用氯化亚锡(SnCl2)还原法制备^99Tc^m-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^99Tc^m-GHSA-IFNα2b标记率的影响;ICR小鼠尾静脉注射99Tc^m-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^99Tc^m-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^99Tc^m-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.