• Title/Summary/Keyword: platelet aggregation inhibitory activity

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The Effect of Manbunbang on Thrombus Disease Related Factors (만분방(漫盆方)이 혈전(血栓) 병웅(病熊) 유관(有關) 인자(因子)에 미치는 영향(影響))

  • Jung, Woo-Suk;Cho, Han-Baek;Kim, Song-Baeg;Choe, Chang-Min;Choi, Chul-Won
    • The Journal of Korean Obstetrics and Gynecology
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    • v.21 no.1
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    • pp.55-82
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    • 2008
  • Purpose: In this study, we evaluated anti-inflammatory activity and anti-thrombosis effect of Manbunbang(MBB) prescribed to chronic PID patients. Methods: We studied inhibitory effect of platelet aggregation, suppression effect of GPIIb/IIIa activity and inhibitory effect of $TXB_2$ and $PGE_2$ biosynthesis which were caused by ADP, epinephrine, collagen and arachidonic acid in vitro. And suppression of pulmonary embolism, changes of related factors in dextran coagulation condition model and anti-oxidative effect of oxidative damage were studied in vivo. Results: MBB extract showed LD50 of $200\;{\mu}g/ml$ or higher in mouse lung fibroblast cells, and significantly decreased the GPT and GPT level in dextran coagulation condition model compared to the control. MBB extract showed dose-dependent inhibition effect on platelet coagulation induced by ADP, epinephrine, collagen, arachidonic acid. MBB extract showed dose-dependent inhibition effect on GPIIb/IIIa activities compared to the control. MBB extract significantly suppressed TXB2 and PGE2 biosynthesis compared to the control. MBB extract suppressed pulmonary embolism triggered by collagen and epinephrine by 37.5% compared to the control. MBB extract significantly suppressed the decrease of speed of bloodstream caused by blood coagulation in dextran coagulation condition model compared to the control. Concluson : The results strongly suggest the anti-inflammatory activity of Manbunbang through anti-thrombus. Various applications using Manbunbang on inflammatory diseases are anticipated. Anti-oxidative efficacy comparison data between the Manbunbang prescription and the drug compositions may be used as important clinical information, and further investigation of anti-oxidative activities of Chrysanthemum indicum and Rhemaniae Radix should be followed.

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Terpene-Strengthened Ginkgo biloba Extract as a Platelet-Activating Factor Antagonist

  • Quan, Zhe-Jiu;Moon, Tae-Chul;Yang, Ju-Hye;Chang, Hyeun-Wook;Park, Young-Hyun;Kim, Young-Ha;Lee, Kyung-Hee;Chi, Yeon-Sook;Lim, Hyun;Kim, Hyoung-Chun;Kim, Hyun-Pyo
    • Biomolecules & Therapeutics
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    • v.14 no.3
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    • pp.160-165
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    • 2006
  • Since platelet-activating factor (PAF) is involved in inflammation, allergic response and anaphylactic shock, PAF receptor antagonists may have potential for controlling these disease conditions. The extract of the leaves of Ginkgo biloba having a higher content of terpenoids (12%) with flavonoids (24%) (YY1224) was prepared in order to obtain the increasing PAF antagonistic activity. As expected, YY1224 showed a higher PAF antagonistic binding affinity ($IC_{50}\;=\;0.09\;{\mu}g/ml$) using $[^3H]PAF$ and rabbit platelets as ligand and receptor source, compared with an $IC_{50}$ of $>\;100\;{\mu}g/ml$ by Egb 761, a standardized extract. YY1224 also showed a higher inhibitory activity against PAF-induced platelet aggregation and NO production from lipopolysaccharide-treated RAW 264.7 cells. In addition, it protected PAF-induced death in mice by oral administration at 15 mg/kg. All these results suggest that YY1224 may show favorable effects on PAF-related disorders.

Aged Garlic Extract and Its Components Inhibit Platelet Aggregation in Rat (흰쥐에서 흑마늘 추출물과 그 성분들에 의한 혈소판 응집억제 효과)

  • Choi, You-Hee;Jeong, Hyung-Min;Kyung, Kyu-Hang;Ryu, Beung-Ho;Lee, Kwang-Youl
    • Journal of Life Science
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    • v.21 no.10
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    • pp.1355-1363
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    • 2011
  • Many clinical trials have demonstrated the beneficial effects of garlic (Allium sativum) on general cardiovascular health. Aged garlic extract (AGE) is known to display diverse biological activities such as in antioxidant, anti-inflammatory and anticancer activities. However, few studies have been directed on the effect of AGE on cardiovascular function. In this study, we aimed to investigate the effect of AGE and its components on platelet activation, a key contributor in thrombotic diseases. In freshly isolated rat platelets, AGE and its components have shown inhibitory activities on thrombin-induced platelet aggregation. These in vitro results were further confirmed in an in vivo platelet aggregation measurement where tail vein injection of garlic oil and S-Allylmercapto-cysteine (SAMC) significantly reduced thrombin and ADP-induced platelet aggregation. Potential active components for antiplatelet effects of AGE were identified to be SAMC and diallyl sulphide through agonist-induced platelet aggregation assay. These results indicate that aged garlic extract can be a novel dietary supplement for the prevention of cardiovascular risks and the improvement of blood circulation.

The Effect of Eungapbang-gagam on Thrombus Disease Related Factors and Oxidative Stress (은갑방가감(銀甲方加減)이 혈전병태유관인자(血栓病態有關因子)와 산화적손상(酸化的損傷)에 미치는 영향(影響))

  • Lee, Soo-Jeong;Kim, Song-Baeg
    • The Journal of Korean Obstetrics and Gynecology
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    • v.21 no.2
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    • pp.125-151
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    • 2008
  • Purpose: In this study, we investigated the anti-thrombotic efficacy of "Eungapbang-gagam(EGB)" currently used in clinical treatment of PID Methods: We studied inhibitory effect of platelet cohesion, suppressive effect of GPIIb/IIIa activity, inhibitory effect of $TXB_2$ and $PGE_2$ biosynthesis, and oxidative damage suppression effects of "EGB" in vitro. Also, suppression of pulmonary embolism and changes of related factors in dextran coagulation condition model were studied in vivo. Results: In this study, EGB extract showed dose-dependent inhibitory effect on platelet coagulation induced by ADP, epinephrine, collagen, arachidonic acid. Also it showed dose-dependent inhibition effect on GPIIb/IIIa activities compared to the control group. EGB extract significantly suppressed the decrease of speed of bloodstream caused by blood coagulation in dextran coagulation condition model and increased the number of platelets and amount of fibrinogen, and decreased the APTT in dextran coagulation condition model compared to the control group. EGB extract showed dose-dependent decrease of oxidative damages caused by DPPH and superoxide anion radicals, whereas dose-dependent increase of superoxide dismutase like activity was observed compared to the control group. Conclusion: We confirmed the anti-thrombosis and anti-oxidative efficacy of "Eungapbang-gagam". Various clinical applications of "Eungapbang-gagam" as well as use of data for the construction of EBM is anticipated.

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Improvement of antithrombotic activity of red ginseng extract by nanoencapsulation using chitosan and antithrombotic cross-linkers: polyglutamic acid and fucoidan

  • Kim, Eun Suh;Lee, Ji-Soo;Lee, Hyeon Gyu
    • Journal of Ginseng Research
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    • v.45 no.2
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    • pp.236-245
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    • 2021
  • Background: Red ginseng (RG) extract, especially ginsenoside Rg1 and Rb1 fractions has been reported to have antithrombotic activities. However, gastric instability and low intestinal permeability are considered to be obstacles to its oral administration. We hypothesized that stability, permeability, and activities of RG might be improved by encapsulation within nanoparticles (NPs) prepared with antithrombotic coating materials. Methods: RG-loaded chitosan (CS) NPs (PF-NPs) were prepared by complex ionic gelation with the antithrombotic wall materials, polyglutamic acid (PGA), and fucoidan (Fu). The concentrations of PGA (mg/mL, X1) and Fu (mg/mL, X2) were optimized for the smallest particle size by response surface methodology. Antithrombotic activities of RG and PF-NPs were analyzed using ex vivo and in vivo antiplatelet activities, in vivo carrageenan-induced mouse tail, and arteriovenous shunt rat thrombosis models. Results: In accordance with a quadratic regression model, the smallest PF-NPs (286 ± 36.6 nm) were fabricated at 0.628 mg/mL PGA and 0.081 mg/mL Fu. The inhibitory activities of RG on ex vivo and in vivo platelet aggregation and thrombosis in in vivo arteriovenous shunt significantly (p < 0.05) increased to approximately 66.82%, 35.42%, and 38.95%, respectively, by encapsulation within PF-NPs. For an in vivo carrageenan-induced mouse tail thrombosis model, though RG had a weaker inhibitory effect, PF-NPs reduced thrombus significantly due to the presence of PGA and Fu. Conclusion: PF-NPs contributed to improve the activities of RG not only by nanoencapsulation but also by antithrombotic coating materials. Therefore, PG-NPs can be suggested as an efficient delivery system for oral administration of RG.

Quality Characteristics and Cardiovascular Activities of Korean Traditional Wines and Liquors

  • Yu, Hyung-Eun;Lee, Dae-Hyoung;Lee, Ju-Hyun;Choi, Sin-Yang;Lee, Jong-Soo
    • Food Science and Biotechnology
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    • v.14 no.6
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    • pp.772-777
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    • 2005
  • The goal of this study was to screen and characterize the physiological functions of Korean traditional wines (TW) and liquors (TL). Forty-two TW and TL were collected and evaluated for quality and cardiovascular activities. Ethanol content ranged from $9.0%{\sim}41%$, and pH ranged from $3.0{\sim}7.8$, and they also contained 0.01% to 0.67% of total acid. Samples contained a maximum of 2.0% of crude protein and $0.1%{\sim}14.0%$ of reducing sugar. Commercial CM-wine showed the highest antihypertensive angiotensin I-converting enzyme (ACE) inhibitory activity, 85.9%. The greatest fibrinolytic activity and platelet aggregation inhibitory activity were also found in commercial CM-wine (31.8U) and commercial SS2-wine (38.6 %), respectively. Commercial SHBI-liquor showed the highest HMG-CoA reductase inhibitory activity, 78%. The ACE inhibitor from commercial CM-wine was a peptide compound and also showed an antihypertensive effect in spontaneous hypertensive rats at a dosage of 1.5 mg/kg.

Anti-oxidant, Anti-coagulation, and Anti-platelet Aggregation Activities of Black Currant (Ribes nigrum L.) (블랙커런트의 항산화, 항응고 및 혈소판 응집저해 활성)

  • Kim, Mi-Sun;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.26 no.12
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    • pp.1400-1408
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    • 2016
  • The black currant (Ribes nigrum L.) is belong to the Grossulariaceae family, and has piquant berries, which can be eaten as raw or as processed foods, such as jams, jelly, juice and syrups. In this study, the fresh juice of black currant (FJBC) from Austria and its subsequent organic solvent fractions, such as hexane fraction, ethylacetate (EA) fraction, butanol fraction and water residue, were prepared and their in-vitro anti-oxidant, anti-coagulation and anti-platelet aggregation activities were evaluated. The FJBC and EA fraction, which has concentrated polyphenol and flavonoid, showed strong radical scavenging activities and reducing power. The $RC_{50}s$ of EA fraction against DPPH anion, ABTS cation, nitrite were 136.3, 66.2 and $115.5{\mu}g/ml$, respectively, those are 1/10, 1/16, and 1/7.7 of $RC_{50}s$ of vitamin C. In anti-coagulation assay, the FJBC, EA and butanol fraction showed significant inhibitory activities against thrombin, prothrombin and coagulation factors. Furthermore, the anti-platelet aggregation activities of EA and butanol fraction were the stronger than that of aspirin. The concentrations required for 50% platelet aggregation inhibition of aspirin, EA and butanol fraction were 0.395, 0.192 and 0.261 mg/ml, respectively. The EA and butanol fraction have no hemolysis activities up to 0.5 mg/ml against human red blood cells. The results suggest that the FJBC and its EA and butanol fraction have high potentials as novel anti-thrombosis agents. This report provides the first evidence of anti-thrombosis activity of black currant.

Screening of Anti-atherosclerotic Effect of Lonicera Flower by Antioxidative and Anti-thrombotic Mechanism (Lonicera Flower의 항산화활성과 LDL 산화 억제효과 및 혈전용해능에 관한 연구)

  • Ju, Shin-Tak;Lee, Min-Ja;Lee, Hye-Sook;Jung, Hyun-Jung;Kim, Hyuck;Kim, Jai-Eun;Park, Sun-Dong;Park, Won-Hwan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.22 no.6
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    • pp.1509-1517
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    • 2008
  • The flowers and buds of Lonicera Flower (LF), are used in Korean herbal medicine for latent-heat-clearing, antipyretic, detoxicant and anti-inflammatory ailments. This plant is used worldwide for the treatment of many types of inflammatory disease including respiratory infections, diabetes mellitus, rheumatoid arthritis and play an important role in immune reaction. These pharmaceutical effects of LF looks like to be related to its antioxidant capacity and phytochemicals containing in LF. In this study, the antioxidant activity of extract from LF was studied 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. The LF extracts were found to have a potent scavenging activity, as well as an inhibitory effect on LDL oxidation and on platelet aggregation. In conclusion, the LF extracts have anti-oxidative and anti-atherosclerotic effects in vitro system, which can be used for developing pharmaceutical drug against oxidative stress and atherosclerosis.

Inhibitory Effects of Epigallocatechin-3-Gallate on Microsomal Cyclooxygenase-1 Activity in Platelets

  • Lee, Dong-Ha;Kim, Yun-Jung;Kim, Hyun-Hong;Cho, Hyun-Jeong;Ryu, Jin-Hyeob;Rhee, Man Hee;Park, Hwa-Jin
    • Biomolecules & Therapeutics
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    • v.21 no.1
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    • pp.54-59
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    • 2013
  • In this study, we investigated the effect of (-)-epigallocatechin-3-gallate (EGCG), a major component of green tea catechins from green tea leaves, on activities of cyclooxygenase (COX)-1 and thromboxane synthase (TXAS), thromboxane $A_2$ ($TXA_2$) production associated microsomal enzymes. EGCG inhibited COX-1 activity to 96.9%, and TXAS activity to 20% in platelet microsomal fraction having cytochrome c reductase (an endoplasmic reticulum marker enzyme) activity and expressing COX-1 (70 kDa) and TXAS (58 kDa) proteins. The inhibitory ratio of COX-1 to TXAS by EGCG was 4.8. These results mean that EGCG has a stronger selectivity in COX-1 inhibition than TXAS inhibition. In special, a nonsteroid anti-inflammatory drug aspirin, a COX-1 inhibitor, inhibited COX-1 activity by 11.3% at the same concentration ($50{\mu}M$) as EGCG that inhibited COX-1 activity to 96.9% as compared with that of control. This suggests that EGCG has a stronger effect than that of aspirin on inhibition of COX-1 activity. Accordingly, we demonstrate that EGCG might be used as a crucial tool for a strong negative regulator of COX-1/$TXA_2$ signaling pathway to inhibit thrombotic disease-associated platelet aggregation.

Evaluation of in-vitro Anti-thrombosis and Anti-oxidation Activity of Lees of Takju (Wookukseng) (우국생 탁주 주박의 항혈전 및 항산화 활성)

  • Kim, Mi-Sun;Lee, Ye-Seul;Kim, Jong Sik;Shin, Woo-Chang;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.25 no.4
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    • pp.425-432
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    • 2015
  • This study was performed to develop high-value-added biomaterials for health and beauty products. Extracts of ethanol and hot water and their subsequent organic solvent fractions were prepared from Lees of Wookukseng (LW), a commercialized Korean traditional rice wine. We investigated their activities on blood coagulation, platelet aggregation, hemolysis against human red blood cells (hRBCs), and anti-oxidation. The water content, pH and brix of the LW were 80.3%, 3.94 and 13.0°, respectively. The yield of ethanol extraction (6.62%) was 3.15 times higher than that of hot-water extraction (2.1%), and the ethyacetate fraction (EAF) of ethanol extract showed the highest content of total polyphenol (128 mg/g) among the various fractions. In anticoagulation activity assay, the EAF of ethanol extract showed a 15-fold extension in TT, PT, and aPTT, indicating that the EAFs contain various inhibitory substances against thrombin, prothrombin and coagulation factors. In anti-platelet aggregation activity assay, the butanol fraction and water residue of ethanol extract showed significant inhibition activity. The activities were comparable to aspirin, a commercial anti-thrombosis agent. The above extracts and fractions did not show hemolysis activity against hRBC up to 5 mg/ml, and had radical scavenging activity against DPPH anion, ABTS cation and nitrite. Our results suggest that the active fractions prepared from LW, which has no specific usage until now, have a high potential as novel resources for anti-thrombosis agents.