Panaxadiol and Panaxatriol Derivatives as Anti-Hepatitis B Virus Inhibitors

doi:10.1007/s13659-014-0018-2

应用天然产物 ›› 2014, Vol. 4 ›› Issue (3): 163-174.DOI: 10.1007/s13659-014-0018-2

• Original article • 上一篇下一篇

Panaxadiol and Panaxatriol Derivatives as Anti-Hepatitis B Virus Inhibitors

Hao Chen^1,2, Li-Jun Wang¹, Yun-Bao Ma¹, Xiao-Yan Huang¹, Chang-An Geng¹, Xue-Mei Zhang¹, Ji-Jun Chen¹

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

收稿日期:2014-04-02 修回日期:2014-04-17 出版日期:2014-06-24 发布日期:2018-02-11
通讯作者: Ji-Jun Chen,e-mail:chenjj@mail.kib.ac.cn
基金资助:
The work was supported by 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.

Panaxadiol and Panaxatriol Derivatives as Anti-Hepatitis B Virus Inhibitors

Hao Chen^1,2, Li-Jun Wang¹, Yun-Bao Ma¹, Xiao-Yan Huang¹, Chang-An Geng¹, Xue-Mei Zhang¹, Ji-Jun Chen¹

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

Received:2014-04-02 Revised:2014-04-17 Online:2014-06-24 Published:2018-02-11
Supported by:
The work was supported by 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/Abstract

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 μM compared with PD. In particular, 3-O-20-thenoyl panaxadiol(4) inhibited not only HBV DNA replication(IC₅₀=16.5 μM, SI>115.7) but also HBsAg(IC₅₀=30.8 μM, SI>62.0) and HBeAg(IC₅₀=18.2 μM, 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

Abstract: 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 μM compared with PD. In particular, 3-O-20-thenoyl panaxadiol(4) inhibited not only HBV DNA replication(IC₅₀=16.5 μM, SI>115.7) but also HBsAg(IC₅₀=30.8 μM, SI>62.0) and HBeAg(IC₅₀=18.2 μM, SI>105.14) secretions. Their structure-activity relationships were discussed for guiding future research toward the discovery of new anti-HBV agents.

Key words: Chemical modification, Panaxadiol and panaxatriol derivatives, Anti-HBV activity, Structure-activity relationships

Hao Chen, Li-Jun Wang, Yun-Bao Ma, Xiao-Yan Huang, Chang-An Geng, Xue-Mei Zhang, Ji-Jun Chen. Panaxadiol and Panaxatriol Derivatives as Anti-Hepatitis B Virus Inhibitors[J]. 应用天然产物, 2014, 4(3): 163-174.

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Panaxadiol and Panaxatriol Derivatives as Anti-Hepatitis B Virus Inhibitors

Panaxadiol and Panaxatriol Derivatives as Anti-Hepatitis B Virus Inhibitors

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