• YAKHAK HOEJI
• /
• v.38 no.3
• /
• pp.322-331
• /
• 1994

For the development new cephalosporin antibiotics with aminothiazolmethoxyimino moiety in the C-7 position and triazolthiomethyl moiety in the C-3 position of cephem ring, $7{\beta}$-[(z)-2-(2-aminothiasol-4-yl)-2-(methoxyimino)acetamido]-3-[5-(aryl or het.)-4-phenyl-4H-1,2,4-triazol-3-yl]thiomethyl-3-cephem-4-carboxylic acids were synthesized. These compounds were tested for antimicrobial activitiy in vitro against ten species of microorganisms. It showed remarkable antibacterial activity against Bacillus subtilis ATCC 6633, Micrococcus luteus ATCC 9341 and Escherichia coli ESS. The antibacterial activity of most new compounds showed more active than cefazoline, but these compounds were lower active than cefotaxime against Pseudomonas aeruginosa IFO 13130.

• Journal of Applied Biological Chemistry
• /
• v.42 no.3
• /
• pp.119-124
• /
• 1999

About two thirds of the naturally occurring antibiotics have been discovered from actinomycetes. Therefore, the probability of discovering further new antibiotics from actinomycetes is declining as many known metabolites are isolated repeatedly. However, various efforts leave been made in order to enhance the probability of discovering novel compounds. In the present study, we have developed new screening strategies based on the antibiotic biosynthetic pathway, and the genetic information, utilizing polymerase chain reaction. We have selected macrolide type polyketides. In order to divide the ansamycin group antibotic of macrolide type polyketides, we have selected 3-amino-5-hydroxybenzoic acid (AHBA) moiety which contains a biosynthetically unique structural element in the group as a target molecules. Oligonucleotide primers were designed to amplify DNA fragments of macrolide type polyketide synthase and AHBA synthase genes from fourteen actinomycetes species. This method was successfully applied to all three of the known macrolide type polyketide produccing actinomycetes tested. In addition, it also identified the presence of potential macrolide type polyketide producing genes from seven actinomycetes that were known to produce none of macrolide type polyketides, and AHBA biosynthetic genes in one actinomycetes. This technique is potentially useful for the screening of new antibiotices and cloning of their biosynthetic genes.

• Journal of Korean Academy of Fundamentals of Nursing
• /
• v.4 no.2
• /
• pp.319-336
• /
• 1997

This study was done to identify the reality in doing the intradermal skin test of injectional antibiotics and to serve a basis to the clinical and educational situations. For the study, the survey was done to the staff nurses who are working at one of the selected 39 hospitals in the capital area, from January 6 to Feburary 8 in 1997. The data analysis was done by mean, standard deviation, Fisher's exact test, t-test, ANOVA through running SAS computer program. The results of the study were as follows : 1. The dilution ratio of the antibiotics was mostly 1 : 10 regardless of what kind of antibitics. Making the contrast was done only for the suspended to the antibiotics. Mostly the reaction was detected after 15 to 20 minutes from its diameter of redness and wheals. Most of the respondents answered they do the intradermal skin test only once for the same antibiotics. 2. In the education on the skin test the 66.7% from the respondents had exposed to the education mostly through the new nurses orientation. The 85,4% from them answered the need of the continuous education which had a significant difference in the number of beds(p=.046). The had experiences of detecting positive reactions(98.3%), and of anaphylaxis(49.5%) which had a significant difference in experience(p=.002) and in their age groups(p=.000). 3. The averge score of the confidence on the intradermal skin test was 3.32 form 4-point scale. Also it had a significant difference from the number of beds(p=.010), the year of experiences(p=.016), and their age groups(p=.046). 4. From the general characteristics of respondents, the injection methods had a significant difference in the amounts of injection, whether adopting the contrast pairing, and the repeatable skin tests for the same antibiotics. 5. Only 15 from 39 hospitals had their protocol about the intradermal skin test provided by nursing department which differs in its contents from that provided by the medical information center. From the results of the study, it is suggested that the continuous education on the intradermal skin test and its unified protocol should be provided. Also it is recomended that the drug manufacturer should notice about its anaphylactic cautions and pack its extra skin test use.

• Proceedings of the Korean Society for Applied Microbiology Conference
• /
• 2000.04a
• /
• pp.3-6
• /
• 2000

Antimicrobial resistance has been a well-recognized problem ever since the introduction of penicillin into clinical use. History of antimicrobial development can be categorized based on the major antibiotics that had been developed against emerging resistant $pathogens^1$. In the first period from 1940 to 1960, penicillin was a dominating antibiotic called as a "magic bullet", although S.aureus armed with penicillinase led antimicrobial era to the second period in 1960s and 1970s. The second stage was characterized by broad-spectrum penicillins and early generation cephalosporins. During this period, nosocomial infections due to gram-negative bacilli became more prevalent, while those caused by S.aureus declined. A variety of new antimicrobial agents with distinct mechanism of action including new generation cephalosporins, monobactams, carbapenems, ${\beta}$-lactamase inhibitors, and quinolones characterized the third period from 1980s to 1990s. However, extensive use of wide variety of antibiotics in the community and hospitals has fueled the crisis in emerging antimicrobial resistance. Newly appeared drug-resistant Streptococcus pneumoniae (DRSP), vancomycin-resistant enterococci (VRE), extended-spectrum ${\beta}$-lactamase-producing Klebsiella, and VRSA have posed a serious threat in many parts of the world. Given the recent epidemiology of antimicrobial resistance and its clinical impact, there is no greater challenge related to emerging infections than the emergence of antibiotic resistance. Problems of antimicrobial resistance can be amplified by the fact that resistant clones or genes can spread within or between the species as well as to geographically distant areas which leads to a global concern$^2$. Antimicrobial resistance is primarily generated and promoted by increased use of antimicrobial agents. Unfortunately, as many as 50 % of prescriptions for antibiotics are reported to be inappropriate$^3$. Injudicious use of antibiotics even for viral upper respiratory infections is a universal phenomenon in every part of the world. The use of large quantities of antibiotics in the animal health industry and farming is another major factor contributing to selection of antibiotic resistance. In addition to these background factors, the tremendous increase in the immunocompromised hosts, popular use of invasive medical interventions, and increase in travel and mixing of human populations are contributing to the resurgence and spread of antimicrobial resistance$^4$. Antimicrobial resistance has critical impact on modem medicine both in clinical and economic aspect. Patients with previously treatable infections may have fatal outcome due to therapeutic failure that is unusual event no more. The potential economic impact of antimicrobial resistance is actually uncountable. With the increase in the problems of resistant organisms in the 21st century, however, additional health care costs for this problem must be enormously increasing.

• Asian-Australasian Journal of Animal Sciences
• /
• v.33 no.11
• /
• pp.1699-1713
• /
• 2020

Bovine mastitis, an inflammation of the mammary gland, is the most common disease of dairy cattle causing economic losses due to reduced yield and poor quality of milk. The etiological agents include a variety of gram-positive and gram-negative bacteria, and can be either contagious (e.g., Staphylococcus aureus, Streptococcus agalactiae, Mycoplasma spp.) or environmental (e.g., Escherichia coli, Enterococcus spp., coagulase-negative Staphylococcus, Streptococcus uberis). Improving sanitation such as enhanced milking hygiene, implementation of post-milking teat disinfection, maintenance of milking machines are general measures to prevent new cases of mastitis, but treatment of active mastitis infection is dependant mainly on antibiotics. However, the extensive use of antibiotics increased concerns about emergence of antibiotic-resistant pathogens and that led the dairy industries to reduce the use of antibiotics. Therefore, alternative therapies for prevention and treatment of bovine mastitis, particularly natural products from plants and animals, have been sought. This review provides an overview of bovine mastitis in the aspects of risk factors, control and treatments, and emerging therapeutic alternatives in the control of bovine mastitis.

• Applied Chemistry for Engineering
• /
• v.27 no.6
• /
• pp.565-572
• /
• 2016

While there have been great demands on improving domestic water pollution issues, the necessity for real time monitoring of particular drug residues in water resources has been raised since drug residues including antibiotics could provoke new trains of drug-resistant bacteria in water environments. Among many different types of drugs used for pharmaceutical treatment, antibiotics are considered to be one of the most hazardous to our ecosystem since they can rapidly promote the spreading of drug-resistant bacteria in water environments. In this mini-review, we will highlight recent developments made on creating in-situ sensing platforms for the fast monitoring of antibiotic residues in aquatic environmental samples focusing on optical and electrochemical techniques. Related recent technology developments and the resulting economy effects will also be discussed.

• Microbiology and Biotechnology Letters
• /
• v.19 no.3
• /
• pp.235-241
• /
• 1991

- A phthalic acid derivative and basic macrolide antibiotics, with antimicrobial activity against Gram positive bacteria and phytopathogenic fungi, respectively, were found to be produced by a strain 88-GT-161 identified as being a variety of Streptomyces melanosporofaciens. This paper describes an isolation procedure of the active compounds produced by this strain, their in vitro and in vivo (pot test) antimicrobial activites, and structure determination of one of the compounds, bis (2-ethylhexyl) phthalate, a phthalic acid derivative antibiotic. This compounds, upon cornparision with authentic bis (2-ethylhexyl) phthalate, dioctyl phthalate, revealed a difference in antimicrobial activity even though physico-chemical properties of these two compounds seemed indentical. This is the first report that dioctyl phthalate is biosynthetically produced by a Streptomyces sp. and shows antimicrobial activity.

• Journal of Periodontal and Implant Science
• /
• v.26 no.2
• /
• pp.356-364
• /
• 1996

The present study was done to evaluate the antibacterial effects of $Minoclin^R$ which was localally delivered on the $Gore-tex^R$ barrier membrane in the guided tissue regeneration(GTR) therapy for treatment of human furcal defects. Beneath the membranes. the antibiotics were applied for 1 week and then changed with new one. The $Minoclin^R$ was removed out one week later. 6 weeks after the GTR therapy. No systemic antibiotics were administered except for oral mouthrinses with chlorhexidines. 2 weeks and 6 weeks following the membrane therapy, the bacterial samples were examined for periodontopathic microorganisms. The results indicated that the locally delivered $Minoclin^R$ successfully inhibited the growth of periodontopathic organisms. This results might be further applied in the subgingival plaque control regimen in the GTR procedure, especialy in patients who is contraindicated for oral administration of systemic antibiotics

• Bulletin of the Korean Chemical Society
• /
• v.30 no.8
• /
• pp.1839-1844
• /
• 2009

A 20-residue hybrid peptide CA(1-8)-MA(1-12) (CAMA) incorporating residues 1-8 of cecropin A (CA) and residues 1-12 of magainin 2 (MA) has high antimicrobial activity without toxicity. To investigate the effects of the total positive charges of CAMA on the antibacterial activity and toxicity, a hybrid peptide analogue (CAMA-syn) was designed with substitutions of $Ile^{10}\;and\;Ser^{16}$ with Lys. According to CD spectra, structure of CAMA-syn with increase of cationicity was very similar to that of CAMA in DPC micelle. CAMA-syn showed antimicrobial activity similar with CAMA while CAMA-syn has no hemolytic activity and much lower cytotoxicity against RAW 264.7 macrophage cells than CAMA. Also, CAMA and CAMA-syn significantly inhibited NO production by LPSstimulated RAW264.7 macrophage at 10.0∼20.0 $\mu$M. CAMA-syn displayed salt resistance on antimicrobial activity against Escherichia coli at the physiological concentrations of $CaCl_2\;and\;MgCl_2$. The combination studies of peptides and antibiotics showed that CAMA-syn has synergistic effects with synthetic compound and flavonoid against Enterococcus faecalis and VREF. CAMA-syn can be a good candidate for the development of new antibiotics with potent antibacterial and synergistic activity but without cytotoxicity.

• Korean Journal of Clinical Pharmacy
• /
• v.9 no.1
• /
• pp.1-14
• /
• 1999

Vancomycin-resistant Enterococci (VRE) have recently emerged in Korean hospitals, as well as in those of other countries. VRE have been partially attributed to the overuse and misuse of vancomycin. The mecbanisms of VRE resistance are related to VanA, VanB, and VanC. Both VanA and VanB produce abnormal ligase enzymes to form D-ala-D-lactate termini in E. faecium and E. faecalis, instead of D-ala-D-ala termini. Meanwhile, Van C produces D-ser-D-ala termini in E. gallinarum and E. casseliflavus. These abnormal termini have a low affinity to vancomycin. As a result, VRE avoid the activity of vancomycin by these mechanisms. Unfortunately, there is no approved therapy for the treatment of VRE. Thus, available but uncommonly prescribed antibiotics (due to their toxicity or unproven efficacy) may become possible options. They include chloramphenicol, novobiocin, fosfomycin, and bacitracin. The combination therapy of available agents may also be the other options. They include high doses of a penicillin- or ampicillin-aminoglycoside combination, high doses of an ampicillin/sulbactam and aminoglyoosidcs combination, an ampicillin and vancomycin combination, and a ciprofloxacin, aminoglycosides, and rifampin combination. With respect to the near future, many types of investigational agents will most likely expand their treatment options for VRE. Teicoplanin, a glycopeptide, can be used for VanB- and VanC-related VRE. LY333328, a new generation of glycopeptide, is effective in treating VanA as well as VanB and VanC. RP59500 (quinupristin/dalfopristin), a streptogramin, is effective in treating vancomycin-resistant E. faecium. New generation quinolones (especially clinatloxacin) are potential options for the treatment of VRE, even though they cannot work as effectively against VRE as they can against Staphylococci. Both glycylcyclines (a new generation of tetracyclines) and ketolides (a new generation of macrolides) show good activity against Enterococci, regardless of vancomycin susceptibility. Oxazolidinones (i. e. eperezolid and 1inezolid) and everninomicins (i. e. SCH27899) are new groups of antibiotics, which also demonstrate good activity against VRE. It is imperative that clinical pharmacists take the responsibility of investigating new treatment options for VRE in order to combat this growing problem throughout the world.