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Antifungal Activity of Gentamicin B1 against Systemic Plant Mycoses

Background: Gentamicin is a broad-spectrum aminoglycoside antibiotic produced by Micromonospora purpurea bacteria, effective against Gram-negative bacterial infections. Major fractions of the gentamicin complex (C1, C1a, C2, C2a) possess weak antifungal activity and one of the minor components (A, A...

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Autor principal: Banfalvi, Gaspar
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287848/
https://www.ncbi.nlm.nih.gov/pubmed/32455775
http://dx.doi.org/10.3390/molecules25102401
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author Banfalvi, Gaspar
author_facet Banfalvi, Gaspar
author_sort Banfalvi, Gaspar
collection PubMed
description Background: Gentamicin is a broad-spectrum aminoglycoside antibiotic produced by Micromonospora purpurea bacteria, effective against Gram-negative bacterial infections. Major fractions of the gentamicin complex (C1, C1a, C2, C2a) possess weak antifungal activity and one of the minor components (A, A1–A4, B, B1, X), gentamicin B1 was found to be a strong antifungal agent. Methods: This work uses in vitro and in vivo dilution methods to compare the antifusarial, antiaspergillic and anticryptococcal effects of gentamicin derivatives and structurally-related congeners. Results: The in vitro antifusarial activity of gentamicin B1 (minimum inhibitory concentration (MIC) 0.4 μg/mL) and structurally-related compounds (MIC 0.8–12.5 μg/mL) suggests that the purpuroseamine ring substituents are responsible for the specific antimycotic effect. The functional groups of the garoseamine and 2-deoxystreptamine rings of gentamicin derivatives are identical in gentamicin compounds and are unlikely to exert a significant antifungal effect. Among soil dermatophytes, Microsporum gypseum was more susceptible to gentamicin B1 (MIC 3.1 µg/mL) than Trichophyton gypseum (MIC 25 µg/mL). The in vitro antifungal effect of gentamicin B1 against plant pathogenic fungi was comparable to primary antifungal agents. Conclusion: Gentamicin is already in medical use. In vitro and preclinical in vivo synergisms of gentamicin B1 with amphotericin B suggest immediate clinical trials starting with subtoxic doses.
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spelling pubmed-72878482020-06-15 Antifungal Activity of Gentamicin B1 against Systemic Plant Mycoses Banfalvi, Gaspar Molecules Article Background: Gentamicin is a broad-spectrum aminoglycoside antibiotic produced by Micromonospora purpurea bacteria, effective against Gram-negative bacterial infections. Major fractions of the gentamicin complex (C1, C1a, C2, C2a) possess weak antifungal activity and one of the minor components (A, A1–A4, B, B1, X), gentamicin B1 was found to be a strong antifungal agent. Methods: This work uses in vitro and in vivo dilution methods to compare the antifusarial, antiaspergillic and anticryptococcal effects of gentamicin derivatives and structurally-related congeners. Results: The in vitro antifusarial activity of gentamicin B1 (minimum inhibitory concentration (MIC) 0.4 μg/mL) and structurally-related compounds (MIC 0.8–12.5 μg/mL) suggests that the purpuroseamine ring substituents are responsible for the specific antimycotic effect. The functional groups of the garoseamine and 2-deoxystreptamine rings of gentamicin derivatives are identical in gentamicin compounds and are unlikely to exert a significant antifungal effect. Among soil dermatophytes, Microsporum gypseum was more susceptible to gentamicin B1 (MIC 3.1 µg/mL) than Trichophyton gypseum (MIC 25 µg/mL). The in vitro antifungal effect of gentamicin B1 against plant pathogenic fungi was comparable to primary antifungal agents. Conclusion: Gentamicin is already in medical use. In vitro and preclinical in vivo synergisms of gentamicin B1 with amphotericin B suggest immediate clinical trials starting with subtoxic doses. MDPI 2020-05-21 /pmc/articles/PMC7287848/ /pubmed/32455775 http://dx.doi.org/10.3390/molecules25102401 Text en © 2020 by the author. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Banfalvi, Gaspar
Antifungal Activity of Gentamicin B1 against Systemic Plant Mycoses
title Antifungal Activity of Gentamicin B1 against Systemic Plant Mycoses
title_full Antifungal Activity of Gentamicin B1 against Systemic Plant Mycoses
title_fullStr Antifungal Activity of Gentamicin B1 against Systemic Plant Mycoses
title_full_unstemmed Antifungal Activity of Gentamicin B1 against Systemic Plant Mycoses
title_short Antifungal Activity of Gentamicin B1 against Systemic Plant Mycoses
title_sort antifungal activity of gentamicin b1 against systemic plant mycoses
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287848/
https://www.ncbi.nlm.nih.gov/pubmed/32455775
http://dx.doi.org/10.3390/molecules25102401
work_keys_str_mv AT banfalvigaspar antifungalactivityofgentamicinb1againstsystemicplantmycoses