• Title, Summary, Keyword: Ellagic

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[ $\beta$ ]-Secretase (BACE1) Inhibitors from Pomegranate (Punica granatum) Husk

  • Kwak Hye-Min;Jeon So-Young;Sohng Bang-Ho;Kim Jong-Guk;Lee Jin-Man;Lee Kyung-Bok;Jeong Hyun­Hee;Hur Jong-Moon;Kang Young-Hwa;Song Kyung-Sik
    • 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.

Ellagic Acid Inhibits Migration and Invasion by Prostate Cancer Cell Lines

  • Pitchakarn, Pornsiri;Chewonarin, Teera;Ogawa, Kumiko;Suzuki, Shugo;Asamoto, Makoto;Takahashi, Satoru;Shirai, Tomoyuki;Limtrakul, Pornngarm
    • 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.

Ellagic acid plays a protective role against UV-B-induced oxidative stress by up-regulating antioxidant components in human dermal fibroblasts

  • Baek, Beomyeol;Lee, Su Hee;Kim, Kyunghoon;Lim, Hye-Won;Lim, Chang-Jin
    • The Korean Journal of Physiology and Pharmacology
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    • v.20 no.3
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    • pp.269-277
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    • 2016
  • Ellagic acid (EA), an antioxidant polyphenolic constituent of plant origin, has been reported to possess diverse pharmacological properties, including anti-inflammatory, anti-tumor and immunomodulatory activities. This work aimed to clarify the skin anti-photoaging properties of EA in human dermal fibroblasts. The skin anti-photoaging activity was evaluated by analyzing the reactive oxygen species (ROS), matrix metalloproteinase-2 (MMP-2), total glutathione (GSH) and superoxide dismutase (SOD) activity levels as well as cell viability in dermal fibroblasts under UV-B irradiation. When fibroblasts were exposed to EA prior to UV-B irradiation, EA suppressed UV-B-induced ROS and proMMP-2 elevation. However, EA restored total GSH and SOD activity levels diminished in fibroblasts under UV-B irradiation. EA had an up-regulating activity on the UV-B-reduced Nrf2 levels in fibroblasts. EA, at the concentrations used, was unable to interfere with cell viabilities in both non-irradiated and irradiated fibroblasts. In human dermal fibroblasts, EA plays a defensive role against UV-B-induced oxidative stress possibly through an Nrf2-dependent pathway, indicating that this compound has potential skin antiphotoaging properties.

Validation of analytical method and antioxidant properties of Eriobotrya japonica Lindl. Leaf extract according to extraction solvent (추출용매 조건에 따른 비파 잎 추출물의 항산화 활성 및 유효성분의 분석법 밸리데이션)

  • Kim, Hyun-Hee;Heo, Mi-Ra;Lee, Songmi;Yim, Soon-Ho
    • Korean Journal of Food Science and Technology
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    • v.51 no.4
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    • pp.301-308
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    • 2019
  • The antioxidant properties of Eriobotrya japonica leaf extract were investigated using DPPH and ABTS radical scavenging assay. The 80% ethanol extract of leaves ($IC_{50}$ values for DPPH and ABTS were 13.9 and $10.9{\mu}g/mL$, respectively) and young leaves ($IC_{50}$ values for DPPH and ABTS were 20.7 and $17.3{\mu}g/mL$, respectively) showed high radical scavenging activity. Additionally, the quantitative method for estimation of ellagic acid and chlorogenic acid from E. japonica leaves was optimized by HPLC/DAD. This method showed high linearity of the calibration curve with a coefficient of correlation ($R^2$) equal to 0.999. The LOD values for ellagic acid and chlorogenic acid were 2.35 and $0.73{\mu}g/mL$, respectively, whereas LOQ values were 7.13 and $2.22{\mu}g/mL$, respectively. Recovery of the two compounds was 99.7-108.0% with RSD values less than 5.31%. These results suggest that 80% ethanol extract of E. japonica leaves could serve as a potential source of natural antioxidant for us in various industrial applications.

Antioxidant activities and Validation of Analytical Method of Marker compounds in strawberry fruits from various cultivars (딸기 품종별 추출물의 항산화활성 및 지표성분 밸리데이션)

  • Yong, Ye Seul;Lee, Songmi;Byun, Na-Young;Sun, Sangouk;Kim, Min-Jung;Jang, Seo Woo;Jang, Won Suk;Lee, Sun Yi;Yim, Soon-Ho
    • Korean Journal of Food Science and Technology
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    • v.51 no.6
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    • pp.517-523
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    • 2019
  • In this study, we investigated antioxidant capacity of 20 strawberry extract using the DPPH and ABTS assay and HPLC-DAD validation method. The total polyphenolic and flavonoids contents of 20 strawberry extracts were 22.77-107.61 mg TAE/100 g FW and 17.58-44.12 mg QE/100 g FW. The Aiberry and Elie star showed the highest total polyphenol and flavonoid contents, respectively. The DPPH radical scavenging activity of what was 1540.6-1124.0 μmol TEAC/100 g FW and Derunoka showed the highest activity. The ABTS radical scavenging activity was 6352.3-4592.3 μmol TEAC/100 g FW and FA23 showed the highest activity. The HPLC-DAD method for the quantitation of ellagic acid results showed high linearity in various concentration ranges, and the limit of detection was 2.35 μg/mL. The limit of quantification was 7.12 μg/mL. Relative standard deviation values from intra-and inter-day precision were less than 5.31%. Recovery rate at 10, 50, and 100 μg/mL, respectively, were 100.0-101.0% with relative standard deviation (RSD) values less than 5.30%. These results provide viable information for the validation of antioxidant capacity in strawberry fruits.

Phenolic Compounds from Aerial Parts of Euphorbia pekinensis (II) (대극 지상부의 페놀성 화합물(제2보))

  • Ahn, Byung-Tae;Kang, Sam-Sik
    • Korean Journal of Pharmacognosy
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    • v.27 no.2
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    • pp.142-145
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    • 1996
  • We have previously reported the isolation of seven hydrolyzable tannins and nine flavonoids from Euphorbia pekinensis Ruprecht. Further investigation about the same plant has led to the isolation of kaempferol, quercetin, kaempferol $3-O-(2'-O-galloyl-{\beta}-_D-glucoside)$, quercetin 3-O-(2'-O-galloylrutinoside), ellagic acid and acetonyl geraniin. These compounds were isolated from this plant for the first time.

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Phenolic compounds from the Stems of Sapium japonicum

  • Kang, Shin-Jung;Hong, Seong-Su;Hwang, Bang-Yeon;Ro, Jai-Seup;Lee, Kyong-Soon;Towers, G.H.N.
    • Natural Product Sciences
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    • v.12 no.3
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    • pp.125-128
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    • 2006
  • A chemical examination of the stems of Sapium japonicum PAX et $H_{OFFM}$ (Euphorbiaceae) has led to the isolation of seven phenolic compounds. On the basis of UV, IR, MS, and NMR spectral data and the chemical reaction, the structures of these compounds were identified as gallic acid (1), ellagic acid (2), 3,3'-di-O-methylellagic acid (3), $4-O-({\beta}-D-xylopyranosyl)-3,3'-di-O-methylellagic$ acid (4), $4-O-({\alpha}-D-arabinofuranosyl)-3,3'-di-O-methylellagic$ acid (5), isoquercitrin (6), and geraniin (7).

Isolation and Characterization of Bioactive Compounds from Root of Rubus coreanus Miquel and their Antimicrobial Activity

  • Jang, Ha Na;Ha, Ji Hoon;Lee, Yoon Ju;Fu, Min Min;Park, Soo Nam
    • 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.

Natural Compounds as Inhibitors of Plasmodium Falciparum Enoyl-acyl Carrier Protein Reductase (PfENR): An In silico Study

  • Narayanaswamy, Radhakrishnan;Wai, Lam Kok;Ismail, Intan Safinar
    • Journal of the Chosun 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.

Inhibitory Effect of the Phenolic Compounds from Geranium thunbergii on Rat Lens Aldose Reductase and Galactitol Formation (현초에서 분리된 페놀성 화합물들의 흰쥐 수정체 유래 알도즈 환원효소 및 갈락티톨 생성 억제 효과)

  • Choi, Se-Jin;Kim, Jin-Kyu;Jang, Jai-Man;Lim, Soon-Sung
    • 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.