Metabolic studies on polychlorinated biphenyls. II. Metabolic fate of 2,4,3',4'-tetrachlorobiphenyl in rats.
Metabolic studies on polychlorinated biphenyls. II. Metabolic fate of 2,4,3',4'-tetrachlorobiphenyl in rats.
复制标题
多氯联苯的代谢研究。
DOI：
10.1248/cpb.21.2231
复制
发表时间：
1973
影响因子：
1.7
通讯作者：
S. Saeki
中科院分区：
文献类型：
--
作者：
H. Yoshimura;H. Yamamoto;S. Saeki
为了了解Kanechlor-400（KC-400，一种多氯联苯的商业制剂）的毒性性质，并确定对这种KC-400中毒患者（所谓的Yusho）的治疗，使用大鼠研究了KC-400的主要成分2，4，3 '，4'-四氯联苯（2，4，3 '，4'-TCB）的代谢命运。结果发现，至少有四种具有酚类性质的代谢物与大量未改变的2，4，3 '，4'-三氯苯一起专门排泄到粪便中。其中，从粪便中分离出一种主要代谢物（M-A2），mp 155-156°，和一种次要代谢物（M-A1），mp 92-98°，并通过紫外、红外、核磁共振和质谱分析表征为单羟基化TCB。大鼠单次口服25毫克/只的2，4，3 '，4'-三氯苯后，在12天内，不到一半的剂量以原型2，4，3 '，4'-三氯苯的形式排泄，其中大部分在第一天内消除。主要代谢产物的排泄在第二天达到最大值，在12天内总M-A2约占剂量的10%。2，4，3 '，4'-TCB及其主要代谢产物在第12天仍有少量但显著的排泄。
In order to understand the toxic nature of Kanechlor-400 (KC-400, a commercial preparation of polychlorinated biphenyls) and establish the treatment of the patients of this KC-400 intoxication (so-called Yusho), metabolic fate of 2, 4, 3', 4'-tetrachlorobiphenyl (2, 4, 3', 4'-TCB), a major component of KC-400, was investigated using rats. It was found that at least four metabolites having phenolic nature were excreted exclusively into the feces together with a large amount of unchanged 2, 4, 3', 4'-TCB. Among these, a major metabolite (M-A2), mp 155-156°, and a minor metabolite (M-A1), mp 92-98°, were isolated from the feces and characterized to be monohydroxylated TCB by ultraviolet, infrared, nuclear magnetic resonance, and mass spectral analyses. After 2, 4, 3', 4'-TCB was orally administered at a single dose of 25 mg/body to the rat, a little less than one half of the dose was excreted as unchanged 2, 4, 3', 4'-TCB during 12 days, most of which were eliminated in the first day. The excretion of major metabolite reached maximum at the second day, and total M-A2 was accounted for about 10% of dose during 12 days. Both 2, 4, 3', 4'-TCB and its major metabolite were still excreted in a small but significant amount on 12th day.