Objective: To screen out the active components from Corydlis Decumbentis Rhizoma (CDR) and investigate their inhibitory effect on β1-AR. Method: A high expression β1 adrenergic receptor/cell membrane chromatography-offline-ultra-performance liquid chromatography/mass spectrometry method (β1-AR/CMC-Offline-UPLC/MS method) was used to scan and identify the effective components from extracts of CDR. β1-AR/CHO-S cells were cultured in metoprolol (10 μmol· L-1) and active components of jatrorrhizine (JAT) (1

5 μmol· L-1) for 24 h. Then

the cells were injured in DMEM containing ISO (50 μmol· L-1) for 10 h. the effect of the active components on β1-AR downstream factors cAMP and PKA was determined by ELISA kits to evaluate their inhibitory effect on β1-AR. Result: JAT was the active component of CDR and the experiment in vivo showed that in JAT and MT groups

concentrations of cAMP and PKA were lower than that in the ISO group (P<0.01). Conclusion: JAT was successfully isolated and identified by the β1-AR/CMC-offline-UPLC/MS system from CDR and had an inhibitory effect on β1-AR. The β1-AR/CMC-Offline-UPLC/MS method can be used to screen out active components with clear action targets in a quick and effective manner. The screening results were found to be significantly consistent with its pharmacological effect.