Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (10): 2176-2183.DOI: 10.6023/cjoc201505011 Previous Articles     Next Articles

Notes

具有肝靶向潜力的马蹄金素衍生物合成及抗乙肝活性研究

袁洁a,b, 刘青川c, 徐广灿a,d, 胡占兴a, 梁光平a, 黄正明c, 刘昌孝e, 梁光义a,d, 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 贵州大学药学院 贵阳 550002;
    c 中国人民解放军第三○二医院 北京 100039;
    d 贵阳中医学院 贵阳 550002;
    e 天津药物研究院 天津 300193
  • 收稿日期:2015-05-07 修回日期:2015-06-08 出版日期:2015-10-25 发布日期:2015-06-19
  • 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 Matijin-Su Derivatives with Potential for Hepatic Targeting

Yuan Jiea,b, Liu Qingchuanc, Xu Guangcana,d, Hu Zhanxinga, Liang Guangpinga, Huang Zhengmingc, Liu Changxiaoe, Liang Guangyia,d, Xu Bixuea   

  1. a Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002;
    b College of Pharmacy, Guizhou University, Guiyang 550002;
    c 302 Hospital of PLA, Beijing 100039;
    d Guiyang College of Traditional Chinese Medicine, Guiyang 550002;
    e Tianjin Institute of Pharmaceutical Research, Tianjin 300193
  • Received:2015-05-07 Revised:2015-06-08 Online:2015-10-25 Published:2015-06-19
  • 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) activity of Matijin-Su [N-(N-benzoyl-l-phenylalanyl)-O-acetyl-L-phenylalanol, MTS] derivatives, five galactosyl derivatives of MTS with potential for hepatic targeting were synthesized and their structures were confirmed by 1H NMR, 13C NMR, 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-effect relationship.

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