2-Aminoimidazole facilitates efficient gene delivery in a low molecular weight poly(amidoamine) dendrimer. Issue 24 (31st May 2018)

• Record Type: Journal Article
• Authors: Wang, Jing; Hu, Xuefeng; Wang, Dongli; Xie, Cao; Lu, Weiyue; Song, Jie; Wang, Ruifeng; Gao, Chunli; Liu, Min
• Is Part Of: Organic & biomolecular chemistry. Volume 16:Issue 24(2018)
• Page Start: 4464
• Page End: 4470
• Publication Date: 2018-05-31
• Subjects: Chemistry, Organic -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1039/c8ob00953h
• Languages: English
• ISSNs: 1477-0520

Abstract

Abstract : 2-Aminoimidazole greatly improved the transfection efficiency of G2. It contributes to condensing DNA into small, monodisperse nanostructures, enhancing cellular penetration and endosome/lysosome escape. Abstract : Functional groups have shown great potential in gene delivery. However, a number of the reported functional groups can only overcome one certain physiological barrier, resulting in limited transfection efficiencies. Based on the structure–activity relationships of both imidazolyl and guanidyl, we designed a novel multifunctional group, 2-aminoimidazole (AM), for gene delivery. On modifying with the AM group, the transfection efficiency of low molecular weight poly(amidoamine) (G2) was 200 times greater than the parent dendrimer in vitro . In contrast, the transfection efficiency of G2 showed a decreasing trend when it was grafted with imidazole. Assays revealed that the AM group played multiple roles in gene delivery, including condensing DNA into monodisperse nanoparticles of 80–90 nm in diameter, achieving nearly ten times higher cellular-uptake efficacy, and enhancing the abilities of endosome/lysosome escape and nuclear localization. What's more, AM showed low toxicity. These results demonstrate that the AM group could be a promising tool in non-viral gene delivery.