Cell membrane chromatography coupled with UHPLC–ESI–MS/MS method to screen target components from Peucedanum praeruptorum Dunn acting on α1A adrenergic receptor

• New screening method based CMC coupled UHPLC–ESI–MS/MS system was established.
• The coupled system can be served as a screening tool for components with α1A–AR activity.
• PA, PB, and PC were screened from Peucedanum praeruptorum Dunn by coupled system.
• TH, PA, PB, and PC could relax the prostate strips pre-contracted by noradrenaline.

Peucedanum praeruptorum Dunn (BaiHuaQianHu in Chinese) is a traditional Chinese medicine that has a long history of use in China. In this study, HEK 293 α1A adrenergic cell membrane chromatography was coupled with UHPLC-ESI-MS/MS and successfully used to identify active components from Peucedanum praeruptorum Dunn. Paeruptorin A, paeruptorin B, and paeruptorin C were identified with α1A adrenergic receptor activity. Pharmacological assays showed that tamsulosin hydrochloride, paeruptorin A, paeruptorin B, and paeruptorin C in concentrations of 1 × 10−8 to 1 × 10−4 mol/mL could relax prostate strips pre-contracted with adrenalin in a concentration dependent manner. Therefore, the HEK293 α1A cell membrane chromatography coupled UHPLC–ESI–MS/MS system may be a potentially useful drug discovery method for screening for medicinal herbal components with α1A adrenergic receptor inhibitory activity.