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设计合成了4个含大环多胺cyclen亲水基团和十二酸疏水基团的两亲小分子化合物8a～8d,其结构经核磁共振谱和高分辨质谱确证.凝胶电泳实验结果表明,此类化合物与Sn-甘油-1,2-二油酰-3-磷酰乙醇胺(DOPE)形成的阳离子脂质体对DNA有很强的包裹能力.4种脂质体中,8a在N/P为4时可完全包裹DNA,8b～8d在N/P为6时即可完全包裹DNA.荧光实验也表明这四种脂质体可以有效减弱溴乙锭(EB)的荧光.另外,此类脂质体的粒径在80～120 nm之间,zeta电位在+25～55 mV之间,且在长达7 d的测量时间内没有明显的变化.此外,我们还将该类脂质体在A549细胞中进行了绿色荧光蛋白的转染实验,8a有中等强度的荧光表达,8b～8d则无荧光表达.结果表明,此类脂质体具备了作为非病毒基因载体的潜在性.
Four amphiphilic compounds 8a ~ 8d containing macrocyclic polyamine cyclen hydrophilic groups and lauric acid hydrophobic groups were designed and synthesized, and their structures were confirmed by NMR and HRMS.The results of gel electrophoresis , These compounds and Sn-glycerol-1,2-dioleyl-3-phosphoethanolamine (DOPE) formed cationic liposomes have a strong ability to wrap DNA in the four liposomes, 8a in N DNA was completely encapsulated at / 4 and DNA was completely encapsulated at 8 and 8 days at N / P of 6. Fluorescence experiments also showed that these four liposomes can effectively reduce the fluorescence of ethidium bromide.In addition, These liposomes have particle sizes between 80 and 120 nm and zeta potentials between +25 and 55 mV, with no significant change over a measuring period of up to 7 d. In addition, Plastids were transfected with green fluorescent protein in A549 cells with medium intensity of 8a fluorescence and no fluorescence after 8 to 8 days.The results showed that these liposomes possessed the potential of being non-viral gene carriers .