A paeonol derivative, YPH-PA3 promotes the differentiation of monocyte/macrophage lineage precursor cells into osteoblasts and enhances their autophagy

Eur J Pharmacol. 2018 Aug 5:832:104-113. doi: 10.1016/j.ejphar.2018.05.024. Epub 2018 May 18.

Abstract

Previous studies have indicated that paeonol inhibits RANKL-induced osteoclastogenesis by inhibiting the ERK, p38, and NF-κB pathway. We modified paeonol to form a new compound, YPH-PA3, and found that it promoted osteoclastogenesis rather than inhibited it the way paeonol does. The aim of this study is to investigate the mechanisms involved in YPH-PA3-promoted osteoclastogenesis. YPH-PA3-promoted differentiation of RAW264.7 cells (human monocytes) into osteoclasts is activated through ERK/p38/JNK phosphorylation, affecting c-FOS, NF-κB, and NFATc2. Real-time quantitative PCR and western blot revealed an increased expression of autophagy-related markers during YPH-PA3-induced osteoclastogenesis. We also demonstrated the relationship between p62/LC3 localization and F-actin ring formation by double-labeling immunofluorescence. Knockdown of p62 small-interfering RNA (siRNA) attenuated YPH-PA3-induced expression of autophagy-related genes. Our study results indicated that p62 may play a role in YPH-PA3-induced autophagy and osteoclastogenesis, which may help to develop a novel therapeutic strategy against osteoclastogenesis-related diseases.

Keywords: Autophagy; Osteoclasts; Osteoporosis; Paeonol; RANKL; p62.

MeSH terms

  • Acetophenones / chemistry
  • Acetophenones / pharmacology*
  • Animals
  • Autophagy / drug effects*
  • Bone Resorption / chemically induced
  • Cell Differentiation / drug effects*
  • Humans
  • Macrophages / cytology*
  • Macrophages / drug effects
  • Mice
  • Mitogen-Activated Protein Kinases / metabolism
  • Monocytes / cytology*
  • Monocytes / drug effects
  • NF-kappa B / metabolism
  • Osteoblasts / cytology*
  • Osteoblasts / drug effects
  • RAW 264.7 Cells
  • Signal Transduction / drug effects

Substances

  • Acetophenones
  • NF-kappa B
  • paeonol
  • Mitogen-Activated Protein Kinases