PUBLICATION

In vitro and in vivo osteogenic activity of licochalcone A

Authors
Kim, S.N., Bae, S.J., Kwak, H.B., Min, Y.K., Jung, S.H., Kim, C.H., and Kim, S.H.
ID
ZDB-PUB-110511-13
Date
2012
Source
Amino Acids   42(4): 1455-1465 (Journal)
Registered Authors
Jung, Seung-Hyun, Kim, Cheol-Hee
Keywords
licochalcone A, Osteogenic activity, ERK, bone morphogenetic protein, zebrafish
MeSH Terms
  • Animals
  • Bone Development/drug effects*
  • Bone Morphogenetic Protein 2
  • Cell Differentiation/drug effects*
  • Cell Line
  • Chalcones/pharmacology*
  • Mice
  • Mice, Inbred ICR
  • Osteoblasts/cytology*
  • Osteoblasts/drug effects
  • Osteoblasts/metabolism
  • Signal Transduction/drug effects
  • Zebrafish
PubMed
21468757 Full text @ Amino Acids
Abstract
We investigated the in vitro and in vivo osteogenic activity of licochalcone A. At low concentrations, licochalcone A stimulated the differentiation of mouse pre-osteoblastic MC3T3-E1 subclone 4 (MC4) cells and enhanced the bone morphogenetic protein (BMP)-2-induced stimulation of mouse bi-potential mesenchymal precursor C2C12 cells to commit to the osteoblast differentiation pathway. This osteogenic activity of licochalcone A was accompanied by the activation of extracellular-signal regulated kinase (ERK). The involvement of ERK was confirmed in a pharmacologic inhibition study. Additionally, noggin (a BMP antagonist) inhibited the osteogenic activity of licochalcone A in C2C12 cells. Licochalcone A also enhanced the BMP-2-stimulated expression of various BMP mRNAs. This suggested that the osteogenic action of licochalcone A in C2C12 cells could be dependent on BMP signaling and/or expression. We then tested the in vivo osteogenic activity of licochalcone A in two independent animal models. Licochalcone A accelerated the rate of skeletal development in zebrafish and enhanced woven bone formation over the periosteum of mouse calvarial bones. In summary, licochalcone A induced osteoblast differentiation with ERK activation in both MC4 and C2C12 cells and it exhibited in vivo osteogenic activity in zebrafish skeletal development and mouse calvarial bone formation. The dual action of licochalcone A in stimulating bone formation and inhibiting bone resorption, as described in a previous study, might be beneficial in treating bone-related disorders.
Genes / Markers
Figures
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Antibodies
Orthology
Engineered Foreign Genes
Mapping