Amphiphilic cationic lipopeptides with RGD sequences as gene vectors
作者： Jing-Xiao Chen , Hui-Yuan Wang , Chang-Yun Quan , Xiao-Ding Xu , Xian-Zheng Zhang
DOI: 10.1039/C003538F
关键词: HeLa 、 Amphiphile 、 Transfection 、 Chemistry 、 Cationic Lipopeptides 、 DNA 、 HEK 293 cells 、 Peptide 、 Biochemistry 、 Cell culture 、 Physical and Theoretical Chemistry 、 Organic chemistry
摘要: Two kinds of arginine-rich amphiphilic lipopeptides with hydrophobic aliphatic tails (C12GR8GDS, LP1 and C18GR8GDS, LP2) were designed synthesized as functional gene vectors. With tail modification, these could bind DNA more efficiently form stable spherical complexes in comparison the control peptide (AcGR8GDS, P1). Moreover, size zeta potential results demonstrated charge density stability vector/DNA be improved increasing length tails. In vitro transfection experiments showed that LP2 induce much higher expression level (luciferase expression) compared P1. Due to incorporation arginine-glycine-aspartic acid (RGD) sequences which specifically recognized by integrins αυβ3 αυβ5 over-expressed on cancer cells, i.e. exhibited relatively efficiency HeLa cell line than P2 P3 without RGD sequence. While efficiencies similar 293T cells. Lipopeptides very low cytotoxicity both lines even at high concentration.
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