• Title/Summary/Keyword: inhibition of platelet aggregation

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Evaluation of Antimicrobial, Antithrombin, and Antioxidant Activity of Fritillaria thunbergii Miquel (패모(Fritillaria thunbergii Miquel)의 항균,항혈전 및 항산화 활성 평가)

  • Shin, Yong-Kyu;Jang, Han-Su;Kim, Jee-In;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.19 no.9
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    • pp.1245-1250
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    • 2009
  • Beimu (Fritillaria thunbergii Miquel), a bulbous plant of Liliaceae found in Korea, Japan and China, has been used as an antitussive and expectorant agent, and is also useful in alleviating stonsillitis and bronchiolitis. Most researches have been focused on micro-propagation and plant regeneration, component analysis, and dormancy relieving of beimu. Reports regarding the biological activity of beimu, such as anti-Helicobacter pyroli or platelet aggregation inhibition activity, are few and not widely available. In this study, methanol extract and its organic solvent fractions were prepared from Fritillaria thunbergii Miquel and their antimicrobial, antithrombin, and antioxidant activities were evaluated, respectively. The methanol extract contained lots of water-soluble materials (58.98%) and hexane-soluble oils (14.85%). The ethylacetate and butanol fraction at $500{\mu}g$/disc concentration showed strong antibacterial activity against tested bacteria, except Escherichia coli. Antifungal activity was not observed in methanol extract and its fractions. The hexane, ethylacetate and butanol fractions showed strong antithrombin activity at 4.8 mg/ml concentration. Especially, the ethylacetate fraction showed 95.4 sec of thrombin time at a concentration of 1.2 mg/ml, which is comparable to aspirin, a widely used antithrombosis agent. For antioxidation activity, the ethylacetate and butanol fraction showed good 1,1-diphenyl-2-picryl hydrazyl scavenging activity ($IC_{50}$ of $344{\sim}368{\mu}g$/ml). In superoxide dismutase-like activity and reducing power, the fractions showed $20{\sim}25%$ of vitamin C, and $51{\sim}54%$ of butyl hydroxytoluene, respectively.

Antioxidation, Antimicrobial and Antithrombosis Activities of Aged Black Garlic (Allium sativum L.) (흑마늘의 항산화, 항균 및 항혈전 활성)

  • Jung, In-Chang;Sohn, Ho-Yong
    • Microbiology and Biotechnology Letters
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    • v.42 no.3
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    • pp.285-292
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    • 2014
  • In the course of study for development of functional food ingredients from aged black garlic (ABG), heat-treated ripe bulbs of Allium sativum L., the water extracts from raw-garlic (RG) and ABG, and the subsequent organic solvent fractions of ABG were prepared, and their antioxidant, antimicrobial, and antithrombosis activities were compared. The extraction yield of ABG was 4-folds higher than that of RG, and the contents of total polyphenol, total flavonoid, total sugar and reducing sugar in the ABG extract were 4-folds, 1.56-folds, 3.36-folds and 6.75-folds higher than those of the RG extract, respectively. In antioxidation activity assay, the extract of ABG showed minor scavenging activity against DPPH anion, but revealed strong scavenging activity against ABTS cation and nitrite. Especially, the ethylacetate fraction from the ABG extract demonstrated stronger antioxidation activity than the RG extract and other fractions. Although the antimicrobial and antithrombosis activities of the RG extract did not appear in the ABG extract, the ethylacetate fraction from the ABG extract had antibacterial activity against Staphylococcus aureus and Bacillus subtilis, and strong antithrombosis activity via the inhibition of prothrombin, blood coagulation factors and platelet aggregation. All extracts and fractions did not show any hemolytic activity against human red blood cells up to 5 mg/ml. Our results suggest that the ethylacetate fraction of ABG could be applicable to the development of functional food ingredients for antithrombosis agents.

Study on Inhibition of Platelet Aggregation of Bioactive constituents from Paeonia lactiflora (작약의 혈소판 응집억제작용에 관한 연구)

  • 서범석;박관혁;손동주;박영현;장성근
    • Proceedings of the KAIS Fall Conference
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    • 2003.06a
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    • pp.320-321
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    • 2003
  • 최근 천연물을 중심으로 한 학문이 발전하면서 천연물이 가지는 생리활성 물질에 대한 관심이 중대되고 있다. 또한 인공합성품의 일부가 안정성의 문제가 제기되면서 천연물의 이용분야는 더욱 확대되고 있다. 급속한 경제발전과 생활수준의 향상으로 식생활을 포함한 생활방식의 다양화로 인하여 과거 감염 위주의 질병이 감소하고 선진국형의 만성퇴행성 질환이 증가하는 추세이다. 혈소판은 혈전증(thrombosis)과 지혈증(haemstasis)에서 중요한 역할을 담당하고 있는 인자로서 현관 내 병적 이상으로 인한 과도한 혈전의 생성은 뇌 -심혈관계 질환의 중요한 유발인자로 작용하므로 뇌ㆍ심혈관계 질환이나 항고지혈증을 연구하는데 유용하게 이용되고 있다. 본 연구에서는 토끼 혈액에서 분리한 세정 혈소판 부유액을 이용하여 작약 MeOH 추출물에서 분리한 천연생리활성물질들을 대상으로 혈소판 응집억제활성에 대하여 연구하였다. 작약 MeOH 추출물의 혈소판 응집억제활성 측정에서 강한 혈소판 응집억제활성 작용을 보였다. 따라서 작약 MeOH 추출물을 크로마토그라피법을 이용하여 분리하였고, NMR을 이용한 분광학적 방법으로 지금까지의 분리한 자료와 비교ㆍ분석하였다. Monoterpene glycoside 계열의 성분들인 15개의 compound와 다수의 fraction들을 HPLC를 이용하여 분리하였으며, collagen으로 유도된 혈소판 응집억제활성측정 방법에서 뛰어난 응집억제활성을 보였다. 표준물질을 이용한 HPLC 분석과 ¹H-NMR 관련 자료의 검색을 통하여 최종적으로 compound 1b가 benzoyloxy-paeoniflorin(2.6%). compound 1d가 paeond(1.3%), compound 2c가 albiflorin(3.2%), compound 2e가 paeoniflorin(33.6%)임을 확인할 수 있었다. Compound 3a의 분석결과 benzoyloxypaeoniflorin과 구조적 유사성은 있으나 동일한 구조식으로 확인할 수 없었다. 그러나 collagen에서 응집억제활성이 90% 이상으로 뛰어난 활성을 나타내므로 benzoyloxypaeoniflorin과 유사한 구조에서 benzoyl group이 다른 작용기로 치환되었거나 R₁ group이 다른 작용기로 치환된 형태로 추측하였다. Benzoyloxypaeoniflorin은 collagen>thrombin>U46616>A.A(arachidonic acid)>PAF의 순으로 활성을 보였다. 이는 paeoniflorin의 glycoside 5-carbon위치에 위치한 OH기 대신에 benzoyl기로 치환된 benzoyl 기가 혈소판 억제 산물로 작용한 것으로 추측했다. Paeoniflorin.은 U46619>thrombin>collagen>A.A>PAF순으로 억제를 보였다. Paeoniflorin이 collagen보다 thrombin에서 강한 억제를 보이는 것으로 Ca/sup 2+/ chelate를 형성함으로 인해 calciu 대사를 저해하는 것으로 추축했다. Compound 3a는 U46619>collagen>A.A>thrombin>PAF순으로 억제율을 보이므로 이 화합물은 paeoniflorin의 benzoyl기에 OH기가 다른 치환기로 바뀌거나 paeoniflorin의 glycoside 5-carbon 위치의 OH기 대신에 다른 작용기로 치환된 것으로 추정하였다. 이러한 결과로 작약의 주성분인 paeoniflorin과 유사한 구조를 가진 다른 monoterpene glycoside 계열의 화합물들과 비교 분석하고 구조를 화인하고 이들 성분이 어떻게 혈소판 응집억제활성에 작용하는지를 연구하였다.

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Effects of Bambusae Caulis in liquamen on inhibition of angiotensin-converting enzyme in vitro and blood flow in mouse model (죽력의 in vitro에서의 angiotensin-converting enzyme 저해효과와 마우스모델에서 혈행개선효과)

  • Kim, Chun dug;Ryu, Min Jung;Chun, Hyoung Sik;Choi, Geun Pyo;Hwang, Kwonteak
    • Food Science and Preservation
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    • v.24 no.7
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    • pp.992-999
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    • 2017
  • The purpose of this study was to investigate the effects of the Bambusae Caulis in liquamen (BCL) on blood circulation in animal models. Previous studies on BCL have shown effects on thrombolytic activity and angiotensin-converting enzyme (ACE) inhibitory activity. In the mouse model, the triglyceride content were 301.5 mg/dL in the high fat diet+BCL II 0.01% group, 289.2 mg/dL in the high fat diet+BCL II 0.05% group, which was significantly lower than the high fat diet group. The total cholesterol content was 311.9 mg/dL in high fat diet+BCL II 0.01% and 293.7 mg/dL in high fat diet+BCL II 0.01% 0.05%, respectively, which was significantly lower than the high fat diet group. The HDL-cholesterol level was 206.0 mg/dL for the high fat diet, 196.6 mg/dL for the high fat diet+BCL II, and 189.2 mg/dL for the high fat diet+BCL II. There was no significant difference between the 0.01% and 0.05% groups. The high-fat diet+0.05% group was significantly improved in the blood flow compare to the high fat diet and the high fat diet+0.01% group. Platelet aggregation inhibition ability was inhibited in the high fat diet+0.01% and 0.05% groups compared to the high fat diet group.

The Effect of Nitric Oxide Donor or Nitric Oxide Synthase Inhibitor on Oxidant Injury to Cultured Rat Lung Microvascular Endothelial Cells (산화질소 공여물과 산화질소 합성효소 길항제가 백서 폐미세혈관 내피세포 산화제 손상에 미치는 영향)

  • Chang, Joon;Michael, John R.;Kim, Se-Kyu;Kim, Sung-Kyu;Lee, Won-Young;Kang, Kyung-Ho;Yoo, Se-Hwa;Chae, Yang-Seok
    • Tuberculosis and Respiratory Diseases
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    • v.45 no.6
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    • pp.1265-1276
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    • 1998
  • Background : Nitric oxide(NO) is an endogenously produced free radical that plays an important role in regulating vascular tone, inhibition of platelet aggregation and white blood cell adhesion to endothelial cells, and host defense against infection. The highly reactive nature of NO with oxygen radicals suggests that it may either promote or reduce oxidant-induced cell injury in several biological pathways. Oxidant injury and interactions between pulmonary vascular endothelium and leukocytes are important in the pathogenesis of acute lung injury, including acute respiratory distress syndrome(ARDS). In ARDS, therapeutic administration of NO is a clinical condition providing exogenous NO in oxidant-induced endothelial injury. The role of exogenous NO from NO donor or the suppression of endogenous NO production was evaluated in oxidant-induced endothelial injury. Method : The oxidant injury in cultured rat lung microvascular endothelial cells(RLMVC) was induced by hydrogen peroxide generated from glucose oxidase(GO). Cell injury was evaluated by $^{51}$chromium($^{51}Cr$) release technique. NO donor, such as S-nitroso-N-acetylpenicillamine(SNAP) or sodium nitroprusside(SNP), was added to the endothelial cells as a source of exogenous NO. Endogenous production of NO was suppressed with N-monomethyl-L-arginine(L-NMMA) which is an NO synthase inhibitor. L-NMMA was also used in increased endogenous NO production induced by combined stimulation with interferon-$\gamma$(INF-$\gamma$), tumor necrosis factor-$\alpha$(TNF-$\alpha$), and lipopolysaccharide(LPS). NO generation from NO donor or from the endothelial cells was evaluated by measuring nitrite concentration. Result : $^{51}Cr$ release was $8.7{\pm}0.5%$ in GO 5 mU/ml, $14.4{\pm}2.9%$ in GO 10 mU/ml, $32.3{\pm}2.9%$ in GO 15 mU/ml, $55.5{\pm}0.3%$ in GO 20 mU/ml and $67.8{\pm}0.9%$ in GO 30 mU/ml ; it was significantly increased in GO 15 mU/ml or higher concentrations when compared with $9.6{\pm}0.7%$ in control(p < 0.05; n=6). L-NMMA(0.5 mM) did not affect the $^{51}Cr$ release by GO. Nitrite concentration was increased to $3.9{\pm}0.3\;{\mu}M$ in culture media of RLMVC treated with INF-$\gamma$ (500 U/ml), TNF-$\alpha$(150 U/ml) and LPS($1\;{\mu}g/ml$) for 24 hours ; it was significantly suppressed by the addition of L-NMMA. The presence of L-NMMA did not affect $^{51}Cr$ release induced by GO in RLMVC pretreated with INF-$\gamma$, TNF-$\alpha$ and LPS. The increase of $^{51}Cr$ release with GO(20 mU/ml) was prevented completely by adding 100 ${\mu}M$ SNAP. But the add of SNP, potassium ferrocyanate or potassium ferricyanate did not protect the oxidant injury. Nitrite accumulation was $23{\pm}1.0\;{\mu}M$ from 100 ${\mu}M$ SNAP at 4 hours in phenol red free Hanks' balanced salt solution. But nitrite was not detectable from SNP upto 1 mM The presence of SNAP did not affect the time dependent generation of hydrogen peroxide by GO in phenol red free Hanks' balanced salt solution. Conclusion : Hydrogen peroxide generated by GO causes oxidant injury in RLMVC. Exogenous NO from NO donor prevents oxidant injury, and the protective effect may be related to the ability to release NO. These results suggest that the exogenous NO may be protective on oxidant injury to the endothelium.

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