新型乳糖苯氮芥衍生物抑制肝癌细胞活性的研究  

The lethal effect of the benzene nitrogen mustard lactose derivate on 7721 hepatocellular cells

作　　者：刘铁梅[1] 李密阳[1] 李殿秋[1] 张丽萍[2] 吴燕华[3] 谢风[1] 

机构地区：[1]吉林大学中日联谊医院,吉林长春130033 [2]东北师范大学生命科学学院,吉林长春130024 [3]吉林大学公共卫生学院,吉林长春130021

出　　处：《东北师大学报（自然科学版）》2008年第3期122-125,共4页Journal of Northeast Normal University(Natural Science Edition)

基　　金：国家重点基础研究发展计划(973计划)项目(2005CB523005);吉林省科技发展计划项目(20070417)

摘　　要：利用乙酰基保护的乳糖三氯乙酰亚胺酯作为糖基的供体,对硝基苯酚作为糖基的受体,合成了一种新型的乳糖苯氮芥衍生物,采用MTT、流式细胞术分析法探讨了其对肝癌7721细胞的生长抑制及其诱导凋亡的作用机制.结果表明,新合成的乳糖苯氮芥衍生物对正常细胞毒性较小,对7721细胞有明显的细胞毒性,能明显抑制肝癌细胞的生长;同时通过流式细胞术显示,诱导细胞凋亡是其抗肿瘤作用的主要机制之一.This is a new synthesis benzene nitrogen mustard, lactose derivate Lactose were converted into glycosyl donors-trichloroacetimidate and the obtained glycosyl donors were glycosylated with p-nitrophenol （glycosyl donors） to form β-1actosyl p-nitrobenzene that were protected by acetyl in a stereoselective manner. To analyze the new synthesis benzene nitrogen mustard lactose derivate inhibit the growth and induce the apoptosis of 7721 hepatumor cells. The experiments were used by MTT and FCM. The new synthesis benzene nitrogen mustard lactose derivate is much lower toxicity to normal cells and much higher toxicity to 7721 cells compared with nitrogen mustard, meanwhile it induce the apoptosis of 7721 cells by the FCM. Result to make clearly the new synthesis benzene nitrogen mustard lactose derivate can inhibit the growth of 7721 hepatumor cells and induce the apoptosis which is the one of the main mechanisms of antitumour.

关 键 词：靶向性治疗 氮芥 乳糖苯氮芥衍生物 肝癌7721细胞 

分 类 号：R979.11[医药卫生—药品]