高等学校化学学报 ›› 2006, Vol. 27 ›› Issue (1): 150-152.

• 研究简报 • 上一篇    下一篇

香豆素类中药有效成分与牛血清白蛋白结合的构效关系

刘雪锋, 夏咏梅, 曹玉华, 方云, 邹珠燕, 毛本刚, 丁漪   

  1. 江南大学化学与材料工程学院, 无锡   214036
  • 收稿日期:2005-02-03 出版日期:2006-01-10 发布日期:2006-01-10
  • 通讯作者: 方云(1957年出生), 男, 教授, 博士生导师, 从事胶体与界面科学和酶催化研究. E-mail: yunfang@126.com
  • 基金资助:

    江南大学自然科学预研基金(批准号: 2004LYY019)资助.

Structure-performance Relationship of some Chinese Herb Components Containing Structural Unit of Coumarin During Binding to Bovine Serum Albumin

 LIU Xue-Feng, XIA Yong-Mei, CAO Yu-Hua, FANG Yun, ZOU Zhu-Yan, MAO Ben-Gang, DING Yi   

  1. School of Chemical and Material Engineering, Southern Yangtze University, Wuxi 214036, China
  • Received:2005-02-03 Online:2006-01-10 Published:2006-01-10
  • Contact: FANG Yun,E-mail: yunfang@126.com

摘要:

本文主要用荧光光谱(FS)、 紫外光谱(UV)从药物分子结构角度研究五种香豆素类中药有效成分CⅠ~CⅤ与牛血清白蛋白(Bovine Serum Albumin, BSA)结合时的构效关系.

关键词: 构效关系; 中药; 香豆素; 牛血清白蛋白; 荧光光谱

Abstract:

The interaction between bovine serum albumin(BSA) and five active components of Chinese Herb CⅠ-CⅤ containing structural unit of coumarin was investigated by ultraviolet(UV) and fluorescence spectroscopy(FS). The intrinsic fluorescence of BSA was quenched by pharmaceuticals via forming pharmaceutical-BSA complexes. The quenching mechanism is mainly a combination of static quenching with  nonradiative energy transfer. The parameters of pharmaceutical-BSA binding process, such as statistic quenching constant KP, the apparent association constant KA, the value of binding site n, the efficiency of energy transfer E, the spatial distance r  and ΔG were obtained. The above parameters disclose the structural-performance relationship of pharmaceutical-BSA interaction as follows. The process of pharmaceutical-BSA binding is promoted strongly by both 4-methyl and 6-hydroxyl in coumarin molecule, but the latter must endure simultaneously some adverse effects caused by increment of molecular polarity and stereo hindrance. Decreasing the polarity of 7-substituent group and increasing the volume of substituting group destroys the pharmaceutical-BSA binding, and the effect is almost totally opposite to that of 6-hydroxyl.

Key words: Structural-performance relationship; Chinese Herb; Coumarin; Bovine serum albumin; Fluorescence spectroscopy

中图分类号: