Journal of pharmaceutical and biomedical analysis · 2015
Screening β1AR inhibitors by cell membrane chromatography and offline UPLC/MS method for protecting myocardial ischemia.
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Yue Yuan, Dou Lili, Wang Xin, Xue Hui, Song Yanhong, Li Xiaoni
Аннотация
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.
Предметные рубрики MeSH
Adrenergic beta-1 Receptor AntagonistsAnimalsApoptosisBerberineBinding, CompetitiveCHO CellsCell MembraneChromatography, High Pressure LiquidCoptisCricetulusDisease Models, AnimalMaleMalondialdehydeMass SpectrometryMetoprololMyocardial InfarctionMyocardiumMyocytes, CardiacPhytotherapyPlant ExtractsPlants, MedicinalRats, WistarReceptors, Adrenergic, beta-1Superoxide DismutaseTransfection