Journal of Pharmacobio-Dynamics
Online ISSN : 1881-1353
Print ISSN : 0386-846X
ISSN-L : 0386-846X
EFFECTS OF ACTIVATION OF UDP-GLUCURONYL TRANSFERASE ON METABOLISM OF BENZO[a]PYRENE WITH RAT LIVER MICROSOMES
NOBUO NEMOTOMARIKO KAWANASHOZO TAKAYAMA
著者情報
キーワード: metabolic activation
ジャーナル フリー

1983 年 6 巻 2 号 p. 105-113

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抄録
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.
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© The Pharmaceutical Society of Japan
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