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Title 

Evaluation of polyphenols from Broussonetia papyrifera as coronavirus protease inhibitors

Authors 

Ji Young ParkHeung Joo YukHyung Won RyuSu Hwan LimKyung Su KimK H ParkYoung Bae RyuWoo Song Lee

Publisher 

Informa Healthcare

Issue Date 

2017

Citation 

Journal of Enzyme Inhibition and Medicinal Chemistry

Keywords 

Broussonetia papyriferacoronaviruspapain-like proteasepolyphenolSARS

Abstract 

he 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.

ISSN 

1475-6366

Link 

http://dx.doi.org/10.1080/14756366.2016.1265519

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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