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2,3-二甲基-4H-呋喃并[3,2-c]香豆素的放射性碘化及其在荷实体瘤小鼠中的生物学评价

Radioiodination of 2,3-dimethyl-4H-furo[3,2-c]coumarin and biological evaluation in solid tumor bearing mice.

作者信息

Abd Elhalim S M, Ibrahim I T

机构信息

Labelled Compounds Department, Radioisotopes Production and Radioactive Sources Division, Hot Laboratories Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt.

出版信息

Appl Radiat Isot. 2015 Jan;95:153-158. doi: 10.1016/j.apradiso.2014.09.011. Epub 2014 Oct 22.

DOI:10.1016/j.apradiso.2014.09.011
PMID:25464192
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4259903/
Abstract

Compound 2,3-dimethyl-4H-furo[3,2-c]coumarin is a coumarin derivative that could be labeled with I. The process of labeling was started using 1mg of the compound, 50µg CAT oxidizing agent, 30min as reaction time at pH with a yield about 95%. The I-coumarin derivative was stable for about 48h. Radiochemical purity of the labeled compound was performed by electrophoresis and HPLC. The labeled compound was separated with purity about 95%. Tumor transplantation to produce a solid tumor in the right leg of albino mice was made by intramuscular injection of 2×10 EAC (Ehrlish acittes carcinoma cells). Biodistribution study of I-coumarin derivative revealed that the uptake in tumor bearing leg was over 5% at 1h and 4h post-injection. This uptake encourages the use of I-coumarin derivative in imaging of tumor sites.

摘要

化合物2,3 - 二甲基 - 4H - 呋喃并[3,2 - c]香豆素是一种可用碘标记的香豆素衍生物。标记过程从使用1毫克该化合物、50微克CAT氧化剂开始,在特定pH值下反应30分钟,产率约为95%。碘标记的香豆素衍生物在约48小时内稳定。标记化合物的放射化学纯度通过电泳和高效液相色谱法进行测定。分离得到的标记化合物纯度约为95%。通过肌肉注射2×10个艾氏腹水癌细胞(EAC),在白化小鼠右腿进行肿瘤移植以产生实体瘤。碘标记香豆素衍生物的生物分布研究表明,在注射后1小时和4小时,荷瘤腿的摄取量超过5%。这种摄取情况促使碘标记香豆素衍生物用于肿瘤部位的成像。

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