文章摘要
于灵芝,杨先乐,王翔凌,喻文娟,胡鲲.草鱼肾细胞中双氟沙星代谢酶的酶动学[J].水产学报,2010,34(3):404~409
草鱼肾细胞中双氟沙星代谢酶的酶动学
Enzymatics on DIF metabolism in kidney cell of grass carp (Ctenopharyngodon idellus
投稿时间:2009-04-28  修订日期:2009-09-03
DOI:10.3724/SP.J.1231.2010.06445
中文关键词: 草鱼  细胞色素P450  双氟沙星  酶动力学  反相高效液相色谱
英文关键词: Ctenopharyngodon idellus  cytochrome P450  difloxacin  kinetics  RP-HPLC
基金项目:“十一五”国家科技支撑计划(2006BAD03B04);农业部行业专项(200803013);现代农业产业技术体系建设专项资金
作者单位E-mail
于灵芝 上海海洋大学 lzyud@stmail.shou.edu.cn 
杨先乐 上海海洋大学  
王翔凌 上海美迪西普亚医药科技有限公司  
喻文娟 上海海洋大学  
胡鲲 上海海洋大学  
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中文摘要:
      细胞色素P450s(CYPs) 主要参与动物体内药物代谢。水产养殖中不合理的联合用药常会导致治疗失败,这通常与CYP活性的诱导有关。然而,关于鱼类CYP的诱导却知之甚少。为获得有关CYP诱导的信息,实验采用反相高效液相色谱(RP-HPLC)的方法测定了草鱼肾细胞(CIK)中CYPs的特异性诱导剂对双氟沙星(DIF)的代谢作用及酶动学分析。对照组和β-萘黄酮(BNF)诱导组的酶动学方程分别为1/V=0.137 5×1/[S]+0.003 和1/V=0.024 5×1/ [S]+ 0.001 3。DIF与经BNF处理的CIK共孵育后,其代谢量增加了1倍,酶动学参数Clint和Vmax值分别增加了7倍和2倍。BNF是CYP1A的特异性诱导剂,因此,CYP1A可能参与了DIF的代谢。
英文摘要:
      Cytochrome P450s (CYPs) is the most important enzyme for drug metabolism in animals. Inappropriate coadministration often causes treatment failure in fisheries owing to induction of CYP activity. However, limited information is available about CYP induction in fish. In order to supply useful information on CYP induction, the present study assessed the effects of fish specific CYP inducers on difloxacin (DIF) metabolism and the enzyme kinetics in kidney cell of grass carp (Ctenopharyngodon idellus) (CIK) by reversed phase high performance liquid chromatography (RP-HPLC). The enzymatic equations of control and groups induced by β-naphthoflavone (BNF)were 1/V= 0.137 5 ×1/[S]+0.003 and 1/V=0.024 5×1/[S]+0.001 3. Results demonstrated that the amounts of DIF metabolism were increased by 1 fold and enzymatic parameters Clint and Vmax of DIF metabolism were significantly increased by 7 and 2 folds due to BNF pretreatment. BNF is the specific inducer of CYP1A in fish. Therefore, CYP1A may be responsible for DIF metabolism. This study provides instructive information to ensure treatment success in fisheries medication with two or more drugs.
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