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目的:牛蒡苷元属于木脂素类化合物,水溶性差,故以牛蒡苷元为先导化合物进行结构修饰,改善其水溶性,进而提高生物度,方便制剂、扩大牛蒡苷元的临床应用范围。方法:采用丙胺与牛蒡苷元在室温下发生氨解反应,通过重结晶方法制备氨解衍生物。采用5种人癌细胞株对氨解衍生物进行抗肿瘤活性研究。结果:合成得到牛蒡苷元氨解衍生物,操作简单,后处理容易,收率较高,并且衍生物的溶解性高于牛蒡苷元。对牛蒡苷元与氨解衍生物进行抗肿瘤活性研究表明氨解衍生物的活性低于牛蒡苷元。结论:牛蒡苷元氨解衍生物的最佳合成条件为:牛蒡苷元与丙胺的质量体积比为1∶0.05,室温反应24 h,收率为64%。经活性研究表明牛蒡苷元的内酯环是抗肿瘤活性关键基团。
OBJECTIVE: Arctigenin belongs to lignan class compound and has poor water solubility. Therefore, arctigenin is used as the lead compound for structural modification to improve its water solubility, thereby increasing the biological degree, facilitating the preparation and expanding the clinical application range of arctigenin. Methods: The aminolysis reaction was carried out at room temperature with propylamine and arctigenin, and the aminolysis derivative was prepared by recrystallization. Five human cancer cell lines were used to study the antitumor activity of aminolysis derivatives. Results: Arctigenin aminolysis derivatives were obtained. It has simple operation, easy post-treatment, high yield and higher solubility of the derivatives than arctigenin. Studies on the anti-tumor activity of arctigenin and aminol derivatives showed that the activity of aminolysis derivatives was lower than arctigenin. CONCLUSION: The optimum conditions for the derivatization of arctigenin derivatives are as follows: the mass volume ratio of arctigenin to propylamine is 1:0.05, and the reaction time is 24 h at room temperature with a yield of 64%. The activity studies show that arctigenin lactone ring is the key group of anti-tumor activity.