尼可刹米与牛血清白蛋白相互作用及共存金属离子的影响

The interactions of Nikethamide with bovine serum albumin and the effect of coexistent metal ions on the reactions

在优化的实验条件下,运用光谱法研究牛血清白蛋白(BSA)与尼可刹米(NI)的相互作用及共存金属离子的影响。研究表明:NI对BSA的荧光有猝灭作用,属于动态猝灭。BSA能运输NI,是一个自发过程,其作用力类型主要为疏水作用力。BSA的亚螺旋域ⅡA是主要结合位置,离酪氨酸残基更近,无药物协同作用。NI对BSA构象产生影响。Mg^(2+)、Cu^(2+)对PDS与BSA结合产生竞争作用,增强药效。Mn^(2+)、Cr^(3+)和Co^(2+)对PDS与BSA结合产生促进作用,延长药效时间。该实验对揭示药物动力学问题及新药的研发提供了理论依据。

Under the optimal conditions,the interactions between bovine serum albumin (BSA)with Nik-ethamide (NI)and the potential effects of metal ions were studied with spectrometry.It was found that the fluorescence of BSA was quenched by NI,which was a dynamic quenching process.BSA could transport NI.The hydrophobic attraction might play an important role in the conjugation reaction of BSA and NI. The primary binding site for NI was located at sub-domain ⅡA of BSA and near by tyrosine residue.There was almost no cooperative effect.The conjugation reaction could affect the conformation of BSA.Mg2+ and Cu2+ competed in the interactions of NI with BSA,increasing medical effectiveness.Mn2+ ,Cr3+ and Co2+promoted on interactions and prolonged drug effect time.The results provided a theoretical basis for revea-ling the pharmacokinetics and further research on development of new drugs.