Inhibition of atopic dermatitis-like skin lesions by topical application of a novel ceramide derivative, K6PC-9p, in NC/Nga mice

Exp Dermatol. 2008 Nov;17(11):958-64. doi: 10.1111/j.1600-0625.2008.00737.x. Epub 2008 Aug 20.

Abstract

Atopic dermatitis (AD) is a chronic inflammatory skin disease that commonly begins in childhood. K6PC-9p (N-(Ethyl dihydrogenphosphate)-2-hexyl-3-oxo-decanamide) is a synthetic ceramide derivative of PC-9S (N-Ethanol-2-mirystyl-3-oxo-staramide), which was known to be effective in atopic patients. In this study, we examined the effect of topical application of K6PC-9p on skin inflammation and AD-like skin lesions in mouse models. K6PC-9p dose-dependently inhibited phorbol ester-induced increase in ear thickness in BALB/c mice. Moreover, topical application of K6PC-9p suppressed dust mite extract-induced AD-like skin lesions in NC/Nga mice. Histopathological analysis revealed that both ear swelling and leucocyte infiltration were suppressed by K6PC-9p treatment. K6PC-9p also suppressed IL-4 and TNF-alpha expression in the ears and mast cell infiltration into the ears in NC/Nga mice. Further study demonstrated that K6PC-9p inhibited ConA-induced IL-4 secretion and LPS-induced macrophage activation. Taken together, our results showed that topical application of K6PC-9p exerts beneficial effects in animal model of skin inflammation and AD, suggesting that K6PC-9p might be a promising topical agent for the treatment of inflammatory skin diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Topical
  • Animals
  • Antigens, Dermatophagoides / pharmacology
  • Cell Movement / drug effects
  • Cell Survival / drug effects
  • Ceramides / chemistry
  • Ceramides / therapeutic use*
  • Dermatitis, Atopic / pathology
  • Dermatitis, Atopic / prevention & control*
  • Dermatitis, Contact / etiology
  • Dermatitis, Contact / pathology
  • Dermatitis, Contact / prevention & control*
  • Disease Models, Animal
  • Ear, External / drug effects
  • Ear, External / metabolism
  • Ear, External / pathology
  • Female
  • Fibroblasts / cytology
  • Fibroblasts / drug effects
  • Gene Expression / drug effects
  • Humans
  • Hydrocortisone / administration & dosage
  • Hydrocortisone / therapeutic use
  • Interleukin-4 / genetics
  • Interleukin-4 / metabolism
  • Keratinocytes / cytology
  • Keratinocytes / drug effects
  • Macrophage Activation / drug effects
  • Mast Cells / cytology
  • Mast Cells / drug effects
  • Mice
  • Mice, Inbred BALB C
  • Mice, Inbred Strains
  • Reverse Transcriptase Polymerase Chain Reaction
  • Tetradecanoylphorbol Acetate / toxicity
  • Tumor Necrosis Factor-alpha / genetics
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Antigens, Dermatophagoides
  • Ceramides
  • Tumor Necrosis Factor-alpha
  • Interleukin-4
  • Tetradecanoylphorbol Acetate
  • Hydrocortisone