Puchkov Pavel A, Kartashova Irina A, Shmendel Elena V, Luneva Anastasya S, Morozova Nina G, Zenkova Marina A, Maslov Mikhail A
Institute of Fine Chemical Technologies, Moscow Technological University, Vernadsky Ave. 86, Moscow 119571, Russia.
Institute of Chemical Biology and Fundamental Medicine SB RAS, Lavrentiev Ave. 8, Novosibirsk 630090, Russia.
Bioorg Med Chem Lett. 2017 Aug 1;27(15):3284-3288. doi: 10.1016/j.bmcl.2017.06.026. Epub 2017 Jun 10.
Three novel polycationic gemini amphiphiles with different spacers were developed and evaluated in terms of their physiochemical properties and transfection efficiencies. Cationic liposomes formed by these amphiphiles and the helper lipid DOPE were able to successfully condense DNA, as shown by gel mobility shift and ethidium bromide intercalation assays. Transfection activity of the liposomes was superior to Lipofectamine 2000 and was dependent on spacer structure, hydrophobicity, and nucleic acid type (pDNA or siRNA). We demonstrated that the cationic liposomes 2X6/DOPE and 2X7/DOPE are potential non-toxic vehicles for gene delivery.
我们开发了三种具有不同间隔基团的新型聚阳离子双子两亲分子，并对其物理化学性质和转染效率进行了评估。如凝胶迁移率变动分析和溴化乙锭嵌入分析所示，由这些两亲分子与辅助脂质DOPE形成的阳离子脂质体能够成功地凝聚DNA。脂质体的转染活性优于Lipofectamine 2000，并且取决于间隔基团结构、疏水性和核酸类型（质粒DNA或小干扰RNA）。我们证明，阳离子脂质体2X6/DOPE和2X7/DOPE是潜在的无毒基因递送载体。
