Folate-equipped pegylated archaeal lipid derivatives: synthesis and transfection properties.
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.
Lainé
Céline
C
Ecole Nationale Supérieure de Chimie de Rennes, UMR CNRS 6226, Equipe Chimie Organique et Supramoléculaire, Av. Général Leclerc, 35700 Rennes, France.
Mornet
Emmanuel
E
Lemiègre
Loïc
L
Montier
Tristan
T
Cammas-Marion
Sandrine
S
Neveu
Cécile
C
Carmoy
Nathalie
N
Lehn
Pierre
P
Benvegnu
Thierry
T
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*
D008055:Lipids; D008081:Liposomes; D011092:Polyethylene Glycols; D004247:DNA; D005492:Folic Acid