Thiabendazole (TBZ) is a broad–spectrum anthelmintic and fungicide used in humans, animals, and agricultural commodities. TBZ residues are present in crops and animal products, including milk, posing a risk to food safety and public health. ABCG2 is a membrane transporter which affects bioavailability and milk secretion of xenobiotics. Therefore, the aim of this work was to characterize the role of ABCG2 in the in vitro transport and secretion into milk of 5–hydroxythiabendazole (5OH–TBZ), the main TBZ metabolite. Using MDCK–II polarized cells transduced with several species variants of ABCG2, we first demonstrated that 5OH–TBZ is efficiently in vitro transported by ABCG2. Subsequently, using Abcg2 knockout mice, we demonstrated that 5OH–TBZ secretion into milk was affected by Abcg2, with a more than 2–fold higher milk concentration and milk to plasma ratio in wild–type mice compared to their Abcg2 counterpart.

中文翻译：

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ABCG2 蛋白在体外转运异生物质噻菌灵并增加其在牛奶中的残留量


噻菌灵 (TBZ) 是一种广谱驱虫剂和杀菌剂，用于人类、动物和农产品。 TBZ 残留物存在于农作物和动物产品（包括牛奶）中，对食品安全和公众健康构成风险。 ABCG2 是一种膜转运蛋白，影响外源物质的生物利用度和乳汁分泌。因此，这项工作的目的是表征 ABCG2 在 5-羟基噻菌灵 (5OH-TBZ)（TBZ 的主要代谢物）体外转运和分泌到乳汁中的作用。使用用 ABCG2 的几种物种变体转导的 MDCK-II 极化细胞，我们首先证明了 5OH-TBZ 可以在体外被 ABCG2 有效转运。随后，使用 Abcg2 敲除小鼠，我们证明 5OH-TBZ 分泌到乳汁中受到 Abcg2 的影响，与 Abcg2 对应物相比，野生型小鼠的乳汁浓度和乳汁与血浆比率高出 2 倍以上。