The novel PARP inhibitor 5-aminoisoquinolinone reduces the liver injury caused by ischemia and reperfusion in the rat

Med Sci Monit. 2002 Nov;8(11):BR444-53.

Abstract

Background: This study was designed to investigate the effects of 5-aminoisoquinolinone (5-AIQ), a water-soluble potent inhibitor of poly-(ADP-ribose) polymerase (PARP) in a rat model of liver ischemia-reperfusion injury.

Material/methods: Male Wistar rats were anesthetised with sodium pentobarbital (60 mg/kg, i.p.) and subjected to liver ischemia (for 30 minutes) and reperfusion (for 2 hours). Liver injury was assessed by measuring (i). the serum levels of transaminases, lactate dehydrogenase, gamma-glutamyl transferase, (ii). lipid peroxidation in liver tissue and (iii). by immunohistochemistry for PARP and intracellular adhesion molecule 1 (ICAM-1).

Results: Pre-treatment of rats (five minutes prior to onset of liver ischemia) with the PARP inhibitor 5-AIQ (3 mg/kg, i.v.) rather than vehicle reduced the rise in the serum levels of transaminases, lactate dehydrogenase, and gamma-glutamyl transferase as well as the degree of lipid peroxidation (measured as levels of malondialdehyde in the liver) caused by ischemia-reperfusion of the liver. Liver sections obtained from 5-AIQ treated rats showed reduced PARP activation and less staining for ICAM-1.

Conclusions: Taken together, these results show that 5-AIQ, a new water-soluble potent inhibitor of poly-(ADP-ribose) polymerase, reduces the tissue injury associated with ischemia-reperfusion of the liver. We propose that 5-AIQ may be useful in the therapy conditions associated with ischemia-reperfusion of the liver which remains an important clinical problem during shock, liver surgery, and liver transplantation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Survival
  • Cells, Cultured
  • Humans
  • Immunohistochemistry
  • Intercellular Adhesion Molecule-1 / blood
  • Isoquinolines / pharmacology*
  • L-Lactate Dehydrogenase / blood
  • Lipid Peroxidation
  • Liver / drug effects*
  • Liver / injuries*
  • Liver / metabolism
  • Male
  • Poly(ADP-ribose) Polymerase Inhibitors*
  • Rats
  • Rats, Wistar
  • Reperfusion Injury
  • Time Factors
  • Transaminases / blood
  • gamma-Glutamyltransferase / blood

Substances

  • 5-aminoisoquinolinone
  • Isoquinolines
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Intercellular Adhesion Molecule-1
  • L-Lactate Dehydrogenase
  • gamma-Glutamyltransferase
  • Transaminases