Skip to Main content Skip to Navigation
Journal articles

Cation substitution in cationic phosphonolipids: A new concept to improve transfection activity and decrease cellular toxicity

Abstract : Cationic lipids have been shown to be an interesting alternative to viral vector-mediated gene delivery into in vitro and in vivo model applications. Prior studies have demonstrated that even minor structural modifications of the lipid hydrophobic domain or of the lipid polar domain result in significant changes in gene delivery efficiency. Previously, we developed a novel class of cationic lipids called cationic phosphonolipids and described the ability of these vectors to transfer DNA into different cell lines and in vivo. Up until now, in all new cationic lipids, nitrogen atoms have always carried the cationic or polycationic charge. Recently we have developed a new series of cationic phosphonolipids characterized by a cationic charge carried by a phosphorus or arsenic atom. In a second step, we have also examined the effects of the linker length between the cation and the hydrophobic domain as regards transfection activity. Transfection activities of this library of new cationic phosphonolipids were studied in vitro in different cell lines (HeLa, CFT1, K562) and in vivo using a luciferase reporter gene. A luminescent assay was carried out to assess luciferase expression. We demonstrated that cation substitution on the polar domain of cationic phosphonolipids (N → P or As) results in significant increase in transfection activity for both in vitro and in vivo assays and decrease of cellular toxicity.
Document type :
Journal articles
Complete list of metadatas

https://hal.univ-brest.fr/hal-01771377
Contributor : Nicolas Renard <>
Submitted on : Thursday, April 19, 2018 - 2:49:05 PM
Last modification on : Wednesday, May 6, 2020 - 4:34:05 PM

Links full text

Identifiers

Collections

Citation

V. Floch, S. Loisel, E. Guenin, A.C. Herve, J.C. Clement, et al.. Cation substitution in cationic phosphonolipids: A new concept to improve transfection activity and decrease cellular toxicity. Journal of Medicinal Chemistry, American Chemical Society, 2000, 43, pp.4617--4628. ⟨10.1021/jm000006z⟩. ⟨hal-01771377⟩

Share

Metrics

Record views

132