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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Evaluation of anti-pigmentary effect of synthetic sulfonylamino chalcone.
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Evaluation of anti-pigmentary effect of synthetic sulfonylamino chalcone.

机译:合成磺酰氨基查尔酮的抗色素沉着评价。

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摘要

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.
机译:相对于仅设计为酪氨酸酶活性的化合物,对具有α-葡萄糖苷酶和酪氨酸酶抑制化学型的4'-(对甲苯磺酰氨基)-4-羟基查尔酮(TSAHC)进行了酪氨酸酶活性和脱色能力的评估。 TSAHC已成为蘑菇酪氨酸酶的竞争性可逆抑制剂。更重要的是,与其他仅靶向酪氨酸酶的抑制剂不同,它还能够将由α-MSH刺激的α-黑色素细胞的黑色素含量恢复至基本水平。涉及黑色素生成的蛋白质表达水平的蛋白质印迹表明,TSAHC显着降低了黑色素生物合成中的三个主要的酪氨酸酶相关蛋白酪氨酸酶,TRP-1和TRP-2。

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