采用氯胺*T法对白蛋白融合干扰素α2b进行^125I标记,PD-10柱纯化,三氯醋酸沉淀法测定放化纯;体外以WISH/VSV系统比较白蛋白融合干扰素α2b和^125I-白蛋白融合干扰素α2b的抗病毒活性;SD大鼠皮下注射^125I-白蛋白融合干扰素α2b,分别于给药后0.5、2、6、24、48、90、180、300h放血处死,取血和相关脏器,称重并测定放射性,计算每克脏器放射性占注入量的百分率(%ID·g^-1)。结果显示,氯胺-T法制备的^125I-白蛋白融合干扰素α2b标记率为82.72%,放化纯95.53%,放射性比活度为0.26MBq/ug;抗病毒活性比较结果表明标记前后的生物学活性几乎无变化;皮下注射大鼠体内分布研究表明,^125I-白蛋白融合干扰素α2b在血中于6h达高峰,消除缓慢,未见特异性组织或器官的浓聚。
^125I-albumin-IFN-alpha2b was prepared with the methods of Ch-T and purified with PD-10 column. The radiochemical purity was measured with TCA (trichloroacetic acid) precipitation. The antiviral activities of ^125I-albumin-IFN-alpha2b and albumin-IFN-alpha2b were compared with WISH/VSV system in vitro. SD rats were injected with ^125I-albumin-IFN-alpha2b subcutaneously and sacrificed at 0.5, 2, 6, 24, 48, 90, 180 and 300 h post-injection. Selected organs were dissected, weighed and their radioactivity was measured using γ-counter. The accumulated radioactivity in the tissues was calculated in terms of percentage of injected dose per gram organ (%ID.g^-1). The labeling yield was 82.72%. The radiochemical purity of 125I-albumin-IFN-alpha2b was 95.53%, and its radioactivity was 0.26 MBq/ug. The antiviral bioactivities of albumin-IFN-alpha2b and ^125I-albumin- IFN-alpha2b did not change. Biodistribution analysis of ^125I-albumin-IFN-alpha2b in rats showed that concentrated ^125I- albumin-IFN-alpha2b in blood reached maximum at 6 h post injection, and eliminated slowly. No specific accumulation was seen in other tissues. ^125I-albumin-IFN-alpha2b could maintain in peripheral blood for a long time and it meant albumin-IFN-alpha2b would be an effective long-term interferon.