Stimulation of HIF-1alpha, HIF-2alpha, and VEGF by prolyl 4-hydroxylase inhibition in human lung endothelial and epithelial cells

Free Radic Biol Med. 2005 Apr 15;38(8):1002-13. doi: 10.1016/j.freeradbiomed.2004.12.004.

Abstract

Diminished alveolar and vascular development is characteristic of bronchopulmonary dysplasia (BPD) affecting many preterm newborns. Hypoxia promotes angiogenic responses in developing lung via, for example, vascular endothelial growth factor (VEGF). To determine if prolyl 4-hydroxylase (PHD) inhibition could augment hypoxia-inducible factors (HIFs) and expression of angiogenic proteins essential for lung development, HIF-1alpha and -2alpha proteins were assessed in human developing and adult lung microvascular endothelial cells and alveolar epithelial-like cells treated with either the HIF-PHD-selective inhibitor PHI-1 or the nonselective PHD inhibitors dimethyloxaloylglycine (DMOG) and deferoxamine (DFO). PHI-1 stimulated HIF-1alpha and -2alpha equally or more effectively than did DMOG or DFO, enhanced VEGF release, and elevated glucose consumption, whereas it was considerably less cytotoxic than DMOG or DFO. Moreover, VEGF receptor Flt-1 levels increased, whereas KDR/Flk-1 decreased. PHI-1 treatment also increased PHD-2, but not PHD-1 or -3, protein. These results provide proof of principle that HIF stimulation and modulation of HIF-regulated angiogenic proteins through PHI-1 treatment are feasible, effective, and nontoxic in human lung cells, suggesting the use of PHI-1 to enhance angiogenesis and lung growth in evolving BPD.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Basic Helix-Loop-Helix Transcription Factors
  • Cells, Cultured
  • Cinnamates / pharmacology
  • Enzyme Inhibitors / pharmacology
  • Epithelial Cells / metabolism
  • Humans
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • Lung / cytology
  • Lung / enzymology*
  • Procollagen-Proline Dioxygenase / antagonists & inhibitors*
  • Trans-Activators / metabolism*
  • Transcription Factors / metabolism*
  • Vascular Endothelial Growth Factor A / metabolism*

Substances

  • Basic Helix-Loop-Helix Transcription Factors
  • Cinnamates
  • Enzyme Inhibitors
  • HIF1A protein, human
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • SU 1498
  • Trans-Activators
  • Transcription Factors
  • Vascular Endothelial Growth Factor A
  • endothelial PAS domain-containing protein 1
  • Procollagen-Proline Dioxygenase