• Title/Summary/Keyword: acetylcholinesterase inhibitor

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Production and Purification of Acetylcholinesterase Inhibitor from Pseudomonas sp960903 (Pseudomonase sp. 960903에 의한 acetylcholinesterase 억제제의 생산 및 정제)

  • 김경자
    • Microbiology and Biotechnology Letters
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    • v.28 no.6
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    • pp.322-328
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    • 2000
  • To screen agent for the treat-ment of Alzhimers Disease several strains of bacteria producing acetylcholinesterase inhibitor ware isolated from soil. Strain 960903 showed strong acetylcholinesteras inhibitory activity and low butyrylcholinesterse inhibitory activity. The strain 960903 was identified as Pseudomonas sp. Acetylcholinesterase inhibitor ws highly achieved in fermentation medium containing soluble starch 3.0%, glycerol 1.0%, pharmamedia 0.5%, KCI 0.3%, $CaCO_3$ 0.2%, MgS $O_4$..$7H_2$O 0.05%, $KH_2$$PO_4$ 0.05%(pH6.5) at $30^{\circ}C$ for 4 days. Acetylcholinesterase inhibitor was purified by Diaion WA-30($OH^{-}$) column charomatography and cellulose column chromatography. Acetylcholinesterase inhibi-tor showd the maximum wavelength at 205 nm and was soluble in water, acetic acid, ethanol, methanol and dime-thyl sulfoxide. The concentration of 50% inhibition($IC_{50}$) of inhibitor against acetylcholinesterase was 25$\mu\textrm{g}$/ml. The inhibitor was inactivated on heating ar $100^{\circ}C$ fro 15 min and more stable in acidic region than alkaline region.n.

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Screening of Potent Anti-dementia Acetylcholinesterase Inhibitor-containing Edible Mushroom Pholiota adiposa and the Optimal Extraction Conditions for the Acetylcholinesterase Inhibitor

  • Kim, Do-Yeon;Bae, Sang-Min;Han, Sang-Min;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.44 no.4
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    • pp.314-317
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    • 2016
  • To develop a new anti-dementia acetylcholinesterase (AChE) inhibitor from edible mushrooms, AChE inhibitory activities were determined on water and ethanol extracts of various edible mushrooms from oriental medicine markets and agriculture markets. As a result, the 70% ethanol extract from Pholiota adiposa fruiting body had the highest AChE inhibitory activity of 30.6, and its water extract also had an AChE inhibitory activity of 23.8%. Therefore, we finally selected P. adiposa as a potent anti-dementia AChE inhibitor-containing mushroom. The AChE inhibitor of P. adiposa was maximally extracted when its fruiting body was treated with water for 3hr at $70^{\circ}C$ and 70% ethanol for 12 hr at $70^{\circ}C$, respectively.

An Acetylcholinesterase Inhibitor Isolated from Corydalis Tuber and Its Mode of Action (현호색의 Acetylcholinesterase 활성 저해 성분 및 그 작용기전)

  • Hwang, Se-Young;Chang, Young-Pyo;Byun, Soon-Jung;Jeon, Mee-Hee;Kim, Young-Choong
    • Korean Journal of Pharmacognosy
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    • v.27 no.2
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    • pp.91-95
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    • 1996
  • In the course of searching for acetylcholinesterase inhibitors from crude drugs, it was found that total MeOH extract of Corydalis Tuber showed significant inhibitory effect on acetylcholinesterase. To isolate acetylcholinesterase inhibitors from Corydalis Tuber, total MeOH extract of the the crude drug was subjected to activity guided fractionation. The MeOH extract was suspended in water and fractionated with methylene chloride and subjected to acid-base fractionation. Silica gel column chromatography of the basic fraction which showed significant inhibitory effect on acetylcholinesterase was carried out and 5 subfractions (1-5) were obtained. From subtraction 4, compound I was isolated. The structure of isolated compound I was identified by spectroscopic parameters of $^1H-NMR$, $^{13}C-NMR$, EI-MS and FAB-MS. The compound I was identified as berberine. It was found from the Lineweaver-Burk plot that berberine was a reversible and specific inhibitor of acetylcholinesterase having 90% inhibitory effect at the concentration of $2.5{\mu}M$.

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Optimal Extraction Condition and Characterization of Antidementia Acetylcholinesterase Inhibitor from Job's Tears (Coix lachrymajobi L.) (율무로부터 항치매성 Acetylcholinesterase 저해물질의 최적추출 조건 및 특성)

  • Seo, Dong-Soo;Jang, Jeong-Hoon;Kim, Na-Mi;Lee, Jong-Soo
    • Korean Journal of Medicinal Crop Science
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    • v.17 no.6
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    • pp.434-438
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    • 2009
  • For the development of a new antidementia functional food or alternative drug using agricultural products, Job's tears (Coix lachrymajobi L.), which shows high acetylcholinesterase (AChE) inhibitory activity (55.1%) was selected and the extraction conditions of AChE inhibitor were optimized. AChE inhibitor of Job's tears was maximally extracted when it was treated with 60% methanol at $40^{\circ}C$ for 6 h. The AChE inhibitor of the methanol extracts was partially purified by systematic solvent extraction, thin layer chromatography, silica gel chromatography and reverse-phase HPLC and the partial purified AChE inhibitor with inhibitory activity ($IC_{50}$) of $0.608\;{\mu}g$ was obtained. The partial purified AChE inhibitor was soluble in methanol and hexane, and insoluble in water. Its maximum absorption spectra was 230 nm and also it was stable in the range of $30^{\circ}C$ and $70^{\circ}C$ and pH 4.0-8.0 for 1 h.

Production of the Acetylcholinesterase Inhibitor from Yarrowia lipolytica S-3

  • Lee, Dae-Hyung;Lee, Ji-Su;Yi, Sung-Hun;Lee, Jong-Soo
    • Mycobiology
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    • v.36 no.2
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    • pp.102-105
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    • 2008
  • The acetylcholinesterase (AChE) inhibitor of Yarrowia lipolytica S-3 was maximally produced when it was incubated at $30^{\circ}C$ for 36 h in an optimal medium containing 1% yeast extract, 2% peptone and 2% glucose, with an initial pH 6.0. The final AChE inhibitory activity under these conditions was an $IC_{50}$ value of 64mg/ml. After partial purification of the AChE inhibitor by means of systematic solvent extraction, the final $IC_{50}$ value of the partially purified AChE inhibitor was 0.75 mg/ml. We prepared a test product by using the partially purified AChE inhibitor and then determined its stability for the development of a new antidementia commercial product. The test product was stable at room temperature for 15 weeks.

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.

Isolation, Identification and Characterization of a Antidementia Acetylcholinesterase Inhibitor-Producing $Yarrowia$ $lipolytica$ S-3

  • Kang, Min-Gu;Yoon, Min-Ho;Choi, Young-Jun;Lee, Jong-Soo
    • Mycobiology
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    • v.40 no.1
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    • pp.42-46
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    • 2012
  • This report describes the isolation and identification of a potent acetylcholinesterase (AChE) inhibitor-producing yeasts. Of 731 species of yeast strain, the S-3 strain was selected as a potent producer of AChE inhibitor. The selected S-3 strain was investigated for its microbiological characteristics. The S-3 strain was found to be short-oval yeast that did not form an ascospore. The strain formed a pseudomycelium and grew in yeast malt medium containing 50% glucose and 10% ethanol. Finally, the S-3 strain was identified by its physiological characteristics and 26S ribosomal DNA sequences as $Yarrowia$ $lipolytica$ S-3.

Biological Predictors of Alzheimer's Disease Treatment (알츠하이머병 치료의 생물학적 예측인자)

  • Joo, Soo-Hyun;Im, Jeejin;Lee, Chang-Uk
    • Korean Journal of Biological Psychiatry
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    • v.21 no.4
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    • pp.115-117
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    • 2014
  • Variety of biomarkers that are related to the Alzheimer's disease and its diagnosis and progress have been found. However, research lacks in predicting the reaction of the treatment. In addition, there is no definite treatment reaction to the disease but rather it is varied. The purpose of this review article is to study the research of the biomarkers that are able to predict the treatment reaction. There was a research that illustrated a relationship between plasma amyloid ${\beta}$ peptide, cerebrospinal fluid tau, neuroanatomical biomarkers and acetylcholinesterase inhibitors. Polymorphisms in genes of the cholinergic markers AChE, BuChE, ChAT and PON-1 were found to be associated with better clinical response to acetylcholinesterase inhibitors. Many pharmacogenetic studies have been conducted to evaluate the impact of the lipoprotein apolipoprotein E (APOE) genotype on treatment response to acetylcholinesterase inhibitor. However, there is no significant influence of the APOE genotypes on treatment response. Further research is needed to find other predictors of treatment with acetylcholinesterase inhibitors in patients with Alzheimer's disease.

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.

Production of Anti-dementia Acetylcholinesterase Inhibitors from the Wild Yeasts Saccharomyces cerevisiae WJSL0113 and Wickerhamomyces anomalus JSF0128

  • Kim, Ji-Yoon;Lee, Sang-Yeop;Han, Sang-Min;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.46 no.4
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    • pp.447-457
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    • 2018
  • In this paper, the screening of potent acetylcholinesterase (AChE) inhibitor - producing yeasts from wild yeasts and the condition for the production of anti-dementia AChE inhibitors are described. Among one hundred and seven non-pathogenic wild yeast strains from the waters and soils of three main rivers in Daejeon metropolitan city and midstream of Yeongsangang river in Sangju, sporogenous Saccharomyces cerevisiae WJSL0113 and asporogenous Wickerhamomyces anomalus JSF0128 were selected as useful strains for the production of potent AChE inhibitors. The AChE inhibitors of S. cerevisiae WJSL0113 and W. anomalus JSF0128 had a maximum yield when they were incubated in yeast extract-peptone-dextrose media (pH 6.0 in S. cerevisiae WJSL0113 and pH 5.0 in W. anomalus JSF0128) for 18 hr at $30^{\circ}C$, respectively.