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Trapidil induces osteogenesis by upregulating the signaling of bone morphogenetic proteins

Bongjun Kim1, Jong-Ho Lee2, Won Jong Jin1

  • 1Department of Cell and Developmental Biology, Dental Research Institute, School of Dentistry, Seoul National University, Seoul 110-749, Republic of Korea.

Cellular Signalling
|June 8, 2018
PubMed

Insights

Inhibiting platelet-derived growth factor receptor (PDGFR) with trapidil significantly enhances bone regeneration and osteogenic differentiation. This occurs by upregulating bone morphogenetic protein receptor (BMPR) activity, promoting osteogenesis in vitro and in vivo.

Area of Science:

  • Regenerative Medicine
  • Orthopedics
  • Molecular Biology

Background:

  • Platelet-derived growth factor receptor (PDGFR) signaling is known to inhibit osteogenesis.
  • The therapeutic potential of PDGFR inhibition for bone regeneration and its precise inhibitory mechanisms remain largely unelucidated.

Purpose of the Study:

  • To investigate the osteogenic effects of inhibiting PDGFR using trapidil, a PDGFR antagonist, in both in vivo and in vitro models.
  • To elucidate the underlying molecular mechanisms by which PDGFR inhibition promotes osteogenesis.

Main Methods:

  • A rat calvarial defect model was utilized to assess in vivo bone regeneration using micro-computed tomography and histology.
  • Primary mouse calvarial osteoblast precursors were cultured in osteogenic differentiation medium with trapidil to examine cellular mechanisms.
  • Western blotting and specific inhibitors (LDN193189, noggin) were employed to investigate signaling pathways, including BMP and MAPK.

Main Results:

  • Trapidil significantly promoted bone regeneration in the rat calvarial defect model and enhanced osteogenic differentiation of osteoblast precursors.
  • Mechanistically, trapidil induced phosphorylation of Smad1/5/9 and MAPK, leading to increased Runx2 expression, a key transcription factor for osteogenesis.
  • The pro-osteogenic effects of trapidil were dependent on bone morphogenetic protein receptor (BMPR) activity, as evidenced by inhibition with LDN193189, ALK3 depletion, and noggin treatment. Trapidil also showed a synergistic effect with BMP2.

Conclusions:

  • Trapidil promotes osteogenesis in vitro and in vivo by upregulating bone morphogenetic protein receptor (BMPR) activity and enhancing BMP signaling.
  • Inhibition of osteogenesis by PDGFR signaling may involve attenuated BMPR activity.
Keywords:
BMPOsteoblastPDGFTrapidil

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