• Title/Summary/Keyword: Water solvent

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Preparation and Release Behavior of Atorvastatin Calcuim - Encapsulated Polyoxalate Microspheres (아토르바스타틴 칼슘을 함유한 폴리옥살레이트 미립구의 제조 및 방출거동)

  • Lee, Cheon Jung;Kim, Su Young;Lee, Hyun Gu;Yang, Jaewon;Park, Jin Young;Cha, Se Rom;Lim, Dong-Kwon;Lee, Dongwon;Khang, Gilson
    • Polymer(Korea)
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    • v.38 no.5
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    • pp.656-663
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    • 2014
  • Atorvastatin calcium-loaded polyoxalate (POX) microspheres were prepared by an emulsion solvent-evaporation/ extraction method of oil-in-oil-in-water ($O_1/O_2/W$) for sustained release. We investigated the release behavior according to initial drug ratio, molecular weight ($M_w$) and concentration of POX and concentration of emulsifier. The microsphere was characterized on the surface, the cross-section morphology and the behavior of atorvastatin calcium release for 10 days by scanning electron microscopy (SEM) and high performance liquid chromatography (HPLC). The analysis of crystallization was analyzed to use X-ray diffraction (XRD), differential scanning calorimeter (DSC) and Fourier transform infrared (FTIR). These results showed that the release behaviors can be controlled by preparation conditions.

Biological Activities and Chemical Characteristics of Monascus-Fermented Korean Red Ginseng (홍국발효홍삼의 이화학적 특성 및 생리활성)

  • Park, Jin-Chul;Cha, Jae-Young;Lee, Chi-Hyeong;Doh, Eun-Soo;Kang, In-Ho;Cho, Young-Su
    • Journal of Life Science
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    • v.19 no.11
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    • pp.1553-1561
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    • 2009
  • This study investigated the biological activities and chemical characteristics of Monascus-fermented Korean red ginseng (MFRG). The comparative activities of water, ethanol, and methanol extracts from MFRGE and Korean red ginseng (RG) were tested in vitro of anti-oxidative models of linoleic acid peroxidation by thiocyanate and thiobarbituric acid (TBA) methods and DPPH ($\alpha,\alpha'$-diphenyl-$\beta$-picrylhydrazyl)radical scavenging activities. In addition, measurements of their bioactive total phenolic compounds and minerals, and extract yield, were obtained. The extract yield of each solvent extracted from MFRG and RG was aqueous by 6.58% and 5.83%, ethanol by 0.62% and 0.98%, and methanol by 1.27% and 3.04%, respectively. Total phenolic compounds were higher in all solvents extracted from MFRG than those from RG. Major mineral contents (ppm) of MFRG and RG were K by 16,936 and 22,386, Ca by 2,310 and 3,693, Mg by 2,703 and 2,647, respectively. The DPPH radical scavenging activities were higher in all solvents extracted from MFRG than those from RG, however, all these extracts exhibited a relatively low level of radical-scavenging activity compared to the butylated hydroxytoluene (BHT). In antioxidative activities determined by TBA method using linoleic acid peroxidation, 70% methanol extract from MFRG and RG showed the highest antioxidative activity at a concentration of 0.1%. These results may provide the basic data to understand the biological activities of bio-active materials derived from MFRG.

Bioactive Compounds and Antioxidant Activity of Jeju Camellia Mistletoe (Korthalsella japonica Engl.) (제주 동백나무 겨우살이의 용매별 기능성 성분 및 항산화 작용)

  • Kang, Da Hee;Park, Eun Mi;Kim, Ji Hye;Yang, Jung Woo;Kim, Jung Hyun;Kim, Min Young
    • Journal of Life Science
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    • v.26 no.9
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    • pp.1074-1081
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    • 2016
  • Mistletoes are hemi-parasitic plant growing on different host tree and shrubs. They are traditionally used in folkloric medicine for the treatment of diarrhea, cough, diabetes, hypertension, cancer and skin infection. The purpose of this study was to determine the contents of phenolics and antioxidant activity of 70% ethanol, 100% methanol and hot water extracts of Jeju camellia mistletoe (Korthalsella japonica Engl.). Ethanol was most effective in extracting total phenols (7,427 mg gallic acid equivalent (GAE)/100 g) and flavonoid (1,777 mg rutin equivalent (RE)/100 g). The free radical scavenging activity, 1,1-diphenyl-2-picryl hydrazyl (DPPH) (EC50 = 7.8 mg/ml) and hydrogen peroxide (H2O2) (EC50 = 1.4 mg/ml), and the capacity for chelating metal ions (EC50 = 8.0 mg/ml) and reducing power (EC50 = 14.9 mg/ml) of the samples also higher in ethanolic extracts. The strong correlation (r2 = −0.996~−0.881) between antioxidant capacities and the phenolic contents implied that phenolic compounds are a major contributor to the antioxidant activity of the ethanolic extracts of Jeju camellia mistletoe. As conclusions, Jeju camellia mistletoe contains bioactive substances with a potential for reducing the physiological as well as oxidative stress and this could explain the suggested cancer preventive effect of these plants as well as their protective role on other major diseases.

Kinetics and Hydrolysis Mechanism of Herbicidal N-(2,6-dimethoxypyrimidin-2-yl)aminocarbonyl-2-(1-hyd roxy-2-fluoroethyl)benzenesulfonamide Derivatives (제초성, N-(2,6-dimethoxypyrimidin-2-yl)aminocarbonyl-2-치환(Z)-6-(1-hyd roxy-2-fluoroethyl)benzenesulfonamide 유도체의 가수분해 반응 메카니즘)

  • Lee, Chan-Bog;Ryu, Jae-Wook;Kim, Dae-Whang;Sung, Nack-Do
    • Applied Biological Chemistry
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    • v.38 no.5
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    • pp.455-462
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    • 1995
  • The new six herbicidal N-[(pyrimidin-2-yl)aminocarbonyl]-2-substituted-6-(1-hydroxy-2-fluoroethyl)benzenesulfonamide derivatives(S) were synthesized and rate constants for the hydrolysis of thier in the range of pH $1.0{\sim}10.0$ have been studied in 15%(v/v) aqueous acetonitrile solution at $45^{\circ}C$. From the basis of the results, pH-effect, solvent effect, ortho-substituent effect, thermodynamic parameters(${\Delta}H^{\neq}$ & ${\Delta}S^{\neq}$), pKa constant(4.80), rate equation, analysis of hydrolysis products(2-(1-hydroxy-2-fluoroethyl)benzenesulfonamide & 4,6-dimethoxyaminopyrimidine), it may be concluded that the general acid catalyzed hydrolysis through $A-S_E2$ mechanism and specific acid catalyzed hydrolysis through A-2 type(or $A_{AC}2$) mechanism proceeds via conjugate acid($SH^+$) and tetrahedral intermediate(I) below pH 8.0, whereas, above pH 9.0, the general base catalyzed hydrolysis by water molecules(B) through $(E_1)_{anion}$ mechanism proceeds via conjugate base(CB). In the range between $pH\;7.0{\sim}pH\;9.0$, these two reactions occur competitively.

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Anti-oxidant and Anti-inflammation Activity of Fractions from Aster glehni Fr. Schm. (섬쑥부쟁이(Aster glehni Fr. Schm.) 분획물의 항산화 및 항염증 활성)

  • Kim, Han-Hyuk;Park, Gun-Hye;Park, Kang-Soo;Lee, Jin-Young;An, Bong-Jeun
    • Microbiology and Biotechnology Letters
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    • v.38 no.4
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    • pp.434-441
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    • 2010
  • The Plants and their extracts containing polyphenol have been shown to be associated with decreased the cause of aging and variety of disease such as reaction oxygen species (ROS) and reactive nitrogen species (RNS) in several recent studies. We conducted to investigate whether the extracts and fractionation isolated from Aster glehni Fr. Schm. has an inhibitory effect association with oxidation or inflammation. The Aster glehni Fr. Schm. 70% aq. MeOH was fractioned according to polarity with n-hexane layer, EtOAc layer, n-BuOH layer and water layer. The electron donating ability of EtOAc, n-BuOH solvent fraction from Aster glehni Fr. Schm. was about 58.0%, 46.4% at $50\;{\mu}g/mL$, respectively. The superoxide anion radical inhibitory effect of EtOAc extracts was about 64.65% at $50\;{\mu}g/mL$, and n-BuOH extracts was 35.66% at $50\;{\mu}g/mL$. EtOAc layer to the inhibition activity of hyaluronidase and lipoxygenase were inhibited about 24.37%, 29.5% at $5\;{\mu}g/mL$. In the anti-inflammation effect of EtOAc layer inhibited the generation of nitric oxide. also, these results showed that EtOAc extract inhibited 81.5% at $50\;{\mu}g/mL$ on the expressions of iNOS protein in Raw264.7 cell line.

Antioxidation, Antimicrobial and Antithrombosis Activities of Aged Black Garlic (Allium sativum L.) (흑마늘의 항산화, 항균 및 항혈전 활성)

  • Jung, In-Chang;Sohn, Ho-Yong
    • Microbiology and Biotechnology Letters
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    • v.42 no.3
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    • pp.285-292
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    • 2014
  • In the course of study for development of functional food ingredients from aged black garlic (ABG), heat-treated ripe bulbs of Allium sativum L., the water extracts from raw-garlic (RG) and ABG, and the subsequent organic solvent fractions of ABG were prepared, and their antioxidant, antimicrobial, and antithrombosis activities were compared. The extraction yield of ABG was 4-folds higher than that of RG, and the contents of total polyphenol, total flavonoid, total sugar and reducing sugar in the ABG extract were 4-folds, 1.56-folds, 3.36-folds and 6.75-folds higher than those of the RG extract, respectively. In antioxidation activity assay, the extract of ABG showed minor scavenging activity against DPPH anion, but revealed strong scavenging activity against ABTS cation and nitrite. Especially, the ethylacetate fraction from the ABG extract demonstrated stronger antioxidation activity than the RG extract and other fractions. Although the antimicrobial and antithrombosis activities of the RG extract did not appear in the ABG extract, the ethylacetate fraction from the ABG extract had antibacterial activity against Staphylococcus aureus and Bacillus subtilis, and strong antithrombosis activity via the inhibition of prothrombin, blood coagulation factors and platelet aggregation. All extracts and fractions did not show any hemolytic activity against human red blood cells up to 5 mg/ml. Our results suggest that the ethylacetate fraction of ABG could be applicable to the development of functional food ingredients for antithrombosis agents.

Synthetic Conditions of an Aspartame Precursorby Immobilized Thermolysin (고정화 Thermolysin을 사용한 아스파탐 전구체의 최적 합성조건 선정)

  • Han, Min-Su;Kim, Woo-Jung
    • Korean Journal of Food Science and Technology
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    • v.27 no.4
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    • pp.564-570
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    • 1995
  • N-Benzoyl-L-aspartyl-L-phenylalanine methyl ester(BzAPM), a novel aspartame precursor, was investigated for its enzymatic synthesis by immobilized thermolysin using a water-miscible organic solvent system. The substrate used were N-benzoyl-L-aspartic acid(BzAsp) and L-phenylalanine methyl ester (PheOMe). Synthetic conditions such as substrates concentration, temperature, pH, and some metallic ions were varied to study their effects on BzAPM synthesis. The synthetic reaction rate increased linearly as the PheOMe concentration increased at a constant concentration of BzAsp(100 mM), and the maximum reaction rate was obtained at BzAsp concentration of 200 mM when 300 mM PheOMe was used. The optimum pH and temperature were found to be 6.1 and $40^{\circ}C$, respectively. The metallic ions such as $Zn^{2+},\;Mg^{2+},\;Mn^{2+},\;Fe^{2+},\;Pb^{2+}\;and\;Cu^{2+}$ at 5 mM level showed inhibitory effect on BzAPM synthesis, while $Co^{2+}$ and $Ca^{2+}$ ion increased synthesis. $Co^{2+}$ ion was also found to have synergistic effect with $Ca^{2+}$ ion. Benzoic acid, L-phenylalanin and NaCl showed inhibitory effect.

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Antimicrobial Activity of Quercus mongolica Leaf Ethanol Extract and Organic Acids against Food-borne microorganisms (식중독균에 대한 신갈나무 잎 추출물과 유기산의 항균효과)

  • Kong, Young-Jun;Park, Boo-Kil;Oh, Deog-Hwan
    • Korean Journal of Food Science and Technology
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    • v.33 no.2
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    • pp.178-183
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    • 2001
  • This study was conducted to determine the optimal extraction condition of temperatures and kinds of extraction solvent, and antimicrobial activity of ethanol extract of Quercus mongolica leaf and organic acid against foodborne microorganisms. The antimicrobial activity of ethanol extract at $60^{\circ}C$ for 6 hour against foodborne microorganisms was stronger than those at $30^{\circ}C\;and\;90^{\circ}C$. Also, the ethanol extract showed stronger antimicrobial activity than those of water and methanol extract. The minimal inhibitory concentrations of the ethanol extract of Quercus mongolica leaf against B. cereus and L. monocytogenes, was $62.5{\sim}125\;{\mu}g/mL$ but, the minimal inhibitory concentration was $250\;{\mu}g/mL$ against S. typhimurium and P. aeruginosa and over $500\;{\mu}g/mL$ against E. coli O157:H7, respectively. The minimal inhibitory concentrations of the lactic, citric, acetic acid and the ethanol extract of Quercus mongolica leaf against B. cereus and L. monocytogenes was 2500, 5000, 1250 and $125\;{\mu}g/mL$, respectively. The combined effect of each organic acid and the ethanol extract against B. cereus was not observed but, synergistic effect was observed against L. monocytogenes. In the meantime, when the ethanol extract was combined with each organic acid at sub-lethal concentration, the combination did not increase the inhibitory effect of the most active single compound alone against E. coli O157:H7, respectively.

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Thermodynamics of the Micellization of Cetylpyridinium Bromide in Some Aqueous Alcohol Solutions (몇 가지 알코올-수용액에서 Cetylpyridinium Bromide의 미셀화의 열역학적 성질)

  • Chung Jong-Jae;Lee Sang-Wook;Choi Joon-Ho
    • Journal of the Korean Chemical Society
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    • v.37 no.1
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    • pp.49-54
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    • 1993
  • The effects of added alcohols on the critical micelle concentration(CMC) of cetylpyridinium bromide(CPB) were investigated by the UV-Vis spectrophotometer at the temperature range of 8∼45$^{\circ}C$. The CMC of CPB was increased with the addition of methanol in the whole temperature region studied, while decreased with the addition of ethanol and propanol. The increase of CMC with the addition of methanol may be attributable to the increasing solvent power of the methanol-water mixture, because methanol was scarcely solubilized into the palisade layer of the micelle of CPB. The decrease of CMC with the inclusion of ethanol and propanol may be derived from the solubilization of alcohols into the micelles. On the other hand, the CMC was decreased with the temperature rise in the low-temperature region below about 25$^{\circ}C$, and the CMC was increased in the high-temperature region above that. The thermodynamic parameters (${\Delta}G_M^{\circ},\;{\Delta}H_M^{\circ},\;and\;{\Delta}S_M^{\circ}$) of the micellization of CPB were obtained in some aqueous alcohol solutions. In the whole temperature region (8∼45$^{\circ}C$), the values of ${\Delta}G_M^{\circ}$ were negative, while those of ${\Delta}S_M^{\circ}$ were positive. And in the temperature region below about 25$^{\circ}C$ the ${\Delta}H_M^{\circ}$ values were positive, while in the temperature region above that the values were negative.

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Formation of TiO(OH)$_2$ Ultrafine Particles by Reverse Micelle (역마이셀에 의한 TiO(OH)$_2$ 미세분말 제조)

  • 장화익;강석원;이광래
    • Journal of the Korean Ceramic Society
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    • v.35 no.6
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    • pp.594-602
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    • 1998
  • Titanium hydroxide (TiO({{{{ {OH }_{2 } }})) fine particles were produced by the reverse micelle technique. For the formation of titanium hydroxide (TiO({{{{ {OH }_{2 } }})) particles with the technique reversed micellar solution was prepared by solubilizing water into organic solvent (isooctane) with a surfactant and titanium alkoxide (tetraisopropyl orthotitanate) diluted with isopropyl alcohol was added to the reversed micellar solution. The hdrolyzed species (TiO({{{{ {OH }_{2 } }})) was formed by the hydrolysis of titanium alkoxide and titanium dioxide is then formed by the condensation of the hydrolyzed species. There are several process variables such as surfactants concentration of surface cosurfactant hydrolysis temperature and pH. In this work the ef-fects of process variables on paticle shapes particle size distribution and paticle agglomeration were bi-nodal for an anionic surfactant(AOT) in the whole range of temperature pH and surfactant concentration of this experiment. The addition of ethanol as a cosurfactant resulted in narrow particle size distribution of the experiment. The additiono of ethanol as a cosurfactant resulted in narrow particle size distribution and 0.12${\mu}{\textrm}{m}$ of smaller average particle diameter. FT-IR spectrum of particles shows the absorption peak of Ti-OH bonding and Ti-O bonding. An exothermic peak around 41$0^{\circ}C$ in TGA-DTA curve shows that crys- tallized anatase phase appears and completely transits to anatase around 45$0^{\circ}C$.

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