• Title/Summary/Keyword: Acetylcholinesterase activity

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Insecticidal activity of thiodicarb on lepidopterous pests (나방류에 대한 thiodicarb의 살충활성)

  • Choi, Yu-Mi;Kim, Gil-Hah
    • The Korean Journal of Pesticide Science
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    • v.8 no.1
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    • pp.16-21
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    • 2004
  • A series of experiments was conducted to determine the toxicities of thiodicarb on the six lepidopterous pests (Pseudaletia separata, Plutella xylostella, Palpita indica, Spodoptera exigua, Helicoverpa assulta, Spodoptera litura) and to elucidate factors insecticidal effects mechanism of thiodicarb. Thiodicarb was very effective against six lepidopterous young larvae, but less effective to the old larvae and it acted slowly. Thiodicarb inhibited acetylcholinesterase and glutathione S-transferase activities, but not inhibit esterase activity.

The Effects of Ethanol on Cholinesterase Inactivation by Organophosphorous (에탄올이 유기인제 농약에 의한 Cholinesterase 불활성화에 미치는 영향)

  • Choi, Hyoung-Chul;Kim, Jong-Ho;Ha, Jeoung-Hee;Lee, Kwang-Yoon;Kim, Won-Joon;Woo, Hyun-Jae;Huh, Chang-Uk;Son, Soo-Min;Chun, Eun-Jin
    • Journal of Yeungnam Medical Science
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    • v.16 no.2
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    • pp.326-332
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    • 1999
  • Background: In korea the agricultural community widely uses organophosphorous, and organophosphorous poisonings are increasing every year. We compared change in activity of acetylcholinesterase and pseudocholinesterase by organophosphorous and by the interaction of ethanol and organophosphorous. We also compared the effect of reversible anticholinesterase drugs, physostigmine and neostigmine The object of this study is to investigate the effects of several anticholinesterase drugs and on how ethanol influences the activity of cholinesterase. Materials and Methods: Fifteen male university students were randomly selected, and blood samples were taken from the antecubital vein. The acetylcholinesterase in the RBC and the pseudocholinesterase in the serum were extracted and separated. The enzyme activity change was measured by the electrometric method. After adding acetylcholine, the pH change was measured with a pH meter. Results and Conclusion: Our results indicated that reversible anticholinesterase drugs decreased the cholinesterase activity more efficiently than organophosphorous. The acetyl cholinesterase and pseudocholinosterase activity were decreased by ethanol. When ethanol was added, oxime a cholinesterase activator, increased acetylcholinesterase activity but does not increased pseudocholinesterase activity.

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Inhibitory Effect of Trans-N-p-Coumaroyl Tryamine from the Twigs of Celtis chinensis on the Acetylcholinesterase

  • Kim, Dae-Keun;Lee, Kie-Seung
    • Archives of Pharmacal Research
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    • v.26 no.9
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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).

Effect of Soy Isoflavone Intake on Water Maze Performance and Brain Acetylcholinesterase Activity in Rats (대두 이소플라본 섭취가 흰쥐에서 미로수행능력과 뇌 중 Acetylcholinesterase 활성에 미치는 영향)

  • Oh Hyun-Kyung;Kim Sun-Hee
    • Journal of Nutrition and Health
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    • v.39 no.3
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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.

Screening of 50 Korean Herbal formulas with Inhibitory Effects on Acetylcholinesterase Activity and Amyloid-β Aggregation (다빈도 한약 처방 50종의 아세틸콜린 분해 효소 활성 및 아밀로이드 베타 단백질 응집 억제 효능 비교 연구)

  • Lim, Hye-Sun;Kim, Yoonju;Kim, Ohn Soon;Jeong, Soo-Jin
    • Korean Journal of Pharmacognosy
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    • v.47 no.3
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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.

Screening of Potent Anti-dementia Acetylcholinesterase Inhibitor-containing Edible Mushroom Pholiota adiposa and the Optimal Extraction Conditions for the Acetylcholinesterase Inhibitor

  • Kim, Do-Yeon;Bae, Sang-Min;Han, Sang-Min;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.44 no.4
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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.

An Acetylcholinesterase Inhibitor Isolated from Corydalis Tuber and Its Mode of Action (현호색의 Acetylcholinesterase 활성 저해 성분 및 그 작용기전)

  • Hwang, Se-Young;Chang, Young-Pyo;Byun, Soon-Jung;Jeon, Mee-Hee;Kim, Young-Choong
    • Korean Journal of Pharmacognosy
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    • v.27 no.2
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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 $2.5{\mu}M$.

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Effect of Mycelial Extract of Clavicorona pyxidata on Acetylcholinesterase and ${\beta}$-Secretase Activity in vitro

  • Lee, Tae-Hee;Park, Young-Il;Han, Yeong-Hwan
    • Journal of Microbiology
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    • v.44 no.5
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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.

Effect of DHA and Environmental Enrichment on Brain Fatty Acid Composition and Acetylcholinesterase Activity (식이 DHA와 환경보충이 흰쥐의 뇌지방조성 및 Acetylcholinesterase활성에 미치는 영향)

  • 김문정
    • Journal of Nutrition and Health
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    • v.29 no.1
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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.

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Quantification of Caffeoylquinic Acids and the Effect of the Cacalia hastata var. orientalis Extract on Acetylcholinesterase Activity and Peroxynitrite Concentration (민박쥐나물 추출물의 Caffeoylquinic Acid 정량 및 Acetylcholinesterase 활성과 Peroxynitrite 농도에 대한 효과)

  • Nugroho, Agung;Choi, Jae Sue;Park, Hee-Juhn
    • Korean Journal of Pharmacognosy
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    • v.48 no.3
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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.