摘要
设计合成汉防己甲素衍生物,并研究其抗肿瘤活性。以汉防己甲素为原料经溴代反应制得关键中间体5-溴汉防己甲素,然后经溴锂交换后形成锂盐与芳香醛加成得到3个新型汉防己甲素衍生物,其结构经^(1)HNMR,^(13)CNMR和ESI-MS验证。采用MTT法初步评价4个样品对人肝癌细胞(HepG2)和人胃癌细胞(BGC-823)的抗肿瘤活性。初筛结果表明:对HepG2细胞抑制最强的为化合物2,对BGC-823细胞抑制最强的为化合物1。汉防己甲素通过结构修饰,其衍生物1、2的抗肿瘤活性大于汉防己甲素。
This study designs and synthesizes tetrandrine derivatives and investigates their anti-tumor activity.The key intermediate 5-bromotetrandrine was synthesized from tetrandrine by bromination,and then exchanged with lithium bromide to form lithium salt.Eight new tetrandrine derivatives were synthesized by the addition of aromatic aldehydes.Their structures were confirmed by ^(1)HNMR,^(13)CNMR,and ESI-MS.MTT assay was used to evaluate the antitumor activities of eight samples against HepG2 and human BGC-823.The preliminary screening results showed that compound 2 had the strongest inhibition on HepG2 cells and compound 1 had the strongest inhibition on BGC-823 cells.Through structural modification,the antitumor activity of derivatives 1 and 2 of tetrandrine is greater than that of tetrandrine.
作者
黄涛
黄小强
李应岩
贾安
刘顺和
茹国华
Huang Tao;Huang Xiaoqiang;Li Yingyan;Jia An;Liu Shunhe;Ru Guohua(Medical School,Huanghe Science&Technology College,Zhengzhou City,Henan Province 450063;College of Pharmacy,Henan University,Kaifeng City,Henan Province 475004)
出处
《黄河科技学院学报》
2024年第2期17-21,共5页
Journal of Huanghe S&T College
基金
河南科技厅科技攻关项目(162103210003)
河南省研究生教育改革与质量提升工程项目(YJS2023JD68)。
