从明日叶中分离出的查耳酮可抑制严重急性呼吸综合征冠状病毒（SARS-CoV）的半胱氨酸蛋白酶。
Chalcones isolated from Angelica keiskei inhibit cysteine proteases of SARS-CoV.
作者信息
Park Ji-Young, Ko Jin-A, Kim Dae Wook, Kim Young Min, Kwon Hyung-Jun, Jeong Hyung Jae, Kim Cha Young, Park Ki Hun, Lee Woo Song, Ryu Young Bae
机构信息
a Eco-friendly Bio Material Research Center, Korea Research Institute of Bioscience and Biotechnology , Jeongeup , Republic of Korea .
b Division of Applied Life Science (BK21 program, IALS) , Graduate School of Gyeongsang National University , Jinju , Republic of Korea , and.
出版信息
J Enzyme Inhib Med Chem. 2016;31(1):23-30. doi: 10.3109/14756366.2014.1003215. Epub 2015 Feb 16.
Two viral proteases of severe acute respiratory syndrome coronavirus (SARS-CoV), a chymotrypsin-like protease (3CL(pro)) and a papain-like protease (PL(pro)) are attractive targets for the development of anti-SARS drugs. In this study, nine alkylated chalcones (1-9) and four coumarins (10-13) were isolated from Angelica keiskei, and the inhibitory activities of these constituents against SARS-CoV proteases (3CL(pro) and PL(pro)) were determined (cell-free/based). Of the isolated alkylated chalcones, chalcone 6, containing the perhydroxyl group, exhibited the most potent 3CL(pro) and PL(pro) inhibitory activity with IC50 values of 11.4 and 1.2 µM. Our detailed protein-inhibitor mechanistic analysis of these species indicated that the chalcones exhibited competitive inhibition characteristics to the SARS-CoV 3CL(pro), whereas noncompetitive inhibition was observed with the SARS-CoV PL(pro).
严重急性呼吸综合征冠状病毒（SARS-CoV）的两种病毒蛋白酶，一种类胰凝乳蛋白酶（3CL蛋白酶）和一种木瓜蛋白酶样蛋白酶（PL蛋白酶）是开发抗SARS药物的有吸引力的靶点。在本研究中，从明日叶中分离出9种烷基化查耳酮（1-9）和4种香豆素（10-13），并测定了这些成分对SARS-CoV蛋白酶（3CL蛋白酶和PL蛋白酶）的抑制活性（无细胞/基于细胞）。在分离出的烷基化查耳酮中，含有全羟基的查耳酮6对3CL蛋白酶和PL蛋白酶表现出最有效的抑制活性，IC50值分别为11.4和1.2 μM。我们对这些物质进行的详细的蛋白质-抑制剂机制分析表明，查耳酮对SARS-CoV 3CL蛋白酶表现出竞争性抑制特征，而对SARS-CoV PL蛋白酶则观察到非竞争性抑制。
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