title: Membrane perturbation activity of cationic phenylene ethynylene oligomers and polymers: selectivity against model bacterial and mammalian membranes.
abstract: Poly(phenylene ethyneylene) (PPE)-based cationic conjugated polyelectrolytes (CPEs) and cationic phenylene ethynylene oligomers (OPEs) exhibit broad-spectrum antimicrobial activity, and their main target is believed to be the cell membrane. To understand better how these antimicrobial molecules interact with membranes, a series of PPE-based CPEs and OPEs with different side chains were studied. Large unilamellar vesicles with lipid compositions mimicking those of mammalian or bacterial membranes were used as model membranes. Among the CPEs and OPEs tested, the anionic CPE, PPE-SO(3)(2-) and the smallest cationic OPE-1 are inactive against all vesicles. Other cationic CPEs and OPEs show significant membrane perturbation ability against bacterial membrane mimics but are inactive against a mammalian cell membrane mimic with the exception of PPE-DABCO and two end-only-functionalized OPEs, which also disrupted a mammalian cell membrane mimic. The results suggest that the phospholipid composition of vesicles dominates the interaction of CPE and OPE with lipid membranes.
authors.affiliation: Department of Chemical and Nuclear Engineering, Center for Biomedical Engineering, University of New Mexico, Albuquerque, New Mexico 87131-1341, USA.
authors.forename: Ying
authors.initials: Y
authors.lastname: Wang
authors.forename: Yanli
authors.initials: Y
authors.lastname: Tang
authors.forename: Zhijun
authors.initials: Z
authors.lastname: Zhou
authors.forename: Eunkyung
authors.initials: E
authors.lastname: Ji
authors.forename: Gabriel P
authors.initials: GP
authors.lastname: Lopez
authors.forename: Eva Y
authors.initials: EY
authors.lastname: Chi
authors.forename: Kirk S
authors.initials: KS
authors.lastname: Schanze
authors.forename: David G
authors.initials: DG
authors.lastname: Whitten
mesh_terms: D000480:Alkynes / Q000737:chemistry*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D002412:Cations / Q000737:chemistry*; D002462:Cell Membrane / Q000737:chemistry* / Q000187:drug effects; D004987:Ethers / Q000737:chemistry*; D008322:Mammals; D011108:Polymers / Q000737:chemistry* / Q000494:pharmacology*; D053835:Unilamellar Liposomes / Q000737:chemistry*
chemical_list: D000480:Alkynes; D000900:Anti-Bacterial Agents; D002412:Cations; D004987:Ethers; D011108:Polymers; D053835:Unilamellar Liposomes; C436384:phenyleneethynylene