Cholesterol derived cationic lipids as potential non-viral gene delivery vectors and their serum compatibility
| Autor: | Chen Li, Yi-Lin Hou, Yi-Yang Jia, Ning Wan, Menglei Huan, Bang-Le Zhang, Xi-Xi Ma, Jia Ju, Si-Yuan Zhou |
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| Rok vydání: | 2015 |
| Předmět: |
0301 basic medicine
Serum Clinical Biochemistry Green Fluorescent Proteins Pharmaceutical Science 02 engineering and technology Gene delivery Transfection Biochemistry 03 medical and health sciences Structure-Activity Relationship Drug Discovery Structure–activity relationship Humans Cationic liposome Particle Size Cytotoxicity Molecular Biology Liposome Chemistry Phosphatidylethanolamines Organic Chemistry HEK 293 cells Cationic polymerization Gene Transfer Techniques Genetic Therapy 021001 nanoscience & nanotechnology Lipids 030104 developmental biology Cholesterol HEK293 Cells Liposomes Molecular Medicine 0210 nano-technology |
| Zdroj: | Bioorganicmedicinal chemistry letters. 26(10) |
| ISSN: | 1464-3405 |
| Popis: | Cholesterol derivatives M1-M6 as synthetic cationic lipids were designed and the biological evaluation of the cationic liposomes based on them as non-viral gene delivery vectors were described. Plasmid pEGFP-N1, used as model gene, was transferred into 293T cells by cationic liposomes formed with M1-M6 and transfection efficiency and GFP expression were tested. Cationic liposomes prepared with cationic lipids M1-M6 exhibited good transfection activity, and the transfection activity was parallel (M2 and M4) or superior (M1 and M6) to that of DC-Chol derived from the same backbone. Among them, the transfection efficiency of cationic lipid M6 was parallel to that of the commercially available Lipofectamine2000. The optimal formulation of M1 and M6 were found to be at a mol ratio of 1:0.5 for cationic lipid/DOPE, and at a N/P charge mol ratio of 3:1 for liposome/DNA. Under optimized conditions, the efficiency of M1 and M6 is greater than that of all the tested commercial liposomes DC-Chol and Lipofectamine2000, even in the presence of serum. The results indicated that M1 and M6 exhibited low cytotoxicity, good serum compatibility and efficient transfection performance, having the potential of being excellent non-viral vectors for gene delivery. |
| Databáze: | OpenAIRE |
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