Inhibitory effect of oolonghomobisflavan B on osteoclastogenesis by suppressing p38 MAPK activation

Bioorg Med Chem Lett. 2020 Sep 15;30(18):127429. doi: 10.1016/j.bmcl.2020.127429. Epub 2020 Jul 21.

Abstract

Suppression of differentiation and/or function of osteoclasts is considered an effective therapeutic strategy for osteolytic bone diseases such as periodontitis and osteoporosis. Evidence regarding the health benefits of oolong tea consumption is accumulating, and tea polyphenols have various pharmacological properties such as anti-cancer and anti-diabetes effects. In this study, we investigated the effect of oolonghomobisflavan B (OFB), a polyphenolic compound in oolong tea, on osteoclast differentiation. OFB suppressed receptor activator of nuclear factor-κB (RANKL)-induced formation of tartate-resistant acid phosphatase-positive multinuclear cells without cytotoxicity. OFB also significantly attenuated p38 phosphorylation, which is essential for RANKL-induced osteoclastogenesis, and inhibited the expressions of nuclear factor of activated T cells, cytoplasmic 1 (NFATc1) and osteoclast-specific target genes, including dendritic cell-specific transmembrane protein and cathepsin K. Our findings suggest that OFB exhibits an anti-osteoclastogenic activity by inhibiting RANKL-mediated p38 activation, which is useful for the prevention and treatment of osteolytic bone diseases.

Keywords: NFATc1; Oolong tea; Oolonghomobisflavan B; Osteoclast differentiation; p38.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cathepsin K / metabolism
  • Cell Differentiation / drug effects*
  • Dendritic Cells
  • Drug Discovery
  • Enzyme Activation / drug effects
  • Humans
  • Membrane Proteins / metabolism
  • NF-kappa B / metabolism
  • Osteoclasts / cytology
  • Osteogenesis / drug effects*
  • Phosphorylation
  • Plant Extracts / chemistry*
  • Plant Extracts / pharmacology
  • Polyphenols / chemistry*
  • Polyphenols / pharmacology
  • RANK Ligand / metabolism
  • Signal Transduction
  • Tea / chemistry*
  • p38 Mitogen-Activated Protein Kinases / metabolism*

Substances

  • Membrane Proteins
  • NF-kappa B
  • Plant Extracts
  • Polyphenols
  • RANK Ligand
  • Tea
  • p38 Mitogen-Activated Protein Kinases
  • Cathepsin K