论文部分内容阅读
介绍了用DTPA(二乙三胺五醋酸)作为双官能团螯合剂与HSA(人血白蛋白)进行偶联,以提高放射性核素标记的HSA的体内稳定性的方法。合成了DTPA酸酐,并将其以固态形式加入HSA水溶液,再经Sephadex G50凝胶柱纯化,得到DTPA-HSA。用~(114)In~m标记的方法,测定了在不同反应介质中DTPA与HSA偶联反应的偶联率。~(114)In~m由~(113)In堆照生产。在邻苯二甲酸盐(pH5)、磷酸盐、Hepes等几种缓冲体系中制备了DTPA-HSA的~(99)Tc~m标记物。小鼠体内分布实验表明,以邻苯二甲酸盐为缓冲介质制备的~(99)Tc~m标记物体内稳定性最好。当HSA浓度为15mg/ml,DTPA与HSA摩尔比(n_(DTPA)/n_(HSA))大于3,Sn~(21)-DTPA摩尔比小于0.5时,标记比较合适。
A method of coupling DTPA (diethylenetriaminepentaacetic acid) as a bifunctional chelator with HSA (Human Albumin) to improve the in vivo stability of radionuclide labeled HSA is described. DTPA anhydride was synthesized and added to aqueous HSA in solid form and purified by Sephadex G50 gel column to give DTPA-HSA. The coupling ratio of DTPA to HSA in different reaction media was determined by ~ (114) In ~ m labeling. ~ (114) In ~ m is produced by ~ (113) In stack. The ~ (99) Tc ~ m marker of DTPA-HSA was prepared in several buffer systems such as Phthalate (pH5), Phosphate, Hepes and so on. In vivo experiments in mice showed that the ~ (99) Tc ~ m labeled with phthalate as buffer medium had the best in vivo stability. When the HSA concentration was 15mg / ml, the molar ratio of DTPA to HSA (n_ (DTPA) / n HSA) was more than 3, and the molar ratio of Sn ~ (21) to DTPA was less than 0.5, the labeling was suitable.