Cloricromene, a coumarine derivative, protects against lethal endotoxin shock in rats

Eur J Pharmacol. 1992 Jan 14;210(2):107-13. doi: 10.1016/0014-2999(92)90660-v.

Abstract

Endotoxin shock was induced in male rats by an intravenous (i.v.) injection of Salmonella enteriditis lipopolysaccharide (LPS; 20 mg/kg i.v.). Survival rate, macrophage and serum tumor necrosis factor (TNF-alpha), mean arterial blood pressure (MAP) and white blood cell count were then evaluated. Furthermore the in vitro effect of cloricromene on peritoneal macrophage phagocytosis and TNF-alpha release by primed peritoneal macrophages was investigated. LPS administration caused animal death (0% survival 24 h after endotoxin challenge), hypotension, marked leukopenia and increased the levels of TNF-alpha in both serum and macrophage supernatants. Cloricromene administration (0.5, 1 and 2 mg/kg i.v. 15 min after endotoxin) protected against LPS-induced lethality (100% survival rate 24 h after endotoxin challenge), reverted LPS-induced hypotension and leukopenia, and decreased TNF-alpha in both serum and macrophage supernatants. Finally, cloricromene, added in vitro to peritoneal macrophages collected from endotoxin-treated rats increased macrophage phagocytosis and reduced TNF-alpha formation by activated mononuclear phagocytes. Our data suggest that cloricromene increases survival rate in endotoxin shock through an inhibition of TNF-alpha production.

MeSH terms

  • Animals
  • Biological Assay
  • Blood Pressure / drug effects
  • Chromonar / analogs & derivatives*
  • Chromonar / pharmacology
  • Chromonar / therapeutic use
  • In Vitro Techniques
  • Leukocyte Count / drug effects
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Male
  • Peritoneal Cavity / cytology
  • Rats
  • Rats, Inbred Strains
  • Shock, Septic / blood
  • Shock, Septic / physiopathology
  • Shock, Septic / prevention & control*
  • Survival Rate
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Tumor Necrosis Factor-alpha
  • cloricromen
  • Chromonar