牛蒡苷元氨解衍生物的合成及其抗肿瘤活性研究

Research on Synthesis of Ammonolysis Derivative of Arctigenin and Antitum or Bioactivity

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： For the lower water sohIbility, arctigenin was used as a lead compound for structure modification to improve the water solubility and the bioavailability and convenient preparation and expand the range of clinical application. Methods： Arctigenin was treated with propylamine aqueous solutions at the room temperature and the ammonolysis derivative was obtained by recrystallization. The five cancer lines were used to examine the bioactivity of arctigenin and ammonolysis derivative. Results： The ammonolysisi derivative was yield and the experiment was easy treatment and simple operation and high yield. The bioactivity result was indicated that the ammonolysis derivative had lower antitumor activity than arctigenin. Conclusion ： The optimal synthesized art was that the ration of arctigenin and propylamine was 1：0.05 and the reaction was carried out at room temperature for 24 hours and the yield was 64%. The bioactivity resuhs showed that lactone ring of arctigenin was the important agent in antitumor activity.