• 제목/요약/키워드: Acetylcholinesterase activity

검색결과 337건 처리시간 0.029초

국내 시판 녹차, 보이차, 우롱차 및 홍차의 폴리페놀 함량, 항산화 및 아세틸콜린에스터레이스 저해 효과 (Phenolic Content, Antioxidant Effect and Acetylcholinesterase Inhibitory Activity of Korean Commercial Green, Puer, Oolong, and Black Teas)

  • 정창호;강수태;주옥수;이승철;신영희;심기환;조성환;최성길;허호진
    • 한국식품저장유통학회지
    • /
    • 제16권2호
    • /
    • pp.230-237
    • /
    • 2009
  • 본 연구에서는 국내에서 시판되고 있는 4종류의 차 즉, 녹차, 보이차, 우롱차 및 홍차 열수추출물의 페놀성 화합물, 항산화 및 퇴행성 뇌신경질환 저해활성에 대하여 조사하였다. 시판 차 열수추출물의 총 페놀성 화합물 함량은 $72.03{\sim}85.62\;mg/g$이었으며, 녹차, 보이차, 우롱차 및 홍차 열수추출물의 총 플라보놀 함량은 각각 350.96, 254.17, 334.48 및 240.23 mg/100 g이었다. 녹차, 보이차, 우롱차 및 홍차 열수추출물의 총 카테킨 함량은 각각 2,920.35, 1,016.23, 2,824.22 및 1,006.51 mg/100 g이었으며, 카페인함량은 녹차 열수추출물에서 가장 높은 함량을 보였다. $ABTS{\cdot}+$ 라디칼 소거활성도 농도 의존적인 경향을 보였으며, FRAP은 다른 차 열수추출물에 비하여 녹차 열수추출물에서 가장 높게 나타났다. $\beta$-carotene과 linoleic acid system을 이용하여 측정한 항산화 활성 및 퇴행성 뇌신경질환효소 억제활성도 녹차 열수추출물에서 가장 높은 효과를 보였다. 따라서 시판 차 4종의 열수추출물을 이용하여 항산화 및 퇴행성 뇌신경질환효소 억제활성을 측정한 결과 녹차 열수추출물이 가장 높은 활성을 보였으며, 홍차 열수추출물이 가장 낮게 나타났다.

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
    • /
    • 제28권1호
    • /
    • pp.40-49
    • /
    • 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.

자성 흰쥐의 파라치온 급성독성 및 대사에 미치는 페노바르비탈 및 SKF-525-A의 영향 (EFFECT OF PHENOBARBITAL AND / OR SKF 525-A ON THE METABOLISM AND ACUTE TOXICITY OF PARATHION IN ADULT FEMALE PATS)

  • 최재화;임혜경;김영철
    • Toxicological Research
    • /
    • 제6권1호
    • /
    • pp.51-59
    • /
    • 1990
  • Effects of altering hepatic mixed-function oxidase (MFO) enzyme activities on the metabolism and acute toxicity of parathio were investigated in adult female rats. In vitro hepatic metabolism of parathion to paraoxon was increased by phenobarbital pretreatment (50 mg/kg/day, ip, for 4 consecutive days) and SKF 525-A (50 mg/kg, ip, 1 hr prior to sacrifice) decreased paraoxon formation indicating that phenobarbital induces that form(s) of cytochrome P-450 catalyzing conversion of parathion to paraoxon. Degradation of paraoxon to p-nitrophenol was increased by phenobarbital pretreatment, but not affected by SKF 525-A suggesting that MFO activities play only a minor role in the detoxification of the active metabolite of this insecticide. The phenobarbital-induced increase in paraoxon formation was partially antagonized by SKF 525-A. Significant activity for both parathion activation and paraoxon degradation was also observed in the lung preparation, however, this extrahepatic parathion and paraoxon metabolizing activity was not induced by phenobarbital or inhibited by SKF 525-A pretreatment. Phenobarbital pretreatment increased paraoxon level in livers of rats when measured 3 hr following parathion injection (2 mg/kg, ip). SKF 525-A did not alter parathion or paraoxon levels in brain, blood and liver. Phenobarbital pretreatment decreased the toxicity of parathion (4mg/kg, ip) or paraoxon (1.5 mg/kg, ip) as determined by decreases in lethality and inhibition of brain and lung acetylcholinesterases. An additional SKF 525-A treatment failed to decrease the protective effects of phenobarbital against parathion or paraoxon toxicity. These results suggest that some unknown factors other than hepatic MFO induction are involved in the protective action of phenobarbital against parathion and paraoxon toxicity.

  • PDF

황백(黃柏)이 Alzheimer's Disease 병태(病態) 모델에 미치는 영향 (Effects of Phellodendron amurense Extract on the Alzheimer's Disease Model)

  • 김영표;정인철;이상룡
    • 동의생리병리학회지
    • /
    • 제19권1호
    • /
    • pp.130-138
    • /
    • 2005
  • This experiment was designed to investigate the effect of Phellodendron amurense(PLDA) on the Alzheimer's disease. The effects of PLDA extract on $IL-1{\beta}$, IL-6, amyloid precursor proteins(APP), acetylcholinesterase(AChE), glial fibrillary acidic protein(GFAP) mRNA of PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$ and AChE activity of PC-12 cell lysate treated by $A{\beta}$ plus $rIL-1{\beta}$ and behavior of memory deficit mice induced by scopolamine and mice glucose, uric acid, AChE activity of memory deficit rats induced by scopolamine were investigated, respectively. PLDA extract suppressed $IL-1{\beta}$, IL-6, APP, AChE, GFAP mRNA in PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$ ; AChE activity in cell lysate of PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$. PLDA extract increased glucose, decreased uric acid and AChE significantly in the serum of the memory deficit rats induced by scopolamine. PLDA extract group showed significantly inhibitory effect on the memory deficit of mice induced by scopolamine in the experiment of Morris water maze. According to the above results, it is suggested that PLDA extract might be usefully applied for prevention and treatment of Alzheimer's disease.

Effects of Single Treatment of Anti-Dementia Drugs on Sleep-Wake Patterns in Rats

  • Jung, Ji-Young;Roh, Moo-Taek;Ko, Kyung-Kyun;Jang, Hwan-Soo;Lee, Seong-Ryong;Ha, Jeoung-Hee;Jang, Il-Sung;Lee, Ho-Won;Lee, Maan-Gee
    • The Korean Journal of Physiology and Pharmacology
    • /
    • 제16권4호
    • /
    • pp.231-236
    • /
    • 2012
  • We studied the effects of acetylcholinesterase inhibitors, donepezil and galantamine, and an N-methyl-D-aspartate (NMDA) receptor blocker, memantine, on sleep-wake architecture in rats. Screw electrodes were chronically implanted into the frontal and parietal cortex for the electroencephalography (EEG). EEG was recorded with a bio-potential amplifier for 8 h from 09:30 to 17:30. Vibration was recorded to monitor animal activity with a vibration measuring device. Sleep-wake states such as wake (W), slow-wave sleep (S) and paradoxical or rapid eye movement sleep (P), were scored every 10 sec by an experimenter. We measured mean episode duration and number of episode to determine which factor sleep disturbance was attributed to. Donepezil and memantine showed a significant increase in total W duration and decreases in total S and P duration and delta activity. Memantine showed increases in sleep latency and motor activity. Changes of S and P duration in memantine were attributed from changes of mean episode duration. Galantamine had little effect on sleep architecture. From these results, it is showed that galantamine may be an anti-dementia drug that does not cause sleep disturbances and memantine may be a drug that causes severe sleep disturbance.

Development of Cholinesterase Inhibitors using 1-Benzyl Piperidin-4-yl (α)-Lipoic Amide Molecules

  • Lee, Seung-Hwan;Kim, Beom-Cheol;Kim, Jae-Kwan;Lee, Hye Sook;Shon, Min Young;Park, Jeong Ho
    • Bulletin of the Korean Chemical Society
    • /
    • 제35권6호
    • /
    • pp.1681-1686
    • /
    • 2014
  • A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and 4-amino-1-benzyl piperidines were synthesized and their in vitro cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)) inhibitory activities were evaluated. Even though the parent compounds did not exhibit any inhibitory activity against cholinesterase (ChE) with the exception of compound 14 ($IC_{50}=255.26{\pm}4.41$ against BuChE), all hybrid molecules demonstrated BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, compound 17 was shown to be an effective inhibitor against both AChE ($IC_{50}=1.75{\pm}0.30{\mu}M$) and BuChE ($IC_{50}=5.61{\pm}1.25{\mu}M$) comparable to galantamine ($IC_{50}=1.7{\pm}0.9{\mu}M$ against AChE and $IC_{50}=9.4{\pm}2.5{\mu}M$ against BuChE). Inhibition kinetic studies using compound 17 indicated a mixed inhibition type for AChE and a noncompetitive inhibition type for BuChE. Its binding affinity ($K_i$) values to AChE and BuChE were $3.8{\pm}0.005{\mu}M$ and $7.0{\pm}0.04{\mu}M$, respectively.

Two Androstane Derivatives from the Cultures of Fungus Marasmiellus ramealis (Bull.) Singer

  • Yang, Ning-Ning;Ma, Qing-Yun;Huang, Sheng-Zhuo;Dai, Hao-Fu;Guo, Zhi-Kai;Yu, Zhi-Fang;Zhao, You-Xing
    • Bulletin of the Korean Chemical Society
    • /
    • 제35권11호
    • /
    • pp.3224-3226
    • /
    • 2014
  • A new androstane derivative, $4{\beta}$-methyl-15-oxa-$14{\beta}$-androstane-7-ene-$4{\alpha}$-carboxylic acid (1) and a known one $4{\beta}$-methyl-15-oxa-$14{\beta}$-androstane-7-ene-$4{\alpha}$-hydroxyl (2) were isolated from the EtOAc extract of the cultures of the fungus Marasmiellus ramealis (Bull.) Singer. Their structures were elucidated on the basis of 1D and 2D NMR as well as MS spectroscopic data analysis. The inhibitory activity of two isolates against acetylcholinesterase (AChE) revealed that compound 1 exhibited definitely inhibitory activity.

Scopolamine 처리에 의한 인지 및 기억력 손상 마우스에서 박하의 효과 (Mentha arvensis Attenuates Cognitive and Memory Impairment in Scopolamine-treated Mice)

  • 이지혜;김혜정;장귀영;서경혜;김미려;최윤희;정지욱
    • 생약학회지
    • /
    • 제51권1호
    • /
    • pp.70-77
    • /
    • 2020
  • Mentha arvensis is used traditional medicine to treat various disorders. In the present study, M. arvensis were extracted by the solid-phase microextraction (SPME) method and analyzed by gas chromatograph-mass spectrometry (GC-MS). We investigated the protective effects and mechanisms of a M. arvensis extract on scopolamine-induced cognitive and memory impairment. Mice were orally pretreated with a M. arvensis extract or normal saline, and then behavior tests were conducted 30 min after scopolamine injection. The antioxidant capacities were analyzed by free radical scavenging (DPPH and ABTS). Acetylcholinesterase (AChE) activity were also measured using Ellman's method ex vivo test. In behavior tests, percent of spontaneous alteration, escape latency and swimming time in target quadrant were improved by the administration of the M. arvensis extract, which suggests that the M. arvensis extract improves memory function in the scopolamine-treated mice model. In addition, M. arvensis extract showed inhibition of the free radical and AChE activity. The results of the present study suggest that the M. arvensis extract ameliorates scopolamine-induced cognitive and memory deficits through the inhibition of free radicals and AChE activity. Therefore, M. arvensis may be a promising neuroprotective agent for management of learning and memory improvements in human dementia patients.

일황련(日黃連)이 치과병태(痴果病態)모델에 미치는 영향(影響) (The Effects of Coptis japonica Makino(CJM) Extract on the Alzheimer's Disease Model)

  • 정인철;이상룡;박지운
    • 동의신경정신과학회지
    • /
    • 제15권1호
    • /
    • pp.87-99
    • /
    • 2004
  • This experiment was designed to investigate the effect of Coptis japonica Makino(CJM) on the Alzheimer's disease. The effects of CJM extract on $IL-1{\beta}$, IL-6, amyloid precursor proteins (APP), acetylcholinesterase(AChE), glial fibrillary acidic protein(GFAP) mRNA of PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$ and AChE activity of PC-12 cell lysate treated by $A{\beta}$ plus $rIL-1{\beta}$ and behavior of memory deficit rats induced by scopolamine and mice glucose, uric acid, AChE activity of memory deficit rats induced by scopolamine were investigated, respectively. The results were summarized as follows ; 1. CJM extract suppressed $IL-1{\beta}$, IL-6 mRNA in PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$ 2. CJM extract suppressed APP, AChE, GFAP mRNA in PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$ 3. CJM extract suppressed AChE activity in cell lysate of PC-12 cell treated by $A{\beta}$ plus $rIL-1{\beta}$ 4. CJM extract group showed significantly inhibitory effect on the memory deficit of mice induced by scopolamine in the experiment of Morris water maze. 5. CJM extract increased glucose, decreased uric acid and AChE significantly in the serum of the memory deficit rats induced by scopolamine. According to the above results, it is suggested that CJM extract might be usefully applied for prevention and treatment of Alzheimer's disease and memory deficit symptom.

  • PDF

Chronic dietary ginseng extract administration ameliorates antioxidant and cholinergic systems in the brains of aged mice

  • Lee, Mi Ra;Ma, Jin Yeul;Sung, Chang Keun
    • Journal of Ginseng Research
    • /
    • 제41권4호
    • /
    • pp.615-619
    • /
    • 2017
  • Background: Black ginseng has a more potent biological activity than non-steamed ginseng. We investigated the effects of long-term intake of dietary black ginseng extract (BG) on antioxidant activity in aged mice. We also compared the effects of BG on cognitive deficits with those of white ginseng extract (WG) and red ginseng extract (RG). Methods: Ten-month-old mice were fed an AIN-93G-based diet containing 10 g/kg (low dose, L) or 30 g/kg (high dose, H) WG powder, RG powder, or BG powder for 24 wk. We measured serum lipids, the activities of antioxidant enzymes, and malondialdehyde levels. Additionally, the protein expression levels of choline acetyltransferase and vesicular acetylcholine transporter, which are presynaptic cholinergic markers in the cortex and hippocampus of the brain, were measured by western blotting. Results: Triglyceride levels were reduced in all the extract-treated mice, except those in the LBG group. High-density lipoprotein cholesterol levels in the HBG group were higher than those in the control group. Total cholesterol levels were reduced in the LBG group. Additionally, glucose levels in the HBG group were significantly reduced by 41.2%. There were lower levels of malondialdehyde in the LBG group than in the control group. Furthermore, glutathione reductase activity increased in the HWG group and the HRG group. The protein expression levels of choline acetyltransferase and vesicular acetylcholine transporter significantly increased in all the ginseng-treated groups. Conclusion: The results suggest that supplementation with the tested ginseng extracts may suppress the cognitive decline associated with aging, via regulation of the cholinergic and antioxidant defense systems.