• 제목/요약/키워드: acetylcholinesterase inhibitory activity

검색결과 142건 처리시간 0.028초

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

  • ;이민웅;윤기남;김혜영;진가헌;최재혁;임경환;이태수
    • 한국버섯학회지
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    • 제12권4호
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    • pp.330-340
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    • 2014
  • 본 연구에서는 메탄올과 열수를 이용해 갈색먹물버섯의 자실체로부터 추출한 물질의 항산화, 항당뇨, 항콜린에스테라아제, 항티로시나제와 항염증 효과를 탐색하였다. 고속액체크로마토그래피를 이용해 추출물의 페놀성 화합물을 분석한 결과 procatechuic acid, chlorogenic acid, (-)-epicatechin, naringin 등 총 4종류의 페놀성 화합물이 확인되었다. 항산화 효과 실험에서 DPPH radical 소거능은 양성대조군으로 사용한 BHT에 비해 낮았지만 효과가 비교적 우수하였고, 철 이온을 제거하는 항산화 효과는 메탄올과 열수 추출물이 양성대조군인 BHT에 비해 30% 높게 나타났으나 환원력은 양성대조군에 비해 43% 정도 낮은 것으로 나타났다. 항당뇨 실험에서 ${\alpha}$-amylase와 ${\alpha}$-glucosidase에 대한 메탄올과 열수추출물의 저해효과는 2.0 mg/ml의 농도에서 각각 62.26%와 67.59%를 보여 양성대조군인 acarbose의 81.81%에 비해 낮았다. 아세틸콜린에스테라아제에 대한 메탄올과 열수추출물의 저해효과는 1.0 mg/ml의 농도에서 각각 94.64%와 74.19%를 보여 양성대조군인 galanthamine의 97.80%에 비해 낮았다. 티로시나아제에 대한 메탄올과 열수추출물의 저해효과는 2.0 mg/ml의 농도에서 각각 91.33%와 91.99%를 나타내 양성대조군인 kojic acid의 99.61%와 매우 유사한 효과를 얻었다. 염증저해 효과 실험에서는 RAW 264.7 대식세포가 배양되고 있는 배지에 갈색먹물버섯 자실체의 메탄올과 열수추출물을 각각 전 처리 한 후 염증매개 물질인 LPS를 투여하여 메탄올과 열수 추출물의 NO 생성 저해효과를 조사한 결과 추출물의 농도가 증가함에 따라 생성된 NO의 양이 감소하는 경향을 나타내었다. 따라서 갈색먹물버섯의 자실체에는 항산화, 항당뇨, 항아세틸콜린에스터라제 항티로시나아제 및 항염증 효과를 나타내는 물질이 함유되어 있어서 천연 건강식품으로 이용이 가능할 것으로 사료된다.

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

  • 정인철;이상룡;채종걸
    • 동의신경정신과학회지
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    • 제13권1호
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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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마미련(馬尾連)이 Alzheimer's Disease 병웅(病熊) 모델에 미치는 영향(影響) (The Effects of Thalictrum foetidum(TFD) on the Alzheimer's Disease Model)

  • 배재용;이상룡;정인철
    • 동의신경정신과학회지
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    • 제18권1호
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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
    • 대한약침학회지
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    • 제22권4호
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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.

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

  • 권영이
    • 약학회지
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    • 제51권6호
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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.

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

  • 이가화;;안창범;제재영
    • 한국식품영양과학회지
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    • 제39권7호
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    • pp.953-959
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    • 2010
  • 본 연구에서는 청각으로부터 생리활성물질을 추출하기 위해서 친환경적인 효소적 방법을 이용하여, 이들 효소 가수 분해물의 TPC, TFC, 항산화 활성, acetylcholinesterase(AChE) 저해 활성 및 항염증 활성을 측정하였다. 청각의 단백질 및 탄수화물 가수분해물의 TPC는 TFC보다 높은 함량을 나타내었으며, 단백질 가수분해물이 탄수화물 가수분해물보다 높은 TPC를 나타내었다. 청각 가수분해물의 항산화 활성은 DPPH radical 소거 활성으로 측정하였고, 단백질 가수분해물에서는 Flavourzyme 가수분해물이 활성이 높았고, 탄수화물 가수분해물에서는 Promozyme 가수분해물이 높은 DPPH radical 소거 활성을 나타내었다. 따라서 두가지 가수분해물을 이용하여 hydrogen peroxide 소거능, $Fe^{2+}$ 킬레이팅 및 reducing power를 측정한 결과 두 가수분해물 모두 우수한 항산화 활성을 나타냄을 알 수 있었다. 또한, hydroxyl radical로 유도된 DNA 손상을 효과적으로 억제하였다. AChE 저해 활성에서는 Flavourzyme 및 Dextrozyme 가수분해물이 각각 우수한 AChE 저해 활성을 나타내었다. 청각 가수분해물의 RAW264.7 세포주에 대한 세포독성을 검토한 결과 세포독성을 나타내지 않았으며, lipopolysaccharide(LPS)로 유도된 nitric oxide(NO) 생성 억제능에서는 모든 가수분해물이 유의적(p<0.05)으로 NO의 생성을 억제하였다.

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

  • 채용병;정경태;김성구;유병홍;김문무
    • 생명과학회지
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    • 제22권5호
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    • pp.657-664
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    • 2012
  • 본 연구의 목적은 인지기능을 가진 약효제를 발굴하는 것이다. 본 연구에서는 토끼의 간과 신경세포로부터 각각 유래한 angiotension converting enzyme과 acetylcholinesterase에 대한 강황 열수추출물(CLWE)의 억제효과 뿐만 아니라 항산화 효과가 조사되었다. 이리하여 먼저 산화적 스트레스와 연관이 있는 환원력과 DPPH radical, superoxide anion, hydroxyl radical, lipid peroxidation에 대한 CLEW의 소거능 및 DNA 산화에 대한 보호효과를 평가하였다. CLEW는 환원력 뿐만 아니라 본 연구에서 시험된 활성산소종 중에서 특히 superoxide anion의 소거능이 가장 우수한 것으로 나타났다. 더욱이 CLEW는 0.25% 이상의 농도에서 angiotensin converting enzyme 활성을 억제효과를 발휘하는 것으로 나타났다. 신경세포에서 CLEW는 또한 산화적 스트레스와 nitric oxide 유발을 억제하였다. 그러므로 이상의 결과는 CLEW의 항산화 효과와 신경세포 보호효과를 입증하여, 이것이 사람의 신경건강을 위한 천연생물소재로 잠재적인 가능성을 가지고 있을 것으로 시사한다.

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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    • 제23권3호
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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 $68.45{\mu}M$.

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

  • 한상민;김지윤;김창무;이종수
    • 한국균학회지
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    • 제47권1호
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    • pp.75-81
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    • 2019
  • 생리기능성을 조사하기 위하여 먼저 충남 금산의 양파와 도라지, 마늘과 생강 등의 재배지 토양시료에서 분리, 동정한 야생효모 중 마늘 재배지에서 분리한 Piskurozyma taiwanensis R4-1 (NIBRFGC000502619), Nadsonia starkeyi-henriciiR6-2 (NIBRFGC000502618), Canadida friedrichiiM12-6 (NIBRFGC000502615) 균주와 생강에서 분리한 Vishniacozyma peneaus I2-9 (NIBRFGC000502617)와 Cryptococcus aspenensisI21-1 (NIBRFGC000502616) 균주의 야생효모를 국내 미기록 효모 균주로 최종 선별하여 이들의 형태학적, 배양학적 특성 등을 조사하였다. 미기록 균주들은 구형~타원형으로 PiskurozymataiwanensisR4-1, Nadsoniastarkeyi-henriciiR6-2들은 자낭포자를 형성하였다. Vishniacozyma peneausI2-9, Cryptococcus aspenensisI21-1, Piskurozyma taiwanensis R4-1, Nadsonia starkeyi-henricii R6-2는 yeast extract-peptone-dextrose (YPD) 배지와 yeast extract-malt extracts (YM) 배지, 비타민을 첨가하지 않은 YPD 배지에서도 모두 생육하였으며 Vishniacozyma peneausI2-9 외 4균주 모두 10% NaCl을 함유한 YPD 배지에서 생육하는 호염성 효모였다.

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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    • 제28권1호
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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.