• Title/Summary/Keyword: acetylcholinesterase inhibitory activity

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In vitro antioxidant, anti-diabetic, anti-cholinesterase, tyrosinase and nitric oxide inhibitory potential of fruiting bodies of Coprinellus micaceus (갈색먹물버섯 자실체의 메탄올과 열수추출물의 항산화, 항당뇨, 항콜린에스테라아제, 항티로시나아제 및 Nitric oxide의 저해 효과)

  • Nguyen, Trung Kien;Lee, Min Woong;Yoon, Ki Nam;Kim, Hye Young;Jin, Ga-Heon;Choi, Jae-Hyuk;Im, Kyung Hoan;Lee, Tae Soo
    • Journal of Mushroom
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    • v.12 no.4
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    • pp.330-340
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    • 2014
  • Coprinellus micaceus, belongs to family Psathyrellaceae of Agaricales, Basidiomycota, has been used for edible purposes in the world. This study was initiated to evaluate the antioxidant, anti-diabetic, anti-cholinesterase, anti-tyrosinase, and nitric oxide inhibitory activities of fruiting bodies from C. micaceus extracted with methanol and hot water. The HPLC analysis of phenolic compounds from the mushroom extracts identified 4 phenolic compounds including procatechuic acid, chlorogenic acid, (-)-epicatechin, and naringin. In 1,1-diphenyl-2-picrylhydrazyl(DPPH) free radical scavenging assay, the scavenging activities of methanol and hot water extracts were lower than that of positive control, BHT. The chelating effects of methanol and hot water extracts were significantly higher than that of BHT, the positive control at the all concentrations tested. In the reducing power assay, methanol and hot water extracts exhibited the lower activities compared with positive control at the 0.125-0.2 mg/ml. The methanol and hot water extracts of the mushroom inhibited the ${\alpha}$-glucosidase activity by 62.26% and 67.59%, respectively at the 2.0 mg/ml, while acarbose, the positive control, inhibited the ${\alpha}$-glucosidase activity by 81.81% at the same concentration. In the acetylcholinesterase(AChE) inhibitory activity assay, methanol and hot water extracts of the mushroom inhibited the AChE by 94.64% and 74.19%, respectively at 1.0 mg/ml, whereas the galanthamine, standard drug, inhibited the AChE activity by 97.80% at the same concentration. The tyrosinase inhibitory activities of methanol and hot water extracts were 91.33% and 91.99% at 2.0 mg/ml, while the inhibitory activity of kojic acid, the positive control, was 99.61% at the same concentration. Nitric oxide(NO) production in lipopolysaccahride (LPS) activated RAW 264.7 cells were inhibited by the methanol and hot water extracts in a concentration dependent manner. Therefore, it is concluded that fruiting bodies of C. micaceus contained natural antioxidant, anti-acetylcholinesterase and ${\alpha}$-glucosidase inhibitory, anti-inflammatory, anti-tyrosinase substances which might be used for promoting human health.

The Effects of Crataegus prinnatiflora BGE. var. major N.E. BR(CPVM) Extract on the the Alzheimer's Disease Model Induced by CT105 (산사육(山査肉)이 CT105로 과도(課導)된 Alzheimer's Disease 병태(病態) 모델에 미치는 영향(影響))

  • Jung, In-Chul;Lee, Sang-Ryong;Chae, Jong-Gul
    • Journal of Oriental Neuropsychiatry
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    • v.13 no.1
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    • pp.79-115
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    • 2002
  • This research investigates the effect of the Crataegus pinnatifida BGE. var. major N.E. BR(CPVM) on Alzheimer's disease. Specifically, the effects of the DYHT extract on (1) $IL-1{\beta}$, IL-6, amyloid precursor proteins(APP), acetylcholinesterase(AChE), and glial fibrillary acidic protein(GFAP) mRNA of PC-12 cells treated with CTI05; (2) the AChE activity and the APP production of PC-12 cell treated with CT105; (3) the behavior; and (4) expression of $IL-1{\beta}$, $TNF-{\alpha}$, reactive oxygen species(ROS), nitrite oxide(NO); and (5) the infarction area of the hippocampus, and brain tissue injury in Alzheimer's diseased mice induced with CT105 were investigated. The results are as follow. 1. The CPVM extract suppressed the expression of $IL-1{\beta}$, IL-6, APP, AChE, and GFAP mRNA in PC-12 cells treated with CT105. 2. The CPVM extract suppressed the AChE activity and the production of APP significantly in PC-12 cells treated with CT105. 3. The CPVM extract group showed a significant inhibitory effect on the memory deficit for the mice with Alzheimer's disease induced by CT105 in the Morris water maze experiment. 4. The CPVM extract suppressed the over-expression of $IL-1{\beta}$, $TNF-{\alpha}$, ROS and NO in the mice with Alzheimer's disease induced by CT105. 5. The CPVM extract reduced the infarction area of hippocampus, and controlled the injury of brain tissue in the mice with Alzheimer's disease induced by CT105. These results suggest that the CPVM extract may be effective for the prevention and treatment of Alzheimer's disease.

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The Effects of Thalictrum foetidum(TFD) on the Alzheimer's Disease Model (마미련(馬尾連)이 Alzheimer's Disease 병웅(病熊) 모델에 미치는 영향(影響))

  • Bae, Jae-Yong;Lee, Sang-Ryong;Jung, In-Chul
    • Journal of Oriental Neuropsychiatry
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    • v.18 no.1
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    • pp.63-78
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    • 2007
  • Objective : This experiment was designed to investigate the effect of Thalictrum foetidum(TFD) on the Alzheimer's disease. Method : The effects of TFD on amyloid precursor proteins(APP), acetylcholinesterase(AChE), glial fibrillary acidic protein(GFAP) mRNA of PC-12 cell treated by amyloid ${\beta}$ $protein(A{\beta})$ and $IL-1{\beta}$, IL-6, $TNF-{\alpha}$ mRNA of THP-l cell treated by lipopolysaccharide(LPS), AChE activity of PC-12 cell lysate treated by $A{\beta}$ and behavior of the memory deficit mice induced by scopolamine, and glucose, AChE in serum of the memory deficit mice induced by scopolamine were investigated, respectively. Results : The results were summarized as follows ; 1. TFD suppressed APP, AChE, GFAP mRNA in PC-12 cell treated by $A{\beta}$. 2. TFD suppressed $IL-1{\beta}$, IL-6, $TNF-{\alpha}$ mRNA in THP-l cell treated by LPS 3.. TFD suppressed AChE activity in cell lysate of PC-12 cell treated by $A{\beta}$. 4. TFD increased glucose and decreased AChE significantly in the serum of the memory deficit mice induced by scopolamine. 5. TFD group showed significantly inhibitory effect on the scopolamine-induced impairment of learning and memory in the experiment of Morris water maze. Conclusion : According to the above results, it is suggested that TFD might be usefully applied for prevention and treatment of Alzheimer's disease.

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An In Vitro and In Vivo Cholinesterase Inhibitory Activity of Pistacia khinjuk and Allium sativum Essential Oils

  • Ghajarbeygi, Peyman;Hajhoseini, Ashraf;Hosseini, Motahare-Sadat;Sharifan, Anoosheh
    • Journal of Pharmacopuncture
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    • v.22 no.4
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    • pp.231-238
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    • 2019
  • Objectives: Alzheimer's disease (AD), an overwhelming neurodegenerative disease, has deleterious effects on the brain that consequently causes memory loss and language impairment. This study was intended to investigate the neuroprotective activity of the two essential oils (EOs) from Iranian Pistacia khinjuk (PK) leaves and Allium sativum (AS) cloves against β-Amyloid 25-35 (Aβ25-35) induced elevation of cholinesterase enzymes in AD. Methods: The EOs of PK (PKEO) and AS (ASEO) were prepared and analyzed in terms of extraction yield, phenolic content, and cholinergic markers in vitro. Moreover, both were administered orally to adult male Wistar rats at concentrations of 1, 2, and 3%. The inhibitory potential of PKEO and ASEO was compared with Donepezil (0.75 mg/kg) against the high activities of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Results: PKEO reached an inhibition rate of 83.6% and 81.4% against AChE and BChE, respectively. ASEO had lower anti-cholinesterase activity (65.4% and 31.5% for the inhibition AChE and BChE). PKEO was found to have more phenolic content than ASEO. A significantly positive correlation was observed between the total phenolics and anti-cholinesterase potential. In rats, both EOs decreased the enzyme activity in a concentration-dependent manner. As compared with Donepezil, the significant difference in the AChE and BChE inhibition occurred as rats were treated with PKEO 3% (p < 0.05). Conclusion: It could be concluded that PKEO and ASEO are potent inhibitors of AChE and BChE in rats that hold promise to be used for the treatment of AD.

In silico Prediction and In vitro Screening of Biological Activities and Pharmacokinetics for the Major Compounds in Chong Myung Tang (가상 검색 및 시험관 시험을 이용한 총명탕 중 주성분들에 대한 약물작용 및 대사 예측)

  • Kwon, Young-Ee
    • YAKHAK HOEJI
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    • v.51 no.6
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    • pp.463-468
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    • 2007
  • Chong Myung Tang is consisted of three medicinal herbs (Acori Graminei Rhizoma, Polygalae Radix and Hoelen cum Radix). It has been used as a medicine for the purpose of learning and memory improvement. In this paper, Chong Myung Tang was screened the biological activities for Alzheimer's disease. The extract (70% ethanol) of Acari Graminei Rhizoma (1 mg/ml) showed that acetylcholinesterase (AChE) and amyloid beta ($A{\beta}$) peptide aggregation inhibitory potency are 43.1% and 76.5%, respectively. The extract of Polygalae Radix showed inhibitory activity against $A{\beta}_{1-42}$ peptide aggregation (51.5%). To predict the drug-likeness, oral absorption ability; blood-brain barrier (BBB) penetraion rate, mutagenecity and carcinogenicity; in silico screening was performed against 16 compounds in the three medicinal herbs. According to the results, all compounds have appropriate chemical structures as medicines. The six compounds in Acori Graminei Rhizoma and the five compounds in Hoelen cum Radix showed excellent oral absorption rate and BBB penetration rate. The four compounds in Polygalae Radix showed excellent oral absorption rate, but their BBB penetration was presented low rate. And, the extract of Hoelen cum Radix didn't show AChE and $A{\beta}_{1-42}$ peptide aggregation inhibitory activities in vitro. Therefore, their activity in brain may be other mechanism. According to all of the results, in silico prediction technology is convenient and effective to determine biological active compounds in medicinal herbs.

Biological Compounds Extracted from Codium fragile by Enzymatic Hydrolysis and Their Biological Activities (효소적 가수분해를 이용한 청각으로부터 생리활성 물질의 추출 및 가수분해물의 생리활성)

  • Lee, Ka-Hwa;Senevirathne, Mahinda;Ahn, Chang-Bum;Je, Jae-Young
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.39 no.7
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    • pp.953-959
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    • 2010
  • We extracted bioactive materials from Codium fragile by enzymatic hydrolysis using four different proteases (Alcalase, Flavourzyme, Neutrase, and Protamex) and seven different carbohydrases (amyloglucosidase (AMG), Celluclast, Dextrozyme, Maltogenase, Promozyme, Termamyl, and Viscozyme), and evaluated their biological activities such as antioxidant, anti-acetylcholinesterase (AChE), and anti-inflammatory effects. All enzymatic hydrolysates showed good DPPH radical scavenging capacities, in particular, Flavourzyme and Promozyme hydrolysates possessed the highest activity. The two hydrolysates also exhibited strong hydrogen peroxide scavenging activity, $Fe^{2+}$ chelating activity, and reducing power in a dose-dependent manner. Furthermore, the two hydrolysates effectively protected DNA damage induced by hydroxyl radical by measuring the conversion of supercoiled DNA to the open circular DNA. All enzymatic hydrolysates also showed high anti-AChE inhibitory activities in a dose-dependent manner, and did not showed any significant cytotoxicity on RAW264.7 cells (p<0.05). In addition, the enzymatic hydrolysates significantly (p<0.05) inhibited lipopolysaccharide induced-nitric oxide production on RAW264.7 cells. These results suggest that the enzymatic extracts from Codium fragile would be good source as an ingredient of functional foods.

Effect of Curcuma longa Hot Water Extract on Activity of Neuronal Cells Related to Oxidative Stress (산화적 스트레스와 관련하여 신경세포의 활성에 미치는 강황 열수추출물의 영향에 대한 연구)

  • Chae, Yong-Byung;Chung, Kyung-Tae;Kim, Sung-Goo;Yoo, Byung-Hong;Kim, Moon-Moo
    • Journal of Life Science
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    • v.22 no.5
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    • pp.657-664
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    • 2012
  • The aim of this study is to screen a therapeutic agent with a cognitive function. The inhibitory effect of $Curcuma$ $longa$ hot water extract (CLWE) on the angiotension-converting enzyme and acetylcholinesterase derived from rabbit lungs and neural cells (PC12), as well as its antioxidant effect, was investigated in this study. Thus, for the first time, the direct scavenging effect of CLWE on DPPH radicals, superoxide anions, hydroxyl radicals, lipid peroxidation, reducing power, and the protective effect of DNA oxidation related to oxidative stress was evaluated in vitro. In addition, it was observed that CLWE especially exhibited a scavenging effect on reducing power and superoxide anions in this study. CLWE showed a protective effect on DNA oxidation produced by hydroxyl radicals. Furthermore, CLWE inhibited the activity of angiotensin-converting enzymes above 0.25%. Additionally, the extract inhibited oxidative stress and inducible nitric oxide in neuronal cells. Therefore, these results demonstrated that CLWE has antioxidant activity and neuronal cell protective effects, suggesting that it may have great potential as a natural source for human health.

Sesquiterpenoids from the heartwood of Juniperu s chinensis

  • Jung, Hee Jin;Min, Byung-Sun;Jung, Hyun Ah;Choi, Jae Sue
    • Natural Product Sciences
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    • v.23 no.3
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    • pp.208-212
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    • 2017
  • A new sesquiterpenoid, 11-hydroxy-valenc-1(10),3(4)-dien-2-one (3), two chemically synthesized but first isolate from nature, $3-oxocedran-8{\beta}-ol$ (1) and valenc-1(10),3(4),11(12)-trien-2-one (2) along with four known compounds, sugiol (4), (+)-nootkatone (5), 11-hydroxy-valenc-1(10)-en-2-one (6), and clovandiol (7), were isolated from the heartwood of Juniperus chinensis. All chemical structures were elucidated using extensive spectroscopic analysis including 1D and 2D NMR spectroscopy. Valenc-1(10),3(4),11(12)-trien-2-one (2) exhibited significant inhibitory activity against butyrylcholinesterase with an $IC_{50}$ value of $68.45{\mu}M$.

Characteristics of Unrecorded Wild Yeasts Obtained from the Soil of Spices Plant Fields and its Physiological Functionality (향신료 재배 토양으로부터 분리한 국내 미기록 야생효모들의 균학적 특성 및 생리활성)

  • Han, Sang-Min;Kim, Ji-Yoon;Kim, Changmu;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.47 no.1
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    • pp.75-81
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    • 2019
  • The goal of this study was to characterize unrecorded wild yeasts from soils of spices plants fields and further, to elucidate its anti-demential activities and tyrosinase inhibitory activity. Piskurozyma taiwanensis R4-1 (NIBRFGC000502619), Nadsonia starkeyi-henricii R6-2 (NIBRFGC000502618), and Canadida friedrichii M12-6 (NIBRFGC000502615) isolated from soil of garlic field represented newly recorded yeast strains in Korea. Vishniacozyma peneaus I2-9 (NIBRFGC000502617) and Cryptococcus aspenensis I21-1 (NIBRFGC000502616) from soil of ginger field represented also newly recorded yeast strains, and microbiological characteristics of its fifteen yeast strains were investigated. All of these unrecorded yeasts exhibited oval-global shape and have ascospores except Canadida friedrichii M12-6. Piskurozyma taiwanensis R4-1 and Canadida friedrichii M12-6 grew well in vitamin-free medium, and Piskurozyma taiwanensis R4-1 was halotolent growing in 10% NaCl-containing yeast extract peptone dextrose (YPD) broth. After prepared cell-free of the unrecorded wild yeasts, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities as anti-dementia activity and tyrosinase inhibitory activity as whitening activity were determined. Cell-free extract from Canadida friedrichii M12-6 had the highest tyrosinase inhibitory activity of 14.4%.

Protective Effect of Fucoidan Extract from Ecklonia cava on Hydrogen Peroxide-Induced Neurotoxicity

  • Park, Seon Kyeong;Kang, Jin Yong;Kim, Jong Min;Park, Sang Hyun;Kwon, Bong Seok;Kim, Gun-Hee;Heo, Ho Jin
    • Journal of Microbiology and Biotechnology
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    • v.28 no.1
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    • pp.40-49
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    • 2018
  • We evaluated the antioxidant activity and neuronal cell-protective effect of fucoidan extract from Ecklonia cava (FEC) on hydrogen peroxide ($H_2O_2$)-induced cytotoxicity in PC-12 and MC-IXC cells to assess its protective effect against oxidative stress. Antioxidant activities were examined using the ABTS radical scavenging activity and malondialdehyde-inhibitory effect, and the results showed that FEC had significant antioxidant activity. Intracellular ROS contents and neuronal cell viability were investigated using the DCF-DA assay and MTT reduction assay. FEC also showed remarkable neuronal cell-protective effect compared with vitamin C as a positive control for both $H_2O_2$-treated PC-12 and MC-IXC cells. Based on the neuronal cell-protective effects, mitochondrial function was analyzed in PC-12 cells, and FEC significantly restored mitochondrial damage by increasing the mitochondrial membrane potential (${\Delta}{\Psi}m$) and ATP levels and regulating mitochondrial-mediated proteins (p-AMPK and BAX). Finally, the inhibitory effects against acetylcholinesterase (AChE), which is a critical hydrolyzing enzyme of the neurotransmitter acetylcholine in the cholinergic system, were investigated ($IC_{50}$ value = 1.3 mg/ml) and showed a mixed (competitive and noncompetitive) pattern of inhibition. Our findings suggest that FEC may be used as a potential material for alleviating oxidative stress-induced neuronal damage by regulating mitochondrial function and AChE inhibition.