BioScience Trends. 2012;6(2):63-69. (DOI: 10.5582/bst.2012.v6.2.63)

Effect of CXCR4 inhibitor AMD3100 on alkaline phosphatase activity and mineralization in osteoblastic MC3T3-E1 cells.

Luan J, Cui YZ, Zhang YY, Zhou XY, Zhang GL, Han JX


The aim of the study was to investigate the effect of C-X-C chemokine receptor type 4 (CXCR4) inhibitor AMD3100 on the osteogenic differentiation of pre-osteoblastic cell line MC3T3-E1. In this study we found that blocking SDF-1/CXCR4 signaling with AMD3100 strongly suppressed osteogenic differentiation in MC3T3-E1 cells, as evidenced by an early decrease in the activity of alkaline phosphatase (ALP), and down-regulation of mRNA expression of the osteogenic master regulator Runx2, ALP, osteocalcin, and progressive ankylosis genes. Moreover, we found that the regulatory effect of AMD3100 might be mediated via intracellular STAT3 activation. However, AMD3100 exerted no significant effect on generation of matrix mineralization at the terminal stage of osteogenic induction. In conclusion, our results demonstrated an inhibitory role of AMD3100 in osteogenic differentiation of MC3T3-E1 cells, especially in the early stage, which provides novel insights into the effect of CXCR4 antagonists on modulation of osteogenesis.

KEYWORDS: SDF-1/CXCR4 signaling, AMD3100, MC3T3-E1, osteogenic differentiation, signal transducer and activator of transcription 3

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