Arbutin, a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses whitening and anticancer properties. The effects of arbutin on melanogenesis and its pro-apoptotic effect on B16 murine melanoma cells have not yet been reported. In the present study, acetylated arbutin was prepared in order to improve the biological effects of arbutin, and it was found to significantly inhibit the biosynthesis of melanin and tyrosinase activity compared with parent arbutin in B16 murine melanoma cells. Interestingly, only acetylated arbutin strongly inhibited B16 murine melanoma cell migration in a dose-dependent manner. Both arbutin and acetylated arbutin significantly reduced cell viability, promoted cell apoptosis, caused G1 cell cycle arrest and induced mitochondrial disruption in B16 murine melanoma cells. Furthermore, reduced expression of B-cell lymphoma‑extra large (Bcl-xL) and Bcl-2 were observed in arbutin- and acetylated arbutin-treated cells. Therefore, arbutin and acetylated arbutin were found to exert pro-apoptotic effects on B16 murine melanoma cells, mediated through the mitochondrial pathway. The findings of the present study also support the use of acetylated arbutin as a new potential candidate agent for skin whitening and melanoma treatment.

中文翻译：

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熊果素及其乙酰化衍生物对小鼠黑色素瘤细胞促凋亡作用的研究。

熊果素是一种从熊果植物Arctostaphylos uvaursi中分离出来的天然多酚，具有美白和抗癌的特性。尚未报道熊果苷对黑素生成的作用及其对B16鼠黑素瘤细胞的促凋亡作用。在本研究中，制备乙酰化熊果素是为了改善熊果素的生物学作用，并且发现它与亲本熊果素相比在B16鼠黑素瘤细胞中显着抑制黑色素的生物合成和酪氨酸酶活性。有趣的是，仅乙酰化熊果苷以剂量依赖性方式强烈抑制B16鼠黑色素瘤细胞迁移。熊果素和乙酰化熊果素均显着降低细胞活力，促进细胞凋亡，引起G1细胞周期停滞并诱导B16鼠黑素瘤细胞发生线粒体破坏。此外，在熊果素和乙酰化熊果素处理过的细胞中观察到B细胞淋巴瘤过大（Bcl-xL）和Bcl-2的表达降低。因此，发现通过线粒体途径介导的熊果素和乙酰化熊果素对B16鼠黑色素瘤细胞具有促凋亡作用。本研究的发现也支持使用乙酰化熊果苷作为美白和黑色素瘤治疗的新的潜在候选药物。