of Genetically Modified Antifungal Wheat

Richner, Heinz

202

Comparison of anti-Candida activity of thyme, pennyroyal, and lemon essential oils versus antifungal drugs against Candida species  

Microsoft Academic Search

Because of resistance and side effects to common antifungal drugs, there have been many studies on the use of herbal antifungal essential oils. In this study, the anti-Candida activities of thyme, pennyroyal and lemon essential oils in comparison to antifungal drugs were assessed. The paper disc diffusion method was used to study the inhibitory effects of the essential oils of

Saeid Mahdavi Omran; Seddighe Esmailzadeh

203

Antifungal leaf-surface metabolites correlate with fungal abundance in sagebrush populations.  

PubMed

A central component in understanding plant-enemy interactions is to determine whether plant enemies, such as herbivores and pathogens, mediate the evolution of plant secondary metabolites. Using 26 populations of a broadly distributed plant species, sagebrush (Artemisia tridentata), we examined whether sagebrush populations in habitats with a greater prevalence of fungi contained antifungal secondary metabolites on leaf surfaces that were more active and diverse than sagebrush populations in habitats less favorable to fungi. Because moisture and temperature play a key role in the epidemiology of most plant-pathogen interactions, we also examined the relationship between the antifungal activity of secondary metabolites and the climate of a site. We evaluated the antifungal activity of sagebrush secondary metabolites against two fungi, a wild Penicillium sp. and a laboratory yeast, Saccharomyces cerevisiae, using a filter-paper disk assay and bioautography. Comparing the 26 sagebrush populations, we found that fungal abundance was a good predictor of both the activity (r2 = 0.36 for Saccharomyces, r2 = 0.37 for Penicillium) and number (r2 = 0.34 for Saccharomyces) of antifungal secondary metabolites. This suggests that selection imposed by fungal pathogens has led to more effective antifungal secondary metabolites. We found that the antifungal activity of sagebrush secondary metabolites was negatively related to average vapor pressure deficit of the habitat (r2 = 0.60 for Saccharomyces, r2 = 0.61 for Penicillium). Differences in antifungal activity among populations were not due to the amount of secondary metabolites, but rather to qualitative differences in the composition of antifungal compounds. Although all populations in habitats with high fungal prevalence had secondary metabolites with high antifungal activity, different suites of compounds were responsible for this activity, suggesting independent outcomes of selection on plants by fungal pathogens. The location of antifungal secondary metabolites on the leaf surface is consistent with their putative defense role, and we found no evidence supporting other functions, such as protection from ultraviolet light or oxidation. That the antifungal activity of sagebrush secondary metabolites was similar for two different fungi provides support for broad antifungal defenses. The incidence and severity of fungal disease in the field (caused by Puccinia tanaceti) were similar in moist and dry habitats, possibly reflecting an equilibrium between plant defense and fungal attack, as sites with greater fungal abundance compensated with more effective secondary metabolites. The geographic correlation between fungal abundance and antifungal secondary metabolites of sagebrush, coupled with our other data showing heritable variation in these metabolites, suggests that pathogenic fungi have selected for antifungal secondary metabolites in sagebrush. PMID:12523559

Talley, Sharon M; Coley, Phyllis D; Kursar, Thomas A

2002-11-01

204

Antifungal activity of gold nanoparticles prepared by solvothermal method  

SciTech Connect

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

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

2013-01-15

205

Time to initiation of antifungal therapy for neonatal candidiasis.  

PubMed

The effect of delayed antifungal therapy in critically ill infants with invasive candidiasis has not been studied. Our objective was to evaluate the effect of time to initiation of antifungal therapy (TIA) on mortality, disseminated disease, and postinfection hospital stay. We conducted a cohort study of critically ill infants with cultures positive for Candida from 1990 to 2008. TIA was defined as the number of hours from the collection of the first positive culture until the start of antifungal therapy. Of 96 infants, 57% were male, the median gestational age was 27 weeks (range, 23 to 41 weeks), and the median birth weight was 956 g (range, 415 to 6,191 g). Most subjects received amphotericin B deoxycholate. TIA was ? 24 h for 35% of infants, between 25 and 48 h for 42%, and >48 h for 23%. Eleven subjects died during hospitalization, and 22% had disseminated candidiasis. The median duration of hospital stay postinfection was 53 days (range, 6 to 217 days). Both univariate and multivariate analyses demonstrated that TIA was not associated with mortality, disseminated disease, or hospital stay postinfection. However, ventilator use for >60 days significantly increased the risk of death (odds ratio [OR], 9.5; 95% confidence interval [CI], 2.2 to 66.7; P = 0.002). Prolonged candidemia increased the risk of disseminated disease by 10% per day of positive culture (OR, 1.1; 95% CI, 1.08 to 1.2; P = 0.007), and low gestational age was associated with increased neonatal intensive care unit (NICU) stay after the first positive Candida culture by 0.94 weeks (95% CI, 0.70 to 0.98; P < 0.001). The TIA was not associated with all-cause mortality, disseminated candidiasis, and postinfection length of hospital stay. PMID:23507285

Le, Jennifer; Tran, Tu T; Bui, Ivilynn; Wang, Mike K; Vo, Andrew; Adler-Shohet, Felice C

2013-06-01

206

A radish seed antifungal peptide with a high amyloid fibril-forming propensity.  

PubMed

The amyloid fibril-forming ability of two closely related antifungal and antimicrobial peptides derived from plant defensin proteins has been investigated. As assessed by sequence analysis, thioflavin T binding, transmission electron microscopy, atomic force microscopy and X-ray fiber diffraction, a 19 amino acid fragment from the C-terminal region of Raphanus sativus antifungal protein, known as RsAFP-19, is highly amyloidogenic. Further, its fibrillar morphology can be altered by externally controlled conditions. Freezing and thawing led to amyloid fibril formation which was accompanied by loss of RsAFP-19 antifungal activity. A second, closely related antifungal peptide displayed no fibril-forming capacity. It is concluded that while fibril formation is not associated with the antifungal properties of these peptides, the peptide RsAFP-19 is of potential use as a controllable, highly amyloidogenic small peptide for investigating the structure of amyloid fibrils and their mechanism of formation. PMID:23665069

Garvey, Megan; Meehan, Sarah; Gras, Sally L; Schirra, Horst J; Craik, David J; Van der Weerden, Nicole L; Anderson, Marilyn A; Gerrard, Juliet A; Carver, John A

2013-08-01

207

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. PMID:22276116

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

2012-01-01

208

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. PMID:22400016

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

2012-01-01

209

Cytotoxic and Antifungal Activities of Diverse ?-Naphthylamine Derivatives  

PubMed Central

Diverse ?-naphthylamine derivatives were easily prepared from corresponding aldimines derived from commercially available ?-naphthaldehyde and anilines or isomeric pyridinecarboxyaldehydes and ?-naphthylamine. The secondary amines obtained were tested as possible antifungal and cytotoxic agents. The diverse N-aryl-N-[1-(1-naphthyl)but-3-enyl]amines obtained were active (IC50 < 10 ?g/mL) against breast (MCF-7), non-small cell lung (H-460), and central nervous system (SF-268) human cancer cell lines, while N-(pyridinylmethyl)-naphthalen-1-amines resulted in activity against (MIC 25–32 ?g/mL) some human opportunistic pathogenic fungi including yeasts, hialohyphomycetes, and dermatophytes. PMID:23264936

Kouznetsov, Vladímir V.; Zacchino, Susana A.; Sortino, Maximiliano; Vargas Méndez, Leonor Y.; Gupta, Mahabir P.

2012-01-01

210

Antifungal effect of dairy propionibacteria--contribution of organic acids.  

PubMed

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 by these bacteria is necessary to understand their inhibitory activity. We evaluated the antifungal activity of the type strains of five dairy propionibacteria, Propionibacterium acidipropionici, P. jensenii, P. thoenii, P. freudenreichii subsp. freudenreichii and P. freudenreichii subsp. shermanii against eight food- and feedborne moulds and yeasts. A dual culture system assayed the inhibitory activity on three different agar media, sodium lactate (SL), de Man Rogosa Sharp (MRS) and MRS without acetate (MRS-ac). The amounts of organic acids produced during growth of propionibacteria in liquid SL, MRS and MRS-ac were also determined. The minimal inhibitory concentration (MIC) values of propionic, acetic and lactic acid were established for all fungi at pH 3, 5 and 7. Propionic acid, followed by acetic acid, was the most potent antifungal acid. Inhibition at pH 7 generally required concentrations above 500 mM for all three acids, at pH 5 the MIC values for propionic and acetic acids were 20-120 mM and above 500 mM for lactic acid. At pH 3, the MIC values were, with one exception, below 10 mM for both propionic and acetic acid and above 160 mM for lactic acid. The yeast Pichia anomala was the fungus most resistant to organic acids. The propionibacteria exhibited a pronounced species variation in antifungal activity on MRS (+/-acetate) agar, with P. thoenii being the most potent. Four of the five propionibacteria species produced more propionic and acetic acid in liquid SL medium than in MRS (+/-acetate) broth. However, when SL agar was used as the growth medium, none of the propionibacteria inhibited fungal growth. PMID:15681043

Lind, Helena; Jonsson, Hans; Schnürer, Johan

2005-02-01

211

Mechanism of Action of Efinaconazole, a Novel Triazole Antifungal Agent  

PubMed Central

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

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

2013-01-01

212

Antifungal activity of Lactobacillus against Microsporum canis, Microsporum gypseum and Epidermophyton floccosum  

PubMed Central

A total of 220 lactic acid bacteria isolates were screened for antifungal activity using Aspergillus fumigatus and Aspergillus niger as the target strains. Four Lactobacillus strains exhibited strong inhibitory activity on agar surfaces. All four were also identified as having strong inhibitory activity against the human pathogenic fungi Microsporum canis, Microsporum gypseum and Epidermophyton floccosum. One of the four lactobacilli, namely Lb. reuteri ee1p exhibited the most inhibition against dermatophytes. Cell-free culture supernatants of Lb. reuteri ee1p and of the non-antifungal Lb. reuteri M13 were freeze-dried and used to access and compare antifungal activity in agar plate assays and microtiter plate assays. Addition of the Lb. reuteri ee1p freeze-dried cell-free supernatant powder into the agar medium at concentrations greater than 2% inhibited all fungal colony growth. Addition of the powder at 5% to liquid cultures caused complete inhibition of fungal growth on the basis of turbidity. Freeze-dried supernatant of the non-antifungal Lb. reuteri M13 at the same concentrations had a much lesser effect. As Lb. reuteri M13 is very similar to the antifungal strain ee1p in terms of growth rate and final pH in liquid culture, and as it has little antifungal activity, it is clear that other antifungal compounds must be specifically produced (or produced at higher levels) by the anti-dermatophyte strain Lb. reuteri ee1p. Reuterin was undetectable in all four antifungal strains. The cell free supernatant of Lb. reuteri ee1p was analyzed by LC-FTMS using an Accela LC coupled to an LTQ Orbitrap XL mass spectrometer. The high mass accuracy spectrum produced by compounds in the Lb. reuteri ee1p strain was compared with both a multianalyte chromatogram and individual spectra of standard anti-fungal compounds, which are known to be produced by lactic acid bacteria. Ten antifungal metabolites were detected. PMID:22539027

Guo, Jiahui; Brosnan, Brid; Furey, Ambrose; Arendt, Elke; Murphy, Padraigin; Coffey, Aidan

2012-01-01

213

The Antifungal Protein from Aspergillus giganteus Causes Membrane Permeabilization  

PubMed Central

We investigated the inhibitory effects of the antifungal protein (AFP) from Aspergillus giganteus on the growth of several filamentous fungi. For this purpose, the MICs of AFP were determined and ranged from 0.1 ?g/ml for Fusarium oxysporum to 200 ?g/ml for Aspergillus nidulans. The antifungal activity of AFP was diminished in the presence of cations. We were able to show that incubation of AFP-sensitive fungi with the protein resulted in membrane permeabilization using an assay based on the uptake of the fluorescent dye SYTOX Green. No permeabilization by AFP could be detected at concentrations below the species-specific MIC. Furthermore, AFP-induced permeabilization could readily be detected after 5 min of incubation. Localization experiments with fluorescein isothiocyanate-labeled AFP and immunofluorescence staining with an AFP-specific antibody supported the observation that the protein interacts with membranes. After treatment of AFP-sensitive fungi with AFP, the protein was localized at the plasma membrane, whereas it was mainly detected inside the cells of AFP-resistant fungi. We conclude from these data that the growth-inhibitory effect of AFP is caused by permeabilization of the fungal membranes. PMID:12543664

Theis, T.; Wedde, M.; Meyer, V.; Stahl, U.

2003-01-01

214

Antifungals: Need to Search for a New Molecular Target  

PubMed Central

In the 1990s, drug resistance has become an important problem in a variety of infectious diseases including human immunodeficiency virus infection, tuberculosis, and other bacterial infections which have profound effects on human health. At the same time, there have been dramatic increase in the incidence of fungal infections, which are probably the result of alterations in immune status associated with the acquired immuno deficiency syndrome epidemic, cancer chemotherapy, and organ and bone marrow transplantation. The rise in the incidence of fungal infections has exacerbated the need for the next generation of antifungal agents, since many of the currently available drugs have undesirable side effects, are ineffective against new or reemerging fungi, or lead to the rapid development of the resistance. This review will focus on the pathogenic yeast Candida albicans, since a large body of work on the factors and mechanism associated with antifungal drug resistance in this organism is reported sufficiently. It will certainly elaborate the probable molecular targets for drug design, discovered to date. PMID:20046765

Sangamwar, A. T.; Deshpande, U. D.; Pekamwar, S. S.

2008-01-01

215

Antifungals: need to search for a new molecular target.  

PubMed

In the 1990s, drug resistance has become an important problem in a variety of infectious diseases including human immunodeficiency virus infection, tuberculosis, and other bacterial infections which have profound effects on human health. At the same time, there have been dramatic increase in the incidence of fungal infections, which are probably the result of alterations in immune status associated with the acquired immuno deficiency syndrome epidemic, cancer chemotherapy, and organ and bone marrow transplantation. The rise in the incidence of fungal infections has exacerbated the need for the next generation of antifungal agents, since many of the currently available drugs have undesirable side effects, are ineffective against new or reemerging fungi, or lead to the rapid development of the resistance. This review will focus on the pathogenic yeast Candida albicans, since a large body of work on the factors and mechanism associated with antifungal drug resistance in this organism is reported sufficiently. It will certainly elaborate the probable molecular targets for drug design, discovered to date. PMID:20046765

Sangamwar, A T; Deshpande, U D; Pekamwar, S S

2008-01-01

216

Lavandula luisieri essential oil as a source of antifungal drugs.  

PubMed

This work reports the antifungal activity of Lavandula luisieri essential oils against yeast, dermatophyte and Aspergillus strains responsible for human infections and food contamination. The oil's cytotoxicity and its effect on the yeast-mycelium transition in Candida albicans, an important virulence factor, were also evaluated. Analyses by GC and GC/MS showed a peculiar composition of irregular monoterpenes. Significant differences between the samples occurred in the amounts of 1,8-cineole, fenchone and trans-?-necrodyl acetate. The oil with higher amounts of irregular monoterpenes was the most effective. The influence of the oils on the dimorphic transition in C. albicans was also studied through the germ tube inhibition assay. Filamentation was completely inhibited at concentrations sixteen times lower than the minimal inhibitory concentration. The results support the use of L. luiseiri essential oils in the development of new phytopharmaceuticals and food preservatives and emphasise its antifungal properties at concentrations not cytotoxic or with very low detrimental effects on mammalian cells. PMID:22953886

Zuzarte, M; Gonçalves, M J; Cruz, M T; Cavaleiro, C; Canhoto, J; Vaz, S; Pinto, E; Salgueiro, L

2012-12-01

217

The impact of antifungals on toll-like receptors  

PubMed Central

Fungi are increasingly recognized as major pathogens in immunocompromised individuals. With the increase in the number of fungal infections each year and the development of resistance to current therapy, new approaches to treatment including stimulation of the immune response in addition to concurrent pharmacotherapy is ongoing. The most common invasive fungal infections are caused by Candida spp., Aspergillus spp., and Cryptococcus spp. Amphotericin B (AmB) has remained the cornerstone of therapy against many fulminant fungal infections but its use is limited by its multitude of side effects. Echinocandins are a newer class of antifungal drugs with activity against Candida spp. and Aspergillus spp. and constitutes an alternative to AmB due to superior patient tolerability and fewer side effects. Due to their oral delivery, azoles continue to be heavily used for simple and complex diseases, such as fluconazole for candidal vaginitis and voriconazole for aspergillosis. The objective of this paper is to present current knowledge regarding the multiple interactions between the broad spectrum antifungals and the innate immune response, primarily focusing on the toll-like receptors. PMID:24672516

Mihu, Mircea R.; Pattabhi, Rodney; Nosanchuk, Joshua D.

2014-01-01

218

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

PubMed

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

2008-02-01

219

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)

2010-09-22

220

Methylxanthine inhibit fungal chitinases and exhibit antifungal activity.  

PubMed

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

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

2012-03-01

221

Chemical composition, antifungal and insecticidal activities of Hedychium essential oils.  

PubMed

The antimicrobial properties of essential oils have been documented, and their use as "biocides" is gaining popularity. The aims of this study were to analyze the chemical composition and assess the biological activities of Hedychium essential oils. Oils from 19 Hedychium species and cultivars were analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) techniques. The antifungal and insecticidal activities of these oils were tested against Colletotrichum acutatum, C. fragariae, and C. gloeosporioides, and three insects, the azalea lace bug (Stephanitis pyrioides), the yellow fever mosquito (Aedes aegypti), and the red imported fire ant (Solenopsis invicta). Hedychium oils were rich in monoterpenes and sesquiterpenes, especially 1,8-cineole (0.1%-42%), linalool (<0.1%-56%), a-pinene (3%-17%), b-pinene (4%-31%), and (E)-nerolidol (0.1%-20%). Hedychium oils had no antifungal effect on C. gloeosporioides, C. fragariae, and C. acutatum, but most Hedychium oils effectively killed azalea lace bugs. The oils also show promise as an adult mosquito repellent, but they would make rather poor larvicides or adulticides for mosquito control. Hedychium oils acted either as a fire ant repellent or attractant, depending on plant genotype and oil concentration. PMID:23579997

Sakhanokho, Hamidou F; Sampson, Blair J; Tabanca, Nurhayat; Wedge, David E; Demirci, Betul; Baser, Kemal Husnu Can; Bernier, Ulrich R; Tsikolia, Maia; Agramonte, Natasha M; Becnel, James J; Chen, Jian; Rajasekaran, Kanniah; Spiers, James M

2013-01-01

222

Antibacterial and antifungal activity of Avarone and Avarol.  

PubMed

The sesquiterpenoid hydroquinone and quinone, Avarol and Avarone, were previously found to be potent antitumor agents (Müller et al., 1984). In the present study it is reported that in aqueous solution (pH 7.2), in the presence of dimethylsulfoxide, Avarol is converted to Avarone. Avarone and to a smaller extent also Avarol were active against a variety of grampositive bacterial species. The highest activity was determined for Streptococcus pneumoniae and Erysipelothrix rhusiopathiae (MIC 0.781 mg/l). The antibacterial activity can be augmented 2 to 4-fold by lowering the pH in the culture medium from 7.0 to 6.0. The efficiency of Avarone and Avarol was abolished in the presence of serum. No antibacterial activity was determined in gramnegative bacterial species. In addition, Avarol and to a smaller extent also Avarone displayed an antifungal activity on Trichophyton species and Microsporum canis (MIC: 15.6-62.5 mg/l), while Avarone and not Avarol was active on Aspergillus niger, no activity was found against Candida species. These data indicate that the antitumor agents Avarol/Avarone display also antibacterial- and antifungal activities against a limited range of microorganisms. PMID:3841441

Seibert, G; Raether, W; Dogovi?, N; Gasi?, M J; Zahn, R K; Müller, W E

1985-11-01

223

Glycerol Enhances the Antifungal Activity of Dairy Propionibacteria  

PubMed Central

Dairy propionibacteria are widely used in starter cultures for Swiss type cheese. These bacteria can ferment glucose, lactic acid, and glycerol into propionic acid, acetic acid, and carbon dioxide. This research examined the antifungal effect of dairy propionibacteria when glycerol was used as carbon source for bacterial growth. Five type strains of propionibacteria were tested against the yeast Rhodotorula mucilaginosa and the molds Penicillium commune and Penicillium roqueforti. The conversion of 13C glycerol by Propionibacterium jensenii was followed with nuclear magnetic resonance. In a dual culture assay, the degree of inhibition of the molds was strongly enhanced by an increase in glycerol concentrations, while the yeast was less affected. In broth cultures, decreased pH in glycerol medium was probably responsible for the complete inhibition of the indicator fungi. NMR spectra of the glycerol conversion confirmed that propionic acid was the dominant metabolite. Based on the results obtained, the increased antifungal effect seen by glycerol addition to cultures of propionibacteria is due to the production of propionic acid and pH reduction of the medium. PMID:21331381

Lind, Helena; Broberg, Anders; Jacobsson, Karin; Jonsson, Hans; Schnürer, Johan

2010-01-01

224

Glycerol enhances the antifungal activity of dairy propionibacteria.  

PubMed

Dairy propionibacteria are widely used in starter cultures for Swiss type cheese. These bacteria can ferment glucose, lactic acid, and glycerol into propionic acid, acetic acid, and carbon dioxide. This research examined the antifungal effect of dairy propionibacteria when glycerol was used as carbon source for bacterial growth. Five type strains of propionibacteria were tested against the yeast Rhodotorula mucilaginosa and the molds Penicillium commune and Penicillium roqueforti. The conversion of (13)C glycerol by Propionibacterium jensenii was followed with nuclear magnetic resonance. In a dual culture assay, the degree of inhibition of the molds was strongly enhanced by an increase in glycerol concentrations, while the yeast was less affected. In broth cultures, decreased pH in glycerol medium was probably responsible for the complete inhibition of the indicator fungi. NMR spectra of the glycerol conversion confirmed that propionic acid was the dominant metabolite. Based on the results obtained, the increased antifungal effect seen by glycerol addition to cultures of propionibacteria is due to the production of propionic acid and pH reduction of the medium. PMID:21331381

Lind, Helena; Broberg, Anders; Jacobsson, Karin; Jonsson, Hans; Schnürer, Johan

2010-01-01

225

A novel antifungal protein of Bacillus subtilis B25.  

PubMed

Bacillus subtilis B25 was isolated from banana rhizosphere soil. It has been confirmed for B25 to have stronger antagonism against Fusarium oxysporum f.sp.cubense, Additionally B25 has good inhibitory to plant pathogens, including Corynespora cassiicola, Alternaria solani, Botrytis cinerea and Colletotrichum gloeosporioides on potato dextrose agar (PDA) plates. The antagonistic substance can be extracted from cell-free culture broth supernatants by 70% (w/v) (NH4)2 SO4 saturation. Clear blank band was observed between the protein and a pathogen. The examination of antagonistic mechanism under light microscope showed that the antifungal protein of B25 appeared to inhibit pathogens by leading to mycelium and spores tumescence, distortion, abnormality. The isolation procedure comprised ion exchange chromatography on DEAE-Sephadex Fast Flow and gel filtration chromatography on SephadexG-100. The purified antifungal fraction showed a single band in sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE). The active fraction was identified by NanoLC-ESI-MS/MS The amino acid sequences of 17 peptides segments were obtained. The analysis of the protein suggested that it was a hypothetical protein (gi154685475), with a relative molecular mass of 38708.67 Da and isoelectric point (pI) of 5.63. PMID:24255843

Tan, Zhiqiong; Lin, Baoying; Zhang, Rongyi

2013-01-01

226

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: nesnow.stephen@epa.gov

2009-01-15

227

Determination of fungicides in wine by mixed-mode solid phase extraction and liquid chromatography coupled to tandem mass spectrometry  

Microsoft Academic Search

A novel procedure for the determination of nine selected fungicides (metalaxyl-M, azoxystrobin, myclobutanil, flusilazole, penconazole, tebuconazole, propiconazole, diniconazole and difenoconazole) in wine samples is presented. Sample enrichment and purification is simultaneously performed using mixed-mode, anion exchange and reversed-phase, OASIS MAX solid-phase extraction (SPE) cartridges. Analytes were determined by liquid chromatography coupled to tandem mass spectrometry using atmospheric pressure electrospray ionization

I. Carpinteiro; M. Ramil; I. Rodríguez; R. Cela

228

Antifungal treatment in allergic bronchopulmonary aspergillosis with and without cystic fibrosis: a systematic review.  

PubMed

Allergic bronchopulmonary aspergillosis (ABPA) is a rare disease that affects patients with asthma or cystic fibrosis. Its debilitating course has led to the search for new treatments, including antifungals and monoclonal antibodies. To evaluate the efficacy and safety of antifungal treatments in patients with ABPA and either asthma or cystic fibrosis, we performed a systematic review of the literature on the effects of antifungal agents in ABPA using three biomedical databases. Quality assessment was performed using the GRADE methodology and, where appropriate, studies with comparable outcomes were pooled for meta-analysis. Thirty-eight studies - four randomized controlled trials and 34 observational studies - met the eligibility criteria. The antifungal interventions described were itraconazole, voriconazole, posaconazole, ketoconazole, natamycin, nystatin and amphotericin B. An improvement in symptoms, frequency of exacerbations and lung function was reported in most of the studies and was more common with oral azoles. Antifungals also had a positive impact on biomarkers and radiological pulmonary infiltrates, but adverse effects were also common. The quality of the evidence supporting these results was low or very low due to a shortage of controlled studies, heterogeneity between studies and potential bias. Antifungal interventions in ABPA improved patient and disease outcomes in both asthma and cystic fibrosis. However, the recommendation for their use is weak and clinicians should therefore weigh up desirable and undesirable effects on a case-by-case basis. More studies with a better methodology are needed, especially in cystic fibrosis, to increase confidence in the effects of antifungal treatments in ABPA. PMID:24809846

Moreira, A S; Silva, D; Ferreira, A Reis; Delgado, L

2014-10-01

229

The calcineurin inhibitor cyclosporin A exhibits synergism with antifungals against Candida parapsilosis species complex.  

PubMed

Candida parapsilosis complex comprises three closely related species, C. parapsilosis sensu stricto, Candida metapsilosis and Candida orthopsilosis. In the last decade, antifungal resistance to azoles and caspofungin among C. parapsilosis sensu lato strains has been considered a matter of concern worldwide. In the present study, we evaluated the synergistic potential of antifungals and the calcineurin inhibitor cyclosporin A (Cys) against planktonic and biofilms of C. parapsilosis complex from clinical sources. Susceptibility assays with amphotericin, fluconazole, voriconazole, caspofungin and Cys were performed by microdilution in accordance with Clinical and Laboratory Standards Institute guidelines. Synergy testing against planktonic cells of C. parapsilosis sensu lato strains was assessed by the chequerboard method. Combinations formed by antifungals with Cys were evaluated against mature biofilms in microtitre plates. No differences in the antifungal susceptibility pattern among species were observed, but C. parapsilosis sensu stricto strains were more susceptible to Cys than C. orthopsilosis and C. metapsilosis. Synergism between antifungals and Cys was observed in C. parapsilosis sensu lato strains. Combinations formed by antifungals and Cys were able to prevent biofilm formation and showed an inhibitory effect against mature biofilms of C. parapsilosis sensu stricto, C. metapsilosis and C. orthopsilosis. These results strengthen the potential of calcineurin inhibition as a promising approach to enhance the efficiency of antifungal drugs. PMID:24722799

Cordeiro, Rossana de Aguiar; Macedo, Ramila de Brito; Teixeira, Carlos Eduardo Cordeiro; Marques, Francisca Jakelyne de Farias; Bandeira, Tereza de Jesus Pinheiro Gomes; Moreira, José Luciano Bezerra; Brilhante, Raimunda Sâmia Nogueira; Rocha, Marcos Fábio Gadelha; Sidrim, José Júlio Costa

2014-07-01

230

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. PMID:22396754

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

2012-01-01

231

In Vitro and In Vivo Activity of a Novel Antifungal Small Molecule against Candida Infections  

PubMed Central

Candida is the most common fungal pathogen of humans worldwide and has become a major clinical problem because of the growing number of immunocompromised patients, who are susceptible to infection. Moreover, the number of available antifungals is limited, and antifungal-resistant Candida strains are emerging. New and effective antifungals are therefore urgently needed. Here, we discovered a small molecule with activity against Candida spp. both in vitro and in vivo. We screened a library of 50,240 small molecules for inhibitors of yeast-to-hypha transition, a major virulence attribute of Candida albicans. This screening identified 20 active compounds. Further examination of the in vitro antifungal and anti-biofilm properties of these compounds, using a range of Candida spp., led to the discovery of SM21, a highly potent antifungal molecule (minimum inhibitory concentration (MIC) 0.2 – 1.6 µg/ml). In vitro, SM21 was toxic to fungi but not to various human cell lines or bacterial species and was active against Candida isolates that are resistant to existing antifungal agents. Moreover, SM21 was relatively more effective against biofilms of Candida spp. than the current antifungal agents. In vivo, SM21 prevented the death of mice in a systemic candidiasis model and was also more effective than the common antifungal nystatin at reducing the extent of tongue lesions in a mouse model of oral candidiasis. Propidium iodide uptake assay showed that SM21 affected the integrity of the cell membrane. Taken together, our results indicate that SM21 has the potential to be developed as a novel antifungal agent for clinical use. PMID:24465737

Yuen, Kwok Yong; Wang, Yu; Yang, Dan; Samaranayake, Lakshman Perera

2014-01-01

232

Combinatorial synthesis of benzimidazole-azo-phenol derivatives as antifungal agents.  

PubMed

A chemically diverse library of benzimidazole-azo-phenol derivatives was efficiently prepared and screened for their antifungal activities against five phytopathogenic fungi. Some compounds exhibited potent antifungal activities. As compared with a commercially available agricultural fungicide, hymexazol, especially compound V-5 showed the most promising broad-spectrum antifungal activities against five phytopathogenic fungi. The EC50 values of V-5 against F. graminearum, A. solani, V. mali, B. cinerea, and C. lunata were 0.09, 0.08, 0.06, 0.07, and 0.11 ?mol/mL, respectively. PMID:24152176

Ke, Yazhen; Zhi, Xiaoyan; Yu, Xiang; Ding, Guodong; Yang, Chun; Xu, Hui

2014-01-01

233

Enhancement of the Antifungal Activity of Antimicrobial Drugs by Eugenia uniflora L.  

PubMed Central

Abstract Candidiasis is the most frequent infection by opportunistic fungi such as Candida albicans, Candida tropicalis, and Candida krusei. Ethanol extract from Eugenia uniflora was assayed, for its antifungal activity, either alone or combined with four selected chemotherapeutic antimicrobial agents, including anphotericin B, mebendazole, nistatin, and metronidazole against these strains. The obtained results indicated that the association of the extract of E. uniflora to metronidazole showed a potential antifungal activity against C. tropicalis. However, no synergistic activity against the other strains was observed, as observed when the extract was associated with the other, not enhancing their antifungal activity. PMID:23819641

Santos, Karla K.A.; Matias, Edinardo F.F.; Tintino, Saulo R.; Souza, Celestina E.S.; Braga, Maria F.B.M.; Guedes, Glaucia M.M.; Costa, Jose G.M.; Menezes, Irwin R.A.

2013-01-01

234

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

PubMed

Candidiasis is the most frequent infection by opportunistic fungi such as Candida albicans, Candida tropicalis, and Candida krusei. Ethanol extract from Eugenia uniflora was assayed, for its antifungal activity, either alone or combined with four selected chemotherapeutic antimicrobial agents, including anphotericin B, mebendazole, nistatin, and metronidazole against these strains. The obtained results indicated that the association of the extract of E. uniflora to metronidazole showed a potential antifungal activity against C. tropicalis. However, no synergistic activity against the other strains was observed, as observed when the extract was associated with the other, not enhancing their antifungal activity. PMID:23819641

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

2013-07-01

235

Molluscicidal and antifungal activity of Erigeron speciosus steam distillate.  

PubMed

The steam-distilled fraction of the aerial parts of Erigeron speciosus (Lindl) DC was tested for activity against strawberry plant pathogenic fungi Botrytis cinerea Pers ex Fr, Colletotrichum acutatum Simmonds, C fragariae Brooks, C gloeosporioides (Penz) Penz & Sacc, and the intermediate host snail Planobdella trivolvis that harbors the trematode, Bolbophorus confusus, that infests and causes severe infections in pond-raised catfish in the Mississippi Delta region of the USA. Bioautography on silica TLC plates demonstrated antifungal activity in the steam distillate. Preliminary bioassays of the steam distillate indicated the presence of phytochemicals toxic to P trivolvis. The bioactive compounds methyl 2Z, 8Z-deca-2,8-diene-4,6-diynoate and its 2E, 8E isomer were isolated by bioassay-guided fractionation and chromatographic techniques and identified by 1H NMR spectroscopy. PMID:12400444

Meepagala, Kumudini M; Sturtz, George; Wise, David; Wedge, David E

2002-10-01

236

Endophytic bacteria from banana cultivars and their antifungal activity.  

PubMed

Endophytic microorganisms consist of fungi, bacteria, and actinomycetes that play important roles in the process of plant adaptation to the environment. Currently, the natural associations between microorganisms and plant species are being explored for a large number of biotechnological applications. In this study, 122 endophytic bacteria were isolated from 5 cultivars of Musa spp from the state of Amazonas (Brazil). Four strains were selected because they exhibited antagonistic activities against Fusarium oxysporum f. sp cubense and Colletotrichum guaranicola, with inhibitions ranging from 19 to 30% and 27 to 35%, respectively. Phylogenetic analysis of the 16S rDNA regions of these bacteria with antifungal activity showed that they are phylogenetically related to 3 different species of Bacillus - B. amyloliquefaciens, B. subtilis subsp subtilis, and B. thuringiensis. PMID:25366756

Souza, A; Cruz, J C; Sousa, N R; Procópio, A R L; Silva, G F

2014-01-01

237

5-Nitroimidazole derivatives as possible antibacterial and antifungal agents.  

PubMed

Some novel 1-[2-[[5-(2-furanyl)-4-substituted 4H-1,2,4-triazol-3-yl[thio[ethyl[-2-methyl-5-nitro-1H-imidazoles (3), 1-[3-[[5-(2-furanyl/2-thienyl)-4-substituted 4H-1,2,4-triazol-3-yl[-thio]-2-hydroxypropyl[-2-methyl-5-nitro-1H- imidazoles (5) and 1-[3-[(N,N-disubstituted thiocarbamoyl)-thio[-2-hydroxypropyl]-2-methyl-5-nitro-1H-imidazoles (7) were synthesized and evaluated for in vitro antibacterial and antifungal activity. Some of 5 were found to be effective against bacteria and fungi (minimum inhibitory concentration (MIC) 7.3-125 micrograms/ml), whereas 7 were found to be effective against fungi (MIC 3-25 micrograms/ml). PMID:10668184

Günay, N S; Capan, G; Ulusoy, N; Ergenç, N; Otük, G; Kaya, D

1999-01-01

238

Antifungal efficacy of bacteria isolated from marine sedentary organisms.  

PubMed

The antibiotic-producing ability of 57 bacteria isolated from 8 marine sedentary organisms, 6 sponges (Spirastrella sp., Phyllospongia sp., Ircinia sp., Aaptos sp., Azorica sp., Axinella sp.), 1 soft coral (Lobophytum sp.) and 1 alga (Sargassum sp.), was evaluated against 6 phytopathogenic fungi (Helminthosporium oryzae, Rhizoctonium solani, Pyricularia oryzae, Fusarium oxysporum, Aspergillus oryzae and A. fumigatus). Bacteria of the genus Bacillus (20%), Pseudomonas (33%) and Flavobacterium (40%) were predominant among the heterotrophic bacteria isolated from the marine sponges, soft coral and alga, respectively. Bioassay results revealed that 36 (63%) bacterial isolates displayed antifungal activity against at least one fungus, the alga (Sargassum sp.) being the source of highest number (80%) of producer strains. Twelve bacterial isolates inhibited all fungi. The MIC of the organic extracts of 12 bacteria ranged from 0.3 to 22.8 mg/L. PMID:11980270

Mohapatra, B R; Bapuji, M; Sree, A

2002-01-01

239

Sertaconazole: updated review of a topical antifungal agent.  

PubMed

Sertaconazole is an imidazole-type antifungal agent that has shown considerable in vitro activity against pathogenic fungi. Various studies carried out in animal models, clinical and toxicologic trials have confirmed the value of sertaconazole in the topical treatment of superficial mycoses in dermatology and gynecology. After several years of clinical experience in the topical treatment of dermatophytosis and Tinea versicolor, the substance has been approved for gynecologic candidiasis in Europe. Sertaconazole has a wide action spectrum that includes yeasts and dermatophyte fungi, and it is also active against bacteria, mainly Gram-positive cocci, making it highly efficient in the treatment of polymicrobial infections. The recent approval of the molecule by the US Food and Drug Administration, and the appearance of a new formulation of sertaconazole for the treatment of onychomycoses on a weekly administrative basis, are all data relevant to the process of marketing the product. PMID:15954850

Carrillo-Muñoz, Alfonso J; Giusiano, Gustavo; Ezkurra, Pilar Ariadna; Quindós, Guillermo

2005-06-01

240

In vitro antifungal susceptibility of Malassezia furfur from bloodstream infections.  

PubMed

Fungaemia caused by Malassezia spp. in hospitalized patients requires prompt and appropriate therapy, but standard methods for the definition of the in vitro antifungal susceptibility have not been established yet. In this study, the in vitro susceptibility of Malassezia furfur from bloodstream infections (BSIs) to amphotericin B (AMB), fluconazole (FLC), itraconazole (ITC), posaconazole (POS) and voriconazole (VRC) was assessed using the broth microdilution (BMD) method of the Clinical and Laboratory Standards Institute (CLSI) with different media such as modified Sabouraud dextrose broth (SDB), RPMI and Christensen's urea broth (CUB). Optimal broth media that allow sufficient growth of M. furfur, and produce reliable and reproducible MICs using the CLSI BMD protocol were assessed. Thirty-six M. furfur isolates collected from BSIs of patients before and during AMB therapy, and receiving FLC prophylaxis, were tested. A good growth of M. furfur was observed in RPMI, CUB and SDB at 32 °C for 48 and 72 h. No statistically significant differences were detected between the MIC values registered after 48 and 72 h incubation. ITC, POS and VRC displayed lower MICs than FLC and AMB. These last two antifungal drugs showed higher and lower MICs, respectively, when the isolates were tested in SDB. SDB is the only medium in which it is possible to detect isolates with high FLC MICs in patients receiving FLC prophylaxis. A large number of isolates showed high AMB MIC values regardless of the media used. In conclusion, SDB might be suitable to determine triazole susceptibility. However, the media, the drug formulation or the breakpoints herein applied might not be useful for assessing the AMB susceptibility of M. furfur from BSIs. PMID:25168965

Iatta, Roberta; Figueredo, Luciana A; Montagna, Maria Teresa; Otranto, Domenico; Cafarchia, Claudia

2014-11-01

241

Study on Mutagenic Breeding of Bacillus Subtilis and Properties of Its Antifungal Substances  

NASA Astrophysics Data System (ADS)

Bacillus subtitles JA isolated by our laboratory produced a large amount of antifungal substances, which had strong inhibitory activity against various plant pathogenic fungi, such as Rhizoctonia solani, Fusarium graminearum and so on. Ion beam implantation as a new mutagenic methods was applied in our studay. After B. subtitles JA was implanted by N+ ions, a strain designated as B. subtitles JA-026 was screened and obtained, which had a higher ability to produce those antifungal substances. A series of experiments indicated that the antifungal substances were thermostable and partially sensitive to proteinases K and tryproteinase. When the fermentating broth was fractionated with ammonium sulphate of a final saturation of 70%, the precipitate-enhanced inhibitory activity while the supernatant lost this activity. It appeared that the antifungal substances were likely to be protein.

Liu, Jing; Yao, Jianming

2004-08-01

242

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 PMID:2168203

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

1990-01-01

243

[Determining the susceptibility of microfungi to antifungals and interpreting the results].  

PubMed

With the rising incidence of fungal infections and a widening range of antifungal agents, determining the in vitro susceptibility of microfungi to antifungals is increasingly important. Recent years have seen standardization of methods suitable for testing the susceptibility of yeasts and filamentous fungi to antifungals and a wider choice of commercially supplied kits for determining susceptibility derived from those standards. The texts surveys standard microdilution quantitative methods, disk diffusion tests and assessment of commercially available tests suitable for routine use in mycology laboratories. The Etest is recommended for its high correlation with the CLSI standards and sophisticated methodology including interpretation, which guarantees high quality and reproducible results. To assess pharmacokinetics, determination of antifungal levels in the patient's serum is recommended. PMID:17929220

Mallátová, Nada

2007-08-01

244

In vitro antifungal activity and mechanism of action of chitinase against four plant pathogenic fungi.  

PubMed

To determine why chitinase has different antifungal activity on different pathogenic fungi in vitro, we purified recombinant rice chitinase from Pichia pastoris and investigated its antifungal activity against four fungi - Rhizopus stolonifer (Ehrenb. et Fr.) Vuill, Botrytis squamosa Walker, Pythium aphanidermatum (eds.) Fitzp, and Aspergillus niger van Tiegh. Scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR) were used to analyze the surface microstructure and proportion of chitin in the cell wall of the four fungi, respectively. The results showed that the chitinase exhibited different antifungal activities against the four fungi, which was directly correlated to the surface microstructure and the proportion of chitin in the fungal cell wall. It will help understanding the antifungal mechanism of the recombinant chitinase and further determining its application scope on crop protection and post-harvest storage of fruits and vegetables. PMID:18720488

Yan, Ruixiang; Hou, Jianhua; Ding, Dongfeng; Guan, Wenqqiang; Wang, Cuiyan; Wu, Zhiqiang; Li, Minggang

2008-08-01

245

Sertaconazole antifungal profile determined by a microdilution method versus nine topical substances against dermatophyte fungi.  

PubMed

Antifungal activity and in vitro inhibition time for sertaconazole (STZ) and 9 other topical drugs, namely amorolfine, bifonazole, clotrimazole, econazole, ketoconazole, miconazole, oxiconazole, terbinafine, and tioconazole were determined against 124 clinical isolates of dermatophyte (12 species) fungi by the microdilution method in a liquid medium and the measurement of optical density. STZ's antifungal activity was not always affected by the tested dermatophyte genus, as was the case with the remaining antifungals. In vitro antifungal activity was at the same level for all the studied azole derivatives, but, in terms of partial inhibitory concentrations, STZ starts its in vitro inhibitory activity in a shorter time than the other tested substances, particularly in those incubation periods when the growth of the dermatophyte fungi was more developed. PMID:23296325

Carrillo-Muñoz, A J; Tur-Tur, C; Cárdenes, D; Rojas, F; Giusiano, G

2012-01-01

246

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

ERIKA J. ERNST; MICHAEL E. KLEPSER; MICHAEL A. PFALLER

2000-01-01

247

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

2005-01-01

248

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

PubMed

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

2013-05-24

249

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

2010-01-01

250

Purification and characterization of a novel anti-fungal protein from Gastrodia elata  

Microsoft Academic Search

An anti-fungal protein GAFP-1 (Gastrodia anti-fungal protein, also called gastrodianin) was purified from Gastrodia elata B1. f. flavida S. Chow (Orchidaceae), a parasitic plant on the fungus Armillaria mellea. It can inhibit the hyphal growth of some phytopathogenic fungi such as Valsa ambiens, Rhizoctonia solani, Gibberella zeae, Ganoderma lucidum and Botrytis cinerea in vitro. GAFP-1 is a monomer with a

Qing Xu; Ying Liu; Xiaochen Wang; Hongya Gu; Zhangliang Chen

1998-01-01

251

In vitro antifungal activity of the berberine and its synergism with fluconazole  

Microsoft Academic Search

Berberine with and without fluconazole was tested by an agar disk diffusion assay in which clinical isolates of Candida albicans were applied onto yeast extract-peptone-dextrose agar plate. Berberine, which had no intrinsic antifungal activity at the\\u000a concentration tested, exerted a powerful antifungal activity in combination of fluzonazole. Combinations of berberine and\\u000a fluconazole were also tested by the checkerboard assay to

Renata Sayuri Iwazaki; Eliana Harue Endo; Tânia Ueda-Nakamura; Celso Vataru Nakamura; Lourdes Botelho Garcia; Benedito Prado Dias Filho

2010-01-01

252

Emperic Antifungal Therapy and Outcomes in Extremely-Low-Birth-Weight Infants with Invasive Candidiasis  

PubMed Central

Objective To assess the impact of emperic antifungal therapy of invasive candidiasis on subsequent outcomes in premature infants. Study design This was a cohort study of infants ?1000 g birth weight cared for at Neonatal Research Network sites. All infants had at least 1 positive culture for Candida. Emperic antifungal therapy was defined as receipt of a systemic antifungal on the day of or the day before the first positive culture for Candida was drawn. We created Cox proportional hazards and logistic regression models stratified on propensity score quartiles to determine the effect of emperic antifungal therapy on survival, time to clearance of infection, retinopathy of prematurity, bronchopulmonary dysplasia, end-organ damage, and neurodevelopmental impairment (NDI). Results 136 infants developed invasive candidiasis. The incidence of death or NDI was lower for infants who received emperic antifungal therapy (19/38, 50%) compared with those who had not (55/86, 64%; odds ratio=0.27 [95% confidence interval 0.08–0.86]). There was no significant difference between the groups for any single outcome or other combined outcomes. Conclusions Emperic antifungal therapy was associated with increased survival without NDI. A prospective randomized trial of this strategy is warranted. PMID:22424952

Greenberg, Rachel G.; Benjamin, Daniel K.; Gantz, Marie G.; Cotten, C. Michael; Stoll, Barbara J.; Walsh, Michele C.; Sánchez, Pablo J.; Shankaran, Seetha; Das, Abhik; Higgins, Rosemary D.; Miller, Nancy A.; Auten, Kathy J.; Walsh, T. J.; Laptook, Abbot R.; Carlo, Waldemar A.; Kennedy, Kathleen A.; Finer, Neil N.; Duara, Shahnaz; Schibler, Kurt; Ehrenkranz, Richard A.; Van Meurs, Krisa P.; Frantz, Ivan D.; Phelps, Dale L.; Poindexter, Brenda B.; Bell, Edward F.; O’Shea, T. Michael; Watterberg, Kristi L.; Goldberg, Ronald N.; Smith, P. Brian

2012-01-01

253

Changes in the proteome of Candida albicans in response to azole, polyene, and echinocandin antifungal agents.  

PubMed

The yeast Candida albicans is an opportunistic human fungal pathogen and the cause of superficial and systemic infections in immunocompromised patients. The classes of antifungal agents most commonly used to treat Candida infections are the azoles, polyenes, and echinocandins. In the present study, we identified changes in C. albicans protein abundance using two-dimensional polyacrylamide gel electrophoresis and matrix-assisted laser desorption ionization-time of flight mass spectroscopy following exposure to representatives of the azole (ketoconazole), polyene (amphotericin B), and echinocandin (caspofungin) antifungals in an effort to elucidate the adaptive responses to these classes of antifungal agents. We identified 39 proteins whose abundance changed in response to ketoconazole exposure. Some of these proteins are involved in ergosterol biosynthesis and are associated with azole resistance. Exposure to amphotericin B altered the abundance of 43 proteins, including those associated with oxidative stress and osmotic tolerance. We identified 50 proteins whose abundance changed after exposure to caspofungin, including enzymes involved in cell wall biosynthesis and integrity, as well as the regulator of beta-1,3-glucan synthase activity, Rho1p. Exposure to caspofungin also increased the abundance of the proteins involved in oxidative and osmotic stress. The common adaptive responses shared by all three antifungal agents included proteins involved in carbohydrate metabolism. Some of these antifungal-responsive proteins may represent potential targets for the development of novel therapeutics that could enhance the antifungal activities of these drugs. PMID:20145080

Hoehamer, Christopher F; Cummings, Edwin D; Hilliard, George M; Rogers, P David

2010-05-01

254

Antifungal activity of Zuccagnia punctata Cav.: evidence for the mechanism of action.  

PubMed

Petroleum ether and dichloromethane extracts of fruits, aerial parts and exudate of Zuccagnia punctata Cav. (Fabaceae) showed moderate antifungal activities against the yeasts C. albicans, S. cerevisiae and C. neoformans (MICs: 62.5 - 250 microg/mL) and very strong antifungal activities against the dermatophytes M. gypseum, T. rubrum and T. mentagrophytes (MICs: 8 - 16 microg/mL) thus supporting the ethnopharmacological use of this plant. Antifungal activity-directed fractionation of active extracts by using bioautography led to the isolation of 2',4'-dihydroxy-3'-methoxychalcone (1) and 2',4'-dihydroxychalcone (2) as the compounds responsible for the antifungal activity. Second-order studies included MIC (80), MIC (50) and MFC of both chalcones in an extended panel of clinical isolates of the most sensitive fungi, and also comprised a series of targeted assays. They showed that the most active chalcone 2 is fungicidal rather than fungistatic, does not disrupt the fungal membranes up to 4 x MFC and does not act by inhibiting the fungal cell wall. So, 2',4'-dihydroxychalcone would act by a different mechanism of action than the antifungal drugs in current clinical use, such as amphotericin B, azoles or echinocandins, and thus appears to be very promising as a novel antifungal agent. PMID:17628836

Svetaz, Laura; Agüero, María Belén; Alvarez, Sandra; Luna, Lorena; Feresin, Gabriela; Derita, Marcos; Tapia, Alejandro; Zacchino, Susana

2007-08-01

255

Establishment of a Novel Model of Onychomycosis in Rabbits for Evaluation of Antifungal Agents ?  

PubMed Central

We developed a novel model of onychomycosis in which we observed fungi in the deep layer of the nail, and we used the model to evaluate the efficacy of two topical antifungal drugs. To establish an experimental, in vivo model of onychomycosis, we applied Trichophyton mentagrophytes TIMM2789 to the nails of the hind limbs of rabbits that underwent steroid treatment. The nails were taken from the rabbits' feet at 0, 2, and 6 weeks after a 2-week infection. The localization of the fungi was evaluated histopathologically. Some fungi were seen to penetrate to the nail bed, and the infection rate in the sample at 0, 2, and 6 weeks after infection was 57, 87, and 93%, respectively. In addition, fungi proliferated and moved proximally into the nail plate in a manner that depended on the duration of infection. Second, using this model we evaluated antifungal efficacy both by the culture recovery method and histopathological examination. Two topical antifungal drugs, 8% ciclopirox nail lacquer and 5% amorolfine nail lacquer, were applied to the nail for 4 weeks in each group. On histopathological examination, two antifungal treatment groups showed no significant difference against the nontreated control group. However, there were a significantly low fungus-positive rate and intensity of the recovery of fungi on culture between antifungal treatment and nontreated control groups. We therefore suggest that we have established an in vivo model of onychomycosis that is useful for the evaluation of the efficacy of antifungal agents. PMID:21555762

Shimamura, Tsuyoshi; Kubota, Nobuo; Nagasaka, Saori; Suzuki, Taku; Mukai, Hideki; Shibuya, Kazutoshi

2011-01-01

256

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...

2013-07-01

257

40 CFR 180.443 - Myclobutanil; tolerances for residues.  

Code of Federal Regulations, 2010 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...

2010-07-01

258

Antifungal, phytotoxic and toxic metabolites produced by Penicillium purpurogenum.  

PubMed

Nine known metabolites, 6,8,1'-tri-O-methyl averantin (1), 6,8-di-O-methyl averufnin (2), 6,8-di-O-methyl averufanin (3), aversin (4), 1,3-dihydroxy-6,8-dimethoxy-9,10-anthraquinone (5), 6,8-di-O-methylnidurufin (6), 6,8-di-O-methyl versiconol (7), 5-methyoxysterigmatocystin (8) and (S)-ornidazole (9), were isolated from the extracts of Penicillium purpurogenum, and their structures were elucidated by using spectroscopic methods. The brine shrimp toxicity, anti-phytopathogenic and phytotoxic effects of these compounds were evaluated. Among them, compounds 1 and 8 exhibited the strongest toxicity against brine shrimp (Artemia salina), with lethality rates of 100% at a low concentration of 10 ?M, comparable to the positive control toosendanin. Compounds 1, 4 and 7 moderately inhibited the growth of Botrytis cinerea. Moreover, 4 displayed moderate antifungal effects on Gibberella saubinettii. In addition, compounds 6, 7 and 9 produced the phytotoxic effects on radish seedlings at 100 ?M. This is the first report on the isolation of these metabolites from this organism. PMID:25103412

Li, He; Wei, Jing; Pan, Shi-Yin; Gao, Jin-Ming; Tian, Jun-Mian

2014-12-01

259

Mono- and sesquiterpenes and antifungal constituents from Artemisia species.  

PubMed

In addition to beta-sitosterol and alpha-amyrin detected in all the investigated species, the extract of the aerial parts of Artemisia giraldii var. giraldii gave stigmasterol, daucosterol, sesamine, luteolin, eupafolin, hispidulin, eupatilin, belamcanidin, pinitol, artemin, ridentin, and a new antifungal monoterpene (named santolinylol) while that of the aerial parts of A. mongolica afforded sesamine, eupafolin, eupatilin, matricarin, and a new germacranolide (3-oxo-11 alpha H-germacra-1(10)E,4Z-dien-12,6 alpha-olide), and that of the aerial parts of A. vestita yielded stigmasterol, daucosterol, umbelliferone, scopolin, scoparone, and isoscopoletin-O-glucoside. Pinitol, first reisolated from Artemisia genus, was shown to inhibit the growth of the human pathogenic fungi Candida albicans, Aspergillus flavus, A. niger, Geotrichun candidum, Trichophyton rubrum, and Epidermophyton floccosum. Umbelliferone was also active against Candida tropicalis, A. flavus, G. candidum, T. rubrum, and E. floccosum. The flavones hispidulin and belamcanidin were almost equally inhibitory to the growth of A. flavus, G. candidum, T. rubrum, and E. floccosum, and santolinylol to C. albicans, A. flavus, A. niger, G. candidum, T. rubrum, and E. floccosum. In addition, ridentin was active against the growth of the plant pathogenic fungus Cladosporium cucumerinum. PMID:10083848

Tan, R X; Lu, H; Wolfender, J L; Yu, T T; Zheng, W F; Yang, L; Gafner, S; Hostettmann, K

1999-02-01

260

Antifungal activity of resveratrol derivatives against Candida species.  

PubMed

trans-Resveratrol (1a) is a phytoalexin produced by plants in response to infections by pathogens. Its potential activity against clinically relevant opportunistic fungal pathogens has previously been poorly investigated. Evaluated herein are the candidacidal activities of oligomers (2a, 3-5) of 1a purified from Vitis vinifera grape canes and several analogues (1b-1j) of 1a obtained through semisynthesis using methylation and acetylation. Moreover, trans-?-viniferin (2a), a dimer of 1a, was also subjected to methylation (2b) and acetylation (2c) under nonselective conditions. Neither the natural oligomers of 1a (2a, 3-5) nor the derivatives of 2a were active against Candida albicans SC5314. However, the dimethoxy resveratrol derivatives 1d and 1e exhibited antifungal activity against C. albicans with minimum inhibitory concentration (MIC) values of 29-37 ?g/mL and against 11 other Candida species. Compound 1e inhibited the yeast-to-hyphae morphogenetic transition of C. albicans at 14 ?g/mL. PMID:25014026

Houillé, Benjamin; Papon, Nicolas; Boudesocque, Leslie; Bourdeaud, Eric; Besseau, Sébastien; Courdavault, Vincent; Enguehard-Gueiffier, Cécile; Delanoue, Guillaume; Guérin, Laurence; Bouchara, Jean-Philippe; Clastre, Marc; Giglioli-Guivarc'h, Nathalie; Guillard, Jérôme; Lanoue, Arnaud

2014-07-25

261

Nest sanitation through defecation: antifungal properties of wood cockroach feces  

NASA Astrophysics Data System (ADS)

The wood cockroach Cryptocercus punctulatus nests as family units inside decayed wood, a substrate known for its high microbial load. We tested the hypothesis that defecation within their nests, a common occurrence in this species, reduces the probability of fungal development. Conidia of the entomopathogenic fungus, Metarhizium anisopliae, were incubated with crushed feces and subsequently plated on potato dextrose agar. Relative to controls, the viability of fungal conidia was significantly reduced following incubation with feces and was negatively correlated with incubation time. Although the cockroach's hindgut contained abundant ?-1,3-glucanase activity, its feces had no detectable enzymatic function. Hence, these enzymes are unlikely the source of the fungistasis. Instead, the antifungal compound(s) of the feces involved heat-sensitive factor(s) of potential microbial origin. When feces were boiled or when they were subjected to ultraviolet radiation and subsequently incubated with conidia, viability was "rescued" and germination rates were similar to those of controls. Filtration experiments indicate that the fungistatic activity of feces results from chemical interference. Because Cryptocercidae cockroaches have been considered appropriate models to make inferences about the factors fostering the evolution of termite sociality, we suggest that nesting in microbe-rich environments likely selected for the coupling of intranest defecation and feces fungistasis in the common ancestor of wood cockroaches and termites. This might in turn have served as a preadaptation that prevented mycosis as these phylogenetically related taxa diverged and evolved respectively into subsocial and eusocial organizations.

Rosengaus, Rebeca B.; Mead, Kerry; Du Comb, William S.; Benson, Ryan W.; Godoy, Veronica G.

2013-11-01

262

Chitinase A from Stenotrophomonas maltophilia shows transglycosylation and antifungal activities.  

PubMed

Stenotrophomonas maltophilia chitinase (StmChiA and StmChiB) genes were cloned and expressed as soluble proteins of 70.5 and 41.6 kDa in Escherichia coli. Ni-NTA affinity purified StmChiA and StmChiB were optimally active at pH 5.0 and 7.0, respectively and exhibited broad range pH activity. StmChiA and StmChiB had an optimum temperature of 40°C and are stable up to 50 and 40°C, respectively. Hydrolytic activity on chitooligosaccharides indicated that StmChiA was an endo-acting enzyme releasing chitobiose and StmChiB was both exo/endo-acting enzyme with the release of GlcNAc as the final product. StmChiA showed higher preference to ?-chitin and exhibited transglycosylation on even chain length tetra- and hexameric substrates. StmChiA, and not StmChiB, was active on chitinous polymers and showed antifungal activity against Fusarium oxysporum. PMID:23428818

Suma, Katta; Podile, Appa Rao

2013-04-01

263

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.  

PubMed

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 (IC(50) = 2.5 microM) 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 on Mono S. Lyophyllin possessed an N-terminal sequence with some similarity to those of plant ribosome-inactivating proteins. It inhibited translation in rabbit reticulocyte lysate with an IC(50) of 1 nM, thymidine uptake by murine splenocytes with an IC(50) of 1 microM and HIV-1 reverse transcriptase activity with an IC(50) of 7.9 nM. Lyophyllin did not manifest ribonuclease or hemagglutinating activity. An antifungal protein, designated Lyophyllum antifungal protein (LAP), with a molecular weight of 14 kDa, and an N-terminal sequence somewhat analogous to those of angiosperm thaumatin-like proteins and thaumatins and an inactive variant of the ubiquitin-conjugating enzyme, was first isolated from Lyophyllum shimeji. LAP was adsorbed on CM-cellulose, Affi-gel blue gel, and Mono S. LAP exerted antifungal activity against P. piricola (IC(50) = 70 nM) and Mycosphaerella arachidicola but not against Rhizoctonia solani, Colletotrichum gossypii, and Coprinus comatus. It exerted very low translation inhibitory activity in a rabbit reticulocyte lysate system (IC(50) = 70 microM) and negligible ribonuclease activity toward yeast transfer RNA and hemagglutinating activity toward rabbit erythrocytes. It inhibited HIV-1 reverse transcriptase with an IC(50) of about 5.2 nM. A synergism in antifungal activities of LAP and lyophyllin against P. piricola was demonstrable. PMID:11556814

Lam, S K; Ng, T B

2001-09-15

264

Comparison of in vitro antifungal activities of efinaconazole and currently available antifungal agents against a variety of pathogenic fungi associated with onychomycosis.  

PubMed

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. PMID:23318803

Jo Siu, William J; Tatsumi, Yoshiyuki; Senda, Hisato; Pillai, Radhakrishnan; Nakamura, Takashi; Sone, Daisuke; Fothergill, Annette

2013-04-01

265

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. PMID:23318803

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

2013-01-01

266

Determination of Antifungal Susceptibility Patterns Among the Clinical Isolates of Candida Species  

PubMed Central

Context: Candida species are opportunistic yeasts that cause infections ranging from simple dermatosis to potentially life-threatening fungemia. The emergence of resistance to antifungal drugs has been increased in the past two decades. Aim: the present study we determined to find out the susceptibility profiles of clinical isolates of Candida species against four antifungal drugs, including amphotericin B, ketoconazole, fluconazole and itraconazole. Materials and Methods: Antifungal susceptibility testing of the yeasts was done in accordance with the proposed guidelines for antifungal disk diffusion susceptibility testing of yeasts based on the CLSI document M44-A. Results: A total of 206 yeast isolates were assessed. Among the evaluated Candida species, the highest rates of resistance to ketoconazole were seen in Candida glabrata (16.6%) and Candida albicans (3.2%). Susceptibility and intermediate response to fluconazole were seen in 96.6% and 3.4% of the Candida isolates, respectively. A total of 19 (9.2%) yeast isolates showed petite phenomenon including 11 C. glabrata, 3 C. albicans, 2 Candida dubliniensis and one isolate of each Candida krusei and Candida parapsilosis. Conclusion: The high number of petite mutation in the isolated yeasts should be seriously considered since it may be one of the reasons of antifungal treatment failure. PMID:22223999

Zomorodian, Kamiar; Rahimi, Mohammad Javad; Pakshir, Kayvan; Motamedi, Marjan; Ghiasi, Moosa Rahimi; Rezashah, Hasanein

2011-01-01

267

In vitro activity of E1210, a novel antifungal, against clinically important yeasts and molds.  

PubMed

E1210 is a new antifungal compound with a novel mechanism of action and broad spectrum of antifungal activity. We investigated the in vitro antifungal activities of E1210 compared to those of fluconazole, itraconazole, voriconazole, amphotericin B, and micafungin against clinical fungal isolates. E1210 showed potent activities against most Candida spp. (MIC(90) of ?0.008 to 0.06 ?g/ml), except for Candida krusei (MICs of 2 to >32 ?g/ml). E1210 showed equally potent activities against fluconazole-resistant and fluconazole-susceptible Candida strains. E1210 also had potent activities against various filamentous fungi, including Aspergillus fumigatus (MIC(90) of 0.13 ?g/ml). E1210 was also active against Fusarium solani and some black molds. Of note, E1210 showed the greatest activities against Pseudallescheria boydii (MICs of 0.03 to 0.13 ?g/ml), Scedosporium prolificans (MIC of 0.03 ?g/ml), and Paecilomyces lilacinus (MICs of 0.06 ?g/ml) among the compounds tested. The antifungal action of E1210 was fungistatic, but E1210 showed no trailing growth of Candida albicans, which has often been observed with fluconazole. In a cytotoxicity assay using human HK-2 cells, E1210 showed toxicity as low as that of fluconazole. Based on these results, E1210 is likely to be a promising antifungal agent for the treatment of invasive fungal infections. PMID:21825291

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

2011-10-01

268

In vitro antifungal activity of three geophytic plant extracts against three post-harvest pathogenic fungi.  

PubMed

Plant extracts appear to be one of the most effective alternative methods of plant diseases control which are less harmful to human beings and environment. In vitro antifungal activity of methanolic extracts of three promising wild geophytic plants against three post-harvest pathogenic fungi using radial growth technique was conducted. These extracts included the shoot system (S) and underground parts (R) of Asparagus stipularis, Cyperus capitatus and Stipagrostis lanata. The tested fungi were Alternaria solani, Aspergillus niger and Rhizopus stolonifer. The results exhibited that, all plant extracts had antifungal activity against the tested fungi. The antifungal activity greatly varied depending on plant parts and/or plant species. R. stolonifer was the most susceptible fungus to the tested plant extracts followed by A. niger and then A. solani. On the other hand, the most effective plant extracts against tested fungi were S. lanata (S) and A. stipularis (R). The most effective plant extracts against R. stolonifer were S. lanata (R) and C. capitatus (S). While, the extracts of A. stipularis (R) and S. lanata (S) were the most effective against A. niger. The extracts of C. capitatus (S) and S. lanata (S) exhibited the highest antifungal activity against A. solani. The results demonstrated that, the methanolic extracts of A. stipularis, C. capitatus and S. lanata had potential antifungal activity against A. solani, A. niger and R. stolonifer. PMID:24506036

Maswada, Hanafey F; Abdallah, Sabry A

2013-12-01

269

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

PubMed

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

2013-08-15

270

Gastrodianin-like mannose-binding proteins: a novel class of plant proteins with antifungal properties.  

PubMed

The orchid Gastrodia elata depends on the fungus Armillaria mellea to complete its life cycle. In the interaction, fungal hyphae penetrate older, nutritive corms but not newly formed corms. From these corms, a protein fraction with in vitro activity against plant-pathogenic fungi has previously been purified. Here, the sequence of gastrodianin, the main constituent of the antifungal fraction, is reported. Four isoforms that encoded two different mature proteins were identified at the cDNA level. Another isoform was detected in sequenced peptides. Because the antifungal activity of gastrodianins produced in and purified from Escherichia coli and Nicotiana tabacum was comparable to that of gastrodianin purified from the orchid, gastrodianins are the active component of the antifungal fractions. Gastrodianin accumulation is probably an important part of the mechanism by which the orchid controls Armillaria penetration. Gastrodianin was found to be homologous to monomeric mannose-binding proteins of other orchids, of which at least one (Epipactis helleborine mannose-binding protein) also displayed in vitro antifungal activity. This establishes the gastrodianin-like proteins (GLIPs) as a novel class of antifungal proteins. PMID:11319032

Wang, X; Bauw, G; Van Damme, E J; Peumans, W J; Chen, Z L; Van Montagu, M; Angenon, G; Dillen, W

2001-03-01

271

Expression in Escherichia coli, purification, refolding and antifungal activity of an osmotin from Solanum nigrum  

PubMed Central

Background Heterologous protein expression in microorganisms may contribute to identify and demonstrate antifungal activity of novel proteins. The Solanum nigrum osmotin-like protein (SnOLP) gene encodes a member of pathogenesis-related (PR) proteins, from the PR-5 sub-group, the last comprising several proteins with different functions, including antifungal activity. Based on deduced amino acid sequence of SnOLP, computer modeling produced a tertiary structure which is indicative of antifungal activity. Results To validate the potential antifungal activity of SnOLP, a hexahistidine-tagged mature SnOLP form was overexpressed in Escherichia coli M15 strain carried out by a pQE30 vector construction. The urea solubilized His6-tagged mature SnOLP protein was affinity-purified by immobilized-metal (Ni2+) affinity column chromatography. As SnOLP requires the correct formation of eight disulfide bonds, not correctly formed in bacterial cells, we adapted an in vitro method to refold the E. coli expressed SnOLP by using reduced:oxidized gluthatione redox buffer. This method generated biologically active conformations of the recombinant mature SnOLP, which exerted antifungal action towards plant pathogenic fungi (Fusarium solani f. sp.glycines, Colletotrichum spp., Macrophomina phaseolina) and oomycete (Phytophthora nicotiana var. parasitica) under in vitro conditions. Conclusion Since SnOLP displays activity against economically important plant pathogenic fungi and oomycete, it represents a novel PR-5 protein with promising utility for biotechnological applications. PMID:18334031

Campos, Magnolia de A; Silva, Marilia S; Magalhaes, Claudio P; Ribeiro, Simone G; Sarto, Rafael PD; Vieira, Eduardo A; Grossi de Sa, Maria F

2008-01-01

272

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

PubMed Central

Topical application of antifungals does not have predictable or well-controlled release characteristics and requires reapplication to achieve therapeutic local concentration in a reasonable time period. In this article, the efficacy of five different US Food and Drug Administration-approved antifungal-loaded (amphotericin B, natamycin, terbinafine, fluconazole, and itraconazole) electrospun gelatin fiber mats were compared. Morphological studies show that incorporation of polyenes resulted in a two-fold increase in fiber diameter and the mats inhibit the growth of yeasts and filamentous fungal pathogens. Terbinafine-loaded mats were effective against three filamentous fungal species. Among the two azole antifungals compared, the itraconazole-loaded mat was potent against Aspergillus strains. However, activity loss was observed for fluconazole-loaded mats against all of the test organisms. The polyene-loaded mats displayed rapid candidacidal activities as well. Biophysical and rheological measurements indicate strong interactions between polyene antifungals and gelatin matrix. As a result, the polyenes stabilized the triple helical conformation of gelatin and the presence of gelatin decreased the hemolytic activity of polyenes. The polyene-loaded fiber mats were noncytotoxic to primary human corneal and sclera fibroblasts. The reduction of toxicity with complete retention of activity of the polyene antifungal-loaded gelatin fiber mats can provide new opportunities in the management of superficial skin infections. PMID:24920895

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

2014-01-01

273

Antifungal compounds from Melia azedarach leaves for management of Ascochyta rabiei, the cause of chickpea blight.  

PubMed

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 (4), 3,5 dimethoxybenzoic acid (5) and maesol (6) were isolated from the chloroform fraction through column chromatography. The in vitro antifungal activity of compounds 2-5 was evaluated against A. rabiei. A commercial fungicide, mancozeb, was used as a positive control. Different concentrations of mancozeb and the isolated compounds, ranging from 0.0039 to 4 mg mL(-1), were used in the antifungal bioassay, and data regarding minimum inhibitory concentration (MIC) was recorded 24, 48 and 72 h after incubation. All concentrations of mancozeb inhibited the fungal spore germination at all three incubation periods. The tested compounds exhibited variable antifungal activity against the target fungal pathogens. All compounds showed their highest antifungal activity after 24 h of incubation. Compound 2 was found to be the most effective, with an MIC of 0.0156 mg mL(-1), followed by compounds 3, 4 and 5, with MIC values of 0.0312, 0.25 and 0.125 mg mL(-1), respectively. PMID:20628965

Jabeen, Khajista; Javaid, Arshad; Ahmad, Ejaz; Athar, Makshoof

2011-02-01

274

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

PubMed

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

2013-10-01

275

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

2005-01-01

276

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

2010-01-01

277

Extraction of Antifungal Substances from Burkholderia cepacia with Antibiotic Activity against Colletotrichum gloeosporioides on Papaya (Carica papaya)  

Microsoft Academic Search

An experiment was conducted to extract and determine the nature of antifungal substances produced by Burkholderia cepacia strain B23 that were inhibitory towards Colletotrichum gloeosporioides. In addition, the effect of different culture media on the production of antifungal substances by B. cepacia B23 was also investigated to have improved efficacy of this biocontrol agent. B. cepacia B23 grew faster in

J. KADIR; M. A. RAHMAN; T. M. M. MAHMUD; R. ABDUL RAHMAN; M. M. BEGUM

278

Antifungal cyclic peptides from the terrestrial blue-green alga Anabaena laxa. I. Isolation and biological properties.  

PubMed

Laxaphycins are responsible for the antifungal and cytotoxic activity of crude ethanolic extracts from the cultured blue-green alga Anabaena laxa. These cyclic peptides exhibit an unusual biological synergism when tested for antifungal or cytotoxic effects. The isolation procedure for the peptides, their characterization and biological activities are described here along with experiments demonstrating synergism between the two major laxaphycins. PMID:1429231

Frankmölle, W P; Larsen, L K; Caplan, F R; Patterson, G M; Knübel, G; Levine, I A; Moore, R E

1992-09-01

279

Seasonal variations in the production of antifungal substances by some dictyotales (brown algae) from the french mediterranean coast  

Microsoft Academic Search

Hexane extracts of some algae belonging to the Dictyotales collected over a 12 month period were tested for their antifungal activity using human pathogenic fungi (yeasts, moulds and dermatophytes) and phytopathogenic fungi responsible for diseases in Mediterranean plants and trees. The three algal species tested (Dictyota dichotoma, Dictyota dichotoma var. implexa, Dilophus spiralis) exhibited a wide spectrum of antifungal activity

J. Moreau; D. Pesando; P. Bernard; B. Caram; J. C. Pionnat

1988-01-01

280

Haliscosamine: a new antifungal sphingosine derivative from the Moroccan marine sponge Haliclona viscosa.  

PubMed

In the aim of searching for new antifungal products from marine origin, we have isolated a sphingosine derivative, (9Z)-2-amino-docos-9-ene-1,3,13,14-tetraol (Haliscosamine) from the Moroccan sea sponge Haliclona viscosa using bio-guided (antifungal) HPLC methods. The molecular structure of this compound was elucidated by spectrometric techniques IR, UV, MS and NMR. The isolated metabolite showed a significant antifungal activity against Cryptococcus and Candida species and a weak general toxicity in the brine shrimp lethality test. Further research is needed to study its in vivo activity, as well as to elucidate the mechanism underlying its activity in the hope of a future use in medical mycology. PMID:23961377

El-Amraoui, Belkassem; Biard, Jean-Fançois; Fassouane, Aziz

2013-01-01

281

Synthesis, Antifungal Activity, and Structure Activity Relationships of Coruscanone A Analogs  

PubMed Central

Coruscanone A, a plant derived cyclopentenedione derivative, showed potent in vitro antifungal activity against Candida albicans and Cryptococcus neoformans, comparable to amphotericin B and fluconazole. A series of analogs have been synthesized by modification of the cyclopentenedione ring, the enolic methoxy functionality, and the side chain styryl moiety of this natural product lead. A structurally close 1,4-benzoquinone analog was also prepared. All the compounds were examined for their in vitro activity against major opportunistic fungal pathogens including C. albicans, C. neoformans and Aspergillus fumigatus, and fluconazole-resistant C. albicans strains, with several analogs demonstrating potent antifungal activity. Structure activity relationship studies indicate that the 2-methoxymethylene-cyclopent-4-ene-1,3-dione structural moiety is the pharmacophore responsible for the antifungal activity of this class of compounds, while the side chain styryl-like moiety plays an important complementary role, presumably contributing to target binding. PMID:17181171

Babu, K. Suresh; Li, Xing-Cong; Jacob, Melissa R.; Zhang, Qifeng; Khan, Shabana I.; Ferreira, Daneel; Clark, Alice M.

2008-01-01

282

Synthesis and antifungal properties of (4-tolyloxy)-pyrimidyl-?-aminophosphonates chitosan derivatives.  

PubMed

A novel class of ?-aminophosphonate chitosan derivatives was investigated. These chitosan derivatives consist of (4-tolyloxy)-pyrimidyl-dimethyl-?-amino-phosphonate chitosan (?-ATPMCS) and (4-tolyloxy)-pyrimidyl-diethyl-?-aminophosphonate chitosan (?-ATPECS). Their structures were well defined. Antifungal activity of them against some crop-threatening pathogenic fungi was tested in vitro. The derivatives were found to have a broad-spectrum antifungal activity that was obviously enhanced compared with chitosan. At 250 mg/L, both ?-ATPMCS and ?-ATPECS even inhibited growth of Phomopsis asparagi (Sacc.) (P. asparagi) and Fusarium oxysporum (F. oxysporum) at 100%, which was even stronger than polyoxin whose antifungal index was 37.2% and 32.1%, respectively. Additionally, the initial mechanism of the chitosan derivatives in F. oxysporum model was studied. It was found that the derivatives may have an effect on membrane permeability of the fungi. The results demonstrated the derivatives may serve as attractive candidates in crop protection. PMID:24183805

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

2014-02-01

283

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

PubMed

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

2012-01-01

284

Facile fabrication of graphene oxide loaded with silver nanoparticles as antifungal materials  

NASA Astrophysics Data System (ADS)

Graphene oxide loaded silver nanoparticles (GO-Ag) were synthesized using a simple method. Our evidence showed that silver nanoparticles (Ag NPs) were successfully loaded on the surface of graphene oxide sheets. The antifungal property of GO-Ag composites was investigated. The results revealed that the obtained GO-Ag composites exhibit enhanced antifungal property in comparison with that of Ag NPs. The toxicity of GO-Ag and Ag NPs were systematically evaluated. The study of cell viability, lactate dehydrogenase, reactive oxygen species, apoptosis/necrosis and hemolysis revealed that GO-Ag composites have lower cytotoxicity and better blood compatibility than Ag NPs. Therefore, these findings provide nanotoxicological information regarding GO-Ag composites which may be alternative antifungal materials in their application of biomedical fields.

Cui, Jianghu; Yang, Yunhua; Zheng, Mingtao; Liu, Yingliang; Xiao, Yong; Lei, Bingfu; Chen, Wei

2014-12-01

285

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

PubMed Central

The genus Candida includes about 200 different species, but only a few species are human opportunistic pathogens and cause infections when the host becomes debilitated or immunocompromised. Candida infections can be superficial or invasive. Superficial infections often affect the skin or mucous membranes and can be treated successfully with topical antifungal drugs. However, invasive fungal infections are often life-threatening, probably due to inefficient diagnostic methods and inappropriate initial antifungal therapies. Here, we briefly review our current knowledge of pathogenic species of the genus Candida and yeast infection causes and then focus on current antifungal drugs and resistance mechanisms. An overview of new therapeutic alternatives for the treatment of Candida infections is also provided. PMID:23878798

Spampinato, Claudia

2013-01-01

286

Sertaconazole: an antifungal agent for the topical treatment of superficial candidiasis.  

PubMed

Sertaconazole is a useful antifungal agent against mycoses of the skin and mucosa, such as cutaneous, genital and oral candidiasis and tinea pedis. Its antifungal activity is due to inhibition of the ergosterol biosynthesis and disruption of the cell wall. At higher concentrations, sertaconazole is able to bind to nonsterol lipids of the fungal cell wall, increasing the permeability and the subsequent death of fungal cells. Fungistatic and fungicidal activities on Candida are dose-dependent. The antifungal spectrum of sertaconazole includes deramophytes, Candida, Cryptococcus, Malassezia and also Aspergillus, Scedosporium and Scopulariopsis. Sertaconazole also shows an antimicrobial activity against streptococci, staphylococci and protozoa (Trichomonas). In clinical trials including patients with vulvovaginal candidiasis, a single dose of sertaconazole produced a higher cure rate compared with other topical azoles such as econazole and clotrimazole, in shorter periods. Sertaconazole has shown an anti-inflammatory effect that is very useful for the relief of unpleasant symptoms. PMID:23566144

Carrillo-Muñoz, Alfonso Javier; Tur-Tur, Cristina; Giusiano, Gustavo; Marcos-Arias, Cristina; Eraso, Elena; Jauregizar, Nerea; Quindós, Guillermo

2013-04-01

287

Human neutrophil-mediated nonoxidative antifungal activity against Cryptococcus neoformans.  

PubMed

It has long been appreciated that polymorphonuclear leukocytes (PMN) kill Cryptococcus neoformans, at least in part via generation of fungicidal oxidants. The aim of this study was to examine the contribution of nonoxidative mechanisms to the inhibition and killing of C. neoformans. Treatment of human PMN with inhibitors and scavengers of respiratory burst oxidants only partially reversed anticryptococcal activity, suggesting that both oxidative and nonoxidative mechanisms were operative. To define the mediators of nonoxidative anticryptococcal activity, PMN were fractionated into cytoplasmic, primary (azurophil) granule, and secondary (specific) granule fractions. Incubation of C. neoformans with these fractions for 18 h resulted in percent inhibition of growth of 67.4 +/- 3.4, 84.6 +/- 4.4, and 29.2 +/- 10.5 (mean +/- standard error, n = 3), respectively. Anticryptococcal activity of the cytoplasmic fraction was abrogated by zinc and depletion of calprotectin. Antifungal activity of the primary granules was significantly reduced by pronase treatment, boiling, high ionic strength, and magnesium but not calcium. Fractionation of the primary granules by reverse phase high-pressure liquid chromatography on a C(4) column over an acetonitrile gradient revealed multiple peaks with anticryptococcal activity. Of these, peaks 1 and 6 had substantial fungistatic and fungicidal activity. Peak 1 was identified by acid-urea polyacrylamide gel electrophoresis (PAGE) and mass spectroscopy as human neutrophil proteins (defensins) 1 to 3. Analysis of peak 6 by sodium dodecyl sulfate-PAGE revealed multiple bands. Thus, human PMN have nonoxidative anticryptococcal activity residing principally in their cytoplasmic and primary granule fractions. Calprotectin mediates the cytoplasmic activity, whereas multiple proteins, including defensins, are responsible for activity of the primary granules. PMID:11035733

Mambula, S S; Simons, E R; Hastey, R; Selsted, M E; Levitz, S M

2000-11-01

288

Laccase catalyzed synthesis of iodinated phenolic compounds with antifungal activity.  

PubMed

Iodine is a well known antimicrobial compound. Laccase, an oxidoreductase which couples the one electron oxidation of diverse phenolic and non-phenolic substrates to the reduction of oxygen to water, is capable of oxidizing unreactive iodide to reactive iodine. We have shown previously that laccase-iodide treatment of spruce wood results in a wash-out resistant antimicrobial surface. In this study, we investigated whether phenolic compounds such as vanillin, which resembles sub-structures of softwood lignin, can be directly iodinated by reacting with laccase and iodide, resulting in compounds with antifungal activity. HPLC-MS analysis showed that vanillin was converted to iodovanillin by laccase catalysis at an excess of potassium iodide. No conversion of vanillin occurred in the absence of enzyme. The addition of redox mediators in catalytic concentrations increased the rate of iodide oxidation ten-fold and the yield of iodovanillin by 50%. Iodinated phenolic products were also detected when o-vanillin, ethyl vanillin, acetovanillone and methyl vanillate were incubated with laccase and iodide. At an increased educt concentration of 0.1 M an almost one to one molar ratio of iodide to vanillin could be used without compromising conversion rate, and the insoluble iodovanillin product could be recovered by simple centrifugation. The novel enzymatic synthesis procedure fulfills key criteria of green chemistry. Biocatalytically produced iodovanillin and iodo-ethyl vanillin had significant growth inhibitory effects on several wood degrading fungal species. For Trametes versicolor, a species causing white rot of wood, almost complete growth inhibition and a partial biocidal effect was observed on agar plates. Enzymatic tests indicated that the iodinated compounds acted as enzyme responsive, antimicrobial materials. PMID:24594755

Ihssen, Julian; Schubert, Mark; Thöny-Meyer, Linda; Richter, Michael

2014-01-01

289

Antifungal drug resistance evoked via RNAi-dependent epimutations.  

PubMed

Microorganisms evolve via a range of mechanisms that may include or involve sexual/parasexual reproduction, mutators, aneuploidy, Hsp90 and even prions. Mechanisms that may seem detrimental can be repurposed to generate diversity. Here we show that the human fungal pathogen Mucor circinelloides develops spontaneous resistance to the antifungal drug FK506 (tacrolimus) via two distinct mechanisms. One involves Mendelian mutations that confer stable drug resistance; the other occurs via an epigenetic RNA interference (RNAi)-mediated pathway resulting in unstable drug resistance. The peptidylprolyl isomerase FKBP12 interacts with FK506 forming a complex that inhibits the protein phosphatase calcineurin. Calcineurin inhibition by FK506 blocks M. circinelloides transition to hyphae and enforces yeast growth. Mutations in the fkbA gene encoding FKBP12 or the calcineurin cnbR or cnaA genes confer FK506 resistance and restore hyphal growth. In parallel, RNAi is spontaneously triggered to silence the fkbA gene, giving rise to drug-resistant epimutants. FK506-resistant epimutants readily reverted to the drug-sensitive wild-type phenotype when grown without exposure to the drug. The establishment of these epimutants is accompanied by generation of abundant fkbA small RNAs and requires the RNAi pathway as well as other factors that constrain or reverse the epimutant state. Silencing involves the generation of a double-stranded RNA trigger intermediate using the fkbA mature mRNA as a template to produce antisense fkbA RNA. This study uncovers a novel epigenetic RNAi-based epimutation mechanism controlling phenotypic plasticity, with possible implications for antimicrobial drug resistance and RNAi-regulatory mechanisms in fungi and other eukaryotes. PMID:25079329

Calo, Silvia; Shertz-Wall, Cecelia; Lee, Soo Chan; Bastidas, Robert J; Nicolás, Francisco E; Granek, Joshua A; Mieczkowski, Piotr; Torres-Martínez, Santiago; Ruiz-Vázquez, Rosa M; Cardenas, Maria E; Heitman, Joseph

2014-09-25

290

In Vitro and In Vivo antifungal activities of selected Cameroonian dietary spices  

PubMed Central

Background Spices and herbs have been used in food since ancient times to give taste and flavor and also as food preservatives and disease remedies. In Cameroon, the use of spices and other aromatic plants as food flavoring is an integral part of dietary behavior, but relatively little is known about their antifungal potential. The present work was designed to assess the antifungal properties of extracts from spices used in Cameroonian dietary. Methods The in vitro antifungal activities of twenty three extracts from twenty one spices were assessed by the broth micro-dilution method against eight fungi. Also, the in vivo activity of Olax subscorpioidea extract (the most active extract) was evaluated in rat model of disseminated candidiasis due to Candida albicans by estimating the fungal burden in blood and kidney. Results Seven extracts (30%) exhibited moderate to significant antifungal activities, inhibiting the growth of the microorganisms at concentrations ranging from 0.048 to 0.39 mg/mL. Olax subscorpioidea extract exhibited the highest antifungal activity particularly against?Candida albicans and Candida tropicalis (MIC of 0.097 mg/mL and 0.048 mg/mL respectively). Sixteen extracts (70%) were weakly active (MICs?>?6.25 mg/mL). Oral administration of O. subscorpioidea extract at the dose 2 g/kg of body weight (bw) to artificially infected rats revealed a drop in the number of colony forming units per milliliter (cfu/mL) of Candida albicans cells in the blood below the detection limit (100 cfu/mL) while a modest decrease was observed in the kidney. Conclusion The present work shows that some of the spices studied possess interesting antifungal properties and could be used to treat candidiasis. Among the plant species tested, Olax subscorpioidea displayed the most promising result. PMID:24533718

2014-01-01

291

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. PMID:6870217

Caporaso, N; Smith, S M; Eng, R H

1983-01-01

292

Experimental and theoretical approach of nanocrystalline TiO2 with antifungal activity  

NASA Astrophysics Data System (ADS)

Using a solvothermal method for this research we synthesized nanocrystalline titanium dioxide (nc-TiO2) anatase particles with a mean diameter of 5.4 nm and evaluated their potential antifungal effect against planktonic cells of Candida albicans without UV radiation. To complement experimental data, we analyzed structural and electronic properties of both the bulk and the (1 0 1) surface of anatase by first-principles calculations. Based on experimental and theoretical results, a reactive O2H and OH species formation mechanism was proposed to explain the key factor which facilitates the antifungal activity.

Longo, Valeria M.; Picon, Francini C.; Zamperini, Camila; Albuquerque, Anderson R.; Sambrano, Julio R.; Vergani, Carlos E.; Machado, Ana L.; Andrés, Juan; Hernandes, Antônio C.; Varela, José A.; Longo, Elson

2013-07-01

293

Bioactivity guided isolation of antifungal compounds from the liverwort Bazzania trilobata (L.) S.F. Gray.  

PubMed

A dichloromethane and a methanol extract of the liverwort Bazzania trilobata showed antifungal activity against the phytopathogenic fungi Botrytis cinerea, Cladosporium cucumerinum, Phythophthora infestans, Pyricularia oryzae and Septoria tritici. Bioautography on thin-layer chromatograms was used to isolate six antifungal sesquiterpenes: 5- and 7-hydroxycalamenene, drimenol, drimenal, viridiflorol, gymnomitrol and three bisbibenzyls: 6 ',8'-dichloroisoplagiochin C, isoplagiochin D and 6'-chloroisoplagiochin D. Furthermore we report the isolation of gymnomitr-8(12)-en-4-one and the new coumarin 7,8-dihydroxycoumarin-7-O-beta-D-glucuronide. Their structures have been elucidated based on extensive NMR spectral evidence. PMID:15451321

Scher, Jochen M; Speakman, John-Bryan; Zapp, Josef; Becker, Hans

2004-09-01

294

An antifungal protein from the culinary-medicinal beech mushroom, Hypsizygus marmoreus (Peck) Bigel. (Agaricomycetideae).  

PubMed

An antifungal protein (HM-af) was purified from the culinary-medicinal mushroom Hypsizygus marmoreus. The results of sodium dodecyl sulfate polyacrylamide gel electrophoresis and matrix-assisted laser desorption ionization time-of-flight mass spectrometry of HM-af indicated that its molecular mass was 9.5 kDa. The N-terminal amino acid sequence of HM-af showed homology to ribonuclease H from Clostridium thermocellum. HM-af showed the antifungal activity against Flammulina velutipes. PMID:22135901

Suzuki, Tomohiro; Umehara, Kanako; Tashiro, Ai; Kobayashi, Yuka; Dohra, Hideo; Hirai, Hirofumi; Kawagishi, Hirokazu

2011-01-01

295

KB425796-A, a novel antifungal antibiotic produced by Paenibacillus sp. 530603.  

PubMed

The novel antifungal macrocyclic lipopeptidolactone, KB425796-A (1), was isolated from the fermentation broth of bacterial strain 530603, which was identified as a new Paenibacillus species based on morphological and physiological characteristics, and 16S rRNA sequences. KB425796-A (1) was isolated as white powder by solvent extraction, HP-20 and ODS-B column chromatography, and lyophilization, and was determined to have the molecular formula C79H115N19O18. KB425796-A (1) showed antifungal activities against Aspergillus fumigatus and the micafungin-resistant infectious fungi Trichosporon asahii, Rhizopus oryzae, Pseudallescheria boydii and Cryptococcus neoformans. PMID:23778117

Kai, Hirohito; Yamashita, Midori; Takase, Shigehiro; Hashimoto, Michizane; Muramatsu, Hideyuki; Nakamura, Ikuko; Yoshikawa, Koji; Ezaki, Masami; Nitta, Kumiko; Watanabe, Masato; Inamura, Noriaki; Fujie, Akihiko

2013-08-01

296

Alveolarin, a novel antifungal polypeptide from the wild mushroom Polyporus alveolaris.  

PubMed

An antifungal polypeptide, with a molecular mass of 28 kDa as judged by gel filtration and appearing as a single band with a molecular mass of 14 kDa in sodium dodecyl suflate-polyacrylamide gel electrophoresis, was isolated from fresh fruiting bodies of the mushroom Polyporus alveolaris. The antifungal polypeptide, designated as alveolarin, demonstrated an inhibitory action on mycelial growth in Botrytis cinerea, Fusarium oxysporum, Mycosphaerella arachidicola and Physalospora piricola. Alveolarin was isolated with a procedure that entailed ion exchange chromatography on DEAE-cellulose, affinity chromatography on Affi-gel blue gel, and gel filtration on Superdex 75 by fast protein liquid chromatography. PMID:15165727

Wang, Hexiang; Ng, T B; Liu, Qinghong

2004-04-01

297

The antibacterial and antifungal activity of a soda-lime glass containing silver nanoparticles.  

PubMed

The antibacterial and antifungal activity of a low melting point soda-lime glass powder containing silver nanoparticles has been studied. Nano-Ag sepiolite fibres containing monodispersed silver nanoparticles (d(50) approximately 11 +/- 9 nm) were used as the source of silver. This powder presents a high antibacterial (against gram-positive and gram-negative bacteria) as well as antifungal (against I. orientalis) activity. The observed high activity against yeast has been explained by considering the inhibitory effect of the Ca(2+) lixiviated from the glass on the growth of the yeast colonies. PMID:19417439

Esteban-Tejeda, L; Malpartida, F; Esteban-Cubillo, A; Pecharromán, C; Moya, J S

2009-02-25

298

[Could antifungal lock be useful in the management of candidiasis linked with catheters?].  

PubMed

Fungal biofilms associated with inserted medical devices such as catheters, represent a major risk factor for candidemia. In addition, these biofilm yeasts show a decreased susceptibility to antifungal agents. Recently, a new therapeutic approach has emerged, the "lock therapy", based on the use of high concentrations of antimicrobials, instilled into the lumen of the catheter and left in place for 8 to 12 h. In vitro or in vivo studies have evaluated the interest of antifungal locks using amphotericin B, an azole or echinocandins. The promising results will permit us to discuss the relevance of this technique. PMID:22920876

Cateau, Estelle; Rodier, Marie-Hélène; Imbert, Christine

2012-01-01

299

Universal antifungal therapy is not needed in persistent febrile neutropenia: a tailored diagnostic and therapeutic approach  

PubMed Central

Background Giving antifungal therapy exclusively to selected patients with persistent febrile neutropenia may avoid over-treatment without increasing mortality. The aim of this study was to validate an innovative diagnostic and therapeutic approach based on assessing patients’ risk profile and clinical criteria in order to select those patients requiring antifungal therapy. The efficacy of this approach was compared to that of universal empirical antifungal therapy. Design and Methods This was a prospective study which included all consecutive adult hematology patients with neutropenia and fever refractory to 5 days of empirical antibacterial therapy admitted to a teaching hospital in Spain over a 2-year period. A diagnostic and therapeutic approach based on clinical criteria and risk profile was applied in order to select patients for antifungal therapy. The sensitivity, specificity and negative predictive value of this approach and also the overall success rate, according to the same criteria of efficacy described in classical clinical trials, were analyzed. Results Eighty-five episodes were included, 35 of them (41.2%) in patients at high risk of invasive fungal infections. Antifungal therapy was not indicated in 33 episodes (38.8%). The overall incidence of proven and probable invasive fungal infections was 14.1%, all of which occurred in patients who had received empirical antifungal therapy. The 30-day crude mortality rate was 15.3% and the invasive fungal infection-related mortality rate was 2.8% (2/72). The overall success rate following the diagnostic and therapeutic approach was 36.5% compared with 33.9% and 33.7% obtained in the trial by Walsh et al. The sensitivity, specificity and negative predictive value of the study approach were 100%, 52.4% and 100%, respectively. Conclusions Based on the high negative predictive value of this diagnostic and therapeutic approach in persistent febrile neutropenia patients with hematologic malignancies or patients who have received a hematopoietic stem cell transplant, the approach is useful for identifying patients who are not likely to develop invasive fungal infection and do not, therefore, require antifungal therapy. The effectiveness of the strategy is similar to that of universal empirical antifungal therapy reported in controlled trials. PMID:22058202

Aguilar-Guisado, Manuela; Martin-Pena, Almudena; Espigado, Ildefonso; Ruiz Perez de Pipaon, Maite; Falantes, Jose; de la Cruz, Fatima; Cisneros, Jose M.

2012-01-01

300

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. PMID:22829829

Ing, Ling Yien; Zin, Noraziah Mohamad; Sarwar, Atif; Katas, Haliza

2012-01-01

301

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

2003-01-01

302

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

DAVID GEORGE; PEGGY MINITER; ANDVINCENT T. ANDRIOLE

1996-01-01

303

Resistant P45051A1 activity in azole antifungal tolerant Cryptococcus neoformans from AIDS patients  

Microsoft Academic Search

Azole antifungal compounds are important in the treatment of Cryptococcosis, a major cause of mortality in AIDS patients. The target of the azole drugs is P450 mediated sterol 14?-demethylase. We have investigated the P450 system of Cryptococcus neoformans with respect to azole tolerance observed in clinical isolates which were obtained following the failure of fluconazole therapy. The clinical failure was

D. C. Lamb; A. Corran; B. C. Baldwin; J. Kwon-Chung; S. L. Kelly

1995-01-01

304

In vitro antifungal activity of sanguinarine and chelerythrine derivatives against phytopathogenic fungi.  

PubMed

In order to understand the antifungal activity of some derivatives of sanguinarine (S) and chelerythrine (C) and their structure-activity relationships, sixteen derivatives of S and C were prepared and evaluated for in vitro antifungal activity against seven phytopathogenic fungi by the mycelial growth rate method. The results showed that S, C and their 6-alkoxy dihydro derivatives S?-S?, C?-C? and 6-cyanodihydro derivatives S?, C? showed significant antifungal activity at 100 µg/mL against all the tested fungi. For most tested fungi, the median effective concentrations of S, S?, C and C? were in a range of 14-50 µg/mL. The structure-activity relationship showed that the C=N+ moiety was the determinant for the antifungal activity of S and C. S?-S? and C?-C? could be considered as the precursors of S and C, respectively. Thus, the present results strongly suggested that S and C or their derivatives S?-S? and C?-C? should be considered as good lead compounds or model molecules to develop new anti-phytopathogenic fungal agents. can't login to work station for 2hrs--took 2 hrs vacation PMID:23124471

Yang, Xin-Juan; Miao, Fang; Yao, Yao; Cao, Fang-Jun; Yang, Rui; Ma, Yan-Ni; Qin, Bao-Fu; Zhou, Le

2012-01-01

305

Biogenic Silver Nanoparticles by Gelidiella acerosa Extract and their Antifungal Effects  

PubMed Central

The synthesis, characterization and application of biologically synthesized nanomaterials are an important aspect in nanotechnology. The present study deals with the synthesis of silver nanoparticles (Ag-NPs) using the aqueous extract of red seaweed Gelidiella acerosa as the reducing agent to study the antifungal activity. The formation of Ag-NPs was confirmed by UV-Visible Spectroscopy, X-Ray Diffraction (XRD) pattern, Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM). The synthesized Ag-NPs was predominately spherical in shape and polydispersed. Fourier Transform Infra-Red (FT-IR) spectroscopy analysis showed that the synthesized nano-Ag was capped with bimolecular compounds which are responsible for reduction of silver ions. The antifungal effects of these nanoparticles were studied against Humicola insolens (MTCC 4520), Fusarium dimerum (MTCC 6583), Mucor indicus (MTCC 3318) and Trichoderma reesei (MTCC 3929). The present study indicates that Ag-NPs have considerable antifungal activity in comparison with standard antifungal drug, and hence further investigation for clinical applications is necessary. PMID:23408653

Vivek, Marimuthu; Kumar, Palanisamy Senthil; Steffi, Sesurajan; Sudha, Sellappa

2011-01-01

306

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

PubMed Central

The Penicillium chrysogenum antifungal protein PAF inhibits the growth of various filamentous fungi. In this study, PAF was found to localize to the cytoplasm of sensitive aspergilli by indirect immunofluorescence staining. The internalization process required active metabolism and ATP and was prevented by latrunculin B, suggesting an endocytotic mechanism. PMID:14576124

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

2003-01-01

307

Identification of an Aminothiazole with Antifungal Activity against Intracellular Histoplasma capsulatum  

PubMed Central

As eukaryotes, fungi possess relatively few molecules sufficiently unique from mammalian cell components to be used as drug targets. Consequently, most current antifungals have significant host cell toxicity. Primary fungal pathogens (e.g., Histoplasma) are of particular concern, as few antifungals are effective in treating them. To identify additional antifungal candidates for the treatment of histoplasmosis, we developed a high-throughput platform for monitoring Histoplasma growth and employed it in a phenotypic screen of 3,600 commercially available compounds. Seven hit compounds that inhibited Histoplasma yeast growth were identified. Compound 41F5 has fungistatic activity against Histoplasma yeast at micromolar concentrations, with a 50% inhibitory concentration (IC50) of 0.87 ?M, and has the greatest selectivity for yeast (at least 62-fold) relative to host cells. Structurally, 41F5 consists of an aminothiazole core with an alicyclic substituent at the 2-position and an aromatic substituent at the 5-position. 41F5 inhibits Histoplasma growth in liquid culture and similarly inhibits yeast cells within macrophages, the actual host environment of this fungal pathogen during infection. Importantly, 41F5 protects infected host cells from Histoplasma-induced macrophage death, making this aminothiazole hit compound an excellent candidate for development as an antifungal for Histoplasma infections. PMID:23817367

Edwards, Jessica A.; Kemski, Megan M.

2013-01-01

308

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.

2011-06-01

309

Antifungal activity and pore-forming mechanism of astacidin 1 against Candida albicans.  

PubMed

In a previous report, a novel antibacterial peptide astacidin 1 (FKVQNQHGQVVKIFHH) was isolated from hemocyanin of the freshwater crayfish Pacifastacus leniusculus. In this study, the antifungal activity and mechanism of astacidin 1 were evaluated. Astacidin 1 exhibited antifungal activity against Candida albicans, Trichosporon beigelii, Malassezia furfur, and Trichophyton rubrum. Also, astacidin 1 had fungal cell selectivity in human erythrocytes without causing hemolysis. To understand the antifungal mechanism, membrane studies were done against C. albicans and T. beigelii. Flow cytometric analysis and K(+) measurement showed membrane damage, resulting in membrane permeabilization and K(+) release-induced membrane depolarization. Furthermore, the calcein leakage from liposomes mimicking C. albicans membrane demonstrated that the membrane-active action was driven by pore-forming mechanism. Live cell imaging using fluorescein isothiocyanate-labeled dextrans of various sizes suggested that the radii of pores formed in the C. albicans membrane were 1.4-2.3 nm. Therefore, the present study suggests that astacidin 1 exerts its antifungal effect by damaging the fungal membrane via pore formation. PMID:24955933

Choi, Hyemin; Lee, Dong Gun

2014-10-01

310

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

Microsoft Academic Search

Propolis samples from different geographic origins were investigated for their antibacterial (against Staphylococcus aureus and Escherichia coli), antifungal (against Candida albicans) and antiviral (against Avian influenza virus) activities. All samples were active against the fungal and Gram-positive bacterial test strains, and most showed antiviral activity. The activities of all samples were similar in spite of the differences in their chemical

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

1999-01-01

311

“In vitro” antifungal activity of ozonized sunflower oil on yeasts from onychomycosis  

PubMed Central

The “in vitro” antifungal activity of ozonized sunflower oil (Bioperoxoil®) was tested on 101 samples of yeasts originating from onychomycosis using the disk diffusion method. The oil was efficacious against several clinical fungal strains: Candida parapsilosis, Candida albicans, Trichosporon asahii, Candida tropicalis and Candida guilliermondii. PMID:24031958

Guerrer, L.V.; Cunha, K. C.; Nogueira, M. C. L.; Cardoso, C. C.; Soares, M. M. C. N.; Almeida, M. T. G.

2012-01-01

312

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

1995-01-01

313

Evaluation of a Capacitance Method for Direct Antifungal Susceptibility Testing of Yeasts in Positive Blood Cultures  

Microsoft Academic Search

The feasibility of using a capacitance method (CM) for direct antifungal susceptibility testing of yeasts in positive blood cultures was evaluated. The CM used the same test conditions as those recommended by the National Committee for Clinical Laboratory Standards. After direct inoculation of positive culture broths into module wells (Bactometer; bioMerieux, Inc., Hazelwood, Mo.), the end-point determination was made by

HSEIN CHANG CHANG; JUI JUNG CHANG; AY HUEY HUANG; TSUNG CHAIN CHANG

314

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

2011-01-01

315

In vitro antifungal activity of phenylheptatriyne from Bidens cernua L. against yeasts  

Microsoft Academic Search

In vitro antifungal activity of phenylheptatriyne from Bidens cernua L. (Asteraceae) was studied using broth macrodilution method against 125 strains of yeasts including 104 clinical and other isolates of Candida spp. (C. albicans, C. krusei, C. tropicalis, C. guilliermondii, C. parapsilosis, C. glabrata, C. inconspicua), 16 strains of basidiomycetous yeasts (Cryptococcus neoformans, C. albidus, Trichosporon cutaneum, Rhodotorula glutinis) and five

N. P. Rybalchenko; V. A. Prykhodko; S. S. Nagorna; N. N. Volynets; A. N. Ostapchuk; V. V. Klochko; T. V. Rybalchenko; L. V. Avdeeva

2010-01-01

316

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. PMID:23109826

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

2012-01-01

317

Broad-spectrum antifungal-producing lactic acid bacteria and their application in fruit models.  

PubMed

A large-scale screen of some 7,000 presumptive lactic acid bacteria (LAB), isolated from animal, human, or plant origin, identified 1,149 isolates with inhibitory activity against the food-spoilage mould Penicillium expansum. In excess of 500 LAB isolates were subsequently identified to produce a broad spectrum of activity against P. expansum, Penicillium digitatum, Penicillium notatum, Penicillium roqueforti, Rhizopus stolonifer, Fusarium culmorum, Aspergillus fumigatus and Rhodotorula mucilaginosa. Partial 16S rRNA sequencing of 94 broad spectrum isolates revealed that the majority of antifungal producers were strains of Lactobacillus plantarum. The remaining population was composed of Weissella confusa and Pediococcus pentosaceous isolates. Characterization of six selected broad-spectrum antifungal LAB isolates revealed that antifungal activity is maximal at a temperature of 30 °C, a pH of 4.0 and is stable across a variety of salt concentrations. The antifungal compound(s) was shown to be neither proteinaceous nor volatile in nature. P. pentosaceous 54 was shown to have protective properties against P. expansum spoilage when applied in pear, plum and grape models, therefore representing an excellent candidate for food-related applications. PMID:23160868

Crowley, Sarah; Mahony, Jennifer; van Sinderen, Douwe

2013-07-01

318

Constituents from the periderm and outer cortex of Ipomoea batatas with antifungal activity against Rhizopus stolonifer  

Microsoft Academic Search

Rhizopus stolonifer invades sweetpotato roots through injuries and infected roots are rapidly consumed by a soft rot. However, not all injuries are equally susceptible to infection; shallow injuries (1–2 mm deep) are less prone to infection than deeper injuries (>5 mm deep). The presence of antifungal compounds in external tissues may partially explain the resistance of shallow injuries to infection.

Richard R Stange; Sharon L Midland; Gerald J Holmes; James J Sims; Richard T Mayer

2001-01-01

319

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

Microsoft Academic Search

Problem statement: Increasing public concern over the level of pestic ide residues in food especially fresh produce has built up adequate pres sure for scientists to look for less hazardous and environmentally safer compounds for controlling post harvest diseases. Essential oils as registered food grade materials have the potential to be appli ed as alternative anti-fungal treatments for fresh fruits

I. Hadizadeh; B. Peivastegan; H. Hamzehzarghani

2009-01-01

320

METHIONINE AUXOTROPH ESCHERICHIA COLI GROWTH ASSAY KINETICS IN ANTIBIOTIC AND ANTIFUNGAL AMENDED SELECTIVE MEDIA  

Microsoft Academic Search

The objective of this work was to determine if Escherichia coli methionine bioassay characteristics were influenced by selective media amended with antibiotics and the antifungal compound cycloheximide. Bacterial cells were grown in minimal media with increasing concentrations of methionine and were incubated at 37°C with vigorous agitation for 6 hours. Addition of antistatic agents to the media did not change

C. A. Froelich; I. B. Zabala Díaz; S. C. Ricke

2002-01-01

321

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

PubMed Central

Malassezia pachydermatis is associated with dermatomycoses and otomycosis in dogs and cats. This study compared the susceptibility of M. pachydermatis isolates from sick (G1) and healthy (G2) animals to azole and polyene antifungals using the M27-A3 protocol. Isolates from G1 animals were less sensitive to amphotericin B, nystatin, fluconazole, clotrimazole and miconazole. PMID:24159302

Weiler, Caroline Borges; de Jesus, Francielli Pantella Kunz; Nardi, Graziela Habib; Loreto, Erico Silva; Santurio, Janio Morais; Coutinho, Selene Dall'Acqua; Alves, Sydney Hartz

2013-01-01

322

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

PubMed

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 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 found in nonrhizosphere bulk soils and different from those found with the low-altitude plants. A total of 122 actinomycete isolates was screened against nine fungal species and six bacterial species for the production of antimicrobial compounds. Four rhizosphere isolates, Streptomyces amakusaensis, S. coeruleorubidus, S. hawaiiensis and S. scabies, showed broad-spectrum antifungal activity against three or more fungal species in plate assays. In liquid antagonism assays, mycelium production by Aspergillus niger was reduced by up to 50% by two of the actinomycete isolates. These results demonstrate the potential of rhizosphere microbiology in the search for new antimicrobials. PMID:16044290

Jiménez-Esquilín, A E; Roane, T M

2005-08-01

323

Antifungal activity of geldanamycin alone or in combination with fluconazole against Candida species.  

PubMed

A standardized broth microdilution method was used to test the antifungal activity of geldanamycin (GA), an inhibitor of heat shock protein 90 (Hsp90), alone or in combination with the antifungal agent fluconazole (FLC) against 32 clinical isolates of Candida spp. In addition, a disk diffusion test was also used to evaluate the antifungal effect of these two drugs against Candida spp. by measuring the inhibition zone diameters. We found that the range of minimal inhibitory concentrations (MICs) for GA alone against Candida spp. was 3.2-12.8 mg/L and the geometric mean of MICs was 6.54 mg/L. In addition, the combination of GA with FLC showed synergistic effects in vitro against 2 FLC-susceptible and 6 FLC-resistant isolates of C. albicans. As for the other isolates, indifference but no antagonism was observed. In the disk diffusion assay, the diameter of inhibition zones for FLC combined with GA against FLC-resistant C. albicans isolates was 30 mm, while no inhibition was observed with FLC alone. These results demonstrate that GA possesses antifungal activity against Candida spp., and the combination of GA with FLC shows in vitro synergistic activity against some C. albicans isolates, especially those resistant to FLC. PMID:23341047

Zhang, Jinqing; Liu, Wei; Tan, Jingwen; Sun, Yi; Wan, Zhe; Li, Ruoyu

2013-04-01

324

Identification of an aminothiazole with antifungal activity against intracellular Histoplasma capsulatum.  

PubMed

As eukaryotes, fungi possess relatively few molecules sufficiently unique from mammalian cell components to be used as drug targets. Consequently, most current antifungals have significant host cell toxicity. Primary fungal pathogens (e.g., Histoplasma) are of particular concern, as few antifungals are effective in treating them. To identify additional antifungal candidates for the treatment of histoplasmosis, we developed a high-throughput platform for monitoring Histoplasma growth and employed it in a phenotypic screen of 3,600 commercially available compounds. Seven hit compounds that inhibited Histoplasma yeast growth were identified. Compound 41F5 has fungistatic activity against Histoplasma yeast at micromolar concentrations, with a 50% inhibitory concentration (IC50) of 0.87 ?M, and has the greatest selectivity for yeast (at least 62-fold) relative to host cells. Structurally, 41F5 consists of an aminothiazole core with an alicyclic substituent at the 2-position and an aromatic substituent at the 5-position. 41F5 inhibits Histoplasma growth in liquid culture and similarly inhibits yeast cells within macrophages, the actual host environment of this fungal pathogen during infection. Importantly, 41F5 protects infected host cells from Histoplasma-induced macrophage death, making this aminothiazole hit compound an excellent candidate for development as an antifungal for Histoplasma infections. PMID:23817367

Edwards, Jessica A; Kemski, Megan M; Rappleye, Chad A

2013-09-01

325

Antifungal and antibacterial activity of Haliclona sp. from the Persian Gulf, Iran.  

PubMed

In this study, antifungal and antibacterial activities of diethyl ether, methanol and aqueous extracts of Haliclona sp. were assessed (in vitro). The antibacterial activity of the extracts was determined by broth dilution methods against clinical Gram-negative bacteria: Escherichia coli, Pseudomonas aeruginosa and Gram-positive bacteria: Staphylococcus aureus aureus, Bacillus subtilis spizizenii. The antifungal activity of the extracts was determined by using a broth microdilution test against clinical fungi Candida albicans and Aspergillus fumigatus. Our results showed diethyl ether extract of Haliclona sp. was active on Gram-positive bacteria. In addition, methanol extract in comparison with diethyl ether extract had better activity against C. albicans (MIC: 0.75 mg/mL, MFC: 1.5mg/mL) and A. fumigatus (MIC: 2mg/mL, MFC: 3mg/mL). Aqueous extract had neither antifungal nor antibacterial activities. Based our results, Haliclona sp. can be considered as a source of novel antibiotic and antifungal. PMID:24934592

Nazemi, M; Alidoust Salimi, M; Alidoust Salimi, P; Motallebi, A; Tamadoni Jahromi, S; Ahmadzadeh, O

2014-09-01

326

Argentinean propolis from Zuccagnia punctata Cav. (Caesalpinieae) exudates: phytochemical characterization and antifungal activity.  

PubMed

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

2010-01-13

327

In vitro antifungal oral drug and drug-combination activity against onychomycosis causative dermatophytes.  

PubMed

We present the results of studies of the in vitro susceptibility of 52 isolates of Trichophyton rubrum and 40 of Trichophyton mentagrophytes to griseofulvin, terbinafine, itraconazole, ketoconazole, fluconazole and cyclopiroxolamine. All test strains were recovered from patients with toe nail onychomycosis and the minimum inhibitory concentration (MIC) of each antifungal against both species was individually assessed. In addition, we investigated the MIC of the combination of cyclopiroxolamine and itraconazole and cyclopiroxolamine and ketoconazole. The NCCLS approved procedure M38-A as modified by Santos and Hamdan was employed. The studies of the two drug combinations were conducted with a checkerboard design. Analysis of the data revealed that terbinafine was the most effective in vitro against all isolates, followed in order by itraconazole, cyclopiroxolamine, ketoconazole and fluconazole. We observed no significant difference in the in vitro susceptibility profiles between either species to any of the antifungals (P<0.05). Our in vitro results confirm that terbinafine is the most effective of the antifungals included in this study. Furthermore, synergistic interactions were found in the two drug combinations with all of the dermatophyte test isolates. The latter results are in agreement with clinical data that show synergism between oral and topical antifungals in the treatment of onychomycosis. PMID:16772230

Santos, D A; Hamdan, J S

2006-06-01

328

Micafungin for empirical antifungal therapy in patients with febrile neutropenia: multicenter phase 2 study.  

PubMed

Empirical antifungal therapy is the current standard of care for patients with febrile neutropenia unresponsive to broad-spectrum antimicrobials. Although a number of antifungal agents are currently available, the need remains for effective but less toxic alternatives for this indication. We therefore conducted a phase 2 study of micafungin for 80 patients with hematologic diseases who were suffering from persistent or recurrent fever after at least 96 h of antibacterial therapy. The patients were treated with micafungin at a fixed dose of 150 mg/day. Of the 78 evaluable patients, 54 (69 %) achieved defervescence by the time of neutrophil recovery, and 56 (72 %) completed the treatment in accordance with the provision of the protocol. Four patients developed invasive fungal infection, nine changed antifungal therapy because of lack of efficacy, and three discontinued micafungin because of drug-related adverse events. Based on the composite end point taking account of these, the overall treatment success rate was 60 %, with the lower limit of a 90 % confidence interval (50.3 %) exceeding the predefined threshold success rate (50 %). These findings show the efficacy and safety of micafungin for empirical antifungal therapy in patients with persistent or recurrent febrile neutropenia, warranting further investigation of this drug in a phase 3 study. PMID:23857638

Mizuno, Hiroki; Sawa, Masashi; Yanada, Masamitsu; Shirahata, Mizuho; Watanabe, Masato; Kato, Tomonori; Nagai, Hirokazu; Ozawa, Yukiyasu; Morishita, Takanobu; Tsuzuki, Motohiro; Goto, Emi; Tsujimura, Akane; Suzuki, Ritsuro; Atsuta, Yoshiko; Emi, Nobuhiko; Naoe, Tomoki

2013-08-01

329

In Vitro Antifungal Activity of Ankaferd Blood Stopper Against Candida albicans  

PubMed Central

Background Candida albicans is a memeber of the oral flora that can lead to various complications in immunosupresive patients after oral surgery processes. Ankaferd Blood Stopper® (ABS) is a medical plant extract that is safe to use in patients with dental surgery bleedings in Turkey. Objective The study evaluated the antifungal activity of ABS medicinal plant extract against C albicans using the agar diffusion and broth microdilution methods. Methods The plant extract antifungal activity was assessed in vitro either by applying the ABS extract directly and by applying different concentrations of ABS onto Candida culture. For these experiments, an agar diffusion method was used. To determine the minimum inhibitory concentration (MIC), a broth microdilution method was used. Results Different volumes of the active substance (10, 20, 30, and 40 ?L) were applied onto Candida (0.5 McFarland solution) cultivated plate; Candida growth was inhibited in accordance with the volumes of ABS. However, when various dilutions of ABS (1:2, 1:20, 1:40, and 1:80) were added as drops containing 20 ?L, no antifungal effects were found. No MIC values were identified using broth microdilution. When different dilutions of ABS containing 100 ?L of 0.5 McFarland solution of C albicans were cultured depending on the time (10, 20, 30, and 40 minutes), the effect of the duration was not significant. Conclusion The various tests were carried out to investigate antifungal effects of ABS on Candida, but none were found. PMID:24648581

Ciftci, Sevgi; Keskin, Fahriye; Keceli Ozcan, Sema; Erdem, Mehmet Ali; Cankaya, Burak; Bingol, Recep; Kasapoglu, Cetin

2011-01-01

330

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

FRANCESCO BARCHIESI; DANIELA ARZENI; ANNETTE W. FOTHERGILL; LUIGI FALCONI DI FRANCESCO; FRANCESCA CASELLI; MICHAEL G. RINALDI; GIORGIO SCALISE

2000-01-01

331

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

PubMed

With an aim to discover novel chitosan derivatives with significant activities against crop-threatening fungi, (1,2,3-triazol-4-yl)methyl nicotinate chitosan (TAMNCS) was prepared via azide-alkyne click reaction. Its structure was characterized by FT-IR, (1)H NMR, elemental analysis, DSC, and SEM. In vitro antifungal properties of TAMNCS against Rhizoctonia solani Kühn (R. solani), Stemphylium solani weber (S. solani), and Alternaria porri (A. porri) were studied at the concentrations ranged from 0.25 mg/mL to 1.0 mg/mL. Experiments conducted displayed the derivative had obviously enhanced antifungal activity after chemical modification compared with original chitosan. Moreover, it was shown that TAMNCS can 94.2% inhibit growth of A. porri at 1.0 mg/mL, while dose at which the fungicide triadimefon had lower inhibitory index (62.2%). The primary antifungal results described here indicate this derivative may be a promising candidate as an antifungal agent. PMID:23732332

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

2013-10-01

332

Antifungal activity of silver and zinc complexes of sulfadrug derivatives incorporating arylsulfonylureido moieties  

Microsoft Academic Search

Two well known antimicrobial sulfonamides, sulfadiazine and sulfamerazine were reacted with arylsulfonyl isocyanates, affording several new arylsulfonylureido derivatives. These compounds were subsequently used as ligands (in the form of conjugate bases, as sulfonamide anions) for the preparation of metal complexes containing silver and zinc. The newly synthesized complexes, unlike the free ligands, proved to act as effective antifungal agents against

Antonio Mastrolorenzo; Andrea Scozzafava; Claudiu T Supuran

2000-01-01

333

Chemical, antifungal and cytotoxic evaluation of the essential oil of Thymus zygis subsp. sylvestris  

Microsoft Academic Search

Several Thymus species are used since olden times in traditional medicine, due to recognized therapeutic properties, namely the antimicrobial activity of their essential oils. In the present study we evaluated the composition and the antifungal activity (MIC and MLC) of four type oils obtained from Thymus zygis subsp. sylvestris, an Iberian endemic Lamiaceae, against yeasts, dermatophyte and Aspergillus strains. Moreover,

M. J. Gonçalves; M. T. Cruz; C. Cavaleiro; M. C. Lopes; L. Salgueiro

2010-01-01

334

Essential oil of Daucus carota subsp. halophilus: Composition, antifungal activity and cytotoxicity  

Microsoft Academic Search

Ethnopharmacological relevance: Essential oils are known to possess antimicrobial activity against a wide spectrum of bacteria and fungi. Daucus carota L. is used since olden times in traditional medicine, due to recognized therapeutic properties, namely the antimicrobial activity of their essential oils.Aim of the study: In the present study the composition and the antifungal activity of the oils of Daucus

Ana Cristina Tavares; Maria José Gonçalves; Carlos Cavaleiro; Maria Teresa Cruz; Maria Celeste Lopes; Jorge Canhoto; Lígia Ribeiro Salgueiro

2008-01-01

335

Draft Genome Sequence of an Antifungal Bacterium Isolated from the Breeding Environment of Dorcus hopei binodulosus  

PubMed Central

Burkholderia sp. strain A1 was isolated from a decaying log present in the breeding environment of a stag beetle. The draft genome sequence indicates that strain A1 harbors many biosynthesis molecules, which have antimicrobial properties, and thus potentially eliminates the fungi by producing antifungal compounds, such as siderophores. PMID:24831148

Kenzaka, Takehiko; Yamada, Yasuhiro

2014-01-01

336

The Mechanism of Antifungal Action of Essential Oil from Dill (Anethum graveolens L.) on Aspergillus flavus  

PubMed Central

The essential oil extracted from the seeds of dill (Anethum graveolens L.) was demonstrated in this study as a potential source of an eco-friendly antifungal agent. To elucidate the mechanism of the antifungal action further, the effect of the essential oil on the plasma membrane and mitochondria of Aspergillus flavus was investigated. The lesion in the plasma membrane was detected through flow cytometry and further verified through the inhibition of ergosterol synthesis. The essential oil caused morphological changes in the cells of A. flavus and a reduction in the ergosterol quantity. Moreover, mitochondrial membrane potential (MMP), acidification of external medium, and mitochondrial ATPase and dehydrogenase activities were detected. The reactive oxygen species (ROS) accumulation was also examined through fluorometric assay. Exposure to dill oil resulted in an elevation of MMP, and in the suppression of the glucose-induced decrease in external pH at 4 µl/ml. Decreased ATPase and dehydrogenase activities in A. flavus cells were also observed in a dose-dependent manner. The above dysfunctions of the mitochondria caused ROS accumulation in A. flavus. A reduction in cell viability was prevented through the addition of L-cysteine, which indicates that ROS is an important mediator of the antifungal action of dill oil. In summary, the antifungal activity of dill oil results from its ability to disrupt the permeability barrier of the plasma membrane and from the mitochondrial dysfunction-induced ROS accumulation in A. flavus. PMID:22272289

Tian, Jun; Ban, Xiaoquan; Zeng, Hong; He, Jingsheng; Chen, Yuxin; Wang, Youwei

2012-01-01

337

Antifungal activity of sourdough fermented wheat germ used as an ingredient for bread making.  

PubMed

This study aimed at investigating the antifungal activity of sourdough fermented (Lactobacillus plantarum LB1 and Lactobacillus rossiae LB5) wheat germ (SFWG). Preliminarily, methanol and water/salt-soluble extracts from SFWG were assayed by agar diffusion towards Penicillium roqueforti DPPMAF1. As shown by hyphal radial growth rate, the water/salt-soluble extract showed the inhibition of various fungi isolated from bakeries. The antifungal activity was attributed to a mixture of organic acids and peptides which were synthesized during fermentation. Formic (24.7mM) acid showed the highest antifungal activity. Four peptides, having similarities with well known antifungal sequences, were identified and chemically synthesized. The minimal inhibitory concentration was 2.5-15.2mg/ml. Slices of bread made by addition of 4% (wt/wt) of freeze dried SFWG were packed in polyethylene bags and stored at room temperature. Slices did not show contamination by fungi until at least 28days of storage and behaved as the calcium propionate (0.3%, wt/wt). PMID:25214083

Rizzello, Carlo Giuseppe; Cassone, Angela; Coda, Rossana; Gobbetti, Marco

2011-08-01

338

In Vitro Antifungal Susceptibilities of Sporothrix schenckii in Two Growth Phases  

PubMed Central

We have determined the antifungal susceptibilities of 34 clinical isolates of the dimorphic fungus Sporothrix schenckii to 11 drugs using a microdilution method. In general, the type of growth phase (mycelial or yeast) and the temperature of incubation (30 or 35°C) exerted a significant influence on the MICs. PMID:16127080

Trilles, Luciana; Fernandez-Torres, Belkys; dos Santos Lazera, Marcia; Wanke, Bodo; de Oliveira Schubach, Armando; de Almeida Paes, Rodrigo; Inza, Isabel; Guarro, Josep

2005-01-01

339

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

2007-01-01

340

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

PubMed

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

2006-11-01

341

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

PubMed

The diversity of marine-derived Penicillium from Korea was investigated using morphological and multigene phylogenetic approaches, analyzing sequences of the internal transcribed spacer region, ?-tubulin gene, and RNA polymerase subunit II gene. In addition, the biological activity of all isolated strains was evaluated. We tested for the extracellular enzyme activity of alginase, endoglucanase, and ?-glucosidase, and antifungal activity against two plant pathogens (Colletotrichum acutatum and Fusarium oxysporum). A total of 184 strains of 36 Penicillium species were isolated, with 27 species being identified. The most common species were Penicillium polonicum (19.6 %), P. rubens (11.4 %), P. chrysogenum (11.4 %), and P. crustosum (10.9 %). The diversity of Penicillium strains isolated from soil (foreshore soil and sand) and marine macroorganisms was higher than the diversity of strains isolated from seawater. While many of the isolated strains showed alginase and ?-glucosidase activity, no endoglucanase activity was found. More than half the strains (50.5 %) showed antifungal activity against at least one of the plant pathogens tested. Compared with other strains in this study, P. citrinum (strain SFC20140101-M662) showed high antifungal activity against both plant pathogens. The results reported here expand our knowledge of marine-derived Penicillium diversity. The relatively high proportion of strains that showed antifungal and enzyme activity demonstrates that marine-derived Penicillium have great potential to be used in the production of natural bioactive products for pharmaceutical and/or industrial use. PMID:24908060

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

2014-08-01

342

Adverse Interactions between Antifungal Azoles and Vincristine: Review and Analysis of Cases  

PubMed Central

Summary Triazole and imidazole antifungal agents inhibit metabolism of vincristine, leading to excess vinca alkaloid exposure and severe neurotoxicity. Recent reports of debilitating interactions between vincristine and itraconazole, as well as posaconazole, voriconazole and ketoconazole underscore the need to improve medical awareness of this adverse combination. We therefore undertook a comprehensive analysis of reports of adverse drug interactions (ADIs) with the combination of vincristine and azole antifungal agents, established a new classification, and provided a detailed summary of these toxicities. In patients who had sufficient data for analysis, forty-seven individuals were identified who had an ADI with the combination of vincristine and antifungal azoles. Median age was 8 years (1.3–68 years) with 33(70%) having a diagnosis of acute lymphoblastic leukemia. Median time to ADI with vincristine was 9.5 days with itraconazole, 13.5 days posaconazole, and 30 days voriconazole. The median number of vincristine doses preceding the ADI was 2 doses with itraconazole, 3 doses posaconazole, and 2 doses voriconazole. The most common severe ADIs included gastrointestinal toxicity, peripheral neuropathy, hyponatremia/SIADH, autonomic neuropathy, and seizures. Recovery from these ADIs occurred in 80.6% of patients. We recommend using alternative antifungal agents if possible in patients receiving vincristine to avoid this serious and potentially life-threatening drug interaction. PMID:22126626

Moriyama, Brad; Henning, Stacey A.; Leung, Janice; Falade-Nwulia, Oluwaseun; Jarosinski, Paul; Penzak, Scott R.; Walsh, Thomas J.

2012-01-01

343

Enzymatic specificity of three ribosome-inactivating proteins against fungal ribosomes, and correlation with antifungal activity.  

PubMed

Ribosome-inactivating proteins (RIPs) are enzymes that cleave a specific adenine base from the highly conserved sarcin/ricin (S/R) loop of the large ribosomal RNA, thus arresting protein synthesis at the translocation step. In the present study, we employed three RIPs to dissect the antifungal activity of RIPs as plant defense proteins. We measured the catalytic activity of RAT (the catalytic A-chain of ricin from Ricinus communis L.), saporin-S6 (from Saponaria officinalis L.), and ME (RIP from Mirabilis expansa R&P) against intact ribosomal substrates isolated from various pathogenic fungi. We further determined the enzymatic specificity of these three RIPs against fungal ribosomes, from Rhizoctonia solani Kuhn, Alternaria solani Sorauer, Trichoderma reesei Simmons and Candida albicans Berkhout, and correlated the data with antifungal activity. RAT showed the strongest toxicity against all tested fungal ribosomes, except for the ribosomes isolated from C. albicans, which were most susceptible to saporin. RAT and saporin showed higher enzymatic activity than ME against ribosomes from all of the fungal species assayed, but did not show detectable antifungal activity. In contrast, ME showed substantial inhibitory activity against fungal growth. Using N-hydroxysuccinimide-fluorescein labeling of RIPs and fluorescence microscopy, we determined that ME was targeted to the surface of fungal cells and transferred into the cells. Thus, ME caused ribosome depurination and subsequent fungal mortality. In contrast, saporin did not interact with fungal cells, correlating with its lack of antifungal activity. PMID:12447536

Park, Sang-Wook; Stevens, Noah M; Vivanco, Jorge M

2002-12-01

344

Antifungal activity and mechanism of fengycin in the presence and absence of commercial surfactin against Rhizopus stolonifer.  

PubMed

The antifungal activity and mechanism of fengycin in the presence and absence of commercial surfactin against Rhizopus stolonifer were investigated. The MIC (minimal inhibitory concentration) of fengycin without commercial surfactin added was 0.4 mg/ml while the MIC of fengycin with commercial surfactin added was 2.0 mg/ml. Fengycin acted on cell membrane and cellular organs and inhibited DNA synthesis. The antifungal effect of fengycin was reduced after commercial surfactin was added. All these results suggest that the fungal cell membrane may be the primary target of fengycin action and commercial surfactin may reduce the antifungal activity of fengycin. PMID:21369992

Tao, Yang; Bie, Xiao-mei; Lv, Feng-xia; Zhao, Hai-zhen; Lu, Zhao-xin

2011-02-01

345

Multidrug-resistant transporter mdr1p-mediated uptake of a novel antifungal compound.  

PubMed

The activity of many anti-infectious drugs has been compromised by the evolution of multidrug-resistant (MDR) pathogens. For life-threatening fungal infections, such as those caused by Candida albicans, overexpression of MDR1, which encodes an MDR efflux pump of the major facilitator superfamily (MFS), often confers resistance to chemically unrelated substances, including the most commonly used azole antifungals. As the development of new and efficacious antifungals has lagged far behind the growing emergence of resistant strains, it is imperative to develop strategies to overcome multidrug resistance. Previous advances have been mainly to deploy combinational therapy to restore azole susceptibility, which, however, requires coordination of two or more compounds. We observed a unique phenotype in which Mdr1p facilitates the uptake of a specific class of compounds. Among them, we describe a novel antifungal small molecule, bis[1,6-a:5',6'-g]quinolizinium 8-methyl-salt (BQM) (U.S. patent application no. 61/793,090,2013), that has potent and broad antifungal activity. Notably, BQM exploits the MDR phenotype in C. albicans to promote the inhibitory effect. Rather than causing an antagonism of MDR strains, it exhibits a highly potentiated activity against a collection of clinical isolates and lab strains that overexpress MDR1. The activity of BQM against MDR1-overexpressing isolates is due to its facilitated intracellular accumulation. Microarray comparisons showed an extensive upregulation of MDR1 as well as polyamine transporter genes in a fluconazole-resistant strain. We then demonstrated that the polyamine transporters augment the accumulation of BQM. Importantly, BQM had greater activity than fluconazole and itraconazole against various fungal pathogens, including MDR Aspergillus fumigatus. Thus, our findings offer a paradigm shift to overcome MDR and the promise of improving antifungal treatment, especially in MDR pathogens. PMID:24041896

Sun, Nuo; Li, Dongmei; Fonzi, William; Li, Xin; Zhang, Lixin; Calderone, Richard

2013-12-01

346

Sensitization of Candida albicans biofilms to various antifungal drugs by cyclosporine A  

PubMed Central

Background Biofilms formed by Candida albicans are resistant towards most of the available antifungal drugs. Therefore, infections associated with Candida biofilms are considered as a threat to immunocompromised patients. Combinatorial drug therapy may be a good strategy to combat C. albicans biofilms. Methods Combinations of five antifungal drugs- fluconazole (FLC), voriconazole (VOR), caspofungin (CSP), amphotericin B (AmB) and nystatin (NYT) with cyclosporine A (CSA) were tested in vitro against planktonic and biofilm growth of C. albicans. Standard broth micro dilution method was used to study planktonic growth, while biofilms were studied in an in vitro biofilm model. A chequerboard format was used to determine fractional inhibitory concentration indices (FICI) of combination effects. Biofilm growth was analyzed using XTT-metabolic assay. Results MICs of various antifungal drugs for planktonic growth of C. albicans were lowered in combination with CSA by 2 to 16 fold. Activity against biofilm development with FIC indices of 0.26, 0.28, 0.31 and 0.25 indicated synergistic interactions between FLC-CSA, VOR-CSA, CSP-CSA and AmB-CSA, respectively. Increase in efficacy of the drugs FLC, VOR and CSP against mature biofilms after addition of 62.5 ?g/ml of CSA was evident with FIC indices 0.06, 0.14 and 0.37, respectively. Conclusions The combinations with CSA resulted in increased susceptibility of biofilms to antifungal drugs. Combination of antifungal drugs with CSA would be an effective prophylactic and therapeutic strategy against biofilm associated C. albicans infections. PMID:23035934

2012-01-01

347

Multidrug-Resistant Transporter Mdr1p-Mediated Uptake of a Novel Antifungal Compound  

PubMed Central

The activity of many anti-infectious drugs has been compromised by the evolution of multidrug-resistant (MDR) pathogens. For life-threatening fungal infections, such as those caused by Candida albicans, overexpression of MDR1, which encodes an MDR efflux pump of the major facilitator superfamily (MFS), often confers resistance to chemically unrelated substances, including the most commonly used azole antifungals. As the development of new and efficacious antifungals has lagged far behind the growing emergence of resistant strains, it is imperative to develop strategies to overcome multidrug resistance. Previous advances have been mainly to deploy combinational therapy to restore azole susceptibility, which, however, requires coordination of two or more compounds. We observed a unique phenotype in which Mdr1p facilitates the uptake of a specific class of compounds. Among them, we describe a novel antifungal small molecule, bis[1,6-a:5?,6?-g]quinolizinium 8-methyl-salt (BQM) (U.S. patent application no. 61/793,090,2013), that has potent and broad antifungal activity. Notably, BQM exploits the MDR phenotype in C. albicans to promote the inhibitory effect. Rather than causing an antagonism of MDR strains, it exhibits a highly potentiated activity against a collection of clinical isolates and lab strains that overexpress MDR1. The activity of BQM against MDR1-overexpressing isolates is due to its facilitated intracellular accumulation. Microarray comparisons showed an extensive upregulation of MDR1 as well as polyamine transporter genes in a fluconazole-resistant strain. We then demonstrated that the polyamine transporters augment the accumulation of BQM. Importantly, BQM had greater activity than fluconazole and itraconazole against various fungal pathogens, including MDR Aspergillus fumigatus. Thus, our findings offer a paradigm shift to overcome MDR and the promise of improving antifungal treatment, especially in MDR pathogens. PMID:24041896

Sun, Nuo; Li, Dongmei; Fonzi, William; Li, Xin; Zhang, Lixin

2013-01-01

348

Species-specific antifungal susceptibility patterns of Scedosporium and Pseudallescheria species.  

PubMed

Since the separation of Pseudallescheria boydii and P. apiosperma in 2010, limited data on species-specific susceptibility patterns of these and other species of Pseudallescheria and its anamorph Scedosporium have been reported. This study presents the antifungal susceptibility patterns of members affiliated with both entities. Clinical and environmental isolates (n = 332) from a wide range of sources and origins were identified down to species level and tested according to CLSI M38-A2 against eight antifungal compounds. Whereas P. apiosperma (geometric mean MIC/minimal effective concentration [MEC] values of 0.9, 2.4, 7.4, 16.2, 0.2, 0.8, 1.5, and 6.8 ?g/ml for voriconazole, posaconazole, isavuconazole, itraconazole, micafungin, anidulafungin, caspofungin, and amphotericin B, respectively) and P. boydii (geometric mean MIC/MEC values of 0.7, 1.3, 5.7, 13.8, 0.5, 1.4, 2.3, and 11.8 ?g/ml for voriconazole, posaconazole, isavuconazole, itraconazole, micafungin, anidulafungin, caspofungin, and amphotericin B, respectively) had similar susceptibility patterns, those for S. aurantiacum, S. prolificans, and S. dehoogii were different from each other. Voriconazole was the only drug with significant activity against S. aurantiacum isolates. The MIC distributions of all drugs except voriconazole did not show a normal distribution and often showed two subpopulations, making a species-based prediction of antifungal susceptibility difficult. Therefore, antifungal susceptibility testing of all clinical isolates remains essential for targeted antifungal therapy. Voriconazole was the only compound with low MIC values (MIC(90) of ? 2 ?g/ml) for P. apiosperma and P. boydii. Micafungin and posaconazole showed moderate activity against the majority of Scedosporium strains. PMID:22290955

Lackner, Michaela; de Hoog, G Sybren; Verweij, Paul E; Najafzadeh, Mohammad J; Curfs-Breuker, Ilse; Klaassen, Corné H; Meis, Jacques F

2012-05-01

349

Essential oil of Juniperus communis subsp. alpina (Suter) ?elak needles: chemical composition, antifungal activity and cytotoxicity.  

PubMed

Essential oils are known to possess antimicrobial activity against a wide spectrum of bacteria and fungi. In the present work the composition and the antifungal activity of the oils of Juniperus communis subsp. alpina (Suter) ?elak were evaluated. Moreover, the skin cytotoxicity, at concentrations showing significant antifungal activity, was also evaluated. The oils were isolated by hydrodistillation and analysed by gas chromatography and gas chromatography-mass spectrometry. Minimal inhibitory concentration (MIC) and minimal lethal concentration (MLC) were used to evaluate the antifungal activity of the oil against dermatophytes (Epidermophyton floccosum, Microsporum canis, M. gypseum, Trichophyton mentagrophytes, T. mentagrophytes var. interdigitale, T. rubrum, T. verrucosum), yeasts (Candida albicans, C. guillermondii, C. krusei, C. parapsilosis, C. tropicalis, Cryptococcus neoformans) and Aspergillus species (Aspergillus flavus, A. fumigatus, A. niger). Cytotoxicity was tested in HaCaT keratinocytes through the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Essential oil of J. communis subsp. alpina needles was predominantly composed of monoterpene hydrocarbons (78.4%), with the main compounds being sabinene (26.2%), ?-pinene (12-9%) and limonene (10.4%). Results concerning the antifungal activity demonstrated the potential of needle oil against dermatophytes, particularly for Microsporum canis and Trichophyton rubrum with MIC and MLC of 0.32 ?L/mL. Furthermore, evaluation of cell viability showed no significant cytotoxicity in HaCaT keratinocytes at concentrations between 0.32 and 0.64 ?L/mL. These results show that it is possible to find appropriate doses of J. communis subsp. alpina oil with both antifungal activity and a very low detrimental effect on keratinocytes. PMID:22294341

Cabral, C; Francisco, V; Cavaleiro, C; Gonçalves, M J; Cruz, M T; Sales, F; Batista, M T; Salgueiro, L

2012-09-01

350

A study to evaluate the price control of antifungal medicines and its practical applicability  

PubMed Central

Background: Superficial fungal infections are common and treatment imposes economic burden on the patients. Government of India had introduced price control over griseofulvin and tolnaftate in 1995; however, this measure can only benefit the needy if the policy is harmonized with the health-care service provider, that is, dermatologists. The aim of this study was to evaluate the existing Government mechanisms over price control of antifungal medications and its reach to the people-in-need. Materials and Methods: A questionnaire-based, cross-sectional study was carried out over a period of 6 months. Questionnaire was mailed to members of a state branch of Indian Association of Dermatologists, Venereologists, and Leprologists. Responses reaching investigators within 2 months from the date of mailing were finally analyzed. Results: Among 93 (41.33%) respondents, only 6 (6.5%) were aware of existing price control over griseofulvin but none about tolnaftate. Thirty-nine (41.9%) respondents were in favor of introducing price control on terbinafine and 42 (45.2%) for itraconazole. The topically preferred antifungals were primarily azoles and terbinafine, while among systemic antifungals, dermatologists mostly preferred fluconazole and terbinafine. The choice of antifungals by the dermatologists matched with the evidence-based dermatology data. Conclusion: Currently, price-controlled antifungal drugs are less commonly used by practitioners. Although the dermatologists favor price control, the initiative undertaken by the Government has not reached them. This shows the need to bridge the gap between policy makers and health-care service providers to help the ailing population. PMID:23248398

Sil, Amrita; Das, Nilay Kanti; Ghosh, Pramit; Datta, Pijush Kanti; Islam, Chowdhury Nazrul; Tripathi, Santanu Kumar

2012-01-01

351

Transcriptomic and morphological profiling of Aspergillus fumigatus Af293 in response to antifungal activity produced by Lactobacillus plantarum 16.  

PubMed

The morphological effects of an antifungal activity produced by Lactobacillus plantarum 16, a malt-production steep water isolate, on two food-associated fungi were examined microscopically. Spore germination was completely inhibited in Aspergillus fumigatus and Rhizopus stolonifer upon treatment with concentrated cell-free supernatant (cCFS) of strain 16. Furthermore, addition of antifungal cCFS to germ tubes and hyphae halted further development compared to untreated controls. Transcriptome analysis of A. fumigatus Af293 following exposure to antifungal cCFS revealed a number of genes with altered transcription involved in a variety of cellular functions, most notably cell metabolism, suggesting a global metabolic shutdown and subsequent cell death. Increased transcription of the global regulator LaeA was also observed indicating that exposure to the antifungal activity caused a cellular stress response. PMID:23876797

Crowley, Sarah; Mahony, Jennifer; Morrissey, John P; van Sinderen, Douwe

2013-10-01

352

Abstract. The inuence of the anti-fungal agent phosphonate (Phi) on the response of oilseed rape  

E-print Network

Abstract. The in¯uence of the anti-fungal agent phosphonate (Phi) on the response of oilseed rape rape suspension cells by the fungicide phosphonate M. Christian Carswell1 , Bruce R. Grant2 , William C

Plaxton, William

353

Syntheses of new rare earth complexes with carboxymethylated polysaccharides and evaluation of their in vitro antifungal activities.  

PubMed

In the present paper, La, Eu and Yb were selected to represent light, middle and heavy rare earths to form complexes with polysaccharides through chelating coordination of carboxyl groups, which were added into polysaccharide chains by means of carboxymethylation. Their antifungal activities against plant pathogenic fungi were evaluated using growth rate method. These rare earth complexes exhibited various antifungal activities against the tested fungi, depending on rare earth elements, polysaccharide types and fungal species. Among these three metal elements (i.e. La, Eu and Yb), Yb formed the complexes with the most effective antifungal properties. Furthermore, the results showed that ligands of carboxymethylated polysaccharides played a key role in promoting cytotoxicity of the rare earth complexes. Carboxymethylated Ganoderma applanatum polysaccharide (CGAP) was found to be the most effective ligand to form complexes with antifungal activities, followed by carboxymethylated lentinan (CLNT) and carboxymethylated Momordica charantia polysaccharide (CMCP). PMID:25256475

Sun, Xiaobo; Jin, Xiaozhe; Pan, Wei; Wang, Jinping

2014-11-26

354

Oral antifungal-exacerbated inflammatory flare-up reactions of dermatomycosis : case reports and review of the literature.  

PubMed

Inflammatory flare-up reactions of some dermatomycoses, particularly those caused by zoophilic fungi, are typical and potentially severe adverse effects following the intake of some oral antifungals. However, this condition has not previously been reported with the most frequently used antifungals in dermatology, namely fluconazole, itraconazole, and terbinafine. In this report, we describe five patients, observed over a 10-year period, who presented with inflammatory exacerbations following oral antifungal therapy for dermatomycoses. We also review the literature on inflammatory reactions exacerbated by oral antifungal agents. Details of the patients' age, sex, occupation, and atopic background; the site of the lesion, its clinical and histologic features, and any systemic signs; the identity of the fungal pathogen; the antifungal agent taken by the patient; the time between drug intake and occurrence of the flare-up; the approach to management; and the outcome were documented for each patient. A PubMed literature search was also conducted, focusing on inflammatory exacerbations induced by griseofulvin, ketoconazole, itraconazole, fluconazole, and terbinafine. The patients were four farmers and one veterinarian (all male). All primary lesions were inflammatory dermatophytoses, including one kerion. Inflammatory exacerbation of the skin lesions started 12-24 hours after the intake of oral antifungals. Mild systemic changes, including slight fever and malaise, occurred in two cases. Itraconazole 400 mg/day was implicated as the causative agent in four cases and terbinafine 250 mg/day in one case. Mycologic cultures grew Trichophytonverrucosum in four cases. Antifungal treatment was discontinued in all patients. Oral and topical corticosteroids were administered to the two patients with systemic changes; the other three patients were treated with topical corticosteroids only. Two days after the onset of corticosteroids, lower doses of itraconazole (100 mg/day) and terbinafine (125 mg/day) were reintroduced. All lesions healed after 4-5 weeks. The PubMed search did not identify any articles that described inflammatory exacerbations of dermatomycoses induced by oral antifungals. Inflammatory flare-up of dermatomycoses is a rare but potentially severe cutaneous complication of oral antifungal use. Occupational contact with animals, inflammatory dermatomycoses, and zoophilic fungi represent common features in these patients. Although evidence-based data are not available, clinical experience shows that, in addition to antifungal therapy, topical and/or systemic corticosteroids are helpful to reduce the inflammatory reactions. The cases described in this article represent the first published report of oral antifungal-exacerbated inflammatory flare-up reactions of dermatomycosis in patients taking itraconazole or terbinafine. PMID:17007544

Nikkels, Arjen F; Nikkels-Tassoudji, Nazli; Piérard, Gérald E

2006-01-01

355

Antifungal susceptibility and growth inhibitory response of oral Candida species to Brucea javanica Linn. extract  

PubMed Central

Background Candida species have been associated with the emergence of resistant strains towards selected antifungal agents. Plant products have been used traditionally as alternative medicine to ease candidal infections. The present study was undertaken to investigate the antifungal susceptibility patterns and growth inhibiting effect of Brucea javanica seeds extract against Candida species. Methods A total of seven Candida strains that includes Candida albicans ATCC14053, Candida dubliniensis ATCCMYA-2975, Candida glabrata ATCC90030, Candida krusei ATCC14243, Candida lusitaniae ATCC64125, Candida parapsilosis ATCC22019 and Candida tropicalis ATCC13803 were used in this study. The antifungal activity, minimum inhibitory concentration and minimum fungicidal concentration of B. javanica extract were evaluated. Each strain was cultured in Yeast Peptone Dextrose broth under four different growth environments; (i) in the absence and presence of B. javanica extract at respective concentrations of (ii) 1 mg/ml (iii) 3 mg/ml and (iv) 6 mg/ml. The growth inhibitory responses of the candidal cells were determined based on changes in the specific-growth rates (?) and doubling time (g). The values in the presence of extract were computed as percentage in the optical density relative to that of the total cells suspension in the absence of extract. Results B. javanica seeds extract exhibited antifungal properties. C. tropicalis showed the highest growth rate; 0.319?±?0.002 h-1, while others were in the range of 0.141?±?0.001 to 0.265?±?0.005 h-1. In the presence of extract, the lag and log phases were extended and deviated the ?- and g-values. B. javanica extract had significantly reduced the ?-values of C. dubliniensis, C. krusei and C. parapsilosis at more than 80% (??antifungal activity against seven oral Candida species. The fungistatic and growth inhibiting effects of B. javanica extract have shown that it has potential to be considered as a promising candidate for the development of antifungal agent in oral health products. PMID:24305010

2013-01-01

356

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

PubMed Central

Purpose. Fusarium, Aspergillus, and Dematiaceous are the most common fungal species causing keratitis in tropical countries. Herein we report a prospective study on fungal keratitis caused by these three fungal species. Methodology. A prospective investigation was undertaken to evaluate eyes with presumed fungal keratitis. All the fungal isolates (n = 73) obtained from keratitis infections were identified using morphological and microscopic characters. Molecular identification using sequencing of the ITS region and antifungal susceptibility tests using microdilution method were done. The final clinical outcome was evaluated in terms of the time taken for resolution of keratitis and the final visual outcome. The results were analyzed after segregating the cases into three groups, namely, Fusarium, Aspergillus, and Dematiaceous keratitis. Results. Diagnosis of fungal keratitis was established in 73 (35.9%) cases out of 208 cases. The spectra of fungi isolated were Fusarium spp. (26.6%), Aspergillus spp. (21.6%), and Dematiaceous fungi (11.6%). The sequence of the ITS region could identify the Fusarium and Aspergillus species at the species complex level, and the Dematiaceous isolates were accurately identified. Using antifungal agents such as fluconazole, natamycin, amphotericin B, and itraconazole, the minimum inhibitory concentrations (MICs) for Fusarium spp. were >32??g/mL, 4–8??g/mL, 0.5–1??g/mL, and >32??g/mL, respectively. Antifungal susceptibility data showed that Curvularia spp. was highly resistant to all the antifungal agents. Overall, natamycin and amphotericin B were found to be the most effective antifungal agents. The comparative clinical outcomes in all cases showed that the healing response in terms of visual acuity of the Dematiaceous group was significantly good when compared with the Fusarium and Aspergillus groups (P < 0.05). The time required for healing in the Fusarium group was statistically significantly less when compared with the Aspergillus and Dematiaceous groups. Conclusion. This study demonstrates important differences in microscopic features of scraping material and antifungal susceptibility between the three groups. Early and accurate identification coupled with the MIC data, and thereby appropriate treatment is crucial for complete recovery. PMID:24260740

Gajjar, Devarshi U.; Pal, Anuradha K.; Ghodadra, Bharat K.; Vasavada, Abhay R.

2013-01-01

357

Chemical Composition and Antifungal Activity of Essential Oils of Some Aromatic Medicinal Plants Growing in the Democratic Republic of Congo  

Microsoft Academic Search

The chemical composition and the antifungal activity of essential oils from 15 aromatic medicinal plant species growing in the Democratic Republic of Congo have been studied. More than 15 constituents in an amount ? 0.1% were identified in each oil. 1,8-Cineole, ?- and ?-pinene, P-cymene, ?-terpineol, camphene and limonene were prevalent constituents. The antifungal activity of these oils (5 ?L

Kanyanga Cimanga; Sandra Apers; Tess de Bruyne; Sabine Van Miert; Nina Hermans; Jozef Totté; Luc Pieters; Arnold J. Vlietinck; Kabangu Kambu; Lutete Tona

2002-01-01

358

Expression turnover profiling to monitor the antifungal activities of amphotericin B, voriconazole, and micafungin against Aspergillus fumigatus.  

PubMed

Eight highly expressed candidate genes were selected for mRNA profiling to monitor the transcriptome kinetics of Aspergillus fumigatus strains exposed to antifungal drugs as potential biomarkers of live cells to assess treatment efficacy. Mycelia were treated with fungicidal drugs amphotericin B and voriconazole, as well as the fungistatic drug micafungin. Transcription was monitored at 0, 4, 8, and 24 h posttreatment. The expression turnover profile provides a possible tool to assess antifungal therapy effects. PMID:22314535

Zhao, Yanan; Paderu, Padmaja; Park, Steven; Dukhan, Aleksandra; Senter, Meredith; Perlin, David S

2012-05-01

359

Screening of Cyanobacteria (Blue-Green algae) from Rice Paddy Soil for Antifungal Activity against Plant Pathogenic Fungi  

PubMed Central

Soil cyanobacteria isolated from the rice paddy fields of 10 different locations across Korea were evaluated by agar plate diffusion test for antifungal activity. Aqueous, petroleum ether, and methanol extracts from one hundred and forty two cyanobacterial strains belonging to the 14 genera were examined for antifungal properties against seven phytopathogenic fungi causing diseases in hot pepper (Capsicum annuum L). Of total cyanobacteria, nine cyanobacteria (6.34%) exhibited antifungal effects. The nine cyanobacteria selected with positive antifungal activities were two species of Oscillatoria, two of Anabaena, three of Nostoc, one of Nodularia, and one of Calothrix. Alternaria alternata and Botrytis cinerea were inhibited by nine and eight species of cyanobacteria, respectively. Rhizopus stolonifer was suppressed by only methanol extract of Nostoc commune FK-103. In particular, Nostoc commune FK-103 and Oscillatoria tenuis FK-109 showed strong antifungal activities against Phytophthora capsici. Their antifungal activity at the late exponential growth phase is related to the growth temperature and not associated with the growth parameters such as cell biomass and chlorophyll-? concentration. The high inhibition levels of antibiotics were 22.5 and 31.8 mm for N. commune FK-103 and O. tenuis FK-109, respectively. The optimal temperature for antibiotic productivity was 35?. PMID:24039487

2006-01-01

360

Antifungal activity, biofilm-controlling effect, and biocompatibility of poly(N-vinyl-2-pyrrolidinone)-grafted denture materials  

PubMed Central

Colonization and biofilm-formation of Candida species on denture surfaces cause Candida-associated denture stomatitis (CADS), a common, recurring disease affecting up to 67% of denture wearers. We developed poly(N-vinyl-2-pyrrolidinone)-grafted denture materials that can be repeatedly recharged with various antifungal drugs to achieve long-term antifungal and biofilm-controlling effects. The monomer, N-vinyl-2-pyrrolidinone (NVP), was grafted onto poly(methyl methacrylate) denture resins through plasma-initiated grafting polymerization. The physical properties and biocompatibility of the resulting resins were not negatively affected by the presence of up to 7.92% of grafted poly (N-vinyl-2-pyrrolidinone) (PNVP). Miconazole and chlorhexidine digluconate (CD) were used as model antifungal drugs. PNVP grafting significantly increased the drug absorption capability of the resulting denture materials. Further, the new materials showed sustained drug release and provided antifungal effects for weeks (in the case of CD) to months (in the case of miconazole). The drug-depleted resins could be recharged with the same or a different class of antifungal drug to further extend antifungal duration. If needed, drugs on the PNVP-grafted denture materials could be “washed out” (quenched) by treating with PNVP aqueous solutions to stop drug release. These results point to great potentials of the new materials in controlling biofilm-formation in a wide range of device-related applications. PMID:23708753

Sun, Xinbo; Cao, Zhengbing; Yeh, Chih-Ko; Sun, Yuyu

2013-01-01

361

Screening of Cyanobacteria (Blue-Green algae) from Rice Paddy Soil for Antifungal Activity against Plant Pathogenic Fungi.  

PubMed

Soil cyanobacteria isolated from the rice paddy fields of 10 different locations across Korea were evaluated by agar plate diffusion test for antifungal activity. Aqueous, petroleum ether, and methanol extracts from one hundred and forty two cyanobacterial strains belonging to the 14 genera were examined for antifungal properties against seven phytopathogenic fungi causing diseases in hot pepper (Capsicum annuum L). Of total cyanobacteria, nine cyanobacteria (6.34%) exhibited antifungal effects. The nine cyanobacteria selected with positive antifungal activities were two species of Oscillatoria, two of Anabaena, three of Nostoc, one of Nodularia, and one of Calothrix. Alternaria alternata and Botrytis cinerea were inhibited by nine and eight species of cyanobacteria, respectively. Rhizopus stolonifer was suppressed by only methanol extract of Nostoc commune FK-103. In particular, Nostoc commune FK-103 and Oscillatoria tenuis FK-109 showed strong antifungal activities against Phytophthora capsici. Their antifungal activity at the late exponential growth phase is related to the growth temperature and not associated with the growth parameters such as cell biomass and chlorophyll-? concentration. The high inhibition levels of antibiotics were 22.5 and 31.8 mm for N. commune FK-103 and O. tenuis FK-109, respectively. The optimal temperature for antibiotic productivity was 35?. PMID:24039487

Kim, Jeong-Dong

2006-09-01

362

Isolation and identification of 5-hydroxyl-5-methyl-2-hexenoic acid from Actinoplanes sp. HBDN08 with antifungal activity.  

PubMed

A bioactivity-guided approach was employed to isolate and determine the chemical identity of bioactive constituents with antifungal activity from Actinoplanes sp. HBDN08. The structure of the antifungal metabolite was elucidated as 5-hydroxyl-5-methyl-2-hexenoic acid on the basis of spectral analysis. This compound showed strong in vitro antifungal activity against Botrytis cinerea, Cladosporium cucumerinum and Corynespora cassiicola, with an IC(50) of 32.45, 27.17, and 30.66 mg/L, respectively; however, it only moderately inhibited hyphal growth of Rhizoctonia solani with an IC(50) of 61.64 mg/L. The in vivo antifungal activity under greenhouse conditions demonstrated that 5-hydroxyl-5-methyl-2-hexenoic acid could effectively control the diseases caused by B. cinerea, C. cucumerinum and C. cassiicola with 71.42%, 78.63% and 65.13% control values at 350 mg/L, respectively. This strong antifungal activity suggests that 5-hydroxyl-5-methyl-2-hexenoic acid might be a promising candidate for new antifungal agents. PMID:20584599

Zhang, Ji; Wang, Xiang-Jing; Yan, Yi-Jun; Jiang, Ling; Wang, Ji-Dong; Li, Bao-Ju; Xiang, Wen-Sheng

2010-11-01

363

Screening of Malian medicinal plants for antifungal, larvicidal, molluscicidal, antioxidant and radical scavenging activities.  

PubMed

A total of 78 different extracts from 20 medicinal plants belonging to 14 plant families from Mali were tested for their antifungal, larvicidal, molluscicidal, antioxidant and radical scavenging activities. Dichloromethane, methanol, water and ethanol extracts were used. TLC autobiography for antifungal activity was run with Cladosporium cucumerinum and Candida albicans. Extracts were also tested on the larvae of the mosquitoes Aedes aegypti, Anopheles gambiae and Culex quinquefasciatus. Molluscicidal activities were established with the snails Biomphalaria glabrata, Biomphalaria pfeifferi and Bulinus truncatus. beta-Carotene and DPPH solutions sprayed on TLC plates were used for antioxidant and radical scavenging assays. Of the extracts investigated, 20% were antioxidant and radical scavengers, 19% fungicidal, 30% were larvicidal and 11% were molluscicidal. Three of the plant extracts, from Cussonia barteri (Araliaceae), Glinus oppositifolius (Aïzoaceae) and Lannea velutina (Anacardiaceae) gave positive responses in all four tests. PMID:11507731

Diallo, D; Marston, A; Terreaux, C; Touré, Y; Paulsen, B S; Hostettmann, K

2001-08-01

364

Antifungal activities of extracts from Thai medicinal plants against opportunistic fungal pathogens associated with AIDS patients.  

PubMed

Summary In this study, 36 extracts derived from 10 plant species were selected to screen for their antifungal activity against clinical isolates of Candida albicans, Cryptococcus neoformans and Microsporum gypseum. Selection was based on their use by traditional Thai healers or their reported antimicrobial activities in an attempt to find bioactive medicines for use in the treatment of opportunistic fungal infections in AIDS patients. The disc diffusion and hyphal extension-inhibition assays were primarily used to test for inhibition of growth. Minimum inhibitory concentration was determined by dilution methods. The chloroform extracts of Alpinia galanga and Boesenbergia pandurata had pronounced antifungal activity against C. neoformans and M. gypseum, but exhibited weak activity against C. albicans. Alpinia galanga and B. pandurata are excellent candidates for the development of a remedy for opportunistic fungal infections in AIDS patients. PMID:16115104

Phongpaichit, Souwalak; Subhadhirasakul, Sanan; Wattanapiromsakul, Chatchai

2005-09-01

365

Synthesis of biocontrol macromolecules by derivative of chitosan with surfactin and antifungal evaluation.  

PubMed

A derivative of chitosan was prepared with chitosan and ?-cyclodextrins, which was synthesized by the immobilization reaction, as a carrier to adsorb surfactin produced from Bacillus amyloliquefaciens and got biological macromolecules. The antifungal activity against three sapstain fungi by a combination of macromolecules was tested. The results showed that the macromolecules inhibited the mycelium growth of sapstain fungi Lasiodiplodia rubropurpurea, L. crassispora, and L. theobromae by about 73.22%, 76.72%, and 70.22%, respectively. The macromolecules were relatively thermally stable with more than 50% of the antifungal activity even after being held at 121°C for 30 min. Meanwhile, the activity of the macromolecules remained more than 55% at a pH value ranging from 4 to 12. The macromolecules were resistant to hydrolysis by most protein-denaturing detergents and other enzymes. The results indicated the macromolecules might provide an alternative bioresource for the bio-control of sapstain. PMID:24530369

Yuan, Bo; Xu, Pei-Yuan; Zhang, Yue-Ji; Wang, Pei-Pei; Yu, Hong; Jiang, Ji-Hong

2014-05-01

366

Purification and characterisation of a novel chitinase from persimmon (Diospyros kaki) with antifungal activity.  

PubMed

A novel chitinase from the persimmon fruit was isolated, purified and characterised in this report. The Diospyros kaki chitinase (DKC) was found to be a monomer with a molecular mass of 29 kDa. It exhibited optimal activity at pH 4.5 with broad pH stability from pH 4.0-9.0. It has an optimal temperature of 60°C and thermostable up to 60°C when incubated for 30 min. The internal peptide sequences of DKC showed similarity with other reported plant chitinases. It has the ability to hydrolyse colloidal chitin into chito-oligomers such as chitotriose, chitobiose and into its monomer N-acetylglucosamine. It can be used to degrade chitin waste into useful products such as chito-oligosacchaarides. DKC exhibited antifungal activity towards pathogenic fungus Trichoderma viride. Chitinases with antifungal property can be used as biocontrol agents replacing chemical fungicides. PMID:23411236

Zhang, Jianzhi; Kopparapu, Narasimha Kumar; Yan, Qiaojuan; Yang, Shaoqing; Jiang, Zhengqiang

2013-06-01

367

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

PubMed Central

The purpose of this study was to isolate and select indigenous soil Pseudomonas and Bacillus bacteria capable of developing multiple mechanisms of action related to the biocontrol of phytopathogenic fungi affecting soybean crops. The screening procedure consisted of antagonism tests against a panel of phytopathogenic fungi, taxonomic identification, detection by PCR of several genes related to antifungal activity, in vitro detection of the antifungal products, and root colonization assays. Two isolates, identified and designated as Pseudomonas fluorescens BNM296 and Bacillus amyloliquefaciens BNM340, were selected for further studies. These isolates protected plants against the damping-off caused by Pythium ultimum and were able to increase the seedling emergence rate after inoculation of soybean seeds with each bacterium. Also, the shoot nitrogen content was higher in plants when seeds were inoculated with BNM296. The polyphasic approach of this work allowed us to select two indigenous bacterial strains that promoted the early development of soybean plants. PMID:20016811

Leon, M.; Yaryura, P. M.; Montecchia, M. S.; Hernandez, A. I.; Correa, O. S.; Pucheu, N. L.; Kerber, N. L.; Garcia, A. F.

2009-01-01

368

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

PubMed

Two hundred and fourteen endophytic fungi were isolated from 500 segments of aquatic/riparian plants Ottelia acuminata, Myriophyllum verticillatum, Equisetum arvense, Cardamine multijuga, and Impatiens chinensis. They were identified to 31 taxa in which Cladosporium, Fusarium, and Geotrichum were the dominant genera. Among all isolates, 169 (79%) were anamorphic fungi, 1 (0.5%) was an teleomorphic ascomycete and 44 (21%) were sterile mycelia. There were significant differences in the colonization frequency of endophytes between the five plant species (X~2=51.128, P<0.001, Chi-square test). The riparian plants harboured more endophytes than the submerged plants. The antifungal activity of these isolates against Fusarium solani and Phytophthora nicotianae in vitro were tested and 28 (13.1%) isolates showed antifungal activities with more than 30% growth inhibition rate against the two pathogens. PMID:20221722

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

2010-02-01

369

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

PubMed Central

Objective To evaluate the additive action of ginger starch on the antifungal activity of honey against Candida albicans (C. albicans). Methods C. albicans was used to determine the minimum inhibitory concentration (MIC) of four varieties of Algerian honey. Lower concentrations of honey than the MIC were incubated with a set of concentrations of starch and then added to media to determine the minimum additive inhibitory concentration (MAIC). Results The MIC for the four varieties of honey without starch against C. albicans ranged between 38% and 42% (v/v). When starch was incubated with honey and then added to media, a MIC drop was noticed with each variety. MAIC of the four varieties ranged between 32% honey (v/v) with 4% starch and 36% honey (v/v) with 2% starch. Conclusions The use of ginger starch allows honey benefit and will constitute an alternative way against the resistance to antifungal agents. PMID:23569909

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

2012-01-01

370

Anti-fungal activity of Citrus reticulata Blanco essential oil against Penicillium italicum and Penicillium digitatum.  

PubMed

The chemical composition of Citrus reticulata Blanco essential oil was analysed using GC/MS. Monoterpene hydrocarbons (C10H16) constituted the majority (88.96%, w/w) of the total oil. The oils dose-dependently inhibited Penicillium italicum and Penicillium digitatum. The anti-fungal activity of the oils against P. italicum was attributed to citronellol, octanal, citral, decanal, nonanal, ?-pinene, linalool, and ?-terpinene, whereas anti-fungal activity against P. digitatum is attributed to octanal, decanal, nonanal, limonene, citral, ?-terpinene, linalool, and ?-terpineol. The oils altered the hyphal morphology of P. italicum and P. digitatum by causing loss of cytoplasm and distortion of the mycelia. The oils significantly altered extracellular conductivity, the release of cell constituents, and the total lipid content of P. italicum and P. digitatum. The results suggest that C. reticulata Blanco essential oils generate cytotoxicity in P. italicum and P. digitatum by disrupting cell membrane integrity and causing the leakage of cell components. PMID:24491729

Tao, Nengguo; Jia, Lei; Zhou, Haien

2014-06-15

371

Antifungal Activity of Denture Soft Lining Material Modified by Silver Nanoparticles--A Pilot Study  

PubMed Central

Soft liner materials in oral cavity environments are easily colonized both by fungi and dental plaque. These factors are the cause of mucosal infections. The microorganism that most frequently colonizes soft liner materials is Candida albicans. Colonization occurs on the surface of materials and within materials. A solution to this problem might involve modification of soft liner materials with silver nanoparticles (AgNPs). In this article, we present results showing the antifungal efficacy of silicone soft lining materials modified with AgNPs. The modification process was conducted by dissolving both material components (base and catalyst) in a colloidal solution of AgNPs and evaporating the solvent. Composites with various AgNP concentrations (10, 20, 40, 80, 120 and 200 ppm) were examined. The in vitro antifungal efficacy (AFE) of composite samples was 16.3% to 52.5%. PMID:21845108

Chladek, Grzegorz; Mertas, Anna; Barszczewska-Rybarek, Izabela; Nalewajek, Teresa; Zmudzki, Jaroslaw; Krol, Wojciech; Lukaszczyk, Jan

2011-01-01

372

Isolation and Characterization of Sesquiterpenes from Celastrus orbiculatus and Their Antifungal Activities against Phytopathogenic Fungi.  

PubMed

Celastrus orbiculatus is an insecticidal plant belonging to the Celastraceae family. In this survey on the secondary metabolites of plants for obtaining bioactive substances to serve agriculture, the chemical constituents of the fruits of C. orbiculatus were investigated. This phytochemical investigation resulted in the isolation of nine new and one known sesquiterpene. Their structures, especially the complicated stereochemical features, were elucidated on the basis of extensive NMR spectroscopic data analyses, time-dependent density functional theory CD calculations, and the CD exciton chirality method. Biological screenings disclosed that these sesquiterpenes showed antifungal activities against six phytopathogenic fungi. The results of our phytochemical investigation further disclosed the chemical components of C. orbiculatus, and biological screening implied that it may be potentially useful to protect crops against phytopathogenic fungi and the bioactive compounds may be regarded as candidate agents of antifungal agrochemicals for crop protection products. PMID:25331421

Wang, Meicheng; Zhang, Qiang; Ren, Quanhui; Kong, Xianglei; Wang, Lizhong; Wang, Hao; Xu, Jing; Guo, Yuanqiang

2014-11-12

373

Itraconazole, a commonly used anti-fungal that inhibits Hedgehog pathway activity and cancer growth  

PubMed Central

SUMMARY In a screen of drugs previously tested in humans we identified itraconazole, a systemic antifungal, as a potent antagonist of the Hedgehog (Hh) signaling pathway that acts by a mechanism distinct from its inhibitory effect on fungal sterol biosynthesis. Systemically administered itraconazole, like other Hh pathway antagonists, can suppress Hh pathway activity and the growth of medulloblastoma in a mouse allograft model and does so at serum levels comparable to those in patients undergoing antifungal therapy. Mechanistically, itraconazole appears to act on the essential Hh pathway component Smoothened (Smo) by a mechanism distinct from that of cyclopamine and other known Smo antagonists, and prevents the ciliary accumulation of Smo normally caused by Hh stimulation. PMID:20385363

Kim, James; Tang, Jean Y; Gong, Ruoyu; Kim, Jynho; Lee, John J.; Clemons, Karl V.; Chong, Curtis R.; Chang, Kris S.; Fereshteh, Mark; Reya, Tannishtha; Liu, Jun O.; Epstein, Ervin H.; Stevens, David A.; Beachy, Philip A.

2014-01-01

374

A glucosinolate metabolism pathway in living plant cells mediates broad-spectrum antifungal defense.  

PubMed

Selection pressure exerted by insects and microorganisms shapes the diversity of plant secondary metabolites. We identified a metabolic pathway for glucosinolates, known insect deterrents, that differs from the pathway activated by chewing insects. This pathway is active in living plant cells, may contribute to glucosinolate turnover, and has been recruited for broad-spectrum antifungal defense responses. The Arabidopsis CYP81F2 gene encodes a P450 monooxygenase that is essential for the pathogen-induced accumulation of 4-methoxyindol-3-ylmethylglucosinolate, which in turn is activated by the atypical PEN2 myrosinase (a type of beta-thioglucoside glucohydrolase) for antifungal defense. We propose that reiterated enzymatic cycles, controlling the generation of toxic molecules and their detoxification, enable the recruitment of glucosinolates in defense responses. PMID:19095900

Bednarek, Pawel; Pislewska-Bednarek, Mariola; Svatos, Ales; Schneider, Bernd; Doubsky, Jan; Mansurova, Madina; Humphry, Matt; Consonni, Chiara; Panstruga, Ralph; Sanchez-Vallet, Andrea; Molina, Antonio; Schulze-Lefert, Paul

2009-01-01

375

Antifungal activity of hypothemycin against Peronophythora litchii in vitro and in vivo.  

PubMed

The antifungal activity of a natural resorcylic acid lactone, hypothemycin (HPM), against Peronophythora litchii in vitro and in vivo was investigated. HPM treatment substantially suppressed spore germination of P. litchi, with the inhibition rate of 100% when 0.78 ?g/mL HPM was applied. Similarly, mycelial growth of P. litchii was efficiently inhibited. Furthermore, HPM caused the ultrastructural modifications of P. litchii, including the disruption of the cell wall and the endomembrane system, especially the plasma membrane, mitochondria, and vacuoles, which led to the destruction of the cellular integrity. Moreover, application of HPM significantly reduced decay and suppressed peel browning of postharvest litchi fruit inoculated with P. litchii during storage at 28 °C. Overall, these findings suggested that HPM exhibited excellent antifungal activity against P. litchii both in vitro and in vivo, which could be helpful for the storage of harvest litchi fruit. PMID:24106914

Xu, Liangxiong; Xue, Jinghua; Wu, Ping; Wang, Duoduo; Lin, Lijing; Jiang, Yueming; Duan, Xuewu; Wei, Xiaoyi

2013-10-23

376

Antifungal treatment of Candida peritonitis in continuous ambulatory peritoneal dialysis patients.  

PubMed

Nine peritonitis episodes caused by Candida sp were diagnosed in eight continuous ambulatory peritoneal dialysis (CAPD) patients. Treatment with intraperitoneal administration of amphotericin B and 5-fluorocytosine while the peritoneal catheter was left in situ was effective in six episodes in five patients. Of the three other patients, two started again with CAPD after peritonitis had been cured, but one patient preferred to stay on hemodialysis. In four episodes, peritoneal white cell counts remained high during treatment despite negative cultures. This was probably the result of irritation of the peritoneal membrane caused by the antifungal treatment, possibly by amphotericin B. Persistently-elevated leukocyte counts during antifungal therapy, with or without signs and symptoms of peritonitis, are not necessarily an indication of treatment failure. PMID:3812482

Struijk, D G; Krediet, R T; Boeschoten, E W; Rietra, P J; Arisz, L

1987-01-01

377

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

PubMed

Bioassay-guided separation with an eye toward antifungal activity led to the isolation of the new alkaloid 5-(1?,1?-dimethylallyl)-8-hydroxyfuro[2-3-b] quinoline (1) and the known biscoumarin daphnoretin (2) as the active constituents of the chloroform extract obtained from the leaves of Ruta chalepensis. The structures of the metabolites were elucidated on the basis of their spectral characteristics (NMR, UV, and MS) and were compared with the literature. The antifungal activity of the isolated compounds was evaluated against the phytopathogenic fungi Rhizoctonia solani, Sclerotium rolfsii, and Fusarium solani, which cause root-rot and wilt diseases in several economically important food crops such as potato, sugar beet, and tomato. PMID:22491304

Emam, A; Eweis, M; Elbadry, M

2010-12-01

378

Synthesis and biological evaluation of novel trichodermin derivatives as antifungal agents.  

PubMed

To discover more potential antifungal agents, 17 novel trichodermin derivatives were designed and synthesized by modification of 3 and 4a. The structures of all the synthesized compounds were confirmed by (1)H NMR, ESI-MS and HRMS. Their antifungal activities against Ustilaginoidea oryzae and Pyricularia oryzae were evaluated. Most of the target compounds showed potent inhibitory activity, in which 4g showed superior inhibitory effects than 4a and commercial fungicide prochloraz. Furthermore, 4h demonstrated comparable inhibitory activity to 4a. Moreover, 4i and 4l exhibited excellent inhibitory activity for Pyricularia oryzae. Additionally, compound 9 was found to be more active against all tested fungal strains than 3, with EC50 values of 0.47 and 3.71 mg L(-1), respectively. PMID:24908609

Zheng, Min; Yao, Ting-Ting; Xu, Xiao-Jun; Cheng, Jing-Li; Zhao, Jin-Hao; Zhu, Guo-Nian

2014-08-01

379

Diversity of Bipolaris Species in Clinical Samples in the United States and Their Antifungal Susceptibility Profiles  

PubMed Central

A set of 104 isolates from human clinical samples from the United States, morphologically compatible with Bipolaris, were morphologically and molecularly identified through the sequence analysis of the internal transcribed space (ITS) region of the nuclear ribosomal DNA (rDNA). The predominant species was Bipolaris spicifera (67.3%), followed by B. hawaiiensis (18.2%), B. cynodontis (8.6%), B. micropus (2.9%), B. australiensis (2%), and B. setariae (1%). Bipolaris cynodontis, B. micropus, and B. setariae represent new records from clinical samples. The most common anatomical sites where isolates were recovered were the nasal region (30.7%), skin (19.2%), lungs (14.4%), and eyes (12.5%). The antifungal susceptibilities of 5 species of Bipolaris to 9 drugs are provided. With the exception of fluconazole and flucytosine, the antifungals tested showed good activity. PMID:23052310

da Cunha, K. C.; Sutton, D. A.; Fothergill, A. W.; Cano, J.; Madrid, H.; De Hoog, S.; Crous, P. W.; Guarro, J.

2012-01-01

380

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

PubMed

The plant 2S albumins exhibit a spectrum of biotechnologically exploitable functions. Among them, pumpkin 2S albumin has been shown to possess RNase and cell-free translational inhibitory activities. The present study investigated the anticancer, DNase and antifungal activities of pumpkin 2S albumin. The protein exhibited a strong anticancer activity toward breast cancer (MCF-7), ovarian teratocarcinoma (PA-1), prostate cancer (PC-3 and DU-145) and hepatocellular carcinoma (HepG2) cell lines. Acridine orange staining and DNA fragmentation studies indicated that cytotoxic effect of pumpkin 2S albumin is mediated through induction of apoptosis. Pumpkin 2S albumin showed DNase activity against both supercoiled and linear DNA and exerted antifungal activity against Fusarium oxysporum. Secondary structure analysis by CD showed that protein is highly stable up to 90°C and retains its alpha helical structure. These results demonstrated that pumpkin 2S albumin is a multifunctional protein with host of potential biotechnology applications. PMID:24814706

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

2014-06-13

381

In vitro Evaluation of Antifungal Activity of the Seed Extract of Embelia Ribes.  

PubMed

Antifungal activity of Embelia ribes was evaluated on eight different fungal species by employing various concentrations of seed extract (0.5-2.0 mg). All the concentrations of seed extract inhibited the fungal growth, whereas maximum activity was observed at 2.0 mg concentration of seed extract. Among different doses, the diameter of inhibition zones ranged from 9 to 18 mm in various fungal species and increased with the increase in the concentration of test solution. Among all the fungi, high inhibition zones were observed in Colletotricum crassipes (18 mm). This was followed by Cladosporium (17.5 mm), Armillaria mellea (17 mm), Colletotricum capsici (17 mm), Aspergillus niger (16.5 mm), Rhizopus oryzae (16.5 mm), respectively. Aspergillus terreus and Candida albicans showed less inhibition zones (15.5 and 16.0 mm) compared to other organisms. The present study clearly demonstrated the antifungal properties of Embelia ribes. PMID:22303075

Rani, A Sabitha; Saritha, K; Nagamani, V; Sulakshana, G

2011-03-01

382

Cytotoxic and antifungal activities of melleolide antibiotics follow dissimilar structure-activity relationships.  

PubMed

The fungal genus Armillaria is unique in that it is the only natural source of melleolide antibiotics, i.e., protoilludene alcohols esterified with orsellinic acid or its derivatives. This class of natural products is known to exert antimicrobial and cytotoxic effects. Here, we present a refined relationship between the structure and the antimicrobial activity of the melleolides. Using both agar diffusion and broth dilution assays, we identified the ?(2,4)-double bond of the protoilludene moiety as a key structural feature for antifungal activity against Aspergillus nidulans, Aspergillus flavus, and Penicillium notatum. These findings contrast former reports on cytotoxic activities and may indicate a different mode of action towards susceptible fungi. We also report the isolation and structure elucidation of five melleolides (6'-dechloroarnamial, 6'-chloromelleolide F, 10-hydroxy-5'-methoxy-6'-chloroarmillane, and 13-deoxyarmellides A and B), along with the finding that treatment with an antifungal melleolide impacts transcription of A. nidulans natural product genes. PMID:24906293

Bohnert, Markus; Nützmann, Hans-Wilhelm; Schroeckh, Volker; Horn, Fabian; Dahse, Hans-Martin; Brakhage, Axel A; Hoffmeister, Dirk

2014-09-01

383

In vitro Evaluation of Antifungal Activity of the Seed Extract of Embelia Ribes  

PubMed Central

Antifungal activity of Embelia ribes was evaluated on eight different fungal species by employing various concentrations of seed extract (0.5-2.0 mg). All the concentrations of seed extract inhibited the fungal growth, whereas maximum activity was observed at 2.0 mg concentration of seed extract. Among different doses, the diameter of inhibition zones ranged from 9 to 18 mm in various fungal species and increased with the increase in the concentration of test solution. Among all the fungi, high inhibition zones were observed in Colletotricum crassipes (18 mm). This was followed by Cladosporium (17.5 mm), Armillaria mellea (17 mm), Colletotricum capsici (17 mm), Aspergillus niger (16.5 mm), Rhizopus oryzae (16.5 mm), respectively. Aspergillus terreus and Candida albicans showed less inhibition zones (15.5 and 16.0 mm) compared to other organisms. The present study clearly demonstrated the antifungal properties of Embelia ribes. PMID:22303075

Rani, A Sabitha; Saritha, K; Nagamani, V; Sulakshana, G

2011-01-01

384

Disseminated mucormycosis in a paediatric patient: Lichthemia corymbifera successfully treated with combination antifungal therapy  

PubMed Central

Mucormycosis is a severe fungal infection that largely affects immunocompromised individuals. It carries a high morbidity and mortality rate and is characterised by extensive angioinvasion and necrosis of host tissue. This case report details success in treating disseminated mucormycosis in a paediatric patient with an underlying haematological malignancy. Treatment included institution of combination antifungal therapy with liposomal amphotericin B and caspofungin, aggressive surgical debridement of infected tissue and reversal of underlying immunosuppression. PMID:25379392

Campbell, Anita; Cooper, Celia; Davis, Stephen

2014-01-01

385

Antifungal activity of drimane sesquiterpenes from Drimys brasiliensis using bioassay-guided fractionation  

Microsoft Academic Search

Purpose. This study describes the antifungal effect of extracts and compounds isolated from Drimys brasiliensis acting against dermatophytes. Methods. The activities were evaluated by using the microbroth dilution method. Results. Bioassay-guided fractionation of the most active extract from the bark (CHCl3) led to the isolation of the sesquiterpene drimanes polygodial, 1- ?-(p-methoxycinnamoyl)-polygodial, drimanial and 1-?-(p-cumaroyloxy)-polygodial, which were selectively active against

Angela Malheiros; Valdir Cechinel Filho; Clarisse B. Schmitt; Rosendo A. Yunes; Andrea Escalante; Laura Svetaz

386

Granulocyte Colony-Stimulating Factor and Azole Antifungal Therapy in Murine Aspergillosis: Role of Immune Suppression  

Microsoft Academic Search

Outbred ICR mice were immune suppressed either with hydrocortisone or with 5-fluorouracil and were infect- ed intranasally with Aspergillus fumigatus. Beginning 3 days before infection some groups of mice were given re- combinant human granulocyte colony-stimulating factor (G-CSF), SCH56592 (an antifungal triazole), or both. Corticosteroid-pretreated mice responded to SCH56592 and had reduced counts in lung tissue and prolonged survival. In

JOHN R. GRAYBILL; ROSIE BOCANEGRA; LAURA K. NAJVAR; DAVID LOEBENBERG; MIKE F. LUTHER

387

Use of Amphotericin B with Azole Antifungal Drugs: What Are We Doing?  

Microsoft Academic Search

Since the 1950s, the standard agent prescribed for systemic antifungal therapy has been amphotericin B (36). Its broad spectrumofactivitymakesitanattractiveagentfortheempiric treatment of patients who may be infected with yeasts or molds.Itstrackrecordastheprimarytherapyformostinvasive mycosesiswellestablished,anditisstillwidelyregardedasthe agent of choice for the treatment of many patients with inva- sive mycoses. However, the toxicity of amphotericin B is well appreciatedandisoftenresponsibleforlimitingtheamountof drugthatcanbeadministered.Giventheimportanceofserious mycoses in clinical medicine and the

ALAN M. SUGAR

388

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

PubMed

Investigations were carried out to evaluate the therapeutic properties of the seeds and leaves of Moringa oleifera Lam as herbal medicines. Ethanol extracts showed anti-fungal activities in vitro against dermatophytes such as Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis. GC-MS analysis of the chemical composition of the essential oil from leaves showed a total of 44 compounds. Isolated extracts could be of use for the future development of anti-skin disease agents. PMID:16406607

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

2007-01-01

389

The effects of antifungal substances on some zoosporic fungi (Kingdom Fungi)  

Microsoft Academic Search

Zoosporic fungi constitute a large group of true fungi which inhabit freshwater, brackish, marine and soil ecosystems. In\\u000a general, very little is known about the effects of antifungal substances on the growth and survival of most species. This\\u000a review focuses on experimental research with those isolates which have been studied, especially in some species of Synchytrium, Olpidium, Batrachochytrium, Allomyces, Blastocladiella,

F. H. Gleason; A. V. Marano

2011-01-01

390

Nutrient sensing G protein-coupled receptors: interesting targets for antifungals?  

Microsoft Academic Search

G protein-coupled receptors (GPCRs) are important targets for various drugs that are on the market. An important area in which we urgently need novel drug targets is the field of antifungals. Recently a new class of nutrient sensing G protein-coupled receptors have been identified in fungi. The founding member of this novel class of GPCRs is Gpr1, the sucrose\\/glucose sensing

Patrick Van Dijck

2009-01-01

391

Suppression of Sclerotinia sclerotiorum by antifungal substances produced by the mycoparasite Coniothyrium minitans  

Microsoft Academic Search

A study was conducted to investigate production of antifungal substances (AFS) by Coniothyrium minitans (Cm), a mycoparasite of Sclerotinia sclerotiorum (Ss), in modified Czapek-Dox (MCD) broth and potato dextrose broth (PDB), and effects of AFS of Cm on mycelial growth and\\u000a germination of sclerotia and ascospores of Ss and incidence of leaf blight of oilseed rape caused by Ss. Results

Rui Yang; Yong Chao Han; Guo Qing Li; Dao Hong Jiang; Hung Chang Huang

2007-01-01

392

Mechanisms of the Antifungal Action of Marine Metagenome-Derived Peptide, MMGP1, against Candida albicans  

PubMed Central

Background Development of resistant variants to existing antifungal drugs continues to be the serious problem in Candida albicans-induced fungal pathogenesis, which has a considerable impact on animal and human health. Identification and characterization of newer drugs against C. albicans is, therefore, essential. MMGP1 is a direct cell-penetrating peptide recently identified from marine metagenome, which was found to possess potent antifungal activity against C. albicans. Methodology/Principal Findings In this study, we investigated the mechanism of antifungal action of MMGP1 against C. albicans. Agarose gel shift assay found the peptide to be having a remarkable DNA-binding ability. The modification of the absorption spectra and fluorescence quenching of the tryptophyl residue correspond to the stacking between indole ring and nucleotide bases. The formation of peptide–DNA complexes was confirmed by fluorescence quenching of SYTO 9 probe. The interaction of peptide with plasmid DNA afforded protection of DNA from enzymatic degradation by DNase I. In vitro transcription of mouse ?-actin gene in the presence of peptide led to a decrease in the level of mRNA synthesis. The C. albicans treated with MMGP1 showed strong inhibition of biosynthetic incorporation of uridine analog 5-ethynyluridine (EU) into nascent RNA, suggesting the peptide’s role in the inhibition of macromolecular synthesis. Furthermore, the peptide also induces endogenous accumulation of reactive oxygen species (ROS) in C. albicans. MMGP1 supplemented with glutathione showed an increased viability of C. albicans cells. The hyper-produced ROS by MMGP1 leads to increased levels of protein carbonyls and thiobarbituric acid reactive substances and it also causes dissipation of mitochondrial membrane potential and DNA fragmentation in C. albicans cells. Conclusion And Significance: Therefore, the antifungal activity of MMGP1 could be attributed to its binding with DNA, causing inhibition of transcription followed by endogenous production of ROS, which triggers cascade of events that leads to cell death. PMID:23844258

Pushpanathan, Muthuirulan; Gunasekaran, Paramasamy; Rajendhran, Jeyaprakash

2013-01-01

393

Extracellular Chitinases of Fluorescent Pseudomonads Antifungal to Fusarium oxysporum f. sp. dianthi Causing Carnation Wilt  

Microsoft Academic Search

Vascular wilt of carnation caused by Fusarium oxysporum f. sp. dianthi (Prill. & Delacr.) W. C. Synder & H.N. Hans inflicts substantial yield and quality loss to the crop. Mycolytic enzymes such\\u000a as chitinases are antifungal and contribute significantly to the antagonistic activity of fluorescent pseudomonads belonging\\u000a to plant-growth-promoting rhizobacteria. Fluorescent pseudomonads antagonistic to the vascular wilt pathogen were studied

Naosekpam Singh Ajit; Rajni Verma; V. Shanmugam

2006-01-01

394

Chemical Composition and Antifungal Activity of Essential Oil from Cymbopogon nardus (Citronella Grass)  

Microsoft Academic Search

The objective of this study was to elucidate the chemical composition of essential oil from Cymbo- pogon nardus (citronella oil) and its antifungal activity. Chemical composition of the citronella oil was determined by capillary gas chromatography (GC) and GC\\/ mass spectrometry. Major constituents of the oil were geraniol (35.7% of total volatiles), trans-citral (22.7%), cis-citral (14.2%), geranyl acetate (9.7%), citronellal

Kazuhiko NAKAHARA; Najeeb S. ALZOREKY; Tadashi YOSHIHASHI; T. T. NGUYEN

2003-01-01

395

Correlation of anti-fungal susceptibility with clinical outcomes in patients with cryptococcal meningitis  

PubMed Central

Background This study aimed to investigate the correlation of minimum inhibiting concentrations (MICs), obtained by broth micro-dilution, and clinical response in patients with cryptococcal meningitis. Methods Using retrospective analyses covering the period 2001–2010, factors affecting clinical therapeutic cure in patients with cryptococcal meningitis 10 weeks after the start of anti-fungal therapy were identified. Specific emphasis was placed on the role of anti-fungal susceptibility. Results Of 46 patients with cryptococcal meningitis identified, 21 were cured after 10 weeks of treatment. Overall, 12 strains (26.1%) were resistant to fluconazole (>8 ?g/ml) and 8 (17.4%) had an MIC >1 ?g/ml for amphotericin B. Twenty-three patients received combination amphotericin B and fluconazole as their initial antifungal therapy, 17 were given amphotericin B only, five received fluconazole only, and one received a combination of amphotericin B and flucytosine. After 2 weeks, all patients received fluconazole (400–600 mg daily for 8 weeks at least, then 200 mg daily thereafter). The presence of isolates resistant to fluconazole (MIC >8 ?g/ml; 4.8% vs. 44%, p?Anti-fungal susceptibility, reflected by fluconazole MIC >8 ?g/ml, was an independent predictor of therapeutic cure at 10-week evaluation (OR?=?15.7; 95% CI: 1.8-135.9; p?=?0.01), but higher MIC of amphotericin B (>1 ?g/ml) was not. Conclusions The MICs of fluconazole, determined by the CLSI method, may be a potential predictor of therapeutic cure in patients with cryptococcal meningitis. PMID:23253817

2012-01-01

396

1-MCP prevents ethylene-induced accumulation of antifungal diene in avocado fruit  

Microsoft Academic Search

The preformed (Z,Z)-1-acetoxy-2-hydroxy-4-oxo-heneicosa-12,15-diene (AFD) is the most active antifungal compound in avocado; it affects the quiescence of Colletotrichum gloeosporioides in unripe fruit. Ethylene treatment (40?gl?1) of freshly harvested avocado fruits cv. Fuerte enhanced the expression patterns of genes encoding ?12 fatty acid desaturase (avfad12-3), fatty acid elongase (AVFAE, avfae1), their respective enzymatic activities, and the level of the AFD. Application

X. Wang; I. Kobiler; A. Lichter; A. Leikin-Frenkel; E. Pesis; D. Prusky

2005-01-01

397

Antifungal and antibacterial activity of seven traditionally used South African plant species active against Candida albicans  

Microsoft Academic Search

Leaf extracts of seven South African plant species with minimal inhibitory concentrations of 0.1 mg\\/ml and below against Candida albicans based on a preliminary screening were evaluated for antibacterial and antifungal activities using microplate dilution method and bioautography. Aspergillus fumigatus, Micrococcus canis, C. albicans, Sporothrix schenckii and Cryptococcus neoformans were the fungal test organisms, while the bacterial species used were Staphylococcus

L. J. Shai; L. J. McGaw; P. Masoko; J. N. Eloff

2008-01-01

398

In vitro and in vivo assessment of dermatophyte acquired resistance to efinaconazole, a novel triazole antifungal.  

PubMed

Efinaconazole is a novel triazole antifungal drug for the topical treatment of onychomycosis, a nail infection caused mainly by dermatophytes. We assessed the potential of efinaconazole to induce resistance in dermatophytes by continuous exposure of Trichophyton rubrum strains to efinaconazole in vitro (12 passages) and in a guinea pig onychomycosis model (8 weeks). There was no evidence of efinaconazole resistance development in the tested strains under the experimental conditions used. PMID:24867968

Iwata, Atsushi; Watanabe, Yoko; Kumagai, Naomichi; Katafuchi-Nagashima, Maria; Sugiura, Keita; Pillai, Radhakrishnan; Tatsumi, Yoshiyuki

2014-08-01

399

In vitro antifungal susceptibility of Cladophialophora carrionii, an agent of human chromoblastomycosis.  

PubMed

A global collection of Cladophialophora carrionii strains (n = 81) was tested against nine antifungal drugs. MIC90s of all strains were as follows in increasing order: itraconazole and posaconazole, 0.063 ?g/ml; terbinafine, 0.125 ?g/ml; isavuconazole and voriconazole, 0.25 ?g/ml; caspofungin, 2 ?g/ml; micafungin, 4 ?g/ml; amphotericin B, 8 ?g/ml; and fluconazole, 64 ?g/ml. PMID:23380718

Deng, S; de Hoog, G S; Badali, H; Yang, L; Najafzadeh, M J; Pan, B; Curfs-Breuker, I; Meis, J F; Liao, W

2013-04-01

400

Mycological profile in Otomycosis and its response to an antifungal agent  

Microsoft Academic Search

Twnty five clinically diagnosed symptontatic patients of Otomycosis were studied for fingal isolates. A potent antifungal\\u000a agent, Tolnaftate, was used topically for treatment. Specimens were collected by syringing prior to use of Tolnaftate and\\u000a after application of this agent at weekly interval. All the specimens were processed for fungus demonstration both by direect\\u000a examination and culture on conventional media.\\u000a \\u000a Majority

C. P. Baveja; P. L. Dhingra; R. Natarajan

1993-01-01

401

Antifungal effect of the essential oil of Thymus broussonetii Boiss endogenous species of Morocco  

Microsoft Academic Search

The aim of the study was to determine the antifungal effects of the essential oil of Thymus broussonetii Boiss (EOT), an endemic plant in Morocco against Candida albicans, Aspergillus fumigatus and the dermatophytes. EOT was extracted by steam distillation. A suspension of up to 500?µL of C. albicans at a concentration of 10?CFU?mL and A. fumigatus at a concentration of

B. Bellete; H. Rabérin; P. Flori; S. El Akssi; R. Tran Manh Sung; M. Taourirte; J. Hafid

2011-01-01

402

Antifungal effect of the essential oil of Thymus broussonetii Boiss endogenous species of Morocco  

Microsoft Academic Search

The aim of the study was to determine the antifungal effects of the essential oil of Thymus broussonetii Boiss (EOT), an endemic plant in Morocco against Candida albicans, Aspergillus fumigatus and the dermatophytes. EOT was extracted by steam distillation. A suspension of up to 500?µL of C. albicans at a concentration of 10?CFU?mL and A. fumigatus at a concentration of

B. Bellete; H. Rabérin; P. Flori; S. El Akssi; R. Tran Manh Sung; M. Taourirte; J. Hafid

2012-01-01

403

Roles of calcineurin and Crz1 in antifungal susceptibility and virulence of Candida glabrata.  

PubMed

A Candida glabrata calcineurin mutant exhibited increased susceptibility to both azole antifungal and cell wall-damaging agents and was also attenuated in virulence. Although a mutant lacking the downstream transcription factor Crz1 displayed a cell wall-associated phenotype intermediate to that of the calcineurin mutant and was modestly attenuated in virulence, it did not show increased azole susceptibility. These results suggest that calcineurin regulates both Crz1-dependent and -independent pathways depending on the type of stress. PMID:20100876

Miyazaki, Taiga; Yamauchi, Shunsuke; Inamine, Tatsuo; Nagayoshi, Yosuke; Saijo, Tomomi; Izumikawa, Koichi; Seki, Masafumi; Kakeya, Hiroshi; Yamamoto, Yoshihiro; Yanagihara, Katsunori; Miyazaki, Yoshitsugu; Kohno, Shigeru

2010-04-01

404

Antifungal activity of compounds extracted from Cortex Pseudolaricis against Colletotrichum gloeosporioides.  

PubMed

Cortex Pseudolaricis is the root bark of Pseudolarix amabilis Rehder, found only in China, and has been widely used in folk antifungal remedies in traditional Chinese medicine. In order to find the natural antifungal agents against mango anthracnose, eight compounds, namely pseudolaric acid A (1), ethyl pseudolaric acid B (2), pseudolaric acid B (3), pseudolaric acid B-O-?-d-glucoside (4), piperonylic acid (5), propionic acid (6), 3-hydroxy-4-methoxybenzoic acid (7), and 4-(3-formyl-5-methoxyphenyl) butanoic acid (8) were isolated from the ethanol extracts of Cortex Pseudolaricis by bioassay-guided fractionation and evaluated for in vitro antifungal activity against Colletotrichum gloeosporioides Penz. Results demonstrated that all of the eight compounds inhibited the mycelial growth of C. gloeosporioides at 5 ?g/mL. Among them, pseudolaric acid B and pseudolaric acid A showed the strongest inhibition with the EC50 values of 1.07 and 1.62 ?g/mL, respectively. Accordingly, both Pseudolaric acid B and Pseudolaric acid A highly inhibited spore germination and germ tube elongation of C. gloeosporioides. Dipping 100 ?g/mL pseudolaric acid B treatment exhibited more effective suppression on postharvest anthracnose in mango fruit when compared to the same concentration of carbendazim. Scanning electron microscopy observations revealed that pseudolaric acid B caused alterations in the hyphal morphology of C. gloeosporioides, including distortion, swelling, and collapse. Pseudolaric acid B caused the mycelial apexes to show an abnormal growth in dimensions with multiple ramifications in subapical expanded areas with irregular shape. These findings warrant further investigation into optimization of pseudolaric acid B to explore a potential antifungal agent for crop protection. PMID:24820992

Zhang, Jing; Yan, Li-Ting; Yuan, En-Lin; Ding, Hai-Xin; Ye, Huo-Chun; Zhang, Zheng-Ke; Yan, Chao; Liu, Ying-Qian; Feng, Gang

2014-05-28

405

Thymosin 1 activates dendritic cells for antifungal Th1 resistance through Toll-like receptor signaling  

Microsoft Academic Search

Dendritic cells (DCs) show a remarkable functional plasticity in the recognition of Aspergillus fumigatus and orchestrate the antifungal immune resistance in the lungs. Here, we show that thymosin 1, a natu- rally occurring thymic peptide, induces functional maturation and interleukin-12 production by fungus-pulsed DCs through the p38 mitogen-activated protein kinase\\/ nuclear factor (NF)-B-dependent path- way. This occurs by signaling through

Luigina Romani; Francesco Bistoni; Roberta Gaziano; Silvia Bozza; Claudia Montagnoli; Katia Perruccio; Lucia Pitzurra; Silvia Bellocchio; Andrea Velardi; Guido Rasi; Enrico Garaci

2004-01-01

406

Population-Based Survey of Filamentous Fungi and Antifungal Resistance in Spain (FILPOP Study)  

PubMed Central

A population-based survey was conducted to investigate the epidemiology of and antifungal resistance in Spanish clinical strains of filamentous fungi isolated from deep tissue samples, blood cultures, and respiratory samples. The study was conducted in two different periods (October 2010 and May 2011) to analyze seasonal variations. A total of 325 strains were isolated in 29 different hospitals. The average prevalence was 0.0016/1,000 inhabitants. Strains were identified by sequencing of DNA targets and susceptibility testing by the European Committee for Antimicrobial Susceptibility Testing reference procedure. The most frequently isolated genus was Aspergillus, accounting for 86.3% of the isolates, followed by Scedosporium at 4.7%; the order Mucorales at 2.5%; Penicillium at 2.2%, and Fusarium at 1.2%. The most frequent species was Aspergillus fumigatus (48.5%), followed by A. flavus (8.4%), A. terreus (8.1%), A. tubingensis (6.8%), and A. niger (6.5%). Cryptic/sibling Aspergillus species accounted for 12% of the cases. Resistance to amphotericin B was found in 10.8% of the isolates tested, while extended-spectrum triazole resistance ranged from 10 to 12.7%, depending on the azole tested. Antifungal resistance was more common among emerging species such as those of Scedosporium and Mucorales and also among cryptic species of Aspergillus, with 40% of these isolates showing resistance to all of the antifungal compounds tested. Cryptic Aspergillus species seem to be underestimated, and their correct classification could be clinically relevant. The performance of antifungal susceptibility testing of the strains implicated in deep infections and multicentric studies is recommended to evaluate the incidence of these cryptic species in other geographic areas. PMID:23669377

Mellado, E.; Pelaez, T.; Peman, J.; Zapico, S.; Alvarez, M.; Rodriguez-Tudela, J. L.; Cuenca-Estrella, M.

2013-01-01

407

Chitinolytic and antifungal activity of a Bacillus pumilus chitinase expressed in Arabidopsis  

Microsoft Academic Search

The Bacillus pumilus SG2 chitinase gene (ChiS) and its truncated form lacking chitin binding (ChBD) and fibronectin type III (FnIII) domains were transformed to Arabidopsis plants and the expression, functionality and antifungal activity of the recombinant proteins were investigated. Results showed\\u000a that while the two enzyme forms showed almost equal hydrolytic activity toward colloidal chitin, they exhibited a significant\\u000a difference

Ali DehestaniKamal; Kamal Kazemitabar; Gholamreza Ahmadian; Nadali Babaeian Jelodar; Ali Hatef Salmanian; Mehdi Seyedi; Heshmat Rahimian; Seyedhadi Ghasemi

2010-01-01

408

Enzymatic specificity of three ribosome-inactivating proteins against fungal ribosomes, and correlation with antifungal activity  

Microsoft Academic Search

Ribosome-inactivating proteins (RIPs) are enzymes that cleave a specific adenine base from the highly conserved sarcin\\/ricin (S\\/R) loop of the large ribosomal RNA, thus arresting protein synthesis at the translocation step. In the present study, we employed three RIPs to dissect the antifungal activity of RIPs as plant defense proteins. We measured the catalytic activity of RAT (the catalytic A-chain

Sang-Wook Park; Noah M. Stevens; Jorge M. Vivanco

2002-01-01

409

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

PubMed

The present study aimed to investigate antifungal activity of a stilbene and diketopiperazine compounds against plant pathogenic fungi, including Phytophthora capsici, P. colocasiae, Botrytis cinerea and Colletotrichum gloeosporioides. Minimal inhibition concentrations (MIC) and minimal fungicidal concentrations (MFC) of stilbenes and diketopiperazines for each fungus were determined using microplate method. Best activity was recorded by stilbenes against P. capsici and P. colocasiae. All four test compounds were effective in inhibiting different stages of the life cycle of test fungi. Stilbenes were more effective than diketopiperazines in inhibiting mycelial growth and inhibiting different stages of the life cycle of P. capsici and P. colocasiae. Rupture of released zoospores induced by stilbenes was reduced by addition of 100 mM glucose. The effects of stilbenes on mycelial growth and zoospore release, but not zoospore rupture, were reduced largely when pH value was above 7. In addition, stilbenes were investigated for its antifungal stability against Phytophthora sp. The results showed that stilbenes maintained strong fungistatic activity over a wide pH range (pH 4–9) and temperature range (70–120 °C). The compound stilbenes exhibited strong and stable broad-spectrum antifungal activity, and had a significant fungicidal effect on fungal cells. Results from prebiocontrol evaluations performed to date are probably useful in the search for alternative approaches to controlling serious plant pathogens. PMID:24122628

Kumar, S Nishanth; Nambisan, Bala

2014-01-01

410

Concepts and Principles of Photodynamic Therapy as an Alternative Antifungal Discovery Platform  

PubMed Central

Opportunistic fungal pathogens may cause superficial or serious invasive infections, especially in immunocompromised and debilitated patients. Invasive mycoses represent an exponentially growing threat for human health due to a combination of slow diagnosis and the existence of relatively few classes of available and effective antifungal drugs. Therefore systemic fungal infections result in high attributable mortality. There is an urgent need to pursue and deploy novel and effective alternative antifungal countermeasures. Photodynamic therapy (PDT) was established as a successful modality for malignancies and age-related macular degeneration but photodynamic inactivation has only recently been intensively investigated as an alternative antimicrobial discovery and development platform. The concept of photodynamic inactivation requires microbial exposure to either exogenous or endogenous photosensitizer molecules, followed by visible light energy, typically wavelengths in the red/near infrared region that cause the excitation of the photosensitizers resulting in the production of singlet oxygen and other reactive oxygen species that react with intracellular components, and consequently produce cell inactivation and death. Antifungal PDT is an area of increasing interest, as research is advancing (i) to identify the photochemical and photophysical mechanisms involved in photoinactivation; (ii) to develop potent and clinically compatible photosensitizers; (iii) to understand how photoinactivation is affected by key microbial phenotypic elements multidrug resistance and efflux, virulence and pathogenesis determinants, and formation of biofilms; (iv) to explore novel photosensitizer delivery platforms; and (v) to identify photoinactivation applications beyond the clinical setting such as environmental disinfectants. PMID:22514547

Dai, Tianhong; Fuchs, Beth B.; Coleman, Jeffrey J.; Prates, Renato A.; Astrakas, Christos; St. Denis, Tyler G.; Ribeiro, Martha S.; Mylonakis, Eleftherios; Hamblin, Michael R.; Tegos, George P.

2012-01-01

411

Antifungal and antibacterial activity of the essential oil of Chamaecyparis lawsoniana from Spain.  

PubMed

The essential oils extracted from the young stems and leaves of Chamaecyparis lawsoniana (A.Murray) Parl. have been analysed by Gas Chromatography and Gas Chromatography coupled to Mass Spectrometry. A total of 66 compounds were identified representing around the 99% of the total oil. The oil was richer in monoterpenes than in sesquiterpenes. The only main component was limonene with a percentage composition of 77.7%. The rest of compounds that contribute to the fragrance had percentage composition lower that the 3.0%: p-cymen-7-ol (3.0%), myrcene (2.4%), camphor (2.1%), delta-elemene (1.6%), oplopanonyl acetate (1.6%), methyl perillate (1.3%), terpinen-4-ol (1.0%) and beta-oplopenone 1.0%. The antibacterial and antifungal activity of this oil was also tested against different microorganisms. The only fungus tested, Candida albicans, was very sensitive to the treatment with an inhibition halos of 20mm. The oil was more effective with the Gram (+) than with Gram (-) bacteria. The inhibition halos were 12mm, 12-13mm and 12-13mm for Bacillus subtilis, Staphylococcus aureus and Micrococcus luteus respectively. We report new data of the antibacterial and antifungal activity of the essential oil of this species. The essential oil of C. lawsoniana could be considered as a good natural antibacterial and antifungal agent. PMID:23157017

Palá-Paúl, Jesús; Usano-Alemany, Jaime; Granda, Elena; Soria, Ana-Cristina

2012-10-01

412

Light-induced antifungal activity of TiO 2 nanoparticles/ZnO nanowires  

NASA Astrophysics Data System (ADS)

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

Haghighi, N.; Abdi, Y.; Haghighi, F.

2011-09-01

413

Metal-based carboxamide-derived compounds endowed with antibacterial and antifungal activity.  

PubMed

A series of three bioactive thiourea (carboxamide) derivatives, N-(dipropylcarbamothioyl)-thiophene-2-carboxamide (L(1)), N-(dipropylcarbamothioyl)-5-methylthiophene-2-carboxamide (L(2)) and 5-bromo-N-(dipropylcarbamothioyl)furan-2-carboxamide (L(3)) and their cobalt(II), copper(II), nickel(II) and zinc(II) complexes (1)-(12) have been synthesized and characterized by their IR,(1)H-NMR spectroscopy, mass spectrometry and elemental analysis data. The Crystal structure of one of the ligand, N-(dipropylcarbamothioyl)thiophene-2-carboxamide (L(1)) and its nickel(II) and copper(II) complexes were determined from single crystal X-ray diffraction data. All the ligands and metal(II) complexes have been subjected to in vitro antibacterial and antifungal activity against six bacterial species (Escherichia coli. Shigella flexneri. Pseudomonas aeruginosa. Salmonella typhi. Staphylococcus aureus and Bacillus subtilis) and for antifungal activity against six fungal strains (Trichophyton longifusus. Candida albicans. Aspergillus flavus. Microsporum canis. Fusarium solani and Candida glabrata). The in vitro antibacterial and antifungal bioactivity data showed the metal(II) complexes to be more potent than the parent ligands against one or more bacterial and fungal strains. PMID:23914928

Hanif, Muhammad; Chohan, Zahid H; Winum, Jean-Yves; Akhtar, Javeed

2014-08-01

414

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

PubMed

No consensus exists about whether contraceptives cause an increased risk of vaginitis, including vulvovaginal candidosis (VVC). We investigated 495 women (252 who used contraceptives; 243 who did not) for the presence of VVC. Antifungal susceptibility testing was performed for five antifungal agents and for boric acid, and three virulence factors were also examined. We recovered 129 (26.1%) monofungal populations from vaginal samples of women with acute VVC (AVVC, n = 18), symptomatic recurrent VVC (RVVC, n = 22) and asymptomatic RVVC (n = 28), as well as of other contraceptive users who carried Candida in their vaginas (n = 61). It is important to note that the women who had VVC used the same contraceptive methods (p > 0.05). Candida albicans was the most common species isolated (45%), followed by C. glabrata (40.3%). Most of the vaginal yeast isolates exhibited low minimum inhibitory concentration levels for the five antifungals tested. However, this was not the case for boric acid. In addition, the yeast fungi that was derived from the AVVC and RVVC patients showed higher amounts of haemolytic activity than the yeast fungi found among the controls (p < 0.05). The use of contraception does not predispose women to VVC (p > 0.05). Also, both host- and organism-related factors were required to achieve optimal clinical treatment for VVC. PMID:24219728

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

2013-11-01

415

Genomic identification of potential targets unique to Candida albicans for the discovery of antifungal agents.  

PubMed

Despite of modern antifungal therapy, the mortality rates of invasive infection with human fungal pathogen Candida albicans are up to 40%. Studies suggest that drug resistance in the three most common species of human fungal pathogens viz., C. albicans, Aspergillus fumigatus (causing mortality rate up to 90%) and Cryptococcus neoformans (causing mortality rate up to 70%) is due to mutations in the target enzymes or high expression of drug transporter genes. Drug resistance in human fungal pathogens has led to an imperative need for the identification of new targets unique to fungal pathogens. In the present study, we have used a comparative genomics approach to find out potential target proteins unique to C. albicans, an opportunistic fungus responsible for severe infection in immune-compromised human. Interestingly, many target proteins of existing antifungal agents showed orthologs in human cells. To identify unique proteins, we have compared proteome of C. albicans [SC5314] i.e., 14,633 total proteins retrieved from the RefSeq database of NCBI, USA with proteome of human and non-pathogenic yeast Saccharomyces cerevisiae. Results showed that 4,568 proteins were identified unique to C. albicans as compared to those of human and later when these unique proteins were compared with S. cerevisiae proteome, finally 2,161 proteins were identified as unique proteins and after removing repeats total 1,618 unique proteins (42 functionally known, 1,566 hypothetical and 10 unknown) were selected as potential antifungal drug targets unique to C. albicans. PMID:24102473

Tripathi, Himanshu; Luqman, Suaib; Meena, Abha; Khan, Feroz

2014-01-01

416

Purification and characterization of a novel antifungal protein from Bacillus subtilis strain B29*  

PubMed Central

An antifungal protein was isolated from a culture of Bacillus subtilis strain B29. The isolation procedure comprised ion exchange chromatography on diethylaminoethyl (DEAE)-52 cellulose and gel filtration chromatography on Bio-Gel® P-100. The protein was absorbed on DEAE-cellulose and Bio-Gel® P-100. The purified antifungal fraction was designated as B29I, with a molecular mass of 42.3 kDa by sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE), pI value 5.69 by isoelectric focusing (IEF)-PAGE, and 97.81% purity by high performance liquid chromatography (HPLC). B29I exhibited inhibitory activity on mycelial growth in Fusarium oxysporum, Rhizoctonia solani, Fusarium moniliforme, and Sclerotinia sclerotiorum. The 50% inhibitory concentrations (IC50) of its antifungal activity toward Fusarium oxysporum and Rhizoctonia solani were 45 and 112 ?mol/L, respectively. B29I also demonstrated an inhibitory effect on conidial spore germination of Fusarium oxysporum and suppression of germ-tube elongation, and induced distortion, tumescence, and rupture of a portion of the germinated spores. PMID:19353744

Li, Jing; Yang, Qian; Zhao, Li-hua; Zhang, Shu-mei; Wang, Yu-xia; Zhao, Xiao-yu

2009-01-01

417

A residue-free green synergistic antifungal nanotechnology for pesticide thiram by ZnO nanoparticles  

NASA Astrophysics Data System (ADS)

Here we reported a residue-free green nanotechnology which synergistically enhance the pesticides efficiency and successively eliminate its residue. We built up a composite antifungal system by a simple pre-treating and assembling procedure for investigating synergy. Investigations showed 0.25 g/L ZnO nanoparticles (NPs) with 0.01 g/L thiram could inhibit the fungal growth in a synergistic mode. More importantly, the 0.25 g/L ZnO NPs completely degraded 0.01 g/L thiram under simulated sunlight irradiation within 6 hours. It was demonstrated that the formation of ZnO-thiram antifungal system, electrostatic adsorption of ZnO NPs to fungi cells and the cellular internalization of ZnO-thiram composites played important roles in synergy. Oxidative stress test indicated ZnO-induced oxidative damage was enhanced by thiram that finally result in synergistic antifungal effect. By reducing the pesticides usage, this nanotechnology could control the plant disease economically, more significantly, the following photocatalytic degradation of pesticide greatly benefit the human social by avoiding negative influence of pesticide residue on public health and environment.

Xue, Jingzhe; Luo, Zhihui; Li, Ping; Ding, Yaping; Cui, Yi; Wu, Qingsheng

2014-07-01

418

Antifungal activity and identification of Lactobacilli, isolated from traditional dairy product "katak".  

PubMed

Filamentous moulds are the main spoilage microorganisms, responsible for significant economic losses and several healthy risks in human food chain. The lactic acid bacteria (LAB), especially lactobacilli could be a natural antagonist of these dangerous organisms. In Bulgaria, a very limited data exists on the antifungal activity of LAB microbiota of fermented dairy products. In the present study, four active strains were isolated from traditional fermented curd/yogurt-like product "katak", produced in Bulgaria from centuries. The new isolates KR3, KR4, KR51 and KR53 were identified by API 50 CH biochemical test and different molecular methods (species-specific PCR, RAPD-PCR and 16S rDNA sequence analysis) as Lactobacillus brevis. According to our knowledge, this is the first data on the molecular characterization of the Lactobacillus microbiota of "katak". A broad spectrum of antifungal activity of the four L. brevis KR strains against test-cultures representatives of carcinogenic, toxigenic, deteriorative and allergenic fungi from the genera Aspergillus, Fusarium, Penicillium and Trichoderma was estimated. Strains L. brevis KR3, KR4 and KR51 completely suppress the growth of Penicillium claviforme, Aspergillus awamori and Aspergillus niger. With regard to Aspergillus flavus and Trichoderma viride, a lower and strain-specific inhibitory activity was observed. The antifungal activity of our new L. brevis isolates seems to be a promising advantage of these four strains, suggesting their potential applications in different food technologies as bio-preservative agents against moulds. PMID:24887637

Tropcheva, Rositsa; Nikolova, Dilyana; Evstatieva, Yana; Danova, Svetla

2014-08-01

419

Antifungal Activities of Biorelevant Complexes of Copper(II) with Biosensitive Macrocyclic Ligands.  

PubMed

Four copper(II) complexes have been prepared using macrocyclic ligands. The macrocyclic ligands have been synthesized by the condensation reaction of diethyl phthalate with Schiff bases derived from o-phenylene diamine and Knoevenagel condensed ?-ketoanilides (obtained by the condensation of acetoacetanilide and substituted benzaldehydes). The ligands and copper complexes have been characterized on the basis of Microanalytical, Mass, UV-Vis., IR and CV spectral studies, as well as conductivity data. On the basis of spectral studies, a square-planar geometry for the copper complexes has been proposed. The in vitro antifungal activities of the compounds were tested against fungi such as Aspergillus niger, Rhizopus stolonifer, Aspergillus flavus, Rhizoctonia bataicola and Candida albicans. All the synthesized copper complexes showed stronger antifungal activities than free ligands. The minimum inhibitory concentrations (MIC) of the copper complexes were found in the range of 8~28 µg/ml. These compounds represent a novel class of metal-based antifungal agents which provide opportunities for a large number of synthetic variations for modulation of the activities. PMID:24039502

Raman, N; Joseph, J; Velan, A Senthil Kumara; Pothiraj, C

2006-12-01

420

Antifungal Activity in Ethanolic Extracts of Carica papaya L. cv. Maradol Leaves and Seeds.  

PubMed

Bioactive compounds from vegetal sources are a potential source of natural antifungic. An ethanol extraction was used to obtain bioactive compounds from Carica papaya L. cv. Maradol leaves and seeds of discarded ripe and unripe fruit. Both, extraction time and the papaya tissue flour:organic solvent ratio significantly affected yield, with the longest time and highest flour:solvent ratio producing the highest yield. The effect of time on extraction efficiency was confirmed by qualitative identification of the compounds present in the lowest and highest yield extracts. Analysis of the leaf extract with phytochemical tests showed the presence of alkaloids, flavonoids and terpenes. Antifungal effectiveness was determined by challenging the extracts (LE, SRE, SUE) from the best extraction treatment against three phytopathogenic fungi: Rhizopus stolonifer, Fusarium spp. and Colletotrichum gloeosporioides. The leaf extract exhibited the broadest action spectrum. The MIC(50) for the leaf extract was 0.625 mg ml(-1) for Fusarium spp. and >10 mg ml(-1) for C. gloeosporioides, both equal to approximately 20% mycelial growth inhibition. Ethanolic extracts from Carica papaya L. cv. Maradol leaves are a potential source of secondary metabolites with antifungal properties. PMID:22282629

Chávez-Quintal, Pedro; González-Flores, Tania; Rodríguez-Buenfil, Ingrid; Gallegos-Tintoré, Santiago

2011-01-01

421

Antifungal Activities of Biorelevant Complexes of Copper(II) with Biosensitive Macrocyclic Ligands  

PubMed Central

Four copper(II) complexes have been prepared using macrocyclic ligands. The macrocyclic ligands have been synthesized by the condensation reaction of diethyl phthalate with Schiff bases derived from o-phenylene diamine and Knoevenagel condensed ?-ketoanilides (obtained by the condensation of acetoacetanilide and substituted benzaldehydes). The ligands and copper complexes have been characterized on the basis of Microanalytical, Mass, UV-Vis., IR and CV spectral studies, as well as conductivity data. On the basis of spectral studies, a square-planar geometry for the copper complexes has been proposed. The in vitro antifungal activities of the compounds were tested against fungi such as Aspergillus niger, Rhizopus stolonifer, Aspergillus flavus, Rhizoctonia bataicola and Candida albicans. All the synthesized copper complexes showed stronger antifungal activities than free ligands. The minimum inhibitory concentrations (MIC) of the copper complexes were found in the range of 8~28 µg/ml. These compounds represent a novel class of metal-based antifungal agents which provide opportunities for a large number of synthetic variations for modulation of the activities. PMID:24039502

Joseph, J.; Velan, A. Senthil Kumara; Pothiraj, C.

2006-01-01

422

Antifungal activity of Cymbopogon winterianus jowitt ex bor against Candida albicans  

PubMed Central

Candida albicans is an opportunistic yeast and a member of the normal human flora that commonly causes infections in patients with any type of deficiency of the immune system. The essential oils have been tested for antimycotic activity and pose much potential as antifungal agents. This work investigated the activity of the essential oil of Cymbopogon winterianus against C. albicans by MIC, MFC and time-kill methods. The essential oil (EO) was obtained by hydrodistillation using a Clevenger-type apparatus. It was tested fifteen strains of C. albicans. The MIC was determined by the microdilution method and the MFC was determined when an aliquot of the broth microdilution was cultivated in SDA medium. The phytochemical analysis of EO showed presence of citronellal (23,59%), geraniol (18,81%) and citronellol (11,74%). The EO showed antifungal activity, and the concentrations 625 µg/mL and 1250 µg/mL inhibited the growth of all strains tested and it was fungicidal, respectively. The antimicrobial activity of various concentrations of EO was analyzed over time, it was found concentration-dependent antifungal activity, whose behavior was similar to amphotericin B and nystatin. PMID:24031651

de Oliveira, Wylly Araujo; de Oliveira Pereira, Fillipe; de Luna, Giliara Carol Diniz Gomes; Lima, Igara Oliveira; Wanderley, Paulo Alves; de Lima, Rita Baltazar; de Oliveira Lima, Edeltrudes

2011-01-01

423

Extracellular chitinases of fluorescent pseudomonads antifungal to Fusarium oxysporum f. sp. dianthi causing carnation wilt.  

PubMed

Vascular wilt of carnation caused by Fusarium oxysporum f. sp. dianthi (Prill. & Delacr.) W. C. Synder & H.N. Hans inflicts substantial yield and quality loss to the crop. Mycolytic enzymes such as chitinases are antifungal and contribute significantly to the antagonistic activity of fluorescent pseudomonads belonging to plant-growth-promoting rhizobacteria. Fluorescent pseudomonads antagonistic to the vascular wilt pathogen were studied for their ability to grow and produce chitinases on different substrates. Bacterial cells grown on chitin-containing media showed enhanced growth and enzyme production with increased anti-fungal activity against the pathogen. Furthermore, the cell-free bacterial culture filtrate from chitin-containing media also significantly inhibited the mycelial growth. Both the strains and their cell-free culture filtrate from chitin-amended media showed the formation of lytic zones on chitin agar, indicating chitinolytic ability. Extracellular proteins of highly antagonistic bacterial strain were isolated from cell-free extracts of media amended with chitin and fungal cell wall. These cell-free conditioned media contained one to seven polypeptides. Western blot analysis revealed two isoforms of chitinase with molecular masses of 43 and 18.5 kDa. Further plate assay for mycelial growth inhibition showed the 43-kDa protein to be antifungal. The foregoing studies clearly established the significance of chitinases in the antagonism of fluorescent pseudomonads, showing avenues for possible exploitation in carnation wilt management. PMID:16550458

Ajit, Naosekpam Singh; Verma, Rajni; Shanmugam, V

2006-04-01

424

Induced production of antifungal naphthoquinones in the pitchers of the carnivorous plant Nepenthes khasiana  

PubMed Central

Nepenthes spp. are carnivorous plants that have developed insect capturing traps, evolved by specific modification of the leaf tips, and are able to utilize insect degradation products as nutritional precursors. A chitin-induced antifungal ability, based on the production and secretion to the trap liquid of droserone and 5-O-methyldroserone, is described here. Such specific secretion uniquely occurred when chitin injection was used as the eliciting agent and probably reflects a certain kind of defence mechanism that has been evolved for protecting the carnivory-based provision of nutritional precursors. The pitcher liquid containing droserone and 5-O-methyldroserone at 3:1 or 4:1 molar ratio, as well as the purified naphthoquinones, exerted an antifungal effect on a wide range of plant and human fungal pathogens. When tested against Candida and Aspergillus spp., the concentrations required for achieving inhibitory and fungicidal effects were significantly lower than those causing cytotoxicity in cells of the human embryonic kidney cell line, 293T. These naturally secreted 1,4-naphthoquinone derivatives, that are assumed to act via semiquinone enhancement of free radical production, may offer a new lead to develop alternative antifungal drugs with reduced selectable pressure for potentially evolved resistance. PMID:20018905

Eilenberg, Haviva; Pnini-Cohen, Smadar; Rahamim, Yocheved; Sionov, Edward; Segal, Esther; Carmeli, Shmuel; Zilberstein, Aviah

2010-01-01

425

Activation of stress signalling pathways enhances tolerance of fungi to chemical fungicides and antifungal proteins.  

PubMed

Fungal disease is an increasing problem in both agriculture and human health. Treatment of human fungal disease involves the use of chemical fungicides, which generally target the integrity of the fungal plasma membrane or cell wall. Chemical fungicides used for the treatment of plant disease, have more diverse mechanisms of action including inhibition of sterol biosynthesis, microtubule assembly and the mitochondrial respiratory chain. However, these treatments have limitations, including toxicity and the emergence of resistance. This has led to increased interest in the use of antimicrobial peptides for the treatment of fungal disease in both plants and humans. Antimicrobial peptides are a diverse group of molecules with differing mechanisms of action, many of which remain poorly understood. Furthermore, it is becoming increasingly apparent that stress response pathways are involved in the tolerance of fungi to both chemical fungicides and antimicrobial peptides. These signalling pathways such as the cell wall integrity and high-osmolarity glycerol pathway are triggered by stimuli, such as cell wall instability, changes in osmolarity and production of reactive oxygen species. Here we review stress signalling induced by treatment of fungi with chemical fungicides and antifungal peptides. Study of these pathways gives insight into how these molecules exert their antifungal effect and also into the mechanisms used by fungi to tolerate sub-lethal treatment by these molecules. Inactivation of stress response pathways represents a potential method of increasing the efficacy of antifungal molecules. PMID:24526056

Hayes, Brigitte M E; Anderson, Marilyn A; Traven, Ana; van der Weerden, Nicole L; Bleackley, Mark R

2014-07-01

426

Characterization of the antifungal protein secreted by the mould Aspergillus giganteus.  

PubMed

An antifungal polypeptide (AFP) of 51 amino acid residues, secreted by the mould Aspergillus giganteus, has been purified to homogeneity and characterized. The inhibitory effect of this protein on the growth of different microorganisms has been studied. Whereas the growth of many of the filamentous fungi assayed is inhibited, no effect has been observed against yeasts or bacteria. The minimal concentration for total inhibition of the growth is in the range 6 to 25 microM. The antifungal polypeptide does not produce any effect on the growth of the producing mould. The polypeptide promotes aggregation of acidic phospholipid vesicles. A remarkable resistance to proteolysis and a low hydrogen x deuterium exchange have been observed for this protein. The protein does not show any thermal transition up to 80 degrees C when studied by differential scanning calorimetry and infrared spectroscopy. The uv absorbance, fluorescence emission, and circular dichroism (CD) characteristics of this protein have been studied. The protein exhibits a strong positive band at 230 nm as a prominent feature of the CD spectrum in the far uv region. All the spectroscopical properties of the antifungal protein are highly influenced by the abundance of tyrosine residues. These can be grouped in two different populations, buried and exposed, based on the results of pH-titration experiments. Fourier-transform infrared spectroscopy reveals a high content of beta-structure in AFP. Reduction and carboxy-amidomethylation produces a rather unstructured polypeptide as deduced from its spectroscopical properties. PMID:8554319

Lacadena, J; Martínez del Pozo, A; Gasset, M; Patiño, B; Campos-Olivas, R; Vázquez, C; Martínez-Ruiz, A; Mancheño, J M; Oñaderra, M; Gavilanes, J G

1995-12-20

427

Antifungal activity of Cymbopogon winterianus jowitt ex bor against Candida albicans.  

PubMed

Candida albicans is an opportunistic yeast and a member of the normal human flora that commonly causes infections in patients with any type of deficiency of the immune system. The essential oils have been tested for antimycotic activity and pose much potential as antifungal agents. This work investigated the activity of the essential oil of Cymbopogon winterianus against C. albicans by MIC, MFC and time-kill methods. The essential oil (EO) was obtained by hydrodistillation using a Clevenger-type apparatus. It was tested fifteen strains of C. albicans. The MIC was determined by the microdilution method and the MFC was determined when an aliquot of the broth microdilution was cultivated in SDA medium. The phytochemical analysis of EO showed presence of citronellal (23,59%), geraniol (18,81%) and citronellol (11,74%). The EO showed antifungal activity, and the concentrations 625 µg/mL and 1250 µg/mL inhibited the growth of all strains tested and it was fungicidal, respectively. The antimicrobial activity of various concentrations of EO was analyzed over time, it was found concentration-dependent antifun