Evaluation of polyphenols from Broussonetia papyrifera as coronavirus protease inhibitors

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Evaluation of polyphenols from Broussonetia papyrifera as coronavirus protease inhibitors
Ji Young Park; Heung Joo Yuk; Hyung Won Ryu; Su Hwan Lim; Kyung Su Kim; K H Park; Young Bae Ryu; Woo Song Lee
Bibliographic Citation
Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 32, no. 1, pp. 504-512
Publication Year
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.
Broussonetia papyriferacoronaviruspapain-like proteasepolyphenolSARS
T&F (Taylor & Francis)
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Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
Ochang Branch Institute > Natural Product Research Center > 1. Journal Articles
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