Discovery of chebulagic acid and punicalagin as novel allosteric inhibitors of SARS-CoV-2 3CLpro

被引：54

作者：

Du, Ruikun ^{[1
,2
,3
]}

Cooper, Laura ^{[4
]}

Chen, Zinuo ^{[1
]}

Lee, Hyun ^{[5
]}

Rong, Lijun ^{[4
]}

Cui, Qinghua ^{[1
,2
,3
]}

机构：

[1] Shandong Univ Tradit Chinese Med, Coll Pharm, Jinan 250355, Peoples R China

[2] Shandong Univ Tradit Chinese Med, Expt Ctr, Jinan 250355, Peoples R China

[3] Shandong Univ Tradit Chinese Med, Qingdao Acad Chinese Med Sci, Qingdao 266122, Peoples R China

[4] Univ Illinois, Coll Med, Dept Microbiol & Immunol, Chicago, IL 60612 USA

[5] Univ Illinois, Dept Pharmaceut Sci, Ctr Bimol Sci, Coll Pharm,Biophys Core Res Resources Ctr, Chicago, IL 60607 USA

来源：

ANTIVIRAL RESEARCH | 2021年 / 190卷

关键词：

SARS-CoV-2; Chebulagic acid; Punicalagin; 3CLpro; Allosteric inhibitor; COVALENT;

D O I：

10.1016/j.antiviral.2021.105075

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The emerging SARS-CoV-2 infection is the cause of the global COVID-19 pandemic. To date, there are limited therapeutic options available to fight this disease. Here we examined the inhibitory abilities of two broad-spectrum antiviral natural products chebulagic acid (CHLA) and punicalagin (PUG) against SARS-CoV-2 viral replication. Both CHLA and PUG reduced virus-induced plaque formation in Vero-E6 monolayer at noncytotoxic concentrations, by targeting the enzymatic activity of viral 3-chymotrypsin-like cysteine protease (3CL(pro)) as allosteric regulators. Our study demonstrates the potential use of CHLA and PUG as novel COVID-19 therapies.

引用

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