• Archives of Pharmacal Research
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• 제25권6호
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• pp.817-819
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• 2002

In the course of screening Korean natural products for acetylcholinesterase (AChE) inhibitory activity, it was found that a methanolic extract of the aerial parts of Corydalis incisa (Papaveraceae) showed significant inhibitory effects on AChE. Corynoline isolated from this plant inhibited AChE activity in a dose-dependent manner, and the $IC_{50}$ value of corynoline was $30.6{\;}{\mu}M$. The AChE inhibitory activity of corynoline was reversible and noncompetitive.

• 한국균학회지
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• 제44권4호
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• pp.314-317
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• 2016

To develop a new anti-dementia acetylcholinesterase (AChE) inhibitor from edible mushrooms, AChE inhibitory activities were determined on water and ethanol extracts of various edible mushrooms from oriental medicine markets and agriculture markets. As a result, the 70% ethanol extract from Pholiota adiposa fruiting body had the highest AChE inhibitory activity of 30.6, and its water extract also had an AChE inhibitory activity of 23.8%. Therefore, we finally selected P. adiposa as a potent anti-dementia AChE inhibitor-containing mushroom. The AChE inhibitor of P. adiposa was maximally extracted when its fruiting body was treated with water for 3hr at $70^{\circ}C$ and 70% ethanol for 12 hr at $70^{\circ}C$, respectively.

• Archives of Pharmacal Research
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• 제26권9호
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• pp.735-738
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• 2003

The methanolic extract of the twigs of Celtis chinensis was found to show inhibitory activity on acetylcholinesterase (AChE), an enzyme that plays a role in the metabolic hydrolysis of ACh. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of N-p-coumaroyl tyramine. as an inhibitor on AChE. This compound inhibited AChE activity in a dose-dependent manner, and the $IC_50$ value of trans-N-p-coumaroyl tyramine was 34.5 $\mu$g/mL (122 $\mu$M).

• Fisheries and Aquatic Sciences
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• 제6권4호
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• pp.225-227
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• 2003

Acetylcholinesterase (AChE) activity is a potential biomarker for phenanthrene exposure in aquatic organisms. Olive flounder (Paralichthys olivaceus) were exposed to three different concentrations (0.5, 1.0 and 2.0, uM) of phenanthrene for four weeks. AChE activities in the brain, heart and eyes were documented. Inhibition of AChE activity was found significant in flounder treated with a concentration greater than $1.0 {\mu}M$ of phenanthrene. This indicates that a chronic exposure to phenanthrene induces damage in various organs (brain, heart and eyes) and changes of AChE activities might be a useful biomarker to assess the impacts induced by polycyclic aromatic hydrocarbon (PAH). Evidence from this study confirms that the measurement of AChE in the brain and eyes of flounder is a valuable tool that along with other biomarkers can maximize an ecotoxicologists' confidence in assessing the impacts of oil and PAH pollution in the aquatic environment.

• Fisheries and Aquatic Sciences
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• 제7권3호
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• pp.171-173
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• 2004

Activity of acetylcholinesterase (AChE) is well known as a biomarker of exposure to organophosphate compounds in aquatic organisms. However, the effect of diethyl phthalate (DEP), a widely used plasticizer, on the chance of AChE activity is not yet known. Olive flounder (Paralichthys olivaceus) were exposed to DEP 300 and 1,000 mg DEP/kg b.w. through three times of intraperitoneal injection and effects were assessed in AChE activity of brain, muscle, heart and eyes of the exposed fish. AChE activity in various tissues of flounder was inhibited after exposure to DEP as a concentration-dependent manner, especially in brain, muscle and heart. Among tissues examined, heart is supposed to be a major part of body which is seriously damaged by DEP exposure. It indicates that DEP induces toxic effects in various organs (brain, muscle and heart), and changes of AChE activities. Such changed activities of AChE might be a useful biomarker to assess the impacts induced by phthalate esters including DEP.

• International Journal of Industrial Entomology and Biomaterials
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• 제1권1호
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• pp.73-78
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• 2000

We investigated some biochemical properties of acetylcholinesterase (AChE) in the Bombyx mori larval head. 1% Triton X-100 (v/v) was suitable for extracting AChE from the silkworm larval head but 1 M NaCl was not suitable. PAGE analysis showed a single band of AChE that was detected by histochemical staining using acetylthiocholine as a substrate. AChE was also partially purified with Sepharose 6B and DEAE-cellulose column. Finally, the specific activity of partially purified enzyme solution was 7.6. The study on inhibitor specificity indicated that the enzyme under study was a true cholinesterase (ChE) or AChE. AChE activity was maximum at the substrate concentration of $5{\times}10^{-4}$ M and the excess substrate inhibited the AChE activity. The optimal pH and temperature were pH 7.0-9.0 and 30-35$^{\circ}C$.

• 한국약용작물학회지
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• 제17권6호
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• pp.434-438
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• 2009

For the development of a new antidementia functional food or alternative drug using agricultural products, Job's tears (Coix lachrymajobi L.), which shows high acetylcholinesterase (AChE) inhibitory activity (55.1%) was selected and the extraction conditions of AChE inhibitor were optimized. AChE inhibitor of Job's tears was maximally extracted when it was treated with 60% methanol at $40^{\circ}C$ for 6 h. The AChE inhibitor of the methanol extracts was partially purified by systematic solvent extraction, thin layer chromatography, silica gel chromatography and reverse-phase HPLC and the partial purified AChE inhibitor with inhibitory activity ($IC_{50}$) of $0.608\;{\mu}g$ was obtained. The partial purified AChE inhibitor was soluble in methanol and hexane, and insoluble in water. Its maximum absorption spectra was 230 nm and also it was stable in the range of $30^{\circ}C$ and $70^{\circ}C$ and pH 4.0-8.0 for 1 h.

• 한국환경과학회지
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• 제17권12호
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• pp.1325-1330
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• 2008

This study was carried out with the detection for multiresidue of the carbamate pesticide such as carbaryl and cabofuran by enzyme-inhibition method. The check time for determination of acetylcholinesterase(AChE) activity was selected at 60 sec. The AChE activity in chicken brain determined by the Ellman's method was $162{\mu}$mol/min/g protein. $I_{50}$ for AChE by carbamate pesticide with wet kit was 0.169mg/L of carbaryl and 0.089mg/L of cabofuran, respectively. The incubation time for enzyme kit with substrate kit was 30min for determination of AChE activity. Enzyme kit with substrate kit was stable at $4^{\circ}C\;and\;25^{\circ}C$ for 5 days. Limit detection concentration of carbaryl with dry kit for AChE was 0.05mg/L. The dry kit such as wet kit applied Enzyme-Inhibition(EI) method with AChE was confirmed the multi residue method to detect the carbamate pesticides.

• 한국응용곤충학회지
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• 제30권2호
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• pp.117-123
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• 1991

벼멸구의 살충제 저항성 기구를 구명하고자 fenobucarb, carbofuran 및 diazinon으로 벼멸구를 14~18세대 누대 도태하여 얻어진 벼멸구를 대상으로 저항성 기구를 조사하였으며, 얻어진 결과중 acetylcholinesterase(AChE)와 esterase의 활성 변화에 대하여 보고하고자 한다. AChE활성은 fenobucarb선발 계통에서 1.6배 증가하였으나 타 계통에서는 차이가 없었고, 세포내 분포도 mitochondrial fraction에서 70% 이상으로 계통간 차이가 없었다. 반면, AChE감수성은 fenobucarb와 carbofuran선발 계통에서 각각의 공시 살충제에 대하여 12.2배, 5.6배 감소하였으나 diazinon선발 계통에서는 diazoxon에 대하여 1.7배 감소에 그쳤다. Esterase활성은 fenobucarb선발계통에서 5.6~6.8배, carbofuran선발계통에서 6.4~7.8배, diazinon선발계통에서 4.0~4.4배 증가하였다. 벼멸구의 저항성 증가에 다른 요인이 관련됨을 배제할 수 없으나, 본 실험 결과 esterase 활성증가와 AChE감수성 저하라는 두 요인이 상승적으로 작용하여 벼멸구 저항성을 유발하였음을 확인하였다.

• 한국환경농학회지
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• 제6권2호
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• pp.77-83
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• 1987

유기인계(有機燐系) 살충제인 phorate 가 병아리의 Acetylcholin esterase 활성(活性) 저해(沮害)에 미치는 영향(影響)을 조사한 결과(結果)는 다음과 같았다. Phorate와 그 대사물(代謝物)에 대(對)한 AChE 및 ChE 활성(活性)의 $I_{50}$값은 phosphorothiolate형(型)(표현불가)이 phosphorodithiolate형(型)(표현불가)보다 약(約) $700{\sim}2500$배(培) 낮았으며, 측쇄(側鎖)의 산화(酸化) 상태별(狀態別)로 보면 sulfide>sulfoxide>sulfone의 순(順)으로 $I_{50}$값이 낮은 경향(傾向)이었다. 병아리에 대(對)한 phorate의 급성경구독성(急性經口毒性)은 1.02mg/kg 이었다. Phorate를 급성경구독성(急性經口毒性) $LD_{50}$값 이하(以下)로 경구(經口) 투여(投與)하였을 때 투여(投與) 후(後) 초기(初期)에는 혈장(血漿) ChE 활성(活性)이 뇌(腦) AChE 활성(活性)보다 더 크게 저해(沮害)되었으나, 효소활성(酵素活性)의 회부(回復)은 뇌(腦) AChE 보다 혈장(血漿) ChE 가 더 빠른 경향(傾向)을 보였다.