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研究人红细胞摄入具有手性配体的铂(Ⅱ)配合物的手性选择性和摄入机制。方法:合成1,2-环己二胺(1,2-diaminocyclohexane,dach)作截体配体,柠檬酸根(cit)作为离去基团的配合物Na[Pt(dach)(cit)],并用元素分析、红外光谱对其组成和结构进行表征;测定人红细胞摄入这些配合物的动力学常数并研究阴离子通道抑制剂(4,4’-diisothiocysnatostilbene-2,2’-disulfonic acid,DIDS)对摄入的影响。结果:人红细胞对[Pt(dach)(cit)]-3种手性异构体的摄入服从一级动力学过程并且具有不同的速率常数, DIDS可抑制 40%～ 50%的铂(Ⅱ)配合物进入细胞。结论:人红细胞对[Pt( dach)( cit)]~-的摄入具有手性选择性,这些配合物可通过简单扩散及阴离子通道进入人红细胞。
To investigate the chiral selectivity and uptake mechanism of human erythrocytes uptake of platinum (II) complexes with chiral ligands. Methods: 1,2-diaminocyclohexane (dach) (dach) (cit)] was synthesized by the reaction of citrate (cit) The composition and structure of the complexes were characterized by elemental analysis and infrared spectroscopy. The kinetic constants of these complexes were determined and the activities of 4’-diisothiocysnatostilbene-2,2’-disulfonic acid (DIDS) Impact on intake. Results: The human erythrocytes upregulated the first order kinetics of Pt (dach) (cit) - 3 chiral isomers and had different rate constants. DIDS inhibited 40% ~ 50% platinum (Ⅱ ) Complex into the cell. CONCLUSION: Human erythrocytes have chiral selectivity for the uptake of [Pt (dach) (cit)] ~ and these complexes enter human erythrocytes via simple diffusion and anion channels.