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Int. J. Mol. Sci. 2015, 16(10), 23867-23880; doi:10.3390/ijms161023867

Effect of Relative Arrangement of Cationic and Lipophilic Moieties on Hemolytic and Antibacterial Activities of PEGylated Polyacrylates

1
Department of Chemistry and Center for Engineered Polymeric Materials, College of Staten Island, Staten Island, New York, NY 10016, USA
2
Ph. D. Program in Chemistry at the Graduate Center of the City University of New York, New York, NY 10016, USA
3
Department of Chemistry, Macaulay Honors College, New York, NY 10016, USA
4
Ph.D. Program in Biochemistry at the Graduate Center of the City University of New York, New York, NY 10016, USA
5
Department of Chemistry and Center for Developmental Neuroscience, College of Staten Island, Staten Island, New York, NY 10016, USA
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Academic Editors: Antonella Piozzi and Iolanda Francolini
Received: 6 September 2015 / Revised: 28 September 2015 / Accepted: 29 September 2015 / Published: 9 October 2015
(This article belongs to the Special Issue Antimicrobial Polymers 2016)
View Full-Text   |   Download PDF [1464 KB, uploaded 9 October 2015]   |  

Abstract

Synthetic amphiphilic polymers have been established as potentially efficient agents to combat widespread deadly infections involving antibiotic resistant superbugs. Incorporation of poly(ethylene glycol) (PEG) side chains into amphiphilic copolymers can reduce their hemolytic activity while maintaining high antibacterial activity. Our study found that the incorporation of PEG has substantially different effects on the hemolytic and antibacterial activities of copolymers depending on structural variations in the positions of cationic centers relative to hydrophobic groups. The PEG side chains dramatically reduced the hemolytic activities in copolymers with hydrophobic hexyl and cationic groups on the same repeating unit. However, in case of terpolymers with cationic and lipophilic groups placed on separate repeating units, the presence of PEG has significantly lower effect on hemolytic activities of these copolymers. PEGylated terpolymers displayed substantially lower activity against Staphylococcus aureus (S. aureus) than Escherichia coli (E. coli) suggesting the deterring effect of S. aureus’ peptidoglycan cell wall against the penetration of PEGylated polymers. Time-kill studies confirmed the bactericidal activity of these copolymers and a 5 log reduction in E. coli colony forming units was observed within 2 h of polymer treatment. View Full-Text
Keywords: antimicrobial polymers; amphiphilic polymers; polyacrylates; drug-resistant bacteria; PEGylated; bactericidal agents antimicrobial polymers; amphiphilic polymers; polyacrylates; drug-resistant bacteria; PEGylated; bactericidal agents
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MDPI and ACS Style

Punia, A.; Lee, K.; He, E.; Mukherjee, S.; Mancuso, A.; Banerjee, P.; Yang, N.-L. Effect of Relative Arrangement of Cationic and Lipophilic Moieties on Hemolytic and Antibacterial Activities of PEGylated Polyacrylates. Int. J. Mol. Sci. 2015, 16, 23867-23880.

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