A high expression β1 AR/cell membrane chromatography method based on a target receptor to screen active ingredients from traditional Chinese medicine.

TitleA high expression β1 AR/cell membrane chromatography method based on a target receptor to screen active ingredients from traditional Chinese medicine.
Publication TypeJournal Article
Year of Publication2013
AuthorsYue Y, Xue H, Wang X, Yang Q, Song Y, Li X
JournalJournal of separation science
Date Published2013 Nov 22
Abstract

β-Adrenergic receptors (are important targets for drug discovery. We have developed a new β1 -adrenergic receptor/cell membrane chromatography (β1 AR/CMC) with offline ultra-performance liquid chromatography (UPLC) and MS method for screening active ingredients from traditional Chinese medicines. In this study, CHO-S cells with high β1 AR expression levels were established and used to prepare a cell membrane stationary phase in a β1 AR/CMC model. 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 β1 AR in similar manner of metoprolol as a control drug. In addition, the biological effects of active component were also investigated in order to search for a new type of β1 AR antagonist. It will be a useful method for drug discovery as a leading compound resource. This article is protected by copyright. All rights reserved.

DOI10.5681/apb.2013.077
Alternate JournalJ Sep Sci