Gao N
Department Environmental Health, Third Military Medical College, Chongqing.
Zhonghua Yu Fang Yi Xue Za Zhi. 1992 Mar;26(2):70-3.
The metabolism of a fungicide Yekuling was studied in rat after oral administration. Four metabolites were isolated and purified by means of reverse-phase HPLC and TLC. They were identified to be acetic acid, 1,3-dithiolan-2-ylidenehydrazide; pyruvic acid, 1,3-dithiolan-2-ylidenehydrazide; benzoic acid and hippuric acid with UV and MS. The latter was further confirmed by chemical synthesis. The experimental results showed that Yekuling was metabolized extensively in rat. Yekuling was hydrolyzed by amidase to produce benzoic acid and 1,3-dithiolan-2-ylidenehydrazide. The latter was further acetylated by N-acetyltransferase to form acetic acid, 1,3-dithiolan-2-ylidenehydrazide, or condensed spontaneously to form pyruvic acid, 1,3-dithiolan-2-ylidenehydrazide. Benzoic acid was further conjugated with glycine to produce hippuric acid.
对大鼠口服杀菌剂叶枯灵后的代谢情况进行了研究。通过反相高效液相色谱法和薄层色谱法分离并纯化了四种代谢物。利用紫外光谱和质谱鉴定它们为乙酸、1,3 -二硫杂环戊烷 - 2 -亚基酰肼；丙酮酸、1,3 -二硫杂环戊烷 - 2 -亚基酰肼；苯甲酸和马尿酸。后者通过化学合成进一步得到证实。实验结果表明，叶枯灵在大鼠体内发生了广泛代谢。叶枯灵被酰胺酶水解生成苯甲酸和1,3 -二硫杂环戊烷 - 2 -亚基酰肼。后者被N - 乙酰转移酶进一步乙酰化形成乙酸、1,3 -二硫杂环戊烷 - 2 -亚基酰肼，或自发缩合形成丙酮酸、1,3 -二硫杂环戊烷 - 2 -亚基酰肼。苯甲酸进一步与甘氨酸结合生成马尿酸。
