• Journal of agriculture & life science
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• v.45 no.6
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• pp.213-226
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• 2011

This study was performed to investigate the effect of essential oils and ethanolic extracts of approximately 650 plant species on acetylcholine esterase (AChE) enzyme activity using Ellman's colorimetric method in 96-well microplates. The results showed that the ethanolic extracts from twig of Sophora subprostrata, twig of Phellodendron amurense, seed of Corylopsis coreana, and essential oil (EO) from Citrus paradisi, Cupressus sempervirens, Ocimum basilicum, Pinus sylvestris and Rosmarinus officinalis inhibited more than 80% of AChE activity. Among these, EO from Pinus sylvestris, C. sempervirens and C paradisi exhibited higher values of AChE inhibitory activity, which were 75, 84 and 99% at a concentration of 50 ug/ml, respectively. Finally, EO from C paradisi (grapefruit, GEO) showed the highest inhibitory activity towards AChE, which showed 91% of inhibition at a concentration of 20 ug/ml. We also examined the anti-dementia effects of GEO in mouse by passive avoidance test and Morris water maze test. The model mouse (male, ICR) of dementia (negative control) was induced by administration of scopolamine (1 mg/kg body weight). The latency time of sample group administrated with GEO (100 mg/kg, p.o.) increased significantly as compared with negative control on passive avoidance test. There were significant recovery from the scopolamine-induced deficits on learning and memory in water maze test through daily administrations with GEO (100 mg/kg, p.o.). From these results, we conclude that GEO treatment might enhance the cognitive function, suggesting that the EO of C. paradis may be a potential candidate for improvement of perceptive ability and dementia.

• Journal of Microbiology and Biotechnology
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• v.23 no.2
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• pp.161-166
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• 2013

At present, acetylcholinesterase (AChE) inhibitors are the first group of drugs to treat mild to moderate Alzheimer's disease (AD). Although beneficial in improving cognitive and behavioral symptoms, the effectiveness of AChE inhibitors has been questioned since they do not delay or prevent neurodegeneration in AD patients. Therefore, in the present study, in order to develop new and effective anti-AD agents from lichen products, both the AChE inhibitory and the neuroprotective effects were evaluated. The AChE inhibitory assay was performed based on Ellman's reaction, and the neuroprotective effect was evaluated by using the MTT method on injured PC12 cells. One AChE inhibitor ($IC_{50}$ = 27.1 ${\mu}g/ml$) was isolated by means of bioactivity-guided isolation from the extract of lichen-forming fungus Cladonia macilenta, which showed the most potent AChE inhibitory activity in previous screening experiment. It was then identified as biruloquinone by MS, and $^1H$- and $^{13}C$-NMR analyses. The inhibitory kinetic assay suggested that biruloquinone is a mixed-II inhibitor on AChE. Meanwhile, biruloquinone improved the viability of the $H_2O_2$- and ${\beta}$-amyloid-injured PC12 cells at 1 to 25 ${\mu}g/ml$. The protective effects are proposed to be related to the potent antioxidant activities of biruloquinone. These results imply that biruloquinone has the potential to be developed as a multifunctional anti- AD agent.

• Food Engineering Progress
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• v.15 no.4
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• pp.289-296
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• 2011

Twenty four fractions by solvent extraction and/or acid precipitation from fruit body and culture broth of Inonotus obliquus were prepared, and their inhibitory effect against acetylcholinesterase (AChE) was investigated. Among these fractions, acid (1 M HCl) precipitates from cell-free culture broth and fruit body exhibited the highest inhibitory effect on AChE in vitro. Acid precipitates inhibited AChE activity in a concentration-dependant manner and $IC_{50}$ values of both acid precipitates were 0.53 mg/mL. The inhibition pattern was general non-competitive inhibition. The energetic parameters were also determined by dual substrate/temperature design. Both acid precipitates increased the values of Ea, ${\Delta}H,/;{\Delta}G$ and ${\Delta}H^{\ast}$ decreasing the value of ${\Delta}S$ for AChE. The results implied that the acid precipitates from I. obliquus increased the thermodynamic barrier, leading to the breakdown of ES complex and the formation of products as inhibitory mechanism.

• 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.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.

• 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.

• Journal of the East Asian Society of Dietary Life
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• v.14 no.1
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• pp.64-69
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• 2004

The deficiency of the neurotransmitter acetylcholine(ACh) is responsible for the initiation of Alzheimer's disease. In addition, there is a simple evidence that oxidative stress significantly increases in persons with Parkinson's disease compared to age-matched healthy persons. Therefore, the objective of the study was to investigate the neurodegeneration inhibitory effect of soybean(Glycine Max) and Yak-Kong(Rhynchosia Nolubilis) by measuring the degree of inhibiting Acetylcholinesterase (AChE) catabolizing the ACh and the free radical scavenger effect in vitro. AChE was measured by the minor modified Ellman assay. Free radical scavenging activity was measured using l-diphenyl-2-picrylhydrazyl (DPPH). First, the MeOH extracts of Soybean and Yak-Kong showed the AChE inhibiting activity of 62.0$\pm$2.43％ and 65.0$\pm$3.29％ at the 5 mg/$m\ell$ concentration. The 50％ inhibitory concentration ($IC_{50}$/) of AChE was 1.96 and 1.31 mg/$m\ell$ in the MeOH extracts of soybean and Yak-Kong. Second, the MeOH extracts of soybean and Yak-Kong showed the free radical scavenger activity of 23.1$\pm$4.26％ and 80.7$\pm$4.61％ at the 5 mg/$m\ell$. IC50 of free radical scavenger activity in Soybean and Yak-Kong was 13.00 and 1.41 mg/$m\ell$ in MeOH extracts and was 5.95 and 2.74 mg/$m\ell$ in hot-water extracts, respectively. In this study, the extracts of Soybean and Yak-Kong showed powerful effects in the AChE inhibition and free radical scavenging. The extracts of Soybean and Yak-Kong were expected to prevent the many neurodegenerative diseases.

• 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.

• Ocean and Polar Research
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• v.39 no.1
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• pp.45-49
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• 2017

During the search for anticholinesterase compounds from marine organisms, we were able to isolate 6,6'-bieckol from a red alga, Grateloupia elliptica. This compound showed moderate acetylcholinesterase (AChE) inhibitory activity in a micromole range ($IC_{50}$ $44.5{\mu}M$). However, for butyrylcholinesterase (BuChE), a new target for the treatment of Alzheimer's disease (AD), it showed particularly potent inhibitory activity ($IC_{50}$ $27.4{\mu}M$), which is more potent compared to AChE. It also inhibits BACE-1, a new target for reducing the generation of ${\beta}-amyloid$.

• 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.