• Archives of Pharmacal Research
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• v.23 no.2
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• pp.116-120
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• 2000

Aspirin has been widely used as analgesic and anti-inflammatory drug. Recently, it was elucidated that aspirin have anti-coaggregatory effect in low dose. This study was carried out to investigate the synthesis of aspirin derivatives from aspirin and aromatic compound of antioxidant and its biological activities. Synthesis of aspirin derivatives was prepared by esterification in the presence of 1, 1-carbonyldiimidazole. Biological activities was examined using effect of anti-coagulant on bleeding time, effect of antioxidant and effect of anti-platelet aggregation. As a result, SJ-101 showed strong antioxidative activity and anti-coagulant activity among four compounds. Anti-platelet aggregation of SJ-101 was examined by collagen, ADP, PAF method. SJ-101 exhibited more stronger activity to aspirin at collagen aggregation reaction. These finding demonstrates that SJ-101 is usefull as care drug of aging and old-disease because of its has antioxidant activity, anti-coagulant activity and anti-platelet activity.

• YAKHAK HOEJI
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• v.55 no.5
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• pp.374-378
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• 2011

This study was performed to evaluate enhanced effect of fermented Galgeun tang (GGT) and Ssanghwa tang (SHT) on the anti-platelet aggregation. Platelet aggregation assay was performed In vitro using human platelet rich plasma(PRP) and In vivo using SD-rat plasma by platelet aggregometer. Pharmacodynamic parameters, $E_{max}$ and $EC_{50}$, were calculated using Winnolin. SD-rats administered 1 g/kg of oriental medicine every 12 hr for 8 days. Platelet aggregation was measured by optical method with collagen inducer (4 ${\mu}g$/ml). In In vitro anti-platelet study, $EC_{50}$ of GGT-A was lower than that of GGT-con about 79.13 ${\mu}g$/ml. And $EC_{50}$ of SHT-A and SHT-B was lower than that of SHT-con about 122.73 and 110.15 ${\mu}g$/ml, respectively. It is assumed that fermented GGT and SHT were more effective than original medicine. In multiple administration study, anti-platelet effect was significantly increased both GGT and SHT. Fermented GGT and SHT were more effective than original herbal medicine on anti-platelet aggregation.

• Journal of Physiology & Pathology in Korean Medicine
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• v.27 no.2
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• pp.239-245
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• 2013

In in vitro study, the anti-platelet aggregation effect of Shiitake mushroom extract was examined by measuring the collagen induced platelet aggregation and the DPPH radical scavenging. In in vitro study, anti-thrombotic effect of Shiitake mushroom extract was examined using the carotid artery thrombosis rat model. Carotid artery thrombosis rat model was made by 35% $FeCl_3$ treatment. After that, we investigate thrombus weight and blood flow. In platelet aggregation test, the extract significantly inhibited platelet aggregation in a concentration dependent manner(p<.001). Also, extract increased DPPH radical scavenging activity in a concentration dependent manner. Extract significantly inhibited thrombus weight to compare with control group. And blood passage time were shorter in the Shiitake mushroom extract supplemented groups than in control group. These results provide experimental evidence that Shiitake mushroom can be used to prevent platelet aggregation and thrombosis, then could apply the clinical diseases such as cardiovascular disease, and so on.

• Biomedical Science Letters
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• v.25 no.4
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• pp.302-312
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• 2019

The aim of this work was to investigate the effect of black tea extract (BTE) on collagen -induced platelet aggregation. In this study, BTE (10~500 ㎍/mL) was shown to inhibit platelet aggregation via thromboxane A₂ (TXA₂) down-regulation by blocking cyclooxygenase-1 (COX-1) activity. Also, BTE decreased intracellular Ca²⁺ mobilization ([Ca²⁺]_i). Additionally, BTE enhanced the levels of both cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), which are aggregation-inhibiting molecules. BTE inhibited the phosphorylation of phospholipase C (PLC) γ2 and syk activated by collagen. BTE regulated platelet aggregation via cAMP-dependent phosphorylation of vasodilator-stimulated phosphoprotein (VASP) Ser¹⁵⁷. The anti-platelet effects of BTE in high fat diet (HFD)-induced obese rats were evaluated. After eight weeks of BTE treatment (300 and 600 mg/kg), the platelet aggregation rate in the treated groups was significantly less than that in the HFD-fed control group. Also, BTE exhibited a hepatoprotective effect and did not exert hepatotoxicity. Therefore, these data suggest that BTE has anti-platelet effects on collagen-stimulated platelet aggregation and may have therapeutic potential for the prevention of platelet-mediated thrombotic diseases.

• YAKHAK HOEJI
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• v.38 no.2
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• pp.191-196
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• 1994

Higenamine is a tetrahydroisoquinoline alkaloid which was isolated as a cardiotonic principle from Aconiti tuber. 1.v. injection of higenamine was reported to increase the cardiac output and heart rate and to decrease the blood pressure and the systemic vascular resistance presumably by stimulating the adrenergic ${\beta}-receptors$. The anti-platelet and anti-thrombotic effects of higenamine were investigated in this paper. Higenamine(0.5 mg/ml) showed mild inhibitory effect against collagen induced platelet aggregation in vitro and the inhibito교 effect was increased with the pre-incubation$(5{\sim}30\;min)$ of platelet rich plasma(PRP) with higenamine. With the 30 min incubation, the platelet aggregation was almost completely inhibited. And the oral administration of higenamine$(50{\sim}200\;mg/kg)$ enhanced the survival in the mouse model of thrombosis and that of endotoxic shock. The anti-thrombotic and anti-septic effects of higenamine thus appear to be due to the ${\beta}-agonistic$ and the anti-platelet effects of this compound.

• Journal of Physiology & Pathology in Korean Medicine
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• v.25 no.3
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• pp.471-481
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• 2011

Clove has been frequently used as anti-diabetic, anti-microbial, anti-inflammatory, anesthetic drug and remedies for stomachache by coldness. In this study, the antioxidant activity of extract from Clove was studied in vitro methods by measuring the antioxidant activity by TEAC, measuring the scavenging effects on reactive oxygen species (ROS) [superoxide anion, hydroxyl radical] and on reactive nitrogen species (RNS) [nitric oxide and peroxynitrite] as well as measuring the inhibitory effect on $Cu^{2+}$-induced human LDL oxidation. Anti-platelet aggregation and anti-thrombotic effects of Clove extracts were studied ex vivo methods by mesuring the inhibitory effect on thrombin induced platelet aggregation and the fibrinolytic activity. The Clove extracts were found to have a potent scavenging activity, as well as an inhibitory effect on LDL oxidation in vitro. Moreover Clove extracts were exhibited remarkable inhibitory effect on platelet aggregation and fibrinolytic activity. In conclusion, the Clove extracts have anti-oxidative and anti-atherosclerotic effects in vitro and ex vivo system, which can be used for developing pharmaceutical drug against oxidative stress and atherosclerosis.

• Journal of Physiology & Pathology in Korean Medicine
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• v.23 no.5
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• pp.980-985
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• 2009

The study was designed to test anti-platelet effect and find out anti-platelet mechanism of extract from Gamisopunghwalheol-tang in vitro. The extract was investigated for the inhibition against the aggregation of human platelet suspensions induced from collagen by aggregometer. And also the extract was investigated for the inhibition against the aggregation of human platelet suspensions who is taking aspirin or clopidogrel induced from collagen by aggregometer. In collagen-induced platelet aggregation test, the extract significantly inhibited collagen-induced platelet aggregation in a concentration-dependent manner(p<0.05). The extract significantly inhibited collagen-induced platelet aggregation of human platelet who is taking aspirin or clopidogrel ing 0 mg/ml concentration(p<0.05). And the extract inhibited more ingpatients who is taking aspirin. These results show that the extract from Gamisopunghwalheol-tang has anti-platelet aggregation effect.

• The Journal of Korean Medicine
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• v.29 no.5
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• pp.52-66
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• 2008

Objectives :Ginkgo-Chunghyul-dan (GCHD) is newly developed herbal medicine to prevent and treat stroke. In this study, we investigated whether the GCHD had antioxidant activity and anti-platelet aggregation effect in vitro and hypolipidemic activities in vivo. Methods :Anti-oxidant activity of GCHD was measured using the Blois method, anti-platelet effect of GCHD was assessed by the Born method, and hypolipidemic activities of GCHD were evaluated in corn oil- or Triton WR-1339-induced and cholesterol-fed rats. Results :GCHD showed anti-oxidant activity in the study inhibiting the formation of 1-diphenyl-2-picrylhydrazyl radicals and xanthine oxidase activity. GCHD had anti-platelet aggregation activity. GCHD significantly lowered total cholesterol (TC), triglyceride (TG), and low density lipoprotein cholesterol (LDL-C) in high cholesterol diet and Triton WR-1339 induced model TG in corn oil-induced model. GCHD had no acute toxicity at a single dosage. Conclusion : These results suggest that GCHD has the potential to treat hyperlipidemia and stroke.

• Biomolecules & Therapeutics
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• v.23 no.2
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• pp.149-155
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• 2015

Our previous study demonstrated that yuzu has an anti-platelet effect in rat blood. In the present study, we examined whether the anti-platelet effect of yuzu can be extended to human blood by investigating its ability to inhibit aggregations induced by various agonists in human platelet rich plasma (PRP). This study also investigated the underlying mechanism of yuzu focusing on ADP granule secretion, $TXB_2$ formations, and $PLC{\gamma}$/Akt signaling. The results from this study showed that ethanolic yuzu extract (YE), and its components, hesperidin and naringin, inhibited human platelet aggregation in a concentration-dependent manner. YE, hesperidin and naringin also inhibited $TXB_2$ formation and ADP release. The phosphorylation of $PLC{\gamma}$ and Akt was significantly inhibited by YE, heperidin and naringin. Furthermore, we demonstrated that YE, heperidin and naringin has anti-platelet effects in rat ex vivo studies, and lower side effects in mice tail bleeding time studies. The results from this study suggest that YE, hesperidin and naringin can inhibit human platelet aggregation, at least partly through the inhibition of $PLC{\gamma}$ and Akt, leading to a decrease in $TXB_2$ formation and granule secretion.

• Biomedical Science Letters
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• v.25 no.2
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• pp.123-130
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• 2019

Platelet aggregation is essential for hemostatic process in case of blood vessels damages. However, excessive platelet aggregation can cause cardiovascular disorders including atherosclerosis, thrombosis and myocardial infarction. Scopoletin is usually found in the roots of genus Scopolia or Artemisia, and is known to have anticoagulant and anti-malarial effects. This study investigated the effect of scopoletin on human platelet aggregation induced by U46619, an analogue of thromboxane $A_2(TXA_2)$. Scopoletin had anti-platelet effects by down-regulating $TXA_2$ and intracellular $Ca^{2+}$ mobilization ($[Ca^{2+}]_i$), the aggregation-inducing molecules generated in activated platelets. On the other hand, scopoletin increased the levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), which are known to be intracellular $Ca^{2+}$ antagonists. This resulted in inhibition of fibrinogen binding to ${\alpha}IIb/{\beta}_3$ in U46619-induced human platelet aggregation. In addition, scopoletin inhibited the release of adenosine trisphosphate (ATP) in dose-dependent manner. This result means that the aggregation amplification activity through the granule secretion in platelets was suppressed by scopoletin. Therefore, we demonstrated that scopoletin has a potent antiplatelet effect and is highly likely to prevent platelet-derived vascular disease.