title: Folate-equipped pegylated archaeal lipid derivatives: synthesis and transfection properties.
abstract: We have previously shown that synthetic archaeal lipid analogues are useful vectors for drug/gene delivery. We report herein the synthesis and gene transfer properties of a series of novel di- and tetraether-type archaeal derivatives with a poly(ethylene glycol) (PEG) chain and further equipped with a folic acid (FA) group. The synthetic strategy and the purification by dialysis ensured complete removal of free FA. The lipids were mixed with a conventional glycine betaine-based cationic lipid and the resulting formulations were tested in transfection assays after complexation with plasmid DNA. All four novel co-lipids afforded efficient in vitro gene transfection. Moreover, the FA-equipped derivatives permitted ligand/receptor-based targeted transfection; their activity was inhibited when free FA was added to the transfection medium. These novel archaeal derivatives equipped with FA-PEG moieties may thus be of great interest for targeted in vivo transfection.
authors.affiliation: Ecole Nationale Supérieure de Chimie de Rennes, UMR CNRS 6226, Equipe Chimie Organique et Supramoléculaire, Av. Général Leclerc, 35700 Rennes, France.
authors.forename: Céline
authors.initials: C
authors.lastname: Lainé
authors.forename: Emmanuel
authors.initials: E
authors.lastname: Mornet
authors.forename: Loïc
authors.initials: L
authors.lastname: Lemiègre
authors.forename: Tristan
authors.initials: T
authors.lastname: Montier
authors.forename: Sandrine
authors.initials: S
authors.lastname: Cammas-Marion
authors.forename: Cécile
authors.initials: C
authors.lastname: Neveu
authors.forename: Nathalie
authors.initials: N
authors.lastname: Carmoy
authors.forename: Pierre
authors.initials: P
authors.lastname: Lehn
authors.forename: Thierry
authors.initials: T
authors.lastname: Benvegnu
mesh_terms: D001105:Archaea / Q000737:chemistry; D004247:DNA / Q000737:chemistry; D005492:Folic Acid / Q000737:chemistry* / Q000235:genetics; D017930:Genes, Reporter; D005822:Genetic Vectors / Q000138:chemical synthesis* / Q000737:chemistry / Q000235:genetics*; D006367:HeLa Cells; D006801:Humans; D008055:Lipids / Q000138:chemical synthesis* / Q000737:chemistry / Q000235:genetics*; D008081:Liposomes / Q000737:chemistry; D008968:Molecular Conformation; D011092:Polyethylene Glycols / Q000737:chemistry; D013237:Stereoisomerism; D014162:Transfection / Q000379:methods*
chemical_list: D008055:Lipids; D008081:Liposomes; D011092:Polyethylene Glycols; D004247:DNA; D005492:Folic Acid