Ontology highlight
ABSTRACT: 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 µM, 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.
SUBMITTER: Yi Y
PROVIDER: S-EPMC8620242 | biostudies-literature | 2022 Feb
REPOSITORIES: biostudies-literature
Journal of advanced research 20211126
<h4>Introduction</h4>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.<h4>Objectives</h4>This work aims to discover natural SARS-CoV-2 inhibitors from the traditional Chinese herbal medicine licorice.<h4>Methods</h4>We screened 125 small molecules from <i>Glycyrrhiza uralensis</i> Fisch. (licorice, Gan-Cao) by virtual li ...[more]