• Title/Summary/Keyword: Anti-acetylcholinesterase

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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.

An Experimental Study on the Anti-inflammatory, Anti-pruritic and Anti-microbial Effects of the Three Herbal Prescription: Eunhwasagan-tang (EST), Sobokchukeo-tang (SCT), Wandae-tang (WDT) (대하(帶下) 처방 3종의 항염, 항소양, 항균 효능에 관한 실험 연구 : 은화사간탕(銀花瀉肝湯), 소복축어탕(少腹逐瘀湯), 완대탕(完帶湯))

  • Lee, Eun-Kyu;Park, Chan-Wook;Kim, Soo-Hyeon;Choi, Yoo-Jin;Park, Kyung-Mi;Yang, Seung-Jeong;Cho, Seong-Hee
    • The Journal of Korean Obstetrics and Gynecology
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    • v.32 no.3
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    • pp.32-56
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    • 2019
  • Objectives: The purpose of this study was to investigate the in vitro anti-inflammatory, anti-pruritic and antimicrobial effects of the three herbal prescription (EST, SCT, WDT), which has been traditionally used for treating leukorrhea induced by various infections in the female genital tract. Methods: In this experiment, the anti-inflammatory effects were evaluated by Nitric oxide (NO), $Interlukine-1{\beta}$ ($IL-1{\beta}$), Interlukine-2 (IL-2), Interlukine-6 (IL-6), Tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$), Prostaglandin $E_2$ ($PGE_2$), Leukotriene $B_4$ ($LTB_4$) production amount and Inducible nitric oxide synthase (iNOS), Nuclear factor kappa B ($NF-{\kappa}B$), Cyclooxygenase-2 (COX-2) gene expression levels in RAW264.7 cells. And the anti-pruritic effects were evaluated by Histamine, Acetylcholine (ACh), Acetylcholinesterase (AChE), Substance P production amount in Mast cell/9 (MC/9) and Pheochromocytoma 12 (PC12) cells. The anti-microbial effect was measured by inhibition zone diameter on Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger. Results: As a result of measuring anti-inflammatory efficacy, $IL-1{\beta}$, IL-2, IL-6, $TNF-{\alpha}$, $PGE_2$, and $LTB_4$ production amounts were significantly reduced in the EST, SCT, WDT extraction groups compared with the control group, and significantly decreased the amount of $NF-{\kappa}B$, iNOS, and COX-2 gene expression and the amount of Phospho-Inhibitor kappa B alpha ($p-I{\kappa}B-{\alpha}$)/Inhibitor kappa B alpha ($I{\kappa}B-{\alpha}$) and $NF-{\kappa}B$ p65 protein expression. In addition, As a result of measuring the anti-pruritic effect, the amounts of histamine, ACh and Substance P were significantly decreased, and AChE production was slightly decreased, but it's significance did not appear. Finally the anti-microbial effects of EST, SCT, WDT extraction groups against Pseudomonas aeruginosa, Candida albicans and Aspergillus niger was inhibited, however the growth of Escherichia coli and Staphylococcus aureus was not inhibited. Conclusions: These data suggest that EST, SCT, WDT can be used to treat patients with leukorrhea.

Nutritional Characteristics and Physiological Functionalities of Polyplant Extracts from Some Vegetables and Medicinal Plants (몇 가지 채소와 약용 식물을 이용하여 제조한 식물 복합 추출물의 영양학적 특성과 생리기능성)

  • Kim, Hyun-Kyung;Lee, Eun-Na;Geum, Jong-Wha;Lee, Jong-Soo
    • The Korean Journal of Food And Nutrition
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    • v.21 no.4
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    • pp.410-415
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    • 2008
  • The nutritional characteristics and functionalities of the polyplant extracts(PPE) from the extraction of various plants were assessed for the development of a new functional food. The PPE contained 42.95 g of glucose, 22.61 g of fructose, and 12.48 g of sucrose per 100 g of PPE as free sugar, and its reducing sugar contents was measured at 480.6 mg per g of PPE. Among free amino acids, proline contents was the highest at 0.58 g per 100 g of PPE, and it contained only 12.65 mg of malic acid and 6.92 mg of tartaric acid per g of PPE as an organic acid. The antioxidant activity of PPE was the highest at 91.6%, whereas SOD-like activity and xanthin oxidase inhibitory activity, which are associated with anti-aging effects, were 21.6% and 9.3%, respectively. HMG-CoA reductase inhibitory activity was 10.0% and anti-dementia acetylcholinesterase inhibitory activity was quite low(5.1%).

Ameliorating Effect of Taraxacum platycarpum Extract in the Scopolamine-induced Cholinergic Blockade Mouse Model (Scopolamine으로 유도된 콜린성 신경계 차단 동물모델에서 포공영(Taraxacum platycarpum) 추출물의 기억력 개선효과)

  • Kwon, Yubeen;Park, Ho Jae;Shin, Bum Young;Ryu, Jong Hoon
    • Korean Journal of Pharmacognosy
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    • v.48 no.2
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    • pp.119-124
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    • 2017
  • Taraxacum platycarpum H. Dahl. (Compositae) has been used as an anti-inflammatory or anti-cancer agent in the clinic. Although its antidepressant effect has been reported, however, its cognitive function is not investigated until yet. In the present study, we investigated whether the water extract of T. platycarpum (WETP) could improve cognitive function in cholinergic blockade-induced amnesia mouse model using the passive avoidance or Y-maze task. WETP (12.5, 25 or 50 mg/kg) significantly ameliorated the scopolamine-induced cognitive impairment both in the passive avoidance test and the Y-maze test. In addition, WETP significantly inhibited acetylcholinesterase (AChE) activity measured by an ex vivo study using the mouse whole brain. These results suggest that WETP alleviates the cognitive dysfunction caused by the cholinergic blockade, in part, via AChE inhibition, and that it may be a useful for treating cognitive dysfunction.

Cholinesterase inhibitory activities of neuroprotective fraction derived from red alga Gracilaria manilaensis

  • Pang, Jun-Rui;How, Sher-Wei;Wong, Kah-Hui;Lim, Siew-Huah;Phang, Siew-Moi;Yow, Yoon-Yen
    • Fisheries and Aquatic Sciences
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    • v.25 no.2
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    • pp.49-63
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    • 2022
  • Anti-cholinesterase (ChE)s are commonly prescribed as the symptomatic treatment of Alzheimer's disease. They are applied to prevent the breakdown of neurotransmitter acetylcholine (ACh) that bind to muscarinic and nicotinic receptors in the synaptic cleft. Seaweeds are one of the richest sources of bioactive compounds for both nutraceuticals and pharmacognosy applications. This study aimed to determine the anti-ChEs activity of Gracilaria manilaensis, one of the red seaweeds notables for its economic importance as food and raw materials for agar production. Methanol extracts (GMM) of G. manilaensis were prepared through maceration, and further purified with column chromatography into a semi-pure fraction. Ellman assay was carried out to determine the anti-acetylcholinesterase (AChE) and anti-butyrylcholinesterase (BuChE) activities of extracts and fractions. Lineweaver-Burk plot analysis was carried out to determine the inhibition kinetic of potent extract and fraction. Major compound(s) from the most potent fraction was determined by liquid chromatography-mass spectrometry (LCMS). GMM and fraction G (GMMG) showed significant inhibitory activity AChE with EC50 of 2.6 mg/mL and 2.3 mg/mL respectively. GMM and GMMG exhibit mixed-inhibition and uncompetitive inhibition respectively against AChE. GMMG possesses neuroprotective compounds such as cynerine A, graveolinine, militarinone A, eplerenone and curumenol. These findings showed a promising insight of G. manilaensis to be served as a nutraceutical for neuronal health care in the future.

Phenolic Profiles of Hardy Kiwifruits and Their Neuroprotective Effects on PC-12 and SH-SY5Y Cells against Oxidative Stress

  • Jeong, Ha-Ram;Kim, Kwan Joong;Lee, Sang Gil;Cho, Hye Sung;Cho, Youn-Sup;Kim, Dae-Ok
    • Journal of Microbiology and Biotechnology
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    • v.30 no.6
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    • pp.912-919
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    • 2020
  • Hardy kiwifruits (Actinidia arguta Planch.) have high amounts of antioxidants, including ascorbic acid (vitamin C) and phenolics. The anti-cholinesterase activity and neuroprotective effects of three different cultivars of hardy kiwifruits, cv. Mansu (A. arguta × A. deliciosa), cv. Haeyeon (A. arguta), and cv. Chiak (A. arguta), on PC-12 and SH-SY5Y cells were evaluated. Extraction of phenolics and vitamin C was carried out using 80% (v/v) aqueous ethanol and metaphosphoric acid assisted with homogenization, respectively. Hardy kiwifruit of cv. Mansu showed higher total phenolic, total flavonoid, and vitamin C contents and antioxidant capacity compared to the other two cultivars of hardy kiwifruits, cv. Haeyeon and cv. Chiak. Analysis of high-performance liquid chromatography results revealed the presence of procyanidin B2, (-)-epicatechin, neochlorogenic acid, cryptochlorogenic acid, rutin, hyperoside, isoquercitrin, and astragalin in hardy kiwifruits. The three cultivars of hardy kiwifruits had a wide range of vitamin C content of 55.2-130.0 mg/100 g fresh weight. All three cultivars of hardy kiwifruits had protective effects on neuronal PC-12 and SH-SY5Y cells exposed to hydrogen peroxide by increasing cell viability and reducing intracellular oxidative stress. Furthermore, the hardy kiwifruits inhibited acetylcholinesterase and butyrylcholinesterase. Collectively, these results suggest that hardy kiwifruits rich in antioxidants like phenolics and vitamin C have good potential as functional materials in neuroprotective applications.

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%.

Chronic Effects of Copper on Antioxidant Enzymes and Acetylcholinesterase Activities in Rock bream Oplegnathus fasciatus (구리에 노출된 돌돔(Oplegnathus fasciatus)의 항산화 효소 및 acetylcholinesterase 활성의 변화)

  • Min, EunYoung;Kang, Ju-Chan
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.47 no.6
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    • pp.874-881
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    • 2014
  • A laboratory experiment was conducted to determine chronic effects of waterborne copper exposure on rock bream Oplegnathus fasciatus using a panel of enzymes. The activities of the following biochemical biomarkers were determined at different concentrations of $CuSO_4$ for 10 and 20 days: alanine aminotransferase (ALT), aspartate aminotransferase (AST), and lactate dehydrogenase (LDH) in plasma; antioxidant enzymes including glutathione (GSH), superoxide dismutase (SOD) and glutathione peroxidase (GPx) in liver and gills; and acethylcholinesterase (AChE) in brain and muscle. After exposure to two $CuSO_4$ concentrations (200 and $400{\mu}g/L$), the activities of plasma ALT in the fish showed a tendency to increase with AST and LDH, depending on $CuSO_4$ concentration. Additionally, GSH levels and SOD activities significantly increased, depending on $CuSO_4$ concentrations in liver and gills. This involved the inactivation of reactive molecules formed during oxidative stress, which could provide protection against oxidative damage induced by $CuSO_4$. However, GPx and AChE activities significantly decreased with $CuSO_4$ in liver and gills. In conclusion, these enzymes may represent convenient biomarkers for monitoring heavy metal pollution in coastal areas. Such chronic exposure studies are necessary for improving our understanding of complementary or deleterious effects of pollutants, and for developing metal toxicity biomarkers.

Detection of Multi-class Pesticide Residues Using Surface Plasmon Resonance Based on Polyclonal Antibody

  • Yang, Gil-Mo;Kang, Suk-Won
    • Food Science and Biotechnology
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    • v.17 no.3
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    • pp.547-552
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    • 2008
  • The detection of carbamate (carbofuran, carbaryl, benfracarb, thiodicarb, and methomil) and organophosphate (diazinon, cadusafos, ethoprofos, parathion-methyl, and chlorpyrifos) pesticide residues with very low detection limits was carried out using surface plasmon resonance (SPR) based equipment. The capacity to develop a portable SPR biosensor for food safety was also investigated. The applied ligand for the immunoassays was polyclonal goat anti-rabbit immunoglobulin (IgG) peroxidase conjugate. Concentration tests using direct binding assays showed the possibility of quantitative analysis. For ligand fishing to find a proper antibody to respond to each pesticide, acetylcholinesterase (AChE), and glutathione-S-transferase (GST) were tested. The reproducibility and precision of SPR measurements were evaluated. With this approach, the limit of detection for pesticide residues was 1 ng/mL and analysis took less than 11 min. Thus, it was demonstrated that detecting multi-class pesticide residues using SPR and IgG antibodies provides enough sensitivity and speed for use in portable SPR biosensors.

Isolation of 6,6'-Bieckol from Grateloupia elliptica and its Antioxidative and Anti-Cholinesterase Activity

  • Lee, Bong Ho;Choi, Byoung Wook;Lee, Soo Young
    • Ocean and Polar Research
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    • v.39 no.1
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    • pp.45-49
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    • 2017
  • During the search for anticholinesterase compounds from marine organisms, we were able to isolate 6,6'-bieckol from a red alga, Grateloupia elliptica. This compound showed moderate acetylcholinesterase (AChE) inhibitory activity in a micromole range ($IC_{50}$ $44.5{\mu}M$). However, for butyrylcholinesterase (BuChE), a new target for the treatment of Alzheimer's disease (AD), it showed particularly potent inhibitory activity ($IC_{50}$ $27.4{\mu}M$), which is more potent compared to AChE. It also inhibits BACE-1, a new target for reducing the generation of ${\beta}-amyloid$.