Zhu Hua, Zhong Xin
School of Chemistry and Chemical Engineering, Mianyang Teacher's College, Mianyang, China.
Dean's office, Mianyang Teacher's College, Mianyang, China.
Sci Rep. 2025 May 9;15(1):16212. doi: 10.1038/s41598-025-00047-w.
Essential oils derived from Eucalyptus globules Labill. (EGEOs) represent a significant class of bioactive metabolites with broad applications in medicinal and pharmaceutical industries. Despite their various biological activities, the potential of EGEOs to inhibit tyrosinase, a key enzyme in melanin biosynthesis, remains unexplored. Then, this study delineates the inhibitory effects of EGEOs on tyrosinase. Our findings indicated that EGEOs acted as one reversible and non-competitive inhibitor toward tyrosinase, presenting an inhibition rate of 59.6% (10 mg/ml). Circular dichroism (CD) spectral analysis suggested that EGEOs induced conformational changes in tyrosinase, potentially disrupting its catalytic function. The binding of EGEOs to tyrosinase, as evidenced by ANS binding assays, led to the exposure of hydrophobic regions within the enzyme, further impairing its activity. Molecular docking studies illustrated the specific interactions between the major metabolite of EGEOs, 1,8-cineole, and tyrosinase. Moreover, the impact of EGEOs on melanin production was assessed in B16F10 melanoma cells, demonstrating a significant reduction in intracellular melanin content upon EGEOs treatment. Collectively, these results suggested EGEOs as one promising natural tyrosinase inhibitor with potential applications in treating hyperpigmentation and associated skin disorders.
从蓝桉(Eucalyptus globules Labill.)中提取的挥发油(EGEOs)是一类重要的生物活性代谢产物,在医药和制药行业有广泛应用。尽管它们具有多种生物活性,但EGEOs抑制酪氨酸酶(黑色素生物合成中的关键酶)的潜力仍未得到探索。因此,本研究描述了EGEOs对酪氨酸酶的抑制作用。我们的研究结果表明,EGEOs对酪氨酸酶起可逆的非竞争性抑制剂作用,在浓度为10mg/ml时抑制率为59.6%。圆二色光谱(CD)分析表明,EGEOs诱导了酪氨酸酶的构象变化,可能破坏其催化功能。ANS结合试验证明,EGEOs与酪氨酸酶的结合导致酶内部疏水区域的暴露,进一步损害其活性。分子对接研究阐明了EGEOs的主要代谢产物1,8-桉叶素与酪氨酸酶之间的特定相互作用。此外,在B16F10黑色素瘤细胞中评估了EGEOs对黑色素生成的影响,结果表明EGEOs处理后细胞内黑色素含量显著降低。总的来说,这些结果表明EGEOs是一种有前景的天然酪氨酸酶抑制剂,在治疗色素沉着过度及相关皮肤疾病方面具有潜在应用价值。