槲皮素-7-硫酸酯钠盐对重组人蛋白激酶CK2全酶的影响

Effects of sodium quercetin-7-sulfate on recombinant human protein kinase CK2 holoenzyme

目的 观察槲皮素 7 硫酸酯钠盐 (SQMS)对重组人CK2全酶的直接作用及酶动力学机制。方法 通过测定转移到CK2底物上的 [γ 3 2 P]ATP的 [3 2 P]放射活度检测不同条件下的重组人CK2全酶的活性。结果 SQMS对重组人CK2全酶有很强的抑制作用 ,IC50 为 1 37μmol·L-1。CK2的动力学研究表明 :SQMS与ATP和酪蛋白分别呈竞争性和非竞争性抑制作用。结论 SQMS是CK2的抑制剂 ,SQMS的抑制作用与ATP呈竞争性。

AIM To study the effects and kinetics of sodium quercetin 7 sulphate (SQMS) on recombinant human protein kinase CK2 holoenzyme. METHODS The recombinant human CK2 holoenzyme activity was assayed by detecting incorporation of 32 P of [γ 32 P]ATP into the substrate at various conditions. RESULTS SQMS was shown to strongly inhibit the holoenzyme activity of recombinant human protein kinase CK2 with an IC 50 of 1 37 μmol·L -1 , Kinetic studies of SQMS on recombinant human CK2 showed: the inhibition was competitive with ATP and noncompetitive with casein. CONCLUSIONSQMS is an inhibitor of protein kinase CK2, and the inhibitory action of SQMS on CK2 is competitive with ATP and noncompetitive with casein.