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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| Format: | Article |
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MDPI AG
2022-10-01
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| Series: | Life |
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| Online Access: | https://www.mdpi.com/2075-1729/12/11/1706 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Ming-Feng He |
| collection | DOAJ |
| description | 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 <i>Glycyrrhizae Radix et Rhizoma</i> is a frequent herb in TCM formulas against COVID-19. The extract of <i>Glycyrrhizae Radix et Rhizoma</i> 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 <i>Glycyrrhizae Radix et Rhizoma</i>, 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. |
| first_indexed | 2024-03-09T18:55:24Z |
| format | Article |
| id | doaj.art-13605ce0b4084270855976f1e3fe1206 |
| institution | Directory Open Access Journal |
| issn | 2075-1729 |
| language | English |
| last_indexed | 2024-03-09T18:55:24Z |
| publishDate | 2022-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Life |
| spelling | doaj.art-13605ce0b4084270855976f1e3fe12062023-11-24T05:29:37ZengMDPI AGLife2075-17292022-10-011211170610.3390/life12111706Glycyrrhizin Inhibits SARS-CoV-2 Entry into Cells by Targeting ACE2Ming-Feng He0Jian-Hui Liang1Yan-Ni Shen2Jin-Wen Zhang3Ying Liu4Kuang-Yang Yang5Li-Chu Liu6Junyi Wang7Qian Xie8Chun Hu9Xun Song10Yan Wang11Foshan Hospital of Traditional Chinese Medicine, Foshan 528000, ChinaCenter for Translation Medicine Research and Development, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, ChinaCenter for Translation Medicine Research and Development, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, ChinaCenter for Translation Medicine Research and Development, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, ChinaCollege of Pharmacy, Shenzhen Technology University, Shenzhen 518118, ChinaFoshan Hospital of Traditional Chinese Medicine, Foshan 528000, ChinaFoshan Hospital of Traditional Chinese Medicine, Foshan 528000, ChinaBluewood Associates Co., Ltd., Suzhou 215134, ChinaCenter for Translation Medicine Research and Development, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, ChinaKey Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, ChinaCollege of Pharmacy, Shenzhen Technology University, Shenzhen 518118, ChinaCenter for Translation Medicine Research and Development, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, ChinaCoronavirus 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 <i>Glycyrrhizae Radix et Rhizoma</i> is a frequent herb in TCM formulas against COVID-19. The extract of <i>Glycyrrhizae Radix et Rhizoma</i> 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 <i>Glycyrrhizae Radix et Rhizoma</i>, 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.https://www.mdpi.com/2075-1729/12/11/1706SARS-CoV-2ACE2glycyrrhizinspike protein RBD |
| spellingShingle | 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 Glycyrrhizin Inhibits SARS-CoV-2 Entry into Cells by Targeting ACE2 Life SARS-CoV-2 ACE2 glycyrrhizin spike protein RBD |
| title | Glycyrrhizin Inhibits SARS-CoV-2 Entry into Cells by Targeting ACE2 |
| title_full | Glycyrrhizin Inhibits SARS-CoV-2 Entry into Cells by Targeting ACE2 |
| title_fullStr | Glycyrrhizin Inhibits SARS-CoV-2 Entry into Cells by Targeting ACE2 |
| title_full_unstemmed | Glycyrrhizin Inhibits SARS-CoV-2 Entry into Cells by Targeting ACE2 |
| title_short | Glycyrrhizin Inhibits SARS-CoV-2 Entry into Cells by Targeting ACE2 |
| title_sort | glycyrrhizin inhibits sars cov 2 entry into cells by targeting ace2 |
| topic | SARS-CoV-2 ACE2 glycyrrhizin spike protein RBD |
| url | https://www.mdpi.com/2075-1729/12/11/1706 |
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