Futaki S, Ohashi W, Suzuki T, Niwa M, Tanaka S, Ueda K, Harashima H, Sugiura Y
Institute for Chemical Research, Kyoto University, Uji, Kyoto 611-0011, Japan.
Bioconjug Chem. 2001 Nov-Dec;12(6):1005-11. doi: 10.1021/bc015508l.
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).
膜通透性富含精氨酸的肽，如HIV-1 Tat-(48 - 60)、HIV-1 Rev-(34 - 50)和禽呼肠孤病毒（FHV）衣壳蛋白-(35 - 49)，已被证明能够像聚精氨酸（分子量5000 - 15000）和聚赖氨酸（分子量9800）一样有效地用荧光素酶编码质粒转染COS-7细胞。不仅这些病毒衍生的阳离子肽，而且4 - 16个残基的寡聚精氨酸也被发现能够转染细胞。就Tat、FHV和八聚精氨酸肽而言，肽的N端硬脂酰化使转染效率提高约100倍，达到与最有效的市售转染试剂之一LipofectAMINE相同的数量级。此外，在硬脂酰-(Arg)n肽（硬脂酰-Rn：n = 4、8、12、16）的转染效率与相应的(Arg)n肽（Rn）的膜通透性之间观察到一定的相关性。
