• Title/Summary/Keyword: acetyl cholinesterase

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Antioxidants and Acetyl-cholinesterase Inhibitory Activity of Solvent Fractions Extracts from Dendropanax morbiferus (황칠나무의 용매 분획별 추출물의 항산화 활성 및 Acetyl-cholinesterase 저해 활성비교)

  • Yu, Ji Min;Moon, Hyung In
    • Korean Journal of Plant Resources
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    • v.31 no.1
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    • pp.10-15
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    • 2018
  • The leaves and stems of Dendropanax morbiferus were separated from organic solvents with methanol. The organic solvent fractions were fractionated with dichloromethane, ethyl acetate and butanol according to the systematic fractionation method. Oxidation in the body induces aging, and antioxidant activity has attracted the attention of many people as a preventive component to suppress negative reactions in the body. To investigate the antioxidant activity of Dendropanax morbiferus were subjected to DPPH free radical assay. In addition, acetyl cholinesterase inhibitions were performed for Alzheimer's disease as an aging neurological disease. As a result, it was confirmed that the antioxidant effect of DPPH was generally good in the antioxidant test. The ethyl acetate fractions of Dendropanax morbiferus stems and leaves were $IC_{50}=30{\mu}g/m{\ell}$. Acetyl cholinesterase inhibition experiments were carried out at a concentration of $250{\mu}g/m{\ell}$. Dendropanax morbiferus stems fractions showed dichloromethane fraction of 57.68%, which significantly inhibited the activity of acetyl cholinesterase.

Isolation of Flavonoid Glycosides with Cholinesterase Inhibition Activity and Quantification from Stachys japonica

  • Nugroho, Agung;Choi, Jae Sue;Seong, Su Hui;Song, Byong-Min;Park, Kyoung-Sik;Park, Hee-Juhn
    • Natural Product Sciences
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    • v.24 no.4
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    • pp.259-265
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    • 2018
  • The three flavone glycosides, 4'-O-methylisoscutellarein 7-O-(6'''-O-acetyl)-${\beta}$-D-allopyranosyl(1${\rightarrow}$2)-${\beta}$-D-glucopyranoside (1), isoscutellarein 7-O-(6'''-O-acetyl)-${\beta}$-D-allopyranosyl(1${\rightarrow}$2)-${\beta}$-D-glucopyranoside (3), and isoscutellarein 7-O-${\beta}$-D-allopyranosyl(1${\rightarrow}$2)-${\beta}$-D-glucopyranoside (4) in addition to a flavonol glycoside, kaempferol 3-O-${\beta}$-D-glucopyranoside (astragalin, 2), were isolated from Stachys japonica (Lamiaceae). In cholinesterase inhibition assay, compound 1 significantly inhibited aceylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities ($IC_{50}s$, $39.94{\mu}g/ml$ for AChE and $86.98{\mu}g/ml$ for BChE). The content of isolated compounds were evaluated in this plant extract by HPLC analysis. Our experimental results suggest that the flavonoid glycosides of S. japonica could prevent the memory impairment of Alzheimer's disease.

Effect of Papaverine and Diphenhydramine on the Action of Cholinesterase Inhibitors (항코린에스테라제 활성에 대한 파파베린 및 디펜히드라민의 효과)

  • 박은희;금정혜;박수선
    • YAKHAK HOEJI
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    • v.35 no.5
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    • pp.438-443
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    • 1991
  • This study was designed to examine the effects of diphenhydramine and papaverine on the toxic manifestations of cholinesterase inhibitors. It was found that papaverine increase acetylcholinesterase activity in cerebral cortex of mice. Papaverine pretreatment tended to increase acetylcholinesterase activity against the actions of neostigmine and physostigmine. When diphenhydramine (20~30 mg/kg, s.c.) was treated 20 min before the administration of cholinesterase inhibitor, it significantly extended the onset latency in the signs of toxicosis which were characteristically produced by physostigmine (0.25~1.5 mg/kg, s.c.) or neostigmine (0.125~0.5 mg/kg, s.c.), and it also prevented lethality in all of the animals.

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A study on the mechanism for reduction of lead-induced toxicity in nervous system by aloe vera (Aloe vera의 연 유도성 신경계 독성 저감 기전에 관한 연구)

  • 정명규;곽영규
    • Journal of Environmental Health Sciences
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    • v.22 no.3
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    • pp.8-16
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    • 1996
  • Effects of water extract of aloe vera on lead-induced neurotoxicity were investigated in sciatic nerve isolated from rat. The mechanism on toxicity reduction by measuring activities of axonal enzymes, metabolism of myo-inositol in nerve, lead concentration in several organs and so on were further examimed. In the lead-treated rats, the transport rate of axonal enzyme, such as acetyl cholinesterase and choline acetyltransferase, was reduced by from 50% to 30% respectively. Reduction in myo-inositol concentration and $Na^+/K^+$ ATPase activity were also observed in sciatic nerve from lead-treated rat. However, the aloe extract administration significantly eliminated the impairment and maintained myo-inositol concentration to about 85% of normal level. Also aloe extract promoted the excretion rate of lead which is accumulated in blood, sciatic nerve and kidney. These results suggest that lead-induced neurotoxicity was significantly reduced by administration of aloe extract and the mechanism might be partly increase in kidney excretion rate of lead and parity normalization of $Na^+/K^+$ ATPase activity which is critical factor in order to keep nerve maintaining normal myo-inositol level.

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Antioxidant and Cholinesterase Inhibitory Activities of Aqueous Extract from Rainbow Trout Oncorhynchus mykiss

  • Baek, Jae-Min;Yoon, Na-Young;Kim, Yeon-Kye;Lee, Doo-Seog;Yoon, Ho-Dong;Park, Jeung-Sook
    • Fisheries and Aquatic Sciences
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    • v.14 no.2
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    • pp.89-92
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    • 2011
  • We investigated the antioxidant and cholinesterase inhibitory activities of the aqueous extract of rainbow trout Oncorhynchus mykiss. The antioxidant activity of O. mykiss aqueous extract was determined by in vitro peroxynitrite scavenging activity and reducing power assays. The aqueous extract of O. mykiss showed potent peroxynitrite radical scavenging activity ($IC_{50}=0.12{\pm}0.001\;mg/mL$) and reducing power (absorbance=$0.47{\pm}0.001$) at the concentration of 1 mg/mL. The in vitro cholinesterase inhibitory activity of O. mykiss aqueous extract was examined using spectrophotometric analyses of acetyl- and butyrylcholinesterase. The aqueous extract of O. mykiss showed acetylcholinesterase inhibitory activity ($IC_{50}=1.61{\pm}0.13\;mg/mL$), but did not exhibit inhibitory activity against butyrylcholinesterase. These results suggest that O. mykiss possesses antioxidant and acetylcholinesterase inhibitory activities and provide scientific evidence for the health benefits of O. mykiss aqueous extract.

New evidences of neurotoxicity of aroclor 1254 in mice brain: potential of coenzyme q10 in abating the detrimental outcomes

  • Majumdar, Anuradha;Nirwane, Abhijit;Kamble, Rahul
    • Environmental Analysis Health and Toxicology
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    • v.29
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    • pp.1.1-1.7
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    • 2014
  • Objectives The present subacute study was designed to evaluate the effect of coenzyme Q 10 (CoQ10) in the 28 days aroclor 1254 exposure induced oxidative stress in mice brain. Methods Biochemical estimations of brain lipid peroxidation (LPO), reduced glutathione (GSH), and activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx) and acetyl cholinesterase (AChE), and histopathological investigations of brain tissue were carried out. Results Oral exposure of aroclor 1254 (5 mg/kg) led to significant decrease in levels of GSH, and activities of SOD, CAT, GPx, and AChE, and increase in LPO. These aberrations were restored by CoQ10 (10 mg/kg, intraperitoneal injection [IP]). This protection offered was comparable to that of L-deprenyl (1 mg/kg, IP) which served as a reference standard. Conclusions Aroclor 1254 exposure hampers the activities of various antioxidant enzymes and induces oxidative stress in the brains of Swiss albino mice. Supplementation of CoQ10 abrogates these deleterious effects of aroclor 1254. CoQ10 also apparently enhanced acetyl cholinesterase activity which reflects its influence on the cholinergic system.

Antiamnesic potentials of Foeniculum vulgare Linn. in mice

  • Joshi, Hanumanthachar;Parle, Milind
    • Advances in Traditional Medicine
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    • v.7 no.2
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    • pp.182-190
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    • 2007
  • Alzheimer's disease is a neurodegenerative disorder associated with a decline in cognitive abilities. Dementia is one of the aged related mental problems and a characteristic symptom of Alzheimer's disease. Nootropic agents like piracetam and cholinesterase inhibitors like $Donepezil^{\circledR}$ are used in situations where there is organic disorder in learning abilities, but the resulting side-effects associated with these agents have limited their utility. Foeniculum (F.) vulgare Linn. is widely used in Indian traditional systems of medicines and also as a house remedy for nervous debility. The present work was undertaken to assess the potential of F. vulgare as a nootropic and anti-cholinesterase agent in mice. Exteroceptive behavioral models such as Elevated plus maze and Passive avoidance paradigm were employed to assess short term and long term memory in mice. To delineate the possible mechanism through which F. vulgare elicits the anti-amnesic effects, its influence on central cholinergic activity was studied by estimating the whole brain acetylcholinesterase activity. Pretreatment of methanolic extract of fruits of F. vulgare Linn. for 8 successive days, ameliorated the amnesic effect of scopolamine (0.4 mg/kg) and aging induced memory deficits in mice. F. vulgare extract significantly decreased transfer latencies of young mice and aged mice, increased step down latency and exhibited significant anti-acetyl cholinesterase effects, when compared to piracetam, scopolamine and control groups of mice. F. vulgare might prove to be a useful memory restorative agent in the treatment of dementia seen in the elderly.

The Effects of Ethanol on Cholinesterase Inactivation by Organophosphorous (에탄올이 유기인제 농약에 의한 Cholinesterase 불활성화에 미치는 영향)

  • Choi, Hyoung-Chul;Kim, Jong-Ho;Ha, Jeoung-Hee;Lee, Kwang-Yoon;Kim, Won-Joon;Woo, Hyun-Jae;Huh, Chang-Uk;Son, Soo-Min;Chun, Eun-Jin
    • Journal of Yeungnam Medical Science
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    • v.16 no.2
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    • pp.326-332
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    • 1999
  • Background: In korea the agricultural community widely uses organophosphorous, and organophosphorous poisonings are increasing every year. We compared change in activity of acetylcholinesterase and pseudocholinesterase by organophosphorous and by the interaction of ethanol and organophosphorous. We also compared the effect of reversible anticholinesterase drugs, physostigmine and neostigmine The object of this study is to investigate the effects of several anticholinesterase drugs and on how ethanol influences the activity of cholinesterase. Materials and Methods: Fifteen male university students were randomly selected, and blood samples were taken from the antecubital vein. The acetylcholinesterase in the RBC and the pseudocholinesterase in the serum were extracted and separated. The enzyme activity change was measured by the electrometric method. After adding acetylcholine, the pH change was measured with a pH meter. Results and Conclusion: Our results indicated that reversible anticholinesterase drugs decreased the cholinesterase activity more efficiently than organophosphorous. The acetyl cholinesterase and pseudocholinosterase activity were decreased by ethanol. When ethanol was added, oxime a cholinesterase activator, increased acetylcholinesterase activity but does not increased pseudocholinesterase activity.

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Effect of Leonurus japonicus Houtt. on Scopolamine-induced Memory Impairment in Mice (Scopolamine 유발 기억 손상 마우스에서 익모초의 효과)

  • Lee, Jihye;Kim, Hye-Jeong;Jang, Gwi Yeong;Seo, Kyung Hye;Kim, Mi Ryeo;Choi, Yun Hee;Jung, Ji Wook
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.34 no.2
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    • pp.81-87
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    • 2020
  • Cognitive impairment is symptoms of dementia, a degenerative brain disease that is drawing attention in a rapidly aging society. This study was conducted to investigate the improvement of cognitive function of Leonurus japonicus on scopolamine-induced memory impairment in mice and the effect and mechanism of memory recovery. In vivo studies were conducted on mice orally pretreated with L. japonicus in doses of 50, 100 and 200 mg/kg (p.o.) and scopolamine (1 mg/kg, i.p.) were injected 30 min before the behavioral task. Antioxidant activity was assessed by 2,2-diphenyl-1-picryl hydrazyl (DPPH) assay and 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay, and acetylcholinesterase (AChE) inhibition activity evaluated by Ellman's method. In behavior studies showed that L. japonicus has an improved the memory of scopolamine-treated mice in Y-maze, passive avoidance and Morris water maze test. In addition, L. japonicus was also exerted free radical scavenging activity and inhibited acetyl cholinesterase activity. These results suggest that L. japonicus improves short-term and long-term memory in scopolamine-induced memory decline model and prevents scopolamine-induced memory impairments through in reduced oxidative stress and acetyl cholinesterase inhibition effect. Thus, L. japonicus is related to functional medicinal materials for prevention and treatment of human dementia patients.

Development of Selective Butyrylcholinesterase Inhibitors Using (R)-Lipoic Acid-Polyphenol Hybrid Molecules

  • Woo, Yeun-Ji;Lee, Bo-Hyun;Yeun, Go-Heum;Kim, Hyun-Ju;Ko, Jang-Myoun;Won, Moo-Ho;Lee, Bong-Ho;Park, Jeong-Ho
    • Bulletin of the Korean Chemical Society
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    • v.32 no.spc8
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    • pp.2997-3002
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    • 2011
  • A series of hybrid molecules between (R)-lipoic acid (ALA) and the acetylated or methylated polyphenol compounds were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were checked. The $IC_{50}$ values of all hybrid molecules for a BuChE inhibition were lower than those of the single parent compounds. Specifically, ALA-acetyl protected caffeic acid (11, ALA-AcCA) was shown as an effective inhibitor of BuChE ($IC_{50}=0.5{\pm}0.2\;{\mu}M$) and also had a great selectivity for BuChE over AChE (more than 800 fold). Inhibition kinetic study indicated that 11 is a mixed inhibition type. Its binding affinity ($K_i$) value to BuChE is $1.52{\pm}0.18\;{\mu}M$.