transfection efficiencies of T-shaped spermine-based cationic lipids with identical and nonidentical tails under high serum conditions

• Published in: Organic & biomolecular chemistry 2023-03, Vol.21 (9), p.1967-1979
• Main Authors: Thongbamrer, Chopaka, Teerakantrakorn, Purichaya, Nongpong, Ussanee, Apiratikul, Nuttapon, Roobsoong, Wanlapa, Kunkeaw, Nawapol, Nguitragool, Wang, Sattabongkot, Jetsumon, Yingyongnarongkul, Boon-ek
• Format: Article
• ISSN: 1477-0520; 1477-0539
• DOI: 10.1039/d2ob02129c

T-shaped spermine-based cationic lipids with identical and nonidentical hydrophobic tails having variable carbon lengths (from C10 to C18) were designed and synthesized. These lipids were characterized, and their structure-activity relationships were determined for DNA binding and transfection ability of these compounds when formulated as cationic liposomes. These liposomes were then applied as non-viral vectors to transfect HEK293T, HeLa, PC3, H460, HepG2, and Calu′3 cell lines with plasmid DNA encoding the green fluorescent protein. ST9 , ST12 and ST13 with nonidentical tails could deliver DNA into HEK293T cells up to 60% under serum-free conditions. The lipid ST15 bearing nonidentical tails was found to be a potent gene transfer agent under 40% serum conditions in HEK293T and HeLa cells. Besides their low cytotoxicity, these lipoplexes also exhibited greater transfection efficiency than the commercially available transfection agent, Lipofectamine 3000. T-shaped spermine-based cationic lipids with nonidentical chains showed excellent transfection efficiency compared to the commercially available transfection agent, Lipofectamine 3000.