The MAP2K4/JNK/c-Jun Signaling Pathway Plays A Key Role In Dexmedetomidine Protection Against Acetaminophen-Induced Liver Toxicity

Drug Des Devel Ther. 2019 Nov 14:13:3887-3898. doi: 10.2147/DDDT.S215473. eCollection 2019.

Abstract

Purpose: Dexmedetomidine [DEX; (S)-4-[1-(2,3-dimethylphenyl)ethyl]-3H-imidazole] is a selective α2-adrenergic receptor (α2-AR) agonist that attenuates the liver damage associated with local or systemic inflammation. However, it remains unclear whether DEX has protective effects against acetaminophen (Paracetamol, PARA)-induced liver toxicity (PILT).

Methods: PILT mice were established by intraperitoneal administration of a hepatotoxic dose of acetaminophen (300 mg/kg). Thirty minutes later, the mice were treated with DEX at a concentration of 0, 5, 25, or 50 μg/kg. Blood and liver samples were obtained for further analysis.

Results: DEX treatment significantly attenuated PILT in mice, with the strongest beneficial effects at a dose of 25 μg/kg. The levels of hepatic cytokines, tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6), in addition to myeloperoxidase (MPO) activity, were significantly decreased following DEX treatment. Moreover, DEX treatment reduced macrophage recruitment around the area of hepatotoxicity and the expression levels of hepatic phosphorylated mitogen-activated protein kinase kinase 4 (MAP2K4), c-jun N-terminal kinase (JNK), and c-Jun expression induced by acetaminophen overdose.

Conclusion: The data suggest that DEX likely downregulates the JNK signaling pathway and its downstream effectors to promote its hepatoprotective effect, providing a clinical application of DEX for the attenuation of PILT.

Keywords: MAP2K4/JNK/c-Jun; acetaminophen-induced liver toxicity; dexmedetomidine.

MeSH terms

  • Acetaminophen / antagonists & inhibitors*
  • Acetaminophen / pharmacology
  • Adrenergic alpha-2 Receptor Agonists / pharmacology*
  • Animals
  • Chemical and Drug Induced Liver Injury / metabolism
  • Chemical and Drug Induced Liver Injury / prevention & control*
  • Dexmedetomidine / pharmacology*
  • Dose-Response Relationship, Drug
  • JNK Mitogen-Activated Protein Kinases / antagonists & inhibitors
  • JNK Mitogen-Activated Protein Kinases / metabolism
  • Liver / drug effects*
  • Liver / metabolism
  • MAP Kinase Kinase 4 / antagonists & inhibitors
  • MAP Kinase Kinase 4 / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Proto-Oncogene Proteins c-jun / antagonists & inhibitors
  • Proto-Oncogene Proteins c-jun / metabolism
  • Signal Transduction / drug effects
  • Structure-Activity Relationship

Substances

  • Adrenergic alpha-2 Receptor Agonists
  • Proto-Oncogene Proteins c-jun
  • Acetaminophen
  • Dexmedetomidine
  • JNK Mitogen-Activated Protein Kinases
  • MAP Kinase Kinase 4
  • MAP2K4 protein, human