Kang T B, Liang N C
Institute of Medical Biochemistry, Guangdong Medical College, Zhanjiang, China.
Zhongguo Yao Li Xue Bao. 1997 Jul;18(4):374-6.
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.
The number of viable cells was counted by a trypan blue dye exclusion test. PKC activity was assayed by incubating PKC with histone III S and [gamma-32P]ATP. TPK activity was assayed by incubating TPK with poly glutamate.tyrosine (4:1).
Que inhibited the proliferation of HL-60 cells in a concentration-dependent manner, its IC50 was 29 (22-37) mumol.L-1 after 48-h treatment; Que strongly inhibited the activity of cytosol PKC and membrane TPK with IC50 31 (20-48) mumol.L-1, 24 (13-45) mumol.L-1, respectively, but did not affect membrane PKC and cytosol TPK from HL-60 cells in vitro.
The inhibitory effect of Que on the growth of tumor cells is related to its inhibitory effects on PKC and/or TPK.
研究槲皮素(Que)对人早幼粒白血病细胞系HL-60细胞胞浆及膜蛋白激酶C(PKC)和酪氨酸蛋白激酶(TPK)活性的体外影响。
采用台盼蓝拒染法计数活细胞数。PKC活性通过将PKC与组蛋白III S和[γ-32P]ATP孵育来测定。TPK活性通过将TPK与聚谷氨酸·酪氨酸(4:1)孵育来测定。
Que以浓度依赖方式抑制HL-60细胞增殖,48小时处理后其IC50为29(22-37)μmol·L-1;Que强烈抑制胞浆PKC和膜TPK活性,IC50分别为31(20-48)μmol·L-1、24(13-45)μmol·L-1,但对HL-60细胞的膜PKC和胞浆TPK活性无影响。
Que对肿瘤细胞生长的抑制作用与其对PKC和/或TPK的抑制作用有关。