Fiche publication


Date publication

janvier 2018

Journal

ACS medicinal chemistry letters

Auteurs

Membres identifiés du Cancéropôle Est :
Dr VANDERESSE Régis


Tous les auteurs :
Le Guern F, Ouk TS, Ouk C, Vanderesse R, Champavier Y, Pinault E, Sol V

Résumé

In order to highlight the potential of photodynamic antimicrobial chemotherapy in case of infections by antibiotic resistant-strains, a new antimicrobial peptide conjugate has been synthesized, consisting of a derivative of polymyxin B and a cationic porphyrin covalently attached together to a spacer. A polymyxin-derived moiety was subjected to a primary structural modification in the replacement of four diaminobutyrate residues with lysine ones. This modification was done in order to strongly reduce bactericidal activity, with the aim to eliminate the potential rise of polymyxin-resistant strains. Despite this modification, this new conjugate displayed a strong photobactericidal activity against Gram-positive as well as Gram-negative bacteria. It was further shown that this conjugate was able to strongly stick to the cell walls of either kind of strain, thus helping to inactivate bacteria through the production of reactive oxygen species under light irradiation.

Référence

ACS Med Chem Lett. 2018 Jan 11;9(1):11-16