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

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Chalcones isolated from Angelica keiskei inhibit cysteine proteases of SARS-CoV
Ji Young Park; Jin-A Ko; D W Kim; Y M Kim; Hyung Jun KwonHyung Jae JeongCha Young Kim; K H Park; Woo Song Lee; Young Bae Ryu
Bibliographic Citation
Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 31, no. 2, pp. 23-30
Publication Year
Two viral proteases of severe acute respiratory syndrome coronavirus (SARS-CoV), a chymotrypsin-like protease (3CLpro) and a papain-like protease (PLpro) 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 (3CLpro and PLpro) were determined (cell-free/based). Of the isolated alkylated chalcones, chalcone 6, containing the perhydroxyl group, exhibited the most potent 3CLpro and PLpro 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 3CLpro, whereas noncompetitive inhibition was observed with the SARS-CoV PLpro.
3CLproAngelica keiskeichalconePLproSARS-CoV
T&F (Taylor & Francis)
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Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
Jeonbuk Branch Institute > 1. Journal Articles
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