• Korean Journal of Pharmacognosy
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• v.43 no.2
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• pp.122-126
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• 2012

The MeOH extract of Evodiae Fructus exhibited a significant inhibition on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), in a dose dependent manner, respectively. The extensive bioactivity-guided fractionation process with the MeOH extract finally isolated four compounds, as rutaecarpine (1), evodiamine (2), limonin (3) and dehydroevodiamine (4). Among them, compound 2 exhibited specific inhibitory activity on BChE with the $IC_{50}$ values 1.7 ${\mu}g/ml$, whereas compound 4 showed the potent inhibition upon both AChE and BChE.

• 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.

• 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.

• Korean journal of applied entomology
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• v.55 no.1
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• pp.27-33
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• 2016

Chlorine dioxide has been used as a disinfectant against microbial pathogens. Recently, its insecticidal activity has been known against stored insect pests by oxidative stress. However, any molecular target of the oxidative stress induced by chlorine dioxide has been not known in insects. This study assessed an enzyme activity of acetylcholinesterase (AChE) as a molecular target of chlorine dioxide in the Indianmeal moth, Plodia interpunctella. AChE activities were varied among developmental stages of P. interpunctella. Injection of chlorine dioxide with lethality-causing doses significantly increased AChE activity of the fifth instar larvae of P. interpunctella. Exposure of the larvae to chlorine dioxide fumigant also significantly increased AChE activity. The fifth instar larvae of P. interpunctella exhibited a negative phototaxis. However, chlorine dioxide treatment significantly interrupted the innate behavior. These results suggest that AChE is one of molecular targets of oxidative stress due to chlorine dioxide in P. interpunctella.

• Journal of Ginseng Research
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• v.34 no.4
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• pp.348-354
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• 2010

Black ginseng and white ginseng were extracted with 80% ethanol and evaluated for relative ginsenoside composition, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, and antioxidant properties. As analyzed by HPLC, black ginseng contained a greater proportion of ginsenoside $Rg_3$ compared to white ginseng. White ginseng was characterized by undetectable ginsenoside $Rg_3$ but it contained more total ginsenosides than black ginseng. Black ginseng extract exhibited higher (p<0.05) free radical-scavenging activity, as well as higher antioxidant activities than white ginseng against 2,2-diphenyl-1-picryl-hydrazyl, superoxide dismutase, and xanthine oxidase, despite the fact that the total saponin content was higher in white ginseng than black ginseng. In addition, the black ginseng extract displayed greater AChE and BChE inhibitory activities. These results suggest that black ginseng has stronger effects on anti-oxidation and AChE and BChE inhibition than white ginseng.

• Journal of the Korean Chemical Society
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• v.60 no.2
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• pp.125-130
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• 2016

With the goal of developing Alzheimer’s disease therapeutics, we have designed and synthesized new triazole linked decursinol derivatives having potency inhibitory activities against cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)]. Since inhibition of cholinesterase (ChE) is still considered to be one of the most effective targets to treat AD patients, many new classes of ChE inhibitors have been synthesized. In an effort of identifying new type of cholinergic drug, decursinol derivatives 11-17 have been synthesized between decursinol and other biological interesting compounds such as lipoic acid, polyphenols, etc by using the click reaction and then evaluated their biological activities. Compound 12 (IC₅₀ = 5.89 ± 0.31 mM against BuChE) showed more effective inhibitory activity against BuChE than galantamine (IC₅₀ = 9.4 ± 2.5 mM). Decursinol derivatives can be considered a new class inhibitor for BuChE and can be applied to be a novel drug candidate to treat AD patients.

• Journal of Oriental Neuropsychiatry
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• v.29 no.3
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• pp.121-134
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• 2018

Objectives: The purpose of this in vivo study is to observe anti-amnesic effects of Yeongkyekamjotanggayonggolmoryo (YGYM), a novel mixed herbal prescription, Ossis Mastodi and Ostreae Testa added Yeongkyekamjo-tang, on scopolamine induced amnesia in C57BL/6 mice through acetylcholine (ACh) and acetylcholinesterase (AChE) activity, Choline acetyltransferase (ChAT) mRNA expression, and antioxidant effects. Methods: Six groups, total 20 intact or 100 Sco treated mice were used in this study after one week of acclimatization period. Half the animals were used for passive avoidance task tests and hippocampus ACh content, AChE activity, and ChAT mRNA expression were measured. The other half was subjected to an underwater maze test and then the cerebral cortex antioxidant defense system was measured. Results: In the passive avoidance experiment, there was significant decrease in residence time in the bright room and in the underwater maze test, escape latency to escape from the esophagus significantly increased compared with the normal control group. At the final sacrifice, ACh content and ChAT mRNA expression decreased, AChE activity increased, and cerebral cortical MDA increased GSH content, SOD and CAT activity in Sco control mice, as compared to intact vehicle control mice. However, these Sco treatment-related memory loss through AChE activation destroyed the cerebral cortex antioxidant defense system, and was inhibited dose-dependently by 28 days consecutive oral pretreatments of YGYM extracts 500, 250, 125 mg/kg. Conclusions: In the above results, YGYM extract that oral administration of YGYM extracts alleviates the antioxidant defense system, through preservation of ACh mediated by upregulation of ChAT mRNA expression, and increase of AChE inhibition and brain antioxidant defense systems.

• Natural Product Sciences
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• v.25 no.2
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• pp.115-121
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• 2019

Alzheimer's disease is a chronic neurodegenerative disorder with no curative treatment. The commercially available drugs, which target acetylcholinesterase, are not satisfactory. The aim of this study was to investigate the cholinesterase inhibitory activity of Solenostemma argel aerial part. Eight compounds were isolated and identified by NMR: kaempferol-3-O-glucopyranoside (1), kaempferol (2), kaempferol-3-glucopyranosyl($1{\rightarrow}6$)rhamnopyranose (3) p-hydroxybenzoic acid (4), dehydrovomifoliol (5), 14,15-dihydroxypregn-4-ene-3,20-dione (6), 14,15-dihydroxy-pregn-4-ene-3,20-dione-$15{\beta}$-D-glucopyranoside (7) and solargin I (8). Two of them (compounds 2 and 3) could inhibit over 50 % of butyrylcholinesterase activity at $100{\mu}M$. Compound (2) displayed the highest inhibitory effect against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with a slight selectivity towards the latter. Molecular docking studies supported the in vitro results and revealed that (2) had made several hydrogen and ${\pi}-{\pi}$ stacking interactions which could explain the compound potency to inhibit AChE and BChE.

• Journal of Environmental Science International
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• v.8 no.1
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• pp.19-26
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• 1999

The degree of pesticides accumulation in tap water in Taejon from June 1995 to Apr 1996 was measured by Ellman's coupled enzyme assay. Since organic phosphate and carbamate pesticides specifically inhibit the neurotransmitter modulating enzyme acetylcholinesterase(AChE), the enzyme activity can be used as a diagnosis for the pesticides accumulation in water and various samples. During the period of this study, the enzyme activity was changed almost every week. The lowest enzyme activity was 64 % of that of the control reaction and there are several days showing about 100 % enzyme activity. In general, the enzyme activity is higher in summer than other seasons especially early spring times. The pH value of tap water was very close to neutral(pH 7.0) and it seems that the enzyme activity was not affected by the small pH changes. Either boiling of tap water or addition of NaOH solution decomposed the pesticide components. These results show that AChE assay is a convenient, sensitive, and reliable method for detection of pesticides in water samples.

• Journal of Life Science
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• v.7 no.1
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• pp.17-23
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• 1997

This study was designed as a part of efforts to investigate the biochemical pollutant markers for diagnosis of maine pollutions by changes in cholinesterase activity of the flounder (Paralichthys olivaceus)in Yellow Sea of Korea. Acetylcholinesterase (AChE) activities in brain and muscle of cultured flounders in Yellow Sea were remarkably lower (40-50% and 40-55%, respectively)than those of wild flounder in Pohang (control) of East Sea, but AChE activities in brain and muscle of wild flounders in Yellow Sea were significantly lower(15-40% and 25-35%, respectively)than those of wild flounder in Pohang of East Sea. Butyrylcholinesterase(BChE) activities in barin and muscle of cultured flounders in Yellow Sea were remarkably lower(70-75% and 65-75%, respectively) than those of wild flounder in Pohang of East Sea, but BChE activities in barin and muscle of wild flounders in Yellow Sea were significantly lower (15-40%and 25-35%, respectively)than those of wild flounder in Pohang of East Sea. Lactate dehydrogenase (LDH) activities in serum of cultured flounders in Yellow Sea were significantly 10-50% higher than those of wild flounder in Pohang of East Sea, but LDH activities in serum of wild flounders in Yellow Sea were significantly 20-25% higher than those of wild flounder in Pohang of East Sea. It suggests that AChE and BChE activities in brain and muscle of cultured and wild flounders of Yellow Sea may be used as the most effective mean in a biochemical markers for diagnosis of pollutant effects by organophosphorus pesticides.