The calcium channel blocker cilnidipine selectively suppresses hypoxia-inducible factor 1 activity in vascular cells

Eur J Pharmacol. 2009 Mar 15;606(1-3):130-6. doi: 10.1016/j.ejphar.2009.01.012. Epub 2009 Jan 21.

Abstract

Calcium ion is one of the most important second messengers of cellular signal transduction including hypoxia-elicited signals. In this study, we investigated the effects of the L-type calcium channel blockers such as nifedipine, efonidipine cilnidipine, diltiazem, and verapamil, on the activity of hypoxia-inducible factor-1 (HIF-1), a key transcription factor in control of hypoxia-induced gene expression. Using the lung carcinoma cell line A549 cells, human aortic smooth muscle cells, and human umbilical vein endothelial cells, we demonstrated that cilnidipine exclusively suppressed HIF-1 activity and the expressions of downstream genes in a cell-type specific manner. We also demonstrated that cilnidipine blocked the synthesis of the HIF-1alpha protein not by affecting activity of the intracellular hypoxia-sensing element prolyl hydroxylases but inhibiting activity of Akt and mitogen-activated protein kinase and that the inhibition is not dependent on the effect on calcium homeostasis.

MeSH terms

  • Calcium / metabolism
  • Calcium Channel Blockers / pharmacology*
  • Cell Line, Tumor
  • Dihydropyridines / pharmacology*
  • Gene Expression Regulation / drug effects
  • Humans
  • Hypoxia-Inducible Factor 1 / antagonists & inhibitors*
  • Hypoxia-Inducible Factor 1 / metabolism*
  • Intracellular Space / drug effects
  • Intracellular Space / metabolism
  • Oxygen / metabolism
  • Stress, Physiological / drug effects

Substances

  • Calcium Channel Blockers
  • Dihydropyridines
  • Hypoxia-Inducible Factor 1
  • cilnidipine
  • Oxygen
  • Calcium