Panaxadiol and Panaxatriol Derivatives as Anti-Hepatitis B Virus Inhibitors  

作　　者：Hao Chen Li-Jun Wang Yun-Bao Ma Xiao-Yan Huang Chang-An Geng Xue-Mei Zhang Ji-Jun Chen 

机构地区：[1]State Key Laboratory of Phytochemistry and Plant Resources in West China,Kunming Institute of Botany,Chinese Academy of Sciences,Kunming 650201,People’s Republic of China [2]University of Chinese Academy of Sciences,Beijing 100049,People’s Republic of China

出　　处：《Natural Products and Bioprospecting》2014年第3期163-174,共12页应用天然产物（英文）

基　　金：the National Natural Science Foundation of China for Distinguished Young Scholars(No.81025023);the National Natural Science Foundation of China(81202436);the West Light Foundation of the Chinese Academy of Sciences,and the Youth Innovation Promotion Association,CAS.

摘　　要：28 Derivatives of panaxadiol(PD)and panaxatriol were synthesized and evaluated for their anti-HBV activity on HepG 2.2.15 cells,of which 17 derivatives inhibited HBV DNA replication.Compounds 4,9,10,14,and 15 showed moderate activity against HBV DNA replication with IC50 values ranged from 7.27 to 28.21 lM compared with PD.In particular,3-O-20-thenoyl panaxadiol(4)inhibited not only HBV DNA replication(IC50=16.5 lM,SI[115.7)but also HBsAg(IC50=30.8 lM,SI[62.0)and HBeAg(IC50=18.2 lM,SI[105.14)secretions.Their structure–activity relationships were discussed for guiding future research toward the discovery of new anti-HBV agents.

关 键 词：Chemical modification Panaxadiol and panaxatriol derivatives Anti-HBV activity Structure-activity relationships 

分 类 号：R51[医药卫生—内科学]