Long-term administration of AMD3100, an antagonist of SDF-1/CXCR4 signaling, alters fracture repair

J Orthop Res. 2012 Nov;30(11):1853-9. doi: 10.1002/jor.22145. Epub 2012 May 16.

Abstract

Fracture healing involves rapid stem and progenitor cell migration, homing, and differentiation. SDF-1 (CXCL12) is considered a master regulator of CXCR4-positive stem and progenitor cell trafficking to sites of ischemic (hypoxic) injury and regulates their subsequent differentiation into mature reparative cells. In this study, we investigated the role of SDF-1/CXCR4 signaling in fracture healing where vascular disruption results in hypoxia and SDF-1 expression. Mice were injected with AMD3100, a CXCR4 antagonist, or vehicle twice daily until euthanasia with the intent to impair stem cell homing to the fracture site and/or their differentiation. Fracture healing was evaluated using micro-computed tomography, histology, quantitative PCR, and mechanical testing. AMD3100 administration resulted in a significantly reduced hyaline cartilage volume (day 14), callus volume (day 42) and mineralized bone volume (day 42) and reduced expression of genes associated with endochondral ossification including collagen Type 1 alpha 1, collagen Type 2 alpha 1, vascular endothelial growth factor, Annexin A5, nitric oxide synthase 2, and mechanistic target of rapamycin. Our data suggest that the SDF-1/CXCR4 signaling plays a central role in bone healing possibly by regulating the recruitment and/or differentiation of stem and progenitor cells.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzylamines
  • Biomechanical Phenomena
  • Chemokine CXCL12 / metabolism*
  • Cyclams
  • Fracture Healing*
  • Heterocyclic Compounds / pharmacology*
  • Immunohistochemistry
  • In Situ Hybridization
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Osteogenesis
  • Polymerase Chain Reaction
  • Receptors, CXCR4 / antagonists & inhibitors
  • Receptors, CXCR4 / metabolism*
  • X-Ray Microtomography

Substances

  • Benzylamines
  • CXCR4 protein, mouse
  • Chemokine CXCL12
  • Cxcl12 protein, mouse
  • Cyclams
  • Heterocyclic Compounds
  • Receptors, CXCR4
  • plerixafor