Improved survival and reversal of endothelial dysfunction by the 21-aminosteroid, U-74389G in splanchnic ischaemia-reperfusion injury in the rat

Br J Pharmacol. 1995 Jun;115(3):395-400. doi: 10.1111/j.1476-5381.1995.tb16346.x.

Abstract

1. Anaesthetized rats subjected to total occlusion of the superior mesenteric artery and the coeliac trunk for 45 min developed a severe shock state (splanchnic artery occlusion, SAO shock) resulting in death within 70-90 min after release of the occlusion. Sham-operated animals were used as controls. 2. Survival rate, survival time, serum tumour necrosis factor (TNF-alpha), white blood cell (WBC) count, mean arterial blood pressure (MAP), plasma malonyladehyde (MAL); myeloperoxidase activity (MPO) and the responsiveness to acetylcholine (ACh 10 nM-10 microM) of aortic rings were investigated. 3. SAO shocked rats had a decreased survival rate and survival time (74 +/- 10 min, while sham-shocked rats survived more than 4 h), reduced mean arterial blood pressure, increased serum levels of TNF-alpha (267 +/- 13 u ml-1) and plasma levels of MAL (57 +/- 7 nmol ml-1), enhanced MPO activity in the ileum (0.23 +/- 0.04 u x 10(-3) g-1 tissue) and in the lung (2.2 +/- 0.8 u x 10(-3) g-1 tissue), leukopenia and reduced responsiveness to ACh of aortic rings. 4. The 21-aminosteroid U-74389G (30 mg kg-1, i.v.) increased survival (survival time = 232 +/- 15 min), lowered the serum levels of TNF-alpha and the plasma levels of MAL, reduced leukopenia and MPO activity both in the ileum (0.021 +/- 0.004 u x 10(-3) g-1 tissue) and in the lung (0.23 +/- 0.03 u x 10(-3) g-1 tissue), improved MAP and restored the responsiveness to ACh of aortic rings. 5. Our data suggest that U-74389G is a potent lipid peroxidation inhibitor and that it has antishock and endothelial protective actions.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholine / pharmacology
  • Analysis of Variance
  • Animals
  • Antioxidants / pharmacology
  • Antioxidants / therapeutic use*
  • Blood Pressure / drug effects
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / physiology
  • Leukocyte Count
  • Leukopenia / physiopathology
  • Lipid Peroxidation / drug effects
  • Male
  • Malondialdehyde / blood
  • Mesenteric Arteries / drug effects
  • Mesenteric Arteries / physiology
  • Mesenteric Vascular Occlusion / drug therapy
  • Mesenteric Vascular Occlusion / mortality
  • Nitroprusside / pharmacology
  • Peroxidase / metabolism
  • Pregnatrienes*
  • Rats
  • Reperfusion Injury / drug therapy*
  • Reperfusion Injury / mortality
  • Splanchnic Circulation / drug effects
  • Splanchnic Circulation / physiology
  • Steroids, Heterocyclic / pharmacology
  • Steroids, Heterocyclic / therapeutic use*
  • Survival Rate
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Antioxidants
  • Pregnatrienes
  • Steroids, Heterocyclic
  • Tumor Necrosis Factor-alpha
  • U 74389F
  • Nitroprusside
  • Malondialdehyde
  • Peroxidase
  • Acetylcholine