Pillar[5]arene-modified peptide-guanidiniocarbonylpyrrol amphiphiles with gene transfection properties  

作　　者：Kaiya Wang Minzan Zuo Tao Zhang Huilan Yue Xiao-Yu Hu 

机构地区：[1]College of Materials Science and Technology,Nanjing University of Aeronautics and Astronautics,Nanjing 211106,China [2]Qinghai Provincial Key Laboratory of Tibetan Medicine Research and Key Laboratory of Tibetan Medicine Research,Northwest Institute of Plateau Biology,Chinese Academy of Sciences,Xining 810008,China

出　　处：《Chinese Chemical Letters》2023年第5期246-249,共4页中国化学快报（英文版）

基　　金：supported by the Natural Science Foundation of Jiangsu Province(Nos.BK20200432,BK20211179);National Natural Science Foundation of China(Nos.22271154,M-0411);the Fundamental Research Funds for the Central Universities(Nos.NG2022003,NS2021040)。

摘　　要：Pillar[5]arene-modified amphiphilic peptides with varying numbers of guanidiniocarbonylpyrrol(GCP)moieties have been successfully synthesized,which can self-assemble to multivalent cationic superstructures in aqueous solutions.These assembled peptides can condense DNA into various compact multimolecular aggregates to achieve successful intracellular DNA delivery and demonstrate great potential for gene transfection.Transfection efficiencies of the self-assembled superstructures have been evaluated in vitro with He La and HEK 293T cells.We demonstrate that GCP moiety could enhance the cell transfection ability,owing to its excellent binding towards cytomembrane.It was also found that subtle structure difference in peptides 2 and 3 could result in distinct transfection efficacy,which makes it possible to gain an in-depth understanding of their structure-activity relationship.This work presents a good example of rational structural design in achieving effective gene transfection vectors.

关 键 词：arene Guanidinocarbonylpyrrole Gene transfection Amphiphiles Structure-activity relationship 

分 类 号：Q78[生物学—分子生物学]