Quercetin, a potent and specific inhibitor of the human P-form phenosulfotransferase.
The natural product quercetin was a potent inhibitor of the human P-form phenolsulfo-transferase with an IC50 value of 0.10 +/- 0.03 microM (mean +/- SEM; N = 5), which was three to four orders of magnitude more potent than its inhibition of other human sulfotransferases. The inhibition was noncompetitive with a Ki value of 0.10 microM. The potency and mechanism of this inhibition appear similar to those of the current standard P-form inhibitor, 2,6-dichloro-4-nitrophenol. Among other flavonoids examined, kaempferol was found to have an IC50 value of 0.39 +/- 0.07 microM, naringenin 10.6 +/- 1.6 microM and naringin 265 +/- 90 microM (N = 3). These observations suggest the potential for clinically important pharmacologic and toxicologic interactions by flavonoid-containing foods and beverages.
Walle
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Department of Cell and Molecular Pharmacology and Experimental Therapeutics, Medical University of South Carolina, Charleston 29425, USA.
Eaton
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EA
Walle
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UK
D015239:Arylsulfotransferase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D003687:Dehydroepiandrosterone / Q000737:chemistry; D004298:Dopamine / Q000737:chemistry; D006801:Humans; D008099:Liver / Q000187:drug effects / Q000201:enzymology; D015335:Molecular Probes; D009596:Nitrophenols / Q000494:pharmacology; D011794:Quercetin / Q000494:pharmacology*; D015238:Sulfotransferases / Q000737:chemistry
D015335:Molecular Probes; D009596:Nitrophenols; D003687:Dehydroepiandrosterone; C015802:2,6-dichloro-4-nitrophenol; D011794:Quercetin; D015238:Sulfotransferases; C019998:dehydroepiandrosterone sulfotransferase; D015239:Arylsulfotransferase; D004298:Dopamine