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Open AccessArticle

Antifungal Activity of Gentamicin B1 against Systemic Plant Mycoses

Department of Molecular Biotechnology and Microbiology, University of Debrecen, 4010 Debrecen, Hungary
Academic Editor: Derek J. McPhee
Molecules 2020, 25(10), 2401; https://doi.org/10.3390/molecules25102401
Received: 7 April 2020 / Revised: 10 May 2020 / Accepted: 13 May 2020 / Published: 21 May 2020
(This article belongs to the Special Issue The Medicinal Chemistry of Antibiotics)
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. View Full-Text
Keywords: gentamicin; antifungal effect; pulmonary diseases; fusariosis; aspergillosis; synergism gentamicin; antifungal effect; pulmonary diseases; fusariosis; aspergillosis; synergism
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MDPI and ACS Style

Banfalvi, G. Antifungal Activity of Gentamicin B1 against Systemic Plant Mycoses. Molecules 2020, 25, 2401.

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