CIRMAP - Centre d'Innovation et de Recherche en Matériaux Polymères CISMA - Centre Interdisciplinaire de Spectrométrie de Masse
Disciplines :
Chemistry
Author, co-author :
MOHY EL DINE'S, Tharwat
Jimmidi, Ravikumar
Diaconu, Andrei
FRANSOLET, Maude
MICHIELS, Carine
De Winter, Julien ; Université de Mons > Faculté des Sciences > Service de Synthèse et spectrométrie de masse organiques
GILLON, Emilie
IMBERTY, Anne
COENYE, Tom
Vincent, Stéphane
Language :
English
Title :
Pillar[5]arene-Based Polycationic Glyco[2]rotaxanes Designed as Pseudomonas aeruginosa Antibiofilm Agents
Publication date :
20 September 2021
Journal title :
Journal of Medicinal Chemistry
ISSN :
0022-2623
eISSN :
1520-4804
Publisher :
American Chemical Society, United States - District of Columbia
Volume :
64
Issue :
19
Pages :
14728-14744
Peer reviewed :
Peer Reviewed verified by ORBi
Research unit :
S816 - Matériaux Polymères et Composites S836 - Synthèse et spectrométrie de masse organiques
Research institute :
R400 - Institut de Recherche en Science et Ingénierie des Matériaux R100 - Institut des Biosciences
Commentary :
[en] Pseudomonas aeruginosa (P.A.) is a human pathogen belonging to the top priorities for the discovery of new
therapeutic solutions. Its propensity to generate biofilms strongly complicates the treatments required to cure P.A. infections. Herein,
we describe the synthesis of a series of novel rotaxanes composed of a central galactosylated pillar[5]arene, a tetrafucosylated
dendron, and a tetraguanidinium subunit. Besides the high affinity of the final glycorotaxanes for the two P.A. lectins LecA and LecB,
potent inhibition levels of biofilm growth were evidenced, showing that their three subunits work synergistically. An antibiofilm assay
using a double ΔlecAΔlecB mutant compared to the wild type demonstrated that the antibiofilm activity of the best glycorotaxane is
lectin-mediated. Such antibiofilm potency had rarely been reached in the literature. Importantly, none of the final rotaxanes was
bactericidal, showing that their antibiofilm activity does not depend on bacteria killing, which is a rare feature for antibiofilm agents.
