• The Korea Journal of Herbology
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• v.34 no.5
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• pp.29-37
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• 2019

Objectives : Bang-poong (Saposhnikovia divaricata; SD) was traditionally used to treat inflammatory disorders. In this study, we aimed to investigate whether Bang-poong and related species including SD, Glehnia littoralis (GL), and Peucedanum japonicum (PJ) possess neuroprotective effects and acetylcholinesterase (AChE) inhibitory activities. Methods : Roots of SD, GL and PJ were extracted with distilled water (DW) or 70% ethanol (EtOH). We assessed 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activities of the extracts. To examine neuroprotective effects, we measured cell viability in PC12 or HT22 cells after treatment of the extracts with $H_2O_2$ or amyloid-beta ($A{\beta}$). To assess anti-neuroinflammatory effects, we measured the nitric oxide (NO) levels after treatment with the extracts and lipopolysaccharide (LPS) in BV2 microglial cells. In addition, we performed AChE inhibition assay to explore effects of the extracts on the cholinergic system. Results : DW and EtOH extracts of SD, GL and PJ showed mild DPPH free radical scavenging activities. Also, DW extracts of GL and PJ showed protective effects against $H_2O_2$-induced toxicity in PC12 cells. In LPS-activated BV2 cells, EtOH extracts of SD, GL and PJ exerted inhibitory effects on NO production. Meanwhile, DW extracts of SD, GL and PJ inhibited the $A{\beta}$-induced cell death in HT22 cells. In addition, DW and EtOH extracts of GL exhibited remarkable inhibitory activities on AChE. Conclusions : We demonstrated that SD, GL and PJ exert anti-oxidative, anti-neuroinflammatory and AChE inhibitory activities. These results indicate that SD, GL and PJ could be potential candidates for neurological disorders.

• Applied Biological Chemistry
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• v.49 no.4
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• pp.315-321
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• 2006

Inhibitors of acetylcholinesterase(AchE), such as organophosphates and carbamates, interfere the action of AchE in nerve and may lead to a severe impairment of nerve functions or even death. Therefore, insect AchE is the biological target of predominant insecticides used in agriculture. Biosensors are sensitive and can be used as dispoisable sensors for environmental control. In recent years, the use of AchEs in biosensor technology has gained enormous attention, in particular with respect to insecticide detection. The principle of biosensors using AchE as a biological recognition element is based on the inhibition the catalytic activity by the agents to be detected. We here present a strip-type biosensor based on AchE inhibition. In this study, acetylcholinesterase and PVA-SbQ(polyvinyl alcohol functionalized with methyl pyridinium methyl sulfate) were co-immobilized on immobilone-P membranes. Immobilization of the enzymes showed a stability in 6 months without activity loss in $4^{\circ}C$ storage. Enzymes immobilized on surfaces of membrane responded to organophosphates and carbamate more sensitivitive than enzyme in solution. Organophosphates and carbamates concentrations could be detected by entrapped and surface immobilized enzymes, in 5 min. For chlorpyrifos, carbofuran, cabaryl, and methidathion, the detection limits of AChE-strip were similar to that of HPLC/GC method.

• 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.

• Journal of The Korean Society of Clinical Toxicology
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• v.6 no.2
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• pp.83-90
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• 2008

Organophosphate (OP) pesticides are the most common source of human toxicity globally, causing high mortality and morbidity despite the availability of atropine as a specific antidote and oximes to reactivate acetylcholinesterase. The primary toxicity mechanism is inhibition of acetylcholinesterase (AchE), resulting in accumulation of the neurotransmitter, acetylcholine, and abnormal stimulation of acetylcholine receptors. Thus, the symptoms (muscarinic, nicotinic, and central nervous system) result from cholinergic overactivity because of AchE inhibition. OP can also cause rhabdomyolysis, pancreatitis, parotitis, and hepatitis. OP therapy includes decontamination, supportive therapy, and the use of specific antidotes such as atropine and oximes. However, there has been a paucity of controlled trials in humans. Here we evaluated the literature for advances in therapeutic strategies for acute OP poisoning over the last 10 years.

• Food Science and Biotechnology
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• v.17 no.2
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• pp.384-388
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• 2008

Alzheimer's disease (AD) is the most common neurodegenerative disorder and is responsible for more than 50% of all dementia cases. There is significant interest in finding new sources of compounds that inhibit acetylcholinesterase (AChE) to be used in the treatment of AD, since only a few AChE inhibitors, such as galanthamine, physostigmine, and tacrine, are available for clinical use. In the present study, ICR mice were treated with a 1 mg/kg scopolamine, which caused impaired cognitive ability. The steady consumption of a water extract of Chrysanthemum indicum Linne flowers for 3 months significantly prevented the scopolamine induced deficit of the spatial cognitive capability of mice. It also improved long-term memory in mice with amnesia induced by scopolamine, as assessed by the Morris water maze and passive avoidance tests. In addition, water extract consumption significantly decreased AChE activity in mouse brain, leading to inhibition of acetylcholine hydrolysis.

• Journal of Life Science
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• v.19 no.5
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• pp.688-691
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• 2009

The methanol extract of muskmelon (Cucumis melo) has been investigated for its cognition enhancing effects by evaluation of inhibitory activities on acetylcholinesterase, a degrading enzyme of acetylcholine, a brain neurotransmitter, and ${\beta}$- secretase, which forms the ${\beta}$-amyloid toxic protein from its precursor protein. A passive avoidance task, one of the animal model experiments for learning and memory, was also performed. As a result, the melon extract showed 15.8% and 35.3% inhibition on acetylcholinesterase and ${\beta}$-secretase, respectively, with a final concentration of 100 mg/ml. In the animal model test, melon extract significantly (p<0.05) lengthened the step-through latency time by 22.7% compared to the control group, suggesting that melon extract has, indeed, an effect on cognition enhancement.

• Journal of Oriental Neuropsychiatry
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• v.13 no.1
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• pp.53-77
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• 2002

Alzheimer's disease(AD) is a progressive neurodegenerative disease, which is pathologically characterized by neuritic plaques and neurofibrillary tangles associated with the acetylcholinesterase, apolipoprotein E and butylcholinesterase, and by mutations in the presenilin genes PS1 and PS2, and amyloid precursor proteins (APPs) overexpression. The present research is to examine the inhibitory effect of KGBH on PS1, PS2 and APPs overexpression detected by Western blotting. To verify the Effects of KGBH on cognitive deficits further, we tested it on the scopolamine(1mg/kg)-induced amnesia model of the mice using the Morris water maze tests, and there were ameliorative effects on memory impairment as a protection against scopolamine. KGBH only partially blocked the increase in blood serum level of acetylcholinesterase and Uric acid induced by scopolamine, where as blood glucose level was shown to attenuate the amnesia induced by scopolamine and inreased extracellular serum level. In conclusion, studies of KGBH that has been known as anti-choline and inhibitory ablilities of APPs overexpression, could also be used further as a important research data for a preventive and promising symptomatic treatment for Alzheimer's disease.

• Journal of Oriental Neuropsychiatry
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• v.13 no.2
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• pp.149-171
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• 2002

Alzheimer's disease(AD) is a progressive neurodegenerative disease, which is pathologically characterized by neuritic plaques and neurofibrillary tangles associated with the acetylcholinesterase, apolipoprotein E and butylcholinesterase, and by mutations in the presenilin genes PS1 and PS2, and amyloid precursor proteins (APPs)'s overexpression. The present research is to examine the inhibitory effect of CWBD on PS1, PS2 and APPs's overexpression detected by Western blotting. To verify further the effects of CWBD on cognitive deficits, we tested it on the scopolamine(1mg/kg)-induced amnesia model of the mice using the Morris water maze tests, and there were ameliorative effects on memory impairment as a protection from scopolamine. CWBD only partially blocked the increase in blood serum level of acetylcholinesterase and Uric acid induced by scopolamine, whereas blood glucose level was shown to attenuate the amnesia induced by scopolamine and increased extracellular serum level. In conclusion, studies of CWBD that has been known as anti-choline and inhibitory ablilities of APPs's overexpression could also be used further as a important research data for a preventive and promising symptomatic treatment for Alzheimer's disease.

• Korean Journal of Pharmacognosy
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• v.23 no.2
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• pp.106-114
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• 1992

The acute toxicity and the effect of steam distillate obtained from several plant mixtures (G-3) on the reactivation of brain, lung, and blood acetylcholinesterase (AChE) activity, and recovery from other toxic symptoms following intoxication by organophosphate pesticides were investigated in mice and mudfish. Administration of G-3 $(50{\sim}100\;ml/kg,\;i.p.)$ immediately or 30 min prior to Diazinon or Sumithion treatments, respectively, resulted in a significant reactivation of AChE activity in brain, lung, and blood, their potencies being almost equipotent to those of 2-PAM, one of well-known antidotes. G-3 itself exhibited almost no acute toxicity even at the highest dose employed, and without effect on the inhibition of hepatic drug metabolism function following organophosphate administrations. G-3 showed a significant diminution of the death rate in mudfish as well as in mice intoxicated by Diazinon.

• International Journal of Industrial Entomology and Biomaterials
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• v.1 no.1
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• pp.73-78
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• 2000

We investigated some biochemical properties of acetylcholinesterase (AChE) in the Bombyx mori larval head. 1% Triton X-100 (v/v) was suitable for extracting AChE from the silkworm larval head but 1 M NaCl was not suitable. PAGE analysis showed a single band of AChE that was detected by histochemical staining using acetylthiocholine as a substrate. AChE was also partially purified with Sepharose 6B and DEAE-cellulose column. Finally, the specific activity of partially purified enzyme solution was 7.6. The study on inhibitor specificity indicated that the enzyme under study was a true cholinesterase (ChE) or AChE. AChE activity was maximum at the substrate concentration of $5{\times}10^{-4}$ M and the excess substrate inhibited the AChE activity. The optimal pH and temperature were pH 7.0-9.0 and 30-35$^{\circ}C$.