Peroxisome proliferator-activated receptor-gamma agonists suppress tissue factor overexpression in rat balloon injury model with paclitaxel infusion

PLoS One. 2011;6(11):e28327. doi: 10.1371/journal.pone.0028327. Epub 2011 Nov 29.

Abstract

The role and underlying mechanisms of rosiglitazone, a peroxisome proliferator-activated receptor-gamma (PPAR-γ) agonist, on myocardial infarction are poorly understood. We investigated the effects of this PPAR-γ agonist on the expression of tissue factor (TF), a primary molecule for thrombosis, and elucidated its underlying mechanisms. The PPAR-γ agonist inhibited TF expression in response to TNF-α in human umbilical vein endothelial cells, human monocytic leukemia cell line, and human umbilical arterial smooth muscle cells. The overexpression of TF was mediated by increased phosphorylation of mitogen-activated protein kinase (MAPK), which was blocked by the PPAR-γ agonist. The effective MAPK differed depending on each cell type. Luciferase and ChIP assays showed that transcription factor, activator protein-1 (AP-1), was a pivotal target of the PPAR-γ agonist to lower TF transcription. Intriguingly, two main drugs for drug-eluting stent, paclitaxel or rapamycin, significantly exaggerated thrombin-induced TF expression, which was also effectively blocked by the PPAR-γ agonist in all cell types. This PPAR-γ agonist did not impair TF pathway inhibitor (TFPI) in three cell types. In rat balloon injury model (Sprague-Dawley rats, n = 10/group) with continuous paclitaxel infusion, the PPAR-γ agonist attenuated TF expression by 70±5% (n = 4; P<0.0001) in injured vasculature. Taken together, rosiglitazone reduced TF expression in three critical cell types involved in vascular thrombus formation via MAPK and AP-1 inhibitions. Also, this PPAR-γ agonist reversed the paclitaxel-induced aggravation of TF expression, which suggests a possibility that the benefits might outweigh its risks in a group of patients with paclitaxel-eluting stent implanted.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Catheterization*
  • Disease Models, Animal
  • Enzyme Activation / drug effects
  • Gene Expression Regulation / drug effects
  • Human Umbilical Vein Endothelial Cells / drug effects
  • Human Umbilical Vein Endothelial Cells / metabolism
  • Humans
  • Infusions, Intra-Arterial
  • Lipoproteins / metabolism
  • Mitogen-Activated Protein Kinases / metabolism
  • Models, Biological
  • Monocytes / drug effects
  • Monocytes / metabolism
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / metabolism
  • PPAR gamma / agonists*
  • Paclitaxel / administration & dosage*
  • Phosphorylation / drug effects
  • Promoter Regions, Genetic / genetics
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Rosiglitazone
  • Sirolimus / pharmacology
  • Thiazolidinediones / pharmacology*
  • Thromboplastin / genetics
  • Thromboplastin / metabolism*
  • Umbilical Arteries / pathology

Substances

  • Lipoproteins
  • PPAR gamma
  • RNA, Messenger
  • Thiazolidinediones
  • lipoprotein-associated coagulation inhibitor
  • Rosiglitazone
  • Thromboplastin
  • Mitogen-Activated Protein Kinases
  • Paclitaxel
  • Sirolimus