title: High-expression β(1) adrenergic receptor/cell membrane chromatography method based on a target receptor to screen active ingredients from traditional Chinese medicines.
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 LC (UPLC) and MS method for screening active ingredients from traditional Chinese medicines. In this study, Chinese hamster ovary-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.
authors.affiliation: College of Pharmacy, Shanxi Medical University, Taiyuan, China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Yue
authors.forename: Hui
authors.initials: H
authors.lastname: Xue
authors.forename: Xin
authors.initials: X
authors.lastname: Wang
authors.forename: Qian
authors.initials: Q
authors.lastname: Yang
authors.forename: Yanhong
authors.initials: Y
authors.lastname: Song
authors.forename: Xiaoni
authors.initials: X
authors.lastname: Li
mesh_terms: D058665:Adrenergic beta-1 Receptor Agonists / Q000737:chemistry*; D000818:Animals; D016466:CHO Cells; D002462:Cell Membrane / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism; D002845:Chromatography / Q000295:instrumentation / Q000379:methods*; D006224:Cricetinae; D003412:Cricetulus; D004353:Drug Evaluation, Preclinical / Q000295:instrumentation / Q000379:methods*; D004365:Drugs, Chinese Herbal / Q000737:chemistry*; D008024:Ligands; D011485:Protein Binding; D018342:Receptors, Adrenergic, beta-1 / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D027343:Rhizome / Q000737:chemistry
chemical_list: D058665:Adrenergic beta-1 Receptor Agonists; D004365:Drugs, Chinese Herbal; D008024:Ligands; D018342:Receptors, Adrenergic, beta-1
keywords: Cell membrane chromatography; Isoimperatorin; Rhizoma et Radix Notopterygii; β1-Adrenergic receptor