Bajaj, Avinash and Kondiah, Paturu and Bhattacharya, Santanu (2007) Design, Synthesis, and in Vitro Gene Delivery Efficacies of Novel Cholesterol-Based Gemini Cationic Lipids and Their Serum Compatibility: A Structure-Activity Investigation. In: Journal of Medicinal Chemistry, 50 (10). pp. 2432-2442.
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Abstract
Five cholesterol-based gemini cationic lipids, which differ in the length of the spacer $[-(CH_2)_n-]$ chain between the head groups, have been synthesized. These lipids are useful as nonviral gene delivery agents, and all cholesterol-based gemini lipids (2a-2e) are better transfecting agents than their monomeric lipid counterpart 1. Transfection efficiency of all the gemini lipids except lipid $2a [-(CH_2)_3-]$ was maintained even when the serum was present during the transfection conditions as compared to the monomeric lipid 1, with which a dramatic decrease in transfection efficiency was observed. With the increase in spacer chain length from propanediyl $[-(CH_2)_3-]$ to pentanediyl $[-(CH_2)_5-]$, transfection efficiency increased both in the absence and presence of serum. However, transfection efficiency decreased with further increase in the length from the pentanediyl $[-(CH_2)_5-]$ to the dodecanediyl $[-(CH_2)_{12}-]$ spacer. Among these gemini lipids 2c showed the highest transfection activity, which was also greater than that of the commercially available formulation.
Item Type: | Journal Article |
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Publication: | Journal of Medicinal Chemistry |
Publisher: | American Chemical Society |
Additional Information: | Copyright of this article belongs to Amerian Chemical Society. |
Department/Centre: | Division of Biological Sciences > Molecular Reproduction, Development & Genetics Division of Chemical Sciences > Organic Chemistry |
Date Deposited: | 13 Jul 2007 |
Last Modified: | 27 Jan 2012 06:08 |
URI: | http://eprints.iisc.ac.in/id/eprint/11543 |
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