RECETOX, Faculty of Science, Masaryk University, Kamenice 753/5, Pavilion A29, 625 00, Brno, Czech Republic.
Arch Toxicol. 2024 Aug;98(8):2631-2645. doi: 10.1007/s00204-024-03766-7. Epub 2024 May 25.
Disruption of the thyroid hormone (TH) system is connected with diverse adverse health outcomes in wildlife and humans. It is crucial to develop and validate suitable in vitro assays capable of measuring the disruption of the thyroid hormone (TH) system. These assays are also essential to comply with the 3R principles, aiming to replace the ex vivo tests often utilised in the chemical assessment. We compared the two commonly used assays applicable for high throughput screening [Luminol and Amplex UltraRed (AUR)] for the assessment of inhibition of thyroid peroxidase (TPO, a crucial enzyme in TH synthesis) using several cell lines and 21 compounds from different use categories. As the investigated cell lines derived from human and rat thyroid showed low or undetectable TPO expression, we developed a series of novel cell lines overexpressing human TPO protein. The HEK-TPOA7 model was prioritised for further research based on the high and stable TPO gene and protein expression. Notably, the Luminol assay detected significant peroxidase activity and signal inhibition even in Nthy-ori 3-1 and HEK293T cell lines without TPO expression, revealing its lack of specificity. Conversely, the AUR assay was specific to TPO activity. Nevertheless, despite the different specificity, both assays identified similar peroxidation inhibitors. Over half of the tested chemicals with diverse structures and from different use groups caused TPO inhibition, including some widespread environmental contaminants suggesting a potential impact of environmental chemicals on TH synthesis. Furthermore, in silico SeqAPASS analysis confirmed the high similarity of human TPO across mammals and other vertebrate classes, suggesting the applicability of HEK-TPOA7 model findings to other vertebrates.
甲状腺激素 (TH) 系统的紊乱与野生动物和人类的多种不良健康后果有关。开发和验证能够测量甲状腺激素 (TH) 系统紊乱的合适体外测定法至关重要。这些测定法对于符合 3R 原则也很重要,旨在替代经常用于化学评估的体外测试。我们比较了两种常用于高通量筛选的测定法 [发光和 Amplex UltraRed (AUR)],用于评估几种细胞系和 21 种来自不同用途类别的化合物对甲状腺过氧化物酶 (TPO,TH 合成的关键酶) 的抑制作用。由于研究的细胞系源自人类和大鼠甲状腺,TPO 表达水平低或无法检测到,因此我们开发了一系列过表达人 TPO 蛋白的新型细胞系。由于所研究的细胞系源自人类和大鼠甲状腺,TPO 表达水平低或无法检测到,因此我们开发了一系列过表达人 TPO 蛋白的新型细胞系。由于所研究的细胞系源自人类和大鼠甲状腺,TPO 表达水平低或无法检测到,因此我们开发了一系列过表达人 TPO 蛋白的新型细胞系。由于所研究的细胞系源自人类和大鼠甲状腺,TPO 表达水平低或无法检测到,因此我们开发了一系列过表达人 TPO 蛋白的新型细胞系。由于所研究的细胞系源自人类和大鼠甲状腺,TPO 表达水平低或无法检测到,因此我们开发了一系列过表达人 TPO 蛋白的新型细胞系。由于所研究的细胞系源自人类和大鼠甲状腺,TPO 表达水平低或无法检测到,因此我们开发了一系列过表达人 TPO 蛋白的新型细胞系。HEK-TPOA7 模型基于高且稳定的 TPO 基因和蛋白表达而被优先用于进一步研究。值得注意的是,发光测定法甚至在没有 TPO 表达的 Nthy-ori 3-1 和 HEK293T 细胞系中也检测到了显著的过氧化物酶活性和信号抑制,表明其缺乏特异性。相反,AUR 测定法对 TPO 活性具有特异性。尽管特异性不同,但两种测定法都鉴定出了类似的过氧化物抑制物。具有不同结构和来自不同用途类别的一半以上的测试化学品均导致 TPO 抑制,包括一些广泛存在的环境污染物,这表明环境化学物质对 TH 合成可能产生潜在影响。此外,基于序列的 SeqAPASS 分析证实了哺乳动物和其他脊椎动物类群之间人类 TPO 的高度相似性,这表明 HEK-TPOA7 模型研究结果可适用于其他脊椎动物。