Glycyrrhizic Acid Exerts Inhibitory Activity Against the Spike Protein of SARS-CoV-2

Overview

Journal Phytomedicine

Specialty Rehabilitation Medicine

Date 2020 Oct 12

PMID 33041173

Citations 69

Authors

Shaopeng Yu

Yuying Zhu

Jiaruo Xu

Guangtao Yao

Pei Zhang

Mengge Wang

Yongfang Zhao

Guoqiang Lin

Hongzhuan Chen

Lili Chen

Jiange Zhang

Affiliations

Soon will be listed here.

Abstract

Coronavirus causes a disease with high infectivity and pathogenicity, especially SARS in 2003, MERS in 2012, and COVID-2019 currently. The spike proteins of these coronaviruses are critical for host cell entry by receptors. Thus, searching for broad-spectrum anti-coronavirus candidates, such as spike protein inhibitors, is vital and desirable due to the mutations in the spike protein. In this study, a combination of computer-aided drug design and biological verification was used to discover active monomers from traditional Chinese medicine. Surface plasmon resonance (SPR) assays and NanoBit assays were used to verify the predicated compounds with their binding activities to spike proteins and inhibitory activities on the SARS-CoV-2 RBD/ACE2 interaction, respectively. Furthermore, an MTT assay was used to evaluate the cell toxicities of active compounds. As a result, glycyrrhizic acid (ZZY-44) was found to be the most efficient and nontoxic broad-spectrum anti-coronavirus molecule in vitro, especially, the significant effect on SARS-CoV-2, which provided a theoretical basis for the study of the pharmacodynamic material basis of traditional Chinese medicine against SARS-CoV-2 and offered a lead compound for further structural modification in order to obtain more effective candidate drugs against SARS-CoV-2.

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