Glycyrrhizin Inhibits SARS-CoV-2 Entry into Cells by Targeting ACE2
Ming-Feng He,
Jian-Hui Liang,
Yan-Ni Shen,
Jin-Wen Zhang,
Ying Liu,
Kuang-Yang Yang,
Li-Chu Liu,
Junyi Wang,
Qian Xie,
Chun Hu,
Xun Song,
Yan Wang
Affiliations
Ming-Feng He
Foshan Hospital of Traditional Chinese Medicine, Foshan 528000, China
Jian-Hui Liang
Center for Translation Medicine Research and Development, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, China
Yan-Ni Shen
Center for Translation Medicine Research and Development, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, China
Jin-Wen Zhang
Center for Translation Medicine Research and Development, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, China
Ying Liu
College of Pharmacy, Shenzhen Technology University, Shenzhen 518118, China
Kuang-Yang Yang
Foshan Hospital of Traditional Chinese Medicine, Foshan 528000, China
Li-Chu Liu
Foshan Hospital of Traditional Chinese Medicine, Foshan 528000, China
Junyi Wang
Bluewood Associates Co., Ltd., Suzhou 215134, China
Qian Xie
Center for Translation Medicine Research and Development, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, China
Chun Hu
Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
Xun Song
College of Pharmacy, Shenzhen Technology University, Shenzhen 518118, China
Yan Wang
Center for Translation Medicine Research and Development, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, China
Coronavirus Disease 2019 (COVID-19) is a highly infectious and pathogenic disease caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Early in this epidemic, the herbal formulas used in traditional Chinese medicine (TCM) were widely used for the treatment of COVID-19 in China. According to Venn diagram analysis, we found that Glycyrrhizae Radix et Rhizoma is a frequent herb in TCM formulas against COVID-19. The extract of Glycyrrhizae Radix et Rhizoma exhibits an anti-SARS-CoV-2 replication activity in vitro, but its pharmacological mechanism remains unclear. We here demonstrate that glycyrrhizin, the main active ingredient of Glycyrrhizae Radix et Rhizoma, prevents the coronavirus from entering cells by targeting angiotensin-converting enzyme 2 (ACE2). Glycyrrhizin inhibited the binding of the spike protein of the SARS-CoV-2 to ACE2 in our Western blot-based assay. The following bulk RNA-seq analysis showed that glycyrrhizin down-regulated ACE2 expression in vitro which was further confirmed by Western blot and quantitative PCR. Together, we believe that glycyrrhizin inhibits SARS-CoV-2 entry into cells by targeting ACE2.
