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首页> 外文期刊>Journal of peptide science: An official publication of the European Peptide Society >The interaction of cell-penetrating peptides with lipid model systems and subsequent lipid reorganization: thermodynamic and structural characterization
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The interaction of cell-penetrating peptides with lipid model systems and subsequent lipid reorganization: thermodynamic and structural characterization

机译：细胞穿透肽与脂质模型系统的相互作用以及随后的脂质重组：热力学和结构表征

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Cell-penetrating peptides (CPPs) are cationic peptides that are able to induce cellular uptake and delivery of large and hydrophilic molecules, that otherwise do not cross the plasma membrane of eukaryotic cells. Despite their potential use for gene transfer and drug delivery, the mode of action of CPPs is still mysterious. Nonetheless, the interaction with phospholipid bilayers constitutes the first step in the process. The interaction of two CPPs with distinct charge distribution, penetratin (nonamphipathic) and RL16 (a secondary amphipathic peptide with antimicrobial properties) with lipid membranes was investigated. For this purpose, we employed three independent techniques, comprising 31 P-nuclear magnetic resonance, differential scanning calorimetry (DSC), and plasmon waveguide resonance (PWR) spectroscopy. In view of the cationic nature of the peptides, their interaction and affinity for zwitterionic versus anionic lipids was investigated. Although a strong affinity was observed when negative charged lipids were present, the peptides' thermodynamic behavior on binding to zwitterionic versus anionic lipids and the induced supramolecular structure organization in those lipids was quite different. The study suggests that the amphipathic profile and charge distribution of CPPs strongly influences the perturbation mechanism of the peptide on the bilayer establishing the frontier between a pure CPP and a CPP with antimicrobial properties. Copyright (C) 2008 European Peptide Society and John Wiley & Sons, Ltd.
机译：细胞穿透肽（CPPs）是阳离子肽，能够诱导大分子和亲水性分子的细胞摄取和传递，否则它们不会穿过真核细胞的质膜。尽管CPP潜在地用于基因转移和药物递送，但其作用方式仍然是未知的。但是，与磷脂双层的相互作用构成了该过程的第一步。研究了具有不同电荷分布的两种CPPs渗透膜（非两亲性）和RL16（具有抗微生物特性的次级两亲性肽）与脂质膜的相互作用。为此，我们采用了三种独立的技术，包括31 P核磁共振，差示扫描量热法（DSC）和等离激元波导共振（PWR）光谱。考虑到肽的阳离子性质，研究了它们对两性离子与阴离子脂质的相互作用和亲和力。尽管当带负电荷的脂质存在时观察到强亲和力，但是该肽与两性离子脂质与阴离子脂质结合时的热力学行为以及在这些脂质中诱导的超分子结构组织完全不同。研究表明，CPP的两亲性和电荷分布强烈影响肽在双层上的扰动机制，从而在纯CPP和具有抗菌特性的CPP之间建立了边界。版权所有（C）2008欧洲肽协会和John Wiley＆Sons，Ltd.

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