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首页> 外文期刊>Bulletin of the Chemical Society of Japan >Synthesis and Evaluation of Cationic Lipids Bearing Cholesteryl Groups for Gene Delivery In Vitro
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Synthesis and Evaluation of Cationic Lipids Bearing Cholesteryl Groups for Gene Delivery In Vitro

机译:带有胆固醇基团的阳离子脂质的合成与体外基因传递评价

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摘要

A series of cationic lipids were designed and synthesized as vectors for gene delivery. The lipids contain a ketal moiety as a linker and a cholesteryl group as a hydrophobic tail. The framework of cholesteryl derivatives could increase the stability of liposomes by stabilizing the bilayers and their complexes with DNA to improve the transfection efficiency. The ketal bonds in lipids should easily degrade in an acidic environment in a cell (pH = 2-5) after transfecftion, resulting in little toxicity; in the neutral environment outside of cells (pH = 7), they should be stable as gene carriers. Gene transfer experiments in vitro with BL-6, 3LL, 293, 3T3, and Hela cells were performed. The results show that the gene transfection activity of three lipids is quite high, with least toxicity to cells under the experimental conditions.
机译:设计并合成了一系列阳离子脂质作为用于基因递送的载体。脂质含有作为连接物的缩酮部分和作为疏水尾巴的胆固醇基。胆固醇衍生物的骨架可以通过稳定双层及其与DNA的复合物来提高脂质体的稳定性,从而提高转染效率。转染后,脂质中的缩酮键应在酸性环境中(pH = 2-5)容易降解,因此毒性很小。在细胞外的中性环境(pH = 7)中,它们应作为基因载体稳定。进行了BL-6、3LL,293、3T3和Hela细胞的体外基因转移实验。结果表明,三种脂质的基因转染活性很高,在实验条件下对细胞的毒性最小。

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