Investigations were performed on the determination of the main components in Berchemia lineata (L.) DC. (BL) and its metabolism with human liver microsomes (HLM). A total of 35 compounds were detected in BL extracts and 25 of them including 6 naphthopyrones, 10 flavonoids, 2 phenolic acids, 2 phenols, 4 fatty acids and 1 quinone were unambiguously or tentatively identified by UPLC-QTOF-MS/MS. Among them, naphthopyrones were first identified in BL extracts and labelled in chromatography. In addition, the weak inhibitory effects of BL extracts (IC50＝149.25 μg/mL) and rubrofusarin-6-O-α-L-rhamnosyl-(1-6)-O-β-D-glu-copyranside (the main component of BL extracts, M0; IC50＝82.14 μM) on CYP3A4 were also proved using testosterone as specific probe drug. The main metabolic pathway of M0 by HLM was hydroxylation in its aglycone, the metabolite was tentatively identified as 10-hydroxy-rubrofusarin-6-O-α-L-rhamnosyl-(1-6)-O-β-D-glucopyranside. Components characterisation and the metabolism with HLM could help the further development and application of BL.
Keywords: Berchemia lineata (L.) DC.; CYP450; UPLC-QTOF-MS/MS; metabolism; structural identification.