Human cytochrome P450 enzymes catalyze oxidative metabolism of pectolinarigenin to generate a more active Nrf2 agonist.

ABSTRACT:

Objective

To characterize the oxidative metabolic pathway(s) of pectolinarigenin (PEC) and reveal the effect of PEC oxidative metabolism on its biological activities including peroxisome proliferator-activated receptors (PPAR) and nuclear factor erythroid 2-related factor 2 (Nrf2) agonist effects, as well as the anti-oxidative and hepatoprotective activities.

Methods

The oxidative metabolites of PEC were identified by liquid chromatography-time of flight-mass spectrometry (LC-TOF-MS/MS). The key enzymes involved in oxidative metabolism of PEC were assigned by P450 reaction phenotyping assays and enzymatic kinetics assays. Luciferase reporter assays and western blotting analysis were used to evaluate the Nrf2 and PPAR agonist effects of PEC and its oxidative metabolites. The

SUBMITTER: Liu P 

PROVIDER: S-EPMC12702440 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature