Synthesis and the biological evaluation of arylnaphthalene lignans as anti-hepatitis B virus agents |
| |
| Authors: | Damodar Janmanchi Ya Ping Tseng Kuei-Chen Wang Ray Ling Huang Chih Hsiu Lin Sheau Farn Yeh |
| |
| Institution: | 1. Institute of Biochemistry and Molecular Biology, National Yang-Ming University, Taipei, Taiwan, ROC;2. Institute of Chemistry, Academia Sinica, Taipei, Taiwan, ROC;3. Department of Biological Science and Technology, Meiho Institute of Technology, Pingtung, Taiwan, ROC |
| |
| Abstract: | We have previously shown that helioxanthin can suppress human hepatitis B virus gene expression. A series of helioxanthin analogues were synthesized and evaluated for their anti-hepatitis B virus activity. Modifications at the lactone rings and methylenedioxy unit of helioxanthin can modulate the antiviral activity. Among them, compound 32 is the most effective anti-HBV agent. Compound 32 can suppress the secretion of viral surface antigen and e antigen in HepA2 cells with EC50 values of 0.06 and 0.14 μM, respectively. Compound 32 not only inhibited HBV DNA with wild-type and lamivudine-resistant strain but also suppressed HBV mRNA, core protein and viral promoters. In this study, a full account of the preparation, structure–activity relationships of helioxanthin analogues, and the possible mechanism of anti-HBV activity of this class of compounds are presented. This type of compounds possesses unique mode of action differing from existing therapeutic drugs. They are potentially new anti-HBV agents. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
