Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (7): 1617-1625.DOI: 10.6023/cjoc201512051 Previous Articles     Next Articles

Articles

吡喃半乳糖糖基化马蹄金素衍生物的合成及抗乙肝病毒活性研究

徐广灿a,c,, 刘青川b, 袁洁a,d, 胡占兴a, 马芳芳a,c, 梁光义a,c, 徐必学a   

  1. a. 贵州省中国科学院天然产物化学重点实验室 贵阳 550002;
    b. 中国人民解放军第三○二医院 北京 100039;
    c. 贵阳中医学院 贵阳 550002;
    d. 贵州大学药学院 贵阳 550002
  • 收稿日期:2015-12-31 修回日期:2016-03-10 出版日期:2016-07-25 发布日期:2016-03-25
  • 通讯作者: 梁光义, 徐必学 E-mail:guangyi_liang@126.com;bixue_xu@126.com
  • 基金资助:

    国家自然科学基金(No.81360472)和西部之光人才(2014年)资助项目.

Synthesis and Anti-Hepatitis B Virus Activities of Galactopyranosyl Derivatives of Matijin-Su

Xu Guangcana,c,, Liu Qingchuanb, Yuan Jiea,d, Hu Zhanxinga, Ma Fangfanga,c, Liang Guangyia,c, Xu Bixuea   

  1. a. Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002;
    b. 302 Hospital of PLA, Beijing 100039;
    c. Guiyang College of Traditional Chinese Medicine, Guiyang 550002;
    d. College of Pharmacy, Guizhou University, Guiyang 550002)
  • Received:2015-12-31 Revised:2016-03-10 Online:2016-07-25 Published:2016-03-25
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 81360472) and the Western Light Talent Culture Project (2014).

To improve the concentration in liver lesion tissue and increase the anti-hepatitis B virus (HBV) activities of Matijin-Su (MTS) derivatives, five hepatic targeting galactopyranosyl derivatives of MTS were synthesized by indirect connecting the liver targeting galactose ligands to MTS using ethanolamin as a linker and their structures were confirmed by 1H NMR, 13CNMR, 1H-1H COSY, HMQC and ESI-MS. The anti-HBV activities of those compounds were evaluated in HepG2 2.2.15 cells. The screening results showed that all target compounds had inhibitory effect on HBV DNA replication in HepG2 2.2.15 cells in a dose-response manner.

Key words: hepatic targeting, derivatives of Matijin-Su, glacatose, anti-hepatitis B virus activity