二乙酰二脱水卫矛醇在体内外的抗瘤作用及其机制  

Antitumor effect of diacetyldianhydrogalactitol and its mechanism

作　　者：杨锦南[1] 潘启超[1] 梁永钜[1] 符立梧[1] 周瑛[2] 

机构地区：[1]中山医科大学肿瘤防治中心肿瘤研究所,广东广州510060 [2]广西中医药研究所,广西南宁530022

出　　处：《癌症》2000年第12期1112-1115,共4页Chinese Journal of Cancer

摘　　要：目的：观察二乙酰二脱水卫矛醇（ diacetyldianhydrogalactitol,DADAG）在体内外的抗肿瘤作用 ,探讨其抗肿瘤作用与诱导细胞凋亡的关系。方法：建立小鼠脑内接种艾氏腹水癌模型，观察 DADAG体内抗瘤作用； MTT法观察 DADAG对人早幼粒白血病细胞株 HL 60和人红白血病细胞株 K562的生长抑制作用， DNA电泳和流式细胞仪分析 HL 60和 K562细胞凋亡的情况。结果： DADAG 10 mg/kg ip,每天 1次，连续给药 7天，可显著延长小鼠中位生存时间；对 HL 60和 K562均有生长抑制作用，药物作用 72h的 IC50分别为 3.7 mg/L和 25.5 mg/L;作用 HL 60和 K562细胞后电泳显示有凋亡细胞特有的“梯状”条带， DNA直方图出现亚 G1峰。结论： DADAG抗肿瘤作用与诱导细胞凋亡有关。Objective: The current study was designed to observe the antitumor effect of diacetyldianhydrogalactitol(DADAG) in vivo and in vitro, and to clarify whether its antitumor activity is related to inducing apoptosis. Methods:We established a model of intracerebrally inoculated Ehrlich ascites carcinoma in mice and the antitumor effect of DADAG was observed in vivo. The growth inhibitory effect of DADAG on human myeloid HL 60 and chronic myelogenous leukemia K562 cell lines was observed by using MTT assay; Cell apoptosis was analyzed by using agarose gel electrophoresis of DNA and flow cytometer. Results:DADAG 10 mg/kg, ip, once a day for continuously 7 days, significantly increased the median lifespan（ MLS） of tumor bearing mice. After incubation for 72 h, DADAG had dramatically growth inhibitory effect on HL 60 and K562 cells in vitro with, IC50 of 3.7 mg/L and 25.5 mg/L, respectively. HL 60 and K562 cells showed typical apoptosis features of“ ladder” and the sub G1 peak in DNA histogram. Conclusions: The antitumor effect of DADAG is relative to inducing cell apoptosis.

关 键 词：二乙酰二脱水卫矛醇 体内外抗瘤作用 细胞凋亡 

分 类 号：R979.1[医药卫生—药品] R73－361[医药卫生—药学]