摘要
合成了二乙烯三胺五乙酸-半乳糖基人血清白蛋白(Diethylenetriamine Pentaacetic Acid-galactosyl-hu-man Serum Albumin,GSA),对其进行了99Tcm标记;进一步研制了无菌GSA一步法冻干药盒,并观察了99Tcm-GSA在正常小鼠以及肝损伤模型小鼠中的生物分布。标记结果显示,99Tcm-GSA的标记率>96%。生物分布结果显示,99Tcm-GSA在正常小鼠肝脏中有较高的摄取,在30 min时,肝脏摄取仍大于70%ID/g,且具有饱和性;在肝损伤模型中,肝摄取值低于正常小鼠(P=0.032 4)。冻干药盒法与湿法标记所得99Tcm-GSA的生物分布相当。所得GSA一步法冻干药盒标记简单可靠,并且标记后的GSA仍有优良的生物性能,可用于进一步临床研究及应用。
methods. Biodistribution of 99Tcm-GSA was investigated in both normal and liver-injury model mice. 99Tcm-GSA showed high liver The ligand GSA （diethylenetriamine pentaacetic acid-galactosyl-human serum albumin） was synthesized by introducing bifunctional chelator DTPA （diethylenetriamine pentaacetic acid） to human serum albumin （HSA） via DTPA anhydride first, and then coupling galactosyl units （2-imino-2-methoxyethyl-thio-galactose） to DTPA-HSA. GSA was labeled with ^99Tc^m by using SnCl2 as reductant and the labeling conditions of ^99Tc^m-GSA were optimized. Lyophilized kit of GSA was also developed for instant preparing of %99 Tc^m- GSA. The labeling yields in excess of 96% by using both of liquid and lyophilized labeling uptake in normal mice （〉 70%ID · g^-1 at 30 min after injection）. The liver uptake in liver-injury model mice is lower than that of in normal mice （P=0. 032 4）. The promising biological properties of ^99Tc^m-GSA combined with the development of reliable and instant lyophilized GSA kit afford the opportunity of liver receptor imaging for routine clinical assessment of hepatocyte function.
出处
《同位素》
CAS
北大核心
2008年第2期88-94,128,共8页
Journal of Isotopes
基金
美国中华医学基金会(China Medical Board of New York
CMB)基金资助(06-837)
