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Inhibitory Potential of Quercetin Derivatives Isolated from the Aerial Parts of Siegesbeckia pubescens Makino against Bacterial Neuraminidase.


ABSTRACT: This study aimed to isolate bacterial neuraminidase (BNA) inhibitory O-methylated quercetin derivatives from the aerial parts of S. pubescens. All the isolated compounds were identified as O-methylated quercetin (1-4), which were exhibited to be noncompetitive inhibitors against BNA, with IC50 ranging from 14.0 to 84.1 μM. The responsible compounds (1-4) showed a significant correlation between BNA inhibitory effects and the number of O-methyl groups on quercetin; mono (1, IC50 = 14.0 μM) > di (2 and 3, IC50 = 24.3 and 25.8 μM) > tri (4, IC50 = 84.1 μM). In addition, the binding affinities between BNA and inhibitors (1-4) were also examined by fluorescence quenching effect with the related constants (KSV, KA, and n). The most active inhibitor 1 possessed a KSV with 0.0252 × 105 L mol-1. Furthermore, the relative distribution of BNA inhibitory O-methylated quercetins (1-4) in S. pubescens extract was evaluated using LC-Q-TOF/MS analysis.

SUBMITTER: Son YG 

PROVIDER: S-EPMC10386613 | biostudies-literature | 2023 Jul

REPOSITORIES: biostudies-literature

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Inhibitory Potential of Quercetin Derivatives Isolated from the Aerial Parts of <i>Siegesbeckia pubescens</i> Makino against Bacterial Neuraminidase.

Son Yun Gon YG   Kim Ju Yeon JY   Park Jae Yeon JY   Kim Kwang Dong KD   Park Ki Hun KH   Kim Jeong Yoon JY  

Molecules (Basel, Switzerland) 20230712 14


This study aimed to isolate bacterial neuraminidase (BNA) inhibitory O-methylated quercetin derivatives from the aerial parts of <i>S. pubescens</i>. All the isolated compounds were identified as O-methylated quercetin (<b>1</b>-<b>4</b>), which were exhibited to be noncompetitive inhibitors against BNA, with IC<sub>50</sub> ranging from 14.0 to 84.1 μM. The responsible compounds (<b>1</b>-<b>4</b>) showed a significant correlation between BNA inhibitory effects and the number of O-methyl groups  ...[more]

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