Antignac E, Koch B, Grolier P, Cassand P, Narbonne J F
Laboratoire de Toxicologie Alimentaire, Université de Bordeaux I, Talence, France.
Toxicol Lett. 1990 Dec;54(2-3):309-15. doi: 10.1016/0378-4274(90)90198-u.
We have determined how prochloraz, an imidazole antifungal agent, affects the metabolism of benzo[a]-pyrene by hepatic microsomes from 3-methylcholanthrene treated male rats. The prochloraz-like 7,8-benzoflavone was a potent inhibitor of total benzo[a]pyrene metabolism while miconazole was a weak inhibitor. The proportion of benzo[a]pyrene dihydrodiols formed was decreased whereas phenols were increased by the in vitro addition of prochloraz. Furthermore, a good correlation was obtained between the effects of prochloraz on the microsomal formation of benzo[a]pyrene metabolites and on the mutagenic activity of benzo[a]pyrene in the Salmonella typhimurium test.
我们已经确定了咪康唑类抗真菌剂咪鲜胺如何影响经3-甲基胆蒽处理的雄性大鼠肝脏微粒体对苯并[a]芘的代谢。与咪鲜胺类似的7,8-苯并黄酮是苯并[a]芘总代谢的强效抑制剂，而咪康唑是一种弱抑制剂。体外添加咪鲜胺会使苯并[a]芘二氢二醇的生成比例降低，而酚类物质增加。此外，在鼠伤寒沙门氏菌试验中，咪鲜胺对苯并[a]芘代谢物微粒体形成的影响与对苯并[a]芘致突变活性的影响之间存在良好的相关性。
