用于基因递送的三肽阳离子脂质
Tri-peptide cationic lipids for gene delivery.
作者信息
Zhao Yinan, Zhang Shubiao, Zhang Yuan, Cui Shaohui, Chen Huiying, Zhi Defu, Zhen Yuhong, Zhang Shufen, Huang Leaf
机构信息
State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116021, Liaoning, China ; SEAC-ME Key Laboratory of Biotechnology and Bio-resources Utilization, Dalian Nationalities University, Dalian 116600, Liaoning, China.
SEAC-ME Key Laboratory of Biotechnology and Bio-resources Utilization, Dalian Nationalities University, Dalian 116600, Liaoning, China.
出版信息
J Mater Chem B. 2015 Jan 7;3(1):119-126. doi: 10.1039/C4TB01312C.
Several novel tri-peptide cationic lipids were designed and synthesized for delivering DNA and siRNA. They have tri-lysine and tri-ornithine as head groups, carbamate group as linker and 12 and 14 carbon atom alkyl groups as tails. These tri-peptide cationic lipids were prepared into cationic liposomes for the study of the physicochemical properties and gene delivery. Their particle size, Zeta potential and DNA-binding were characterized to show that they were suitable for gene transfection. The further results indicate that these lipids can transfer DNA and siRNA very efficiently into NCI-H460 and Hep-2 tumor cells. The selected lipid, CDO14, was able to deliver combined siRNAs against c-Myc and VEGF for silencing distinct oncogenic pathways in lung tumors of mice, with little and toxicity.
设计并合成了几种新型三肽阳离子脂质用于递送DNA和siRNA。它们以三赖氨酸和三鸟氨酸作为头部基团，以氨基甲酸酯基团作为连接基团，以含有12和14个碳原子的烷基作为尾部。将这些三肽阳离子脂质制备成阳离子脂质体以研究其理化性质和基因递送情况。对它们的粒径、Zeta电位和DNA结合能力进行了表征，结果表明它们适合用于基因转染。进一步的结果表明，这些脂质能够非常有效地将DNA和siRNA转染到NCI-H460和Hep-2肿瘤细胞中。所选择的脂质CDO14能够递送针对c-Myc和VEGF的联合siRNA，以沉默小鼠肺部肿瘤中不同的致癌途径，且几乎没有毒性。
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