2,4,5-T的抑制作用,2,4-D,草甘膦和百草枯对蘑菇酪氨酸酶氧化L-DOPA的二酚酶活性的研究已经通过动力学测量,荧光光谱和计算对接分析。2,4,5-T和2,4-D按照竞争机制抑制酶的二酚酶活性,而根据Lineweaver-Burk动力学分析,草甘膦是一种混合抑制剂。抑制活性遵循草甘膦>2,4,5-T>2,4-D的顺序,IC50值为65,90和106μM,分别。固有酪氨酸酶荧光猝灭和计算对接分析表明,2,4,5-T和2,4-D通过疏水相互作用与酶的活性位点相互作用,而草甘膦还通过氢键和亲水相互作用与酶活性位点的外部残基相互作用,诱导蛋白质结构的构象变化。
The inhibitory effect of 2,4,5-T, 2,4-D, glyphosate and paraquat on the diphenolase activity of mushroom tyrosinase for oxidation of L-DOPA has been investigated by kinetic measurements, fluorescence spectroscopy and computational docking analysis. 2,4,5-T and 2,4-D inhibit the diphenolase activity of the enzyme following a competitive mechanism, while glyphosate is a mixed inhibitor according to Lineweaver-Burk kinetic analysis. The inhibitory activity follows the order glyphosate >2,4,5-T > 2,4-D with IC50 values of 65, 90 and 106 μM, respectively. Intrinsic tyrosinase fluorescence quenching and computational docking analysis suggest that 2,4,5-T and 2,4-D interact with the active site of the enzyme through hydrophobic interactions, while glyphosate also interacts with external residues of the active site of the enzyme by hydrogen bonding and hydrophilic interactions inducing conformational changes in the protein structure.