• 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.

• 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.

• Food Science and Biotechnology
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• 제15권5호
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• pp.728-734
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• 2006

The tannins represent a highly heterogeneous group of water-soluble plant polyphenols that may play an important role in antimutagenic and antioxidant properties. We investigated the antioxidant function of tannic acid in comparison to other phenolic compounds including catechin, chlorogenic acid, cinnamic acid, ellagic acid, and gallic acid for their ability to scavenge several stable radicals and reactive oxygen species (ROS) such as ${\bullet}DPPH^+$, ${\bullet}ABTS^+$, hydrogen peroxide, hydroxyl radical, and superoxide radical. The ability of tannic acid to decrease paraquat-induced lipid oxidation in mouse liver and lung through its antioxidant properties was also assessed. The results showed that almost all the tested compounds have stable radical scavenging activity except cinnamic acid. Tannic acid, gallic acid, and ellagic acid demonstrated remarkable ROS scavenging properties toward $H_2O_2$, ${\bullet}OH^-$, ${\bullet}O_2^-$ and especially only tannic acid could inhibit paraquat-induced lipid peroxidation effectively in mouse liver and lung. Based on these results, it appears that increased number of galloyl and ortho-hydroxyl groups enhances the antioxidant activity of phenolic compounds and tannic acid is evaluated as the most effective antioxidant among all the tested compounds. These results suggest that the tannins, especially tannic acid, can be used as therapeutic agent for various diseases caused by ROS.

• 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 $K^-Ras$).

• 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.

• 원예과학기술지
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• 제32권1호
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• pp.115-122
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• 2014

유용성분 함량이 많고 생리기능성이 우수한 산딸기 품종의 육성을 위해 국내 농가에서 재배되고 있는 7종의 산딸기와 야생에서 자생하는 2종의 산딸기를 복분자 연구소에서 재배한 후 이들을 대상으로 과실의 품질특성, 유용성분의 함량, 항산화능을 측정하였다. 충남 아산의 야생 산딸기가 크기는 작았지만 당도는 16.20%로 시료 산딸기 중 가장 높고 산도는 가장 낮았다. 경북 울릉도의 야생 산딸기는 작은 크기에 당도 및 산도가 매우 낮아 과실로서의 이용가치는 매우 낮았으나, 총 페놀성 화합물과 ellagic acid 함량은 각각 182.97, $55.25mg{\cdot}100g^{-1}FW$로 시료 중 가장 높았다. 경남 김해에서 재배되는 산딸기 중 '왕딸'은 크기가 크고 당도는 12.80%로 다소 낮은 반면, 품종이 불명확한 다른 산딸기는 야생 산딸기 정도로 크기는 작지만 당도는 14.4%로 '왕딸' 보다 높았다. 김해 지역에서 재배되는 '왕딸'과 품종이 불명확한 산딸기의 총 페놀성 화합물(159.62, $165.94mg{\cdot}100g^{-1}FW$) 및 ellagic acid(45.7, $52.1mg{\cdot}100g^{-1}FW$) 함량은 울릉도 야생 산딸기보다 낮았으나, 총 플라보노이드 화합물(14.28, $14.90mg{\cdot}100g^{-1}FW$)과 총 안토시아닌(28.69, $30.48mg{\cdot}100g^{-1}FW$) 함량은 이보다 높았다. 경북 울릉도 야생 산딸기, 김해 지역의 '왕딸' 및 품종이 불명확한 산딸기는 FRAP법에 의한 항산화능과 DPPH 및 ABTS radical 소거능도 다른 품종의 산딸기보다 현저하게 높아 육종 소재 및 기능성 성분 소재로서의 이용 가치가 높은 것으로 사료된다.

• Preventive Nutrition and Food Science
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• 제14권3호
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• pp.214-219
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• 2009

The pomegranate (Punica granatum L.) is a promising source of functional food, which contains several phytochemicals that perform important roles in reducing the risk of pathological diseases. Chemical compositions, such as the total sugar, uronic acid, polyphenols, and anthocyanin contents, and radical scavenging activity were determined and compared among PEs from six different cultivation areas. Total anthocyanin contents (TAC) and total polyphenol contents (TPC) from various growing areas were detected in the following order, respectively: Spain (19.08 ${\mu}g$/mL)> Turkey (12.91 ${\mu}g$/mL)> Iran-A (6.67 ${\mu}g$/mL)> Taiwan (4.77 ${\mu}g$/mL)> Uzbekistan (1.88 ${\mu}g$/mL)> Iran-B (0.76 ${\mu}g$/mL) and Turkey (639.52 ${\mu}g$/mL)> Uzbekistan (502.19 ${\mu}g$/mL)> Spain (306.40 ${\mu}g$/mL)> Iran-B (249.20 ${\mu}g$/mL)> Taiwan (162.78 ${\mu}g$/mL)> Iran-A (143.93 ${\mu}g$/mL). PEs from six different cultivation areas were determined to vary in ellagic acid content from 8.90 ${\mu}g$/mL to 332.52 ${\mu}g$/mL. The amounts of total sugars in PE from Iran-A evidenced relatively high total sugar contents, but low uronic acid levels (11.92 mg/mL). DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging activities were as follows: Turkey> Uzbekistan $\gg$ Spain> Iran-B> Iran-A> Taiwan. ABTS [2,20-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)] radical scavenging activities were detected in the following order: Turkey$\geq$ Uzbekistan$\gg$ Spain> Iran-B> Iran-A> Taiwan. These results indicate that the PEs from Turkey with higher levels of TPC, TAC, ellagic acid, and higher radical scavenging activity may constitute a promising functional source for the prevention of several degenerative diseases.

• Journal of Applied Biological Chemistry
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• 제58권2호
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• pp.189-194
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• 2015

전통생약으로서 다양한 효능과 염색제로서 사용되어온 A. catechu의 식물화학적 성분연구를 위해 열수추출물 중 ethyl acetate 분획으로부터 9종의 flavonoid와 1종의 tannin을 단리하였으며, 이들의 물리화학적 성상과 spectral data로부터 구조를 확인한 결과 (+)-catechin (1), (-)-epicatechin (2), (+)-afzelechin (3), (-)-epiafzelechin (4), (+)-mesquitol (5), kaempferol (6), quercetin (7), quercetin 3-methyl ether (8) caryatin (9) 및 ellagic acid (10)로 각각 확인 동정하였다. 이들 화합물 중 caryatin (9)은 Acacia 속으로부터 처음으로 분리되었다.

• 한국환경성돌연변이발암원학회:학술대회논문집
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• 한국환경성돌연변이발암원학회 2001년도 Korean Environmental Mutagen Society
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• pp.110-110
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• 2001

• 약학회지
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• 제39권2호
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• pp.200-204
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• 1995

Chemical examination of the leaves of Rubus coreanum has led to the isolation and characterization of six phenolic compounds. The structures of these compounds were elucidated as kaempferol(l), quercetin(2), sodium salt of quercetin 3-O-$\beta$-D-glucuronide(3), sodium carboxylate of quercetin 3-O-$\beta$-D-glucuronide(4), ellagic acid(5) and sanguiin H-5(6) on the basis of physicochemical and spectroscopic evidences.