• Environmental Analysis Health and Toxicology
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• 제18권1호
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• pp.21-25
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• 2003

카바메이트계 농약인 카보푸란은 어류에 대한 독성이 매우 높으며, 낮은 농도에서 어류의 척추기형이나 행동이상을 유발한다. 이러한 카보푸란의 독성기전을 밝히기 위한 일환으로 신경물질대사와 관련이 깊은 acetylcholine esterase(AChE)와 monoamine oxidase(MAO)에 미치는 농약의 효과를 송사리(Oryzias latipes; Medaka fish)를 이용하여 평가하였다. Medaka fish에 대한 카보푸란의 반수치사농도(LC$_{50}$)는 2.5 ppm이었으며, 1 ppb 카보푸란에 24시간 노출된 경우, AChE 효소활성이 머리와 몸통부위에서 각각 30, 20%씩 감소되었다. 한편, MAO 효소활성은 카보푸란의 농도가 증가함에 따라 머리부위에서는 감소한 반면, 몸통부위에서는 증가하는 경향을 보였다. 특히 카보푸란의 농도가 1 ppb에서도 송사리의 MAO 효소활성이 영향을 받는 것으로 나타나, 카보푸란에 의한 송사리의 행동이상은 AChE 활성 뿐 아니라 MAO활성의 변화에 의한 복합적인 효과일 가능성이 높다.

• 농업생명과학연구
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• 제45권6호
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• pp.213-226
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• 2011

아세틸콜린 분해효소(acetylcholine esterase, AChE) 억제제는 아세틸콜린 함량을 높여 콜린성 neuron을 활성화함으로써 기억 능력의 개선 및 치매 개선을 가져와 현재 다양한 AChE 억제제들이 개발되어 사용되고 있다. 본 연구에서는 AChE에 대한 억제 활성을 갖는 천연물을 다양한 식물추출물 및 에센스오일로부터 탐색하였으며, 탐색한 추출물의 scopolamine으로 기억손상을 유발한 쥐의 기억력 개선 활성을 치매 치료제로 사용하고 있는 donepizil과 비교 분석하였다. 그 결과 자몽(Citrus paradisi) 유래의 에센스 오일이 AChE 억제 활성이 가장 높아 20 ug/ml의 농도로 처리하였을 때 90% 이상의 효소 억제 활성을 나타내었다. 수동회피 실험 결과, 자몽 유래의 에센스오일(100 mg/kg, p.o.)을 투여한 쥐는 치매 치료제로 사용하고 있는 donepizile (0.5 mg/kg)을 투여한 쥐와 유사한 latency time을 나타내어 인지기능이 개선되었다. 또한, 수중미로 시험 결과, 자몽 유래 에센스오일(100 mg/Kg, p.o.)을 투여한 쥐는 donepizile(0.5 mg/kg)을 투여한 쥐와 유사한 latency time을 나타내어 인지기능이 개선되었다. 이상의 결과로부터 자몽 유래 에센스오일은 매우 효과적으로 기억력을 개선하여 인지기능을 개선해 줄 수 있는 안전하고 효과적인 후보물질이라고 사료된다.

• 동의생리병리학회지
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• 제25권3호
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• pp.406-416
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• 2011

In this study, we have verified the memory and cognitive enhancing effect of Longanae Arillus, the fruit of Euphoria longana Lamarck, which has been used as a tonic and for the treatment of amnesia, insomnia, and palpitations in oriental medicine. To investigate the effect of Longanae Arillus water extract(LAE) on the memory and cognitive dysfunction, scopolamine (1 mg/kg, i.p.) was injected in C57BL/6 mice and several behavior tests including Y-maze, Morris water-maze, passive avoidance and fear conditioning tests were conducted. Administration of LAE (100 or 200 mg/kg/day, p.o.) effectively improved scopolamine-induced memory impairment and dysfunction. To further determine the possible molecule mechanism of LAE, we have examined the activity and/or mRNA expression of diverse proteins involved in the acetylcholine metabolism. LAE particularly increased the amount of acetylcholine in the cortex which was mediated by suppression of acetylcholine esterase (AchE) activity. In addition, LAE elevated the mRNA expression of muscarinic acetylcholine receptors (mAchRs) without affecting the mRNA levels of choline acetyltransferase (ChAT) and acetylcholine esterase (AchE). In another experiment, LAE effectively inhibited mRNA expression of pro-inflammatory cytokines such as tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) and interleukin-$1{\beta}$ (IL1-${\beta}$), which seemed to be mediated by inhibition of upstream transcription factor NF-${\kappa}B$ and extracellular-regulated kinase 1/2 (ERK1/2). These results demonstrate that Longanae Arillus can increase acetylcholine amount the cortex via regulation of AchE activity as well as mAchRs expression and decrease pro-inflammatory responses via inhibition of NF-${\kappa}B$ signaling pathway, thereby having therapeutic potential to improve memory and cognitive deficit in amnesia.

• Bulletin of the Korean Chemical Society
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• 제31권1호
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• pp.157-161
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• 2010

A sensory element against carbaryl, as a widely used pesticide was prepared based on adsorbed acetylcholine esterase (AChE) from Torpedo california. Octadecyl was substituted on macro-porous silica, confirmed by infra-red (IR) spectroscopy and quantitatively estimated through thermo-gravimetric analysis (TGA). Immobilization of the enzyme was achieved by adsorption on this support. Activity of the immobilization product was measured as a function of the loaded enzyme concentration, and maximum binding capacity of the support was estimated to be 43.18 nmol.mg-1. The immobilized preparations were stable for more than two months at storage conditions and showed consistency in continuous operations. Possible application of the immobilized AChE for quantitative analysis of carbaryl is proposed in this study.

• Journal of Acupuncture Research
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• 제23권3호
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• pp.117-127
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• 2006

Alzheimer's disease (AD) is the most prevalent form of neurodegenerative disease associated with aging in the human population. This disease is characterized by the following 4 structural changes : Atrophy of the Cortex, Parasympathetic, and other neural cells, the existence of Neurofibrillary tangles (NFTs), and the accumulation of Senile plaques. NFTs and Senile plaques is known to be the index of this disease. Senile plaques disturbs the neutro transmission and depletes of Acetylcholine. So, Recovery of Acetylcholine is the primal objective for treating Alzheimer's disease. So, Inhibiting the activity of Acetylcholine Esterase (AChE), which causes the hydrolysus of acetylcholine into choline and acetate, can be seen as a key role for treating Alzheimer's disease. Increasing body of evidence has been demonstrated that Bee Venom Acupuncture (BV) could compete with complex protein involving in multiple step of $NF-_{\kappa}B$ activation and exert the anti-inflammatory potential of combined inhibition of the prostanoid and nitric oxide synthesis systems by inhibition of IKK and $NF-_{\kappa}B$. BV dose-dependently attenuated Scopolamine-induced Acetylcholine esterase activities in cerebral cortex and hippocampus of the mice brain. This study therefore suggests that BV acupuncture method may be useful for prevention of development or progression of AD.

• Applied Biological Chemistry
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• 제42권4호
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• pp.336-343
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• 1999

담자균류로부터 치매 예방 및 치료 효과를 갖는 생물활성물질을 탐색하기 위한 기초 자료를 확립하기 위하여 56종의 배양 균사체 메탄을 추출물 및 배양 여액의 ethylacetate(EtOAc) 가용성 분획에 대하여 prolylendopeptidase(PEP), acetylcholine esterase(AChE) 및 혈전 응고에 대한 저해활성을 측정하였다. 그 결과 PEP에 대하여 Amanita aspera, Phellinus chrysoloma의 균사체 추출물 및 배양여액의 EtOAc 가용성 분획이 40ppm에서 모두 90% 이상의 저해활성을 나타내었으며 분홍껍질고약버섯(Peniophora quercina), 잎새버섯(Grifola frondosa), Wolfiporia extensa, 좀나무싸리버섯(Clavicorona pyxidata) 및 Phanerochaete soy교교의 배양액이 90% 이상의 저해활성을 나타내었다. AChE에 대하여는 40ppm 농도에서 어느 것도 강한 활성을 나타내지 못하였으나 조개껍질버섯(Lenzites betulina), Phellinus chrysoloma, Wolfiporia extensa, Phanerochaete sordida의 균사체 추출물과 Hypocrea nigricans, Coriolus azureus, 팽나무버섯(Flammuzina velutipes), Phlebiopsis gigantea 및 Bondarzewia montana의 배양여액 EtOAc 가용성 분획이 40% 정도의 저해활성을 나타내었다. 한편 혈전응고 저해활성의 지표로 삼은 thrombin times(TT) assay에서는 Amanita aspera, Oxyporus latemarginata, 분홍껍질고약버섯(Peniophora quercina), 말굽버섯(Fomes fomefarius)의 배양여액 EtOAc 추출물과 Clitocybe clavipes, Trametes versicolor, Phlebiopsis gigantea의 균사체 추출물이 550 ppn의 농도에서 혈전 생성에 걸리는 시간을 2배 내지 3배 연장하는 효과를 나타내었으나 activated partial thromplastin times(APTT) assay에서는 어느 것도 효과를 인정할 수 없었다.

• 생명과학회지
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• 제12권1호
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• pp.26-31
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• 2002

촉매화된 acetylcholine esterase가수분해의 기질로 사용될 choline ester를 두 가지 방법으로 합성하였다. 먼저, ethylene sulfide를 출발물질로 하여 2-chloroethyl thiohex-anoate, 2-chloroethyl thioheptanoate, 2-chloroethyl thiooc-tanoate를 각각 합성하였고 여기에 trimethyl amine을 첨가하여 hexanonyl thiocholine, octanonyl thiocholine을 합성하였다. 두 번째 방법으로 ethylene sulfide에 dimethyl amine을 첨가시켜 acid anhydride로 acylation 시킨 후 methyl iodide를 첨가하여 heptanoyl thiocholine, decanoyl thiocholine을 합성하였다. 합성된 hexanonyl thiocholine을 기질로 하여 butyrylcholine esterase와의 반응을 연구 하고자 한다. 또한 본 연구에서는 한국 과학 기술원 도핑컨트롤 센터와 연계하여 acetylcholine esterase와 기질인 acyl-thiocholine과의 입체적으로 둘러싸인 acyl-binding site를 분자 조형하고자 노력 중에 있다.

• Current Research on Agriculture and Life Sciences
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• 제32권2호
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• pp.63-66
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• 2014

The effects of a newly developed flower thinning formulation (FTF) on the vitality of the honey bee Apis mellifera were examined by measuring the activities of various digestive enzymes in adult worker bees. First, direct spraying of the FTF solution did not cause any behavioral changes or lethal effects for the honey bees based on 24 h observation. Second, oral ingestion of a sugar solution containing the FTF did not produce any significant change in the activities of amylase, proteinases, lipase, or acetylcholine esterase (AChE) in the worker bees 6 h or 24 h after treatment. Meanwhile, a commercial formulation containing sulfur compounds showed slightly reduced activities for several digestive enzymes and AChE, although no behavioral disturbance. Thus, the results of the present study suggest that the FTF is not toxic for honey bees, in terms of contact and ingestion. Therefore, this newly developed FTF can be used for flower thinning without any detrimental effects on pollinating insects.

• 동의생리병리학회지
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• 제17권2호
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• pp.553-559
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• 2003

In order to make the efficient prescription and cope with various senile dementia, learning and memory functions of Sprague-Dawley model rats were tested with Morris water maze at first. And to evaluate the effects of the sample drug(GM) on choline acetyltranferase and acetylcholine esterase, immunoreactive measurement and enzymatic activity measuring were carried out. Rats were injected with ibotenic acid through hippocampus CA1 and CA3 area. The results are as following. GM improves the learning ability in tile acquisition test and memory function in the retention test significantly. And GM increases the level of ChAT which is synthesizing acetylcholine in CA3 area, and at the same time it increases the level of AChE which is resolving acetylcholine. These results show that GM improve the cholinergic catabolism and anabolism, and the increment of metabolic activity of cholinergic system contributes to the recovery of damaged learning and memory function by ibotenic acid. So it can be concluded that GM will be helpful to cholinergic brain disease induced by primary or senile reduction of acetylcholine secretive activity.

• 동의생리병리학회지
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• 제16권6호
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• pp.1236-1242
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• 2002

In order to make an efficient prescription and cope with dementia, learning and memory functions of Sprague-Dawley model rats were tested with Morris water maze. And to evaluate the effect of the sample drug(CHM) on choline acetyltranferase and acetylcholine esterase, immunoreactive measurement and enzymatic activity measuring were carried out. Rats were injected with ibotenic acid through hippocampus CA1 and CA3 area. The results are as following. CHM improves the learning ability in the acquisition test and memory function in the retention test significantly. And CHM increases the level of AChE which is resolving acetylcholine. Though it doesn't increase the level of ChAT significantly which is synthesizing acetylcholine, but it shows the tendency of increase. So these results show that CHM improve the cholinergic catabolism and anabolism, and the increment of metabolic activity of cholinergic system. Thus it can be concluded that CHM will be helpful to cholinergic brain disease induced by primary or senile reduction of acetylcholine secretive activity.