Effect of disodium quercetin-7,4′-disulfate on enzyme activity of recombinant human phosphoinositide 3-kinase p110 catalytic subunit / 中草药

ABSTRACT

Objective To study the effect of disodium quercetin-7,4′-disulfate (SQDS) on activity ofrecombinant human phosphoinositide 3-kinase (PI3-K) p110?catalytic subunit. Methods Recombinanthuman PI3-K p110?catalytic subunit was expressed by gene engineering. PI3-K activity was assayed byincubating recombinant PI3-K p110?with phosphatidylinositol-4,5-bisphosphate and [?-32P] ATP;the32P-radiolabeled lipids were extracted with chloroform and methanol,then assessed by scintillation counter.Results SQDS showed inhibition on the recombinant p110?catalytic subunit with IC5014.88?mol/L.Conclusion SQDS is an inhibitor of PI3-K. The recombinant PI3-K p110?catalytic subunit might be usedas a molecular target for simpler screening and development of more effective inhibitors of PI3-K.