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咖啡酸与牛血清白蛋白相互作用的体外研究

In vitro study of caffeic acid-bovine serum albumin interaction.

作者信息

Adzet T, Camarasa J, Escubedo E, Merlos M

机构信息

Dep Farmacognosia y Farmacodinamia, Facultad de Farmacia, Universidad de Barcelona, Nucleo Universitario de Pedralbes, Espana.

出版信息

Eur J Drug Metab Pharmacokinet. 1988 Jan-Mar;13(1):11-4. doi: 10.1007/BF03189921.

DOI:10.1007/BF03189921
PMID:3396607
Abstract

Caffeic acid, a natural product with pharmacological properties, such as DOPA-decarboxylase and 5-lipooxygenase inhibition, has been tested in vitro for its binding ratio to bovine serum albumin. This study was carried out by means of four analytical methods. Equilibrium dialysis has been proved to be the most reliable in determination of total binding sites, while acid precipitation has been evaluated as a model of irreversible binding. A binding ratio between 61 and 95% was observed, also varying according the caffeic acid and albumin concentration, pH and protein conformation. Binding constants were calculated by mathematical fitting to a hyperbolic plot. Other cinnamic acids non-o-diphenolic (ferulic acid, m- and p-coumaric acids) have been proved to have a binding ratio to bovine serum albumin of less than 10%.

摘要

咖啡酸是一种具有药理特性的天然产物,如抑制多巴脱羧酶和5-脂氧合酶,其与牛血清白蛋白的结合率已在体外进行了测试。本研究通过四种分析方法进行。平衡透析已被证明是测定总结合位点最可靠的方法,而酸沉淀已被评估为不可逆结合的模型。观察到的结合率在61%至95%之间,也会根据咖啡酸和白蛋白的浓度、pH值和蛋白质构象而变化。通过对双曲线图进行数学拟合来计算结合常数。已证明其他非邻二酚的肉桂酸(阿魏酸、间香豆酸和对香豆酸)与牛血清白蛋白的结合率小于10%。

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本文引用的文献

1
Starch-gel electrophoresis of "purified" albumins.“纯化”白蛋白的淀粉凝胶电泳
Arch Biochem Biophys. 1961 Mar;92:409-19. doi: 10.1016/0003-9861(61)90379-4.
2
Scatchard plot: common misinterpretation of binding experiments.斯卡查德图:结合实验中常见的错误解读
Anal Biochem. 1980 Mar 1;102(2):318-20. doi: 10.1016/0003-2697(80)90160-8.
3
Molecular aspects of ligand binding to serum albumin.配体与血清白蛋白结合的分子层面
Pharmacol Rev. 1981 Mar;33(1):17-53.
4
Improved procedure for the determination of protein binding by conventional equilibrium dialysis.通过传统平衡透析法测定蛋白质结合的改进程序。
J Pharm Sci. 1983 Aug;72(8):918-21. doi: 10.1002/jps.2600720819.
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Caffeic acid is a selective inhibitor for leukotriene biosynthesis.咖啡酸是白三烯生物合成的选择性抑制剂。
Biochim Biophys Acta. 1984 Jan 17;792(1):92-7.
6
Protein binding of timiperone, 4'-fluoro-4-[4-(2-thioxo-1-benzimidazolinyl)piperidino]butyrophenone, a neuroleptic.替米哌隆(4'-氟-4-[4-(2-硫代-1-苯并咪唑啉基)哌啶基]丁酰苯)的蛋白结合情况,替米哌隆是一种抗精神病药物。
Chem Pharm Bull (Tokyo). 1983 Apr;31(4):1411-4. doi: 10.1248/cpb.31.1411.
7
A model for the pH dependence of drug-protein binding.药物-蛋白质结合的pH依赖性模型。
J Pharm Pharmacol. 1981 Mar;33(3):179-82. doi: 10.1111/j.2042-7158.1981.tb13747.x.
8
Protein bindings. VI. Binding of phenols to bovine serum albumin.蛋白质结合。VI. 酚类与牛血清白蛋白的结合。
Chem Pharm Bull (Tokyo). 1969 Feb;17(2):320-3. doi: 10.1248/cpb.17.320.
9
[Quantitative determination of protein binding of drugs by gel filtration].[通过凝胶过滤法定量测定药物的蛋白质结合率]
Arzneimittelforschung. 1968 Mar;18(3):287-9.
10
Mechanisms of denaturation of bovine serum albumin by urea and urea-type agents.尿素及尿素类试剂使牛血清白蛋白变性的机制
Biochim Biophys Acta. 1969;188(2):247-54. doi: 10.1016/0005-2795(69)90072-5.