Synergistic Activity of Hydrophilic Modification in Antibiotic Polymers

Sellenet, Philippe H; Allison, Bradley C.; Applegate, Bruce; Youngblood, Jeffrey P.

doi:10.1021/bm0605513

Cited by 121 publications

(109 citation statements)

References 25 publications

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“…Efforts to turn these biocidal polymers into selective AMMs is underway in at least a few laboratories. [49,68,231] Scientifically, the control of physicochemical properties and biological activities is an important challenge. It also appears there is significant practical impact for antimicrobial molecules that limit the spread of infectious disease.…”

Section: Discussionmentioning

confidence: 99%

Infectious disease: Connecting innate immunity to biocidal polymers

Gabriel

Som

Madkour

et al. 2007

Materials Science and Engineering: R: Reports

253

258

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Infectious disease is a critically important global healthcare issue. In the U.S. alone there are 2 million new cases of hospital-acquired infections annually leading to 90,000 deaths and 5 billion dollars of added healthcare costs. Couple these numbers with the appearance of new antibiotic resistant bacterial strains and the increasing occurrences of community-type outbreaks, and clearly this is an important problem. Our review attempts to bridge the research areas of natural host defense peptides (HDPs), a component of the innate immune system, and biocidal cationic polymers. Recently discovered peptidomimetics and other synthetic mimics of HDPs, that can be short oligomers as well as polymeric macromolecules, provide a unique link between these two areas. An emerging class of these mimics are the facially amphiphilic polymers that aim to emulate the physicochemical properties of HDPs but take advantage of the synthetic ease of polymers. These mimics have been designed with antimicrobial activity and, importantly, selectivity that rivals natural HDPs. In addition to providing some perspective on HDPs, selective mimics, and biocidal polymers, focus is given to the arsenal of biophysical techniques available to study their mode of action and interactions with phospholipid membranes. The issue of lipid type is highlighted and the important role of negative curvature lipids is illustrated. Finally, materials applications (for instance, in the development of permanently antibacterial surfaces) are discussed as this is an important part of controlling the spread of infectious disease.

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Section: Discussionmentioning

confidence: 99%

Infectious disease: Connecting innate immunity to biocidal polymers

Gabriel

Som

Madkour

et al. 2007

Materials Science and Engineering: R: Reports

253

258

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“…For this reason iodide counter anion of QA-PEI nanoparticles was exchanged with nitrate ion using precipitation method with AgNO 3 and with acetate using 1 N acetic acid solution. QA-PEI nanoparticles were characterized prior and following exchange reaction for their iodine (%I) content, apparent particle size (ALV, nm), and zeta potential as shown in [29]. For this reason QA-PEI was modified with increasing amounts of MPEG (Scheme 1(c)).…”

Section: Antibacterial Activity Of Qa-pei Nanoparticles As a Functionmentioning

confidence: 99%

Quaternary Ammonium Polyethyleneimine: Antibacterial Activity

Yudovin-Farber

Golenser

Beyth

et al. 2010

Journal of Nanomaterials

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Quaternary ammonium polyethyleneimine-(QA-PEI-) based nanoparticles were synthesized using two synthetic methods, reductive amination and N-alkylation. According to the first method, QA-PEI nanoparticles were synthesized by cross-linking with glutaraldehyde followed by reductive amination with octanal and further N-methylation with methyl iodide. The second method is based on crosslinking with dialkyl halide followed by N-alkylation with octyl halide and further N-methylation with methyl iodide. QA-PEI nanoparticles completely inhibited bacterial growth (>10 6 bacteria), including both Gram-positive, that is, Staphylococcus aureus at 80 μg/mL, and Gram-negative, that is, Escherichia coli at 320 μg/mL. Activity analysis revealed that the degree of alkylation and N-methylation of the QA-PEI nanoparticles plays a significant role in antibacterial activity of the reagent. The most potent compound was octyl alkylated QA-PEI alkylated at 1 : 1 mole ratio (primary amine of PEI monomer units/alkylating agent). Also, cytotoxicity studies on MAT-LyLu and MBT cell lines were performed with QA-PEI nanoparticles. These findings confirm previous reports that polycations bearing quaternary ammonium moieties inhibit bacterial growth in vitro and have a potential use as additives in medical devices which need antibacterial properties.

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“…Specifically, they are limited because they can cause irritation to skin and are well-known biocides. [20] In most cases, only antibacterial activity was reported without any studies on hemolytic activity (or activity against other mammalian cells [21] ). Here we report the antibacterial and hemolytic activity of quaternary pyridinium functionalized polynorbornenes.…”

Section: Introductionmentioning

confidence: 99%

Antibacterial and Hemolytic Activities of Quaternary Pyridinium Functionalized Polynorbornenes

Eren

Som

Rennie

et al. 2008

Macro Chemistry & Physics

147

163

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In this study, amphiphilic polyoxanorbornene with different quaternary alkyl pyridinium side chains were synthesized. The biological efficiencies of these polymers, with various alkyl substituents, were determined by bacterial growth inhibition assays and hemolytic activity (HC 50 ) against human red blood cells (RBCs) to provide selectivity of these polymers for bacterial over mammalian cells. A series of polymers with different alkyl substituents (ethyl, butyl, hexyl, octyl, decyl and phenylethyl) and two different molecular weights (3 and 10 kDa) were prepared. The impact of alkyl chain length divided the biological activity into two different cases: those with an alkyl substituent containing four or fewer carbons had a minimum inhibitory concentration (MIC) of 200 mg Á mL À1 and a HC 50 greater than 1 650 mg Á mL À1 , while those with six or more carbons had lower MICs 12.5 mg Á mL À1 and HC 50 250 mg Á mL À1 . Using MSI-78, the potent Magainin derivative which has an MIC ¼ 12.0 mg Á mL À1 and HC 50 ¼ 120 mg Á mL À1 , as a comparison, the polymers with alkyl substituents C 4 (four carbons) were not very potent, but did show selectivity values greater than or equal to MSI-78. In contrast, those with alkyl substituents !C 6 were as potent, or more potent, than MSI-78 and in three specific cases demonstrated selectivity values similar to, or better than, MSI-78. To understand if these polymers were membrane active, polymer induced lipid membrane disruption activities were evaluated by dye leakage experiments. Lipid composition and polymer hydrophobicity were found to be important factors for dye release.

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Synergistic Activity of Hydrophilic Modification in Antibiotic Polymers

Cited by 121 publications

References 25 publications

Infectious disease: Connecting innate immunity to biocidal polymers

Infectious disease: Connecting innate immunity to biocidal polymers

Quaternary Ammonium Polyethyleneimine: Antibacterial Activity

Antibacterial and Hemolytic Activities of Quaternary Pyridinium Functionalized Polynorbornenes

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