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首页> 外文期刊>The journal of physical chemistry, B. Condensed matter, materials, surfaces, interfaces & biophysical >Characterization of Cell-Penetrating Lipopeptide Micelles by Spectroscopic Methods
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Characterization of Cell-Penetrating Lipopeptide Micelles by Spectroscopic Methods

机译：光谱法表征细胞穿透脂肽胶束

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摘要

The transport of bioactive compounds to the site of action is a great challenge. A promising approach to overcome application-related problems is the development of targeting colloidal transport systems, such as micelles which are equipped with uptake mediating moieties. Here, we investigated a set of novel lipopeptides which exhibit a surfactant-like structure due to attachment of two palmitoyl chains to the N-terminus of cationic or anionic amino acid sequences. We analyzed the association behavior of these lipopeptides by using 5(6)-carboxyfluorescein (CF)-labeled derivatives as a fluorescent probe and different spectroscopic methods such as fluorescence anisotropy and fluorescence correlation spectroscopy (FCS). The photophysical properties as well as the diffusion and rotational movements of the CF-labeled lipopeptides were exploited to determine the cmc and the size of the micelles consisting of lipopeptides. We could distinguish cationic and anionic lipopeptides by their association behavior and by studying the interactions with mouse brain capillary endothelial cells (b.end3). The cationic derivatives turned out to be very strong surfactants with a very low cmc in the micromolar range (0.5—14 μM). The unique combination of micelle-forming property and cell-penetrating ability can pave the road for the development of a novel class of efficient drug Carrier systems.
机译：生物活性化合物向作用部位的运输是一个巨大的挑战。克服与应用相关的问题的一种有前途的方法是开发靶向胶体运输系统，例如配备有摄取介导部分的胶束。在这里，我们研究了一组新颖的脂肽，该脂肽由于两个棕榈酰基链与阳离子或阴离子氨基酸序列的N端相连而表现出类似表面活性剂的结构。我们通过使用5（6）-羧基荧光素（CF）标记的衍生物作为荧光探针和不同的光谱方法，如荧光各向异性和荧光相关光谱（FCS），分析了这些脂肽的缔合行为。利用CF标记的脂肽的光物理性质以及扩散和旋转运动来确定由脂肽组成的胶束的cmc和大小。我们可以通过它们的缔合行为以及研究与小鼠脑毛细血管内皮细胞的相互作用来区分阳离子和阴离子脂肽（b.end3）。阳离子衍生物证明是非常强的表面活性剂，其微摩尔范围（0.5-14μM）中的cmc非常低。胶束形成特性和细胞穿透能力的独特结合可以为新型高效药物载体系统的开发铺平道路。

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