Premium
Folate‐Equipped Pegylated Archaeal Lipid Derivatives: Synthesis and Transfection Properties
Author(s) -
Lainé Céline,
Mornet Emmanuel,
Lemiègre Loïc,
Montier Tristan,
CammasMarion Sandrine,
Neveu Cécile,
Carmoy Nathalie,
Lehn Pierre,
Benvegnu Thierry
Publication year - 2008
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.200800950
Subject(s) - transfection , ethylene glycol , chemistry , peg ratio , biochemistry , folate receptor , liposome , in vivo , cationic polymerization , gene delivery , in vitro , betaine , combinatorial chemistry , gene , biology , organic chemistry , genetics , microbiology and biotechnology , finance , cancer , cancer cell , economics
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.