Investigations on the use of fluorescence dyes for labeling dendrimers: cytotoxicity, accumulation kinetics, and intracellular distribution.
Fluorescent dyes (e.g., dansyl, fluoresceine isothiocyanate, or naphthalimide groups) are widely used as markers to study biological properties of drugs. In order to evaluate possible mediated cytotoxicity, we attached three molecules each to 1,3,5-tris(3-propylamino)benzene initially synthesized as core molecule for the design of dendrimers. Cytotoxic effects were only observed for the NO(2)-substituted naphthalimide conjugate. The intracellular distribution was visualized via confocal fluorescence microscopy and pointed to an accumulation in the endosome or nucleus, dependent on the cell line used.
Institute of Pharmacy, Freie Universität Berlin, Berlin, Germany.
A M
AM
Scutaru
M
M
Krüger
M
M
Wenzel
J
J
Richter
R
R
Gust
D000230:Adenocarcinoma / Q000188:drug therapy / Q000473:pathology; D001555:Benzene Derivatives / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D002467:Cell Nucleus / Q000187:drug effects / Q000648:ultrastructure; D002470:Cell Survival / Q000187:drug effects; D003619:Dansyl Compounds / Q000737:chemistry / Q000493:pharmacokinetics* / Q000633:toxicity; D050091:Dendrimers / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D011992:Endosomes / Q000187:drug effects / Q000648:ultrastructure; D005260:Female; D016650:Fluorescein-5-isothiocyanate / Q000737:chemistry / Q000493:pharmacokinetics* / Q000633:toxicity; D005453:Fluorescence; D005456:Fluorescent Dyes / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D006801:Humans; D007700:Kinetics; D018613:Microscopy, Confocal; D053644:Naphthalimides / Q000737:chemistry / Q000493:pharmacokinetics* / Q000633:toxicity
D001555:Benzene Derivatives; D003619:Dansyl Compounds; D050091:Dendrimers; D005456:Fluorescent Dyes; D053644:Naphthalimides; D016650:Fluorescein-5-isothiocyanate