• Journal of Pharmacopuncture
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• v.22 no.4
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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.

• Natural Product Sciences
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• v.18 no.4
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• pp.233-238
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• 2012

Nine compounds (1 - 9), ${\alpha}$-linolenic acid (1), cis-5,8,11,14,17-elcosapentaenoic acid (2), phytol (3), loliolide (4), uridine (5), thymidine (6), deoxyadenosine (7), adenine (8), and adenosine (9), were isolated from the n-hexane, methylene chloride, ethyl acetate and n-butanol fractions of Capsosiphon fulvescens. The structures of these compounds were elucidated on the basis of spectroscopic evidence. Compounds 1 - 9 exhibited acetylcholinesterase (AChE) inhibitory activities with $IC_{50}$ values ranging from 114.91 to $252.40{\mu}M$, whereas 2 - 4 showed butyrylcholinesterase (BChE) inhibitory activities with $IC_{50}$ values ranging from 251.18 to $499.16{\mu}M$.

• Korean Journal of Pharmacognosy
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• v.47 no.2
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• pp.192-196
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• 2016

The herb of Agastache rugosa (Lamiaceae) called Korean mint as a spice or Agastache Herba as a crude drug is known to contain highly fragrant volatile substances. This research aimed to establish the quantitative gas chromatography (GC) method on the essential oil of A. rugosa using the three standard compounds, estragole, methyleugenol, pulegone, and to find whether the essential oil has anti-Alzheimer's activity. The GC quantification method was established by determining the linearity of calibration curve ($R^2$), linear range, and both limit-of-detection (LOD) and limit-of-quantification (LOQ). The $IC_{50}$ of the essential oil on the activities of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) were determined to be $69.06{\pm}0.26$ and $76.71{\pm}0.58{\mu}g/ml$, respectively.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.30 no.4
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• pp.614-619
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• 1997

This study was designed to investigate the biochemical pollutant markers for diagnosis of marine pollutions by changes in cholinesterase activity of the flounder (Pleuronichthys cornutus) in the Yellow Sea of Korea. Acetylchotinesterase (AChE) activities in brain and muscle of wild flounders in the Yellow Sea were significantly lower $(20\~30\%\;and\;10\~40\%,\;respectively)$ than those of wild flounder in Pohang (control) of the last Sea. Butyrylcholinesterase (BChE) activities in brain and muscle of wild flounders in the Yellow Sea were significantly lower $(10\~30\%\;and\;35\~45\%,\;respectively)$ than those of wild flounder in Pohang of the East Sea. lactate dehydrogenase (LDH) activities in serum of wild flounders in the yellow Sea were significantly $(about\;30\%)$ lower than those of wild flounder in Pohang of the East Sea. These results suggest that AChE and BChE activities in brain and muscle of wild flounders of the Yellow Sea may be used as the most effective mean in a biochemical marker for diagnosis of pollutant effects by organophosphorus pesticides.

• Journal of Ginseng Research
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• v.36 no.1
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• pp.93-101
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• 2012

This study evaluated the anti-cholinesterases (ChEs) and antioxidant activities of white ginseng (WG) and black ginseng (BG) roots of Panax ginseng (PG), P. quinquefolium (PQ), and P. notoginseng (PN). Ginsenosides $Rg_1$, Re, Rf, $Rb_1$, Rc, $Rb_2$, and Rd were found in white PG, whereas Rf was not found in white PQ and Rf, Rc, and $Rb_2$ were not detected in white PN. The major ginsenoside content in steamed BG including $RK_3$, $Rh_4$, and 20(S)/(R)-$Rg_3$ was equivalent to approximately 70% of the total ginsenoside content. The WG and BG inhibited acetylcholinesteras (AChE) and butyrylcholinesterase (BChE) in a dose dependent manner. The efficacy of BG roots of PG, PQ, and PN on AChE and BChE inhibition was greater than that of the respective WG roots. The total phenolic contents and 2, 2-diphenyl-1-picryl-hydrazyl (DPPH) scavenging activity were increased by heat treatment. Among the three WG and BG, white PG and steamed black PQ have significantly higher contents of phenolic compounds. The best results for the DPPH scavenging activity were obtained with the WG and BG from PG. These results demonstrate that the steamed BG roots of the three studied ginseng species have both high ChEs inhibition capacity and antioxidant activity.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.255.3-256
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• 2003

Marine Algae of order Chordariales are rich resources of bioactive metabolites. Methanolic extracts of the brown alga /shige Okamurae exhibited potent antioxidative and butyrylcholinesterase(BChE) inhibitory effects. Bio-guided purification [solvent partition, ODS flash, silica flash, gel-filtration on Sephadex LH 20, ODS HPLC] of them gave a compound 1. Its structure was elucidated by detailed analysis of spectroscopic data of 1 and comparison of literature data. A variety of bioassay for 1 is in progress.

• Journal of Life Science
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• v.12 no.1
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• pp.32-42
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• 2002

It was researched to react horse serum-BChE with hefanoylthiocholine chosen among choline esters. According as number of carbon of acyl group in choline esters was increased, reactivity was decreased but strength of ES complex was increased (Km=0,140mM). The pH-V/K profile for BChE-catalyzed hydrolysis of hexanoylthiocholine yields a p $K_{a}$ =4.974$\pm$0.028. This value is equal to recent literature that shows systematic shift from dependence of activity on the basic form fo a residue that huts a p $K_{a}$ =6.2~6.4 to catalysis by a residue or residues that has a p $K_{a}$ =4.7~5.0. The resulting kinetic solvent isotope effect of hexanoylthiocholine is $^{D/V}$K=1.18. The magnitude of the isotope effect suggests that proton transfer is not an element of transition-state stabilization.n.

• Natural Product Sciences
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• v.24 no.4
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• pp.259-265
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• 2018

The three flavone glycosides, 4'-O-methylisoscutellarein 7-O-(6'''-O-acetyl)-${\beta}$-D-allopyranosyl(1${\rightarrow}$2)-${\beta}$-D-glucopyranoside (1), isoscutellarein 7-O-(6'''-O-acetyl)-${\beta}$-D-allopyranosyl(1${\rightarrow}$2)-${\beta}$-D-glucopyranoside (3), and isoscutellarein 7-O-${\beta}$-D-allopyranosyl(1${\rightarrow}$2)-${\beta}$-D-glucopyranoside (4) in addition to a flavonol glycoside, kaempferol 3-O-${\beta}$-D-glucopyranoside (astragalin, 2), were isolated from Stachys japonica (Lamiaceae). In cholinesterase inhibition assay, compound 1 significantly inhibited aceylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities ($IC_{50}s$, $39.94{\mu}g/ml$ for AChE and $86.98{\mu}g/ml$ for BChE). The content of isolated compounds were evaluated in this plant extract by HPLC analysis. Our experimental results suggest that the flavonoid glycosides of S. japonica could prevent the memory impairment of Alzheimer's disease.

• Natural Product Sciences
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• v.26 no.2
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• pp.165-170
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• 2020

Carica papaya is a medicinal and fruit plant owing biological activities including antioxidant, antiviral, antibacterial and anticancer. The present study aims to investigate the acetyl (AChE) and butyryl (BChE) cholinesterase inhibitory potentials of C. papaya extracts as well as their chemical compositions. The chemical composition of the active extract was identified using a gas chromatography-mass spectrometry (GC-MS). Ellman enzyme inhibition assay showed that the alkaloid-enriched leaf extract of C. papaya possessed significant anti-BChE activity with an enzyme inhibition of 75.9%. GC-MS analysis showed that the alkaloid extract composed mainly the carpaine (64.9%) - a major papaya alkaloid, and some minor constituents such as aliphatic hydrocarbons, terpenes and phenolics. Molecular docking of carpaine revealed that this molecule formed hydrogen bond and hydrophobic interactions with choline binding site and acyl pocket. This study provides some preliminary findings on the potential use of C. papaya leaf as an herbal supplement for the prevention and treatment of Alzheimer's disease.

• Korean Journal of Clinical Laboratory Science
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• v.50 no.3
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• pp.225-235
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• 2018

Phellinus gilvus is a medicinal mushroom used that has been used in folk medicine in Asian countries for centuries. The aim of this study was to investigate the anti-xanthine oxidase, anti-cholinesterase, and anti-inflammatory activities of methanol (ME) and hot water (HW) extracts prepared from fruiting bodies of Ph. gilvus. ME and HW had good anti-xanthine oxidase (XO) activities compared to allopurinol, an inhibitor of xanthine oxidase. ME showed comparable and slightly lower inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), respectively, than galanthamine, a standard AChE and BChE inhibitor. ME also showed a protective effect against glutamate-induced cytotoxicity at 40 mg/mL and 100 mg/mL in PC-12 cells. ME (0.5~2.0 mg/mL) significantly inhibited nitric oxide (NO) production in RAW 264.7 murine macrophage cells stimulated with lipopolysaccharide (LPS). Carrageenan-induced hind-paw edema in rats was significantly reduced 2~6 hr after treatment with 50 mg/kg of ME, which was comparable to administration of 5 mg/kg of indomethacin, the positive control. These results demonstrate that ME and HW of Ph. gilvus fruiting bodies possess good anti-xanthine oxidase, anti-cholinesterase, and anti-inflammatory activities.