摘要
顺铂(cis-DDP)和顺式1,1-环丁烷二羧基二胺合铂(Ⅱ)(即卡铂,CBDCA)具有良好的抗癌活性,其主要靶分子均为DNA。但这些配合物与DNA作用前必须首先通过细胞膜。离体肿瘤对顺铂的摄入要比卡铂快得多,海拉细胞(Helas-3)摄入顺铂的速度要比摄入K_2PtCl_4或K_2PtCl_6慢。Binks等研究了鼠小肠摄取顺铂和卡铂的动力学机理。
In the synthetic plasma, the uptake kinetics of cis-platin and it' s related compounds in human erythrocytes was studied. The experimental results show that the across-membrane transport of all the platinum compounds studied follows a first-order kinetic process in the initial stage. The entry of these compounds into the human red blood cell is considered to follow a passive diffusion mechanism. The uptake rate constants of seven platinum( Ⅱ ) compounds were determined. The uptake rates are related to the polarity, charge and hydrolysis rate of the coordination compounds.
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
1993年第10期1351-1354,共4页
Chemical Journal of Chinese Universities
基金
国家自然科学基金
国家教育委员会博士点基金
关键词
膜传递
动力学
铂
络合物
Platium compounds, Membrane transport, Kinetics