• Applied Biological Chemistry
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• 제41권8호
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• pp.613-615
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• 1998

Antithrombotic function of doenjang was investigated using thoroughly desalted aqueous extract. In the presence of the extract, thrombin suffered loss of its fibrin-clotting activity, whose extent increased in a dose-dependent manner. The active substance involved in thrombin inhibition showed a high thermal stability. Results of Sephadex G-25 permeation chromatography indicated that there were at least two soluble thrombin inhibitors in doenjang with different molecular sizes.

• Bulletin of the Korean Chemical Society
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• 제33권9호
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• pp.3048-3054
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• 2012

The use of aspirin is widely recommended for the prevention of heart attacks owing to its ability to inhibit platelet activation by irreversibly blocking cyclooxygenase 1. However, aspirin also affects the fibrinolytic and hemostatic pathways by mechanisms that are not well understood, causing severe hemorrhagic complications. Here, we investigated the ability of aspirin and aspirin metabolites to inhibit thrombin-activatable fibrinolysis inhibitor (TAFI), the major inhibitor of plasma fibrinolysis. TAFI is activated via proteolytic cleavage by the thrombin-thrombomodulin complex to TAFIa, a carboxypeptidase B-like enzyme. TAFIa modulates fibrinolysis by removing the C-terminal arginine and lysine residues from partially degraded fibrin, which in turn inhibits the binding of plasminogen to fibrin clots. Aspirin and its major metabolites, salicylic acid, gentisic acid, and salicyluric acid, inhibit TAFIa carboxypeptidase activity. Salicyluric acid effectively blocks activation of TAFI by thrombin-thrombomodulin; however, salicylates do not inhibit carboxypeptidase N or pancreatic carboxypeptidase B. Aspirin and other salicylates accelerated the dissolution of fibrin clots and reduced thrombus formation in an in vitro model of fibrinolysis. Inhibition of TAFI represents a novel hemostatic mechanism that contributes to aspirin's therapy-associated antithrombotic activity and hemorrhagic complications.

• 한국식품영양학회지
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• 제20권2호
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• pp.114-119
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• 2007

Our research objective was to examine the in vitro biological activity of deer antler(Nogyong in Korean) extract, including the antioxidative, nitrite scavenging, and tyrosinase inhibitory effects, as well as the antithrombotic, and angiotensin I converting enzyme(ACE) inhibitory activities. The carbohydrate, protein, fat, and mineral contents of the deer antler were 7.6%, 65.3%, 3.2% and 23.9%, respectively. The electron donating ability(EDA) by the reduction of 2,2'-diphenyl-1-picrylhydrazyl(DPPH) was 67.1%, and the inhibition rate of lipid peroxidation by the thiocyanate method using linoleic acid was 92.1% in 100 mg/ml of extract. The nitrite scavenging effects were pH dependent, and were highest at pH 1.2 and lowest at pH 6.0. The sample inhibition rate against tyrosinase was above 64.0%. The platelet aggregation induced by ADP(adenosine-5'diphosphate) was inhibited up to 51.7%, and the inhibitory effect was dependent on the sample concentration. Lastly, the inhibition rate of ACE was 47.5% in 100 mg/ml of deer antler extract.

• Bulletin of the Korean Chemical Society
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• 제34권4호
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• pp.1212-1220
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• 2013

The human coagulation factor XI (FXI) is a serine protease that plays a significant role in blocking of the blood coagulation cascade as an attractive antithrombotic target. Selective inhibition of FXIa (an activated form of factor XI) disrupts the intrinsic coagulation pathway without affecting the extrinsic pathway or other coagulation factors such as FXa, FIIa, FVIIa. Furthermore, targeting the FXIa might significantly reduce the bleeding side effects and improve the safety index. This paper reports on a docking-based three dimensional quantitative structure activity relationship (3D-QSAR) study of the potent FXIa inhibitors, the chloro-phenyl tetrazole scaffold series, using comparative molecular field analysis (CoMFA) and comparative molecular similarity analysis (CoMSIA) methods. Due to the characterization of FXIa binding site, we classified the alignment of the known FXIa inhibitors into two groups according to the docked pose: S1-S2-S4 and S1-S1'-S2'. Consequently, highly predictive 3D-QSAR models of our result will provide insight for designing new potent FXIa inhibitors.

• Archives of Pharmacal Research
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• 제14권4호
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• pp.352-356
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• 1991

The anti-platelet activity of ilexoside D isolated from the roots of Ilex pubescens Hook. et Arn. was investigated in in vitro and ex vivo models of platelet aggregation induced by ADP, thrombin or collagen in rats. In vitro ilexoside D inhibited more effectively platelet aggregation induced by ADP and thrombin than by collagen as compared with aspirin. Ex vivo ilexoside D also inhibited platelet aggregation induced by ADP and collagen, but not by thrombin, and the inhibitory action of ilexoside D was more effective than that of aspirin. However, in vitro ilexoside D inhibited very poorly the generation of malonyldialdehyde, which is known to be concomitantly released with thromboxane $A_2$ during platelet aggregation. These results suggest that the anti-platelet activity of ilexoside D may not be responsible for prostaglandin synthesis in platelets.

• Journal of Ginseng Research
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• 제47권3호
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• pp.353-358
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• 2023

Sepsis and septic shock affect millions of people worldwide each year with high clinical mortality rates. At present, basic research on sepsis has emerged in an endless stream, but there are few effective clinical translation results. Ginseng, a medicinal and edible representative of Araliaceae plants, contains a variety of biologically active compounds including ginsenosides, alkaloids, glycosides, polysaccharides, and polypeptides. Neuromodulation, anticancer activity, blood lipid regulation, and antithrombotic activity have been linked to ginseng treatment. At present, basic and clinical research have suggested various applications of ginseng in sepsis. In view of the different effects of various ginseng components on the pathogenesis of sepsis, and in order to further understand and develop the possible value of ginseng in sepsis, this manuscript reviews the application of various components of ginseng in the treatment of sepsis in recent years.

• 생명과학회지
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• 제16권2호
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• pp.360-364
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• 2006

Fibrin clots of blood vessels are one of the serious factor caused cardiovascular disease. The development of a antithrombotic and thrombolysis solvent is necessary to prevent and treat these diseases. It has been reported that a strong fibrin-specific fibrinolytic enzyme was produced from a Korean fermented soybean paste similar to Japanese miso. We have been screened the known or novel fibrinolytic enzymes by activity-based and sequence-based screening from soil DNA metagenome library containing all kinds of environmental genomic DNA. The activity-based screening was determined the protease activity on 0.5% skim milk. For sequence-based screening, we designed a set of primer expanding gene sequence of fibrinolytic enzyme, performed PCR and selected clones showing the expected size of amplicons from metagenome library. Transformation of the gene encoding fibrinolytic enzyme was carried out with commercial vectors and their transformants were selected. Finally, we found 15 positive clones from metagenome library. Then each of sequences were analyzed and identified as similar or known the clones of nattokinase. We are going to perform full sequence of each clones, ligate with expression vector, transform into competent cells and then determine activity of expressed enzymes.

• 대한화학회지
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• 제46권2호
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• pp.151-156
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• 2002

Fucoidan은 갈조류에 다량 함유되어있는 다당류로서 항암작용, 항혈응고작용, 항혈전작용, 항염증작용, 항virus작용과 같은 생리활성작용력을 가지고 있어 최근 많은 연구가 수행되어지고 있다. 본 논문은 갈조류에서 fucoidan을 추출 하여 그 항암활성을 SV40 DNA replication assay, RPA-ssDNA binding assay, 그리고 MCF7 cell growth inhibition assay를 이용하여 알아보았으며 이 항암활성은 fucoidan의 황산기가 중요한 역할을 하고 있음을 알아내었다. 화학적으로 황산기의 함유량을 증가시킨 fucoidan이 황산기의 함유량을 제거시킨 fucoidan보다 항암활성이 뛰어났고, 이는 RPA의 ssDNA 결함력을 떨어 EM리기 때문이라 예측되어 진다. 본 연구는 한국산 갈조류에서 추출한 황산기를 함유한 fucoidan의 항암활성능력을 보여주었다.

• Journal of Nutrition and Health
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• 제36권9호
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• pp.889-897
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• 2003

This study was carried out to determine the effect of dietary ${\gamma}$-linolenic acid on decreasing the plasma lipid levels and the thrombotic activity in rats. Sprague-Dawley male rats (B.W 120 g) were fed a experimental diet containing 5% lard (46.05% saturated fatty acids) , corn oil (51.36% linoleic acid) , evening primrose oil (EPO,72.80% linoleic acid and 9.16% ${\gamma}$-linolenic acid) or borage oil (BO,40.29% linoleic acid and 24.25% ${\gamma}$-liolenic acid) for 30 days. Although there were no significant differences in the food intake among the groups, the body weight gain of the BO group was significantly lower than that of the other groups. The bleeding time of the BO group was significantly longer than that of the other groups. There were significantly differences in the whole blood clotting time among the groups except for the EPO and corn oil groups, where the whole blood clotting time of the BO group was the highest among the groups, and that of the lard group was the lowest. The plasma triacyglyceride (TAG) , total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) concentrations were the lowest in the BO group, but highest in the lard group, and there were significant differences among the groups. The plasma HDL-C concentrations were in the following order: BO, EPO, corn oil and lard groups and there were significant differences among the groups. The excretions of fecal neutial steroids and acidic steroids of the BO group were the highest among the groups, and there were significant differences compared to the other groups. The results suggest that dietary EPO and BO containing ${\gamma}$-linolenic acid has an antithrombotic activity, and inhibits the increasing of plasma TAG, TC and LDL-C concentrations compared to lard, which contains saturated fatty acids, or corn oil, which contains linoleic acid.

• 대한한의학방제학회지
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• 제6권1호
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• pp.199-214
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• 1998

This study was performed to prove the antithrombotic effects of DoHongYeum fluid by way of experimental methods. The thrombosis was induced by injection of collagen the mixture (0.1ml/10g, 2mg/kg B.W)plus serotonin (5mg/kg B.W) into the caudal vein of rat, 2 hours after liquid extract of DoHongYeum was oral administration. The effect of the fluid of DoHongYeum was rxamined by the number of RBC and platelets, bleeding time, blood clotting time, death rate, platelet aggregation, plasmacoagulation factor activity, exvivo and fibrinolytic activity of englobulin fracture in the rats. The results were summerized as followings. 1. The number of RBC and platelets was significantly increased in DoHomeYeum group incomparison with the control group. 2. Bleeding time was significantly shortened in DHY group in comparison with the controlgroup. 3. Blood clotting time was significantly prolonged in DHY group in comparison with the control group. 4. The death rate of mouse was inhibited in DHY group in comparison with the control group. 5. The platelet aggregation was inhibited in DHY group in comparison with the control group. 6. The prothrombin time and activated partial thromboplastin time on the test of plasmacoagulation factor activity was prolonged but was not valuable in DHY group. 7. Fibrinogen lyses time of rat was reduced and lyses area was increased in DHY group incomparison with the control group. 8. Fibrinogen lyses time of rat in vitro assay was reduced in DHY group. From the above results, it was thought that the DoHongYeum could be applied effectively in the thrombosis.