Anti-platelet effects of bioactive compounds isolated from the bark of Rhus verniciflua Stokes.
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.
Jeon
Won Kyung
WK
Quality Control of Herbal Medicine Department, Korea Institute of Oriental Medicine, Daejeon 461-24, South Korea.
Lee
Ju Hyun
JH
Kim
Ho Kyoung
HK
Lee
A Yeong
AY
Lee
Sung Ok
SO
Kim
Young Sup
YS
Ryu
Shi Yong
SY
Kim
Soo Young
SY
Lee
Yong Jin
YJ
Ko
Byoung Seob
BS
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
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