Effects of 5-aminoisoquinolinone, a water-soluble, potent inhibitor of the activity of poly (ADP-ribose) polymerase, in a rodent model of lung injury

Biochem Pharmacol. 2002 Jan 15;63(2):293-304. doi: 10.1016/s0006-2952(01)00864-4.

Abstract

Poly (ADP-ribose) polymerase (PARP), a nuclear enzyme activated by strand breaks in DNA, plays an important role in the tissue injury associated with ischaemia--reperfusion injury and inflammation. The aim of the present study was to evaluate the effects of a novel and potent inhibitor of PARP activity on neutrophil recruitment in the acute inflammation induced by zymosan-activated plasma. Intra-thoracic administration of zymosan-activated plasma leads to an increase in neutrophil infiltration of the lung at 24hr. The potent PARP inhibitor 5-aminoisoquinolinone (5-AIQ) reduced the degree of lung injury and attenuated the expression of P-selectin and ICAM-1 as well as the recruitment of neutrophils into the injured lung. The up-regulation/expression of P-selectin and ICAM-1 in human endothelial cells exposed to oxidative stress (peroxynitrite) or to a pro-inflammatory cytokine (tumor necrosis factor alpha, TNFalpha) was also attenuated by 5-AIQ. These findings provide the first evidence that the activation of PARS participates in neutrophil-mediated lung injury by regulating the expression of P-selectin and ICAM-1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Survival / drug effects
  • Cytokines / metabolism
  • Disease Models, Animal
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / metabolism
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Female
  • Humans
  • Intercellular Adhesion Molecule-1 / metabolism
  • Isoquinolines / pharmacology*
  • Isoquinolines / therapeutic use
  • Mice
  • Mice, Inbred BALB C
  • NAD / metabolism
  • P-Selectin / metabolism
  • Peroxynitrous Acid / pharmacology
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Poly(ADP-ribose) Polymerases / metabolism*
  • Respiratory Distress Syndrome / drug therapy
  • Respiratory Distress Syndrome / enzymology*
  • Up-Regulation

Substances

  • 5-aminoisoquinolinone
  • Cytokines
  • Enzyme Inhibitors
  • Isoquinolines
  • P-Selectin
  • Poly(ADP-ribose) Polymerase Inhibitors
  • NAD
  • Intercellular Adhesion Molecule-1
  • Peroxynitrous Acid
  • Poly(ADP-ribose) Polymerases