Diaz M J, Chinje E, Kentish P, Jarnot B, George M, Gibson G G
School of Biological Sciences, University of Surrey, Guildford, U.K.
Biochem Pharmacol. 1993 Sep 14;46(6):1076-80. doi: 10.1016/0006-2952(93)90673-k.
Male Wistar albino rats were treated for a 7 day period with equimolar doses of the trimer and tetramer oligomers of chlorotrifluoroethylene (CTFE), resulting in significant hepatomegaly for both compounds. In addition, both trimer and tetramer significantly induced the peroxisomal beta-oxidation of fatty acids as assessed by increases in palmitoyl-coenzyme A (CoA) oxidation, thus confirming these oligomers as peroxisome proliferators. Consistent with these conclusions, both trimer and tetramer increased the hydroxylation of lauric acid indicating that the CTFEs were inducers of the CYP4A subfamily, a conclusion further supported by substantial increases in the steady-state levels of the cognate CYP4A1 mRNA as determined by northern blotting. The liver appeared to be more susceptible to induction than the kidney and the CTFE tetramer was more potent than the trimer. These results are discussed with respect to both the differential hepatotoxicity, and biotransformation/disposition of the two polyhalogenated oligomers.
雄性Wistar白化大鼠用等摩尔剂量的三氟氯乙烯(CTFE)三聚体和四聚体低聚物处理7天,两种化合物均导致显著的肝脏肿大。此外,三聚体和四聚体均通过棕榈酰辅酶A(CoA)氧化增加显著诱导脂肪酸的过氧化物酶体β-氧化,从而证实这些低聚物为过氧化物酶体增殖剂。与这些结论一致,三聚体和四聚体均增加月桂酸的羟基化,表明CTFEs是CYP4A亚家族的诱导剂,通过Northern印迹法测定的同源CYP4A1 mRNA稳态水平的大幅增加进一步支持了这一结论。肝脏似乎比肾脏更容易受到诱导,并且CTFE四聚体比三聚体更有效。就两种多卤代低聚物的不同肝毒性以及生物转化/处置对这些结果进行了讨论。