新型常春藤皂苷元衍生物的合成及其体外抗HBV活性

Synthesis and In vitro Anti-HBV Activities of Novel Hederagenin Derivatives

以常春藤皂苷元为原料,对其3,23-羟基和28-羧基进行乙酰化、醚化、苯甲酰化及酯化等反应合成了8个常春藤皂苷元衍生物(2~9),其中6个未见文献报道,其结构经~1H NMR,^(13)C NMR,IR和MS表征。采用MTT法测定了2~9的体外抗HBV活性。结果表明:3~9随浓度增大,对细胞活力的抑制率明显增加,特别是7和9抑制率最明显,用药浓度为1×10-6mol·L^(-1)时,抑制率均为9.46±0.47%。对2~9抑制HepG2.2.15细胞表达表面抗原(HBsAg)进行了测试。结果表明:2~9对HBs Ag的分泌表达有一定的抑制作用。

Eight derivatives（2-9） of hederagenin were synthesized by acetylation,etherification,benzoylation and esterification,et al,on 3,23-hydroxyl and 28-carboxyl of hederagenin.Among them,six derivatives were not reported.The structures were characterized by ^1H NMR,^13C NMR,IR and MS.The anti-HBV activities of the compounds were determined by MTT method.The results showed that cell viabilities of 3-9 was significantly inhibited with increasing of concentration.In particular,inhibition ratio of 7 and 9 were 9.46 ± 0.47% at concentration of 1×10^-6mol·L^-1.The inhibition abilities on HepG2.2.15 cells expressing HBs Ag were tested.The results showed that 2-9 have certain inhibitory effect on the secretory expression of HBs Ag.