Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 31, Issue 1, Pages 23-30Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2014.1003215
Keywords
Angelica keiskei; 3CL(pro); chalcone; PLpro; SARS-CoV
Funding
- KRIBB Research Initiative Program and Fishery Commercialization Technology Development Program through KIMST (Korea Institute of Marine Science & Technology promotion) - Ministry of Oceans and Fisheries (MOF), Republic of Korea
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Two viral proteases of severe acute respiratory syndrome coronavirus (SARS-CoV), a chymotrypsin-like protease (3CL(pro)) 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 (3CL(pro) and PLpro) were determined (cell-free/based). Of the isolated alkylated chalcones, chalcone 6, containing the perhydroxyl group, exhibited the most potent 3CL(pro) and PLpro inhibitory activity with IC50 values of 11.4 and 1.2 mu M. 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 PLpro.
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