๐ Evaluation of polyphenols from Broussonetia papyrifera as coronavirus protease inhibitors
Published by Informa UK Limited, trading as Taylor & Francis Group. The current study was designed to assess the inhibitory activity of Broussonetia papyrifera-derived polyphenols against 3-chymotrypsin-like and papain-like coronavirus cysteine proteases. The isolated compounds were broussochalcone B (1), broussochalcone A (2), 4-hydroxyisolonchocarpin (3), papyriflavonol A (4), 3โฒ-(3-methylbut-2-enyl)-3โฒ,4,7-trihydroxyflavane (5), kazinol A (6), kazinol B (7), broussoflavan A (8), kazinol F (9), and kazinol J (10). All polyphenols were more potent against papain-like protease (PLpro) than against 3-chymotripsin-like protease (3CLpro); therefore, we investigated their structural features that were responsible for this selectivity. Compound 4 was the most potent inhibitor of PLpro with an IC50 value of 3.7 ฮผM. The active compounds displayed kinetic behaviors, and the binding constants of their interaction with PLpro were determined from surface plasmon resonance analysis. Our results suggest B. papyrifera constituents as promising candidates for development into potential anti-coronaviral agents.
author
๐ค Park, Ji Young
๐ค Yuk, Heung Joo
๐ค Ryu, Hyung Won
๐ค Lim, Su Hwan
๐ค Kim, Kyung Su
๐ค Park, Ki Hun
๐ค Ryu, Young Bae
๐ค Lee, Woo Song
year
โฐ 2017
issn
๐ 14756374 14756366
volume
32
number
1
page
504-512
citedbycount
15
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