1. Quercetin is a natural ¯avonoid present in vegetables, fruit and wine, and is known to inhibit sulphotransferase. Drugs are often taken orally and the intestinal mucosa is an early site of drug metabolism. The aims of this investigation were to study the inhibition of dopamine, (¡)-salbutamol, minoxidil and paracetamol sulphation by quercetin in the duodenal mucosa and liver and to compare the IC50 in these tissues. 2. The rates (pmolmin¡1 mg¡1) of sulphation of 4-nitrophenol were 343 92 (liver) and 164 22 (duodenum; p ˆ 0:031), of dopamine were 15 11 (liver) and 656 516 (duodenum; p ˆ 0:049), of (¡)-salbutamol were 153 31 (liver) and 654 277 (duodenum; p ˆ 0:018), of minoxidil were 156 47 (liver) and 105 7 (duodenum; n:s:), and of paracetamol were 229 86 (liver) and 328 187 (duodenum; n.s.). 3. The IC50 of quercetin for 4-nitrophenol was 48 11 nM (liver) and 56 1 nM (duodenum, n.s.), for dopamine was 5:7 0:7 mM (liver) and 170 12mM (duodenum, p < 0:0001), for (¡)-salbutamol was 54 4 nM (liver) and 16 8 mM (duodenum; p ˆ 0:025†, for minoxidil was 134 22 nM (liver) and 3 0:3 mM (duodenum, p ˆ 0:013), and for paracetamol was 57 7 nM (liver) and 35 1 mM (duodenum; p ˆ 0:0002). 4. Quercetin inhibited the sulphation of 4-nitrophenol, dopamine, (¡)-salbutamol, minoxidil and paracetamol both in liver and duodenum. With dopamine, (¡)-salbutamol, minoxidil and paracetamol as substrates, quercetin was a more potent inhibitor in the liver than the duodenum. Such a di erence may re¯ect the di erent composition of sulphotransferase forms in the liver and duodenum.
|Autori:||Marchetti F; De Santi C; Vietri M; Pietrabissa A; Spisni R; Mosca F; Pacifici GM|
|Titolo:||Differential inhibition of humanliver and duodenum sulphotransferase activities by quercetin, a flavonoid present in vegetables, fruit, wine|
|Anno del prodotto:||2001|
|Digital Object Identifier (DOI):||10.1080/00498250110069159|
|Appare nelle tipologie:||1.1 Articolo in rivista|