Effect of sodium quercetin-7-sulfate on enzyme activity of recombinant human phosphoinositide 3-kinase p110? catalytic subunit / 中国药理学通报

ABSTRACT

Aim To study the effect of sodium quercetin-7-sulfate (SQMS) on activity of recombinant human phosphoinositide 3-kinase (PI3-K) p110? catalytic subunit.Methods Recombinant human PI3-K p110? catalytic subunit was expressed by gene engineering.PI3-K activity was assayed by incubating recombinant PI3-K p110? with phosphatidylinositol-4,5-bisphosphate and [?-~ ~32 P]ATP; the ~ ~32 P-radiolabeled lipids were extracted with chloroform and methanol, and assessed by scintillation counter.Results SQMS showed inhibition on the recombinant p110? catalytic subunit with IC_~50 13.14 ?mol?L~-1 .Conclusions SQMS is an inhibitor of PI3-K. The recombinant PI3-K p110? catalytic subunit might be used as a molecular target for simpler target screening more effective inhibitors of PI3-K.