Effect of fasudil on Rho-kinase and nephropathy in subtotally nephrectomized spontaneously hypertensive rats

Kidney Int. 2003 Dec;64(6):2009-19. doi: 10.1046/j.1523-1755.2003.00300.x.

Abstract

Background: Although Rho-kinase is reported to play an important role in vascular injury, the contribution of Rho-kinase to the progression of renal injury remains unestablished.

Methods: We examined the effect of fasudil, a Rho-kinase inhibitor, on the progression of renal injury in subtotally nephrectomized spontaneously hypertensive rats (SHR). Rats were randomly assigned to three groups: sham-operated SHR; salt-loaded subtotally nephrectomized rats (SHR-subtotal nephrectomy); SHR-subtotal nephrectomy given fasudil for 6 weeks (SHR-subtotal nephrectomy + fasudil; 3 mg/kg/day). Renal morphologic and molecular analysis as well as urinary protein excretion was evaluated.

Results: In SHR-subtotal nephrectomy treated with fasudil, systolic blood pressure was not significantly different from that in SHR-subtotal nephrectomy without fasudil (208 +/- 8 mm Hg vs. 217 +/- 14 mm Hg). Urinary protein excretion was markedly increased in SHR-subtotal nephrectomy (124 +/- 16 mg/day), but this increase was significantly suppressed by fasudil (79 +/- 12 mg/day). Renal histologic examination revealed that fasudil improved glomerular and tubulointerstitial injury scores with parallel amelioration of proliferating cell nuclear antigen-positive and ED-1-positive cell infiltration. Furthermore, Western blot analyses showed that both expression and activity of Rho-kinase were enhanced in SHR-subtotal nephrectomy, compared with those in SHR without nephrectomy, and fasudil suppressed Rho-kinase activity. Finally, fasudil up-regulated the expression of p27kip1, a cyclin-dependent kinase inhibitor, and increased the p27kip1 immunopositive cells in both glomeruli and tubulointerstitium with the use of immunohistochemistry.

Conclusion: Rho-kinase pathway is involved in the pathogenesis of renal injury. Furthermore, the inhibition of Rho-kinase may constitute a therapeutic strategy for the treatment of renal injury in part through the p27kip1 up-regulation and the subsequent inhibition of cell proliferation and macrophage recruitment.

MeSH terms

  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / analogs & derivatives*
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / pharmacology*
  • Animals
  • Blood Pressure / drug effects
  • Cell Cycle Proteins / metabolism
  • Cell Division / drug effects
  • Cyclin-Dependent Kinase Inhibitor p21
  • Cyclin-Dependent Kinase Inhibitor p27
  • Cyclins / metabolism
  • Ectodysplasins
  • Hypertension / complications*
  • Intracellular Signaling Peptides and Proteins
  • Isoenzymes / metabolism
  • Kidney / drug effects
  • Kidney / pathology
  • Kidney Diseases / etiology*
  • Macrophages / metabolism
  • Macrophages / pathology
  • Membrane Proteins / metabolism
  • Myosin-Light-Chain Phosphatase / metabolism
  • Nephrectomy / methods*
  • Phosphorylation / drug effects
  • Protein Kinase Inhibitors*
  • Protein Serine-Threonine Kinases / antagonists & inhibitors*
  • Proteinuria / urine
  • Rats
  • Rats, Inbred SHR
  • Tumor Suppressor Proteins / metabolism
  • rho-Associated Kinases

Substances

  • Cdkn1a protein, rat
  • Cdkn1b protein, rat
  • Cell Cycle Proteins
  • Cyclin-Dependent Kinase Inhibitor p21
  • Cyclins
  • Ectodysplasins
  • Intracellular Signaling Peptides and Proteins
  • Isoenzymes
  • Membrane Proteins
  • Protein Kinase Inhibitors
  • Tumor Suppressor Proteins
  • Cyclin-Dependent Kinase Inhibitor p27
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine
  • Protein Serine-Threonine Kinases
  • rho-Associated Kinases
  • Myosin-Light-Chain Phosphatase
  • fasudil