• 제목/요약/키워드: acetylcholinesterase inhibitory activity

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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.

Analysis of Marker Components of Fermented Opuntia ficus-indica var. saboten Stem Extracts (유산균 발효에 의한 손바닥선인장 줄기추출물의 지표물질 함량 변화 분석)

  • Shin, Dong Won;Lee, Sang Ho;Lee, Soyeon;Han, Eun Hye
    • Analytical Science and Technology
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    • v.31 no.6
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    • pp.219-224
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    • 2018
  • The fruit and stem of Opuntia ficus-indica var. aboten (OFS), a native plant of Jeju Island, are considered a safe food source. Moreover, stem extracts have been previously reported to possess a variety of biological effects (e.g. anti-inflammatory and anti-oxidant, including the ability to partially ameliorate cognitive impairment), suggesting that this plant may have utility as a functional food. The present study investigated whether fermentation by lactic acid bacteria enhances the biological effects of OFS extracts. The acetylcholinesterase (AChE) inhibitory activity of fermented or non-fermented OFS extracts was evaluated, and the content of marker components dihydrokaempferol (DHK) and quercetin-3-methyl ether (3-MeQ) was analyzed using high-performance liquid chromatography. Fermented (relative to non-fermented) OFS extracts exhibited improved AChE inhibitory activity ($IC_{50}=28.35 mg/mL$), with AChE inhibitory activity resulting from fermentation by L. plantarum ($IC_{50}=12.56mg/mL$) exceeding that resulting from fermentation by L. fermentum ($IC_{50}=17.71mg/mL$). Furthermore, fermented (relative to non-fermented) OFS extracts exhibited a 16.7 % increase in DHK content, and 3-MeQ content of OFS extracts fermented by L. plantarum and L. fermentum increased by 28.6 % and 21.4 %, respectively. Therefore, OFS stem extract AChE inhibitory activity, as well as DHK and 3-MeQ content, was enhanced by fermentation with Lactobacillus spp. This suggests that fermented OFS extracts may contribute to prevention or improvement of cognitive impairment. These data are anticipated to be useful in the development of enhanced-efficacy OFS products.

Antioxidant, Physiological Activities, and Acetylcholinesterase Inhibitory Activity of Portulaca oleracea Extracts with Different Extraction Methods (추출방법에 따른 쇠비름의 항산화, 생리활성 및 Acetylcholinesterase 저해활성)

  • Kwon, Yu-Ri;Cho, Sung-Mook;Hwang, Seung-Pil;Kwon, Gi-Man;Kim, Jae-Won;Youn, Kwang-Sup
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.43 no.3
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    • pp.389-396
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    • 2014
  • The physiological properties of 70% ethanol extracts from Portulaca oleracea with different extraction methods (reflux extraction, RE; autoclave extraction, AE; low temperature high pressure extraction, LTPE) were investigated. The freeze-dried powder yields of RE, AE, and LTPE were 33.78%, 30.80%, and 11.05%, respectively. The color values of L and b were higher in LTPE, and the chroma values were higher in AE and LTPE compared to RE. The total polyphenolics and proanthocyanidin contents in LTPE were significantly higher than in other extracts. The amount of substances related to flavonoids contents was highest in RE (4.30 mg/g), followed by AE (4.06 mg/g), and LTPE (4.00 mg/g). DPPH radical scavenging ability with a concentration of 500 mg% (w/v) were in the following order; LTPE (88.87%)> RE (83.84%)> AE (80.67%). Further, the reducing power, ABTS radical scavenging ability, and nitrite scavenging activity was observed in the same tendency as seen with the DPPH radical scavenging ability. However, the ferrous ion chelating activity of RE (85.45%) and AE (83.88%) was significantly higher than that of LTPE (75.60%). ${\alpha}$-Glucosidase inhibitory activities of RE and LTPE with a concentration of 100 mg% were significantly higher than AE. Xanthine oxidase, and acetylcholinesterase inhibitory activities of LTPE were higher than the other extracts. These results suggest that the extracts from Portulaca oleracea have the potential to act as functional materials, and components of Portulaca oleracea could be effective in the prevention of Alzheimer's disease, and may be used to develop various functional food products.

Antioxidant Property and Inhibitory Effects of an Water Extract of Hwang-Ryun-Chung-Sim-Um on the Acetylcholinesterase (황련청심음(黃連淸心飮)의 항산화 및 AChE 억제 효과에 관한 연구)

  • Yoo, Jong-Ho;Lee, Sang-Taek;Han, Yun-Seung;Kim, Geun-Woo;Koo, Byung-Soo;Kim, Hun-Il
    • Journal of Oriental Neuropsychiatry
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    • v.17 no.1
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    • pp.1-16
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    • 2006
  • Objective: An water extract of the Hwang-Ryun-Chung-Sim-Um (HRC) was assessed to determine the mechanisms of its antioxidant activity. In addition, the HRC was examined in vitro for the inhibitory effect on the acetylcholinesterse (AChE). Methods: The HRC exhibited a concentration-treatment; scavenging ${\alpha},{\alpha}-diphenyl-{\beta}-picrylhydrazyl$ (DPPH) radical, linoleic acid oxidation in a thiocyanate assay system, hydroxyl radical-induced DNA nicking. We investigated mRNA levels such as catalase activity, superoxide-dismutase and glutathione peroxidase. The water extract of HRC showed inhibitory effect on AChE activity. Result: The HRC extract showed dose-dependent free radical scavenging activity, including DPPH radicals and hydroxyl radicals, using different system. The HRC was also found to be effective in protecting plasmid DNA against the strand breakage induced by Hydroxyl radicals in Fenton's reaction mixture. Futhermore, catalase mRNA expression levels increased, but SOD1 and MnSOD was not expressed. HRC in a various concentration-dependent decreased AChE mRNA levels and inhibitory effect showed AChE. Conclusion: According to the above results, it is supposed that HRC is applicable to the Dementia-type of Alzheimer clinically.

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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.

Nutritional Characteristics and Physiological Functionality of Lipase Inhibitor-Containing Desmodium oxyphyllum DC. Extracts (지질분해효소 저해물질 함유 도둑놈의 갈고리 추출물의 영양특성 및 생리기능성)

  • Lee, Jong-Kug;Kang, Min-Gu;Lee, Jong-Soo
    • The Korean Journal of Food And Nutrition
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    • v.24 no.2
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    • pp.153-158
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    • 2011
  • This study was performed to develop new anti-obesity agents from medicinal plants for functional food industry. We prepared lipase inhibitor-containing ethanol extracts from Desmodium oxyphyllu DC. and its nutritional characteristics, stability of temperature and pH and physiological functionalities were investigated. Crude lipid content and curde protein content of ethanol extract from Desmodium oxyphyllum DC. were 26.5% and 5.7%, respectively and its asparagine content was 4,860 mg/100 g, dry basis. The ethanol extracts were also stable from pH 3.0 to pH 9.0 and below $80^{\circ}C$. The ethanol extract were showed high lipase inhibitory activity of 74.2% and acetylcholinesterase inhibitory activity of 68.4%.

Antioxidant and Anticholinesterase Potential of Two Nigerian Bitter Yams Using a Simulated Gastrointestinal Digestion Model and Conventional Extraction

  • Salawu, Sule Ola;Ajiboye, Praise Blessing;Akindahunsi, Akintunde Afolabi;Boligon, Aline Augusti
    • Preventive Nutrition and Food Science
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    • v.22 no.2
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    • pp.107-117
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    • 2017
  • The purpose of this study was to evaluate the antioxidant and anticholinesterase activities of yellow and white bitter yams from South Western Nigeria using methanolic extraction and simulated gastrointestinal digestion models. The phenolic compounds in the bitter yam varieties were evaluated by high performance liquid chromatography with a diode array detector (HPLC-DAD). The total phenolic content of the bitter yams was measured by the Folin-Ciocalteu method, reductive potential by assessing the ability of the bitter yam to reduce $FeCl_3$ solution, and the antioxidant activities were determined by the 2,2-diphenyl-1-picrylhydrazyl radical ($DPPH^{\cdot}$) scavenging activity, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation ($ABTS^{{\cdot}+}$) scavenging activity, nitric oxide radical ($NO^{\cdot}$) scavenging ability, hydroxyl radical scavenging ability, and ability to inhibit $Fe^{2+}$-induced lipid oxidation. The HPLC-DAD analysis revealed the presence of some phenolic compounds in the studied bitter yam varieties, with varying degree of quantitative changes after cooking. The antioxidant indices (total phenolic content, total flavonoid content, reducing power, $DPPH^{\cdot}$ scavenging activity, $ABTS^{{\cdot}+}$ scavenging activity, and $NO^{\cdot}$ scavenging activity) were higher in the simulated gastrointestinal digestion model compared to the methanolic extract, with the in vitro digested cooked white bitter yam ranking higher. Similarly, the in vitro digested yams had a higher inhibitory action against lipid oxidation compared to the methanolic extracts, with the cooked white bitter yam ranking high. The methanolic extracts and in vitro enzyme digests showed no acetylcholinesterase inhibitory abilities, while methanolic extracts and the in vitro enzyme digest displayed some level of butyrylcholinesterase inhibitory activities. Therefore the studied bitter yams could be considered as possible health supplements.

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
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    • v.35 no.6
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    • pp.1681-1686
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    • 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.

Boswellic Acid Improves Cognitive Function in a Rat Model Through Its Antioxidant Activity - Neuroprotective effect of Boswellic acid -

  • Ebrahimpour, Saeedeh;Fazeli, Mehdi;Mehri, Soghra;Taherianfard, Mahnaz;Hosseinzadeh, Hossein
    • Journal of Pharmacopuncture
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    • v.20 no.1
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    • pp.10-17
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    • 2017
  • Objectives: Boswellic acid (BA), a compound isolated from the gum-resin of Boswellia carterii, is a pentacyclic terpenoid that is active against many inflammatory diseases, including cancer, arthritis, chronic colitis, ulcerative colitis, Crohn's disease, and memory impairment, but the mechanism is poorly understood. This study investigated the effects of boswellic acid on spatial learning and memory impairment induced by trimethyltin (TMT) in Wistar rats. Methods: Forty male Wistar rats were randomly divided into 5 groups: Normal group, TMT-administrated rats (8.0 mg/kg, Intraperitoneally, i.p.) and TMT + BA (40, 80 and 160 mg/kg, i.p.)-administrated rats. BA was used daily for 21 days. To evaluate the cognitive improving of BA, we performed the Morris water maze test. Moreover, to investigate the neuroprotective effect of BA, we determined the acetylcholinesterase (AchE) activity, the malondialdehyde (MDA) level as a marker of lipid peroxidation, and the glutathione (GSH) content in the cerebral cortex. Results: Treatment with TMT impaired learning and memory, and treatment with BA at a dose of 160 mg/kg produced a significant improvement in learning and memory abilities in the water maze tasks. Consistent with behavioral data, the activity of AChE was significantly increased in the TMT-injected rats compared to the control group (P < 0.01) whereas all groups treated with BA presented a more significant inhibitory effect against AChE than the TMT-injected animals. In addition, TMT reduced the GSH content and increased the MDA level in the cerebral cortex as compared to the control group) P < 0.01). On the other hand, treatment with BA at 160 mg/kg slightly increased the GSH content and reduced the MDA level in comparison to the TMT-administered group (P < 0.01). Conclusion: The above results suggest that the effect of BA in improving the cognitive function may be mediated through its antioxidant activity.

Study on White Ginseng Extract Preparation for Cognition Improvement (인지능 개선 효과 증진을 위한 백삼 추출물 조제 연구)

  • Lee, Seung Eun;Kim, Geum Sook;Lee, Dae Young;Kim, Hyung Don;Lee, Jae Won;Lee, Young Sup;Park, Chun Geun;Ahn, Young Sup
    • Korean Journal of Medicinal Crop Science
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    • v.24 no.5
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    • pp.375-385
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    • 2016
  • Background: The study was conducted to elucidate the extraction conditions under which white ginseng has cognition-improving efficacy. Methods and Results: Extracts from white ginseng under different solvent and temperature conditions were analyzed for ginsenoside content and inhibitory effect on N-methyl-D-aspartate (NMDA) receptor and acetylcholinesterase. The total ginsenoside contents and amounts of ginsenoside Rb1 plus ginsenoside Rg1 from the 1st extracts (prepared with EtOH/$H_2O$ as solvent) were higher than those from the 2nd extracts (extracted with $H_2O$ after the 1st EtOH/$H_2O$ extraction). The contents in the 1st and 2nd extracts produced at $80^{\circ}C$ were also higher than those obtained at $50^{\circ}C$. Samples from the 1st extraction at $80^{\circ}C$ indicated higher inhibitory activities on NMDA receptors-whose excessive activation is thought to mediate the calcium-dependent neurotoxicity associated with several neurodegenerative diseases-than those from the 2nd extraction. Among the samples prepared at varying temperatures, the extract prepared at $50^{\circ}C$ showed the highest suppression activity on NMDA receptors. Note, however, that the extracts from the 2nd extraction at $50^{\circ}C$ inhibited acetylcholinesterase-whose inhibition could be a therapeutic strategy for neurodegenerative diseases with cognitive deficits and memory malfunction-more effectively than those from the 1st extraction. Conclusions: To enhance the cognition-improving activity of white ginseng extract, it is suggested that the extracts be utilized after being combined the 1st extracts (made with EtOH/$H_2O$ solvent) and the 2nd extracts (prepared with $H_2O$) at low temperature.