• Title/Summary/Keyword: inhibition of platelet aggregation

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Antiplatelet Activity of 2-(4-Cyanophenyl) amino-1,4-naphthalenedione-3-pyridinium perchlorate (PQ5) (2-(4-시아노페닐) 아미노 -1,4-나프탈렌디온-3-피리디니움 퍼클로레이트 (PQ5)의 항혈소판작용)

  • 김도희;이수환;최소연;문창현;문창현;김대경;유충규
    • YAKHAK HOEJI
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    • v.43 no.6
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    • pp.809-817
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    • 1999
  • The effect of 2-(4-cyanophenyl)amino-1,4-naphthalenedione-3-pyridinium perchlorate (PQ5) on pla-telet aggregation and its action mechanisms were investigated with rat platelet. PQ5 inhibited the platelet aggregation induced by collagen ($6{\;}{\mu\textrm{g}}/ml$), thrombin (0.4 U/ml) and A23187 ($3{\mu}M$) in concentration-dependent manner with $IC_{50}$ values of 5.50, 25.89 and $37.12{\;}{\mu}M$, respectively. PQ5 also significantly reduced the thromboxane $A_2$ (TXA2) formation in a concentration dependent manner. The collagen-induced arachidonic acid (AA) release in [-3H]-AA incorporated platelet, an indication of the phospholipase $A_2$ activity, was decreased by PQ5 pretreatment PQ5 significantly inhibited the activity of thormboxane synthase only at high concentration ($100{\mu}M$), but did not affect the cyclooxygenase activity at all. Collagen-induced ATP release was significantly reduced by PQ5. Calcium-induced platelet aggregation experiment suggests that the elevation of intracellular free $Ca^{2+}$ concentration ($[Ca^{2+}]_i$) by collagen stimulation is decreased by the pretreatment of PQ5, which is due to the inhibition of calcium release from intracellular store and influx from outside of the cell. PQ5 did not showed the effect of anticoagulation as prothrombin time (PT) or activated partial thromboplastin time (APTT). Form these results, it is suggested that PQ5 exerts its antiplatelet activity through the inhibition of the intracellular $Ca^{2+}$ mobilization and the decrease of the $TXA_2$ synthesis.

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Pharmacological Effects of Asaronaldehyde Isolated from Acorus gramineus Rhizome

  • Kim, Hyo-Gyung;Jeon, Ju-Hyun;Kim, Moo-Key;Lee, Hoi-Seon
    • Food Science and Biotechnology
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    • v.14 no.5
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    • pp.685-688
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    • 2005
  • Antibacterial and antiplatelet activities of Acorus gramineus rhizome-derived asaronaldehyde and asaron were analyzed using platelet aggregometer and six human intestinal bacteria. Active constituent of A. gramineus rhizome was isolated and characterized as asaronaldehyde by spectral analyses. At 2 and 1 mg/disk, asaronaldehyde exhibited strong inhibition of Clostridium perfringens and C. difficile without adverse effects on growth of beneficial bacteria such as Bifidobacterium bifidum, Lactobacillus acidophilus, and L. casei. Asaron also revealed moderate growth inhibition against C. perfringens and C. difficile at 2 mg/disk, no growth-inhibiting activity was observed on B. bifidum, L. acidophilus, L. casei, and E. coli. At 50% inhibitory concentration ($IC_{50}$) value, asaronaldehyde was effective in inhibiting platelet aggregation induced by collagen ($IC_{50}$, $27.6\;{\mu}M$) and arachidonic acid ($IC_{50}$, $53.7\;{\mu}M$). These results suggest asaronaldehyde may be useful as lead compound for inhibiting platelet aggregation induced by collagen and arachidonic acid.

Study on Anti-thrombotic Activity, Superoxide Generation in Human Neutrophils and Platelet Aggregation in Human Blood of Hwao-tang

  • Park Won Hwan;Park Soo Young;Park Tae Woo;Kim Jong Gu;Kim Seog Ha;Kim Cherl Ho
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.18 no.5
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    • pp.1494-1504
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    • 2004
  • The present paper reports the effects of Hwaotang an atherosclerosis using a spontaneous experimental model, We have also investigated the pharmacological effect of Hwaotang on collagen- and ADP-induced blood platelet aggregation, thrombin-induced conversion of fibrinogen and fibrinolysis in in vitro experiments, and various effects on stimuli-induced superoxide generation in human neutrophils. Hwao-tang was shown to have inhibitory effect on collagen- and ADP-induced blood platelet aggregation, on thrombin-induced conversion of fibrinogen to fibrin and on the activity of plasminogen or plasmin. Hwao-tang also significantly inhibited fMLP-induced superoxide generation in a concentration-dependent manner, but not that induced by arachidonic acid. Hwao-tang inhibited neutrophil functions, including degranulation, superoxide generation, and leukotriene B4 production, without any effect on 5-lipoxygenase activity. In conclusion, the protection of extracts of Hwao-tang on the ischemic infarction induced artificially might be involved to their inhibition of thrombotic action. The results also indicate that Hwao-tang exerts the effects on superoxide generation related to the inhibition of neutrophil functions.

Euchrestaflavanone A can attenuate thrombosis through inhibition of collagen-induced platelet activation

  • Shin, Jung-Hae;Kwon, Hyuk-Woo
    • Journal of Applied Biological Chemistry
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    • v.63 no.4
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    • pp.339-345
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    • 2020
  • Euchrestaflavanone A (EFA) is a flavonoid found in the root bark of Cudrania tricuspidata. C. tricuspidata extract, widely used throughout Asia in traditional medicine, has been investigated phytochemically and biologically and is known to have anti-obesity, anti-inflammatory, and anti-tumor effects. It has been reported that C. tricuspidata extract also possesses anti-platelet effects; however, the mechanism of its anti-platelet and anti-thrombotic activities is yet to be elucidated. In this study, we investigated the effects of EFA on the modulation of platelet function using collagen-induced human platelets. Our results showed that EFA markedly inhibited platelet aggregation. Furthermore, it downregulated glycoprotein IIb/IIIa (αIIb/β3)-mediated signaling events, including platelet adhesion, granule secretion, thromboxane A2 production, and clot retraction, but upregulated the cyclic adenosine monophosphate-dependent pathway. Taken together, EFA possesses strong anti-platelet and anti-thrombotic properties and is a potential therapeutic drug candidate to prevent platelet-related thrombosis and cardiovascular disease.

A Study of Mechanism Involved in Cadmium-induced Platelet Aggregation

  • Song Cheul-Soo;Hong Ki-Whan
    • The Korean Journal of Pharmacology
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    • v.20 no.1 s.34
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    • pp.41-46
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    • 1984
  • Cadmium (Cd) was administered by a series of weekly intraperitoneal injections at dose of 2mg/kg in rabbits and rats. The levels of malondialdehyde (MDA) and thromboxane $B^2(TXB_2)$ in platelet-rich plasma from Cd-poisoned animals were significantly higher than those of the control group. Furthermore, the inhibition of 6-keto-prostaglandin $F_{1{\alpha}}$, production in Cd-treated aorta ring was inversely related to the enhancement of platelet aggregation. These results suggest that Cd not only inhibits prostacyclin synthesis in the arterial endothelium, but also stimulates the platelet aggregation by enhancing thromboxane AZ production. These findings are assumed to support the evidence of an effect of Cd toxicity on the vascular wall and platelet function in raising arteriall pressure.

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The Biological Activity of Deer Antler Extract in vitro (In vitro에 의한 녹용 추출물의 생리 활성 효과)

  • Lee, Kyung-Ae;Chung, Hae-Young
    • The Korean Journal of Food And Nutrition
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    • v.20 no.2
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    • pp.114-119
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    • 2007
  • Our research objective was to examine the in vitro biological activity of deer antler(Nogyong in Korean) extract, including the antioxidative, nitrite scavenging, and tyrosinase inhibitory effects, as well as the antithrombotic, and angiotensin I converting enzyme(ACE) inhibitory activities. The carbohydrate, protein, fat, and mineral contents of the deer antler were 7.6%, 65.3%, 3.2% and 23.9%, respectively. The electron donating ability(EDA) by the reduction of 2,2'-diphenyl-1-picrylhydrazyl(DPPH) was 67.1%, and the inhibition rate of lipid peroxidation by the thiocyanate method using linoleic acid was 92.1% in 100 mg/ml of extract. The nitrite scavenging effects were pH dependent, and were highest at pH 1.2 and lowest at pH 6.0. The sample inhibition rate against tyrosinase was above 64.0%. The platelet aggregation induced by ADP(adenosine-5'diphosphate) was inhibited up to 51.7%, and the inhibitory effect was dependent on the sample concentration. Lastly, the inhibition rate of ACE was 47.5% in 100 mg/ml of deer antler extract.

Antiplatelet Effects of Garlic and Chitosan: a Comparative Study between Fermented and Non-Fermented Preparations

  • Irfan, Muhammad;Kim, Minki;Kwon, Hyuk-Woo;Rhee, Man Hee;Kim, Hyun-Kyoung
    • Biomedical Science Letters
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    • v.24 no.3
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    • pp.280-284
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    • 2018
  • 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. Chitosan is a natural polysaccharide obtained from chitin, and derivatives of chitosan have been shown to inhibit platelet aggregation and adhesion. 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.

Effect of Silsosangami on Platelet Aggregation, Hemolysis and Inducible Nitric Oxide Synthase

  • Kim Chang Hwan;Kim Han Geu;Ahan Jong Chan;Lee Soo Kyung;Chung Tae Wook;Kim June Ki;Choi Dall Yeong;Kim Cherl Ho;Park Won Hwan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.16 no.6
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    • pp.1277-1283
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    • 2002
  • Silsosangami(SSG) is a formula of treaditional korean medicines as an effective biological response modifier for augmenting host homeostasis of body circulation. Little is known of the biological activity of SSG and previous studies have focused mainly on their anti-thrombosis8). There is a growing interest in the pharmacological potential of the SSG due to the recent finding by our group that SSG and each constituent herbs of SSG were able to inhibit NO and prostaglandin E2 (PGE2) synthesis in murine peritoneal macrophages stimulated with bacterial endotoxin. In this paper, the effects of SSG on platelet aggregation and hemolysis in human blood were studied. SSG provoked remarkable inhibiting effect on platelet aggregation, and APTT were sensitive to the presence of this SSG. Using an in vitro system, APTT was delayed with the increment of the concentrations of these seven compounds. These results suggested that SSG might be used as a novel antithrombotic therapeutic agents in post-myocardial infarction. A SSG reduced NO production in mouse peritoneal macrophages stimulated with lipopolysaccharide, without the influence on the activity of iNOS being observed. SSG significantly reduced mouse paw edema induced by carrageenan. Western blot analysis showed that SSG reduced the expression of iNOS. The results indicate that SSG exerts anti-inflammatory effects related to the inhibition of NO production, which could be due to a decreased expression of iNOS.

The Effect of Capsosiphon fulvecense extract on Inhibition of Platelet Aggregation and Serum Lipid Level in Ovariertomized Rats (매생이 추출물이 난소를 절제한 흰쥐의 혈소판 응집과 혈청 내 지질 조성에 미치는 영향)

  • Park Mi-Hwa;kim Mihyang
    • Journal of Life Science
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    • v.15 no.6 s.73
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    • pp.1028-1033
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    • 2005
  • Estrogen deficiency in peri-and postmenopausal women results in variety of neurovegetative, psychic and somatic symptoms, and may contribute to severe diseases within the aged female population. Capsosiphon fulvecense (CF), green algae, loaded with large amount of proteins, calcium and ion. This seaweed is distributed in the Southern coast in Korea and widely throughout the world. Our objective was to investigate the effects of Capsosiphon fulvecense (CF) extract on serum lipid concentration and platelet aggregation in ovariectomized rats. Three groups were surgically ovariectomized (OVX). The fourth group was sham operated. Sprague-Dawley female rats were randomly assigned to the following groups : sham-operated rats (Sham), ovariectomized control rats (OVX-Control), ovariectomized rats supplemented with CF at 50mg/kg bw/d (OVX-CF5O) and ovariectomized rats supplemented with CF at 200mg/kg bw/d (OVX-CF200). The serum triglyceride level was significantly decreased after supplemented with the CF extracts. The serum HDL-cholesterol level in the OVX-CF group was significantly higher than the level in the OVX-control group. The ability of platelet aggregation treated with CF extract (CF group) was $7\%$ less than OVX-control group. Taken these together, CF extract may be used to improve the quality of life in menopausal women.

Anti-thrombosis Activities of the Root Extract of Moringa oleifera Lam (모링가 지하부의 항혈전 활성)

  • Kwon, Chong Suk;Sung, Hwa-Jung;Sohn, Ho-Yong
    • Microbiology and Biotechnology Letters
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    • v.47 no.1
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    • pp.20-24
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    • 2019
  • Moringa oleifera Lam (MOL) has been used as a traditional medicine to treat various cancers and inflammation. Whereas the bioactivities of the MOL leaf and seed are well reported, the study of the root is still rudimentary. In this study, the ethanol extract of MOL (EEMOL) and its subsequent organic solvent fractions were prepared and their anticoagulation activity in vitro and platelet aggregation inhibitory activity were evaluated. The EEMOL had negligible anticoagulation and strong platelet aggregation activities. However, the hexane and ethyl acetate fractions of EEMOL showed significant inhibition against thrombin, prothrombin, coagulation factors, and platelet aggregation, without hemolytic activity up to 1.0 mg/ml. Our results suggest that the active fractions of MOL root have potential as new anti-thrombosis agents.