High-expression β_1 adrenergic receptor/cell membrane chromatography method based on a target receptor to screen active ingredients from traditional Chinese medicines

摘要

β-Adrenergic receptors are important targets for drug discovery. We have developed a new β_1-adrenergic receptor cell membrane chromatography (β_1AR-CMC) with offline ultraperformance LC (UPLC) and MS method for screening active ingredients from traditional Chinesemedicines. In this study, Chinese hamster ovary-S cells with high β_1AR expression levels were established and used to prepare a cell membrane stationary phase in a β_1ARCMCmodel. The retention fractions were separated and identified by the UPLC-MS system. The screening results found that isoimperatorin from Rhizoma et Radix Notopterygii was the targeted component that could act on β_1AR in similarmanner ofmetoprolol as a control drug. In addition, the biological effects of active component were also investigated in order to search for a new type of β_1AR antagonist. It will be a useful method for drug discovery as a leading compound resource.