title: Anti-platelet effects of bioactive compounds isolated from the bark of Rhus verniciflua Stokes.
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.
authors.affiliation: Quality Control of Herbal Medicine Department, Korea Institute of Oriental Medicine, Daejeon 461-24, South Korea.
authors.forename: Won Kyung
authors.initials: WK
authors.lastname: Jeon
authors.forename: Ju Hyun
authors.initials: JH
authors.lastname: Lee
authors.forename: Ho Kyoung
authors.initials: HK
authors.lastname: Kim
authors.forename: A Yeong
authors.initials: AY
authors.lastname: Lee
authors.forename: Sung Ok
authors.initials: SO
authors.lastname: Lee
authors.forename: Young Sup
authors.initials: YS
authors.lastname: Kim
authors.forename: Shi Yong
authors.initials: SY
authors.lastname: Ryu
authors.forename: Soo Young
authors.initials: SY
authors.lastname: Kim
authors.forename: Yong Jin
authors.initials: YJ
authors.lastname: Lee
authors.forename: Byoung Seob
authors.initials: BS
authors.lastname: Ko
mesh_terms: D000244:Adenosine Diphosphate / Q000494:pharmacology; D000328:Adult; D000818:Animals; D016718:Arachidonic Acid / Q000494:pharmacology; D001792:Blood Platelets / Q000737:chemistry / Q000187:drug effects*; D002118:Calcium / Q000378:metabolism; D003094:Collagen / Q000494:pharmacology; D005260:Female; D005434:Flow Cytometry; D006801:Humans; D047348:Hydrolyzable Tannins / Q000378:metabolism; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D019007:P-Selectin / Q000737:chemistry / Q000378:metabolism; D024301:Plant Bark / Q000737:chemistry*; D015539:Platelet Activation; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000627:therapeutic use*; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000037:antagonists & inhibitors / Q000378:metabolism; D010980:Platelet Membrane Glycoproteins; D011655:Pulmonary Embolism / Q000188:drug therapy*; D029045:Rhus
chemical_list: D047348:Hydrolyzable Tannins; D019007:P-Selectin; D010975:Platelet Aggregation Inhibitors; D019039:Platelet Glycoprotein GPIIb-IIIa Complex; D010980:Platelet Membrane Glycoproteins; D016718:Arachidonic Acid; C435084:pentagalloylglucose; D000244:Adenosine Diphosphate; D003094:Collagen; D002118:Calcium