The inhibitory effects of H+ K+ ATPase inhibitors on human neutrophils in vitro: restoration by a K+ ionophore

Inflamm Res. 2007 Mar;56(3):105-11. doi: 10.1007/s00011-006-6127-6.

Abstract

Objective: This study investigated the ability of proton pump inhibitors (PPI), such as omeprazole and pantoprazole, to inhibit neutrophil migration, calcium mobilization and the mechanisms involved in this inhibition.

Methods: Neutrophils were incubated with different concentrations of omeprazole and pantoprazole for 30 min and stimulated to migrate with fMLP and IL-8. Treatment toxicity was assessed by MTT assay. The intracellular calcium levels were analyzed in neutrophils pre-treated with omeprazole and pre-loaded with FURA-2AM, when stimulated with fMLP. The activity of p38 MAP Kinase was evaluated by Western blot after treatment with omeprazole.

Results: Omeprazole is able to inhibit neutrophil chemotaxis to fMLP and IL-8. Pantoprazole demonstrated the same ability. This inhibitory effect was not due to a toxic effect of the proton pump inhibitors. Inhibition of v-ATPase by bafilomycin did not modify the ability of fMLP or IL-8 to induce neutrophil migration. Omeprazole was also able to decrease intracellular calcium availability. The addition of a potassium ionophore, nigericin, restored the migratory ability, as well as the intracellular calcium levels. The activity of p38 MAP Kinase was decreased in neutrophils pretreated with omeprazole.

Conclusion: Proton pump inhibitors promote inhibition of H+ K+ ATPase in neutrophils, resulting in cationic flow disturbances through the cellular membrane that, consequently, inhibit migratory and intracellular events such as calcium influx and p38 MAP Kinase activation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 2-Pyridinylmethylsulfinylbenzimidazoles / pharmacology
  • Apoptosis / drug effects
  • Calcium / metabolism
  • Cell Movement / drug effects
  • Cells, Cultured
  • Gastric Acid / metabolism
  • H(+)-K(+)-Exchanging ATPase / metabolism
  • Humans
  • Interleukin-8 / pharmacology
  • Ionophores / pharmacology*
  • Macrolides / pharmacology
  • N-Formylmethionine Leucyl-Phenylalanine / pharmacology
  • Neutrophils / cytology
  • Neutrophils / drug effects*
  • Neutrophils / enzymology*
  • Nigericin / pharmacology*
  • Omeprazole / pharmacology
  • Pantoprazole
  • Potassium / metabolism*
  • Protein Kinase Inhibitors / pharmacology
  • Proton Pump Inhibitors*
  • p38 Mitogen-Activated Protein Kinases / metabolism

Substances

  • 2-Pyridinylmethylsulfinylbenzimidazoles
  • Interleukin-8
  • Ionophores
  • Macrolides
  • Protein Kinase Inhibitors
  • Proton Pump Inhibitors
  • bafilomycin A
  • N-Formylmethionine Leucyl-Phenylalanine
  • Pantoprazole
  • p38 Mitogen-Activated Protein Kinases
  • H(+)-K(+)-Exchanging ATPase
  • Omeprazole
  • Nigericin
  • Potassium
  • Calcium