Shi Jia, Yu Shijun, Zhu Jie, Zhi Defu, Zhao Yinan, Cui Shaohui, Zhang Shubiao
Liaoning Normal University School of Chemistry & Chemical Engineering, Liaoning, Dalian 116029, China; SEAC-ME Key Laboratory of Biochemical Engineering, Dalian Nationalities University, Liaoning, Dalian 116600, China.
Liaoning Normal University School of Chemistry & Chemical Engineering, Liaoning, Dalian 116029, China.
Colloids Surf B Biointerfaces. 2016 May 1;141:417-422. doi: 10.1016/j.colsurfb.2016.02.018. Epub 2016 Feb 10.
A series of carbamate-linked cationic lipids containing saturated or unsaturated hydrocarbon chains and quaternary ammonium head were designed and synthesized. After recrystallization, carbamate-linked cationic lipids with high purity (over 95%) were obtained. The structures of these lipids were proved by IR spectrum, HR-ESI-MS, HPLC, (1)H NMR and (13)C NMR. The liposomes were prepared by using these cationic lipids and neutral lipid DOPE. Particle size and zeta-potential were studied to show that they were suitable for gene transfection. The DNA-bonding ability of C12:0, C14:0 and C18:1 cationic liposomes was much better than others. The results of transfection showed that hydrophobic chains of these lipids have great effects on their transfection activity. The lipids bearing C12:0, C14:0 saturated chains or C18:1 unsaturated chain showed relatively higher transfection efficiency and lower cytotoxicity. So these cationic lipids could be used as non-viral gene carriers for further studies.
设计并合成了一系列含有饱和或不饱和烃链以及季铵头基的氨基甲酸酯连接的阳离子脂质。重结晶后，得到了高纯度（超过95%）的氨基甲酸酯连接的阳离子脂质。通过红外光谱、高分辨电喷雾电离质谱、高效液相色谱、核磁共振氢谱和核磁共振碳谱对这些脂质的结构进行了证实。使用这些阳离子脂质和中性脂质二油酰磷脂酰乙醇胺制备了脂质体。研究了粒径和zeta电位，结果表明它们适用于基因转染。C12:0、C14:0和C18:1阳离子脂质体的DNA结合能力比其他脂质体要好得多。转染结果表明，这些脂质的疏水链对其转染活性有很大影响。带有C12:0、C14:0饱和链或C18:1不饱和链的脂质表现出相对较高的转染效率和较低的细胞毒性。因此，这些阳离子脂质可作为非病毒基因载体用于进一步研究。
