Effect of semi-synthesized quercetin water-soluble derivatives on recombinant human phosphatidylinositol 3-kinase p110beta catalytic subunit.
Abstract
AIM: 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).
CONCLUSION: 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.
Keywords:
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).
CONCLUSION: 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.