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Preparation and evaluation of [125I]troxacitabine: L-nucleoside model of a potential agent for tumor diagnosis and radiotherapy

✍ Scribed by O. A. El-Kawy; A. M. Hashem; M. A. Amin; A. S. El-Wetery

Publisher
John Wiley and Sons
Year
2010
Tongue
French
Weight
207 KB
Volume
54
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

In this study, the optimization of troxacitabine labeling with iodine‐125 and its biological evaluation were described. Troxacitabine was labeled via direct electrophilic substitution using chloramine‐T as oxidizing agent. The optimum amounts of reactants were: 50 µg troxacitabine, 75 µg Chloramine‐T and ∼19 kBq carrier free Na^125^I. The labeled troxacitabine was stable for more than 24 h. Results of the in‐vivo evaluation revealed that the new tracer, [^125^I]troxacitabine, tends to localize in tissues with high proliferation rate with preferential accumulation in cancerous tissues. Imaging should be carried at 3 h postinjection. The in vitro cell growth inhibition assay showed that the effect of [^125^I]troxacitabine was stronger than the effect of cold troxacitabine, which strongly suggested that its cytotoxicity was mainly due to radiotoxicity rather than chemotherapeutic activity. The binding assay revealed that [^125^I]troxacitabine uptake by the Ehrlich and the ARAC8C cells was high and that it bounded well to DNA. Copyright © 2010 John Wiley & Sons, Ltd.

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