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多溴联苯醚对大鼠肝细胞CYP1A2依赖性MROD活性的影响
作者姓名:聂芳红  陈进军  Bunce  Nigel
作者单位:广东海洋大学食品科技学院,广东海洋大学动物医学系,Dept.of Chemistry and Biochemistry University of Guelph,Guelph,Ontario,N1G 2W1,Canada,广东湛江 524088,广东湛江 524088
基金项目:教育部留学回国人员科研启动基金(教外司留[20031406号):广东海洋大学SCI源刊作者奖励基金(0412130).
摘    要:采用未成熟SD大鼠肝细胞微粒体为试验材料,以2,3,7,8-四氯-二苯基-并-二哑噁英(2,3,7,8- tetrachlorobenzo-p-dioxin,TCDD)作为参照,利用甲氧基-异酚噁脱甲基酶(methoxyresorufin-O- demethylase,MROD)竞争性抑制动力学和荧光光谱法分析法,测定了5种多溴联苯(polybrominated diphenyl ethers,PBDEs)对7-甲氧基-异酚噁唑脱甲基反应的影响,间接研究了这些PBDEs对CYP1A2 的竞争性抑制作用。结果表明,和TCDD相比,PBDEs对MROD活性的抑制作用较弱,亦即对CYP1A2的 竞争性抑制作用较弱。

关 键 词:MROD分析法  CYP  1A2  多溴联苯醚  大鼠

MROD Analysis of Competitive Inhibition from Polybrominated Diphenyl Ethers to CYP 1A2 in Rat Hepatocytic Microsomes
Authors:Nie Fanghong  Chen Jinjun  Bunce Nigel
Institution:1College of Food Science, Guangdong Ocean University, Zhanjiang, Guangdong 524088; 2Dept. of Veterinary Medicine, Guangdong Ocean University, Zhanjiang, Guangdong 524088; 3Dept. of Chemistry and Biochemistry, University of Guelph, Guelph, Ontario, N1G 2W
Abstract:The role of a number of polybrominated diphenyl ethers (PBDEs) as inhibitors of the demethylation of 7 -methoxyresorufin, a process that is selectively catalyzed by cytochrome P450 1A2 (CYP1A2), was examined, using methoxyresorufin -O -demethylase (MROD) fluorescent assay and competitive inhibition constant Ki determination. It was found that those examined PBDEs showed punier inhibiting effects to MROD / CYP1A2 than that of 2,3,7,8-Tetrachlorobenzo-p-dioxin (TCDD) which is the strongest inhibitor of MROD / CYP1A2 activity in dioxin-like compounds.
Keywords:MROD assay  CYP 1A2  Polybrominated diphenyl ethers  Rat
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