Yang Jun-Li, Ha Thi-Kim-Quy, Dhodary Basanta, Pyo Euisun, Nguyen Ngoc Hieu, Cho Hyomoon, Kim Eunhee, Oh Won Keun
Korea Bioactive Natural Material Bank, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University , Sillim-dong, Gwanak-gu, Seoul 151-742, Republic of Korea.
J Med Chem. 2015 Feb 12;58(3):1268-80. doi: 10.1021/jm501567f. Epub 2015 Feb 3.
Porcine epidemic diarrhea virus (PEDV) infections have resulted in a severe economic loss in the swine industry in many countries due to no effective treatment approach. Fifteen oleanane triterpenes (1-15), including nine new ones (1-4 and 10-14), were isolated from the flowers of Camellia japonica, and their molecular structures were determined by extensive spectroscopic methods. These compounds were evaluated for their antiviral activity against PEDV replication, and the structure-activity relationships (SARs) were discussed. Compounds 6, 9, 11, and 13 showed most potent inhibitory effects on PEDV replication. They were found to inhibit PEDV genes encoding GP6 nucleocapsid, GP2 spike, and GP5 membrane protein synthesis based on RT-PCR data. Western blot analysis also demonstrated their inhibitory effects on PEDV GP6 nucleocapsid and GP2 spike protein synthesis during viral replication. The present study suggested the potential of compounds 6, 9, 11, and 13 as promising scaffolds for treating PEDV infection via inhibiting viral replication.
由于没有有效的治疗方法，猪流行性腹泻病毒（PEDV）感染已在许多国家的养猪业中造成了严重的经济损失。从山茶花的花朵中分离出了15种齐墩果烷三萜（1-15），其中包括9种新的（1-4和10-14），并通过广泛的光谱方法确定了它们的分子结构。对这些化合物针对PEDV复制的抗病毒活性进行了评估，并讨论了构效关系（SARs）。化合物6、9、11和13对PEDV复制表现出最强的抑制作用。根据逆转录-聚合酶链反应（RT-PCR）数据，发现它们可抑制PEDV编码GP6核衣壳、GP2刺突和GP5膜蛋白的基因合成。蛋白质免疫印迹分析也证明了它们在病毒复制过程中对PEDV GP6核衣壳和GP2刺突蛋白合成的抑制作用。本研究表明，化合物6、9、11和13具有通过抑制病毒复制来治疗PEDV感染的潜在前景。
