The antithrombotic and antiplatelet effects of two fucoidan fractions with low molecular weight and different sulfate content from Laminaria japonica were compared in order to examine the influence of chemical charact...The antithrombotic and antiplatelet effects of two fucoidan fractions with low molecular weight and different sulfate content from Laminaria japonica were compared in order to examine the influence of chemical character on their antithrombotic activity and the possible mechanism. Both LMW fucoidan fractions exhibited favorable antithrombotic activity in an Fecl3-induced arterial thrombosis. The antithrombotic activity of LMW fucoidan was related with decrease of TXB2 and whole blood viscosity and hematocrit. LMW fucoidan showed a correlation between anticoagulant, antiaggregant and antithrombotic effects in vivo. For LMW fucoidan, antithrombotic activity required high dose of 5-10 nmol kg-1, concomitantly with increase in anticoagulant activity and inhibition of platelet aggregation. Administration of LMW fucoidan significantly promoted the 6-keto-PGF1α content and decreased the TXB2 content, indicating its inhibition of tissue factor pathway and regulation of metabolism of arachidonic acid. By comparison, highly sulfated fucoidan LF2 with Mw 3900 seemed to be a more suitable choice for antithrombotic drug for its antithrombotic activity accompanied with specific inhibitory activity on platelet aggregation, low anticoagulant activity and low hemorrhagic risk in vivo.展开更多
After entering 2010, as main varieties patents of the global non-peptide angiotensin II receptor antagonists （ARB） expire, strong growth of anti-hypertensive drug market will tend to slow down. In drugs acting on th...After entering 2010, as main varieties patents of the global non-peptide angiotensin II receptor antagonists （ARB） expire, strong growth of anti-hypertensive drug market will tend to slow down. In drugs acting on the cardiovascular and blood system, antithrombotie drugs will become a new attraction on the market. Antithrombotic drugs are primarily formed by the anti-platelet aggregation, coagulation system activation of plasminogen thrombolytic drugs and the like. Antiplatelet drugs have both prevention and treatment effect, are the main category of antithrombotic drugs. According to IMS Health data, in 2008, sale of anti-thrombosis drug in global market is 180 million U.S. dollars, an increase of 16 %, while in 2009 the growth rate is only 7.95%, reaching $ 19.5 billion, growth rate of antithrombotic drugs is 7.13% in the world＇ s major pharmaceutical market.展开更多
基金supported in part by the Notional Natural Science Foundation of China (No.30800858)the Shandong Natural Science Foundation (No.ZR2010 CQ020)
文摘The antithrombotic and antiplatelet effects of two fucoidan fractions with low molecular weight and different sulfate content from Laminaria japonica were compared in order to examine the influence of chemical character on their antithrombotic activity and the possible mechanism. Both LMW fucoidan fractions exhibited favorable antithrombotic activity in an Fecl3-induced arterial thrombosis. The antithrombotic activity of LMW fucoidan was related with decrease of TXB2 and whole blood viscosity and hematocrit. LMW fucoidan showed a correlation between anticoagulant, antiaggregant and antithrombotic effects in vivo. For LMW fucoidan, antithrombotic activity required high dose of 5-10 nmol kg-1, concomitantly with increase in anticoagulant activity and inhibition of platelet aggregation. Administration of LMW fucoidan significantly promoted the 6-keto-PGF1α content and decreased the TXB2 content, indicating its inhibition of tissue factor pathway and regulation of metabolism of arachidonic acid. By comparison, highly sulfated fucoidan LF2 with Mw 3900 seemed to be a more suitable choice for antithrombotic drug for its antithrombotic activity accompanied with specific inhibitory activity on platelet aggregation, low anticoagulant activity and low hemorrhagic risk in vivo.
文摘After entering 2010, as main varieties patents of the global non-peptide angiotensin II receptor antagonists （ARB） expire, strong growth of anti-hypertensive drug market will tend to slow down. In drugs acting on the cardiovascular and blood system, antithrombotie drugs will become a new attraction on the market. Antithrombotic drugs are primarily formed by the anti-platelet aggregation, coagulation system activation of plasminogen thrombolytic drugs and the like. Antiplatelet drugs have both prevention and treatment effect, are the main category of antithrombotic drugs. According to IMS Health data, in 2008, sale of anti-thrombosis drug in global market is 180 million U.S. dollars, an increase of 16 %, while in 2009 the growth rate is only 7.95%, reaching $ 19.5 billion, growth rate of antithrombotic drugs is 7.13% in the world＇ s major pharmaceutical market.
