Hussein G, Miyashiro H, Nakamura N, Hattori M, Kakiuchi N, Shimotohno K
Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, 2630 Sugitani, Toyama 930-0194, Japan.
Phytother Res. 2000 Nov;14(7):510-6. doi: 10.1002/1099-1573(200011)14:7<510::aid-ptr646>3.0.co;2-b.
One hundred fifty-two methanol and water extracts of different parts of 71 plants commonly used in Sudanese traditional medicine were screened for their inhibitory effects on hepatitis C virus (HCV) protease (PR) using in vitro assay methods. Thirty-four extracts showed significant inhibitory activity (>/=60% inhibition at 100 microg/mL). Of these, eight extracts, methanol extracts of Acacia nilotica, Boswellia carterii, Embelia schimperi, Quercus infectoria, Trachyspermum ammi and water extracts of Piper cubeba, Q. infectoria and Syzygium aromaticum, were the most active (>/=90% inhibition at 100 microg/mL). From the E. schimperi extract, two benzoquinones, embelin (I) and 5-O-methylembelin (II), were isolated and found as potent HCV-PR inhibitors with IC(50) values of 21 and 46 microM, respectively. Inhibitory activities of derivatives of I against HCV-PR as well as their effects on other serine proteases were also investigated.
采用体外试验方法，对苏丹传统医学常用的71种植物不同部位的152种甲醇提取物和水提取物进行了筛选，以检测它们对丙型肝炎病毒（HCV）蛋白酶（PR）的抑制作用。34种提取物表现出显著的抑制活性（在100微克/毫升时抑制率≥60%）。其中，8种提取物，即阿拉伯胶树、卡氏乳香树、施氏酸藤子、没食子树、阿育吠陀、荜澄茄、没食子树和丁香的甲醇提取物，活性最强（在100微克/毫升时抑制率≥90%）。从施氏酸藤子提取物中分离出两种苯醌，即紫铆因（I）和5-O-甲基紫铆因（II），发现它们是有效的HCV-PR抑制剂，IC50值分别为21和46微摩尔。还研究了I的衍生物对HCV-PR的抑制活性及其对其他丝氨酸蛋白酶的影响。
