• The Korea Journal of Herbology
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• v.37 no.4
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• pp.39-48
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• 2022

Objectives : In the present study, we assessed the effects of water extract of Ulmus davidiana(UED) on the learning and memory impairments induced by scopolamine in mice through its favorable acetylcholinesterase (AChE) activity and antioxidant effect. Methods : The memory and cognitive enhancing effect of the UDE was investigated using a passive avoidance test, the Morris water maze test and Y-maze test in mice. In addition, to examine the mechanism of UDE using acetylcholinesterase (AChE) and antioxidant activity. Results : The water extract of UDE (100, and 200 mg/kg) significantly reversed the scopolamine-induced cognitive impairments in the passive avoidance test (P < 0.05). Moreover, UDE (100, and 200 mg/kg) also improved escape latencies in training trials and increased swimming times and distances within the target zone of the Morris water maze (P < 0.05). On the Y-maze test, UDE (100, and 200 mg/kg) also significantly reversed scopolamine-induced cognitive impairments in mice (P < 0.05). In an in vitro study, UDE was found to inhibit acetylcholinesterase, changes in neurotrophic factor (CREB), and antioxidant activity in a dose-dependent manner. Conclusions : The water extract of UDE dramatically possesses the anti-amnestic and cognitive-enhancing activities related to the memory processes, and these activities were parallel to treatment duration and dependent on the learning models. These results suggest that the administration of UDE enhances learning and memory, and that this effect is partially mediated by ERK-CREB-BDNF signaling and the survival of immature neurons.

• Food Science and Preservation
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• v.20 no.6
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• pp.840-845
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• 2013

This study investigated the effects (i.e., the acetylcholinesterase activity, lipid peroxidation, and neuronal survival) of 20 kinds of medicinal water extracts. The water extracts of three medicinal plants - Cornus officinalis, Glycyrrhiza glabra, and Angelica gigas - were found to be the most effective on acetylcholinesterase inhibitory activity. In the lipid peroxidation-generating system induced by $H_2O_2/FeSO_4$ in rat brain homogenates, Perilla frutescens, Polygonum multiflorum, Cinnamomun cassia, and G. glabra exhibited protective activity against lipid peroxidation. The neuronal cell death induced by L-glutamate in PC12 was suppressed by the water extracts of G. glabra, Cinnamomun cassia, Platycodon grandiflorum, and Mentha arvensis at the concentration of $100{\mu}g/mL$. Taken together, these results showed that the water extract of G. glabra has the potential anti-dementia activity, which suggests that it might provide an effective strategy for improving dementia.

• Natural Product Sciences
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• v.29 no.2
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• pp.74-82
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• 2023

Nepeta sibirica L. or Siberian catmint is a medicinal plant species used in Mongolian traditional medicine for curing human different disorders and veterinary practices. The previous study of the whole plant concentrated on the determination of its essential oil composition and reported that the major ones are sesquiterpenes, including nepetalactone. The aim of this study was to reveal a new biological activity of the above-ground parts of N. sibirica L. and compare the activity of different extracts correlating with the content of biologically active compounds and evaluate their toxicity. For this purpose, anti-oxidative and acetylcholinesterase inhibitory activities of the above-ground parts of N. sibirica L. aqueous and ethanol (EtOH) (40%, 70%) extracts were assayed spectrophotometrically. The aqueous extract showed positive anti-oxidative activity by both tested DPPH and FRAP assays with IC₅₀ 134.24 ± 1.42 mg/mL and FRAP value 1385.15 ± 8.12 µmol/L at 200 ㎍/mL, in contrast to 40% and 70% EtOH extracts. The 70% EtOH extract presented the highest acetylcholinesterase inhibitory activity (IC₅₀ 77.29 ± 0.38 mg/mL) followed by 40% EtOH extract (176.72 ± 0.35 mg/mL) and aqueous extract (275.41 ± 0.23 mg/mL). Total phenolics were found to be gallic acid equivalent, % 3.74 ± 0.05 (70% EtOH), 3.94 ± 0.04 (40% EtOH), and 3.79 ± 0.16 (aqueous), whereas the total flavonoids as a rutin equivalent, % as 2.01 ± 0.12, 1.44 ± 0.17 and 1.99 ± 0.02, each. The aqueous extract showed the best anti-oxidative and lowest activity against the acetylcholinesterase; however, the 70% EtOH extract showed the opposite effects than that of the aqueous. No mortality incidence was visible at various doses, indicating that the oral median lethal dose of aqueous and 70% EtOH extracts were considered greater than 5000 mg/kg. N. sibirica L. belongs to the non-toxic category of the OECD 423 classification.

• Journal of Life Science
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• v.23 no.12
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• pp.1525-1531
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• 2013

Baegilju is a famous traditional Korean wine made over the course of 100 days. The physiological functionalities of Baegilju were evaluated using different tests. The spectrophotometric method was used to determine the total concentration of polyphenolics and flavonoids and DPPH and ABTS radicals. A nitrite scavenging assay was used to evaluate antioxidant activity. The fibrin plate method was used for fibrinolysis and to evaluate angiotensin I converting enzyme (ACE) inhibitory activity; finally, the colorimetric determination method was used to evaluate acetylcholinesterase (AChE) inhibitory activity. The total polyphenolic content of non-sterilized Baegilju and sterilized Baegilju were 391.59 ${\mu}g$ and 401.33 ${\mu}g$ tannic acid equivalents/ml, respectively; and the flavonoids contents were 284.75 ${\mu}g$ and 308.35 ${\mu}g$ quercetin equivalents/ml, respectively. Baegilju exhibited more excellent antioxidant activities (DPPH and ABTS radicals, nitrite scavenging activity) than did Cheongju. In addition, the fibrinolytic activity and AChE inhibitory activity were found to be higher in Baegilju than they were in Cheongju. The ACE inhibitory activity of non-sterilized Baegilju, sterilized Baegilju, and Cheongju were 23.62%, 19.99%, and 38.91%, respectively. Therefore, these results suggest that Baegilju has potential as an antioxidant agent and anti-thrombosis agent.

• Biomolecules & Therapeutics
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• v.26 no.3
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• pp.274-281
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• 2018

A previous study in humans demonstrated the sustained inhibitory effects of donepezil on acetylcholinesterase (AChE) activity; however, the effective concentration of donepezil in humans and animals is unclear. This study aimed to characterize the effective concentration of donepezil on AChE inhibition and impaired learning and memory in rodents. A pharmacokinetic study of donepezil showed a mean peak plasma concentration of donepezil after oral treatment (3 and 10 mg/kg) of approximately $1.2{\pm}0.4h$ and $1.4{\pm}0.5h$, respectively; absolute bioavailability was calculated as 3.6%. Further, AChE activity was inhibited by increasing plasma concentrations of donepezil, and a maximum inhibition of $31.5{\pm}5.7%$ was observed after donepezil treatment in hairless rats. Plasma AChE activity was negatively correlated with plasma donepezil concentration. The pharmacological effects of donepezil are dependent upon its concentration and AChE activity; therefore, we assessed the effects of donepezil on learning and memory using a Y-maze in mice. Donepezil treatment (3 mg/kg) significantly prevented the progression of scopolamine-induced memory impairment in mice. As the concentration of donepezil in the brain increased, the recovery of spontaneous alternations also improved; maximal improvement was observed at $46.5{\pm}3.5ng/g$ in the brain. In conclusion, our findings suggest that the AChE inhibitory activity and pharmacological effects of donepezil can be predicted by the concentration of donepezil. Further, $46.5{\pm}3.5ng/g$ donepezil is an efficacious target concentration in the brain for treating learning and memory impairment in rodents.

• 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 Soil Science and Fertilizer
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• v.40 no.4
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• pp.274-279
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• 2007

The toxicitiy of organic sludge such as municipal sewage sludge (MSS), industrial sewage sludge (ISS), alcohol fermentation processing sludge (AFPS) and leather processing sludge (LPS) were evaluated with three environmental biomarkers as acetylcholinesterase, cytochrome P450, and heat shock protein 70 extracted from earthworm (Eisenia fetida). Their toxicities were compared with those of pig manure compost (PMC). MSS, ISS, LPS, and AFPS did not significantly affect the acetylcolinesterase activity, whereas only the elutriate of PMC slightly was increased the activity. MSS, AFPS, and PMC tended to slightly inhibit the cytochrome $P_{450}$ activity, but ISS and LPS showed significantly the inhibitory effect on cytochrome $P_{450}$. The hsp70 expression began to increase after treatments and showed high induction at 6 hour, followed by zero level at around 12 hour. The quantity of the hsp70 expressed by elutriate treatments of PMC, AFPS, MSS, ISS, and LPS was 1.9, 3.0, 3.3, 4.4, and 4.7 fold higher than that of distilled water. These results indicate that in toxicity tests of five organic waste materials, four kinds of sludge materials appeared more toxic than PMC. Results of AChE, P450, and hsp70 of earthworm might be useful for expecting or assessing an effect by exposure of organic wastes to earthworms in soil.

• Applied Biological Chemistry
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• v.41 no.4
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• pp.213-217
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• 1998

An assay for cytochrome P450 monooxygenase activity by determination of the products of organophosphate oxidation via inhibition of acetylcholinesterase was described. Extracts from strains of Oryzaephilus surinamensis selected for resistance to chlorpyrifos-methyl (QVOS 102), fenitrothion (VOS F) and malathion (VOS 3), and a standard susceptible strain VOS 48, were incubated with an organophosphate in the presence of a NADPH-generating system and acetylcholinesterase. The degree of inhibition of the acetylchoinesterase activity was converted to manooxygenase activity using standard curves for the inhibition of acetylcholiesterase by chlorpyrifos-methyl-oxon, fenitrooxon and malaoxan. Activity was detectable in VOS 48 and was present at different increased levels with the different organophosphates in the three resistant strains, suggesting that different forms of P450 might be involved in organophosphate oxidation in these insects. The assays were carried out using crude insect homogenates and much smaller samples of insect material than the standard aldrin to dieldrin assay. It should be possible to use the method for determination of monooxygenase activity in single insert.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.856-859
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• 2002

In the course of finding Korean natural products for acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the roots of Angelica dahurica showed significant inhibitory effects on AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of three furanocoumarins, isoimperatorin (1), imperatorin (2) and oxypeucedanin (3), as active principles. These compounds inhibited AChE activity in a dosedependent manner, and the $IC_{50}$ values of compounds 1-3 were 74.6, 63.7 and 89.1 uM, respectively.

• YAKHAK HOEJI
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• v.35 no.5
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• pp.438-443
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• 1991

This study was designed to examine the effects of diphenhydramine and papaverine on the toxic manifestations of cholinesterase inhibitors. It was found that papaverine increase acetylcholinesterase activity in cerebral cortex of mice. Papaverine pretreatment tended to increase acetylcholinesterase activity against the actions of neostigmine and physostigmine. When diphenhydramine (20~30 mg/kg, s.c.) was treated 20 min before the administration of cholinesterase inhibitor, it significantly extended the onset latency in the signs of toxicosis which were characteristically produced by physostigmine (0.25~1.5 mg/kg, s.c.) or neostigmine (0.125~0.5 mg/kg, s.c.), and it also prevented lethality in all of the animals.