NOVEL CATIONIC CAROTENOID-BASED LIPIDS FOR CELLULAR NUCLEIC ACID UPTAKE

摘要

The synthesis and self-assembling properties of a model compound in a new class of cationic phospholipids with a highly unsaturated conjugated carotenoid fatty acid are described. In addition, the potential of this new lipid as a nucleic acid carrier was evaluated through lipoplex formulations employing 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) as helper lipid with and without the polycationic peptide, protamine, together with a plasmid DNA (pDNA). Lipoplexes composed of this novel unsaturated lipid exhibited pDNA binding and protection from DNase I degradation when formulated with protamine. Cellular uptake of the liposomes could be monitored by the visible color of the carotenoid moieties. The new cationic lipid gene delivery vector revealed comparable transfection efficiency to the commercial lipid, 1,2-dimyristoyl-sn-glycero-3-ethylphophocholine (EPC), in Chinese hamster ovary-K1 (CHO-K1) cells and performed equally to Lipofectamine 2000 when the formulation included protamine.