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目的对九节龙皂苷Ⅰ进行结构修饰得到新的结构类似物,并对其抗肿瘤活性进行研究。方法通过对九节龙皂苷Ⅰ的30位醛基进行氧化、还原或氨基化合物的缩合得到一系列新的化合物,并采用MTT法对合成的衍生物进行9种人癌细胞毒活性研究,通过IC50来评价其抗肿瘤活性。结果得到的新化合物a、b、d和中间体c,分别为氢化九节龙皂苷Ⅰ、加氧九节龙皂苷Ⅰ、九节龙皂苷缩4-苄基-3-氨基硫脲和九节龙皂苷缩肼基二硫代甲酸甲酯;其中化合物a和中间体c对常见的9种人癌细胞IC50相比原皂苷均降低(P<0.05),说明其对肿瘤细胞的抑制能力较原皂苷增强。结论通过对九节龙皂苷I进行结构修饰,能够使其抗肿瘤活性增强。
OBJECTIVE: To study the antitumor activity of giuxongyin Ⅰ by structural modification. Methods A series of new compounds were obtained by the oxidation, reduction or condensation of the amino groups at the 30-position of the aconitine Ⅰ, and 9 kinds of cytotoxic activity of the synthesized derivatives were studied by MTT method. The IC50 To evaluate its anti-tumor activity. The results of the new compounds a, b, d and the intermediate c, respectively, hydrogenated giuisone Ⅰ, plus giganotonin Ⅰ, giusenoside 4-benzyl-3-thiosemicarbazone and nine (P <0.05), which showed that compound a and intermediate c had lower inhibitory effect on tumor cells than the original IC50 of 9 kinds of human cancer cells Saponin enhancement. Conclusion The structural modification of gynostemma pentaphylla I can increase its anti-tumor activity.