Department of Physical Pharmacy, Faculty of Pharmacy, Medical University of Silesia, Sosnowiec, Poland.
J Pharm Biomed Anal. 2010 Jan 5;51(1):273-7. doi: 10.1016/j.jpba.2009.07.025. Epub 2009 Jul 30.
Localization of high and low affinity binding sites of furosemide in human serum albumin (HSA) as well as the influence of myristic acid on the drug binding to the albumin using fluorescence quenching method was investigated. Two independent classes of binding site in subdomain IIA of HSA structure were found. Alteration of protein affinity towards the drug and the participation of tryptophanyl and tyrosil residues in drug-albumin interaction for the determined binding sites were studied. It was concluded that association of myristic acid in its low affinity binding sites which corresponds to elevated fatty acid level in vivo, significantly decreases albumin affinity towards furosemide.
用荧光猝灭法研究了人血清白蛋白(HSA)中呋塞米高亲和和低亲和结合位点的定位,以及豆蔻酸对药物与白蛋白结合的影响。发现 HSA 结构的 IIA 亚域中有两个独立的结合位点类别。研究了药物与蛋白质亲和力的变化以及色氨酸和酪氨酸残基在确定的结合位点上与药物-白蛋白相互作用的参与。结论是,体内脂肪酸水平升高时,低亲和结合部位的豆蔻酸的缔合会显著降低白蛋白对呋塞米的亲和力。