ArticleChinese herbal medicines2025
Human cytochrome P450 enzymes catalyze oxidative metabolism of pectolinarigenin to generate a more active Nrf2 agonist.
Article in Chinese herbal medicines, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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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 intracellular levels of total reactive oxygen species (ROS), mitochondrial membrane potential (MMP), lactate dehydrogenase (LDH) and glutathione (GSH) in acetaminophen (APAP)-challenged hepatocytes were also tested. Results: PEC could be readily metabolized to form two Conclusion: CYPs catalyze PEC-4'-
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