Phenolic phytochemical displaying SARS-CoV papain-like protease inhibition from the seeds of Psoralea corylifolia
Phenolic phytochemical displaying SARS-CoV papain-like protease inhibition from the seeds of Psoralea corylifolia
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DOI：
10.3109/14756366.2012.753591
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发表时间：
2014-02-01
影响因子：
5.6
通讯作者：
Park, Ki Hun
中科院分区：
文献类型：
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作者：
Kim, Dae Wook;Seo, Kyung Hye;Park, Ki Hun
严重急性呼吸综合征冠状病毒（SARS- cov）木瓜蛋白酶（PLpro）是在SARS病毒复制过程中起重要作用的关键酶。补骨脂种子乙醇提取物对SARS-CoV PLpro具有较高的抑制活性，IC50值为15 μ g/ml。由于其药效，随后对乙醇提取物进行生物活性引导分离得到6种芳香化合物（1-6），鉴定为巴伐利亚素(1)、新巴伐利亚异黄酮(2)、异巴伐利亚酮(3)、4′- o -甲基巴伐利亚酮(4)、补骨脂素(5)和堇青花醇A(6)。所有分离的黄酮类化合物（1-6）均以剂量依赖性的方式抑制PLpro， IC50在4.2 ~ 38.4 μ M. Lineweaver-Burk和Dixon图之间，它们的二次重图表明抑制剂（1-6）是PLpro的混合抑制剂。K-I和K-IS值分析证明，两个最有希望的化合物（3和5）具有可逆的混合I型机制。
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 mu g/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 mu M. Lineweaver-Burk and Dixon plots and their secondary replots indicated that inhibitors (1-6) were mixed inhibitors of PLpro. The analysis of K-I and K-IS values proved that the two most promising compounds (3 and 5) had reversible mixed type I mechanisms.