亲和色谱法研究β_2-肾上腺素受体与盐酸巴马汀和盐酸药根碱的相互作用  

Investigation on the Interaction of Palmatine and Jatrorrhizine with β_2-Adrenoceptor by High-performance Affinity Chromatography

作　　者：何媛 姚苏洋[1] 郑晓晖[2] 卫引茂[1] 

机构地区：[1]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 [2]西北大学生命科学学院,西安710069

出　　处：《化学学报》2012年第2期121-127,共7页Acta Chimica Sinica

基　　金：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);国家基础科学人才培养基金(No.J0830417)资助项目~~

摘　　要：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.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 chromatog-raphy.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 as-sociation 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.

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 

分 类 号：R96[医药卫生—药理学]