• Title/Summary/Keyword: Acetylcholinesterase (AChE) activity

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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.

Screening of 50 Korean Herbal formulas with Inhibitory Effects on Acetylcholinesterase Activity and Amyloid-β Aggregation (다빈도 한약 처방 50종의 아세틸콜린 분해 효소 활성 및 아밀로이드 베타 단백질 응집 억제 효능 비교 연구)

  • Lim, Hye-Sun;Kim, Yoonju;Kim, Ohn Soon;Jeong, Soo-Jin
    • Korean Journal of Pharmacognosy
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    • v.47 no.3
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    • pp.287-294
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    • 2016
  • Acetylcholinesterase (AChE) activation and amyloid-${\beta}$ ($A{\beta}$) aggregation are major biological markers of Alzheimer's disease. In the present study, we evaluated the inhibitory effects of 50 kinds of herbal formulas on AChE activity and $A{\beta}$ aggregation. Among them, Hwanglyeonhaedok-tang, Cheonwangbosim-dan, Makmundong-tang, and Gamisoyo-san had a potent effects on the inhbition of AChE activity. Sosiho-tang, Samsoeum, Cheonsimyeunjaeum, and Bunsimgieum exerted to have the inhibitory activity on $A{\beta}$ aggregation. In addition, these 8 herbal formulas showed the 3-ethyl-benzothiazoline-6-sulfonic acid (ABTS) radical scavenging activity, indicating their antioxidant activities.

Isolation of Acetylcholinesterase Inhibitors from the Flowers of Chrysanthemum indicum Linne

  • Lim, Soon-Sung;Han, Sag-Myung;Kim, Sun-Young;Bae, Young-Soo;Kang, Il-Jun
    • Food Science and Biotechnology
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    • v.16 no.2
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    • pp.265-269
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    • 2007
  • There is significant interest in finding new sources of acetylcholinesterase (AChE) inhibitors for use in treating Alzheimer's disease, since only a few AChE inhibitors are available for clinical use, such as galanthamine, physostigmine, and tacrine. The ethanol extract of Chrysanthemum indicum Linne flowers was analyzed and found to markedly decrease AChE activity. Acaciin and $acacetin-7-O-{\beta}-D-galactopyranoside$ were identified as the active compounds responsible for the AChE inhibition by using an activity-guided fractionation strategy. The relationship between structure and activity for five flavonoids (acaciin, $acacetin-7-O-{\beta}-D-galactopyranoside$, luteolin, and two other commercially available flavonoids, i.e., apigenin and acacetin) was also investigated, revealing that the presence of methoxy groups at C-4' in the B ring and a sugar at O-7 in ring A appear to be essential for the inhibition of AChE.

Acetylcholinesterase Inhibition and Behavioral Changes of Crucian carp (Carassius auratus) Exposed to the Waterborne Parathion (Parathion에 노출된 붕어(Carassius auratus)의 Acetylcholinesterase 억제와 행동변화)

  • Cho, Kyu-Seok;Park, Jong-Ho;Lee, Won-Ho;Kang, Ju-Chan
    • Journal of Korean Society on Water Environment
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    • v.22 no.2
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    • pp.364-369
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    • 2006
  • The investigation of the Acetylcholinesterase (AChE) activity in tissues (brain, eye, muscle and serum) of crucian carp (Carassius auratus) exposed to the waterborne parathion was carried out for application as biomarker of organophosphate pesticides. The AChE activities were significantly inhibited in the experimental organs of C. auratus treated ${\geq}63{\mu}g/L$ of concentrations of parathion. The AChE activity of C. auratus was significantly reduced in response to brain (79.1~92.4%), eye (76.0~91.5%), muscle (89.7~97.6%) and serum (68.9~78.0%) after 30 days exposure. No significant mortality occurred during the experiment duration but behavioral changes occurred in the carp after exposure to the parathion were erratic swimming and convulsions. The anomaly in the carp exposed to parathion were observed in the form of scoliosis. The use of AChE activity and other adverse responses of the carp might be use as a reliable monitoring tool to detect parathion in aquatic ecosystem which might produce significant population changes.

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.

Potency of Several Structurally Different Acetylcholinesterase Reactivators to Reactivate House Fly and Bovine Acetylcholinesterases Inhibited by Paraoxon and DFP

  • Park, No-Jung;Jung, Young-Sik;Musilek, Kamil;Jun, Daniel;Kuca, Kamil
    • Bulletin of the Korean Chemical Society
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    • v.27 no.9
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    • pp.1401-1404
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    • 2006
  • Eight structurally different acetylcholinesterase reactivators derived from currently commercially available oximes were tested for their potency to reactivate acetylcholinesterase inhibited by pesticide paraoxon (P) and DFP (D). Housefly AChE (F) and bovine red blood cell AChE (B) were used as the source of the cholinesterases. Ellman's method was taken to examine cholinesterases activity. The results show that four AChE reactivators are potent AChE reactivators, able to reach reactivation potency of more than 30% in all cases - PF, PB, DF and DB. Their reactivation potency was comparable with that of pralidoxime and even higher compared with that of HI-6, standard AChE reactivators currently available on the market.

Antioxidant and Acetylcholinesterase Inhibition Activity of Mulberry Fruit Extracts

  • Lee, Young-Ju;Lee, Ka-Hwa;Ahn, Chang-Bum;Chun, Soon-Sil;Je, Jae-Young
    • Food Science and Biotechnology
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    • v.18 no.6
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    • pp.1532-1536
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    • 2009
  • The objective of this study was to evaluate the antioxidant effects and acetylcholinesterase (AChE) inhibition activity of mulberry fruit extracts prepared by hot water (MFH) and 80% ethanol (MFE). Total polyphenolic contents of MFH and MFE were $195{\pm}3.4\;mg$ gallic acid equivalents/g MFH and $185{\pm}2.8\;mg$ gallic acid equivalents/g MFE. MFH and MFE significantly quenched 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydrogen peroxide dose-dependently, and showed high chelating ability and reducing power in non-cellular systems. MFH and MFE also inhibited the formation of intracellular reactive oxygen species and lipid peroxidation, and elevated intracellular glutathione (GSH) levels in RAW264.7 cells. In addition, MFH and MFE also dose-dependently suppressed AChE activity.

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.

Identification of the Component with Anti-acetylcholinesterase Activity from the Essential Oil of Artemisia iwayomogi (더위지기 정유로부터 아세틸콜린에스테라제 억제활성 성분의 동정)

  • Choi, Jae Sue;Song, Byong-Min;Park, Hee-Juhn
    • Korean Journal of Plant Resources
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    • v.30 no.1
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    • pp.17-21
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    • 2017
  • Since the acetylcholinesterase (AChE) inhibitor is used to treat Alzheimer's disease, the present study aimed to analyze the component with anti-AChE activity from the essential oil of Artemisia iwayomogi (Compositae). The four major components of the essential oil were identified to be camphor (29.8%), borneol (28.0%), eucalyptol (5.81%) and coumarin (5.49%) from a gas chromatography-mass spectrometry (GC-MS). The essential oil and its three components, camphor, borneol, and coumarin, were subjected to anti-AChE assay. The $IC_{50}$ values of the essential oil and coumarin were shown to be $0.298mg/m{\ell}$ and $0.236mg/m{\ell}$, though those of other two components, camphor and borneol, were more than $0.250mg/m{\ell}$. These results suggest that coumarin is an active substance of this essential oil with anti-AChE activity.

Inhibitory effect of Capparis zeylanica Linn. on acetylcholinesterase activity and attenuation of scopolamine-induced amnesia

  • Chaudhary, Amrendra Kumar;Solanki, Ruchi;Singh, Vandana;Singh, Umesh Kumar
    • CELLMED
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    • v.2 no.2
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    • pp.19.1-19.6
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    • 2012
  • $Capparis$ $zeylanica$ Linn. a 'Rasayana' drug is used for its memory enhancing effects in the traditional Ayurvedic system of medicine. The aim of this study was to evaluate acetylcholinesterase (AChE) inhibitory and memory enhancing activities of $Capparis$ $zeylanica$ Linn. The$in-vitro$ and $ex-vivo$ models of AChE inhibitory activity were used along with Morris water maze test to study the effect on memory in rats. The anticholinesterase effect of methanolic and aqueous extracts of $Capparis$ $zeylanica$ was measured by spectrophotometric Ellman method at 0.1, 0.3, 1.0, 3.0, 10 and 30 mg/ml and brain monoamine oxidase (MAO-A and MAO-B) activity was assessed by Naoi's method. The results $in-vitro$ and $ex-vivo$ AChE assay revealed that methanolic and aqueous extracts of $Capparis$ $zeylanica$ inhibit AChE activity, whereas these extracts did not alter MAO activity at any concentration tested as compared to moclobemide and L-deprenyl. The results indicate that $Capparis$ $zeylanica$ improves scopolamine-induced memory deficits through inhibition of AChE activity, and not by direct MAO inhibition.