Cationic lipids bearing succinic-based, acyclic and macrocyclic hydrophobic domains: Synthetic studies and in vitro gene transfer

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• 作者：Emile Jubeli<sup>asup> ; Amanda B. Maginty<sup>bsup> ; Nada Abdul Khalique<sup>csup> ; Liji Raju<sup>csup> ; David G. Nicholson<sup>dsup> ; Helge Larsen<sup>esup> ; Michael D. Pungente<sup>fsup><sup> ; sup><sup>mdp2001@qatar-med.cornell.edusup> ; William P.D. Goldring<sup>bsup><sup> ; sup><sup>goldring@ruc.dksup>
• 关键词：Macrocyclic lipids ; Cationic ; Succinic ; Lipoplex formulation ; In vitro DNA transfer
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：225-232
• 全文大小：960 K
• 卷排序：125

文摘

Succinic-based acyclic (non-rigid) and macrocyclic (rigid) cationic lipids were synthesized. The synthetic lipids were formulated with plasmid DNA and a neutral lipid. The in vitro transfection and cytotoxicity of formulations was evaluated using CHO-K1 cells. Introduction of the succinic unit within the hydrophobic domain improved lipid hydration. Mismatched (rigid lipid blended with a non-rigid lipid) outperformed matched formulations.