Department of Pharmaceutical Engineering, Institute of Agricultural and Life Science (IALS), Anti-Aging Bio Cell Factory Regional Leading Research Center (ABC-RLRC), Gyeongsang National University, Jinju 52725, Republic of Korea.
Division of Applied Life Science (BK21 Four), Institute of Agricultural and Life Science (IALS), Anti-Aging Bio Cell Factory Regional Leading Research Center (ABC-RLRC), Gyeongsang National University, Jinju 52828, Republic of Korea.
Molecules. 2023 Jul 12;28(14):5365. doi: 10.3390/molecules28145365.
This study aimed to isolate bacterial neuraminidase (BNA) inhibitory O-methylated quercetin derivatives from the aerial parts of . All the isolated compounds were identified as O-methylated quercetin (-), which were exhibited to be noncompetitive inhibitors against BNA, with IC ranging from 14.0 to 84.1 μM. The responsible compounds (-) showed a significant correlation between BNA inhibitory effects and the number of O-methyl groups on quercetin; mono (, IC = 14.0 μM) > di ( and , IC = 24.3 and 25.8 μM) > tri (, IC = 84.1 μM). In addition, the binding affinities between BNA and inhibitors (-) were also examined by fluorescence quenching effect with the related constants (, , and ). The most active inhibitor possessed a with 0.0252 × 10 L mol. Furthermore, the relative distribution of BNA inhibitory O-methylated quercetins (-) in extract was evaluated using LC-Q-TOF/MS analysis.
本研究旨在从 的地上部分中分离出具有抑制细菌神经氨酸酶 (BNA) 活性的 O-甲基化槲皮素衍生物。所有分离得到的化合物均被鉴定为 O-甲基化槲皮素 (-)，它们对 BNA 的抑制作用呈非竞争性，IC 范围为 14.0 至 84.1 μM。负责的化合物 (-) 显示出 BNA 抑制作用与槲皮素上 O-甲基化基团的数量之间存在显著相关性；单 (，IC = 14.0 μM) > 二 ( 和 ，IC = 24.3 和 25.8 μM) > 三 (，IC = 84.1 μM)。此外，还通过荧光猝灭效应研究了 BNA 与抑制剂 (-) 之间的结合亲和力，并得到了相关常数 (，，和 )。最具活性的抑制剂 具有 0.0252 × 10 L mol 的 。此外，还通过 LC-Q-TOF/MS 分析评估了 提取物中具有抑制 BNA 活性的 O-甲基化槲皮素 (-) 的相对分布。
