抗疟药物α-二丁基氨基甲基-2,6-双（三氟甲基苯基）-4-吡啶甲醇与人血清白蛋白的相互作用。

Interaction of the antimalarial alpha-dibutylaminomethyl-2,6-bis(trifluoromethylphenyl)-4-pyridinemethanol with human serum albumin.

作者信息

Bouwsma O J, Stewart J T, Vallner J J

出版信息

J Pharm Sci. 1979 Jan;68(1):45-8. doi: 10.1002/jps.2600680116.

Abstract

Binding of the antimalarial alpha-dibutylaminomethyl-2,6-bis(trifluoromethylphenyl)-4-pyridinemethanol with human serum albumin was studied using difference spectroscopy, fluorescence quenching, and equilibrium dialysis. Results indicated that the number of high affinity binding sites of the drug on protein is 0.45, with the total number of binding sites being 3.3--4.0. The binding constants were in the range of 0.57--4.00 x 10(6) M-1. The drug was bound more strongly to a nonionic detergent than to either a cationic or anionic detergent. Interpretation of these data and fluorescence quenching results indicated that the drug is possibly bound to a hydrophobic site on human serum albumin.

摘要

采用差示光谱法、荧光猝灭法和平衡透析法研究了抗疟药α-二丁基氨基甲基-2,6-双（三氟甲基苯基）-4-吡啶甲醇与人血清白蛋白的结合情况。结果表明，该药物在蛋白质上的高亲和力结合位点数量为0.45，结合位点总数为3.3 - 4.0。结合常数在0.57 - 4.00×10⁶ M⁻¹范围内。该药物与非离子型去污剂的结合比与阳离子型或阴离子型去污剂的结合更强。对这些数据和荧光猝灭结果的解释表明，该药物可能与人血清白蛋白上的一个疏水位点结合。