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  • 标题:EFFECTS OF ACTIVATION OF UDP-GLUCURONYL TRANSFERASE ON METABOLISM OF BENZO[a]PYRENE WITH RAT LIVER MICROSOMES
  • 本地全文:下载
  • 作者:NOBUO NEMOTO ; MARIKO KAWANA ; SHOZO TAKAYAMA
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1983
  • 卷号:6
  • 期号:2
  • 页码:105-113
  • DOI:10.1248/bpb1978.6.105
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The effects of Brij 58 on microsome-mediated benzo[a]pyrene (BP)-metabolism were investigated. At a concentration of 0.01%, which did not decompose the microsomal mixed-function oxidase system, Brij 58 increased UDP-glucuronyl transferase activity on 3-hydroxy-BP to 560% of the control level. Quantitative changes of BP-metabolites by glucuronidation were found by high performance liquid chromatography. On incubation in the presence of UDP-glucuronic acid, the amounts of phenols decreased but the amounts of dihydrodiols did not change. Brij 58 enhanced the decrease in phenol metabolites. Unexpectedly, the binding of BP-metabolites to DNA was found to be higher in the presence of UDP-glucuronic acid, and Brij 58 also enhanced the binding in the presence of UDP-glucuronic acid. The ratio of bound adducts with BP-7, 8-dihydrodiol-9, 10-oxide to those with 9-hydroxy-BP-4, 5-oxide, which were separated by Sephadex LH-20 column chromatography, was increased by UDP-glucuronic acid and further enhanced by Brij 58. These results are discussed in relation to the role of glucuronidation in metabolism of BP.
  • 关键词:metabolic activation
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