• Title/Summary/Keyword: platelet aggregation inhibitory activity

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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.

Preventive Effects of Peony Root Extracts on Oxidative Stress, Thrombosis and Atherosclerosis (백작약 추출물이 항산화활성, LDL 산화 억제 및 혈전용해에 미치는 영향)

  • Park, Soon-Gi;Lee, Min-Ja;Jung, Hyun-Jung;Lee, Hye-Sook;Kim, Hyuck;Na, Sun-Taek;Park, Sun-Dong;Park, Won-Hwan
    • The Journal of Korean Medicine
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    • v.30 no.2
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    • pp.88-103
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    • 2009
  • Objectives: There is currently increased interest in the identification of natural antioxidant compounds derived from various plants. Peony Root (PR) is used worldwide for the treatment of many types of cardiovascular disease including atherosclerosis and hypertension. It has been used in Korean traditional medicine for the treatment of glycosuria, hypertension and cancer. However, to date, no studies concerning the antioxidant properties of PR have been conducted. Therefore, this study was conducted to evaluate the in vitro scavenging activity, inhibitory effect of LDL oxidation of pro-oxidant reactive species and anti-thrombosis effect in response to treatment with PR using various screening methods including biological and non-biological oxidants. Methods: In this study, the antioxidant activity of extract from PR was studied with in vitro methods by measuring the antioxidant activity by TEAC, measuring the scavenging effects on reactive oxygen species (ROS) [superoxide anion, hydroxyl radical] and on reactive nitrogen species (RNS) [nitric oxide and peroxynitrite] as well as measuring the inhibitory effect on $Cu^{2+}$-induced human LDL oxidation and the inhibitory effect on collagen-induced platelet aggregation. Results: The PR extracts were found to have a potent scavenging activity of oxidative stress [DPPH, superoxide anion, hydroxyl radical, nitric oxide and peroxynitrite, etc.] as well as an inhibitory effect on LDL oxidation and on platelet aggregation. Conclusions: The PR extracts have anti-oxidative and anti-atherosclerotic effects in vitro system, which can be used for developing pharmaceutical drugs against oxidative stress and atherosclerosis.

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A Trend of Yin-tonifying Formulas Compared with Yang-tonifying Formulas on Anti-platelet and Anti-thrombotic Activity

  • Jeon, Won-Kyung;Yoo, Bo-Kyung;Ahn, Sang-Young;Lee, Ju-Hyun;Ahn, Sang-Woo;Ko, Byoung-Seob
    • The Journal of Korean Medicine
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    • v.30 no.6
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    • pp.1-8
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    • 2009
  • Objectives: Formulas for treatment of yin or yang deficiency conditions have been commonly used in traditional Korean medicine. The aim of this study is to examine the possible inhibitory effects of yin- or yang-tonifying formulas on in vivo anti-platelet activity and in vivo anti-thrombotic activity. Methods: We tested the effects of 26 types of yin- or yang-tonifying formulas on platelet aggregation induced by collagen in human whole blood using the impedance method of aggregometry and accessed a biomarker of platelet activation using thromboxane $B_2$ immunoassay. We also tested the anti-thrombotic effects of effective candidates on experimental models of thrombosis in mice. Results: 3 types of yin-tonifying formulas and 3 types of yin-yang-tonifying formulas were selected to be the most effective candidates (p<0.01). Also, through in vivo study, the antithrombotic activities of Igyeong-tang, Gamisipjeondaebo-tang, and Gamisoyo-san-treated groups, with recovery rate of 60, 50, and 45.45%, respectively, were observed to be higher than those of the control group (saline, 36.8%) in mouse acute thrombosis. Conclusion: These results show that yin-tonifying formulas are more effective in anti-platelet and anti-thrombotic activity than yang-tonifying formulas.

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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.

Anti-coagulation and Anti-platelet Aggregation Activity of the Mature Fruit of Sorbus commixta (성숙 마가자의 혈액 응고저해 및 혈소판 응집저해 활성)

  • Kim, Mi-Sun;Sohn, Ho-Yong
    • Microbiology and Biotechnology Letters
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    • v.43 no.4
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    • pp.373-377
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    • 2015
  • The mature fruit of Sorbus commixta is known as magaja in Korea and is consumed in the form of tea and wine. In addition, it has been used to treat hypertension and articular neuralgia in folk medicine. In this study, the ethanol extract of magaja and its subsequent organic solvent fractions were prepared, and their in vitro anti-coagulation, and platelet aggregation inhibitory activities were evaluated. Among the fractions, the ethylacetate fraction demonstrated significant inhibition against thrombin, prothrombin, blood coagulation factors and platelet aggregation, without hemolysis activity up to 0.5 mg/ml. Our results suggest that the ethylacetate fraction of magaja has the potential to be used as a new anti-coagulation agent.

Inhibitory Effects of Cordycepin (3'-Deoxyadenosine), a Component of Cordyceps militaris, on Human Platelet Aggregation Induced by Thapsigargin

  • Cho, Hyun-Jeong;Cho, Jae-Youl;Rhee, Man-Hee;Kim, Hyeong-Soo;Lee, Hyun-Sub;Park, Hwa-Jin
    • Journal of Microbiology and Biotechnology
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    • v.17 no.7
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    • pp.1134-1138
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    • 2007
  • Cordycepin (3'-deoxyadenosine) is an adenosine analog, isolated from Cordyceps militaris, and it has been used as an anticancer and anti-inflammation ingredient in traditional Chinese medicine. We investigated the effects of cordycepin (3'-deoxyadenosine) on human platelet aggregation, which was induced by thapsigargin, a tumor promoter, and determined the cytosolic free $Ca^{2+}$ levels ($[Ca^{2+}]_i$) (an aggregation-stimulating molecule) and cyclic-guanosine monophosphate (cGMP) (an aggregation-inhibiting molecule). Cordycepin inhibited thapsigargin-induced platelet aggregation in a dose-dependent manner, and it clearly reduced the levels of $[Ca^{2+}]_i$, which was increased by thapsigargin ($1\;{\mu}M$) or U46619 ($3\;{\mu}M$). Cordycepin also increased the thapsigargin-reduced cGMP levels. Accordingly, our data demonstrated that cordycepin may have a beneficial effect on platelet aggregation-mediated thrombotic diseases through the $[Ca^{2+}]_i$-regulating system such as cGMP.

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.

Ginseng Intestinal Bacterial Metabolite IH901 as a New Anti-Metastatic Agent

  • Hideo Hasegawa;Sung, Jong-Hwan;Huh, Jae-Doo
    • Archives of Pharmacal Research
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    • v.20 no.6
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    • pp.539-544
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    • 1997
  • Anti-metastatic activities of IH901, an intestinal bacterial metabolic derivative formed from Ginseng protopanaxadiol saponins, was determined in vitro and in vivo. Under in vitro conditions, IH901 inhibited the migration of bovine aortic endothelial cells 25 times stronger than suramin and suppressed the invasion of HT1080 human fibrosarcoma cells into reconstituted basement membrane components of Matrigel 1000 times stronger than RGDS peptide. IH901 also showed inhibitory effect on type-IV collagenase secretion from HT 1080 cells and platelet aggregation. When the anti-metastatic activity of IH901 was evaluated in comparison with that of 5-FU using a spontaneous lung metastatic model of Lewis lung carcinoma, the administration of IH901 (10 mg/kg p. o.) to tumor-bearing mice led to a significant decrease in lung metastasis (43% of untreated control), which was slightly more effective than that obtained with 5-FU (56% of control). Thus, IH901 seems to exhibit its anti-metastatic activity partly through the inhibition of tumor invasion which results from the blockade of type IV collagenase secretion and also through anti-platelet and anti-angiogenic activities.

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BMS-191095, a Cardioselective Mitochondrial $K_{ATP}$ Opener, Inhibits Human Platelet Aggregation by Opening Mitochondrial $K_{ATP}$ Channels

  • Cho Mi-Ra;Park Jung-Wook;Jung In-Sang;Yi Kyu-Yang;Yoo Sung-Eun;Chung Hun-Jong;Yun Yeo-Pyo;Kwon Suk-Hyung;Shin Hwa-Sup
    • Archives of Pharmacal Research
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    • v.28 no.1
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    • pp.61-67
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    • 2005
  • We evaluated the antiplatelet effects of two classes of ATP-sensitive potassium channel openers $(K_{ATP}\;openers)$ on washed human platelets, and the study's emphasis was on the role of mitochondrial $K_{ATP}$ in platelet aggregation. Collagen-induced platelet aggregation was inhibited in a dose dependent manner by lemakalim and SKP-450, which are potent cardio-nonselective $K_{ATP}$ openers, and also by cardioselective BMS-180448 and BMS-191095 $(IC_{50}\;:\;1,130,\;>\;1,500,\;305.3\;and\;63.9\;{\mu}M,\;respectively)$, but a significantly greater potency was noted for the cardioselective $K_{ATP}$ openers. The latter two $K_{ATP}$ openers also inhibited platelet aggregation induced by thrombin, another important blood-borne platelet activator, with similar rank order of potency $(IC_{50}\;:\;498.0\;and\;104.8{\mu}M\; for\;BMS-180448\;and\;BMS-191095,\;respectively)$. The inhibitory effects of BMS-191095 on collagen-induced platelet aggregation were significantly blocked by a 30-min pretreatment of platelets with glyburide $(1{\mu}M)$ or sodium 5-hydroxyde­canoate$(5-HD,\;100{\mu}M)$, a nonselective and selective mitochondrial $K_{ATP}$ antagonist, respectively, at similar magnitudes; this indicates the role of mitochondrial $K_{ATP}$ in the antiplatelet activity of BMS-191095. However, glyburide and 5-HD had no effect when they were added to the platelet cuvette immediately prior to the addition of BMS-191095. These findings indicate that cardioselective mitochondrial $K_{ATP}$ openers like BMS-191095 are able to exert cardioprotective effects in cardiac ischemia/reperfusion injury via dual mechanisms directed at the inhibition of platelet aggregation and the protection of cardiomyocytes, and both these mechanisms are mediated by mitochondrial$K_{ATP}$.