• Title/Summary/Keyword: Acetylcholinesterase activity

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Effect of Defatted Sesame and Perilla Methanol Extracts on Cognitive Function and Antioxidant Activity in SAMP8 Mice (노화촉진마우스에 있어서 참깨박 및 들깨박의 메탄올 추출물이 인지기능 및 항산화능에 미치는 영향)

  • Um, Min-Young;Choi, Won-Hee;An, Ji-Yun;Kim, Sung-Ran;Ha, Tae-Youl
    • Korean Journal of Food Science and Technology
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    • v.36 no.4
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    • pp.637-642
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    • 2004
  • Effects of defatted sesame and perilla methanol extracts on cognitive function and antioxidant activity of learning- and memory-impaired animal model SAMP8 mice. Animals were divided into 4 groups and fed with diets containing 0.3%(w/w) defatted sesame (S) or defatted perilla methanol extracts (P) for 12 weeks. Step through latency of SAMP8 control group was significantly higher than that of SAM R1 normal group, whereas significantly increased in S and P groups compared with SAMP8 control on passive avoidance test (p<0.001). Acetylcholinesterase activity of brain in SAMP8 increased compared with SAMR1 but no difference between SAMP8 control group and sample-treated group. Brain TBARS contents of SAMP8 control significantly increased compared with SAMR1 and were lowered significantly by supplementation of defatted sesame and perilla methanol extracts. Defatted sesame and perilla methanol extracts attenuated increased brain superoxide dismutase and glutathione peroxidase activities in SAMP8. These results suggest defatted sesame and perilla methanol extracts could attenuate cognitive deficits induced by aging possibly through activation of antioxidant activity of defatted sesame and perilla methanol extracts.

Cloning and Characterization of a Novel Carboxylesterase Gene from Cow Rumen Metagenomic Library (소 반추위 메타게놈에서 새로운 carboxylesterase 유전자 클로닝 및 유전산물의 특성)

  • Asraful Islam, Shah Md.;Kim, Min-Keun;Renukaradhya, K. Math;Srinivasa, Reddy R.N.;Kim, Eun-Jin;Kim, Jung-Ho;Kim, Hoon;Yun, Han-Dae
    • Journal of Life Science
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    • v.20 no.9
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    • pp.1306-1313
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    • 2010
  • The gene encoding esterase enzyme was cloned from a metagenomic library of cow rumen bacteria. The esterase gene (est1R) was 2,465 bp in length, encoding a protein of 366 amino acid residues, and the molecular weight of the enzyme was 61,166 Da. Est1R of rumen cosmid library shared 5.9% amino acid identity with Est1R (P37967) of PNB carboxylesterase, 6.1% with Est1R (1EEAA) of acetylcholinesterase and 6.1% with Est1R (1H23A) of chain A. BlastP in NCBI database analysis of Est1R revealed that it was not homologous to previous known lipases and esterases. Est1R showed optimum activity at pH 7.0 and $40^{\circ}C$. On the other hand, the enzyme was found to be most active without organic solvent, followed by 95% activity with methanol, and the enzyme activity was highly affected by hexane (lost 51% activity). Therefore, the novel esterase gene est1R is likely obtainable from cow rumen metagenome and may be utilized for industrial purposes.

A Comparative Study of GABA, Glutamate Contents, Acetylcholinesterase Inhibition and Antiradical Activity of the Methanolic Extracts from 10 Edible Plants (10가지 식용식물 추출물의 가바, 글루탐산 함량, 아세틸콜린에스테라제 억제 및 라디컬 소거능 비교)

  • Jung, Yeon-Seop;Park, Sung-Jin;Kim, Ji-Eun;Yang, Seun-Ah;Park, Jung-Hyun;Kim, Jung-Hyun;Jhee, Kwang-Hwan;Lee, Sam-Pin;Lee, In-Seon
    • Korean Journal of Food Science and Technology
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    • v.44 no.4
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    • pp.447-451
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    • 2012
  • In order to investigate the efficacies for cognitive function of edible plants, we measured the inhibitory effects of acetylcholinesterase(AChE) activity, radical scavenging activities, and the contents of GABA and glutamate in the plant extracts. Among the plant extracts, Schizandra chinensis contained the highest GABA 14.8 mg/g and the extracts of Cnidium officinale and Polygonum multiflorum also had a relatively high GABA. On the other hand, plant extracts except, Acorus gramineus, showed similar glutamate contents. S. chinensis, Hovenia dulcis, Thuja orientalis, and Eleutherococcus senticosus exhibited high inhibition against AChE activities at about 18-33% at 1 mg/mL. In addition, strong radical scavenging activities were also detected in those extracts which showed high AChE inhibition. Taken together, H. dulcis, T. orientalis, E. senticosus, and S. chinensis could be effective resources for enhancing cognitive function. Further, it was suggested that the AChE inhibitory activities of plant extracts might be related to antioxidative activity.

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.

Gossypii Semen oil alleviates memory dysfunction in scopolamine-treated mice (면화자 정유의 기억력 손상 완화 효과)

  • Lee, Jihye;Jung, Eun Mi;Lee, Eunhong;Jang, Gwi Yeong;Seo, Kyung Hye;Kim, Mi Ryeo;Jung, Ji Wook
    • The Korea Journal of Herbology
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    • v.36 no.2
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    • pp.1-9
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    • 2021
  • Objectives : Gossypium arboreum (cotton) is traditionally used to treat various health disorders. However, anti-amnesic effect of G. arboreum has not been reported. The objective of this study was to investigate in-vivo the anti-amnesic effects along with in vitro antioxidant and acetylcholinesterase (AChE) inhibition potential in G. arboreum seed essential oil. Methods : The essential oil of G. arboreum obtained by solid phase microextraction (SPME) techniques were identified by gas chromatography-mass spectroscopy (GC-MS). 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay were performed to determine the antioxidant activity at various concentrations (312.5, 625, 1250, 2500, 5000, 10000 ㎍/㎖. Y-maze, passive avoidance and Morris water maze tests were carried out to evaluate improved effect on scopolamine (1 mg/kg)-induced memory dysfunction at the dose level of 50, 100 and 200 mg/kg. Donepezil (5 mg/kg) was used as a positive drug control. We performed acetylcholinesterase (AChE) activity assay in ex vivo. Results : Five volatile compounds were identified in G. arboreum. The assays of DPPH and ABTS revealed that G. arboreum increased antioxidant activity in a dose-dependent manner. G. arboreum ameliorated the percent of spontaneous alternation in the Y-maze test, shortened step-through latency in the passive avoidance test, and increased swimming time in the target zone in the Morris water maze test. In addition, G. arboreum inhibited the AChE activity. Conclusions : Based on these findings, G. arboreum may aid in the prevention and treatment of learning and memory-deficit disorders through antioxidant and AChE inhibitory activities.

LDH/ AChE and LDH/BChE Ratios (Paralichthys olivaceus) as Biomarkers of Coastal Pollution on Coast of Korea.

  • Choi Jin-Ho;Kim Dong-Woo;Kim Chang-Mok;Yang Dong Beom
    • Fisheries and Aquatic Sciences
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    • v.2 no.2
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    • pp.167-171
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    • 1999
  • This study was designed to develop biomarkers of coastal pollution using biochemical indices of flounder (Paralichthys olivaceus) by changes in lactate dehydrogenase (LDH) activity in the serum and cholinesterase activities in brain membranes. For this purpose acetylcholiesterase (AChE) activity, butyrylcholinesterase (BChE) activity, LDH/AChE ratio and LDH/BChE ratio of cultured flounders at 5 different sites on the southern coast of Korea were compared to those of wild flounders caught in the Pohang, eastern coast of Korea as a control group. Relatively high LDH activities were measured in the serum of flounders cultured on the southern coast of Korea (0.101-0.145 unit) than those in the Pohang control group (0.093 unit). AChE activities were significantly low $(about\;10-20\%)$ in brain membranes of cultured flounders compared to those in the Pohang control group. The ratios of LDH/AChE and LDH/BChE were consistently higher $(136-178\%,\; 155-214\%)$ in cultured flounders than those of Pohang control group. Thus, we propose that the ratios of LDH/AChE and LDH/BChE in flounders could be applicable for the diagnosis of marine pollution.

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Comparative Study of Korean White, Red, and Black Ginseng Extract on Cholinesterase Inhibitory Activity and Cholinergic Function

  • Lee, Mi-Ra;Yun, Beom-Sik;In, Oh-Hyun;Sung, Chang-Keun
    • Journal of Ginseng Research
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    • v.35 no.4
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    • pp.421-428
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    • 2011
  • This study evaluated cholineresterase inhibitory activity of Korean white ginseng extract (WGE), red ginseng extract (RGE), and black ginseng extract (BGE) and the cholinergic effect on scopolamine (SCOP)-induced amnesic mice. WGE, RGE, and BGE inhibited acetylcholineserase (AChE), as well as butyrylcholineserase (BuChE) in a concentration-dependent manner. BGE presented strong inhibition of AChE with an $IC_{50}$ value of 1.72 mg/mL, followed by WGE (5.89 mg/mL), RGE (6.30 mg/mL), respectively. The inhibitory activity of the three ginseng extracts on BuChE showed similar values among the groups. To better understand the mechanisms of the possible effect of ginseng extract on the cholinergic function, this study assessed the expression of the cholinergic markers of choline acetyltransferase (ChAT) and AChE using western blot and RT-PCR analysis in the brains of amnesic mice. Treatment with ginseng extracts led to inhibition of AChE expression and, the activation of ChAT expression in the hippocampus and the cerebral cortex of amnesic mice as induced by SCOP. The results suggest that ginseng extracts including BGE, appear to modulate the metabolism of acetylchoine (ACh), which would greatly increase synaptic ACh levels and most potently revert SCOP-induced amnesia.

Effects of Erythropoietin on Memory Deficits and Brain Oxidative Stress in the Mouse Models of Dementia

  • Kumar, Rohit;Jaggi, Amteshwar Singh;Singh, Nirmal
    • The Korean Journal of Physiology and Pharmacology
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    • v.14 no.5
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    • pp.345-352
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    • 2010
  • The present study was undertaken to explore the potential of erythropoietin in memory deficits of mice. Memory impairment was produced by scopolamine (0.5 mg/kg, $i.p.$) and intracerebroventricular streptozotocin (i.c.v STZ, 3 mg/kg, $10{\mu}l$, $1^{st}$ and $3^{rd}$ day) in separate groups of animals. Morris water-maze test was employed to assess learning and memory. The levels of brain thio-barbituric acid reactive species (TBARS) and reduced glutathione (GSH) were estimated to assess degree of oxidative stress. Brain acetylcholinesterase enzyme (AChE) activity was also measured. Scopolamine/streptozotocin administration induced significant impairment of learning and memory in mice as indicated by marked decrease in Morris water-maze performance. Scopolamine/streptozotocin administration also produced a significant enhancement of brain AChE activity and brain oxidative stress (an increase in TBARS and a decrease in GSH) levels. Treatment of erythropoietin (500 and 1,000 IU/Kg i.p.) significantly reversed scopolamine- as well as streptozotocin-induced learning and memory deficits along with attenuation of those-induced rise in brain AChE activity and brain oxidative stress levels. It may be concluded that erythropoietin exerts a beneficial effect in memory deficits of mice possibly through its multiple actions including potential anti-oxidative effect.

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 $2.91{\pm}0.15{\mu}M$.

Protective Effect of Physostigmine and Neostigmine against Acute Toxicity of Parathion in Rats

  • Jun, Jung-Won;Kim, Young-Chul
    • Archives of Pharmacal Research
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    • v.14 no.4
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    • pp.330-335
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    • 1991
  • The effects of physostigmine and neostigmine on the parathin induced toxicity were examined in adult female rats. Physostigmine $(100\;{\mu}g/kg,\;ip)$ or neostigmine $(200\;{\mu}g/kg,\;ip)$ inhibited acetylcholinesterase (AChE) and cholinesterase (ChE) activities in blood, brain and lung when the enzyme activity was measured 30 min after the treatment. At the doses of two carbamates equipotent on brain AChE, neostigmine showed greater inhibition on peripheral AChE/ChE. The enzyme activity returned to normal in 120 min following the carbamates except in the lung of rats treated with neostigmine. Carbamates administered 30 min prior to parathion (2 mg/kg) antagonized the inhibition of AChE/ChE by parathion when the enzyme activity was measured 2 hr following parathion. Neostigmine showed greater protective effect on peripheral AChE/ChE. The effect of either carbamate on AChE/ChE was not significant 2 hr beyond the parathion treatment. Carbamates decreased the mortality of rats challenged with a lethal dose of parathion (4 mg/kg, ip) either when treated alone or in combination with atropine (10 mg/kg, ip). Lethal action of paraoxon (1.5 mg/ks ip), the active metabolite of parathion was also decreased by the carbamate treatment indicating that the protection was not mediated by competitive inhibition of metabolic conversion of parathion to paraoxon. The results suggest that carbamylation of the active sites may not be the sole underlying mechanism of protection provided by the carbamates.

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