Effect of semi-synthesized quercetin water-soluble derivatives on recombinant human phosphatidylinositol 3-kinase p110beta catalytic subunit.
OBJECTIVE
To study the effect of semi-synthesized quercetin water-soluble derivatives sodium quercetin-7-sulfate (SQMS) and disodium quercetin-7,4 -disulfate (SQDS) on recombinant human phosphatidylinositol 3-kinase (PI3-K) p110 beta catalytic subunit.


METHODS
Recombinant human PI3-K p110 beta catalytic subunit was expressed by gene engineering. PI3 -K was assayed by incubating recombinant PI3-K p110beta with phosphatidylinositol-4,5-bisphosphate and [gamma-32P]ATP; the [32 P]-radiolabeled lipids were extracted with chloroform and methanol, assessed by thin layer chromatography and visualized by autoradiography.


RESULTS
Wortmannin, a specific inhibitor o f PI3-K, showed inhibition on recombinant PI3-K p110beta catalytic subunit in a concentration-dependent manner (2.5 - 20 nmol/L); SQMS and SQD S showed inhibition on recombinant PI3-K p110beta catalytic subunit in a concentration-dependent manner (2.5 - 20 micromol/L).


CONCLUSIONS
Semi-synthesized quercetin water-soluble derivatives were a type of inhibitors of PI3-K. The recombinant PI3-K p110beta catalytic subunit might be used as a molecular target for simpler filtrating and development of more effective inhibitors of PI3-K.
Liu
Wen
W
Institute of Biochemistry and Molecular Biology, Guangdong Medical College, Zhanjiang 524023, China. liuwen317@263.net
Liang
Nian-Ci
NC
D000730:Androstadienes / Q000494:pharmacology; D020134:Catalytic Domain / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006801:Humans; D019869:Phosphatidylinositol 3-Kinases / Q000378:metabolism; D000081082:Phosphoinositide-3 Kinase Inhibitors; D011794:Quercetin / Q000031:analogs & derivatives* / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000494:pharmacology; D000077191:Wortmannin
D000730:Androstadienes; D019869:Phosphatidylinositol 3-Kinases; D000081082:Phosphoinositide-3 Kinase Inhibitors; D011794:Quercetin; D011994:Recombinant Proteins; D000077191:Wortmannin; C437392:disodium quercetin-7,4'-disulfate