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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Cationic lioposomes with folic acid as targeting ligand for gene delivery
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Cationic lioposomes with folic acid as targeting ligand for gene delivery

机译:以叶酸为靶向配体的阳离子脂质体,用于基因递送

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In our previous Letter, we have carried out the synthesis of a novel DDCTMA cationic lipid which was formulated with DOPE for gene delivery. Herein, we used folic acid (FA) as targeting ligand and cholesterol (Chol) as helper lipid instead of DOPE for enhancing the stability of the liposomes. These liposomes were characterized by dynamic laser scattering (DLS), transmission electron microscopy (TEM) and agarose gel electrophoresis assays of pDNA binding affinity. The lipoplexes were prepared by using different weight ratios of DDCTMA/Chol (1:1, 2:1, 3:1, 4:1) liposomes and different concentrations of FA (50-200 mu g/mL) combining with pDNA. The transfection efficiencies of the lipoplexes were evaluated using pGFP-N2 and pGL3 plasmid DNA against NCI-H460 cells in vitro. Among them, the optimum gene transfection efficiency with DDCTMA/Chol (3:1)/FA (100 mu g/mL) was obtained. The results showed that FA could improve the gene transfection efficiencies of DDCTMA/Chol cationic liposome. Our results also convincingly demonstrated FA (100 mu g/mL)-coated DDCTMA/Chol (3:1) cationic liposome could serve as a promising candidate for the gene delivery. (C) 2016 Elsevier Ltd. All rights reserved.
机译:在我们之前的信中,我们已经合成了一种新的DDCTMA阳离子脂质,该脂质与DOPE配制用于基因传递。在本文中,我们使用叶酸(FA)作为靶向配体,使用胆固醇(Chol)作为辅助脂质代替DOPE来增强脂质体的稳定性。这些脂质体的特征在于动态激光散射(DLS),透射电子显微镜(TEM)和pDNA结合亲和力的琼脂糖凝胶电泳分析。通过使用不同重量比的DDCTMA / Chol(1:1,2:1,3:1,4:1)脂质体和不同浓度的FA(50-200μg / mL)与pDNA制备脂质体。使用pGFP-N2和pGL3质粒DNA体外评估NCI-H460细胞对脂质复合物的转染效率。其中,获得了用DDCTMA / Chol(3:1)/ FA(100μg / mL)的最佳基因转染效率。结果表明,FA可以提高DDCTMA / Chol阳离子脂质体的基因转染效率。我们的结果也令人信服地证明,FA(100μg / mL)包被的DDCTMA / Chol(3:1)阳离子脂质体可以作为有希望的基因传递候选物。 (C)2016 Elsevier Ltd.保留所有权利。

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