• 제목/요약/키워드: Inhibition dose

검색결과 2,173건 처리시간 0.031초

Contrasting Correlation in the Inhibition Response of ADP-induced Platelet Aggregation and the Anti-coagulant Activities of Algal fucoidans Derived from Eisenia bicyclis and Undaria pinnatifida sporophylls (Mekabu)

  • Jeong, Eui-Sook;Yoon, Yeon-Hee;Kim, Jong-Ki
    • Fisheries and Aquatic Sciences
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    • 제12권3호
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    • pp.194-202
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    • 2009
  • Sulfated fucans are known to have both anti-thrombotic and anti-coagulant activities. In this study, the variation in platelet aggregation and anti-coagulant activities was investigated in vitro with regard to administered dose, molecular weight distribution, sulfate content, and sugar composition in two algal fucoidans from Eisenia bicyclis and Undaria pinnatifida sporophylls (Mekabu). The anti-coagulant activity largely correlated with sulfate content and with molecular weight distribution in a dose-dependent manner. However, both fucoidans demonstrated inhibitory responses to ADP-induced platelet aggregation in dose- and structure-dependent manners that contrasted with the anti-coagulant activity. Neither molecular weight distribution nor sulfate content greatly affected platelet-aggregation inhibition (PA-inhibition) by the fucoidan fractions, whereas anti-coagulant activity was sensitive to these structural factors. Interestingly, an E. bicyclis fucoidan fraction exhibited almost complete PA-inhibition at a treatment dose of 500 mg/mL while retaining weak anti-coagulant activity. In conclusion, these observations suggest that fucoidan may be a useful anti-thrombotic or anti-platelet agent in various arterial thrombotic disorders, including post-vascular intervention with controlled bleeding complications, due to its anti-coagulant modulating activity.

부자(附子)의 우울증 억제효과에 관한 연구 (Anti-depressant Effect of the Extracts of Aconitum carmichaeli)

  • 장문규;김근우;구병수
    • 동의신경정신과학회지
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    • 제20권3호
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    • pp.49-64
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    • 2009
  • Objectives : The water and methanol extracts of Aconitum carmichaeli(Aconiti Tuber Preparat) were investigated for their anti-depressant effects. Methods : In this study, reserpine-induced hypothermia test, tail suspension test and hot plate test. Additionally, the brain monoamine oxidase activity was determined in vivo. Results: In the reserpine-induced hypothermia test, both extracts suppressed the fall of body temperature compared to the control group in a dose-dependent manner, suggesting the inhibition on hypothermia. In the tail suspension test, the methanol extract dose-dependently reduced the duration of immobility by 28.4% at a dose of 1 g/kg compared to control group, which is more effective than the water extract. In the hot plate test, the water extract and methanol extract increased the jump latency time compared to the control group, showing the inhibition rate of 198% and 182%, respectively, at a dose of 1 g/kg. Methanol extracts potently inhibited the brain monoamine oxidase activity in an in vivo assay compared to the control group, showing 84.6% inhibition, but the water extract revealed very weak activity. Conclusions : Above results suggested that the extract of Aconitum carmichaeli can be useful for the prevention and treatment of depression.

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Dopaminergic influences on prolactin synthesis and release from rat anterior pituitary cultures

  • Kim, Kwang-Chul;Burkman, Allan
    • Archives of Pharmacal Research
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    • 제3권2호
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    • pp.85-86
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    • 1980
  • Dopaminergic influences on prolactin release from lactotrophs have been studied using the rat anterior pituitary cell culture. The prolactin inhibiting activity of hypothalamic extracts was examined in relation to dopamine. Dopamine inhibited prolactin secretion from the rat anterior pituitary cell culture in a dose dependent fashion. The median effective dose was $2{\times}10^{-7}$ / M and the maximal inhibition (70-90 % of the control value) was shown by 10$^{-5}$ / M dopamine. Further increase in dopamine concentration did not result in any further inhibition of prolactin secretion.nhibition of prolactin secretion.

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The Inhibition Effect of Water Extract of Acanthopanax senticosus Harms Roots on the 5-HT Induced Vasocontraction in Rat

  • Kim, Hyung-Hwan;Ahn, Duk-Kyun;Yook, Chang-Soo;Choi, Ho-Young
    • 대한한의학회지
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    • 제24권4호
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    • pp.82-86
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    • 2003
  • Objective : To examine the inhibition of 5-Hydroxytryptamine(5-HT) induced vasocontraction of the water extract of Acanthopanax senticosus Harms roots (ASR) on rat thoracic Aorta and mesenteric artery with and without endothelium. Methods : Segments of thoracic aorta and mesenteric artery obtained from rats immediately after delivery were mounted in organ baths superfused on a polygraph. Results : We found that the thoracic aorta segments responded to the water extract of ASR with a dose-dependent and concentration-dependent vasorelaxation. 5-HT produced a concentration-dependent contraction of the thoracic aorta and mesenteric artery. At high concentrations of ASR, the inhibition responses were 93.7% (Jang-su), 93.5% (Heok-ryong-kang-sung), 92.8% (Mt. Back-doo), and 83.5% (Yeon-byun) of the maximum 5-HT induced contraction. At high concentrations of ASR, the relaxational response at thoracic aorta and mesenteric artery wi1h endothelium were 95.2% and 94.6%; without endothelium were 93.5% and 92.5% of 1he maximum 5-HT induced contraction. Conclusions : In conclusion, the effect of water extract of ASR had potent inhibition at 5-HT and the effect of ASR in isolated thoracic aorta and mesenteric artery showed dose-dependent inhibition but endothelium-independent response.

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의약품(醫藥品)의 병용(倂用) 투여(投與) 효과에 관한 연구(硏究)(I) -갈근탕(葛根湯) 엑기스와 Aspirin의 병용(倂用) 투여(投與)가 항염(抗炎) 및 진통작용(鎭痛作用)에 미치는 영향(影響)- (Studies on the Concurrent Administration of Medicines(I) -Anti-inflammatory and Analgesic Actions of Galgun-tang and Aspirin-)

  • 조의환;김일혁
    • 생약학회지
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    • 제16권1호
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    • pp.7-11
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    • 1985
  • The extract of Galgun-tang at oral doses of 200 and 400 mg/kg showed remarkable inhibition of 42.5% and 45.0%, respectively, on the carrageenin edema in rat paw. In case of combined oral administration of the extract at each dose of 100, 200 and 400mg/kg with 100mg/kg of aspirin, the inhibitions were 70.5%, 83.6% and 80.7% respectively. These results showed the remarkable effects as compared with those of aspirin which showed 50.3% and 69.4% of inhibition at doses of 100 and 200mg/kg, respectively. On the other hand, on the writhing syndrome in mice induced by 0.7% acetic acid solution, the oral administration of the extract showed remarkable inhibition of 18.5 and 47.7% at doses of 200 and 400mg/kg, respectively. In case of combined oral administration of the extract at each dose of 100, 200 and 400mg/kg with 100mg/kg of aspirin, the inhibition percentages of writhing syndromes were 66.6, 72.3 and 80.8, respectively, whereas the inhibition at doses of 100 and 200mg/kg of aspirin showed 59.9 and 69.5%, respectively.

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Antiulcerogenic and Anticancer Activities of Korean Red Ginseng Extracts Bio-transformed by Paecilomyces tenuipes

  • Kim, Young-Man;Choi, Won-Sik;Kim, Hye Jin;Lee, Eun-Woo;Park, Byeoung-Soo;Lee, Hoi-Seon;Yum, Jong Hwa
    • Journal of Applied Biological Chemistry
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    • 제57권1호
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    • pp.41-45
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    • 2014
  • In the present study, red ginseng extracts were fermented by Paecilomyces tenuipes and the protopanaxdiol-type ginsenosides in the extracts were bio-transformed to F2, Rg3, Rg5, Rk1, Rh2, and CK determined by a high-pressure liquid chromatography analysis. It indicates that P. tenuipes is a microorganism to biotransform protopanaxdiol-type ginsenosides to their less glucosidic metabolites. Other biotransformed metabolites during fermentation were also analyzed using a GC-MS and identified as 2-methyl-benzaldehyde, 4-vinyl-2-methylphenol, palmitic acid, and linoleic acid. Antiulcerogenic activity of the fermented red ginseng extract (FRGE) on gastric mucosal damage induced by 0.15 M HCl in ethanol in rats was evaluated. FRGE was shown to have a potent protective effect on gastritis with 60.5% of inhibition rate at the dose of 40 mg/kg when compared to 54.5% of the inhibition rate at the same dose for stillen, the currently used medicine for treating gastritis. Linoleic acid showed a strong inhibition on gastritis with 79.3% of inhibition rate at the dose of 40.0 mg/kg. FRGE exhibited a distinct anticancer activity including growth inhibition of the two human colon cancer cells HT29 and HCT116. HT29 cells were less susceptible to FRGE in comparison with HCT116 cells. Taken together, fungal fermentation of the red ginseng extract induced hydrolysis of some ginsenosides and FRGE exhibited potent antiulcerogenic and anticancer activities. These results refer to use FRGE as a new source for treating human diseases.

Lymphoblastosis Inhibition and Plaque-forming Cell Response of Several Anti-inflammatory Steroids in Mice

  • Choi, Hong-Pil;Kim, Kilhyoun;Kim, Hyun-Pyo
    • Archives of Pharmacal Research
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    • 제15권2호
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    • pp.169-175
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    • 1992
  • Anti-inflammatory glucocorticoid (GC) derivatives have been clinically used in immune-malfunctional diseases for their immunosuppressive activity. However, there is still a lack of knowledge on the relationship between anti-inflammatory and immunosuppressive activities. In order to compare immunosuppressive activities with the known anti-inflammatory activities of the GC derivatives, eight clinically used GC derivatives including hydrocortisone, prednislone, 6$\alpha$-methyl prednisolone, triamcinolone, dexamethasone, betamethasone, triamcinolone acetonide and fluocinolone acetonide were selected, and lymphoblastosis inhibition and plaque-forming cell (PFC) response in mice were studied as immunological parameters. In Con A-induced lymphoblatosis inhibition invitro, all derivatives showed potent inhibition $IC_{50}$ values of the derivaties except methyl prednisolone and triamcinolone were less than $10^{-7}$M and good dose dependency was obtained. This result was well correlated with that of their anti-inflammatory potencies obtained. This result was well correlated with that of their anti-inflammatory potencies and their receptor binding affinities. However, in PFC response, consistent result were not obtained. Total numbers of PFCs per spleen were decreased by some derivatives, but numbers of PFCs per $10^6$ cells were not decreased by systemic administration of but numbers of PFCs per $10^6$ cells were not decreased by systemic administration of GC at the dose of 0.05 mg/mouse. Furthermore, at the dose of 0.1 mg/mouse, numbers of PFCs per $10^6$ cells were found to be increased, although total PFCs per spleen were decreased.

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부자의 메탄올 추출물에 의한 신세포암의 증식억제 및 세포사멸 유도 (Inhibition of Cell Proliferation and Induction of Apoptosis by Methanolic Extract of Aconiti Tuber in Human Renal Cell Carcinoma Cells)

  • 김종환;최영현;황원덕
    • 대한한방내과학회지
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    • 제29권1호
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    • pp.42-66
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    • 2008
  • Aconiti Tuber is a traditional medicinal plant generally used in Oriental medicine therapy. In this study, we investigated the biochemical mechanisms of anti-proliferative effects by the methanol extract of Aconiti tuber (MEBJ) in Caki-1 human renal cell carcinoma cells. It was found that MEBJ could inhibit, in a dose-dependent manner, cell growth which was associated with apoptotic cell death such as formation of apoptotic bodies, DNA fragmentation and increased populations of apoptotic-sub G1 phase. Apoptosis of Caki-1 cells by MEBJ was associated with an up-regulation of pro-apoptotic Bax expression, and a down-regulation of anti-apoptotic Bcl-2 in a dose-dependent manner; however, the levels of IAP family were not affected. MEBJ treatment also induced the proteolytic activation of caspase-3 and -8, and a inhibition of poly(ADP-ribose) polymerase (PARP) and $PLC{\gamma}1$ protein. Furthermore, MEBJ treatment caused a dose-dependent inhibition of iNOS and cyclooxygenase-2 (Cox-2). Though further studies will be needed to identify the active compounds that confer the anti-cancer activity of MEBJ, the present findings provide important new insights into the possible molecular mechanisms of the apoptotic activity of MEBJ in cancer cells.

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양파 페놀성분획물의 생리활성기능탐색 (Screening of Biological Activity for Phenolic Fraction from Onion)

  • 안봉전;이진태
    • 한국식품저장유통학회지
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    • 제8권2호
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    • pp.224-230
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    • 2001
  • To develop a material for functional food, the fraction Ⅰ,II and Ⅲ of onion extract were separated by Sephadex LH-20 column. The revealed purification levels of each fraction were 5.2%-6.5%, 12.2%-14.5% and 82.6%-86.7%, respectively. A functional activity test was performed with fraction Ⅲ. The ACE inhibition activity was about 50% at 5mg and about 80% at 10mg. The XOase inhibition activity of Korean Changnyong Daego was 84%, which was the highest. At the experiment of tyrosinase inhibition was detected 21-36% at 10mg. The cholesterol dose in mice blood was as low as low as 79$\pm$5(mg/100 mL) after the intake of fraction Ⅲ. Cholestrol dose in liver was decreased to below 50%. The results show that Sephadex LH-20 column method was very useful as a fraction method for the development of functional food material nsing onions.

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천연물의 항염증작용에 관한 연구 (Studies on the Antiinflammatory Effects of Natural Products)

  • 유태무;이숙영;정수연;승상애;류항묵;양지선;이은방
    • Biomolecules & Therapeutics
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    • 제6권3호
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    • pp.269-275
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    • 1998
  • These studies were conducted to investigate the antiinflammatory effects and the mechanism of action of natural products. We used the methods of "carrageenan induced foot edema" , "PAF (platelet activating factor) induced foot edema" , "inhibition test of vascular permeability" , "inhibition test of white blood cell migration" , "formation of granuloma" and "adjuvant induced arthritis" to examine the antiinflammatory erects of Angelica gigas, Ledebouriella seseloides, Ginkgo biloba and Bamboo salt (Jukyom). The oral administration of the water extract of Angelica gigantis radix, the methanolic extract of Ginkgo folium and the aqueous solution of Bamboo salt showed antiinflammatory effect on carrageenan and PAF induced foot edema in SD rat at a dose of 1 g/kg. The same administration of methanolic extract of Ginkgo folium also inhibited the vascular permeability in mice. The aqueous solution of Bamboo salt inhibited the formation of ganuloma in SD rats at a oral dose of 1 g/kg. Angelica gigantis radix seems to have antiinflammatory effect by inhibition of PAF.

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