Glycyrrhizin Inhibits SARS-CoV-2 Entry into Cells by Targeting ACE2

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...

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Bibliographic Details
Published in:Life (Basel, Switzerland) Switzerland), 2022-10, Vol.12 (11), p.1706
Main Authors: He, Ming-Feng, Liang, Jian-Hui, Shen, Yan-Ni, Zhang, Jin-Wen, Liu, Ying, Yang, Kuang-Yang, Liu, Li-Chu, Wang, Junyi, Xie, Qian, Hu, Chun, Song, Xun, Wang, Yan
Format: Article
Language:English
Subjects:
ACE2
Angiotensin
Angiotensin converting enzyme
Angiotensin-converting enzyme 2
Care and treatment
Chinese medicine
Coronaviruses
COVID-19
Drug targeting
Epidemics
Glycyrrhizin
Health aspects
Herbal medicine
Kinases
Medicine, Botanic
Medicine, Chinese
Medicine, Herbal
Methods
Peptidyl-dipeptidase A
Protein binding
Respiratory diseases
RNA
Saponins
SARS-CoV-2
Severe acute respiratory syndrome
Severe acute respiratory syndrome coronavirus 2
Spike protein
spike protein RBD
Traditional Chinese medicine
Venn diagrams
Viral diseases
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Summary: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.
ISSN:2075-1729
2075-1729
DOI:10.3390/life12111706