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化学学报
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化学学报 ›› 1995, Vol. 53 ›› Issue (12): 1193-1197. 上一篇    下一篇

研究论文

荧光法研究药物分子与人血清白蛋白的结合作用

马贵斌;高尺;任斌知;杨频   

  1. 山西大学化学系
  • 发布日期:1995-12-15

Study on the interaction of human serum albumin and drug molecules by the fluorescence method

MA GUIBIN;GAO CHE;REN BINZHI;YANG PIN   

  • Published:1995-12-15

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761

被引次数

222 | 55

本文应用荧光光谱和能量转移技术首次研究了心血管病药物盐酸地尔硫卓、盐酸川芎嗪和甘草酸三种药物分子与人血清白蛋白的结合作用。研究结果表明, 盐酸川芎嗪和盐酸地尔硫卓在溶液中与白蛋白形成缔合物, 荧光猝灭机理符合静态机制, 缔合物的稳定常数分别为: 盐酸川芎嗪Ks=1.12×10^4(mol/L)^-^1(25℃),Ks=6.95×10^3 (mol/L)^-^1(40℃); 盐酸地尔硫卓Ks=4.71×10^2(mol/L)^-^1(25℃), Ks=3.00×10^2(mol/L)^-^1(40℃)。甘草酸与白蛋白的作用符合动态猝灭机理, 动态猝灭常数为Kd=4.76×10^(mol/L)^-^1(25℃), Kd=6.19×10^2(mol/L)^-^1(40℃)。基于Forster 偶极-偶极无辐射能量转移机理确定了药物分子盐酸川芎嗪在人血清白蛋白中与第214位色氨酸残基之间的距离R=1.76nm(25℃), R=1.80nm(40℃)。

关键词: 血清, 清蛋白, 心血管系统用药, 荧光分光光度法, 甘草酸, 山西省青年科学基金, 盐酸地尔硫卓, 药物分子, 盐酸川芎嗪

In this paper, applying fluorescence quenching method and energy transfer technique, we have firstly studied the interaction of human serum albumin (HSA) with cardiovascular drugs such as dilthiazem, tetramethylpyrazine and glycyrrhizic acid. The results show that dilthiazem and tetramethylpyrazine can form association molecules with HSA in the solution. The mechanism of quenching belongs to static quenching and the association constants between tetramethylpyrazine and HSA are Ks=1.12×10^4(mol/L)^-^1(25℃), 6.95×10^3 (mol/L)^-^1(40℃), and those between dilthiazem and HSA are 4.71×10^2(mol/L)^-^1(25℃), 3.00×10^2(mol/L)^-^1(40℃), respectively. The interaction between HSA and glycyrrhizic acid is dynamic quenching. The dynamic quenching constants are KD=4.76×10^(mol/L)^-^1(25℃), 6.19×10^2(mol/L)^-^1(40℃ ).Based on the mechanism of energy transfer of dipole-dipole interaction between the donor and acceptor, we have determined the distance between 214--tryptophane residue of HSA and drug molecule tetramethylpyrazine to be R=1.76nm(25℃) and .nm(40℃), respectively.

Key words: SERUM, ALBUMINE, CARDIOVASCULAR DRUG, FLUOROSPECTROPHOTOMETRY, GLYCYRRHETINIC ACID

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