摘要
以几种不同方法活化的聚乙二醇 5 0 0 0对干扰素进行化学修饰 ,并对修饰条件、修饰后干扰素生物活性进行了初步比较。相同反应条件下 ,单甲氧基聚乙二醇甲酸琥珀酰亚胺酯 (SC mPEG)的选择性较单甲氧基聚乙二醇琥珀酸琥珀酰亚胺酯 (SS mPEG)高 ,聚乙二醇甲酸琥珀酰亚胺酯 (BSC PEG)由于有两个活性基团 ,选择性与SS mPEG相近。以聚乙二醇活化的修饰剂会使干扰素分子见形成交联 ,修饰后生物活性损失较大 ,而单甲氧基聚乙二醇活化的修饰剂修饰干扰素 ,修饰率保持在 30
Recombined human interferon α 2b is modified by polyethylene glycol which is activated by several different methods. Under the same condition, SC mPEG has higher selectivity than that of SS mPEG, selectivity of BSC PEG is similar to SS mPEG because of its two active groups. Reagent derived from polyethylene glycol can lead to crosslinkage between molecules of interferon, so modified interferon will lose a majority of biological activity. Interferon, however, modified by reagent derived from monomethoxy(polyethylene glycol) can remain a higher biological activity when degree of modification of primary amines is lower than 30%.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2000年第1期74-77,共4页
Journal of China Pharmaceutical University
