Use of xanthine oxidase inhibitor febuxostat inhibits renal interstitial inflammation and fibrosis in unilateral ureteral obstructive nephropathy

Clin Exp Nephrol. 2012 Aug;16(4):549-56. doi: 10.1007/s10157-012-0609-3. Epub 2012 Feb 18.

Abstract

Background: Renal interstitial fibrosis is the common pathway in progressive renal diseases, where oxidative stress promotes inflammation and macrophage infiltration. Febuxostat is a novel nonpurine xanthine oxidase (XO)-specific inhibitor for treating hyperuricemia. While some reports suggest a relationship between hyperuricemia and chronic kidney disease (CKD), the renoprotective mechanism of an XO inhibitor in CKD remains unknown. Recent reports have focused on XO as a source of oxidative stress.

Methods: Here, we investigate the potential of febuxostat to reduce fibrogenic and inflammatory responses in an established interstitial fibrosis model-unilateral ureteric obstruction (UUO). Male Sprague-Dawley rats were divided into three groups: sham-operated group, vehicle-treated UUO group, and febuxostat-treated UUO group.

Results: Treatment with febuxostat diminished XO activity in obstructed kidneys, and suppressed nitrotyrosine, a marker of oxidative stress. Consequently, febuxostat inhibited early proinflammatory cytokine expression, followed by a reduction of interstitial macrophage infiltration. In addition, febuxostat suppressed transforming growth factor-β messenger RNA expression, thereby ameliorating smooth muscle alpha actin and type I collagen expression.

Conclusion: Our results provide evidence for the renoprotective action of febuxostat against the formation of interstitial fibrosis. A decrease in macrophage infiltration and interstitial fibrosis, along with a decrease of the oxidative stress marker, strongly suggests the existence of a causal relationship between them. Febuxostat may have therapeutic value in slowing or preventing interstitial fibrosis in patients with CKD.

MeSH terms

  • Animals
  • Cell Movement
  • Cytokines / metabolism
  • Disease Models, Animal
  • Febuxostat
  • Fibrosis
  • Kidney / metabolism
  • Kidney / pathology*
  • Kidney Diseases / etiology*
  • Kidney Diseases / metabolism
  • Kidney Diseases / pathology*
  • Macrophages / pathology
  • Male
  • Nephritis, Interstitial / pathology
  • Nephritis, Interstitial / prevention & control*
  • Oxidative Stress / drug effects
  • Rats
  • Rats, Sprague-Dawley
  • Thiazoles / pharmacology
  • Thiazoles / therapeutic use*
  • Transforming Growth Factor beta / metabolism
  • Ureteral Obstruction / complications*
  • Xanthine Oxidase / antagonists & inhibitors*

Substances

  • Cytokines
  • Thiazoles
  • Transforming Growth Factor beta
  • Febuxostat
  • Xanthine Oxidase