铂类抗癌新药双环铂的体内外抗肿瘤活性  

In Vitro and In Vivo Antitumour Activity of Dicycloplatin,A New Active Platinum Complex

作　　者：颜冬梅[1] 屠凌岚[1] 彭小英[1] 李文钧[1] 沈正荣[1] 

机构地区：[1]浙江省医学科学院药物所,杭州310013

出　　处：《中国现代应用药学》2007年第5期352-356,共5页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的观察铂类抗癌新药双环铂的体内外抗肿瘤活性及其对细胞周期的影响。方法MTT法观察双环铂对人肿瘤细胞增殖的抑制作用;小鼠动物肿瘤模型观察双环铂对肿瘤的体内抑制作用;碘化丙锭PI染色流式细胞术分析药物所致人卵巢癌细胞A2780细胞的周期变化。结果双环铂于体外抑制多种人肿瘤细胞增殖,体内抑制小鼠肉瘤S180、肝癌Heps及黑色素瘤B16的生长,并导致A2780细胞S期细胞明显增加及G2/M期细胞少许增加。结论双环铂具有明显的体内外抗肿瘤活性,并影响肿瘤细胞的细胞周期分布。　OBJECTIVE To evaluate the antitumor activity of dicycloplatin in vitro and in vivo.METHODS The cytotoxities against 8 human cancer cell lines in vitro of dicycloplatin were evaluated MTT method,the growth inhibitory for murine tumor models in vivo and the effect of dicycloplatin on A2780 cell cycle were also investigated. RESULTS Dicycloplatin showed significant cytotoxity in a panel of human tumour cell in vitro.in vivo,dicycloplatin exhibited activity,broadly comparable to cisplatin,across murine sarcoma S180,hepatoma Heps and melanoma B16.The growth inhibitory of dicycloplatin is 95.8% against S180,92.1% against Heps and 75.5% against B16 at ip dose 60 mg kg-1.The cell cycle of human ovarian carcinoma A2780 was arrested with blocking the G1-S transition by dicycloplatin.CONCLUSION Dicycloplatin showed significant cytotoxity in vitro,the growth inhibitory to murine tumor models in vivo and induces cell cycle arrest.

关 键 词：双环铂 顺铂 抗肿瘤药 细胞周期 

分 类 号：R916.696[医药卫生—药学] TQ462.8[化学工程—制药化工]