Inhibition of Fibroblast Growth Factor Receptor by AZD4547 Protects Against Inflammation in Septic Mice

Inflammation. 2019 Dec;42(6):1957-1967. doi: 10.1007/s10753-019-01056-4.

Abstract

Sepsis is a life-threatening condition caused by the dysregulated host immune response to infection characterized by excessive secretion of inflammatory factors. AZD4547 is a selective inhibitor of fibroblast growth factor receptors that participates in the inflammatory response. The aim of this study was to investigate the inflammation-targeting effects and related molecular mechanisms of AZD4547 in sepsis using a cecal ligation and puncture model and RAW264.7 macrophages stimulated with lipopolysaccharide. AZD4547 improved the survival of CLP mice and exhibited a robust protective function against lung damage histologically. Pretreatment with AZD4547 significantly alleviated the expression of the pro-inflammatory factors IL-1β, IL-6, TNF-α, MMP9, and CXCL10 both in vivo and in vitro. In addition, AZD4547 suppressed the proliferative activity of macrophages in lung tissue and RAW264.7 macrophages. In addition, the LPS-induced phosphorylation of key proteins of NF-κB/MAPK/STAT3 pathways in RAW264.7 macrophages, such as p65, IκB-α, Erk1/2, JNK, and STAT3 proteins, could be inhibited by AZD4547 pretreatment. In conclusion, AZD4547 exerts a protective effect against excessive inflammatory damage in septic mice and may have the potential for use as an effective drug for the management of sepsis.

Keywords: AZD4547; Cytokine; FGFR; Inflammation; Macrophage; Sepsis.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Benzamides / pharmacology*
  • Inflammation / drug therapy
  • Inflammation / prevention & control*
  • Macrophages / drug effects
  • Mice
  • Mitogen-Activated Protein Kinases / metabolism
  • NF-kappa B / metabolism
  • Phosphorylation / drug effects
  • Piperazines / pharmacology*
  • Pyrazoles / pharmacology*
  • RAW 264.7 Cells
  • Receptors, Fibroblast Growth Factor / antagonists & inhibitors*
  • STAT3 Transcription Factor / metabolism

Substances

  • AZD4547
  • Antineoplastic Agents
  • Benzamides
  • NF-kappa B
  • Piperazines
  • Pyrazoles
  • Receptors, Fibroblast Growth Factor
  • STAT3 Transcription Factor
  • STAT3 protein, human
  • Mitogen-Activated Protein Kinases