• CELLMED
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• v.4 no.2
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• pp.11.1-11.6
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• 2014

Cinnamomum zeylanicum (C. zeylanicum) is a tropical evergreen tree of Lauraceae family. It is one of the oldest culinary spices known and used traditionally in many cultures for centuries. In addition to its culinary uses, cinnamon also possesses as a folk remedy of many health disease condition including analgesic, antiseptic, antispasmodic, aphrodisiac, astringent, carminative, haemostatic, insecticidal, and parasiticide and memory enhancing property. This study was aimed to assess the acetylcholinesterase and butyrylcholinesterase inhibitory activity of standardized methanol extract of the C. zeylanicum. Gas chromatography - mass spectrometry (GC-MS) and high performance liquid chromatography (HPLC) analysis were done to identify the presence of eugenol as chemical component and support the neuroprotective activity in the extract. Anticholinesterase inhibitory activity of crude methanol extract of C. zeylanicum leaves and cinnamon oil were evaluated by 96-well microtiter plate assay and thin layer chromatography bioassay detection methods. This study revealed that cinnamon oil ($IC_{50}:45.88{\pm}1.94{\mu}g/ml$) has better anticholinesterase activity than methanol extract ($IC_{50}:77.78{\pm}0.03{\mu}g/ml$). In HPLC analysis, retention time of eugenol in cinnamon oil was found to be 15.81 min which was comparable with the retention time (15.99 min) of the reference standard, eugenol. Seven chemical compounds were identified by GC-MS analysis, in which eugenol as an important phytoconstituents. Thus the phytochemicals from C. zeylanicum methanol leaves extract could be developed as potential source of anticholinesterase activity, with particular benefit in the symptomatic treatment of Alzheimer's disease.

• Preventive Nutrition and Food Science
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• v.22 no.2
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• pp.107-117
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• 2017

The purpose of this study was to evaluate the antioxidant and anticholinesterase activities of yellow and white bitter yams from South Western Nigeria using methanolic extraction and simulated gastrointestinal digestion models. The phenolic compounds in the bitter yam varieties were evaluated by high performance liquid chromatography with a diode array detector (HPLC-DAD). The total phenolic content of the bitter yams was measured by the Folin-Ciocalteu method, reductive potential by assessing the ability of the bitter yam to reduce $FeCl_3$ solution, and the antioxidant activities were determined by the 2,2-diphenyl-1-picrylhydrazyl radical ($DPPH^{\cdot}$) scavenging activity, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation ($ABTS^{{\cdot}+}$) scavenging activity, nitric oxide radical ($NO^{\cdot}$) scavenging ability, hydroxyl radical scavenging ability, and ability to inhibit $Fe^{2+}$-induced lipid oxidation. The HPLC-DAD analysis revealed the presence of some phenolic compounds in the studied bitter yam varieties, with varying degree of quantitative changes after cooking. The antioxidant indices (total phenolic content, total flavonoid content, reducing power, $DPPH^{\cdot}$ scavenging activity, $ABTS^{{\cdot}+}$ scavenging activity, and $NO^{\cdot}$ scavenging activity) were higher in the simulated gastrointestinal digestion model compared to the methanolic extract, with the in vitro digested cooked white bitter yam ranking higher. Similarly, the in vitro digested yams had a higher inhibitory action against lipid oxidation compared to the methanolic extracts, with the cooked white bitter yam ranking high. The methanolic extracts and in vitro enzyme digests showed no acetylcholinesterase inhibitory abilities, while methanolic extracts and the in vitro enzyme digest displayed some level of butyrylcholinesterase inhibitory activities. Therefore the studied bitter yams could be considered as possible health supplements.

• Journal of Yeungnam Medical Science
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• v.16 no.2
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• pp.326-332
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• 1999

Background: In korea the agricultural community widely uses organophosphorous, and organophosphorous poisonings are increasing every year. We compared change in activity of acetylcholinesterase and pseudocholinesterase by organophosphorous and by the interaction of ethanol and organophosphorous. We also compared the effect of reversible anticholinesterase drugs, physostigmine and neostigmine The object of this study is to investigate the effects of several anticholinesterase drugs and on how ethanol influences the activity of cholinesterase. Materials and Methods: Fifteen male university students were randomly selected, and blood samples were taken from the antecubital vein. The acetylcholinesterase in the RBC and the pseudocholinesterase in the serum were extracted and separated. The enzyme activity change was measured by the electrometric method. After adding acetylcholine, the pH change was measured with a pH meter. Results and Conclusion: Our results indicated that reversible anticholinesterase drugs decreased the cholinesterase activity more efficiently than organophosphorous. The acetyl cholinesterase and pseudocholinosterase activity were decreased by ethanol. When ethanol was added, oxime a cholinesterase activator, increased acetylcholinesterase activity but does not increased pseudocholinesterase activity.

• CELLMED
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• v.2 no.2
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• pp.19.1-19.6
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• 2012

$Capparis$ $zeylanica$ Linn. a 'Rasayana' drug is used for its memory enhancing effects in the traditional Ayurvedic system of medicine. The aim of this study was to evaluate acetylcholinesterase (AChE) inhibitory and memory enhancing activities of $Capparis$ $zeylanica$ Linn. The$in-vitro$ and $ex-vivo$ models of AChE inhibitory activity were used along with Morris water maze test to study the effect on memory in rats. The anticholinesterase effect of methanolic and aqueous extracts of $Capparis$ $zeylanica$ was measured by spectrophotometric Ellman method at 0.1, 0.3, 1.0, 3.0, 10 and 30 mg/ml and brain monoamine oxidase (MAO-A and MAO-B) activity was assessed by Naoi's method. The results $in-vitro$ and $ex-vivo$ AChE assay revealed that methanolic and aqueous extracts of $Capparis$ $zeylanica$ inhibit AChE activity, whereas these extracts did not alter MAO activity at any concentration tested as compared to moclobemide and L-deprenyl. The results indicate that $Capparis$ $zeylanica$ improves scopolamine-induced memory deficits through inhibition of AChE activity, and not by direct MAO inhibition.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.7
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• pp.2763-2769
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• 2015

Background: Cancer is an unnatural type of tissue growth in which the cells exhibit unrestrained division, leading to a progressive increase in the number of dividing cells. It is now the second largest cause of death in the world. The present study concerned antioxidant, anticancer and anticholinesterase activities and protocatechuic, catechin, caffeic acid, syringic acid, p-coumaric acid and o-coumaric concentrations in methanol extracts of flowers, fruits and seeds of Hypericum amblysepalum. Materials and Methods: Antioxidant properties including free radical scavenging activity and reducing power, and amounts of total phenolic compounds were evaluated using different tests. Protocatechuic, catechin, caffeic acid, syringic acid, p-coumaric acid and o-coumaric concentrations in extracts were determined by HPLC. Cytotoxic effects were determined using the MTT test with human cervix cancer (HeLa) and rat kidney epithelium cell (NRK-52E) lines. Acetyl and butyrylcholinesterase inhibitory activities were measured by by Ellman method. Results: Total phenolic content of H. amblysepalum seeds was found to be higher than in fruit and flower extracts. DPPH free radical scavenging activity of the obtained extracts gave satisfactory results versus butylated hydroxyanisole and butylated hydroxytoluene as controls. Reducing power activity was linearly proportional to the studied concentration range: $10-500{\mu}g/mL\;LC_{50}$ values for H. amblysepalum seeds were 11.7 and 2.86 respectively for HeLa and NRK-52E cell lines. Butyryl-cholinesterase inhibitory activity was $76.9{\pm}0.41$ for seed extract and higher than with other extracts. Conclusions: The present results suggested that H. amblysepalum could be a potential candidate anti-cancer drug for the treatment of human cervical cancer, and good source of natural antioxidants.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.248.3-249
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• 2003

A series of tetrahydroaminoacridine and their analogues were synthesized. Tetrahydroaminoacridine(tacrine) is an anticholinesterase agent used in the treatment of Alzheimer's disease. Introduction of piperidine group at the para position enhanced anti-inflamatory activity for Alzheimer's disease. We investigated their ability to inhibit cyclooxygenase-1 and 2 isoforms. (omitted)

• Korean Journal of Veterinary Research
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• v.4 no.1
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• pp.15-17
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• 1964

Scabby burley collected in Kyong Sang Nam Do fed to healthy dogs, age less than 2 years, old and determined the Choline-Esterase Activity in blood of dogs. The results obtained in this investigation are summarized as follows. 1. Choline-Esterase Activity in the blood of dogs fed Scabby barley has been decreased. 2. The poisionous component of the Scabby barley thought to be Anticholinesterase.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.856-859
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• 2002

In the course of finding Korean natural products for acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the roots of Angelica dahurica showed significant inhibitory effects on AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of three furanocoumarins, isoimperatorin (1), imperatorin (2) and oxypeucedanin (3), as active principles. These compounds inhibited AChE activity in a dosedependent manner, and the $IC_{50}$ values of compounds 1-3 were 74.6, 63.7 and 89.1 uM, respectively.

• Ocean and Polar Research
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• v.39 no.1
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• pp.45-49
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• 2017

During the search for anticholinesterase compounds from marine organisms, we were able to isolate 6,6'-bieckol from a red alga, Grateloupia elliptica. This compound showed moderate acetylcholinesterase (AChE) inhibitory activity in a micromole range ($IC_{50}$ $44.5{\mu}M$). However, for butyrylcholinesterase (BuChE), a new target for the treatment of Alzheimer's disease (AD), it showed particularly potent inhibitory activity ($IC_{50}$ $27.4{\mu}M$), which is more potent compared to AChE. It also inhibits BACE-1, a new target for reducing the generation of ${\beta}-amyloid$.

• Korean Journal of Food Science and Technology
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• v.36 no.6
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• pp.974-978
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• 2004

Brown-alga-derived natural agent NX42, mainly composed of algal polysaccharides and phlorotannins, showed mild but dose-dependent inhibition of acetylcholinesterase with $IC_{50}=600-700\;{\mu}g/mL$. Phlorotannin-rich fraction of NX42 showed substantial increase of the activity by more than one order of magnitude ($IC_{50}=54\;{\mu}g/mL$) and significant protection of SK-N-SH cells from oxidative stress by $H_2O_2$. Learning trials of mice for 5 consecutive days revealed electric-shock treatment during learning period significantly retarded learning process, whereas NX42-treated mice showed significant resistance against leaning deficiency possibly mainly due to anticholinesterase and neuroprotective activities of phlorotannin.