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
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Bone Resorption / pathology*
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Cell Survival / drug effects
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Cells, Cultured
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Chalcones / chemistry
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Chalcones / pharmacology*
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Enzyme Activation / drug effects
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Gene Expression Regulation / drug effects
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I-kappa B Proteins / metabolism
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Macrophage Colony-Stimulating Factor / pharmacology
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Mice
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Mice, Inbred BALB C
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Mitogen-Activated Protein Kinases / metabolism
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NF-KappaB Inhibitor alpha
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NFATC Transcription Factors / genetics
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NFATC Transcription Factors / metabolism
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Osteoclasts / drug effects*
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Osteoclasts / enzymology
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Osteoclasts / pathology*
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RANK Ligand / pharmacology
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RNA, Messenger / genetics
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RNA, Messenger / metabolism
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Transcription Factor AP-1 / genetics
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Transcription Factor AP-1 / metabolism
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Transcription Factor RelA / metabolism
Substances
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Chalcones
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I-kappa B Proteins
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NFATC Transcription Factors
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Nfkbia protein, mouse
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RANK Ligand
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RNA, Messenger
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Transcription Factor AP-1
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Transcription Factor RelA
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NF-KappaB Inhibitor alpha
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Macrophage Colony-Stimulating Factor
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Mitogen-Activated Protein Kinases
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licochalcone A