Division of Applied Life Science (BK21 plus), IALS, Gyeongsang National University, Jinju 52828, Korea.
Division of Applied Life Science (BK21 plus), PMBBRC, Gyeongsang National University, Jinju 52828, Korea.
Molecules. 2020 May 18;25(10):2344. doi: 10.3390/molecules25102344.
Puerol A () from showed highly potent inhibition against both monophenolase (IC = 2.2 μM) and diphenolase (IC = 3.8 μM) of tyrosinase. We tried to obtain a full story of enzyme inhibitory behavior for inhibitor because the butenolide skeleton has never been reported as a tyrosinase inhibitor. Puerol A was proved as a reversible, competitive, simple slow-binding inhibitor, according to the respective parameters; = 0.0279 μM min and = 0.003 min. A longer lag-phase and a reduced static-state activity of the enzyme explained that puerol A had a tight formation of the complex with E. Dose-dependent inhibition was also confirmed by high-performance liquid chromatography (HPLC) analysis using -acetyl-l-tyrosine as a substrate, which was completely inhibited at 20 μM. A high binding affinity of to tyrosinase was confirmed by fluorescence quenching analysis. Moreover, puerol A decreased melanin content in the B16 melanoma cell dose-dependently with an IC of 11.4 μM.
来自 的紫堇醇 A () 对酪氨酸酶的单酚酶 (IC = 2.2 μM) 和二酚酶 (IC = 3.8 μM) 均显示出很强的抑制作用。我们试图获得抑制剂的完整酶抑制行为的故事，因为丁烯内酯骨架从未被报道为酪氨酸酶抑制剂。根据各自的参数，紫堇醇 A 被证明是一种可逆的、竞争性的、简单的慢结合抑制剂； = 0.0279 μM min 和 = 0.003 min。较长的滞后期和酶的静态活性降低表明，紫堇醇 A 与 E 形成了紧密的复合物。使用 -乙酰-l-酪氨酸作为底物的高效液相色谱 (HPLC) 分析也证实了剂量依赖性抑制，当浓度为 20 μM 时，该抑制剂完全被抑制。荧光猝灭分析证实了 对酪氨酸酶的高结合亲和力。此外，紫堇醇 A 以剂量依赖性方式降低 B16 黑色素瘤细胞中的黑色素含量，IC 为 11.4 μM。
