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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

Lv, Guiyuan, Lou, Zhaohuan, Chen, Suhong, Gu, Hui, Shan, Letian
Journal of ethnopharmacology 2011 v.137 no.1 pp. 449-456
in vivo studies, traditional medicine, anti-inflammatory activity, liver, brain, health promotion, tissue distribution, body fluids, blood-brain barrier, reversed-phase high performance liquid chromatography, lungs, rats, testes, oral administration, pharmacokinetics, herbal medicines, Reynoutria multiflora
ETHNOPHARMACOLOGICAL RELEVANCE: 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. MATERIALS AND 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 r²>0.99) over the range of 0.27–185.00μg/ml. The intra- and inter-day variations were less than 3% at concentration range of 8.7–131.2μg/ml and good overall recoveries (97.7–101.5%) were obtained at the same range. The maximum concentration (Cₘₐₓ) and the time to reach this concentration (Tₘₐₓ) of PM-SG were 31.9μg/ml and 40.0min, 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±20.8μg/g and 86.8±9.0μg/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.