^(125)I-白蛋白融合干扰素α2b大鼠体内排泄研究

Excretion of ^(125)I-HSA-IFNα2b Fusion Protein in Rats

为研究125I-白蛋白融合干扰素α2b大鼠体内排泄行为,利用氯胺-T法制备了125I-白蛋白融合干扰素α2b,其标记率为82.72%,放化纯度为95.53%,放射性比活度为0.26MBq/μg。体外WISH/VSV系统抗病毒活性比较分析表明,白蛋白融合干扰素α2b和125I-白蛋白融合干扰素α2b具有相近的抗病毒活性。SD大鼠皮下注射125I-白蛋白融合干扰素α2b后,0～6、6～12、12～24、24～48、48～96、96～192和192～300h7个不同时段的尿、粪的放射性分析结果表明,125I-白蛋白融合干扰素α2b主要通过肾脏排泄,部分可通过粪便排泄,300h时尿、粪中平均累积排泄率分别为80.10%和16.00%;0～1、1～2、2～4、4～6、6～12、12～24和24～30h7个不同时段的胆汁的放射性分析结果表明,125I-白蛋白融合干扰素α2b也可通过肝脏代谢后经胆汁排泄,但这不是它的主要排泄途径,30h时,胆汁中的平均累积排泄率仅为1.61%。

12SI-HSA-IFNα2b was prepared with Ch-T method. The labeling yield is 82.72%, the radiochemical purity is 95.53%, and the specific activity is 0.26 MBq/μg. The antiviral activities of 125I-HSA-IFNα2b are almost same as HSA-IFNα2b analyzed with WlSH/VSV system in vitro. After SD rats injected with 125I-HSA-IFNα2b subcu- taneously, the radioactivity in urine and faeces in seven different periods of 0-6, 6-12, 12-24, 24-48, 48-96, 96-192 and 192-300 h shows that 125I-HSA-IFNα2b is excreted mainly by kidneys, partly by diachorema, and average accumulation excretory rates of 300 h in urine and feces are 80.10% and 16.00%, respectively; the radioactivity in bile in seven periods of 0-1, 1-2, 2-4, 4-6, 6-12, 12-24 and 24-30 h shows that 125I-HSA- IFNα2b also can be excreted by bile after being metabolized by liver, and average accu- mulation excretory rate of 30 h in bile is only 1.61%.