• Title/Summary/Keyword: action spectrum

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Physicochemical Properties, Stabilities and Pharmacokinetics of Cephalosporin 3'-Quinolone Dithiocarbamate (세팔로스포린 3'-퀴놀론의 물리화학적 성질, 안정성 및 체내약물동태)

  • 나성범;공재양;김완주;지웅길
    • YAKHAK HOEJI
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    • v.37 no.6
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    • pp.638-646
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    • 1993
  • A cepfialosporin with an aminothiazoiylmethoxyimino-type side chain at the 7 position and bicyclic quinolone dithicarbamate at the 3' position was synthesized. It has broad and potent antivacterial activity in vitro. The antibacterial spectrum reflects contributions of both the cephalosporin moiety and the quinolone moiety. Thus, this compound was named DACD implying a dualaction cephalosporin derivative. In this paper, the physicochemical proper-ties (lipid-water partition, pKa), stability and pharmacokinetics of DACD were determined and compared with cefotaxime 3'-norfloxacin dithiocarbamate (CENO). Stability tests were studied in pH 1.20, 6.80 and 8.00 buffers and in the presence of AB type human plasma, rat liver homogenate and its .betha.-lactamase. The pharmacokinetic parameters of DACD were evaluated in mice after a single intravenous dose of 40 mg/kg. The results are as follows. The lipid-water partition coefficient of DACD was higher than that of CENO. The calculated pKa values of CENO and DACD, were 6.82$\pm$0.03, 7.53$\pm$0.21, respectively. In the hydrolysis test, half-lives (t$^{1/2}$) of CENO and DACD was 66.0 hr and 80.0 hr in pH 6.80 buffer, 190 hr and 91.4 hr in pH 8.00 buffer. CENO and DACD were rapidly hydrolyzed in human plasma and in rat liver hornogenate. Half-lives (t$_{1/2}$ of CENO and DACD were 1.29 hr and 1.15 hr in hyman plasma, 0.62 hr and 0.71 hr rat liver homogenate. In $\beta$-lactamase stability test, CENO and DACD were very stable to the .betha.-lactamases obtained from three different strains. Half-life (t$_{1/2}$) and areas under the curve (AUC) in mice were 2.33 hr and 15.97 (mg.h/1), respectively.

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A Helix-induced Oligomeric Transition of Gaegurin 4, an Antimicrobial Peptide Isolated from a Korean Frog

  • Eun, Su-Yong;Jang, Hae-Kyung;Han, Seong-Kyu;Ryu, Pan-Dong;Lee, Byeong-Jae;Han, Kyou-Hoon;Kim, Soon-Jong
    • Molecules and Cells
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    • v.21 no.2
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    • pp.229-236
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    • 2006
  • Gaegurin 4 (GGN4), a novel peptide isolated from the skin of a Korean frog, Rana rugosa, has broad spectrum antimicrobial activity. A number of amphipathic peptides closely related to GGN4 undergo a coil to helix transition with concomitant oligomerization in lipid membranes or membrane-mimicking environments. Despite intensive study of their secondary structures, the oligomeric states of the peptides before and after the transition are not well understood. To clarify the structural basis of its antibiotic action, we used analytical ultracentrifugation to define the aggregation state of GGN4 in water, ethyl alcohol, and 1,1,1,3,3,3-hexafluoro-2-propanol (HFIP). The maximum size of GGN4 in 15% HFIP corresponded to a decamer, whereas it was monomeric in buffer. The oligomeric transition is accompanied by a cooperative 9 nm blue-shift of maximum fluorescence emission and a large secondary structure change from an almost random coil to an ${\alpha}$-helical structure. GGN4 induces pores in lipid membranes and, using electrophysiological methods, we estimated the diameter of the pores to be exceed $7.3{\AA}$, which suggests that the minimal oligomer structure responsible is a pentamer.

Toward Research Collaboration Between Korea And Russia: Ksgpc'S Research Activities And Corporational Issues In Geomatics

  • Kim, Kamlae;Lee, Honam;Kim, Uknam;Shin, Bong-Ho
    • Proceedings of the Korean Society of Surveying, Geodesy, Photogrammetry, and Cartography Conference
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    • 2004.02a
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    • pp.16-21
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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 photography, 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 outcomes 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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A Study on the Development of Power-Line EMI Filter for the Prevention of Conduction Noise by Coil Loads. (코일성 부하에 의한 전도 노이즈 방지 목적의 전원용 EMI필터 개발 연구)

  • Kim, Byeong Jun;Joo, Jae-hun;Kim, Jin Ae;Baek, Pan Keun;Choi, Jung-Keyng
    • Proceedings of the Korean Institute of Information and Commucation Sciences Conference
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    • 2009.05a
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    • pp.175-179
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    • 2009
  • this paper proposes a filter design that makes to be satisfied EMC spec. in reliability test of analogue switch for electronic equipment and air conditioning load unit. A designed electromagnetic wave filter was applied to minimize an mutual interference and surrounding environment and improve the product's quality being satisfied to EMC standard. By simulation, using a spectrum analyzer at the 30MHz~1GHz band, ISO/JASO standard frequency range, and simplified EMI chamber, energy distribution of a specific frequency band was analyzed and the capacity of the element which composed the filter was determined in order to implement the most suitable electromagnetic wave filter.In fact, it was certificated that noise decrease by filter addition to the analogue switch for electronic equipment and air conditioning load unit in Certification Authority, and confirmed that the unit is carried out a normal action without electromagnetic wave interference.

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Antimicrobial Characteristic of Methanolic Extracts from Prunus mune Byproducts Against Food Spoilage Microorganisms (매실박 메탄올 추출물의 항균 특성)

  • Ha, Myung-Hee;Park, Woo-Po;Lee, Seung-Cheol;Heo, Ho-Jin;Cho, Sung-Hwan
    • Food Science and Preservation
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    • v.14 no.2
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    • pp.183-187
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    • 2007
  • The antimicrobial properties of methanolic extract (PML) from Prunus nune byproducts after liquor manufacturing weremeasured using various putrefactive and food spoilage microorganisms. PML showed remarkable antimicrobial effects against various putrefactive and food spoliage microorganisms when used at 500g/mL. The antimicrobial properties were stable for 30 min at 100C and at pH 3 11. PML seems to be a natural antimicrobial agent with high effectiveness, and shows both thernal and pH stability. In addition, the mode of antimicrobial action suggests that the active components may synergistically perturb microbial membrane functions.

Antitumor profiles and cardiac electrophysiological effects of aurora kinase inhibitor ZM447439

  • Lee, Hyang-Ae;Kwon, Miso;Kim, Hyeon-A;Kim, Ki-Suk
    • The Korean Journal of Physiology and Pharmacology
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    • v.23 no.5
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    • pp.393-402
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    • 2019
  • Aurora kinases inhibitors, including ZM447439 (ZM), which suppress cell division, have attracted a great deal of attention as potential novel anti-cancer drugs. Several recent studies have confirmed the anti-cancer effects of ZM in various cancer cell lines. However, there have been no studies regarding the cardiac safety of this agent. We performed several cytotoxicity, invasion and migration assays to examine the anti-cancer effects of ZM. To evaluate the potential effects of ZM on cardiac repolarisation, whole-cell patch-clamp experiments were performed with human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) and cells with heterogeneous cardiac ion channel expression. We also conducted a contractility assay with rat ventricular myocytes to determine the effects of ZM on myocardial contraction and/or relaxation. In tests to determine in vitro efficacy, ZM inhibited the proliferation of A549, H1299 (lung cancer), MCF-7 (breast cancer) and HepG2 (hepatoma) cell lines with $IC_{50}$ in the submicromolar range, and attenuated the invasive and metastatic capacity of A549 cells. In cardiac toxicity testing, ZM did not significantly affect $I_{Na}$, $I_{Ks}$ or $I_{K1}$, but decreased $I_{hERG}$ in a dose-dependent manner ($IC_{50}$: $6.53{\mu}M$). In action potential (AP) assay using hiPSC-CMs, ZM did not induce any changes in AP parameters up to $3{\mu}M$, but it at $10{\mu}M$ induced prolongation of AP duration. In summary, ZM showed potent broad-spectrum anti-tumor activity, but relatively low levels of cardiac side effects compared to the effective doses to tumor. Therefore, ZM has a potential to be a candidate as an anti-cancer with low cardiac toxicity.

A Review on Control of Mites Using Neem, Chrysanthemum, Shrubby Sophora Extracts and their Effects on Natural Enemies (님, 제충국, 고삼 추출물의 응애류 방제와 천적에 미치는 영향에 대한 고찰)

  • Hyo Jung Kim;Do-ik Kim;Song Hee Han;Young Cheol Kim
    • Korean journal of applied entomology
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    • v.62 no.3
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    • pp.193-205
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    • 2023
  • Botanical insecticides derived from plant extracts exhibit repellent, antifeedant and enzyme-inhibiting activities against insect pests. Among such pests, phytophagous mites are major threats to horticultural crops. Botanical extracts derived from neem, chrysanthemum, and shrubby sophora are employed as field acaricides. These botanical extracts have low toxicities against natural enemies of the insect pests and, thus, are valuable in pest management. This review focuses on the potential for botanical extracts in the controls of mites, with comparisons of the spectrum of activity, the lethal dose and times and their mode of action. This information will enable better formulation of botanical extracts in integrated mite control.

Automatic Indexing Algorithm of Golf Video Using Audio Information (오디오 정보를 이용한 골프 동영상 자동 색인 알고리즘)

  • Kim, Hyoung-Gook
    • The Journal of the Acoustical Society of Korea
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    • v.28 no.5
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    • pp.441-446
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    • 2009
  • This paper proposes an automatic indexing algorithm of golf video using audio information. In the proposed algorithm, the input audio stream is demultiplexed into the stream of video and audio. By means of Adaboost-cascade classifier, the continuous audio stream is classified into announcer's speech segment recorded in studio, music segment accompanied with players' names on TV screen, reaction segment of audience according to the play, reporter's speech segment with field background, filed noise segment like wind or waves. And golf swing sound including drive shot, iron shot, and putting shot is detected by the method of impulse onset detection and modulation spectrum verification. The detected swing and applause are used effectively to index action or highlight unit. Compared with video based semantic analysis, main advantage of the proposed system is its small computation requirement so that it facilitates to apply the technology to embedded consumer electronic devices for fast browsing.

Synergistic action of pesticide mixtures using glutathione-s-transferase- and esterase-inhibiting properties in diamondback moth (Plutella xylostella L.) (Glutathione-S-transferase와 esterase 효소 저해특성을 이용한 농약의 혼합 상승효과)

  • Yu, Yong-Man;Hong, S.S.;Kim, S.;Hur, J.H.
    • The Korean Journal of Pesticide Science
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    • v.7 no.1
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    • pp.38-44
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    • 2003
  • In vitro inhibitory activity of 34 insecticides and 31 fungicides to glutathione-S-transferase and esterases extracted from rats was determined. Of tested pesticides, the pesticides with high activity on both detoxifying enzymes were mixed with pesticides that are known to be detoxified by detoxifying enzymes. Glutathione-S-transferase was inhibited by thiodicarb $(I_{50}:1.87\times10^{-4}M)$, thiocyclam $(7.40\times10^{-4}M)$, dithianon $(7.55\times10^{-5}M)$, and tolylfluanide $(8.66\times10^{-5}M)$, while esterases by dichlorvos $(8.95\times10^{-8}M)$, pirimicarb $(2.74\times10^{-6}M)$, pyrazophos $(3.31\times10^{-5}M)$, and benomyl $(4.96\times10^{-5}M)$. After acephate known to be detoxified by glutathione-S-transferase was mixed with glutathione-S-transferase-inhibiting pesticides and phenthoate known to be detoxified by esterases was mixed with esterases-inhibiting pesticides, insecticidal activities of such mixtures were determined against diamondback moth (PlutelLa xylostella L.). Synergistic action was observed in all pesticide combinations. The highest synergistic action was obtained when phenthoate was combined with dichlorvos, showing that co-toxicity coefficients were 1512 and 1877 after 24 and 48 hours of treatment, respectively. Several other combinations of pesticides, such as phenthoate with benomyl, and acephate with dithianon, also showed synergism, showing that their co-toxicity coefficients were about 1,000 and 500, after 24 hours of treatment, respectively. Our results showed that combinations of pesticides inhibited by detoxifying enzymes and ones detoxified by detoxifying enzymes resulted in increased toxicities of pesticides, suggesting that such combinations could be used to develop pesticide mixtures with more broad spectrum and high effectiveness.

Superovulation-Oocyte and Uterine Function (과배란-난자 및 자궁기능)

  • 문영석
    • Korean Journal of Animal Reproduction
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    • v.20 no.4
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    • pp.379-384
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    • 1997
  • Superovulation with exogenous gonadotropins creates a spectrum of pre or periovulatory hormonal changes with subsequent detrimental effects on oocyte quality, fertilization, embryo development, implantation and maintenance of pregnancy. Our recent study determined potential roles for insulin-like growth factor-1 (IGF-1) in uterine environment regulation and preimplant tation in the rat. The evidence indicates that IGF-l may play an important role in the main tenance of a receptive uterine environment for embryonic development and the regulation of decidualization. Embryonic loss and failure of implantations following superovulation may be partially attributed to disturbances in uterine IGF-l action as observed in this study. We investigated the effects of superovulatory doses of gonadotropins on frequency of chromosomal a abnormalities of mouse embryos. Chromosome a analysis of mouse zygotes and 8- to 16-cell stage embryos from spontaneously ovulated, 5, 10, and l 15 lU pregnant mare serum gonadotropin (PMSG) superovulated mice was carried out. Aneuploidy, polyploidy and structural chrom- osomal abnormalities were detected among the four groups. However, only polyploidy was correlated with superovulation. In 10 and 15 IV PMSG treated groups, the rate of polypoidy was 2.9% and 10.5%, respectively. Furthermore, there was a dose reponse relationship between the PMSG dose and the incidence of embryonic p polyploidy (P

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