• Korean Journal of Environmental Agriculture
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• v.14 no.2
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• pp.171-178
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• 1995

The purpose of this study was to investigate the identification and the toxicological effects of some impurities present in the technical grade phosalone (94.4%). In instrumental analyses of the technical phosalone, the five impurities such as phosalone oxon, 6-chloro-3-methylthio-2-oxobenzoxazole, 6-chloro-2-oxobenzoxazole, O,O,S-triethyl phosphorodithioate (OOSTEPDT) and dichlorophosalone were identified. The bimolecular inhibition rate constants ($k_i$) indicated that the technical phosalone inhibited both AChE and BuChE about ten times faster than the purified phosalone did. From in vivo studies the technical phosalone showed greater inhibition for mouse brain AChE, rat blood ChE's and mouse cytosolic non-specific esterases. It was presumed that some impurities present in the technical phosalone such as phosalone oxon cause such inhibition patterns of the technical phosalone observed in this study.

• The Korean Journal of Pesticide Science
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• v.7 no.1
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• pp.45-50
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• 2003

This study was conducted to understand the role of oxidative enzyme cytochrome $P_{450}$ in the bioactivation of benfuracarb and to know metabolites of benfuracarb by cytochrome $P_{450}$. The bimolecular imhibition rate constant $(k_i)$ of benfuracarb on acetylcholinesterase (AChE) was as low as $1.1{\times}10^3\;M^{-1}\;min^{-1}$, suggesting that benfuracarb should be activated for its toxic action. The potency of benfuracarb on AChE in the oxidase system (cytochrome $P_{450}$ + NADPH) in vitro was 10-fold higher than that of control (cytochrome $P_{450}$). Such a similar result was also found in the oxidase + PBO system. In vivo the $I_{50}$ of benfuracarb was 22.7mg $kg^{-1}$, but pie-treatment of piperonyl butoxide (PBO) reduced the $I_{50}$ by >100mg $kg^{-1}$. This result suggests that cytochrome $P_{450}$ was involved in the activation of benfuracarb. Using microsomal oxidase system, metabolites of benfuracarb were elucidated. Fifty-eight percent of benfuracarb was converted to carbofuran, a major toxic metabolite, in the oxidase system, while only less than two percent of benfuracarb was converted to carbofuran in the oxidase + PBO system. These results also suggest that cytochrome $P_{450}$ was involved in the activation of benfuracarb. Overall results indicate that cytochrome $P_{450}$ could be involved in the bioactivation of benfuracarb to carbofuran.

• Food Science and Preservation
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• v.19 no.5
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• pp.751-756
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• 2012

Antioxidant capacity and acetylcholinesterase (AChE) inhibitory activity of the aqueous methanolic extract of Rhus javanica were investigated in vitro. The antioxidant properties was measured by radical scavenging assays using DPPH and $ABTS^+$ radicals. The AChE inhibitory efficacy of R. javanica was tested by Ellman's assay and the total phenolic content was determined using a spectrophotometric method. All tested samples showed a dose-dependent AChE inhibitory and radical scavenging activities. In particularly, ethyl acetate (EtOAc)-soluble portion from the methanolic extract of R. javanica showed significantly higher inhibitory activity than other organic solvent soluble-portions in an AChE and radical scavenging assay systems. These results suggest that R. javanica may be possess potential benefits which might be useful in development of antioxidant and anti-alzheimer's disease ingredient.

• Journal of the Korean Society of Food Science and Nutrition
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• v.41 no.4
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• pp.443-449
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• 2012

This study was conducted to investigate the antioxidant and acetylcholinesterase (AChE) inhibitory activities of extracts from various seaweed. The extracts of $Sargassum$ $thunbergii$ (91.3%), $Polysiphonia$ $morrowii$ (90.7%), $Ecklonia$ $cava$ (89.9%), and $Artemisia$ $fukudo$ (85.9%) showed over 80% high radical scavenging activities at the final concentration of 40 ${\mu}g$/mL. The $Artemisia$ $fukudo$ extract showed the highest inhibition activity of 30.2% on AChE at the final concentration of 10 ${\mu}g$/mL. The extract of $Porphyra$ $tenera$, $Costaria$ $costata$, $Monostroma$ $nitidum$, $Ecklonia$ $cava$, and $Agarum$ $clathratum$ against AChE at a concentration of 10 ${\mu}g$/mL exhibited inhibition of 26.6%, 25.3%, 23.4%, 21.7%, 20.4% and 19.9%, respectively. The bioautography results showed that the mixtures of structurally diverse compounds were thought to affect AChE inhibitory activity. These results suggest that extracts from seaweed with their high quality components may be effective in the prevention of Alzheimer's disease and may be used to develop various functional food products.

• 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.

• Environmental Analysis Health and Toxicology
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• v.17 no.3
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• pp.265-272
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• 2002

This study was carried out with the detection for multiresidue of the organophosphorus pesticides such as malathion, parathion. diazinon, and carbamate pesticide such as carbaryl, by enzyme-inhibition method. The acetylcholinesterase (AChE) and cholinesterase (ChE) activities in chicken brain determined by the Ellman's method were 166.6 and 5.8 $\mu$mol/min/g protein, and in chicken plasma were 23.1 and 8.3 $\mu$mol/min/g protein, respectively. The optimum pH of AChE and ChE was 8.2 and 7.8, respectively. The Km of AChE and ChE was 0.034 and 0.045 mM, respectively. I$\_$50/ for AChE and ChE by some organophosphorus was 55.82 and 99.42 mg/L of malathion, 31.16 and 29.13 mg/L of parathion, and 17.89 and 19.62 mg/L of diazinon, respectively. I$\_$50/ for AChE and ChE by carbaryl of carbamate was 0.10 and 0.05 mg/L, respectively. The 0.07 mg/L of drinking water advisory level for carbaryl could be detected with I$\_$50/ of AChE and ChE. Enzyme-Inhibition (EI) method with AChE and ChE was used the multiresidue method to detect the 1 mg/L of the carbamate pesticides.

• The Korean Journal of Food And Nutrition
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• v.23 no.2
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• pp.226-232
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• 2010

새로운 항치매성 건강식품을 개발하기 위해 아세틸콜린에스터레이즈(AChE)를 강력하게 저해하는 추출물을 곡류와 두류의 다양한 추출물로부터 선발한 후 최적 추출 조건을 조사하였다. 추출물 중 수수 메탄올 추출물이 63.4%의 가장 높은 AChE 저해 활성을 보였다. 수수를 80% 메탄올로 $40^{\circ}C$에서 12시간 추출했을 때 최대의 AChE 저해 활성을 나타내었다. AChE를 저해하는 수수 메탄올 추출물의 영양성과 생리 기능성을 조사하였다. 메탄올 추출물은 유리당으로 고형물 100 g당 4.78 g의 포도당과 4.13 g의 자당 및 0.97 g의 과당을 함유하였다. 또한, 수수 메탄올 추출물의 고형물 100 g에 linoleic acid 273.82 mg, oleic acid 215.65 mg, palmitic acid 122.03 mg, stearic acid 4.96 mg을 함유하고 있었고, 주요 유기산으로 주석산 27.45 mg, 말론산 15.43 mg, 사과산 9.94 mg이 메탄올 추출물 1 g에 함유되어 있었다. 수수 메탄올 추출물은 항치매 활성 외에도 콜레스테롤 합성을 저해하는 HMG-CoA reductase 저해 활성이 50.2%이었고, 항산화 활성은 56.1%를 보였다.

• Korean Journal of Environmental Agriculture
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• v.6 no.2
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• pp.77-83
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• 1987

Present study was carried out to elucidate the effect of phorate (0,0-dietyl S-ethylthiomethyl phosphorodithioate), an organophosphorus insecticide on the acetylcholinesterase(AChE) and cholinesterase(ChE) activity in the chicken brain and plasma. The inhibitory effect of phorate and its metabolites on AChE and ChE activity was also increased in the order of phorate (p=S,S)$(p=S,SO_2)<phoratoxon$ (p=O,S)$(P=O,SO_2)$. Acute oral $LD_{50}$ of phorate was 1.02mg/kg. After oral administration of phorate, the activity of plasma ChE was inhibited more rapidly then that of brain AChE, whereas recovery of plasma ChE activity was more rapid than that of brain AChE activity.

• 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.

• KSBB Journal
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• v.22 no.1
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• pp.30-36
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• 2007

The water-soluble or ethanol-soluble materials extracted from fruit bodies and cultured products (mycelium and broth) of H. erinaceum were prepared, and their inhibitory effect on acetylcholinesterase (AChE) activity from Electrophorous electricus was investigated. Inhibition of 75-85% for AChE activity at concentration of 10 mg/ml was obtained and the mechanism was due to general non-competitive inhibition. Especially, the supernatant of culture broth by ethanol treatment, exhibited a strong inhibition activity of 94% at 10 mg/ml. The samples from fruit body, mycelium and broth (supernatant and precipitate by ethanol treatment) which were extracted from H. erinaceum, were very effective to inhibit the initial stage oxidation of a linoleic acid at concentration of 0.1 mg/ml. The antioxidative activity of these samples were superior than rutin, vitamin C and tocopherol as antioxidative standards by FTC (ferric thiocyanate) method, and also showed the very strong antioxidative activity of 95% without significant difference of the samples by TBA-RS (thiobarbituric acid-reactive substance) method.