Evaluation of polyphenols from Broussonetia papyrifera as coronavirus protease inhibitors.

Abstract:

: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), 3'-(3-methylbut-2-enyl)-3',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 μM. 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.

authors

Park JY,Yuk HJ,Ryu HW,Lim SH,Kim KS,Park KH,Ryu YB,Lee WS

doi

10.1080/14756366.2016.1265519

subject

Has Abstract

pub_date

2017-12-01 00:00:00

pages

504-515

issue

1

eissn

1475-6366

issn

1475-6374

journal_volume

32

pub_type

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