小眼畸形相关转录因子
酪氨酸酶
黑色素
蛋白激酶B
MAPK/ERK通路
皮肤美白
磷酸化
类黄酮
PI3K/AKT/mTOR通路
p38丝裂原活化蛋白激酶
免疫印迹
生物
药理学
信号转导
化学
生物化学
抗氧化剂
酶
基因
活性成分
作者
Horng‐Huey Ko,Yu-Ting Chiang,Ming-Horng Tsai,Cher‐Wei Liang,Lee-Fen Hsu,Shuyu Li,Moo–Chin Wang,Feng‐Lin Yen,Chiang‐Wen Lee
标识
DOI:10.1016/j.jep.2013.10.054
摘要
In hyperpigmentation disorders marked by melanin overproduction in the skin, including melisma and freckles, melanogenesis is caused by tyrosinase overexpression. Natural medicinal resources, like Phyla nodiflora, a traditional Chinese herbal medicine, have been used for a long time to management of dermatological conditions, such as skin inflammation and melanogenesis. Eupafolin, a functional flavonoid isolated from Phyla nodiflora, is an herbal tea constituent and possesses anti-inflammatory and anticancer activities. However, molecular mechanisms of eupafolin-mediated antimelanogenesis remain unknown. We thus focused on its antimelanogenesis effects in B16F10 mouse melanoma cells. B16F10 cells were treated with eupafolin (0.01, 0.1, 1, and 10 μM) in a dose-escalation-dependent manner for the determination of melanin, tyrosinase activity and melanogenesis protein levels by ELISA or western blot analysis. Eupafolin treatment significantly reduced cellular melanin content and tyrosinase activity in a dose-dependent manner (P<0.05), and no cytotoxic effects were observed. Eupafolin was associated with reduction in the levels of phospho-cAMP response element-binding protein and microphthalmia-associated transcription factor (MITF), and downregulation of tyrosinase synthesis and tyrosinase-related protein expression, leading to inhibit melanin production. In addition, eupafolin significantly induced the phosphorylation of ERK1/2 and p38 MAPK, whereas the decreased effect was observed in the phosphorylation of Akt. Moreover, inhibitors of these signals recovered or attenuated the inhibitory effects of eupafolin on melanogenesis. Our results seem that inhibition of Akt and activation of phospho-ERK or p38 MAPK may lead to the suppression of melanogenesis in eupafolin-treated B16F10 mouse melanoma cells.
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