ONO-5046, an elastase inhibitor, attenuates liver mitochondrial dysfunction after endotoxin

Crit Care Med. 1998 Jan;26(1):138-41. doi: 10.1097/00003246-199801000-00029.

Abstract

Objective: To investigate the effect of ONO-5046, an elastase inhibitor, on liver mitochondrial dysfunction after endotoxin administration.

Design: Prospective, randomized, controlled animal study.

Setting: Research laboratory.

Subjects: Male Hartley guinea pigs.

Interventions: Endotoxin shock was induced by intravenous infusion of Escherichia coli lipopolysaccharide endotoxin (50 mg/kg). Six guinea pigs were treated with endotoxin and saline. Twenty-four guinea pigs received 5, 10, and 30 mg/kg/hr of ONO-5046 after endotoxin administration. Six guinea pigs received only saline.

Measurements and main results: We measured oxygen uptake in state 3 (substrate and adenosine 5'-diphosphate [ADP]) and state 4 (excess substrate, no ADP), as well as the respiratory control ratio (state 3/state 4), adenosine 5'-diphosphate/oxygen ratio (ADP/O), and arterial ketone body ratio. ONO-5046 was dose dependently effective in liver mitochondrial oxidative phosphorylation, such as oxygen uptake in stage 4, respiratory control ratio, adenosine triphosphate synthesis, ADP/O, and arterial ketone body ratio when ONO-5046 was started 30 mins after endotoxin. The administration of 30 mg/kg/hr of ONO-5046 improved mean blood pressure, which had decreased after endotoxin.

Conclusion: ONO-5046 attenuates the endotoxin-induced liver mitochondrial dysfunctions that may be related to increased liver blood flow.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Diphosphate / metabolism
  • Animals
  • Blood Pressure / drug effects
  • Chemical and Drug Induced Liver Injury
  • Dose-Response Relationship, Drug
  • Escherichia coli*
  • Glycine / analogs & derivatives*
  • Glycine / pharmacology
  • Guinea Pigs
  • Ketone Bodies / metabolism
  • Leukocyte Elastase / antagonists & inhibitors*
  • Lipopolysaccharides / toxicity*
  • Liver Diseases / enzymology
  • Liver Diseases / prevention & control*
  • Male
  • Mitochondria, Liver / drug effects*
  • Mitochondria, Liver / enzymology
  • Oxygen / metabolism
  • Phosphorylation
  • Respiration / physiology
  • Serine Proteinase Inhibitors / pharmacology*
  • Sulfonamides / pharmacology*

Substances

  • Ketone Bodies
  • Lipopolysaccharides
  • Serine Proteinase Inhibitors
  • Sulfonamides
  • Adenosine Diphosphate
  • sivelestat
  • Leukocyte Elastase
  • Oxygen
  • Glycine