杨梅素、槲皮素和山萘黄素对重组人PI3K p110β催化亚基活性的影响

Effects of myricetin,quercetin and kaempferol on activity of recombinant human phosphoinositide 3-kinase p110β subunit

目的:研究杨梅素、槲皮素和山萘黄素对重组人肌醇磷脂3-激酶(P I3K)p110β催化亚基的直接作用。方法:通过基因工程技术的方法获得P I3K p110β催化亚基。用P tdIns(4,5)P2,[γ3-2P]ATP与重组P I3K p110β催化亚基一起保温的方法测定P I3K的活性;32P标记的磷脂用氯仿和甲醇抽提,加闪烁液于液闪计数仪计数。结果:杨梅素和槲皮素对重组人P I3K p110β催化亚基有抑制作用,IC50分别为2.93μm o l/L和9.91μm o l/L,而山萘黄素对P I3K p110β催化亚基则无抑制作用。结论:杨梅素和槲皮素是P I3K的抑制剂,杨梅素和槲皮素对P I3K p110β催化亚基的抑制作用与浓度成正比关系。

Objeetive： To study the effects of myricetin, quercetin and kaempferol on the activity of recombinant human phospho- inositide 3-kinase （PI3K） p110β subunit. Methods： Recombinant human PI3K p110β subunit was constructed by gene engineering, and then incubated with phosphatidylinositol-4, 5-bisphosphate,^32P-labeled ATP and myricetin, quercetin or kaempferol, ^32P-labeled phospholipid was extracted with chloroform and methanol, and PI3K activity was assayed by scintillation counter. Results： Myricetin and quercetin other than kaempferol showed the inhibitory effects against p110β PI3K, and their IC50 was 2.93μmol/L and 9.91 μmol/L, respectively. Coneluslon： Myricetin and quercetin are inhibitors of PI3K, The inhibitory effects against p110β PI3K of myricetin and quercetin are dose-dependent.