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首页> 外文期刊>Chemistry: A European journal >Anchor dependency for non-glycerol based cationic lipofectins:mixed bag of regular and anomalous transfection profiles
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Anchor dependency for non-glycerol based cationic lipofectins:mixed bag of regular and anomalous transfection profiles

机译：基于非甘油的阳离子lipofectins的锚依赖性：常规和异常转染曲线的混合袋

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摘要

Although detailed structureactivity,physicochemical and biophysicalinvestigations in probing tha anchor influence in liposomal gene delivery have been reported for glycerol-based transfection lipids,the corresponding investigation for non-glycerol based simple monocationic transfection lipids have not yet been undertaken.Towards this end,harein.we delieateour structure-activity and physicochemical approach in deciphering the anchor dependency in liposomal gene delivery using fifteen new structural analogues(lipids 1-15)of recently reported nonglycerol based monocationic transfection lipids.The C_(14) analogues in both series 1(lipids 1-6) and series 2 (lipids 7-15) showed maximum efficiency in transfecting COS-1 and CHO cells.However,the C_(12)analogue ofthe ether series (lipid 3) exhibited a seemingly anomalous behavior compared with its transfection efficient C_(10) and C_(14) analogues (lipids 2 and 4) in being completely inefficient to transfect both COS-1 and CHO cells.The present structure-activity investigation also convincingly demonstrates that enhancement of transfection efficiencies through incorporation of menbrane reorganizing unsaturation elements in the hydrophobic anchor of cationic lipids is not universal but cell dependent.The strength of the interaction of lipids 1-15 with DNA was assessed by their ability to exclude ethidium bromide bound to the DNA.Cationic lipids with long hydrophobic talis were found,in general,to be efficient in excluding EtBr from DNA.Gel to liquid crystalline transition temperatures of the lipids was measured by fluorescence anisotropy measurement technique.In general(lipid 2 being an exception),transfection efficient lipids were found to have their mid transition temperatures at or below physiological temperatures(37degC).
机译：尽管已经报道了基于甘油的转染脂质的详细结构活性，物理化学和生物物理研究在探查锚定在脂质体基因传递中的影响，但尚未进行相应的针对非甘油的简单单阳离子转染脂质的研究。我们使用最近报道的基于非甘油的单阳离子转染脂质的15个新的结构类似物（脂质1-15），揭示了我们的结构活性和理化方法来破译脂质体基因传递中的锚依赖性。两个系列1中的C_（14）类似物（脂质1） -6）和系列2（脂质7-15）在转染COS-1和CHO细胞方面显示出最高效率。然而，与醚系列（脂质3）的C_（12）类似物相比，其转染效率C_表现出看似异常的行为（10）和C_（14）类似物（脂质2和4）完全不能有效转染COS-1和CHO细胞。结构活性研究也令人信服地表明，通过在阳离子脂质的疏水性锚基中掺入膜重组不饱和元素来增强转染效率不是普遍的，而是细胞依赖性的。脂质1-15与DNA相互作用的强度由其能力评估通常，发现具有长疏水性塔利斯的阳离子脂质可以有效地从DNA中排除EtBr。通过荧光各向异性测量技术测量脂质的凝胶到液晶的转变温度。脂质2是一个例外），发现转染有效的脂质的中间转变温度等于或低于生理温度（37°C）。

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