• Title/Summary/Keyword: action spectrum

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Studies on the Antifungal Antibiotics Produced by a Streptomyces sp. (Part 4) The Occurrence of Tetraene Substance and Its Physiological Properties (Streptomyces sp. 가 생산하는 항진균성 항생물질에 관한 연구 (제4보) Tetraene계 항진균성 항생물질의 생성및 그의 성장)

  • Ko, Young-Hee;Bae, Moo
    • Microbiology and Biotechnology Letters
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    • v.10 no.3
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    • pp.211-215
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    • 1982
  • Streptomyces griseorubiginosus var. soyoensis previously identified, produced two kinds of antifungal antibiotics, trans-cinnamamide and another new substance. The latter was identified to be a new substance of tetraene family by establishment of UV, IR, NMR, mass spectra and chemical reactions and rotatively named as Tetraene KM-A. Through an antimicrobial activity test using serial agar dilution method, Tetraene KM-A showed strong growth inhibitory activity against fungi and yeasts, but not against procaryotes tested. The inhibitory action of Tetraene KM-A on fungi was remarkably ineffective when some of sterols were added to the cultural media. $LD_{50}$ of the Tetrene KM-A to mice and rats by intravenous injection were 84.3 and 90.4 mg/kg respectively. $LD_{50}$ to mice by oral feeding was 1503mg/kg.

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Wide Spectrum of Inhibitory Effects of Sertraline on Cardiac Ion Channels

  • Lee, Hyang-Ae;Kim, Ki-Suk;Hyun, Sung-Ae;Park, Sung-Gurl;Kim, Sung-Joon
    • The Korean Journal of Physiology and Pharmacology
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    • v.16 no.5
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    • pp.327-332
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    • 2012
  • Sertraline is a commonly used antidepressant of the selective serotonin reuptake inhibitors (SSRIs) class. In these experiments, we have used the whole cell patch clamp technique to examine the effects of sertraline on the major cardiac ion channels expressed in HEK293 cells and the native voltage-gated $Ca^{2+}$ channels in rat ventricular myocytes. According to the results, sertraline is a potent blocker of cardiac $K^+$ channels, such as hERG, $I_{Ks}$ and $I_{K1}$. The rank order of inhibitory potency was hERG > $I_{K1}$ > $I_{Ks}$ with $IC_{50}$ values of 0.7, 10.5, and 15.2 ${\mu}M$, respectively. In addition to $K^+$ channels, sertraline also inhibited $I_{Na}$ and $I_{Ca}$, and the $IC_{50}$ values are 6.1 and 2.6 ${\mu}M$, respectively. Modification of these ion channels by sertraline could induce changes of the cardiac action potential duration and QT interval, and might result in cardiac arrhythmia.

Potential Application of Bacteriocin Produced from Lactic Acid Bacteria

  • El Issaoui, Kaoutar;Senhaji, Nadia Skali;Zinebi, Sanae;Zahli, Rajae;Haoujar, Imane;Amajoud, Nadia;Abrini, Jamal;Khay, El Ouardy
    • Microbiology and Biotechnology Letters
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    • v.48 no.3
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    • pp.237-251
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    • 2020
  • Lactic acid bacteria prevent the contamination of food products by inhibiting proliferation of pathogenic bacteria. This is done mainly by the production of lactic acid and antimicrobial peptides (AMPS) known as bacteriocins. The interest in these molecules resides in both their antimicrobial spectrum and safety for human health. The application of bacteriocins or producer strains has been considered to avoid the development of pathogenic bacteria, as most bacteriocins have significant inhibitory activity against food pathogens, such as Listeria monocytogenes. This article describes the classification, structure, mode of action, biosynthesis, and main applications of bacteriocins in different fields: agri-food, aquaculture, and medicine.

The various mechanisms of Korean traditional medicines for anti-cancer (한약의 다양한 항암기전)

  • Park, Yeong-Chul;Park, Yong-Ki;Lee, Sun-Dong
    • The Korea Journal of Herbology
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    • v.27 no.3
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    • pp.39-55
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    • 2012
  • Objectives : Recently there have been encouraging results, from a western perspective, in the cancer research field regarding the anticancer effects of herbal medicine. This paper was aimed to review herbal medicine playing its anticancer role in terms of apoptosis, inflammation control, differentiation and telomerase. Methods : New studies for tang, medicinal herb itself or effective ingradients of medicinal herb showing anti-cancer effectiveness were reviewed and summarized in terms of pharmacological action. Results : Ethanol extracts of $Spatholobus$ $suberectus$ greatly inhibited cancer cell growth inducing cell apoptosis and cytotoxic effects. $Scutellaria$ $baicalensis$ may be responsible for its anticancer activity showing inhibition of $PGE_2$ synthesis via suppression of COX-2 expression. Saikosaponins isolated from $Bupleurum$ induced the differentiation of C6 glioma cells, cancer cells, into astrocytes, normal cells. Acetone extract of $Bupleurum$ $scorzonerifolium$ inhibited proliferation of human lung cancer cells via inducing apoptosis and suppressing telomerase activity. Conclusions : Herbal medicine inhibited cancer cell growth inducing cell apoptosis and cytotoxic effects. Inflammation persisting for a decade eventually elevates the risk of cancer sufficiently that it is discernible in case control epidemiological studies. Differentiation therapy is defined as a therapy to treat cancers by inducing differentiation of the stem cells. Telomerase expression is a hallmark of cancer. Nearly the complete spectrum of human tumors has been shown to be telomerase positive.

Study on the Effect of a New Antiseptic Preparation ″Swi-Se-Yo″ on the Carry-Over Cocoons in Silk Reeling Process (새로 개발한 조월견방부제 ″쉬세요(Swi-Se-Yo)″의 효과에 관하여)

  • 이장낙;정태암;송기언;하정근
    • Journal of Sericultural and Entomological Science
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    • v.18 no.2
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    • pp.107-110
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    • 1976
  • In silk reeling process the carry-over cocoons must be submerged in the reeling baths filled with reeling water and left until reopening the operation. Under the detention the carry-over cocoons are apt to decay without any antiseptic treatment. Thus an useful antiseptic for the cocoons is urgently needed, and various antseptic agents have been tested for their applicability to the process. However, such an useful agent has not been developed yet. Formalin has been the only chemical used for antisepticizing carry-over cocoons, although it has many defects as the antiseptic for the cocoons. In these circumstances, recently we newly prepared an antiseptic useful for preventing the carryover cocoons from decaying. We named the new antiseptic preparation "Swi-Se-Yo." The Korean term "Swi-Se-Yo" literally means "please take a rest". Through a series of experiments with Swi-Se-Yo we obtained the following results: 1) Swi-Se-Yo, in 0.05% aqueous solution, exerted a good antiseptic effect on the boiled Cocoons submerged in the reeling baths and the effect lasted for 45 hours. The duration of the effect is about two times longer than that of Formalin. 2) The percentage of cocoon reel ability of the carry-over cocoons treated with Swi-Se-Yo was 6% higher than that of Formalin and was equal to that of flowing cold water. 3) The percentage of raw silk yield of the carry-over cocoons treated with Swi-Se-Yo was almost equal to that of Formalin and to that of flowing cold water. 4) The quality of raw silk of the carry-over cocoons treated with Swi-Se-Yo is the same as that of flowing cold water. Besides the above favourable results, Swi-Se-Yo has many advantages as an antiseptic. Chemically it is very stable. Its antimicrobial action is very strong and the spectrum is very broad. It can be available in water-soluble powder and in small bulk. And it is not harmful to human and domestic animals. Considering these profitable properties of Swi-Se-Yo, it will have a good reputation as a carry-over cocoon antiseptic. (The chemical composition and manufacturing method of Swi-Se-Yo will be published in the near future.)

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Virulence, Resistance Genes, and Transformation Amongst Environmental Isolates of Escherichia coli and Acinetobacter spp.

  • Doughari, Hamuel James;Ndakidemi, Patrick Alois;Human, Izanne Susan;Benade, Spinney
    • Journal of Microbiology and Biotechnology
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    • v.22 no.1
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    • pp.25-33
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    • 2012
  • The association of verotoxic E. coli and Acinetobacter spp. with various antibiotic-resistant, diarrhogenic, and nosocomial infections has been a cause for concern worldwide. E. coli and A. haemolyticus isolated on a number of selective media were screened for virulence factors, antibiotic resistance, and transformation of resistance genes. Out of 69 E. coli isolates obtained, 25 (35.23%), 14 (20.30%), and 28 (40.58%) were positive for Vtx1&2, Vtx1, and Vtx2, respectively, 49 (71.015%) for extendedspectrum beta-lactamases (ESBLs), 34 (49.28%) for serum resistance, 57 (82.61%) for cell surface hydrophobicity, 48 (69.57%) for gelatinase production, and 37 (53.62%) for hemolysin production. For the 14 A. haemolyticus isolates, only 2 (14.29%) in each case from all the samples investigated were positive for Vtx1, Vtx2 and Vtx1&2 respectively, 8 (57.14%) for ESBLs, 7 (50.00%) for serum resistance, 11 (78.57%) for cell surface hydrophobicity, 4 (28.57%) for gelatinase production, and 8 (57.14%) for hemolysin production. Although transformation occurred among the E. coli and Acinetobacter isolates (transformation frequency: $13.3{\times}10^{-7}-53.4^{-7}$), there was poor curing of the plasmid genes, a confirmation of the presence of stable antibiotic-resistant genes (DNA concentration between 42.7 and 123.8 ${\mu}g$) and intragenetic transfer of multidrug-resistant genes among the isolates. The isolates were potentially virulent and contained potentially transferable antibiotic resistance genes. Detection of virulence factors, antibiotic resistance genes, and transformation among these isolates is a very significant outcome that will influence approaches to proactive preventive and control measures and future investigations. However, continued surveillance for drug resistance among these bacteria and further investigation of the mechanism of action of their virulence factors are a necessity.

Lovastatin Induces Apoptotic Cell Death by Activation of Intracellular Ca2+ Signal in HepG2 Human Hepatoma Cells

  • Lee, Yong-Soo
    • Biomolecules & Therapeutics
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    • v.15 no.3
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    • pp.137-144
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    • 2007
  • Although lovastatin, a competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMGCoA) reductase, has been shown to have anti-cancer actions, the effect on human hepatoma cells was not investigated. Moreover, the exact mechanism of this action is not fully understood. In this study we investigated the mechanism by which lovastatin induces apoptosis using HepG2 human hepatoblastoma cells. Lovastatin induced apoptotic cell death in a dose-dependent manner in the cells, assessed by the flow cytometric analysis. Treatment with mevalonic acid, a precursor of cholesterol, did not significantly suppress the lovastatin-induced apoptosis. Lovastatin induced a rapid and sustained increase in intracellular $Ca^{2+}$ concentration. Treatment with EGTA, an extracellular $Ca^{2+}$ chelator did not significantly alter the lovastatin-induced intracellular $Ca^{2+}$ increase and apoptosis, whereas intracellular $Ca^{2+}$ reduction with BAPTA/AM and intracellular $Ca^{2+}$ release blockers (dantrolene and TMB-8) completely blocked these actions of lovastatin. In addition, the lovastatin-induced apoptosis was significantly reduced by a calpain inhibitor, a broad spectrum caspase inhibitor z-VAD-fmk and inhibitors specific for caspase-9 and caspase-3 (z-LEHD-fmk and z-DEVD-fmk, respectively), but not by an inhibitor specific for caspase-8 (z-IETD-fmk). Collectively, these results suggest that lovastatin induced apoptosis of HepG2 hepatoma cells through intracellular $Ca^{2+}$ release and calpain activation, leading to triggering mitochondrial apoptotic pathway. These results further suggest that lovastatin may be valuable for the therapeutic management of human hepatoma.

Action Mechanism of LB10522, a New Catechol-Substituted Cephalosporin (카테콜 치환체를 가진 세파로스포린계 항생제 LB10522의 작용기전)

  • Kim, Mu-Yong;Oh, Jeong-In;Paek, Kyoung-Sook;Kim, In-Chull;Kwak, Jin-Hwan
    • YAKHAK HOEJI
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    • v.40 no.1
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    • pp.102-111
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    • 1996
  • LB10522 is a new parenteral broad spectrum cephalosporin with a catechol moiety at C-7 position of beta-lactam ring. This compound can utilize tonB-dependent iron transp ort system in addition to porin proteins to enter bacterial periplasmic space and access to penicillin-binding proteins (PBPs) which are the lethal targets of ${\beta}$-lactam antibiotics. The chelating activity of LB10522 to metal iron was measured by spectrophotometrically scanning the absorbance from 200 to 900nm. When $FeCl_3$ was added, optical density was increased between 450 and 800nm. LB10522 was more active against gram-negative strains in iron-depleted media than in iron-replete media. This is due to the increased expression of iron transport channels in iron-depleted condition. LB10522 showed a similar activity against E. coli DC2 (permeability mutant) and E. coli DCO (wild type strain) in both iron-depleted and iron-replete media, indicating a minimal permeaility barrier for LB10522 uptake. LB10522 had high affinities to PBP 3 and PBP 1A, 1B of E. coli. By blocking these proteins, LB10522 caused inhibition of cell division and the eventual death of cells. This result was correlated well with the morphological changes in E. coli exposed to LB10522. Although the in vitro MIC of LB10522 against P. aeruginosa 1912E mutant (tonB) was 8-times higher than that of the P. aeruginosa 1912E parent strain, LB10522 showed a similar in vivo protection efficacy against both strains in the mouse systemic infection model. This result suggested that tonB mutant, which requires a high level of iron for normal growth, might have a difficulty in surviving in their host with an iron-limited environment.

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Effect of Antibiotics upon the Antibacterial Activity of Platelet Microbicidal Protein against Streptococcus rattus BHT

  • Kim, Jae-Wook;Choe, Son-Jin;Lee, Si-Young
    • International Journal of Oral Biology
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    • v.34 no.1
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    • pp.43-48
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    • 2009
  • Thrombin-induced platelet microbicidal protein (tPMP) is a small cationic peptide that exerts potent in vitro microbicidal activity against a broad spectrum of human pathogens, including Staphylococcus aureus and Streptococcus rattus BHT. Earlier evidence has suggested that tPMP targets and disrupts the bacterial membrane. However, it is not yet clear whether membrane disruption itself is sufficient to kill the bacteria or whether subsequent, presumably intracellular, events are also involved in this process. In this study, we investigated the microbicidal activity of rabbit tPMP toward S. rattus BHT cells in the presence or absence of a pretreatment with antibiotics that differ in their mechanisms of action. The streptocidal effects of tPMP on control cells (no antibiotic pretreatment) were rapid and concentration-dependent. Pretreatment of S. rattus BHT cells with either penicillin or amoxicillin (inhibitors of bacterial cell wall synthesis) significantly enhanced the anti-S. rattus BHT effects of tPMP compared with the effects against the respective control cells over most tPMP concentration ranges tested. On the other hand, pretreatment of S. rattus BHT cells with tetracycline or doxycycline (30S ribosomal subunit inhibitors) significantly decreased the streptocidal effects of tPMP over a wide peptide concentration range. Furthermore, pretreatment with rifampin (an inhibitor of DNA-dependent RNA polymerase) essentially blocked the killing of S. rattus BHT by tPMP at most concentrations compared with the respective control cells. These results suggest that tPMP exerts anti-S. rattus BHT activity through mechanisms involving both the cell membrane and intracellular targets.

Development of Monte Carlo Simulation Code for the Dose Calculation of the Stereotactic Radiosurgery (뇌 정위 방사선수술의 선량 계산을 위한 몬테카를로 시뮬레이션 코드 개발)

  • Kang, Jeongku;Lee, Dong Joon
    • Progress in Medical Physics
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    • v.23 no.4
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    • pp.303-308
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    • 2012
  • The Geant4 based Monte Carlo code for the application of stereotactic radiosurgery was developed. The probability density function and cumulative density function to determine the incident photon energy were calculated from pre-calculated energy spectrum for the linac by multiplying the weighting factors corresponding to the energy bins. The messenger class to transfer the various MLC fields generated by the planning system was used. The rotation matrix of rotateX and rotateY were used for simulating gantry and table rotation respectively. We construct accelerator world and phantom world in the main world coordinate to rotate accelerator and phantom world independently. We used dicomHandler class object to convert from the dicom binary file to the text file which contains the matrix number, pixel size, pixel's HU, bit size, padding value and high bits order. We reconstruct this class object to work fine. We also reconstruct the PrimaryGeneratorAction class to speed up the calculation time. because of the huge calculation time we discard search process of the ThitsMap and used direct access method from the first to the last element to produce the result files.