Sakai T, Takadate A, Otagiri M
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
Biol Pharm Bull. 1995 Dec;18(12):1755-61. doi: 10.1248/bpb.18.1755.
The interaction of uremic toxins including indole-3-acetic acid (IA), indoxyl sulfate (IS), hippuric acid (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropanoic acid (CMPF) with human serum albumin (HSA) has been investigated by three methods of fluorescent probe displacement, ultrafiltration and equilibrium dialysis. The binding parameter of CMPF was found to have the strongest affinity (10(7)M-1) among all the uremic toxins studied. Competitive experiment based on the method of Kragh-Hansen suggested that IA, IS and HA bind to site II, whereas CMPF binds to site I. The present limited data indicated that the four uremic toxins caused inhibition to any endo- or exogenous substances on HSA.
通过荧光探针置换、超滤和平衡透析三种方法,研究了包括吲哚 - 3 - 乙酸(IA)、硫酸吲哚酚(IS)、马尿酸(HA)和3 - 羧基 - 4 - 甲基 - 5 - 丙基 - 2 - 呋喃丙酸(CMPF)在内的尿毒症毒素与人血清白蛋白(HSA)的相互作用。在所有研究的尿毒症毒素中,发现CMPF的结合参数具有最强的亲和力(10⁷M⁻¹)。基于Kragh - Hansen方法的竞争性实验表明,IA、IS和HA结合到位点II,而CMPF结合到位点I。目前有限的数据表明,这四种尿毒症毒素对HSA上的任何内源性或外源性物质都有抑制作用。