• Title/Summary/Keyword: AChE활성저해

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Screening of a Potent Antidementia Acetylcholinesterase Inhibitor-containing Fruits and Optimal Extraction Conditions (항치매성 아세틸콜린에스터라제(Acetylcholinesterase) 저해 물질 함유 과일의 선발 및 저해 물질의 추출 최적 조건)

  • Lee, Eun-Na;Song, Jung-Hwa;Lee, Jong-Soo
    • The Korean Journal of Food And Nutrition
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    • v.23 no.3
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    • pp.318-323
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    • 2010
  • 아세틸콜린에스터라아제(AChE) 저해제에 의한 아세틸콜린 분해 억제는 알츠하이머 질병의 가장 확실한 치료 방법 중의 하나로 알려져 있다. 본 연구는 최근 웰빙 건강 소재로 각광을 받고 있는 과일과 채소로부터 새로운 AChE 저해제를 개발하여 항치매 식품이나 대체 의약품 생산에 응용하기 위해 과일과 채소로부터 AChE 저해 활성이 우수한 시료를 선별하고, AChE 저해 물질의 추출조건을 최적화하였다. AChE 저해 활성은 호두의 메탄올 추출물에서 72.6% ($IC_{50}=14.2\;{\mu}g$)로 가장 높았고, 호두의 AChE 저해 물질은 80% 메탄올로 $40^{\circ}C$에서 12시간 동안 처리하였을 때 가장 많이 추출되었다.

Effect of Terbufos on the Activity of Acetylcholinesterase in the Chicken (Terbufos가 병아리 중(中) Acetylcholinesterase에 미치는 영향(影響))

  • Hong, Jong-Uck;Kim, Jung-Ho;Kim, Jang-Eok
    • Applied Biological Chemistry
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    • v.29 no.3
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    • pp.324-330
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    • 1986
  • The responses of brain acetylcholinesterase(Ach-E) and plasma cholinesterase (Ch-E) activities were studied in chicknes given oral doses of Terbufos(S-tert-butyl thiomethyl 0,0-diethyl phosphorodithioate), an organophosphorus insecticide. The acute oral $LD_{50}$ of terbufos was 1.82mg/kg. The activity of plasma Ch-E was inhibited more rapidly than that of brain Ach-E, whereas recovery of plasma Ch-E activity was more rapid than that of brain Ach-E. Recovery of brain Ach-E and plasma Ch-E was followed the model $Y=a+b(log_{10}X)$. Brain Ach-E activity and plasma Ch-E were inhibited 83% and 94%, respectively, at 60min after administered oral $LD_{50}$. Brain Ach-E and plasma Ch-E was inhibited in vitro by Terbufos

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Screening of Natural Plant Resources with Acetylcholinesterase Inhibition and Antioxidant Activity (천연 식물자원으로부터 Acetylcholinesterase 저해 및 항산화 활성 탐색)

  • Kim, Dae-Ik;Lee, Sung-Hyeon;Hur, Eun-Young;Cho, Soo-Muk;Park, Hong-Ju
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.34 no.3
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    • pp.427-432
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    • 2005
  • This study was performed to investigate the effect of natural plant extracts on acetylcholinesterase (AChE) activity and the free radical scavenging activity. The methanolic extracts of plants were tested for AChE inhibitory activity using Ellman's colorimetric method in 96-welled microplates and antioxidant activity as the scavenging effect of 1, 1-diphenyl-2-picryl hydrazyl radical (DPPH). The results showed that AChE activities were inhibited (about 20-30%) in whole plant extract of Daucus carota var. sativa, Hypericum erectum and Fragaria yezoensis. AChE activities were inhibited (about 32-34%) in stems extract of Gingko biloba and leaves extract of Rhododendrondron yedoensa var. poukhanense. Fruit extract of Zanthoxylum schinifolium inhibited (about 18%) AChE activity. And the DPPH scavenging effects as antioxidant activity were similar to L-ascorbic acid in whole plant extract of Fragaria yezoensis and fruits extract of Comus officinalis.

Inhibition of Acetylcholinesterase and Butyrylcholinesterase by Phosalone via Bioactivation (Phosalone의 활성화과정을 통한 acetylcholinesterase와 butyrylcholinesterase에 대한 활성 저해)

  • Lim, Geum-Choon;Han, Dae-Sung;Hur, Jang-Hyun
    • Applied Biological Chemistry
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    • v.38 no.2
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    • pp.174-178
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    • 1995
  • The purpose of this study was to investigate a role of cytochrome $P_{450}$, for the toxicity of the phosalone in in vitro and in vivo bioactivation systems. The bimolecular inhibition rate constants$(k_i)$ of the phosalone to acetylcholinesterase(AChE) and butyrylcholinesterase(BuChE) were approximately $10^2M^{-1}{\cdot}min^{-1}$, respectively, which meant a poor inhibitor. The potency of the phosalone as an inhibitor of AChE and BuChE was increased about 300 and 40 fold, respectively, when the inhibitor and the ChE were incubated with microsomes fortified with NADPH compared with microsome alone. Piperonyl butoxide(PB) addition to these coupled systems greatly reduced the inhibition of both target enzymes by blocking a bioactivation process. The $I_{50}$ value of the Phosalone alone for rat brain AChE was 170 mg/kg. When PB was pretreated, that value was altered to 42.5 mg/kg. PB pretreatment synergized the inhibition of brain AChE with four times. Rat blood erythrocyte AChE and plasma BuChE were similarly inhibited in vivo by the phosalone and PB pretreatment didn't affect significantly the pattern of the inhibition. The in vivo studies showed different results in the role of cytochrome $P_{450}$ from those of the in vitro studies.

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Antioxidant Activities and Acetylcholinesterase Inhibitory Activities from Seaweed Extracts (해조류의 항산화 활성 및 아세틸콜린에스테라제 저해 활성)

  • Jeon, Young-Eun;Yin, Xing-Fu;Lim, Soon-Sung;Chung, Cha-Kwon;Kang, Il-Jun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.4
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    • pp.443-449
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    • 2012
  • This study was conducted to investigate the antioxidant and acetylcholinesterase (AChE) inhibitory activities of extracts from various seaweed. The extracts of $Sargassum$ $thunbergii$ (91.3%), $Polysiphonia$ $morrowii$ (90.7%), $Ecklonia$ $cava$ (89.9%), and $Artemisia$ $fukudo$ (85.9%) showed over 80% high radical scavenging activities at the final concentration of 40 ${\mu}g$/mL. The $Artemisia$ $fukudo$ extract showed the highest inhibition activity of 30.2% on AChE at the final concentration of 10 ${\mu}g$/mL. The extract of $Porphyra$ $tenera$, $Costaria$ $costata$, $Monostroma$ $nitidum$, $Ecklonia$ $cava$, and $Agarum$ $clathratum$ against AChE at a concentration of 10 ${\mu}g$/mL exhibited inhibition of 26.6%, 25.3%, 23.4%, 21.7%, 20.4% and 19.9%, respectively. The bioautography results showed that the mixtures of structurally diverse compounds were thought to affect AChE inhibitory activity. These results suggest that extracts from seaweed with their high quality components may be effective in the prevention of Alzheimer's disease and may be used to develop various functional food products.

Acetylcholinesterase Inhibitory Effect of Green Tea Extracts According to Storage Condition (저장 조건에 따른 녹차 추출물의 acetylcholinesterase(AChE) 저해 효과)

  • Kwak, Ji Hyun;Jeong, Chang-Ho;Kim, Ji Hye;Choi, Gwi Nam;Shin, Young-Hee;Lee, Seung-Cheol;Cho, Sung Hwan;Choi, Sung-Gil;Heo, Ho Jin
    • Korean Journal of Food Science and Technology
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    • v.41 no.4
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    • pp.435-440
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    • 2009
  • Acetylcholinesterase (AChE) inhibitors, which enhance cholinergic transmission by reducing the enzymatic degradation of acetylcholine, are the only source of the compound that is currently approved for the treatment of Alzheimer's disease (AD). In these experiments, the concentration samples of green tea extracts were 100, 500, and 1,000 ${\mu}g$/mL. Among them, the highest concentration (1,000 ${\mu}g$/mL) of fresh green tea extracts showed the most potent inhibitory effect on AChE by reducing more than 40% of enzyme activity, and in a concentration-dependent pattern. In addition, we examined the effect of other storing conditions on AChE inhibition. In order to maintain storage for 3 months, the materials were held at the certain storing conditions of temperature (room temperature, 4 and $-20^{\circ}C$) and for water activity (0.81, 0.69, and 0.23). In these storing conditions, the difference in temperature did not contribute to the AChE inhibitory effect. Our presented data showed that the AChE inhibitory effect was affected by the concentration of green tea extract and by water activity (0.81). These results suggest that green tea may serve as a potential dietary source of AChE inhibitor.

Evaluation of Acetylcholinesterase Inhibitory and Antioxidative Activities of Rhus javanica (오배자 추출물의 Acetylcholinesterase 저해 및 항산화 활성 평가)

  • Bae, Jong-Sup;Lee, Hyun-Shik;Lee, Ha Yeong;Yoo, Byung-Hyuk;Kim, Taewan;Kim, Yong Han;Kim, Tae Hoon
    • Food Science and Preservation
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    • v.19 no.5
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    • pp.751-756
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    • 2012
  • Antioxidant capacity and acetylcholinesterase (AChE) inhibitory activity of the aqueous methanolic extract of Rhus javanica were investigated in vitro. The antioxidant properties was measured by radical scavenging assays using DPPH and $ABTS^+$ radicals. The AChE inhibitory efficacy of R. javanica was tested by Ellman's assay and the total phenolic content was determined using a spectrophotometric method. All tested samples showed a dose-dependent AChE inhibitory and radical scavenging activities. In particularly, ethyl acetate (EtOAc)-soluble portion from the methanolic extract of R. javanica showed significantly higher inhibitory activity than other organic solvent soluble-portions in an AChE and radical scavenging assay systems. These results suggest that R. javanica may be possess potential benefits which might be useful in development of antioxidant and anti-alzheimer's disease ingredient.

Production of Anti-dementia Acetylcholinesterase Inhibitor from Pleurotus ostreatus (Heuktari) and Inhibitory Effect on PC12 Neuron Apoptosis (흑타리버섯으로부터 항치매성 Acetylcholinesterase 저해물질의 생산 및 PC12 신경세포사 저해 효과)

  • Han, Sang-Min;Kim, Ji-Yoon;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.47 no.4
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    • pp.337-346
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    • 2019
  • To develop a new antidementia acetycholinesterase (AChE) inhibitor from edible mushrooms, the inhibitory effects on AChE of water and ethanol extracts from various edible mushrooms were measured. Among the tested compounds, 70% ethanol extracts from Tremella fuciformis showed the highest AChE inhibitory activity, at 25.3% (IC50: 9.9 mg). Water extracts from the fruiting body of Pleurotus ostreatus (Heuktari) showed AChE inhibitory activity of 20.2% (IC50: 12.4 mg). However, the yield (40.8%) from Pleurotus ostreatus (Heuktari) was higher than that from Tremella fuciformis (5.0%). Therefore, we selected Pleurotus ostreatus (Heuktari) as the most promising candidate for a mushroom containing anti-dementia AChE inhibitors. The AChE inhibitor from Pleurotus ostreatus (Heuktari) was optimally extracted when its fruiting body was treated with water for 6 h at 30℃. The anti-dementia effects of the partially purified AChE inhibitor from Pleurotus ostreatus (Heuktari) were observed in PC12 nerve cells.

Effect of Phorate, an Organophosphorus Insecticide on the Activity of Acetylcholinesterase (유기인계(有機燐系) 살충제 Phorate 가 Acetylcholinesterase 활성(活性)에 미치는 영향(影響))

  • Jung-Ho, Kim;Hong, Jong-Uck
    • Korean Journal of Environmental Agriculture
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    • v.6 no.2
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    • pp.77-83
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    • 1987
  • Present study was carried out to elucidate the effect of phorate (0,0-dietyl S-ethylthiomethyl phosphorodithioate), an organophosphorus insecticide on the acetylcholinesterase(AChE) and cholinesterase(ChE) activity in the chicken brain and plasma. The inhibitory effect of phorate and its metabolites on AChE and ChE activity was also increased in the order of phorate (p=S,S)$(p=S,SO_2)<phoratoxon$ (p=O,S)$(P=O,SO_2)$. Acute oral $LD_{50}$ of phorate was 1.02mg/kg. After oral administration of phorate, the activity of plasma ChE was inhibited more rapidly then that of brain AChE, whereas recovery of plasma ChE activity was more rapid than that of brain AChE activity.

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Toxicological Test Methods and AChE Inhibition of Organophosphorus Acaricides of Twospotted Spider Mite, Tetranychus urticae (점박이응애의 독성 시험방법과 유기인계 살비제 AChE 활성저해에 관한 연구)

  • 김도익;이승찬
    • Korean journal of applied entomology
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    • v.31 no.1
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    • pp.1-6
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    • 1992
  • These studies were carried out to compare toxicological test methods of two spotted spider mite, Tetranychus urticae Koch,; and to investigate relationship between in vivo resistant level of highly acaricide-selected population, and in vitro insensitivity of the AChE in the same population to carbophenothion and ethion. The slide dip method (CV = 8.7%) was of more accuracy and suitability than that of the leaf dip method(CV=12.2%) and leaf disc method (CV= 13.6 %) in determination of the resistant levels of twospotted spider mite to acaricides. The slide dip method also had the advantages of simple treatment with different populations on a slide at the same time, standardization of post-treatement conditions and living plants exclud¬ed from the test. Even though the topical application method(CV =8.1 %) showed high accuracy, it had the demerits of the much time consuming, need of expensive equipment and difficulty of test manipulation. For a limited time, the 22nd successive carbophenothion-selected population of two-spotted spider mite showed 156- and 128-fold resistant levels to carbophenothion and ethion(both alPs), respectively. However, the 24th successive ethion-selected population revealed 64.1- and 65-fold resistant levels to ethion and carbophenothion, respectively. In the inhibition of AChE activity, the carbophenothion-selected population showed 3.3- and 2.7-fold insensitivity in AChE activity to carbophenothion and ethion, respectively. Likewise, the ethion -selected population exhibited 3- and 2.6-fold insensitivity in AChE activity to carbophenothion and ethion, respectively, as compared with that of susceptible population. As a result, a good relation was recognized between in vivo resistance to organophosphorous acaricides and in vitro insensitivity of the AChE to corresponding inhibitors.

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