• Title/Summary/Keyword: Thrombin inhibitory activity

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Biological Activities of Water Extract and Solvent Fractions of an Edible Mushroom, Hericium erinaceus (노루궁뎅이버섯 물 추출물 및 유기용매 분획물의 생리활성 효과)

  • Kim, Jun-Ho
    • The Korean Journal of Mycology
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    • v.40 no.3
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    • pp.159-163
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    • 2012
  • This study was performed to investigate the biological activities of Hericium erinaceus fruiting body, including antioxidative, fibrinolytic, thrombin inhibitory and ${\alpha}$-glucosidase inhibitory activities. The water extract of H. erinaceus was fractionated into hexane, chloroform, ethyl acetate, butanol and water fractions, and each of these fractions was individually assayed. The water extract showed high antioxidative activity at 87.78%. The water fraction showed the highest extraction yield at 35.68% (w/w). In the fraction activity tests, butanol and water fractions showed strong antioxidative activities at 87.91% and 92.27%, respectively. Assays for fibrinolytic activity indicated that only the ethyl acetate fraction has significant efficacy at 2.96 plasmin units/mL. The 10-fold dilution of hexane fraction showed high thrombin inhibitory activity, and ${\alpha}$-glucosidase inhibitory activity at 77.67% and 90.53%, respectively. In conclusion, solvent fractions of H. erinaceus can be used as materials for the development of biofunctional foods to prevent cardiovascular diseases.

Physiological activities of water extract and solvent fractions of Grifola frondosa (잎새버섯 물추출물 및 유기용매 분획물의 생리활성)

  • Kim, Eun-Jung;Kim, Jun-Ho
    • Journal of Mushroom
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    • v.13 no.3
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    • pp.192-198
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    • 2015
  • This study was performed in order to analyze the fibrinolytic, thrombin inhibitory, anti-oxidative, acetylcholinesterase inhibitory, and immuno-enhancing activities of the water extract and solvent fractions isolated from Grifola frondosa. Fibrinolytic activity was analyzed using the fibrin plate method, and thrombin inhibitory activity was assayed using the substrate H-D-Phe-piparg- pna. Anti-oxidative activity was estimated using the DPPH assay, and AChE inhibitory activity was measured using the spectrophotometric method. Immuno-enhancing activity was examined using the nitric oxide (NO) production in RAW 264.7 macrophage cells. Cell viability was determined using the MTS assay. Fibrinolytic activities were the highest in water extract (1.55 plasmin units/mL) followed by water fraction (0.85 plasmin units/mL). The thrombin inhibitory activities of the water and ethyl acetate fractions were determined to be 76.43% and 72.59%, respectively. The acetylcholinesterase inhibitory activities of chloroform and hexane fractions exhibited values of 95.14% and 94.74%, respectively. The butanol fraction showed the highest anti-oxidative activity at 94.47%. Anti-proliferating activity against Raw 264.7 cells showed no cytotoxicity. The production of NO in Raw 264.7 cells increased up to 2-fold by adding the water fraction compared to the untreated control. These results suggest that Grifola frondosa may serve as a useful functional food for the enhancement of immune function and the prevention and therapy of cardiovascular diseases.

Physiological Activities of Water Extract and Solvent Fractions of an Edible Mushroom, Pholiota adiposa (검은비늘버섯 물 추출물 및 유기용매 분획물의 생리활성 효과)

  • Kim, Jun-Ho
    • The Korean Journal of Mycology
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    • v.42 no.3
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    • pp.207-212
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    • 2014
  • This study was conducted in order to investigate the physiological activities, including antioxidative, fibrinolytic, thrombin inhibitory, and ${\alpha}$-glucosidase inhibitory activities of the water extract and solvent fractions isolated from Pholiota adiposa. The antioxidative activities of the water extract and water fraction were 57.57% and 48.27%, respectively. The fibrinolytic activity was strong only in the ethyl acetate fraction at 0.70 plasmin units/mL. The ethyl acetate fraction showed high thrombin inhibitory activity, and a-glucosidase inhibitory activity at 77.67% and 89.32%, respectively. The ethyl acetate fraction hydrolyzed both $A{\alpha}$ and $B{\beta}$ subunits of human fibrinogen, but did not show reactivity for the ${\gamma}$ form of human fibrinogen. Fibrinolytic activity of the ethyl acetate fraction was not decreased by heating for 10 min at $100^{\circ}C$.

Screening of Thrombin Inhibitor from Medicinal and Wild Plants (II) (약용 및 야생식물로부터 트롬빈 저해물질의 탐색 (II))

  • Ryu, Hee-Young;Kwon, Yun-Sook;Kum, Eun-Joo;Kwon, Chong-Suk;Kwon, Gi-Seok;Kim, Kun-Woo;Son, Kun-Ho;Sohn, Ho-Yong
    • Korean Journal of Pharmacognosy
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    • v.36 no.4 s.143
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    • pp.263-272
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    • 2005
  • To develop safe and new anticoagulation agents from natural resources, the inhibitory activities of 291 methanol extracts, which were prepared from different parts of 197 medicinal and wild plants, against human thrombin were evaluated. Based in anti-coagulation activity determined by thrombin time and activated partial thromboplastin time, the extract of leaf of Myrica rubra was finally selected. The extract of M. rubra showed a strong thrombin inhibitory activity (above 1,819%) at 0.5 mg/ml as a final concentration, whereas aspirin showed 337% inhibition at concentration of 1.5 mg/ml. The activity of the extract remained more than 85% and 60% by heat treatment at $100^{\circ}C$ for 30min, and acid treatment at pH 2 for 60 min, respectively. Our results suggested that the extract of Myrica rubra could be the potential source as thrombin inhibitor.

Hexane and Chloroform Fractions of Laetiporus sulphrueus var. miniatus Inhibit Thrombin-treated Matrix Metalloproteinase-2/9 Expression in Human Oral Squamous Carcinoma YD-10B Cells

  • Kim, Eun-Jung;Yoo, Kwan-Hee;Kim, Yang-Sup;Seok, Soon-Ja;Kim, Jun-Ho
    • The Korean Journal of Mycology
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    • v.45 no.3
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    • pp.175-187
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    • 2017
  • Laetiporus sulphrueus var. miniatus is widely distributed worldwide, and has commonly been used as a medicinal mushroom. In the present study, we investigated the effects of water extract and solvent fractions from the Laetiporus miniatus as possible antioxidant, anti-thrombin and anti-invasive agents against phorbol 12-myristate 13-acetate (PMA)- or thrombin-induced matrix metalloproteinase-2 (MMP-2) and MMP-9 activities. Samples were fractionated into n-hexane, $CHCl_3$, ethyl acetate, n-butanol, and water fractions, and individually analysed. The water fraction had the highest extraction yield at 34.90% (w/w), while the n-butanol fraction demonstrated the highest anti-oxidative activity at 81.44%. In the thrombin inhibitory activity test, the water fraction exhibited the highest activity at 94.64%. Even at the concentration of $40{\mu}g/mL$, evaluation of anti-proliferating activity in YD-10B cells did not reveal any cytotoxic effects. Although MMP-9 expression in YD-10B cells increased after the addition of PMA and thrombin, MMP-2 did not. Additionally, MMP-2/-9 levels in PMA-treated YD-10B cells (i.e., both mRNA expression and protein activation) were highly inhibited in the hexane and chloroform fractions. Compared with MMP-2 levels, MMP-9 mRNA expression and proteolytic activity were inhibited to a greater extent by the hexane and chloroform fractions in thrombin-treated YD-10B cells. Taken together, these results support that thrombin induces tumor invasion through MMP-2/9 and suggest that the L. miniatus may act as an effective functional food, conferring anti-oxidative, anti-thrombotic and anti-cancer activities.

Biological Activities of Wild Sparassis crispa Extracts (야생 꽃송이버섯 추출물의 생리활성)

  • Kim, Eun-Jung;Yoo, Kwan-Hee;Kim, Yang-Sup;Seok, Soon-Ja;Kim, Jun-Ho
    • The Korean Journal of Mycology
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    • v.43 no.1
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    • pp.40-46
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    • 2015
  • Physiological activities of solvent extracts of Sparassis crispa were investigated for fibrinolytic, thrombin inhibitory, anti-oxidative and anti-inflammatory activities. The fibrinolytic activity was the highest in ethyl acetate extract (2.03 plasmin units/mL) followed by butanol extract (0.70 plasmin units/mL). The ethyl acetate extract exhibited the highest anti-oxidative activity as assessed by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging rate with a value of 95.94%. The chloroform extract showed thrombin inhibitory activity up to 83.87%. The chloroform extract also showed the highest anti-inflammatory effects on the production of nitric oxide (NO) in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. These findings suggest that Sparassis crispa may be a useful material for development of drugs and functional foods.

Evaluation of Anti-oxidative, Anti-thrombin, Anti-invasive and Pro-apoptotic Activities of Paeonia japonica (백작약(Paeonia japonica)의 항산화, 트롬빈 저해, 암전이 억제 및 암세포사멸 평가)

  • Kim, Jun-Ho;Kim, Eun-Jung
    • Korean Journal of Plant Resources
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    • v.31 no.1
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    • pp.16-23
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    • 2018
  • Paeonia japonica is a perennial flowering plant used in traditional medicine therapy. The purpose of this study was to investigate the effect of water extract and solvent fractions obtained from P. japonica on anti-oxidative, anti-thrombin, anti-invasive and pro-apoptotic activities in YD-10B cells, human oral squamous carcinoma cell line. Water fraction revealed the highest extraction yield at 11.44% (w/w). Anti-oxidative activity was the highest in ethyl acetate fraction (85.13%). In the thrombin inhibitory activity test, ethyl fraction was the highest, with a value of 87.54%. Release and activation of MMP-2/pro-MMP-2 ratio in thrombin-treated YD-10B cells were significantly inhibited in the ethyl acetate fraction. At a concentration of $120{\mu}g/m{\ell}$ water extract and solvent fractions of P. japonica inhibited cell proliferation in YD-10B cells except water fraction. Pro-apoptotic effect on human oral squamous carcinoma cell using the Bax/Bcl-2 ratio analysis was higher in water extract than other fractions. These findings suggest that the ethyl acetate fraction of P. japonica potentiates a promising antioxidant, anti-thrombin and anti-invasive agents.

Screening of Thrombin Inhibitor and its DPPH Radical Scavenging Activity from Wild Insects. (자생곤충으로부터 트롬빈 저해물질의 탐색 및 DPPH radical 소거활성)

  • Ryu, Hee-Young;Heo, Jin-Cheol;Hwang, Jae-Sam;Kang, Seok-Woo;Yun, Chi-Young;Lee, Sang-Han;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.18 no.3
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    • pp.363-368
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    • 2008
  • The in vitro thrombin inhibitory activities of 304 crude extracts from 76 kinds of korean wild insects were evaluated. Measurement of thrombin time showed that the DMSO extracts of Acrida cinerea cinerea (Thunberg), Anax parthenope julius Brauer, Eurydema rugosa Motschulsky, and Stethophyma magister (Rehn) and the water extracts of Dolycoris baccarum Linne, Lixus divaricatus Motschulsky, Metrioptera bonneti, Moechotypa diphysis (Pascoe), Nicrophorus concolor sp., and Tomapoderus ruficollis (Fabricius) had strong thrombin inhibitory activity. No prominent changes of activated partial thromboplastin time by treatment of the selected extracts suggested direct inhibition of thrombin activity by the insect extracts. DPPH scavenging activity of selected extracts showed that the extract of A. cinerea cinerea (Thunberg), D. baccarum Linne, L. divaricatus Motschulsky and N. concolor sp. has good antioxidant activity as well as antithombin activity. Our results suggested that some of korean wild insects could be developed as a natural source of antithrombosis.

Screening of Thrombin Inhibitors from Medicinal and Wild Plants (약용 및 야생식물로부터 트롬빈 저해물질의 탐색)

  • Kwon, Yun-Sook;Kim, Young-Sook;Kwon, Ha-Young;Kwon, Gi-Seok;Kim, Kyung-Jae;Kwon, Chong-Suk;Son, Kun-Ho;Sohn, Ho-Yong
    • Korean Journal of Pharmacognosy
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    • v.35 no.1 s.136
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    • pp.52-61
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    • 2004
  • Inhibitory activities of 264 methanol extracts, which were prepared from different parts of 210 kinds of wild and medicinal plants, against human thrombin were evaluated. Based on the anti-coagulation activity determined by thrombin time and activated partial thromboplastin time, the 14 extracts were screened. The fibrinolytic activity, heat stability and inhibition of other proteolytic digestive enzymes, such as pepsin, papain, trypsin and chymotrypsin, of the 14 extracts were further determined, and Ginko biloba (herba), Ephedra sinica (radix), Reynoutria elliptica (herba), Amomum tsao-ko Crevost (fructus), and Magnolia officinalis Rehd. et Wils (bark) were finally selected as possible plant sources for anti-thrombosis agent. These results suggested that medicinal and wild plants could be the potential source of thrombin inhibitor.

Antithrombotic activities of saponins from Ilex pubescens

  • Han, Yong-Nam;Baik, Soung-Kyung;Kim, Tae-Hee;Han, Byung-Hoon
    • Archives of Pharmacal Research
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    • v.10 no.2
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    • pp.115-120
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    • 1987
  • Methanol extract of Ilex pubescens roots prolonged bleeding time threefold, and inhibited the generation of malondialdehyde released during platelet aggregation inducted by thrombin. Through several purification procedures, its saponin, named ilexoside, was proved to be responsible for the antithrombotic activities of the plant. Ilexosides A, -D and -J and 24-carboxypomolic acid showed strong inhibitory activities on platelet aggregation induced by thrombin.

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