• 한국독성학회:학술대회논문집
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• 한국독성학회 2001년도 International Symposium on Dietary and Medicinal Antimutgens and Anticarcinogens
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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)

• 한국약용작물학회지
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• 제20권4호
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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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• 제14권5호
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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.

• 통합자연과학논문집
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• 제10권1호
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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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• 제28권12호
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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.

• 한국미생물·생명공학회지
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• 제47권1호
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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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• 제17권2호
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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 $K^-Ras$).

• 한국식품저장유통학회지
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• 제20권3호
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• pp.342-347
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• 2013

본 연구는 고흥산과 수입산 석류의 화학적 성분분석 및 생리활성 기능을 분석하여 기능성 물질의 소재 개발과 착즙 후 버려지는 부산물 활용 방안에 기여하고자 하였다. 석류 과즙 중 주요 유기산은 citric acid, malic acid가 확인되었으며 주요 유리당으로는 fructose, glucose가 확인되었다. 석류의 폴리페놀 함량은 고흥산 과피에서 149.91 mg/g으로 가장 높았고 가장 낮은 함량을 보인 과즙보다는 약 100배 정도 높게 함유되어 있었다. 석류의 부위별 ellagic acid 함량을 분석한 결과 고흥산 과피에서 14.22 mg/g으로 미국산에 비해 두 배 이상 높게 나타났으며, 고흥산과 미국산 모두 과즙이나 씨 보다는 과피에서 ellagic acid 함량이 월등히 높게 나타났다. 석류 부위별 추출물은 농도 의존적으로 항산화 활성이 증가하였으며, 고흥산과 미국산 모두 과피, 씨, 과즙 순으로 높은 활성도를 나타냈다. 고흥산과 미국산 부위별 추출물의 전립선암 세포증식 억제능을 분석한 결과 산지에 관계없이 과피, 과즙, 씨 순으로 암세포 성장억제능이 높게 나타났으며 특히 과즙과 씨에서는 고흥산이 미국산에 비해서 암세포 성장억제능이 더 우수하였으며 과피 추출물에서는 미국산이 더 우수하였다.

• 한국자원식물학회지
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• 제25권5호
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• pp.561-567
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• 2012

본 연구는 EA에 의한 대식세포의 활성화를 매개로 한 항암효과와 항암작용과 관련된 대식세포의 면역조절효과를 확인하였다. 연구 결과 EA에 의해 RAW264.7세포 및 peritoneal macrophage 모두에서 항암효과가 증가하였으며, 증가된 대식세포의 항암효과는 TLR4 signaling을 blocking하는 CLI-095을 함께 처리하였을 때 일부 감소되었다. 이는 EA에 의한 항암 효과가 부분적으로 TLR4를 경유하는 기전으로 나타나는 것을 의미한다. 또한, EA에 대한 대식세포의 NO 분비조절효과를 측정하였으며, EA는 대식세포의 NO 생성을 증가시켰으나, 인위적으로 염증을 유발시켜 NO를 과도하게 분비한 상태에서는 NO 분비를 오히려 억제시키는 결과를 나타내었다. 이와 같이 EA에 의한 NO조절에 대한 이중 효과는 인체에 면역증강과 항염증 효과라는 긍정적인 효과를 나타내는 방향으로 조절하고 있으므로 EA를 이용한 항암요법의 보조제 및 면역보조제로써의 활용에 유익할 것으로 사료된다. 향후 EA에 대한 항암 작용 및 NO 조절에서 세포내 신호전달 작용기전에 대한 심도 있는 연구가 진행되어야 할 것으로 보인다.

• Rapid Communication in Photoscience
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• 제2권1호
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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.