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以芳香亚胺为连接剂的聚乙烯亚胺衍生物的合成及体外活性研究 预览

Synthesis and biological evaluation of polyethyleneimine derivatives with aromatic imine conjuction
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摘要 通过有机合成的方法合成新型聚阳离子载体聚五乙烯六胺对苯二甲醛-1,4-二亚胺(PEHA-TPAI),产物结构经核磁共振氢谱(1H NMR)和傅里叶红外光谱(FT-IR)确定系目标产物。采用琼脂糖凝胶电泳实验观察PEHATPAI包裹小干扰RNA(siRNA)的能力,并用粒度仪和Zeta电位仪对PEHA-TPAI/siRNA复合物进行表征。结果表明:PEHA-TPAI和siRNA复合后可形成稳定且粒径均一的纳米颗粒,在PEHA-TPAI/siRNA复合物质量比为10∶1的条件下,颗粒粒径为(129.90±1.02)nm,Zeta电位为(21.1±0.54)mV。体外细胞毒性实验和转染实验的结果表明:PEHA-TPAI的细胞毒性显著低于商业化转染试剂聚乙烯亚胺(PEI,分子量为25 000)(P〈0.001)且具有良好的转染效率,有作为低毒性、高转染效率的基因输送载体的潜力。 A novel cationic polymer poly pentaethylenehexamine terephthalaldehyde-1,4-diimine(PEHATPAI) was synthesized,and the structure of PEHA-TPAI was determined by nuclear magnetic resonance hydrogen spectrometer(~1H NMR) and Fourier transform infrared radiation spectrometer(FT-IR).The capability of small interfering RNA(siRNA) condensation was detected by agarose gel electrophoresis,and the particle size and Zeta potential of PEHA-TPAI/siRNA complex were measured by laser particle size and Zeta potential analyzer.Results showed that PEHA-TPAI could effectively bind siRNA and form stable and uniform PEHA-TPAI/siRNA complex with an average particle size of(129.90±1.02) nm,and Zeta potential of(21.1±0.54) mV in the mass ratio of 10∶1.The in vitro cytotoxicity and transfection tests indicated that the cytotoxicity of PEHA-TPAI was significantly lower than polyethyleneimine(PEI,molecular weight 25 000)(P〈0.001),a commercial transfection reagent,and the transfection efficiency of PEHA-TPAI/siRNA complex was significantly higher than naked siRNA,which showed a highpotential to be an excellent candidate with the advantage of low cytotoxicity and high transfection efficiency for gene delivery system.
作者 吴晨琛 白光 薛涌尔 金拓 WU Chenchen,BAI Guang,XUE Yonger,JIN Tuo(School of Pharmacy,Shanghai Jiao Tong University,Shanghai 200240,China)
出处 《南京工业大学学报:自然科学版》 北大核心 2017年第6期46-51,67共7页 Journal of Nanjing University of Technology
基金 国家自然科学基金(81373352)
关键词 非病毒载体 基因输送 细胞毒性 转染效率 non-viral vector gene delivery cytotoxicity transfection efficiency
作者简介 吴晨琛(1992-),女,江苏南京人,硕士,主要研究方向为基因输送;;金拓(联系人),教授,E-mail:tjin@sjtu.edu.cn
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