title: Cationic lipids: molecular structure/ transfection activity relationships and interactions with biomembranes.
abstract: Abstract Synthetic cationic lipids, which form complexes (lipoplexes) with polyanionic DNA, are presently the most widely used constituents of nonviral gene carriers. A large number of cationic amphiphiles have been synthesized and tested in transfection studies. However, due to the complexity of the transfection pathway, no general schemes have emerged for correlating the cationic lipid chemistry with their transfection efficacy and the approaches for optimizing their molecular structures are still largely empirical. Here we summarize data on the relationships between transfection activity and cationic lipid molecular structure and demonstrate that the transfection activity depends in a systematic way on the lipid hydrocarbon chain structure. A number of examples, including a large series of cationic phosphatidylcholine derivatives, show that optimum transfection is displayed by lipids with chain length of approximately 14 carbon atoms and that the transfection efficiency strongly increases with increase of chain unsaturation, specifically upon replacement of saturated with monounsaturated chains.
authors.affiliation: Ohio State University College of Pharmacy, 517 Parks Hall, 500 W 12th Ave, Columbus, OH 43210, USA. rkoynova@gmail.com
authors.forename: Rumiana
authors.initials: R
authors.lastname: Koynova
authors.forename: Boris
authors.initials: B
authors.lastname: Tenchov
mesh_terms: D002412:Cations / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D008055:Lipids / Q000138:chemical synthesis / Q000737:chemistry*; D015394:Molecular Structure; D009696:Nucleic Acids / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D014162:Transfection
chemical_list: D002412:Cations; D008055:Lipids; D009696:Nucleic Acids