Premium
Motuporamine Derivatives as Antimicrobial Agents and Antibiotic Enhancers against Resistant Gram‐Negative Bacteria
Author(s) -
Borselli Diane,
Blanchet Marine,
Bolla JeanMichel,
Muth Aaron,
Skruber Kristen,
Phanstiel Otto,
Brunel Jean Michel
Publication year - 2017
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201600532
Subject(s) - efflux , enterobacter aerogenes , antimicrobial , antibiotics , bacteria , gram negative bacteria , chemistry , antibiotic resistance , depolarization , in vitro , microbiology and biotechnology , biochemistry , biophysics , biology , escherichia coli , genetics , gene
Dihydromotuporamine C and its derivatives were evaluated for their in vitro antimicrobial activities and antibiotic enhancement properties against Gram‐negative bacteria and clinical isolates. The mechanism of action of one of these derivatives, MOTU‐N44, was investigated against Enterobacter aerogenes by using fluorescent dyes to evaluate outer‐membrane depolarization and permeabilization. Its efficiency correlated with inhibition of dye transport, thus suggesting that these molecules inhibit drug transporters by de‐energization of the efflux pump rather than by direct interaction of the molecule with the pump. This suggests that depowering the efflux pump provides another strategy to address antibiotic resistance.