Benidipine, a long-acting calcium-channel blocker, prevents the progression to end-stage renal failure in a rat mesangioproliferative glomerulonephritis

Nephron. 2000 Nov;86(3):315-26. doi: 10.1159/000045787.

Abstract

Background: Although the renoprotective effect of calcium-channel blockers (CCBs) has been examined in several models of hypertensive nephropathy, it remains unclear. It also remains to be clarified whether CCBs prevent the progression to end-stage renal failure in chronic progressive glomerulonephritis (GN). A new rat model of progressive mesangioproliferative GN was used to study the effect of benidipine hydrochloride, a long-acting dihydropyridine CCB, on the clinical features and morphological lesions.

Methods: This animal model of progressive GN was induced by a single intravenous injection of anti-Thy-1 monoclonal antibody (MoAb 1-22-3) two weeks after unilateral nephrectomy. After 10 weeks of treatment with benidipine (1, 3, and 5 mg/kg body weight, p.o.) or hydralazine (5 mg/kg body weight, p.o.), systolic blood pressure (SBP), urinary protein excretion, creatinine clearance, glomerulosclerosis index, tubulointerstitial lesion index, glomerular cross-sectional area, and glomerular expression of transforming growth factor-beta (TGF-beta) and alpha-smooth muscle actin (alpha-SMA) were measured.

Results: Untreated rats developed hypertension, massive proteinuria, renal dysfunction, severe glomerular and tubulointerstitial injury, higher glomerular size, and marked glomerular staining for TGF-beta and alpha-SMA, while uninephrectomized control rats did not. Each dose of benidipine and hydralazine equally reduced SBP to uninephrectomized control levels. Three and five mg/kg/day of benidipine increased creatinine clearance, ameliorated glomerular and tubulointerstitial injury, and reduced glomerular staining for TGF-beta and alpha-SMA, but 1 mg/kg/day of benidipine and hydralazine failed. Only a dose of 5 mg/kg/day of benidipine reduced glomerular size, although it did not reduce the size to control levels.

Conclusion: These results indicate that in a rat model of progressive mesangioproliferative GN, benidipine prevents the progression to end-stage renal failure in a dose-dependent manner. This renoprotective action is associated with the suppression of glomerular expression of TGF-beta and alpha-SMA.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Actins / analysis
  • Animals
  • Blood Pressure
  • Body Weight
  • Calcium Channel Blockers / pharmacology*
  • Creatinine / metabolism
  • Dihydropyridines / pharmacology*
  • Disease Models, Animal
  • Disease Progression
  • Fluorescent Antibody Technique
  • Glomerulonephritis, Membranoproliferative / drug therapy*
  • Glomerulonephritis, Membranoproliferative / pathology
  • Hydralazine / pharmacology
  • Kidney Failure, Chronic / drug therapy*
  • Kidney Failure, Chronic / pathology
  • Kidney Failure, Chronic / prevention & control*
  • Kidney Glomerulus / chemistry
  • Kidney Glomerulus / pathology
  • Male
  • Nephrectomy
  • Proteinuria / drug therapy
  • Proteinuria / pathology
  • Rats
  • Rats, Wistar
  • Transforming Growth Factor beta / analysis
  • Vasodilator Agents / pharmacology

Substances

  • Actins
  • Calcium Channel Blockers
  • Dihydropyridines
  • Transforming Growth Factor beta
  • Vasodilator Agents
  • Hydralazine
  • benidipine
  • Creatinine