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박은경,추민경,Hae-KyungYoon,김동현 대한약학회 2002 Archives of Pharmacal Research Vol.25 No.4
To evaluate the antithrombotic and antiallergic properties of rhaponticin extracted from RheiRhizoma, the in vitro and ex vivo inhibitory activities of rhaponticin and its metabolite, rhapontigenin,were measured. These compounds inhibited in vitro ADP- and collagen-induced plateletaggregation. Rhapontigenin was more potent, with IC50 values of 4 and 70 mg/ml,respectively. In ex vivo ADP- and collagen-induced rat platelet aggregation, these compoundsalso exhibited a potent inhibitory effect. The antiplatelet aggregation effects of rhaponticin andrhapontigenin were more potent than those of aspirin. Rhapontigenin showed significant protectionfrom death due to pulmonary thrombosis in mice. Rhapontigenin also showed thestrongest inhibitory activity against b-hexosaminidase release induced by DNP-BSA. Thesecompounds inhibited PCA reaction in mice. Rhapontigenin intraperitoneally administeredshowed the strongest inhibitory activity and significantly inhibited PCA at doses of 25 and 50mg/kg, with inhibitory activities of 48 and 85%, respectively. The inhibitory activity of orallyadministered rhaponticin was stronger than that of intraperitoneally administered rhaponticin. These results suggest that rhaponticin, in the rhizome of Rhei Rhizoma, is a prodrug that hasextensive antiallergic and antithrombotic properties.