Tyrphostin AG 556 improves survival and reduces multiorgan failure in canine Escherichia coli peritonitis

J Clin Invest. 1997 Apr 15;99(8):1966-73. doi: 10.1172/JCI119364.

Abstract

Tyrosine kinase-dependent cell signaling is postulated to be a pivotal control point in inflammatory responses initiated by bacterial products and TNF. Using a canine model of gram-negative septic shock, we investigated the effect of tyrosine kinase inhibitors (tyrphostins) on survival. Animals were infected intraperitoneally with Escherichia coli 0111: B4, and then, in a randomized, blinded fashion, were treated immediately with one of two tyrphostins, AG 556 (n = 40) or AG 126 (n = 10), or with control (n = 50), and followed for 28 d or until death. All animals received supplemental oxygen, fluids, and antibiotics. Tyrphostin AG 556 improved survival times when compared to controls (P = 0.05). During the first 48 h after infection, AG 556 also improved mean arterial pressure, left ventricular ejection fraction, cardiac output, oxygen delivery, and alveolar-arterial oxygen gradient compared to controls (all P < or = 0.05). These improvements in organ injury were significantly predictive of survival. Treatment with AG 556 had no effect on clearance of endotoxin or bacteria from the blood (both P = NS); however, AG 556 did significantly lower serum TNF levels (P = 0.03). These data are consistent with the conclusion that AG 556 prevented cytokine-induced multiorgan failure and death during septic shock by inhibiting cell-signaling pathways without impairing host defenses as determined by clearance of bacteria and endotoxin.

MeSH terms

  • Animals
  • Benzylidene Compounds / pharmacology
  • Disease Models, Animal
  • Dogs
  • Enzyme Inhibitors / pharmacology*
  • Escherichia coli Infections / complications
  • Escherichia coli Infections / drug therapy*
  • Escherichia coli Infections / physiopathology
  • Heart / drug effects
  • Heart / physiopathology
  • In Vitro Techniques
  • Lung / drug effects
  • Lung / physiopathology
  • Multiple Organ Failure / etiology
  • Multiple Organ Failure / prevention & control*
  • Nitriles / pharmacology*
  • Peritonitis / complications
  • Peritonitis / drug therapy*
  • Peritonitis / physiopathology
  • Phenols / pharmacology*
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Shock, Septic / complications
  • Shock, Septic / drug therapy
  • Shock, Septic / physiopathology
  • Signal Transduction / drug effects
  • Tumor Necrosis Factor-alpha / metabolism
  • Tyrphostins*
  • gamma-Glutamyltransferase / blood

Substances

  • Benzylidene Compounds
  • Enzyme Inhibitors
  • Nitriles
  • Phenols
  • Tumor Necrosis Factor-alpha
  • Tyrphostins
  • AG 127
  • AG 556
  • gamma-Glutamyltransferase
  • Protein-Tyrosine Kinases