黄芩提取物和黄芩素抑制 SARS-CoV-2 及其 3CL 样蛋白酶的复制。
extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease .
机构信息
BNLMS, Peking-Tsinghua Center for Life Sciences at College of Chemistry and Molecular Engineering, Peking University, Beijing, China.
NHC Key Laboratory of Biosafety, National Institute for Viral Disease Control and Prevention, China CDC, Beijing, China.
出版信息
J Enzyme Inhib Med Chem. 2021 Dec;36(1):497-503. doi: 10.1080/14756366.2021.1873977.
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.
新型冠状病毒（COVID-19）已在全球范围内广泛传播，因此急需研发针对该病毒的药物（SARS-CoV-2）。SARS-CoV-2 的 3C 样蛋白酶（3CL）是广谱抗冠状病毒药物研发的首选靶点。我们研究了 和其成分的抗 SARS-CoV-2 活性。我们发现， 的乙醇提取物及其主要成分黄芩素对 SARS-CoV-2 3CL 的抑制活性的 IC₅₀分别为 8.52 µg/ml 和 0.39 µM。它们都能以 EC₅₀为 0.74 µg/ml 和 2.9 µM 抑制 SARS-CoV-2 在 Vero 细胞中的复制。黄芩素主要在病毒进入后阶段发挥作用，而乙醇提取物也能抑制病毒进入。我们进一步从其他草药中鉴定出四种黄芩素类似物，它们在 µM 浓度下抑制 SARS-CoV-2 3CL 活性。所有活性化合物和 提取物还抑制 SARS-CoV 3CL，表明它们具有广谱抗冠状病毒的潜力。
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