• Applied Biological Chemistry
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• v.42 no.4
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• pp.336-343
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• 1999

Fifty six mycelial cultured Basidiomycetes were screened for their inhibitory effects against prolyl endopeptidase(PEP), acetylcholine esterase(AChE) and thrombus coagulation. Out of them, methanolic extract of mycelium and/or ethylacetate(EtOAc) soluble fraction from culture broth of Peniophora quercina, Amanita aspera, Phellinus chrysoloma, Grifola frondosa, Wolfiporia extensa, Clavicorona pyxidata and Phanerochaete sordida inhibited more than 90% of PEP activity at 40 ppm. The extracts of Lenzites betulina, Phellinus chrysoloma, Wolfiporia extensa, Phanerochaete sorrlida, Hypocrea nigricans, Coriolus azureus, Flammulina velutipes, Phlebiopsis gigantea and Bondarzewia montana exhibited about 40% of inhibitory activity against AChE at 40 ppm. In thrombin times assay, the extracts of Amanita aspera, Oxyporus latemarginata, Peniophora quercina, Fomes fomenfarius, Trametes versicolor, and Phlebiopsis gigantea delayed coagulation of thrombus about two to three times over control at ca 550 ppm. In activated partial thromboplastin times assay, none of the tested Basidiomycetes showed significant effect.

• Journal of The Korean Society of Clinical Toxicology
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• v.7 no.2
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• pp.90-96
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• 2009

Purpose: This study explored and evaluated the systemic complications resulting from the bite of Korean venomous snake, focussing on hematologic and neurologic features. Methods: Medical records (demographic data, clinical measurements including laboratory results, severity score, and amount of antidote administration, and hospitalization course) of consecutive patients who presented with snakebites to two university teaching hospital during a 10-year period were retrospectively reviewed. Subgroup analysis was conducted for evaluations of anti-acetylcholine esterase administration in complicated victims. Results: The 170 patients displayed occurrence rates of hematologic and neurologic complications of 12.9% and 20.6%, respectively. Among 22 patients with hematologic complications, isolated thrombocytopenia was evident in eight patients (36.4%), prothrombin time (PT) / activated partial thromboplastin time (aPTT) prolongation in 11 patients (50.0%), and both in three patients (13.6%). The mean time to recovery was $4.5{\pm}1.8$ days for isolated thrombocytopenia, and $5.1{\pm}1.8$ days for PT and aPTT prolongation. Hematologic complications could occur suddenly 1?4 days after hospitalization. Among 35 patients with neurologic complications, dizziness was evident in 16 patients (45.7%), and diplopia / blurred vision in 19 patients (54.3%). The mean time to recovery was $3.4{\pm}0.6$ days in patients receiving anti-acetylcholine esterase and $6.9{\pm}1.8$ days in those not receiving anti-acetylcholine esterase (p=0.00). Conclusion: Occurrence rates of hematologic and neurologic complications following venomous snake bite differed as compared to other studies conducted in Korea. Onset of hematologic complications can occur rapidly days after admittance. Anti-acetylcholine esterase administration may be effective in treating neurologic complications.

• Journal of agriculture & life science
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• v.45 no.6
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• pp.213-226
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• 2011

This study was performed to investigate the effect of essential oils and ethanolic extracts of approximately 650 plant species on acetylcholine esterase (AChE) enzyme activity using Ellman's colorimetric method in 96-well microplates. The results showed that the ethanolic extracts from twig of Sophora subprostrata, twig of Phellodendron amurense, seed of Corylopsis coreana, and essential oil (EO) from Citrus paradisi, Cupressus sempervirens, Ocimum basilicum, Pinus sylvestris and Rosmarinus officinalis inhibited more than 80% of AChE activity. Among these, EO from Pinus sylvestris, C. sempervirens and C paradisi exhibited higher values of AChE inhibitory activity, which were 75, 84 and 99% at a concentration of 50 ug/ml, respectively. Finally, EO from C paradisi (grapefruit, GEO) showed the highest inhibitory activity towards AChE, which showed 91% of inhibition at a concentration of 20 ug/ml. We also examined the anti-dementia effects of GEO in mouse by passive avoidance test and Morris water maze test. The model mouse (male, ICR) of dementia (negative control) was induced by administration of scopolamine (1 mg/kg body weight). The latency time of sample group administrated with GEO (100 mg/kg, p.o.) increased significantly as compared with negative control on passive avoidance test. There were significant recovery from the scopolamine-induced deficits on learning and memory in water maze test through daily administrations with GEO (100 mg/kg, p.o.). From these results, we conclude that GEO treatment might enhance the cognitive function, suggesting that the EO of C. paradis may be a potential candidate for improvement of perceptive ability and dementia.

• Journal of Physiology & Pathology in Korean Medicine
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• v.25 no.3
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• pp.406-416
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• 2011

In this study, we have verified the memory and cognitive enhancing effect of Longanae Arillus, the fruit of Euphoria longana Lamarck, which has been used as a tonic and for the treatment of amnesia, insomnia, and palpitations in oriental medicine. To investigate the effect of Longanae Arillus water extract(LAE) on the memory and cognitive dysfunction, scopolamine (1 mg/kg, i.p.) was injected in C57BL/6 mice and several behavior tests including Y-maze, Morris water-maze, passive avoidance and fear conditioning tests were conducted. Administration of LAE (100 or 200 mg/kg/day, p.o.) effectively improved scopolamine-induced memory impairment and dysfunction. To further determine the possible molecule mechanism of LAE, we have examined the activity and/or mRNA expression of diverse proteins involved in the acetylcholine metabolism. LAE particularly increased the amount of acetylcholine in the cortex which was mediated by suppression of acetylcholine esterase (AchE) activity. In addition, LAE elevated the mRNA expression of muscarinic acetylcholine receptors (mAchRs) without affecting the mRNA levels of choline acetyltransferase (ChAT) and acetylcholine esterase (AchE). In another experiment, LAE effectively inhibited mRNA expression of pro-inflammatory cytokines such as tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) and interleukin-$1{\beta}$ (IL1-${\beta}$), which seemed to be mediated by inhibition of upstream transcription factor NF-${\kappa}B$ and extracellular-regulated kinase 1/2 (ERK1/2). These results demonstrate that Longanae Arillus can increase acetylcholine amount the cortex via regulation of AchE activity as well as mAchRs expression and decrease pro-inflammatory responses via inhibition of NF-${\kappa}B$ signaling pathway, thereby having therapeutic potential to improve memory and cognitive deficit in amnesia.

• Proceedings of the Korean Society of Life Science Conference
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• 2005.09a
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• pp.77-77
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• 2005

• Journal of Physiology & Pathology in Korean Medicine
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• v.17 no.1
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• pp.50-56
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• 2003

This research was done to make the effective prescription and cope with various senile dementia. So Sprague-Dawley rats were injected with ibotenate to make a damage on learning and memory functions. At first acquisition test and retention rest were done in the Morris water maze. And to evaluate the effects of the sample drug(TBM) on choline acetyltranferase and acetylcholine esterase, immunoreactive measurement and enzymatic activity measuring were carried out. The ibotenic acid were injected to hippocampus CA1 and CA3 area. The results were as following. TBM improved the learning ability in the acquisition test and memory function in the retention test significantly. And TBM increased the level of ChAT which is synthesizing acetylcholine in CA3 area, and at the same time it increased the level of AChE which is resolving acetylcholine. These results show that T8M improved the cholinergic catabolism and anabolism, and the increment of metabolic activity of cholinergic system. In other words, it contributes to the recovery of damaged learning and memory function by ibotenic acid. So it can be concluded that TBM will be helpful to cholinergic brain damage induced by primary or senile reduction of acetylcholine secretive activity.

• Bulletin of the Korean Chemical Society
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• v.33 no.12
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• pp.3943-3949
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• 2012

A series of aromatic hydrazides 3a-j were prepared by refluxing esters 2a-j with hydrazine hydrate in methanol, which were prepared by the esterification of 1a-j. Acetohydrazides 3a-j upon treatment with carbon disulfide and methanolic potassium hydroxide yielded potassium dithiocarbazate salts 4a-j, which on refluxing with hydrazine hydrate yielded substituted 4-amino-5-aryl-3H-1,2,4-triazole-3-thiones 5a-j. The target compounds 6a-j were synthesized by condensing furan-3-carboxylic acid in the presence of polyphosphoric acid under reflux. The structures of newly synthesized compounds were characterized by IR, $^1H$ NMR, $^{13}C$ NMR, elemental analysis and mass spectrometric studies. All the synthesized compounds were screened for their urease, acetylcholine esterase inhibition, antioxidant and alkaline phosphatase inhibition activity. Almost all of the compounds 6a-j showed good to excellent activities against urease and acetylcholine esterase more than the reference drugs. Compounds 6f and 6g were more potent scavenger of free radicals than the reference n-propyl gallate. Compound 6b and 6h showed excellent activities of alkaline phosphatase as compare to the reference $KH_2PO_4$.

• The Korean Journal of Mycology
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• v.26 no.4 s.87
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• pp.519-524
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• 1998

Four minor compounds were isolated from fruiting bodies of Polyozellus multiflex by consecutive chromatographic separation. Their structures were identified as ergost-4,6,8,22-tetraen-3-one, 4-methoxy-6-methyl-2H-pyran-2-one, p-anisic acid, and p-hydroxybenzoic acid by spectral analysis. They could not inhibit prolyl endopeptidase nor acetylcholine esterase at the concentration up to 100 ppm.

• Current Research on Agriculture and Life Sciences
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• v.32 no.2
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• pp.63-66
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• 2014

The effects of a newly developed flower thinning formulation (FTF) on the vitality of the honey bee Apis mellifera were examined by measuring the activities of various digestive enzymes in adult worker bees. First, direct spraying of the FTF solution did not cause any behavioral changes or lethal effects for the honey bees based on 24 h observation. Second, oral ingestion of a sugar solution containing the FTF did not produce any significant change in the activities of amylase, proteinases, lipase, or acetylcholine esterase (AChE) in the worker bees 6 h or 24 h after treatment. Meanwhile, a commercial formulation containing sulfur compounds showed slightly reduced activities for several digestive enzymes and AChE, although no behavioral disturbance. Thus, the results of the present study suggest that the FTF is not toxic for honey bees, in terms of contact and ingestion. Therefore, this newly developed FTF can be used for flower thinning without any detrimental effects on pollinating insects.

• Journal of Physiology & Pathology in Korean Medicine
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• v.16 no.6
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• pp.1151-1156
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• 2002

This research was done to make the effective prescription and cope with various senile dementia. Sprague-Dawley rats were injured by ibotenic acid to make a damage on learning and memory functions of model rats. At first acquisition test and retention rest were done in the Morris water maze. And to evaluate the effects of the sample drug(GSD) on choline acetyltranferase and acetylcholine esterase, immunoreactive measurement and enzymatic activity measuring were carried out. The ibotenic acid were injected to hippocampus CA1 and CA3 area. Conclusion : GSD improved the learning ability in the acquisition test and memory function in the retention test significantly. And GSD increased the level of ChAT which is synthesizing acetylcholine in CA1 area, and at the same time it increased the level of AChE which is resolving acetylcholine. These results show that GSD improved the cholinergic catabolism and anabolism, and the increment of metabolic activity of cholinergic system. In other words, it contributes to the recovery of damaged learning and memory function by ibotenic acid. So it can be concluded that GSD will be helpful to cholinergic brain damage induced by primary or senile reduction of acetylcholine secretive activity.