Giuliani Cesidio
Unit of Endocrinology, Department of Medicine and Sciences of Aging, and Ce.S.I.-Me.T., University of Chieti-Pescara, 66100 Chieti, Italy.
Antioxidants (Basel). 2019 Apr 29;8(5):112. doi: 10.3390/antiox8050112.
Previous studies have shown that quercetin inhibits thyroid function both in vitro and in vivo. An attempt to evaluate the effect of quercetin at the promoter level of the thyroid-specific genes led to the observation that this compound induces the basal activity of the reporter vector. Therefore, the action of quercetin has been evaluated on the basal activity of several reporter vectors: The PGL3 basic, promoter and control vectors from Promega, and a pSV-based chloramphenicol acetyltransferase (CAT) reporter vector. In the Fisher Rat Thyroid cell Line FRTL-5 thyroid cells transiently transfected, quercetin 10 μM increased the basal activity of all the reporter vectors evaluated, although the degree of the effect was significantly different among them. The analysis of the difference among the regulatory regions of these vectors identified the activator protein 1 (AP-1) binding site as one of the potential sites involved in the quercetin effect. Electromobility shift assay experiments showed that the treatment with quercetin induced the binding of a protein complex to an oligonucleotide containing the AP-1 consensus binding site. This is the first study showing an effect of quercetin on AP-1 activity in thyroid cells. Further studies are in progress to understand the role of AP-1 activation in the effects of quercetin on thyroid function.
先前的研究表明,槲皮素在体外和体内均能抑制甲状腺功能。一项在甲状腺特异性基因启动子水平评估槲皮素作用的尝试发现,该化合物可诱导报告载体的基础活性。因此,已对槲皮素在几种报告载体基础活性上的作用进行了评估:Promega公司的PGL3基本载体、启动子载体和对照载体,以及一种基于pSV的氯霉素乙酰转移酶(CAT)报告载体。在瞬时转染的Fisher大鼠甲状腺细胞系FRTL-5甲状腺细胞中,10 μM的槲皮素增加了所有评估的报告载体的基础活性,尽管它们之间的作用程度存在显著差异。对这些载体调控区域差异的分析确定,激活蛋白1(AP-1)结合位点是参与槲皮素作用的潜在位点之一。电泳迁移率变动分析实验表明,槲皮素处理可诱导一种蛋白复合物与含有AP-1共有结合位点的寡核苷酸结合。这是第一项显示槲皮素对甲状腺细胞中AP-1活性有影响的研究。目前正在进行进一步的研究,以了解AP-1激活在槲皮素对甲状腺功能影响中的作用。