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有机化学 ›› 2014, Vol. 34 ›› Issue (5): 973-979.DOI: 10.6023/cjoc201312003 上一篇    下一篇

研究论文

NO供体型马蹄金素衍生物的合成及其初步的抗乙肝病毒活性

梁光平a,b, 曹佩雪a, 杨秀虾a,b, 黄正明c, 刘青川c, 梁光义a, 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 贵阳中医学院 贵阳 550002;
    c 中国人民解放军第三○二医院 北京 100039
  • 收稿日期:2013-12-02 修回日期:2014-01-03 发布日期:2014-01-03
  • 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）、贵阳中医学院研究生教育创新计划（No. ZYYCX12018）资助项目.

Synthesis and Anti-hepatitis B Virus Activities of Nitric Oxide-Releasing Derivatives of Matijin-Su

Liang Guangpinga,b, Cao Peixuea, Yang Xiuxiaa,b, Huang Zhengmingc, Liu Qingchuanc, Liang Guangyia, Xu Bixuea   

  1. a Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002;
    b Guiyang College of Traditional Chinese Medicine, Guiyang 550002;
    c 302 Hospital of PLA, Beijing 100039
  • Received:2013-12-02 Revised:2014-01-03 Published:2014-01-03
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 81360472), and the Graduate Education Innovation Project of Guiyang College of Traditional Chinese Medicine (No. ZYYCX12018).

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被引次数

9 | 5

以马蹄金素[N-（N-苯甲酰基-L-苯丙氨酰基）-O-乙酰基-L-苯丙氨醇，MTS]为先导化合物，设计并合成了11个NO供体型马蹄金素衍生物，所有目标产物均未见文献报道，其结构经 NMR，ESI-MS确认. 以HepG2 2.2.15细胞为乙肝病毒载体，对合成的马蹄金素衍生物进行了抗乙肝病毒活性测试. 结果表明，在测试浓度范围内，化合物6d，6e，6g具有抗HBV活性，其半数抑制浓度分别为6.88，37.51，11.07 μmol/L. 其中，化合物6d和6g的半数抑制浓度优于MTS （11.16 μmol/L），且具有较高的抑制率，具有进一步研究开发的价值.

关键词: 马蹄金素衍生物, 一氧化氮供体, 合成, 抗乙肝病毒活性

By using N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol, named Matijin-Su, as a lead compound, a series of nitric oxide-releasing derivatives of Matijin-Su were synthesized and evaluated for their anti-hepatitis B virus activities in HepG2 2.2.15 cells. Compounds 6d, 6e and 6g exhibited significant anti-HBV activities. The 50% inhibitory concentrations of these compounds towards HepG2 2.2.15 cells were 6.88, 37.51 and 11.07 μmol/L. Compounds 6d and 6g were less than Matijin-Su (IC50: 11.16 μmol/L). Compound 6d has potent in vitro anti-HBV activity, and could be worth of further research.

Key words: derivatives of Matijin-Su, nitric oxide donor, synthesis, anti-hepatitis B virus activity