作者
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
发表日期
2016/1/2
期刊
Journal of enzyme inhibition and medicinal chemistry
卷号
31
期号
1
页码范围
23-30
出版商
Taylor & Francis
简介
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 (19) and four coumarins (1013) 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.
引用总数
201720182019202020212022202320247215870604514
学术搜索中的文章
JY Park, JA Ko, DW Kim, YM Kim, HJ Kwon, HJ Jeong… - Journal of enzyme inhibition and medicinal chemistry, 2016