Roflumilast reverses polymicrobial sepsis-induced liver damage by inhibiting inflammation in mice

Lab Invest. 2017 Sep;97(9):1008-1019. doi: 10.1038/labinvest.2017.59. Epub 2017 Jun 26.

Abstract

Sepsis is a life-threatening syndrome accompanied by an overwhelming inflammatory response and organ dysfunction. Selective targeting of phosphodiesterase 4 (PDE4) is currently being investigated as an effective therapeutic approach for inflammation-associated diseases. Roflumilast is a selective PDE4 inhibitor, used for the treatment of severe chronic obstructive pulmonary disease in clinic. However, its role in the treatment of sepsis-induced liver damage remains unclear. In the present study, we evaluated the effects of roflumilast in mice with cecal ligation and puncture-induced sepsis, and investigated the underlying mechanism. We found that roflumilast treatment improved survival in septic mice by reducing bacterial load locally and systemically, inhibiting the expression of pro-inflammatory cytokines interleukin-6 and tumor necrosis factor alpha, and alleviating liver injury. These effects were associated with the inhibition of nuclear translocation of nuclear factor-kappa B (NF-κB), as well as degradation of NF-κB inhibitory protein alpha. The phosphorylation of p38 mitogen-activated protein kinase (MAPK) was also markedly inhibited by roflumilast. Moreover, roflumilast significantly suppressed the activation of signal transducer and activator of transcription 3 (STAT3) and its upstream Janus kinase 1 and Janus kinase 2. Taken together, these results indicate that roflumilast prevents polymicrobial sepsis likely by suppressing NF-κB, p38 MAPK, and STAT3 pathways.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminopyridines / pharmacology
  • Aminopyridines / therapeutic use*
  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use*
  • Bacterial Load
  • Benzamides / pharmacology
  • Benzamides / therapeutic use*
  • Cyclopropanes / pharmacology
  • Cyclopropanes / therapeutic use
  • Cytokines
  • Inflammation / drug therapy*
  • Inflammation / metabolism
  • Inflammation / microbiology
  • Liver / drug effects
  • Liver / microbiology
  • Liver / pathology
  • Liver Diseases / drug therapy*
  • Liver Diseases / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • NF-kappa B / metabolism
  • STAT3 Transcription Factor
  • Sepsis / microbiology
  • Sepsis / physiopathology*
  • Survival Analysis

Substances

  • Aminopyridines
  • Anti-Inflammatory Agents
  • Benzamides
  • Cyclopropanes
  • Cytokines
  • NF-kappa B
  • STAT3 Transcription Factor
  • Stat3 protein, mouse
  • Roflumilast