Wu Yan, Wu Zheng-Rong, Chen Peng, Deng Wan-Rong, Wang You-Quan, Li Hong-Yu
Gansu College of Traditional Chinese Medicine, 35 Dingxi East Road, Lanzhou 730000, People's Republic of China.
School of Pharmaceutics, Lanzhou University, 222 Tian Shui South Road, Lanzhou 730000, People's Republic of China.
Bioorg Med Chem Lett. 2015 Apr 1;25(7):1476-8. doi: 10.1016/j.bmcl.2015.02.028. Epub 2015 Feb 19.
In our searching for novel tyrosinase inhibitors from natural sources, (S)-N-trans-feruloyloctopamine isolated from garlic skin was found to be a potential mushroom tyrosinase inhibitor. Here, we examined the effects of the potential tyrosinase inhibitor in B16F10 cells on intracellular melanin contents, cytotoxicity, and the signaling mechanism involved in the expression of tyrosinase. The results showed the inhibitor displayed little or no cytotoxicity at all concentrations examined and decreased the relative melanin contents in a dose-dependent manner in the α-MSH-stimulated B16F10 cells. Real-time PCR and Western blot analysis showed that it inhibits melanogenesis signaling by down-regulates mRNA and protein expression levels of tyrosinase, which leads to a lower melanin contents. These results suggested that (S)-N-trans-feruloyloctopamine was an ideal tyrosinase inhibitor, and could be used in food and medical industry.
在我们从天然来源寻找新型酪氨酸酶抑制剂的过程中，从蒜皮中分离出的（S）-N-反式阿魏酰章鱼胺被发现是一种潜在的蘑菇酪氨酸酶抑制剂。在此，我们研究了这种潜在的酪氨酸酶抑制剂在B16F10细胞中对细胞内黑色素含量、细胞毒性以及酪氨酸酶表达所涉及的信号传导机制的影响。结果表明，在所有检测浓度下，该抑制剂几乎没有细胞毒性，并且在α-MSH刺激的B16F10细胞中以剂量依赖的方式降低了相对黑色素含量。实时PCR和蛋白质印迹分析表明，它通过下调酪氨酸酶的mRNA和蛋白质表达水平来抑制黑色素生成信号传导，从而导致黑色素含量降低。这些结果表明，（S）-N-反式阿魏酰章鱼胺是一种理想的酪氨酸酶抑制剂，可用于食品和医药行业。
