Dehydrocostus lactone inhibits NFATc1 via regulation of IKK, JNK, and Nrf2, thereby attenuating osteoclastogenesis

BMB Rep. 2020 Apr;53(4):218-222. doi: 10.5483/BMBRep.2020.53.4.220.

Abstract

Excessive and hyperactive osteoclast activity causes bone diseases such as osteoporosis and periodontitis. Thus, the regulation of osteoclast differentiation has clinical implications. We recently reported that dehydrocostus lactone (DL) inhibits osteoclast differentiation by regulating a nuclear factor of activated T-cells, cytoplasmic 1 (NFATc1), but the underlying mechanism remains to be elucidated. Here we demonstrated that DL inhibits NFATc1 by regulating nuclear factor-κB (NF-κB), activator protein-1 (AP-1), and nuclear factor-erythroid 2- related factor 2 (Nrf2). DL attenuated IκBα phosphorylation and p65 nuclear translocation as well as decreased the expression of NF-κB target genes and c-Fos. It also inhibited c-Jun N-terminal kinase (JNK) but not p38 or extracellular signalregulated kinase. The reporter assay revealed that DL inhibits NF-κB and AP-1 activation. In addition, DL reduced reactive oxygen species either by scavenging them or by activating Nrf2. The DL inhibition of NFATc1 expression and osteoclast differentiation was less effective in Nrf2-deficient cells. Collectively, these results suggest that DL regulates NFATc1 by inhibiting NF-κB and AP-1 via down-regulation of IκB kinase and JNK as well as by activating Nrf2, and thereby attenuates osteoclast differentiation. [BMB Reports 2020; 53(4): 218-222].

MeSH terms

  • Animals
  • Bone Resorption / metabolism
  • Cell Differentiation / drug effects
  • Female
  • I-kappa B Kinase / metabolism
  • Lactones / pharmacology*
  • MAP Kinase Signaling System / drug effects
  • Male
  • Mice
  • Mice, Knockout
  • NF-E2-Related Factor 2 / metabolism
  • NF-kappa B / metabolism
  • NFATC Transcription Factors / metabolism
  • NFATC Transcription Factors / physiology
  • Osteoclasts / drug effects
  • Osteoclasts / metabolism*
  • Osteogenesis / drug effects*
  • Osteogenesis / physiology
  • Proto-Oncogene Proteins c-fos / metabolism
  • RANK Ligand / pharmacology
  • RAW 264.7 Cells
  • Sesquiterpenes / pharmacology*
  • Signal Transduction / drug effects
  • Transcription Factor AP-1 / metabolism

Substances

  • Lactones
  • NF-E2-Related Factor 2
  • NF-kappa B
  • NFATC Transcription Factors
  • NFATC1 protein, human
  • NFE2L2 protein, human
  • Proto-Oncogene Proteins c-fos
  • RANK Ligand
  • Sesquiterpenes
  • Transcription Factor AP-1
  • dehydrocostus lactone
  • I-kappa B Kinase