目的研究茵陈中3个香豆素小分子与牛血清白蛋白(BSA)结合作用的机制。方法荧光猝灭法和紫外吸收光谱法。结果茵陈香豆素类小分子能够插入牛血清白蛋白内部与牛血清白蛋白形成复合物导致牛血清白蛋白内源性荧光猝灭,药物分子的极性对内源性荧光猝灭有一定的影响,猝灭机制主要为静态猝灭和非辐射能量转移。结合过程的热力学参数变化表明,上述相互作用过程是一个熵增的自发分子间作用过程。结论牛血清白蛋白与茵陈香豆素类小分子间有较强的结合作用,且结合力以疏水作用为主,其中东莨菪内酯还存在偶极-偶极作用。
Abstract
OBJECTIVE To study the interaction between three coumarins from Artemisa capillaris Thunb. and BSA. METHODS Spectrophotometry and fluorescence quenching method were used. RESULTS The testing coumarins were inserted into the hydrophobic pockets of BSA, quenching the inner fluorescence of BSA by forming the pharmaceutical-BSA complex. Both static quenching and nonradiative energy transferring were confirmed to result in the fluorescence quenching. The enlargement of molecular polarity and volume of the pharmaceutics had the effect on the quenching efficiency. The process of binding coumarin molecule on BSA was a spontaneous molecular interaction procedure in which entropy was increased. CONCLUSION The interaction between coumarins and BSA is stronger and the main binding force is hydrophobic interactions whereas both hydrophobic force and dipole-dipole force coexisted in 6-Methylesculetin-BSA.
关键词
茵陈 /
香豆素 /
牛血清白蛋白 /
荧光法
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Key words
Artemisia capillaries Thumb. /
coumarin /
bovine serum albumin /
fluorescence spectroscopy
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参考文献
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脚注
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基金
教育部跨世纪人才基金项目(教技函[2002]48号)
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