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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 %以内时生物活性较好
Several different methods of activation of polyethylene glycol 50000 on the chemical modification of interferon, and the modified conditions, biological activities of the modified interferon were initially compared. Under the same reaction conditions, the selectivity to monomethoxy polyethylene glycol monosuccinate (SC mPEG) is higher than that of monomethoxy polyethylene glycol succinate succinate (SS mPEG) Glycolic Formic Acid Succinimidyl Ester (BSC PEG) Due to the two active groups, selectivity is similar to that of SS mPEG. Polyethylene glycol-activated modifier will make the formation of cross-linked interferon molecules, biological activity after modification greater loss, and monomethoxy polyethylene glycol-activated modifier modified interferon, the modification rate was maintained at 30% Within the biological activity is better