Since 1996,a new type of biological affinity chromatography named cell membrane chromatography(CMC)has been introduced by Langchong He and his colleagues.Nowadays,CMC has been demonstrated as an effective method to screen active compounds from complex systems[1].With the use of cell lines with high expression of specific receptors,CMC can be used to recognize active components acting on these receptor[2,3].Traditional Chinese medicine(TCM)has been used in China for thousands of years.An increasing number of people have been giving their attention to TCM for the treatment of benign prostatic hyperplasia(BPH),which is a common disease in elderly men,and the main symptoms including frequency,urgency,and nocturia[4].In this study,α1A/CMC column was constructed with high expressed α1A adrenoreceptor HEK293 cell lines.The suitability and reliability of α1A/CMC column were investigated by positive and negative control drugs.Then α1A/CMC column was combined with HPLC/MS system via a ten port two position switch valve.Positive control drug was used to investigate the suitability of α1A/CMC online HPLC/MS system.Results shown the specificity,selectivity,reproducibility,and the lifetime of the α1A/CMC column,the suitability of the two dimensional liquid chromatography system were all met the requirement of the experiment.Then the two dimensional liquid chromatography was used to screen,analyze,and identify active compounds acting on α1A from Fructus piperis and Caulis spatholobi.The screening results showed that piperine and formononetin were the targeted component which could act on α1A specificity.The results of the competitive binding assay and molecular docking assay demonstrated that the binding region of piperine was the same as for tamsulosin.The pharmacological effect for treatment of BPH needs further study.