Please use this identifier to cite or link to this item: https://doi.org/10.1128/AAC.00469-17
Title: Antimicrobial activity and cell selectivity of synthetic and biosynthetic cationic polymers
Authors: Venkatesh, M
Barathi, V.A 
Goh, E.T.L
Anggara, R
Fazil, M.H.U.T
Ng, A.J.Y
Harini, S
Aung, T.T
Fox, S.J
Liu, S 
Yang, L
Barkham, T.M.S 
Loh, X.J 
Verma, N.K
Beuerman, R.W 
Lakshminarayanan, R 
Keywords: allylamine
antiinfective agent
aziridine
benzalkonium chloride
chlorhexidine
epsilon polylysine
guanidine
polyethyleneimine
polylysine
polymer
tobramycin
unclassified drug
allylamine
antiinfective agent
antimicrobial cationic peptide
aziridine derivative
polyethyleneimine
polylysine
polymer
animal experiment
animal model
antimicrobial activity
Article
bacterial keratitis
bacterial strain
bactericidal activity
biocompatibility
biofilm
cell membrane
controlled study
cornea
cornea injury
fibroblast
fungus
Gram negative bacterium
Gram positive bacterium
human
human cell
in vivo study
nonhuman
priority journal
Pseudomonas infection
Staphylococcus infection
wound closure
animal
Candida albicans
candidiasis
cell line
chemistry
disease model
drug effect
keratitis
Leporidae
microbial sensitivity test
microbiology
Pseudomonas aeruginosa
Pseudomonas infection
Staphylococcus aureus
Staphylococcus infection
Allylamine
Animals
Anti-Bacterial Agents
Antimicrobial Cationic Peptides
Aziridines
Candida albicans
Candidiasis
Cell Line
Cell Membrane
Disease Models, Animal
Fibroblasts
Humans
Keratitis
Microbial Sensitivity Tests
Polyethyleneimine
Polylysine
Polymers
Pseudomonas aeruginosa
Pseudomonas Infections
Rabbits
Staphylococcal Infections
Staphylococcus aureus
Issue Date: 2017
Publisher: American Society for Microbiology
Citation: Venkatesh, M, Barathi, V.A, Goh, E.T.L, Anggara, R, Fazil, M.H.U.T, Ng, A.J.Y, Harini, S, Aung, T.T, Fox, S.J, Liu, S, Yang, L, Barkham, T.M.S, Loh, X.J, Verma, N.K, Beuerman, R.W, Lakshminarayanan, R (2017). Antimicrobial activity and cell selectivity of synthetic and biosynthetic cationic polymers. Antimicrobial Agents and Chemotherapy 61 (10). ScholarBank@NUS Repository. https://doi.org/10.1128/AAC.00469-17
Rights: Attribution 4.0 International
Abstract: The mammalian and microbial cell selectivity of synthetic and biosynthetic cationic polymers has been investigated. Among the polymers with peptide backbones, polymers containing amino side chains display greater antimicrobial activity than those with guanidine side chains, whereas ethylenimines display superior activity over allylamines. The biosynthetic polymer ε-polylysine (εPL) is noncytotoxic to primary human dermal fibroblasts at concentrations of up to 2,000 μg/ml, suggesting that the presence of an isopeptide backbone has greater cell selectivity than the presence of α-peptide backbones. Both εPL and linear polyethylenimine (LPEI) exhibit bactericidal properties by depolarizing the cytoplasmic membrane and disrupt preformed biofilms. εPL displays broad-spectrum antimicrobial properties against antibiotic-resistant Gram-negative and Gram-positive strains and fungi. εPL elicits rapid bactericidal activity against both Gram-negative and Gram-positive bacteria, and its biocompatibility index is superior to those of cationic antiseptic agents and LPEI. εPL does not interfere with the wound closure of injured rabbit corneas. In a rabbit model of bacterial keratitis, the topical application of εPL (0.3%, wt/vol) decreases the bacterial burden and severity of infections caused by Pseudomonas aeruginosa and Staphylococcus aureus strains. In vivo imaging studies confirm that εPL-treated corneas appeared transparent and nonedematous compared to untreated infected corneas. Taken together, our results highlight the potential of εPL in resolving topical microbial infections. © 2017 Venkatesh et al.
Source Title: Antimicrobial Agents and Chemotherapy
URI: https://scholarbank.nus.edu.sg/handle/10635/179258
ISSN: 0066-4804
DOI: 10.1128/AAC.00469-17
Rights: Attribution 4.0 International
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