Endothelin A receptor blockade decreases expression of growth factors and collagen and improves matrix metalloproteinase-2 activity in kidneys from stroke-prone spontaneously hypertensive rats

J Cardiovasc Pharmacol. 2002 Jun;39(6):892-900. doi: 10.1097/00005344-200206000-00015.

Abstract

This study hypothesizes that endothelin-1 induces renal damage by increasing expression of growth/inflammatory factors, important in renal fibrosis. Male stroke-prone spontaneously hypertensive rats (SHRSPs) (8-weeks, n = 24) were randomized into three groups: control group, high-salt group (4% NaCl), and salt plus an endothelin A receptor antagonist, BMS 182874 (40 mg/kg/d). After 20 weeks treatment, rats were killed. Messenger RNA (mRNA) expression of renal preproendothelin-1, endothelin A and B receptors, and procollagen I and III was evaluated by reverse transcription polymerase chain reaction. Expression of transforming growth factor (TGF)-beta1 and basic fibroblast growth factor (bFGF) was determined by immunoblotting. Matrix metalloproteinase-2 (MMP-2) activity was measured by zymography. In salt-loaded SHRSPs, preproendothelin-1 mRNA expression was increased 1.6-fold, and endothelin A receptor mRNA expression was decreased (70% of control). Salt-loaded SHRSPs had increased renal expression of TGF-b1 and procollagens. MMP-2 activity was augmented fivefold. BMS decreased (p < 0.01) expression of TGF-beta1, bFGF, and procollagen I and reduced MMP-2 activity. Thus severe hypertension and renal dysfunction in salt-loaded SHRSPs are associated with increased expression of renal endothelin-1, growth factors, and collagen. BMS treatment alleviated these effects, suggesting that nephroprotection by endothelin A receptor blockade is mediated by normalizing expression of growth factors, reducing extracellular matrix deposition, and decreasing MMP activity.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antihypertensive Agents / pharmacology
  • Antihypertensive Agents / therapeutic use
  • Collagen / antagonists & inhibitors*
  • Collagen / biosynthesis*
  • Endothelin Receptor Antagonists*
  • Growth Substances / biosynthesis
  • Growth Substances / metabolism*
  • Hypertension / drug therapy
  • Hypertension / enzymology
  • Kidney / drug effects
  • Kidney / enzymology*
  • Male
  • Matrix Metalloproteinase 2 / metabolism*
  • Rats
  • Rats, Inbred SHR
  • Receptor, Endothelin A
  • Receptors, Endothelin / biosynthesis
  • Receptors, Endothelin / physiology*
  • Stroke / drug therapy
  • Stroke / enzymology*

Substances

  • Antihypertensive Agents
  • Endothelin Receptor Antagonists
  • Growth Substances
  • Receptor, Endothelin A
  • Receptors, Endothelin
  • Collagen
  • Matrix Metalloproteinase 2