Stearylated Arginine-Rich Peptides: A New Class of Transfection Systems

Membrane-permeable arginine-rich peptides, such as HIV-1 Tat-(48−60), HIV-1 Rev-(34−50), and flock house virus (FHV) coat-(35−49), have been shown to possess the ability to transfect COS-7 cells with luciferase-coding plasmid as efficiently as polyarginine (MW 5000−15 000) and polylysine (MW 9800). Not only these virus-derived cationic peptides but also oligoarginines of 4−16 residues were found to be able to transfect cells. In the case of the Tat, FHV, and octaarginine peptides, N-terminal stearylation of the peptides increases the transfection efficiency by approximately 100 times to reach the same order of magnitude as that of LipofectAMINE, one of the most efficient commercially available transfection agents. Also, a certain correlation was observed between the transfection efficiency of stearyl-(Arg)n peptides (stearyl-Rn: n = 4, 8, 12, 16) and the membrane permeability of the corresponding (Arg)n peptides (Rn).