Department of Functional Crop, NICS, RDA, Miryang 627-803, Republic of Korea.
Eur J Med Chem. 2010 May;45(5):2010-7. doi: 10.1016/j.ejmech.2010.01.049. Epub 2010 Jan 28.
The 4'-(p-toluenesulfonylamino)-4-hydroxychalcone (TSAHC), which bears inhibitory chemotypes for both alpha-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 alpha-melanocyte stimulated by alpha-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.
4'-(对甲苯磺酰氨基)-4-羟基查耳酮（TSAHC）具有抑制α-葡萄糖苷酶和酪氨酸酶的化学结构，其酪氨酸酶活性和美白能力已被评估，与仅针对酪氨酸酶活性设计的化合物相比。TSAHC 被证明是一种竞争性可逆的蘑菇酪氨酸酶抑制剂。更重要的是，它还能够使α-MSH 刺激的α-黑素细胞的黑色素含量恢复到基础水平，而不像其他仅针对酪氨酸酶的抑制剂。参与黑色素生成的蛋白质表达水平的 Western blot 显示，TSAHC 显著降低了黑色素生物合成中三个主要的与酪氨酸酶相关的蛋白质，即酪氨酸酶、TRP-1 和 TRP-2。
