• Title/Summary/Keyword: Inhibitory Activity

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Screening of Inhibitory Activity of Plant Extracts against Farnesyl Protein Transferase (식물추출물의 파네실 전달효소 저해활성 검색)

  • Kang, Hyun-Mi;Lee, Seung-Ho;Ryu, Shi-Yong;Son, Kwang-Hee;Yang, Deok-Cho;Kwon, Byoung-Mog
    • Korean Journal of Pharmacognosy
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    • v.34 no.1 s.132
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    • pp.91-99
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    • 2003
  • Ras proteins play an important role in intracellular signal transduction pathways involved in cell growth and the mutated twas genes have been found in thirty percent of human cancers. Ras proteins (H-, K- and N-Ras) are small guanine nucleotide binding proteins that undergo a series of posttranslational modifications including the farnesylation onto cysteine 186 at C-terminal of Ras by farnesyl protein transferase (FPTase). This is a mandatory process for retention of transforming ability. Therefore, inhibitors of FPTase have a promising to be effective antitumor agents. In our screening program for FPTase inhibitors, the methanol extracts of 193 plants were screened for the inhibitory activity against FPTase partially purified from the rat brain. Extracts of 7species plants including Areca catechu, Saururus chinensis, Curcuma longa, Artemisa princeps, Paeonia suffruticosa, Spatholobus suberectus, Cinnamomum cassia, Cinnamomum japonicum inhibited more than 60% of FPTase activity at a concentration of $100\;{\mu}g/ml$.

Inhibitory Activity against Helicobacter pylori of Isolated Compounds from Pinus koraiensis Siebold et Zucc Leaves

  • Jo, Bun-Sung;Cho, Young-Je
    • Journal of Applied Biological Chemistry
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    • v.59 no.1
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    • pp.19-23
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    • 2016
  • A phenol substance was extracted from Pinus koraiensis Siebold et Zucc leaf extracts and its biological efficacy was measured. The highest content of the phenol substance contained in Pinus koraiensis Siebold et Zucc leaves was 13.5 mg/g, which was obtained when it was extracted with 80% ethanol. At a concentration of 200 mg/mL, the phenolic substances extracted with 80% ethanol and water showed antimicrobial activities against Helicobacter pylori, producing clear zones of 10 and 12 mm diameter, respectively. Pinus koraiensis Siebold et Zucc. leaf extracts were separated using a Sephadex LH-20 column and 4 fractions were obtained (fractions A-D). Fractions C and D showed the greatest inhibitory activity against Helicobacter pylori producing 10.1 and 12.3 mm clear zones, respectively. These two fractions were purified using a Sephadex LH-20 and MCI-gel column ($H_2O{\rightarrow}100%$ ethanol). Purified compounds A and B were identified as syringic acid and compound C was identified as p-coumaric acid based on $^1H$-nuclear magnetic resonance (NMR), $^{13}C$-NMR, and fast atom bombardment mass spectrometry spectra. When two or more purified compounds were mixed, a synergistic effect of anti-Helicobacter pylori activity was evident. This result indicates that extracts of Pinus koraiensis Siebold et Zucc leaves could be considered a functional food because of their high antimicrobial properties.

The Effects of Chicken Leg Bone Extract on Antioxidative Properties under Different Heating Condition

  • Cheng, Fu-Yuan;Wan, Tien-Chun;Huang, Chao-Wei;Tominaga, Kana;Lin, Liang-Chuan;Sakata, Ryoichi
    • Asian-Australasian Journal of Animal Sciences
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    • v.21 no.12
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    • pp.1815-1820
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    • 2008
  • The aim of this study was to extract chicken leg bone, which is a by-product of industrial poultry processing, using different heating temperatures (80, 90 and $100^{\circ}C$) and durations (5, 10 and 15 min). The pH value, soluble protein content, peptide content and antioxidative properties, including superoxide anion scavenging ability, 1, 1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging ability, reducing capacity and inhibitory activity of linoleic acid peroxidation, were measured. The results showed no significant differences (p>0.05) in pH value among all treatments. Decreased soluble protein content and peptide content were observed in chicken leg bone extract obtained under higher heating temperatures (90 or $100^{\circ}C$) and longer heating durations (10 or 15 min). In antioxidative properties, the extracts which were heated at 90 or $100^{\circ}C$ for 15 min exhibited significantly higher superoxide anion scavenging ability, DPPH free radical scavenging ability, reducing capacity and inhibitory activity of linoleic acid peroxidation (p<0.05).

솔잎 추출물의 항균성 검색

  • Choi, Moo-Young;Choi, Eun-Jung;Lee, Eun;Rhim, Tae-Jin;Cha, Bae-Cheon;Park, Hee-Juhn
    • Microbiology and Biotechnology Letters
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    • v.25 no.3
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    • pp.293-297
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    • 1997
  • To develope natural food preservatives of pine needle (Pinus densiflora Seib et Zucc.) extract, pine needle sap, ethanol and ether extracts were prepared for investigation of antimicrobial activities against food-related bacteria and yeasts. All extracts exhibited growth inhibiting activities for most of microorganisms tested. However, in general, growth inhibiting activities were higher in ethanol extract than in sap or ether extract. Minimum inhibitory concentrations (MIC) of ethanol extract for Lactobacillus casei, Pseudomonas aeruginosa or Escherchia coli were as low as 0.1 mg/ml, whereas MIC of sap or ether extract for most bacteria and yeasts were 0.25-0.8mg/ml, indicating that the ethanol extract showed the antimicrobial activity by 2.5 $\sim$8 times higher than the sap and ether extract. The antimicrobial activity of the ethanol extract was reduced by heating or alkali treatment. Moreover, growth of Pseudomonas aeruginosa was completely inhibited within 24 hours by the addition of at least 50ppm of ethanol extract. These findings suggest that pine needle, specially the ethanol extrat may play a role for natural food preservatives.

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Inhibition of Melanogenesis by Dioctyl Phthalate Isolated from Nigella glandulifera Freyn

  • Nguyen, Duc T. M.;Nguyen, Dung H.;Hwa-La, Lyun;Lee, Hyang-Bok;Shin, Jeong-Hyun;Kim, Eun-Ki
    • Journal of Microbiology and Biotechnology
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    • v.17 no.10
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    • pp.1585-1590
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    • 2007
  • Although a number of melanogenesis inhibitors have recently been reported and used as cosmetic additives, none is completely satisfactory, leaving a need for novel skin-depigmenting agents. Thus, to develop a novel skin depigmenting agent from natural sources, the inhibition of melanogenesis by Chinese plants was evaluated. A methanolic extract of Nigella glandulifera Freyn was found to inhibit the melanin synthesis of murine B16F10 melanoma cells by 43.7% and exhibited a low cytotoxicity (8.1%) at a concentration of $100\;{\mu}g/ml$. Thus, to identify the melanogenesis-inhibiting mechanism, the inhibitory activity towards tyrosinase, the key enzyme of melanogenesis, was further evaluated, and the results showed inhibitory effects on the activity of intracellular tyrosinase yet not on mushroom tyrosinase. Finally, to isolate the compounds with a hypopigmenting capability, activity-guided isolation was performed, and Dioctyl phthalate identified as inhibiting melanogenesis.

Effects of Oxidation Reduction Potential and Organic Compounds on Anammox Reaction in Batch Cultures

  • Viet, Truong Nguyen;Behera, Shishir Kumar;Kim, Ji-Won;Park, Hung-Suck
    • Environmental Engineering Research
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    • v.13 no.4
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    • pp.210-215
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    • 2008
  • The present study investigates the effect of oxidation-reduction potential (ORP) and organic compounds on specific anaerobic ammonium oxidation activity (SAA) using batch experiments. The batch tests were based on the measurement of nitrogen gas production. The relationship between ORP and dissolved oxygen (DO) concentration was found to be ORP (mV) = 160.38 + 68 log [$O_2$], where [$O_2$] is the DO concentration in mg/L. The linear relationship obtained between ORP and SAA ($R^2$ = 0.99) clearly demonstrated that ORP can be employed as an operational parameter in the Anammox process. At ORP value of -110 mV, the SAA was $0.272{\pm}0.03\;g\;N_2-N\;(g\;VSS)^{-1}\;d^{-1}$. The investigation also revealed inhibitory effect of glucose on the SAA while acetate concentration up to 640 mg COD/L (corresponding to 10 mM) had stimulating effect on the SAA. However, acetate concentration beyond 640 mg COD/L had inhibitory effect on the Anammox activity. The results indicated that nitrogen rich wastewaters containing low level organic matter could be better treated by Anammox microorganisms in real-world conditions after some acidification process.

Purification and Characterization of an Antilisterial Bacteriocin Produced by Leuconostoc sp. W65

  • Oh, Se-Jong;Kim, Myung-Hee;Churey, John-J.;Worobo, Randy-W.
    • Journal of Microbiology and Biotechnology
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    • v.13 no.5
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    • pp.680-686
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    • 2003
  • This study was carried out to characterize the antilisterial substances produced by Leuconostoc sp. W65 and to evaluate the effects of pH, temperature, and time on inhibitory activity using response surface methodology. Leucocin W65, an antilisterial substance produced by Leuconostoc sp. W65, markedly inhibited the growth of Listeria monocytogenes, L. innocua, and L. ivanovii, whereas other pathogens including Gram-negative bacteria were not susceptible. The pH was the most effective factor with regard to bacteriocin activity, while temperature and time of heat treatment had no significant effect. Fifty percent of inhibitory activity remained after 22.8 min at pH 4.2 and $121^{\circ}C$. Leucocin W65 was purified by ammonium sulfate precipitation, hydrophobic interaction chromatography, and tricine-SDS-PAGE. Compositional analysis originally estimated the peptide to be 56 amino acids in length without asparagine, glutamine, and tryptophane. The sequence of partial N-terminal amino acid residues of purified bacteriocin was identified as follows: $NH_{2}-XGXAGVXPXGGQQPXVPLXYP$.

Effect of Acasia (Robinia pseudo-acasia) Flower on the Physiological Functionality of Korean Traditional Rice Wine. (아카시아 꽃(Robinia pseudo-acasia)의 첨가가 전통주의 생리기능성에 미치는 영향)

  • 서승보;김재호;김나미;최신양;이종수
    • Microbiology and Biotechnology Letters
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    • v.30 no.4
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    • pp.410-414
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    • 2002
  • In order to develop a Korean traditional rice wine which by acasia flower added alcohol fermentation was investigated by addition of 5%, 10'h, 15% nuruk and 10% acasia into the wine mash. The maximum amount of ethanol (16.4%) was obtained when 10% acasia flower and 15% nuruk were added in cooked rice for the fermentation by Saccharomyces cerevisiae at $25^{\circ}C$ for 20 days. The overall acceptability and physiological functionalities of the rice wine prepared by addition of different concentration (5-50%) of acasia flower into mash were investigated and compared. The A-15 rice wine which was brewed by addition of 15% acasia flower into mash showed the best acceptability. Its angiotensin-converting enzyme inhibitory activity and tyrosinase inhibitory activity were 80.3% and 94.2%, respectively. The electron-donating ability (23.4%) and nitrite scavenging activity (21.5%) were also higher than those of traditional rice wine.

Lactic Acid Bacteria Increase Antiallergic Effect of Artemisia princeps Pampanini SS-1

  • Lee, Seung-Hoon;Shin, Yong-Wook;Bae, Eun-Ah;Lee, Bo-Mi;Min, Sung-Won;Baek, Nam-In;Chung, Hae-Gon;Kim, Nam-Jae;Kim, Dong-Hyun
    • Archives of Pharmacal Research
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    • v.29 no.9
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    • pp.752-756
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    • 2006
  • Artemisia princeps Pampanini, which is called Ssajuarissuk in Korean (SS-1), was fermented with lactic acid bacteria (LAB) and their passive cutaneous anaphylaxis reaction-inhibitory activity was investigated. Of these fermented agents, SS-1 extract fermented with Bifidobacterium infantis K-525 (F-SS-1) most effectively inhibited the release of ${\beta}$-hexosamindase from RBL-2H3 cells induced IgE. In IgE-induced RBL-2H3 cells, F-SS-1 inhibited proinflammatory cytokines IL-6 and $TNF-{\alpha}$ mRNA expression. Oral administration of SS-1 and F-SS-1 to mice inhibited passive cutaneous anaphylaxis (PCA) reaction induced by IgE and scratching behaviors induced by compound 48/80. The inhibitory activity of F-SS-1 against scratching behaviors was more effective than that of SS-1. These findings suggest that the fermentation of SS-1 with LAB can increase its antiallergic activity.

Comparative Molecular Field Analyses (CoMFA) on the Mela-nogenesis Inhibitory Activities of Alkyl-3,4-dihydroxybenzoyl Derivatives.

  • Kim, Sang-Jin;Sung, Nack-Do;Lee, Tack-Hyuck
    • Proceedings of the SCSK Conference
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    • 2003.09a
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    • pp.225-231
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    • 2003
  • To search and development a new material with superior melanogenesis inhibitory activity, the bioactivities (obs. pl$_{50}$) of alkyl-3,4-dihydroxybenzoyl esters and N-alkyl-3,4-dihydroxybenz-oyl amides as substrate molecules were measured in mouse melanoma cells. And also, we have studied that 3-D QSARs (3 dimensional Quantitative Structure-Activity Relationships) between molecular interaction field of substrates and the bioactivities were analyzed using CoMFA (Comparative Molecular Field Analyses) method. When cross-validation value (q$^2$) is 0.68 at 3 components, the Pearson correlation coefficient ($r^2$) is 0.900. From the basis on the findings, the model was appeared by the contour map such as steric field and electrostatic field relationships between quantitative structure and the bioactivity of the various substrate derivatives. Measured bioactivities (obs. pl$_{50}$) of unknown compounds are very similar to predicted activity (pred. pl$_{50}$) according to the CoMFA model. As the results of prediction, we could conclude that the bioactivities were increased by creation of R$_1$ substitution of 5,5-dime-thylhexoxy, 6,6-dimethylheptyl, 1-amino-6,6-dimethylheptyl group etc and R$_2$ substitution of hydroxy, methyl, methoxy group etc.p etc.

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