Forgue S T, Allen J R
Chem Biol Interact. 1982 Jun;40(2):233-45. doi: 10.1016/0009-2797(82)90103-x.
Tritiated 2,2'5,5'-tetrachlorobiphenyl (3H-TCB) was incubated with phenobarbital(PB)-induced rat liver microsomes in the presence of an epoxide hydrase inhibitor and brominated analog (BrAO) of the expected metabolic intermediate, 2,2',5,5'-tetrachlorobiphenyl-3,4-oxide (TCBAO). A putative arene oxide intermediate (3H-AO), which was radiolabeled, was separated from 3H-TCB and BrAO by column chromatography, high pressure liquid chromatography (HPLC) and thin-layer chromatography (TLC), and was analyzed for TCBAO by methods that were independent of radiometric techniques. The retention times (Rt's) of TCBAO and 3H-AO on two gas chromatography (GC) columns were the same, both before and after acid catalyzed rearrangement. 3H-AO was further characterized by rearrangement to a mixture of 3- and 4-hydroxy-TCB that was identified by gas chromatography-mass spectroscopy (GC-MS). The rate of TCB metabolism and the production of 3H-AO by liver microsomes from a PB-induced, adult male rhesus monkey was less than that observed with rat microsomes. The 3H-AO from the monkey was also characterized as TCBAO by rearrangement to the characteristic TCB phenols that were analyzed by GC-MS using selective ion monitoring. This study is the first in which an arene oxide of a polychlorinated biphenyl (PCB) was actually isolated as a mammalian metabolite and subjected to direct chemical analysis.
在环氧化物水解酶抑制剂和预期代谢中间体2,2',5,5'-四氯联苯-3,4-氧化物(TCBAO)的溴化类似物(BrAO)存在的情况下,将氚标记的2,2',5,5'-四氯联苯(3H-TCB)与苯巴比妥(PB)诱导的大鼠肝微粒体一起孵育。通过柱色谱、高压液相色谱(HPLC)和薄层色谱(TLC)从3H-TCB和BrAO中分离出一种放射性标记的假定芳烃氧化物中间体(3H-AO),并通过独立于放射性技术的方法对其进行TCBAO分析。在酸催化重排前后,TCBAO和3H-AO在两根气相色谱(GC)柱上的保留时间(Rt)相同。3H-AO通过重排为3-和4-羟基-TCB的混合物进一步表征,该混合物通过气相色谱-质谱联用(GC-MS)进行鉴定。PB诱导的成年雄性恒河猴肝微粒体对TCB的代谢速率和3H-AO的产生速率低于大鼠微粒体。通过重排为特征性的TCB酚类物质(使用选择性离子监测通过GC-MS进行分析),来自猴子的3H-AO也被表征为TCBAO。这项研究首次实际分离出多氯联苯(PCB)的芳烃氧化物作为哺乳动物代谢产物并进行直接化学分析。