Jump to main content
Jump to site search

Issue 5, 2015
Previous Article Next Article

Synthesis of a new HYNIC-DAPI derivative for labelling with 99mTechnetium and its in vitro evaluation in an FRTL5 cell line

Author affiliations

Abstract

4′,6-Diamidine-2-phenylindole (DAPI) is a common fluorochrome that is able to bind to deoxyribonucleic acid (DNA) with distinct, sequence-dependent enhancement of fluorescence. This work presents the synthesis of a new multifunctional compound that includes the fluorescent dye as a 99mTechnetium (99mTc) carrier. A new technique for the bioconjugation of DAPI with 6-hydrazinonicotinic acid (HYNIC) through an amide linkage was developed. The radiolabelling was performed with HYNIC as a chelator and N-(2-hydroxy-1,1-bis(hydroxymethyl)ethyl)glycine (tricine) as a coligand. Furthermore, experimental evidence showed that 99mTc complexes with DAPI as DNA-binding moieties are detectable in living Fischer rat thyroid follicular cell line 5 (FRTL5) and their nuclei. The investigations indicated further that the new HYNIC-DAPI derivative is able to interact with double-stranded DNA. This establishes the possibility of locating 99mTc in close proximity to biological structures of living cells, of which especially the genetic information-carrying cell compartments are at the centre of interest. In this context, further investigations are related to the radiotoxic effects of DNA-bound 99mTc-HYNIC-DAPI derivatives and dosimetric calculations.

Graphical abstract: Synthesis of a new HYNIC-DAPI derivative for labelling with 99mTechnetium and its in vitro evaluation in an FRTL5 cell line

Back to tab navigation

Article information


Submitted
24 Dec 2014
Accepted
06 Mar 2015
First published
23 Mar 2015

Med. Chem. Commun., 2015,6, 887-897
Article type
Concise Article
Author version available

Synthesis of a new HYNIC-DAPI derivative for labelling with 99mTechnetium and its in vitro evaluation in an FRTL5 cell line

S. Ferl, G. Wunderlich, R. Smits, A. Hoepping, A. Naumann and J. Kotzerke, Med. Chem. Commun., 2015, 6, 887
DOI: 10.1039/C4MD00574K

Search articles by author

Spotlight

Advertisements