量研学術機関リポジトリ「QST-Repository」は、国立研究開発法人 量子科学技術研究開発機構に所属する職員等が生み出した学術成果（学会誌発表論文、学会発表、研究開発報告書、特許等）を集積しインターネット上で広く公開するサービスです。 Welcome to QST-Repository where we accumulates and discloses the academic research results(Journal Publications, Conference presentation, Research and Development Report, Patent, etc.) of the members of National Institutes for Quantum Science and Technology.
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Evaluation of radiobromine-labeled 5-bromo-4'-thio-2'-deoxyuridine uptake in ACHN cells after treatment with 5-fluorouracil: comparison with 3H-FLT uptake.
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Objectives: We have recently developed the radiobromine-labeled 5-bromo 4'-thio-2'-deoxyuridine (BTdU) as an imaigng agent for tumor proliferation. The aim of this study was to evaluate the potential usefulness of radiobromine-labeled BTdU as an imaging agent for detecting the early therapeutic effects of 5-fluorouracil (5-FU) compared with 3H-FLT uptake.
\nMethods: The radiolabeling of BTdU with 77Br was achieved by a destannylation reaction of tributylstannyl precursor. 3H-FLT was commerically available. The cells of human renal cacinoma cell line, ACHN, were treated with various concentrations of 5-FU (0.01-300 µM). At 36 hr after 5-FU addition, double tracer cell uptake studies were performed. 2.0x10-2 MBq of 77Br-BTdU and 3.7x10-2 MBq of 3H-FLT were simaltaneously added to the cells and incubated for 15min, 30min, 60min. After 3 times washing, cells were lysed, and then the radioactivity and protein content were measured.
\nResults: The radiochemical yield of 77Br-BTdU was about 40% and the radiochemical purity was more than 99%. Uptakes of 77Br-BTdU and 3H-FLT were increased with time. There was not significant differences between the uptake of 77Br-BTdU and that of 3H-FLT in control group at 60min (77Br-BTdU: 18.5 +- 2.0,3H-FLT: 20.3 +- 2.7 %ID/mg protein). Compared with control the uptake of 77Br-BTdU was significantlty decreased from 0.3 µM of 5-FU (One-way ANOVA with a post hoc Dunnett's Multiple Comparison Test). However, the uptake of 3H-FLT was significantly decreased from 300 µM of 5-FU. These results suggest that 77Br-BTdU could detect the earlier effect of 5-FU compared with 3H-FLT.
\nConclusions: Radiobromine-labeled BTdU is potentially useful as an imaging agent for detecting the early therapeutic effects of anticancer therapy with 5-FU in patients with renal cell carcinoma
Evaluation of radiobromine-labeled 5-bromo-4'-thio-2'-deoxyuridine uptake in ACHN cells after treatment with 5-fluorouracil: comparison with 3H-FLT uptake.
