农药叶枯灵在大鼠原位灌流肝中的代谢研究

Studies on Metabolism of a New Fungicide Yekuling in Situ Perfused Rat Liver

采用反相HPLC、TLC、UV、IR和MS对农药叶枯灵经大鼠原位灌流肝代谢后所形成的代谢产物进行分离和鉴定。结果表明,叶枯灵在大鼠肝脏中进行了广泛的代谢,包括S-氧化作用、水解作用、丙酮酸缩合作用和乙酰化作用,共分离鉴定出5种代谢产物。

The metabolism of a new fungicide Yekuling was studied in situ perfused rat liver. Five metabolites were isolated and purified by means of HPLC and TLC. They were identified at 1 , 3-dithiolan-2-ylidenehydrazine; acetic acid, 1,3-dithiolan-2-ylidenehydrazide; benzoic acid, 1,3-dithiolan-2-ylidenehydrazide-S-oxide; pyruvic acid, 1,3-dithiolan-2-ylide-nehydrazide and benzoic acid by UV, IR and MS. The latter was further confirmed by chemical synthesis. It is obvious that Yekuling was metabolized extensively in rat liver. Yeku ling was sulfoxidated by rat liver microsomal mixed-function oxidase in the presence of NADPH to produce sulfoxide. Yekuling was also hydrolyzed by amidase to form benzoic acid and 1,3-dithiolan-2-ylidenehydrazine. The latter was further acetylated by N-acetyltrans ferase to form acetic acid, 1,3-dithiolan-2-ylidenehydrazide, and condensed to form pyruvic acid, 1,3-dithiolan-2-ylidenehydrazide.