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某些苯基茚满二酮类抗凝血剂与人血清白蛋白的相互作用。

Interactions of some phenylindanedione anticoagulants with human serum albumin.

作者信息

Paubel J, Niviere P, Payard M, Rabadeux J C, Pinazzi C P

出版信息

Eur J Drug Metab Pharmacokinet. 1981;6(4):241-8. doi: 10.1007/BF03189520.

Abstract

This study enabled us, to define the quantitative parameters of the interactions which give rise to the formation of complexes between five phenylindanediones and albumin or polymethacryate. The existence of three attachment sites were demonstrated, by which these ligands are bound to the macromolecule. The results from the thermodynamic study of this phenomenon, together with the information supplied by; various spectroscopic methods; the formation of a complex between a synthetic polymer carrying amine functions, and the study of ligands in the presence of surfactant, were all in agreement. Furthermore, a significant correlation between the association constant and physiochemical parameters lipophilic character and acidity was obtained, leading to the conclusion that; the interactions permitting the formation of the complexes between albumin and the five anionic ligands seem to be principally hydrophobic and, to a lesser degree, electrostatic. The latter only occurred in a particular medium at sites which were mainly hydrophobic.

摘要

本研究使我们能够定义导致五种苯基茚满二酮与白蛋白或聚甲基丙烯酸酯形成复合物的相互作用的定量参数。已证明存在三个结合位点,通过这些位点这些配体与大分子结合。对该现象的热力学研究结果,以及各种光谱方法提供的信息、带有胺官能团的合成聚合物之间复合物的形成以及表面活性剂存在下配体的研究结果均一致。此外,关联常数与亲脂性和酸度等物理化学参数之间存在显著相关性,从而得出结论:白蛋白与五种阴离子配体之间形成复合物的相互作用似乎主要是疏水的,且在较小程度上是静电的。后者仅在特定介质中的主要疏水位点发生。

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