Imatinib improves insulin resistance and inhibits injury-induced neointimal hyperplasia in high fat diet-fed mice

Eur J Pharmacol. 2021 Jan 5:890:173666. doi: 10.1016/j.ejphar.2020.173666. Epub 2020 Oct 24.

Abstract

Imatinib, a PDGF receptor tyrosine kinase inhibitor, has been shown to suppress intimal hyperplasia in different animal models under normal metabolic milieu, diabetic, and/or hypercholesterolemic conditions. However, the impact of imatinib treatment on injury-induced neointimal hyperplasia has not yet been investigated in the setting of insulin resistance without frank diabetes. Using a mouse model of high fat diet (HFD)-induced insulin resistance and guidewire-induced arterial injury, the present study demonstrates that intraperitoneal administration of imatinib (25 mg/kg/day) for ~3 weeks resulted in a marked attenuation of neointimal hyperplasia (intima/media ratio) by ~78% (n = 6-9 per group; P < 0.05). Imatinib treatment also led to significant improvements in key metabolic parameters. In particular, imatinib improved insulin resistance and glucose tolerance, as revealed by complete inhibition of HFD-induced increase in HOMA-IR index and AUCIPGTT, respectively. In addition, imatinib treatment led to diminutions in HFD-induced increases in plasma total cholesterol and triglycerides by ~73% and ~59%, respectively. Furthermore, imatinib decreased HFD-induced increase in visceral fat accumulation by ~51% (as determined by epididymal white adipose tissue weight). Importantly, imatinib treatment in HFD-fed mice enhanced plasma levels of high-molecular-weight adiponectin by ~2-fold without affecting total adiponectin. However, there were no significant changes in mean arterial pressure in insulin-resistant state or after imatinib exposure, as measured by tail-cuff method. Together, the present findings suggest that targeting PDGF receptor tyrosine kinase using imatinib may provide a realistic treatment option to prevent injury-induced neointimal hyperplasia and diet-induced insulin resistance in obesity.

Keywords: Adiponectin; Arterial injury; Imatinib; Insulin resistance; Neointimal hyperplasia; PDGF.

MeSH terms

  • Animals
  • Diet, High-Fat / adverse effects*
  • Femoral Artery / drug effects*
  • Femoral Artery / metabolism
  • Femoral Artery / pathology
  • Hyperplasia / drug therapy
  • Hyperplasia / etiology
  • Hyperplasia / pathology
  • Imatinib Mesylate / pharmacology
  • Imatinib Mesylate / therapeutic use*
  • Insulin Resistance* / physiology
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Neointima / drug therapy*
  • Neointima / metabolism
  • Neointima / pathology
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use*

Substances

  • Protein Kinase Inhibitors
  • Imatinib Mesylate