Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 23, Pages 7045-7049Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.09.098
Keywords
Cationic lipids; Triazacyclononane; DNA condensation; Gene delivery
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Funding
- National Science Foundation of China [20902062, 20972104, 20732004, 20725206]
- Program for Changjiang Scholars and Innovative Research Team in University
- Chinese Ministry of Education in China
- Scientific Fund of Sichuan Province for Outstanding Young Scientist
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A series of novel cationic lipids based on 1,4,7-triazacyclononane (TACN) with different hydrophobic chains were synthesized via the formation of a biodegradable ester bond. These lipids were found to have good buffering capacity at the pH range of 5.0-6.5, which is similar to that of the acidic endosomal compartments. The liposomes formed from these lipids and DOPE could condense DNA into nanoparticles with proper sizes. In vitro experiments showed moderate to good gene transfection efficiency of the formed lipoplexes. The structure-activity relationships of this type of lipids were discussed. (C) 2011 Elsevier Ltd. All rights reserved.
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