Laboratory of Semi-Arid Bioprospecting (Lab-Bioprospec), Department of Biological Chemistry, DQB/URCA, Crato, Ceará, Brazil.
Laboratory of Microbiology and Molecular Biology (LMBM), Department of Biological Chemistry, DQB/URCA, Crato, Ceará, Brazil.
J Bioenerg Biomembr. 2021 Apr;53(2):157-167. doi: 10.1007/s10863-021-09886-4. Epub 2021 Mar 8.
The objective of this work was to evaluate the inhibitory effect of quercetin on S. aureus Efflux Pumps. The MIC of Quercetin was evaluated through the broth microdilution method, as well as the Efflux Pump inhibition assay through the method of reducing the antibiotic minimum inhibitory concentration as well as that of ethidium bromide. The in silico approach through bioinformatics was performed to demonstrate the molecular mechanism of interaction of the substrate and the binding cavity. The Quercetin inhibition concentration was not clinically relevant. With respect to the reversal of bacterial resistance effect by efflux pump inhibition, this effect was observed with the strains carrying the TetK and NorA pumps. Regarding the interaction between the Quercetin complex and the NorA pump, the extra stability was provided by hydrogen bonds produced by the hydroxyl group.
本工作旨在评估槲皮素对金黄色葡萄球菌外排泵的抑制作用。通过肉汤微量稀释法评估槲皮素的 MIC,以及通过降低抗生素最小抑菌浓度和溴化乙锭的外排泵抑制试验来评估。通过生物信息学的计算方法来证明底物和结合腔的相互作用的分子机制。槲皮素的抑制浓度与临床无关。关于外排泵抑制逆转细菌耐药性的效果,在携带 TetK 和 NorA 泵的菌株中观察到这种效果。关于槲皮素配合物与 NorA 泵之间的相互作用,通过羟基产生的氢键提供了额外的稳定性。