Glucuronidation of piceatannol by human liver microsomes: major role of UGT1A1, UGT1A8 and UGT1A10.

Objectives: Piceatannol, a dietary polyphenol present in grapes and wine, is known for its promising anticancer and anti-inflammatory activity. The aim of this study was to analyse the concentration-dependent glucuronidation of piceatannol in vitro.

Methods: To determine the glucuronidation of piceatannol, experiments were conducted with human liver microsomes as well as using a panel of 12 recombinant UDP-glucuronosyltransferase isoforms.

Expression of sulfotransferases and sulfatases in human breast cancer: impact on resveratrol metabolism.

Resveratrol is a naturally occurring anticancer compound present in grapes and wine that undergoes pronounced metabolism in human intestine and liver. In order to determine whether resveratrol is also bio-transformed in human breast carcinoma, metabolism experiments were conducted in breast tumor and adjacent non-tumorous specimens from 13 patients. Resveratrol was metabolized in cytosolic tissue fractions to resveratrol-3-O-sulfate: the formation rates were up to 33.

Antitumor activity of resveratrol and its sulfated metabolites against human breast cancer cells.

Resveratrol (3,4',5-trihydroxy- trans-stilbene) is a naturally occurring polyphenolic compound found in grapes, wine and medicinal plants with a variety of biological and pharmacological activities including pronounced anticancer properties. These effects are observed despite its extremely low bioavailability and rapid clearance from the circulation due to extensive sulfation and glucuronidation in the intestine and liver. In order to determine whether its metabolites demonstrate any cytotoxic properties, three major human sulfated conjugates of resveratrol were synthesized and their anticancer activity evaluated against three breast cancer cell lines (two hormone-dependent: MCF-7 and ZR-75-1; one hormone-independent: MDA-MB-231) and one immortalized breast epithelial cell line (MCF-10A).

In-vitro sulfation of piceatannol by human liver cytosol and recombinant sulfotransferases.

Objectives: The aim of this study was to investigate the concentration-dependent sulfation of piceatannol, a dietary polyphenol present in grapes and wine and known for its promising anticancer and anti-inflammatory activity.

Methods: Sulfation of piceatannol was investigated in human liver cytosol as well as using a panel of recombinant sulfotransferase isoforms. Furthermore, the chemical structures of novel sulfates were identified by liquid chromatography/mass spectrometry (LC/MS).

Metabolism of resveratrol in breast cancer cell lines: impact of sulfotransferase 1A1 expression on cell growth inhibition.

Resveratrol is a polyphenolic compound present in grapes and wine with anticancer activities that undergoes pronounced metabolism in humans. In order to determine whether metabolism of resveratrol also occurs in tumor cells and whether biotransformation has any impact on cytotoxicity, metabolism experiments were conducted with hormone-dependent ZR-75-1 and hormone-independent MB-MDA-231 human breast cancer cells. Along with resveratrol, it was possible to identify one metabolite, namely, resveratrol-3-O-sulfate in both cell lines.

Pharmacokinetics of voriconazole during continuous venovenous haemodiafiltration.

Objectives: Voriconazole is a new triazole antifungal agent that is frequently used in intensive care patients with severe fungal infections. Continuous venovenous haemodiafiltration (CVVHDF) is an important extracorporal renal replacement therapy in critically ill patients suffering from severe infections and multiple organ failure. This study investigates the pharmacokinetics of voriconazole in anuric patients undergoing CVVHDF.

Uptake of diet resveratrol into the human low-density lipoprotein. Identification and quantification of resveratrol metabolites by liquid chromatography coupled with tandem mass spectrometry.

In this paper, a sensitive, precise, and selective analytical method has been developed for the identification and quantification of resveratrol metabolites in human low-density lipoprotein (LDL) after moderate consumption of red wine, using high-performance liquid chromatography electrospray in tandem mass spectrometry (LC-ESI-MS/MS). From different extraction procedures tested, solid-phase extraction was selected to minimize matrix effects reaching the highest sensitivity. Standard calibration curves prepared in human LDL for trans-resveratrol were linear over a range of 0.