Effects of a selective glucocorticoid receptor agonist on experimental keratoplasty

Graefes Arch Clin Exp Ophthalmol. 2005 May;243(5):450-5. doi: 10.1007/s00417-004-0991-y. Epub 2005 Apr 9.

Abstract

Background: New insights into the molecular mechanisms of corticosteroid-mediated actions have revealed new substances, such as selective glucocorticoid receptor agonists (SEGRA), for the treatment of inflammatory diseases. We set out to evaluate the effect of a SEGRA compound following topical application on the course of experimental orthotopic corneal grafts.

Methods: A total of 42 female Lewis rats received 3.5-mm MHC I/II-incompatible corneal grafts from DA donors. Recipients were randomly assigned to receive either no therapy, 0.25% cyclodextrin-encapsulated SEGRA compound in a new microemulsion formulation or carrier system only. All treatments started on the day of surgery and were given five times daily for 35 days. Grafts were graded every day and a rejection score was generated based on cornea clarity and edema. In addition, intragraft mRNA expression of CD3, IFN-gamma, TNF-alpha, IL-10 and IL-4 was analyzed using real-time RT-PCR analysis at day 7 after transplantation before rejection occurred in additional control animals.

Results: Topical application of a SEGRA compound was highly effective in prolonging the mean survival time of corneal grafts (42.2+/-4.0 days) compared with untreated controls (11.7+/-1.2 days, p=0.00003) or animals that received the vehicle only (15.0+/-1.5 days, p=0.114). In addition, real-time RT-PCR analysis of SEGRA-treated grafts revealed lower mRNA expression of intragraft cytokines; the difference was significant for IL-4 (p<0.05).

Conclusions: Our results indicate that topical application of a SEGRA compound significantly prolongs corneal graft survival in an experimental keratoplasty model. It further suggests that SEGRA can be a potentially useful drug to suppress the immune response.

MeSH terms

  • Administration, Topical
  • Animals
  • CD3 Complex / genetics
  • CD3 Complex / metabolism
  • Cornea / metabolism
  • Cyclodextrins
  • Drug Carriers
  • Female
  • Graft Rejection / metabolism
  • Graft Rejection / prevention & control*
  • Graft Survival / drug effects*
  • Heterocyclic Compounds, 2-Ring / administration & dosage*
  • Hydrocarbons, Halogenated / administration & dosage*
  • Interferon-gamma / genetics
  • Interferon-gamma / metabolism
  • Interleukin-10 / genetics
  • Interleukin-10 / metabolism
  • Interleukin-4 / genetics
  • Interleukin-4 / metabolism
  • Keratoplasty, Penetrating*
  • RNA, Messenger / metabolism
  • Rats
  • Rats, Inbred Lew
  • Receptors, Glucocorticoid / agonists*
  • Reverse Transcriptase Polymerase Chain Reaction
  • Tumor Necrosis Factor-alpha / genetics
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • CD3 Complex
  • Cyclodextrins
  • Drug Carriers
  • Heterocyclic Compounds, 2-Ring
  • Hydrocarbons, Halogenated
  • RNA, Messenger
  • Receptors, Glucocorticoid
  • Tumor Necrosis Factor-alpha
  • Interleukin-10
  • Interleukin-4
  • Interferon-gamma