Diethylstilbestrol glucuronide (DESG): synthesis, labeling with radioiodine and in vivo/in vitro evaluations

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dc.contributor.authorYilmaz, Tayfun
dc.contributor.authorUnak, Perihan
dc.contributor.authorMuftuler, Fazilet Zumrut Biber
dc.contributor.authorMedine, Emin Ilker
dc.contributor.authorSakarya, Serhan
dc.contributor.authorIchedef, Cigdem Acar
dc.contributor.authorUnak, Turan
dc.date.accessioned2019-10-27T21:53:18Z
dc.date.available2019-10-27T21:53:18Z
dc.date.issued2013
dc.departmentEge Üniversitesien_US
dc.description.abstractDiethylstilbestrol (DES) is a synthetic non-steroidal estrogen, pharmacologic effects of which resemble natural estrons; today it is being used to treat some types of postmenopausal breast cancer and advanced prostate cancer. The aim of current study is conjugation of glucuronic acid (G) to DES and to evaluate radiopharmaceutical potential of this estrogen glucuronide derivative (DESG) which is specific to beta glucuronidase enzyme consisting tumor cells. Taking into consideration the compatibility to the chemical structures of the synthesized product, I-131 and I-125 were chosen as the appropriate radionuclides and DESG was labeled with these radionuclides utilizing iodogen method. The radiochemical yields of I-125/131-DESG were over 90 % according to thin layer radio chromatography method. The biodistribution of I-131-DESG in healthy female Wistar Albino rats has been investigated and the range of the breast/blood and breast/muscle ratios were approximately 2 and 13 in 240 min for ER unsaturated studies. Effects of the radioiodinated DES and DESG on the cells were examined using MCF-7, A-549, Caco-2 cell lines. I-125-DESG has higher incorporation percentages than I-125-DES on MCF-7 cells. The radioiodinated DESG has the desired radiopharmaceutical properties which could be candidate radiopharmaceuticals for diagnosis and especially radionuclide therapy of breast tumors.en_US
dc.description.sponsorshipEge University Scientific Research FundEge University [2009NBE001]en_US
dc.description.sponsorshipAuthors thank to Dr. Turkan ERTAY and PhD student Ilknur DEMIR INCI for biodistribution studies, PhD student Ayfer YURT KILCAR for technical help and also Ege University Scientific Research Fund with the Project Number 2009NBE001 for the financial support.en_US
dc.identifier.doi10.1007/s10967-012-2226-8
dc.identifier.endpage1404en_US
dc.identifier.issn0236-5731
dc.identifier.issn1588-2780
dc.identifier.issn0236-5731en_US
dc.identifier.issn1588-2780en_US
dc.identifier.issue2en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.startpage1395en_US
dc.identifier.urihttps://doi.org/10.1007/s10967-012-2226-8
dc.identifier.urihttps://hdl.handle.net/11454/47862
dc.identifier.volume295en_US
dc.identifier.wosWOS:000313713300082en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.language.isoenen_US
dc.publisherSpringeren_US
dc.relation.ispartofJournal of Radioanalytical and Nuclear Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectDiethylstilbestrol (DES)en_US
dc.subjectRadiolabeleden_US
dc.subjectI-125/131en_US
dc.subjectDiethylstilbestrol glucuronide (DESG)en_US
dc.titleDiethylstilbestrol glucuronide (DESG): synthesis, labeling with radioiodine and in vivo/in vitro evaluationsen_US
dc.typeArticleen_US

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