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Panaxadiol and Panaxatriol Derivatives as Anti-Hepatitis B Virus Inhibitors |
| Hao Chen1,2, 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 |
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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.
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| Keywords
Chemical modification
Panaxadiol and panaxatriol derivatives
Anti-HBV activity
Structure-activity relationships
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| Fund: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. |
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Issue Date: 11 February 2018
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