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A novel lophine-based fluorescence probe and its binding to human serum albumin

机译:一种新型的基于lophine的荧光探针及其与人血清白蛋白的结合

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摘要

The binding of a lophine-based fluorescence probe, 4-[4-(4-dimethylaminophenyl)-5-phenyl-1H-imidazol-2-yl]benzoic acid methyl ester (DAPIM) with human serum albumin (HSA) was investigated by fluorescence spectroscopy under physiological conditions. While DAPIM shows extreme low fluorescence in aqueous solution, DAPIM binding with HSA emits strong fluorescence at 510nm. The binding constant and binding number determined by Scatchard plot was 3.65×106M-1 and 1.07, respectively. Competitive binding between DAPIM and other ligands such as warfarin, valproic acid, diazepam and oleic acid, were also studied fluorometrically. The results indicated that the primary binding site of DAPIM to HSA is site II at subdomain IIIA. DAPIM can be a useful fluorescence probe for the characterization of drug-binding sites. In addition to the interaction study, because the fluorescence intensity of DAPIM increased in proportion to HSA concentration, its potential in HSA assay for serum sample was also evaluated.
机译:通过以人为基础的荧光探针,研究4- [4-(4-二甲基氨基苯基)-5-苯基-1H-咪唑-2-基]苯甲酸甲酯(DAPIM)与人血清白蛋白(HSA)的结合。生理条件下的荧光光谱。 DAPIM在水溶液中显示出极低的荧光,而DAPIM与HSA的结合在510nm处发出强荧光。通过Scatchard图测定的结合常数和结合数分别为3.65×106M-1和1.07。还用荧光法研究了DAPIM与其他配体(如华法林,丙戊酸,地西epa和油酸)之间的竞争性结合。结果表明,DAPIM与HSA的主要结合位点是亚域IIIA的位点II。 DAPIM可能是用于表征药物结合位点的有用的荧光探针。除了相互作用研究外,由于DAPIM的荧光强度与HSA浓度成正比,因此还评估了其在血清样品的HSA分析中的潜力。

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