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[各种药物对血清白蛋白中胆红素结合位点的影响]

[The effects of various drugs on the binding site of bilirubin in serum albumin].

作者信息

Hasegawa J, Nozaki M, Fujimura H

出版信息

Nihon Yakurigaku Zasshi. 1984 Jan;83(1):79-83.

PMID:6714852
Abstract

In the presence of various drugs, the concentration of free bilirubin which was released from the first binding site of bilirubin in serum albumin was evaluated, using a sensitive method based on static fluorescence quenching of dansyl serum albumin. Bilirubin bound to human serum albumin more strongly than to bovine serum albumin. Non-steroidal anti-inflammatory drugs, fenamates and allylphenyl propionic acids, affected the bilirubin-serum albumin interaction. Flufenamic acid and ketoprofen released bilirubin from human serum albumin. The bilirubin bound to the serum albumin was not influenced by the presence of indomethacin, but clidanac strongly dissociated bilirubin from the bilirubin-serum albumin complex. Sulfa-drugs, antibiotics, steroidal agents, warfarine, tolubutamide and phenytoin showed no significant effects on the bilirubin-serum albumin interaction. The fluorescence quenching method may be useful to evaluate the interaction of drug-bilirubin-serum albumin.

摘要

利用基于丹磺酰血清白蛋白静态荧光猝灭的灵敏方法,对在多种药物存在的情况下从血清白蛋白中胆红素的第一个结合位点释放出来的游离胆红素浓度进行了评估。胆红素与人血清白蛋白的结合比与牛血清白蛋白的结合更强。非甾体抗炎药、灭酸类药物和烯丙基苯基丙酸会影响胆红素 - 血清白蛋白的相互作用。氟芬那酸和酮洛芬会使人血清白蛋白释放胆红素。与血清白蛋白结合的胆红素不受吲哚美辛存在的影响,但氯达诺会使胆红素从胆红素 - 血清白蛋白复合物中强烈解离。磺胺类药物、抗生素、甾体类药物、华法林、甲苯磺丁脲和苯妥英对胆红素 - 血清白蛋白的相互作用无显著影响。荧光猝灭法可能有助于评估药物 - 胆红素 - 血清白蛋白的相互作用。

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