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Biochemical Characterization of Ferulic Acid and Caffeic Acid Which Effectively Inhibit Melanin Synthesis via Different Mechanisms in B16 Melanoma Cells
Biological and Pharmaceutical Bulletin Pub Date : 2018-05-01 , DOI: 10.1248/bpb.b17-00892
Hiroko Maruyama 1 , Fumitaka Kawakami 2 , Thet-Thet Lwin 3 , Motoki Imai 1 , Fazel Shamsa 4
Affiliation  

In this study, we examined the inhibitory effects of ferulic acid and caffeic acid on melanin production using a murine B16 melanoma cell line. The mechanisms by which the two acids inhibit melanin production were investigated by evaluating their effects on the activity of tyrosinase, which is involved is the first step of melanin biosynthesis. Ferulic acid showed no toxicity against the melanoma cells at any dose, whereas caffeic acid exerted cellular toxicity at concentrations higher than 0.35 mM. Both ferulic and caffeic acids effectively inhibited melanin production in the B16 melanoma cells. Ferulic acid reduced tyrosinase activity by directly binding to the enzyme, whereas no binding was observed between caffeic acid and tyrosinase. Both ferulic acid and caffeic acid inhibited casein kinase 2 (CK2)-induced phosphorylation of tyrosinase in a dose-dependent manner in vitro. Ferulic acid was found to be a more effective inhibitor of melanin production than caffeic acid; this difference in the inhibitory efficacy between the two substances could be attributable to the difference in their tyrosine-binding activity. Our analysis revealed that both substances also inhibited the CK2-mediated phosphorylation of tyrosinase.

中文翻译:

阿魏酸和咖啡酸的生化特性,可通过不同的机制有效抑制B16黑色素瘤细胞中黑色素的合成

在这项研究中,我们使用鼠B16黑色素瘤细胞系研究了阿魏酸和咖啡酸对黑色素生成的抑制作用。通过评估它们对酪氨酸酶活性的影响,研究了这两种酸抑制黑色素生成的机制,这是黑色素生物合成的第一步。阿魏酸在任何剂量下均未显示出对黑素瘤细胞的毒性,而咖啡酸在高于0.35 mM的浓度下具有细胞毒性。阿魏酸和咖啡酸均可有效抑制B16黑色素瘤细胞中黑色素的产生。阿魏酸通过直接结合酶而降低了酪氨酸酶的活性,而在咖啡酸和酪氨酸酶之间未观察到结合。阿魏酸和咖啡酸在体外均以剂量依赖性方式抑制酪蛋白激酶2(CK2)诱导的酪氨酸酶磷酸化。阿魏酸被发现比咖啡酸更有效地抑制黑色素的产生。两种物质之间抑制功效的差异可能归因于其酪氨酸结合活性的差异。我们的分析表明,这两种物质也均抑制CK2介导的酪氨酸酶磷酸化。
更新日期:2018-05-01
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