Issue 2, 2010
From the journal:

New Journal of Chemistry

Synthesis and characterization of a highly stable dendritic catechol-tripod bearing technetium-99m†

Annabelle Bertin,a   Anne-Isabelle Michou-Gallani,b   Jérôme Steibel,c   Jean-Louis Gallania  and  Delphine Felder-Flesch*a  

* Corresponding authors

a IPCMS/DMO, UMR CNRS/UDS 7504, 23 rue du loess, BP 43 67034 Strasbourg cedex 2, France
E-mail: Delphine.Felder@ipcms.u-strasbg.fr
Fax: + 33 3 88 10 72 46
Tel: + 33 3 88 10 71 63

b siRNA Therapeutics, NIBR Biologics center, Novartis Institute for Biomedical Research, Inc. 4002 Basel, Switzerland

c LINC, UMR CNRS/UDS 7191, 12 rue Goethe, 67000 Strasbourg, France

Abstract

The synthesis and preliminary biological tests (in vitro toxicity, in vitro stability) of new Tc(III)-radiolabelled dendro-chelates are presented. A dendritic 99mTc chelate 1 derived from a pre-organized tripodal tris-catecholamide exhibits a kinetic stability by far more important than its corresponding diethylenetriamine pentaacetic acid (DTPA) homologue 2. This permitted an assessment of the real impact of the pre-organized tripodal structure on kinetic inertness (and thus toxicity), an important issue to address when considering in vivo applications. Radiolabelling was performed using the stannous chloride reduction method; while DTPA-homologue 2 showed a high radiolabelling efficiency (96% radiolabelling yield after 30 min), tripodal complex 1 induced a 93% complexation yield after 45 min. In contrast, radiocomplex 1 derived from the most rigid and organized structure has a higher kinetic stability than 2. Indeed, while dissociation of 2 reached 50% after 1 h 30 min in physiological media like phosphate buffer saline (PBS) and bovine serum albumin (BSA), over 80% of 1 remained stable during the half-life of the radionucleide (6.02 h for 99mTc). Measurements of the cell leakage resulting from membrane damage of neuronal cells treated with increasing concentrations of dendritic ligand 16, together with pictures of treated neurons after staining, showed no detectable toxicity.

Graphical abstract: Synthesis and characterization of a highly stable dendritic catechol-tripod bearing technetium-99m

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Article information

DOI
https://doi.org/10.1039/B9NJ00305C
Article type
Paper
Submitted
02 Jul 2009
Accepted
28 Sep 2009
First published
29 Oct 2009

New J. Chem., 2010,34, 267-275

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Synthesis and characterization of a highly stable dendritic catechol-tripod bearing technetium-99m

A. Bertin, A. Michou-Gallani, J. Steibel, J. Gallani and D. Felder-Flesch, New J. Chem., 2010, 34, 267 DOI: 10.1039/B9NJ00305C

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