scholarly journals Comparison ofIn VitroAntifungal Activities of Efinaconazole and Currently Available Antifungal Agents against a Variety of Pathogenic Fungi Associated with Onychomycosis

2013 ◽  
Vol 57 (4) ◽  
pp. 1610-1616 ◽  
Author(s):  
William J. Jo Siu ◽  
Yoshiyuki Tatsumi ◽  
Hisato Senda ◽  
Radhakrishnan Pillai ◽  
Takashi Nakamura ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
Trichophyton Rubrum ◽  
Yeast Species ◽  
Pathogenic Fungi ◽  
Trichophyton Mentagrophytes ◽  
Antifungal Drugs ◽  
Content Type ◽  
Comprehensive Survey ◽  
Nail Infection

ABSTRACTOnychomycosis is a common fungal nail infection in adults that is difficult to treat. Thein vitroantifungal activity of efinaconazole, a novel triazole antifungal, was evaluated in recent clinical isolates ofTrichophyton rubrum,Trichophyton mentagrophytes, andCandida albicans, common causative onychomycosis pathogens. In a comprehensive survey of 1,493 isolates, efinaconazole MICs againstT. rubrumandT. mentagrophytesranged from ≤0.002 to 0.06 μg/ml, with 90% of isolates inhibited (MIC90) at 0.008 and 0.015 μg/ml, respectively. Efinaconazole MICs against 105C. albicansisolates ranged from ≤0.0005 to >0.25 μg/ml, with 50% of isolates inhibited (MIC50) by 0.001 and 0.004 μg/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 13T. rubrumtoenail 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 againstTrichophyton,Microsporum,Epidermophyton,Acremonium,Fusarium,Paecilomyces,Pseudallescheria,Scopulariopsis,Aspergillus,Cryptococcus,Trichosporon, andCandidaand 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.

scholarly journals Synthesis, Characterization and in Vitro Antifungal Effect of Some Butyltin(IV) N-substituted 2-aminoethanethiolates

2001 ◽  
Vol 8 (3) ◽  
pp. 165-169 ◽  
Author(s):  
A. Smicka ◽  
V. Buchta ◽  
K. Handlir
Keyword(s):  
Candida Glabrata ◽  
Pathogenic Fungi ◽  
Trichophyton Mentagrophytes ◽  
Candida Krusei ◽  
Antifungal Drugs ◽  
Antifungal Effect ◽  
Absidia Corymbifera ◽  
Structure Activity ◽  
Trichosporon Beigelii

Six new N-substituted di- and tributyltin 2-aminoethanethiolates (cysteaminates) have been prepared and characterised by H1, C13 and S119n NMR spectroscopy. All these compounds exhibit a good in vitro antifungal effect against selected types of human pathogenic fungi (Candida albicans, Candida krusei, Candida tropicalis, Candida glabrata, Trichosporon beigelii, Aspergillus fumigatus, Absidia corymbifera, Trichophyton mentagrophytes) and their activity is comparable with that of some antifungal drugs commonly used in the clinical use like ketoconazole. The structure-activity relationships in these compounds are discussed.

scholarly journals Acylhydrazones as Antifungal Agents Targeting the Synthesis of Fungal Sphingolipids

2018 ◽  
Vol 62 (5) ◽  
Author(s):  
Cristina Lazzarini ◽  
Krupanandan Haranahalli ◽  
Robert Rieger ◽  
Hari Krishna Ananthula ◽  
Pankaj B. Desai ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Antifungal Agents ◽  
Fungal Infections ◽  
Antifungal Drugs ◽  
Fungal Resistance ◽  
Content Type ◽  
Highly Active ◽  
Pharmacokinetic Properties ◽  
Pass Through

ABSTRACTThe incidence of invasive fungal infections has risen dramatically in recent decades. Current antifungal drugs are either toxic, likely to interact with other drugs, have a narrow spectrum of activity, or induce fungal resistance. Hence, there is a great need for new antifungals, possibly with novel mechanisms of action. Previously our group reported an acylhydrazone called BHBM that targeted the sphingolipid pathway and showed strong antifungal activity against several fungi. In this study, we screened 19 derivatives of BHBM. Three out of 19 derivatives were highly active againstCryptococcus neoformansin vitroand had low toxicity in mammalian cells. In particular, one of them, called D13, had a high selectivity index and showed better activity in an animal model of cryptococcosis, candidiasis, and pulmonary aspergillosis. D13 also displayed suitable pharmacokinetic properties and was able to pass through the blood-brain barrier. These results suggest that acylhydrazones are promising molecules for the research and development of new antifungal agents.

scholarly journals In vitro evaluation of the antifungal activity of Marco (Ambrosia arborescens Mill.) and Matico (Aristeguietia glutinosa Lam.) on the pathogenic fungi that cause dermatomycosis (ringworm)

F1000Research ◽  
2018 ◽  
Vol 7 ◽  
pp. 559
Author(s):  
Tatiana de los Ángeles Mosquera Tayupanta ◽  
Sandra Elizabeth Ayala Valarezo ◽  
Tatiana Alexandra Vasquez Villareal ◽  
María Belén Montaluisa Álvarez
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Trichophyton Rubrum ◽  
Therapeutic Potential ◽  
Pathogenic Fungi ◽  
Trichophyton Mentagrophytes ◽  
Microsporum Canis ◽  
The One ◽  
One Way Anova

Background: Currently, there is a trend towards using natural and ethnopharmacological species with therapeutic potential. This investigation evaluated the antifungal activity of two species in the Ecuadorian Andes, which are used in treating dermatomycosis: Ambrosia arborescens Mill. (Marco) and Aristeguietia glutinosa Lam. (Matico). Methods: We worked with seven concentrations (100 to 700ppm) of Ambrosia arborescens Mill. extract and ten concentrations (0.5 to 5%) of essential oil (EO) of Aristeguietia glutinosa Lam. on Trichophyton mentagrophytes ATCC 9533, Trichophyton rubrum ATCC 28188, Microsporum canis ATCC 36299 and Candida albicans ATCC 10231. The methodology used was a modified version of the Kirby-Bauer method, using diffusion in agar wells. Results: The Tukey test, after the one-way Anova, determined effective concentrations of EO: 5% for Trichophyton mentagrophytes, 4.5% for Trichophyton rubrum, 5% for Microsporum canis and 2% for Candida albicans. In the extracts, the concentration of 700ppm was used for Trichophyton mentagrophytes, Trichophyton rubrum, and 600ppm for Microsporum canis and Candida albicans. Conclusions: The evaluation of the antifungal activity of the Ambrosia arborescens extract showed inhibition in the studied dermatophytes in each one of the planted concentrations (100 to 700ppm). The evaluation of the antifungal activity of Aristeguietia glutinosa EO showed inhibition in the studied dermatophytes in each of the planted concentrations (0.5 to 5%).

scholarly journals In Vitro Antifungal Susceptibility Of Griseofulvin, Fluconazole, Itraconazole And Terbinafine Against Clinical Isolates Of Trichophyton Rubrum And Trichophyton Mentagrophytes

2014 ◽  
Vol 2 (1) ◽  
Author(s):  
K R Reddy ◽  
S Ram Reddy
Keyword(s):  
Trichophyton Rubrum ◽  
Clinical Laboratory ◽  
Antifungal Susceptibility ◽  
Trichophyton Mentagrophytes ◽  
Drug Susceptibility ◽  
Antifungal Drugs ◽  
Clinical Isolates ◽  
National Committee ◽  
In Vitro Antifungal Susceptibility

Investigations on antifungal drug susceptibility were carried out on 90 clinical isolates of Trichophyton rubrum, and Trichophyton mentagrophytes with four antifungal drugs, namely griseofulvin, fluconazole, itraconazole and terbinafine as suggested by National Committee for Clinical Laboratory Standards (NCCLS) M27–A (1997) document by broth macrodilution method to standardize in vitro antifungal susceptibility testing and to find out the Minimum Inhibitory Concentration (MIC) of the drugs. In this study, terbinafine was found to be the most efficient drug for all isolates. Terbinafine had the lowest MIC range of 0.001 g/ml to 0.09 g/ml and MIC50 was low at 0.005 g/ml and MIC90 was also low at 0.04 g/ml against T.rubrum; and MIC range of 0.001μg/ml to 0.19μg/ml with a MIC50 of 0.01μg/ml and MIC90 at 0.09μg/ml against T.mentagrophytes. Itraconazole showed antifungal activity superior to that of fluconazole, with a MIC range of 0.04g/ml to 1.56g/ml, with MIC50 at 0.19μg/ml and MIC90 at 1.56g/ml against T.rubrum; and MIC range of 0.04μg/ml to 1.56μg/ml, with MIC50 at 0.19μg/ml and MIC90 at 0.78μg/ml against T.mentagrophytes. Griseofulvin appears to be still a potent drug for management of dermatophytoses. Griseofulvin had a MIC range of 0.15g/ml to 5.07 g/ml with MIC50 at1.26 g/ml and MIC90 at 2.53 g/ml against T.rubrum; and MIC range of 0.31μg/ml to 5.07μg/ml with MIC50 at 1.26μg/ml and MIC90 at 2.53μg/ml against T.mentagrophytes. Fluconazole showed a high MIC range of 0.19 g/ml to 50 g/ml and MIC50 was high at 1.56g/ml and MIC90 was also high at 12.5 g/ml against T.rubrum; and a high MIC range of 0.09μg/ml to 25.0μg/ml, with MIC50 at 1.56μg/ml and MIC90 at 12.5μg/ml towards T.mentagrophytes. The technique was found to be easy to perform and reliable with consistent results.

scholarly journals Evaluation of susceptibility of Trichophyton mentagrophytes and Trichophyton rubrum clinical isolates to antifungal drugs using a modified CLSI microdilution method (M38-A)

2007 ◽  
Vol 56 (4) ◽  
pp. 514-518 ◽  
Author(s):  
Maria Elisabete da Silva Barros ◽  
Daniel de Assis Santos ◽  
Júnia Soares Hamdan
Keyword(s):  
Antifungal Agents ◽  
Susceptibility Testing ◽  
Incubation Temperature ◽  
Trichophyton Rubrum ◽  
Trichophyton Mentagrophytes ◽  
Antifungal Drugs ◽  
Standard Protocol ◽  
Broth Microdilution ◽  
Microdilution Method ◽  
Broth Microdilution Method

Onychomycosis is a common adult human mycosis, and dermatophytes of the Trichophyton genera are the most common causative agent. Many antimycotic agents are safe and highly effective for the treatment of dermatophytosis, and are available for clinical practice. Successful treatment depends on the ability of antifungal drugs to eradicate the fungal isolates. The aim of this work was to determine the MICs of four antifungal drugs (fluconazole, itraconazole, terbinafine and griseofulvin) recognized for ungual dermatophytosis treatment caused by Trichophyton species, especially Trichophyton mentagrophytes and Trichophyton rubrum. MICs were determined using a broth microdilution method in accordance with Clinical and Laboratory Standards Institute approved standard M38-A with some modifications, such as an incubation temperature of 28 °C, an incubation time of 7 days and inocula constituted of only microconidia. The results showed that the activities of terbinafine and itraconazole were significantly higher (MICs of <0.007–0.031 and 0.015–0.25 μg ml−1, respectively) than other tested agents. All isolates had reduced susceptibility to fluconazole (1–64 μg ml−1). The MIC of griseofulvin varied among strains (MICs of 0.062–1 μg ml−1). The parameters adopted to perform susceptibility testing of T. rubrum and T. mentagrophytes to antifungal agents appeared to be suitable and reliable, and could contribute to the possible development of a standard protocol.

scholarly journals In Vitro Antifungal Susceptibility Profiles of 12 Antifungal Drugs against 55 Trichophyton schoenleinii Isolates from Tinea Capitis Favosa Patients in Iran, Turkey, and China

2016 ◽  
Vol 61 (2) ◽  
Author(s):  
Shuwen Deng ◽  
Saham Ansari ◽  
Macit Ilkit ◽  
Haleh Rafati ◽  
Mohammad T. Hedayati ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
Antifungal Susceptibility ◽  
Antifungal Drugs ◽  
Content Type ◽  
Microdilution Method ◽  
Broth Microdilution Method ◽  
In Vitro Antifungal Susceptibility ◽  
Trichophyton Schoenleinii ◽  
Susceptibility Profiles

ABSTRACT Trichophyton schoenleinii is an anthropophilic dermatophyte mainly causing tinea favosa of the scalp in certain regions of the world, especially Africa and Asia. We investigated the in vitro susceptibilities of 55 T. schoenleinii isolates collected over the last 30 years from Iran, Turkey, and China to 12 antifungals using the CLSI broth microdilution method. Our results revealed that terbinafine and ketoconazole were the most potent antifungal agents among those tested, independently of the geographic regions where strains were isolated.

scholarly journals Antifungal Activities of SCY-078 (MK-3118) and Standard Antifungal Agents against Clinical Non-Aspergillus Mold Isolates

2015 ◽  
Vol 59 (7) ◽  
pp. 4308-4311 ◽  
Author(s):  
Frédéric Lamoth ◽  
Barbara D. Alexander
Keyword(s):  
Antifungal Agents ◽  
Antifungal Drugs ◽  
Paecilomyces Variotii ◽  
Glucan Synthase ◽  
Content Type ◽  
Antifungal Activities ◽  
Highly Active ◽  
Scedosporium Prolificans ◽  
Synthase Inhibitor

ABSTRACTThe limited armamentarium of active and oral antifungal drugs against emerging non-Aspergillusmolds is of particular concern. Current antifungal agents and the new orally available beta-1,3-d-glucan synthase inhibitor SCY-078 were testedin vitroagainst 135 clinical non-Aspergillusmold isolates. Akin to echinocandins, SCY-078 showed no or poor activity againstMucoromycotinaandFusariumspp. However, SCY-078 was highly active againstPaecilomyces variotiiand was the only compound displaying some activity against notoriously panresistantScedosporium prolificans.

In vitro antifungal susceptibility of griseofulvin, fluconazole, itraconazole and terbinafine against clinical isolates of Trichophyton rubrum and Trichophyton mentagrophytes

2014 ◽  
Vol 1 (4) ◽  
pp. 26-28
Author(s):  
KR Reddy ◽  
SR Reddy
Keyword(s):  
Trichophyton Rubrum ◽  
Clinical Laboratory ◽  
Antifungal Susceptibility ◽  
Trichophyton Mentagrophytes ◽  
Drug Susceptibility ◽  
Antifungal Drugs ◽  
Clinical Isolates ◽  
National Committee ◽  
In Vitro Antifungal Susceptibility

Investigations on antifungal drug susceptibility were carried out on 90 clinical isolates of Trichophyton rubrum, and Trichophyton mentagrophytes with four antifungal drugs, namely griseofulvin, fluconazole, itraconazole and terbinafine as suggested by National Committee for Clinical Laboratory Standards (NCCLS) M27A (1997) document by broth macrodilution method to standardize in vitro antifungal susceptibility testing and to find out the Minimum Inhibitory Concentration (MIC) of the drugs. In this study, terbinafine was found to be the most efficient drug for all isolates. Terbinafine had the lowest MIC range of 0.001 g/mlto 0.09 g/ml and MIC50 was low at 0.005 g/ml and MIC90 was also low at 0.04 g/ml against T. rubrum; and MIC range of 0.001pg/ml to 0.19pg/ml with a MIC50 of 0.01pg/ml and MIC90 at 0.09 pg/ml against T. mentagrophytes. Itraconazole showed antifungal activity superior to that of fluconazole, with a MIC range of 0.04g/ml to l.56g/ml, with MIC50 at 0.19pg/m land MIC90 at l.56g/ml against T. rubrum; and MIC range of 0.04.g/ml to 1.56pg/ml, with MIC50 at 0.19pg/ml and MIC90 at 0.78pg/ml against T. mentagrophytes. Griseofulvin appears to be still a potent drug for management of dermatophytoses. Griseofulvin had a MIC range of 0.15g/ml to 5.07 g/ml with MIC50 at l.26 g/ml and MIC90 at 2.53 g/ml against T. rubrum; and MIC range of 0.31pg/ml to 5.07pg/ml with MIC50 at 1.26pg/ml and MIC90 at 2.53pg/ml against T. mentagrophytes. Fluconazole showed a high MIC range of 0.19 g/ml to 50 g/ml and MIC50 was high at 1.56g/ml and MIC90 was also high at 12.5 g/ml against T. rubrum; and a high MIC range of 0.09pg/ml to 25.0pg/ml, with MIC50 at 1.56pg/ml and MIC90 at 12.5pg/ml towards T. mentagrophytes. The technique was found to be easy to perform and reliable with consistent results.DOI: http://dx.doi.org/10.3126/jucms.v1i4.9569 Journal of Universal College of Medical Sciences (2013) Vol.1 No.04: 26-28

scholarly journals In VitroandIn VivoAssessment of Dermatophyte Acquired Resistance to Efinaconazole, a Novel Triazole Antifungal

2014 ◽  
Vol 58 (8) ◽  
pp. 4920-4922 ◽  
Author(s):  
Atsushi Iwata ◽  
Yoko Watanabe ◽  
Naomichi Kumagai ◽  
Maria Katafuchi-Nagashima ◽  
Keita Sugiura ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Trichophyton Rubrum ◽  
Acquired Resistance ◽  
Continuous Exposure ◽  
Experimental Conditions ◽  
Resistance Development ◽  
Content Type ◽  
Induce Resistance ◽  
Nail Infection

ABSTRACTEfinaconazole 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 ofTrichophyton rubrumstrains to efinaconazolein 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.

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