대한화장품학회:학술대회논문집 (Proceedings of the SCSK Conference)
- 대한화장품학회 2003년도 IFSCC Conference Proceeding Book I
- /
- Pages.268-284
- /
- 2003
Di-acetyl-nor-aporphines: Novel molecules and a novel mechanism to inhibit melanogenesis
- Lintner, Karl (Sederma, 29 rue du Chemin Vert, 78612 Le Perray) ;
- Peschard, Olivier (Sederma, 29 rue du Chemin Vert, 78612 Le Perra) ;
- Leroux, Richard (Sederma, 29 rue du Chemin Vert, 78612 Le Perra) ;
- Mondon, Philippe (Sederma, 29 rue du Chemin Vert, 78612 Le Perra) ;
- Lamy, Francois (Sederma, 29 rue du Chemin Vert, 78612 Le Perray)
- 발행 : 2003.09.01
초록
Nor-aporphine derivatives have been discovered which interfere with the flux of Calcium into and out of the cell interior. It has been shown that adrenergic antagonists that block the Calcium exchange lead to an inhibition of Protein kinase C activity, thus blocking tyrosinase activation. Di-acetyl-dimethoxy-methyl-nor-aporphine is a semi-synthetic molecule of natural origin with very high potency. On B16 melanocytes as well as in normal human melanocytes the decrease in melanin synthesis reaches -50% at a level of 40 ppm in the culture medium. On a molar concentration basis, this is 50 to 70 times stronger than Kojic acid inhibition. Yet, the cell viability is not affected. Reversibility studies show that after washing out of the active compound, melanogenesis returns to normal levels. Possible mechanisms of the activity are discussed. Tests carried out on SkinEthic(R) three-dimensional models of the epidermis and in vivo clinical studies on Asian population confirm the strong inhibition of melanogenesis. Safety evaluation of these molecules, on the other hand, demonstrates good skin tolerance and absence of toxicity.