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首页> 外文期刊>Journal of the Korean Society for Applied Biological Chemistry >In vitro Metabolism of Flucetosulfuron by Artificial Gastrointestinal Juices
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In vitro Metabolism of Flucetosulfuron by Artificial Gastrointestinal Juices

机译：人工胃肠液对氟磺隆的体外代谢

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摘要

To investigate the metabolism of pesticides by gastrointestinal (GI) juices, artificial GI juices were incubated with threo- and erythro-isomers of flucetosulfuron. The metabolites produced in each reaction mixture of artificial GI juices were unambiguously identified using liquid chromatography-tandem mass spectrometry. Flucetosulfuron was observed to be stable in saliva. However, in the intestinal juices, approximately 18% of flucetosulfuron was degraded, producing N-(4,6-dimethoxypyrimidin-2-ylcarbomoyl)-2-(2-fluoro-1-hydroxypropyppyri midine-3-sulfonamid (M1). In artificial gastric juices, about 85% of flucetosulfuron was rapidly degraded, producing the metabolites 2-(2-fluoro-1-hydroxypropyl) pyridine-3-sulfonamide (M2), 4,6-dimethoxypyrimiclin-2-amine (M3), and 2-fluoro-1-(3-sulfamoylpyridin-2-yl)propyl 2-methoxyacetate (M4). These results indicate that the sulfonylurea bridge and ester bond of flucetosulfuron are hydrolyzed in artificial GI juices. No significant differences were noted in the degradation patterns between the two isomers of flucetosulfuron in the artificial GI juices that were tested. Considering the rapid degradation of flucetosulfuron in vitro by artificial GI juices, it is likely that there would be no significant absorption of flucetosulfuron from the GI tract into the blood stream after oral administration.
机译：为了研究胃肠道（GI）汁液对农药的代谢作用，将人工GI汁液与氟磺隆的苏式和赤式异构体一起孵育。使用液相色谱-串联质谱法明确鉴定了人工胃肠液的每种反应混合物中产生的代谢物。氟嘧磺隆在唾液中稳定。但是，在肠液中，大约18％的氟磺隆被降解，生成N-（4,6-二甲氧基嘧啶-2-基氨基甲酰基）-2-（2-氟-1-羟基丙氨嘧啶-3-磺酸钠（M1）。人工胃液中，大约85％的氟磺隆迅速降解，产生代谢物2-（2-氟-1-羟丙基）吡啶-3-磺酰胺（M2），4,6-二甲氧基嘧啶-2-胺（M3）和结果表明，2-氟-1-（3-氨磺酰基吡啶-2-基）丙基2-甲氧基乙酸酯（M4）表明，氟丁磺隆中的磺酰脲桥和酯键被水解，降解没有显着差异。测试的人工胃肠液中氟磺隆的两个异构体之间的模式。考虑到人工胃肠液在体外迅速降解氟磺隆，氟磺隆从胃肠道吸收后很可能不会显着吸收到血液中口服。

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