Osteopromotive activity of a novel pyrazole carboxamide derivative.

Future medicinal chemistry

PubMedID: 23360138

Han QQ, Yu MJ, Ge SH, Guo HM, Zhang J, Zhao BX, Yang PS. Osteopromotive activity of a novel pyrazole carboxamide derivative. Future Med Chem. 2013;5(2):125-34.
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.