Metabolic profiling of triptophenolide in rat plasma, urine, bile and faeces after intragastric administration

Triptophenolide, a major diterpenoid extracted from <i>Tripterygium wilfordii</i> Hook. f., has been reported to possess significant anti-tumour, anti-androgen and anti-inflammatory activities. However, the metabolic fate of triptophenolide remains unknown. Therefore, this study focused on the metabolic profiling of triptophenolide in rat plasma, urine, bile and faeces following intragastric administration. An ultraperformance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry with combination of extracted ion chromatogram strategy based on 71 typical metabolic reactions was established to comprehensively profile the metabolites of triptophenolide. This strategy allowed for the identification of 17 metabolites from the biosamples. Reduction, oxidation, glucuronide conjugation, and hydroxylation were considered as its main metabolic pathways <i>in vivo</i>. The present study will be greatly helpful for the further pharmacological studies on triptophenolide and would provide valuable information for its clinical application.