聚乙二醇活性酯对干扰素α_(2b)化学修饰的初步研究

Chemical Modification of rhIFNα_(2b) with Activated Polyethylene Glycol

目的 探讨聚乙二醇活性酯（ｍＰＥＧ－ｓｓＭＷ ５０００和ＭＷ ２００００）修饰重组人干扰素α２ｂ（ｒｈＩＦＮ α２ｂ）的 最佳反应条件。方法 在不同反应条件下，用聚乙二醇活性酯修饰ｒｈＩＦＮα２ｂ，采用ＶＳＶ－Ｗｉｓｈ细胞病变抑制法测定 修饰后ｒｈＩＦＮα２ｂ的生物学活性。结果 随着 ＰＥＧ对ｒｈＩＦＮα２ｂ摩尔比的增加或修饰反应时间的延长，ｒｈＩＦＮα２ｂ的修怖产 物相对分子质量和不均一性增加，且随着ｒｈＩＦＮα２ｂ修饰度的提高，其生物学活性逐渐降低。结论 初步确立了ＰＥＧ 修饰ｒｈＩＦＮα２ｂ的反应条件，反应印尔比与聚乙二醇活性酯的相对分子质量是影响反应的关键因素。

Objective To explore the optimal condition of modifying rhIFN α2b by activated polyethylene glycol with relative molecular qqqqqqqqqqq weqights of 5000 and 20000.Methods rhIFNα2b was modified with activated polyethylene glycol under various conditions, and the bioactivity of the modified IFNα2b was analyzed by VSV-Wish system. Results Along with the increase of the ratio of PEG to rhIFN α2b as well as the reaction time, the relative molecular weight and inhomogeneity of the modified rhIFNα2b, were also increased. And the bio-activity of PEG-rhIFNα2b, was reduced with the improvement of modification degree. Conclusion The optimal condition of modifying rhIFN α2b with activated polyethylene glycol is preliminarily determined.The molar ratio of PEG to rhIFN α2b, and the relative molecular weight of PEG play important roles in the modification.