a School of Life Sciences , Xiamen University , Xiamen , China.
J Enzyme Inhib Med Chem. 2019 Dec;34(1):990-998. doi: 10.1080/14756366.2019.1609467.
The novel kojic acid derivatives KAD1 and KAD2 have been demonstrated that they exhibited potent anti-melanogenesis activity in our previous report. In this study, we further study the inhibitory mechanism on mushroom tyrosinase. The inhibitory types of both KADs on diphenolase were classified as mixed type based on the results of the kinetic model. The interaction between KADs and tyrosinase was illustrated by fluorescence quenching, molecular docking and copper chelate activity. The KADs were also evaluated with respect to their antioxidant activities by DPPH and ABTS assays. The results showed that KADs have more potent antioxidant activities than kojic acid. Our study could provide new ideas for the development of new anti-tyrosinase and antioxidant agents.
我们之前的报告表明，新型曲酸衍生物 KAD1 和 KAD2 具有很强的抗黑色素生成活性。在本研究中，我们进一步研究了其对蘑菇酪氨酸酶的抑制机制。根据动力学模型的结果，两种 KAD 对二酚酶的抑制类型均被归类为混合型。通过荧光猝灭、分子对接和铜螯合活性来阐明 KAD 与酪氨酸酶的相互作用。还通过 DPPH 和 ABTS 测定法评估了 KADs 的抗氧化活性。结果表明，KADs 比曲酸具有更强的抗氧化活性。我们的研究为开发新型酪氨酸酶抑制剂和抗氧化剂提供了新的思路。
