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将具有抗癌作用的L-天门冬酰胺酶用N,O-羧甲基壳聚糖进行化学修饰,以降低酶的抗原性,提高其在体内的半衰期.实验结果表明,修饰酶的表观K_m值与自由酶相差不多,分别为2.6×10~(-4)mol/L和2.2×10~(-4)mol/L(20℃),而抗胰蛋白酶和糜蛋白酶水解能力有很大提高.酶经修饰后抗原性大大降低,且修饰剂分子量越高,降低抗原性的效果越好.自由酶在兔体内的半衰期为1.2h,而修饰酶为40h,提高了33倍.
The anti-cancer L-asparaginase is chemically modified with N, O-carboxymethyl chitosan to reduce the antigenicity of the enzyme and increase its half-life in vivo. The experimental results show that the appearance of the modified enzyme The value of K_m was about 2.6 × 10 -4 mol / L and 2.2 × 10 -4 mol / L (20 ℃), while the ability of hydrolysis of trypsin and chymotrypsin was very high , The antigenicity of the enzyme was greatly reduced, and the higher the molecular weight of the modifier, the better the antigenicity was reduced.The half-life of the free enzyme in rabbits was 1.2h, while the modification enzyme was 40h, increased by 33 times.