title: Effect of Relative Arrangement of Cationic and Lipophilic Moieties on Hemolytic and Antibacterial Activities of PEGylated Polyacrylates.
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.
authors.affiliation: Department of Chemistry and Center for Engineered Polymeric Materials, College of Staten Island, Staten Island, New York, NY 10016, USA. apunia@gradcenter.cuny.edu.|Ph. D. Program in Chemistry at the Graduate Center of the City University of New York, New York, NY 10016, USA. apunia@gradcenter.cuny.edu.
authors.forename: Ashish
authors.initials: A
authors.lastname: Punia
authors.affiliation: Department of Chemistry, Macaulay Honors College, New York, NY 10016, USA. kevin.lee@macaulay.cuny.edu.
authors.forename: Kevin
authors.initials: K
authors.lastname: Lee
authors.affiliation: Department of Chemistry, Macaulay Honors College, New York, NY 10016, USA. edward.he@macaulay.cuny.edu.
authors.forename: Edward
authors.initials: E
authors.lastname: He
authors.affiliation: Ph.D. Program in Biochemistry at the Graduate Center of the City University of New York, New York, NY 10016, USA. smukherjee@gradcenter.cuny.edu.
authors.forename: Sumit
authors.initials: S
authors.lastname: Mukherjee
authors.affiliation: Ph.D. Program in Biochemistry at the Graduate Center of the City University of New York, New York, NY 10016, USA. amancuso@gradcenter.cuny.edu.
authors.forename: Andrew
authors.initials: A
authors.lastname: Mancuso
authors.affiliation: Department of Chemistry and Center for Developmental Neuroscience, College of Staten Island, Staten Island, New York, NY 10016, USA. probal.banerjee@csi.cuny.edu.
authors.forename: Probal
authors.initials: P
authors.lastname: Banerjee
authors.affiliation: Department of Chemistry and Center for Engineered Polymeric Materials, College of Staten Island, Staten Island, New York, NY 10016, USA. nanloh.yang-cepm@csi.cuny.edu.|Ph. D. Program in Chemistry at the Graduate Center of the City University of New York, New York, NY 10016, USA. nanloh.yang-cepm@csi.cuny.edu.
authors.forename: Nan-Loh
authors.initials: NL
authors.lastname: Yang
mesh_terms: D000179:Acrylates / Q000737:chemistry / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D002412:Cations / Q000737:chemistry; D002473:Cell Wall / Q000187:drug effects; D024881:Drug Resistance, Bacterial; D004912:Erythrocytes / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects*; D006461:Hemolysis / Q000187:drug effects; D057927:Hydrophobic and Hydrophilic Interactions; D008826:Microbial Sensitivity Tests; D011092:Polyethylene Glycols / Q000737:chemistry / Q000494:pharmacology*; D011108:Polymers / Q000737:chemistry / Q000494:pharmacology; D011109:Polymethacrylic Acids / Q000737:chemistry; D013211:Staphylococcus aureus / Q000187:drug effects*; D013501:Surface-Active Agents / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000179:Acrylates; D000900:Anti-Bacterial Agents; D002412:Cations; D011108:Polymers; D011109:Polymethacrylic Acids; D013501:Surface-Active Agents; D011092:Polyethylene Glycols
keywords: PEGylated; amphiphilic polymers; antimicrobial polymers; bactericidal agents; drug-resistant bacteria; polyacrylates