• Title/Summary/Keyword: action spectrum

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Inhibition of Human Neutrophil Elastase by NSAIDs and Inhibitors, and Molecular Pharmacological Mechanism of the Inhibition (비스테로이드성 항염증제와 효소 억제제에 의한 사람 중성구 Elastase의 활성도 억제 및 분자약리학적 기전)

  • Kang, Koo-Il;Kim, Woo-Mi;Hong, In-Sik;Lee, Moo-Sang
    • The Korean Journal of Pharmacology
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    • v.32 no.3
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    • pp.425-431
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    • 1996
  • Human neutrophil elastases (HNElastase, EC 3.4.21.37), a causative factor of inflammatory diseases, are regulated by plasma proteinase inhibitors, alpha-proteinase inhibitor and ${\alpha}_2-macroglobulin$. Under certain pathological conditions, however, released enzymes or abnormal function of inhibitors may cause various inflammatory disease. NSAIDs have been clinically applied for treatment of inflammatory diseases. Inhibition of cyclooxygenase is a known mechanism of action of NSAIDs in the treatment of inflammatory disease. In in vitro experiments, HNElastase was inhibited by naproxen, phenylbutazone, and oxyphenbutazone, but ibuprofen, ketoprofen, aspirin, salicylic acid, and tolmetin did not inhibit elastase. HNElastase was also inhibited by chelating agents, EDTA & EGTA, and tetracyclines. Removal of divalent metal ions by EDTA caused inhibition of elastase, and reconstitution of the metal ions recovered the enzyme activity to a certain level. Frequencies and contours in the Raman spectra of various conditions of human neutrophil elastase undergo drastic changes upon partial removal and/or reconstitution of calcium and zinc ions. The metal ion content dependent activities and change of the contour of the Raman spectrogram suggest us that the mechanism of action of a chelator or chelator-like agents on neutrophil elastase may be related to the conformational change at/or near the active site, especially -C=O radical or -COOH radical.

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Anti-proliferation Effects of Isorhamnetin on Lung Cancer Cells in Vitro and in Vivo

  • Li, Qiong;Ren, Fu-Qiang;Yang, Chun-Lei;Zhou, Li-Ming;Liu, Yan-You;Xiao, Jing;Zhu, Ling;Wang, Zhen-Grong
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.7
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    • pp.3035-3042
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    • 2015
  • Background: Isorhamnetin (Iso), a novel and essential monomer derived from total flavones of Hippophae rhamnoides that has long been used as a traditional Chinese medicine for angina pectoris and acute myocardial infarction, has also shown a spectrum of antitumor activity. However, little is known about the mechanisms of action Iso on cancer cells. Objectives: To investigate the effects of Iso on A549 lung cancer cells and underlying mechanisms. Materials and Methods: A549 cells were treated with $10{\sim}320{\mu}g/ml$ Iso. Their morphological and cellular characteristics were assessed by light and electronic microscopy. Growth inhibition was analyzed by MTT, clonogenic and growth curve assays. Apoptotic characteristics of cells were determined by flow cytometry (FCM), DNA fragmentation, single cell gel electrophoresis (comet) assay, immunocytochemistry and terminal deoxynucleotidyl transferase nick end labeling (TUNEL). Tumor models were setup by transplanting Lewis lung carcinoma cells into C57BL/6 mice, and the weights and sizes of tumors were measured. Results: Iso markedly inhibited the growth of A549 cells with induction of apoptotic changes. Iso at $20{\mu}g/ml$, could induce A549 cell apoptosis, up-regulate the expression of apoptosis genes Bax, Caspase-3 and P53, and down-regulate the expression of Bcl-2, cyclinD1 and PCNA protein. The tumors in tumor-bearing mice treated with Iso were significantly smaller than in the control group. The results of apoptosis-related genes, PCNA, cyclinD1 and other protein expression levels of transplanted Lewis cells were the same as those of A549 cells in vitro. Conclusions: Iso, a natural single compound isolated from total flavones, has antiproliferative activity against lung cancer in vitro and in vivo. Its mechanisms of action may involve apoptosis of cells induced by down-regulation of oncogenes and up-regulation of apoptotic genes.

Industrial Application for Aquaculture of Fermented Soybean with Bacillus polyfermenticus SCD (양식업에서 바실러스 폴리퍼멘티쿠스 콩발효물의 상업적 응용)

  • Lee, Jin Young;Kim, Kang Min;Kang, Jae Seon
    • Journal of Marine Bioscience and Biotechnology
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    • v.2 no.1
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    • pp.48-54
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    • 2007
  • Bacillus polyfermenticus SCD (B. polyfermenticus SCD) has been appropriately used for the therapy of long-term intestinal disorders, because live strains in the form of active endospores can successfully reach the target intestine in humans. B. polyfermenticus SCD produces the most antibiotic-related materials. In the present study, B. polyfermenticus SCD was fermented with soybeans (BPFS) and its probiotic properties were investigated. B. polyfermenticus SCD and BPFS showed a broad spectrum of antimicrobial activity against pathogenic Gram-positive (Streptococcus parauberis, Streptococcus iniae, Lactococcus garviae) and Gram-negative (Flexibacter tractuosus, Vibrio harveyi, Vibrio vulnificus, Vibrio ordalii) bacteria and moulds (Aspergillus niger, Aspergillus oryzae). Sebastes schlegeli were used to examine survival rate and cleanup action by BPFS. Bacterial infection resulted in a mortality of up to 99% in the commercial fodder fed groups. BPFS both enhanced the growth rate of fry by improving their appetite and had cleaned by decreased eutrophication. Therefore, it seems appropriate that BPFS should be developed as an antibiotic replacement, favorable fodder additive, and antifungal material in fish farming systems.

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Effects of Polyamine on Flowering in Lemna gibba G3 (좀개구리밥(Lemna gibba G3)의 개화에 미치는 Polyamine의 영향)

  • 김강창
    • Journal of Plant Biology
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    • v.35 no.4
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    • pp.403-408
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    • 1992
  • The flowering in Lemna gibba G3, a long-day plant, was promoted under continuous light by agmatine, putrescine, spermidine and spermine present in the culture medium. Methylglyoxal-bis (guanylhydrazone) (MGBG) and cyc10hexylamine (CHA), inhibitors of polyamine biosynthesis, were found to suppress the flowering in the plants. The vegetative grov.1h rate was kept constant while the flowering was being promoted by the pOlyamines, and the inhibitors with depressive effect on flowering showed stimulatory effect on vegetative grov.1h. The pattern of vegetative growth during floral promotion or depression was an indication that the promotive action of the pOlyamines and the suppressive effect of the inhibitors may be outcome of their possible involvement specifically in the flowering process rather than in broad spectrum of growth of L. gibba G3. The degree of promotive action of spermdine and spermine could not be altered (or lessened) by simultaneous application of their inhibitors to the medium. This phenomenon indicates that the flowering process in L. gibba G3 may largely be dependent to the status of endogenous spermidine and spermine. Endogenous level of spermidine in florally induced Lemna, was found to rapidly increase. In 24 h of floral induction, the content reached at the level 2 times higher than that in non-induced plants. The elevated level of spermidine provides an additional, though premature, evidence supporting the postulation that endogenous polyamine status might play an important role in the very early stage of floral induction in L. gibba G3.bba G3.

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A New Approach for Practical Classification of Herbicide and for Effective Use by Two-dimensional Ordination Analysis (Two-Dimensional Ordination 분석법에 의한 제초제살초 Spectrum 분류와 효과적인 사용법)

  • Kim Soon Chul
    • Korean journal of applied entomology
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    • v.22 no.2 s.55
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    • pp.147-159
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    • 1983
  • In general, herbicides have been classified according to selectivity, mobility. time of application, methods of application, mode of action and chemical property and structure. However, there was no generally accepted classification system for practical use in the field. The primary processes affected by the majority of herbicides are the growth process through cell elongation and/or cell division, the photosynthetic process specifically the light reaction, the oxidative phosphorylation and the integrity of the membrane systems. The usual approach in the study of the mechanism by which herbicides kill or inhibit the growth of plants is to initially determine the morphological phototoxicity systems, The mechanism by which a herbicide kills a plant or suppresses its development is actually the resultant effect of primary and secondary(or side) effects. In most instances, the death of the plant is due to the secondary effects. To induce the desired response, a herbicide must be able to gain entry into the plants and once inside, to be transported within the plant to its site(s) of activity in concentrations great enough. Obstacles to the entry and movement of herbicides in plants are generally classified by leaf and soil obstacles, translocation obstacles and biochemical obstacles, and these obstacles are also strongly influenced by plant species and by environmental factors such as light, temperature, rainfall and relative humidity. And hence, in most instances, results obtained from laboratory or greenhous vary from those of field experiment. Author attempted to classify herbicides from the field experiment using the two-dimensional ordination analysis to obtain practical information for selecting effective herbicides or to choose effective herbicide combinations for increasing herbicidal efficacy or reducing the chemical cost. Based on this two-dimensional diagram, desired herbicides or combinations were selected and further investigated for the interaction effects whether these combinations are synergistic, additive or antagonistic. From the results, it was concluded that these new approach could possibly be give more comprehensive informations about effective use of herbicide than any other systems.

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The physical properties and the dyeability of the easily dyeable polyester yarn under atmospheric pressure (상압가염형 폴리에스테르 섬유의 물성과 염색성)

  • Kim, Tae Gyeong;Yun, Seok Han;Sin, Sang Yeop;Im, Yong Jin;Jo, Gyu Min
    • Textile Coloration and Finishing
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    • v.13 no.6
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    • pp.33-33
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    • 2001
  • The physical properties and the dyeability of the easily dyeable polyester yarn(EDY) were investigated and compared with those of regular polyester (REG-PET). The EDY, copolymerized with small amount of polyethylene glycol(PEG), showed higher intensity of aliphatic CH peak in IR spectrum, lower density and lower compactness than those of the REG-PET from the analysis of IR, density gradient column and XRD respectively. In the physical properties, the EDY has lowers $T_g,\;T_m$, specific stress and initial modulus, and also has higher strain than that of the REG-PET. The EDY can be dyed under atmospheric pressure and its dyeing rate was faster than REG-PET due to low $T_d$, and this seems to be caused by the increased flexibility of Polymer chain in amorphous region of the EDY due to the copolymerization of PEG.ns being within the experimental error, the average values of lifetim. $\tau$(t) are taken for further calculations. Rate constants such as Stern-Volmer quenching constants K$_{sv}$, quenching rate parameters k$_q$ and k''$_q$, static quenching constant V and kinetic distance r are determined using the modified Stern-Volmer eq.tion and sphere of action static quenching model. In order to see whether the reactions are diffusion limited, equations k$_q$ = e$^{-Eq/RT}$ and k''$_q$ = e$^{-Eq/RT}$ are used to determine the values of E$_q$ and E''$_q$, the activati. energies for collisional quenching and the values of E$_q$ are 14.53, 17.28 and 16.20 kJ mole$^{-1}$ for MPNO1, MPNO2 and 2-PI respectively and the values of E''$_q$ are 14.62 and 17.73 for MPNO1 and MPNO2 respectively. From the magnitudes of various quantities it has.een concluded that the reactions are diffusion limited and the observed positive deviations in the S-V plot are due to static and dynamic quenching.

Toward Research Collaboration Between Korea and Russia: KSGPC's Research Activities and Corporational Issues in Geomatics

  • KIM, Kam-Lea;LEE, Ho-Nam;KIM, Uk-Nam
    • Korean Journal of Geomatics
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    • v.3 no.2
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    • pp.81-86
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    • 2004
  • In recent years, the importance of geospatial data have been emphasized not only for the national GIS programs and but also in the value added commercial and industry markets. There is no doubt that GIS, GPS, aerial and satellite imagery data were provided powerful tools to support national information infrastructure for geospatial database. While great emphasis has been laid on the geospatial data, there has been little analysis or evaluation of how to maximize the benefits of using these information sources. Also, with the proliferation of geographic data and information sources such as satellite imagery, digital aerial photograph, digital topographic and vector data, there is a great need to inform professionals from all disciplines as to the benefits of these information sources and how to best put them to use within any given application. From the first publication of KSGPC(Korean Society of Geodesy, Photogrammetry and Cartography) papers in 1981, our objective was, and is, to help develop the wider spectrum of GIS in the academy and industry by exposing new users to the benefits of GIS, remote sensing, mapping, GPS and photogrammetry. In this presentation, we will introduce KSGPC works and will evaluate GIS-related governmental policies and programs in Korea for the past and the future to present different status between Korea and Russia. It is now important to investigate lessons learnt from two countries' experiences and developed an empirical framework to combine outcome from GIS-related researches in Korea and Russia. This may enable GIS professionals to gain a wider range of experiences in the international context, and consequently, help them to develop new markets for GIS. Therefore, we arranged the possible action items and interesting points to corporate and to promote the academic growth in the practice of GIS.

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Pharmaceutical Studies on Microencapsulated Pivampicillin Hydrochloride (염산피밤피실린의 마이크로캅셀에 관(關)한 약제학적(藥劑學的) 연구(硏究))

  • Lee, Wan-Ha;Jee, Ung-Kil;Lee, Young-Hwan;Kim, Sang-Rin
    • Journal of Pharmaceutical Investigation
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    • v.15 no.2
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    • pp.53-62
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    • 1985
  • Pivampicillin hydrochloride is a kind of broad spectrum antibiotics with bactericidal action, and is used in many countries, although it has bitter taste, unpleasant odour and side effects of irritating gastric mucosa, nausea, penicillin allergy, etc. For the improvement of such side effects of pivampicillin hydrochloride, microcapsules, with wall of ethylcellulose, have been prepared by coacervation method. The shape was observed through the scanning electron microscope, the release of the drug into an aqueous medium was studied and the effects of core: ethylcellulose ratio were interpreted as well as making sensory evaluation of taste and odour. There was decreasing trend in dissolution rate of the drug with the increase of core: ethylcellulose ratios, and the smaller microcapsules released their contents more rapidly. A linear relationship was established between the amount of ethylcellulose and the time for 60% release of the drug, and the release pattern was found to have similar characteristics to the release of the drug from an insoluble porous matrix. The release of the drug in the artificial intestinal fluids (pH 6.8) was found to be similar to that in water, while the release in the artificial gastric juice (pH 1.2) was slightly slower. Bioavailability of microcapsule was compared with that of pivampicillin hydrochloride in rabbits using serum concentration and urinary excretion measurements. Microcapsule gave showed slightly higher serum level than pivampicillin hydrochloride from 2 hours after administration, while no significant difference was observed in the accumulated urinary excretion rate between pivampicillin hydrochloride and microcapsule. The ulcer index of pivampicillin hydrochloride administered group was 2.6, and microcapsule administered group was 1.5, while control group was 0.8. Therefore it may be concluded that microencapsulation of pivampicillin hydrochloride is a useful pharmaceutical approach to protect the gastrointestinal tract from being injured by direct contact of pivampicillin hydrochloride without any significant difference of bioavailability.

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A 2H solid-state NMR study on the lipid phase change in the presence of an antimicrobial peptide (항균성 펩타이드와 혼합된 인지질 분자의 상 변화에 대한 고체 중수소 핵자기 공명 연구)

  • Choi, Hyung Geun;Kim, Chul
    • Analytical Science and Technology
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    • v.26 no.1
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    • pp.61-66
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    • 2013
  • The activity of an antimicrobial peptide, protegrin-1, on the well-aligned lipid bilayer deposited on a thin coverglass plate was investigated by $^2H$ solid-state NMR spectroscopy. Orientational distribution and molecular motion in the lipid bilayer were determined from $^2H$ solid-state NMR spectrum. Reorientational motion of lipid molecules in the vacuum-dried state was found to be small but their orientational distribution was not able to be determined. As storage times were longer, the order of the alignment of lipid molecules in the lipid bilayer and percentages involved in the toroidal pore structures increased. We found that much longer time is required to get the equilibrium state of the peptide-lipid mixture under our experimental condition for investigating the action of the antimicrobial peptide like protegrin-1 on the lipid bilayers deposited on the thin coverglass plates.

Nonlinear response of stiffened triceratops under impact and non-impact waves

  • Chandrasekaran, Srinivasan;Nassery, Jamshed
    • Ocean Systems Engineering
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    • v.7 no.3
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    • pp.179-193
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    • 2017
  • Dynamic response analysis of offshore triceratops with stiffened buoyant legs under impact and non-impact waves is presented. Triceratops is relatively new-generation complaint platform being explored in the recent past for its suitability in ultra-deep waters. Buoyant legs support the deck through ball joints, which partially isolate the deck by not transferring rotation from legs to the deck. Buoyant legs are interconnected using equally spaced stiffeners, inducing more integral action in dispersing the encountered wave loads. Two typical nonlinear waves under very high sea state are used to simulate impact and non-impact waves. Parameters of JONSWAP spectrum are chosen to produce waves with high vertical and horizontal asymmetries. Impact waves are simulated by steep, front asymmetric waves while non-impact waves are simulated using Stokes nonlinear irregular waves. Based on the numerical analyses presented, it is seen that the platform experiences both steady state (springing) and transient response (ringing) of high amplitudes. Response of the deck shows significant reduction in rotational degrees-of-freedom due to isolation offered by ball joints. Weak-asymmetric waves, resulting in non-impact waves cause steady state response. Beat phenomenon is noticed in almost all degrees-of-freedom but values in sway, roll and yaw are considerably low as angle of incidence is zero degrees. Impact waves cause response in higher frequencies; bursting nature of pitch response is a clear manifestation of the effect of impact waves on buoyant legs. Non-impact waves cause response similar to that of a beating phenomenon in all active degrees-of-freedom, which otherwise would not be present under normal loading. Power spectral density plots show energy content of response for a wide bandwidth of frequencies, indicating an alarming behaviour apart from being highly nonlinear. Heave, being one of the stiff degrees-of-freedom is triggered under non-impact waves, which resulted in tether tension variation under non-impact waves as well. Reduced deck response aids functional requirements of triceratops even under impact and non-impact waves. Stiffened group of buoyant legs enable a monolithic behaviour, enhancing stiffness in vertical plane.