• 생약학회지
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• 제53권2호
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• pp.64-69
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• 2022

When blood vessels are damaged, a rapid hemostatic response should occur in order to lower blood loss and keep normal circulation, and platelet activation and aggregation are essential. Nevertheless, abnormal or excessive platelet aggregation can be a reason of cardiovascular diseases including thrombosis, atherosclerosis, and stroke. Therefore, the screening for a substance which can regulate platelet activation and suppress aggregation reaction is very important for treatment and prevention of cardiovascular diseases. Artemether is a methyl ether derivative of artemisinin, which is isolated from the antimalarial plant Artemisia annua, but research on platelet aggregation or its mechanisms is still insufficient. This study identified the effects of artemether on U46619-induced human platelet aggregation and their granule secretion (ATP and serotonin release). In addition, the effects of artemether on the phosphorylation of PI3K/Akt or MAPK, which are related to signal transduction in platelet aggregation, were studied. As the results, artemether significantly lowered PI3K/Akt and MAPK phosphorylation, which inhibited platelet aggregation through granule secretion (ATP and serotonin release) dose-dependently. Therefore, we suggest that artemether is an antiplatelet substance that regulates PI3K/Akt and MAPK pathway and is of value as a therapeutic and preventive agent for platelet-derived cardiovascular diseases.

• Journal of Applied Biological Chemistry
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• 제63권2호
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• pp.131-136
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• 2020

When blood vessels are damaged, a fast hemostatic response should occur to minimize blood loss and maintain normal circulation. Platelet activation and aggregation are essential in this process. However, excessive platelet aggregation or abnormal platelet aggregation may be the cause of cardiovascular diseases such as thrombosis, stroke, and atherosclerosis. Therefore, finding a substance capable of regulating platelet activation and suppressing agglutination reaction is important for the prevention and treatment of cardiovascular diseases. 6,7-Dimethoxy-2H-chromen-2-one (Scoparone), found primarily in the roots of Artemisia or Scopolia plants, has been reported to have a pharmacological effect on immunosuppression and vasodilation, but studies of platelet aggregation and its mechanisms are still insufficient. This study confirmed the effect of scoparone on collagen-induced human platelet aggregation, TXA₂ production, and major regulation of intracellular granule secretion (ATP and serotonin release). In addition, the effect of scoparone on the phosphorylation of the phosphoproteins PI3K/Akt and mitogen-activated protein kinases (MAPK) involved in signal transduction in platelet aggregation was studied. As a result, scoparone significantly inhibited the phosphorylation of PI3K/Akt and MAPK, which significantly inhibited platelet aggregation through TXA₂ production and intracellular granule secretion (ATP and serotonin release). Therefore, we suggest that scoparone is an antiplatelet substance that regulates the phosphorylation of phosphoproteins such as PI3K/Akt and MAPK and is of value as a preventive and therapeutic agent for platelet-derived cardiovascular disease.

• 약학회지
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• 제46권6호
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• pp.441-447
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• 2002

It has been well known that vanadium shows various physiological and pharmacological properties such as an insulin-mimetic effect. In view of the reported toxic effects there is the problems that the safety margin is narrow because of its strong toxicity, Vanadate was tested for its ability to cause blood aggregation. Although vanadate or $H_2O$$_2$ alone had little effect on platelet aggregation, treatment of vanadate and $H_2O$$_2$ together induced platelet aggregation indicated that it was occurred by pervandate or hydroxyl radical produced from the reaction of vanadate and $H_2O$$_2$. It was dependent on extracellular $Ca^{2+}$ion. Platelet aggregation caused by vanadate and $H_2O$$_2$ was inhibited by ascorbic acid, tocopherol, catalase, mannitol, and Tiron. In contrast to vanadate, vanadium yeast prepared by uptaking vanadate in yeast cells did not induce platelet aggregation in the presence of $H_2O$$_2$.>.

• 생약학회지
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• 제51권3호
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• pp.151-157
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• 2020

When blood vessels are damaged, a rapid hemostatic reaction occurs to minimize blood loss and maintain normal circulation. Platelet activation and aggregation is essential in this process. However, excessive platelet aggregation or abnormal platelet aggregation may be the cause of cardiovascular disease, such as thrombosis, stroke and atherosclerosis. Therefore, it is important to prevent and treat cardiovascular disease by finding substances that can regulate platelet activation and suppress aggregation reactions. Isoscopoletin, which is mainly found in the roots of plants Artemisia or Scopolia, has been reported to have potential pharmacological effects on anticancer and Alzheimer's disease, but its role and mechanisms for platelet aggregation and thrombus formation are unknown. This study confirmed the effect of isoscopoletin on major regulation of collageninduced human platelet aggregation, TXA₂ production and intracellular granular secretion (ATP and serotonin release). In addition, the effects of isoscopoletin on phosphorylation of phosphorylated proteins PI3K/Akt and MAPK involved in signal transduction in platelet aggregation was studied. As a result, isoscopoletin significantly inhibited the phosphorylation of PI3K/Akt and MAPK, significantly inhibiting platelet aggregation through TXA₂ production and intracellular granular secretion (ATP and serotonin release). Therefore, we suggest that isoscopoletin is an anti-platelet substance that regulates phosphorylation of phosphorus proteins such as PI3K/Akt and MAPK and is valuable as a preventive and therapeutic agent for platelet-derived cardiovascular disease.

• 동의생리병리학회지
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• 제27권2호
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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.

• Journal of Nutrition and Health
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• 제32권5호
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• pp.561-569
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• 1999

In the atherosclerotic subjects, arterial endothelial cell injury and plaque formation are suspected to be strong causable factors in developing acute coronary syndrome, and it was revealed that platelets have a very important role in this case. Women are exposed to atherosclerosis at a different degree after menopause or oral contraception. The purpose of this study was to determine the effects of endogenous and exogenous estrogen on the degree of platelet aggregation in platelet rich plasma(PRP) in twenty nonsmoking healthy Korean women for 12 weeks. The subjects were assigned to three groups: (1) eight women aged 49 to 60(yr) for the postmenopausel(Pst) group, (2) eight, aged 22 to 30(yr) for the premenopausa(Pre) group, (3) four, aged 23 to 30(yr) for the oral contraceptive (OC) group which used triphasic OC formulation. Fasting blood sample were obtained from the subjects, (1) once per 6 weeks in the Pst group, (2) every phase of the menstrual cycle in the Pre group, (3) each once during and after OC administration in the OC group. ADP, collagen and epinephrine were used as aggregating reagents, and platelet aggregation and time(Δt: time reaching to the maximum point of aggregation) in PRP were measured at the maximum point of aggregation in five minutes. All the data were adjusted for dietary effects, personality type and body mass index(BMI) by using analysis of covariation(ANCOVA). Platelet aggregation to ADP and collagen(MADP and MCOLL) were not significantly different among the three groups, and Δt to ADP and collagen(TADP and TCOLL) were not either. But maximum platelet aggregability and Δt to epinephrine(MEPIN and TEPIN) were significantly different among the three groups, and the OC group showed the lowest value (p<0.01). Maxtimum platelet aggregability and Δt during the menstrual cycle were not significantly different in the Pre group. Any other significant differences in the maximum platelet aggregability and Δt were found between oral contraception phase and washing out phase(menstruation) in the OC group. In results, maximum platelet aggregability and aggregation time to ADP and collagen seemed not to be affected by endogenous and exogenous estrogen, even though MEPIN and TEPIN showed significantly low in the OC group among the three groups.

• 약학회지
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• 제55권5호
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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.

• Food Science and Biotechnology
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• 제15권5호
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• pp.763-767
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• 2006

The anticoagulant properties of compounds derived from fennel (Foeniculum vulgare Gaertner) fruits were evaluated using a platelet aggregometer and compared with aspirin. The active constituents of fennel fruits were isolated and identified as (+)-fenchone and extragole by various spectral analysis techniques. With regard to the 50% inhibitory concentration ($IC_{50}$), (+)-fenchone effectively inhibited platelet aggregation induced by treatment with collagen ($IC_{50}$, $3.9\;{\mu}M$) and arachidonic acid (AA) ($IC_{50}$, $27.1\;{\mu}M$), and estragole inhibited collagen-induced platelet aggregation ($IC_{50}$, $4.7\;{\mu}M$). By way of comparison, (+)-fenchone and estragole proved to be significantly more potent than aspirin at inhibiting platelet aggregation induced by collagen. The inhibitory activity of (+)-fenchone toward platelet aggregation induced by AA was 1.3 times stronger than that of aspirin. These results indicate that (+)- fenchone and estragole may be useful as lead compounds for inhibiting platelet aggregation induced by arachidonic acid and collagen.

• Journal of Nutrition and Health
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• 제33권4호
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• pp.374-385
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• 2000

The purpose of the present study was to investigate the effect of Korea leek on plasm lipids and platelet aggregation in hypercholesterolemic rats fed different dietary fat. Sprague-Dawley rats were fed with hyperlipidemic diet for 4 weeks in order to induce hyperlipidemia, followed by the feeding of experimental diets for additonal 4 weeks. We used three kinds of lipid(perilla oil, corn oil and lard). Korean leek of experimental diets was prepared by drying and milling. Powdered Cellulose and powdered Korean leek were added to experimental diets at the level of 5% (w/w). Serum concentrations of total lipid, total triglyceride, total cholesterol and LDL-cholesterol decreased in the order of perilla oil, corn oil and lard. Korean leek significantly decreased total lipid, total cholesterol, LDL-cholesterol, platelet count, prothrombin time, and platelet aggregation in rats fed a lard diet. The present observation indicates that Korean leek might be helpful for the prevention and threapy of hyperlipidemia and platelet aggregation.

• Journal of Ginseng Research
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• 제47권5호
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• pp.638-644
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• 2023

Background: The anti-platelet activity of the saponin fraction of Korean Red Ginseng has been widely studied. The saponin fraction consists of the panaxadiol fraction (PDF) and panaxatriol fraction (PTF); however, their anti-platelet activity is yet to be compared. Our study aimed to investigate the potency of anti-platelet activity of PDF and PTF and to elucidate how well they retain their anti-platelet activity via different administration routes. Methods: For ex vivo studies, Sprague-Dawley rats were orally administered 250 mg/kg PDF and PTF for 7 consecutive days before blood collection via cardiac puncture. Platelet aggregation was conducted after isolation of the washed platelets. For in vitro studies, washed platelets were obtained from Sprague-Dawley rats. Collagen and adenosine diphosphate (ADP) were used to induce platelet aggregation. Collagen was used as an agonist for assaying adenosine triphosphate release, thromboxane B2, serotonin, cyclic adenosine monophosphate, and cyclic guanosine monophosphate (cGMP) release. Results: When treated ex vivo, PDF not only inhibited ADP and collagen-induced platelet aggregation, but also upregulated cGMP levels and reduced platelet adhesion to fibronectin. Furthermore, it also inhibited Akt phosphorylation induced by collagen treatment. Panaxadiol fraction did not exert any antiplatelet activity in vitro, whereas PTF exhibited potent anti-platelet activity, inhibiting ADP, collagen, and thrombin-induced platelet aggregation, but significantly elevated levels of cGMP. Conclusion: Our study showed that in vitro and ex vivo PDF and PTF treatments exhibited different potency levels, indicating possible metabolic conversions of ginsenosides, which altered the content of ginsenosides capable of preventing platelet aggregation.