RT Journal Article
T1 Screening of Bacterial Quorum Sensing Inhibitors in a Vibrio fischeri LuxR-Based Synthetic Fluorescent E. coli Biosensor
A1 Qin, Xiaofei
A1 Vila Sanjurjo, Celina
A1 Singh, Ratna
A1 Philipp, Bodo
A1 Goycoolea, Francisco M.
K1 Compounds screening
K1 Quorum sensing inhibition
K1 Antibacterial
K1 Molecular docking
AB A library of 23 pure compounds of varying structural and chemical characteristics was screened for their quorum sensing (QS) inhibition activity using a synthetic fluorescent Escherichia coli biosensor that incorporates a modified version of lux regulon of Vibrio fischeri. Four such compounds exhibited QS inhibition activity without compromising bacterial growth, namely, phenazine carboxylic acid (PCA), 2-heptyl-3-hydroxy-4-quinolone (PQS), 1H-2-methyl-4-quinolone (MOQ) and genipin. When applied at 50 µM, these compounds reduced the QS response of the biosensor to 33.7% ± 2.6%, 43.1% ± 2.7%, 62.2% ± 6.3% and 43.3% ± 1.2%, respectively. A series of compounds only showed activity when tested at higher concentrations. This was the case of caffeine, which, when applied at 1 mM, reduced the QS to 47% ± 4.2%. In turn, capsaicin, caffeic acid phenethyl ester (CAPE), furanone and polygodial exhibited antibacterial activity when applied at 1mM, and reduced the bacterial growth by 12.8% ± 10.1%, 24.4% ± 7.0%, 91.4% ± 7.4% and 97.5% ± 3.8%, respectively. Similarly, we confirmed that trans-cinnamaldehyde and vanillin, when tested at 1 mM, reduced the QS response to 68.3% ± 4.9% and 27.1% ± 7.4%, respectively, though at the expense of concomitantly reducing cell growth by 18.6% ± 2.5% and 16% ± 2.2%, respectively. Two QS natural compounds of Pseudomonas aeruginosa, namely PQS and PCA, and the related, synthetic compounds MOQ, 1H-3-hydroxyl-4-quinolone (HOQ) and 1H-2-methyl-3-hydroxyl-4-quinolone (MHOQ) were used in molecular docking studies with the binding domain of the QS receptor TraR as a target. We offer here a general interpretation of structure-function relationships in this class of compounds that underpins their potential application as alternatives to antibiotics in controlling bacterial virulence
PB MDPI
YR 2020
FD 2020
LK http://hdl.handle.net/10347/23631
UL http://hdl.handle.net/10347/23631
LA eng
NO Qin, X.; Vila-Sanjurjo, C.; Singh, R.; Philipp, B.; Goycoolea, F.M. Screening of Bacterial Quorum Sensing Inhibitors in a Vibrio fischeri LuxR-Based Synthetic Fluorescent E. coli Biosensor. Pharmaceuticals 2020, 13, 263
NO X.Q. was recipient of a fellowship from China Scholarship Council. CVS was supported by a pre-doctoral fellowship of the Xunta de Galicia and by a FPU fellowship of the ‘‘Ministerio de Educación y Ciencia” of Spain, by a research fellowship of the DAAD (Germany), and research fellowship of the Fundación Pedro Barrié de la Maza (Spain). We acknowledge support from D.F.G., Germany (Project GRK 1549 International Research Training Group ‘Molecular and Cellular GlycoSciences’); the research leading to these results has also received funding from the European Union’s Seventh Framework Programme for research, technological development and demonstration under grant agreement no. 613931. We are also indebted to Antje von Schaewen for generous access to the Safire Tecan-F129013 Microplate Reader
DS Minerva
RD 4 may 2026