Tomatidine Alleviates Intervertebral Disc Degeneration by Activating the Nrf2/HO-1/GPX4 Signaling Pathway

Drug Des Devel Ther. 2024 Dec 27:18:6313-6329. doi: 10.2147/DDDT.S481714. eCollection 2024.

Abstract

Purpose: Intervertebral disc degeneration (IDD) is a leading cause of low back pain, and developing new molecular drugs and targets for IDD is a new direction for future treatment strategies. The aim of this study is to investigate the effects and mechanisms of tomatidine in ameliorating lumbar IDD.

Methods: Nucleus pulposus cells (NPCs) exposed to lipopolysaccharides were used as an in vitro model to investigate changes in the expression of extracellular matrix components and associated signaling pathway molecules. A lumbar instability model was used to simulate IDD. Tomatidine (Td) was then administered intraperitoneally, and its effects were evaluated through histopathological analysis.

Results: In vitro, Td significantly promoted ECM anabolism, inhibited ECM catabolism, and reduced oxidative stress and ferroptosis in LPS-stimulated NPCs. When Nrf2 expression was inhibited, oxidative stress and ferroptosis were exacerbated, and the protective effects of Td on NPCs were lost, suggesting the Nrf2/HO-1/GPX4 axis is critical for the therapeutic effects of Td. In vivo, histopathological analysis demonstrated that Td ameliorated IDD in a murine model.

Conclusion: Td alleviates IDD in vitro and in vivo by activating the Nrf2/HO-1/GPX4 pathway to inhibit ferroptosis in NPCs. This mechanism suggests Td is a promising candidate for IDD treatment.

Keywords: GPX4; Nrf 2; ferroptosis; intervertebral disc degeneration; tomatidine.

MeSH terms

  • Animals
  • Cells, Cultured
  • Heme Oxygenase-1 / metabolism
  • Humans
  • Intervertebral Disc Degeneration* / drug therapy
  • Intervertebral Disc Degeneration* / metabolism
  • Intervertebral Disc Degeneration* / pathology
  • Lipopolysaccharides / pharmacology
  • Male
  • Mice
  • Mice, Inbred C57BL
  • NF-E2-Related Factor 2* / metabolism
  • Nucleus Pulposus / drug effects
  • Nucleus Pulposus / metabolism
  • Nucleus Pulposus / pathology
  • Oxidative Stress / drug effects
  • Rats
  • Rats, Sprague-Dawley
  • Signal Transduction* / drug effects
  • Tomatine* / analogs & derivatives
  • Tomatine* / pharmacology

Substances

  • NF-E2-Related Factor 2
  • tomatidine
  • Tomatine
  • Heme Oxygenase-1
  • Lipopolysaccharides

Grants and funding

This research was partially supported by the Basic Public Welfare Research Project of Zhejiang Province (LGF19H060004), the Science and Technology Program of Traditional Chinese Medicine Science and Technology of Zhejiang Province (2018ZB138), the Science and Technology Planning Program of Taizhou City (1802KY04), and the Taizhou Social Development Science and Technology Project of Zhejiang Province (21ywa54).