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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.
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?:doi
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?:doi
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10.1080/14756366.2021.1873977
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Journal_of_enzyme_inhibition_and_medicinal_chemistry
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document_parses/pdf_json/0e9827512377db04963de987ee531ce334a619d3.json
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document_parses/pmc_json/PMC7850424.xml.json
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?:title
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Scutellaria baicalensis extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease in vitro
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