Thabrew M I, Emerole G O
Eur J Drug Metab Pharmacokinet. 1983 Oct-Dec;8(4):321-7. doi: 10.1007/BF03188764.
Investigations have been carried out to determine the effects of the herbicide 1.1.1 trifluoro-N-(2-methyl-4-phenyl sulfonyl) methane sulfonamide (Destun) on some hepatic microsomal drug metabolizing enzymes in rat. Administration of 100 mg herbicide/kg rat (i.p. or oral) resulted in a stimulation of aniline hydroxylase and p-aminopyrene N-demethylase activities by 1.3 fold and 1.6 fold respectively. A dose-related increase in enzyme activities was observed with a maximum effect at about 100 mg Destun/kg rat. The increased microsomal protein content, liver weight: body weight ratio and decreased sleeping time in the herbicide-treated animals indicated the possibility of Destun being an "inducer". Results of investigations on the kinetic properties of aniline hydroxylase and p-aminopyrene-N-demethylase on administration of Destun suggests that in addition to its inducer effect, the herbicide could stimulate the enzyme activities by decreasing the affinity of these enzymes for their respective substrates.
已开展研究以确定除草剂1.1.1-三氟-N-(2-甲基-4-苯基磺酰基)甲磺酰胺（敌草隆）对大鼠某些肝微粒体药物代谢酶的影响。给大鼠腹腔注射或口服100毫克/千克除草剂后，苯胺羟化酶和对氨基芘N-脱甲基酶的活性分别提高了1.3倍和1.6倍。观察到酶活性随剂量增加，在约100毫克敌草隆/千克大鼠时达到最大效应。除草剂处理动物的微粒体蛋白含量增加、肝重与体重之比增加以及睡眠时间减少，表明敌草隆可能是一种“诱导剂”。关于给予敌草隆后苯胺羟化酶和对氨基芘-N-脱甲基酶动力学特性的研究结果表明，除了其诱导作用外，该除草剂还可通过降低这些酶对各自底物的亲和力来刺激酶活性。
