含没食子酸单元的马蹄金素衍生物的合成及其抗HBV活性研究

Synthesis and anti-HBV activity evaluation of Matijin-Su derivatives containing gallic acid moiety

摘要: 本文以马蹄金素（Matijin-Su，MTS）为先导化合物进行结构优化，通过加入没食子酸结构单元，设计并合成了11个新的衍生物。对所合成的目标化合物以HepG2 2.2.15细胞进行体外抗HBV活性测试，结果表明：除4a和4b外，其余目标化合物均有一定的体外抗HBV活性，其中5c、6c和6d显示较强的抗HBV 活性，其IC₅₀达到了6.12、8.44、9.86 μmol·L^-1，说明含有没食子酸结构的马蹄金素衍生物具有进一步研究的价值。

Abstract: In this study, eleven containing gallic acid moiety derivatives of Matijin-Su(MTS)were synthesized and evaluated for their anti-HBV activities in HepG2 2.2.15 cells in an effort to find novel effective anti-hepatitis B virus(HBV)agents. Compounds 5c, 6c and 6d exhibited significant anti-HBV activity with IC₅₀ values of 6.12, 8.44 and 9.86 μmol·L^-1, respectively. Incorporation of gallic acid moiety into MTS derivatives can lead to profound changes in their anti-HBV activity, and could be worth of further research.