title: In Vitro/In Vivo Evaluation of Radiolabeled [(99m)Tc(CO)3](+)-Hydroxyurea and Fluorescein Isothiocyanate-Hydroxyurea.
abstract: The aim of current study is to examine hydroxyurea (HU), which is an antineoplastic drug used for the treatment of leukemia, sickle-cell disease, HIV, psoriasis, thrombocythemia, and various neoplastic diseases in two aspects. The active ingredient hydroxyurea was obtained by purification of the capsule form drug, commercially named as HYDREA. Then, [(99m)Tc(CO)3](+)core radiolabeling with HU was performed as first aspect. Quality control studies of (99m)Tc(CO)3-HU complex were performed by thin-layer radiochromatography and high-performance liquid radiochromatography methods. The results demonstrated that the radiolabeling yield was quite high (98.43% ± 2.29%). Also, (99m)Tc(CO)3-HU complex has good stability during the 24-hour period. Biological behavior of (99m)Tc(CO)3-HU complex is evaluated by biodistribution studies on Wistar Albino rats. Fluorescein isothiocyanate (FITC) labeling of HU was performed as second aspect. Fluorometric evaluation of binding efficacy and fluorescence imaging studies on MCF7 and Hela cell lines were carried out. It was thought that the knowledge achieved in this study would contribute to using (99m)Tc(CO)3-HU complex as an imaging agent, which inhibits the DNA synthesis selectively, by inhibiting ribonucleotide reductase enzyme. It was observed that FITC-HU has noteworthy incorporation on both cell lines.
authors: Institute of Nuclear Sciences, Ege University , Izmir, Turkey .
authors: Baris
authors: B
authors: Yilmaz
authors: Institute of Nuclear Sciences, Ege University , Izmir, Turkey .
authors: Serap
authors: S
authors: Teksoz
authors: Institute of Nuclear Sciences, Ege University , Izmir, Turkey .
authors: Ayfer Yurt
authors: AY
authors: Kilcar
authors: Institute of Nuclear Sciences, Ege University , Izmir, Turkey .
authors: Eser
authors: E
authors: Ucar
authors: Institute of Nuclear Sciences, Ege University , Izmir, Turkey .
authors: Cigdem
authors: C
authors: Ichedef
authors: Institute of Nuclear Sciences, Ege University , Izmir, Turkey .
authors: Emin Ilker
authors: EI
authors: Medine
authors: Institute of Nuclear Sciences, Ege University , Izmir, Turkey .
authors: Kadir
authors: K
authors: Ari
mesh_terms: D000818:Animals; D001943:Breast Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000473:pathology; D003911:Dextrans / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000737:chemistry; D005260:Female; D016650:Fluorescein-5-isothiocyanate / Q000031:analogs & derivatives* / Q000737:chemistry; D006918:Hydroxyurea / Q000737:chemistry*; D066298:In Vitro Techniques; D008297:Male; D061848:Optical Imaging; D015609:Organotechnetium Compounds / Q000493:pharmacokinetics*; D010051:Ovarian Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000473:pathology; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D014407:Tumor Cells, Cultured
chemical_list: D003911:Dextrans; D004791:Enzyme Inhibitors; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C015219:fluorescein isothiocyanate dextran; D016650:Fluorescein-5-isothiocyanate; D006918:Hydroxyurea
keywords: [99mTc(CO)3]+ core; antineoplastic; fluorescence imaging; hydroxyurea; in vitro/in vivo