title: Pharmacokinetics and tissue distribution of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside from traditional Chinese medicine Polygonum multiflorum following oral administration to rats.
abstract: BACKGROUND
  Polygonum multiflorum is an important traditional Chinese medicine used for health promotion and disease treatment. One major bioactive compound in P. multiflorum is a stilbene glycoside (2,3,5,4'-tetrahydroxystilbene-2-O-β-d-glucoside, PM-SG), which possesses antioxidative, anti-inflammatory and endothelial-protective activities.
  
  
  METHODS
  The purpose of the present study was to investigate in vivo pharmacokinetics and tissue distribution of PM-SG after oral administration of Polygonum multiflorum extract to rats by using a reversed-phase high-performance liquid chromatography coupled with liquid-liquid phase extraction. The pharmacokinetic parameters were determined using both compartmental and non-compartmental analyses.
  
  
  RESULTS
  All calibration curves for PM-SG in rat plasma and tissues were linear (all r(2)>0.99) over the range of 0.27-185.00 μg/ml. The intra- and inter-day variations were less than 3% at concentration range of 8.7-131.2 μg/ml and good overall recoveries (97.7-101.5%) were obtained at the same range. The maximum concentration (C(max)) and the time to reach this concentration (T(max)) of PM-SG were 31.9 μg/ml and 40.0 min, respectively. The pharmacokinetic profiles estimated by fitting two-compartment and non-compartment models revealed that PM-SG was rapidly absorbed into the body fluids and widely distributed throughout the body, with great efficiency of utility, followed by quick elimination. The highest PM-SG levels were detected in liver and lungs (90.3 ± 20.8 μg/g and 86.8 ± 9.0 μg/g, respectively) whereas little in brain and testes, indicating PM-SG can hardly penetrate the blood-brain and blood-testicle barriers.
  
  
  CONCLUSIONS
  This was the first report on the favorable pharmacokinetic profiles of PM-SG in rat plasma and tissues after oral administration. It may provide a meaningful basis for clinical application of such a bioactive compound of herbal medicines.
authors.affiliation: Institute of Materia Medica, Zhejiang Chinese Medical University, Hangzhou 310053, China.
authors.forename: Guiyuan
authors.initials: G
authors.lastname: Lv
authors.forename: Zhaohuan
authors.initials: Z
authors.lastname: Lou
authors.forename: Suhong
authors.initials: S
authors.lastname: Chen
authors.forename: Hui
authors.initials: H
authors.lastname: Gu
authors.forename: Letian
authors.initials: L
authors.lastname: Shan
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002138:Calibration; D002851:Chromatography, High Pressure Liquid / Q000592:standards; D056148:Chromatography, Reverse-Phase / Q000592:standards; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage* / Q000302:isolation & purification / Q000493:pharmacokinetics*; D005960:Glucosides / Q000008:administration & dosage* / Q000097:blood / Q000302:isolation & purification / Q000493:pharmacokinetics*; D059625:Liquid-Liquid Extraction / Q000592:standards; D008297:Male; D008516:Medicine, Chinese Traditional; D008954:Models, Biological; D018517:Plant Roots; D019664:Polygonaceae / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012015:Reference Standards; D015203:Reproducibility of Results; D013056:Spectrophotometry, Ultraviolet / Q000592:standards; D013267:Stilbenes / Q000008:administration & dosage* / Q000097:blood / Q000302:isolation & purification / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: C489707:2',3',4',5'-tetrahydroxystilbene-2-O-beta-D-glucoside; D004365:Drugs, Chinese Herbal; D005960:Glucosides; D013267:Stilbenes