Division of Applied Life Science (BK21 Program), IALS and.
J Enzyme Inhib Med Chem. 2014 Feb;29(1):59-63. doi: 10.3109/14756366.2012.753591. Epub 2013 Jan 16.
Severe acute respiratory syndrome coronavirus (SARS-CoV) papain-like protease (PLpro) is a key enzyme that plays an important role in SARS virus replication. The ethanol extract of the seeds of Psoralea corylifolia showed high activity against the SARS-CoV PLpro with an IC50 of value of 15 µg/ml. Due to its potency, subsequent bioactivity-guided fractionation of the ethanol extract led to six aromatic compounds (1-6), which were identified as bavachinin (1), neobavaisoflavone (2), isobavachalcone (3), 4'-O-methylbavachalcone (4), psoralidin (5) and corylifol A (6). All isolated flavonoids (1-6) inhibited PLpro in a dose-dependent manner with IC50 ranging between 4.2 and 38.4 µM. Lineweaver-Burk and Dixon plots and their secondary replots indicated that inhibitors (1-6) were mixed inhibitors of PLpro. The analysis of KI and KIS values proved that the two most promising compounds (3 and 5) had reversible mixed type I mechanisms.
严重急性呼吸综合征冠状病毒（SARS-CoV）木瓜蛋白酶样蛋白酶（PLpro）是一种关键酶，在 SARS 病毒复制中发挥重要作用。补骨脂种子的乙醇提取物对 SARS-CoV PLpro 表现出很高的活性，IC50 值为 15 µg/ml。由于其效力，随后对乙醇提取物进行基于生物活性的分段分离得到了六个芳香族化合物（1-6），它们被鉴定为补骨脂素（1）、新补骨脂异黄酮（2）、异补骨脂查尔酮（3）、4'-O-甲基补骨脂查尔酮（4）、补骨脂定（5）和补骨脂 A（6）。所有分离得到的类黄酮（1-6）均以剂量依赖的方式抑制 PLpro，IC50 值在 4.2 和 38.4 µM 之间。Lineweaver-Burk 和 Dixon 图及其二次重绘表明，抑制剂（1-6）是 PLpro 的混合抑制剂。KI 和 KIS 值的分析证明，两种最有前途的化合物（3 和 5）具有可逆的混合 I 型机制。
