Abstract：
Brassinin is a phytoalexin abundant in plants, especially in cabbage, and has been reported to act as an anti-cancer and anti-inflammatory agent. However, limited studies are available to elucidate the functionalities of brassinin. Here, we tested the effects of brassinin on melanogenesis using cell-free and cell-based biochemical analysis and docking simulation. Cell-free experiments exhibited that brassinin has antioxidant and anti-tyrosinase activities. When applied to B16F10 cells stimulated with a melanogenesis inducer α-MSH, brassinin pretreatment significantly reduced melanin accumulation and cellular tyrosinase activity. Docking simulation indicates that the docking score of brassinin to the binding pocket of tyrosinase is better than that of kojic acid or arbutin, anti-melanogenic positive controls, indicating that brassinin inhibits melanogenesis at least partially by binding to and inactivating tyrosinase. In addition, qPCR results showed that brassinin reduced tyrosinase mRNA levels. Together, these results suggest that brassinin exerts anti-melanogenesis effects by inhibiting both the activity and mRNA expression levels of tyrosinase. Therefore, our study showed that brassinin has the potential to be used in pharmaceutical or cosmetic products for depigmentation.
摘要：
油菜素是一种在植物中含量丰富的植物抗毒素，尤其是卷心菜，并已被报道作为抗癌和抗炎剂。然而,有限的研究可用于阐明油菜素的功能。这里,我们使用无细胞和基于细胞的生化分析和对接模拟测试了油菜素对黑素生成的影响。无细胞实验表明，油菜素具有抗氧化和抗酪氨酸酶活性。当应用于黑素生成诱导剂α-MSH刺激的B16F10细胞时，油菜素预处理显着降低黑色素积累和细胞酪氨酸酶活性。对接模拟表明，油菜素与酪氨酸酶结合袋的对接得分优于曲酸或熊果苷。抗黑色素生成阳性对照，表明油菜素至少部分通过结合酪氨酸酶并使其失活来抑制黑素生成。此外,qPCR结果显示油菜素降低酪氨酸酶mRNA水平。一起,这些结果表明，油菜素通过抑制酪氨酸酶的活性和mRNA表达水平发挥抗黑素生成作用。因此,我们的研究表明，油菜素有可能被用于药物或化妆品的脱色。
