In this study, a novel technique for the preparation of 125I-5-trimethylstannyl-1-（2-deoxy-2-fluoro-beta-D-arabinofuranosyl） urail （FIAU） was developed, 125I-FIAU biodistribution profile was detected in Kunming mi...In this study, a novel technique for the preparation of 125I-5-trimethylstannyl-1-（2-deoxy-2-fluoro-beta-D-arabinofuranosyl） urail （FIAU） was developed, 125I-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 （125I）. 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 125I-FIAU in Kunming mice was also detected. The results showed that 125I-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. 125I-FIAU was stable when incubated in normal human serum or in saline at 37°C, with a radiochemical purity 〉96% during a 0.5-24 h time period. Biological experiments exhibited rapid clearance of 125I-FIAU from the blood pool. 125I-FIAU was mostly excreted by kidneys. 125I-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 125I-FIAU is easy, highly effective and stable in vivo. The biodistribution of 125I-FIAU in Kunming mice showed it can serve as an imaging probe for myocardial reporter genes.展开更多
基金sponsored by the grants from the Scientific Research Foundation for the Returned Overseas Chinese Scholars of the Ministry of Education of China (No. [2008]890)the National Natural Science Foundation of China (Nos. 30872652, 30830041, 30772208)Fund of Doctoral Programs for New College Teachers of the Ministry of Education (No. 20070487160)
文摘In this study, a novel technique for the preparation of 125I-5-trimethylstannyl-1-（2-deoxy-2-fluoro-beta-D-arabinofuranosyl） urail （FIAU） was developed, 125I-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 （125I）. 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 125I-FIAU in Kunming mice was also detected. The results showed that 125I-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. 125I-FIAU was stable when incubated in normal human serum or in saline at 37°C, with a radiochemical purity 〉96% during a 0.5-24 h time period. Biological experiments exhibited rapid clearance of 125I-FIAU from the blood pool. 125I-FIAU was mostly excreted by kidneys. 125I-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 125I-FIAU is easy, highly effective and stable in vivo. The biodistribution of 125I-FIAU in Kunming mice showed it can serve as an imaging probe for myocardial reporter genes.
