• Korean Journal of Pharmacognosy
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• v.38 no.1
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• pp.27-30
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• 2007

We examined the inhibitory activities against monoamine oxidase (MAO) of Chrysanthemum indicum L. in vitro and in vivo methods. Methanolic extract of C. indicum showed significant inhibitory activities on MAO-A that were prepared from rat brain in vitro. The inhibitory activities were measured by serotonin as a substrate. The $IC_{50}$ value of methanolic extract of C. indicum was 0.24 mg/ml for the inhibition of MAO-A. The ethylacetate fraction of methanolic extract of C. indicum exhibited the best activity toward MAO-A with $IC_{50}$ value of 0.05 mg/ml in vitro. It was observed that those activities in vivo tests have different tendency each other. Ethanolic extract of C. indicum was have no effect on rat MAO by the oral administration (p<0.05). However, MAO inhibitory activities of ethanolic extract of C. indicum by the oral administration have similar tendency to those of iproniazid. Consequently, we suggest that C. indicum may have the effects on the inhibitory activities against MAO both in vitro and in vivo. These results indicates that the C. indicum extract has properties indicative of potential neuroprotective ability.

• Asian-Australasian Journal of Animal Sciences
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• v.16 no.9
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• pp.1369-1373
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• 2003

ACE (Angiotensin-I converting enzyme) inhibitory peptides derived from foods are thought to suppress high blood pressure by inhibiting ACE. We tried to make efficient production of the ACE inhibitory hydrolysate from egg albumen. A hydrolysate digested by neutrase presented the highest ACE inhibitory activity ($IC_50\;value=256.35{\mu}g/ml$) and the proper proteolysis was occurred by 1.0% enzyme addition and 4 h incubation at $47^{\circ}C$. Antihypertensive effect of neutrase hydrolysate was investigated in spontaneously hypertensive rats (SHR, n=5). Systolic blood pressure (SBP) was decrease by 6.88% (-14.14 mmHg, p<0.05) at 3 h after oral administration of 300 mg/kg body weight, and by 13.33% (-27.72 mmHg, p<0.05) by emulsified hydrolysate. These results showed that it is very effective to utilize egg albumen as a protein source for the production of ACE inhibitory peptides. However, further studies are required to investigate the methods to increase recovery yield and the isolation of active peptide is necessary for determining its sequence responsible for ACE inhibitory activity.

• Journal of Biomedical Engineering Research
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• v.23 no.4
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• pp.329-332
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• 2002

We have investigated the role of slow inhibitory neurons in spontaneous activity using a model network controlled by stochastic mean field theory based on Integrated-and-Fire excitatory and fast inhibitory neurons. It is found that inputting slow inhibitory neurons to such network induces stable spontaneous activity at a much lower threshold than without slow inhibitory neurons in the network. This threshold range is low enough to be considered as biological threshold of cortical neurons. Only slow inhibitory neurons can give adjustable negative feedback in the network keeping lower rate and lower threshold.

• Fisheries and Aquatic Sciences
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• v.19 no.2
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• pp.11.1-11.7
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• 2016

In this study, purified peptides from shrimp waste hydrolysates (SWHs) were examined for their inhibitory effects against ${\beta}$-secretase. During consecutive purification using a Sephadex G-25 column chromatography and high performance liquid chromatography on a C18 column, a potent ${\beta}$-secretase inhibitory peptide Asp-Val-Leu-Phe-His (629 Da) was isolated and identified from SWH24 by Q-TOF MS/MS and the $IC_{50}$ value was determined to be $92.70{\mu}M$. The ${\beta}$-secretase inhibition patterns of the purified peptides were found to be competitive. Among synthesized ${\beta}$-secretase inhibitory peptides, Leu-Phe-His had higher ${\beta}$-secretase inhibitory activity than the others. The result of this study suggests that the ${\beta}$-secretase inhibitory peptide derived from SWH24 could be potential candidates to develop nutraceuticals and pharmaceuticals.

• Korean Journal of Pharmacognosy
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• v.38 no.4
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• pp.312-320
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• 2007

The screening of anti-cancer activity for the MeOH extracts of 163 natural sources, which were registered as edible plants by Korea Food & Drug Administration, exhibited 9 extracts to have significant inhibitory effects on farnesyl-protein transferase (FPTase) and phosphatase of regenerating liver-3 (PRL-3). In order to confirm the inhibitory activity of these active extracts, the activity assay was repeated for some fractions obtained from the active extracts using Medium Pressure Liquid Chromatography (MPLC). Some fractions of Carya illinoensis, Chlorella vulgaris, Panicum miliaceum, Perilla frutescens, Rosmarinus officinalis showed over 50% inhibitory activity on FPTase as well as those of Capsella bursa-pastoris, C. illinoensis, C. vulgaris, Coix lacrymajobi, Myristica fragrans, P. miliaceum, R. officinalis did over 50% inhibitory activity on PRL-3.

• Journal of Pharmaceutical Investigation
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• v.33 no.2
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• pp.105-112
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• 2003

Selective COX (cyclooxygenase)-2 inhibitors including celecoxib have been shown to induce apoptosis and cell cycle changes in various tumor cells. New inhibitors are recently being developed as chemomodulating agents. We evaluated celecoxib and screened 150 synthetic compounds for anti-proliferative activities in vitro. Effects of celecoxib on COX activity, cell growth, cell cycle distribution, and apoptosis induction were determined in A549 COX-2 overexpressing human non-small cell lung cancer (NSCLC) cells. The COX inhibition of celecoxib increased with concentration up to 82% at $1\;{\mu}M$ after 24 hr exposure. Forty ${\mu}M$ and $50\;{\mu}M$ of ce1ecoxib induced $G_1$ arrest, and TUNEL-positive apoptotic cells, respectively. Among 150 compounds, several compounds were selected for having greater COX-2 inhibitory activity and higher selectivity than celecoxib with growth inhibitory activity. Celecoxib showed concentration-dependent COX inhibitory activity, and ability to induce cell cycle arrest and apoptosis in human NSCLC cells in vitro. Among synthetic analogues screened, several compounds showed promising in vitro activity as COX-2 inhibitory anticancer agents, which warrant further evaluation in vitro and in vivo.

• YAKHAK HOEJI
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• v.52 no.1
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• pp.62-66
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• 2008

In this study, we examined the inhibitory effects of propenone derivatives, 1,3-diphenyl-propenone (DPhP), 3-phenyl-1-thiophen-2-yl-propenone (PhT2P), 3-phenyl-1-thiophen-3-yl-propenone (PhT3P) and 1-furan-2-yl-3-phenyl-propenone (FPhP), on $TNF-{\alpha}$-induced nuclear factor (NF)-${\kappa}B$ activity and interleukin (IL)-8-induced monocyte adhesion to colon epithelial cells. 1-Furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) that is previously reported as a $NF-{\kappa}B$ inhibitor suppressed $TNF-{\alpha}$-induced monocyte-epithelial cell adhesion in a concentration-dependent manner. The propenone derivatives, DPhP, PhT2P, PhT3P, FPhP, also inhibited $TNF-{\alpha}$-induced $NF-{\kappa}B$ activation in a similar degree to FPP-3. In a DPPH radical scavenging assay, none of the compounds showed DPPH radical scavenging activity, indicating that the inhibitory actions of the propenone derivatives on redox-sensitive $NF-{\kappa}B$ activity is not due to a simple free radical scavenging activity. In addition, the propenone derivatives also suppressed the IL-8-induced monocyte adhesion to colon epithelial cells. Furthermore, the effective concentrations of the propenone derivatives on both $NF-{\kappa}B$ activation as well as IL-8 induced monocyte-epithelial cell adhesion were 1000 times lower than 5-aminosalicylic acid (5-ASA), a clinically used drug for inflammatory bowel disease. These results suggest that the propenone derivatives may be a potential lead having a strong inhibitory activity against inflammatory cytokine-induced epithelial inflammation.

• Korean Journal of Medicinal Crop Science
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• v.25 no.1
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• pp.10-15
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• 2017

Background: We investigated the antioxidative and tyrosinase inhibitory activities of 70% ethanol extract, and its fractions, of the root of Rumex japonicus HOUTT. Methods and Results: The total phenolic compound contents of the 70% ethanol extract and ethyl acetate fraction were 168.99 mg/g and 651.78 mg/g, respectively. The antioxidant activity was compared through the DPPH radical and nitric oxide (NO) scavenging assays. The ethyl acetate fraction showed the highest DPPH radical and NO scavenging abilities, which confirmed the antioxidant activity. Specifically, the ethyl acetate fraction showed a higher DPPH radical scavenging ability than ascorbic acid. These results were related to the total phenolic compound content of the ethyl acetate fraction. Moreover, in the tyrosinase inhibition assay, the ethyl acetate fraction exhibited stronger inhibitory activity than arbutin, which was used as the positive control. The cell viability of L929 cells was analyzed by MTT assay after treatment with 70% ethanol extract and all fractions; no changes in viability were observed, which demonstrated the nontoxic nature of the extract and fractions. Conclusions: These results suggested that the extract from the root of R. japonicus and its ethyl acetate fraction could be a novel resource for the development of a cosmetic with antioxidant and tyrosinase inhibitory activity.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.28 no.1
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• pp.1-10
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• 2015

Objectives : Oxidation by active oxygen in the body, phototoxicity and photoallergic interest has grown, antioxidant and phototoxicity inhibiting substances for research progress. The purpose of this study was to examine the effects on antioxidant and phototoxicity of Rubus coreanus Fruits. Meterial and Methods : Hs68 cell lines using the DPPH radical scavenging activity, cytotoxic, phototoxic inhibitory activity and apoptosis were measured. Results : 1. In MTT assay, the concentrations of Rubus coreanus Fruits that were used on the test had no cytotoxicity. 2. In DPPH radical scavenging activity, the concentration of $50{\mu}g/ml$, $100{\mu}g/ml$ anti-oxidant effect of Rubus coreanus Fruits was statistically significant increased than control group in dose-dependantly. 3. In phototoxic inhibitory activity, Rubus coreanus Fruits dose-dependently increased the cell viability of Hs68 cell lines. 4. The concentration of $50{\mu}g/ml$ Rubus coreanus Fruits inhibited the enrichment of nucleus in the Hs68 cell stimulated with UVB. Conclusions : These results indicate that Rubus coreanus Fruits has anti-oxidant effects and Phototoxic Inhibitory Activity. If further study is performed, the use of Rubus coreanus Fruits will be valuable and beneficial in the therapy of skin aging and damage.

• The Korean Journal of Food And Nutrition
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• v.27 no.5
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• pp.837-844
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• 2014

This study was carried out to analyze the differences in p-hydroxylbenzyl alcohol (HBA) content, antitumor and anti-obesity activities and tyrosinase inhibitory activity between non-fermented G. elata (NFGP) and fermented G. elata powder. The HBA content, which is an index-component of G. elata decreased from 1.58 mg/g before fermentation to 1.07, 0.32, and 0.13 mg/g after the $1^{st}$ fermentation ($1^{st}$ FGP), $2^{nd}$ fermentation ($2^{nd}$ FGP) and $3^{rd}$ fermentation ($3^{rd}$ FGP), respectively. The anti-proliferation effects on the cell lines HT29 and AGS were significantly higher for the fermented G. elata than the NFGP. The antitumor activity was also increased in a fermentation number-dependent manner. During adipocyte differentiation, the ethanol extract of the $3^{rd}$ FGP inhibited lipid accumulation in 3T3-L1 cells significantly better than NFGP and the $1^{st}$ FGP, treated at the concentration of $10{\mu}g/mL$. The tyrosinase inhibitory activity of the $2^{nd}$ FGP at $600{\mu}g/mL$ over was higher than that of kojic acid. At the concentration of $1,000{\mu}g/mL$, the tyrosinase inhibitory activity was increased in a fermentation number-dependent manner. From these results, the fermented G. elata, especially the $3^{rd}$ FGP, is expected to be good candidate for the development of functional food and agents with antitumor, anti-obesity, and tyrosinase inhibitory potential.