• Title/Summary/Keyword: acetylcholinesterase inhibitory activity

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Effect of Phorate, an Organophosphorus Insecticide on the Activity of Acetylcholinesterase (유기인계(有機燐系) 살충제 Phorate 가 Acetylcholinesterase 활성(活性)에 미치는 영향(影響))

  • Jung-Ho, Kim;Hong, Jong-Uck
    • Korean Journal of Environmental Agriculture
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    • v.6 no.2
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    • pp.77-83
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    • 1987
  • Present study was carried out to elucidate the effect of phorate (0,0-dietyl S-ethylthiomethyl phosphorodithioate), an organophosphorus insecticide on the acetylcholinesterase(AChE) and cholinesterase(ChE) activity in the chicken brain and plasma. The inhibitory effect of phorate and its metabolites on AChE and ChE activity was also increased in the order of phorate (p=S,S)$(p=S,SO_2)<phoratoxon$ (p=O,S)$(P=O,SO_2)$. Acute oral $LD_{50}$ of phorate was 1.02mg/kg. After oral administration of phorate, the activity of plasma ChE was inhibited more rapidly then that of brain AChE, whereas recovery of plasma ChE activity was more rapid than that of brain AChE activity.

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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%).

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 ${\beta}-amyloid$.

Development of Cholinesterase Inhibitors Using (a)-Lipoic Acid-benzyl Piperazine Hybrid Molecules

  • Kim, Beom-Cheol;Lee, Seung-Hwan;Jang, Mi;Shon, Min Young;Park, Jeong Ho
    • Bulletin of the Korean Chemical Society
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    • v.34 no.11
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    • pp.3322-3326
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    • 2013
  • A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and benzyl piperazines were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibitory activities were evaluated. Even though the parent compounds did not show any inhibitory activity against cholinesterase (ChE), all hybrid molecules showed BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, ALA-1-(3-methylbenzyl)piperazine (15) was shown to be an effective inhibitor of both BuChE ($IC_{50}=2.3{\pm}0.7{\mu}M$) and AChE ($IC_{50}=30.31{\pm}0.64{\mu}M$). An inhibition kinetic study using compound 15 indicated a mixed inhibition type. Its binding affinity ($K_i$) value to BuChE is $2.91{\pm}0.15{\mu}M$.

Evaluation of Antioxidant, Anti-cholinesterase, and Anti-inflammatory Effects of Culinary Mushroom Pleurotus pulmonarius

  • Nguyen, Trung Kien;Im, Kyung Hoan;Choi, Jaehyuk;Shin, Pyung Gyun;Lee, Tae Soo
    • Mycobiology
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    • v.44 no.4
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    • pp.291-301
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    • 2016
  • Culinary mushroom Pleurotus pulmonarius has been popular in Asian countries. In this study, the anti-oxidant, cholinesterase, and inflammation inhibitory activities of methanol extract (ME) of fruiting bodies of P. pulmonarius were evaluted. The 1,1-diphenyl-2-picryl-hydrazy free radical scavenging activity of ME at 2.0 mg/mL was comparable to that of butylated hydroxytoluene, the standard reference. The ME exhibited significantly higher hydroxyl radical scavenging activity than butylated hydroxytoluene. ME showed slightly lower but moderate inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase than galantamine, a standard AChE inhibitor. It also exhibited protective effect against cytotoxicity to PC-12 cells induced by glutamate ($10{\sim}100{\mu}g/mL$), inhibitory effect on nitric oxide (NO) production and inducible nitric oxide synthase protein expression in lipopolysaccharide-stimulated RAW 264.7 macrophages, and carrageenan-induced paw edema in a rat model. High-performance liquid chromatography analysis revealed the ME of P. pulmonarius contained at least 10 phenolic compounds and some of them were identified by the comparison with known standard phenolics. Taken together, our results demonstrate that fruiting bodies of P. pulmonarius possess antioxidant, anti-cholinesterase, and inflammation inhibitory activities.

Anti-aging and Anti-dementia Activities of Different Solvent Extracts from Silvetia siliquosa (뜸부기(Silvetia siliquosa) 추출물의 항노화 및 항치매 활성)

  • Ji-Won Choi;Yeon-Ji Lee;Won-Suk Kim;Soo-Kyung Moon;Yong-Tae Kim
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.56 no.4
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    • pp.526-531
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    • 2023
  • This study investigated the ingredients, anti-aging and anti-dementia activities of the Korean marine algae Silvetia siliquosa. The S. siliquosa solvent extracts were prepared with 70% ethanol, 80% methanol, and distilled water. The extraction yield range of various solvent extracts was 15.82-49.98%. The ethanol and methanol extracts had higher tyrosinase and collagenase inhibitory activities than those of the water extract. Meanwhile, all extracts exhibited high elastase inhibitory activity. Conversely, the methanol and water extracts exhibited the highest acetylcholinesterase inhibitory activity (IC50, 0.40 mg/mL) and β-secretase inhibitory activity (IC50, 0.81 ㎍/mL), respectively. These results indicate that S. siliquosa may be useful in food and pharmaceutical materials as a cosmetic and functional.

Antioxidant and Acetylcholinesterase Inhibitory Effect of Aged Raw Garlic Extracts (생마늘 추출 숙성물의 항산화 및 아세틸콜린에스터라아제 저해 효과)

  • Jeong, Hee-Rok;Jeong, Ji-Hee;Jo, Yu-Na;Shin, Jung-Hye;Kang, Min-Jung;Sung, Nak-Ju;Heo, Ho-Jin
    • Journal of agriculture & life science
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    • v.45 no.4
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    • pp.113-120
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    • 2011
  • In vitro antioxidant activities and acetylcholinesterase (AChE) inhibitory effects of solvent fractions from aged raw garlic extracts were investigated. Total phenolics fractioned by hexane, chloroform, ethyl acetate and water from Aged raw garlic extracts were 3.70, 23.63, 31.27 and 2.35 mg/g, respectively. We found that ethyl acetate fractions had the highest in ABTS radical scavenging activities, ferric reducing antioxidant power and inhibitory effect on auto-oxidation of linoleic acid. Intracellular ROS accumulation resulting from $H_2O_2$ treatment of PC12 cells was significantly reduced when ethyl acetate fractions were present in the medium compared to PC12 cells treated with $H_2O_2$ only. In addition, we found that ethyl acetate fractions from aged raw garlic extracts resulted in a dose-dependent manner on AChE inhibition. Consequently, our results suggest that ethyl acetate fractions from aged raw garlic extracts may be useful as decreasing agents of oxidative stress and AChE inhibitors.

Antioxidant and Cholinesterase Inhibitory Activities of Antarctic Krill Eupausia superba

  • Yoon, Na-Young;Xie, Chengliang;Shim, Kil-Bo;Kim, Yeon-Kye;Lee, Doo-Seog;Yoon, Ho-Dong
    • Fisheries and Aquatic Sciences
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    • v.14 no.4
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    • pp.289-293
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    • 2011
  • The antioxidant and cholinesterase inhibitory activities of methanol, pretanol, and acetone extracts of Eupausia superba were investigated and their bioactivities compared. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis[3-ethylbenzthiazoline-6-sulfonic acid] ($ABTS^+$) radical-scavenging activities and reducing power assays were used to determine antioxidant activities, and Ellman's colorimetric methods were applied to evaluate cholinesterase inhibitory activity. Although all extracts were positive, Acetone extract of E. superba showed the highest activities. However, these showed moderate or no inhibitory activity against butyrylcholinesterase. Moreover, the total carotenoid contents of the organic solvent extracts followed the same order as their antioxidant and acetylcholinesterase inhibitory activities. These results suggest that E. superba is a potential source of natural antioxidants and cholinesterase inhibitors.

Development and Validation of an HPLC-PDA Method for Quantitation of Ten Marker Compounds from Eclipta prostrata (L.) and Evaluation of Their Protein Tyrosine Phosphatase 1B, α-Glucosidase, and Acetylcholinesterase Inhibitory Activities

  • Nguyen, Duc Hung;Le, Duc Dat;Ma, Eun Sook;Min, Byung Sun;Woo, Mi Hee
    • Natural Product Sciences
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    • v.26 no.4
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    • pp.326-333
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    • 2020
  • The aerial parts of Eclipta prostrata is used as a traditional medicine and vegetable. In traditional folk medicine, it is used for treatment of hemorrhages, hepatic, disease, renal injuries, hair loss, tooth mobility, and viper bites. In this study, ten compounds (1 - 10) were isolated from the aerial parts of E. prostrata. A reliable high performance liquid chromatography equipped with photometric diode array detector (HPLC-PDA) method was developed to simultaneously quantitate 10 marker compounds [chlorogenic acid (1), paratensein 7-O-��-ᴅ-glucoside (2), quercetin 7-O-��-ᴅ-glucoside (3), luteolin 7-O-��-ᴅ-glucoside (4), apigenin 7-O-��-ᴅ-glucoside (5), apigenin 4'-O-��-ᴅ-glucoside (6), apigenin (7), luteolin (8), wedelolactone (9), and paratensein (10)]. In addition, compounds 5 and 6 showed considerable inhibitory effects against protein-tyrosine phosphatase 1B (PTP1B) enzyme. Moreover, compounds 6 - 8, and 10 exhibited potent α-glucosidase inhibitory effects with IC50 values of 24.5 ± 1.9, 33.0 ± 0.5, 45.5 ± 0.1, and 23.8 ± 1.0 µM, respectively. All compounds (1 - 10) showed considerable acetylcholinesterase (AChE) inhibitory effects with IC50 ranging from 30.1 to 75.2 µM.

Antioxidant, Anti-acetylcholinesterase and Composition of Biochemical Components of Russian Deer Velvet Antler Extracts

  • Je, Jae-Young;Park, Pyo-Jam;Lim, Dong-Hwan;Jeon, Byong-Tae;Kho, Kang-Hee;Ahn, Chang-Bum
    • Food Science of Animal Resources
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    • v.31 no.3
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    • pp.349-355
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    • 2011
  • Russian deer velvet antlers were divided into three parts and subjected to a extraction process using hot water at 100, 110, and $120^{\circ}C$ or an extraction with 70% ethanol. Each extract was analyzed for its biochemical components, including uronic acid, sulfated-glycosaminoglycans (sulfated-GAGs), and sialic acid, and the antioxidant and anti-acetylcholinesterase activities were investigated. Different levels of uronic acid and sulfated-GAGs were observed in the extracts according to the water temperature used for the extraction, and contents decreased with increasing extraction temperature. The upper layer of each extract showed high amounts of uronic acid and sulfated-GAGs, followed by the middle and base layers. Ethanol extraction was more effective for recovering uronic acid than sulfated-GAGs. Sialic acid content was the highest in the $110^{\circ}C$ extracts but was not observed in the ethanol extracts. Velvet antler extracts showed strong antioxidant activities against DPPH and hydrogen peroxide as well as strong reducing power in a dose-dependent manner. However, the antioxidant activities were different in each layer and according to the extraction method. Additionally, velvet antler extracts exhibited inhibitory activity against acetylcholinesterase, which is associated with Alzheimer's disease, in a dose-dependent manner. These results suggest that velvet antler extracts are useful as a functional food ingredient and/or a pharmaceutical.