• Title/Summary/Keyword: Inhibition efficiency

Search Result 345, Processing Time 0.023 seconds

Effect of ion Pairing on the Cellular Transport of Antisense Oligonucleotide

  • Song, Kyung;Kim, Kyoung-Mi;Kim, Jae-Baek;Ko, Geon-Il;Sohn, Dong-Hwan
    • Archives of Pharmacal Research
    • /
    • v.20 no.5
    • /
    • pp.438-442
    • /
    • 1997
  • Antisense oligonucleotide represents an interesting tool for selective inhibition of gene expression. However, their low efficiency of introduction within intact cells remains to be overcome. Antisense-$TGF{\beta}$ (25 mer) and antisense-$TGF{\beta}$ (18 mer) were used to study the cellular transport and biological function of antisense oligonucleotide in vitro. Since TGF and TNF play on important role in regulating the nitric oxide production from macrophages, the action of the above antisense oligonucleotides was easily monitored by the determination of nitrite. Poly-L-lysine, benzalkonium chloride and tetraphenylphosphonium chloride were used as polycations, which neutralize the negative charge of antisense oligonucleotide. The production of nitric oxide mediated by .gamma.-IFN in mouse peritoneal macrophage was increased by antisense-TGF.betha. in a dose-dependent manner. Antisense-$TGF{\beta}$ reduced the nitric oxide release from activated RAW 264.7 cells. Significant enhancement in the nitric oxide production was investigated by the cotreatment of poly-L-lysine with antisense-$TGF{\beta}$On the meanwhile, inhibition effect of antisense-$TGF{\beta}$ is not changed by the addition of poly-L-lysine. These results demonstrate that control of expression of $TGF{\beta}$ and TNF.alpha. gene is achieved using antisense technology and the cellular uptake of antisense oligonucleotide could be enhanced by ion-pairing.

  • PDF

Conversion of Acidic Polysaccharide and Phenolic Compound of Changed Ginseng by 9 Repetitive Steaming and Drying Process, and Its Effects of Antioxidation (인삼의 구증구포에 의한 산성다당체, 페놀성화합물의 변환 및 항산화능)

  • Kim, Do-Wan;Lee, Yun-Jin;Min, Jin-Woo;Kim, Yu-Jin;Rho, Young-Deok;Yang, Deok-Chun
    • Journal of Physiology & Pathology in Korean Medicine
    • /
    • v.23 no.1
    • /
    • pp.121-126
    • /
    • 2009
  • Korean ginseng (Panax ginseng C. A. Meyer) has been used as an important medicinal plant in the Orient for a long time. It has been claimed that ginseng has many beneficial bioactive effects on human health, such as antitumor, antistress, antiaging and enhancing immune functions. Red ginseng possibly have new ingredients converted during steaming and dry process from fresh ginseng. In this study, pharmacological efficacy and ingredient conversion of ginseng by 9 repetitive steaming and drying process were investigated measuring conversion efficiency of acidic-polysaccharide, phenolic compounds and inhibition of peroxide lipides. It was found that acidic-polysaccarides were increased by heat treatment. In addition, maltol of phenolic compounds, strong antioxidant, produced during the process of red ginseng by Maillard reaction. Acidic-polysaccarides and maltol were increased after the 1st and 3rd steaming and drying treatments, but they were decreased gradually after 5th, 7th, and 9th treatments. Antioxidant activity was increased as increasing treatment times of steaming and drying without significance. Effect of red ginseng extract on inhibition of peroxide was increased gradually until after the 7th treatment, but remarkably decreased after the 9th treatment.

Corrosion Inhibitive and Adsorption Properties of a Flavonoid compound for Mild Steel in Acidic Medium (산성 조건에서 부드러운 강철용 부식억제제로 사용되는 플라보노이드계 화합물의 부식억제성질과 흡착성질)

  • Ezhilarasi, J. Christy;Nagarajan, Prabavathy
    • Journal of the Korean Chemical Society
    • /
    • v.55 no.3
    • /
    • pp.495-501
    • /
    • 2011
  • The corrosion inhibitive nature of a flavonoid compound, 3-Hydroxy-7-methoxy-2-phenylchromen-4-one (HMPC), the synergistic effect between HMPC and n-Tetrabutylammonium bromide (TBAB) and their adsorption behavior on mild steel in hydrochloric acid solution were studied by weight loss, potentiodynamic polarization and electrochemical impedance spectroscopy (EIS) measurements. The results of weight loss study at different temperatures revealed that the inhibition efficiency increases with inhibitor concentration and decreases with increase in the temperature of the system. The electrochemical studies showed that the inhibitor acts through mixed mode of inhibition and the inhibitor molecules adsorb on the metal - solution interface forming a protective layer. The adsorption of the inhibitor molecules over the metal surface was supported by the obeyed Langmuir's adsorption isotherm, Scanning Electron Microscopic analysis (SEM) and Fourier Transform Infrared (FT-IR) spectroscopic studies.

Influence of Gamma Irradiation on Greening of Mung Bean Seedlings

  • Kim, Jin-Hong;Moon, Yu-Ran;Kim, Jae-Sung;Lee, Min-Hee;Lee, Seung-Sik;Chung, Byung-Yeoup
    • Korean Journal of Environmental Biology
    • /
    • v.26 no.1
    • /
    • pp.15-21
    • /
    • 2008
  • Ionizing radiation causes many alterations in photosynthetic machineries. However, there is no information about effects of ionizing radiation on the development of photosynthetic machineries in plants. We investigated the greening of etiolated mung bean seedlings after gamma-irradiation of 50 to 300 Gy. The irradiation inhibited seedling growth with great dependence on the radiation dose. In particular, growth of stems was more affected than that of hypocotyls. Irradiated leaves showed inhibition in growth, aberration in morphology, and yellowing in color depending on the radiation dose. Contents of photosynthetic pigments such as chlorophylls and carotenoids were significantly decreased in the irradiated leaves. The apparent electron transport rate for photosynthesis, ETR, was similarly changed depending on the radiation dose. However, the maximal photochemical efficiency of Photosystem II (PSII), Fv/Fm, was little affected by the irradiation. Moreover, the 50-Gy seedlings maintained the control level of light saturating for photosynthesis and showed slightly higher Fv/Fm values in spite of significant decreases in the photosynthetic pigment content and ETR. These results suggest that the inhibition of the overall photosynthetic capacity couldn’t be causally relatqaed with the repression in the initial development of irradiated seedlings and that the overall photosynthetic machineries can develop and work to some extent as a concerted system for photosynthesis even after exposure to acute doses of ionizing radiation.

Laboratory Simulation of Formation, prevention and breaking of Water-in-oil Emulsion (수분함유 기름 에멀젼의 형성경향, 생성방해 및 파괴에 관한 실험적 예측)

  • 강성현;오재룡
    • 한국해양학회지
    • /
    • v.26 no.4
    • /
    • pp.324-331
    • /
    • 1991
  • Laboratory experiments were undertaken in mixing chamber to study the water-in-oil emulsion formation tendency, stability and formation rate of 16 crude oils. Arabian, Iran, Dubai, Isthmus and Daekyung crudes showed high emulsion formation tendency and had water contents of 80-90%. Emulsions of crude oils of middle East were very stable, while Isthmus and Daekyung sudes formed unstable emulsion. Emulsion formation tendency rate, and stability showed significant correlations with asphaltene content of crude oil. To evaluate the possibility of preventing mousse formation, inhibition ability of several dispersants and demulsifier was tested. They inhibited mousse formation at 0.1-0.2% concentrations (v/v). Emulsion inhibition by chemical treatment delayed the time of formation, but did not decrease water content. Demulsifying ability of dispersants and demulsifier was tested because biscous emulsion causes formidable problems in skimming, pumping and recovery operation. British demulsifier Alcohol 0 showed excellent emulsion breaking efficiency at 0.1% of emulsion Vol..

  • PDF

EPS Production, PHB Accumulation and Abiotic Stress Endurance of Plant Growth Promoting Methylobacterium Strains Grown in a High Carbon Concentration

  • Woo, Sung-Man;Subramanian, Parthiban;Ramasamy, Krishnamoorthy;Joe, M. Melvin;Sa, Tong-Min
    • Korean Journal of Soil Science and Fertilizer
    • /
    • v.45 no.4
    • /
    • pp.572-581
    • /
    • 2012
  • In this study, we compared growth pattern, floc yield, Exo-polysaccharides (EPS) production, Poly-${\beta}$-hydroxybutyrate (PHB) accumulation, resistance to osmotic and acid stress in Methylobacterium strains CBMB20, CBMB27, CBMB35, and CBMB110. Modified high C:N ratio medium denoted as HCN-AMS medium was used with a C:N ratio of 30:1. The HCN-AMS medium favored increased growth in all the studied strains. All Methylobacterium strains tested positive for EPS production and showed positive fluorescence with calcoflour stain. Elevated levels of EPS production from 4.2 to 75.0% was observed in HCN-AMS medium. Accumulation of PHB in HCN-AMS medium increased by 3.8, 36.7, and 12.0% in strains CBMB27, CBMB35, and CBMB110 respectively. Among the abiotic stresses, osmotic stress-induced growth inhibition of Methylobacterium strains was found to be lowered when grown in HCN-AMS medium. Likewise, growth inhibition due to acid stress at pH 5.0 was lower for strains grown in HCN-AMS medium compared to growth in AMS medium. Enhanced survivability under stress conditions may be attributed to the high EPS and PHB production at increased carbon concentration in the growth medium.

Enhancement of L-Lactic Acid Production in Lactobacillus casei from Jerusalem Artichoke Tubers by Kinetic Optimization and Citrate Metabolism

  • Ge, Xiang-Yang;Qian, He;Zhang, Wei-Guo
    • Journal of Microbiology and Biotechnology
    • /
    • v.20 no.1
    • /
    • pp.101-109
    • /
    • 2010
  • Efficient L-lactic acid production from Jerusalem artichoke tubers, by Lactobacillus casei G-02, using simultaneous saccharification and fermentation (SSF) in a fed-batch culture, is demonstrated. A kinetic analysis of the SSF revealed that the inulinase activity was subjected to product inhibition, whereas the fermentation activity of G-02 was subjected to substrate inhibition. It was also found that the intracellular NADH oxidase (NOX) activity was enhanced by the citrate metabolism, which dramatically increased the carbon flux of the Embden-Meyerhof-Parnas (EMP) pathway, along with the production of ATP. As a result, when the SSF was carried out at $40^{\circ}C$ after an initial hydrolysis of 1 h and included a sodium citrate supplement of 10 g/l, an L-lactic acid concentration of 141.5 g/l was obtained after 30 h, with a volumetric productivity of 4.7 g/l/h. The conversion efficiency and product yield were 93.6% of the theoretical lactic acid yield and 52.4 g lactic acid/l00 g Jerusalem artichoke flour, respectively. Such a high concentration of lactic acid with a high productivity from Jerusalem artichokes has not been reported previously, making G-02 a potential candidate for the economic production of L-lactic acid from Jerusalem artichokes on a commercial scale.

Computational Drug Discovery Approach Based on Nuclear Factor-κB Pathway Dynamics

  • Nam, Ky-Youb;Oh, Won-Seok;Kim, Chul;Song, Mi-Young;Joung, Jong-Young;Kim, Sun-Young;Park, Jae-Seong;Gang, Sin-Moon;Cho, Young-Uk;No, Kyoung-Tai
    • Bulletin of the Korean Chemical Society
    • /
    • v.32 no.12
    • /
    • pp.4397-4402
    • /
    • 2011
  • The NF-${\kappa}B$ system of transcription factors plays a crucial role in inflammatory diseases, making it an important drug target. We combined quantitative structure activity relationships for predicting the activity of new compounds and quantitative dynamic models for the NF-${\kappa}B$ network with intracellular concentration models. GFA-MLR QSAR analysis was employed to determine the optimal QSAR equation. To validate the predictability of the $IKK{\beta}$ QSAR model for an external set of inhibitors, a set of ordinary differential equations and mass action kinetics were used for modeling the NF-${\kappa}B$ dynamic system. The reaction parameters were obtained from previously reported research. In the IKKb QSAR model, good cross-validated $q^2$ (0.782) and conventional $r^2$ (0.808) values demonstrated the correlation between the descriptors and each of their activities and reliably predicted the $IKK{\beta}$ activities. Using a developed simulation model of the NF-${\kappa}B$ signaling pathway, we demonstrated differences in $I{\kappa}B$ mRNA expression between normal and different inhibitory states. When the inhibition efficiency increased, inhibitor 1 (PS-1145) led to long-term oscillations. The combined computational modeling and NF-${\kappa}B$ dynamic simulations can be used to understand the inhibition mechanisms and thereby result in the design of mechanism-based inhibitors.

Kinetic Studies on the Effects of Divalent Cations on the ATPase Activity of the Fragmented Sarcoplasmic Reticulum of Rabbit Skeletal Muscle (골격근 小胞體의 ATPase活性에 미치는 二價金屬이온의 영향)

  • Park, Young-Soon;Ha, Doo-Bong
    • The Korean Journal of Zoology
    • /
    • v.23 no.3
    • /
    • pp.137-148
    • /
    • 1980
  • The effects of divalent cations, $Hg^{2+}, Cu^{2+}, Pb^{2+}, Cd^{2+}$, and $Mn^{2+}$ on the total ATPase activity of the fragmented sarcoplasmic reticulum isolated from rabbit skeletal muscle were investigated. The inhibitory effects of the cations on the enzyme activity increased as the concentrations of the ions increased with the order of efficiency of $Hg^{2+}$ > $Cu^{2+}$ > $Pb^{2+}$ > $Cd^{2+}$ > $Mn^{2+}$ in the concentration range between 10 and 500$\mu$M. The 50% inhibition for each ion was almost identical with the inhibition constant (Ki) value for each ion. The Ki's were 10, 30 130, and 350$\mu$M for $Hg^{2+}, Cu^{2+}, Pb^{2+}, and Cd^{2+}$, respectively. $Mn^{2+}$ seemed to be an activator at lower concentrations and an inhibitor at higher concentrations. The presence of the cations did not change the Km values, suggesting that the ions act as a reversible noncompetitive inhibitor on the FSR ATPase. The energy of activation of the enzyme was aproximately 19 Kcal/mole. The presence of the ions decreased the value slightly. A possible mechanism for the reversible noncompetitive inhibitory effect of the cations was discussed.

  • PDF

Antioxidant Activity of the Aerial Part of Epimedium koreanum NAKAI (음양곽의 항산화활성)

  • 이종원;도재호;이성계
    • Journal of the Korean Society of Food Science and Nutrition
    • /
    • v.29 no.4
    • /
    • pp.732-736
    • /
    • 2000
  • The purpose of this study was to investigate the extraction method of phenolic compounds and antioxidant activities of the aerial part of Epimedium koreanum NAKAI (EKN). The antioxidant activities of EKN were tested with by hydrogen donating ability, inhibition of lipid peroxidation, and inhibition of LDL oxidation. The most suitable conditions for the extraction of phenolic compounds from EKN were to use 60% ethanol by 3 times, and the yield of extract (dry basis) was 22%. In the extraction efficiency of phenolic compounds, 60% ethanol as extracting solvent was superior to water. Sixty% ethanol extract of EKN was found to have an ability of hydrogen donating to DPPH. MDA determination showed the 95% inhibitory effect against linoleic acid oxidation by the addition of 700 ppm EKN extract. Also, about 70% of LDL oxidation was inhibited by the addition of 500 ppm.

  • PDF