Co-inhibition of Angiotensin II Receptor and Endothelin-1 Attenuates Renal Injury in Unilateral Ureteral Obstructed Mice

Kidney Blood Press Res. 2016;41(4):450-9. doi: 10.1159/000443446. Epub 2016 Jul 15.

Abstract

Background/aims: Both endothelin-1 (ET-1) and the renin-angiotensin system (RAS) may play important roles in renal fibrosis in the obstructed kidney. However, there have been few clear demonstrations of a relationship between their activation and additive or synergistic roles in renal fibrosis. We investigated the protective roles and relationship between renal RAS and ET-1 in unilateral ureteral obstruction (UUO) mice.

Methods: 8-week-old male C57BL/6 mice were divided into seven groups: sham, bosentan+sham, valsartan+sham, vehicle+UUO, bosentan+UUO, valsartan+UUO, and valsartan+bosentan+UUO. Valsartan and bosentan were administered orally using an NG tube (valsartan 10 mg/kg/day, bosentan 100 mg/kg/day for 8 days, after which the molecular and structural kidney parameters were evaluated. Bosentan treatment elevated plasma renin activity, renal renin, and AT1R expression in UUO mice.

Results: Although valsartan decreased plasma ET-1 in these mice, it did not affect ET(A) or ET(B) in their kidneys. Co-treatment with valsartan and bosentan decreased ET-1 in these mice compared to the single treatments. Bosentan, but not valsartan, elevated eNOS expression in their kidneys. Co-treatment with valsartan and bosentan reduced TGF-β, α-SMA, and collagen IV expression, and the Masson's trichrome stained area in their kidneys.

Conclusions: Bosentan and valsartan acted complementarily, and co-treatment with both drugs had an additive protective effect against renal fibrosis.

MeSH terms

  • Acute Kidney Injury / drug therapy
  • Acute Kidney Injury / prevention & control
  • Animals
  • Antihypertensive Agents / pharmacology
  • Antihypertensive Agents / therapeutic use
  • Bosentan
  • Drug Synergism
  • Endothelin-1 / antagonists & inhibitors*
  • Liver Cirrhosis / drug therapy*
  • Liver Cirrhosis / prevention & control
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Receptors, Angiotensin / drug effects*
  • Sulfonamides / pharmacology*
  • Sulfonamides / therapeutic use
  • Ureteral Obstruction / drug therapy*
  • Valsartan / pharmacology*
  • Valsartan / therapeutic use

Substances

  • Antihypertensive Agents
  • Endothelin-1
  • Receptors, Angiotensin
  • Sulfonamides
  • Valsartan
  • Bosentan