• Title/Summary/Keyword: Antithrombotic agent

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NQ304, A NOVEL ANTITHROMBOTIC AGENT, INHIBITS THE PROLIFERATION OF VASCULAR SMOOTH MUSCLE CELLS

  • Kim, Jin-Ho;Kim, Tack-Joong;Ryu, Chung-Kyu;Hong, Jin-Tae;Yun, Yeo-Pyo
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2002.05a
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    • pp.119-119
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    • 2002
  • Several 1,4-naphthoquinone derivatives have been reported to possess many pharmacological effects such as anti-viral, anti-fungal, anti-cancer and anti-platelet activities. However, little has been known about functional role in vascular smooth muscle cells (VSMCs).(omitted)

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Antithrombotic Therapy for Ischemic Stroke (허혈성 뇌졸중에서의 항혈전 치료)

  • Hah, Jung-Sang;Lee, Jun
    • Journal of Yeungnam Medical Science
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    • v.20 no.1
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    • pp.1-12
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    • 2003
  • Ischemic stroke is among the principal causes of death and disability in the elderly. Although control of blood pressure, decreased cigarette smoking, and modified dietary habits are among important reasons for stroke decline, the use of antithrombotic therapy, rigorously prescribed. Several antiplatelet agents are approved to reduce the risk of recurrent stroke. Aspirin is the best-studied and most widely used antiplatelet agent for stroke prevention; it provides approximately 15% to 25% relatively risk reduction for secondary prevention of stroke or the major vascular death. Combining 2 antiplatelet agents with different mechanism of action was demonstrated to provide a substantial increase in efficacy in several studies. Anticoagulation should be considered first with potential cardiac sources of embolism. Heparin reduces development of erythrocyte-fibrin thrombi that form in regions of vascular stasis especially within the heart, in severely stenosed arteries sometimes engrafted on white thrombi, in acute arterial occlusion. Heparin should not be indiscriminately given to all acute brain ischemia patients, but may contribute to treatment of large artery occlusion and severe stenosis, cardiogenic embolism with a high acute recurrence risk, and dural sinus and cerebral venous thromobosis.

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The Changes of Body Fat Accumulation, Serum Lipids and Platelet Functions in Rat Fed the Diet Containing Different Common Oils in Korea: Sesame oil, Perilla oil, Rice Bran oil and Mixed oil (급원이 다른 식이 지방이 흰쥐의 지방대사와 혈소판 성상에 미치는 영향 -참깨유, 들깨유, 미강유 중심으로-)

  • 김숙희
    • Journal of Nutrition and Health
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    • v.26 no.5
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    • pp.513-523
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    • 1993
  • In this experiment, we investigated the hypolipidemic and antithrombotic effects of rats fed diets with different common oils in Korea for different feeding periods(4 weeks or 12 weeks), using Korean sesame oil, perilla oil, rice bran oil and mixed oil. W-3/w-6 ratio of each group was 0.001, 1.44, 0.03 and 0.112, respectively. P/S ratio of each group was 9.64, 10.49, 5.58 and 1.68, respectively. The result were as follows: 1) According to the age, body fat accumulation was increased. 2) Perilla oil(w-3 rich) decreased total lipid, triglyceride and total cholesterol, and increased HDL/total cholesterol ratio. 3) With regard to the compositono of platelet fatty acids, Perilla oil increased w-3/w-6 ratio of the platelet. Perilla oil lengthened bleeding time and decreased MDA(MalonDAdehyde) formation which determined in place of Thromboxane A2(TXA2) in platelet. This result can suggest that linoleic acid of perrilla oil seem to supress the conversion of linoleic acid to arachidonic acid(AA 20:4, w-6) and eicosapentaenoic acid(EPA, 20:5, w-3) trannnsformed from linolenic acid to suppress the conversion of arachidonic acid to TXA2. Since TXA2 is platelet-aggregating and vasoconstricting agent, the reduction of TXA2 tgeneration by platelet with increased linolenic acid intakes shows prologed bleeding time. In conclusion, w-3 rich perilla oil has strong hypolipidemic and antithrombotic effects by changing fatty acid profiles of the platelet.

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An antithrombotic agent, NQ301, inhibits thromboxane $A_2$ synthase activity and blocks thromboxane $A_2$ receptor in rabbit platelets

  • Jin, Yong-Ri;Ryu, Chung-Kiu;Cho, Mi-Ra;Shin, Hwa-Sup;Yoo, Hwan-Soo;Yun, Yeo-Pyo
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.110.3-111
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    • 2003
  • In the previous studies, we have reported that NQ30l, a synthetic l,4-naphthoquinone derivative, displayed a potent antithrombotic activity, and that this might be due to antiplatelet effect, which was mediated by inhibition of cytosolic $Ca^{2+}$ mobilization in activated platelets. In the present study, the effect of NQ301 on arachidonic acid cascade in activated platlets was examined. NQ301 concentration-dependently inhibited washed rabbit platelet aggregation induced by collagen (10 $\mu$g/ml), arachidonic acid (100 $\mu$M) and U46619 (1 $\mu$M), a thromboxane $A_2$receptor agonist, with $IC_50$ values of 0.60$\pm$0.02, 0.79$\pm$0.04 and 0.58$\pm$0.04 $\mu$M, respectively. (omitted)

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Antiplatelet and Antithrombotic Activities of Lindera obtusiloba Extract in vitro and in vivo

  • Lee, Jung-Ok;Kim, Chul-Young;Lee, Seung-Woo;Oak, Min-Ho
    • Biomolecules & Therapeutics
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    • v.18 no.2
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    • pp.205-210
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    • 2010
  • Several studies have shown that plant-derived polyphenols reduce cardiovascular accidents in high-risk patients and the inhibition of platelet function may be responsible for part of this benefit. Lindera obtusiloba is widely used in traditional herbal medicine for the treatment of cardiovascular and inflammatory diseases. Therefore, the antiplatelet and antithrombotic activities of Lindera obtusiloba Extracts (LOE) on in vitro platelet aggregation, radical scavenging activity and in vivo murine pulmonary thrombosis were examined. LOE was able to directly scavenge the stable DPPH radical in a concentration-dependent manner and its $IC_{50}$ value was 3.9 ${\pm}$ 0.1 ${\mu}g$/ml. LOE significantly inhibited collagen- and ADP-induced platelet aggregation in a concentration-dependent manner and its $IC_{50}$ value is 0.9 ${\pm}$ 0.1 mg/ml and 0.4 ${\pm}$ 0.1 mg/ml respectively. The inhibitory effect of LOE was comparable to aspirin ($IC_{50}$ values were 1.0 ${\pm}$ 0.5 and 1.0 ${\pm}$ 0.7 mg/ml, respectively). Furthermore, oral administration of LOE suppressed the death of mice with pulmonary thrombosis induced by intravenous injection of collagen plus epinephrine. Taken together, our results suggest LOE may be a promising candidate for antithrombotic agent, and the antithrombotic effect of LOE may be due to, at least in part, antiplatelet activity.

Effect of the Geijibokryunghwan Water Extracts on Stimulus-induced Superoxide Generation and Tyrosyl Phosphorylation in Human Neutrophils

  • Choi, Meung-Hee;Park, Won-Han
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.20 no.2
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    • pp.477-481
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    • 2006
  • A clinical report indicates that 'Geijibokryunghwan(GBH) is very effective in treating thrombosis in those patients who have difficulties with more conventional antithrombotic drugs. The isolation and identification of various compounds from this plant and the same genus have been reported by several groups. However, the pharmaceutical effect of the GBH on superoxide generation in human neutrophils has not been studied. In the present report, we investigated the possibility of using herbal medicine as an alternative therapy. In particular, we studied tremor in antiatheroscleosis. In this report, we shows the GBH extract can be used as a potential atherosclerosis preventive agent in human. The effect of GBH on stimulus-induced superoxide generation and phosphorylation of tyrosine residues of protein in human neutrophils was investigated. In a conclusion, GBH suppressed tyrosine phosphorylase in a dose-dependent manner, and may have pharmacoceutical applications. These data suggest that GBH extracts merits investigation as a potential anti-atherosclerogenic agent in humans.

Evidence for Existence of a Water-Extractable Anticoagulant in an Earthworm, Lumbricus rubellus

  • Woo, Jeong-Im;Bahk, Yun-Kyung;Yu, Kyoung-Hee;Paik, Seung-R.;Chang, Chung-Soon
    • BMB Reports
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    • v.29 no.6
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    • pp.500-506
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    • 1996
  • We have isolated a water-extracted novel regulator for blood coagulation from an earthworm, Lumbricus rubellus. As a folk remedy, the earthworm has been known to facilitate blood circulation. After complete heat inactivation of endogenous proteases in the earthworm, an anticoagulant(s) was purified through ammonium sulfate fractionation and three consecutive gel permeation chromatography of Sephacryl S-300, Sephadex G-75, and G-150 by measuring activated partial thromboplastin time (APTT) The anticoagulant was further purified to 2,800 fold with a C4 reversed-phase HPLC This activity was stable under heat ($100^{\circ}C$ for 30 min) and acidic conditions (0.4 N HCl). The effects of this partially purified anticoagulant on thrombin were observed with various substrates such as N${\alpha}$-benzoyl-DL-arginine-p-nitroanilide (BApNA), H-D-phenylalanyl-L-pipecoyl-L-arginine-p-nitroanilide (S-2238), N${\alpha}$-p-tosyl-L-arginine methyl ester (TAME), and fibrinogen as a natural substrate. Only TAME hydrolysis, due to an esterase activity of the enzyme, was inhibited among the chromogenic substrates. In addition, the anticoagulant not only inhibited the conversion of fibrinogen to fibrin but also prolonged the fibrin clot formation monitored with the in vitro coagulation test. Based on these observations, we suggest the significance of measuring the ability of antithrombotic drugs to inhibit the esterase activity of thrombin. In this report, it was also shown that the earthworm indeed contained a water-extractable, heat- and acid-stable anticoagulant which could be used as a novel antithrombotic agent.

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A Case Report of dcrease of hypodense region on CT images in ischemic cerebrovascular disease patient treated with Antiplatelet agent and Cheonghyulgangki-tang (항혈소판제제와 청혈강기탕(淸血降氣湯)을 병용 투여하여 CT영상에서 저음영부위의 감소를 보인 허혈성 뇌혈관질환 환자의 증례 보고)

  • Shin, Woo-Jae;Cha, Ji-Hye;Kim, Tae-Yeon;Park, Yu-Jin;Ko, Heung;Kim, Gi-Tae;Sin, Sun-Mi
    • The Journal of Internal Korean Medicine
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    • v.31 no.2
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    • pp.380-387
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    • 2010
  • The ischemic penumbra represents part of the hypoperfused region associated with focal brain ischemia. A practical approach is to define this region as that portion of the ischemic territory that can potentially be salvaged by timely intervention. For the prevention and treatment of ischemic stroke, antithrombotic therapy is prescribed. But medication of antiplatelet agent is only validated as prevention effect. Cheonghyulgangki-tang has been used for cerebral apoplexy, hypertension, etc. In this case report, an acute ischemic stroke patient was treated with an antiplatelet agent named Plavix and Cheonghyulgangki-tang and remarkable reduction of ischemic portion in the brain CT was observed. The result of this case suggests that oriental medical therapy could be a safe and effective intervention in acute ischemic stroke.