• Title/Summary/Keyword: 에스테라제 활성

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Screening of Plant Extracts with Cholinesterase Inhibition Activity (콜린 에스테라제 저해효과 보유 식물 추출물 탐색)

  • Park, Saet-Byul;Lee, Jeong-Hoon;Kim, Hyung-Don;Soe, Kyung-Hae;Jeong, Hyeon-Soo;Kim, Dong-Hwi;Lee, Seung-Eun
    • Korean Journal of Plant Resources
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    • v.31 no.5
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    • pp.433-452
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    • 2018
  • This study was conducted to select candidates from plant resources for the purpose of improving or treating Alzheimer's disease, a type of dementia. One hundred and eighty-four plant extracts at a final concentration of $100{\mu}g/ml$ were screened to determine their capacity to inhibit acetylcholinesterase (AChE) by in vitro assay. From this AChE assay, seven plant extracts - including methanol ext. and water ext. of Phellaodendron amurense Rupr. (bark), methanol ext. of Nelumbo nucifera Gaertn (stamen/ovary), methanol ext. of Persicaria tinctoria H. GROSS (flower), methanol ext. of Coptis chinensis (rhizome), ethanol ext. of Cinnamomum cassia Blume(bark) and ethanol ext. of Carthamus tinctorius L. (fruit) - showed effective inhibition activity ranging from 18.7% to 63.1%. The selected extracts were testified their inhibition activities on AChE and BuChE (butyrylcholinesterase) at concentrations of 25, 50, 100, $200{\mu}g/ml$. In the AChE assay, five extracts including methanol ext. of Nelumbo nucifera Gaertn. (stamen/ovary), methanol ext. of Persicaria tinctoria H. GROSS (flower), methanol ext. of Coptis chinensis (rhizome), methanol ext. and water ext. of Phellaodendron amurense Rupr. (bark) showed inhibition activity of 15.0%~73.5%, 19.5%~63.5%, 81.6%~58.5%, 69.9%~80.5%, and 54.8%~78.3%, respectively, at concentrations of 25, 50, 100, $200{\mu}g/ml$. In the BuChE assay, the extracts of Nelumbo nucifera Gaertn. (stamen/ovary), Persicaria tinctoria H. GROSS (flower), and Coptis chinensis (rhizome) showed inhibitory capacities of 58.9~81.6%, 45.8%~72.4%, and 33.1%~55.4% at concentrations of 25, 50, 100, $200{\mu}g/ml$, respectively. In conclusion, it is suggested that Nelumbo nucifera Gaertn. (stamen/ovary), Persicaria tinctoria H. GROSS, Coptis chinensis (rhizome) and Phellaodendron amurense Rupr. (bark) could be selected as candidate materials for improving or treating Alzheimer's disease on the basis of further study.

A Possible Mechanism Related with Non-spinning Syndrome of Bombyx mori that Intimidates the Sericultural Industry in Northern Kyungbuk (경북 북부지역의 양잠산업에 피해를 주고 있는 누에(Bombyx mori) 미화용 기작에 관한 연구)

  • Kim, Yong-Kyun;Bae, Sang-Ki;Lee, Sun-Young;Ji, Dong-Jin;Kim, Jin;Hong, Yong-Pyo;Kim, Gil-Ho
    • Korean journal of applied entomology
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    • v.43 no.2
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    • pp.143-153
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    • 2004
  • Non-spinning syndrome of Bombyx mori has been serious issue in sericulture industry near Kyungbuk area. This study was focused on the analysis of the mechanism and on screening candidate chemicals inducing the anti-metamorphosis of the silkworms. Rearing temperatures or initial body weight of the final instar larvae did not affect a normal larval to pupal metamorphosis of B. mori. However, pyriproxyfen (a juvenile hormone (JH) agonist) induced follicle patency significantly even at its 10$\^$-8/ M concentration and inhibited metamorphosis of B. mori in both developmental time and dose dependent manners. Pyriproxyfen induced JH esterase (JHE) activity and downregulated expression of JH binding protein of 5. mori. These results suggests that pyriproxyfen induced JHE activity as a JH agonist and that the elevated JHE activity degraded endogenous JH and resulted in JHBP gene expression. Based on the fact that the JH agonist induced follicle patency and inhibited metamorphosis of B. mori, follicle patency bioassay suggested that three commercial pesticides including simazine, molinate or alachlor were proved to give potent JH agonistic effect on B. mori. Further direct exposure experiments to these candidates are required to determine the chemicals responsible for the non-spinning syndrome of 8. mori.

Regulation of Haemolymph Juvenile Hormone Esterase Activity in Larvae of the Silkworm, Bombyx mori (누에 유충의 혈림프 유약호르몬 에스테라제 활성의 조절에 관한 연구)

  • 손흥대;강필돈
    • Journal of Sericultural and Entomological Science
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    • v.34 no.1
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    • pp.15-20
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    • 1992
  • Effects of starvation, ligation, refeeding and methoprene treatment in the feeding phase of the fifth instar larvae of Bombyx mori on the regulation of juvenile hormone esterase(JHE) activity were investigated. Starvation and ligation contributed to the reduction of JHE activity, however, JHE levels in starved larvae were slightly higher than in legated larvae. Haemolymph JEH activity of starved larvae was increased by refeeding, and duration of increasing time of JHE activity after starvation was related to duration of starvation. When starved larvae were applied methoprene topically, JHE activity were not changed at day 0 and 1, but were increased by 1.3-1.4 times between day 2 and 5. When ligated larvae were applied methoprene topically, JHE activity was not changed at day 0, but were increased by 1.9-2.3 times between day 1 and 5. These results suggest that head factor, juvenile hormone(JH) and nutrient are major factors in the regulation of JHE in the feeding phase of the fifth instar larvae of Bombyx mori. Especially JHE might be regulated by the co-operative action of head factor and JH. However, head factor plays important role in the early stage, while JH plays important role thereafter.

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The Effects of Fruit and Vegetable Bark Extract on Learning Ability and Memory Improvement (과채류껍질 추출물의 학습능력수행 및 기억력증진에 미치는 효과)

  • Kim, Hyun Kyoung
    • The Journal of the Convergence on Culture Technology
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    • v.4 no.3
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    • pp.261-267
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    • 2018
  • In the present study, we assessed the effecs of fruit and vegetable bark resources rich in beneficial substances on the learning ability and memory improvement. It functions to inhibit the activity of acetylcholinesterase in brain tissue and improve cognitive functions in a simulation model of cognitive impairment induced by scopolamine. Hence, it can promote memory and learning ability. The formulation of the fruit and vegetable bark uses the extract of fruit and vegetable peels, which has 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, the present study is a very beneficial study in the environment-friendly aspect in association with recycling of resources as it is based on the novel efficacies of fruit and vegetable barks which have been conventionally disposed as a refuse of fruits due to their poor sensory qualities despite the content of beneficial substances.

Insecticide Resistance Mechanism in the Spiraea Aphid, Aphis citricola (van der Goot) (조팝나무진딧물의 살충제 저항성 메카니즘에 관한 연구)

  • ;;本山直樹
    • Korean journal of applied entomology
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    • v.34 no.2
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    • pp.89-94
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    • 1995
  • Resistance mechanism of organophosphorus insecticides (OPs) in the spiraea aphid, whose populations were originated from several apple orchards where various OPs were frequently sprayed, was investigated. For Wonju population to which insecticides were not sprayed, resistance ratios (BRs) for pirimicarb, phosphamidon, and demeton S-methyl re 49, 31, and 5, respectively. However, for Yesan population to which OPs were sprayed 5 times, RRs for pirimicarb, phosphamidn, and dementon were 830, 536, and 204, respectively. The esterase activities of Wonju and Yesean populations increased by 44.5 and 92.0% compare to that of Kwagju population. R/S a values (S clone Kwangju population; R clone: Iechon opulation) for acetylcholinesterase (AChE) inhibition (${I}_{50}$) by pirimicarb and phosphamidon were 299.2 and 186.0, respectively. Our results indicate that increase of esterase activity and reduction of AChE sensitivity seemed to contribute insecticide resistance of the spiraea aphid.

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Study on the Acetylcholinesterase Inhibitory Activity of Coumarin Derivatives (쿠마린 유도체의 아세틸콜린 에스테라제 저해활성 연구)

  • Nam, Seung-Ok;Yun, Yong-Don;Park, Dong-Hyun;Ryu, Jong-Hoon;Lee, Yong-Sup
    • YAKHAK HOEJI
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    • v.55 no.6
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    • pp.473-477
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    • 2011
  • Alzheimer's disease (AD), one of the most common forms of dementia, is a progressive neurodegenerative disorder symptomatically characterized by the decline in memory and cognitive abilities. To date, the successful therapeutic strategy to treat AD is to maintain the levels of acetylcholine (ACh) by inhibiting acetylcholinesterase (AChE) to lead five drugs in clinical use. In this study, several coumarin derivatives were designed based on the lead structure of scopoletin and evaluated for their AChE inhibitory activities.

Effect of Papaverine and Diphenhydramine on the Action of Cholinesterase Inhibitors (항코린에스테라제 활성에 대한 파파베린 및 디펜히드라민의 효과)

  • 박은희;금정혜;박수선
    • YAKHAK HOEJI
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    • v.35 no.5
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    • pp.438-443
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    • 1991
  • This study was designed to examine the effects of diphenhydramine and papaverine on the toxic manifestations of cholinesterase inhibitors. It was found that papaverine increase acetylcholinesterase activity in cerebral cortex of mice. Papaverine pretreatment tended to increase acetylcholinesterase activity against the actions of neostigmine and physostigmine. When diphenhydramine (20~30 mg/kg, s.c.) was treated 20 min before the administration of cholinesterase inhibitor, it significantly extended the onset latency in the signs of toxicosis which were characteristically produced by physostigmine (0.25~1.5 mg/kg, s.c.) or neostigmine (0.125~0.5 mg/kg, s.c.), and it also prevented lethality in all of the animals.

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Effects of HX106N, a Water-Soluble Botanical Formulation on Scopolamine-Induced Memory Impairment in Mice (식물성 열수 추출물 HX106N이 스코폴라민으로 유도한 생쥐 기억력 저하에 미치는 효과에 관한 연구)

  • Lee, Doo Suk;Jeong, Jae-Gyun;Kim, Sunyoung
    • The Korean Journal of Food And Nutrition
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    • v.27 no.4
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    • pp.673-677
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    • 2014
  • HX106N은 용안육, 맥문동, 단삼 및 천마 등의 4가지 식물로 구성된 추출물로서, 선행 연구에서 amyloid ${\beta}$ peptide에 의한 생쥐의 기억력 저하 및 산화 손상을 억제하는 것으로 밝혀졌다. 이 연구에서는 HX106N이 비선택적 무스카린 수용체 길항제로 잘 알려진 스코폴라민(scopolamine)으로 유도한 콜린성 건망증(cholinergic amnesia)에 어떤 영향을 미치는지를 평가하였다. ICR 생쥐에게 스코폴라민(1 mg/kg body weight, i.p.)을 주입하기 1시간 전에 HX106N(100 mg/kg body weight, p.o.)을 투여하였다. 30분 후 수행한 Y-미로 시험(Y-maze test) 및 수동 회피 시험(passive avoidance test)에서 HX106N는 스코폴라민에 의해 감소되는 자발적 변경 행동(spontaneous alternation) 및 지체시간(step-through latency)을 유의미하게 억제하여 건망증을 개선시키는 것으로 나타났다. 또한 HX106N을 투약 1시간 후 생쥐의 해마와 대뇌피질 부위의 아세틸콜린에스테라제(acetylcholinesterase; AChE)의 활성을 측정한 결과 통계적으로 유의미한 정도의 활성 감소가 관찰되었다. 이러한 결과들을 종합할 때 HX106N은 AD에서 관찰되는 콜린성신경전달 장애로 인한 기억력 저하 억제에 사용될 수 있는 가능성을 가진 것으로 판단된다.

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.

Antioxidant Activities and Acetylcholinesterase Inhibitory Activities from Seaweed Extracts (해조류의 항산화 활성 및 아세틸콜린에스테라제 저해 활성)

  • Jeon, Young-Eun;Yin, Xing-Fu;Lim, Soon-Sung;Chung, Cha-Kwon;Kang, Il-Jun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.4
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    • pp.443-449
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    • 2012
  • This study was conducted to investigate the antioxidant and acetylcholinesterase (AChE) inhibitory activities of extracts from various seaweed. The extracts of $Sargassum$ $thunbergii$ (91.3%), $Polysiphonia$ $morrowii$ (90.7%), $Ecklonia$ $cava$ (89.9%), and $Artemisia$ $fukudo$ (85.9%) showed over 80% high radical scavenging activities at the final concentration of 40 ${\mu}g$/mL. The $Artemisia$ $fukudo$ extract showed the highest inhibition activity of 30.2% on AChE at the final concentration of 10 ${\mu}g$/mL. The extract of $Porphyra$ $tenera$, $Costaria$ $costata$, $Monostroma$ $nitidum$, $Ecklonia$ $cava$, and $Agarum$ $clathratum$ against AChE at a concentration of 10 ${\mu}g$/mL exhibited inhibition of 26.6%, 25.3%, 23.4%, 21.7%, 20.4% and 19.9%, respectively. The bioautography results showed that the mixtures of structurally diverse compounds were thought to affect AChE inhibitory activity. These results suggest that extracts from seaweed with their high quality components may be effective in the prevention of Alzheimer's disease and may be used to develop various functional food products.