曲酸
化学
酪氨酸酶
MTT法
黑色素
细胞毒性
立体化学
体外
生物化学
酶
作者
Gerhard Schmaus,Gabriele Vielhaber,Karin Jacobs,Helge Franke
标识
DOI:10.1111/j.1467-2494.2007.00355_6.x
摘要
There is an increasing world‐wide demand for skin lightening active ingredients. Many common lightening ingredients on the market are either unsafe or ineffective at low concentrations. We therefore screened a series of hydroxy‐stilbene derivatives for tyrosinase inhibitory activity. By chemical synthesis, the structures were optimized for efficacy and stability. The final candidate, 4‐(1‐phenylethyl)1,3‐benzenediol, was found to be stable and to inhibit mushroom tyrosinase 22 times more effectively than kojic acid. In an assay with B16V melanoma cells, 4‐(1‐phenylethyl)1,3‐benzenediol was the most potent inhibitor of melanin synthesis with an IC 50 of 2 μM among the compounds investigated. The lightening effect of 4‐(1‐phenylethyl)1,3‐benzenediol was not due to cytotoxicity as proved by an MTT assay on B16V cells. On pigmented 3D epidermis models, 0.1% of 4‐(1‐phenylethyl)1,3‐benzenediol led to an almost complete suppression of melanin synthesis after 14 days of incubation. Finally, an in vivo test on Asian subjects proved that 4‐(1‐phenylethyl)1,3‐benzenediol efficiently lightens human skin at 0.5% dosage. Optimal results are achieved when 4‐(1‐phenylethyl)1,3‐benzenediol is applied in formulations with low oil content. In summary, we have demonstrated that 4‐(1‐phenylethyl)1,3‐benzenediol is a potent, stable and safe skin lightener.
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