• Title/Summary/Keyword: anti-platelet aggregation

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Inhibitory Effects of Euchrestaflavone B on Thrombus Formation via Regulation of Cyclic Nucleotides in Collagen-induced Platelets (콜라겐 유도의 혈소판에서 사이클릭 뉴클레오티드의 조절을 통한 Euchrestaflavone B의 혈전 형성 억제 효과)

  • Kwon, Hyuk-Woo
    • Korean Journal of Pharmacognosy
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    • v.51 no.4
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    • pp.231-237
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    • 2020
  • Euchrestaflavanone B (EFB) is a flavonoid that can be found in root bark, particularly in Cudrania tricuspidata (C. tricuspidata). The extract of C. tricuspidata is widespread throughout Asia and used in traditional medicine. In a previous study, we found anti-platelet effects of substances isolated from C. tricuspidata on collagen-induced human platelets. However, the C. tricuspidata still contains numerous substances, thus, we have searched new candidate, EFB isolated from C. tricuspidata for anti-platelet effect. Our results showed that EFA inhibited collagen-induced platelet aggregation and glycoprotein IIb/IIIa (αIIb/β3)-mediated signaling events, including platelet adhesion, granule secretion, thromboxane A2 production and clot retraction. These results suggest that EFA has inhibitory effects on human platelet activities and thrombus formation and has potential value as a natural substance for preventing platelet-induced thrombosis.

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.

Extracts from Rhizopus oryzae KSD-815 of Korean Traditional Nuruk Confer the Potential to Inhibit Hypertension, Platelet Aggregation, and Cancer Metastasis in vitro

  • Lee, Sang-Jin;Bae, Hyun-Jin;Ryu, Ji-Yeon;Lee, Dae-Young;Kim, Gye-Won;Baek, Na-Min;Kwon, Moo-Sik;Hong, Sung-Youl
    • Food Science and Biotechnology
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    • v.18 no.6
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    • pp.1423-1429
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    • 2009
  • Rhizopus oryzae KSD-815 was isolated from nuruk that has been used to make Korean traditional wines. This study was performed to investigate the effect of cultures of R. oryzae KSD-815 on cardiovascular disorders and cancer metastasis. Firstly, these cultures were sequentially fractionationed with n-hexane (TAHe), ethylacetate (TAE), n-butanol (TAB), and $H_2O$ (TAW). The TAE inhibited the activity of angiotensin-converting enzyme (ACE) and TAB suppressed platelet aggregation in vitro. TAE and TAB inhibited cell motility of human breast cancer cells. Furthermore, TAW interrupted the formation of neovasculature and tube-like structure, and down-regulated the expression of angiogenic factors, basic fibroblast growth factor (bFGF), tumor necrosis factor-$\alpha$ (TNF-$\alpha$), and hypoxia-inducible factor-$1{\alpha}$ (HIF-$1{\alpha}$) in breast cancer cells. These results indicated that cultures of R. oryzae KSD-815 display the inhibitory activities on hypertension, platelet aggregation, and metastasis, and suggest that these cultures might be further probed for the purposes as therapeutic agents or dietary supplements.

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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Anti-platelet Effect of the Phenolic Constituents Isolated from the Leaves of Magnolia obovata

  • Pyo, Mi-Kyung;Koo, Yean-Kyoung;YunChoi, Hye-Sook
    • Natural Product Sciences
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    • v.8 no.4
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    • pp.147-151
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    • 2002
  • In the course of our work on anti-platelet constituents from plants, eight phenolic compounds, $({\pm})-syringaresinol$ (1), 4-hydroxybenzaldehyde (2), 4-hydroxybenzoic acid (3), vanillic acid (4), 4-hydroxy cinnamic acid (5), quercetin 3-O-rhamnoside (6), rutin (7), and quercetin $3-(2^G-rhamnosylrutinoside)$ (8) were isolated from the methanol extract of the leaves of Magnolia obovata. The compounds were identified based on the spectroscopic data. Compound 2, 3, 5, 6, 7 and 8 were isolated for the first time from genus Magnolia. 1 and 6 showed same order of inhibitory potencies as acetylsalicylic acid (ASA) to rat platelet aggregation induced by all the stimulators tested. The remaining six compounds showed only mild effects.

Study on Anti-thrombotic Activities of KIOM2003-080 (KIOM2003-080 처방에 대한 항혈전 효능 연구)

  • Jeon, Won-Kyung;Kim, Ho-Kyoung;Lee, Ju-Hyun;Ko, Byoung-Seob;Lee, A-Yeong;Lee, Kyung-Goo;Shin, Hyeun-Kyoo
    • Korean Journal of Oriental Medicine
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    • v.13 no.2 s.20
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    • pp.143-148
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    • 2007
  • The present study examined inhibitory effects of 20 efficient experience prescriptions on platelet aggregation induced by collagen in human whole blood using the impedance method of aggregometry. Among them, a hot water extract of KIOM 2003-080 was selected to be the most effective candidate. In an in vivo study using a mouse acute thrombosis model, the anti-thrombotic effects of the KIOM2003-080 crude extract were also observed. In addition, we accessed bio-marker of platelet activation using thromboxane B2 by ELISA assay. A significantly decrease in thromboxane B2 production was seen in the presence of KIOM2003-080. Consequently, the results from this experiment provide pharmacological evidence for the traditional use of KIOM2003-080 prescription, suggesting that its hot water extracts could be used to prevent platelet aggregation and thrombosis disease.

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The Experimental Study on Anti-thrombotic Effect of Jogantanggagambang (JGTG) (조간탕가감방(調肝湯加減方)의 항혈전작용(抗血栓作用)에 대한 실험적(實驗的) 연구(硏究))

  • Lee, Seung-Ah;Lim, Hyun-Jung;Shin, Sun-Mi;Yoo, Dong-Youl
    • The Journal of Korean Obstetrics and Gynecology
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    • v.22 no.1
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    • pp.110-124
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    • 2009
  • Purpose: This study was performed to evaluate anti-thrombotic effect of Jogantanggagambang extract (JGTG). Methods: Blood flow rate through the regular volume of glass tube after the blood was diluted five times with ACD solution. Antithrombotic effect was calculated as a percentage of the experimental animal figure protected from the paralysis of hind legs or death of the mouse that was caused from the administration of platelet aggregation regent. Results: 1. JGTG inhibited the platelet aggregation induced by ADP, epinephrine, collagen and arachidonic acid as compared with the control group. 2. JGTG inhibited pulmonary embolism induced by collagen and epinephrine (inhibitory rate is 37.5%). 3. JGTG increased platelet number and fibrinogen amount significantly and also JGTG shortened PT and APTT significantly as compared with the control group in thrombus model induced by dextran. 4. JGTG increased blood flow rate significantly as compared with the control group in vivo. Conclusion: These results suggest that JGTG can be used for treating various female diseases caused by thrombosis.

The Experimental Study on Anti-thrombotic Effect of Cheongyeoljohyeoltangkamibang (CYJHT) (청열조혈탕가미방(淸熱調血湯加味方)의 항혈전작용(抗血栓作用)에 대한 실험적(實驗的) 연구(硏究))

  • Lee, Gui-Hee;Lim, Hyun-Jung;Shin, Sun-Mi;Yoo, Dong-Youl
    • The Journal of Korean Obstetrics and Gynecology
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    • v.22 no.1
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    • pp.79-94
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    • 2009
  • Purpose: This study was performed to evaluate anti-thrombotic effect of Cheongyeoljohyeoltangkamibang extract (CYJHT). Methods: Blood flow rate through the regular volume of glass tube after the blood was diluted five times with ACD soulution. Antithrombotic effect was calculated as a percentage of the experimental animal figure protected from the paralysis of hind legs or death of the mouse that is caused from the administration of platelet aggregation regent. Results: 1. CYJHT inhibited the platelet aggregation induced by ADP, epinephrine, collagen and arachidonic acid as compared with the control group. 2. CYJHT inhibited pulmonary embolism induced by collagen and epinephrine (inhibitory rate is 50%). 3. CYJHT increased platelet number and fibrinogen amount significantly and also CYJHT shortened PT and APTT significantly as compared with the control group in thrombus model induced by dextran. 4. CYJHT increased blood flow rate insignificantly as compared with the control group in vivo. Conclusion: These results suggest that CYJHT can be useful in treating various female diseases caused by thrombosis, such as menstrual pain, menstrual disorder and so on.

DK-MGAR101, an extract of adventitious roots of mountain ginseng, improves blood circulation by inhibiting endothelial cell injury, platelet aggregation, and thrombus formation

  • Seong, Hye Rim;Wang, Cuicui;Irfan, Muhammad;Kim, Young Eun;Jung, Gooyoung;Park, Sung Kyeong;Kim, Tae Myoung;Choi, Ehn-Kyoung;Rhee, Man Hee;Kim, Yun-Bae
    • Journal of Ginseng Research
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    • v.46 no.5
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    • pp.683-689
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    • 2022
  • Background: Since ginsenosides exert an anti-thrombotic activity, blood flow-improving effects of DK-MGAR101, an extract of mountain ginseng adventitious roots (MGAR) containing various ginsenosides, were investigated in comparison with an extract of Korean Red Ginseng (ERG). Methods: In Sprague-Dawley rats orally administered with DK-MGAR101 or ERG, oxidative carotid arterial thrombosis was induced with FeCl3 (35%), and their blood flow and occlusion time were measured. To elucidate underlying mechanisms, the cytoprotective activities on rat aortic endothelial cells (RAOECs) exposed to hydrogen peroxide (H2O2) were confirmed. In addition, the inhibitory activities of DK-MGAR101 and ERG on agonist-induced platelet aggregation, thromboxane B2 production, and ATP granule release from stimulated platelets as well as blood coagulation were analyzed. Results: DK-MGAR101 containing high concentrations of Rb1, Rg1, Rg3, Rg5, and Rk1 ginsenosides (55.07 mg/g) was more effective than ERG (ginsenosides 8.45 mg/g) in protecting RAOECs against H2O2 cytotoxicity. DK-MGAR101 was superior to ERG not only in suppressing platelet aggregation, thromboxane B2 production, and granule release, but also in delaying blood coagulation, FeCl3-induced arterial occlusion, and thrombus formation. Conclusions: The results indicate that DK-MGAR101 prevents blood vessel occlusion by suppressing platelet aggregation, thrombosis, and blood coagulation, in addition to endothelial cell injury.

Anti-thrombotic effects of ginsenoside Rk3 by regulating cAMP and PI3K/MAPK pathway on human platelets

  • Hyuk-Woo Kwon ;Jung-Hae Shin ;Man Hee Rhee ;Chang-Eun Park ;Dong-Ha Lee
    • Journal of Ginseng Research
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    • v.47 no.6
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    • pp.706-713
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    • 2023
  • Background and objective: The ability to inhibit aggregation has been demonstrated with synthetically derived ginsenoside compounds G-Rp (1, 3, and 4) and ginsenosides naturally found in Panax ginseng 20(S)-Rg3, Rg6, F4, and Ro. Among these compounds, Rk3 (G-Rk3) from Panax ginseng needs to be further explored in order to reveal the mechanisms of action during inhibition. Methodology: Our study focused to investigate the action of G-Rk3 on agonist-stimulated human platelet aggregation, inhibition of platelet signaling molecules such as fibrinogen binding with integrin αIIbβ3 using flow cytometry, intracellular calcium mobilization, dense granule secretion, and thromboxane B2 secretion. In addition, we checked the regulation of phosphorylation on PI3K/MAPK pathway, and thrombin-induced clot retraction was also observed in platelets rich plasma. Key Results: G-Rk3 significantly increased amounts of cyclic adenosine monophosphate (cAMP) and led to significant phosphorylation of cAMP-dependent kinase substrates vasodilator-stimulated phosphoprotein (VASP) and inositol 1,4,5-trisphosphate receptor (IP3R). In the presence of G-Rk3, dense tubular system Ca2+ was inhibited, and platelet activity was lowered by inactivating the integrin αIIb/β3 and reducing the binding of fibrinogen. Furthermore, the effect of G-Rk3 extended to the inhibition of MAPK and PI3K/Akt phosphorylation resulting in the reduced secretion of intracellular granules and reduced production of TXA2. Lastly, G-Rk3 inhibited platelet aggregation and thrombus formation via fibrin clot. Conclusions and implications: These results suggest that when dealing with cardiovascular diseases brought upon by faulty aggregation among platelets or through the formation of a thrombus, the G-Rk3 compound can play a role as an effective prophylactic or therapeutic agent.