Enzymatic synthesis of uracil glucuronide, labeling with 125/131I, and in vitro evaluation on adenocarcinoma cells

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dc.contributor.authorMedine I.E.
dc.contributor.authorUnak P.
dc.contributor.authorSakarya S.
dc.contributor.authorToksöz F.
dc.date.accessioned2019-10-27T08:34:52Z
dc.date.available2019-10-27T08:34:52Z
dc.date.issued2010
dc.departmentEge Üniversitesien_US
dc.description.abstractHuman UDP-glucuronosyltransferases (UGTs) are a family of membrane-bound enzymes of the endoplasmic reticulum. They catalyze the glucuronidation of various endogenous and exogenous compounds, converting them into more polar glucuronides. In this study, uracil glucuronide was enzymatically synthesized using a UGT-rich microsome preparate, which was separated from Hutu-80 cells. Two different glucuronide derivatives were obtained, with a total reaction yield of 22.95% ± 2.4% (n = 4). The glucuronide ligands were defined as uracil-n-glucuronide (UNG) and uracil-o-glucuronide (UOG). These were then analyzed by high-performance liquid chromatography-mass spectrometry and labeled with I-125 and I-131, separately. The radiolabeled 125/131I-UNG and 125/131I-UOG presented good incorporation ratios for Hutu-80, Caco-2, Detroit 562, and ACBRI 519 cells. The incorporation ratios of 125/131I-UOG were higher than those of 125/131I-UNG and of other labeled components for all cell types, and were also statistically significant compared to the values of 125/131I-UNG for primary human intestinal epithelial cells (ACBRI 519) and human intestinal adenocarcinoma cells. Cell incorporation rates of n-glucuronides and o-glucuronides were higher compared to uracil, with o-glucuronides being more selective. The results suggest that both I-125- and I-131-labeled glucuronides can be used in imaging and therapy, and further research should be done in preclinical stages. © 2010, Mary Ann Liebert, Inc. 2010.en_US
dc.identifier.doi10.1089/cbr.2009.0727en_US
dc.identifier.endpage344en_US
dc.identifier.issn1084-9785
dc.identifier.issue3en_US
dc.identifier.pmid20578839en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.startpage335en_US
dc.identifier.urihttps://doi.org/10.1089/cbr.2009.0727
dc.identifier.urihttps://hdl.handle.net/11454/27126
dc.identifier.volume25en_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.relation.ispartofCancer Biotherapy and Radiopharmaceuticalsen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subject125Ien_US
dc.subject131Ien_US
dc.subjectadenocarcinoma cell linesen_US
dc.subjectUDP glucuronidaseen_US
dc.subjecturacil glucuronideen_US
dc.titleEnzymatic synthesis of uracil glucuronide, labeling with 125/131I, and in vitro evaluation on adenocarcinoma cellsen_US
dc.typeArticleen_US

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