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首页> 外文期刊>Chemistry: A European journal >Folate-Equipped Pegylated Archaeal Lipid Derivatives: Synthesis and Transfection Properties
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Folate-Equipped Pegylated Archaeal Lipid Derivatives: Synthesis and Transfection Properties

机译：叶酸装备的聚乙二醇化古细菌脂质衍生物：合成和转染特性。

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摘要

We have previously shown that synthetic archaeal lipid analogues are useful vectors for drug/gene delivery. We report herein the synthesis and gene transfer properties of a series of novel di- and tetraether-type archaeal derivatives with a poly(ethylene glycol) (PEG) chain and further equipped with a folic acid (FA) group. The synthetic strategy and the purification by dialysis ensured complete removal of free FA. The lipids were mixed with a conventional glycine betaine-based cationic lipid and the resulting formulations were tested in transfection assays after complexation) with plasmid DNA. All four novel co-lipids afforded efficient in vitro gene transfection. Moreover, the FA-equipped derivatives permitted ligand/reccptor-based targeted transfection: their activity was inhibited when free FA was added to the transfection medium. These novel archaeal derivatives equipped with FA-PEG moieties may thus be of great interest for targeted in vivo transfection.
机译：先前我们已经表明，合成的古细菌脂质类似物是用于药物/基因递送的有用载体。我们在此报告了一系列具有聚（乙二醇）（PEG）链并进一步配备叶酸（FA）基团的新型二醚和四醚型古细菌衍生物的合成和基因转移特性。合成策略和通过透析纯化确保完全去除游离FA。将脂质与常规的基于甘氨酸甜菜碱的阳离子脂质混合，并在与质粒DNA复合后在转染测定中测试所得制剂。所有四种新型共脂质都提供了有效的体外基因转染。此外，配备FA的衍生物允许进行基于配体/受体的靶向转染：将游离FA添加到转染培养基中会抑制其活性。这些具有FA-PEG部分的新颖的古细菌衍生物因此对于靶向体内转染可能具有极大的兴趣。

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