• Title/Summary/Keyword: platelet aggregation inhibitory activity

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Anti-thrombosis Activity of the Aerial Part of Aruncus dioicus var kamtschaticus (눈개승마 지상부의 항혈전 활성)

  • Kim, Mi-Sun;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.24 no.5
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    • pp.515-521
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    • 2014
  • The oriental traditional medicine, Aruncus dioicus var kamtschaticus (ADK) is used for hemostasis (blood stopping) and the promotion of blood circulation. Recently, the demands of the aerial part of ADK as edible mountain herbs are rapidly increased due to its unique fragrance and bioactivity. In this study, to evaluate the anti-thrombosis activity of ADK, ethanol extract and organic solvent fractions were prepared from aerial parts of ADK, and their anticoagulation and anti-platelet aggregation activities were determined. In an anticoagulation activity assay, the ethanol extract of ADK increased the thrombin time, prothrombin time, and activated partial thromboplastin time (aPTT) 1.4-2.3 times at a concentration of 5 mg/ml. Among the fractions, the ethylacetate fraction showed strong inhibitory effects against blood clotting factors, as shown in an extension of the aPTT. In contrast, the butanol fraction strongly promoted blood clotting. In an anti-platelet aggregation assay, the activity of the ethanol extract was comparable to that of aspirin, a commercial anti-platelet aggregation agent, and the butanol fraction showed 2-fold higher aggregation inhibitory activity than aspirin. The aforementioned ethanol extract and active fractions have ignorable hemolytic activity against human red blood cells up to a concentration of 0.5 mg/ml. Considering the high content of total polyphenol, total flavonoid, and total sugar of the ethylacetate and butanol fractions, the purified active substances have potential as safe and novel anti-thrombosis agents. This report provides the first evidence of anti-thrombosis activity of ADK.

Benzylamides from Salvadora persica

  • Khalil, Ashraf Taha
    • Archives of Pharmacal Research
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    • v.29 no.11
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    • pp.952-956
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    • 2006
  • A phytochemical investigation of stems from Salvadora persica resulted in the first isolation of four benzylamides from a natural source. The isolated compounds were identified as butanediamide, $N^{1},\;N^{4}$-bis(phenylmethyl)-2(S)-hydroxy-butanediamide (1), N-benzyl-2-phenylacetamide (2), N-benzylbenzamide (3) and benzylurea (4). The structure elucidation was accomplished using spectroscopic methods, especially 2D NMR and HREIMS. Compound 2 revealed a significant inhibitory effect on human collagen-induced platelet aggregation, and a moderate antibacterial activity against Escherichia coli.

Ethoxy-hydroxy-benzoic Acid; A Platelet Antiaggregating Substance from Acanthopanacis Cortex (오가피로부터 혈소판 응집억제작용 물질 Ethoxy-hydroxy-benzoic Acid의 분리)

  • Yun, Hye-Sook;Kim, Sun-Ok;Kim, Jae-Hoon;Cho, Han-Ik
    • Korean Journal of Pharmacognosy
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    • v.14 no.4
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    • pp.175-177
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    • 1983
  • The BuOH fraction prepared from the methanol extract of Acanthopanacis Cortex showed inhibitory activity against ADP-induced platelet aggregation. The inhibitory activity remained in ether layer when the BuOH fraction was refluxed with 5% aq. HCl-EtOH (1 : 1 mixture) and extracted with ether. From the ether layer, ethoxy-hydroxy-benzoic acid $(m.p.\;128{\sim}130^{\circ}C)$, a platelet antiaggregating substance, was isolated.

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Cordycepin (3'-deoxyadenosine) Has an Anti-platelet Effect by Regulating the cGMP-Associated Pathway of Human Platelet Activation

  • Cho, Hyun-Jeong;Rhee, Man-Hee;Cho, Jae-Youl;Kim, Hyeong-Soo;Ok, Woo-Jeong;Kang, Hee-Jin;Park, Hwa-Jin
    • Preventive Nutrition and Food Science
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    • v.12 no.3
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    • pp.141-147
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    • 2007
  • Cordycepin (3'-deoxyadenosine), which comes from Cordyceps militaris, the Chinese medicinal fungal genus Cordyceps, is used in the treatment of various diseases such as cancer and chronic inflammation. We recently reported that cordycepin has a novel antiplatelet effect through the down regulation of $[Ca^{2+}]_{i}$ and the elevation of cGMP/cAMP production. In this study, we further investigated the effect of cordycepin on collagen-induced platelet aggregation in the presence of cGMP-dependent protein kinase (PKG)- or cAMP-dependent protein kinase (PKA)-inhibitor. PKG inhibitor Rp-8-pCPT-cGMPS potentiated the collagen-induced platelet aggregation, but PKA inhibitor Rp-8-Br-cAMPS did not. However, both Rp-8-pCPT-cGMPS and Rp-8-Br-cAMPS reduced inhibition by cordycepin of collagen-induced platelet aggregation. Moreover, cordycepin inhibited $Ca^{2+}-dependent$ phosphorylation of both 47 kDa- and 20 kDa-protein in the presence of both PKG inhibitor and PKA inhibitor. Taken altogether, these results suggest that the inhibitory effect of cordycepin on collagen-induced platelet aggregation is associated with cGMP/PKG- and cAMP/PKA-pathways, and thus cordycepin may be an efficacious intervention against platelet aggregation-mediated thrombotic disease.

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.

Effects of Sparganii Rhizoma Processed on Rat Lens Aldose Reductase and Anti-oxidant Activities (흑삼릉의 수치에 따른 Aldose Reductase 및 항산화활성에 미치는 영향)

  • 정상훈;신국현;신현경;임순성
    • YAKHAK HOEJI
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    • v.48 no.5
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    • pp.291-296
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    • 2004
  • Sparganium stoloniferum Buch.-Ham. (Sparganiaceae) is a perennial herb which has been used as treatments for menstrual disorder, galactagogue and endometriosis in folk remedies. The Sparganii Rhizoma processed, heated with vinegar, used to different purpose compared with origin in medicine. In order to estimate the different effects between processed (PSR) and unprocessed (USR) Sparganii Rhizoma, extraction and systemic fractionation of the rhizomes were archived. Inhibitory effects of the extracts as well as the fractions of PSR and USR on rat lens aldose reductase and on rat platelet aggregation were investigated for the prevention or the treatment of chronic diabetic complications. Their antioxidant effects, measured using lipid peroxidation of liver tissue and radical scavenging activities on 1,1-diphenyl-picrylhydrazyl in vitro, were evaluated. The most of biological activities tested except rat platelet aggregation, fractions from PSR were shown to exhibit stronger activities than those from USR. It seems that caused by changing of the chemical components by heating process in conditioned with acetic acid. Compounds isolated were shown to significant inhibitory activity on rat lens aldose reductase. Inhibitory activity of compounds isolated on rat lens aldose reductase have been tested in vitro. $IC_{50}$/ (6.31 $\mu$M) of cerebroside I (V) was nearly equal to that (6.32 $\mu$M) of a reference compound, tetrametbylene glutaric acid (TMG).

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.

The inhibitory mechanism of crude saponin fraction from Korean Red Ginseng in collagen-induced platelet aggregation

  • Jeon, Bo Ra;Kim, Su Jung;Hong, Seung Bok;Park, Hwa-Jin;Cho, Jae Youl;Rhee, Man Hee
    • Journal of Ginseng Research
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    • v.39 no.3
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    • pp.279-285
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    • 2015
  • Background: Korean Red Ginseng has been used as a traditional oriental medicine to treat illness and to promote health for several thousand years in Eastern Asia. It is widely accepted that ginseng saponins, ginsenosides, are the major active ingredients responsible for Korean Red Ginseng's therapeutic activity against many kinds of illness. Although the crude saponin fraction (CSF) displayed antiplatelet activity, the molecular mechanism of its action remains to be elucidated. Methods: The platelet aggregation was induced by collagen, the ligand of integrin ${\alpha}_{II}{\beta}_I$ and glycoprotein VI. The crude saponin's effects on granule secretion [e.g., calcium ion mobilization and adenosine triphosphate (ATP) release] were determined. The activation of mitogen-activated protein kinases (MAPKs), including extracellular signal-regulated protein kinase 1/2 (ERK1/2), c-Jun N-terminal kinases (JNKs), and p38 MAPK, and phosphoinositide 3-kinase (PI3K)/Akt was analyzed by immunoblotting. In addition, the activation of integrin ${\alpha}_{II}b{\beta}_{III}$ was examined by fluorocytometry. Results: CSF strongly inhibited collagen-induced platelet aggregation and ATP release in a concentration-dependent manner. It also markedly suppressed $[Ca^{2+}]_i$ mobilization in collagen-stimulated platelets. Immunoblotting assay revealed that CSF significantly suppressed ERK1/2, p38, JNK, PI3K, Akt, and mitogen-activated protein kinase kinase 1/2 phosphorylation. In addition, our fraction strongly inhibited the fibrinogen binding to integrin ${\alpha}_{IIb}{\beta}_3$. Conclusion: Our present data suggest that CSF may have a strong antiplatelet property and it can be considered as a candidate with therapeutic potential for the treatment of cardiovascular disorders involving abnormal platelet function.

Synthesis of Substituted Cinnamoyl-tyramine Derivatives and their platelet Anti-aggregatory Activities

  • Woo, Nam-Tae;Jin, Sun-Yong;Cho, Jin-Cho;Kim, Nam-Sun;Bae, Bae-Eun-Hyung;Han, Ducky;Han, Byung-Hoon;Kang, Young-Hwa
    • Archives of Pharmacal Research
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    • v.20 no.1
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    • pp.80-84
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    • 1997
  • Substituted cinnamoyl-tyramine derivatives were synthesized by DCC-coupling of substituted cinnamic acid with tyramine or tyramine methyl-1-ether to evaluate PAF-receptor binding antagonistic activities and inhibitory activities on PAF-induced platelet aggregation with interest on structure-activity relations. The results show that 3,4-dimethoxy-cinnamoyl tyramine-amide or its methyl ether have significant PAF-receptor binding antagonistic activity and platelet anti-aggregatory activities.

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The Antithrombotic and Fibrinolytic Effect of Natto in Hypercholesterolemia Rats

  • Park, Kum-Ju;Kang, Jung-Il;Kim, Tae-Seok;Yeo, Ik-Hyun
    • Preventive Nutrition and Food Science
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    • v.17 no.1
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    • pp.78-82
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    • 2012
  • Antithrombotic and fibrinolytic activity of natto was evaluated on platelet aggregation in vitro and in vivo. Natto showed inhibitory effects on platelet aggregation induced by adenosine 5’diphosphate (ADP) and collagen. Orally administered natto also showed fibrinolytic activity in hypercholesterolemia rats. Normal levels of natto, when administered for four weeks, shortened euglobulin clot lysis time (ECLT) and prolonged partial thromboplastin time (PATT) significantly compared to non-treated group. In addition, the natto treatment decreased total cholesterol in serum. These results showed that intake of normal levels of natto can elicit antithrombotic and fibrinolytic effects, suggesting its consumption may improve blood circulation.