二乙酰二脱水卫矛醇抗瘤作用的实验研究

Experimental study of antitumor effect of 1,2:5,6-dianhydro-3,4-diacetylgalactitol against tumor

目的 探讨二乙酰二脱水卫矛醇 (1 ,2 :5 ,6 -Dianhydro - 3 ,4-diacetylgalactitol,DADAG)的体内外抗肿瘤作用。方法 用MTT法观察DADAG对人肿瘤细胞株的抗增殖作用 ;以小鼠脑内移植艾氏腹水癌 (Ehrlichascitescarcinoma,EAC)和DBA/ 2小鼠脑内移植白血病L1 2 1 0为移植瘤模型 ,观察DADAG的体内抗瘤效果。结果 DADAG对HL60细胞和K562细胞有较强的抑制作用 ,IC50 值分别为 3 .7μg·ml- 1 和 2 5 .5μg·ml- 1 。DADAG的高剂量(1 0 .0mg·kg- 1 )对小鼠脑内移植EAC有一定的抑制作用 ,对小鼠的生存期延长率 (increaseoflifespan ,ILS)是 30 % (P <0 .0 5) ;而DADAG的低剂量 6 .4mg·kg- 1 、中剂量 8.0mg·kg- 1 和高剂量 1 0 .0mg·kg- 1 对小鼠脑内移植白血病L1 2 1 0均有明显的抑制作用 ,ILS分别为 35 %、47%和 55 % (P值均 <0 .0 1 )。

Objective To evaluate the effects of antitumor of 1,2:5,6-dianhydro-3,4-diacetylgalactitol (DADAG) chemotherapy in vitro and in vivo. Methods The antiproliferative activity of DADAG for tumor cell strain in vitro using MTT assay and the antitumor effect of DADAG in vivo using intracerebrally inoculated.Ehrlich ascites carcinoma(EAC) or L1210 leukemia in mice were observed. Results DADAG had potential antiproliferative activity on human HL-60 cells and K562 cells,the IC 50 value was 3.7?μg·ml -1 and 25.5?μg·ml -1 ,respectively. The high dose of DADAG(10.0?mg·kg -1 ,ip) inhibited intracerebrally inoculated EAC in mice, and the increase of life span(ILS) was 30%(P<0.05 ). While DADAG at doses of 6.4?mg·kg -1 , 8.0?mg·kg -1 and 10.0?mg·kg -1 exhibited significantly inhibitory effects on intracerebrally inoculated L1210 leukimia in mice compared with NS treatment,the ILSes were 35%,47% and 55%(P<0.01,respectively).Conclusion DADAG possesses potential antitumor activity in vitro and in vivo.