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用荧光及园二色谱对人红细胞收缩蛋白(SP)与不同组成和构型的Pt(I)络合物的作用进行了研究。结果表明,SP有47×102个顺铂(CDDP)结合部位。其中,最高亲和性部位70个,K1>347×106;较高亲和性的18×102个,其K2=347×106;其余22×102个为低亲和性的,其K3=877×105。Pt(I)络合物与SP的结合导致SP构象变化,这种变化与Pt(I)络合物浓度及络合物与SP的浓度比有关。CDDP及顺式二水二氨合铂(I)与SP的作用在初始1h内遵从双阶段一级动力学,动力学常数也已测定。反应1h后,为络合物与SP作用的后续变化阶段,这一阶段可能涉及SP的构象改变、聚合及解聚。值得注意的是,SP与1,2环己二胺不同异构体作为载体配体的Pt(I)络合物作用时,空间匹配性比Pt(I)与SP的巯基的亲和性显得更为重要。
The effects of human erythrocyte contractile protein (SP) on Pt (I) complexes of different composition and configuration were investigated by fluorescence and circular dichroism. The results showed that SP has 4 7 × 102 cisplatin (CDDP) binding sites. Among them, the highest affinity sites 70, K1> 3 47 × 106; higher affinity 1 8 × 102, the K2 = 3 47 × 106; the remaining 2 2 × 102 for the low pro And sexual, the K3 = 8 77 × 105. The binding of the Pt (I) complex to SP results in a conformational change in SP, which is related to the Pt (I) complex concentration and the complex to SP concentration ratio. The effects of CDDP and cisplatin (I) cisplatin on SP follow a two-stage first-order kinetic within the initial 1 h and kinetic constants have also been determined. After reaction for 1h, the subsequent phase of the interaction of the complex with SP may involve the conformational changes, polymerization and depolymerization of SP. It is noteworthy that the SP matches the Pt (I) complex of different isomers of 1,2cyclohexanediamine as the carrier ligand, and the spatial matching is better than the affinity of Pt (I) and the thiol of SP It is even more important.