• 한국자원식물학회지
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• 제31권1호
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• pp.10-15
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• 2018

황칠나무 잎과 줄기를 분리하여 각각 methanol 추출하여, 계통분획상법에 따라 dichloromethane, ethyl acetate, butanol로 분획하였다. 분획물로 실시한 TLC에서 알칼로이드 성분으로 분리되는 성분을 확인할 수 있었다. 잎과 줄기 모두 ethyl acetate분획물은 $IC_{50}$ $30{\mu}g/m{\ell}$으로 높게 측정 되었으며, ethyl acetate, dichloromethane, butanol분획물 순으로 저해 활성이 높게 나타났다. Acetyl cholinesterase inhibition assay를 실시한 결과 황칠나무 잎과 줄기 모두 dichloromethane, ethyl acetate, butanol 분획물 순으로 저해 활성이 높은 것으로 나타났으며, 가장 높은 활성을 보인 황칠나무 줄기와 잎의 dichloromethane 분획물의 알칼로이드 함량이 상대적으로 높은 것으로 보아 알칼로이드 성분에 의한 것으로 유추 할 수 있으므로, 알칼로이드 성분의 동정 및 성분구조의 규명을 통하여 AChE저해 활성을 이용한 신경관련 질환에 도움을 줄 수 있는 천연물의 개발이 가능할 것으로 사료된다.

• 약학회지
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• 제35권5호
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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.

• 한국환경보건학회지
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• 제22권3호
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• pp.8-16
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• 1996

Effects of water extract of aloe vera on lead-induced neurotoxicity were investigated in sciatic nerve isolated from rat. The mechanism on toxicity reduction by measuring activities of axonal enzymes, metabolism of myo-inositol in nerve, lead concentration in several organs and so on were further examimed. In the lead-treated rats, the transport rate of axonal enzyme, such as acetyl cholinesterase and choline acetyltransferase, was reduced by from 50% to 30% respectively. Reduction in myo-inositol concentration and $Na^+/K^+$ ATPase activity were also observed in sciatic nerve from lead-treated rat. However, the aloe extract administration significantly eliminated the impairment and maintained myo-inositol concentration to about 85% of normal level. Also aloe extract promoted the excretion rate of lead which is accumulated in blood, sciatic nerve and kidney. These results suggest that lead-induced neurotoxicity was significantly reduced by administration of aloe extract and the mechanism might be partly increase in kidney excretion rate of lead and parity normalization of $Na^+/K^+$ ATPase activity which is critical factor in order to keep nerve maintaining normal myo-inositol level.

• Fisheries and Aquatic Sciences
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• 제14권2호
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• pp.89-92
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• 2011

We investigated the antioxidant and cholinesterase inhibitory activities of the aqueous extract of rainbow trout Oncorhynchus mykiss. The antioxidant activity of O. mykiss aqueous extract was determined by in vitro peroxynitrite scavenging activity and reducing power assays. The aqueous extract of O. mykiss showed potent peroxynitrite radical scavenging activity ($IC_{50}=0.12{\pm}0.001\;mg/mL$) and reducing power (absorbance=$0.47{\pm}0.001$) at the concentration of 1 mg/mL. The in vitro cholinesterase inhibitory activity of O. mykiss aqueous extract was examined using spectrophotometric analyses of acetyl- and butyrylcholinesterase. The aqueous extract of O. mykiss showed acetylcholinesterase inhibitory activity ($IC_{50}=1.61{\pm}0.13\;mg/mL$), but did not exhibit inhibitory activity against butyrylcholinesterase. These results suggest that O. mykiss possesses antioxidant and acetylcholinesterase inhibitory activities and provide scientific evidence for the health benefits of O. mykiss aqueous extract.

• Natural Product Sciences
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• 제24권4호
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• pp.259-265
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• 2018

The three flavone glycosides, 4'-O-methylisoscutellarein 7-O-(6'''-O-acetyl)-${\beta}$-D-allopyranosyl(1${\rightarrow}$2)-${\beta}$-D-glucopyranoside (1), isoscutellarein 7-O-(6'''-O-acetyl)-${\beta}$-D-allopyranosyl(1${\rightarrow}$2)-${\beta}$-D-glucopyranoside (3), and isoscutellarein 7-O-${\beta}$-D-allopyranosyl(1${\rightarrow}$2)-${\beta}$-D-glucopyranoside (4) in addition to a flavonol glycoside, kaempferol 3-O-${\beta}$-D-glucopyranoside (astragalin, 2), were isolated from Stachys japonica (Lamiaceae). In cholinesterase inhibition assay, compound 1 significantly inhibited aceylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities ($IC_{50}s$, $39.94{\mu}g/ml$ for AChE and $86.98{\mu}g/ml$ for BChE). The content of isolated compounds were evaluated in this plant extract by HPLC analysis. Our experimental results suggest that the flavonoid glycosides of S. japonica could prevent the memory impairment of Alzheimer's disease.

• Journal of Yeungnam Medical Science
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• 제16권2호
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• pp.326-332
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• 1999

이 연구에서는 유기인제 농약으로 인한 acetylcholinesterase와 pseudolcholinesterase의 활성도 변화와 알콜과 유기인제 농약의 상호 작용시 효소 활성도 변화를 비교하고, 임상적으로 쓰이고 있는 가역성 항콜린에스터라제 약물과도 비교하여 여러 항콜린에스터라제 약물의 효능과 알콜 섭취가 콜린에스터라제 활성도에 미치는 영향을 파악하는 것에 이 실험의 목적을 두었다. 남자 대학생 15명을 무작위 추출하여 상박부 정맥에서 채혈하여 혈액중 적혈구내에 존재하는 acetylcholinesterase와 혈장에 존재하는 acetylcholinesterase를 분리하였고 cholinesterase가 acetylcholine을 acetic acid와 choline으로 가수분해한다는 점을 이용하여 각 효소에 acetylcholine을 기질로서 주입한 후 1시간 후 생성된 acetic acid에 의해 변화된 pH를 pH meter로 측정하여 간접적으로 활성도를 알아내는 electrometric method를 이용하여 활성도 변화를 측정하였다. 위 실험 조건에서 가역성 항콜린에스터라제 약물이 유기인제 농약보다 콜린에스터라제 활성도를 감소시켰고, 유기인제로 인한 acetylcholinesterase와 pseudocholinesterase의 활성도 변화는 에탄올 처치시 더욱 현저하게 감소되는 것으로 나타났으며, 콜린에스터라제 활성제인 oxime은 acetylcholinesterase에 대해서는 효소 활성도를 높이지만 pseudocholinesterase의 효소 활성도에는 영향을 미치지 않는 것으로 나타났다.

• Advances in Traditional Medicine
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• 제7권2호
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• pp.182-190
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• 2007

Alzheimer's disease is a neurodegenerative disorder associated with a decline in cognitive abilities. Dementia is one of the aged related mental problems and a characteristic symptom of Alzheimer's disease. Nootropic agents like piracetam and cholinesterase inhibitors like $Donepezil^{\circledR}$ are used in situations where there is organic disorder in learning abilities, but the resulting side-effects associated with these agents have limited their utility. Foeniculum (F.) vulgare Linn. is widely used in Indian traditional systems of medicines and also as a house remedy for nervous debility. The present work was undertaken to assess the potential of F. vulgare as a nootropic and anti-cholinesterase agent in mice. Exteroceptive behavioral models such as Elevated plus maze and Passive avoidance paradigm were employed to assess short term and long term memory in mice. To delineate the possible mechanism through which F. vulgare elicits the anti-amnesic effects, its influence on central cholinergic activity was studied by estimating the whole brain acetylcholinesterase activity. Pretreatment of methanolic extract of fruits of F. vulgare Linn. for 8 successive days, ameliorated the amnesic effect of scopolamine (0.4 mg/kg) and aging induced memory deficits in mice. F. vulgare extract significantly decreased transfer latencies of young mice and aged mice, increased step down latency and exhibited significant anti-acetyl cholinesterase effects, when compared to piracetam, scopolamine and control groups of mice. F. vulgare might prove to be a useful memory restorative agent in the treatment of dementia seen in the elderly.

• Environmental Analysis Health and Toxicology
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• 제29권
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• pp.1.1-1.7
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• 2014

Objectives The present subacute study was designed to evaluate the effect of coenzyme Q 10 (CoQ10) in the 28 days aroclor 1254 exposure induced oxidative stress in mice brain. Methods Biochemical estimations of brain lipid peroxidation (LPO), reduced glutathione (GSH), and activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx) and acetyl cholinesterase (AChE), and histopathological investigations of brain tissue were carried out. Results Oral exposure of aroclor 1254 (5 mg/kg) led to significant decrease in levels of GSH, and activities of SOD, CAT, GPx, and AChE, and increase in LPO. These aberrations were restored by CoQ10 (10 mg/kg, intraperitoneal injection [IP]). This protection offered was comparable to that of L-deprenyl (1 mg/kg, IP) which served as a reference standard. Conclusions Aroclor 1254 exposure hampers the activities of various antioxidant enzymes and induces oxidative stress in the brains of Swiss albino mice. Supplementation of CoQ10 abrogates these deleterious effects of aroclor 1254. CoQ10 also apparently enhanced acetyl cholinesterase activity which reflects its influence on the cholinergic system.

• 동의생리병리학회지
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• 제34권2호
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• pp.81-87
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• 2020

Cognitive impairment is symptoms of dementia, a degenerative brain disease that is drawing attention in a rapidly aging society. This study was conducted to investigate the improvement of cognitive function of Leonurus japonicus on scopolamine-induced memory impairment in mice and the effect and mechanism of memory recovery. In vivo studies were conducted on mice orally pretreated with L. japonicus in doses of 50, 100 and 200 mg/kg (p.o.) and scopolamine (1 mg/kg, i.p.) were injected 30 min before the behavioral task. Antioxidant activity was assessed by 2,2-diphenyl-1-picryl hydrazyl (DPPH) assay and 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay, and acetylcholinesterase (AChE) inhibition activity evaluated by Ellman's method. In behavior studies showed that L. japonicus has an improved the memory of scopolamine-treated mice in Y-maze, passive avoidance and Morris water maze test. In addition, L. japonicus was also exerted free radical scavenging activity and inhibited acetyl cholinesterase activity. These results suggest that L. japonicus improves short-term and long-term memory in scopolamine-induced memory decline model and prevents scopolamine-induced memory impairments through in reduced oxidative stress and acetyl cholinesterase inhibition effect. Thus, L. japonicus is related to functional medicinal materials for prevention and treatment of human dementia patients.

• Natural Product Sciences
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• 제26권2호
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• pp.165-170
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• 2020

Carica papaya is a medicinal and fruit plant owing biological activities including antioxidant, antiviral, antibacterial and anticancer. The present study aims to investigate the acetyl (AChE) and butyryl (BChE) cholinesterase inhibitory potentials of C. papaya extracts as well as their chemical compositions. The chemical composition of the active extract was identified using a gas chromatography-mass spectrometry (GC-MS). Ellman enzyme inhibition assay showed that the alkaloid-enriched leaf extract of C. papaya possessed significant anti-BChE activity with an enzyme inhibition of 75.9%. GC-MS analysis showed that the alkaloid extract composed mainly the carpaine (64.9%) - a major papaya alkaloid, and some minor constituents such as aliphatic hydrocarbons, terpenes and phenolics. Molecular docking of carpaine revealed that this molecule formed hydrogen bond and hydrophobic interactions with choline binding site and acyl pocket. This study provides some preliminary findings on the potential use of C. papaya leaf as an herbal supplement for the prevention and treatment of Alzheimer's disease.