• Proceedings of the Korean Society of Toxicology Conference
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• 2001.10a
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• pp.110-110
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• 2001

Inner shell of chestnut (Castanea Mollissima, Fagaceae) is well-known anti-wrinkle agent, which has been used for long time in the treatment of skin aging. In this study, the extract of chestnut inner shell (CMIE) and its major component, ellagic acid (EA), were studied for their protective effects against free radical generation and hydrogen peroxide-induced oxidative DNA damages in the mammalian cells.(omitted)

• Korean Journal of Medicinal Crop Science
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• v.20 no.4
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• pp.222-230
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• 2012

We evaluated the inhibitory effects of extracts and components of Geranium thunbergii on aldose reductase (AR) and galactitol formation in rat lenses with high levels of galactose as a part of our ongoing search of natural sources for therapeutic and preventive agents for diabetic complications. The inhibitory effects of water, methanol and ethanol extracts of G. thunbergii on rat lens AR (RLAR) were determined. Comparing inhibitory effects of various solvent extracts, ethanol extract showed RLAR inhibitory activity ($IC_{50}$ values, 5.24 and $6.39{\mu}g/m{\ell}$, respectively). The ethanol extract was fractionated to chloroform, ethyl acetate and water. Of these, the ethyl acetate fraction from ethanol extract of G. thunbergii exhibited RLAR inhibitory activity ($IC_{50}$ value, $2.64{\mu}g/m{\ell}$). In order to identify the bioactive components of ethyl acetate soluble fraction of ethanol extract from G. thunbergii, eight compounds, namely gallic acid (1), protocatechuic acid (2), p-hydroxybenzoic acid (3), brevifolin carboxylic acid (4), geraniin (5), ellagic acid (6), kaempferol-3-O-arabinofuranosyl-7-O-rhamnopyranoside (7), kaempferitrin (8) were isolated. The isolates were subjected to in vitro bioassays to evaluate their inhibitory activity on RLAR and galactitol formation in rat lenses. The ellagic tannins (5, 6) and flavonoid (7) exhibited strong inhibitory effects on RLAR. Also, these three compounds (5, 6 and 7) suppressed galactitol accumulation in rat lens under high galactose conditions, demonstrating the potential to prevent galactitol accumulation exo vivo. These results suggest that the extracts and components of G. thunbergii are a promising agent in the prevention or treatment of diabetic complications.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.5
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• pp.2859-2863
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• 2013

Polyphenolic compounds from pomegranate fruit extracts (PFEs) have been reported to possess antiproliferative, pro-apoptotic, anti-inflammatory and anti-invasion effects in prostate and other cancers. However, the mechanisms responsible for the inhibition of cancer invasion remain to be clarified. In the present study, we investigated anti-invasive effects of ellagic acid (EA) in androgen-independent human (PC-3) and rat (PLS10) prostate cancer cell lines in vitro. The results indicated that non-toxic concentrations of EA significantly inhibited the motility and invasion of cells examined in migration and invasion assays. The EA treatment slightly decreased secretion of matrix metalloproteinase (MMP)-2 but not MMP-9 from both cell lines. We further found that EA significantly reduced proteolytic activity of collagenase/gelatinase secreted from the PLS-10 cell line. Collagenase IV activity was also concentration-dependently inhibited by EA. These results demonstrated that EA has an ability to inhibit invasive potential of prostate cancer cells through action on protease activity.

• Journal of Integrative Natural Science
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• v.10 no.1
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• pp.1-6
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• 2017

Demand for a new anti-malarial drug has been dramatically increasing in the recent years. Plasmodium falciparum enoyl-acyl carrier protein reductase (PfENR) plays a vital role in fatty acid elongation process, which now emerged as a new important target for the development of anti-microbial and anti-parasitic molecules. In the present study, 19 compounds namely alginic acid, atropine, chlorogenic acid, chrotacumine A & B, coenzyme $Q_1$, 4-coumaric acid, curcumin, ellagic acid, embelin, 5-O-methyl embelin, eugenyl glucoside, glabridin, hyoscyamine, nordihydroguaiaretic acid, rohitukine, scopolamine, tlatlancuayin and ursolic acid were evaluated on their docking behaviour on P. falciparum enoyl-acyl carrier protein reductase (PfENR) using Auto dock 4.2. The docking studies and binding free energy calculations exhibited that glabridin gave the highest binding energy (-8.07 kcal/mol) and 4-coumaric acid in contrast showed the least binding energy (-4.83 kcal/mol). All ligands except alginic acid, ellagic acid, hyoscyamine and glabridin interacted with Gln409 amino acid residue. Interestingly four ligands namely coenzyme $Q_1$, 4-coumaric acid, embelin and 5-O-methyl embelin interacted with Gln409 amino acid residue present in both chains (A & B) of PfENR protein. Thus, the results of this present study exhibited the potential of these 19 ligands as P. falciparum enoyl-acyl carrier protein reductase (PfENR) inhibitory agents and also as anti-malarial agents.

• Archives of Pharmacal Research
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• v.28 no.12
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• pp.1328-1332
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• 2005

In the course of screening for anti-dementia agents from natural products, two $\beta$-secretase (BACE1) inhibitors were isolated from the husk of pomegranate (Punica granatum) by activity-guided purification. They were identified as ellagic acid and punicalagin with $IC_{50}$ values of 3.9 $\times$$10^{-6}$ and 4.1$\times$$10^{-7}$ M and Ki values of 2.4$\times$$10^{-5}$and 5.9$\times$$10^{-7}$ M, respectively. The compounds were non-competitive inhibitors with a substrate in the Dixon plot. Ellagic acid and punicalagin were less inhibitory to $\alpha$-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, thus indicating that they were relatively specific inhibitors of BACE1.

• Microbiology and Biotechnology Letters
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• v.47 no.1
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• pp.54-63
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• 2019

Rubus coreanus Miquel (RCM), also known as Korean blackberry or bokbunja, is used as a South Korean traditional medicine to treat acne and inflammatory skin conditions. The antimicrobial activity of RCM root and its active compounds remain unclear. In this study, we prepared a 50% ethanol fraction, ethyl acetate fraction, and acid-treated ethyl acetate fraction (aglycone fraction) of RCM root, and evaluated antibacterial activities against the skin pathogens Staphylococcus aureus, Pseudomonas acnes, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa. In a paper disc assay, all fractions of RCM root showed antimicrobial activities against the five skin pathogens. The ethyl acetate fraction displayed 6-, 12-, and 2-fold higher minimal inhibitory concentration (MIC) than the 50% ethanol fraction against S. aureus, E. coli, and P. acnes, respectively. The aglycone fraction displayed 2-fold higher MIC than methyl paraben against P. acnes, S. aureus, E. coli, and P. aeruginosa. The ethyl acetate fraction displayed a minimal bactericidal concentration (MBC) similar to that of methyl paraben, and the aglycone fraction showed 2- to 4-fold higher MBCs than those of methyl paraben. In particular, the ethyl acetate fraction was not cytotoxic and showed thermal stability after incubation at high temperatures ($60-121^{\circ}C$). Finally, the ethyl acetate fraction was separated and four components were identified: procyanidin C, propelagonidin dimer, ellagic acid, and methyl ellagic acid acetyl pentose. The compounds showed high antibacterial activities. These results suggest that RCM root is potentially applicable as a natural preservative in cosmetics.

• Asian Pacific Journal of Cancer Prevention
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• v.17 no.2
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• pp.743-748
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• 2016

Background: $K^-Ras$ activation is an early event in colorectal carcinogenesis and associated mutations have been reported in about 40% of colorectal cancer patients. These mutations have always been responsible for enhancing malignancy and silencing them is associated with attenuation of tumorigenicity. Among downstream effectors are the RAF/MEK/ERK and the PI3K/Akt signaling pathways. PI3K/Akt signaling leads to reduction of apoptosis, stimulated cell growth and enhanced proliferation. Ellagic acid (EA), a naturally occurring antioxidant, has recently emerged as a promising anti-cancer agent. Purpose: To evaluate the impact of cellular genetic makeup of two colon cancer cell lines with different genetic backgrounds, HCT-116 ($K^-Ras^-/p53^+$) and Caco-2 ($K^-Ras^+/p53^-$), on response to potential anti-tumour effects of EA. In addition, the influence of $K^-Ras$ silencing in HCT-116 cells was investigated. Materials and Methods: Cellular proliferation, morphology and cell cycle analysis were carried out in addition to Western blotting for detecting total Akt and p-Akt (at Thr308 and Ser473) in the presence and absence of different concentrations of EA. Cell proliferation was also assessed in cells transfected with different concentrations of $K^-Ras$ siRNA or incubated with ellagic acid following transfection. Results: The results of the present study revealed that EA exerts anti-proliferative and dose-dependent pro-apoptotic effects. Cytostatic and cytotoxic effects were also observed. p-Akt (at Thr308 and Ser473) was downregulated. Moreover, EA treatment was found to (i) reduce $K^-Ras$ protein expression; (ii) in cells transfected with siRNA and co-treated with EA, pronounced anti-proliferative effects as well as depletion of p-Akt (at Thr308) were detected. Conclusions: Cellular genetic makeup ($K^-Ras^-/p53^-$) was not likely to impose limitations on targeting EA in treatment of colon cancer. EA had a multi-disciplinary pro-apoptotic anti-proliferative approach, having inhibited Akt phosphorylation, induced cell cycle arrest and showed an anti-proliferative potential in HCT-116 cells (expressing mutant $K^-Ras$).

• Food Science and Preservation
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• v.20 no.3
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• pp.342-347
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• 2013

In recent years, polyphenol-rich herbs, fruits and processed foods, which are made of plant origin, have attracted much attention due to their potential health benefits. Pomegranate (Punica granatum L.) is an important source of bioactive compounds and has been used to treat diseases because of its medicinal properties. This research was focused on characterizing Korea's national cultivar and a similar product from California, USA. To evaluate their bioactive compounds and pharmacological activities, their anti-oxidation and cancer inhibition properties, as well as their organic acid and free sugar contents, were investigated. The national cultivar had low total sugar and high organic acid contents, contrary to the imported product. The results showed that the peel of national cultivar had high polyphenol and ellagic acid contents compared to imported product. The free radical scavenging capacity was evaluated via 2,2-diphenyl-1-picrylhydrazyl (DPPH) and its positive correlation with the total polyphenol contents was found. The anti-cancer activity of methanol extracts revealed growth inhibition against the prostate cancer cell. These results signify that while pomegranate, national cultivar, is more sour than the imported product, its health benefits could be excellent. Also, the polyphenol compound content of the non-edible part (such as the peel and the seed) was higher than that of the juice. Thus, it is suggested that the byproduct of the juice extraction could be potentially used in other fields such as medicine or dietary agents.

• Korean Journal of Plant Resources
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• v.25 no.5
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• pp.561-567
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• 2012

Ellagic acid (EA) is a phenolic compound in fruits and nuts including raspberries, strawberries, grapes and walnuts. Previous studies have indicated that EA possesses antioxidant activity, growth-inhibition and apoptosis-promoting activity in cancer cells. However, macrophage mediated cytotoxicity and immunomodulating effects on cancer cells have not been clarified. In the present study, we show that EA increased effects on macrophage mediated tumoricidal activity and NO production without direct tumor cell cytotoxicity. To further determine whether TLR4 (toll like receptor 4) is involved in anti-tumor activity, cells were treated TLR4 signaling inhibitor, CLI-095 in the presence of EA. CLI-095 treatment partially reduced macrophage-mediated tumoridial activity. EA also has inhibitory effects of NO production induced by LPS, whereas phagocytic activity was not changed. These results suggest that EA induces macrophage mediated tumoricidal activity which is partially related to TLR4 signaling and has a potential adjuvant in cancer therapy.

• Rapid Communication in Photoscience
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• v.2 no.1
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• pp.28-30
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• 2013

The extract of Punica granatum peel was separated and confirmed by HPLC, and punicalagin, one of the extract, was better antibacterial activity against Salmonella.