• Title/Summary/Keyword: new antibiotics

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Estrogen Receptor Enhances the Antiproliferative Effects of Trichostatin A and HC-toxin in Human Breast Cancer Cells

  • Min, Kyung-Nan;Cho, Min-Jung;Kim, Dae-Kee;Sheen, Yhun-Yhong
    • Archives of Pharmacal Research
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    • v.27 no.5
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    • pp.554-561
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    • 2004
  • Trichostatin A, an antifungal antibiotics, and HC-toxin are potent and specific inhibitors of histone deacetylase activity. Histone deacetylase inhibitors are new class of chemotherapeutic drugs able to induce tumor cell apoptosis and/or cell cycle arrest. In this study, the antiproliferative activities of trichostatin A and HC-toxin were compared between estrogen receptor positive human breast cancer cell MCF-7 and estrogen receptor negative human breast cancer cell MDA-MB-468. Trichostatin A and HC-toxin showed potent antiproliferative activity in both MCF-7 and MDA-MB-468 cells. In MCF-7 cells that contain high level estrogen receptor, trichostatin A and HC-toxin brought about three-times more potent cell growth inhibitory effect than estrogen receptor negative MDA-MB-468 cells. Both trichostatin A and HC-toxin showed cell cycle arrest at G$_2$/M phases of MCF-7 and MDA-MB-468 cells in a dose- and time- depen- dent manner. Trichostatin A and HC-toxin also induced apoptosis from MCF-7 and MDA-MB-468 cells in a dose- and time-dependent manner. Results of this study suggested that antipro-liferative effects of trichostatin A and HC-toxin might be involved in estrogen receptor signaling pathway, but cell cycle arrest and apoptosis of trichostatin A and HC-toxin might not be involved in estrogen receptor system of human breast cancer cells.

Studies on the Synthesis and Antibacterial Activity of New $\beta$-Lactam Antibiotics (새로운 베타락탐 항생물질의 합성과 생물활성에 관한 연구)

  • Tae Heung Song;Young Ho Kim
    • Journal of the Korean Chemical Society
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    • v.36 no.2
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    • pp.293-300
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    • 1992
  • The synthesis of a series of 7-[(Z)-2-(2-aminothiazol-4-yl)-2-oxyiminoacetamido]-3-(4,6-diamino-1-alkyl-1,3,5-triazinium-2-yl)thiomethyl-3-cephem-4-carboxylates is described. Variations of an oxyimino moiety in the 7-side chain and quaternary ammonium moiety in the 3-side chain were examined and structure-activity relationship was studied. The 4,6-diamino-1-methyl-1,3,5-triazinium-2-yl derivative of the 7-$\alpha$-methoxyimino series of cephalospoins, particularly 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetamido]-3-(4,6-diamino-1-methyl-1,3,5-triazinium-2-yl)thiomethyl-3-cephem-4-carboxylate(C-1), exhibited broad antibacterial activity against Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa.

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Susceptibility of Oral Bacterial to Sophoraflavanone G isolated from the Root of Sophora flavescens

  • Kim, Kyong-Heon;Kim, Baek-Cheol;Yun, Ju-Bong;Jeong, Seung-Il;Kim, Hong-Jun;Ju, Young-Sung
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.17 no.3
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    • pp.33-37
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    • 2004
  • Objective: The aim of this work is to investigate the antibacterial activity of the Sohporaflavanone G isolated from Sophora flavescens (S. flavescens), as the development of microbial resistance to antibiotics make it essential to constantly look for new and active compounds effective against pathogenic bacteria. Method : Sophoraflavanone G was isolated from the dried roots of Sophora flavescens Aiton (Leguminosae) by bioassay?guided fractionation. We investigated the effect of sophoraflavanone G on oral bacterial at various concentrations after incubation of 24 h in strains in the dose?dependent manner. Results: The structure of active compound, Sophoraflavanone G having a lavandulyl group at C?8, was elucidated on the basis of spectral data especially 1H?NMR and I3C?NMR. The antimicrobial activity showed that Sophoraflavanone G exhibited antimicrobial activilies against all the bacteria tested (MICs, 0.39 - 6.25 ㎍/ml). Sophoraflavanone G showed the strong antimicrobial activity against all the facultative bacteria and microaerophilic bacteria (MICs, 0.78 - 1.56 ㎍/ml) and also Sophoraflavanone G showed the strong antimicrobial activity against obligate anaerobic bacteria (MICs, 0.39 - 6.25 ㎍/ml).

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Improved Selective Medium for Isolation and Enumeration of Bifidobacterium sp. (개량된 Bifidobacterium의 선택배지 개발)

  • Ji, Geun-Eog;Lee, Se-Kyung;Kim, In-Hee
    • Korean Journal of Food Science and Technology
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    • v.26 no.5
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    • pp.526-531
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    • 1994
  • In order to develop a new improved selective medium for the Bifidobacterium sp. from the human fecal samples, one hundred eight Bifidobacterium strains were isolated and identified. Sensitivity test for the antibiotics and antimetabolites and test for the specific substrate were performed to obtain basic data for the development of the Bifidobacterium selective medium. TOS(transgalactosylated oligosaccharide) was shown to be preferentially used by Bifidobacterium sp.. Sodium propionate promoted the growth of Bifidobacterium while inhibiting other intestinal bacteria. Upon these results, TP medium was designed and shown to be very effective for the selection of Bifidobacterium and better than Mitsuoka BS medium.

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A New Deoxyhexose Biosynthetic Gene Cluster in Streptomyces griseus ATCC10137: Heterologous Expression of dTDP-D-Glucose 4,6-Dehydratase Gene

  • Kim, Sang Suk;Bang, Jung-Hee;Hyun, Chang-Gu;Kim, Joo-Woo;Han, Jae-Jin;Suh, Joo-Won
    • Journal of Applied Biological Chemistry
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    • v.43 no.3
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    • pp.136-140
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    • 2000
  • A novel 6-deoxyhexose biosynthetic gene cluster different from the one for the biosynthesis of streptomycin was isolated from Streptomyces griseus using specifically designed PCR primers to compare the sequence of known dTDP-glucose synthase genes. We cloned a 5.8-kb DNA from Streptomyces griseus ATCC10137, which contained the 4-ketoreductase homologue (grsB), dTDP-glucose synthase (grsD), and dTDP-glucose 4, 6-dehydratase (grsE) genes. Escherichia coli cultures containing plasmid of the PCR product which encoded the grsE region under the controUed T7 promoter were able to catalyze the formation of dTDP-4-keto-6-deoxy-D-glucose from TDP-glucose. The enzyme showed high substrate specificity, being specific to only dTDP-glucose that is known to be incorporated into secondary metabolites such as antibiotics.

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Antimicrobial Activity of Antimicrobial Peptide LPcin-YK3 Derived from Bovine Lactophoricin

  • Kim, Ji-Sun;Jeong, Ji-Ho;Cho, Jang-Hee;Lee, Dong-Hee;Kim, Yongae
    • Journal of Microbiology and Biotechnology
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    • v.28 no.8
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    • pp.1299-1309
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    • 2018
  • We previously reported on lactophoricin (LPcin), a cationic ${\alpha}-helical$ antimicrobial peptide derived from bovine milk, which has antimicrobial effects on Candida albicans as well as Gram-positive and Gram-negative bacteria. In this study, we designed the LPcin-YK3 peptide, a shorter analog of LPcin, and investigated its antimicrobial activity. This peptide, consisting of 15 amino acids with + 3 net charges, was an effective antimicrobial agent against the on the Gram-positive strain, Staphylococcus aureus (MIC: $0.62{\mu}g/ml$). In addition, the hemolytic activity assay revealed that the peptide was not toxic to mouse and human erythrocytes up to $40{\mu}g/ml$. We also used circular dichroism spectroscopy to confirm that peptide in the presence of lipid has ${\alpha}-helical$ structures and later provide an overview of the relationship between each structure and antimicrobial activity. This peptide is a member of a new class of antimicrobial agents that could potentially overcome the problem of bacterial resistance caused by overuse of conventional antibiotics. Therefore, it could be used as a therapeutic or natural additive, particularly in the cosmetics industry.

Triple antibiotic paste: momentous roles and applications in endodontics: a review

  • Parhizkar, Ardavan;Nojehdehian, Hanieh;Asgary, Saeed
    • Restorative Dentistry and Endodontics
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    • v.43 no.3
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    • pp.28.1-28.16
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    • 2018
  • This study investigated the latest findings and notions regarding 'triple antibiotic paste' (TAP) and its applications in dentistry, particularly endodontics. TAP is a combination of 3 antibiotics, ciprofloxacin, metronidazole, and minocycline. Despite the problems and pitfalls research pertaining to this paste has unveiled, it has been vastly used in endodontic treatments. The paste's applications vary, from vital pulp therapy to the recently introduced regeneration and revascularisation protocol. Studies have shown that the paste can eliminate the root canal microorganisms and prepare an appropriate matrix for further treatments. This combination is able to remove diverse groups of obligate and facultative gram-positive and gram-negative bacteria, providing an environment for healing. In regeneration protocol cases, this allows the development, disinfection, and possible sterilization of the root canal system, so that new tissue can infiltrate and grow into the radicular area. Moreover, TAP is capable of creating a discipline in which other wanted and needed treatments can be successfully performed. In conclusion, TAP, as an antibacterial intracanal medication, has diverse uses. Nevertheless, despite its positive effects, the paste has shown drawbacks. Further research concerning the combined paste and other intracanal medications to control microbiota is a must.

Post-Antibiotic Effect of LB20304, A New Quinolone Antibiotic (새로운 퀴놀론 항생제 LB20304의 Post-Antibiotic Effect)

  • Ahn, Mi-Jeong;Paek, Kyoung-Sook;Kim, Mu-Yong;Kim, In-Chull;Kwak, Jin-Hwan
    • YAKHAK HOEJI
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    • v.40 no.3
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    • pp.347-350
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    • 1996
  • The post-antibiotic effect (PAE), which is defined as the period of time lag that the target organisms resume normal growth rate after complete removal of the antibiotics, of LB 20304 and ciprofloxacin was evaluated against Staphylococcus aureus 6538p and Escherichia coli 3190Y, respectively. The PAE was estimated by adding each antibiotic to a log phase of growth and incubating at $37^{\circ}$C for 1 h.Antibiotic was removed by centrifugation, and total viable cell counts were determined hourly for a further 10 h. The PAEs of LB20304 against S. aureus at concentrations of $1{\times}MIC\;and\;2{\mu}g/ml$ were 10 min and 93min, respectively. LB20304 showed a comparable PAE to ciprofloxacin. Against E. coli, the PAE of LB20304 was also similar to that of ciprofloxacin at concentration of $4{\times}MIC$ but it was much longer than that of ciprofloxacin at concentration of 2${\mu}g/ml$. LB20304 showed higher lethality than ciprofloxacin against both S. aureus and E. coli strains.

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Microbial Composition and Pattern of Antibiotic Resistance in Subgingival Microbial Samples From Patients With Refractory Periodontitis (난치성 치주염환자로부터 채취한 치은연하 세균의 구성과 항생제 내성에 관한 연구)

  • Chang, Beom-seok
    • Journal of Periodontal and Implant Science
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    • v.30 no.4
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    • pp.725-736
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    • 2000
  • It is becoming increasingly apparent that periodontitis consists of mixture of diseases, most of which respond favorably to traditional mechanical therapy. Among these variants of the disease, some appear to be associated with unusual microbial infections and defective host defenses. Many of these fail to respond to conventional treatment. The recognition that some forms of periodontitis are refractory to standard periodontal therapy has given rise to a new classification of peridontitis. A series of 1692 subgingival microbial samples sent to a diagnostic microbiology laboratory included 738 samples that could be identified as compatible with a clinical diagnosis of refractory or recurrent periodontitis. In descending order of prevalence the associated microbiota included Bacteroides forsythus(85%) ,Fusobacterium species(78%), Spirochetes(67%), Campylobacter rectus(64%), Porphyromonas gingivalis(59%), Peptostreptococcus micros(58%), motile rods(46%), Prevotella intermedia(33%), Eikenella corrodens(13%), Capnocytophaga species(12%) ,and Actinobacillus actinomycetemcomitans(6%). Antibiotic resistance to tetracycline, penicillin G, or metronidazole was particularly noticeable for Fusobacterium species, Capnocytophaga species, and Actinobacillus actinomycetemcomitans. It was largely absent for Campylobacter rectus. No antibiotic data were obtained for Porphyromonas gingivalis or Bacteroides forsythus, as these species were detected by immunofluorescence. The results indicate that a substantial number of microorganisms associated with refractory periodontitis are variably resistant to commonly-used antibiotics. Diagnostic microbiology must be considered an essential adjunct to the therapist faced with periodontal lesions refractory to conventional treatment.

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Synthesis and Biological Activity of 3 - (Substituted) Tetrazolylmethyl Cephalosporins (3- (치환) 테트라조일메칠세파로스포린의 합성과 생리활성)

  • Ko, Ok-Hyun;Kim, Young-Soo;Ko, Bong-Suk;Lee, Jae-Young;Ha, Jai-Chun;Bang, Hee-Jae;Yoo, Jin-Cheol;Kang, Hyung-Ryong
    • YAKHAK HOEJI
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    • v.42 no.1
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    • pp.12-24
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    • 1998
  • For the development of new cephalosporin antibiotics with aminothiazolcarboxymethylethoxyimino moiety on the C-7 position and tetrazolymethyl moiety on the C-3 position of cephe m ring, 7${\beta}$-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[5-(substituted)tetrazol-2-yl]methyl-3-cephem-4-carboxylic acids(28-35) were synthesized. These compounds were tested for antimicrobial activity in vitro against Gram(+) and Gram(-) bacteria. They showed remarkable antibacterial activity against Escherichia coli AB 1157, Escherichia coli AB 0111, Escherichia coli BE 1186, Micrococcus luteus ATCC 9341, Salmonella typhimurium TV 119, Salmonella typhimurium SL 1102, Staphylococcus aureus IFO 12732, Staphylococcus aureus R-209, but these compounds were not active against Pseudomonas aeruginosa N-10.

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