Low molecular weight polyethyleneimine modified by 2-aminoimidazole achieving excellent gene transfection efficiency
Low molecular weight polyethyleneimine modified by 2-aminoimidazole achieving excellent gene transfection efficiency
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DOI：
10.1016/j.eurpolymj.2020.110017
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发表时间：
2020
期刊：
影响因子：
--
通讯作者：
Min Liu
中科院分区：
文献类型：
--
作者：
Jie Song;Dongli Wang;Jing Wang;Qing Shen;Cao Xie;Weiyue Lu;Ruifeng Wang;Min Liu
The transfection efficiency and cytotoxicity of polyethyleneimine (PEI), as a non-viral vector, increase with.molecular weight. Low molecular weight PEI, such as branched PEI1800 (Mw ~ 1800 kDa), has negligible.transfection efficiency but low cytotoxicity. Given the low efficiency of PEI1800, a variety of modifications were.explored. A structure-integrated group of guanidyl and imidazolyl, 2-aminoimidazole was designed (Scheme 1)..To verify the molecular interaction between 2-aminoimidazole and gene, molecular docking experiment, 1H.NMR, FTIR and isothermal titration calorimetry (ITC) measurement were carried out. Studies confirmed that 2-.aminoimidazole form double hydrogen bonds with phosphate group, which enhanced the thermodynamic interaction.between 2-aminoimidazole and gene. Hence, we synthesized 2-aminoimidazole modified PEI1800, and.as controls, guanidyl and imidazolyl modified PEI1800 were synthesized respectively. As expected, the results.showed that 2-aminoimidazole modified PEI1800 could condense DNA into a higher positively charged complex.with 116 ~ 120 nm in diameter and improve the cellular uptake. EGFP assay and luciferase assay showed that 2-.aminoimidazole modified PEI1800 exhibited much better transfection than PEI1800, guanidyl modified.PEI1800, imidazolyl modified PEI1800 both in HEK 293 T cells and SGC-7901 cells. Besides, MTT assay showed.2-aminoimidazole modified PEI1800 exhibited better biocompatibility than PEI25 K. These results highlight the.critical role that 2-aminoimidazole played in non-viral gene delivery
