Determination of piceatannol in rat serum and liver microsomes: pharmacokinetics and phase I and II biotransformation

Abstract

A method of analysis of piceatannol in biological fluids is necessary to study the kinetics of in vitro and in vivo metabolism and determine its concentration in foodstuffs. A novel and simple high-performance liquid chromatographic method was developed for simultaneous determination of piceatannol and products of its metabolism in rat serum and liver microsomes. Serum, or microsomes (0.1 mL), were precipitated with acetonitrile after addition of the internal standard, 4-methylumbelliferone. Separation was achieved on a phenomenex C(18) column (250 x 4.6 mm i.d., 5 microm) equipped with a phenomenex C(18) (4 x 3.0 mm i.d., 5 microm) guardcolumn with fluorescence excitation at 320 nm and emission at 420 nm. Separation was also possible with UV detection at 310 nm. The fluorescent calibration curves were linear ranging from 0.05 to 100 microg/mL. The mean extraction efficiency was >95%. Precision of the assay was <10% (coefficient of variation), and was within 10% at the limit of quantitation (0.05 ng/mL). Bias of the assay was lower than 7%. The limit of detection was 50 ng/mL for a 0.1 mL sample. The assay was applied successfully to the in vitro kinetic study of metabolism of piceatannol in rat liver microsomes and pharmacokinetics in rats. Three metabolites of piceatannol have been identified. .

Effect of long-term piceatannol treatment on eNOS levels in cultured endothelial cells

“…These results indicate that even low concentrations of piceatannol can increase eNOS expression when the duration of piceatannol exposure is extended. Although the pharmacokinetics of piceatannol is yet to be elucidated, the initial serum piceatannol level after intravenous administration at 10 mg/kg was reported to be 8.5 lg/mL (35 lM) [35].…”

Determination and assay validation of pinosylvin in rat serum: application to drug metabolism and pharmacokinetics

“…Male rat liver microsomes were prepared from adult male Sprague-Dawley rats using a previously published procedure [9,10]. The fresh rat livers were cut from euthanized rats and put into ice-cold saline, weighed, and minced.…”

A high‐performance liquid chromatographic analysis and preliminary pharmacokinetic characterization of 3′‐hydroxypterostilbene in rats

“…The disposition pattern of this 3′-hydroxylated stilbene is unique but the disposition shares some similarities with other stilbenes we have previously characterized in our laboratory in the rat model (Remsberg et al, 2007Roupe et al, 2004Roupe et al, , 2005aRoupe et al, ,b, 2006aWang et al, 2008).…”