• Title/Summary/Keyword: Acetylcholinesterase inhibitory activity

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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.

Inhibitory Activitv of (1,3-Dioxolan-2-yl and Dioxan-2-yl)methylaminium Derivatives against Acetylcholinesterase (Acetylcholinesterase에 대한 (1,3-Dioxolan-2-yl 및 Dioxan-2-yl)methylaminium유도체의 저해 작용)

  • Phi, Taek-San;Kim, Yun-Bae;Kim, Jee-Cheon;Cho, Young;Sok, Dai-Eun;Cha, Seung-Hee;Seo, Won-Jun
    • YAKHAK HOEJI
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    • v.38 no.5
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    • pp.511-515
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    • 1994
  • We examined the inhibitory activity of (1,3-dioxolan-2-yl and 1,3-dioxan-2-yl)methylaminium derivatives(A; 1-8) against acetylcholinesterase. Derivatives of six-membered 1,3-dioxane exhibited more potent inhibitory effect than corresponding 5-membered 1,3-dioxolanes. The presence of methyl group at C4 position of dioxane ring was effective to increase the inhibitory potency of heterocyclic analogues. The activity of N-phenacyl-aminiums was greater than that of N,N,N-trimethyl-aminiums. In general, the terminal methyl group on 1,3-dioxane ring and the phenacyl group in ammonium compound A were assumed to be important factors to enhance the inhibitory action.

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Physiological activities of water extract and solvent fractions of Grifola frondosa (잎새버섯 물추출물 및 유기용매 분획물의 생리활성)

  • Kim, Eun-Jung;Kim, Jun-Ho
    • Journal of Mushroom
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    • v.13 no.3
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    • pp.192-198
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    • 2015
  • This study was performed in order to analyze the fibrinolytic, thrombin inhibitory, anti-oxidative, acetylcholinesterase inhibitory, and immuno-enhancing activities of the water extract and solvent fractions isolated from Grifola frondosa. Fibrinolytic activity was analyzed using the fibrin plate method, and thrombin inhibitory activity was assayed using the substrate H-D-Phe-piparg- pna. Anti-oxidative activity was estimated using the DPPH assay, and AChE inhibitory activity was measured using the spectrophotometric method. Immuno-enhancing activity was examined using the nitric oxide (NO) production in RAW 264.7 macrophage cells. Cell viability was determined using the MTS assay. Fibrinolytic activities were the highest in water extract (1.55 plasmin units/mL) followed by water fraction (0.85 plasmin units/mL). The thrombin inhibitory activities of the water and ethyl acetate fractions were determined to be 76.43% and 72.59%, respectively. The acetylcholinesterase inhibitory activities of chloroform and hexane fractions exhibited values of 95.14% and 94.74%, respectively. The butanol fraction showed the highest anti-oxidative activity at 94.47%. Anti-proliferating activity against Raw 264.7 cells showed no cytotoxicity. The production of NO in Raw 264.7 cells increased up to 2-fold by adding the water fraction compared to the untreated control. These results suggest that Grifola frondosa may serve as a useful functional food for the enhancement of immune function and the prevention and therapy of cardiovascular diseases.

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.

Flavonoid Glycosides as Acetylcholinesterase Inhibitors from the Whole Plants of Persicaria thunbergii

  • Kim, Se Young;Park, Jun Young;Park, Pil Sung;Bang, Sang Ho;Lee, Kyung Min;Lee, Yu Ra;Jang, Yong Hyun;Kim, Myong Jo;Chun, Wanjoo;Heo, Moon Young;Kwon, Yongsoo
    • Natural Product Sciences
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    • v.20 no.3
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    • pp.191-195
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    • 2014
  • The n-BuOH soluble fraction of the whole plant of Persicaria thungergii showed acetylcholinesterase inhibitory activity. Four flavonoid glycosides and a flavonoid were isolated from this fraction, and identified as quercitrin (1), luteolin-4'-O-${\beta}$-D-glucopyranoside (2), quercetin (3), quercetin-3-O-glucuronide (4), and isorahmnetin-3-O-glucuronid (5), by chromatographed and spectral data, respectively. All isolated compounds were showed acetylcholinesterase inhibitory activity, with $IC_{50}$ values of 243.1, 10.5, 39.1, 8.2 and $23.2{\mu}M$, respectively.

Antioxidant, anti-acetylcholinesterase and xanthine oxidase inhibitory activities of three extracts from Phellinus igniarius

  • Jin, Ga-Heon;Lee, Min Woong;Im, Kyung Hoan;Lee, Tae Soo
    • Journal of Mushroom
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    • v.12 no.1
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    • pp.1-7
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    • 2014
  • This study was initiated to investigate antioxidant, anti-acetylcholinesterase, and xanthine oxidase inhibitory activities and properties of fruiting bodies, mycelia, and fermentation culture filtrates from Phellinus igniarius. The contents of total phenols and flavonoid of fruit bodies, mycelia, and culture filtrate were 15.35-1.36 mg/g, 10.35-7.85 mg/g, and 8.25-5.36 mg/g. The 1,1-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging abilities of the extracts from the fruiting bodies, mycelia, and culture filtrates were 90.25-95.60%, 78.82-85.24%, and 76.32-82.50% at $50-400{\mu}g/mL$, respectively. The chelating ability of fruiting body extract on ferrous ions was higher than those of mycelia and culture filtrates tested. The anti-acetylcholinesterase inhibitory activity of the fruiting body extract at 400 ${mu}g/mg$ exhibited 91.10% on AChE, which is lower than that of positive control, galanthamine (94.82%). The xanthine oxidase inhibitory activities of the fruiting bodies, mycelia, and culture extract were 85.47%, 78.13%, and 72.49% at 400 ${\mu}g/mL$, respectively. Overall, the fruiting body extract has better anti-acetylcholinesterase, antioxidant and xanthine oxidase inhibitory activities than those from mycelia and culture filtrate.

Acetylcholinesterase Inhibitors from Angelica polymorpha Stem

  • Kwon, Yongsoo;Kim, Hyun Pyo;Kim, Myong Jo;Chun, Wanjoo
    • Natural Product Sciences
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    • v.23 no.2
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    • pp.97-102
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    • 2017
  • Fourteen compounds were isolated from the stem of Angelica polymorpha. On the basis of spectral data, these compounds were identified as isoimperatorin (1), phellopterin (2), bergapten (3), xanthyletin (4), cnidilin (5), geijerine (6), (-)-3'-acetyl hamaudol (7), 7-demethylsuberosine (8), dehydrogeijerin (9), (-)-hamaudol (10), (+)-visamminol (11), divaricatol (12), scopoletin (13), and decursidate (14), respectively. Among them, compounds 4-6, 8, 9, 13, and 14 were isolated for the first time from A. polymorpha. Dehydrogeijerin (6) and geijerin (9) were isolated for the first time from genus Angelica. All isolates tested for inhibitory activity against acetylcholinesterae. Compounds 1 to 13 showed acetylcholinesterase inhibitory activity with $IC_{50}$ values ranging from 1.4 to $37.5{\mu}M$.

Antioxidant and Cholinesterase Inhibitory Activities of Aqueous Extract from Rainbow Trout Oncorhynchus mykiss

  • Baek, Jae-Min;Yoon, Na-Young;Kim, Yeon-Kye;Lee, Doo-Seog;Yoon, Ho-Dong;Park, Jeung-Sook
    • Fisheries and Aquatic Sciences
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    • v.14 no.2
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    • pp.89-92
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    • 2011
  • We investigated the antioxidant and cholinesterase inhibitory activities of the aqueous extract of rainbow trout Oncorhynchus mykiss. The antioxidant activity of O. mykiss aqueous extract was determined by in vitro peroxynitrite scavenging activity and reducing power assays. The aqueous extract of O. mykiss showed potent peroxynitrite radical scavenging activity ($IC_{50}=0.12{\pm}0.001\;mg/mL$) and reducing power (absorbance=$0.47{\pm}0.001$) at the concentration of 1 mg/mL. The in vitro cholinesterase inhibitory activity of O. mykiss aqueous extract was examined using spectrophotometric analyses of acetyl- and butyrylcholinesterase. The aqueous extract of O. mykiss showed acetylcholinesterase inhibitory activity ($IC_{50}=1.61{\pm}0.13\;mg/mL$), but did not exhibit inhibitory activity against butyrylcholinesterase. These results suggest that O. mykiss possesses antioxidant and acetylcholinesterase inhibitory activities and provide scientific evidence for the health benefits of O. mykiss aqueous extract.

Evaluation of Antioxidant and Cognition Improvement Effects of 10 Wild Vegetables Cultivated in Gangwon Province (강원도 10종 산채류의 항산화 및 인지능력개선 효능 평가)

  • Han, Xionggao;Choi, Sun-Il;Kim, Min-Jong;Lee, Ok-Hwan
    • The Korean Journal of Food And Nutrition
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    • v.32 no.6
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    • pp.662-668
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    • 2019
  • The purpose of this study was to investigate effect of methanolic extracts of 10 kinds of wild vegetables cultivated in Gangwon province on antioxidant activity, acetylcholinesterase, and β-secretase inhibitory activities. Results showed that among the wild vegetables, Aralia elata(Miq.) Seem shoot extract exhibited the highest total phenol content (84.65±1.08 mg GAE/g) and total flavonoids content (70.77±0.55 mg RE/g), respectively. The antioxidant activity of wild vegetables extracts was measured by using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay. Aralia elata(Miq.) Seem shoot extracts had the highest DPPH and ABTS scavenging activity (90.16%, 40.18% at 2 mg/mL). As a result, Aralia elata(Miq.) Seem shoot extract was the most effective in terms of acetylcholinesterase inhibitory activity (35.94% at 1 mg/mL). In the β-secretase activity assay, all 10 kinds wild vegetables extracts showed low inhibitory activity, and Aralia elata(Miq.) Seem shoot extract had highest inhibitory activity among the 10 wild vegetables extracts was 14.99%. Taken together, these results showed that Aralia elata(Miq.) Seem shoot extract has potential cognition improvement impact, suggesting that it may provide an effective strategy for improving cognition.