Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka Suita, Osaka 565-0871, Japan.
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1598-600. doi: 10.1016/j.bmcl.2010.01.084. Epub 2010 Jan 21.
By use of the model virus, expressing the HCV envelope proteins E1 and E2, bioassay guided separation of the MeOH extract from Rosa rugosa Thunb. disclosed tellimagrandin I (1) together with eugeniin (2) and casuarictin (3) as the potent HCV invasion inhibitors. Furthermore, structure-activity relationship analysis of some relative tannins including the synthesized analogs elucidated the partial structures crucial for potent activity of 1.
利用表达 HCV 包膜蛋白 E1 和 E2 的模式病毒,对皱皮木瓜 MeOH 提取物进行生物活性导向分离,发现鞣花单宁 I(1)、杨梅素(2)和老鹳草素(3)具有较强的 HCV 入侵抑制活性。此外,对包括合成类似物在内的一些相关单宁进行的构效关系分析阐明了 1 发挥强活性的部分结构。