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目的:合成九节龙皂苷衍生物并研究其抗肿瘤活性。方法:以九节龙皂苷Ⅰ为先导物,对其30位醛基进行结构修饰,合成一系列衍生物,通过体外细胞培养方法检测其对9种常见肿瘤细胞系的抗肿瘤活性。结果:获得了3个新的皂苷修饰物,其中化合物1和化合物3对常见的9种瘤株的IC_(50)与原皂苷相比均降低(P<0.05),化合物1和化合物3对肿瘤细胞的抑制率较原皂苷增强。结论:通过对九节龙皂苷进行结构修饰,能增加其抗肿瘤活性。
OBJECTIVE: To synthesize nine ginsenoside derivatives and study their anti-tumor activity. Methods: A series of derivatives were synthesized through the structural modification of the 30 aldehyde groups with the preconcentration of Jiulongsong saponin Ⅰ. The antitumor activities of the nine common tumor cell lines were tested by in vitro cell culture. Results: Three novel saponin modified compounds were obtained. Among them, compound 1 and compound 3 showed a lower (P <0.05) IC9 (50) compared with the original saponin in 9 common tumor strains. The effect of compound 1 and compound 3 on tumor Cell inhibition rate than the original saponin enhanced. Conclusion: The structural modification of Gynostemma pentaphylla can increase its anti-tumor activity.