受体毛细管电泳对赤芍中扩血管活性成分的筛选研究

项目名称： 受体毛细管电泳对赤芍中扩血管活性成分的筛选研究

项目编号： No.81202492

项目类型： 青年科学基金项目

立项/批准年度： 2013

项目学科： 药物学、药理学

项目作者： 刘春叶

作者单位： 西安医学院

项目金额： 23万元

中文摘要： 中药活性成分的筛选是实现中药现代化的关键。根据蛋白与药物相互作用原理，毛细管电泳为建立中药活性成分筛选新方法提供了可能。本研究以心血管疾病类药物靶点beta2-肾上腺素受体（beta2-adrenceptor，beta2-AR）作为靶标蛋白，将其以共价键定向键合在毛细管内表面，以提高受体的稳定性和生物活性。阐明受体的定向固定化技术在研究药物与受体相互作用中的先进性。采用结合常数、结合位点等多参数表征受体对药物的选择性相互作用，以beta2-AR阳性药为例验证定向键合受体毛细管电泳在药物筛选中的特异性。以赤芍为研究对象，对其扩血管活性成分进行筛选，最终建立以受体毛细管电泳为核心的中药抗心血管疾病活性成分筛选新方法，并结合在线质谱联用技术对活性成分进行结构鉴定。该项目的实施，可为中药活性成分的毛细管电泳高通量筛选研究提供新思路，为建立基于受体毛细管电泳为核心的中药活性成分筛选研究提供新方法。

中文关键词： 毛细管电泳；药物筛选；中药；受体；

英文摘要： Screening of the active components is very important for modernization of traditional Chinese medicine. Relied on the interaction between protein and drugs, novel screening methods of active ingredients from traditional Chinese medicine could be established based on capillary electrophoresis (CE). CE has its inherent characteristics such as high separation selectivity, small sample size requirement, high speed of analysis, high efficiency, and excellent mass sensitivity. One of the attractive main features of capillary electrophoresis is the capability to simultaneously separate a wide variety of analytes which is benefit to analysis of the complicated system of traditional Chinese medicine. Drug target of cardiovascular disease, beta2 - adrenergic receptor (beta2-AR), was chosen as the target protein in the work. First, beta2-AR was oriented bonded to the inner surface of capillary by covalent bond to improve its stability and biological activity. Second, the capillary containing oriented immobilized selectors was used as an affinity ligand to capture specific analyte, i.e., to screen active components of cardiovascular diseases from traditional Chinese medicine by capillary electrophoresis. The advances of oriented immobilization technology of receptor in interactions study between drug and receptor were evalu

英文关键词： Capillary electrophoresis；Drug screening；Traditional Chinese medicine；Receptor；