OECD 体外稳定转染转录激活测定法评估用于牲畜和养殖鱼类的兽用药品的人类雌激素受体激动/拮抗效应。
Assessment of human estrogen receptor agonistic/antagonistic effects of veterinary drugs used for livestock and farmed fish by OECD in vitro stably transfected transcriptional activation assays.
机构信息
Food Safety Risk Assessment Division, National Institute of Food and Drug Safety Evaluation, Chungcheongbuk-do 28159, Republic of Korea.
Food Safety Risk Assessment Division, National Institute of Food and Drug Safety Evaluation, Chungcheongbuk-do 28159, Republic of Korea.
出版信息
Toxicol In Vitro. 2019 Aug;58:256-263. doi: 10.1016/j.tiv.2019.02.003. Epub 2019 Feb 10.
The presence of veterinary drug residues in foods and the environment could potentially cause adverse effects on humans and wildlife. Several veterinary drugs were reported to exhibit endocrine disrupting effects via binding affinities to sexual hormone receptors such as estrogen and androgen receptors. Therefore, we confirmed the human estrogen receptor (ER) agonistic/antagonistic effects of 135 chemicals that were used as veterinary drugs in Korea by the official Organization for Economic Cooperation and Development (OECD) in vitro ER transcriptional activation (TA) assay using the VM7Luc4E2 cell line. In the case of ER agonist screening, 7 veterinary drugs (cefuroxime, cymiazole, trenbolone, zeranol, phoxim, altrenogest and nandrolone) were determined to be ER agonists. In addition, only zeranol was found to exhibit weak ER antagonistic activity. These 7 veterinary drugs, which were determined as ER agonists and/or antagonists by an OECD in vitro assay, were also found to have binding affinity to ERs. These results indicate that various veterinary drugs possess potential (anti-)estrogenic effects. However, further study is needed to determine the precise endocrine-disrupting effects of these compounds.
食品和环境中存在兽药残留可能会对人类和野生动物造成不良影响。有报道称，一些兽药通过与性激素受体（如雌激素受体和雄激素受体）的结合亲和力表现出内分泌干扰作用。因此，我们使用经官方经济合作与发展组织（OECD）批准的 VM7Luc4E2 细胞系，通过体外雌激素受体转录激活（TA）试验，对在韩国用作兽药的 135 种化学物质的人类雌激素受体（ER）激动/拮抗剂效应进行了确认。在 ER 激动剂筛选中，有 7 种兽药（头孢呋辛、氰咪唑、群勃龙、玉米赤霉醇、辛硫磷、烯丙孕素和诺龙）被确定为 ER 激动剂。此外，仅玉米赤霉醇表现出微弱的 ER 拮抗活性。通过 OECD 体外试验确定为 ER 激动剂和/或拮抗剂的这 7 种兽药也被发现与 ER 具有结合亲和力。这些结果表明，各种兽药具有潜在的（抗）雌激素作用。然而，需要进一步的研究来确定这些化合物的确切内分泌干扰作用。
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