常春藤皂苷元的糖化学修饰与体外抗COLO205细胞增殖活性  

Glycochemical Modification of Hederagenin and Anti-COLO205 CellProliferation Activities In Vitro

作　　者：杨诗雯 李军 洪开文 王欢 张勇民[4] 董登祥 YANG Shi-Wen;LI Jun;HONG Kai-Wen;WANG Huan;ZHANG Yong-Min;DONG Deng-Xiang(College of Pharmacy, Guizhou College of Traditional Chinese Medicine, Guiyang 550025,China;Applied Medical Department, Vocational and Technical College of Anshun, Anshun 561000, China;R&D Department, Guizhou Weimen Pharmaceutical Co., Ltd., Guiyang 550018, China;CNRS UMR 8232, Université Paris Ⅵ, Paris 75005, France)

机构地区：[1]贵州中医药大学药学院,贵州贵阳550025 [2]安顺职业技术学院应用医药系,贵州安顺561000 [3]贵州威门药业股份有限公司研发部,贵州贵阳550018 [4]巴黎第六大学法国国家科研中心,法国巴黎75005

出　　处：《合成化学》2020年第8期688-695,共8页Chinese Journal of Synthetic Chemistry

基　　金：黔合院士工作站[(2014)4013]。

摘　　要：通过连接不同糖片段的三氯乙酰亚胺酯衍生物、甲基衍生物、对甲基苯硫酚衍生物等合成了4个常春藤皂苷元衍生物(4~7,其中6和7为新化合物),其结构经1H NMR和13C NMR表征。采用MTT法检测了化合物对人结肠癌细胞COLO205的抑制活性。结果表明:4和5对COLO205细胞有部分抑制作用,与浓度正相关;6对COLO205只在高浓度(1.00×10-4mmol/L)有较好抑制作用(98.36±0.43%);7只在中等浓度(1.00×10-5mmol/L)对COLO205有微弱抑制作用(2.75±1.22%)。Four hederagenin derivatives(4~7)were synthesized by connecting different sugar fragments of linking trichloroacetimidate derivatives,methyl derivatives,p-methylthiophenol derivatives,etc.6 and 7 were new compound.The structures were characterized by 1H NMR and 13C NMR.The inhibition effect of compounds against human colon cancer cell line COLO205 was examined by cell MTT assay.The results showed that 4 and 5 had partial inhibitory effect on COLO205 cells,which was positively correlated with concentration;6 had little effect of COLO205 cells and only had a good inhibitory effect at high concentration of 1.00×10-4 mmol/L,which could reach 98.36±0.43%;7 had a weak inhibitory effect on COLO205 at a moderate concentration of 1.00×10-5mmol/L,which was 2.75±1.22%.

关 键 词：常春藤皂苷元 结构修饰 人结肠癌细胞COLO205 噻唑蓝法 合成 抑制活性 

分 类 号：O621.3[理学—有机化学] O629.2[理学—化学]