Hepatoprotective effect of tiliroside and characterization of its metabolites in human hepatocytes by ultra-high performance liquid chromatography-high resolution mass spectrometry

Abstract

Tiliroside, as a dietary flavonoid, has great potential in preventing or treating non-alcoholic fatty liver disease (NAFLD). However, research on tiliroside metabolism remains unclear, limiting its further utilization in healthcare. Herein, we explored the hepatoprotective effect of tiliroside and performed an UHPLC-Q-Exactive Orbitrap/MS-based set of experiments to identify metabolites and metabolic pathways of tiliroside in human hepatocytes. Results showed that tiliroside can exert antioxidant activity to protect against palmitic acid (PA)-induced oxidative injury in hepatocytes. Moreover, tiliroside was found to be considerably transformed through metabolism in human hepatocytes based on full MS and MS/MS analysis. Fifteen metabolites derived from the glucuronidation, sulfation, hydrolysis, and oxidation of tiliroside were identified. Glucuronidation and sulfation played key roles in tiliroside metabolism, accounting for approximately 32% and 20% of metabolism after 240 min incubation, respectively. The findings could provide a scientific basis for a more rational and effective application of tiliroside in healthcare.

Keywords

• Tiliroside
• Hepatoprotective
• Metabolism
• Human hepatocytes
• UHPLC-Q-Exactive Orbitrap/MS