Agents to control melanogenesis are in demand for the development of cosmetics to improve pigmentation disorders of skin and hair. In this study, we examined and evaluated the effects of flavonoids on melanogenesis in the melanogenic cells model, murine B16F10 melanoma cells. In the course of this study, we found that incubation of the cells in a medium containing 10 μM of the 4'-O-methylated flavonoids, diosmetin (4'-O-methylluteolin), acacetin (4'-O-methylapigenin) or kaempferide (4'-O-methylkaempferol), increased the melanin contents of the cells 3- to 7-fold higher than the control cells. The concentration-dependence test revealed that 20 μM acacetin showed the highest effect, up to 33-fold higher than the vehicle. On the other hand, the corresponding 4'-OH-type flavonoids, luteolin, apigenin and kaempferol, had a significantly smaller effect. Furthermore, by evaluating the melanogenic proteins, we found that the cells treated with 4'-O-methylated flavonoids showed higher tyrosinase activity, as well as upregulation of tyrosinase expression, preceded by activation of cAMP response element binding protein (CREB) and extracellular signal-regulated kinases types 1 and 2 (ERK1/2). These results indicate that the 4'-O-methyl group of flavonoids plays an important role in the induction of melanogenesis by activating its major signal transduction pathway through the upregulation of phospho-CREB in murine B16F10 melanoma cells.

译文

控制黑素生成的药物是化妆品开发的需求,以改善皮肤和头发的色素沉着疾病。在这项研究中,我们检查并评估了类黄酮对黑色素生成细胞模型鼠B16F10黑素瘤细胞中黑色素生成的影响。在这项研究的过程中,我们发现细胞在含有10μm的4 '-O-甲基化类黄酮,地奥美汀 (4'-O-methylluteolin),acacetin (4 '-O-methyapigenin) 或kaempferide (4'-O-methylameferol),使细胞的黑色素含量比对照细胞高3至7倍。浓度依赖性测试表明,20μm acacetin的效果最高,比媒介物高33倍。另一方面,相应的4 '-OH型类黄酮木犀草素,芹菜素和山奈酚的作用明显较小。此外,通过评估黑素蛋白,我们发现用4 '-O-甲基化类黄酮处理的细胞显示出更高的酪氨酸酶活性以及酪氨酸酶表达的上调,在激活cAMP反应元件结合蛋白 (CREB) 和细胞外信号调节激酶类型1和2 (ERK1/2) 之前。这些结果表明,类黄酮的4 '-O-甲基通过上调小鼠B16F10黑素瘤细胞的磷酸化CREB激活其主要信号转导途径,在黑素生成的诱导中起重要作用。

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