Keratinocyte-derived vascular endothelial growth factor biosynthesis represents a pleiotropic side effect of peroxisome proliferator-activated receptor-gamma agonist troglitazone but not rosiglitazone and involves activation of p38 mitogen-activated protein kinase: implications for diabetes-impaired skin repair

Mol Pharmacol. 2008 Oct;74(4):952-63. doi: 10.1124/mol.108.049395. Epub 2008 Jul 3.

Abstract

The peroxisome proliferator-activated receptors (PPARs) represent pharmacological target molecules to improve insulin resistance in type 2 diabetes mellitus. Here we assessed a functional connection between pharmacological activation of PPAR and vascular endothelial growth factor (VEGF) expression in keratinocytes and during diabetes-impaired acute skin repair in obese/obese (ob/ob) mice. PPARbeta/delta agonist 4-[3-[4-acetyl-3-hydroxy-2-propylphenoxy)propoxy]phenoxy]acetic acid (L165,041) and PPARgamma agonists ciglitazone and troglitazone, but not rosiglitazone, potently induced VEGF mRNA and protein expression from cultured keratinocytes. Inhibitor studies revealed a strong functional dependence of troglitazone- and L165,041-induced VEGF expression on p38 and p42/44 mitogen-activated protein kinase (MAPK) activation in keratinocytes. Rosiglitazone also induced activation of p38 MAPK but failed to mediate the activation of p42/44 MAPK in the cells. Functional ablation of PPARbeta/delta and PPARgamma from keratinocytes by small interfering RNA did not abrogate L165,041- and troglitazone-induced VEGF biosynthesis and suggested VEGF induction as a pleiotropic, PPAR-independent effect of both drugs in the cells. In accordance with the in vitro situation, we found activated p38 MAPK in wound keratinocytes from acute wounds of rosiglitazone- and troglitazone-treated diabetic obese/obese mice, whereas keratinocyte-specific VEGF protein signals were only prominent upon troglitazone treatment. In summary, our data from cell culture and wound healing experiments suggested p38 MAPK activation as a side effect of thiazolidinediones; however, only troglitazone, but not rosiglitazone, seemed to translate p38 MAPK activation into a PPARgamma-independent induction of VEGF from keratinocytes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Survival / drug effects
  • Cells, Cultured
  • Chromans / metabolism*
  • Chromans / pharmacology
  • Diabetes Mellitus / metabolism
  • Dose-Response Relationship, Drug
  • Enzyme Activation
  • Female
  • Immunohistochemistry
  • Keratinocytes / metabolism*
  • Mice
  • Mice, Inbred C57BL
  • Mice, Mutant Strains
  • PPAR gamma / agonists*
  • RNA, Messenger / metabolism
  • Rosiglitazone
  • Thiazolidinediones / metabolism*
  • Thiazolidinediones / pharmacology
  • Time Factors
  • Troglitazone
  • Vascular Endothelial Growth Factor A / biosynthesis*
  • Wound Healing
  • p38 Mitogen-Activated Protein Kinases / metabolism*

Substances

  • Chromans
  • PPAR gamma
  • RNA, Messenger
  • Thiazolidinediones
  • Vascular Endothelial Growth Factor A
  • Rosiglitazone
  • p38 Mitogen-Activated Protein Kinases
  • Troglitazone