Suppression of skin inflammation in keratinocytes and acute/chronic disease models by caffeic acid phenethyl ester

Arch Dermatol Res. 2015 Apr;307(3):219-27. doi: 10.1007/s00403-014-1529-8. Epub 2014 Dec 12.

Abstract

Skin inflammation plays a central role in the pathophysiology and symptoms of diverse chronic skin diseases including atopic dermatitis (AD). In this study, we examined if caffeic acid phenethyl ester (CAPE), a skin-permeable bioactive compound from propolis, was protective against skin inflammation using in vitro cell system and in vivo animal disease models. CAPE suppressed TNF-α-induced NF-κB activation and expression of inflammatory cytokines in human keratinocytes (HaCaT). The potency and efficacy of CAPE were superior to those of a non-phenethyl derivative, caffeic acid. Consistently, topical treatment of CAPE (0.5 %) attenuated 12-O-tetradecanoylphorbol-13-acetate(TPA)-induced skin inflammation on mouse ear as CAPE reduced ear swelling and histologic inflammation scores. CAPE suppressed increased expression of pro-inflammatory molecules such as TNF-α, cyclooxygenase-2 and inducible NO synthase in TPA-stimulated skin. TPA-induced phosphorylation of IκB and ERK was blocked by CAPE suggesting that protective effects of CAPE on skin inflammation is attributed to inhibition of NF-κB activation. Most importantly, in an oxazolone-induced chronic dermatitis model, topical application of CAPE (0.5 and 1 %) was effective in alleviating AD-like symptoms such as increases of trans-epidermal water loss, skin thickening and serum IgE as well as histologic inflammation assessment. Collectively, our results propose CAPE as a promising candidate for a novel topical drug for skin inflammatory diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acute Disease
  • Animals
  • Caffeic Acids / administration & dosage*
  • Caffeic Acids / metabolism
  • Cell Line
  • Chronic Disease
  • Cyclooxygenase 2 / metabolism
  • Dermatitis, Atopic / drug therapy*
  • Dermatitis, Atopic / immunology
  • Disease Models, Animal
  • Humans
  • Immunoglobulin E / blood
  • Inflammation / chemically induced
  • Inflammation / drug therapy*
  • Inflammation / immunology
  • Keratinocytes / drug effects*
  • Keratinocytes / immunology
  • Mice
  • Mice, Inbred Strains
  • NF-kappa B / antagonists & inhibitors
  • Oxazolone / metabolism
  • Phenylethyl Alcohol / administration & dosage
  • Phenylethyl Alcohol / analogs & derivatives*
  • Phenylethyl Alcohol / metabolism
  • Propolis / metabolism
  • Skin / drug effects*
  • Skin / immunology
  • Skin / pathology
  • Tetradecanoylphorbol Acetate / metabolism
  • Tumor Necrosis Factor-alpha / immunology
  • Water Loss, Insensible / drug effects

Substances

  • Caffeic Acids
  • NF-kappa B
  • Tumor Necrosis Factor-alpha
  • Oxazolone
  • Immunoglobulin E
  • Propolis
  • Cyclooxygenase 2
  • caffeic acid phenethyl ester
  • Phenylethyl Alcohol
  • Tetradecanoylphorbol Acetate