Journal article
Inhibition of rat hepatic aryl sulphotransferase IV by dihydrodiol derivatives of benzo[a]pyrene and naphthalene
Xenobiotica, Vol.22(2), pp.247-255
1992
DOI: 10.3109/00498259209046623
PMID: 1632113
Abstract
1. Although neither the (+)- nor (-)-enantioner of trans-benzo[a]pyrene-7,8-dihydrodiol was a substrate for aryl sulphotransferase IV from rat liver, both enantiomers inhibited the enzyme-catalysed sulphation of 1-naphthalenemethanol with Ki values of 3.7 ± 0.4 μM for the (+)-enantiomer, and 4.4 ± 0.3 μM for the (-)-enantiomer.
2. Based on the magnitude of the Ki values, the binding affinity of these dihydrodiols for the aryl sulphotransferase was significantly greater than that for the corresponding phenolic derivatives of benzo[a]pyrene. That is 7-hydroxybenzo[a]pyrene and 8-hydroxybenzo[a]pyrene were both substrates for aryl sulphotransferase IV, with apparent Km values of 280 ± 41 μM and 370 ± 72 μM, respectively.
3. Both (+)- and (-)-trans-naphthalene-1,2-dihydrodiols were also inhibitors of aryl sulphotransferase IV, but with higher Ki values than would be expected from previously determined apparent Km and Ki values for (R)-(-)- and (S)-(+)-1,2,3,4-tetrahydro-1-naphthols, respectively.
Details
- Title: Subtitle
- Inhibition of rat hepatic aryl sulphotransferase IV by dihydrodiol derivatives of benzo[a]pyrene and naphthalene
- Creators
- S. I. Rao - University of IowaM. W. Duffel - University of Iowa
- Resource Type
- Journal article
- Publication Details
- Xenobiotica, Vol.22(2), pp.247-255
- Publisher
- Informa UK Ltd
- DOI
- 10.3109/00498259209046623
- PMID
- 1632113
- ISSN
- 0049-8254
- eISSN
- 1366-5928
- Language
- English
- Date published
- 1992
- Academic Unit
- Pharmaceutical Sciences and Experimental Therapeutics; Medicinal and Natural Products Chemistry
- Record Identifier
- 9984303162902771
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