[Effect of three flavones on enzyme activity of recombinant human phosphoinositide 3-kinase p110beta catalytic subunit].
OBJECTIVE
To study the effect of three flavones-luteolin, apigenin and genistein on activity of recombinant human phosphoinositide 3-kinase (PI3-K) p110beta catalytic subunit.


METHODS
Recombinant human P13-K p110beta catalytic subunit was expressed by gene engineering. PI3-K activity was assayed by incubation recombinant PI3-K p110beta with phosphatidylinostiol-4,5-bisphosphate and [gamma-32P] ATP; the 32P-radiolabeled lipids were extracted with cholroform and methanol, and assessed by scintillation counter.


RESULTS
Luteolin and apigenin showed inhibition on the recombinant p110beta catalytic subunit with IC50 8. 65 micromol/L and 11.56 micromol/L, but genistein had no inhibition.


CONCLUSIONS
Luteolin and apigenin are inhibitors of P13-K. The recombinant P13-K p1100 catalytic subunit may be used as a molecular target for simpler screening and development of more effective inhibitors of P13-K.
Liu
Wen
W
Institute of Biochemistry and Molecular Biology, Guangdong Medical College, Zhanjiang 524023, China.
Liang
Nian-Ci
NC
Huang
Ren-Bin
RB
D047310:Apigenin / Q000494:pharmacology; D020134:Catalytic Domain / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005419:Flavonoids / Q000494:pharmacology*; D019833:Genistein / Q000494:pharmacology; D047311:Luteolin / Q000494:pharmacology; D019869:Phosphatidylinositol 3-Kinases / Q000378:metabolism; D000081082:Phosphoinositide-3 Kinase Inhibitors; D010936:Plant Extracts / Q000494:pharmacology*
D047310:Apigenin; D004791:Enzyme Inhibitors; D005419:Flavonoids; D019833:Genistein; D047311:Luteolin; D019869:Phosphatidylinositol 3-Kinases; D000081082:Phosphoinositide-3 Kinase Inhibitors; D010936:Plant Extracts