ME3738 protects from concanavalin A-induced liver failure via an IL-6-dependent mechanism

Eur J Immunol. 2003 Aug;33(8):2251-61. doi: 10.1002/eji.200323651.

Abstract

ME3738 is a new compound that attenuates liver disease in several models of acute and chronic liver inflammation. We used the concanavalin A (Con A) model to elucidate the molecular mechanisms of ME3738 to block liver cell damage. Pretreatment of BALB/c mice with ME3738 prior to Con A injection resulted in a significant reduction in liver injury. The protective effect of ME3738 prior to Con A injection was associated with a reduction in IL-6 serum levels and NF-kappaB DNA binding in liver nuclear extracts. However, STAT3 DNA binding was induced via ME3738 prior to Con A injection. Further analysis showed that ME3738 induces IL-6 serum levels and activates STAT3 DNA binding and target gene transcription. The relevance of this finding was assessed in IL-6(-/-) mice. In these animals, ME3738 induced no increase in IL-6 serum expression, and activation of IL-6-dependent pathways was not found. In addition, ME3738 did not protect IL-6(-/-) animals from Con A-induced liver failure, while IL-6 injection was still effective. Therefore, we demonstrate that ME3738 triggers IL-6 expression, which activates pathways that are relevant to protect from Con A-induced liver failure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acute-Phase Reaction / genetics
  • Acute-Phase Reaction / immunology
  • Animals
  • Concanavalin A / toxicity
  • DNA-Binding Proteins / metabolism
  • Gene Expression / drug effects
  • Immunosuppressive Agents / chemistry
  • Immunosuppressive Agents / pharmacology*
  • Interleukin-6 / deficiency
  • Interleukin-6 / genetics
  • Interleukin-6 / metabolism*
  • Liver Failure / chemically induced
  • Liver Failure / immunology*
  • Liver Failure / pathology
  • Liver Failure / prevention & control*
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mice, Knockout
  • NF-kappa B / metabolism
  • Oleanolic Acid / analogs & derivatives*
  • Oleanolic Acid / chemistry
  • Oleanolic Acid / pharmacology*
  • STAT3 Transcription Factor
  • Trans-Activators / metabolism
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • DNA-Binding Proteins
  • Immunosuppressive Agents
  • Interleukin-6
  • ME3738
  • NF-kappa B
  • STAT3 Transcription Factor
  • Stat3 protein, mouse
  • Trans-Activators
  • Tumor Necrosis Factor-alpha
  • Concanavalin A
  • soyasapogenol A
  • Oleanolic Acid