• Title/Summary/Keyword: acetylcholinesterase inhibitory activity

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In vitro screening of the acetylcholinesterase inhibition, antioxidant activity, and neuronal cell protective effect of medicinal plant extracts (생약추출물의 acetylcholinesterase 저해, 항산화 및 신경세포보호 효과 in vitro 탐색)

  • Um, Min Young;Ha, Tae Youl;Seong, Ki Seung;Kim, Yong Sik
    • Food Science and Preservation
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    • v.20 no.6
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    • pp.840-845
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    • 2013
  • This study investigated the effects (i.e., the acetylcholinesterase activity, lipid peroxidation, and neuronal survival) of 20 kinds of medicinal water extracts. The water extracts of three medicinal plants - Cornus officinalis, Glycyrrhiza glabra, and Angelica gigas - were found to be the most effective on acetylcholinesterase inhibitory activity. In the lipid peroxidation-generating system induced by $H_2O_2/FeSO_4$ in rat brain homogenates, Perilla frutescens, Polygonum multiflorum, Cinnamomun cassia, and G. glabra exhibited protective activity against lipid peroxidation. The neuronal cell death induced by L-glutamate in PC12 was suppressed by the water extracts of G. glabra, Cinnamomun cassia, Platycodon grandiflorum, and Mentha arvensis at the concentration of $100{\mu}g/mL$. Taken together, these results showed that the water extract of G. glabra has the potential anti-dementia activity, which suggests that it might provide an effective strategy for improving dementia.

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.

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

  • Lee, Ji-Young;Cha, Mi-Ran;Choi, Chun-Whan;Kim, Young-Sup;Lee, Bong-Ho;Ryu, Shi-Yong
    • Korean Journal of Pharmacognosy
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    • v.43 no.2
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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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    • v.37 no.3
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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.

The Assessment of Toxicity on organic Sludge Using Acetylcholinesterase, Cytochrome P450, and Hsp70 Extracted from Earthworm (Eisenia fetida) (지렁이에서 추출한 Acetylcholinesterase, Cytochrome P450, and Heat Shock protein 70을 이용한 유기성슬러지 독성 평가)

  • Na, Young-Eun;Bang, Hae-Son;Kim, Myung-Hyun;Kim, Min-Kyoung;Roh, Kee-An;Lee, Jung-Taek;Ahn, Young-Joon;Yoon, Seong-Tak
    • Korean Journal of Soil Science and Fertilizer
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    • v.40 no.4
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    • pp.274-279
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    • 2007
  • The toxicitiy of organic sludge such as municipal sewage sludge (MSS), industrial sewage sludge (ISS), alcohol fermentation processing sludge (AFPS) and leather processing sludge (LPS) were evaluated with three environmental biomarkers as acetylcholinesterase, cytochrome P450, and heat shock protein 70 extracted from earthworm (Eisenia fetida). Their toxicities were compared with those of pig manure compost (PMC). MSS, ISS, LPS, and AFPS did not significantly affect the acetylcolinesterase activity, whereas only the elutriate of PMC slightly was increased the activity. MSS, AFPS, and PMC tended to slightly inhibit the cytochrome $P_{450}$ activity, but ISS and LPS showed significantly the inhibitory effect on cytochrome $P_{450}$. The hsp70 expression began to increase after treatments and showed high induction at 6 hour, followed by zero level at around 12 hour. The quantity of the hsp70 expressed by elutriate treatments of PMC, AFPS, MSS, ISS, and LPS was 1.9, 3.0, 3.3, 4.4, and 4.7 fold higher than that of distilled water. These results indicate that in toxicity tests of five organic waste materials, four kinds of sludge materials appeared more toxic than PMC. Results of AChE, P450, and hsp70 of earthworm might be useful for expecting or assessing an effect by exposure of organic wastes to earthworms in soil.

Comparative Study of Korean White, Red, and Black Ginseng Extract on Cholinesterase Inhibitory Activity and Cholinergic Function

  • Lee, Mi-Ra;Yun, Beom-Sik;In, Oh-Hyun;Sung, Chang-Keun
    • Journal of Ginseng Research
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    • v.35 no.4
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    • pp.421-428
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    • 2011
  • This study evaluated cholineresterase inhibitory activity of Korean white ginseng extract (WGE), red ginseng extract (RGE), and black ginseng extract (BGE) and the cholinergic effect on scopolamine (SCOP)-induced amnesic mice. WGE, RGE, and BGE inhibited acetylcholineserase (AChE), as well as butyrylcholineserase (BuChE) in a concentration-dependent manner. BGE presented strong inhibition of AChE with an $IC_{50}$ value of 1.72 mg/mL, followed by WGE (5.89 mg/mL), RGE (6.30 mg/mL), respectively. The inhibitory activity of the three ginseng extracts on BuChE showed similar values among the groups. To better understand the mechanisms of the possible effect of ginseng extract on the cholinergic function, this study assessed the expression of the cholinergic markers of choline acetyltransferase (ChAT) and AChE using western blot and RT-PCR analysis in the brains of amnesic mice. Treatment with ginseng extracts led to inhibition of AChE expression and, the activation of ChAT expression in the hippocampus and the cerebral cortex of amnesic mice as induced by SCOP. The results suggest that ginseng extracts including BGE, appear to modulate the metabolism of acetylchoine (ACh), which would greatly increase synaptic ACh levels and most potently revert SCOP-induced amnesia.

Inhibitory Effects of Extract of Rosae Rugosae Flos on the Acetylcholinesterase, β-secretase, and β-amyloid Aggregation (매괴화(玫瑰花) 추출물의 아세틸콜린에스테라제, 베타 시크리타제 및 베타 아밀로이드 응집에 대한 저해효과)

  • Kim, Hyo Shin;Kim, Ju Eun;Leem, Jae-Yoon
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.30 no.1
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    • pp.33-39
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    • 2016
  • Alzheimer's disease(AD), one of the most common forms of dementia, is characterized pathologically by the presence of intracellular neurofibrillary tangles and deposition of β-amyloid(Aβ) peptides of 40-42 residues. Aβ has been believed to be neurotoxic and now is also considered to have a role on the mechanism of memory dysfunction. Only a few acetylcholinesterase(AChE) inhibitors have been developed for treatment of AD, although the numbers of patients are rapidly increasing within aging society. Here, we show that ethanol extract of Rosae Rugosae Flos(RR) or its butanol fraction reduce the enzyme activity of AChE and BACE1(β-site APP cleaving enzyme 1). Furthermore, We found that RR inhibits Aβ aggregation and removes Aβ aggregates by Transmission electron microscopy(TEM). In addition, RR reduces the free radical of 2, 2-diphenyl-1-picrylhydrazyl(DPPH). We suggest that Rosae Rugosae Flos may be useful as a herbal medicine to treat AD.

Acetycholinesterase Inhibiting Effect and Free Radical Scavenging Effect of Soybean(Glycine max) and Yak-Kong(Rhynchosia nolubilis) (대두와 약콩의 Acetylcholinesterase 활성 억제효과와 항산화 효과)

  • 강순아;한진아
    • Journal of the East Asian Society of Dietary Life
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    • v.14 no.1
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    • pp.64-69
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    • 2004
  • The deficiency of the neurotransmitter acetylcholine(ACh) is responsible for the initiation of Alzheimer's disease. In addition, there is a simple evidence that oxidative stress significantly increases in persons with Parkinson's disease compared to age-matched healthy persons. Therefore, the objective of the study was to investigate the neurodegeneration inhibitory effect of soybean(Glycine Max) and Yak-Kong(Rhynchosia Nolubilis) by measuring the degree of inhibiting Acetylcholinesterase (AChE) catabolizing the ACh and the free radical scavenger effect in vitro. AChE was measured by the minor modified Ellman assay. Free radical scavenging activity was measured using l-diphenyl-2-picrylhydrazyl (DPPH). First, the MeOH extracts of Soybean and Yak-Kong showed the AChE inhibiting activity of 62.0$\pm$2.43% and 65.0$\pm$3.29% at the 5 mg/$m\ell$ concentration. The 50% inhibitory concentration ($IC_{50}$/) of AChE was 1.96 and 1.31 mg/$m\ell$ in the MeOH extracts of soybean and Yak-Kong. Second, the MeOH extracts of soybean and Yak-Kong showed the free radical scavenger activity of 23.1$\pm$4.26% and 80.7$\pm$4.61% at the 5 mg/$m\ell$. IC50 of free radical scavenger activity in Soybean and Yak-Kong was 13.00 and 1.41 mg/$m\ell$ in MeOH extracts and was 5.95 and 2.74 mg/$m\ell$ in hot-water extracts, respectively. In this study, the extracts of Soybean and Yak-Kong showed powerful effects in the AChE inhibition and free radical scavenging. The extracts of Soybean and Yak-Kong were expected to prevent the many neurodegenerative diseases.

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Cholinesterase-inhibitory Farnesylacetone Derivatives from the Brown Alga Sargassum sagamianum

  • Park, Soo-Hee;Hwang, Jeong-Won;Lee, Bong-Ho;Choi, Byoung-Wook;Ryu, Geon-Seek
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.206.2-206.2
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    • 2003
  • In continuing search for bioactive compounds from Korean marine algae, we found cholinesterase-inhibitory activity in the methanolic extract of brown alga Sargassum sagamianum. After partitioning between CHCl$_3$ and 30% MeOH, the former layer was purified by a series of ODS flash, silica column, gel-filtration on Sephadex LH-20, and HPLC to give two farnesylacetone derivatives. Their structures were identified by comparison with the literature data. Compounds 1 and 2 showed moderate acetylcholinesterase and butyrylcholinesterase inhibitory activities with IC$\sub$50/ values of 65.0∼48.0 ${\mu}$M and 34.0∼23.0 ${\mu}$M, respectively. (omitted)

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Screening of Natural Plant Resources with Acetylcholinesterase Inhibition and Antioxidant Activity (천연 식물자원으로부터 Acetylcholinesterase 저해 및 항산화 활성 탐색)

  • Kim, Dae-Ik;Lee, Sung-Hyeon;Hur, Eun-Young;Cho, Soo-Muk;Park, Hong-Ju
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.34 no.3
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    • pp.427-432
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    • 2005
  • This study was performed to investigate the effect of natural plant extracts on acetylcholinesterase (AChE) activity and the free radical scavenging activity. The methanolic extracts of plants were tested for AChE inhibitory activity using Ellman's colorimetric method in 96-welled microplates and antioxidant activity as the scavenging effect of 1, 1-diphenyl-2-picryl hydrazyl radical (DPPH). The results showed that AChE activities were inhibited (about 20-30%) in whole plant extract of Daucus carota var. sativa, Hypericum erectum and Fragaria yezoensis. AChE activities were inhibited (about 32-34%) in stems extract of Gingko biloba and leaves extract of Rhododendrondron yedoensa var. poukhanense. Fruit extract of Zanthoxylum schinifolium inhibited (about 18%) AChE activity. And the DPPH scavenging effects as antioxidant activity were similar to L-ascorbic acid in whole plant extract of Fragaria yezoensis and fruits extract of Comus officinalis.