CAJ | 학술논문

为拓展脱氧葡萄糖(DG)在肿瘤代谢显像中的应用,以新型核素64Cu标记葡萄糖胺-1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸(DOTA-DG).通过优化反应条件,于25℃反应30 min后得到高放化纯度和高比活度的标记化合物64 Cu-DOTA-DG,标记产物经放射性高效液相色谱( Radio-HPLC)检测.体外稳定性实验结果表明,64 Cu-DOTA-DG有良好的稳定性.将64 Cu-DOTA-DG通过尾静脉注射入荷瘤肝癌细胞( Hep-G2)裸鼠体内,分别于注射后1和3 h进行小动物正电子发射断层扫描( Micro-PET)显像.结果表明,其在肿瘤部位有所富集.64 Cu-DOTA-DG的合成及分子显像研究拓宽了以18 F-氟代脱氧葡萄糖为代表的肿瘤代谢类显像剂的应用范围,为新型核素标记肿瘤代谢显像剂提供一种新途径.
위탁전탈양포도당(DG)재종류대사현상중적응용,이신형핵소64Cu표기포도당알-1,4,7,10-사담잡배십이완-1,4,7,10-사을산(DOTA-DG).통과우화반응조건,우25℃반응30 min후득도고방화순도화고비활도적표기화합물64 Cu-DOTA-DG,표기산물경방사성고효액상색보( Radio-HPLC)검측.체외은정성실험결과표명,64 Cu-DOTA-DG유량호적은정성.장64 Cu-DOTA-DG통과미정맥주사입하류간암세포( Hep-G2)라서체내,분별우주사후1화3 h진행소동물정전자발사단층소묘( Micro-PET)현상.결과표명,기재종류부위유소부집.64 Cu-DOTA-DG적합성급분자현상연구탁관료이18 F-불대탈양포도당위대표적종류대사류현상제적응용범위,위신형핵소표기종류대사현상제제공일충신도경.
2-(4-Isothiocyanatobenzyl)-1,4,7,10-tetraazacyclo-dodecane-1,4,7,10-tetraacetic acid-D-glucose ( DOTA-DG) was synthesized and radiolabeled with 64 Cu. The DOTA-DG dissolved in sodium acetate buffer (pH=5. 5) was added to the eluent of64Cu. The solution was stirred and placed at 25℃ for 30 min. The la-beling efficiency and radiochemical purity of 64 Cu-DOTA-DG were all over 95%, as determined by radio-HPLC. The in vitro stability of the conjugates was analyzed in 0.1 mol/L PBS and 0.1 mol/L NaAc and it showed excellent in vitro stability. 14. 8 MBq of64 Cu-DOTA-DG was injected to Hep-G2 xenograft models via tale vein. Positron emission tomography images were taken 1 and 3 h after the injection. These images sugges-ted that there was high tumor uptake of 64 Cu-DOTA-DG. The results suggested that 64 Cu-DOTA-DG could provide images much clearer than the DG labeled with 99m Tc, 111 In and 68 Ga, and observation of the metabo-lism of DG much longer. These preliminary data show that 64 Cu-DOTA-DG appears to be useful in PET ima-ging.