Anti-platelet effects of bioactive compounds isolated from the bark of Rhus verniciflua Stokes.

Quality Control of Herbal Medicine Department, Korea Institute of Oriental Medicine, Daejeon 461-24, South Korea.
Journal of Ethnopharmacology (Impact Factor: 2.94). 07/2006; 106(1):62-9. DOI: 10.1016/j.jep.2005.12.015
Source: PubMed

ABSTRACT It has previously been shown that EtOAc extracts of Rhus verniciflua Stokes (RVS) inhibit the platelet aggregation response. In this report, bioassay-guided fractionation using ADP-, arachidonic acid-, and collagen-induced human platelet aggregation by a whole blood aggregometer yielded the bioactive compounds isomaltol and pentagalloyl glucose from different highly effective fractions. In addition, column chromatography of fractions from RVS yielded another five compounds: butin, fisetin, sulfuretin, butein and 3,4',7,8-tetrahydroxyflavone. We investigated the effects of bioactive compounds from RVS fractions on several markers of platelet activation using receptor expression on platelet membranes, including glycoprotein IIb/IIIa (CD41), GPIIb/IIIa-like expression (PAC-1) and P-selectin (CD62), and intracelluar calcium mobilization responses by flow cytometry in healthy subjects. Dose-dependent inhibition of platelet aggregation and significantly decreased platelet activation were observed for the isomaltol- and pentagalloyl glucose-treated platelets, respectively. These results show that isomaltol and pentagalloyl glucose from the bark of Rhus verniciflua Stokes have potent anti-platelet activity and emphasize the need to further examine the mechanism of these active compounds for platelet modulation.

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    ABSTRACT: Abstract Rhus verniciflua stokes (RVS) is known to promote blood circulation by preventing blood stasis, although the active ingredients and the underlying mechanism are unclear. Platelets are the primary cells that regulate circulation and contribute to the development of diverse cardiovascular diseases by aggregation and thrombosis. The study assessed the antiplatelet activity of RVS and sought to identify the active constituents. Pretreatment of washed platelets with RVS heartwood extract blunted the aggregatory response of platelets to collagen. In the subfractions, fisetin, butein, and sulfuretin were identified as effective inhibitors of platelet aggregation by collagen, thrombin, and adenosine-5'-diphosphate. Antiplatelet activities of all three compounds were concentration dependent, and fisetin had longer in vitro duration of action compared with butein or sulfuretin. Extracellular signal-regulated kinase (ERK) mitogen-activated protein kinase activation by collagen was prevented by fisetin, whereas butein and sulfuretin failed to inhibit ERK and p38 activation was not affected by any of the compounds. Rats orally administered 100 mg/(kg·day(-1)) fisetin for 7 days were resistant to arterial thrombosis, although total extract of RVS heartwood exhibited little effect at a dose of 1000 mg/(kg·day(-1)). RVS heartwood may have cardiovascular protective activity by inhibiting platelet aggregation. The active constituents are fisetin, butein, and sulfuretin, and fisetin is orally effective against thrombosis.
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    ABSTRACT: Rhus verniciflua Stokes has been used as a traditional herbal medicine, a food additive, and a material for lacquer in Korea. In this study, hot water extracts of R. verniciflua Stokes xylem (RVE) and purified compounds were examined for estrogenic activity. RVE showed estrogenic activity mediated by estrogen receptors (ER) with a higher binding affinity and activity to ER beta than to ER alpha in ER alpha- or ER beta-transfected cells. It also exhibited estrogenic activity in a uterotrophic assay using rats. All of RVE compounds had high affinity to ER beta compared with ER alpha in reporter gene assay and ER binding assay. Among seven RVE compounds, butin, butein, sulfuretin, and garbanzol had a strong estrogenic activity in ERE-mediated reporter gene assay. Butein and sulfuretin had stronger ER beta binding affinity compared with others. Collectively, these results demonstrate an estrogenic activity of RVE and suggest its potential value for postmenopausal women.
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