• Title/Summary/Keyword: acetylcholinesterase

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In vitro Screening of Oxime Reactivators on the Model of Paraoxon-inhibited Acetylcholinesterase-SAR Study

  • Holas, Ondrej;Musilek, Kamil;Pohanka, Miroslav;Kuca, Kamil;Opletalova, Veronika;Jung, Young-Sik
    • Bulletin of the Korean Chemical Society
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    • v.31 no.6
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    • pp.1609-1614
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    • 2010
  • Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Standard in vitro test was chosen using a rat brain homogenate as the source of AChE. Screening of reactivation potency was performed with two concentration of reactivator (1000 ${\mu}M$ and 10 ${\mu}M$). Results were compared to established reactivators pralidoxime, methoxime, HI-6, trimedoxime and obidoxime. More than 30 novel reactivators performed equal or better reactivation ability of POX-inhibited AChE compared to currently used reactivators. The structure-activity relationship for reactivators of paraoxon-inhibited AChE was developed.

Acetylcholinesterase Inhibitors from the Twigs off Vaccinium oldhami Miquel

  • Lee, Jae-Hyeok;Lee, Ki-Taek;Yang, Jae-Heon;Baek, Nam-In;Kim, Dae-Keun
    • Archives of Pharmacal Research
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    • v.27 no.1
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    • pp.53-56
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    • 2004
  • In the course of finding Korean natural products with acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the twigs of Vaccinium oldhami significantly inhibited AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of two compounds, taraxerol (1) and scopoletin (2), as active constituents. These compounds inhibited AChE activity in a dose-dependent manner, and the $IC_{50}$/ values of compounds 1 and 2 were 33.6 (79 $\muM$) and 10.0 (52 $\muM$) $\mu$g/mL, respectively.

Production of Anti-dementia Acetylcholinesterase Inhibitors from the Wild Yeasts Saccharomyces cerevisiae WJSL0113 and Wickerhamomyces anomalus JSF0128

  • Kim, Ji-Yoon;Lee, Sang-Yeop;Han, Sang-Min;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.46 no.4
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    • pp.447-457
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    • 2018
  • In this paper, the screening of potent acetylcholinesterase (AChE) inhibitor - producing yeasts from wild yeasts and the condition for the production of anti-dementia AChE inhibitors are described. Among one hundred and seven non-pathogenic wild yeast strains from the waters and soils of three main rivers in Daejeon metropolitan city and midstream of Yeongsangang river in Sangju, sporogenous Saccharomyces cerevisiae WJSL0113 and asporogenous Wickerhamomyces anomalus JSF0128 were selected as useful strains for the production of potent AChE inhibitors. The AChE inhibitors of S. cerevisiae WJSL0113 and W. anomalus JSF0128 had a maximum yield when they were incubated in yeast extract-peptone-dextrose media (pH 6.0 in S. cerevisiae WJSL0113 and pH 5.0 in W. anomalus JSF0128) for 18 hr at $30^{\circ}C$, respectively.

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.

Evaluation of antioxidant, α-glucosidase inhibition and acetylcholinesterase inhibition activities of Allium hookeri root grown in Korea and Myanmar (국내 및 미얀마에서 재배된 삼채뿌리의 항산화, α-Glucosidase 저해 및 Acetylcholinesterase 저해 활성)

  • Park, Joo Young;Yoon, Kyung Young
    • Food Science and Preservation
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    • v.23 no.2
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    • pp.239-245
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    • 2016
  • This study was conducted to compare the functionality (antioxidant, anti-diabetic, and anti-dementia activities) of the methanol extract of Allium hookeri root grown in Korea (KR) and Myanmar (MR). The total polyphenol and flavonoid contents of KR and MR were 5.27 and 4.80 mg GAE/g, and 0.35 and 0.24 mg QE/g, respectively. KR contained significantly higher levels of total polyphenols and total flavonoids than those of MR (p<0.05). The IC50 values of KR and MR were 6.53 and 5.31 mg/mL, respectively, for DPPH radical scavenging activity. However, KR had a significantly higher ABTS radical scavenging activity, $Fe^{2+}$ chelating ability, and reducing power compared with those of MR (p<0.05). In the evaluation of anti-diabetic activity, KR showed significantly higher ${\alpha}-glucosidase$ inhibition activity than acarbose and MR at whole concentrations (p<0.05). KR and MR had acetylcholinesterase inhibition activities that of 51.44% and 44.33%, respectively, at a 50 mg/mL concentration. These results suggested that roots of A. hookeri, especially KR, could be useful in improving diabetic and dementia disorders due to their high antioxidant, anti-diabetic, and anti-dementia activities.

Acetylcholinesterase Inhibitory Activity and Protective Effect against Cytotoxicity of Perilla Seed Methanol Extract (들깨 메탄올 추출물의 acetylcholinesterase 억제활성 및 세포독성 보호효과)

  • Choi, Won-Hee;Um, Min-Young;Ahn, Ji-Yun;Kim, Sung-Ran;Kang, Myung-Hwa;Ha, Tae-Youl
    • Korean Journal of Food Science and Technology
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    • v.36 no.6
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    • pp.1026-1031
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    • 2004
  • Acetylcholinesterase inhibitory activity and protective effect against cytotoxicity of PC 12 cell induced by beta-amyloid protein and glutamate were examined in perilla seed methanol extract and its solvent fractions. Methanol extract of perilla seed showed dose-dependent acetylcholinesterase inhibitory activity, with n-butanol fraction showing strongest activity. Perilla seed methanol extract also decreased glutamate- and ${\beta}-amyloid$ protein $(A{\beta})-induced$ cytotoxicities of PC 12 cells dose-dependently. Formation of TBARS induced by $FeSO_{4^-}H_2O_2$ in rat brain was significantly reduced by perilla seed methanol extract, with strongest protective activity formation of TBARS shown in n-butanol fraction. Results suggest perilla seed methanol extract may attenuate actylcholinesterase activity and cytotoxicity induced by glutamate and ${\beta}-amyloid$ protein through suppression of oxidative stress.

Variation in Insecticide Susceptibilities of the Beet Armyworm, Spodoptera exigua (Hubner): Esterase and Acetylcholinesterase Activities (파밤나방(Spodoptera exigua (Hubner))의 살충제 감수성 변이-에스테라제와 아세틸콜린에스테라제 활력)

  • 김용균;이준익;강성영;한상찬
    • Korean journal of applied entomology
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    • v.36 no.2
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    • pp.172-178
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    • 1997
  • There was a great variation in insecticide susceptibilities among field and laboratory populations of the beet armyworm, Spodoptera exigua (Hiibner). Unselected laboratory population, which had been reared for 6-7 generations in our laboratory without exposure to insecticides, was more susceptible than its parental field population in all tested insecticides. Two selected laboratory populations with parathion or deltamethrin showed much higher insecticide tolerance than did the unselected laboratory population in their own selection insecticide. The variation of the insecticide susceptibilities was highly correlated with esterase and acetylcholinesterase activities. Field and the selected laboratory populations had lower acetylcholinesterase activities and higher esterase activities than did the unselected laboratory population. Acetylcholinesterase of the field and the selected laboratory populations had higher Km values than did that of the unselected. In a population, Km values were varied among different developmental stages; acetylcholinesterase of the fifth instar larvae had the highest Km value among those of the other larval stages. Twenty one esterase bands were separated on 6.5% nondenaturing polyacrylamide gel from the whole body extracts of the fifth instar larvae. E2, E7, E8, Ell, El6, and El7 esterase bands were developed more frequently in the insecticides-selected populations than in the unselected population. These results suggest that the variation of insecticide susceptibilities of the beet armyworm includes both biochemical mechanisms: target site insensitivity and enhanced activity of detoxification enzyme.

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EFFECT OF PHYSOSTIGMINE PRETREATMENT ON PARATHION TOXICITY IN RATS

  • Kim, Sung-Y;Park, Kwon-H;Lee, Myung-G;Kim, Young-C
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2002.05a
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    • pp.123-123
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    • 2002
  • Abstract The protective effects of physostigmine against the toxicity of parathion (diethyl-4-nitrophenyl phosphorothionate) were examined in male Sprague-Dawley rats. Physostigmine (100 or 1,000 ㎎/㎏, ip) injected 30 min before decreased the inhibition of acetylcholinesterase (AChE) activities in brain, lung and blood induced by parathion (2 ㎎/㎏, ip).(omitted)

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