Efficient Delivery of Plasmid DNA Using Cholesterol-Based Cationic Lipids Containing Polyamines and Ether Linkages

International Journal of Molecular Sciences

Bieong-Kil Kim¹  Young-Bae Seu¹  Yun-Ui Bae³  Tae-Won Kwak¹  Hyungu Kang¹  Ik-Jae Moon²  Guen-Bae Hwang¹  So-Young Park³ 

[1] School of Life Sciences & Biotechnology, Kyungpook National University, 1370 Sangyeokdong, Bookgu, Daegu 702-701, Korea; E-Mails:;WelGENE Inc., 71B-4L, Hightech Sector 2, Sungseo Industrial Park 3, Dalseogu, Daegu 704-230, Korea; E-Mail:;Department of Physiology, Yeungnam University College of Medicine, 317-1 Daemyungdong, Daegu 705-717, Korea; E-Mails:

关键词: cholesterol;    cationic lipids;    cyanoethylation;    transfection;    gene delivery;    macropinocytosis;   

DOI  :  10.3390/ijms15057293

来源: mdpi

【 摘 要 】

Cationic liposomes are broadly used as non-viral vectors to deliver genetic materials that can be used to treat various diseases including cancer. To circumvent problems associated with cationic liposome-mediated delivery systems such as low transfection efficiency and serum-induced inhibition, cholesterol-based cationic lipids have been synthesized that resist the effects of serum. The introduction of an ether-type linkage and extension of the aminopropyl head group on the cholesterol backbone increased the transfection efficiency and DNA binding affinity compared to a carbamoyl-type linkage and a mono aminopropyl head group, respectively. Under optimal conditions, each liposome formulation showed higher transfection efficiency in AGS and Huh-7 cells than commercially available cationic liposomes, particularly in the presence of serum. The following molecular structures were found to have a positive effect on transfection properties: (i) extended aminopropyl head groups for a strong binding affinity to plasmid DNA; (ii) an ether linkage that favors electrostatic binding to plasmid DNA; and (iii) a cholesterol backbone for serum resistance.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland