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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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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2020
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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. |
format | Online Article Text |
id | pubmed-7287848 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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 |