• 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.

• Bulletin of the Korean Chemical Society
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• 제33권8호
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• pp.2741-2747
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• 2012

A new series of 2,5-disubstituted-1,3,4-thiadiazoles 6a-i was synthesized by overnight stirring various 1,4-disubstituted thiosemicarbazides 5a-i in polyphosphoric acid followed by neutralization. The structures of newly synthesized compounds 5a-i and 6a-i were characterized by IR, $^1H$ and $^{13}C$ NMR, elemental analysis and mass spectrometric studies. All the synthesized compounds were evaluated for their urease and acetylcholine esterase inhibition activities. Thiosemicarbazides 5a-i are found to possess excellent potential for urease inhibition, more than the standard drug. Thiosemicarbazides 5a-i are more potent urease inhibitor than their cyclic analogues thiadiazoles 6a-i. Almost all of the compounds are excellent inhibitors of acetylcholine esterase. The inhibition of acetylcholine esterase of compounds 5a, 5c, 5d, 5g, 5i, 6e, 6f, 6g, and 6i is much more than that of standard drug.

• 한국식품영양학회지
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• 제17권4호
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• pp.347-355
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• 2004

초석잠 메탄올 추출물이 뇌신경전달물질과 관련이 있는 acetylcholine esterase, monoamine oxidase 및 xanthine oxidase의 활성억제효과에 대하여 실험하였다. 실험관내에서 초석잠 추출물을 각각 100 및 200mg/kg씩 첨가한 다음 실험한 결과 첨가농도가 증가할수록 과산화지질의 생성을 억제하여 용량 의존형으로 나타났다. 쥐를 대상으로 20일간 투여한 동물실험에서는 초석잠 추출물 100 mg/kg을 식이에 혼합하여 투여한 결과 지질 과산화의 생성을 억제하였다. Acetylcholine esterase의 활성의 경우 초석잠 추출물을 100 mg/kg 투여한 결과 대조군에 비하여 효소활성이 23.11%로 억제되었고, monoamine oxidase 및 xanthine oxidase 활성이 각각 21.93% 및 63.58%로 억제되었다. 그리고 초석잠 추출물을 100 mg/kg을 투여한 경우 xanthine dehydrogenase로부터 xanthine oxidase로의 형전환비율은 28%로 현저하게 억제되었다. 또한, Xanthine dehydrogenase로부터 oxidase로의 형전환비율을 실험한 결과 정상상태에 비하여 억제됨을 알 수 있었다.

• 동의신경정신과학회지
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• 제14권1호
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• pp.75-84
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• 2003

Object : The present experiments were designed to study on the memory enhancement of the extract of Gongjadaesungjichimjung-bang(GDJB). Methods : The water extract of GCJB has been tested for its activities on memory enhancement by passive avoidance task in vivo and for its inhibitory effect on the acetylcholine esterase activity. Results : GDJB water extract significantly enhanced the memory at a concentration of 50mg/kg, but this effect did not proportionally increased at a dose of l00mg/kg and significantly inhibited the acetylcholine esterase activity in a dose-dependent manner in in vitro assay with IC50 value of 1.57mg/ml and also in in vivo assay. Conclusion : The extract of GDJB showed a memory enhancement as well as the inhibitory effect on acetylcholine esterase activity, which suggest that this prescription may be applied for the treatment of memory impairment.

• 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.

• Environmental Analysis Health and Toxicology
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• 제14권3호
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• pp.81-85
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• 1999

Diazinon, an organophosphate pesticide, is relatively highly toxic to fish and causes vertebral malformation and behavioral change of fish at relatively low concentrations. To elucidate biochemical mechanism of the behavioral change of Oryzias latipes (killifish) caused by diazinon, the effect of the insecticide on acetylcholine esterase activities and the levels of some neurotransmitters were evaluated. Acetylcholine esterase activities in both head and body were significantly lowered at the concentration of 10 ppb of diazinon and acetylcholine contents in head tended to be upregulated with increasing concentration of diazinon. Exposure of killifish to 5000 ppb diazinon resulted in gradual decrease in acetylcholine content in body part with exposure time. Norepinephrine and serotonin concentrations in killifish head and body were highest at 1000 ppb of diazinon while neurotransmitter were relatively low in fish unexposed or exposed to lower dose of the pesticide, suggesting that increased norepinephrine and serotonin can partially account for diazinon-induced behavioral abnormality.

• 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.

• 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.

• 대한한방내과학회지
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• 제22권3호
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• pp.321-330
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• 2001

Objectives: This study was undertaken to investigate the action mechanism of Holotrichia (HT) at parameter related to dementia. Methods: HT was tested for the effects on acetylchonine esterase and monoamine oxidase activities, lipid peroxidation, antioxidation in brain of lead acetate-treated rats. Lead acetate were treated firstly into samples for 10 days, and then lead acetate and HT were set with them for 20 days. Results: The level of lipid peroxide, acetylcholine esterase and monoamine oxidase activities, enzyme activities and ratio of type conversion of xanthine oxidase increased in lead acetate-treated rats were decreased as highly as normal group by HT. Superoxide dismutase, catalase and glutathione peroxidase activities, the level of acetylcholine decreased in lead acetate-treated rats were increased as lowly as normal group by HT. Conclusions : These results suggest that HT might have an effect on treatment of dementia according to decreasing the activities of acetylcholine esterase, monoamine oxidase and level of lipid peroxide in brain.

• 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.