• Korean Journal of Medicinal Crop Science
• /
• v.17 no.6
• /
• pp.434-438
• /
• 2009

For the development of a new antidementia functional food or alternative drug using agricultural products, Job's tears (Coix lachrymajobi L.), which shows high acetylcholinesterase (AChE) inhibitory activity (55.1%) was selected and the extraction conditions of AChE inhibitor were optimized. AChE inhibitor of Job's tears was maximally extracted when it was treated with 60% methanol at $40^{\circ}C$ for 6 h. The AChE inhibitor of the methanol extracts was partially purified by systematic solvent extraction, thin layer chromatography, silica gel chromatography and reverse-phase HPLC and the partial purified AChE inhibitor with inhibitory activity ($IC_{50}$) of $0.608\;{\mu}g$ was obtained. The partial purified AChE inhibitor was soluble in methanol and hexane, and insoluble in water. Its maximum absorption spectra was 230 nm and also it was stable in the range of $30^{\circ}C$ and $70^{\circ}C$ and pH 4.0-8.0 for 1 h.

• The Korea Journal of Herbology
• /
• v.24 no.4
• /
• pp.121-126
• /
• 2009

Objectives : To evaluate the radical scavenging and acetylcholinesterase (AChE) inhibitory activities of the ethylacetate (EtOAc)-soluble portion of a methanolic extract of Aster yomena, three different assay systems were performed. Methods : The antioxidant activity of A. yomena extract was tested as its capacity to scavenging free radicals of DPPH and $ABTS^+$, which has been widely used to evaluate the antioxidant activity of natural products from plant sources. AChE inhibitory activity was tested against mouse brain AChE by spectrophotometric method of Ellman using ELISA microplate reader. Results : The methanolic extract of A. yomena was fractionated and the EtOAc-soluble portion showed significant AChE inhibitory and free radical scavenging effects. Also the EtOAc-soluble portion revealed the highest phenolic contents as compared to the other extracts. Conclusions : These results indicate that phenolic compounds may be important constituents that give rise to the anti-AChE and antioxidative activities of A. yomena extract. Further phytochemical studies on this plant, for nutraceutical or pharmaceutical application, are warranted.

• Applied Biological Chemistry
• /
• v.38 no.2
• /
• pp.174-178
• /
• 1995

The purpose of this study was to investigate a role of cytochrome $P_{450}$, for the toxicity of the phosalone in in vitro and in vivo bioactivation systems. The bimolecular inhibition rate constants$(k_i)$ of the phosalone to acetylcholinesterase(AChE) and butyrylcholinesterase(BuChE) were approximately $10^2M^{-1}{\cdot}min^{-1}$, respectively, which meant a poor inhibitor. The potency of the phosalone as an inhibitor of AChE and BuChE was increased about 300 and 40 fold, respectively, when the inhibitor and the ChE were incubated with microsomes fortified with NADPH compared with microsome alone. Piperonyl butoxide(PB) addition to these coupled systems greatly reduced the inhibition of both target enzymes by blocking a bioactivation process. The $I_{50}$ value of the Phosalone alone for rat brain AChE was 170 mg/kg. When PB was pretreated, that value was altered to 42.5 mg/kg. PB pretreatment synergized the inhibition of brain AChE with four times. Rat blood erythrocyte AChE and plasma BuChE were similarly inhibited in vivo by the phosalone and PB pretreatment didn't affect significantly the pattern of the inhibition. The in vivo studies showed different results in the role of cytochrome $P_{450}$ from those of the in vitro studies.

• BMB Reports
• /
• v.43 no.8
• /
• pp.573-578
• /
• 2010

Several organophosphorus (OP) insecticides can selectively kill the silkworm maggot, Exorista sorbillans (Es) (Diptera: Tachinidae), while not obviously affecting the host (Bombyx mori) larvae, but the mechanism is not yet clear. In this study, the cDNA encoding an acetylcholinesterase (AChE) from the field Es was isolated. One point mutation (Gly353Ala) was identified. The Es-353G AChE and Es-353A AChE were expressed in baculovirus-insect cell system, respectively. The inhibition results showed that for eserine and Chlorpyrifos, Es-353A AChE was significantly less sensitive than Es-353G AChE. Meanwhile, comparison of the I50 values of eserine, dichlorvos, Chlorpyrifos and omethoate of recombinant Es AChEs with its host (Bombyx mori) AChEs indicated that, both Es AChEs are more sensitive than B. mori AChEs. The results give an insight of the mechanism that some OP insecticides can selectively kills Es while without distinct effect on its host, B. mori.

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

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.41 no.10
• /
• pp.1395-1401
• /
• 2012

This study investigated the cognition-related effects on antioxidant activities, ${\gamma}$-aminobutyric acid (GABA) contents, and AChE inhibitory activities in ethanol extracts from Zingiber officinale Rosc. (Korea), Curcuma longa L. (Korea), Curcuma longa L. (Myanmar), and Curcuma aromatica Salisb. (India). These extracts were investigated to determine the relationships among total polyphenols as well as DPPH and ABTS radical scavenging activities, GABA contents, and acetylcholinestrase (AChE) inhibitory activity. For the results, C. longa L. from Myanmar exhibited the highest contents of curcumin (97.1 ${\mu}g/mg$), total polyphenols (98.4 ${\mu}g/mg$), and GABA (1.31 ${\mu}g/mg$), as well as the strongest radical scavenging activities and AChE inhibitory activity. In addition, C. aromatica Salisb from India, which had the highest total polyphenol content (98.4 ${\mu}g/mg$) and strongest radical scavenging activities, exhibited relatively high AChE inhibitory activity similar to that of C. longa L. from Myanmar. On the other hand, Z. officinale Rosc. and C. longa L. from Korea showed low contents of curcumin (12.2 ${\mu}g/mg$) and polyphenols (85.7 ${\mu}g/mg$), as well as low AChE inhibitory activities. However, we could detect 1.11 ${\mu}g/mg$ of GABA in these extracts, which was similar to that of C. longa L. from Myanmar. Therefore, GABA content was not correlated with AChE inhibitory activity. Based on the results, AChE inhibitory activity is highly correlated with polyphenol contents in Zingibearceae family. Overall, among the Zingiberaceae tested, C. longa L. from Myanmar might be a strong candidate as a cognitive-enhancing ingredient.

• Korean journal of applied entomology
• /
• v.30 no.2
• /
• pp.117-123
• /
• 1991

Acetylcholinesterase(AChE) and esterase activities as mechanisms of resistance to fenobucarb, carbofuran and diazinon in the insecticide-selected brown planthopper strains were investigated. Although there was no significant difference in AChE activity from suscept tible and resistant strains, AChE insensitivity was highly increased in the carbam없e insecticide-selected strains. On the other hand, esterase activity was moderately increa잃d in all the s selected strains. It is concluded that the cross-resistance and the level of resistance in the b brown planthopper can be explained by the combination of altered AChE and high esterase a activity, although a possible involvement of other factor(s) can not be excluded.

• The Korean Journal of Pesticide Science
• /
• v.2 no.2
• /
• pp.10-15
• /
• 1998

The bimolecular inhibition rate constants of carbofuran and N-dimethylphosphinothioyl carbofuran(PSC) to acetylcholinesterase(AChE) were $7.7{\times}10^{5}\;M^{-1}{\cdot}min^{-1}$ and $1.2{\times}10^{3}\;M^{-1}{\cdot}min^{-1}$, respectively. These results showed that PSC required a bioactivation process for its toxic action because it didn't inhibit the target enzyme effectively. The potency of PSC as an inhibitor of AChE increased when PSC and AChE were incubated with microsomes fortified with NADPH compared with microsome alone. Piperonyl butoxide(PBO) addition to these coupled systems greatly reduced the inhibition of the target enzyme by blocking the bioactivation process. In vivo inhibition study of mouse brain AChE, $I_{50}$ value for AChE was 28 mg/kg for PSC and the value increased to 57 mg/kg when PBO was pretreated. This result showed that cytochrome $P_{450}$ would also play a role in the bioactivation process of PSC in vivo. And conversioin of carbofuran from PSC was 55 % in a chemical oxidation system using meta-chloroperoxybenzoic acid. The oxidative activation of PSC to carbofuran was shown to be essential for showing its toxicological action and cytochrome $P_{450}$ was identified as an important enzyme which participated in this process.

• Bulletin of the Korean Chemical Society
• /
• v.35 no.6
• /
• pp.1681-1686
• /
• 2014

A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and 4-amino-1-benzyl piperidines were synthesized and their in vitro cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)) inhibitory activities were evaluated. Even though the parent compounds did not exhibit any inhibitory activity against cholinesterase (ChE) with the exception of compound 14 ($IC_{50}=255.26{\pm}4.41$ against BuChE), all hybrid molecules demonstrated BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, compound 17 was shown to be an effective inhibitor against both AChE ($IC_{50}=1.75{\pm}0.30{\mu}M$) and BuChE ($IC_{50}=5.61{\pm}1.25{\mu}M$) comparable to galantamine ($IC_{50}=1.7{\pm}0.9{\mu}M$ against AChE and $IC_{50}=9.4{\pm}2.5{\mu}M$ against BuChE). Inhibition kinetic studies using compound 17 indicated a mixed inhibition type for AChE and a noncompetitive inhibition type for BuChE. Its binding affinity ($K_i$) values to AChE and BuChE were $3.8{\pm}0.005{\mu}M$ and $7.0{\pm}0.04{\mu}M$, respectively.

• Journal of Nutrition and Health
• /
• v.37 no.3
• /
• pp.176-181
• /
• 2004

This study was designed to investigate the effects of buthanol (BuOH) fraction of pine (Pinus densiflora Sieb et Zucc) needle on cholesterol and lipofuscin (LF) accumulations, acetylcholine (ACh) and its related enzyme activities such as choline acetyltransferase (CAhT) and acetylcholinesterase (AChE), and monoamone oxidase-B (MAO-B) activity, which destroyed the catecholamine-related neurotransmitters in brain membranes of Sprague-Dawley (SD) rats. Male SD rats were fed basic diets (control group) or experimental diets (BuOH-25, BuOH-50 and BuOH-100) for 45 days. Cholesterol accumulations in mitochondria and microsomes were significantly inhibited (about 14 - 17％ and 23 - 34％, respectvely) in BuOH-50 and BuOH-100 groups, whereas LF levels were significantly inhibited (about 10 - 14％) in BuOH-50 and BuOH-100 groups compared with control group. ACh levels and ChAT activities were significantly increased (about 11 - 17％ and 11 - 23％, respectively) in membranes of BuOH-50 and BuOH-100 groups compared with control group. AChE activities were significantly increased (about 14 - 17％) in membranes of BuOH-50 and BuOH-100 groups. There was no significant difference in MAO-B activities between control and experimental diet groups. The results suggest that butanol fraction of pine needle may play an effective role in an antiaging effect and improving a learning and memory impairments.