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Inhibitory effect of quercetin on OVCA 433 cells and presence of type II oestrogen binding sites in primary ovarian tumours and cultured cells.

机译:槲皮素对OVCA 433细胞的抑制作用以及原发性卵巢肿瘤和培养细胞中II型雌激素结合位点的存在。

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摘要

We investigated the effect of the flavonoid quercetin (Q) on the proliferation of the ovarian cancer cell line OVCA 433. Growth experiments demonstrated that Q exerted a reversible dose-dependent inhibition of cell proliferation in the range of concentrations between 10 nM and 10 microM. Two other flavonoids tested, rutin and hesperidin, were ineffective in inhibiting cell growth. Cell cycle analysis showed that the growth inhibitory effect of Q was due to a blocking effect in the GO/G1 phase. Using a whole cell assay with (6.7-3H) oestradiol (3H-E2) as tracer we demonstrated that OVCA 433 cells contain type II oestrogen binding sites (type II EBS). Competition analysis showed that Q competed for 3H-E2 binding to type II EBS while both rutin and hesperidin did not. Appreciable amounts of type II EBS were also detected in seven primary ovarian tumours. Our results suggest that Q may regulate ovarian cancer cell growth through a mechanism involving a binding interaction with type II EBS. This mechanism could also be active in vivo since primary ovarian tumours contain type II EBS.
机译:我们研究了类黄酮槲皮素(Q)对卵巢癌细胞系OVCA 433增殖的影响。生长实验表明,在10 nM和10 microM之间的浓度范围内,Q对细胞增殖具有可逆的剂量依赖性抑制作用。测试的其他两种类黄酮,芦丁和橙皮苷在抑制细胞生长方面无效。细胞周期分析表明,Q的生长抑制作用归因于GO / G1期的阻断作用。使用以(6.7-3H)雌二醇(3H-E2)作为示踪剂的全细胞分析,我们证明OVCA 433细胞包含II型雌激素结合位点(II EBS型)。竞争分析表明Q竞争3H-E2与II型EBS的结合,而芦丁和橙皮苷均不竞争。在七个原发性卵巢肿瘤中也发现了相当数量的II型EBS。我们的结果表明,Q可能通过涉及与II型EBS结合相互作用的机制来调节卵巢癌细胞的生长。由于原发性卵巢肿瘤含有II型EBS,因此这种机制在体内也可能是活跃的。

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