Dent J G, Roes U, Netter K J, Gibson J E
J Toxicol Environ Health. 1977 Nov;3(4):651-61. doi: 10.1080/15287397709529599.
The pattern of stimulation of hepatic microsomal mixed function oxidases has been studied in female NMRI mice following a single ip injection of 150 mg/kg polybrominated biphenyls (PBBs) and compared to the patterns produced by phenobarbital (PB), 3 X 100 mg/kg; 3-methylcholanthrene (MC), 3 X 20 mg/kg; and these two agents administered together at these doses. Cytochrome P450, ethylmorphine N-demethylase, and epoxide hydratase reached maximums of 200, 200, and 350% of control values, respectively, at 48 hr after treatment with PBBs. Ethoxycoumarin O-deethylase and arylhydrocarbon hydroxylase were maximally increased to 400 and 180% of control values, respectively, 96 hr after PBBs. The reduced cytochrome P450 ethylisocyanide difference spectra and the inhibition of ethoxycoumarin O-deethylase and arylhydrocarbon hydroxylase activity by metyrapone and alpha-naphthoflavone indicated that the characteristics of the cytochrome P450 and the cytochrome P450-dependent enzymes changed with time after administration of PBBs. These results indicate that the enzyme-stimulating properties of PBBs alter, changing from PB-like to MC-like, with time after administration. These findings provide an explanation for the effects of PBBs on the toxicity of bromobenzene, indicating that PBBs represent a new and previously unrecognized calss of toxicity-modifying agents sharing properties of both PB and MC.
在雌性NMRI小鼠单次腹腔注射150mg/kg多溴联苯(PBBs)后,研究了其对肝微粒体混合功能氧化酶的刺激模式,并与苯巴比妥(PB)(3×100mg/kg)、3-甲基胆蒽(MC)(3×20mg/kg)以及这两种药物按此剂量联合给药所产生的模式进行了比较。在用PBBs处理后48小时,细胞色素P450、乙基吗啡N-脱甲基酶和环氧化物水化酶分别达到对照值的200%、200%和350%的最大值。在用PBBs处理96小时后,乙氧香豆素O-脱乙基酶和芳烃羟化酶分别最大增加到对照值的400%和180%。细胞色素P450乙基异氰化物差光谱的降低以及甲吡酮和α-萘黄酮对乙氧香豆素O-脱乙基酶和芳烃羟化酶活性的抑制表明,在给予PBBs后,细胞色素P450和细胞色素P450依赖性酶的特性随时间发生了变化。这些结果表明,PBBs的酶刺激特性会随着给药后的时间而改变,从类似PB转变为类似MC。这些发现为PBBs对溴苯毒性的影响提供了解释,表明PBBs代表了一类新的、以前未被认识的毒性修饰剂,兼具PB和MC的特性。