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铂(Ⅱ)配合物跨人红细胞膜传递的动力学研究
The Kinetic Studies of Across-Erythrocyte Membrane Transport of Platinium( Ⅱ ) Complexes
【摘要】 <正> 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K2PtCl4或K2PtCl6慢。Binks等研究了鼠小肠摄取顺铂和卡铂的动力学机理,指出这两种配合物
【Abstract】 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.
- 【文献出处】 高等学校化学学报 ,Chemical Research In Chinese Universities , 编辑部邮箱 ,1993年10期
- 【被引频次】7
- 【下载频次】37