Document Detail

Enzymatic synthesis of uracil glucuronide, labeling with 125/131I, and in vitro evaluation on adenocarcinoma cells.
MedLine Citation:
PMID:  20578839     Owner:  NLM     Status:  MEDLINE    
Human 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 (125/131)I-UNG and (125/131)I-UOG presented good incorporation ratios for Hutu-80, Caco-2, Detroit 562, and ACBRI 519 cells. The incorporation ratios of (125/131)I-UOG were higher than those of (125/131)I-UNG and of other labeled components for all cell types, and were also statistically significant compared to the values of (125/131)I-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.
Ilker Emin Medine; Perihan Unak; Serhan Sakarya; Feriha Toksöz
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Publication Detail:
Type:  Evaluation Studies; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Cancer biotherapy & radiopharmaceuticals     Volume:  25     ISSN:  1557-8852     ISO Abbreviation:  Cancer Biother. Radiopharm.     Publication Date:  2010 Jun 
Date Detail:
Created Date:  2010-06-28     Completed Date:  2011-01-31     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9605408     Medline TA:  Cancer Biother Radiopharm     Country:  United States    
Other Details:
Languages:  eng     Pagination:  335-44     Citation Subset:  IM    
Department of Nuclear Applications, Institute of Nuclear Sciences, Ege University, Bornova, Izmir, Turkey.
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MeSH Terms
Adenocarcinoma / enzymology,  metabolism*
Cell Line
Cell Line, Tumor
Chromatography, High Pressure Liquid
Glucuronidase / metabolism
Glucuronides / biosynthesis*,  chemistry,  metabolism
Glucuronosyltransferase / isolation & purification,  metabolism*
Hydrophobic and Hydrophilic Interactions
Iodine Radioisotopes / chemistry*
Isotope Labeling / methods*
Microsomes / chemistry,  enzymology
Molecular Structure
Spectrometry, Mass, Electrospray Ionization
Tandem Mass Spectrometry
Uracil / analogs & derivatives*,  biosynthesis*,  chemistry,  metabolism
Uridine Diphosphate Glucuronic Acid / metabolism
Reg. No./Substance:
0/Glucuronides; 0/Iodine Radioisotopes; 2616-64-0/Uridine Diphosphate Glucuronic Acid; 66-22-8/Uracil; EC; EC 1A9; EC

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