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J Antibiot (Tokyo) ; 74(5): 317-323, 2021 05.
Artículo en Inglés | MEDLINE | ID: mdl-33558649

RESUMEN

Fungi are important resources for drug development, as they have a diversity of genes, that can produce novel secondary metabolites with effective bioactivities. Here, five depsidone-based analogs were isolated from the rice media of Chaetomium brasiliense SD-596. Their structures were elucidated using NMR and mass spectrometry analysis. Five compounds, including three new depsidone analogs, mollicellin S (1), mollicellin T (2), and mollicellin U (3), and two known compounds, mollicellin D (4) and mollicellin H (5), exhibited significant inhibition against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA), with MIC values ranging from 6.25 to 12.5 µg ml-1. Herein, we identified the predicted plausible biosynthetic cluster of the compounds and discussed the structure-activity relationship. Finally, we found that the introduction of aldehyde and methoxyl groups provide marked improvement for the inhibition against MRSA.


Asunto(s)
Antibacterianos/química , Antibacterianos/farmacología , Depsidos/farmacología , Lactonas/farmacología , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Sordariales/química , Depsidos/química , Descubrimiento de Drogas , Fermentación , Genoma Fúngico , Lactonas/química , Estructura Molecular , Sordariales/genética , Sordariales/metabolismo
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