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Article Publish Status: FREE
Abstract Title:

Chalcones isolated from Angelica keiskei inhibit cysteine proteases of SARS-CoV.

Abstract Source:

J Enzyme Inhib Med Chem. 2016 ;31(1):23-30. Epub 2015 Feb 16. PMID: 25683083

Abstract Author(s):

Ji-Young Park, Jin-A Ko, Dae Wook Kim, Young Min Kim, Hyung-Jun Kwon, Hyung Jae Jeong, Cha Young Kim, Ki Hun Park, Woo Song Lee, Young Bae Ryu

Article Affiliation:

Ji-Young Park

Abstract:

Two viral proteases of severe acute respiratory syndrome coronavirus (SARS-CoV), a chymotrypsin-like protease (3CL(pro)) and a papain-like protease (PL(pro)) are attractive targets for the development of anti-SARS drugs. In this study, nine alkylated chalcones (1-9) and four coumarins (10-13) were isolated from Angelica keiskei, and the inhibitory activities of these constituents against SARS-CoV proteases (3CL(pro) and PL(pro)) were determined (cell-free/based). Of the isolated alkylated chalcones, chalcone 6, containing the perhydroxyl group, exhibited the most potent 3CL(pro) and PL(pro) inhibitory activity with IC50 values of 11.4 and 1.2 µM. Our detailed protein-inhibitor mechanistic analysis of these species indicated that the chalcones exhibited competitive inhibition characteristics to the SARS-CoV 3CL(pro), whereas noncompetitive inhibition was observed with the SARS-CoV PL(pro).

Study Type : In Vitro Study

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