A Novel Technique for the Preparation of 125I-5-trimethylstannyl-1-(2-deoxy-2-fluoro-beta-D-arabino-furanosyl) Urail and Its Biodistribution Pattern in Kunming Mice
A Novel Technique for the Preparation of 125I-5-trimethylstannyl-1-(2-deoxy-2-fluoro-beta-D-arabino-furanosyl) Urail and Its Biodistribution Pattern in Kunming Mice
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DOI：
10.1007/s11596-011-0584-z
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发表时间：
2011-10-01
影响因子：
--
通讯作者：
Lan, Xiaoli
中科院分区：
文献类型：
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作者：
Hu, Jia;Zhang, Yongxue;Lan, Xiaoli
本研究开发了一种制备i -125-5-三甲基锡基-1-（2-脱氧-2-氟- β -d -阿拉伯氟烷基）尿嘧啶（FIAU）的新技术，检测了I-125-FIAU在昆明小鼠体内的生物分布谱，并探讨了利用FTAU放射标记进行报告基因成像的可能性。用放射性碘（I-125）标记5-三甲基锡基-1-（2-脱氧-2-氟- β -d -阿拉伯烷氧基）铀酰（FTAU）。采用旋转蒸发法去除过量甲醇。通过Sep-Pak C18反相柱纯化。采用硅胶薄层色谱法测定其放射化学纯度和体内稳定性。同时检测了I-125-FIAU在昆明小鼠体内的生物分布。结果表明，FTAU能有效标记I-125-FIAU，平均标记率为（81 +/- 0.38）% （n = 5）。经反相Sep-park柱纯化，平均放射化学纯度为（98.01 +/- 0.40）% （n = 5）。I-125-FIAU在37℃的正常人血清或生理盐水中孵育时稳定，0.5-24 h的放射化学纯度为bb0 96%。生物实验显示I-125-FIAU从血液池中迅速清除。I-125-FIAU主要由肾脏排出。心肌I-125-FIAU在8 h后明显下降，24 h后几乎没有保留。由此可见，采用新的FTAU放射碘化制备I-125-FIAU的方法简便、高效、体内稳定。I-125-FIAU在昆明小鼠体内的生物分布表明，它可以作为心肌报告基因的成像探针。
In this study, a novel technique for the preparation of I-125-5-trimethylstannyl-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) urail (FIAU) was developed, I-125-FIAU biodistribution profile was detected in Kunming mice and the possibility of using FTAU radio-labeling for reporter gene imaging was explored. 5-trimethylstannyl-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) urail (FTAU) was labeled with radioiodine (I-125). A rotary evaporation method was used to remove excess methanol. The reactant was purified through a Sep-Pak C18 reversal phase column. The radiochemical purity and in vivo stability were determined using silica gel thin layer chromatography (TLC). The biodistribution of I-125-FIAU in Kunming mice was also detected. The results showed that I-125-FIAU could be radiolabeled effectively with FTAU, with mean labeling rate being (81 +/- 0.38)% (n = 5). The mean radiochemical purity of (98.01 +/- 0.40)% (n = 5) was achieved after a reversal phase Sep-park column purification. I-125-FIAU was stable when incubated in normal human serum or in saline at 37 degrees C, with a radiochemical purity > 96% during a 0.5-24 h time period. Biological experiments exhibited rapid clearance of I-125-FIAU from the blood pool. I-125-FIAU was mostly excreted by kidneys. I-125-FIAU in myocardium dropped conspicuously after 8 h and there was hardly retention at 24 h. We were led to concluded that the new method of radioiodinization of FTAU for the preparation of I-125-FIAU is easy, highly effective and stable in vivo. The biodistribution of I-125-FIAU in Kunming mice showed it can serve as an imaging probe for myocardial reporter genes.