Screening β1AR inhibitors by cell membrane chromatography and offline UPLC/MS method for protecting myocardial ischemia.
A high expression β1AR/cell membrane chromatography (β1AR-CMC) and offline UPLC/MS method has been developed for screening active ingredients from Coptis chinensis. In this study, the fractions retained by CMC column were separated and identified by UPLC/MS system. Using metoprolol as a positive control drug, coptisine from C. chinensis was identified as the active component which could inhibit β1AR. Compared with the control group: coptisine could attenuate the infarct size and release malondialdehyde (MDA) while increasing superoxide dismutase (SOD) activity, suggesting a role in reducing myocardial injury. In vitro, coptisine could decrease apoptosis, showing their protective effects upon cardiomyocytes. This β1AR-CMC-offline-UPLC/MS method can be applied for screening active components acting on β1AR from traditional Chinese medicines.
College of Pharmacy, Shanxi Medical University, No 56 Xinjian South Road, Taiyuan 030001, China.
Yuan
Y
Yue
College of Pharmacy, Shanxi Medical University, No 56 Xinjian South Road, Taiyuan 030001, China.
Lili
L
Dou
College of Pharmacy, Shanxi Medical University, No 56 Xinjian South Road, Taiyuan 030001, China.
Xin
X
Wang
College of Pharmacy, Shanxi Medical University, No 56 Xinjian South Road, Taiyuan 030001, China.
Hui
H
Xue
Shanxi Institute of Feed, Supervision and Veterinary Drug, Taiyuan 030001, China.
Yanhong
Y
Song
College of Pharmacy, Shanxi Medical University, No 56 Xinjian South Road, Taiyuan 030001, China. Electronic address: ninili1235@163.com.
Xiaoni
X
Li
D058671:Adrenergic beta-1 Receptor Antagonists / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D001599:Berberine / Q000031:analogs & derivatives* / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology; D001667:Binding, Competitive; D016466:CHO Cells; D002462:Cell Membrane / Q000187:drug effects* / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D039323:Coptis / Q000737:chemistry; D003412:Cricetulus; D004195:Disease Models, Animal; D008297:Male; D008315:Malondialdehyde / Q000378:metabolism; D013058:Mass Spectrometry; D008790:Metoprolol / Q000378:metabolism; D009203:Myocardial Infarction / Q000378:metabolism / Q000473:pathology / Q000517:prevention & control; D009206:Myocardium / Q000378:metabolism / Q000473:pathology; D032383:Myocytes, Cardiac / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D008517:Phytotherapy; D010936:Plant Extracts / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D010946:Plants, Medicinal; D017208:Rats, Wistar; D018342:Receptors, Adrenergic, beta-1 / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism; D013482:Superoxide Dismutase / Q000378:metabolism; D014162:Transfection
C547789:Adrb1 protein, rat; D058671:Adrenergic beta-1 Receptor Antagonists; D010936:Plant Extracts; D018342:Receptors, Adrenergic, beta-1; C034384:coptisine; D001599:Berberine; D008315:Malondialdehyde; D013482:Superoxide Dismutase; D008790:Metoprolol
Cell membrane chromatography; Coptis chinensis; Coptisine; UPLC/MS; β1-Adrenergic receptors