RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Identifying the inductive constituents of cytochrome P450 (CYP) enzymes is important in characterizing the safety of ethnopharmacological herbal preparations. AIM OF THE STUDY: This study provides a rapid and accurate method for screening CYP inducers in Shenmai injection (SMI), a traditional Chinese medicine. MATERIALS AND METHODS: We combined a pregnane X receptor (PXR) reporter gene assay and liquid chromatography time-of-flight mass spectrometry (LC-TOF-MS) analysis to screen ethanol and aqueous extracts of SMI for CYP-inducing constituents. RESULTS: The ethanol extract exhibited stronger PXR activity than the aqueous extract. Of the 29 chemical compounds identified, 7 compounds with high relative concentrations in the ethanol extract were further evaluated for PXR activity. The highest activity was exhibited by methyl ophiopogonanone B and ginsenoside F2, indicating that they are CYP inducers. CONCLUSIONS: The identification method applied in this study was rapid and accurate and is suitable for screening CYP inducers in herbal preparations.