P-糖蛋白（P-gp）富含在脂筏区域，选择性调控P-gp的临床意义重大。许多中药具有P-gp 调控活性，但其有效组分的筛选研究尚停留在“先分离再行活性分析”的研究思路。亲和色谱法针对单一靶点筛选中药中的有效成分已取得一定成果。然而，我们在前期以脂筏为固定相的亲和色谱研究中，发现脂筏固定相上存在多个靶蛋白，且筛选出的中药提取物的作用机制正是通过这些靶蛋白介导的信号通路实现的。因此，我们推测脂筏色谱本质上是多靶点的亲和体系。在此基础上，本项目拟构建富含P-gp的新型多靶点脂筏色谱系统，以脂筏固定相上的脂质、蛋白微环境研究为切入点，探讨脂筏微环境对色谱保留行为的影响以及脂筏色谱多靶点的亲和特性。将构建的脂筏色谱用于以P-gp调控为目的的中药活性组分群筛选，讨论具有P-gp抑制作用的活性组分群间的功效关联和相互作用，为发展多靶点亲和色谱技术及其在中药活性组分群筛选和作用机制研究提供新的策略和思路。

P-glycoprotein (P-gp) is enriched in lipid rafts. It is of great significance to selectively regulate P-gp in clinical application. Many Traditional Chinese Medicines (TCMs) had P-gp regulation activity. However, investigations on their active components have been stuck in the research mode of “separation first and activity analysis second”. So far, there have been considerable achievements using monotarget affinity chromatography to separate active ingredients from TCMs. Our previous research which employed lipid rafts as the stationary phase has found that there were multiple target proteins on the lipid raft-based stationary phase. Moreover, the extractions screened by this lipid raft-based stationary phase showed action mechanisms that were achieved by pathways mediated through the same proteins in the lipid rafts. Therefore, lipid raft chromatography is essentially a multitargets affinity system. On this basis, this project will construct a P-gp enriched novel multitarget lipid raft system. With the study on microenvironment of lipids and proteins on the lipid raft-based stationary phase as an entry point, this project aims to explore the influence of this microenvironment on chromatographic retention, and the affinity property of the multitargets lipid raft chromatography, employ this system to sift out active component groups associated with P-gp regulation from TCMs, and analyze the effects and interactions of the active component groups that have inhibitive effects on P-gp. This project will provide new strategies and insights for the development of multitargets affinity chromatography and its application in screening active component groups from TCMs as well as the mechanism research.