Department of Pharmaceutical Engineering, Sangji University, 83 Sangjidae-gil, Wonju 26339, Korea.
Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA, Eumseong 27709, Korea.
Molecules. 2022 Sep 4;27(17):5703. doi: 10.3390/molecules27175703.
The enzyme tyrosinase plays a key role in the early stages of melanin biosynthesis. This study evaluated the inhibitory activity of anthocyanidin () and anthocyanins (-) on the catalytic reaction. Of the six derivatives examined, - showed inhibitory activity with IC values of 3.7 ± 0.1, 10.3 ± 1.0, and 41.3 ± 3.2 μM, respectively. Based on enzyme kinetics, - were confirmed to be competitive inhibitors with values of 2.8, 9.0, and 51.9 μM, respectively. Molecular docking analysis revealed the formation of a binary encounter complex between - and the tyrosinase catalytic site. Luteolinidin () and petunidin 3--glucoside () may serve as tyrosinase inhibitors to block melanin production.
酶酪氨酸酶在黑色素生物合成的早期阶段发挥关键作用。本研究评估了花色苷（）和花色苷（-）对催化反应的抑制活性。在所检查的六种衍生物中，-显示出抑制活性，IC 值分别为 3.7±0.1、10.3±1.0 和 41.3±3.2 μM。基于酶动力学，-被确认为竞争性抑制剂， 值分别为 2.8、9.0 和 51.9 μM。分子对接分析表明，-与酪氨酸酶催化部位形成二元遭遇复合物。木犀草素（）和锦葵色素 3--葡萄糖苷（）可能作为酪氨酸酶抑制剂阻断黑色素生成。
