中文摘要：

目的观察替莫唑胺（TMZ）类水溶性衍生物2T-P400、2T-P600对人脑胶质瘤的抑制效应。方法体外抑瘤实验：以MTT法测定2T-P400、2T-P600、PEG400、PEG600、TMZ相对于空白对照组对胶质瘤细胞SHG-44的抑制率。体内抑瘤实验：制备荷SHG44人脑胶质瘤裸小鼠模型,将荷瘤鼠随机分为TMZ组、2T-P400组、2T-P600组、聚乙二醇（PEG）组及生理盐水组,TMZ口服给药,其他药物均为鼠尾静脉注射给药,每4天测量肿瘤体积。结果体外抑瘤效应：2T-P400和2T-P600对SHG44细胞的杀伤效果与TMZ相近,均明显优于PEG400和PEG600（P〈0.01）。体内抑瘤效应：TMZ组、2T-P400组和2T-P600组抑瘤率亦明显高于PEG组及生理盐水组（P〈0.05）,未见明显药物不良反应。结论 2T-P400、2T-P600保留TMZ的抑瘤活性,为胶质瘤病人在术后TMZ类药物化疗提供新的药物及用药途径选择。

英文摘要：

Objective To observe the tumor suppression effect of temozolomide（TMZ） water-soluble derivatives（2T-P400,2T-P600） against human gliomas.Methods Anti-tumor test in vitro： The tumor control rate of 2T-P400,2T-P600,PEG400,PEG600 and TMZ were assayed by MTT method in the blank control group.Anti-tumor test in vivo： SHG44 glioma-bearing nude mice models were prepared,and divided randomly into TMZ group,2T-P400 group,2T-P600 group,PEG group and normal saline（NS） group.TMZ was administered orally,and the other drugs were administered via tail vein injection.Tumor volumes of the mice were measured once every four days.Results Anti-tumor effect in vitro： The anti-glioma effects of 2T-P400 and 2T-P600 were almost the same level with that of TMZ against SHG44 cells,and the effects were much better than those in PEG group and NS group（P 0.01）.Anti-tumor test in vivo： Tumor inhibition ratios in TMZ,2T-P400 and 2T-P600 groups were higher than those in PEG and NS groups（P 0.05）.No obvious adverse drug reactions occurred.Conclusions 2T-P400 and 2T-P600 retain anti-tumor activity of TMZ,and will provide new drugs and treatment option for chemotherapy with TMZs in post-operative glioma patients.