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新型PET核素68Ga标记D-脱氧葡萄糖的合成及生物学评价

     

摘要

Starting from D-glucosamine (DG), the precursor compound 2-(4-isothiocyanatobenzyl)- 1,4,7,10-tetraazacyclo-dodecane- 1,4,7,10-tetraacetic acid-D-glucose (DG-DOTA) was synthesized for potential radioactive imaging agents. Its structure was characterized by infrared, 1H NMR, LC-MS and ESI-HRMS. 6SGa is a generator-produced nuclide and does not require cyclotron on site. By careful selection of radiolabeling conditions, 68Ga-DOTA-DG was synthesized in short time and high yield by microwave synthesis system. Then, its binding affinity was tested by K-562, Hela and A431 tumor cell lines. The synthesis and evaluation of 68Ga-labeled DOTA-DG, not only provides a useful assessment of the stage of can- cer by imaging tumor metabolites compared with 1SF-FDG, but also develops a PET imaging agent.%以2-氨基-2-脱氧-D-葡萄糖为原料,通过微波加热法合成得到可用于核素标记的葡萄糖胺-1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸(DOTA)前体化合物.产物通过IR,^1HNMR,HPLC-MS,ESI-HRMS表征.通过标记条件的优化设计,在微波作用下,与新型正电子显像核素Ga-68进行放射性标记,高产率得到68Ga—DOTA—DG.而后对该标记化合物进行了K-562,Hela,A431等肿瘤细胞摄取实验,测定了对肿瘤的特异性.68Ga—DOTA—DG的合成,拓宽了以18F-FDG为首的肿瘤代谢类显像剂的新应用,为PET(Positronemissiontomography)显像肿瘤代谢情况提供了一种新的途径.

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