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化学学报
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化学学报 ›› 2012, Vol. 70 ›› Issue (02): 121-127.DOI: 10.6023/A1109141 上一篇    下一篇

研究论文

亲和色谱法研究β2-肾上腺素受体与盐酸巴马汀和盐酸药根碱的相互作用

何媛a, 姚苏洋a, 郑晓晖b, 卫引茂a   

  1. a 西北大学合成与天然功能分子化学教育部重点实验室 化学与材料科学学院 西安 710069;
    b 西北大学生命科学学院 西安 710069
  • 投稿日期:2011-09-14 修回日期:2011-11-20 发布日期:2012-02-25
  • 通讯作者: 卫引茂 E-mail:ymwei@nwu.edu.cn
  • 基金资助:

    国家自然科学基金(Nos.20975080, 20875074);教育部新世纪优秀人才支持计划(No.NCET-08-0892)和国家基础科学人才培养基金(No.J0830417)资助项目.

Investigation on the Interaction of Palmatine and Jatrorrhizine with β2-Adrenoceptor by High-performance Affinity Chromatography

He Yuana, Yao Suyanga, Zheng Xiaohuib, Wei Yinmaoa   

  1. a Key Laboratory of Synthetic and Natural Function Molecule Chemistry of Ministry of Education, College of Chemistry & Material Science, Northwest University, Xi'an 710069;
    b College of Life Sciences, Northwest University, Xi'an 710069
  • Received:2011-09-14 Revised:2011-11-20 Published:2012-02-25
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos.20975080 and 20875074);Program for New Century Excellent Talents in University (No.NCET-08-0892) and Chinese National Science Foundation for Talent Training (No.J0830417).

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采用亲和色谱法研究了β2-肾上腺素受体(β2-AR)与中药活性小分子盐酸巴马汀(Pa)和盐酸药根碱(Ja)的相互作用. 前沿色谱法说明Pa 与β2-AR 之间存在一类结合位点, Ja 与β2-AR 之间存在两类结合位点. 在pH 7.4, 25 ℃时, 用竞争洗脱法测得了Pa 与β2-AR 的结合常数为2.93×104 L·mol-1, 结合位点浓度为1.13×10-4 mol·L-1, Ja 在β2-AR 低、高亲和力位点上的结合常数分别为1.93×104 和1.56×105 L·mol-1, 对应的结合位点浓度分别为1.25×10-4 mol·L-1 和1.00×10-5 mol·L-1, 两类结合位点数的比值为93:7, 且Pa 和Ja 在低亲和力位点上存在竞争作用. 热力学研究表明, 静电力是这两种药物与β2-AR 之间作用的主要驱动力.

关键词: 小分子-生物大分子相互作用, 亲和色谱, β2-肾上腺素受体, 盐酸巴马汀, 盐酸药根碱

The interaction of two bioactive components of Chinese traditional herb, palmatine (Pa) and jatrorrhizine (Ja), with β2-adrenoceptor (β2-AR) was investigated by high-performance affinity chromatography. The binding isotherms of two drugs were determined by frontal analysis, and the results showed that Pa had one kind of binding site, and Ja had two kinds of binding sites on β2-AR molecular. The association constants and binding sites were determined by zonal elution, at pH 7.4 and 25 ℃. The association constant for Pa was 2.93×104 L·mol-1, and the concentration of the binding sites was 1.13×10-4 mol·L-1. The association constants for Ja at the low and high binding sites were 1.93×104 and 1.56×105 L·mol-1, and the concentration of the two binding sites were 1.25×10-4 and 1.00×10-5 mol·L-1, respectively. The ratio of two binding sites was 93:7. It was further proved that Pa and Ja competed the low binding site on β2-AR. Thermodynamic results indicated that the interaction between the two drugs and β2-AR was mainly drived by electrostatic force.

Key words: small molecular-biopolymer interaction, β2-adrenoceptor, palmatine, jatrorrhizine, high-perfor-mance affinity chromatography