摘要
目的:研究三种黄酮类化合物———木犀草素、芹菜素和金雀异黄素对重组人肌醇磷脂3-激酶(PI3-K)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PI3-K p110β催化亚基。用PtdIns(4,5)P2,[γ3-2P]ATP与重组PI3-K p110β催化亚基一起保温的方法测定PI3-K的活性;32P标记的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:木犀草素和芹菜素对重组人PI3-K p110β催化亚基有抑制作用,IC50分别为8.65μmol/L和11.56μmol/L,而金雀异黄素对PI3-K p110β催化亚基则无抑制作用。结论:木犀草素和芹菜素是PI3-K的抑制剂。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的抑制剂的分子靶点。
Objective： To study the effect of three flavones—luteolin, apigenin and genistein on activity of recombinant human phosphoinositide 3-kinase （PI3-K） p110β catalytic subunit. Methods： Recombinant human PI3-K p110β catalytic subunit was expressed by gene engineering. PI3-K activity was assayed by incubation recombinant PI3-K p110β with phosphatidylinostiol-4,5-bisphosphate and [γ-^32P] ATP： the ^32P-radiolabeled lipids were extracted with eholroform and methanol, and assessed by scintillation counter. Resuhs： Luteolin and apigenin showed inhibition on the recombinant p110β catalytic subunit with IC50 8.65 μmoL/L and 11. 56μmoL/L, but gcnistein had no inhibition. Conclusion： Luteolin anti apigenin are inhibilors of PI3-K. The recombinant PI3-K p1100β catalytic subunit may be used as a molecular target for simpler screening and development of more effective inhibitors of PI3-K.
出处
《中药材》
CAS
CSCD
北大核心
2006年第1期33-36,共4页
Journal of Chinese Medicinal Materials
基金
广东省重点学科基金资助课题(9306)
