Osteopromotive activity of a novel pyrazole carboxamide derivative

Future Med Chem. 2013 Feb;5(2):125-34. doi: 10.4155/fmc.12.209.

Abstract

Aims: To investigate the effect of 1-(4-(tert-butyl)benzyl)-N-(4-methoxyphenyl)-3-phenyl-1H-pyrazole-5-carboxamide (Pyr-C) on the proliferation and osteogenic differentiation of MC3T3-E1 cells.

Materials & methods: MTT and BrdU incorporation assay were used to determine cell survival and proliferation. The gene expression levels of osteogenic markers were determined using real-time PCR and ALP activity was detected. Western-blot analysis was used to determine the protein expression of BSP and OPN. The long-term effect of Pyr-C on mineralization deposition was measured by Alizarin Red Staining.

Results: Pyr-C inhibited cell proliferation and increased ALP activity. Gene expression of ALP, BSP, OCN, Runx2, and Osterix was up-regulated in Pyr-C-induced group. Pyr-C increased the protein expression of BSP at day 7, 14 and 21, and OPN at day 14, 21 and 28. Meanwhile, Pyr-C enhanced the mineral deposition.

Conclusion: Pyr-C inhibits proliferation and stimulates osteogenic differentiation of MC3T3-E1 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3T3 Cells
  • Animals
  • Cell Differentiation / drug effects*
  • Cell Differentiation / physiology
  • Cell Line
  • Cell Proliferation / drug effects*
  • Mice
  • Osteoblasts / drug effects*
  • Osteoblasts / physiology
  • Osteogenesis / drug effects*
  • Osteogenesis / physiology
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology*

Substances

  • Pyrazoles