• Natural Product Sciences
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• 제8권2호
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• pp.66-70
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• 2002

The in vitro anticoagulant and fibrinolytic activities of crude extracts from insects were evaluated in order to find effective therapeutic drugs for the treatment of myocardial and cerebral thrombosis. We prepared three types of extracts (water, methanol and ethylacetate) from 28 insects for use as raw materials for the activity assays. The fibrinolytic activity was tested using the fibrin plate method and the activated partial thromboplastin time and thrombin time were measured for blood clotting activity. With regards to the fibrinolytic system, water extracts of six kinds of insects displayed a remarkable level of activity with a plasmin-like action. The water extracts of [Catharsius molossus, Eupolyphaga sinensis, Huechys sanguinea, Mantidis $o\ddot{o}theca$, Mimela splendens, and Polistes mandarinus (Vespae Nidus)] exhibited the activity. On the other hand, the methanol extracts did not display any fibrinolytic activity. In terms of the coagulation system, an aqueous extract of silkworm Tongchunghacho (Paecilomyces japonica), Oxya japonica japonica and Buthus martensi (Scorpion) increased the clotting time significantly longer (181 times) than the control. These results suggest that crude drugs from insects are useful sources for the development of new drugs for use in treatments involving blood coagulation and fibrinolysis.

• Biomolecules & Therapeutics
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• 제9권4호
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• pp.258-262
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• 2001

In the advanced age, cardiovascular disease is more serious than any other disease. Especially, the thrombus causes the serious disease like apoplexia, carebri and myocardial infarction. Thrombosis is caused by the injury of endothelium and the alterations in normal blood flow. To investigate activities of Carthamus tinctorius L. Semen butanol fraction for blood coagulation system, endotoxin (4000EU/kg) was injected (i..v) to rats at 1hr after administration of Carthamus tinctorius L. Semen butanole fraction (500 mg/kg, p.o.). Carthamus tinctorius L. Semen butanol fraction was found to have antiplatelet activity in vitro. In vivo it showed a delay of blood clotting time, and prothrombin time, and reduction of fibrinogen and FDP It also increased SOD activity, and decreased MDA content. These results suggest that the antithrombosis effect of Carthamus tinctorius L. Semen butanol frac tion results from suppressive activity for a blood coagulation system and antioxidative activity.

• 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.

• 대한임상검사과학회지
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• 제47권4호
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• pp.237-242
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• 2015

aPTT 참고치의 정상범위 내에서 하한 측 10% (29.1~30.9 sec)와 상한 측 10% (38.0~41.9 sec)에 포함된 정상성인의 혈액응고인자 활성도를 분석하여 하한 측과 상한 측간에 혈액응고인자의 종류와 각각의 활성도가 성별, 연령 및 ABO 혈액형 등에 통계학적으로 유의한 차이를 보이는지 알아보고자 하였다. 성별에 따른 혈액응고인자들의 활성도 차이를 분석한 결과 하한 측에서 IX (p=0.0088)만 남성이 여성보다 높았으며, 상한 측에서 IX (p<0.0001)와 X (p=0.0013)은 남성이 여성보다 높았다. 연령군간 혈액응고인자들의 활성도 차이 검정은 하한 측에서 VIII (p<0.0001), IX (p=0.0050)는 60세 이상이 60세 미만보다 높았으며, XII (p=0.0285)는 60세 이상보다 60세 미만이 높았다. 상한 측에서 V (p=0.0219), VIII (p=0.0005), IX (p=0.0014)는 60세 이상이 60세 미만보다 높았다. O형과 non-O형의 혈액형 구분에 의한 혈액응고인자들의 활성도 차이는 VIII (p<0.001)은 양쪽 그룹에서 non-O형이 O형보다 높았으며, XII (p=0.016)는 상한 측에서 non-O형이 O형보다 낮았다.

• BMB Reports
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• 제29권3호
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• pp.225-229
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• 1996

Effects on thrombin by an amphipathic cation, dequalinium, which has been recognized as an anticarcinoma agent were investigated with small chromogenic substrates such as Na-benzoyl-DL-argininep-nitroanilide (BApNA), H-D-phenylalanyl-L-pipecoyl-L-arginine-p-nitroanilide (S-2238), and Na-p-tosyl-L-arginine methyl ester (TAME). Among them, only TAME hydrolysis due to an esterase activity of the enzyme was significantly activated to 81% at 20 ${\mu}M$ dequalinium in the absence of NaCl. This stimulation became even higher in the presence of 0.2 M NaCl to 3.5-fold at 60 ${\mu}M$ dequalinium. This specific activation of thrombin was well correlated with the results of in vitro coagulation tests measuring the activated partial thromboplastin time (APTT) and the prothrombin time (PT) It is pertinent. therefore, to suggest that the esterase activity should be examined in addition to the effects on 5-2238 hydrolysis when especially any regulators not directed to an active site of thrombin need to be studied. We also expect that dequalinium could be a useful tool for studying structure-function relationship of thrombin and blood coagulation.

• 한국입자에어로졸학회지
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• 제4권2호
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• pp.69-75
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• 2008

Nanosize ZnO particles were prepared by oxidation of zinc vapor and the particle growth was modeled by a coagulation model by assuming that the characteristic time for reaction was much shorter than coagulation time and residence time (${\tau}_{reaction}{\ll}{\tau}_{coagulation}{\ll}{\tau}_{residence}$). Experimental measurement of zinc oxide particles diameter was consistent with the predicted result from the coagulation model. For practical purpose of predicting zinc oxide size in areosol reactor, the constant kernel solution is concluded to be sufficient, Uniqueness of nano-scale property of zinc oxide was confirmed by the higher photocatalytic activity of zinc oxide than nanosize titania particles.

• 한국식생활문화학회지
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• 제29권5호
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• pp.415-420
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• 2014

This study was conducted to establish optimum conditions for coagulation of konjac jelly as well as antimicrobial activity by concentration of $Ca(OH)_2$. Hardness, gumminess, and chewiness of konjac jelly increased according to concentration of konjac powder, the key material of konjac jelly. The highest sensory evaluation score was acquired with konjac jelly made with 3% konjac powder. A $Ca(OH)_2$ concentration of 0.4-0.6% as a coagulation agent was optimum for coagulation of konjac jelly. Further, sensory score was highest at a $Ca(OH)_2$ concentration of 0.6%. All populations of bacteria, yeast, and mold in konjac jelly were restrained by $Ca(OH)_2$ in a concentration- dependent manner. Furthermore, all tested microorganisms were strictly restrained at $1.0{\times}10^{-2}$ N of $Ca(OH)_2$.

• 대한한방부인과학회지
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• 제21권1호
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• pp.55-82
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• 2008

Purpose: In this study, we evaluated anti-inflammatory activity and anti-thrombosis effect of Manbunbang(MBB) prescribed to chronic PID patients. Methods: We studied inhibitory effect of platelet aggregation, suppression effect of GPIIb/IIIa activity and inhibitory effect of $TXB_2$ and $PGE_2$ biosynthesis which were caused by ADP, epinephrine, collagen and arachidonic acid in vitro. And suppression of pulmonary embolism, changes of related factors in dextran coagulation condition model and anti-oxidative effect of oxidative damage were studied in vivo. Results: MBB extract showed LD50 of $200\;{\mu}g/ml$ or higher in mouse lung fibroblast cells, and significantly decreased the GPT and GPT level in dextran coagulation condition model compared to the control. MBB extract showed dose-dependent inhibition effect on platelet coagulation induced by ADP, epinephrine, collagen, arachidonic acid. MBB extract showed dose-dependent inhibition effect on GPIIb/IIIa activities compared to the control. MBB extract significantly suppressed TXB2 and PGE2 biosynthesis compared to the control. MBB extract suppressed pulmonary embolism triggered by collagen and epinephrine by 37.5% compared to the control. MBB extract significantly suppressed the decrease of speed of bloodstream caused by blood coagulation in dextran coagulation condition model compared to the control. Concluson : The results strongly suggest the anti-inflammatory activity of Manbunbang through anti-thrombus. Various applications using Manbunbang on inflammatory diseases are anticipated. Anti-oxidative efficacy comparison data between the Manbunbang prescription and the drug compositions may be used as important clinical information, and further investigation of anti-oxidative activities of Chrysanthemum indicum and Rhemaniae Radix should be followed.

• 한국응용과학기술학회지
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• 제3권1호
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• pp.15-22
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• 1986

The purpose of this study was to investigate the effects of garlic diet on blood coagulation in cholesterol-fed rats. 36 male rats were divided into six groups and fed experimental diet for three weeks. Two-levels (2% and 4%) of fresh and boiled garlic were supplemented to the stock diet with 2% cholesterol and 0.25% bile salt for the experimental diet. After the rats fed with experimental diets during 3 weeks, the whole blood coagulation time, the content of plasma fibrinogen, the fibrinolytic activity and the prothrombin time were measured. The results are summarized as follows; 1. Garlic diet have no influence on body weight and food consumption in rats. 2. In the case of cholesterol-fed group, the whole blood coagulation time was decreased 24.3% compared with the normal group(A). But garlic diet group(C) was similar to the normal group(A) and groupD-F was increased 4.9-11.5%. 3. The content of plasma fibrinogen of cholesterol-fed group was higher 114.5% than that of normal gropu(A). In the garlic diets(C-F) the contents of plasma fibrinogen were increased 33.1-63.8%. 4. The fibrinolytic activity of cholesterol diet was decreased 16.2% compared with the normal group(A) but was increased 10.9-44.5% compared to the garlic diets(C-F). 5. The prothrombin time of cholesterol-fed group was decreased 8.9% compared with normal group(A) but was increased 8.0-46.3% in garlic diets(C-F). As mentioned above, the garlic diets increased whole blood coagulation time, prothrombin time and fibrinolytic activity and decreased the content of fibrinogen. For that reason it is thought that the garlic diets have a anticoagulation effect regulating the fibrinogen synthesis in liver.

• Biomolecules & Therapeutics
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• 제8권3호
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• pp.223-227
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• 2000

Propolis, a natural resinous compound collected from honey bees, contains many biochemical constituents and has been used for traditional medicines as early as 300 B .C. Recently, it has been reported to possess many biological activities such as antibacterial, antiviral, fungicidal, local anaesthetic, immunostimulating, antiinflammatory and free radical scavenging properties. To investigate activities of chrysin, one of propolis effective compounds for blood coagulation system was injected endotoxin (4000 EU/kg, i.v.) in rats at 1 hr after administered chrysin (20 mg/kg, p.o.). This study was resulted that chrysin has antiplatelet aggregation activity in vitro, delay of blood clotting time and prothrombin time, and reduction of fibrinogen and FDP in vivo. Chrysin has increased SOD activity, GSH content and GST activity, and decreased MDA content in liver. The result suggests that the antithrombosis effect of chrysin is suppressive activity for a blood coagulation system and antioxidative activity.