• 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.

• Journal of Oriental Neuropsychiatry
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• v.29 no.3
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• pp.121-134
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• 2018

Objectives: The purpose of this in vivo study is to observe anti-amnesic effects of Yeongkyekamjotanggayonggolmoryo (YGYM), a novel mixed herbal prescription, Ossis Mastodi and Ostreae Testa added Yeongkyekamjo-tang, on scopolamine induced amnesia in C57BL/6 mice through acetylcholine (ACh) and acetylcholinesterase (AChE) activity, Choline acetyltransferase (ChAT) mRNA expression, and antioxidant effects. Methods: Six groups, total 20 intact or 100 Sco treated mice were used in this study after one week of acclimatization period. Half the animals were used for passive avoidance task tests and hippocampus ACh content, AChE activity, and ChAT mRNA expression were measured. The other half was subjected to an underwater maze test and then the cerebral cortex antioxidant defense system was measured. Results: In the passive avoidance experiment, there was significant decrease in residence time in the bright room and in the underwater maze test, escape latency to escape from the esophagus significantly increased compared with the normal control group. At the final sacrifice, ACh content and ChAT mRNA expression decreased, AChE activity increased, and cerebral cortical MDA increased GSH content, SOD and CAT activity in Sco control mice, as compared to intact vehicle control mice. However, these Sco treatment-related memory loss through AChE activation destroyed the cerebral cortex antioxidant defense system, and was inhibited dose-dependently by 28 days consecutive oral pretreatments of YGYM extracts 500, 250, 125 mg/kg. Conclusions: In the above results, YGYM extract that oral administration of YGYM extracts alleviates the antioxidant defense system, through preservation of ACh mediated by upregulation of ChAT mRNA expression, and increase of AChE inhibition and brain antioxidant defense systems.

• Korean Journal of Pharmacognosy
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• v.33 no.3 s.130
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• pp.211-218
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• 2002

The methanol extracts of 340 kinds of Korean medicinal herbs were examined in vitro for the inhibitory effect on the acetylcholinesterase (AChE, E.C. 3.1.1.7) from electric eel using acetylthiocholine as a substrate. Among tested, the extracts of Coptidis Rhizoma, Phellodendri Cortex, Evodiae Fructus, Myrrha, Arecae Semen and Piperis nigri Fructus were found to exhibit a significant inhibition upon the acetylcholinesterase in a dose dependent manner, respectively.

• Mycobiology
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• v.43 no.2
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• pp.137-149
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• 2015

In the search for novel potent fungi-derived bioactive compounds for bioinsecticide applications, crude ethyl acetate culture filtrate extracts from 110 mangrove fungal endophytes were screened for their toxicity. Toxicity tests of all extracts against brine shrimp (Artemia salina) larvae were performed. The extracts with the highest toxicity were further examined for insecticidal activity against Spodoptera litura larvae and acetylcholinesterase (AChE) inhibition activity. The results showed that the extracts of five isolates exhibited the highest toxicity to brine shrimp at 50% lethal concentration ($LC_{50}$) values of 7.45 to 10.24 ppm. These five fungal isolates that obtained from Rhizophora mucronata were identified based on sequence data analysis of the internal transcribed spacer region of rDNA as Aspergillus oryzae (strain BPPTCC 6036), Emericella nidulans (strains BPPTCC 6035 and BPPTCC 6038), A. tamarii (strain BPPTCC 6037), and A. versicolor (strain BPPTCC 6039). The mean percentage of S. litura larval mortality following topical application of the five extracts ranged from 16.7% to 43.3%. In the AChE inhibition assay, the inhibition rates of the five extracts ranged from 40.7% to 48.9%, while eserine (positive control) had an inhibition rate of 96.8%, at a concentration of 100 ppm. The extracts used were crude extracts, so their potential as sources of AChE inhibition compounds makes them likely candidates as neurotoxins. The high-performance liquid chromatography profiles of the five extracts differed, indicating variations in their chemical constituents. This study highlights the potential of culture filtrate ethyl acetate extracts of mangrove fungal endophytes as a source of new potential bioactive compounds for bioinsecticide applications.

• 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.

• 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.

• Bulletin of the Korean Chemical Society
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• v.32 no.8
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• pp.2593-2598
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• 2011

Polyphenols (PPs) are known as antioxidant compounds having benign biological activities. In this paper, a series of hybrid molecules between the free or acetyl protected polyphenol compounds were synthesized and their in vitro antioxidant activity (DPPH assay) and cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were evaluated. As expected, free phenolic hybrid compounds (6 and 8) showed better antioxidant activity than acetyl protected hybrid compounds (5 and 7) from DPPH assay. But the contrast result was obtained from BuChE inhibition assay. Acetyl protected hybrid compounds (5 and 7) showed better inhibition activity for BuChE than free phenolic hybrid compounds (6 and 8). Specifically, 10 (AcFA-AcFA) were shown as an effective inhibitor of BuChE ($IC_{50}=2.3{\pm}0.3{\mu}M$) and also had a great selectivity for BuChE over AChE (more than 170 fold). Inhibition kinetic studies with acetyl protected compounds (5, 7, 9, and 10) indicated that 5, 7 and 10 are a hyperbolic mixed-type inhibition and 10 is a competitive inhibition type. The binding affinity (Ki) value of 10 to BuChE is $2.32{\pm}0.15{\mu}M$.

• 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 ${\beta}-amyloid$.

• The Korea Journal of Herbology
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• v.34 no.5
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• pp.29-37
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• 2019

Objectives : Bang-poong (Saposhnikovia divaricata; SD) was traditionally used to treat inflammatory disorders. In this study, we aimed to investigate whether Bang-poong and related species including SD, Glehnia littoralis (GL), and Peucedanum japonicum (PJ) possess neuroprotective effects and acetylcholinesterase (AChE) inhibitory activities. Methods : Roots of SD, GL and PJ were extracted with distilled water (DW) or 70% ethanol (EtOH). We assessed 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activities of the extracts. To examine neuroprotective effects, we measured cell viability in PC12 or HT22 cells after treatment of the extracts with $H_2O_2$ or amyloid-beta ($A{\beta}$). To assess anti-neuroinflammatory effects, we measured the nitric oxide (NO) levels after treatment with the extracts and lipopolysaccharide (LPS) in BV2 microglial cells. In addition, we performed AChE inhibition assay to explore effects of the extracts on the cholinergic system. Results : DW and EtOH extracts of SD, GL and PJ showed mild DPPH free radical scavenging activities. Also, DW extracts of GL and PJ showed protective effects against $H_2O_2$-induced toxicity in PC12 cells. In LPS-activated BV2 cells, EtOH extracts of SD, GL and PJ exerted inhibitory effects on NO production. Meanwhile, DW extracts of SD, GL and PJ inhibited the $A{\beta}$-induced cell death in HT22 cells. In addition, DW and EtOH extracts of GL exhibited remarkable inhibitory activities on AChE. Conclusions : We demonstrated that SD, GL and PJ exert anti-oxidative, anti-neuroinflammatory and AChE inhibitory activities. These results indicate that SD, GL and PJ could be potential candidates for neurological disorders.

• Journal of Oriental Neuropsychiatry
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• v.29 no.4
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• pp.207-221
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• 2018

Objectives: The objective of this study was to observe the anti-amnesic effects of Yukmijihwang-tang (YMJHT), on the scopolamine (Sco)-induced memory impairment in C57BL/6 mice through its favorable acetylcholine (ACh). Also, to observe acetylcholinesterase (AChE) activity, Choline acetyltransferase (ChAT) mRNA expressions, and antioxidant effect. Methods: Six groups, with a total of 20 normal and 100 Sco treated mice were selected based on their body weights after 1 week of acclimatization, were used in this study as follows. Half of the mice in each group were used for passive avoidance task tests and hippocampus ACh content, AChE activity and ChAT mRNA expression measurement, and the remaining half in each group used for Morris water maze test and measurement of cerebral antioxidant defense system. Results: Amnesia due to AChE activations and destroyed cerebral cortex antioxidant defense systems were markedly and dose-dependently inhibited after 28 days of continuous oral pre-treatment with YMJHT 400, 200 and 100 mg/kg, respectively. The overall effects of YMJHT 400 mg/kg were similar to those of tacrine 10 mg/kg. Conclusions: Based on the results, it was established that oral administration of YMJHT favorably alleviates Sco-induced memory impairment, through preservation of ACh, mediated by up-regulation of ChAT mRNA expressions and related AChE inhibition and augmentation of cerebral antioxidant defense system, at least in a condition of this experiment. The overall effects of YMJHT 400 mg/kg were similar to those of tacrine 10 mg/kg.