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某些新型水溶性金属席夫碱配合物与牛血清白蛋白的亲和力及抗癌活性

Affinity to bovine serum albumin and anticancer activity of some new water-soluble metal Schiff base complexes.

作者信息

Asadi Mozaffar, Asadi Zahra, Zarei Leila, Sadi Somaye Barzegar, Amirghofran Zahra

机构信息

Chemistry Department, College of Sciences, Shiraz University, Shiraz 71454, Islamic Republic of Iran.

Chemistry Department, College of Sciences, Shiraz University, Shiraz 71454, Islamic Republic of Iran.

出版信息

Spectrochim Acta A Mol Biomol Spectrosc. 2014 Dec 10;133:697-706. doi: 10.1016/j.saa.2014.05.031. Epub 2014 Jun 18.

Abstract

Metal Schiff-base complexes show biological activity but they are usually insoluble in water so four new water-soluble metal Schiff base complexes of Na2[M(5-SO3-1,2-salben]; (5-SO3-1,2-salben denoted N,N'-bis(5-sulphosalicyliden)-1,2-diaminobenzylamine and M=Mg, Mn, Cu, Zn) were synthesized and characterized. The formation constants of the metal complexes were determined by UV-Vis absorption spectroscopy. The interaction of these complexes with bovine serum albumin (BSA) was studied by fluorescence spectroscopy. Type of quenching, binding constants, number of binding sites and binding stoichiometries were determined by fluorescence quenching method. The results showed that the mentioned complexes strongly bound to BSA. Thermodynamic parameters indicated that hydrophobic association was the major binding force and that the interaction was entropy driven and enthalpically disfavoured. The displacement experiment showed that these complexes could bind to the subdomain IIA (site I) of albumin. Furthermore the synchronous fluorescence spectra showed that the microenvironment of the tryptophan residues was not apparently changed. Based on the Förster theory of non-radiation energy transfer, the distance between the donor (Trp residues) and the acceptor metal complexes was obtained. The growth inhibitory effect of complexes toward the K562 cancer cell line was measured.

摘要

金属席夫碱配合物具有生物活性,但它们通常不溶于水,因此合成并表征了四种新的水溶性金属席夫碱配合物Na2[M(5-SO3-1,2-salben];(5-SO3-1,2-salben表示N,N'-双(5-磺基水杨醛)-1,2-二氨基苄胺,M = Mg、Mn、Cu、Zn)。通过紫外可见吸收光谱法测定了金属配合物的形成常数。通过荧光光谱法研究了这些配合物与牛血清白蛋白(BSA)的相互作用。采用荧光猝灭法测定了猝灭类型、结合常数、结合位点数量和结合化学计量比。结果表明,上述配合物与BSA有强烈的结合。热力学参数表明,疏水缔合是主要的结合力,且相互作用是由熵驱动的,焓变不利。置换实验表明,这些配合物可以与白蛋白的亚结构域IIA(位点I)结合。此外,同步荧光光谱表明色氨酸残基的微环境没有明显变化。基于福斯特非辐射能量转移理论,得到了供体(色氨酸残基)与受体金属配合物之间的距离。测定了配合物对K562癌细胞系的生长抑制作用。

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