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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.
J Ethnopharmacol. 2011 Sep 01; 137(1):449-56.JE

Abstract

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 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.

Links

Publisher Full Text

Authors+Show Affiliations

Lv G
Institute of Materia Medica, Zhejiang Chinese Medical University, Hangzhou 310053, China.
Lou Z
No affiliation info available
Chen S
No affiliation info available
Gu H
No affiliation info available
Shan L
No affiliation info available

MeSH

Administration, OralAnimalsCalibrationChromatography, High Pressure LiquidChromatography, Reverse-PhaseDrugs, Chinese HerbalGlucosidesLiquid-Liquid ExtractionMaleMedicine, Chinese TraditionalModels, BiologicalPlant RootsPolygonaceaeRatsRats, Sprague-DawleyReference StandardsReproducibility of ResultsSpectrophotometry, UltravioletStilbenesTissue Distribution

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

21679759

Citation

Lv, Guiyuan, et al. "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." Journal of Ethnopharmacology, vol. 137, no. 1, 2011, pp. 449-56.
Lv G, Lou Z, Chen S, et al. 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. J Ethnopharmacol. 2011;137(1):449-56.
Lv, G., Lou, Z., Chen, S., Gu, H., & Shan, L. (2011). 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. Journal of Ethnopharmacology, 137(1), 449-56. https://doi.org/10.1016/j.jep.2011.05.049
Lv G, et al. 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. J Ethnopharmacol. 2011 Sep 1;137(1):449-56. PubMed PMID: 21679759.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 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. AU - Lv,Guiyuan, AU - Lou,Zhaohuan, AU - Chen,Suhong, AU - Gu,Hui, AU - Shan,Letian, Y1 - 2011/06/06/ PY - 2011/03/05/received PY - 2011/05/16/revised PY - 2011/05/28/accepted PY - 2011/6/18/entrez PY - 2011/6/18/pubmed PY - 2011/12/28/medline SP - 449 EP - 56 JF - Journal of ethnopharmacology JO - J Ethnopharmacol VL - 137 IS - 1 N2 - 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 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. SN - 1872-7573 UR - https://www.unboundmedicine.com/medline/citation/21679759/Pharmacokinetics_and_tissue_distribution_of_2354'_tetrahydroxystilbene_2_O_β_D_glucoside_from_traditional_Chinese_medicine_Polygonum_multiflorum_following_oral_administration_to_rats_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-8741(11)00414-4 DB - PRIME DP - Unbound Medicine ER -