Licochalcone A inhibits the formation and bone resorptive activity of osteoclasts.
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.
Laboratory of Chemical Genomics, Korea Research Institute of Chemical Technology, Department of Biology, Chungnam National University, Daejeon 305-764, Republic of Korea.
Soon Nam
SN
Kim
Myung Hee
MH
Kim
Yong Ki
YK
Min
Seong Hwan
SH
Kim
D000818:Animals; D001862:Bone Resorption / Q000473:pathology*; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology*; D004789:Enzyme Activation / Q000187:drug effects; D005786:Gene Expression Regulation / Q000187:drug effects; D020672:I-kappa B Proteins / Q000378:metabolism; D016173:Macrophage Colony-Stimulating Factor / Q000494:pharmacology; D051379:Mice; D008807:Mice, Inbred BALB C; D020928:Mitogen-Activated Protein Kinases / Q000378:metabolism; D000072000:NF-KappaB Inhibitor alpha; D050778:NFATC Transcription Factors / Q000235:genetics / Q000378:metabolism; D010010:Osteoclasts / Q000187:drug effects* / Q000201:enzymology / Q000473:pathology*; D053245:RANK Ligand / Q000494:pharmacology; D012333:RNA, Messenger / Q000235:genetics / Q000378:metabolism; D018808:Transcription Factor AP-1 / Q000235:genetics / Q000378:metabolism; D051996:Transcription Factor RelA / Q000378:metabolism
D047188:Chalcones; D020672:I-kappa B Proteins; D050778:NFATC Transcription Factors; C000606205:Nfkbia protein, mouse; D053245:RANK Ligand; D012333:RNA, Messenger; D018808:Transcription Factor AP-1; D051996:Transcription Factor RelA; D000072000:NF-KappaB Inhibitor alpha; D016173:Macrophage Colony-Stimulating Factor; D020928:Mitogen-Activated Protein Kinases; C070840:licochalcone A