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Labeling, biodistribution and evaluation of [125I] gemcitabine: 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
2009
Tongue
French
Weight
429 KB
Volume
52
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

In this study, the optimization of gemcitabine labeling with iodine‐125 and its biological evaluation are described. Gemcitabine was labeled via direct electrophilic substitution using chloramine‐T as an oxidizing agent. The optimum amounts of reactants were 75 µg gemcitabine, 75 µg chloramine‐T and 18 MBq carrier‐free Na^125^I. The labeled gemcitabine was stable for more than 20 h. Results of the in vivo evaluation revealed that the new tracer, [^125^I] gemcitabine, tends to localize in tissues with high proliferation rate with preferential accumulation in cancerous tissues. Imaging should be carried at 2‐h postinjection. The in vitro cell growth inhibition assay showed that the effect of [^125^I] gemcitabine was stronger than the effect of tenfold cold gemcitabine, which strongly suggested that its cytotoxicity was mainly due to radiotoxicity rather than chemotherapeutic activity. The binding assay revealed that [^125^I] gemcitabine uptake by the Ehrlich cells was high and that it bound well to DNA where the decay of the radionuclide introduced lethal irreversible double‐strand breaks. Copyright © 2009 John Wiley & Sons, Ltd.

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