• Fisheries and Aquatic Sciences
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• 제14권2호
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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.

• Fisheries and Aquatic Sciences
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• 제14권4호
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• pp.289-293
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• 2011

The antioxidant and cholinesterase inhibitory activities of methanol, pretanol, and acetone extracts of Eupausia superba were investigated and their bioactivities compared. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis[3-ethylbenzthiazoline-6-sulfonic acid] ($ABTS^+$) radical-scavenging activities and reducing power assays were used to determine antioxidant activities, and Ellman's colorimetric methods were applied to evaluate cholinesterase inhibitory activity. Although all extracts were positive, Acetone extract of E. superba showed the highest activities. However, these showed moderate or no inhibitory activity against butyrylcholinesterase. Moreover, the total carotenoid contents of the organic solvent extracts followed the same order as their antioxidant and acetylcholinesterase inhibitory activities. These results suggest that E. superba is a potential source of natural antioxidants and cholinesterase inhibitors.

• Fisheries and Aquatic Sciences
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• 제17권4호
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• pp.421-425
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• 2014

The antioxidant and cholinesterase inhibitory activities of the acetone and dichloromethane ($CH_2Cl_2$) extracts of the by-products (heads, shells, and tails) of Pandalus borealis, Pandalus hypsinotus, and Pandalopsis japonica belonging to the family Pandalidae were investigated and their bioactivities were compared. The antioxidant and cholinesterase inhibitory activities of the organic solvent extracts of three shrimp by-products were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-Azino-bis[3-ethylbenzothiazoline-6-sulfonic acid] ($ABTS^+$) radical scavenging activities, reducing power and xanthine oxidase (XO) inhibitory activity assays and Ellman's colorimetric method. The extracts of P. hypsinotus exhibited the highest antioxidant and cholinesterase inhibitory activities. The acetone extracts showed more potent activities toward antioxidant and cholinesterase inhibition compared with the $CH_2Cl_2$ extracts. Furthermore, the total carotenoid contents of the acetone extracts were higher than those of the $CH_2Cl_2$ extracts. Thus, the carotenoid contents may affect antioxidant and cholinesterase inhibition. Our results suggest that the shrimp by-products could act as a nutraceutical agent to prevent oxidative stress and Alzheimer's disease.

• Mycobiology
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• 제44권4호
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• pp.291-301
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• 2016

Culinary mushroom Pleurotus pulmonarius has been popular in Asian countries. In this study, the anti-oxidant, cholinesterase, and inflammation inhibitory activities of methanol extract (ME) of fruiting bodies of P. pulmonarius were evaluted. The 1,1-diphenyl-2-picryl-hydrazy free radical scavenging activity of ME at 2.0 mg/mL was comparable to that of butylated hydroxytoluene, the standard reference. The ME exhibited significantly higher hydroxyl radical scavenging activity than butylated hydroxytoluene. ME showed slightly lower but moderate inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase than galantamine, a standard AChE inhibitor. It also exhibited protective effect against cytotoxicity to PC-12 cells induced by glutamate ($10{\sim}100{\mu}g/mL$), inhibitory effect on nitric oxide (NO) production and inducible nitric oxide synthase protein expression in lipopolysaccharide-stimulated RAW 264.7 macrophages, and carrageenan-induced paw edema in a rat model. High-performance liquid chromatography analysis revealed the ME of P. pulmonarius contained at least 10 phenolic compounds and some of them were identified by the comparison with known standard phenolics. Taken together, our results demonstrate that fruiting bodies of P. pulmonarius possess antioxidant, anti-cholinesterase, and inflammation inhibitory activities.

• Natural Product Sciences
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• 제17권2호
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• pp.108-112
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• 2011

Several isoquinoline alkaloids (1 - 18), which have basic chemical structures as protoberberine and aporphine skeletones, were evaluated for their inhibitory activities on AChE and BuChE. Among them, compounds 3, 4, 6, 8 and 12 showed the potent AchE activity with the $IC_{50}$ values ranging from $10.2{\pm}0.5\;{\mu}M$ to $24.5{\pm}1.6\;{\mu}M$, meanwhile, compound 14 - 17 exhibited strong inhibitory activity with $IC_{50}$ values from $2.1{\pm}0.2$ to $5.5{\pm}0.3\;{\mu}M$. Compounds 14 - 17 exhibited selective inhibition for AChE compared with BuChE. The isoquinoline alkaloid possesses aromatic methylenedioxy groups and quaternary nitrogen atoms are crucial for the anti-cholinesterase inhibitory activity.

• Bulletin of the Korean Chemical Society
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• 제34권11호
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• pp.3322-3326
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• 2013

A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and benzyl piperazines were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibitory activities were evaluated. Even though the parent compounds did not show any inhibitory activity against cholinesterase (ChE), all hybrid molecules showed BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, ALA-1-(3-methylbenzyl)piperazine (15) was shown to be an effective inhibitor of both BuChE ($IC_{50}=2.3{\pm}0.7{\mu}M$) and AChE ($IC_{50}=30.31{\pm}0.64{\mu}M$). An inhibition kinetic study using compound 15 indicated a mixed inhibition type. Its binding affinity ($K_i$) value to BuChE is $2.91{\pm}0.15{\mu}M$.

• 한국자원식물학회지
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• 제31권1호
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• pp.10-15
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• 2018

황칠나무 잎과 줄기를 분리하여 각각 methanol 추출하여, 계통분획상법에 따라 dichloromethane, ethyl acetate, butanol로 분획하였다. 분획물로 실시한 TLC에서 알칼로이드 성분으로 분리되는 성분을 확인할 수 있었다. 잎과 줄기 모두 ethyl acetate분획물은 $IC_{50}$ $30{\mu}g/m{\ell}$으로 높게 측정 되었으며, ethyl acetate, dichloromethane, butanol분획물 순으로 저해 활성이 높게 나타났다. Acetyl cholinesterase inhibition assay를 실시한 결과 황칠나무 잎과 줄기 모두 dichloromethane, ethyl acetate, butanol 분획물 순으로 저해 활성이 높은 것으로 나타났으며, 가장 높은 활성을 보인 황칠나무 줄기와 잎의 dichloromethane 분획물의 알칼로이드 함량이 상대적으로 높은 것으로 보아 알칼로이드 성분에 의한 것으로 유추 할 수 있으므로, 알칼로이드 성분의 동정 및 성분구조의 규명을 통하여 AChE저해 활성을 이용한 신경관련 질환에 도움을 줄 수 있는 천연물의 개발이 가능할 것으로 사료된다.

• Natural Product Sciences
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• 제25권2호
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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.

• Bulletin of the Korean Chemical Society
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• 제35권6호
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• pp.1681-1686
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• 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.

• 대한약침학회지
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• 제22권4호
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• pp.231-238
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• 2019

Objectives: Alzheimer's disease (AD), an overwhelming neurodegenerative disease, has deleterious effects on the brain that consequently causes memory loss and language impairment. This study was intended to investigate the neuroprotective activity of the two essential oils (EOs) from Iranian Pistacia khinjuk (PK) leaves and Allium sativum (AS) cloves against β-Amyloid 25-35 (Aβ25-35) induced elevation of cholinesterase enzymes in AD. Methods: The EOs of PK (PKEO) and AS (ASEO) were prepared and analyzed in terms of extraction yield, phenolic content, and cholinergic markers in vitro. Moreover, both were administered orally to adult male Wistar rats at concentrations of 1, 2, and 3%. The inhibitory potential of PKEO and ASEO was compared with Donepezil (0.75 mg/kg) against the high activities of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Results: PKEO reached an inhibition rate of 83.6% and 81.4% against AChE and BChE, respectively. ASEO had lower anti-cholinesterase activity (65.4% and 31.5% for the inhibition AChE and BChE). PKEO was found to have more phenolic content than ASEO. A significantly positive correlation was observed between the total phenolics and anti-cholinesterase potential. In rats, both EOs decreased the enzyme activity in a concentration-dependent manner. As compared with Donepezil, the significant difference in the AChE and BChE inhibition occurred as rats were treated with PKEO 3% (p < 0.05). Conclusion: It could be concluded that PKEO and ASEO are potent inhibitors of AChE and BChE in rats that hold promise to be used for the treatment of AD.