期刊
JOURNAL OF ADVANCED RESEARCH
卷 36, 期 -, 页码 201-210出版社
ELSEVIER
DOI: 10.1016/j.jare.2021.11.012
关键词
COVID-19; SARS-CoV-2; Licorice; Licorice-saponin A3; Glycyrrhetinic acid
资金
- National Natural Science Foundation of China [81891010/81891011, 81725023, 82173950, 82003614, 81802002, 81873579, 31770192, 32070187]
- National Key Research and Development Program of China [2017YFC1700405]
- Science & Technology Department of Xinjiang Uygur Autonomous Region [2018AB012]
- Youth Innovation Promotion Association CAS
This study discovered potential natural inhibitors of SARS-CoV-2 from licorice, a traditional Chinese herbal medicine. Two compounds, licorice-saponin A3 and glycyrrhetinic acid, were found to potently inhibit SARS-CoV-2 infection and could be promising candidates for antiviral drug development.
Introduction: The COVID-19 global epidemic caused by severe acute respiratory syndrome coronavirus (SARS-CoV-2) is a great public health emergency. Discovering antiviral drug candidates is urgent for the prevention and treatment of COVID-19. Objectives: This work aims to discover natural SARS-CoV-2 inhibitors from the traditional Chinese herbal medicine licorice. Methods: We screened 125 small molecules from Glycyrrhiza uralensis Fisch. (licorice, Gan-Cao) by virtual ligand screening targeting the receptor-binding domain (RBD) of SARS-CoV-2 spike protein. Potential hit compounds were further evaluated by ELISA, SPR, luciferase assay, antiviral assay and pharmacokinetic study. Results: The triterpenoids licorice-saponin A3 (A3) and glycyrrhetinic acid (GA) could potently inhibit SARS-CoV-2 infection, with EC50 of 75 nM and 3.17 mu M, respectively. Moreover, we reveal that A3 mainly targets the nsp7 protein, and GA binds to the spike protein RBD of SARS-CoV-2. Conclusion: In this work, we found GA and A3 from licorice potently inhibit SARS-CoV-2 infection by affecting entry and replication of the virus. Our findings indicate that these triterpenoids may contribute to the clinical efficacy of licorice for COVID-19 and could be promising candidates for antiviral drug development. (C) 2021 The Authors. Published by Elsevier B.V. on behalf of Cairo University.
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