Chalcones isolated from<i>Angelica keiskei</i>inhibit cysteine proteases of SARS-CoV

Ji Young Park(Korea Research Institute of Bioscience and Biotechnology), Jin-A Ko(Korea Research Institute of Bioscience and Biotechnology), Dae Wook Kim(Gyeongsang National University), Young‐Min Kim(Chonnam National University), Hyung-Jun Kwon(Korea Research Institute of Bioscience and Biotechnology), Hyung Jae Jeong(Korea Research Institute of Bioscience and Biotechnology), Cha Young Kim(Korea Research Institute of Bioscience and Biotechnology), Ki Hun Park(Gyeongsang National University), Woo Song Lee(Korea Research Institute of Bioscience and Biotechnology), Young Bae Ryu(Korea Research Institute of Bioscience and Biotechnology)
Journal of Enzyme Inhibition and Medicinal Chemistry
February 16, 2015
10.3109/14756366.2014.1003215
Cited by 227Open Access
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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).

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