7,315
Views
209
CrossRef citations to date
0
Altmetric
Original Article

Evaluation of polyphenols from Broussonetia papyrifera as coronavirus protease inhibitors

, , , , , , & show all
Pages 504-512 | Received 19 Aug 2016, Accepted 16 Nov 2016, Published online: 22 Jan 2017
 

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.

Disclosure statement

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.

Funding

This research was supported by the KRIBB Research Initiative Program and Fishery Commercialization Technology Development Program through KIMST (Korea Institute of Marine Science & Technology promotion), funded by the Ministry of Oceans and Fisheries (MOF), Republic of Korea.