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首页> 外文期刊>Chemical and Pharmaceutical Bulletin >A kinetic study of protein binding to ecabet sodium using quartz-crystal microbalance.
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A kinetic study of protein binding to ecabet sodium using quartz-crystal microbalance.

机译：使用石英晶体微量天平对蛋白质与依卡贝钠的结合进行动力学研究。

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摘要

To define the mechanism of the protection by ecabet sodium of the gastric mucosa, the characteristics of protein binding of this drug were investigated using a quartz-crystal microbalance (QCM) method. The binding rate constants (kb) and the binding amounts (delta m) were obtained from time courses of the frequency decrease (mass increase) of the QCM. The binding constants to proteins of two ecabet analogues (G1, ecabet type and G2, non-ionic ecabet type) were dependent on the pH, leading to large kb values at the acidic region. Furthermore, the kb values of G1 with the addition of bovine serum albumin (BSA) and bovine serum fibrinogen (BSF) at the acid region were larger than those of G2. The difference in kb values between G1 and G2 for porcine gastric mucin (PGM) is hardly discernible. Ecabet seems to be more heavily distributed in the ulcerous areas than in the intact mucosa, judging from the large binding constants of this drug to BSA and BSF compared with those to PGM. It is suggested that ecabet is bound to proteins by hydrophobic interaction, moreover, the electrostatic interaction between this drug and proteins (BSA and BSF) occurs at acidic pH region. On account of these interactions, ecabet sodium seems to have a more protective effect on an ulcer at intraluminal acidity than sucralfate. Finally, QCM was found to be a useful technique for detecting quantitatively the time course of binding proteins with drug.
机译：为了确定依卡倍特钠对胃粘膜的保护作用机理，使用石英晶体微量天平（QCM）方法研究了该药物的蛋白质结合特性。结合速率常数（kb）和结合量（δm）是从QCM的频率降低（质量增加）的时间过程获得的。两种依卡贝特类似物（G1，依卡贝特类型和G2，非离子依卡贝特类型）与蛋白质的结合常数取决于pH值，导致酸性区域的kb值较大。此外，在酸性区域添加牛血清白蛋白（BSA）和牛血清纤维蛋白原（BSF）的G1的kb值大于G2。猪胃粘蛋白（PGM）的G1和G2之间的kb值差异几乎无法辨认。依卡贝特似乎在溃疡区域的分布要比完整黏膜的分布要大，这是因为该药物与BSA和BSF的结合常数较高，而与PGM的结合常数较大。提示依卡贝糖通过疏水相互作用与蛋白质结合，此外，该药物与蛋白质（BSA和BSF）之间的静电相互作用发生在酸性pH区域。由于这些相互作用，依卡贝酸钠在腔内酸度下似乎比硫糖铝对溃疡具有更好的保护作用。最后，发现QCM是定量检测蛋白与药物结合的时程的有用技术。

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