Lichens are evolutionary conserved symbiotic organisms of fungi and algae. These poorly studied organisms develop and survive under harsh climate including UV-exposure. Lichens present various colours: white, black red according to the species and metabolite localizations. Researchers made the hypothesis that lichens may produce original compounds that may modulate pigmentation.
Extract from the lichen, Cetraria islandica was proved to modulate pigmentation. One active molecule has been identified to down regulate pigmentation. It is a unique lichen structure : aliphatic lactone.
This aliphatic lactone can be synthetized in 7 steps. Starting from this active compound, derived molecules have been synthetized in an enantioselective manner. Two of them induce higher depigmentation. These tests have been performed using pigmented cell lines (MNT1, B16) and cultured human skin explants (Nativskin® ).
No toxicity have been detected
Depigmentation effect was higher than the one induced by control molecules (hydroquinone, arbutin) with a 20% reduction of the melanin content.
Electronic microscopy imaging demonstrate that the molecule acts on melanosomes, the melanin producing organelle. Structure/function analysis predicts that this molecule may interact with a melanosomal receptor.
- Natural derivative
- Better activity than hydroquinone (reference molecule)
- No toxicity
- IC50 = 1 microM
- Chemical synthesis of the compound: 7 steps (3 weeks)
- Possible biotechnological production
- Health market: Melasma, Vitiligo (softening the colour contrast)
- Cosmetic market: Skin lightening cream, skin discoloration
Stade de développement
IN VIVO - Preuve de concept
Laboratoire de recherche
UMR 6290 - IGDR
Équipe de recherche
Equipe Expression des Gènes et Oncogenèse (GEO)
Propriété intellectuelle associée
FR : FR1253585 - filed on the 04-18-2012
WO - BE,DE,EP,FR,GB,IT,JP,US