Systemic and hepatosplanchnic hemodynamic and metabolic effects of the PARP inhibitor PJ34 during hyperdynamic porcine endotoxemia

Shock. 2003 May;19(5):415-21. doi: 10.1097/01.shk.0000048904.46342.22.

Abstract

Activation of the poly(ADP-ribose)polymerase (PARP), a highly energy-consuming DNA-repairing enzyme, plays a crucial role in the pathogenesis of multiorgan failure. Most results, however, were derived from experiments with hypodynamic shock states characterized by a markedly decreased cardiac output (CO) and/or using a pretreatment approach. Therefore, we investigated the effects of the novel potent and selective PARP-1 inhibitor PJ34 in a posttreatment model of long-term, volume-resuscitated porcine endotoxemia. Anesthetized, mechanically ventilated and instrumented pigs received continuous intravenous (i.v.) lipopolysaccharide (LPS) over 24 h. Hydroxyethyl starch was administered to maintain a mean arterial pressure > 65 mmHg. After 12 h of LPS infusion, the animals were randomized to receive either vehicle (Control, n = 9) or i.v. PJ34 (n = 6; 10 mg/kg over 1 h followed by 2 mg/kg/h until the end of the experiment). Measurements were performed before as well as at 12, 18, and 24 h of LPS infusion. In all animals CO increased because of reduced systemic vascular resistance (SVR) and fluid resuscitation. PJ34 further raised CO (P < 0.05 vs. control group) as the result of a higher stroke volume indicating its positive inotropic effect. In addition, it diminished the rise in the ileal mucosal-arterial PCO2 gap, which returned to baseline levels at 24 h of LPS, and improved the gut lactate balance (P = 0.093 PJ34 vs. control) together with significantly lower portal venous lactate/pyruvate ratios. By contrast, it failed to influence the LPS-induced derangements of liver metabolism. Incomplete PARP inhibition because of dilutional effects and/or an only partial efficacy when used in post-treatment approaches may account for this finding.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acid-Base Equilibrium / drug effects
  • Animals
  • Disease Models, Animal
  • Endotoxemia / blood
  • Endotoxemia / chemically induced
  • Endotoxemia / physiopathology*
  • Enzyme Inhibitors / therapeutic use*
  • Female
  • Hemodynamics / drug effects*
  • Lactates / metabolism
  • Lipopolysaccharides / toxicity
  • Liver / drug effects
  • Liver / metabolism
  • Liver Circulation / drug effects*
  • Male
  • Oxygen / blood
  • Oxygen Consumption / drug effects
  • Phenanthrenes / therapeutic use*
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Reference Values
  • Splanchnic Circulation / drug effects*
  • Swine

Substances

  • Enzyme Inhibitors
  • Lactates
  • Lipopolysaccharides
  • N-(oxo-5,6-dihydrophenanthridin-2-yl)-N,N-dimethylacetamide hydrochloride
  • Phenanthrenes
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Oxygen