Molecular design of amphiphiles with DNA transfer ability into cell

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Cationic amphiphiles which have aquaternary ammonium head, hydrocarbon tailsanda glutamic acid connector with methylenespacer have been used for delivery ofDNA into eukaryotic cells. we studied thecorrelation between the efficiency ofvarious cationic amphiphiles in DNA transfection and their physicochemical properties1.We found that one of dialkyl ammonium amphiphile, didodecyl N- [ p- ( 2-trimethylammonioethoxy ) benzoyl ] -L-glutamate bromide, had a higher DNA transfection than commercially available lipid, DOTMA,and that there was a good correlation between their efficiencies in gene transfer and physicochemical characteristics.Amphiphilic compounds tthe phase transition temperatures ( Tc )of which are lower than the culture temperature and which form small stable vesicles are good carriers of DNA into cultured cells.2.The result makes it possible to design compounds with a more efficient DNA transfection ability, and we designed and obtained a new cationic amphiphile with higher activity.3.We investigated interaction the structural between cationic amphiphilesandDNA,bymeans of electron microscopy, CDandNMRspectroscopies, and fluoroscopy. Amphiphiles with phenylene in the spacer regionare restricted their mobility by bindingwith DNA while others are flexibleenough for arranging along DNA helix. Ontheother hand, conformation of DNA is forced to change by bilayr-forming amphiphiles at lower temperature than their Tc's.