Flavone deglycosylation increases their anti-inflammatory activity and absorption

Gregory Hostetler, Ken Riedl, Horacio Cardenas, Mayra Diosa-Toro, Daniel Arango, Steven Schwartz, Andrea I. Doseff*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

67 Scopus citations


Scope: Flavones have reported anti-inflammatory activities, but the ability of flavone-rich foods to reduce inflammation is unclear. Here, we report the effect of flavone glycosylation in the regulation of inflammatory mediators in vitro and the absorption of dietary flavones in vivo. Methods and results: The anti-inflammatory activities of celery extracts, some rich in flavone aglycones and others rich in flavone glycosides, were tested on the inflammatory mediators tumor necrosis factor α (TNF-α) and nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) in lipopolysaccharide-stimulated macrophages. Pure flavone aglycones and aglycone-rich extracts effectively reduced TNF-α production and inhibited the transcriptional activity of NF-κB, while glycoside-rich extracts showed no significant effects. Deglycosylation of flavones increased cellular uptake and cytoplasmic localization as shown by high-performance liquid chromatography (HPLC) and microscopy using the flavonoid fluorescent dye diphenylboric acid 2-aminoethyl ester (DPBA). Celery diets with different glycoside or aglycone contents were formulated and absorption was evaluated in mice fed with 5 or 10% celery diets. Relative absorption in vivo was significantly higher in mice fed with aglycone-rich diets as determined by HPLC-MS/MS (where MS/MS is tandem mass spectrometry). Conclusion: These results demonstrate that deglycosylation increases absorption of dietary flavones in vivo and modulates inflammation by reducing TNF-α and NF-κB, suggesting the potential use of functional foods rich in flavones for the treatment and prevention of inflammatory diseases.

Original languageEnglish (US)
Pages (from-to)558-569
Number of pages12
JournalMolecular Nutrition and Food Research
Issue number4
StatePublished - Apr 2012


  • Apigenin
  • Bioactive food components
  • Flavones
  • Inflammation
  • Macrophages

ASJC Scopus subject areas

  • Biotechnology
  • Food Science


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