几种因素在L-天冬酰胺酶化学修饰中对酶活力及抗原性的影响

EFFECT OF SEVERAL FACTORS ON ENZYMIC ACTIVITY AND ANTIGENICITY IN CHEMICAL MODIFICATION OF L-ASPARAGINASE

为了寻求在较好地保持酶活力的同时解除L-天冬酰胺酶抗原性的方法,采用不同分子量的乙酸酐、右旋糖酐和单甲氧基聚乙二醇,作为修饰剂和不同的修饰方法对该酶进行了化学修饰。结果表明在保持酶活性和降低抗原性方面,大分子修饰剂右旋糖酐、单甲氧基聚乙二醇优于小分子乙酸酐,底物保护修饰优于直接修饰;活化PEG,优于活化PEG_1。在底物保护下的PEG,修饰酶其抗原性完全解除的同时,酶活力保持在30%以上。

Acetic anhydride, dextran and monomethoxypolyethylene glycol and different modification methods were used for modification of L - asparaginase to maintain enzyme activity and completely remove its antigenicity. The results showed that the macromolecular modifiers PEG and dextran were better than the small molecular modifier acetic anhydride. For maintenance of enzyme activity and removal of antigenicity modificationin the presence of substrate was better than absence of substrate and activated PEG_2 was better than activated PEG_1. When PEG_2-L-asparaginase was modified in the presence of substrate, its antigenicity was completely removed, while more than 30% of native enzyme activity were still retained.