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在脂肪酸存在的情况下,对乙酰己脒与糖化血清白蛋白结合的体外研究。

In Vitro Investigations of Acetohexamide Binding to Glycated Serum Albumin in the Presence of Fatty Acid.

机构信息

Department of Physical Pharmacy, Faculty of Pharmaceutical Siences in Sosnowiec, Medical University of Silesia in Katowice, 40-001 Katowice, Poland.

Institute of Sport Sciences, Jerzy Kukuczka Academy of Physical Education in Katowice, 40-001 Katowice, Poland.

出版信息

Molecules. 2020 May 17;25(10):2340. doi: 10.3390/molecules25102340.

Abstract

The interaction of drugs with human serum albumin (HSA) is an important element of therapy. Albumin affects the distribution of the drug substance in the body, as well as its pharmacokinetic and pharmacodynamic properties. On the one hand, inflammation and protein glycation, directly associated with many pathological conditions and old age, can cause structural and functional modification of HSA, causing binding disorders. On the other hand, the widespread availability of various dietary supplements that affect the content of fatty acids in the body means that knowledge of the binding activity of transporting proteins, especially in people with chronic diseases, e.g., diabetes, will achieve satisfactory results of the selected therapy. Therefore, the aim of the present study was to evaluate the effect of a mixture of fatty acids (FA) with different saturated and unsaturated acids on the affinity of acetohexamide (AH), a drug with hypoglycaemic activity for glycated albumin, simulating the state of diabetes in the body. Based on fluorescence studies, we can conclude that the presence of both saturated and unsaturated FA disturbs the binding of AH to glycated albumin. Acetohexamide binds more strongly to defatted albumin than to albumin in the presence of fatty acids. The competitive binding of AH and FA to albumin may influence the concentration of free drug fraction and thus its therapeutic effect.

摘要

药物与人体血清白蛋白(HSA)的相互作用是治疗的一个重要因素。白蛋白影响药物在体内的分布,以及其药代动力学和药效学特性。一方面,与许多病理状况和衰老直接相关的炎症和蛋白质糖化作用会导致 HSA 的结构和功能发生改变,从而引起结合紊乱。另一方面,各种影响体内脂肪酸含量的膳食补充剂的广泛应用意味着,了解转运蛋白的结合活性,特别是在患有慢性疾病(如糖尿病)的人群中,将为选定的治疗方案取得满意的效果。因此,本研究的目的是评估混合脂肪酸(FA)对乙酰己脒(AH)与糖化白蛋白亲和力的影响,AH 是一种具有降血糖活性的药物,用于模拟体内糖尿病的状态。基于荧光研究,我们可以得出结论,饱和和不饱和 FA 的存在会干扰 AH 与糖化白蛋白的结合。在存在脂肪酸的情况下,乙酰己脒与去脂白蛋白的结合比与白蛋白的结合更强。AH 和 FA 与白蛋白的竞争性结合可能会影响游离药物部分的浓度,从而影响其治疗效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1bb4/7287933/1cb8e7ac2022/molecules-25-02340-sch001.jpg

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