• Title/Summary/Keyword: Acetylcholinesterase activity

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Screening of the Biologoical Activity from Water Extracts of the Medicinal Plants and the Protective Effect of R. palmatum on MTPT-induced Neurotoxicity (한약재 물 추출물의 생리활성 검색 및 MPTP-유도 신경독성에 대한 대황의 보호효과)

  • Kim Tae Eun;Yoon Yeo Min;Park Yong In;Kim Youn Seok;Jeon Byung Hun;Kim Myung Dong
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.18 no.6
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    • pp.1666-1685
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    • 2004
  • This present study was designed to screen medicinal plants for the treatment of brain diseases such as Parkinson's disease or aging. We tested the effects of the water extracts from 38 species medicinal plants on antioxidant capacity, monoamine oxidase B (MAO-B) inhibitory activity, acetylcholinesterase (AChE) inhibition and antiperoxidation activity in vitro. The water extracts from 38 species were tested on their antioxidant activity using radical scavenging effects against ABTS+. The water extract of C. sappan was showed the highest antioxidant capacity, the antioxidant activity at 1 Jig of herbal extract being 0.38mM TE. Lipid peroxidation in brain homogenates induced by NADPH and ADP-Fe/sup 2+/ was strong inhibited by C. sappan and R. palmatum extracts. Among the 38 medicinal plants investigated, R. palmatum showed significant biological activity (antioxidant capacity, MAO-B inhibiory activity, and AChE inhibitory activity). The protective efficacy of R. palmatum water extract on 1-methyl-4­phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced parkinsonism and its possible mechanism were studied in C57BL/6 mice. Treatment of R. palmatum water extract protected biomacromolecules such as lipids from oxidative damage induced by MPTP. The content of MDA in brain tissue was decreased significantly by R. palmatum extract. These results suggest that R. palmatum water extract plays on effective role in attenuating MPTP-induced neurotoxicity in mice. This protective effect of R. palmatum might be estimated the result from the inhibitory activity on monoamine oxidase B and the enhancement of antioxidant activity.

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 Insecticide Carbofuran and Phenobarbital Sodium and 3-Methylcholanthrene on Activity of Enzyme in Israeli Carp(Cyprinus israeli carpio L.) (살충제 Carbofuran과 Phenobarbital Sodium 및 3-Methylcholanthrene이 이스라엘 잉어의 효소활성에 미치는 영향)

  • Rim, Yo-Sup;Jeong, Jae-Hun;Han, Seong-Soo
    • Applied Biological Chemistry
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    • v.39 no.1
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    • pp.77-83
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    • 1996
  • Effects of insecticide carbofuran and Phenobarbital sodium(PB) or 3-methylcholanthrene(3-MC) on activities of several enzymes in israeli carps were investigated. Survival number of Israeli carp was the same as that of control when PB and 3-MC only was treated, individually and that was low compared to control when carbofuran only was treated. But survival rate of Israeli carp was high compared to individual treatment of carbofuran when combination treatment of carbofuran and PB or 3-MC was carried out. These results indicate that PB and 3-MC can intervene to detoxify carbofuran exposed to israeli carp. In in vivo test for the effect of this chemicals on activity of enzyme in israeli carp, activities of acetylcholinesterase(AChE) and glutathione S-transferase(GST) were inhibited in carbofuran treatment, but did not in combination treatment of carbofuran and P3 or 3-MC. Activities of UDP-glucuronosyltransfe-rase (UDPGT) and cytochrome P-450-dependent monooxygenase increased in individual or combined treatments of carbofuran and PB or 3-MC. These results suggest that a simultaneous application of carbofuran and PB or 3-MC is critical for the enhancement of activity of AChE, GST, UDPGT and monooxygenase and the protection of Israeli carp from carbofuran toxicity.

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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.

Effects of Hwangryunhaedok-Tang Decoction & Hwangryunhaedok-Tang Pharmacopuncture Solution on the Cognitive & Memory Impairment Induced by Scopolamine in Mouse Model (황련해독탕 전탕액과 약침액이 치매유발생쥐의 인지와 기억에 미치는 영향)

  • Kwon, Young-Wan;Kang, Tae-Ri;Lee, Sang-Ryong
    • Korean Journal of Acupuncture
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    • v.36 no.4
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    • pp.230-240
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    • 2019
  • Objectives : This research was performed to investigate the effects of Hwangryunhaedok-tang decoction and Hwangryunhaedok-tang Pharmacopuncture at BL10 on cognition and memory impairment in a mouse dementia model induced by scopolamine. Methods : Fifty ICR mice were divided into 6 groups : Normal group (n=5), Control group (n=9), Positive control group for pharmacopuncture group (n=9, Donepezil 0.75 mg/kg), Positive control group for oral administration group (n=9, Donepezil 5 mg/kg), Pharmacopuncture group (n=9, Hwangryunhaedok-tang Pharmacopuncture undiluted solution 10 ml/kg), and Oral administration group (n=9, Hwangryunhaedok-tang 200 mg/kg). For a mouse dementia model, 1 mg/kg scopolamine was intraperitoneally administered to ICR mice. Hwangryunhaedok-tang pharmacopuncture was administered on BL10 for 4 weeks at intervals of 2 days. Hwangryunhaedok-tang decoction was given orally for 4 weeks every day. Morris water maze and passive avoidance test were conducted followed by measurement of acetylcholine concentration, acetylcholinesterase activity, and the amount of BDNF and p-CREB in the brain. Results : 1. In the Morris water maze test, the time spent staying around the platform significantly increased in the pharmacopuncture group and oral administration group than in the control group. 2. In the passive avoidance test, the time spent in the bright room significantly increased in the pharmacopuncture group and oral administration group than in the control group. 3. The level of acetylcholine in brains increased in the pharmacopuncture group and oral administration group than in the control group. Also, the activity of acetylcholinesterase decreased in the pharmacopuncture group and oral administration group than in the control group. 4. The expression of BDNF and p-CREB decreased in the control group, but increased in the pharmacopuncture group and oral administration group. Conclusions : These results suggest that Hwangryunhaedok-tang decoction and Hwangryunhaedok-tang pharmacopuncture at BL10 may have cognition and memory-enhancing effect in scopolamine-induced dementia in ICR mice via controlling the content of acetylcholine and the activity of acetylcholinesterase, and activating BDNF and p-CREB.

Linear Free Energy Relationship on the Phosphorylation of Acetylcholinesterase by Insecticidal O,O-Diethylphenylphosphate Derivatives (살충성(殺蟲性) O,O-Diethylphenylphosphate유도체(誘導體)들에 의(依)한 Acetylcholinesterase의 Phosphorylation에 미치는 자유(自由)에너지 관계(關係))

  • Sung, Nack-Do
    • Korean Journal of Agricultural Science
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    • v.11 no.1
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    • pp.176-181
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    • 1984
  • Linear free energy relation ship(LFER) on the insecticidal activity of O,O-diethylphenylphosphate (A) and 3,5-dimethylphenyl-O,O-diethylphosphate (B) derivatives were studied by EHT MO calculation method and regression analysis method. LFER between varying substituent constants and $pI_{50}$ constants of phosphates, (A) & (B) were calculated with applying Hammett, Okamoto-Brown, Taft and Swain-Lupton's DSP equations;percent resonance effect(R) and field effect(F) of (A) were %R=33.5 & %F=66.5 and also that of (B) were %R=2 & %F=98, respectively. On the basis of above findings, the insecticidal activities were similar for both (A) and (B), but (B) have larger field and inductive contribution than (A), due to the 3,5-dimethyl group of (B).

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Effect of Pine Needle Extract (PNE) on Physilolgical Activity of SD Rats III. Feeding Effect of PNE on Fluidity and Neurotransmitter-Related Enztmes in Brain Membranes of SD Rats (흰쥐의 생리활성에 미치는 송엽(松葉) 추출물(PNE)의 영향 III. 뇌세포막의 유동성 및 신경전달관련 효소의 활성에 미치는 PNE의 투여효과)

  • Choi, Jin-Ho;Kim, Jung-Hwa;Kim, Dong-Woo;Hwang, Chan-Ho;Kim, Dae-Ik;Lee, Jong-Soo
    • Journal of Life Science
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    • v.8 no.2
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    • pp.167-172
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    • 1998
  • To investigate the effect of pine needle extract (PNE) on membrane fluidirt and neurotransmiter-related enzymes in brain of Spragu-Dawley(SD), male SD rats were fed basic diets (control group), and experimantal diets (PNE group)with 0.5% and 0.1% fo PNE for 6 weeks. pine (pinus tabulaeformis C$_{ARR}$ is one of the popular plant drugs which has used as a medicine in Asia. Cholesterol levels in brain mitochondria of 0.5%-PNE and 0.1%-PNDE groups were significantly decreased in 15% and 25%, respectively, compared with control group, but cholesterol levels in brain microsomes of these PNE groups howed almost no change compared with control group. Lipofuscin accumulations in brain membranes of 0.5%-PNE and 0.1%-PNE groups were sgnificantly inhibited in 18% and 21%, respectively, compared with control group. Brain memberance fluidity was also activated in 50% and 100% by the administration of 0.5%-PNE and 0.1%-PNE. higher acetylcholinesterase(15% and25%) and lower monoamine oxidase B (25% and 15%0 activities were effectively modulated by the administration of 0.5%-PNE and 0.1%-PNDE. These results suggest that more beneficial effects such as inhibition of cholesterol and lipofuscin, increase of membrane fluidity, higher acetylcholinesterase and lower monoamone oxidase activities in brain membranes of SD rats may be effectively modulated by administration of pine needle extract (PNE).

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Effect of Aloe on Learming and Memory lmpaiments in Dementia Animal Model SAMP8 (치매동물모델 SAMP8에 있어서 기억. 학습장해에 미치는 알로에의 영향 III. SAMP8의 신경전달물질 및 그 대사산물에 미치는 알로에의 투여효과)

  • Choi, Jin-Ho;Kim, Dong-Woo;Kim, Jae-il;Han, Sang-Seop;Shim, Chang-Sub
    • Journal of Life Science
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    • v.6 no.2
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    • pp.142-148
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    • 1996
  • Aloe(Aloe arborescens M$_{ILL}$) has been used as a home medicine for the past several thousand in the world, and has been studied on anti-bacterial and anti-fungal activities, hypotension, atherosclerosis, myocardiac infartion, apoplexy, diabetes as a chronic digenerative disease, tumors, gastrointestinal tract, liver and pancreas' diseases, and genitourinary tract etc. SAMP8 as a learing and memory impairment animal model were fed basic and/or experimental diets with 1.0% freezing dried(FD)-aloe for 8 months. The passive avoidance tests such as acqusition trial and retention test were significantly higher in aloe group than in control group. Grading score of senescence resulted in a marked decreases in aloe group compared with control group. Acetylcholinesterase(AChE) activity was remarkably increased in aloe group compared with control group. Neurotransmitters such as dopamine(DA) and serotonin(5-HT) almost did not change by the feeding of aloe-added diet, but their metabolites such as homovanillic acid(HVA) and 5-hydroxy-indole acetic acid(5-HIAA) in aloe group were significantly increased compared with control group. Therefore, the ratios of HVA/DA and 5-HIAA/5-HT as a ratio of metabolite on neurotransmitter were significantly increased by the feeding of aloe-added diet. These results suggest that aloe vara may be activated acetylcholinesterase, the metabolite of neurotransmitter, and ratios of metabolite on neurotransmitter, resulting ina greater prevention of learning and memory impairments such as Alzheimertype dementia.

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Biruloquinone, an Acetylcholinesterase Inhibitor Produced by Lichen-Forming Fungus Cladonia macilenta

  • Luo, Heng;Li, Changtian;Kim, Jin Cheol;Liu, Yanpeng;Jung, Jae Sung;Koh, Young Jin;Hur, Jae-Seoun
    • Journal of Microbiology and Biotechnology
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    • v.23 no.2
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    • pp.161-166
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    • 2013
  • At present, acetylcholinesterase (AChE) inhibitors are the first group of drugs to treat mild to moderate Alzheimer's disease (AD). Although beneficial in improving cognitive and behavioral symptoms, the effectiveness of AChE inhibitors has been questioned since they do not delay or prevent neurodegeneration in AD patients. Therefore, in the present study, in order to develop new and effective anti-AD agents from lichen products, both the AChE inhibitory and the neuroprotective effects were evaluated. The AChE inhibitory assay was performed based on Ellman's reaction, and the neuroprotective effect was evaluated by using the MTT method on injured PC12 cells. One AChE inhibitor ($IC_{50}$ = 27.1 ${\mu}g/ml$) was isolated by means of bioactivity-guided isolation from the extract of lichen-forming fungus Cladonia macilenta, which showed the most potent AChE inhibitory activity in previous screening experiment. It was then identified as biruloquinone by MS, and $^1H$- and $^{13}C$-NMR analyses. The inhibitory kinetic assay suggested that biruloquinone is a mixed-II inhibitor on AChE. Meanwhile, biruloquinone improved the viability of the $H_2O_2$- and ${\beta}$-amyloid-injured PC12 cells at 1 to 25 ${\mu}g/ml$. The protective effects are proposed to be related to the potent antioxidant activities of biruloquinone. These results imply that biruloquinone has the potential to be developed as a multifunctional anti- AD agent.