Quercetin inhibits IL-1β-induced inflammation, hyaluronan production and adipogenesis in orbital fibroblasts from Graves' orbitopathy

PLoS One. 2011;6(10):e26261. doi: 10.1371/journal.pone.0026261. Epub 2011 Oct 19.

Abstract

Management of Graves' orbitopathy (GO) is challenging, as no reliable, specific, and safe medical therapeutic agents have yet been developed. We investigated the effect of quercetin in primary cultured orbital fibroblasts from GO, targeting pathways of inflammation, aberrant accumulation of extracellular matrix macromolecules, and adipose tissue expansion. Quercetin significantly attenuated intercellular adhesion molecule-1 (ICAM-1), interleukin (IL) -6, IL-8, and cyclooxygenase (COX) -2 mRNA expression, and inhibited IL-1β-induced increases in ICAM-1, IL-6, and IL-8 mRNA. Increased hyaluronan production induced by IL-1β or tumor necrosis factor-α was suppressed by quercetin in a dose- and time-dependent manner. Treatment with noncytotoxic doses of quercetin inhibited accumulation of intracytoplasmic lipid droplets and resulted in a dose-dependent decrease in expression of peroxisome proliferator-activated receptor γ, CCAAT/enhancer-binding protein (C/EBP) α, and C/EBPβ proteins. In conclusion, inhibition of inflammation, hyaluronan production, and adipogenesis by the natural plant product quercetin in vitro provides the basis for further study of its potential use in the treatment of GO.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adipogenesis / drug effects*
  • Graves Disease / metabolism*
  • Graves Disease / pathology
  • Humans
  • Hyaluronic Acid / biosynthesis*
  • Inflammation / prevention & control*
  • Interleukin-1beta / antagonists & inhibitors*
  • Interleukin-1beta / genetics
  • Interleukin-1beta / physiology
  • NF-kappa B / metabolism
  • Orbit / cytology
  • Orbit / drug effects*
  • Quercetin / pharmacology*
  • RNA, Messenger / genetics
  • Transcription Factors / metabolism

Substances

  • Interleukin-1beta
  • NF-kappa B
  • RNA, Messenger
  • Transcription Factors
  • Hyaluronic Acid
  • Quercetin