Chrysophanol-8-O-glucoside, an anthraquinone derivative in rhubarb, has antiplatelet and anticoagulant activities.
Rhubarb is a widely used traditional medicine and has been reported to elicit a number of biological effects including anti-inflammatory and antiplatelet effects. In the present study, we investigated the effects of anthraquinone derivatives isolated from rhubarb on platelet activity. Of four anthraquinone derivatives isolated from rhubarb examined, chrysophanol-8-O-glucoside (CP-8-O-glc) was found to have the most potent inhibitory effect on collagen- and thrombin-induced platelet aggregation. CP-8-O-glc-treated mice showed significantly prolonged bleeding times. Furthermore, CP-8-O-glc was found to have a significant inhibitory effect on rat platelet aggregation ex vivo and on thromboxane A(2) formation in vitro. In coagulation tests, CP-8-O-glc did not alter prothrombin time, and it prolonged the activated partial thromboplastin time. However, CP-8-O-glc only inhibited platelet phosphatidylserine exposure, but not exert direct inhibition on intrinsic factors. This study demonstrates the antiplatelet and anticoagulant effects of CP-8-O-glc and suggests that this compound might be of therapeutic benefit for the prevention of platelet-related cardiovascular diseases.
Department of Physiology, Ajou University School of Medicine, Republic of Korea.
Eun Ji
EJ
Seo
Tran Minh
TM
Ngoc
Sun-Mee
SM
Lee
Yeong Shik
YS
Kim
Yi-Sook
YS
Jung
D000818:Animals; D000880:Anthraquinones / Q000302:isolation & purification / Q000494:pharmacology*; D000925:Anticoagulants / Q000302:isolation & purification / Q000494:pharmacology*; D001777:Blood Coagulation / Q000187:drug effects; D003094:Collagen / Q000494:pharmacology; D005960:Glucosides / Q000302:isolation & purification / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D010314:Partial Thromboplastin Time; D010975:Platelet Aggregation Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D011517:Prothrombin Time; D051381:Rats; D017207:Rats, Sprague-Dawley; D012250:Rheum / Q000737:chemistry*; D013917:Thrombin / Q000494:pharmacology; D013928:Thromboxane A2 / Q000378:metabolism
D000880:Anthraquinones; D000925:Anticoagulants; D005960:Glucosides; D010975:Platelet Aggregation Inhibitors; D013928:Thromboxane A2; C523695:chrysophanol 8-O-glucoside; D003094:Collagen; D013917:Thrombin