| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1396531 | European Journal of Medicinal Chemistry | 2017 | 8 Pages |
The 4′-(p-toluenesulfonylamino)-4-hydroxychalcone (TSAHC), which bears inhibitory chemotypes for both α-glucosidase and tyrosinase, was evaluated for tyrosinase activity and depigmenting ability relative to compounds designed to only target tyrosianse activity. TSAHC emerged to be a competitive reversible inhibitor of mushroom tyrosinase. More importantly, it was also able to return the melanin content of α-melanocyte stimulated by α-MSH to base levels unlike other inhibitors that only targeted tyrosinase. The Western blot for expression levels of proteins involved in melanogenesis showed that TSAHC significantly decreased three main tyrosinase related protein in melanin biosynthesis, tyrosinase, TRP-1 and TRP-2.
Graphical abstractThe sulfonylamino chalcone deriviatives were synthesized, characterized and evaluated for depigmenting effects.Figure optionsDownload full-size imageDownload as PowerPoint slide
