Author: Haixia Su; Sheng Yao; Wenfeng Zhao; Minjun Li; Jia Liu; Weijuan Shang; Hang Xie; Changqiang Ke; Meina Gao; Kunqian Yu; Hong Liu; Jingshan Shen; Wei Tang; Leike Zhang; Jianping Zuo; Hualiang Jiang; Fang Bai; Yan Wu; Yang Ye; Yechun Xu
Title: Discovery of baicalin and baicalein as novel, natural product inhibitors of SARS-CoV-2 3CL protease in vitro Document date: 2020_4_14
ID: ixun0c8g_4
Snippet: The pivotal role of the 3CL protease in processing polyproteins into individual functional proteins for viral replication and a highly conserved substrate specificity of the enzyme among various CoVs make it a promising target for screening of inhibitors. A fluorescence resonance energy transfer (FRET) protease assay was applied to measure the proteolytic activity of the recombinant SARS-CoV-2 3CLpro on a fluorogenic substrate. The detail of the .....
Document: The pivotal role of the 3CL protease in processing polyproteins into individual functional proteins for viral replication and a highly conserved substrate specificity of the enzyme among various CoVs make it a promising target for screening of inhibitors. A fluorescence resonance energy transfer (FRET) protease assay was applied to measure the proteolytic activity of the recombinant SARS-CoV-2 3CLpro on a fluorogenic substrate. The detail of the assay is described in the Experimental section. This FRET-based protease assay was utilized to screen natural products as novel inhibitors of SARS-CoV-2 3CLpro. It was first used to determine the inhibitory activities of the total aqueous extract, fractionations, and purified compounds from S. baicalensis against SARS-CoV-2 3CLpro (see Supplementary Materials, Fig. S1 ). As the result, two fractions from S. baicalensis showed significant inhibition on SARS-CoV-2 3CLpro at 10.0 ïg/mL (Table S1) . Surprisingly, baicalin, the major component in fraction 8, shows an IC50 of 6.41 ïM against the protease, while baicalein, the major component in fraction 12, has author/funder. All rights reserved. No reuse allowed without permission.
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