The synthesis of cholesterol-based cationic lipids with trimethylamine head and the effect of spacer structures on transfection efficiency

被引：18
|
作者：
Kim, Bieong-Kil [1 ]
Bae, Yun-Ui [2 ]
Doh, Kyung-Oh [2 ]
Hwang, Guen-Bae [1 ]
Lee, Sung-Hye [2 ]
Kang, Hyungu [1 ]
Seu, Young-Bae [1 ]
机构：
[1] Kyungpook Natl Univ, Sch Life Sci & Biotechnol, Taegu 702701, South Korea
[2] Yeungnam Univ, Dept Physiol, Coll Med, Taegu 705717, South Korea
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 12期
关键词：
Cholesterol; Cationic liposome; Transfection; Gene transfer technique; GENE DELIVERY; ETHER LINKAGE; HEADGROUP; SKELETON; THERAPY; SYSTEMS; RISK;
D O I：
10.1016/j.bmcl.2011.04.071
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Five cholesterol-based cationic lipids were newly synthesized based on cholest-5-en-3 beta-oxyethane-N,N,N-trimethylammonium bromide (Chol-ETA) structure where the cholesterol backbone is linked to cationic head via various lengths of ether-linked carbon spacer. The transfection efficiency of these compounds was increased in order of three (Chol-PRO) < four (Chol-BTA) < two (Chol-ETA) methylene unit in their spacer, and was decreased by an addition of isomethyl group to Chol-PRO spacer. In case of the presence of multiple bonds in the spacer, it required the more cationic lipids in liposome formulation than single bond in the spacer to present similar transfection efficiency. Crown Copyright (C) 2011 Published by Elsevier Ltd. All rights reserved.
引用
收藏
页码：3734 / 3737
页数：4
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