奥扎格雷对蘑菇酪氨酸酶的抑制机理研究

Inhibition Mechanism of Ozagrel on Mushroom Tyrosinase

以L-DOPA为底物,抗血小板凝聚药奥扎格雷对酪氨酸酶具有很强抑制性,导致酶活力下降50%的奥扎格雷浓度(IC50)为3.45 mmol/L。奥扎格雷对酪氨酸酶抑制作用表现为可逆的竞争性和反竞争性混合型的抑制。按邹承鲁[1]所介绍的酶失活过程中的底物反应动力学方法测定奥扎格雷对酪氨酸酶的抑制作用动力学,1.0 mmol/L的奥扎格雷对酪氨酸酶和酪氨酸酶-底物复合物的抑制作用动力学常数分别为87.28和66.07μmol/L。

This investigation showed that ozagrel, an antithrombotic drug, strongly inhibited the activity of mushroom tyrosinase when L- DOPA was used as a substrate. The IC50（50% inhibitory concentration） value for ozagrel was 3.45 mmol/L. It was estimated to be a competitive and reversible mixed- type inhibitor of mushroom tyrosinase. Its inhibition kinetics had been studied by using the kinetic method of the substrate reaction described by TSOU[1]. The constants of tyrosinase and tyrosinase-substrate complex inhibited by 1.0 mmol/L ozagrel had been determined to be 87.28 and 66.07 μmol/L, respectively.