• Journal of Ginseng Research
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• v.35 no.4
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• pp.421-428
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• 2011

This study evaluated cholineresterase inhibitory activity of Korean white ginseng extract (WGE), red ginseng extract (RGE), and black ginseng extract (BGE) and the cholinergic effect on scopolamine (SCOP)-induced amnesic mice. WGE, RGE, and BGE inhibited acetylcholineserase (AChE), as well as butyrylcholineserase (BuChE) in a concentration-dependent manner. BGE presented strong inhibition of AChE with an $IC_{50}$ value of 1.72 mg/mL, followed by WGE (5.89 mg/mL), RGE (6.30 mg/mL), respectively. The inhibitory activity of the three ginseng extracts on BuChE showed similar values among the groups. To better understand the mechanisms of the possible effect of ginseng extract on the cholinergic function, this study assessed the expression of the cholinergic markers of choline acetyltransferase (ChAT) and AChE using western blot and RT-PCR analysis in the brains of amnesic mice. Treatment with ginseng extracts led to inhibition of AChE expression and, the activation of ChAT expression in the hippocampus and the cerebral cortex of amnesic mice as induced by SCOP. The results suggest that ginseng extracts including BGE, appear to modulate the metabolism of acetylchoine (ACh), which would greatly increase synaptic ACh levels and most potently revert SCOP-induced amnesia.

• BMB Reports
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• v.31 no.3
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• pp.296-302
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• 1998

A potentiometric flow injection biosensor for the analysis of anti-cholinesterases (anti-ChEs), based on inhibition of enzyme activity, was developed. The sensor system consists of a reactor with acetylcholinesterase (AChE) immobilized on controlled pore glass and a detector with an $H^{+}-selective$ PVC-based membrane electrode. The principle of the analysis is based on the fact that the degree of inhibition of AChE by an anti-ChE is dependent on the concentration of the anti-ChE in contact with AChE. The sensor system was optimized by changing systematically the operating parameters of the sensor to evaluate the effect of the changes on sensor response to ACh. The optimized biosensor was applied to the analysis of paraoxon, an organophosphorus pesticide. Treatment of the inhibited enzyme with pyridine-2-aldoxime fully restored the enzyme activity allowing repeated use of the sensor.

• Korean Journal of Food Science and Technology
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• v.44 no.4
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• pp.447-451
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• 2012

In order to investigate the efficacies for cognitive function of edible plants, we measured the inhibitory effects of acetylcholinesterase(AChE) activity, radical scavenging activities, and the contents of GABA and glutamate in the plant extracts. Among the plant extracts, Schizandra chinensis contained the highest GABA 14.8 mg/g and the extracts of Cnidium officinale and Polygonum multiflorum also had a relatively high GABA. On the other hand, plant extracts except, Acorus gramineus, showed similar glutamate contents. S. chinensis, Hovenia dulcis, Thuja orientalis, and Eleutherococcus senticosus exhibited high inhibition against AChE activities at about 18-33% at 1 mg/mL. In addition, strong radical scavenging activities were also detected in those extracts which showed high AChE inhibition. Taken together, H. dulcis, T. orientalis, E. senticosus, and S. chinensis could be effective resources for enhancing cognitive function. Further, it was suggested that the AChE inhibitory activities of plant extracts might be related to antioxidative activity.

• Molecular & Cellular Toxicology
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• v.2 no.3
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• pp.216-221
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• 2006

The cholinesterase-inhibiting organophosphorous (OP) compounds known as nerve agents are highly toxic. The principal toxic mechanism of OP compounds is the inhibition of acethylcholine esterase (AChE) by phosphorylation of its catalytic site. The reversible competitive inhibition of AChE may prevent the subsequent OP intoxication. In this study, three-dimensional quantitative structure-activity relationship (3D-QSAR) was performed to investigate the relationship between the 29 compounds with structural diversity and their bioactivities against AChE. In particular, predictive models were constructed using the comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA). The results indicate reasonable model for CoMFA ($q^{2}=0.453,\;r^{2}=0.697$) and CoMSIA ($q^{2}=0.518,\;r^{2}=0.696$). The presence of steric and hydophobic group at naphtyl moiety of the model may lead to the design of improved competitive inhibitors for organophosphorous intoxication.

• 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.

• Journal of Pharmacopuncture
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• v.22 no.4
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• pp.231-238
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• 2019

Objectives: Alzheimer's disease (AD), an overwhelming neurodegenerative disease, has deleterious effects on the brain that consequently causes memory loss and language impairment. This study was intended to investigate the neuroprotective activity of the two essential oils (EOs) from Iranian Pistacia khinjuk (PK) leaves and Allium sativum (AS) cloves against β-Amyloid 25-35 (Aβ25-35) induced elevation of cholinesterase enzymes in AD. Methods: The EOs of PK (PKEO) and AS (ASEO) were prepared and analyzed in terms of extraction yield, phenolic content, and cholinergic markers in vitro. Moreover, both were administered orally to adult male Wistar rats at concentrations of 1, 2, and 3%. The inhibitory potential of PKEO and ASEO was compared with Donepezil (0.75 mg/kg) against the high activities of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Results: PKEO reached an inhibition rate of 83.6% and 81.4% against AChE and BChE, respectively. ASEO had lower anti-cholinesterase activity (65.4% and 31.5% for the inhibition AChE and BChE). PKEO was found to have more phenolic content than ASEO. A significantly positive correlation was observed between the total phenolics and anti-cholinesterase potential. In rats, both EOs decreased the enzyme activity in a concentration-dependent manner. As compared with Donepezil, the significant difference in the AChE and BChE inhibition occurred as rats were treated with PKEO 3% (p < 0.05). Conclusion: It could be concluded that PKEO and ASEO are potent inhibitors of AChE and BChE in rats that hold promise to be used for the treatment of AD.

• Korean Journal of Environmental Agriculture
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• v.14 no.2
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• pp.171-178
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• 1995

The purpose of this study was to investigate the identification and the toxicological effects of some impurities present in the technical grade phosalone (94.4%). In instrumental analyses of the technical phosalone, the five impurities such as phosalone oxon, 6-chloro-3-methylthio-2-oxobenzoxazole, 6-chloro-2-oxobenzoxazole, O,O,S-triethyl phosphorodithioate (OOSTEPDT) and dichlorophosalone were identified. The bimolecular inhibition rate constants ($k_i$) indicated that the technical phosalone inhibited both AChE and BuChE about ten times faster than the purified phosalone did. From in vivo studies the technical phosalone showed greater inhibition for mouse brain AChE, rat blood ChE's and mouse cytosolic non-specific esterases. It was presumed that some impurities present in the technical phosalone such as phosalone oxon cause such inhibition patterns of the technical phosalone observed in this study.

• 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.

• Journal of Physiology & Pathology in Korean Medicine
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• v.16 no.2
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• pp.215-219
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• 2002

Over the past decade there has been a resurgence of interest in botanical products for their medicinal uses. This present study was designed to screen medicinal plants for the treatment of brain diseases such as Alzheimer's disease or aging. We tested the effects of the water extracts from 41 species medicinal plants on acetylcholinesterase (AChE) inhibition and antioxidant activity in vitro. Among them, Euodia rutaecarpa, Rubus coreanus, Achyranthes japonica, Morus alba, Salvia miltiorrhiza, Liriope platyphylla, and Rheum palmatum showed relatively AChE inhibition potency over 80%. Among the 7 medicinal plants investigated, E. rutaecarpa showed an 25%, 65%, and 93% inhibitions on AChE activity at 2.5, 12.5, and 25 ㎍/㎖ of the extract, respectively and was found to be one of most potent AChE inhibitor. The water extracts from 4 species (E. rutaecarpa, R. coreanus, A. iaponica, and M. alba) were tested on their antioxidant capacities using radical scavenging effect against ABTS/sup ㆍ+/. Among the 4 medicinal plants investigated, both R. coreanus and E. rutaecarpa showed significant antioxidant capacity. Therefore, E. rutaecarpa and R. coreanus are expected to ameliorate the clinical symptoms in Alzheimer's disease due to significant AChE inhibition and radical scavenging effect.

• Fisheries and Aquatic Sciences
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• v.25 no.2
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• pp.49-63
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• 2022

Anti-cholinesterase (ChE)s are commonly prescribed as the symptomatic treatment of Alzheimer's disease. They are applied to prevent the breakdown of neurotransmitter acetylcholine (ACh) that bind to muscarinic and nicotinic receptors in the synaptic cleft. Seaweeds are one of the richest sources of bioactive compounds for both nutraceuticals and pharmacognosy applications. This study aimed to determine the anti-ChEs activity of Gracilaria manilaensis, one of the red seaweeds notables for its economic importance as food and raw materials for agar production. Methanol extracts (GMM) of G. manilaensis were prepared through maceration, and further purified with column chromatography into a semi-pure fraction. Ellman assay was carried out to determine the anti-acetylcholinesterase (AChE) and anti-butyrylcholinesterase (BuChE) activities of extracts and fractions. Lineweaver-Burk plot analysis was carried out to determine the inhibition kinetic of potent extract and fraction. Major compound(s) from the most potent fraction was determined by liquid chromatography-mass spectrometry (LCMS). GMM and fraction G (GMMG) showed significant inhibitory activity AChE with EC₅₀ of 2.6 mg/mL and 2.3 mg/mL respectively. GMM and GMMG exhibit mixed-inhibition and uncompetitive inhibition respectively against AChE. GMMG possesses neuroprotective compounds such as cynerine A, graveolinine, militarinone A, eplerenone and curumenol. These findings showed a promising insight of G. manilaensis to be served as a nutraceutical for neuronal health care in the future.