Flavonoid biotransformation: pharmacokinetic and pharmacodynamic effects of flavonoid glycosylation

Flavonoid biotransformation: pharmacokinetic and pharmacodynamic effects of flavonoid glycosylation.

Purpose: Flavonoids are a class of polyphenolic compounds found in nature, specifically in fruits, vegetables, nuts, tea, and wine. The diversity of metabolism among flavonoid compounds makes this a germane topic for pharmacy. The elucidation of metabolic pathways and corresponding activity of metabolites is crucial towards the rational incorporation of these compounds in therapy. One primary aim of this review is to use structure activity relationship information pertaining to flavonoids to obtain a more precise understanding of the activity and metabolism of flavonoids. The pharmacokinetic and pharmacodynamic effects of flavonoid in vivo glycosylation will be addressed.

Methods: Information pertaining to flavonoid biotransformation will be gathered from PubMed, UK PubMed Central, and American Chemical Society databases. PubMed will be searched with structured MeSH search terms “flavonoids,” “biotransformation,” and “glycosylation.” Additionally, the tertiary reference Natural Medicines Comprehensive Database will be utilized.

Results: Glycosylation generally decreases flavonoid lipophilicity, has variable effects on antioxidant activity, and variable effects on bioavailability. In vivo sites of glycosylation and deglycosylation were identified for specific flavonoid dietary supplements, and the corresponding implications on extent of absorption based on metabolic outcome were noted.

Conclusion: Flavonoids demonstrate a diversity of biotransformation routes which affect their bioavailability and subsequent clinical utility. This review article consolidated recent research into the pharmacokinetic and pharmacodynamic properties of various flavonoids. An expanded clinical utilization of flavonoids is predicated on further research into how the glycosylation of flavonoids affects function.