人红细胞摄取环己二胺合铂(Ⅱ)配合物的手性选择性研究

Studies on the Chiral Selectivity of Transmembrane Transport of the Pt(II) Complexes with 1,2 - Diaminocyclohexane as Carrier Ligand into Human Erythrocytes

合成了六种以不同手性的1,2-环己二胺(1,2-dach)作为载体配体的铂(II)配合物,用元素分析、红外及分子图形方法对其组成和结构进行了表征.测定了它们跨入红细胞膜的一级反应动力学常数、用膜蛋白巯基滴定、荧光标记、自旋标记ESR谱等方法研究了它们与膜蛋白、膜脂的相互作用;用脂质体模拟了这些配合物的细胞摄入.结果表明:这些配合物主要通过简单扩散进入红细胞,其跨膜速率对环己二胺的手性具有明显的选择性.这种选择性主要来源于配合物与膜脂作用过程中的手性识别.

Six Pt (II) complexes with chiral 1,2- diaminocyclohexane as carrier ligand were synthesized, their compositions and structures were characterized by elemental analysis, IR spectroscopy and molecular modeling. The first - order rate constants for the transmembrane transport of the complexes into human erythrocytes were detennined and the mechanism was studied on the basis of the interactions of these complexes with cellular membranes and liposome by ESR, fluorescence technique, mercapto measurement and gelchromatography. The results show that the transmembrane transport of the complexes studied exhibited a chiral selectivity, and the selectivity is mainly due to chiral recognition of membrane phospholipid with the chiral complexes.