• Title/Summary/Keyword: Acetylcholinesterase (AChE)

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Inhibitory effect of Capparis zeylanica Linn. on acetylcholinesterase activity and attenuation of scopolamine-induced amnesia

  • Chaudhary, Amrendra Kumar;Solanki, Ruchi;Singh, Vandana;Singh, Umesh Kumar
    • CELLMED
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    • v.2 no.2
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    • pp.19.1-19.6
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    • 2012
  • $Capparis$ $zeylanica$ Linn. a 'Rasayana' drug is used for its memory enhancing effects in the traditional Ayurvedic system of medicine. The aim of this study was to evaluate acetylcholinesterase (AChE) inhibitory and memory enhancing activities of $Capparis$ $zeylanica$ Linn. The$in-vitro$ and $ex-vivo$ models of AChE inhibitory activity were used along with Morris water maze test to study the effect on memory in rats. The anticholinesterase effect of methanolic and aqueous extracts of $Capparis$ $zeylanica$ was measured by spectrophotometric Ellman method at 0.1, 0.3, 1.0, 3.0, 10 and 30 mg/ml and brain monoamine oxidase (MAO-A and MAO-B) activity was assessed by Naoi's method. The results $in-vitro$ and $ex-vivo$ AChE assay revealed that methanolic and aqueous extracts of $Capparis$ $zeylanica$ inhibit AChE activity, whereas these extracts did not alter MAO activity at any concentration tested as compared to moclobemide and L-deprenyl. The results indicate that $Capparis$ $zeylanica$ improves scopolamine-induced memory deficits through inhibition of AChE activity, and not by direct MAO inhibition.

Study on Biochemical Pollutant Markers for Diagnosis of Marine Pollution XI. Changes in Cholinesterase Activity of the Mussel (Mytilus coruscus) in the South Sea (해양오염의 진단을 위한 생화학적 오염지표에 관한 연구 XI. 남해산 홍합 (Mytilus coruscus)의 콜린에스테라아제의 변화)

  • 최진호;김대익;박수현;김동우;박청길;양동범
    • Journal of Life Science
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    • v.9 no.3
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    • pp.282-288
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    • 1999
  • This study was designed as a part of efforts to investigate the biochemical pollutant markers for diagnosis of marine pollutions by changes in cholinesterase activity of the mussel (Mytilus coruscus) in South Sea of Korea. Acetylcholinesterase (AChE) activities in muscle of cultured mussels in South Sea were remarkably lower (20∼41%, respectively) than those of wild mussel in Pohang(control) of East Sea. Acetylcholine (Ach) activities in muscle of cultured mussels in South Sea were remarkably lower (15∼30%, respectively) than those of wild mussel in Pohang of East Sea. Monoamineoxidase (MAO-B) activities in muscle of cultured mussels in South Sea were significantly 2∼19% higher than those of wild mussel in Pohang of East Sea. It suggests that AChE, ACh and MAO-B activities in muscle of cultured mussels of South Sea may be used as the most effective mean in a biochemical markers for early warning of environmental damages caused by organophosphorus pesticides.

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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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Influence of Toxoplasma gondii Acute Infection on Cholinesterase Activities of Wistar Rats

  • Tonin, Alexandre Alberto;da Silva, Aleksandro Schafer;Thorstenberg, Maria Luiza;Castilhos, Livia Gelain;Franca, Raqueli Teresinha;Leal, Daniela Bitencourt Rosa;Duarte, Marta Maria Medeiros Frescura;Vogel, Fernanda Silveira Flores;de La Rue, Mario L.;dos Anjos Lopes, Sonia Terezinha
    • Parasites, Hosts and Diseases
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    • v.51 no.4
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    • pp.421-426
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    • 2013
  • Several studies have shown the mechanisms and importance of immune responses against Toxoplasma gondii infection and the notable role of cholinesterases in inflammatory reactions. However, the association between those factors has not yet been investigated. Therefore, the aim of this study was to evaluate the acetylcholinesterase (AChE) activity in blood and lymphocytes and the activity of butyrylcholinesterase (BChE) in serum of rats experimentally infected with T. gondii during the acute phase of infection. For that, an in vivo study was performed with evaluations of AChE and BChE activities on days 5 and 10 post-infection (PI). The activity of AChE in blood was increased on day 5 PI, while in lymphocytes its activity was enhanced on days 5 and 10 PI (P<0.05). No significant difference was observed between groups regarding to the activity of BChE in serum. A positive (P<0.01) correlation was observed between AChE activity and number of lymphocytes. The role of AChE as an inflammatory marker is well known in different pathologies; thus, our results lead to the hypothesis that AChE has an important role in modulation of early immune responses against T. gondii infection.

Inhibition of acetylcholinesterase activity by impurities in technical grades and purified flupyrazofos (Flupyrazofos 원제 및 정제품의 불순물 조성과 Acetylcholinesterase에 대한 저해 비교)

  • You, Kyoung-Youl;Cho, Boo-Yeon;Park, Dong-Sik;Hur, Jang-Hyun
    • The Korean Journal of Pesticide Science
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    • v.9 no.1
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    • pp.97-101
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    • 2005
  • Flupyrazofos (O,O-diethyl O-1-phenyl-3-trifluoromethylpyrazo-5-yl phosphorothioate) is an organophosphorus insecticide with a pyrazole moiety which is newly developed and commercialized by SUNGBO chemical company and Korean Research Institute of Chemical Technology for effectively control against diamond back moth. This study was conducted to determine the composition and quantity of impurities in technical 1 (94.5%), technical 2 (97.6%) and purified (99.2%) flupyrazofos using GLC/MSD. Bimolecular inhibition rate constant($k_i$) with acethylcholinesterase (in vitro) and $I_{50}$ with mouse brain acetylcholinesterase (in vivo) were measured for comparing inhibitory patterns of two technicals and purified flupyrazofos. Impurities of flupyrazofos were identified as O,O,O-triethylthio-phosphoric acid (TEA), 1-phenyl-3-trifluoromethyl-5-ethoxy pyrazole(PTMEP), O,O-diethyl O-1-phenyl-3-trifluoromethylpyrazo-5-yl phosphoric acid ester(flupyrazofos oxen), O,S-diethyl O-1-phenyl-3-trifluoromethylpyrazo-5-yl phosphorothionate (S-ethyl flupyrazofos). In in vitro, technical 1 showed the fastest inhibition on AChE activity among them. And technical 1 and 2 showed 40% higher in vivo inhibition against mouse brian AChE than purified flupyrazofos did. These results could be caused by the impurities such as flupyrazofos oxen and S-methyl flupyrazofos contained in technical grades of flupyrazofos.

Effect of Papaverine on Acetylcholinesterase in Rat Brain

  • Park, Eun-Hee;Eun, Chung
    • Archives of Pharmacal Research
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    • v.12 no.1
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    • pp.34-38
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    • 1989
  • Papaverine administration produced significant increases in acetylcholinesterase activity in cerebral cortex and striatum of rat brain. Two related compounds, tetrahydropapaverine and tetrahydropapaveroline, also gave similar effects. However, their actions seem to be indirect because papaverine has no in vitro effect on the enzymatic activity.

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Effects of white ginseng and red ginseng extract on learning performance and acetylcholinesterase activity inhibition (백삼과 홍삼추출물의 학습수행과 Acetylcholinesterase 억제에 미치는 효과)

  • Lee, Mi-Ra;Sun, Bai-Shen;Gu, Li-Juan;Wang, Chun-Yan;Mo, Eun-Kyoung;Yang, Sun-Ah;Ly, Sun-Young;Sung, Chang-Keun
    • Journal of Ginseng Research
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    • v.32 no.4
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    • pp.341-346
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    • 2008
  • In the present study, we assessed the effects of white ginseng and red ginseng extract on the learning and memory impairments induced by scopolamine. The cognition-enhancing effect of ginseng extracts was investigated using the Morris water maze and Y-maze test. Drug-induced amnesia was induced by treating animals with scopolamine (2 mg/kg, i.p.), an antagonist of muscarinic acetylcholine (ACh) receptor. Tacrine was used a positive control. Ginseng extract (200 mg/kg, p.o.), tacrine (10 mg/kg, p.o.) administration significantly reduced the escape latency during training in the Morris water maze (p<0.05). At the probe trial session, scopolamine significantly increased the escape latency on day 5 in comparison with control (p<0.01). The effect of ginseng extracts on spontaneous alternation in Y-maze was similar to that of scopolamine treated group. In addition, numbers of arm entries were similar in all experimental groups. Moreover, red ginseng extract significantly inhibited acetylcholinesterase activity in the cortex and serum (p<0.05). Brain ACh contents of ginseng extract treated groups increased more than that of scopolamine group, which did not show statistically significant. These results suggest that ginseng extract may be useful for the treatment of cognitive impairment.

Effects of Malathion on the Ultrastructure and the Acetylcholinesterase Activity of the Developing Spinal Cord in Chick Embryos (Malathion이 발생중(發生中)인 개배(鷄胚) 척수(脊髓)의 미세구조(微細構造)와 acetylcholinesterase 활성(活性)에 미치는 영향(影響))

  • Kim, Wan-Jong;Deung, Young-Kun;Choe, Rim-Soon
    • Applied Microscopy
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    • v.18 no.1
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    • pp.60-76
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    • 1988
  • Chick embryos which have received a single injection of the organophosphate compound, malathion (0.1 mg/0.05 ml, 0.5 mg/0.05 ml, 1.0 mg/0.05 ml or 2.0 mg/0.05 ml) via the yolk sac at certain times (2 days, 4 days or 6 days after incubation) have been investigated. After 9 days of incubation, chick embryos were harvested to examine the effects of malathion on the ultrastructure and the acetylcholinesterase(AChE) activity of the developing spinal cord. The effects of simultaneous injection of malathion and nicotinamide were also compared. On ultrastructural findings, neurons in the ventral horn of spinal cord showed to be inhibited in their differentiation by malathion; nuclear irregularity, separation of nuclear membranes, reduction of ribosomal distribution, and cytoplasmic vacuoles were observed. In the younger embryos treated with relatively high doses of malathion, nucleus and cytoplasmic organelles of neurons were severely destroyed, and the neurons were shown to be necrotic. On cytochemical study of AChE by electron microscope, the positive reaction products of AChE were localized at the membranes of nucleus and endoplasmic reticulum of neurons. Inhibition of AChE activity was severe in groups treated with relatively low doses of malathion. Nicotinamide (5.0 mg/0.05 ml) alleviated malathion-induced morphological alterations. In conclusion, it is suggested that malathion changes the ultrastructure and reduces. AChE activity in differentiating neurons, and the severity of which is consistently dose- and age-dependent.

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Acetylcholinesterase Inhibitors from the Roots of Angelica dahurica

  • Kim, Dae-Keun;Lim, Jong-Pil;Yang, Jae-Heon;Eom, Dong-Ok;Eun, Jae-Soon;Leem, Kang-Hyun
    • Archives of Pharmacal Research
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    • v.25 no.6
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    • pp.856-859
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    • 2002
  • In the course of finding Korean natural products for acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the roots of Angelica dahurica showed significant inhibitory effects on AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of three furanocoumarins, isoimperatorin (1), imperatorin (2) and oxypeucedanin (3), as active principles. These compounds inhibited AChE activity in a dosedependent manner, and the $IC_{50}$ values of compounds 1-3 were 74.6, 63.7 and 89.1 uM, respectively.

EVIDENCE FOR HE CHANGES IN THE DOPAMINERGIC ACTIVITY AFTER THE SUBACUTE ADMINSTRATION WITH PHYSOSTIGMINE

  • Lim, Dong-Koo;Lee, Kyung-Min;Moon, Ae-Ra
    • Toxicological Research
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    • v.8 no.1
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    • pp.71-81
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    • 1992
  • Rats were treated with physostigamine acutely and subacutely for 7 days. The duration of tremor, striatal acetylcholinesterase(AChE) activity and the occurrences of dopaminal antagonist-induced catalepsy were measured. During the daily treatment with 0.75mg/kg of physostigmine, the durations of tremor were markedly reduced. However, the tremors were ot occurred in the continuous infusion up to 0.20mg/kg/hr. Striatal AChE activities were significantly inhibited(8.25%) early hour, but twenty-four hour after daily administration with physostigmine AChE activities during the continuous infusion with physostigmine were also significantly inhibites (30-60%).

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