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首页> 外文期刊>Cell biology international. >A novel antioestrogen agent (3R,6R)-bassiatin inhibits cell proliferation and cell cycle progression by repressing cyclin D1 expression in 17beta-oestradiol-treated MCF-7 cells.
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A novel antioestrogen agent (3R,6R)-bassiatin inhibits cell proliferation and cell cycle progression by repressing cyclin D1 expression in 17beta-oestradiol-treated MCF-7 cells.

机译：一种新型的抗雌激素剂（3R，6R）-茉莉素通过抑制17β-雌二醇处理的MCF-7细胞中细胞周期蛋白D1的表达来抑制细胞增殖和细胞周期进程。

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Bassiatin [(3R,6R)-bassiatin] was isolated from the endogenous fungus Fusarium oxysporum J8-1-2. We found that oestrogen-dependent cell growth was inhibited by bassiatin in MCF-7 ERalpha (oestrogen receptor alpha)-positive breast cancer cells. In addition, the mRNA and protein levels of ERalpha and the oestrogen-responsive gene cyclin D1 were down-regulated by bassiatin in the presence of 17beta-oestradiol. Co-treatment of 17beta-oestradiol and bassiatin increased phospho-cyclin D1 (Thr286), an indicator of cyclin D1 phosphorylation-dependent degradation. However, this effect was not obvious in the absence of 17beta-oestradiol, suggesting that bassiatin may play a role in the metabolism of cyclin D1 by decreasing cyclin D1 protein expression in the presence of 17beta-oestradiol. Cyclin D1, known as a key cell cycle regulator, regulates the transition of G1- and S-phase. Decreased cyclin D1 was found to be involved in bassiatin-induced MCF-7 cell cycle arrest. Collectively, our study showed that bassiatin induced cell cycle arrest and exerted an antioestrogen effect. It may prove to be a potential drug target for antioestrogen therapy in ERalpha-positive breast cancer.
机译：从内源真菌尖孢镰刀菌J8-1-2中分离出巴萨丁[（3R，6R）-巴萨丁]。我们发现在MCF-7 ERalpha（雌激素受体α）阳性乳腺癌细胞中，bassatin抑制了雌激素依赖性细胞的生长。此外，在存在17β-雌二醇的情况下，bassiaatin可以下调ERalpha的mRNA和蛋白水平以及雌激素反应性基因cyclin D1。共同处理17β-雌二醇和贝塞丁会增加磷酸化细胞周期蛋白D1（Thr286），这是细胞周期蛋白D1磷酸化依赖性降解的指标。但是，在不存在17β-雌二醇的情况下，这种作用并不明显，这表明bassatin可能通过在17β-雌二醇的存在下降低细胞周期蛋白D1的蛋白表达而在细胞周期蛋白D1的代谢中发挥作用。 Cyclin D1被称为关键细胞周期调节剂，可调节G1和S期的转变。发现减少的细胞周期蛋白D1参与了巴西素诱导的MCF-7细胞周期停滞。总的来说，我们的研究表明，basdiatin诱导细胞周期停滞并发挥抗雌激素作用。它可能被证明是ERalpha阳性乳腺癌抗雌激素治疗的潜在药物靶标。

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