木犀草素对蛋白激酶CK2的抑制作用  

Inhibitory effect of luteolin on protein kinase CK2

作　　者：林小聪[1] 刘新光[1] 陈小文[2] 陈伟珠[1] 梁念慈[1] 

机构地区：[1]广东医学院生物化学与分子生物学研究所,广东湛江524023 [2]深圳市儿童医院儿科研究所,广东深圳518026

出　　处：《中国药理学通报》2006年第11期1314-1319,共6页Chinese Pharmacological Bulletin

基　　金：教育部科学技术研究重点资助项目(No03096);广东省科技计划资助项目(No2002C30109);湛江市科技局科技攻关计划资助项目(No020101)

摘　　要：目的观察体外以及细胞内木犀草素对蛋白激酶CK2活性的抑制效果及进行酶动力学分析以确定其抑制作用类型。方法将利用基因工程技术获得的重组人CK2α′及β亚基在体外等摩尔混合构成CK2全酶。通过测定药物作用后转移到CK2底物上的[γ3-2P]ATP的32P的放射性活度,探讨木犀草素对重组人CK2全酶以及HL-60细胞内CK2活性的抑制作用,并采用L ineweaver-Burk作图法分析其酶动力学机制。结果木犀草素能显著抑制重组人CK2活性(IC50=0.86μmol.L-1)以及HL-60细胞内的CK2活性,其对细胞内CK2的作用效果要强于阳性对照TBB。酶动力学分析表明,木犀草素与ATP呈竞争性抑制CK2的活性(Ki=0.19μmol.L-1),与酪蛋白则呈混合性抑制CK2的活性(Ki=0.11μmol.L-1)。结论木犀草素是一种有效的蛋白激酶CK2的抑制剂。Aim To observed the inhibitory effects of luteolin on protein kinase CK2 in vitro and in vivo and investigated its kinetics. Methods Recombinant human protein kinase CK2 α′and β subunits were mixed at equal molar ratio to reconstitute CK2 holoenzyme. The CK2 activity was assayed by detecting incorporation of ^32p of [ γ-32P] ATP into the substrate for the inhibitory effect by luteolin in vitro and in vivo, and CK2 kinetic analysis were carried out by using the Lin-eweaver-Burk plot. Results Luteolin was shown to inhibit the activity of protein kinase CK2 strongly in vitro（ IC50 = 0. 86 μmol · L^-1 ） and in HL-60 cells. Kinetic studies of luteolin on recombinant human CK2 showed that luteolin acted as an of competitive inhibitor with ATP（Ki =0. 19 μmol · L^-1） and mixed types with casein （ Ki = 0. 11 μmol · L^-1 ）. Conclusion Luteolin is an effective inhibitor of protein kinase CK2.

关 键 词：蛋白激酶CK2 木犀草素 酶动力学 

分 类 号：R284.1[医药卫生—中药学] R329.2[医药卫生—中医学]