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目的:研究人工半合成槲皮素水溶性衍生物—槲皮素-7-硫酸酯钠盐(SQMS)和槲皮素-7,4′-二硫酸酯二钠(SQDS)对重组人磷脂酰肌醇3-激酶(PI3-K)p110β催化亚基的影响.方法:利用基因工程的方法获得PI3-K p110β催化亚基.用磷脂酰肌醇-4,5-二磷酸,[γ-~(32)P]ATP与重组PI3-K p110β催化亚基起保温的方法测定PI3-K的活性;~(32)P标记的磷脂用氯仿和甲醇抽提、板薄层层析和放射自显影来分析.结果:Wortmannin是PI3-K特异的抑制剂,Wortmannin(2.5-20nmol/L)对重组PI3-K p110β亚基有抑制作用;SQMS和SQDS(2.5-20μmol/L)对重组人PI3-K p110β催化亚基有抑制作用.结论:人工半合成槲皮素水溶性衍生物是一种类型的PI3-K抑制剂.重组人PI3-K p110β催化亚基可作为一种较为简便地筛选和开发有效的PI3-K抑制剂的分子靶点.
Objective: To study the effect of quercetin-7-sulfate sodium salt (SQMS) and quercetin-7,4’-disulfate disodium salt (SQDS) on the activity of recombinant human phosphatidylcholine (PI3-K) p110β catalytic subunit.Methods: The PI3-K p110β catalytic subunit was obtained by genetic engineering method.Methods: (32) P] ATP was incubated with recombinant PI3-K p110β catalytic subunit for determination of the activity of PI3-K; ~ (32) P-labeled phospholipid was extracted with chloroform and methanol and extracted by thin layer chromatography and autoradiography Wortmannin (2.5-20nmol / L) inhibited the recombinant PI3-K p110β subunit; SQMS and SQDS (2.5-20μmol / L) inhibited the proliferation of recombinant human PI3- K p110β catalytic subunit was inhibited.Conclusion: Artificial semi-synthetic quercetin water-soluble derivatives is a type of PI3-K inhibitor.The recombinant human PI3-K p110β catalytic subunit can be used as a simple and convenient screening Develop effective molecular targets for PI3-K inhibitors.