Regiospecific methylation of a dietary flavonoid scaffold selectively enhances IL-1β production following toll-like receptor 2 Stimulation in THP-1 monocytes

Abstract

Background: Plant natural products typically contain regiospecific modifications in their side chains that lead to different bioactivities. Results: Only 3-O-methylated flavonols enhance IL-1β production in THP-1 cells costimulated with the Toll-like receptor 2 agonist Pam3CSK4. Conclusion: Regiospecific methylation of flavonols controls their bioactivity as immunomodulators. Significance: This study provides a platform to explore the use of regiospecific-modified natural products as novel immunomodulators. © 2013 by The American Society for Biochemistry and Molecular Biology, Inc.