首页> 外文期刊>Archives of Toxicology >Uptake of triclopyr (3,5,6-trichloro-2-pyridinyloxyacetic acid) and dicamba (3,6-dichloro-2-methoxybenzoic acid) from the apical membranes of the human intestinal Caco-2 cells
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Uptake of triclopyr (3,5,6-trichloro-2-pyridinyloxyacetic acid) and dicamba (3,6-dichloro-2-methoxybenzoic acid) from the apical membranes of the human intestinal Caco-2 cells

机译:从人肠道Caco-2细胞的顶膜摄取麦草畏(3,5,6-三氯-2-吡啶基氧基乙酸)和麦草畏(3,6-二氯-2-甲氧基苯甲酸)

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摘要

We investigated whether the uptake of triclopyr (3, 5, 6-trichloro-2-pyridinyloxyacetic acid) and dicamba (3,6-dichloro-2-methoxybenzoic acid) across the apical membrane of Caco-2 cells was mediated via proton-linked monocarboxylic acid transporters (MCTs). The uptake of triclopyr from the apical membranes was fast, pH-, temperature-, and concentration dependent, required metabolic energy to proceed, and was competitively inhibited by monocarboxylic acids such as benzoic acid and ferulic acid (substrates of l-lactic acid-insensitive MCTs), but not by l-lactic acid. Thus, the uptake of triclopyr in Caco-2 cells appears to be mediated mainly via l-lactic acid-insensitive MCTs. In contrast, the uptake of dicamba (a benzoic acid derivative) was slow, and it was both pH- and temperature dependent. Coincubation with ferulic acid did not decrease the uptake of dicamba, although coincubation with benzoic acid moderately decreased it. The uptake of dicamba appears to be mediated mainly via passive diffusion, which is in contrast to the uptake of benzoic acid via MCTs. We speculate that the substituted groups in dicamba may inhibit uptake via MCTs.
机译:我们调查了是否通过质子连接介导Caco-2细胞顶膜对麦草畏(3,5,6-三氯-2-吡啶基氧基乙酸)和麦草畏(3,6-二氯-2-甲氧基苯甲酸)的吸收一元羧酸转运蛋白(MCT)。根尖细胞对毛状tric虫的吸收速度快,pH值,温度和浓度依赖性,需要代谢能量才能继续进行,并被苯甲酸和阿魏酸等单羧酸竞争性抑制(对L-乳酸不敏感的底物MCTs),但不能使用l-乳酸。因此,Caco-2细胞中对草甘膦的摄取似乎主要是通过对乳酸不敏感的MCT介导的。相反,麦草畏(苯甲酸衍生物)的吸收较慢,并且与pH和温度有关。与阿魏酸共孵育不会降低麦草畏的吸收,尽管与苯甲酸共孵育会适度降低麦草畏的摄取。麦草畏的吸收似乎主要是通过被动扩散来介导的,这与通过MCT吸收苯甲酸相反。我们推测麦草畏中的取代基可能会抑制通过MCT的吸收。

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