Celastrol reduces IL-1β induced matrix catabolism, oxidative stress and inflammation in human nucleus pulposus cells and attenuates rat intervertebral disc degeneration in vivo

Biomed Pharmacother. 2017 Jul:91:208-219. doi: 10.1016/j.biopha.2017.04.093. Epub 2017 Apr 28.

Abstract

Celastrol has been reported to exert therapeutic potential on pro-inflammatory diseases including asthma, Crohn's disease, arthritis and neurodegenerative disorders via inhibiting NF-κB pathway. While the effect of celastrol on intervertebral disc degeneration (IDD), which is also a pro-inflammatory disease, remains unknown. In this study, we evaluated the effect of celastrol on IDD in IL-1β treated human nucleus pulposus cells in vitro as well as in puncture induced rat IDD model in vivo. Our results showed that celastrol reduced the expression of catabolic genes (MMP-3, 9, 13, ADAMTS-4, 5), oxidative stress factors (COX-2, iNOS) and pro-inflammatory factors (IL-6, TNF-a) induced by IL-1β in nucleus pulposus cells, also phosphorylation of IκBα and p65 were attenuated by celastrol, indicating NF-κB pathway was inhibited by celastrol in nucleus pulposus cells. In vivo study showed that celastrol treated rats had stronger T2-weighted signal than vehicle-treated rats at 2 weeks and 6 weeks' time point, suggesting celastrol could attenuate intervertebral disc degeneration in vivo. Together, our study demonstrates that celastrol could reduce IL-1β induced matrix catabolism, oxidative stress and inflammation in human nucleus pulposus cells and attenuates rat intervertebral disc degeneration in vivo, which shows its potential to be a therapeutic drug for IDD.

Keywords: Celastrol; Inflammation; Intervertebral disc degeneration; NF-κB.

MeSH terms

  • ADAMTS5 Protein / metabolism
  • Aggrecans / genetics
  • Aggrecans / metabolism
  • Animals
  • Cell Death / drug effects
  • Cell Nucleus / drug effects
  • Cell Nucleus / metabolism
  • Cell Survival / drug effects
  • Collagen Type II / genetics
  • Collagen Type II / metabolism
  • Cyclooxygenase 2 / metabolism
  • Cytoprotection / drug effects
  • Extracellular Matrix / metabolism*
  • Gene Expression Regulation / drug effects
  • Humans
  • Inflammation / pathology*
  • Interleukin-1beta / pharmacology*
  • Interleukin-6 / metabolism
  • Intervertebral Disc Degeneration / genetics
  • Intervertebral Disc Degeneration / pathology*
  • Magnetic Resonance Imaging
  • Male
  • NF-kappa B / metabolism
  • Nitric Oxide Synthase Type II / metabolism
  • Nucleus Pulposus / pathology*
  • Oxidative Stress* / drug effects
  • Pentacyclic Triterpenes
  • Protein Transport / drug effects
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Rats, Sprague-Dawley
  • Transforming Growth Factor beta / metabolism
  • Triterpenes / pharmacology
  • Triterpenes / therapeutic use*
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Aggrecans
  • Collagen Type II
  • Interleukin-1beta
  • Interleukin-6
  • NF-kappa B
  • Pentacyclic Triterpenes
  • RNA, Messenger
  • Transforming Growth Factor beta
  • Triterpenes
  • Tumor Necrosis Factor-alpha
  • Nitric Oxide Synthase Type II
  • Cyclooxygenase 2
  • ADAMTS5 Protein
  • ADAMTS5 protein, human
  • celastrol