• Title/Summary/Keyword: 아세틸콜린

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Identification of the Component with Anti-acetylcholinesterase Activity from the Essential Oil of Artemisia iwayomogi (더위지기 정유로부터 아세틸콜린에스테라제 억제활성 성분의 동정)

  • Choi, Jae Sue;Song, Byong-Min;Park, Hee-Juhn
    • Korean Journal of Plant Resources
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    • v.30 no.1
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    • pp.17-21
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    • 2017
  • Since the acetylcholinesterase (AChE) inhibitor is used to treat Alzheimer's disease, the present study aimed to analyze the component with anti-AChE activity from the essential oil of Artemisia iwayomogi (Compositae). The four major components of the essential oil were identified to be camphor (29.8%), borneol (28.0%), eucalyptol (5.81%) and coumarin (5.49%) from a gas chromatography-mass spectrometry (GC-MS). The essential oil and its three components, camphor, borneol, and coumarin, were subjected to anti-AChE assay. The $IC_{50}$ values of the essential oil and coumarin were shown to be $0.298mg/m{\ell}$ and $0.236mg/m{\ell}$, though those of other two components, camphor and borneol, were more than $0.250mg/m{\ell}$. These results suggest that coumarin is an active substance of this essential oil with anti-AChE activity.

Enzymatic Spectrophotometric Determinations of Acetylcholine and Choline in the Biological Samples (생체 시료 중 아세틸콜린 및 콜린에 대한 효소-분광학적 정량분석)

  • Nam, Myung-Hwa;Lee, Sung-Ho;Kim, Ke-Tack;Hahn, Young-Hee
    • YAKHAK HOEJI
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    • v.56 no.4
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    • pp.222-229
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    • 2012
  • In order to determine acetylcholine and choline in the biological samples, the specific enzymes of acetylcholinesterase (AChE) and choline oxidase (ChO), which utilize acetylcholine and choline as substrates, were employed to convert substrates to $H_2O_2$. The produced $H_2O_2$ was coupled to 4-aminoantipyrine/phenol with peroxidase (PO) yielding quinoneimine dye which was measured at 508 nm. In the present enzymatic spectrophotometric analysis the product at the equilibrium state was measured considering accuracy, precision, time and cost of the analysis. The developed analytical method yielded good linearity (calibration curve; $A_{508}$=9534[acetylcholine]+0.009, correlation coefficient ($R^2$); 0.999) with detection limit of $1.11{\times}10^{-7}M$, reasonable precision (relative standard deviation; 0.10~1.62% at $2.5{\times}10^{-6}M{\sim}1.25{\times}10^{-4}M$) and accuracy (relative error; -0.24~0.97% at $4.13{\times}10^{-6}M{\sim}1.01{\times}10^{-4}M$) for acetylcholine chloride standard solution. The concentrations of acetylcholine and choline in human serum were found as $3.20{\times}10^{-5}M$ and $1.14{\times}10^{-4}M$, respectively. The brain tissues of Sprague-Dawley strain rat contained 9.82${\mu}g/g$ of acetylcholine and 6.53 ${\mu}g/g$ of choline in the cerebrum, while 7.37 ${\mu}g/g$ of acetylcholine and 5.34 ${\mu}g/g$ of choline in the cerebellum.

Reaction Mechanism of Acetylcholinesterase Catalyzed Hydrolysis of Thiocholine Esters (아세틸콜린에스터라제 촉매에 의한 티오에스테르의 가수분해 반응 메카니즘 연구)

  • 정대일;최순규;이용균;박유미;곽문정;신영주;최병욱;이봉호;한정태
    • Journal of Life Science
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    • v.12 no.1
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    • pp.32-42
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    • 2002
  • It was researched to react horse serum-BChE with hefanoylthiocholine chosen among choline esters. According as number of carbon of acyl group in choline esters was increased, reactivity was decreased but strength of ES complex was increased (Km=0,140mM). The pH-V/K profile for BChE-catalyzed hydrolysis of hexanoylthiocholine yields a p $K_{a}$ =4.974$\pm$0.028. This value is equal to recent literature that shows systematic shift from dependence of activity on the basic form fo a residue that huts a p $K_{a}$ =6.2~6.4 to catalysis by a residue or residues that has a p $K_{a}$ =4.7~5.0. The resulting kinetic solvent isotope effect of hexanoylthiocholine is $^{D/V}$K=1.18. The magnitude of the isotope effect suggests that proton transfer is not an element of transition-state stabilization.n.

Studies on the Biological Activity of Pleurotus ferulea (아위버섯(Pleurotus ferules) 추출물의 생리활성 탐색)

  • 홍기형;김병용;김혜경
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.33 no.5
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    • pp.791-796
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    • 2004
  • This study was peformed to screen the biological activities of Pleurotus ferulea (K5 and K8 strains). The cap of K5 strain is well developed than stalk, and vice versa in K8. The ethanol extract of Pleurotus ferulea exhibited significant free radical scavenging activity (35∼36%), suggesting possible effect on many degenerative diseases originated from the reaction of oxygen species. Acetylcholinesterase inhibitor is proven to be the most effective factor for Alzheimer disease induction, and ethanol extract of Pleurotus ferulea significantly inhibited acetylcholinesterase activity (25∼35%) in uitro. Moreover, ethanol extract of Pleurotus ferulea suppressed liver fibrosis by 3∼12% in uitro. However, Pleurotus ferulea feruled to inhibit glucose uptake in human intestinal cell line. Viability of gastric and colon cancer cells was also not affected by Pleurotus ferulea extract. In conclusion Pleurotus ferulea exhibited significant effect on free radical scavenging, acetylcholinesterase inhibiton and brain cell protection. However, Pleurotus ferulea failed to affect glucose uptake, and cytotoxicity of gastric and cancer cells. In general, K8 revealed more significant effects than K5.

Comparative Study of Bang-poong (root of Saposhnikovia divaricata Schischkin) and Related Species on Neuroprotective and Acetylcholinesterase Inhibitory Effects (방풍류(防風類) 약재(藥材)의 신경세포보호효과 및 아세틸콜린에스터라제 저해 효과 비교)

  • Ju, In Gyoung;Lee, Seungmin;Choi, Jin Gyu;Oh, Myung Sook
    • The Korea Journal of Herbology
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    • v.34 no.5
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    • pp.29-37
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    • 2019
  • Objectives : Bang-poong (Saposhnikovia divaricata; SD) was traditionally used to treat inflammatory disorders. In this study, we aimed to investigate whether Bang-poong and related species including SD, Glehnia littoralis (GL), and Peucedanum japonicum (PJ) possess neuroprotective effects and acetylcholinesterase (AChE) inhibitory activities. Methods : Roots of SD, GL and PJ were extracted with distilled water (DW) or 70% ethanol (EtOH). We assessed 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activities of the extracts. To examine neuroprotective effects, we measured cell viability in PC12 or HT22 cells after treatment of the extracts with $H_2O_2$ or amyloid-beta ($A{\beta}$). To assess anti-neuroinflammatory effects, we measured the nitric oxide (NO) levels after treatment with the extracts and lipopolysaccharide (LPS) in BV2 microglial cells. In addition, we performed AChE inhibition assay to explore effects of the extracts on the cholinergic system. Results : DW and EtOH extracts of SD, GL and PJ showed mild DPPH free radical scavenging activities. Also, DW extracts of GL and PJ showed protective effects against $H_2O_2$-induced toxicity in PC12 cells. In LPS-activated BV2 cells, EtOH extracts of SD, GL and PJ exerted inhibitory effects on NO production. Meanwhile, DW extracts of SD, GL and PJ inhibited the $A{\beta}$-induced cell death in HT22 cells. In addition, DW and EtOH extracts of GL exhibited remarkable inhibitory activities on AChE. Conclusions : We demonstrated that SD, GL and PJ exert anti-oxidative, anti-neuroinflammatory and AChE inhibitory activities. These results indicate that SD, GL and PJ could be potential candidates for neurological disorders.

The Effect of Vitis labruscana B. Leaves Ethanol Extract on the Expression of Amyloid Precursor Protein in Neuroblastoma Cells and on the Acetylcholinesterase Activity (캠벨얼리(Vitis labruscana B.) 잎 에탄올 추출물이 신경세포에서 아밀로이드 전구 단백질의 발현과 아세틸콜린에스테라제 활성에 미치는 영향)

  • Choi, Ha Yeon;Kim, Ju Eun;Ma, Sang Yong;Cho, Hyung Kwon;Kim, Dae Sung;Leem, Jae Yoon
    • Korean Journal of Pharmacognosy
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    • v.53 no.2
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    • pp.102-110
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    • 2022
  • Alzheimer's disease (AD) is the most common form of dementia, and the accumulation of β-amyloid (Aβ) in the brain triggers AD, followed by hyperphosphorylation of tau protein, neurofibrillary tangles, and synapses loss, neuronal cell death, and cognitive decline occur in a chain. In APPswe neuronal cell line, 50 ㎍/ml of Campbell early (Vitis labruscana B.) leaves 50% ethanol extract (VLL) treatment inhibited the secretion of Aβ1-42 by about 63% and the secretion of Aβ1-40 by about 50%. VLL did not target the enzymatic activity of the amyloidogenic pathway and decreased the protein expression of APP. As a result of RT-qPCR (Reverse transcription-quantitative real-time PCR) of the APPswe cell line treated with VLL, it is thought that the protein expression of APP was reduced by inhibiting the transcription process of the APP gene. In addition, VLL inhibited acetylcholinesterase (AChE) enzyme activity in vitro by 27.6% and 54.7%, respectively, at 50 and 100 ㎍/ml concentrations. We found that VLL inhibited the production of Aβ, a dementia-inducing substance, by suppressing the transcription of the APP gene, and that VLL inhibited AChE activity. We suggest that VLL has the potential as a natural drug material that modulates the alleviation of dementia symptoms.

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.

Protective effect of ethyl acetate fraction from Actinidia arguta sprout against high glucose-induced in vitro neurotoxicity (포도당으로 유도된 in vitro 뇌신경세포 독성에 대한 다래 순 아세트산에틸 분획물의 보호 효과)

  • Yoo, Seul Ki;Park, Seon Kyeong;Kim, Jong Min;Kang, Jin Yong;Park, Su Bin;Han, Hye Ju;Kim, Chul-Wo;Lee, Uk;Heo, Ho Jin
    • Korean Journal of Food Science and Technology
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    • v.50 no.5
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    • pp.517-527
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    • 2018
  • The current study investigated in vitro anti-diabetic and neuroprotective effects of the ethyl acetate fraction in Actinidia arguta sprouts (EFAS), on $H_2O_2$ and high glucose-induced cytotoxicity in human neuroblastoma MC-IXC cells. EFAS had high total phenolic and total flavonoid contents. An assessment of 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging activity of EFAS, as well as its potential for inhibiting malondialdehyde production, indicated that EFAS may possess significant antioxidant properties. EFAS exerted inhibitory effects on ${\alpha}-glucosidase$ via glycemic regulation which forms advanced glycation end products. In addition, EFAS exhibited significant acetylcholinesterase inhibitory effects. Moreover, EFAS displayed protective effects against $H_2O_2$ and high glucose-induced cell death, and inhibited the generation of reactive oxygen species in MC-IXC cells. Finally, the main physiological compound of EFAS was identified via high performance liquid chromatography as a rutin.

Nutritional composition, antioxidant capacity, and brain neuronal cell protective effect of cultivars of dried persimmon (Diospyros kaki) (품종별 곶감(Diospyros kaki)의 영양성분 분석, 산화방지 효과 및 뇌 신경세포 보호효과)

  • Kim, Jong Min;Park, Seon Kyeong;Kang, Jin Yong;Park, Sang Hyun;Park, Su Bin;Yoo, Seul Ki;Han, Hye Ju;Lee, Su-Gwang;Lee, Uk;Heo, Ho Jin
    • Korean Journal of Food Science and Technology
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    • v.50 no.2
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    • pp.225-237
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    • 2018
  • This study was conducted to compare nutritional analysis and neuroprotective effect of 5 cultivars of Diospyros kaki (Dungsi, Godongsi, Gojongsi, Gabjubaekmok, and Bansi). In nutritional analysis, three free sugars: sucrose, glucose, and fructose, and six fatty acids: tartaric acid, hexadecanoic acid, palmitic acid, oleic acid, octadecenamide, and octadecane, were detected. Potassium and phosphorus levels were the highest in inorganic component analysis, and glutamic acid and aspartic acid were the highest contents in amino acid analysis. Vitamin C was detected in all cultivars. Total phenolic content was the highest in Dungsi. Antioxidant activities such as ABTS (3-ethylbenzothiazoline-6-sulfonic acid), DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging activities, FRAP (ferric reducing/antioxidant power), and MDA (malondialdehyde) inhibitory effect were the highest in Gabjubaekmok. Acetylcholinesterase inhibitory activity, cell viability, intracellular reactive oxygen species (ROS) accumulation, and lactate dehydrogenase (LDH) release were measured to confirm the neuroprotective effect in MC-IXC cells. Gabjubaekmok showed significant acetylcholinesterase (AChE) inhibition and neuroprotection.

Memory improvement effect of Artemisia argyi H. fermented with Monascus purpureus on streptozotocin-induced diabetic mice (스트렙토조토신으로 유도된 당뇨 마우스에서 Monascus purpureus을 이용한 발효 쑥의 기억력 개선 효과)

  • Lee, Chang Jun;Lee, Du Sang;Kang, Jin Yong;Kim, Jong Min;Park, Seon Kyeong;Kang, Jeong Eun;Kwon, Bong Seok;Park, Sang Hyun;Park, Su Bin;Ha, Gi-Jeong;Heo, Ho Jin
    • Korean Journal of Food Science and Technology
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    • v.49 no.5
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    • pp.550-558
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    • 2017
  • The effect of Artemisia argyi H. under liquid-state fermentation by Monascus purpureus (AAFM) on cognitive impairments has been studied in a mice model of diabetes-associated cognitive decline induced by streptozotocin (STZ). C57BL/6 mice (9 weeks of age, male) were separated into four groups: a normal control, STZ-induced diabetic mouse group (STZ group), Artemisia argyi H. (AA) 10 group (diabetic mouse+AA 10 mg/kg/day), AAFM 10 group (diabetic mouse+AAFM 10 mg/kg/day). Administration of AA and AAFM significantly improved glucose tolerance, as shown by the intraperitoneal glucose tolerance test (IPGTT), and ameliorated cognitive deficit, as shown by the behavioral tests including passive avoidance, Morris water maze, and Y-maze tests. After behavioral tests, the cholinergic system was examined by assessment of the acetylcholine (ACh) level and acetylcholinesterase (AChE) inhibitory activity, and the antioxidant system was also assessed by measuring malondialdehyde (MDA) and superoxide dismutase (SOD) levels in the brain and liver.