木犀草素对人白血病HL-60细胞内蛋白激酶C的抑制作用

目的　观察木犀草素对HL- 60细胞内蛋白激酶C活性的影响。方法　采用台盼蓝拒染法,在不同条件下测定细胞增殖的抑制率。PKC活性通过测定转移到CK2 底物上的γ 32P]ATP的32P的放射性活度来检测。结果　木犀草素能够显著地抑制HL- 60细胞内PKC的活性并呈剂量依赖性关系,其IC50为2.38μmol/L,作用效果强于阳性对照槲皮素(IC50=2.54μmol/L)。结论　木犀草素作为一种细胞内的PKC抑制剂具有潜在的抗肿瘤临床应用价值。

Inhibitory effect of luteolin in protein kinase C in human leukemic cells(HL-60)

Objective To observed the influence of luteolin on protein kinase C activity in human leukemic cells (HL-60).Methods The inhibitory rates of cell growth were tested by trypan blue stain assay in the different conditions. The PKC activity was assayed by detecting incorporation of 32P ofγ- 32P]ATP into the substrate. Results Luteolin was shown to strongly inhibit the endogenous activity of protein kinase C in a dependent dose with IC 50 of 2.38 μmol/L, which was more effective than the positive control( quercetin, IC 50=2.54 μmol/L).Conclusion Acted as a potential PKC inhibitor, luteolin might has anti-neoplastic therapeutic application.