Amphoteric poly(amido amine)s with adjustable balance between transfection efficiency and cytotoxicity for gene delivery
Amphoteric poly(amido amine)s with adjustable balance between transfection efficiency and cytotoxicity for gene delivery
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用于基因递送的转染效率和细胞毒性之间可调节平衡的两性聚（酰胺基胺）
DOI：
10.1016/j.colsurfb.2018.11.045
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发表时间：
2019
期刊：
影响因子：
--
通讯作者：
Pingtian Ding
中科院分区：
文献类型：
--
作者：
Yanping Sun;Hui Liu;Tianzhi Yang;Lang Lang;Lin Cheng;Haonan Xing;Li Yang;Pingtian Ding
为了平衡转染效率和细胞毒性以及筛选最佳的基因载体聚合物，合成了一系列由胍丁胺（AGM）和γ-氨基丁酸（GABA）组成的两性共聚物（poly（CBA-AGM/GABA）s）。含正电荷胍基的AGM用于提高转染效率，而含负电荷羧基的GABA用于降低细胞毒性。假设以两种组分的最佳比例合成的两性聚（CBA-AGM/GABA）将很好地平衡转染效率和细胞毒性。通过比较这些聚合物在基因传递中的基本特征，优化了AGM和GABA的理想比例。AGM 80含有80%AGM和20%GABA，具有良好的基因传递性能，包括适度的DNA浓缩能力、高细胞摄取、强核定位能力、高转染效率和低细胞毒性，表明该聚合物是一种非常有前途的高效无毒基因载体。
In order to balance transfection efficiency and cytotoxicity as well as screen the optimal polymers for gene delivery, a series of amphoteric copolymers (poly(CBA-AGM/GABA)s) composed of different ratios between agmatine (AGM) and γ-aminobutyric acid (GABA) monomers were synthesized. The AGM containing positively charged guanidinium groups was used to improve transfection efficiency, while the GABA containing negatively charged carboxyl groups was used to decrease cytotoxicity. It is hypothesized that the amphoteric poly(CBA-AGM/GABA)s synthesized at the optimal ratio of both components would well balance transfection efficiency and cytotoxicity. By comparing these polymers’ essential features in gene delivery, the ideal ratio between AGM and GABA was optimized. AGM80, which contained 80% AGM and 20% GABA, showed favorable properties for gene delivery, including moderate DNA condensation capacity, high cellular uptake, strong nuclear localization ability, high transfection efficiency, and low cytotoxicity, indicating that this polymer is very promising as a potent and nontoxic gene carrier.