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On the Mechanism of Eukaryotic Cell Penetration by α ‐ and β ‐Oligoarginines – Targeting Infected Erythrocytes
Author(s) -
Kamena Faustin,
Monnanda Bopanna,
Makou Danielle,
Capone Stefania,
PatoraKomisarska Krystyna,
Seebach Dieter
Publication year - 2011
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201000318
Subject(s) - plasmodium falciparum , confocal microscopy , chemistry , nucleolus , parasite hosting , organelle , microbiology and biotechnology , cell penetrating peptide , cell , penetration (warfare) , fluorescence microscope , confocal , flow cytometry , cell membrane , biophysics , fluorescence , cytoplasm , biochemistry , malaria , biology , immunology , physics , geometry , mathematics , operations research , quantum mechanics , world wide web , computer science , engineering
Abstract Fluorescein‐labeled α ‐ and β ‐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 β ‐octaarginine amide also uses multiple pathways to enter cells. There was no difference between the α ‐ and the β ‐OAs. Like other cell‐penetrating peptides (CPPs), the β ‐octaarginine eventually winds up in the nucleoli of the cell nuclei ( cf. Chem. Biodiversity , 2004 , 1 , 65). Surprisingly, there was no entry of α ‐ or β ‐OA into intact and healthy human erythrocytes (which do not possess a nucleus). Blood cells infected by Plasmodium falciparum (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.