Premium
A Surface‐Modified Dendrimer Set for Potential Application as Drug Delivery Vehicles: Synthesis, In Vitro Toxicity, and Intracellular Localization
Author(s) -
Fuchs Sabine,
Kapp Timo,
Otto Henning,
Schöneberg Torsten,
Franke Peter,
Gust Ronald,
Schlüter A. Dieter
Publication year - 2004
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.200305386
Subject(s) - dendrimer , internalization , cytotoxicity , hela , intracellular , confocal microscopy , in vitro , chemistry , biophysics , fluorescence microscope , toxicity , drug delivery , confocal , cell culture , fluorescence , biochemistry , cell , microbiology and biotechnology , biology , organic chemistry , physics , geometry , mathematics , genetics , quantum mechanics
Abstract The synthesis, cytotoxicity, and behavior in cell culture of a new set of first‐ (G1) and second‐generation (G2) dendrimers is reported. The surface functionality of these dendrimers has been varied to see whether structure/toxicity relations can be observed. The outermost functional groups are amines that are decorated either with protons, tert ‐butoxycarbonyl (Boc) or benzyloxycarbonyl (Cbz) protecting groups, Boc‐protected or unprotected natural amino acid residues, ethylenediamine ligands, and/or dansyl fluorescence labels. The cytotoxicity was determined in vitro in concentration‐dependent assays using the human MCF‐7 breast cancer cell line. Cellular uptake and intracellular distribution was monitored by confocal fluorescence microscopy after internalization of the dansyl‐labeled dendrimers by HeLa cells.