Journal Article 2,2ʼ,3,4,4ʼ,5,6ʼ-七塩素化ビフェニル(CB182)のラット,モルモットおよびヒト肝ミクロゾームによる代謝
Metabolism of 2,2ʼ,3,4,4ʼ,5,6ʼ-Heptachlorobiphenyl (CB182) by Rat, Guinea Pig and Human Liver Microsomes

太田, 千穂  ,  藤井, 由希子  ,  原口, 浩一  ,  加藤, 善久  ,  木村, 治  ,  遠藤, 哲也  ,  古賀, 信幸

108 ( 3 )  , pp.51 - 57 , 2017-03-25 , 福岡医学会
The in vitro metabolism of 2,2ʼ,3,4,4ʼ,5,6ʼ-heptachlorobiphenyl (CB182) by rat, guinea pig and human liver microsomes was compared and the effects of cytochrome P450 (CYP) inducers, phenobarbital (PB) and 3-methylcholanthrene (MC), on CB182 metabolism were examined. Only one metabolite was produced by rat, guinea pig and human liver microsomes and the order of the activity was rat (PB-treated)>> guinea pig (PB-treated)> guinea pig (untreated, MC-treated)> human > rat (untreated). Pretreatment of PB resulted in the remarkable increase of the metabolite in rats (1,370 pmol/hr/mg protein) and a slight increase in guinea pigs (27 pmol/hr/mg protein). In contrast, MC treatment to rats and guinea pigs decreased M-1. By comparison of GC-MS data of the methylated M-1 with a synthesized authentic sample, M-1 was determined to be 3ʼ-hydroxy (OH)-CB182. These results suggest that 3ʼ-OH-CB182 is a major metabolite formed by PB-inducible CYP2B enzymes in both animals and rat CYP2B enzymes possess much higher activity to hydroxylate CB182 than guinea pig and human CYP2B enzymes.

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