Licochalcone A inhibits the formation and bone resorptive activity of osteoclasts

Cell Biol Int. 2008 Sep;32(9):1064-72. doi: 10.1016/j.cellbi.2008.04.017. Epub 2008 May 2.

Abstract

Licochalcone A on the formation and bone resorptive activity of osteoclasts up to 5muM significantly inhibited the receptor activator of nuclear factor kappaB (NF-kappaB) ligand (RANKL)-induced activity of tartrate-resistant acid phosphatase (TRAP) activity and formation of osteoclasts without any effect on cell viability. Interestingly, licochalcone A was shown to inhibit the RANKL-induced activation of extracellular signal-regulated kinase, translocation of NF-kappaB into nucleus and mRNA expression of Fra-2. Licochalcone A also inhibited the bone resorptive activity of mature osteoclasts and the expression of bone resorption-related genes. Inhibitory effects of licochalcone A on the formation and bone resorptive activity of mouse bone marrow macrophage-derived osteoclasts were also observed. In conclusion, licochalcone A has the potential to inhibit the formation of osteoclasts as well as the bone resorptive activity of mature osteoclasts.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Bone Resorption / pathology*
  • Cell Survival / drug effects
  • Cells, Cultured
  • Chalcones / chemistry
  • Chalcones / pharmacology*
  • Enzyme Activation / drug effects
  • Gene Expression Regulation / drug effects
  • I-kappa B Proteins / metabolism
  • Macrophage Colony-Stimulating Factor / pharmacology
  • Mice
  • Mice, Inbred BALB C
  • Mitogen-Activated Protein Kinases / metabolism
  • NF-KappaB Inhibitor alpha
  • NFATC Transcription Factors / genetics
  • NFATC Transcription Factors / metabolism
  • Osteoclasts / drug effects*
  • Osteoclasts / enzymology
  • Osteoclasts / pathology*
  • RANK Ligand / pharmacology
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Transcription Factor AP-1 / genetics
  • Transcription Factor AP-1 / metabolism
  • Transcription Factor RelA / metabolism

Substances

  • Chalcones
  • I-kappa B Proteins
  • NFATC Transcription Factors
  • Nfkbia protein, mouse
  • RANK Ligand
  • RNA, Messenger
  • Transcription Factor AP-1
  • Transcription Factor RelA
  • NF-KappaB Inhibitor alpha
  • Macrophage Colony-Stimulating Factor
  • Mitogen-Activated Protein Kinases
  • licochalcone A