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采用元素分析和红外光谱法确证所合成的口服铂族抗癌药JM 2 2 1[c,t ,c -Pt (IV )Cl2 (O2CPr) 2 (NH2 c -Hexyl) (NH3) ]的化学结构 ;以人卵巢癌细胞株HO - 8910及相应的裸小鼠移植瘤为模型测定JM 2 2 1的体内外抗肿瘤活性 ,并用Bliss法计算其小鼠经口的半数致死剂量LD50 .结果显示 ,合成的JM 2 2 1对人卵巢癌细胞株HO - 8910的增殖具有明显的抑制作用 ,IC50 为 0 5 2 μmol·L-1;口服剂量为 90mg kg-1时 ,对HO - 8910裸小鼠移植瘤的生长抑制率达 60 % ;经口服给药的LD50 为 2 64 85mg·kg-1.以上结果提示口服铂族抗癌药JM 2 2 1的合成是成功的 .
The chemical structure of the synthesized platinum group anticancer drug JM 2 2 1[c,t,c-Pt(IV )Cl2(O2CPr) 2 (NH2 c -Hexyl) (NH3)] was confirmed by elemental analysis and infrared spectroscopy. The human ovarian cancer cell line HO-8910 and the corresponding nude mouse xenograft tumor model were used to determine the anti-tumor activity of JM221 in vitro and in vivo, and the LD50 of mice’s oral lethal dose LD50 was calculated by Bliss method. The synthesized JM 2 1 1 had a significant inhibitory effect on the proliferation of human ovarian cancer cell line HO-8910 with an IC50 of 052 μmol·L -1 and an oral dose of 90 mg kg -1 for HO - 8910 nude mice. The growth inhibition rate of transplanted tumors was up to 60%; the oral administration of LD50 was 2 64 85 mg·kg-1. The above results suggest that the synthesis of oral platinum group anticancer drug JM 2 2 1 was successful.