• BMB Reports
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• v.46 no.10
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• pp.484-489
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• 2013

Piperlonguminine (PL), an important component of Piper longum fruits, is known to exhibit anti-hyperlipidemic, antiplatelet and anti-melanogenic activities. Here, the anticoagulant activities of PL were examined by monitoring activated-partial-thromboplastin-time (aPTT), prothrombin-time (PT), and the activities of thrombin and activated factor X (FXa). The effects of PL on the expressions of plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) were also tested in tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) activated HUVECs. The results showed that PL prolonged aPTT and PT significantly and inhibited the activities of thrombin and FXa. PL inhibited the generation of thrombin and FXa in HUVECs. In accordance with these anticoagulant activities, PL prolonged in vivo bleeding time and inhibited TNF-${\alpha}$ induced PAI-1 production. Furthermore, PAI-1/t-PA ratio was significantly decreased by PL. Collectively, our results suggest that PL possesses antithrombotic activities and that the current study could provide bases for the development of new anticoagulant agents.

• Natural Product Sciences
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• v.8 no.2
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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.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.177-177
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• 1998

In the previous report, tetrandrine (TET) and fangchinoline (FAN) showed antithrombotic and antiplatelet aggregation activities. The present study was undertaken to investigate the effects of tetrandrine and fangchinoline on human platelet aggregation, formation of thromboxane B$_2$ and coagulation of platelet poor plasma. TET and FAN inhibited platelet activating factor (PAF) induced human platelet aggregation, but didn't inhibit the specific binding of PAF to its receptor. Meanwhile, TET and FAN also inhibited PAF, thrombin and arachidonic acid induced thromboxane B$_2$ formation in human washed platelets. In addition, neither TET nor FAN showed any anticoagulation activities in the measurement of the activated partial thromboplastin time (APTT), prothrombin time (PT) and thrombin time (TT) using human platelet poor plasma. These results suggest that antithrombotic effects of TET and FAN in mice may be mainly related to the antiplatelet aggregation activities, and the antiplatelet aggregation effects may be related to the intracellular messenger system such as TXA$_2$ formation etc., but not to the binding of PAF to PAF-receptor on the platelet membrane directly.

• Archives of Pharmacal Research
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• v.26 no.12
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• pp.1102-1108
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• 2003

We studied the effects of phytolaccosides, saponins from Phytolacca americana, on the intestinal absorption of heparin in vitro and in vivo. The absorption enhancing activity of these compounds (phytolaccosides B, $D_2$, E, F, G and I) was determined by changes in transepithelial electrical resistance (TEER) and the transport amount of heparin disaccharide, the major repeating unit of heparin, across Caco-2 cell monolayers. With the exception of phytolaccoside G, all of them decreased TEER values and increased the permeability in a dose-dependent and time-dependent manner. In vitro, phytolaccosides B,$D_2$, and E showed significant absorption enhancing activities, while effects by phytolaccoside F and I were mild. In vivo, phytolaccoside E increased the activated partial thromboplastin time (APTT) and thrombin time, indicating that phytolaccoside E modulated the transport of heparin in intestinal route. Our results suggest that a series of phytolaccosides from Phytolacca americana can be applied as pharmaceutical excipients to improve the permeability of macromolecules and hydrophilic drugs having difficulty in absorption across the intestinal epithelium.

• Journal of Ginseng Research
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• v.34 no.4
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• pp.355-362
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• 2010

In this study, the anticoagulant compounds in Korean red ginseng (KRG) were investigated. KRG powder was extracted using hot methanol, and the methanol extract was fractionated into n-hexane, ethylacetate, n-butanol, and aqueous fractions by solvent partitioning. The remains from the methanol extraction were further extracted with water and then dialyzed to obtain low and high molecular weight fractions. The anticoagulant activities of the seven fractions were evaluated in terms of thrombin time, prothrombin time, and activated partial thromboplastin time. Among these fractions, the ethylacetate fraction showed the most potent anticoagulant activity. The active components in the ethylacetate fraction were identified as the phenolic compounds vanillic, caffeic, ferulic, and p-coumaric acid via TLC and HPLC. These findings suggest that the anticoagulant activities of phenolic compounds contribute to the cardiovascular effects of KRG.

• Journal of Haehwa Medicine
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• v.4 no.2
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• pp.91-103
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• 1996

This study was performed to prove the clinical effects of Kyejibokryoung hwan(KBH), Jeodangtang(JDT), Kyejibokryounghwan & Jeo-dangtang(KJT) by way of experimental methods. The intravascular coagulation was induced by injection of endotoxin into the caudal vein of rats. And liquid extracts of Kyejibokryounghwan, Jeodangtang, Kyejibokryounghwan & Jeodang- tang were administerd orally to the rats. Then the number of platelets, concentration of fibrinogen, FDP(fibrin-fibrinogen degradation products), prothrombin time and PTT(partial thromboplastin time) were measured. The results were obtained as follows ; 1. The number of platelets was significantly increased in KBH and KJT-treated groups in comparison with the control group. 2. Fibrinogen was significantly increased in all sample groups as compared with the control group. 3. FDP was insignificantly decreased in all sample groups but have not significant. 4. Prothrombin time was significantly shortened in JDT and KJT-treated groups as compared with the control group. 5. PTT was significantly shortened in only KJT -treated groups as compared with the control group. From the above results, it was concluded that Kyejibokryounghwan, Jeodang tang, Kyejibokryounghwan & Jeodangtang can be applied effectively in the disease of thrombosis.

• Journal of Veterinary Clinics
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• v.34 no.2
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• pp.65-69
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• 2017

Thromboembolic complications are increasing in veterinary medicine. Thromboelastography (TEG) is a more comprehensive method for assessing the clotting process than standard plasma-based coagulation tests. This study compared the ability of TEG and standard coagulation tests to analyze the overall hemostatic state of dogs. The study involved 40 dogs with underlying diseases that predispose to hypercoagulability, including neoplasia, hyperadrenocorticism, immune-mediated diseases, gastrointestinal diseases, and protein-losing nephropathies and enteropathies, and 20 healthy dogs. Their overall hemostatic functional state was evaluated by TEG and routine coagulation assays, including activated partial thromboplastin time, prothrombin time, platelet count, and D-dimer concentration. TEG analysis showed significant differences in clot formation time, ${\alpha}$ angle, and maximum amplitude (MA) between diseased and control dogs (P < 0.001 each). Increased MA was the most frequent abnormality on TEG and was indicative of hypercoagulability. TEG was useful in detecting hemostatic dysfunction in dogs with diseases associated with hypercoagulability. Dogs with TEG tracings indicative of hypercoagulability are likely to be in procoagulant states. Future prospective studies are needed to evaluate whether TEG tracings indicative of hypercoagulability are predictive of thrombosis in dogs.

• Biomolecules & Therapeutics
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• v.4 no.2
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• pp.184-189
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• 1996

General pharmacological studies of LB20304a (a mesylate salt form of a new quinolone antibiotic LB20304 following oral administration of 300 mg/kg and 1000 mg/kg, almost maximum tolerance dose in mice and rat, respectively, were performed in terms of effects on general behaviour, central nervous system, gastrointestinal system, and blood coagulation system in mice and rats. With regards to general behaviour of mice, at oral dose of 300 mg/kg, LB20304a reduced muscle tone and locomotor activity. In terms of CNS, at oral treatment of 300 mg/kg, LB20304a showed some analgesic effects in mice, and oral dose of 1000 mg/kg caused drop in normal body temperature of rat, while it enhanced the pentylenetetrazole-induced clonic convulsion to tonic convulsion and/or death in mice at the doses of unto 300 mg/kg. In addition, LB20304a increased hexobarbital-induced sleeping time two and three times in mice at oral doses of 20 mg/kg and 300 mg/kg, respectively. Rota-rod and traction test in mice were not influenced by the dose of 300 mg/kg and 200 mg/kg, respectively. LB20304a reduced gastric secretion of rat at dose of 1000 mg/kg, and increased intestinal motility of mice at dose of 300 mg/kg. In rats, blood coagulation index, such as PT (prothrombin time) and aPTT (activated partial thromboplastin time) were not affected by the treatment of upto 1000 mg/kg of LB 20304a.

• YAKHAK HOEJI
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• v.36 no.4
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• pp.350-356
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• 1992

Anticoagulant activities were tested for the fifteen kinds of medicinal plants by measuring activated partial thromboplastin time (aPTT). Of them five kinds or species (Artemisia princeps, Sanguisorba officinalis, Artemisia apiacea, Eclipa alba, Schizonepeta tenuifolia) were selected and fractionated for the preparation of acidic polysaccharides. They were extracted with water by refluxing and the extracts were precipitated with ethanol. The precipitates were separated based on charge using a DEAE-Sephadex. The low salt and high salt fractions were sulfated with anhydrous pyridine and chlorosulfonic acid complex. In vitro anticoagulant activities of sulfated polysaccharides were tested by measuring aPTT, prothrombin time (PT), and factor Xa clotting time using normal human plasma. No relationship was found between the amount of uronic acids and anticoagulant activities, but the sulfated ones show the increase of activities. In vivo anticoagulant properties of the sulfated polysaccharide from Artemisia apiacea were also tested by the intraveneous administration of three different doses (3,5 and 10 mg/kg) to rats. APTT and PT were increased significantly and the action of factor Xa and thrombin mediated through antithrombin III were inhibited slightly.

• Korean Journal of Food Science and Technology
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• v.48 no.2
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• pp.153-158
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• 2016

The principal objective of this study was to produce a chitosan nanoparticle (NP) system for improving blood circulation. Chitosan NPs were prepared using fucoidan and $poly-{\gamma}-glutamic$ acid (PGA), denoted as CS/Fu and CS/Fu/PGA NPs, respectively. As the chitosan concentration was increased, the activated partial thromboplastin time (APTT) of the NPs significantly increased (p<0.05). When the concentration of fucoidan and ${\gamma}-PGA$ was 5-20 and $1-10{\mu}g/mL$, respectively, the size of the CS/Fu and CS/Fu/PGA NPs was approximately 200 and 100 nm, respectively. With an increase in the fucoidan and PGA concentration, the APTT of CS/Fu and CS/Fu/PGA NPs significantly increased (p<0.05). These results suggest that CS/Fu and CS/Fu/PGA NPs could be used as a potent NP system for improving blood circulation.