The effects of a newly synthesized cisplatin derivative (=PyPt) agains malignant brain tumor

新合成的顺铂衍生物4- ppyridoxate二胺羟基铂（PyPt）对脑肿瘤的体外和体内抗肿瘤作用进行了评价，并与顺铂进行了比较。用MIT法测定了大鼠（9L和C6）和人（T98G和A172）恶性胶质瘤细胞系的体外化学敏感性。PtPy达到50%生长抑制（1C50）所需的Thc浓度显著高于9L、C6和T98G，而A172显著低于顺铂。这表明PyPt对人A172胶质瘤细胞系比顺铂更有效。在体内实验中，大鼠脑接种9L镓，选择性颈动脉内灌注PyPt （2.0mg kg-1）和顺铂（1.4 mg kg-1）。与对照动物相比，生存时间有显著改善。虽然PyPt在9L细胞系的体外抗肿瘤活性明显低于顺铂，但在体内的抗肿瘤活性与顺铂几乎相等。PyPt治疗后脑肿瘤内铂浓度为30 n-tin，显著高于顺铂治疗组2.4倍。这表明PyPt对9L胶质瘤的药物递送效率高于顺铂。PyPt是治疗脑肿瘤的一种有效的顺铂衍生物。

Antiturnor effects of a newly synthesized cisplatin derivative, 4-Ppyyridoxate diammine hydroxy platinum (PyPt), against brain tumors in-vitro and in-vivo were evaluated and compared with cisplatin.In-vitro chemosensitivity of rat (9L and C6) arid human (T98G and A172) malignant glioma cell lines was measured using the MIT assay method. Thc concentration required for 50% growth inhibition (1C50) for PtPy was significantly higher than cisplatin for 9L, C6 and T98G, but significantly lower for A172. This indicates that PyPt is more effective than cisplatin against the human A172 glioma cell line. For in-vivo experiments, rat brain inoculated with 9L gallium, and PyPt (2.0mg kg-1) and cisplatin (1,4mg kg-1) were administered as selective intracarotid infusions. A significant improvement in survival time compared with control animals was found.Although in-vitro antitumor activity of PyPt was significantly lower than cisplatin in the 9L cell line, in-vivo activity was almost equal to that of cisplatin. Platinum concentration in the brain tumor, 30 n-tin after administration of PyPt, was 2.4 times dignificantly higher than with cisplatin. This suggests that drug delivery efficiency t the 9L glioma is greater for PyPt than cisplatin. PyPt is an effective cisplatin derivative for the treatment of brain tumors.