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首页> 外文期刊>Environmental Science & Technology >Benzotriazole Ultraviolet Stabilizers Show Potent Activities as Human Aryl Hydrocarbon Receptor Ligands
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Benzotriazole Ultraviolet Stabilizers Show Potent Activities as Human Aryl Hydrocarbon Receptor Ligands

机译：苯并三唑紫外线稳定剂作为人的芳烃受体配体显示出强大的活性

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摘要

Benzotriazole ultraviolet stabilizers (BUVSs) used in consumer products are raising concerns as new pollutants in the aquatic environment. We determined the agonistic activities of eight BUVSs and a chemically distinct UV absorber (4-methylbenzylidinecamphor) toward the human aryl hydrocarbon receptor (AhR) and thyroid hormone receptors alpha and beta. Although none of the BUVSs showed ligand activity against the thyroid hormone receptors, four of them (UV-P, UV-9, UV-326, and UV-090) showed significant AhR ligand activity. Their half-maximal effective concentrations (EC_(50)) were 130 nM for UV-P, 460 nM for UV-9, and 5.1 μM for UV-090 (a value for UV-326 could not be determined). Of the numerous AhR ligands, it is well-known that those considered nontoxic are quickly metabolized by enzymes such as CYP1A1, which destroys their ability to function as ligands. Accordingly, we established a new yeast assay for simultaneous monitoring of both the strength of AhR ligand activity and ligand degradation by CYP1A1. We found the AhR ligand activities of the above four BUVSs to be stable in the presence of CYP1A1; therefore, they have the potential to accumulate and exert potent physiological effects in humans, analogous to polycyclic aromatic hydrocarbons and dioxins, which are known stable and toxic ligands.
机译：消费产品中使用的苯并三唑紫外线稳定剂（BUVS）作为水生环境中的新污染物正在引起人们的关注。我们确定了八个BUVS和一种化学上独特的UV吸收剂（4-甲基苄基樟脑）对人芳烃受体（AhR）和甲状腺激素受体α和β的激动活性。尽管没有一个BUVS显示出针对甲状腺激素受体的配体活性，但是其中四个（UV-P，UV-9，UV-326和UV-090）显示出显着的AhR配体活性。它们的半最大有效浓度（EC_（50））对于UV-P为130 nM，对于UV-9为460 nM，对于UV-090为5.1μM（无法确定UV-326的值）。在众多的AhR配体中，众所周知，那些无毒的配体会被诸如CYP1A1之类的酶迅速代谢，从而破坏了它们作为配体的功能。因此，我们建立了一种新的酵母检测方法，用于同时监测AhR配体活性的强度和CYP1A1对配体的降解。我们发现上述四个BUVS的AhR配体活性在CYP1A1存在下是稳定的。因此，它们有可能在人体中积累和发挥强大的生理作用，类似于已知的稳定和有毒的配体多环芳烃和二恶英。

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  • 来源
    《Environmental Science & Technology》 |2015年第1期|578-587|共10页
  • 作者

    Haruna Nagayoshi; Kensaku Kakimoto; Sokichi Takagi; Yoshimasa Konishi; Keiji Kajimura; Tomonari Matsuda;

  • 作者单位

    Osaka Prefectural Institute of Public Health, 1-3-69 Nakamichi, Higashinari-ku, Osaka, 537-0025, Japan;

    Osaka Prefectural Institute of Public Health, 1-3-69 Nakamichi, Higashinari-ku, Osaka, 537-0025, Japan;

    Osaka Prefectural Institute of Public Health, 1-3-69 Nakamichi, Higashinari-ku, Osaka, 537-0025, Japan;

    Osaka Prefectural Institute of Public Health, 1-3-69 Nakamichi, Higashinari-ku, Osaka, 537-0025, Japan;

    Osaka Prefectural Institute of Public Health, 1-3-69 Nakamichi, Higashinari-ku, Osaka, 537-0025, Japan;

    Research Center for Environmental Quality Management, Kyoto University, 1-2 Yumihama, Otsu, 520-0811, Japan;

  • 收录信息 美国《科学引文索引》(SCI);美国《工程索引》(EI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
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