Bajaj, Avinash and Kondaiah, Paturu and 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. In: Journal of Medicinal Chemistry, 51 (8). pp. 2533-2540.
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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 $(-(CH_2)_5-; 1)$, hydrophobic rigid $(-C_6H_4-; 2)$, and hydrophilic flexible $(-CH_2-CH_2-O-CH_2-CH_2-; 3)$ 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: | Journal Article |
|---|---|
| Publication: | Journal of Medicinal Chemistry |
| Publisher: | American Chemical Society |
| Additional Information: | Copyright of this article belongs to American Chemical Society. |
| Department/Centre: | Division of Biological Sciences > Molecular Reproduction, Development & Genetics Division of Chemical Sciences > Organic Chemistry |
| Date Deposited: | 18 May 2008 |
| Last Modified: | 19 Sep 2010 04:45 |
| URI: | http://eprints.iisc.ac.in/id/eprint/14006 |
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