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

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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.