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
收稿日期: 2013-12-02
修回日期: 2014-01-03
网络出版日期: 2014-01-03
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
Received date: 2013-12-02
Revised date: 2014-01-03
Online 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).
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.
梁光平 , 曹佩雪 , 杨秀虾 , 黄正明 , 刘青川 , 梁光义 , 徐必学 . 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[J]. 有机化学, 2014 , 34(5) : 973 -979 . DOI: 10.6023/cjoc201312003
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.
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