Pharmacokinetic profile of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside in mice after oral administration of Polygonum multiflorum extract

Drug Dev Ind Pharm. 2012 Feb;38(2):248-55. doi: 10.3109/03639045.2011.597763. Epub 2011 Sep 5.

Abstract

Context: Stilbene glycoside (2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside) is a main bioactive component of Polygonum multiflorum, a traditional Chinese medicine (TCM) commonly used in clinic for anti-aging treatment. Its medicinal activities, such as anti-oxidation, anti-inflammation and endothelial protection, have been extensively studied, but its pharmacokinetic property is still unclear.

Objective: A pharmacokinetic study was undertaken to quantitatively determine P. multiflorum stilbene glycoside (PM-SG) in mouse plasma after oral administration of 100 mg/kg P. multiflorum extract.

Materials and methods: A sensitive reversed-phase high-performance liquid chromatography (RP-HPLC) coupled with liquid-liquid phase extraction method was employed for this study. Pharmacokinetic parameters of PM-SG were determined in mice applying both compartmental and non-compartmental analyses.

Results and discussion: The calibration curve for PM-SG in the plasma was linear (r(2) > 0.99) over the range of 0.66 to 56.40 μg/ml, and the concentration-time curve was plotted with the maximum concentration (C(max)) and time to reach maximum concentration (T(max)) of 29.62 μg/ml and 60 min, respectively. The intra- and inter-day variations were less than 3% for relative standard deviation (RSD) and relative error (RE), with a good recovery of more than 97% (RSD <3%). All pharmacokinetic parameters estimated by compartmental and non-compartmental models reached a same conclusion that PM-SG was rapidly absorbed and widely distributed throughout the body with a great efficiency of utility, followed by quick elimination and clearance.

Conclusions: This was the first report on determination of the pharmacokinetic profile of PM-SG in mice after oral administration. The result may provide a meaningful basis for evaluating the clinical applications of such a bioactive compound from herbal medicines.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Chromatography, High Pressure Liquid
  • Chromatography, Reverse-Phase
  • Drugs, Chinese Herbal / pharmacokinetics*
  • Glucosides / pharmacokinetics*
  • Male
  • Medicine, Chinese Traditional
  • Mice
  • Models, Animal
  • Plant Preparations / pharmacokinetics*
  • Plant Roots
  • Plants, Medicinal
  • Polygonum / chemistry
  • Stilbenes / pharmacokinetics*

Substances

  • Drugs, Chinese Herbal
  • Glucosides
  • Plant Preparations
  • Stilbenes
  • 2,3,5,4'-tetrahydroxystilbene 2-O-glucopyranoside