期刊
CHEMISTRY & BIODIVERSITY
卷 8, 期 1, 页码 1-12出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbdv.201000318
关键词
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资金
- German Federal Ministry of Research and Education (BMBF)
- Swiss National Science Foundation [200020-109065, 200020-117586]
- Novartis Pharma AG Basel
Fluorescein-labeled alpha- and beta-octaarginine amides were synthesized. The route, by which these oligoarginine (OA) derivatives enter cells (hepatocytes, fibroblasts, macrophages), was investigated by confocal fluorescence microscopy. Comparisons (by co-localization experiments) with compounds of known penetration modes revealed that the beta-octaarginine amide also uses multiple pathways to enter cells. There was no difference between the alpha- and the beta-OAs. Like other cell-penetrating peptides (CPPs), the beta-octaarginine eventually winds up in the nucleoli of the cell nuclei (cf Chem. Biodiversity, 2004, 1, 65). Surprisingly, there was no entry of alpha- or beta-OA into intact and healthy human erythrocytes (which do not possess a nucleus). Blood cells infected by Plasmodium fakiparum (malaria parasite) were, however, entered readily, and the OAs went all the way through a couple of membranes into the parasite. The potential of these results for delivering specific antimalarial drugs directly into the parasite is discussed.
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