Sildenafil increases endothelial progenitor cell function and improves ischemia-induced neovascularization in hypercholesterolemic apolipoprotein E-deficient mice

Hypertension. 2009 Nov;54(5):1043-9. doi: 10.1161/HYPERTENSIONAHA.109.139451. Epub 2009 Sep 21.

Abstract

Hypercholesterolemia is associated with impaired neovascularization in response to ischemia. Potential mechanisms include defective NO bioactivity and a reduction in the number/function of endothelial progenitor cells (EPCs). Here we tested the hypothesis that sildenafil, a phosphodiesterase 5 inhibitor that increases NO-driven cGMP levels, could stimulate EPC function and improve ischemia-induced neovascularization in hypercholesterolemic conditions. Apolipoprotein E-deficient (ApoE(-/-)) mice were treated (or not treated) with sildenafil (40 mg/kg per day in water), and hindlimb ischemia was surgically induced by femoral artery removal. Sildenafil treatment led to an improved blood flow recovery, an increased capillary density, and a reduction of oxidative stress levels in ischemic muscles at day 7 after surgery. Sildenafil therapy is associated with an increased activation of angiogenic transduction pathways, including Akt, p44/42 mitogen-activated protein kinase, and p38. In vitro, sildenafil increases cellular migration and tubule formation of mature endothelial cells (human umbilical vascular endothelial cells) in a cGMP-dependent manner. In vivo, ApoE(-/-) mice treated with sildenafil exhibit a significant increase in the number of bone marrow-derived EPCs. Moreover, the angiogenic activities of EPCs (migration and adhesion) are significantly improved in ApoE(-/-) mice treated with sildenafil. In summary, this study demonstrates that sildenafil treatment is associated with improved ischemia-induced neovascularization in hypercholesterolemic ApoE(-/-) mice. The mechanisms involve beneficial effects on angiogenic transduction pathways together with an increase in the number and the functional activity of EPCs. Sildenafil could constitute a novel therapeutic strategy to reduce tissue ischemia in atherosclerotic diseases.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analysis of Variance
  • Animals
  • Apolipoproteins E / deficiency*
  • Blotting, Western
  • C-Reactive Protein / analysis
  • Cell Movement / drug effects
  • Cell Movement / physiology
  • Cells, Cultured
  • Disease Models, Animal
  • Endothelial Cells / drug effects*
  • Endothelial Cells / physiology
  • Hindlimb / blood supply
  • Hypercholesterolemia / physiopathology
  • Immunohistochemistry
  • Ischemia / drug therapy
  • Mice
  • Mice, Inbred C57BL
  • Neovascularization, Physiologic / drug effects*
  • Neovascularization, Physiologic / physiology
  • Piperazines / pharmacology*
  • Probability
  • Purines / pharmacology
  • Random Allocation
  • Sildenafil Citrate
  • Stem Cells / drug effects
  • Stem Cells / metabolism
  • Sulfones / pharmacology*

Substances

  • Apolipoproteins E
  • Piperazines
  • Purines
  • Sulfones
  • C-Reactive Protein
  • Sildenafil Citrate