The effect of Malononitrilamides (FK778) on phenotypic properties of human peripheral dendritic cells

Transplant Proc. 2009 Jun;41(5):1859-61. doi: 10.1016/j.transproceed.2009.02.068.

Abstract

Background: FK778, a malononitrilamide analogue of lefunomide, is currently a promising immunosuppressive drug. Because the cellular and molecular mechanisms underlying the effects of FK778 are not entirely clarified. We studied its effects on human peripheral dendritic cells.

Methods: Peripheral blood mononuclear cells (PBMC) from 12 healthy volunteers were isolated by density separation over Ficoll solution. After resuspension in adaptive immunotherapy medium (AIM)-V medium, they were cultured without exogenous growth factors. The study group was treated with FK 778 (50 microg/mL) or Rapamycin (10 ng/mL). The phenotype of dendritic cell was ascertained by indirect immunoflurescence for analysis by flow cytometry.

Results: Compared with the Rapamycin-treated controls, the expressions of CD80, CD83, CD86, HLA-DA, CD54, CD62, CCR5, and CCR7 in the FK778-treated myeloid dendritic cells and the expression of CD80, CD83, CD86, HLA-DA, and CD54 in the FK778-treated plasmacytoid dendritic cells were significantly down-regulated.

Conclusion: FK778 inhibited the differentiation and maturation of dendritic cells.

MeSH terms

  • Adjuvants, Immunologic / pharmacology
  • Alkynes / pharmacology*
  • Antigens, CD / drug effects
  • Antigens, CD / immunology
  • Cell Differentiation / drug effects
  • Cell Survival / drug effects
  • Cells, Cultured
  • Dendritic Cells / cytology*
  • Dendritic Cells / drug effects
  • Dendritic Cells / immunology*
  • Flow Cytometry
  • Humans
  • Isoxazoles / pharmacology*
  • Leflunomide
  • Nitriles / pharmacology*
  • Phenotype
  • Reference Values
  • Sirolimus / pharmacology

Substances

  • Adjuvants, Immunologic
  • Alkynes
  • Antigens, CD
  • Isoxazoles
  • Nitriles
  • 2-cyano-3-hydroxy-N-(4-(trifluoromethyl)phenyl)-2-hepten-6-ynamide
  • Leflunomide
  • Sirolimus