GUANIDINIUM-CHOLESTEROL CATIONIC LIPIDS - EFFICIENT VECTORS FOR THE TRANSFECTION OF EUKARYOTIC CELLS

Two cationic lipids, bis-guanidinium-spermidine-cholesterol (BGSC) and bis-guanidinium-trencholesterol (BGTC)-cholesterol derivatives bearin g two guanidinium groups-have been synthesized and tested as artificia l vectors for gene transfer. They combine the membrane compatible feat ures of the cholesterol subunit and the favorable structural and high pK(a) features of the guanidinium functions for binding DNA via its ph osphate groups. Reagent BGTC is very efficient for transfection into a variety of mammalian cell lines when used as a micellar solution. In addition, both BGTC and BGSC present also a high transfection activity when formulated as liposomes with the neutral phospholipid dioleoylph osphatidyl ethanolamine. These results reveal the usefulness of choles terol derivatives bearing guanidinium groups for gene transfer.