Institute of Food Chemistry and Toxicology, Faculty of Chemistry, University of Vienna, Waehringer Strasse 38, 1090 Vienna, Austria.
Institute of Biological Chemistry, Faculty of Chemistry, University of Vienna, Waehringer Strasse 38, 1090 Vienna, Austria.
Chem Commun (Camb). 2019 Aug 21;55(65):9649-9652. doi: 10.1039/c9cc02215e. Epub 2019 Jul 24.
Intracellular delivery of bioactive polyphenols is currently evaluated as a protective strategy for cells under pharmaceutical stress. To this end, the 20mer R5 peptide from the marine diatom C. fusiformis was N-terminally modified with a quercetin derivative. This polyphenol-peptide conjugate was used to generate homogeneous silica particles under biomimetic conditions that are efficiently taken up by eukaryotic cells without being cytotoxic. However, not only was accumulation in the cytoplasm of living cells observed via electron and fluorescence microscopy but also translocation into the nucleus. The latter was only seen when the quercetin-peptide conjugate was present within the silica particles and provides a novel targeting option for silica particles to nuclei.
目前，人们将生物活性多酚的细胞内递呈评估为细胞在药物应激下的一种保护策略。为此，从海洋硅藻 C. fusiformis 中提取的 20 肽 R5 的 N 端被槲皮素衍生物修饰。该多酚-肽缀合物在仿生条件下被用来生成均匀的硅颗粒，这些硅颗粒可有效地被真核细胞摄取，而没有细胞毒性。然而，不仅通过电子和荧光显微镜观察到在活细胞的细胞质中的积累，还观察到易位到细胞核中。当槲皮素-肽缀合物存在于硅颗粒中时，才会出现后一种情况，这为硅颗粒进入细胞核提供了一种新的靶向选择。
