• Journal of Acupuncture Research
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• v.25 no.2
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• pp.1-9
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• 2008

목적 : Acetylcholine은 콜린과 아세트산의 에스테르로 인체에서 중요한 신경전달물질로 Acetylcholine-sterase(AChE)라는 효소에 의해 분해된다. Alzheimer's disease, ataxia, myasthenia gravis, Parkinson' disease 등의 질환에 AChE 억제제가 사용되어 왔으며 최근 한약재의 AChE 억제 효능에 관한 연구들도 진행되고 있다. 봉독은 관절염, 통풍 등의 질환에 응용되어 왔으며 진통효과 및 항염증작용에 대한 임상적, 실험적 연구가 많이 보고되어 왔으나 AChE 억제효과에 대한 연구는 아직까지 보고된 바 없다, 본 연구에서는 봉독약침액과 봉독의 과민반응 유발항원 중 하나인 Phospholipase A2 억제효능이 있는 것으로 알려진 상백피를 혼합한 상백피봉독약침액의 AChE 억제효과를 알아보았다. 방법 : PC12 세포주에서 추출한 AChE와 0.1, 0.01 and $0.001mg/m{\ell}$ 농도의 봉독약침액 및 상백피봉독약침액을 60분간 반응시켰다. 효소면역측정법(ELISA)을 이용하여 흡광도를 10분, 30분, 60분 경과시 각각 측정한 후 효소활성저해도(%)를 계산하였다. 효소활성저해도(%) = [(Cc - Ce)/Cc] ${\times}$ 100 Cc : 대조군 흡광도, Ce : 실험군 흡광도 결과 : 1. 봉독약침액은 0.1, 0.01, $0.001m{\ell}/mg$의 농도에서 30분 경과 후부터 유의성 있는 억제효과를 나타내었다. 2. 상백피봉독약침액은 $0.1m{\ell}/mg$ 농도에서 10분 경과 후부터 유의성 있는 억제효과를 나타내었고, $0.01m{\ell}/mg$ 농도에서 30분경과 시 유의성 있는 억제효과를 나타내었다. 3. 봉독약침액과 상백피봉독약침액의 AChE 억제효과 비교에서 봉독약침액의 억제효과가 상백피봉독약침액 보다 뛰어났다. 요약 : 봉독약침액과 상백피봉독약침액의 AChE 억제효과를 확인하여 두 군 모두 유의성 있는 결과를 얻을 수 있었다. 앞으로 알츠하이머병이나 치매와 같은 신경퇴행성 질환에 대한 봉독의 임상적 활용 및 보다 넓은 범위에 대한 연구가 필요할 것이라 사료된다.

• The Korean Journal of Pesticide Science
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• v.10 no.1
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• pp.50-55
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• 2006

A field-resistant strain of the diamondback-moth(Plutella xylostella L.), collected from Chinese cabbage alpine farmland at Gangwon-do, Korea, was used for determination of the characteristics of resistance to chlorpyrifos using the activities of esterases and glutathione-S-transferase(GST), protein sequestration and AChE insenstivity. Although the activities of esterases extracted from resistant strain and susceptible strain were not significantly different, isozyme bands shown on the electrophoresis were different. GST activity from field resistant strain was 1.5-fold higher than that of susceptible. No differences were shown between resistant and susceptible ones in protein sequestration. The insensitivities of AChE to chlorpyrifos, however, extracted from susceptible strain was 460-fold higher than those of resistant. These results indicated that the insensitivity of AChE is the major factor for developing the resistance and activities of GST might be a minor factor.

• Korean Journal of Food Science and Technology
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• v.41 no.4
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• pp.435-440
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• 2009

Acetylcholinesterase (AChE) inhibitors, which enhance cholinergic transmission by reducing the enzymatic degradation of acetylcholine, are the only source of the compound that is currently approved for the treatment of Alzheimer's disease (AD). In these experiments, the concentration samples of green tea extracts were 100, 500, and 1,000 ${\mu}g$/mL. Among them, the highest concentration (1,000 ${\mu}g$/mL) of fresh green tea extracts showed the most potent inhibitory effect on AChE by reducing more than 40% of enzyme activity, and in a concentration-dependent pattern. In addition, we examined the effect of other storing conditions on AChE inhibition. In order to maintain storage for 3 months, the materials were held at the certain storing conditions of temperature (room temperature, 4 and $-20^{\circ}C$) and for water activity (0.81, 0.69, and 0.23). In these storing conditions, the difference in temperature did not contribute to the AChE inhibitory effect. Our presented data showed that the AChE inhibitory effect was affected by the concentration of green tea extract and by water activity (0.81). These results suggest that green tea may serve as a potential dietary source of AChE inhibitor.

• CELLMED
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• v.2 no.2
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• pp.19.1-19.6
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• 2012

$Capparis$ $zeylanica$ Linn. a 'Rasayana' drug is used for its memory enhancing effects in the traditional Ayurvedic system of medicine. The aim of this study was to evaluate acetylcholinesterase (AChE) inhibitory and memory enhancing activities of $Capparis$ $zeylanica$ Linn. The$in-vitro$ and $ex-vivo$ models of AChE inhibitory activity were used along with Morris water maze test to study the effect on memory in rats. The anticholinesterase effect of methanolic and aqueous extracts of $Capparis$ $zeylanica$ was measured by spectrophotometric Ellman method at 0.1, 0.3, 1.0, 3.0, 10 and 30 mg/ml and brain monoamine oxidase (MAO-A and MAO-B) activity was assessed by Naoi's method. The results $in-vitro$ and $ex-vivo$ AChE assay revealed that methanolic and aqueous extracts of $Capparis$ $zeylanica$ inhibit AChE activity, whereas these extracts did not alter MAO activity at any concentration tested as compared to moclobemide and L-deprenyl. The results indicate that $Capparis$ $zeylanica$ improves scopolamine-induced memory deficits through inhibition of AChE activity, and not by direct MAO inhibition.

• Journal of Korean Society of Occupational and Environmental Hygiene
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• v.22 no.2
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• pp.91-99
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• 2012

Airborne chlorpyrifos concentrations in formulation workplaces have not been determined in Korea. The aim of the study was to evaluate chlorpyrifos concentrations of air in a formulation workplace and recognize the RBC cholinesterase activities for the formulation workers. 30 air samples (personal or area sampling) were collected and bood samples from 10 workers were collected for RBC chlorinesterase (RBC AChE) activity in a factory on May 2008. Air samples were collected by the National Institute for Occupational Safety and Health (NIOSH) method and were analyzed by GC-MS. Airborne chlorpyrifos concentrations ranged from 0.003 to $12.90mg/m^3$ and geometric mean (GM) was $0.15\;mg/m^3.$ Compared to Korean Occupational Exposure Limit (KOEL) of 0.1 (2011) or $0.2\;mg/m^3$ (2008), at 95% confidence, airborne concentrations exceeded the KOEL 69.7% or 56.1% of the time or less, indicating that this concentration level was unacceptable according to exposure assessment using a LogNorm2$^{(R)}$. Since the workers were continually at work on the organophosphate or carbamate pesticides formulation, individual baseline for RBC AChE activity was not determined. As the results of comparison with reference average value of RBC AChE activity, it was found that a worker was below 70% RBC AChE activity and five workers were abnormal.

• 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.

• Molecular & Cellular Toxicology
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• v.2 no.3
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• pp.216-221
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• 2006

The cholinesterase-inhibiting organophosphorous (OP) compounds known as nerve agents are highly toxic. The principal toxic mechanism of OP compounds is the inhibition of acethylcholine esterase (AChE) by phosphorylation of its catalytic site. The reversible competitive inhibition of AChE may prevent the subsequent OP intoxication. In this study, three-dimensional quantitative structure-activity relationship (3D-QSAR) was performed to investigate the relationship between the 29 compounds with structural diversity and their bioactivities against AChE. In particular, predictive models were constructed using the comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA). The results indicate reasonable model for CoMFA ($q^{2}=0.453,\;r^{2}=0.697$) and CoMSIA ($q^{2}=0.518,\;r^{2}=0.696$). The presence of steric and hydophobic group at naphtyl moiety of the model may lead to the design of improved competitive inhibitors for organophosphorous intoxication.

• Archives of Pharmacal Research
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• v.19 no.6
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• pp.520-528
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• 1996

The involvement of the cyclic AMP (cAMP) effector system in the release of endogenous dopamine and acetylcholine from the rat neostriatum was assessed. Forskolin, an activator of adenylate cyclase, was used to enhance cAMP production, and the consequence of this enhancement on the spontaneous and potassium stimulated release of dopamine and acetylcholine was evaluated. Neostriatal slices were prepared from Fischer 344 rats and after a preincubation period the release of each endogenous neurotransmitter was measured from the same slice preparation. To measure acetylcholine release the slice acetylcholinesterase (AChE) activity was inhibited with physostigmine, but the release from slices with intact AChE activity was also determined (choline, instead of acetylcholine was detected in the medium). Under both conditions forskolin induced a significant dose-dependent increase in the potassium-evoked release of dopamine. In the same tissue preparations the release of neither acetylcholine (AChE inhibited) nor choline (AChE intact) was affected by forskolin. The results indicate that the CAMP second messenger system might be involved in neuronal mechanisms that enhance neostriatal dopamine release, but stimulation of this second messenger by forskolin does not further enhance neostriatal acetylcholine release.

• The Korean Journal of Mycology
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• v.46 no.4
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• pp.447-457
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• 2018

In this paper, the screening of potent acetylcholinesterase (AChE) inhibitor - producing yeasts from wild yeasts and the condition for the production of anti-dementia AChE inhibitors are described. Among one hundred and seven non-pathogenic wild yeast strains from the waters and soils of three main rivers in Daejeon metropolitan city and midstream of Yeongsangang river in Sangju, sporogenous Saccharomyces cerevisiae WJSL0113 and asporogenous Wickerhamomyces anomalus JSF0128 were selected as useful strains for the production of potent AChE inhibitors. The AChE inhibitors of S. cerevisiae WJSL0113 and W. anomalus JSF0128 had a maximum yield when they were incubated in yeast extract-peptone-dextrose media (pH 6.0 in S. cerevisiae WJSL0113 and pH 5.0 in W. anomalus JSF0128) for 18 hr at $30^{\circ}C$, respectively.

• Applied Microscopy
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• v.27 no.2
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• pp.131-144
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• 1997

The present study was carried out to investigate the processes of the ultrastructural differentiation and the acetylcholinesterase (AChE) activities of the developing rat retina. The results are as follows. The retina of fetal rat on the 13th day of gestation showed the early stage of differentiation. Briefly, there appeared dividing chromosomes, the plentiful free ribosomes, and the high ratio of nucleus to cytoplasm. The reaction products by AChE were localized at the membrane of endoplasmic reticulum and on the outer membrane of nucleus. Ultrastructures and AChE activities in the retina of the fetal rats on the 18th day of gestation were similar to those of the prior stages, except the appearence of rough endoplasmic reticulum and Golgi apparatus. According to the ultrastructural observations, the rat retina was still in immature state at birth, but the pigment epithelial cells were fully differentiated, e. g. the increase of melanin granules, the development of mitochondria and Golgi apparatus. The AChE activity was weekly detected. The differentiated retinal layers and the outer segment of photoreceptor cells were observed on the 7th postnatal day. And the pigment epithelium appeared to be fully differentiated. On the 14th postnatal day, rat retina were completely differentiated. In other words, the rat retina was characterized by the prominent outer segments, phagocytosed residues in the pigment epithelium, and the localization of reaction products by AChE in the synapses. In conclusion, the differentiation of rat retina is charaterized by the changes of cell shape, the increase of retinal layers, and the alterations of AChE activities. It seems that rat retina is to be functional from 2 weeks of birth onward, coinciding with the eye opening of the juvenile rats.