^99Tc^m-半乳糖基化人血清白蛋白融合干扰素α2b的制备和生物分布  

Preparation and biodistribution of ^(99)Tc^m-GHSA-IFNα2b

作　　者：周桂楼[1,2] 蒋孟军[2] 张荣军[2] 蔡刚明[2] 周尧远[2] 张波[2] 顾晓波[2] 叶万忠[2] 金坚 曹国宪[2] 包建东[2] 周杏琴[2] 

机构地区：[1]江南大学医药学院,无锡214036 [2]江苏省原子医学研究所,卫生都核医学重点实验室,无锡214063

出　　处：《核技术》2008年第8期633-636,共4页Nuclear Techniques

基　　金：国家自然科学基金(30670589);卫生部科研基金(wkj2006-2-5);江苏省人事厅“六大人才高峰”(06-B-026);江苏省医学重点人才(RC2007097);无锡市“学术技术带头人培养工程”项目

摘　　要：用氯化亚锡(SnCl2)还原法制备99Tcm-半乳糖基化人血清白蛋白融合干扰素α2b(GHSA-IFNα2b),研究了SnCl2和GHSA-IFNα2b的用量以及溶液pH对99Tcm-GHSA-IFNα2b标记率的影响;ICR小鼠尾静脉注射99Tcm-GHSA-IFNα2b(0.286MBq/只,n=6),于5、10、15、30、60、120min取脏器和血,称重、计数,计算%ID(organ)-1和%ID·g-1;并对99Tcm-GHSA-IFNα2b的SD大鼠显像进行了研究。结果表明,在pH=3.0~4.5、GHSA-IFNα2b的用量≥0.3mg、SnCl2的用量为3~60μg时,37℃反应30min,可得标记率>90%的99Tcm-GHSA-IFNα2b,并在6h内保持基本稳定;肝脏组织中的99Tcm-GHSA-IFNα2b在注射后10min高达52.51%ID(organ)-1,能够被肝脏特异性摄取,主要通过胆道、肠道排泄;大鼠静脉注射15~30min时,即可获得清晰的肝显像。The work is to evaluate the liver-targeting ability of ^99Tc^m-GHSA-IFNα2b. ^99Tc^m-GHSA-IFNα2b was prepared by the reduction of Na^99Tc^mO4 with SnCl2. Effects of the SnCl2 or GHSA-IFNα2b amount and pH value on the labeling yield of ^99Tc^m-GHSA-IFNα2b were investigated. The biodistfibution was studied with ICR mice. 0.2 mL（0.286 MBq）^99Tc^m-GHSA-IFNα2b solution containing 2 μg GHSA-IFNα2b was iv injected to each animal through the tail. The mice were decapitated at 5, 10, 15, 30, 60 and 120 rain. The organs of interest were excised, weighed, and counted. The ID%/organ and ID%/g were calculated. Liver scan of ^99Tc^m-GHSA-IFNα2b was performed on a rat. The results showed that labeling yield of 99Tc^m-GHSA-IFNα2b could be over 90% under the followng labeling conditions： pH 3.0 - 4.5, over 0.3 mg of GHSA-IFNα2b, 3 μg-60μg of SnCl2, and 30 min labeling at 37℃. Biodistribution in mice showed a peak of liver uptake of 99Tc^m-GHSA-IFNα2b in 10 min after injection, being excreted mainly via the biliary system and gastrointestinal tract. Clear liver images were obtained in 15-30 rain after injection. It can be concluded that GHSA-IFNα2b is a promising interferon with good liver-targeting ability, and 99Tc^m-GHSA-IFNα2b is a potential hepatic receptor imaging agent.

关 键 词：半乳糖基化人血清白蛋白融合干扰素α2b 99^Tc^m 肝受体显像 生物分布 

分 类 号：R817.9[医药卫生—影像医学与核医学] R978.7[医药卫生—放射医学]