Radioiodination and biological evaluation of Cladribine as potential agent for tumor imaging and therapy
Bayoumi, NA; Amin, AM; Ismail, NSM; Abouzid, Khaled; El-Kolaly, MT;
Abstract
Cladribine, a purine analogue antimetabolite, was radioiodinated with 125I via direct electrophilic substitution reaction. The maximum radiochemical yield (92.5 ± 0.8%) was obtained when the reaction was done at ambient temperature for 30 min using 100 μg of Cladribine and 10 μg N-chlorosuccinamide (NCS) in 150 μL of 0.2 M phosphate buffer, pH 7. In vitro stability studies of HPLC purified 125I-Cladribine sample dissolved in 0.5 ml of 0.2 M phosphate buffer pH 7 at ambient temperature showed that 125I-Cladribine is stable up to 12 h post labeling. Biodistribution results revealed excretion of 125I-Cladribine mainly by kidneys. The uptake of 125I-Cladribine in the induced Ehrlich Ascites Carcinoma was 2.8 ± 0.4 %ID/g at 1 h post injection with maximum tumor/muscle ratio of 5.5. The good uptake of 125I-Cladribine confirms the molecular docking studies results which indicate that iodinated Cladribine binds with polymerase enzyme with a good -CDOCKER energy. As a result, radioiodinated Cladribine may be used as a valuable agent for tumor diagnosis and therapy.
Other data
Title | Radioiodination and biological evaluation of Cladribine as potential agent for tumor imaging and therapy | Authors | Bayoumi, NA; Amin, AM; Ismail, NSM; Abouzid, Khaled ; El-Kolaly, MT | Keywords | Cladribine;radioiodination;N-chlorosuccinamide (NCS);tumor;diagnosis;therapy;ENERGY | Issue Date | 2015 | Publisher | WALTER DE GRUYTER GMBH | Journal | Radiochimica Acta | Volume | 103 | Issue | 11 | ISSN | 0033-8230 | DOI | 10.1515/ract-2014-2357 | Scopus ID | 2-s2.0-84946232440 | Web of science ID | WOS:000363907500004 |
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