苯并[a]蒽在人肝微粒体中的代谢。

Metabolism of benz[a]anthracene by human liver microsomes.

作者信息

Sahali Y, Kidd L R, Skipper P L, Tannenbaum S R

机构信息

Division of Toxicology, Massachusetts Institute of Technology, Cambridge 02139.

出版信息

Cancer Lett. 1994 Aug 15;83(1-2):299-303. doi: 10.1016/0304-3835(94)90333-6.

DOI:10.1016/0304-3835(94)90333-6

PMID:8062227

Abstract

The metabolism of benz[a]anthracene (BA) by human hepatic microsomes was investigated. Only dihydrodiols were observed when BA was the substrate. No tetrahydrotetrols were detected, indicating lack of diol epoxide formation. The BA-dihydrodiols identified by GCMS analysis and comparison to authentic standards were BA-8,9-dihydrodiol (42.4% of total metabolites), BA-5,6-dihydrodiol (25%), BA-10,11-dihydrodiol (24.8%), BA-3,4-dihydrodiol (5.3%), and BA-1,2-dihydrodiol (< 1.5%). BA-dihydrodiols were also used individually as substrates. Only BA-1,2-dihydrodiol, the least abundant isomer produced from BA, was converted efficiently to a tetrahydrotetrol (> 72% conversion). BA-10,11-dihydrodiol was converted to BA-8,9,10,11-tetrahydrotetrols in < 12% yield. BA-10,11- and BA-3,4-dihydrodiols were not converted to tetrahydrotetrols.

摘要

对苯并[a]蒽（BA）在人肝微粒体中的代谢情况进行了研究。以BA为底物时，仅观察到二氢二醇。未检测到四氢四醇，表明没有形成二醇环氧化物。通过气相色谱 - 质谱联用（GCMS）分析并与标准品比较鉴定出的BA - 二氢二醇有：BA - 8,9 - 二氢二醇（占总代谢物的42.4%）、BA - 5,6 - 二氢二醇（25%）、BA - 10,11 - 二氢二醇（24.8%）、BA - 3,4 - 二氢二醇（5.3%）和BA - 1,2 - 二氢二醇（<1.5%）。BA - 二氢二醇也分别用作底物。只有BA - 1,2 - 二氢二醇（由BA产生的含量最少的异构体）能高效转化为四氢四醇（转化率>72%）。BA - 10,11 - 二氢二醇转化为BA - 8,9,10,11 - 四氢四醇的产率<12%。BA - 10,11 - 二氢二醇和BA - 3,4 - 二氢二醇未转化为四氢四醇。