• 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.

• 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.

• Food Science and Biotechnology
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• v.15 no.5
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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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• 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 $K^-Ras$).

• 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.

• Horticultural Science & Technology
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• v.32 no.1
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• pp.115-122
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• 2014

In order to select the raspberry cultivars that have high contents of bioactive constituents and high antioxidant activities, 7 cultivated and 2 wild raspberries which were selected and cultivated in the Bokbunja Institute were evaluated for their physicochemical characteristics, bioactive constituents, and antioxidant activities. The wild raspberry of Asan was the smallest among the sample raspberries but it had the highest sugar and lowest acid contents among the raspberries. Another wild raspberry of Ulleungdo had the highest total phenolic compound and ellagic acid contents, 182.97, $55.25mg{\cdot}100g^{-1}FW$, respectively, although it was small and had low sugar and high acid contents. Among the widely cultivated raspberry cultivars in Kimhae, 'Wangttal' cultivar was a big raspberry with 12.80% sugar content, and another unknown raspberry cultivar was as small as the wild raspberry with 14.60% sugar content. Although 'Wangttal' and the unknown raspberry cultivars cultivated in Kimhae possess lower contents of total phenolic compound (159.62, $165.94mg{\cdot}100g^{-1}$) and ellagic acid (45.7, $52.1mg{\cdot}100g^{-1}$ ) than the wild raspberry of Ulleungdo, the contents of total flavonoids (14.28, $14.90mg{\cdot}100g^{-1}$) and total anthocyanins (28.69, $30.48mg{\cdot}100g^{-1}$) were higher. Also the wild raspberry of Ulleungdo, 'Wangttal', and the unknown raspberry cultivar of Kimhae had higher antioxidant activities measured by FRAP (Ferric reducing antioxidant power), DPPH (2,2-diphenyl-1-picrylhydrazyl), and ABTS (2,2' azinobis-(3-ethylbenzothiazoline-6-sulphonic acid) assays. The present study shows that three raspberry cultivars could be potent resources for raspberry breeding and functional material development.

• Preventive Nutrition and Food Science
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• v.14 no.3
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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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• v.58 no.2
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• pp.189-194
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• 2015

Ten compounds were isolated from the ethanolic extract of the leaves of Acacia catechu (Fabaceae), and their structures were identified as nine flavonoids [(+)-catechin (1), (-)-epicatechin (2), (+)-afzelechin (3), (-)-epiafzelechin (4), (+)-mesquitol (5), kaempferol (6), quercetin (7), quercetin 3-methyl ether (8), and caryatin (9)] and an ellagic acid (10). The chemical structures of these compounds were identified on the basis of spectroscopic methods (mass spectrometry, 1D and 2D nuclear magnetic resonance) and comparison with literature values. This is the first time that the isolation of caryatin (9) has been reported from Acacia genus.

• Proceedings of the Korea Environmental Mutagen Society Conference
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• 2001.10b
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• pp.110-110
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• 2001

• YAKHAK HOEJI
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• v.39 no.2
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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.