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Article Dans Une Revue Journal of Medicinal Chemistry Année : 2014

Antiadhesive properties of glycoclusters against Pseudomonas aeruginosa lung infection.

Emilie Gillon
  • Fonction : Auteur
Stéphane Havet
  • Fonction : Auteur
Benoît Darblade
  • Fonction : Auteur
Susan E Matthews
  • Fonction : Auteur
Sophie de Bentzmann
  • Fonction : Auteur
Anne Imberty

Résumé

Pseudomonas aeruginosa lung infections are a major cause of death in cystic fibrosis and hospitalized patients. Treating these infections is becoming difficult due to the emergence of conventional antimicrobial multiresistance. While monosaccharides have proved beneficial against such bacterial lung infection, the design of several multivalent glycosylated macromolecules has been shown to be also beneficial on biofilm dispersion. In this study, calix[4]arene-based glycoclusters functionalized with galactosides or fucosides have been synthesized. The characterization of their inhibitory properties on Pseudomonas aeruginosa aggregation, biofilm formation, adhesion on epithelial cells, and destruction of alveolar tissues were performed. The antiadhesive properties of the designed glycoclusters were demonstrated through several in vitro bioassays. An in vivo mouse model of lung infection provided an almost complete protection against Pseudomonas aeruginosa with the designed glycoclusters.

Domaines

Chimie organique
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Dates et versions

hal-01147368 , version 1 (30-04-2015)

Identifiants

Citer

Amine M. Boukerb, Audric Rousset, Nicolas Galanos, Jean-Baptiste Méar, Marion Thépaut, et al.. Antiadhesive properties of glycoclusters against Pseudomonas aeruginosa lung infection.. Journal of Medicinal Chemistry, 2014, 57 (24), pp.10275-10289. ⟨10.1021/jm500038p⟩. ⟨hal-01147368⟩
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