Enalaprilat directly ameliorates in vitro cyclosporin nephrotoxicity in human tubulo-interstitial cells

Nephron. 2000 Dec;86(4):473-81. doi: 10.1159/000045837.

Abstract

Background/aims: Several recent studies have suggested that angiotensin-converting enzyme (ACE) inhibitors ameliorate chronic cyclosporin A (CyA) tubulo-interstitial disease by mechanisms independent of their antihypertensive effects. The aim of the present study was to determine whether ACE inhibition exerts a direct beneficial effect on the tubulo-interstitium in an in vitro model of chronic CyA nephropathy.

Methods: Primary cultures of human proximal tubular cells (PTC) and renal cortical fibroblasts (CF) were exposed for 24 h to CyA in the presence or absence of enalaprilat. Parameters of tubulo-interstitial nephrotoxicity were then measured including collagen synthesis (proline incorporation), tubular viability and function (thymidine incorporation, lactate dehydrogenase release, and apical sodium-hydrogen exchange), and secretion of insulin-like growth factor I, transforming growth factor beta 1 (TGFbeta1), and platelet-derived growth factor.

Results: CyA promoted CF collagen synthesis, PTC cytotoxicity (suppressed viability, growth and sodium transport), and tubulo-interstitial fibrogenic cytokine release (CF secretion of insulin-like growth factor I and PTC secretion of TGFbeta1 and platelet-derived growth factor). Enalaprilat completely reversed the stimulatory effects of CyA on CF collagen synthesis (CyA + enalaprilat 6.40 +/- 0.50% vs. CyA alone 8.33 +/- 0.56% vs. control 6.57 +/- 0.62% vs. enalaprilat alone 5.55 +/- 0.93%, p < 0.05) and PTC secretion of TGFbeta1 (0.71 +/- 0.11, 1.13 +/- 0.09, 0.89 +/- 0.07, and 0.67 +/- 0.09 ng/mg protein/day, respectively, p < 0.05). However, the other manifestations of CyA toxicity were not significantly reversed by concomitant enalaprilat administration.

Conclusions: ACE inhibition directly prevents CyA-induced interstitial fibrosis, but not proximal tubule cytotoxicity, independently of haemodynamic and systemic renin-angiotensin system effects. Renoprotection may be partially afforded by directly preventing the tubular secretion of TGFbeta1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiotensin II / metabolism
  • Angiotensin-Converting Enzyme Inhibitors / pharmacology*
  • Cell Division / drug effects
  • Cell Survival / drug effects
  • Cells, Cultured
  • Collagen / biosynthesis
  • Culture Media, Conditioned
  • Cyclosporine / antagonists & inhibitors*
  • Cyclosporine / toxicity
  • Cytokines / biosynthesis
  • Enalaprilat / pharmacology*
  • Fibroblasts
  • Humans
  • Immunosuppressive Agents / antagonists & inhibitors*
  • Immunosuppressive Agents / toxicity
  • Kidney Cortex / cytology
  • Kidney Tubules, Proximal / pathology
  • Nephritis, Interstitial / chemically induced
  • Nephritis, Interstitial / pathology
  • Nephritis, Interstitial / prevention & control*

Substances

  • Angiotensin-Converting Enzyme Inhibitors
  • Culture Media, Conditioned
  • Cytokines
  • Immunosuppressive Agents
  • Angiotensin II
  • Cyclosporine
  • Collagen
  • Enalaprilat