Benzothiazole head group based cationic lipids: Synthesis and application for gene delivery

Abstract

A series of benzothiazole based lipids (1–10) containing different derivatives of benzothiazole in the head group region were synthesized to determine the structure–activity relationship for gene delivery. The liposomes formulated were mixed with plasmid DNA encoding green fluorescent protein (α5GFP) or β-galactosidase (pCMV-SPORT-β-gal) and transfected into B16F10 (Human melanoma cancer cells), CHO (Chinese hamster ovary), A-549 (Human lung carcinoma cells) and MCF-7 (Human breast carcinoma cells) types of cell lines. The efficiencies of lipids 9 and 10 in particular, were found to be comparable and even more when compared to that of LipofectAmine-2000. The transfection profiles of the efficient lipids are proved to be maintained even in the presence of serum. Thus, the benzothiazole head group based lipids developed have the potential to be used as transfection reagents in vitro and in vivo.