• Title/Summary/Keyword: antiplatelet activity

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The Effects of Anti-Thrombotic Activities and Cardiovascular Improvement of Fermented Garlic Extracts (발효마늘 추출물의 항혈전 및 심혈관개선 효과)

  • Kim, Hyun Kyoung
    • The Journal of the Convergence on Culture Technology
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    • v.6 no.2
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    • pp.567-572
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    • 2020
  • The purpose of this study was to investigate the effects of Anti-Thrombotic Activities and Cardiovascular Improvement of Fermented Garlic Extracts. The incidence of cardiovascular diseases (CVDs) is increasing rapidly in developed countries, with CVDs now representing the leading cause of morbidity and mortality. Natural products and ethnomedicines have been shown to reduce the risk of CVDs. Garlic is a medicinal plant used throughout the world for its anti-inflammatory, antioxidant, and antiplatelet activities. We hypothesized that fermented preparations of these products may possess stronger antiplatelet effects than the non-fermented forms owing to the increased bioavailability of the bioactive compounds produced during fermentation. Therefore, we compared these compounds via in vitro and ex vivo platelet aggregation assays by using standard light transmission aggregometry and ex vivo granule secretions from rat platelets. We found that fermented preparations exerted more potent and significant inhibition of platelet aggregation both in vitro and ex vivo. Likewise, ATP release from dense granules of platelets was also significantly inhibited in fermented preparation-treated rat platelets compared to that in non-fermented preparation-treated ones. We concluded that fermented preparations exerted more potent effects on platelet function both in vitro and ex vivo, possibly as a result of the increased bioavailability of active compounds produced during fermentation. We therefore suggest that fermented products may be potent therapeutics against platelet-related CVDs and can be used as antiplatelet and antithrombotic agents.

Antithrombotic and Antiplatelet Activity of Extract from Prunella vulgaris (하고초 추출물의 항혈전 효능 및 혈소판 응집 억제작용)

  • Yang, Won-Kyung;Sung, Yoon-Young;Kim, Ho-Kyoung
    • Journal of Life Science
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    • v.21 no.10
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    • pp.1422-1427
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    • 2011
  • This study was performed to develop effective antithrombotic agents from traditional herb extracts. Prunella vulgaris L. has been used traditionally as a medical resource in cancer therapy, as well as treatment of hypertension and inflammation, and as a diuretic. However, the effects of Prunella vulgaris on thrombosis and platelet activation have not been clearly understood. Antithrombotic and antiplatelet activities of oriental medicinal herbs were investigated by evaluating the effect of the aqueous extract from Prunella vulgaris on the blood coagulation, platelet aggregation and fibrinolysis. Prunella vulgaris extracts showed effective anticoagulant activity in coagulation times such as activated partial thromboplastin time (APTT) and prothrombin time (PT). Prunella vulgaris also inhibited adenosine diphosphate (ADP)- and collagen-induced platelet aggregation. In addition, evaluation of fibrinolytic activity showed that the Prunella vulgaris extracts have high solubility. From these results, it is suggested that Prunella vulgaris can be a potential candidate for anticoagulants and antiplatelets, as well as fibrinolytic agents.

Effect of Korean Red Ginseng Extract on Blood Circulation in Healthy Volunteers: A Randomized, Double-Blind, Placebo-Controlled Trial (건강한 지원자에서 홍삼농축액의 혈행 개선 효과: 무작위, 이중맹검, 위약-대조 시험)

  • Shin, Kyeong-Seob;Lee, Jung-Jin;Kim, Yeong-Il;Yu, Ji-Yeon;Park, Eun-Seok;Im, Ji-Hyun;You, Soon-Hyang;Oh, Ki-Wan;Lee, Myung-Koo;Wee, Jae-Joon;Kim, Young-Sook;Yun, Yeo-Pyo
    • Journal of Ginseng Research
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    • v.31 no.2
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    • pp.109-116
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    • 2007
  • Korean red ginseng has broad efficacious effects against hypertension, diabetes, nociception, and cancer, and it counteracts weakness. It has been reported that Korean red ginseng is able to normalize blood pressure, improve cholesterol and lower blood glucose levels. We have recently reported that Korean red ginseng extract (KRGE) significantly prevented rat carotid arterial thrombosis in vivo, and inhibited platelet aggregation ex vivo and in vitro in a dose-dependent manner. The purpose of this study was to examine the effects of KRGE on blood circulation in human by measuring ex vivo platelet aggregation, plasma coagulation and serum lipid profiles in healthy volunteers. Subjects were randomly divided into three groups (placebo-group, KRGE-low dose group, KRGE-high dose group). Administration of KRGE to subjects significantly inhibited ADP-induced platelet aggregations both in KRGE-low dose group from $72.79{\pm}20.53$ to $62.00{\pm}23.06%$ (p=0.0009), and in KRGE-high dose group from $75.14{\pm}21.86$ to $64.52{\pm}24.72%$ (p=0.0039), respectively. Administration of KRGE to subjects also significantly inhibited collagen-induced platelet aggregations both in KRGE-low dose group from $85.52{\pm}12.57$ to $79.62{\pm}20.47%$ (p=0.0916), and in KRGE-high dose group from $80.24{\pm}18.11$ to $70.31{\pm}25.93%$ (p=0.0565), respectively. Whereas, KRGE has no significant effects on coagulation system, such as prothrombin time (PT) and activated partial thromboplastin time (APTT), and serum lipid profiles, such as total cholesterol, low density lipoprotein cholesterol, high density lipoprotein cholesterol and triglyceride. KRGE also has no significant effects on hematological and serum biochemical profiles. These results suggest that KRGE has a potential to improve blood circulation through antiplatelet activity in human, and KRGE intake may be beneficial for the individuals with high risks of thrombotic and cardiovascular diseases.

The anti-platelet activity of panaxadiol fraction and panaxatriol fraction of Korean Red Ginseng in vitro and ex vivo

  • Yuan Yee Lee;Yein Oh;Min-Soo Seo;Min-Goo Seo;Jee Eun Han;Kyoo-Tae Kim;Jin-Kyu Park;Sung Dae Kim;Sang-Joon Park;Dongmi Kwak;Man Hee Rhee
    • Journal of Ginseng Research
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    • v.47 no.5
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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.

Evaluation of the in vivo Antithrombotic, Anticoagulant and Fibrinolytic Activities of Lumbricus rubellus Earthworm Powder

  • Hahn, Bum-Soo;Jo, You-Young;Yang, Kyung-Youl;Wu, Song-Ji;Pyo, Mi-Kyung;Yunchoi, Hye-Sook;Kim, Yeong-Shik
    • Archives of Pharmacal Research
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    • v.20 no.1
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    • pp.17-23
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    • 1997
  • A saline suspension of Lumbricus rubellus earthworm powder (EWP) was administered to rats (1 g/kg/day) orally for 15 days to evaluate an oral effectiveness for thrombotic disorders. Blood was drawn at 2-day interval after the administration. Several parameters for antithrombotic, anticoagulant and fibrinolytic activities were measured, including platelet aggregation, clotting time, plasmin activity and the levels of FDP (fibrin/fibrinogen degradation products), D-dimer, and t-PA antigen. It did not affect platelet aggregation induced by ADP and collagen but anticoagulant activity (aPTT and TT) was gradually increased to two-folds for the first 5 days of administration and back to normal. Fibrinolytic activity of euglobulin fraction was highest on the 11 th day after the administration. The level of FDP was elevated to be comparable to the positve control$ (5-10 {\mu}g/ml)$ after 9-day treatment. Oral administration of the EWP could also reduce the formation of venous thrombus induced with viper venom. Complete blood count (CBC) profiles were within normal ranges except for a slight increase in white blood cells after the oral administration for 15 days. These results suggested that the EWP may be valuable for the prevention and/or treatment of thrombotic diseases.

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Anticoagulant Properties of Compounds Derived from Fennel (Foeniculum vulgare Gaertner) Fruits

  • Lee, Hoi-Seon
    • Food Science and Biotechnology
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    • v.15 no.5
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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.

Aqueous Fraction from Korean Red Ginseng Inhibits the Protein Phosphorylation Induced by Tumor Promoter (고려홍삼의 수용성 분획은 종양촉진인자에 의해 유도되는 단백질 인산화반응을 억제한다)

  • Park, Hwa-Jin;Park, Kyeong-Mee;Rhee, Man-Hee;Park, Ki-Hyun
    • Journal of Ginseng Research
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    • v.17 no.2
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    • pp.135-138
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    • 1993
  • Aqueous fractions from Korean red ginseng inhibited the phosphorylations of 40 KD and 20 KD polypeptides which were induced by phorbol-12-myristate-13-acetate (100 nM) in human platelets. Much more carbohydrates were contained in the aqueous fractions than proteins. An aqueous fraction extracted with methanol, mainly, consists of glycoproteins, molecular weights of which were below 18 KD. We may infer that the aqueous fraction from Korean red ginseng do antitumorous and antiplatelet functions.

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Improvement of Haemostasis Mediated by Anti-Platelet Activities by Plant Vinegar (목초액의 혈소판 응집억제를 통한 혈행개선 작용에 관한 연구)

  • 김영대;배옥남;정승민;정진호
    • Toxicological Research
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    • v.20 no.2
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    • pp.137-142
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    • 2004
  • We investigated the effects of plant vinegar on platelets and blood coagulation system. Plant vinegar inhibited in vitro platelet aggregation in a concentration dependent manner, when platelets were activated by thrombin and collagen. In addition, plant vinegar showed inhibitory effects on the serotonin secretion induced by thrombin in a concentration dependent manner. However, treatment with plant vinegar to platelets did not induce any cytotoxicity, as determined by the release of lactate dehydrogenase. Plant vinegar did not change the coagulation parameters such as activated partial thromboplastin time (aPTT) and prothrombin time (PT) using rat citrated plasma. In vivo study revealed that, treatment with plant vinegar prolonged the bleeding time from mouse tail. All these results suggest that plant vinegar might improve blood hemostasis mediated via anti platelet activities.

Effects of Brazilin on the Phospholipase $A_2$ Activity and Changes on Intracellular Free Calcium Concentration in Rat Platelets

  • Hwang, Gwi-Seo;Kim, Ji-Young;Chang, Tong-Shin;Jeon, Sun-Duck;So, Dhong-Su;Moon, Chang-Kiu
    • Archives of Pharmacal Research
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    • v.21 no.6
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    • pp.774-778
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    • 1998
  • Brazilin [7,11b-dihydrobenz[b]indeno[1,2-d]pyran-3,6a,9,10(6H)-tetrol] inhibited thrombin-, collagen- and ADP-induced aggregation of washed rat platelets. T hrombin- and collagen-induced ATP release were also inhibited by brazilin in a concentration-dependent manner. Brazilin inhibited the formation of platelet thromboxane $A_2$ caused by thrombin, whereas it had no effect on the prostaglandin $D_2$ formation. Brazilin inhibited $^3H$-arachidonic acid liberation from membrane phospholipids of thrombin-stimulated platelets. Brazilin inhibited the rise of intracellular free calcium caused by thrombin. These results indicate that the inhibition of phospholipase ($PLA_2$) activity and [$[Ca^{2+}]_1$ elevation might be at least a part of antiplatelet mechanism of brazilin.

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Antiplatelet Action of Ilexoside D, a Triterpenoid Saponin from Ilex pubescens

  • Lee, Dug-Keun;Lee, Hye-Sun;Huh, Min-Do;Lee, Chul-Hoon;Lee, Young-Su;Kim, Hyun-Su;Han, Yong-Nam
    • Archives of Pharmacal Research
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    • v.14 no.4
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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.

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