摘要
目的：研究槲皮素（Ｑｕｅ）对ＨＬ６０细胞中细胞溶质和胞膜蛋白激酶Ｃ（ＰＫＣ）、酪氨酸蛋白激酶（ＴＰＫ）活性的影响．方法：活细胞数的计数用苔盼兰拒染法；用组蛋白ⅢＳ、［γ３２Ｐ］ＡＴＰ与ＰＫＣ酶液一起保温测定ＰＫＣ活性；用聚谷氨酸·酪氨酸（４∶１）多肽）、［γ３２Ｐ］ＡＴＰ与ＴＰＫ酶液一起保温测定ＴＰＫ活性．结果：Ｑｕｅ对ＨＬ６０细胞的增殖有抑制作用，呈剂量依赖关系，处理４８小时后，其ＩＣ５０为２９（２２－３７）μｍｏｌ·Ｌ－１；在体外，Ｑｕｅ能强烈抑制细胞溶质ＰＫＣ和胞膜ＴＰＫ活性，其ＩＣ５０分别为：３１（２０－４８）μｍｏｌ·Ｌ－１，２４（１３－４５）μｍｏｌ·Ｌ－１，但不影响胞膜ＰＫＣ和细胞溶质ＴＰＫ活性．结论：这为Ｑｕｅ对癌细胞的生长有抑制作用与其抑制ＰＫＣ和／或ＴＰＫ有关提供了直接证据．
IM: To study the effect of quercetin (Que) on the activities of cytosol and membrane protein kinase C (PKC) and tyrosine protein kinase (TPK) from HL 60 cells in vitro . METHODS: The number of viable cells was counted by a trypan blue dye exclusion test. PKC activiy was assayed by incubating PKC with histone ⅢS and [γ 32 P]ATP. TPK activity was assayed by incubating TPK with poly glutamate·tyrosine (4∶1). RESULTS: Que inhibited the proliferation of HL 60 cells in a concentration dependent manner, its IC 50 was 29 (22-37) μmol·L -1 after 48 h treatment; Que strongly inhibited the activity of cytosol PKC and membrane TPK with IC 50 31 (20-48) μmol·L -1 , 24 (13-45) μmol·L -1 , respectively, but did not affect membrane PKC and cytosol TPK from HL 60 cells in vitro . CONCLUSION: The inhibitory effect of Que on the growth of tumor cells is related to its inhibitory effects on PKC and/or TPK.
出处
《中国药理学报》
CSCD
1997年第4期374-376,共3页
Acta Pharmacologica Sinica
关键词
HL-60细胞
槲皮素
蛋白激酶C
酪氨酸
HL 60 cells
quercetin
protein kinase C
tyrosine
protein kinases
enzyme inhibitors
cultured tumor cells
