Fasudil, a Rho-kinase inhibitor, attenuates glomerulosclerosis in Dahl salt-sensitive rats

J Hypertens. 2004 Sep;22(9):1787-96. doi: 10.1097/00004872-200409000-00024.

Abstract

Objective: The present study was designed to clarify whether the Rho-Rho-kinase pathway is involved in the process of hypertensive glomerulosclerosis and to assess the therapeutic effect of fasudil, a specific Rho-kinase inhibitor.

Method and results: Dahl salt-sensitive rats (DS) and Dahl salt-resistant rats (DR) were fed a high-salt diet at 6 weeks of age. Fasudil (30 mg/kg per day) was administered for 7 weeks to DS starting at the age of 11 weeks. After 7 weeks, untreated DS were characterized by decreased kidney function, increased proteinuria, abnormal morphological findings, increased adrenomedullin and atrial natriuretic peptide (ANP) levels, and increased renal messenger RNA expression of RhoB, Rho-kinasealpha, Rho-kinasebeta, collagen I and collagen III, and transforming growth factor-beta (TGF-beta) in the renal cortex compared with DR. Chronic fasudil treatment significantly improved renal function (serum creatinine, -26%; blood urea nitrogen, -41%; creatinine clearance, +42%), proteinuria (-24%) and histological findings (glomerular injury score, -49%; afferent arteriolar injury score, -17%) without changing blood pressure compared with untreated DS. Interestingly, long-term fasudil treatment decreased the plasma adrenomedullin (-25%) and ANP (-49%), but did not change the plasma renin or aldosterone. Furthermore, fasudil significantly decreased the messenger RNA expression of TGF-beta (-20%), collagen I (-23%), and collagen III (-24%) in the renal cortex. However, there were still significant differences in the aforementioned parameters between DR and fasudil-treated DS.

Conclusion: These results suggest that the Rho-Rho-kinase pathway may be partly responsible for the pathogenesis of hypertensive glomerulosclerosis independently of blood pressure in DS, and that chronic inhibition of the Rho-Rho-kinase pathway may be a new strategy for treating hypertensive nephrosclerosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / analogs & derivatives*
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / pharmacology*
  • Animals
  • Arterioles / pathology
  • Blood Pressure / drug effects
  • Blotting, Western
  • Collagen Type I / genetics
  • Collagen Type III / genetics
  • Glomerulosclerosis, Focal Segmental / drug therapy*
  • Glomerulosclerosis, Focal Segmental / pathology
  • Hypertension, Renal / drug therapy*
  • Hypertension, Renal / pathology
  • Hypertension, Renal / prevention & control
  • Intracellular Signaling Peptides and Proteins
  • Kidney Cortex / blood supply
  • Kidney Cortex / pathology
  • Kidney Cortex / physiology
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Serine-Threonine Kinases / antagonists & inhibitors*
  • Protein Serine-Threonine Kinases / genetics
  • RNA, Messenger / analysis
  • Rats
  • Rats, Inbred Dahl
  • Transforming Growth Factor beta / genetics
  • Transforming Growth Factor beta / metabolism
  • rho GTP-Binding Proteins / genetics
  • rho-Associated Kinases
  • rhoA GTP-Binding Protein / genetics
  • rhoB GTP-Binding Protein / genetics

Substances

  • Collagen Type I
  • Collagen Type III
  • Intracellular Signaling Peptides and Proteins
  • Protein Kinase Inhibitors
  • RNA, Messenger
  • Transforming Growth Factor beta
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine
  • Protein Serine-Threonine Kinases
  • rho-Associated Kinases
  • rho GTP-Binding Proteins
  • rhoA GTP-Binding Protein
  • rhoB GTP-Binding Protein
  • fasudil