• 제목/요약/키워드: Acetylcholinesterase activity

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파밤나방(Spodoptera exigua (Hubner))의 살충제 감수성 변이-에스테라제와 아세틸콜린에스테라제 활력 (Variation in Insecticide Susceptibilities of the Beet Armyworm, Spodoptera exigua (Hubner): Esterase and Acetylcholinesterase Activities)

  • 김용균;이준익;강성영;한상찬
    • 한국응용곤충학회지
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    • 제36권2호
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    • pp.172-178
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    • 1997
  • 파밤나방(Spodoptera exigua (Hubner))은 야외집단과 실내집단들간에 살충제 감수성에서 큰 변이를 보였다. 조사된 모든 약제에서 야외집단은 비선발 실내집단보다 높은 약제 저항능력을 보였다. 약제 선발된 실내집단은 선발 약제에 대해 저항능력을 높게 발현시켰다. 이러한 약제 저항능력의 변이가 아세틸콜린에스테라제와 에스테라제 활력 변이와 비교 분석되었다. 약제 저항능력이 높은 집단일수록 아세틸콜린에스테라제 활력이 낮아지고 에스테라제활력은 높아졌다. 아세틸콜린에스테라제의 Km(Michaelis-Menten constant)값은 약제저항능력이 높은 집단일수록 증가하는 것으로 기질에 대한 이 효소의 친화도가 낮아졌다. 이 효소의 효소활력 변이는 같은 집단일수록 증가하는 것으로 기질에 대한 이 효소의 친화도가 낮아졌다. 이 효소의 효소활력 변이는 같은 집단 내에서 발육단계에 따라 차이를 나타내어 2, 3, 4령충보다는 5령충에서 특히 Km값이 증가하였다. 파밤나방의 에스테라제는 6.5% 비변성조건의 겔에서 21개 밴드를 보였다. 이중 E2, E7, E8, E11, E16, E7 밴드들은 약제저항능력이 높은 집단일수록 발현 빈도수가 높았다. 이상의 결과는 파밤나방의 살충제 감수성변이에 해독효소활력증가와 작용점변환이 포함됨을 나타낸다.

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Synthesis and in vitro Assay of New Triazole Linked Decursinol Derivatives Showing Inhibitory Activity against Cholinesterase for Alzheimer’s Disease Therapeutics

  • Park, Jung-Youl;Shin, Sujeong;Park, Kyoung Chan;Jeong, Eunju;Park, Jeong Ho
    • 대한화학회지
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    • 제60권2호
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    • pp.125-130
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    • 2016
  • With the goal of developing Alzheimer’s disease therapeutics, we have designed and synthesized new triazole linked decursinol derivatives having potency inhibitory activities against cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)]. Since inhibition of cholinesterase (ChE) is still considered to be one of the most effective targets to treat AD patients, many new classes of ChE inhibitors have been synthesized. In an effort of identifying new type of cholinergic drug, decursinol derivatives 11-17 have been synthesized between decursinol and other biological interesting compounds such as lipoic acid, polyphenols, etc by using the click reaction and then evaluated their biological activities. Compound 12 (IC50 = 5.89 ± 0.31 mM against BuChE) showed more effective inhibitory activity against BuChE than galantamine (IC50 = 9.4 ± 2.5 mM). Decursinol derivatives can be considered a new class inhibitor for BuChE and can be applied to be a novel drug candidate to treat AD patients.

비타민 E와 비타민 C 첨가가 Scopolamine에 의한 인지능력 감퇴에 미치는 영향 (Effects of Vitamin E and Vitamin C Supplementation on the Decrease in Cognitive Function Induced by Scopolamin)

  • 안향숙
    • Journal of Nutrition and Health
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    • 제32권3호
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    • pp.239-247
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    • 1999
  • With the increasing elderly population in Korea, dementia has become a mojor health problem in Korea. Several studies have been conducted on the association between dementia and dietary intake, especially vitamin E and vitamin C. The purpose of this study was to investigate the effect of vitamin E and vitamin C supplementation on the decrease in cognitive function induced by scopolamine(300mg/kg) in rats. Rats were divided into three groups : control, vitamin C, and vitamin E supplementation(2.4g Vit C or Vit E /100g diet) and fed the diets for 6 weeks. There were significant decreases in active avoidance response and brain acetylcholinesterase activity in the control group, but no significant differences were observed in the vitamin E and C groups after scopolamine treatment. Brain dopamine concentration of vitamin E and C groups was significantly higher than those of control group after scopolamine injection. The concentrations of brain norepinephrine also showed similar tendence, even though it was not statistically significant. These results indicate that vitamin E and vitamin C may protect against the cognitive function decrease induced by scopolamine. However, it is still unclear how vitamin E and C influence brain neurotransmitters and improve cognitive function. Further study is need to elucidate the role of vitamin E and C supplementation in the prevention of dementia.

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해양오염의 진단을 위한 생화학적 오염지표에 관한 연구 XI. 남해산 홍합 (Mytilus coruscus)의 콜린에스테라아제의 변화 (Study on Biochemical Pollutant Markers for Diagnosis of Marine Pollution XI. Changes in Cholinesterase Activity of the Mussel (Mytilus coruscus) in the South Sea)

  • 최진호;김대익;박수현;김동우;박청길;양동범
    • 생명과학회지
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    • 제9권3호
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    • pp.282-288
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    • 1999
  • This study was designed as a part of efforts to investigate the biochemical pollutant markers for diagnosis of marine pollutions by changes in cholinesterase activity of the mussel (Mytilus coruscus) in South Sea of Korea. Acetylcholinesterase (AChE) activities in muscle of cultured mussels in South Sea were remarkably lower (20∼41%, respectively) than those of wild mussel in Pohang(control) of East Sea. Acetylcholine (Ach) activities in muscle of cultured mussels in South Sea were remarkably lower (15∼30%, respectively) than those of wild mussel in Pohang of East Sea. Monoamineoxidase (MAO-B) activities in muscle of cultured mussels in South Sea were significantly 2∼19% higher than those of wild mussel in Pohang of East Sea. It suggests that AChE, ACh and MAO-B activities in muscle of cultured mussels of South Sea may be used as the most effective mean in a biochemical markers for early warning of environmental damages caused by organophosphorus pesticides.

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오수유의 Cholinesterase 저해활성 성분 (Cholinesterase Inhibitors Isolated from the Fruits Extract of Evodia officinalis)

  • 이지영;차미란;최춘환;김영섭;이봉호;유시용
    • 생약학회지
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    • 제43권2호
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    • pp.122-126
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    • 2012
  • The MeOH extract of Evodiae Fructus exhibited a significant inhibition on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), in a dose dependent manner, respectively. The extensive bioactivity-guided fractionation process with the MeOH extract finally isolated four compounds, as rutaecarpine (1), evodiamine (2), limonin (3) and dehydroevodiamine (4). Among them, compound 2 exhibited specific inhibitory activity on BChE with the $IC_{50}$ values 1.7 ${\mu}g/ml$, whereas compound 4 showed the potent inhibition upon both AChE and BChE.

Nutritional and Physicochemical Characteristics of the Antidementia Acetylcho-linesterase-Inhibiting Methanol Extracts from Umbilicaria esculenta

  • Lee, Ji-Su;Min, Gyung-Hun;Lee, Jong-Soo
    • Mycobiology
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    • 제37권3호
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    • pp.203-206
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    • 2009
  • To develop new antidementia nutraceuticals, a potent acetylcholinesterase (AChE)-inhibiting extract was screened from various extracts of nutritional mushrooms and lichens nutritional and its physicochemical properties were investigated. Among the several extracts tested, methanol extracts of Umbilicaria esculenta fruiting body showed the highest AChE inhibitory activity of 22.4%. U. esculenta AChE inhibitor was maximally extracted when fruiting bodies were treated with 80% methanol at $40^{\circ}C$ for 18 h. The methanol extracts contained 18.9% crude lipid, 18.8% crude protein, and 11.6% total sugar. In addition, they contained 444 mg/g glutamic acid, 44 mg/g histidine, and 41 mg/g aspartic acid. The methanol extracts were soluble in a solution of methanol and 20% dimethylsulfoxide, insoluble in n-hexane, chloroform, and water, and were stable at $20{\sim}60^{\circ}C$ and pH $1.0{\sim}5.0$ for 1 h.

Development of Fruit and Vegetable Peels Extracts for Memory Improvement of Prevention and Treatment of Cognitive Impairment

  • Kim, Hyun-Kyoung
    • International journal of advanced smart convergence
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    • 제7권3호
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    • pp.1-7
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    • 2018
  • This study relates to a composition for improvement of memory or prevention and treatment of cognitive impairment using waste resources rich in beneficial substances. This study makes good effects to inhibit the activity of acetylcholinesterase in brain tissue and to improve the cognitive functions in a simulation model of cognitive impairment induced by scopolamine, so it can be available in the promotion of memory and the prevention and treatment of cognitive impairment. The composition uses the extract of fruit peels, which have long been used without causing toxicity in a wide range of food applications; therefore, it can be used safely without a risk of side effects, even in the case of a long-term administration for the preventive purpose. Furthermore, this research is a very beneficial invention in the environment-friendly aspect in association with the recycling of resources, as it is based on the novel efficacies of fruit peels, which have been conventionally disposed as a refuse of fruits due to their poor sensory qualities despite the content of beneficial substances.

Effect of Black Ginseng on Memory Improvement in the Amnesic Mice Induced by Scopolamine

  • Lee, Mi-Ra;Yun, Beom-Sik;Liu, Lei;Zhang, Dong-Liang;Wang, Zhen;Wang, Chun-Ling;Gu, Li-Juan;Wang, Chun-Yan;Mo, Eun-Kyung;Sung, Chang-Keun
    • Journal of Ginseng Research
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    • 제34권1호
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    • pp.51-58
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    • 2010
  • This study compared the effects of black, white, and red ginseng extracts (WGE, RGE, BGE, 200 mg/kg, p.o.) on learning and memory deficits associated with scopolamine treatment (SCOP, 2 mg/kg, i.p.). Tacrine (THA, 10 mg/kg, p.o.) was used as a positive control. Ginseng significantly reversed SCOP-induced memory impairment in the passiveavoidance test and also reduced escape latency in training trials of the Morris water maze test. The increased acetylcholinesterase (AChE) activity produced by SCOP was significantly inhibited by WGE and RGE (p<0.001). SCOP administration had no effect on choline acetyltransferase (ChAT) activity, but RGE and BGE significantly increased ChAT activity (p<0.05). SCOP administration increased oxidative damage in the brain. Treatment of amnesic mice with ginseng extracts decreased malondialdehyde (MDA) levels and restored superoxide dismutase (SOD) and catalase (CAT) activity to control levels. These results suggest that black ginseng enhances cognitive activity by regulation of cholinergic enzymes and antioxidant systems.