Antifungal Activity of : From the Chemical Composition to the Mitochondrial Toxic Effects and Tyrosinase Inhibition.

Antibiotics (Basel)

REQUIMTE/LAQV, Laboratório de Farmacognosia, Departamento de Química, Faculdade de Farmácia, Universidade do Porto, 4050-313 Porto, Portugal.

Published: May 2023


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Article Abstract

Pest resistance against fungicides is a widespread and increasing problem, with impact on crop production and public health, making the development of new fungicides an urgent need. Chemical analyses of a crude methanol extract (CME) of leaves revealed the presence of sugars, phospholipids, phytosterols, guieranone A, porphyrin-containing compounds, and phenolics. To connect chemical composition with biological effects, solid-phase extraction was used to discard water-soluble compounds with low affinity for the C18 matrix and obtain an ethyl acetate fraction (EAF) that concentrates guieranone A and chlorophylls, and a methanol fraction (MF) dominated by phenolics. While the CME and MF exhibited poor antifungal activity against , and , the EAF demonstrated antifungal activity against these filamentous fungi, particularly against . Studies with yeasts revealed that the EAF has strong effectiveness against , and with MICs of 8, 8 and 16 μg/mL, respectively. A combination of in vivo and in vitro studies shows that the EAF can function as a mitochondrial toxin, compromising complexes I and II activities, and as a strong inhibitor of fungal tyrosinase (Ki = 14.40 ± 4.49 µg/mL). Thus, EAF appears to be a promising candidate for the development of new multi-target fungicides.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10215606PMC
http://dx.doi.org/10.3390/antibiotics12050869DOI Listing

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