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Bioorg Chem ; 99: 103760, 2020 06.
Artículo en Inglés | MEDLINE | ID: mdl-32251946

RESUMEN

Eight unexpected vibralactone homodimers, bisvibralactones A-H (1-8), and three new vibralactone monomers, hirsutumins A-C (9-11), were isolated from the culture of Stereum hirsutum. Their structures and absolute configurations were determined by detailed analyses of NMR, optical rotations, ECD, and high-resolution mass spectra as well as chemical transformation. Compounds 1-8 are unusual vibralactone dimers formed by the esterification of two vibralactone monomers. The absolute configurations of compounds 1 and 5 were determined by chemical conversions. All of the isolated compounds were evaluated for Porcine Pancreatic Lipase (PPL) inhibitory activities, and compound 10 showed significant inhibitory activity against PPL, with an IC50 value of 8.31 ± 1.04 µM.


Asunto(s)
Basidiomycota/química , Inhibidores Enzimáticos/farmacología , Lactonas/farmacología , Lipasa/antagonistas & inhibidores , Animales , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/metabolismo , Lactonas/química , Lactonas/metabolismo , Lipasa/metabolismo , Estructura Molecular , Páncreas/enzimología , Relación Estructura-Actividad , Porcinos
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