• The Journal of Korean Medicine
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• v.39 no.3
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• pp.1-16
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• 2018

Objectives: The purpose of this study was to investigate the effects of 56 herbal formulae covered by the National Health Insurance Corporation (NHIC) on dementia-related biomarkers and neuronal cell changes. Methods: The 56 herbal formulae were extracted with 70% ethanol at $100^{\circ}C$ for 2 h. The antioxidant properties was measured by radical scavenging assay using ABTS+ radical. The acetylcholinesterase (AChE) activity was tested by Ellman's assay and $amyloid-{\beta}$ ($A{\beta}$) aggregation was determined using fluorescence method. To estimate the inhibitory effects of herbal formulae on neuronal cell death and inflammation using HT22 hippocampal cells and BV-2 microglia, respectively. Results: Among the 56 herbal formulae, Dangguiyukhwangtang, Banhasasimtang, Samhwangsasimtang, Cheongwiesan, Hwangryunhaedoktang, Banhabaekchulchunmatang, Jaeumganghwatang, Cheongseoikgitang, and Hoechunyanggyuksan has a significant inhibitory effects on acetylcholinesterase (AChE) activity. Doinseunggitang and Samhwangsasimtang exerted the effect on the inhibition of $amyloid-{\beta}$ ($A{\beta}$) aggregation. Additionally, 10 herbal formulae affected AChE and $A{\beta}$ aggregation revealed antioxidant activity as well as neuroprotective and anti-neuroinflammation effects in neuronal cell lines. Conclusions: 10 herbal formulae that have been shown to be effective against the major dementia markers have been shown to have antioxidant activity, neuronal cell protection and inhibition of brain inflammation. Further investigation of these herbal formulae will need to be validated in dementia animal models.

• Korean Journal of Food Science and Technology
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• v.41 no.4
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• pp.435-440
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• 2009

Acetylcholinesterase (AChE) inhibitors, which enhance cholinergic transmission by reducing the enzymatic degradation of acetylcholine, are the only source of the compound that is currently approved for the treatment of Alzheimer's disease (AD). In these experiments, the concentration samples of green tea extracts were 100, 500, and 1,000 ${\mu}g$/mL. Among them, the highest concentration (1,000 ${\mu}g$/mL) of fresh green tea extracts showed the most potent inhibitory effect on AChE by reducing more than 40% of enzyme activity, and in a concentration-dependent pattern. In addition, we examined the effect of other storing conditions on AChE inhibition. In order to maintain storage for 3 months, the materials were held at the certain storing conditions of temperature (room temperature, 4 and $-20^{\circ}C$) and for water activity (0.81, 0.69, and 0.23). In these storing conditions, the difference in temperature did not contribute to the AChE inhibitory effect. Our presented data showed that the AChE inhibitory effect was affected by the concentration of green tea extract and by water activity (0.81). These results suggest that green tea may serve as a potential dietary source of AChE inhibitor.

• Mycobiology
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• v.36 no.2
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• pp.102-105
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• 2008

The acetylcholinesterase (AChE) inhibitor of Yarrowia lipolytica S-3 was maximally produced when it was incubated at $30^{\circ}C$ for 36 h in an optimal medium containing 1% yeast extract, 2% peptone and 2% glucose, with an initial pH 6.0. The final AChE inhibitory activity under these conditions was an $IC_{50}$ value of 64mg/ml. After partial purification of the AChE inhibitor by means of systematic solvent extraction, the final $IC_{50}$ value of the partially purified AChE inhibitor was 0.75 mg/ml. We prepared a test product by using the partially purified AChE inhibitor and then determined its stability for the development of a new antidementia commercial product. The test product was stable at room temperature for 15 weeks.

• Korean Journal of Food Science and Technology
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• v.49 no.4
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• pp.438-443
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• 2017

The biological activity of crude polyphenol fractions (WphF, EphE, VphF, and SphF) extracted from Cedrela sinensis using hot water, ethanol, and enzymes such as Viscozyme and Shearzyme was examined in this study. The yield of VphF was the highest (43.44%) among all fractions. The total polyphenol and flavonoid content of the fractions were highest after ethanol extraction (447.98 and 337.49 mg/g, respectively). Fractions obtained after hot water and ethanol treatment showed high antioxidant activity. All fractions, except for WphF, showed a significantly higher ${\alpha}$-glucosidase inhibitory activity than the acarbose. EphF and WphF showed the high acetylcholinesterase inhibition activity. All fractions showed more than 50% tyrosinase inhibition activity at 2 mg/mL concentration. According to these results, the crude polyphenol fractions from C. sinensis showed high antioxidative, ${\alpha}$-glucosidase inhibitory, and tyrosinase inhibitory activities. This study suggests that crude polyphenol fractions from C. sinensis, especially the WphF and EphF fractions, are good sources of functional food.

• Journal of Microbiology and Biotechnology
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• v.23 no.2
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• pp.161-166
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• 2013

At present, acetylcholinesterase (AChE) inhibitors are the first group of drugs to treat mild to moderate Alzheimer's disease (AD). Although beneficial in improving cognitive and behavioral symptoms, the effectiveness of AChE inhibitors has been questioned since they do not delay or prevent neurodegeneration in AD patients. Therefore, in the present study, in order to develop new and effective anti-AD agents from lichen products, both the AChE inhibitory and the neuroprotective effects were evaluated. The AChE inhibitory assay was performed based on Ellman's reaction, and the neuroprotective effect was evaluated by using the MTT method on injured PC12 cells. One AChE inhibitor ($IC_{50}$ = 27.1 ${\mu}g/ml$) was isolated by means of bioactivity-guided isolation from the extract of lichen-forming fungus Cladonia macilenta, which showed the most potent AChE inhibitory activity in previous screening experiment. It was then identified as biruloquinone by MS, and $^1H$- and $^{13}C$-NMR analyses. The inhibitory kinetic assay suggested that biruloquinone is a mixed-II inhibitor on AChE. Meanwhile, biruloquinone improved the viability of the $H_2O_2$- and ${\beta}$-amyloid-injured PC12 cells at 1 to 25 ${\mu}g/ml$. The protective effects are proposed to be related to the potent antioxidant activities of biruloquinone. These results imply that biruloquinone has the potential to be developed as a multifunctional anti- AD agent.

• Journal of the Korean Society of Food Science and Nutrition
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• v.45 no.7
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• pp.966-972
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• 2016

We investigated that methanolic extracts of 20 kinds of seaweeds from Jeju Island for their antioxidant activities, acetylcholinesterase and ${\beta}$-secretase inhibitory activities, and neuronal survival in order to evaluate their potentials as anti-dementia agents. Ecklonia cava extracts had the highest total polyphenol content among the 20 seaweed extracts. The antioxidant activity of seaweed extracts was measured by using 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay. It was found that Ecklonia kurome extracts had the highest ABTS scavenging activity ($IC_{50}=0.07{\pm}0.01mg/mL$). As a result, Ecklonia cava, Ecklonia kurome, and Myelophycus simplex extracts were found to be the most effective in terms of acetylcholinesterase inhibitory activity. In the ${\beta}$-secretase activity assay, Ecklonia cava and Ecklonia kurome extracts were effectively inhibited ($84.41{\pm}1.70%$ and $81.17{\pm}2.43%$, respectively). As expected, neuronal cell death induced by $H_2O_2$ in SH-SY5Y cells was diminished by Ecklonia cava, Ecklonia kurome, and Sargassum yezoense extracts. Taken together, these results showed that Ecklonia cava extract has potential anti-dementia activity, which suggests that it might provide an effective strategy for improving dementia.

• Journal of Mushroom
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• v.17 no.3
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• pp.152-161
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• 2019

Phallus impudicus var. impudicus L. is an edible mushroom that has long been used as folk medicine in China. The aim of this study was to evaluate the antioxidant, anti-cholinesterase, and inflammation inhibitory activities of a methanol extract of fruiting bodies of P. impudicus var. impudicus L. The extract exhibited good 1,1-diphenyl-2-picrylhydrazyl scavenging activity, excellent ferrous ion chelating activity, and moderate hydroxyl radical scavenging activity compared with BHT at 2.0 mg/ml. However, the reducing power of the extract was significantly lower than that the BHT positive control. Although the inhibitory activities of methanol extract on acetylcholinesterase and butyryl cholinesterase were significantly lower than the galanthamine positive control at the concentration tested, the inhibition of acetylcholinesterase and butyryl cholinesterase was 52.83% and 55.17%, respectively, at 1.0 mg/ml. The methanol extract also demonstrated excellent inhibition of inflammation-related activities, such as production of nitric oxide in lipopolysaccharide-induced RAW 264.7 macrophage cells and acute edema induced by administration of carrageenan on the hind paw of rats. The collective results suggest that the fruiting body of P. impudicus var. impudicus L. might be a good source of antioxidant, anti-cholinesterase, and anti-inflammation compounds.

• Journal of Ginseng Research
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• v.34 no.4
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• pp.348-354
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• 2010

Black ginseng and white ginseng were extracted with 80% ethanol and evaluated for relative ginsenoside composition, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, and antioxidant properties. As analyzed by HPLC, black ginseng contained a greater proportion of ginsenoside $Rg_3$ compared to white ginseng. White ginseng was characterized by undetectable ginsenoside $Rg_3$ but it contained more total ginsenosides than black ginseng. Black ginseng extract exhibited higher (p<0.05) free radical-scavenging activity, as well as higher antioxidant activities than white ginseng against 2,2-diphenyl-1-picryl-hydrazyl, superoxide dismutase, and xanthine oxidase, despite the fact that the total saponin content was higher in white ginseng than black ginseng. In addition, the black ginseng extract displayed greater AChE and BChE inhibitory activities. These results suggest that black ginseng has stronger effects on anti-oxidation and AChE and BChE inhibition than white ginseng.

• Korean Journal of Pharmacognosy
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• v.46 no.4
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• pp.327-333
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• 2015

Alzheimer's disease (AD) is a progressive neurodegenerative disorder symptomatically characterized by impairment in memory and cognitive abilities. AD is characterized pathologically by the deposition of ${\beta}$-amyloid ($A{\beta}$) peptides of 40-42 residues, which are generated by processing of amyloid precursor protein (APP). $A{\beta}$ has been believed to be neurotoxic and now is also considered to have a role on the mechanism of memory dysfunction. In this study, we tested that EtOH extract of the fruits of Chaenomeles sinensis Koehne (CSE) affects on the processing of APP from the APPswe over-expressing Neuro2a cell line. We found that CSE increased over 2 folds of the $sAPP{\alpha}$ secretion level, a metabolite of ${\alpha}$-secretase. We showed that CSE reduced the secretion level of $A{\beta}42$ and $A{\beta}40$ by down regulation of ${\beta}$-secretase (BACE) without cytotoxicity. Furthermore, we found that CSE inhibited BACE and acetylcholinesterase activity in vitro. We suggest that Chaenomelis Fructus may be an useful source to develop a herbal medicine for AD.

• Archives of Pharmacal Research
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• v.26 no.10
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• pp.796-799
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• 2003

Two known farnesylacetone derivatives (1 and 2) were isolated from the Korean brown alga Sargassum sagamianum off Jeju Island, Korea. Compounds 1 and 2 were identified as (5E,10Z)-6, 10, 14-trimethylpentadeca-5, 10-dien-2, 12-dione and (5E,9E,13E)-6, 10,4-trimethylpentadeca-5,9,13-trien-2,12-dione, respectively, by comparison with the literature data. Compounds 1 and 2 showed moderate acetylcholinesterase and butyrylcholinesterase inhibitory activities with $IC_{50}$ values of 65.0∼48.0 and 34.0∼23.0 $\muM$, respectively.