摘要
目的:设计并合成11个积雪草酸C2,3,23,28衍生物,并对其体外抗肿瘤活性进行测试。方法:以积雪草酸为先导化合物,对其C2,3,23及28位进行结构改造,合成11个积雪草酸衍生物。采用MTT法,选用高表达人癌细胞SGC-7901和A549,对目标化合物进行初步的体外抗肿瘤活性测试。结果:目标化合物对2种细胞株的抑制率均高于积雪草酸,其中化合物14和15的抗肿瘤活性与阳性对照紫杉醇相当。结论:经过结构改造后得到的积雪草酸衍生物具有一定的抗肿瘤活性,值得进一步研究。
Objective: To design and synthesize 11 asiatic acid derivatives,and to study their anti-tumor activities in vitro. Methods: Asiatic acid was used as starting material to synthesize eleven asiatic acid derivatives by structural modification at C-2,3,23 and C-28 carboxyl group. Their cytotoxicity in vitro against various cancer cell lines SGC-7901 and A549 was evaluated by MTT assay. Results: The target compounds were characterized by MS and1 H NMR. The results of experiments indicated that the inhibitory activities of asiatic acid derivatives were higher than those of asiatic acid in vitro. Compound 14 and 15 have similar anti-tumor activity to the positive control drug paclitaxel. Conclusion: The novel asiatic acid derivatives which were synthesized by structure modification have good anti-tumor activities,and are worthy further study.
作者
孟艳秋
崔华博
潘洪双
于婷婷
MENG Yan-qiu;CUI Hua-bo;PAN Hong-shuang;YU Ting-ting(Department of Pharmaceutical Engineering,Shenyang University of Chemical Technology,Shenyang 110142,China)
出处
《中国新药杂志》
CAS
CSCD
北大核心
2018年第19期2308-2314,共7页
Chinese Journal of New Drugs
基金
辽宁省自然科学基金资助项目(201605288)
沈阳市科学技术计划资助项目(F-16-230-6-00)
国家自然科学基金资助项目(21372156)
关键词
积雪草酸衍生物
结构改造
抗肿瘤活性
asiatic acid derivatives
structure modification
anti-tumor activity