化学学报 ›› 2011, Vol. 69 ›› Issue (02): 247-251. 上一篇    

研究简报

原小檗碱类生物碱与抗凋亡蛋白Bcl-2相互作用的光谱法研究

张艳霞1,2,张秀凤1,唐亚林*,1,向俊锋1,田明月1,3   

  1. (1中国科学院化学研究所 分子动态与稳态国家重点实验室 北京 100190)
    (2中国科学院研究生院 北京 100049)
    (3北京师范大学生命科学学院 北京 100875)
  • 投稿日期:2010-06-02 修回日期:2010-08-18 发布日期:2010-09-27
  • 通讯作者: 唐亚林 E-mail:tangyl@iccas.ac.cn

Studies of the Interactions between Three Protoberberine Alkaloids and Bcl-2 by Fluorescence Spectroscopy

Zhang Yanxia1,2 Zhang Xiufeng1 Tang Yalin*,1 Xiang Junfeng1 Tian Mingyue1,3   

  1. (1 State Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190)
    (2 Graduate University of Chinese Academy of Sciences, Beijing 100049)
    (3 College of Life Science, Beijing Normal University, Beijing 100875)
  • Received:2010-06-02 Revised:2010-08-18 Published:2010-09-27

应用荧光光谱法研究三种原小檗碱类生物碱: 盐酸小檗碱(Berberine hydrochloride)、药根碱(Jatrorrhizine)和盐酸巴马汀(Palmatine hydrochloride)与抗凋亡蛋白Bcl-2之间的相互作用, 探讨了这三种生物碱对Bcl-2蛋白的荧光淬灭机理, 分别测定其结合常数和结合位点数. 实验结果表明, 盐酸小檗碱、药根碱和盐酸巴马汀等三种原小檗碱类生物碱都能够使Bcl-2蛋白的内源性荧光发生淬灭, 其荧光淬灭过程是静态淬灭过程. 通过比较三种生物碱与Bcl-2蛋白的相互作用, 发现随着分子柔性增强, 其与Bcl-2蛋白的结合能力增强. 因此, 增强生物碱的分子柔性有可能增强其靶向Bcl-2蛋白的能力.

关键词: 盐酸小檗碱, 药根碱, 盐酸巴马汀, Bcl-2, 荧光光谱

The interactions between Bcl-2 and three protoberberine alkaloids: berberine hydrochloride, jatrorrhizine and palmatine hydrochloride were studied by fluorescence spectroscopy. The binding constants and the number of binding sites were measured, respectively, and the quenching mechanism was proposed. The results indicated that the protoberberine alkaloids could decrease the intrinsic fluorescence of Bcl-2 mainly through static quenching. By comparing the structures of the three alkaloids, it was found that the binding affinity to Bcl-2 protein increased with molecular flexibility of the alkaloids.

Key words: berberine hydrochloride, jatrorrhizine, palmatine hydrochloride, Bcl-2, fluorescence spectroscopy