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首页> 外文期刊>Life sciences >LINKAGE OF REDUCTION IN 1-PHOSPHATIDYLINOSITOL 4-KINASE ACTIVITY AND INOSITOL 1,4,5-TRISPHOSPHATE CONCENTRATION IN HUMAN OVARIAN CARCINOMA CELLS TREATED WITH QUERCETIN
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LINKAGE OF REDUCTION IN 1-PHOSPHATIDYLINOSITOL 4-KINASE ACTIVITY AND INOSITOL 1,4,5-TRISPHOSPHATE CONCENTRATION IN HUMAN OVARIAN CARCINOMA CELLS TREATED WITH QUERCETIN

机译：槲皮素处理人卵巢癌细胞中1-磷脂酰肌醇4-激酶活性的降低与肌醇中1,4,5-三磷酸肌苷浓度的降低之间的联系

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摘要

Quercetin inhibited 1-phosphatidylinositol (Pl) 4-kinase, EC 2.7.1.67 (Pl kinase) activity in a concentration-dependent manner (IC50 = 4 mu M) in particulate extracts from human ovarian carcinoma. In OVCAR-5 cells quercetin produced growth inhibition (IC50 = 63 mu M) and cytotoxicity (LC(50) = 17 mu M). The growth inhibition by quercetin was accompanied by an 80% decrease in Pl kinase activity and a 65% decrease in the concentration of the second messenger, inositol 1,4,5-trisphosphate (IP3). When human OVCAR-5 cells were plated and expressed their neoplastic proliferative program in the log phase, Pl kinase and Pl 4-phosphate 5-kinase, EC 2.7.1.68 (PlP kinase) activities coordinately increased to a peak of 5.8- and 4.5-fold, respectively. The results demonstrate for the first time inhibition by quercetin of the enhanced capacity for operation of signal transduction in human ovarian carcinoma cells, thus providing a novel target in cancer cells. [References: 16]
机译：槲皮素以浓度依赖性方式（IC50 = 4μM）抑制人卵巢癌颗粒提取物中的1-磷脂酰肌醇（Pl）4-激酶，EC 2.7.1.67（Pl激酶）活性。在OVCAR-5细胞中，槲皮素产生生长抑制作用（IC50 = 63μM）和细胞毒性（LC（50）= 17μM）。槲皮素对生长的抑制作用伴随着P1激酶活性的降低80％和第二种信使肌醇1,4,5-三磷酸（IP3）的浓度降低了65％。当将人OVCAR-5细胞铺板并在对数期，Pl激酶和Pl 4-磷酸5激酶中表达其肿瘤增生程序时，EC 2.7.1.68（PlP激酶）活性协同增加至5.8-和4.5-分别折叠。结果首次证明槲皮素抑制人卵巢癌细胞中信号转导功能的增强，从而为癌细胞提供了新的靶标。 [参考：16]

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