• 농약과학회지
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• 제8권1호
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• pp.16-21
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• 2004

본 연구는 6종 나방류(멸강나방, 배추좀나방, 목화바둑명나방, 파밤나방, 담배나방, 담배거세미나방) 대한 유충영기별 thiodicarb의 살충활성을 조사하였으며, 살충효과 구명을 위하여 효소활성(esterase, acetylcholinesterase, glutathione S-transferase)등을 검토하였다. 이 약제는 6종의 나방류 어린유충에 대해서 높은 살충효과를 나타내었으나, 노숙유충에 대한 살충효과는 상대적으로 낮았고, 발현속도는 느렸다. 담배거세미나방을 대상으로 한 효소활성저해 실험에서 acetylcholinesterase와 glutathione S-transferase 활성을 저해하였으나, esterase 활성을 저해하지는 않았다.

• 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.

• 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).

• Journal of Nutrition and Health
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• 제39권3호
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• pp.219-224
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• 2006

This study was performed to determine the effect of soy isoflavones on brain development and function in rats. Forty Sprague-Dawley male rats were provided diets containing different levels of soy isoflavones for 6 weeks; 0 ppm (control), 50 ppm (low isoflavone intake; LI), 250 ppm (medium isoflavone intake; MI) and 500 ppm (high isoflavone intake; HI). Learning ability was evaluated by a Y-shaped water maze and the activity of acetylcholinesterase in brain was assayed after decapitation. Food intake and body weights as well as weights of brain, liver, spleen, heart and kidney showed no significant difference among the four groups, which means 500 ppm of isoflavones is safe. In the water maze test, the frequency of error counted when rats entered one end of the alley without platform was significantly lower in the HI group than in the control group, and the escape latency as swim time taken to escape on the hidden platform was significantly shorter in the HI group than in the LI and control groups. The activity of acetylcholinesterase of the brain was significantly higher in the HI and MI groups than in the control group. Therefore, the results indicate that isoflavones may improve the cognitive function without adverse effects.

• 생약학회지
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• 제47권3호
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• pp.287-294
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• 2016

Acetylcholinesterase (AChE) activation and amyloid-${\beta}$ ($A{\beta}$) aggregation are major biological markers of Alzheimer's disease. In the present study, we evaluated the inhibitory effects of 50 kinds of herbal formulas on AChE activity and $A{\beta}$ aggregation. Among them, Hwanglyeonhaedok-tang, Cheonwangbosim-dan, Makmundong-tang, and Gamisoyo-san had a potent effects on the inhbition of AChE activity. Sosiho-tang, Samsoeum, Cheonsimyeunjaeum, and Bunsimgieum exerted to have the inhibitory activity on $A{\beta}$ aggregation. In addition, these 8 herbal formulas showed the 3-ethyl-benzothiazoline-6-sulfonic acid (ABTS) radical scavenging activity, indicating their antioxidant activities.

• 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.

• 생약학회지
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• 제27권2호
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• pp.91-95
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• 1996

In the course of searching for acetylcholinesterase inhibitors from crude drugs, it was found that total MeOH extract of Corydalis Tuber showed significant inhibitory effect on acetylcholinesterase. To isolate acetylcholinesterase inhibitors from Corydalis Tuber, total MeOH extract of the the crude drug was subjected to activity guided fractionation. The MeOH extract was suspended in water and fractionated with methylene chloride and subjected to acid-base fractionation. Silica gel column chromatography of the basic fraction which showed significant inhibitory effect on acetylcholinesterase was carried out and 5 subfractions (1-5) were obtained. From subtraction 4, compound I was isolated. The structure of isolated compound I was identified by spectroscopic parameters of $^1H-NMR$, $^{13}C-NMR$, EI-MS and FAB-MS. The compound I was identified as berberine. It was found from the Lineweaver-Burk plot that berberine was a reversible and specific inhibitor of acetylcholinesterase having 90% inhibitory effect at the concentration of $2.5{\mu}M$.

• Journal of Microbiology
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• 제44권5호
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• pp.502-507
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• 2006

In a previous study, an extract of Clavicorona pyxidata DGUM 29005 mycelia demonstrated an inhibitory effect against enzyme-associated perceptual disorders. We have attempted to determine whether this mycelial extract is also capable of inhibiting the activities of acetylcholinesterase (AChE) and ${\beta}$-secretase (BACE) activity. Butanol, ethanol, and water extracts of C. pyxidata DGUM 29005 mycelia were shown to inhibit AChE activity by 99.3%, 93.7%, and 91.7%, respectively. The inhibitory value of the butanol extract was more profound than that of tacrine (95.4%). The ethanol extract also exerted an inhibitory effect against BACE activity; this fraction may harbor the potential for development into a pharmocotherapeutic modality for the treatment of Alzheimer's disease (AD) patients. Rat pheochromocytoma PC12 cells in culture were not determined to be susceptible to the cytotoxic activity evidenced by the mycelial extract. The ethanol extract inhibited endogenous AChE activity in PC12 cellular homogenates, with an $IC_{50}\;of\;67.5{\mu}g/ml$, after incubation with intact cells, and also inhibited BACE activity in a dose-dependent fashion. These results suggest that the C. pyxidata mycelial extract has the potential to enhance cholinergic function and, therefore, may perform a function in the amelioration of the cholinergic deficit observed in cases of AD, as well as other types of age-associated memory impairment.

• Journal of Nutrition and Health
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• 제29권1호
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• pp.32-40
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• 1996

To investigate the effect of dietary docosahexaenoic acid(DHA) and environmental enrichment on brain fatty acid composition and acetylcholinesterase(AChE) activity, two groups of was fed isocaloric diets containing 10 or 12% dietary lipids for 7 weeks. A third group was fed 10% (w/w) dietary lipids with supplemented 2% DHA-rich fish oil. Each diet group was housed either in a stainless steel cage individually or in a large enriched cage with toys where 7 rats were kept together. The fatty acid composition of plasma and brain was significantly affected by dietary lipid composition but not by environmental enrichment. Fish oil supplementation significanlty decreased plasma levels of monounsaturated fatty acids(MUFA) and increased polyunsaturated fatty acids(PUFA). Fish oil supplemented groups also maintained lower plasma n-6 fatty acids and higher n-3 fatty acids levels than unsupplemented groups. The fish oil supplementation significantly decreased arachidonic acid and increased eicosapentaenic, docosapentaenoic acids, and DHA in brain fatty acid composition. In addition, brain DHA level in supplemented groups tended higher than the unsupplemented. Brain, AChE activity significantly increased by the environmental enrichment but not by the fish oil supplementation. These finding suggest that the 2% fish oil (0.57% DHA & 0.31% EPA, per diet weigth) supplementation is enough to accumulate n-3 fatty acids and to change the n-6 n-3 ratio in brain and environmental enrichment might promote the learning ability.

• 생약학회지
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• 제48권3호
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• pp.243-247
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• 2017

To find the anti-Alzheimer's activity of Cacalia hastata var. orientalis (Compositae), caffeoylquinic acids were analyzed in this plant by HPLC and the inhibitory activities of the extract on cholinesterases including acetylcholinesterase (AChE) and butyrylcholinesterse (BChE) and peroxynitrite ($ONOO^-$) were assayed. Sum of caffeoylquinic acids in the 80% MeOH extract was quantitatively higher in leaves (35.8% of the extract) than in stems (3.7%). The compound, 3,5-dicaffeoylquinic acid, was contained in the highest amount in the leaf (44.32 mg/g dry weight). The $IC_{50}s$ of the 80% MeOH extract were shown to be $67.45{\mu}g/ml$ for AChE, and $8.59{\mu}g/ml$ (for $ONOO^-$), respectively, suggesting that the leaves would have the anti-Alzheimer's activity due to the high content of caffeoylquinic acids.