Impairment of H+-K+-ATPase-dependent proton transport and inhibition of gastric acid secretion by ethanol

Am J Physiol Gastrointest Liver Physiol. 2001 Jun;280(6):G1331-40. doi: 10.1152/ajpgi.2001.280.6.G1331.

Abstract

Ethanol (1-20% vol/vol) caused a dose-dependent reduction in the basal rate of acid formation in isolated rabbit gastric glands with a calculated EC(50) value of 4.5 +/- 0.2%. Ethanol also reduced ATP levels in isolated gastric glands and in cultured parietal cells (EC(50): 8.8 +/- 0.4% and 8.5 +/- 0.2%, respectively) and decreased both basal and forskolin-stimulated cAMP levels. In studies carried out in gastric gland microsomes, ethanol inhibited the hydrolytic activity of H+-K+-ATPase(EC(50): 8.5 +/- 0.6%), increased passive proton permeability (EC(50): 7.9%), and reduced H+-K+-ATPase-dependent proton transport (EC(50): 3%). Our results show that the inhibition of gastric acid secretion observed at low concentrations of ethanol (< or =5%) is mainly caused by the specific impairment of H+-K+-ATPase-dependent proton transport across cell membranes rather than inhibition of the hydrolytic activity of H+-K+-ATPase, reduction in the cellular content of ATP, or increase in the passive permeability of membranes to protons, although these changes, in combination, must be relevant at concentrations of ethanol > or =7%.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / metabolism
  • Animals
  • Biological Transport / drug effects
  • Biological Transport / physiology
  • Cells, Cultured
  • Coloring Agents / pharmacokinetics
  • Cyclic AMP / metabolism
  • Ethanol / pharmacology*
  • Gastric Acid / metabolism*
  • Gastric Mucosa / drug effects
  • Gastric Mucosa / metabolism
  • Gastric Mucosa / pathology
  • H(+)-K(+)-Exchanging ATPase / physiology*
  • Intracellular Membranes / metabolism
  • Male
  • Microsomes, Liver / metabolism
  • Parietal Cells, Gastric / drug effects
  • Parietal Cells, Gastric / metabolism
  • Permeability
  • Protons*
  • Rabbits
  • Trypan Blue / pharmacokinetics

Substances

  • Coloring Agents
  • Protons
  • Ethanol
  • Adenosine Triphosphate
  • Cyclic AMP
  • H(+)-K(+)-Exchanging ATPase
  • Trypan Blue