• Title/Summary/Keyword: anti-platelet aggregation

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Gallocatechin Gallate Inhibits Platelet Aggregation by Arachidonic Acid Liberation and $TxA_2$ Synthase Activity

  • Cho, Mi-Ra;Lee, Kyung-Sup;Lee, Jung-Jin;Jin, Yong-Ri;Son, Dong-Ju;Yun, Yeo-Pyo
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.78.2-78.2
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    • 2003
  • We have previously reported that green tea catechins (GTC) displayed anti-thrombotic activity, and that this might be due to anti-platelet rather than anti-coagulation effects. In the present study, we have studied the anti-platelet activity and mechanism of gallocatechin gallate (GCG), which is a component of GTC. GCG inhibited the collagen- and U46619-induced aggregation of rabbit platelets, with IC$\^$50/ values of 63.0 and 48.3 ${\mu}$M, respectively. GCG also inhibited collagen-induced serotonin release and TxB$_2$ formation in a similar manner of platelets aggregation. (omitted)

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Pharmacological actions of morusinol on modulation of platelet functions via integrin αIIb/β3 signaling

  • Hyuk-Woo Kwon
    • Journal of Applied Biological Chemistry
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    • v.66
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    • pp.171-178
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    • 2023
  • Morus alba, a popular medicinal plant belonging to the family Moraceae, has long been used commonly in traditional medicine and has various physiological activities, including antidiabetic, anti-microbial, diuretic, anti-oxidant, and anti-cancer activities. Morusinol was isolated from the root bark of M. alba; however, its biological effects have not yet been reported. Therefore, we examined the inhibitory effects of morusinol on human platelet aggregation, Ca2+ mobilization, and αIIb/β3 activity. Our data showed that collagen-induced human platelet aggregation was inhibited by morusinol without cytotoxicity. In this study, we examined whether morusinol inhibits platelet aggregation through the regulation of integrin αIIb/β3 and its associated signaling molecules. We observed that morusinol inhibited αIIb/β3 activation by regulating vasodilator-stimulated phosphoprotein, phosphatidylinositol-3 kinase, Akt (protein kinase B), and glycogen synthase kinase-3α/β. These results show that morusinol inhibited fibronectin adhesion, fibrinogen binding, and clot retraction. Taken together, morusinol shows strong antiplatelet and anti-clot retraction effects and is a potential therapeutic drug candidate to prevent platelet-related thrombosis and cardiovascular disease.

Anti-platelet Aggregation Effect of Cheongpyesagan-tang In Vitro (청폐사간탕(淸肺瀉肝湯)의 혈소판 응집억제 작용에 대한 in vitro 연구)

  • Park, Young-Ju;Kim, Seul-Ji;Yang, Ga-Eun;Lee, Mi-Jung;Lee, Ji-Sook;Kang, Deok-Hui;Kim, Young-Chan;Lee, Woo-Kyung;Ryu, Jae-Hwan
    • The Journal of Internal Korean Medicine
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    • v.31 no.4
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    • pp.714-721
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    • 2010
  • Objective : The study was designed to test the anti-platelet effect of the extract Cheongpyesagan-tang and compare it with aspirin in vitro. Methods : The extract from Cheongpyesagan-tang was made by the pharmacy department of Kyung Hee Oriental Medical Hospital. The extract was investigated for inhibition against the collagen induced aggregation of human platelet suspensions on aggregometry. Aspirin and aspirin-Cheongpyesagan-tang were investigated together. Results : 1. In collagen induced human platelet aggregation test, the extract from Cheongpyesagan-tang significantly inhibited in concentration 30mg/ml (p<0.05), 40mg/ml, 50mg/ml (p<0.001) and the effect depended on concentration over 20mg/ml. 2. Aspirin and aspirin-Cheongpyesagan-tang inhibited collagen induced human platelet aggregation significantly (p<0.001). Aspirin-extract of Cheongpyesagan-tang inhibition rate was higher than aspirin only (p<0.05). Conclusions : The extract of Cheongpyesagan-tang has anti-platelet aggregation and synergic effect with aspirin on human platelet in vitro.

Platelet Anti-Aggregating Plant Materials

  • YunChoi, Hye-Sook;Kim, Jae-Hoon;Kim, Sun-Ok;Lee, Jong-Ran
    • Korean Journal of Pharmacognosy
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    • v.17 no.2
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    • pp.161-167
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    • 1986
  • The smear method developed by Velaskar and Chitre was modified to allow the screening of plant extracts and/or fractions for platelet anti-aggregating activity. The modified smear method was also found suitable for massive screening of pure compounds. Sample fractions prepared from various plant extracts were examined for their effects against ADP, arachidonic acid (AA) or collagen induced platelet aggregations. Several solvent fractions of plant extracts including water fraction prepared from the methanol extract of Acanthopanax sp. was inhibitory against rat platelet aggregations. The activity guided treatments and fractionations of the water fraction from A. senticosus Max yielded two anti-platelet aggregatory substances, 3, 4-dihydroxybenzoic acid (I) and its artefact ethyl 3, 4-dihydroxybenzoate(II). The inhibitory activities of I and II against rat platelet aggregation were compared with that of aspirin, a known inhibitor of platelet aggregation. Discussions also included the results of the investigations on the structural activity relationships among the various dihydroxybenzoic acid derivatives against platelet aggregations induced by either one of ADP, AA or collagen.

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Ethyl Acetate Extract from Tissue-Cultured Mountain Ginseng Adventitious Roots Inhibits In Vitro Platelet Aggregation in Whole Human Blood and Augments Peripheral Blood Flow in Mice

  • Lee, In-Sun;Kim, Seul-Ki;Jeon, Min-Hwa;Jeon, Won-Kyung
    • Journal of Ginseng Research
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    • v.35 no.4
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    • pp.442-448
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    • 2011
  • We previously reported that in vitro anti-platelet activity of tissue-cultured mountain ginseng (TCMG) ethanol extracts show improved efficacy when compared with commercial ginseng products such as Korean red ginseng and Panax ginseng. However, information on the anti-platelet activity of the ethyl acetate fraction from TCMG adventitious roots is limited. Therefore, in this study, we further investigated the effects of an ethyl acetate extract of TCMG (EA-TCMG) adventitious roots on in vitro antiplatelet activity in whole human blood and its effect on peripheral blood flow in mice. We found that EA-TCMG inhibited platelet aggregation with $IC_{50}$ values of 271, 180, and 147 ${\mu}g$/mL induced by collagen, adenosine-5'-diphosphate, and arachidonic acid, respectively. Among the three agonists used, thromboxane $A_2$ formation induced by arachidonic acid was markedly suppressed. Furthermore, EA-TCMG improved the peripheral circulatory disturbance by improving vascular blood flow. In conclusion, these results suggest that ethyl acetate extracts from TCMG adventitious roots might inhibit vascular platelet aggregation and thrombus formation.

Inhibitory Effects of Scopoletin in Collagen-induced Human Platelet Aggregation (콜라겐으로 유도한 사람 혈소판 응집에 미치는 Scopoletin의 억제 효과)

  • Kwon, Hyuk-Woo;Shin, Jung-Hae;Park, Chang-Eun;Lee, Dong-Ha
    • Korean Journal of Clinical Laboratory Science
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    • v.51 no.1
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    • pp.34-41
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    • 2019
  • Platelet aggregation is essential for the formation of a hemostatic plug in the case of blood vessel damage. On the other hand, excessive platelet aggregation may cause cardiovascular disorders, such as thrombosis, atherosclerosis, and myocardial infarction. Scopoletin, which found in the root of plants in the genus Scopolia or Artemisia, has anti-coagulation and anti-malaria effects. This study examined the effects of scopoletin on human platelet aggregation induced by collagen. Scopoletin had anti-platelet effects via the down-regulation of thromboxane $A_2$ ($TXA_2$) production and intracellular $Ca^{2+}$ mobilization ($[Ca^{2+}]_i$), which are aggregation-inducing molecules produced in activated platelets. On the other hand, scopoletin increased both the cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) levels, which are known as intracellular $Ca^{2+}$-antagonists and aggregation-inhibiting molecules. In particular, scopoletin increased the potently cAMP level more than cGMP, which led to suppressed fibrinogen binding to ${\alpha}IIb/{\beta}_3$ in collagen-induced human platelet aggregation. In addition, scopoletin inhibited collagen-elevated adenosine triphosphate (ATP) release in a dose-dependent manner. The results suggest that aggregation amplification through granule secretion is inhibited by scopoletin. Therefore, scopoletin has potent anti-platelet effects and may have potential for the prevention of platelet-derived vascular diseases.

Platelet Anti-aggregating Triterpene and Sterol Constituents from the Leaves of Acanthopanax senticosus

  • Jin, Jing-Ling;Lee, Sang-Hyun;Lee, Yong-Yook;Kim, Jeong-Mi;Heo, Jung-Eun;YunChoi, Hye-Sook
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.206.1-206.1
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    • 2003
  • From methanol extract of Acanthopnanax senticosus, six platelet anti-aggregating compounds, chiisanogenin (1), chiisanoside (2), ursolic acid (3), oleanolic acid (4), b-sitosterol (5) and daucosterol (6) were isolated. All of the isolated compounds showed dose-dependent inhibitory activities to rat platelet aggregation induced by all the agonist employed. Compound 1 showed about 50 folds higher potency than acetylsalicylic acid (ASA) on U46619 induced platelet aggregation (IC$\sub$50/ : 6.21 ${\mu}$M) and 10 ∼ 20 folds higher effect than ASA on epinephrine and arachidonic acid (AA) induced aggregation (IC$\sub$50/ ; 2.50 and 4.81 ${\mu}$M, respectively). (omitted)

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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.

Experimental Study of Ginkgo-Chunghyul-dan on Anti-oxidant, Anti-platelet Aggregation, and Anti-hyperlipidemic Activity

  • Yun, Sang-Pil;Bae, Hyung-Sup;Park, Seong-Uk;Jung, Woo-Sang;Moon, Sang-Kwan;Park, Jung-Mi;Ko, Chang-Nam;Cho, Ki-Ho;Kim, Young-Suk
    • 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.

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