Ebselen is a new skin depigmenting agent that inhibits melanin biosynthesis and melanosomal transfer

Exp Dermatol. 2012 Jan;21(1):19-24. doi: 10.1111/j.1600-0625.2011.01394.x. Epub 2011 Nov 15.

Abstract

We assessed the ability of ebselen, a glutathione peroxidase mimic, to reduce pigmentation in various models. In murine B16 melanocytes, 25 μm ebselen inhibited melanogenesis and induced a depolymerisation of actin filaments. In co-cultures of B16 melanocytes with BDVII keratinocytes, a pretreatment of melanocytes with ebselen resulted in a strong inhibition of melanosome transfer to keratinocytes, as shown under optical and electron microscopy. In reconstructed epidermis, topical 0.5% ebselen led to a twofold decrease of melanin without affecting the density of active melanocytes. A similar result was obtained with topical 0.5% ebselen in black guinea pig ears. Ebselen induced a decrease of epidermal melanin parallel to a localisation of melanin and melanosomes in the basal layer. Ebselen appears as a new depigmenting compound that inhibits melanin synthesis and melanosome transfer to keratinocytes.

MeSH terms

  • Actin Cytoskeleton / drug effects
  • Animals
  • Antioxidants / pharmacology*
  • Azoles / pharmacology*
  • Cell Line
  • Cell Survival
  • Coculture Techniques
  • Ear, External
  • Female
  • Guinea Pigs
  • Humans
  • Isoindoles
  • Keratinocytes / drug effects
  • Keratinocytes / ultrastructure
  • Melanins / biosynthesis*
  • Melanocytes / drug effects
  • Melanocytes / ultrastructure
  • Melanosomes / drug effects*
  • Mice
  • Microscopy, Electron
  • Microtubules / drug effects
  • Monophenol Monooxygenase / metabolism
  • Organoselenium Compounds / pharmacology*
  • Skin Pigmentation / drug effects*

Substances

  • Antioxidants
  • Azoles
  • Isoindoles
  • Melanins
  • Organoselenium Compounds
  • ebselen
  • Monophenol Monooxygenase