RT Journal Article
SR Electronic
T1 <em>Scutellaria baicalensis</em> extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease <em>in vitro</em>
JF bioRxiv
FD Cold Spring Harbor Laboratory
SP 2020.04.10.035824
DO 10.1101/2020.04.10.035824
A1 Liu, Hongbo
A1 Ye, Fei
A1 Sun, Qi
A1 Liang, Hao
A1 Li, Chunmei
A1 Lu, Roujian
A1 Huang, Baoying
A1 Tan, Wenjie
A1 Lai, Luhua
YR 2020
UL http://biorxiv.org/content/early/2020/04/12/2020.04.10.035824.abstract
AB COVID-19 has become a global pandemic that threatens millions of people worldwide. There is an urgent call for developing effective drugs against the virus (SARS-CoV-2) causing this disease. The main protease of SARS-CoV-2, 3C-like protease (3CLpro), is highly conserved across coronaviruses and is essential for the maturation process of viral polyprotein. Scutellariae radix (Huangqin in Chinese), the root of Scutellaria baicalensis has been widely used in traditional Chinese medicine to treat viral infection related symptoms. The extracts of S. baicalensis have exhibited broad spectrum antiviral activities. We studied the anti-SARS-CoV-2 activity of S. baicalensis and its ingredient compounds. We found that the ethanol extract of S. baicalensis inhibits SARS-CoV-2 3CLpro activity in vitro and the replication of SARS-CoV-2 in Vero cells with an EC50 of 0.74 μg/ml. Among the major components of S. baicalensis, baicalein strongly inhibits SARS-CoV-2 3CLpro activity with an IC50 of 0.39 μM. We further identified four baicalein analogue compounds from other herbs that inhibit SARS-CoV-2 3CLpro activity at microM concentration. Our study demonstrates that the extract of S. baicalensis has effective anti-SARS-CoV-2 activity and baicalein and analogue compounds are strong SARS-CoV-2 3CLpro inhibitors.Competing Interest StatementThe authors have declared no competing interest.