Bajaj, Avinash ; Kondaiah, Paturu ; Bhattacharya, Santanu (2008) Effect of the nature of the spacer on gene transfer efficacies of novel thiocholesterol derived gemini lipids in different cell lines: a structure-activity investigation Journal of Medicinal Chemistry, 51 (8). pp. 2533-2540. ISSN 0022-2623
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Official URL: http://pubs.acs.org/doi/abs/10.1021/jm7010436
Related URL: http://dx.doi.org/10.1021/jm7010436
Abstract
A structure-activity investigation was undertaken to see the effect of the nature of the spacer on the gene transfection efficacies of thiocholesterol-derived cationic gemini lipids possessing disulfide linkage between the cationic headgroup and the thiocholesterol moiety. Three gemini cationic lipids possessing hydrophobic flexible (-(CH2)5-; 1), hydrophobic rigid (-C6H4-; 2), and hydrophilic flexible (-CH2-CH2-O-CH2-CH2-; 3) spacer segments were synthesized. In HeLa cells, lipid formulations 1 and 2 were found to be more effective as compared to lipid 3 formulation. In HT1080 cell line, the order of transfectability was 3 > 1 > 2. Transfection studies in HeLa and HT1080 cell line also showed 40-50% transfection efficacy in the presence of 10% serum conditions. These formulations were also able to transfect gene across difficult cells like HaCaT. Cytotoxic studies showed the nontoxic nature of these lipid-DNA complexes at different N/P ratios used for transfection studies.
Item Type: | Article |
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Source: | Copyright of this article belongs to American Chemical Society. |
ID Code: | 20958 |
Deposited On: | 20 Nov 2010 13:16 |
Last Modified: | 21 Jan 2011 06:22 |
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