田基黄体外抗乙型肝炎病毒活性成分的研究

天然产物研究与开发 ›› 2014, Vol. 26 ›› Issue (9): 1350-1356.

田基黄体外抗乙型肝炎病毒活性成分的研究

郑超1，刘敏2*，李健2

1 汕头大学理学院生物系，汕头 515063；2 中国人民解放军防化学院，北京 102205

出版日期:2014-09-30 发布日期:2014-11-02

Study on Anti-HBV Active Ingredient of Hypericum japonicum

ZHENG Chao1, LIU Min2*, LI Jian2

1 Department of Biology, Shantou University, Shantou 515063, China; 2 Institute of Chemical Defense, Beijing 102205, China

Online:2014-09-30 Published:2014-11-02

摘要/Abstract

摘要： 为了研究田基黄抗HBV活性成分，采用硅胶、Sephadex LH-20及薄层色谱等方法从田基黄60%乙醇提取物中筛选、分离纯化抗乙型肝炎病毒的活性成分，通过波谱解析和理化鉴别进行结构鉴定。以HepG 22.2.15细胞株为筛选工具，用MTT法检测药物的细胞毒性；以酶联免疫法（ELISA）检测细胞培养上清液的乙型肝炎病毒表面抗原（HBsAg）和乙型肝炎病毒e抗原（HBeAg）的滴度。从乙酸乙酯的活性部位分离得到槲皮素-7-O-鼠李糖苷（1）、（2R, 3R）双氢槲皮素-7-O-α-L-鼠李糖苷（2）、槲皮苷（3）和1,3,6,7-四羟基咕吨酮（4）4种化合物，其中化合物4 是体外抗乙型肝炎病毒活性最高的化合物，其对HepG22.2.15细胞HBeAg分泌的抑制率最高，为67.66%，IC₅₀值为40.25 μg/mL，治疗指数TI>2。

关键词: 田基黄, 乙型肝炎病毒, e抗原, 治疗指数

Abstract: In this study,silicagel, Sephagex LH-20 and thin layer chromatography were used to screen and isolate active anti-hepatitis B virus compounds from Hypericum japonicum Thunb.ex Murray extracted with 60% ethanol. Four compounds were isolated from the ethyl acetate extract of H.japonicum and their structures were characterized by spectral, chemical and structural analyses. In addition, using HepG22.2.15 cell line, the cytotoxicity and inhibitory effect on secretion of HBeAg and HBsAg of the 4 isolated compounds were examined by MTT and enzyme-linked immunosorbent assays. The 4 isolated compounds were determined to be vincetoxicoside (1), (2R,3R) double hydrogen quercetin-7-O-α-L-rhamnoside (2), quercitrin (3) and 1,3,6,7-tetrahydorxxynahtnoni (4). Among these 4 compounds, compound 4 exhibited highest activity in inhibiting secretion of HBeAg in HepG 22.2.15 cells, with inhibition rate of 67.66%,IC₅₀of 40.25 μg/mL and therapeutic index TI > 2.

Key words: Hypericum japonicum, HBV, HBeAg, TI

中图分类号:

R93

郑超1，刘敏2*，李健2. 田基黄体外抗乙型肝炎病毒活性成分的研究[J]. 天然产物研究与开发, 2014, 26(9): 1350-1356.

ZHENG Chao1, LIU Min2*, LI Jian2. Study on Anti-HBV Active Ingredient of Hypericum japonicum[J]. NATURAL PRODUCT RESEARCH AND DEVELOPMENT, 2014, 26(9): 1350-1356.

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