Melanin provides photoprotection against UV irradiation, but excessive melanin accumulation can cause several problems such as darkened skin, melasma, and freckles. Although many anti-melanogenic agents have been developed for skin-whitening cosmetics, safety issues have been raised regarding these products. As natural substances are often non-toxic and are considered by some to be safer than synthetic compounds, various attempts have been made to synthesize active derivatives from natural substances. In this study, we evaluated the anti-melanogenic effects of four synthesized derivatives (compound 2a, 2b, 2c, and 2d) of kojic and hydroxycinnamic acids which are natural anti-melanogenic substances. Three of these derivatives (2a, 2b, and 2c) inhibited tyrosinase, which catalyzes a rate-limiting step of melanogenesis. Additionally, cell viability and melanin formation were investigated using B16F10 melanoma cells. Compounds 2b and 2c exhibited cytotoxicity towards B16F10 melanoma cells, while compound 2a caused a significant decrease in melanin formation without cytotoxicity. Thus, compound 2a may be viable as a potent skin-whitening agent derived from natural compounds.

黑色素对紫外线的照射提供了光保护，但是黑色素的过多积聚会引起一些问题，例如皮肤变黑，黄褐斑和雀斑。尽管已经开发出许多用于皮肤增白化妆品的抗黑色素形成剂，但是关于这些产品已经提出了安全问题。由于天然物质通常是无毒的，并且被某些人认为比合成化合物更安全，因此人们进行了各种尝试来从天然物质合成活性衍生物。在这项研究中，我们评估了天然的抗黑素物质曲酸和羟基肉桂酸的四种合成衍生物（化合物2a，2b，2c和2d）的抗黑素作用。这些衍生物中的三个（2a，2b和2c）抑制了酪氨酸酶，催化了黑色素生成的限速步骤。另外，使用B16F10黑色素瘤细胞研究了细胞活力和黑色素形成。化合物2b和2c对B16F10黑色素瘤细胞表现出细胞毒性，而化合物2a导致黑色素形成显着减少，而无细胞毒性。因此，化合物2a作为衍生自天然化合物的有效的皮肤增白剂可能是可行的。