赛特铂抗肿瘤作用的临床前观察

Preclinical observation of the antitumor activity of satraplatin

目的 :观察赛特铂临床前抗肿瘤作用。方法 :体外观察赛特铂对人卵巢癌细胞A2 780 ,肺腺癌细胞A5 4 9,结肠癌细胞HCT8,乳腺癌细胞MCF7和前列腺癌细胞DU14 5等 10株人肿瘤细胞的细胞毒作用。体内观察赛特铂对人卵巢癌A2 780 ,小鼠肉瘤S180和小鼠肝癌HepS的生长抑制作用。结果 :赛特铂的体外体内作用强度与对照药顺铂相当。对 10种肿瘤细胞的半数抑制浓度IC50 为 0 5 1～ 3 2 9μmol·L-1,平均IC50 为 (1 4 4± 0 32 )μmol·L-1;体内口服给药明显抑制裸鼠人卵巢癌A2 780 ,小鼠肉瘤S180和小鼠肝癌HepS的生长 ,抑制率分别为6 1 3% ,5 7 9%和 5 0 6 %。结论 :赛特铂的体外细胞毒和体内口服抗小鼠肿瘤生长抑制作用均与顺铂相仿。

Objective:To observe preclinically the anti-tumor activity of satraplatin. Methods: The cytotoxicity of satraplatin in 10 human cancer cell lines in vivo and the growth inhibitory effect of satraplatin in vivo in human ovary cancer A2780,murine sarcoma S180 and murine hepatoma HepS were examined. Results: The cytotoxicity of satraplatin in vitro was similar to that of cisplatin.The IC_ 50 for 10 human cancer cell lines in vitro was 0.51～3.29μmol·L -1 with a mean of(1.44±0.32)μmol·L -1 .The growth of human ovarian A2780 in nude mouse model,murine sarcoma S180,and murine heptoma HepS were significantly inhibited with a inhibitory rate of 61.3%for A2780,57.9%for S180,and 50.6%for HepS. Conclusion: The in vivo cytotoxicity and in vivo inhibitory effect on the growth of tumor for satraplatin were similar to that of cisplatin.