Porret Estelle, Fleury Jean-Baptiste, Sancey Lucie, Pezet Mylène, Coll Jean-Luc, Le Guével Xavier
Cancer Targets & Experimental Therapeutics, Institute for Advanced Biosciences (IAB), University of Grenoble Alpes (UGA)/INSERM-U1209/CNRS-UMR 5309 Grenoble France
Experimental Physics and Center for Biophysics, Saarland University D-66123 Saarbrücken Germany.
RSC Adv. 2020 Feb 11;10(11):6436-6443. doi: 10.1039/c9ra10047d. eCollection 2020 Feb 7.
A library of ultra-small red photoluminescent gold nanoclusters (Au NCs) were synthesized with an increasing amount of positive charges provided by the addition of mono-, di- or trivalent-glutathione modified arginine peptides. We then studied how the arginine content impacted on the interaction of Au NCs with negatively charged artificial lipid bilayers and cell membranes. Results indicated that increasing the arginine content enhanced Au NCs' adsorption on lipid bilayers and on cell membranes followed by an increased cellular uptake in melanoma cells (COLO 829). Surprisingly, the presence of up to 40% serum for highly positively charged Au NCs did not hinder their interaction with lipid bilayers that contain glycolipids, suggesting a reduced opsonization of these Au NCs. In addition, these Au NCs are usually not toxic, except those with the highest arginine contents. Thus, controlled grafting of arginine peptides onto Au NCs is an elegant strategy to improve their binding and internalization by tumor cells while still keeping their anti-fouling properties.
通过添加单、二或三价谷胱甘肽修饰的精氨酸肽来提供越来越多的正电荷，合成了超小红色光致发光金纳米团簇（Au NCs）库。然后，我们研究了精氨酸含量如何影响Au NCs与带负电荷的人工脂质双层和细胞膜的相互作用。结果表明，增加精氨酸含量可增强Au NCs在脂质双层和细胞膜上的吸附，随后黑色素瘤细胞（COLO 829）对其细胞摄取增加。令人惊讶的是，对于高正电荷的Au NCs，高达40%血清的存在并不妨碍它们与含有糖脂的脂质双层的相互作用，这表明这些Au NCs的调理作用降低。此外，这些Au NCs通常无毒，除了那些精氨酸含量最高的。因此，将精氨酸肽可控地接枝到Au NCs上是一种巧妙的策略，可提高它们与肿瘤细胞的结合和内化，同时仍保持其抗污性能。
