A dual inhibitor of TNF-alpha and IL-1 mitigates liver and kidney dysfunction and improves survival in rat endotoxemia

Hepatogastroenterology. 2005 Sep-Oct;52(65):1507-10.

Abstract

Background/aims: Endotoxin shock induces multiple organ dysfunction syndromes that are associated with a substantial increase in mortality. In this study, we evaluated the effect of FR167653, a potent suppressant of tumor necrosis factor-alpha (TNF-alpha) and interleukin-1 (IL-1) production, on lipopolysaccharide (LPS)-induced liver and kidney injury and lethality in rats.

Methodology: Male Sprague-Dawley rats weighing from 200 to 270g received an injection of LPS. The FR group received an infusion of FR167653 at 0.2 mg/kg/hr, commencing 30 min prior to the LPS injection and continuing for 5.5 hr, while the control group received an infusion of a vehicle in the same fashion. Separate groups of animals were used for the survival study (n=5 each), and for blood sampling (n=5 each group, each time point).

Results: The FR group showed a significantly better survival rate'than the control group. Serum levels of GOT, Cr, and BUN were significantly lower in the FR group than in the control group. The elevation of TNF-alpha and IL-1beta at 2 hr after LPS administration was significantly lower in the FR group than in the control group.

Conclusions: FR167653 administration is effective in decreasing serum TNF-alpha and IL-1beta levels and associated injury to liver and kidney caused by LPS-induced endotoxemia, as well as decreasing mortality.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Endotoxemia / drug therapy*
  • Endotoxemia / physiopathology*
  • Interleukin-1 / blood
  • Lipopolysaccharides
  • Liver Diseases / drug therapy*
  • Liver Diseases / physiopathology
  • Liver Function Tests
  • Lung Diseases / drug therapy*
  • Lung Diseases / physiopathology
  • Male
  • Pyrazoles / pharmacology*
  • Pyridines / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Tumor Necrosis Factor-alpha / analysis
  • Tumor Necrosis Factor-alpha / antagonists & inhibitors*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • FR 167653
  • Interleukin-1
  • Lipopolysaccharides
  • Pyrazoles
  • Pyridines
  • Tumor Necrosis Factor-alpha