Scutellaria baicalensis extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease in vitro

COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CL pro ) of SARS-CoV-2 is a preferred target for broad spectrum anti-coronavirus drug discovery. We studied the anti-SARS-CoV-2 activity of S. baicalensis and...

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Published in	Journal of enzyme inhibition and medicinal chemistry Vol. 36; no. 1; pp. 497 - 503
Main Authors	Liu, Hongbo, Ye, Fei, Sun, Qi, Liang, Hao, Li, Chunmei, Li, Siyang, Lu, Roujian, Huang, Baoying, Tan, Wenjie, Lai, Luhua
Format	Journal Article
Language	English
Published	England Taylor & Francis 01.01.2021 Taylor & Francis Group
Subjects	3C-like protease Animals Antiviral Agents - pharmacology baicalein Chlorocebus aethiops Coronavirus 3C Proteases - antagonists & inhibitors COVID-19 COVID-19 - drug therapy COVID-19 - enzymology COVID-19 - virology Drug Discovery Enzyme Inhibitors - pharmacology Flavanones - pharmacology Humans In Vitro Techniques Models, Molecular Plant Extracts - pharmacology Protease Inhibitors - pharmacology Research Paper SARS-CoV-2 SARS-CoV-2 - drug effects SARS-CoV-2 - enzymology Scutellaria baicalensis Vero Cells Virus Replication - drug effects COVID-19 3C-like protease SARS-CoV-2 baicalein Scutellaria baicalensis
Online Access	Get full text
ISSN	1475-6366 1475-6374 1475-6374
DOI	10.1080/14756366.2021.1873977

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Abstract	COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CL pro ) of SARS-CoV-2 is a preferred target for broad spectrum anti-coronavirus drug discovery. We studied the anti-SARS-CoV-2 activity of S. baicalensis and its ingredients. We found that the ethanol extract of S. baicalensis and its major component, baicalein, inhibit SARS-CoV-2 3CL pro activity in vitro with IC 50 's of 8.52 µg/ml and 0.39 µM, respectively. Both of them inhibit the replication of SARS-CoV-2 in Vero cells with EC 50 's of 0.74 µg/ml and 2.9 µM, respectively. While baicalein is mainly active at the viral post-entry stage, the ethanol extract also inhibits viral entry. We further identified four baicalein analogues from other herbs that inhibit SARS-CoV-2 3CL pro activity at µM concentration. All the active compounds and the S. baicalensis extract also inhibit the SARS-CoV 3CL pro , demonstrating their potential as broad-spectrum anti-coronavirus drugs.
AbstractList	COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CLpro) of SARS-CoV-2 is a preferred target for broad spectrum anti-coronavirus drug discovery. We studied the anti-SARS-CoV-2 activity of S. baicalensis and its ingredients. We found that the ethanol extract of S. baicalensis and its major component, baicalein, inhibit SARS-CoV-2 3CLpro activity in vitro with IC50’s of 8.52 µg/ml and 0.39 µM, respectively. Both of them inhibit the replication of SARS-CoV-2 in Vero cells with EC50’s of 0.74 µg/ml and 2.9 µM, respectively. While baicalein is mainly active at the viral post-entry stage, the ethanol extract also inhibits viral entry. We further identified four baicalein analogues from other herbs that inhibit SARS-CoV-2 3CLpro activity at µM concentration. All the active compounds and the S. baicalensis extract also inhibit the SARS-CoV 3CLpro, demonstrating their potential as broad-spectrum anti-coronavirus drugs. COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CL pro ) of SARS-CoV-2 is a preferred target for broad spectrum anti-coronavirus drug discovery. We studied the anti-SARS-CoV-2 activity of S. baicalensis and its ingredients. We found that the ethanol extract of S. baicalensis and its major component, baicalein, inhibit SARS-CoV-2 3CL pro activity in vitro with IC 50 's of 8.52 µg/ml and 0.39 µM, respectively. Both of them inhibit the replication of SARS-CoV-2 in Vero cells with EC 50 's of 0.74 µg/ml and 2.9 µM, respectively. While baicalein is mainly active at the viral post-entry stage, the ethanol extract also inhibits viral entry. We further identified four baicalein analogues from other herbs that inhibit SARS-CoV-2 3CL pro activity at µM concentration. All the active compounds and the S. baicalensis extract also inhibit the SARS-CoV 3CL pro , demonstrating their potential as broad-spectrum anti-coronavirus drugs. COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CLpro) of SARS-CoV-2 is a preferred target for broad spectrum anti-coronavirus drug discovery. We studied the anti-SARS-CoV-2 activity of S. baicalensis and its ingredients. We found that the ethanol extract of S. baicalensis and its major component, baicalein, inhibit SARS-CoV-2 3CLpro activity in vitro with IC50's of 8.52 µg/ml and 0.39 µM, respectively. Both of them inhibit the replication of SARS-CoV-2 in Vero cells with EC50's of 0.74 µg/ml and 2.9 µM, respectively. While baicalein is mainly active at the viral post-entry stage, the ethanol extract also inhibits viral entry. We further identified four baicalein analogues from other herbs that inhibit SARS-CoV-2 3CLpro activity at µM concentration. All the active compounds and the S. baicalensis extract also inhibit the SARS-CoV 3CLpro, demonstrating their potential as broad-spectrum anti-coronavirus drugs.COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CLpro) of SARS-CoV-2 is a preferred target for broad spectrum anti-coronavirus drug discovery. We studied the anti-SARS-CoV-2 activity of S. baicalensis and its ingredients. We found that the ethanol extract of S. baicalensis and its major component, baicalein, inhibit SARS-CoV-2 3CLpro activity in vitro with IC50's of 8.52 µg/ml and 0.39 µM, respectively. Both of them inhibit the replication of SARS-CoV-2 in Vero cells with EC50's of 0.74 µg/ml and 2.9 µM, respectively. While baicalein is mainly active at the viral post-entry stage, the ethanol extract also inhibits viral entry. We further identified four baicalein analogues from other herbs that inhibit SARS-CoV-2 3CLpro activity at µM concentration. All the active compounds and the S. baicalensis extract also inhibit the SARS-CoV 3CLpro, demonstrating their potential as broad-spectrum anti-coronavirus drugs. COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CL ) of SARS-CoV-2 is a preferred target for broad spectrum anti-coronavirus drug discovery. We studied the anti-SARS-CoV-2 activity of and its ingredients. We found that the ethanol extract of and its major component, baicalein, inhibit SARS-CoV-2 3CL activity with IC 's of 8.52 µg/ml and 0.39 µM, respectively. Both of them inhibit the replication of SARS-CoV-2 in Vero cells with EC 's of 0.74 µg/ml and 2.9 µM, respectively. While baicalein is mainly active at the viral post-entry stage, the ethanol extract also inhibits viral entry. We further identified four baicalein analogues from other herbs that inhibit SARS-CoV-2 3CL activity at µM concentration. All the active compounds and the extract also inhibit the SARS-CoV 3CL , demonstrating their potential as broad-spectrum anti-coronavirus drugs. COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CL pro ) of SARS-CoV-2 is a preferred target for broad spectrum anti-coronavirus drug discovery. We studied the anti-SARS-CoV-2 activity of S. baicalensis and its ingredients. We found that the ethanol extract of S. baicalensis and its major component, baicalein, inhibit SARS-CoV-2 3CL pro activity in vitro with IC 50 ’s of 8.52 µg/ml and 0.39 µM, respectively. Both of them inhibit the replication of SARS-CoV-2 in Vero cells with EC 50 ’s of 0.74 µg/ml and 2.9 µM, respectively. While baicalein is mainly active at the viral post-entry stage, the ethanol extract also inhibits viral entry. We further identified four baicalein analogues from other herbs that inhibit SARS-CoV-2 3CL pro activity at µM concentration. All the active compounds and the S. baicalensis extract also inhibit the SARS-CoV 3CL pro , demonstrating their potential as broad-spectrum anti-coronavirus drugs.
Author	Tan, Wenjie Li, Siyang Ye, Fei Sun, Qi Liang, Hao Li, Chunmei Lai, Luhua Huang, Baoying Liu, Hongbo Lu, Roujian
Author_xml	– sequence: 1 givenname: Hongbo surname: Liu fullname: Liu, Hongbo organization: BNLMS, Peking-Tsinghua Center for Life Sciences at College of Chemistry and Molecular Engineering, Peking University – sequence: 2 givenname: Fei surname: Ye fullname: Ye, Fei organization: NHC Key Laboratory of Biosafety, National Institute for Viral Disease Control and Prevention, China CDC – sequence: 3 givenname: Qi surname: Sun fullname: Sun, Qi organization: BNLMS, Peking-Tsinghua Center for Life Sciences at College of Chemistry and Molecular Engineering, Peking University – sequence: 4 givenname: Hao surname: Liang fullname: Liang, Hao organization: BNLMS, Peking-Tsinghua Center for Life Sciences at College of Chemistry and Molecular Engineering, Peking University – sequence: 5 givenname: Chunmei surname: Li fullname: Li, Chunmei organization: Center for Quantitative Biology, Academy for Advanced Interdisciplinary Studies, Peking University – sequence: 6 givenname: Siyang surname: Li fullname: Li, Siyang organization: Center for Quantitative Biology, Academy for Advanced Interdisciplinary Studies, Peking University – sequence: 7 givenname: Roujian surname: Lu fullname: Lu, Roujian organization: NHC Key Laboratory of Biosafety, National Institute for Viral Disease Control and Prevention, China CDC – sequence: 8 givenname: Baoying surname: Huang fullname: Huang, Baoying organization: NHC Key Laboratory of Biosafety, National Institute for Viral Disease Control and Prevention, China CDC – sequence: 9 givenname: Wenjie surname: Tan fullname: Tan, Wenjie organization: NHC Key Laboratory of Biosafety, National Institute for Viral Disease Control and Prevention, China CDC – sequence: 10 givenname: Luhua surname: Lai fullname: Lai, Luhua organization: Center for Quantitative Biology, Academy for Advanced Interdisciplinary Studies, Peking University
BackLink	https://www.ncbi.nlm.nih.gov/pubmed/33491508$$D View this record in MEDLINE/PubMed
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Keywords	COVID-19 3C-like protease SARS-CoV-2 baicalein Scutellaria baicalensis
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Notes	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 These authors contributed equally to this work. Supplemental data for this article can be accessed here.
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Snippet	COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CL pro ) of... COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CL ) of... COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CLpro) of...
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SubjectTerms	3C-like protease Animals Antiviral Agents - pharmacology baicalein Chlorocebus aethiops Coronavirus 3C Proteases - antagonists & inhibitors COVID-19 COVID-19 - drug therapy COVID-19 - enzymology COVID-19 - virology Drug Discovery Enzyme Inhibitors - pharmacology Flavanones - pharmacology Humans In Vitro Techniques Models, Molecular Plant Extracts - pharmacology Protease Inhibitors - pharmacology Research Paper SARS-CoV-2 SARS-CoV-2 - drug effects SARS-CoV-2 - enzymology Scutellaria baicalensis Vero Cells Virus Replication - drug effects
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Title	Scutellaria baicalensis extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease in vitro
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