Suppr超能文献

正丁基缩水甘油醚在F344大鼠和B6C3F1小鼠体内的代谢与处置

Metabolism and disposition of n-butyl glycidyl ether in F344 rats and B6C3F1 mice.

作者信息

Chen L-J, Lebetkin E H, Nwakpuda E I, Burka L T

机构信息

Laboratory of Pharmacology and Chemistry, National Institute of Environmental Health Sciences, Research Triangle Park, NC, USA.

出版信息

Drug Metab Dispos. 2007 Dec;35(12):2218-24. doi: 10.1124/dmd.107.016931. Epub 2007 Sep 17.

Abstract

The disposition of [(14)C]-labeled n-butyl glycidyl ether (BGE, 3-butoxy-1,2-epoxypropane) was studied in rats and mice. The majority of a single p.o. dose (2-200 mg/kg) was excreted in urine (rats, 84-92%; mice, 64-73%) within 24 h. The rest of the dose was excreted in feces (rats, 2.6-7.7%; mice, 5.3-12%) and in expired air as (14)CO(2) (rats, 1.5%; mice, 10-18%), or remained in the tissues (rats, 2.7-4.4%; mice, 1.5-1.7%). No parent BGE was detected in rat or mouse urine. Fifteen urinary metabolites were identified, including 3-butoxy-2-hydroxy-1-propanol and its monosulfate or monoglucuronide conjugates, 3-butoxy-2-hydroxypropionic acid, O-butyl-N-acetylserine, butoxyacetic acid, 2-butoxyethanol, and 3-butoxy-1-(N-acetylcystein-S-yl)-2-propanol, the mercapturic acid metabolite derived from conjugation of glutathione (GSH) with BGE at the C-1 position. Some of these metabolites underwent further omega-1 oxidation to form a 3'-hydroxybutoxy substitution. One urinary metabolite was from omega-oxidation of 3-butoxy-1-(N-acetylcystein-S-yl)-2-propanol to yield the corresponding carboxylic acid. Oxidative deamination of 3-butoxy-1-(cystein-S-yl)-2-propanol gave the corresponding alpha-keto acid and alpha-hydroxy acid metabolites that were present in mouse urine but not in rat urine. An in vitro incubation of BGE with GSH showed that the conjugation occurred only at the C-1 position with or without the addition of GSH S-transferase.

摘要

对[(14)C]标记的正丁基缩水甘油醚(BGE,3-丁氧基-1,2-环氧丙烷)在大鼠和小鼠体内的处置情况进行了研究。单次口服剂量(2 - 200毫克/千克)的大部分在24小时内通过尿液排出(大鼠为84 - 92%;小鼠为64 - 73%)。其余剂量通过粪便排出(大鼠为2.6 - 7.7%;小鼠为5.3 - 12%),并以(14)CO₂的形式从呼出气体中排出(大鼠为1.5%;小鼠为10 - 18%),或留在组织中(大鼠为2.7 - 4.4%;小鼠为1.5 - 1.7%)。在大鼠或小鼠尿液中未检测到母体BGE。鉴定出了15种尿液代谢产物,包括3-丁氧基-2-羟基-1-丙醇及其单硫酸盐或单葡萄糖醛酸共轭物、3-丁氧基-2-羟基丙酸、O-丁基-N-乙酰丝氨酸、丁氧基乙酸、2-丁氧基乙醇以及3-丁氧基-1-(N-乙酰半胱氨酸-S-基)-2-丙醇,后者是谷胱甘肽(GSH)与BGE在C-1位结合形成的硫醚氨酸代谢产物。其中一些代谢产物会进一步发生ω-1氧化,形成3'-羟基丁氧基取代物。一种尿液代谢产物是由3-丁氧基-1-(N-乙酰半胱氨酸-S-基)-2-丙醇的ω-氧化生成相应的羧酸。3-丁氧基-1-(半胱氨酸-S-基)-2-丙醇的氧化脱氨反应产生了相应的α-酮酸和α-羟基酸代谢产物,这些产物存在于小鼠尿液中,但不存在于大鼠尿液中。BGE与GSH的体外孵育表明,无论是否添加GSH S-转移酶,结合反应仅在C-1位发生。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验