• Fisheries and Aquatic Sciences
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• 제19권10호
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• pp.45.1-45.5
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• 2016

As a novel strategy to remove ${\beta}$-lactam antibiotic residues from fish tissues, utilization of ${\beta}$-lactamase, enzyme that normally degrades ${\beta}$-lactam structure-containing drugs, was explored. The enzyme (TEM-52) selectively degraded ${\beta}$-lactam antibiotics but was completely inactive against tetracycline-, quinolone-, macrolide-, or aminoglycoside-structured antibacterials. After simultaneous administration of the enzyme with cefazolin (a ${\beta}$-lactam antibiotic) to the carp, significantly lowered tissue cefazolin levels were observed. It was confirmed that the enzyme successfully reached the general circulation after intraperitoneal administration, as the carp serum obtained after enzyme injection could also degrade cefazolin ex vivo. These results suggest that antibiotics-degrading enzymes can be good candidates for antibiotic residue depuration.

• 대한본초학회지
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• 제20권2호
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• pp.171-179
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• 2005

Objectives & Methods : In order to evaluate the in vivo synergic effect of Mawhangyounpye-tang which was a traditional poly-herbal formula has been used in the treatment of respiratory diseases in Korea, with quinolone antibiotic, ciprofloxacin (CPFX), the viable bacterial number and histopathological changes were monitored after experimental respiratory infection with Klebsiella peumoniae NCTC 9632. Results : The obtained results were as follows : 1. In CPFX group, the viable bacterial numbers were significantly decreased compared to that of control group and these were more dramatically decreased compared to that of single treatment with CPFX, respectively in concomitant treated groups with Mawhangyounpye-tang. 2. In control group, severe infiltration of inflammatory cells, hemorrhage and hypertrophy of alveolar linings were demonstrated at microscopical levels. However, these abnormal histopathological changes were significantly decreased compared to that of control group in CPFX group, and these were more dramatically decreased compared to that of single treatment with CPFX, respectively in concomitant treated groups with Mawhangyounpye-tang. 3. In CPFX group, the LSA (luminal surface of alveoli %) were significantly increased compared to that of control group and these were more dramatically decreased compared to that of single treatment with CPFX, respectively in concomitant treated groups with Mawhangyounpye-tang. Conclusions : It is considered that in vivo antibacterial activity of CPFX was dramatically increased by concomitant use of Mawhangyounpye-tang against Kebsiella pneumoniae NCTC 9632 infection of respiratory tract.

• Mycobiology
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• 제29권1호
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• pp.11-14
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• 2001

A preparation of water soluble components(EA) was made from carpophores of Elfvingia applanata(Pers.) Karst and its in vitro antibacterial activity on a number of bacterial species was examined by macrobroth dilution assay. Among 16 species of bacteria tested, the most potent antibacterial activity was observed against Staphylococcus epiderrnidis and Proteus vulgaris, of which MICs were 1.25 mg/ml. To investigate the antibacterial effects in combinations of EA with quinolone antibiotics, such as ciprofloxacin, enoxacin, lomefloxacin, norfloxacin, and ofloxacin, the fractional inhibitory concentrations(FICs) and the fractional inhibitory concentration indices(FICIs) for four bacterial strains were determined by macrobroth dilution checkerboard assay. Combinations of EA and quinolones exhibited either additive or indifferent effects of antibacterial activity in most instances. However, both synergistic and antagonistic effects were not observed in any cases.

• Environmental Engineering Research
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• 제25권4호
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• pp.488-497
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• 2020

The present study investigates the feasibility of nitrogenous heterocyclic compounds (NHCs) (Pyridine-Quinoline) degradation by catalytic wet peroxidation (CWPO) in the presence of nanoscale zerovalent iron supported on granular activated carbon (nFe⁰/GAC) using statistical optimization technique. Response surface methodology (RSM) in combination with Box-Behnken design (BBD) was used to optimize the process parameters of CWPO process such as initial pH, catalyst dose, hydrogen peroxide dose, initial concentration of pyridine (Py) and quinolone (Qn) were chosen as the main variables, and total organic carbon (TOC) removal and total Fe leaching were selected as the investigated response. The optimization of process parameters by desirability function showed the ~85% of TOC removal with process condition of initial solution pH 3.5, catalyst dose of 0.55 g/L, hydrogen peroxide concentration of 0.34 mmol, initial concentration of Py 200 mg/L and initial concentration of Qn 200 mg/L. Further, for TOC removal the analysis of variance results of the RSM revealed that all parameter i.e. initial pH, catalyst dose, hydrogen peroxide dose, initial concentration of Py and initial concentration of Qn were highly significant according to the p values (p < 0.05). The quadratic model was found to be the best fit for experimental data. The present study revealed that BBD was reliable and effective for the determination of the optimum conditions for CWPO of NHCs (Py-Qn).

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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• pp.118-118
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• 1993

퀴놀론 모핵의 합성은 기존에 알려진 합성 방법인 Could-Jacobs방법과 Bayer방법에 의해서 Intermediate로 사용된 7-chloro-1-ethyl-6-fluoro-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid와 1-cyclopropyl-7-chloro-6-Fluoro-1,4-dihydro-4-oxoquinolne-3-carboxylic acid를 합성하였다. Heteroaromatic tin compound는 furan, thiophene, 3-bromopyridine, 2-fluoropyridine에 n-BuLi을 사용하여 metallation 한후 electrophile로 tributyltin chloride를 사용하여 2-tributylstannofuran, 2-tributylst-annothiophene, 3-tributylstannopyridine, 2- fluoro-2-tributylstannop-yridine을 합성할 수 있었다. 이상의 Intermediate와 tin compounds를 p-alladium 촉매하에서 반응시켜 1-ethyl-7-(2-furanyl)-6-fluoro-1,4-dihy-dro-4-oxo-3-quinoline-carboxylic acid (compound 3), 1-ethyl-7-(2-th-iophenyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinol in carboxylic acid(compound 5), 1-ethyl-7-(3-pyridinyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 7), 1-ethyl-7-(2-fluoro-3-pyrid-nyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 9), 1-cyclopropyl-7-(2-furanyl) -6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 4), 1-cyclopropyl-7-(2-thiophenyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 6) ,1-cyclopropyl-7-(3-pyridinyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 8), 1-cyclopropyl-7-(2-fluoro-3-pyridinyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acid (compound 10)를 합성하였다.

• 한국동물위생학회지
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• 제28권3호
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• pp.245-251
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• 2005

The purposes of this study were to evaluate the distribution of quinolone and to investigate the effects of quinolones (enrofloxacin, ciprofloxacin) in blood(plasma) and eggs of laying hens. Animals were fed quinolones which supplemented with 20, 50, 80 mg/kg of body weight. Blood and egg samples were collected after oral administration and analyzed for quinolones (enrofloxacin, ciprofloxacin) by HPLC. In laying hens, the residue period of enrofloxacin were longer than that of ciprofloxacin and the levels of residues were elavated by drug dosage.

• 대한수의학회지
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• 제34권1호
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• pp.153-163
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• 1994

A study on quinolone antibacterial (pefloxacin methanesulfonate) was performed to use for the drug of fisheries. Petloxacin was proved excellent in antibacterial activity and resistance against fish pathogens when compared with the existing antibacterials. And any side effect was not observed during the period of indicated use. An outline of MIC(Minimal Inhibitory Concentration) was $1.6{\sim}6.4{\mu}g/ml$, $TLm_{48h}$ value were 380~420 ppm in Israeli carp(Cyprinus caprio) and 2100~2300 ppm in flounder(Paralichthys olivaceus). The residual time of fish body was less than 15 days. So we can treat some bacterial disease of fish by the dosage of 100 g/day/ton of fish body weight for 3 days and pefloxacin is thought to be used effectively and widely against most bacterial fish pathogens.

• 약학회지
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• 제55권1호
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• pp.11-15
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• 2011

Zabofloxacin is a novel broad spectrum fluoroquinolone with excellent anti-pneumococcal activity. We investigated the in vitro activity of zabofloxacin against clinical isolates of gram-positive bacteria and the in vivo activity against systemic infection in mice. Zabofloxacin was very active against gram-positive bacteria except QRSA (Quinolone-resistant S. aureus) and VRE(Vancomycin-resistant Enterococci). Especially, zabofloxacin was extremely potent against clinical isolates of Streptococci. Zabofloxacin was as active as gemifloxacin against systemic infection in mice. In view of its improved antibacterial activities against gram-positive bacteria and good pharmacokinetic profiles in animals, the clinical usefulness of zabofloxacin should be established by further studies.

• Bulletin of the Korean Chemical Society
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• 제28권9호
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• pp.1573-1578
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• 2007

Fluorescence quenching of norfloxacin (NOR) by Cu2+, Ni2+, Co2+ and Mn2+ was studied in water. The change in the fluorescence intensity and lifetime was measured as a function of quencher concentration at various temperatures. According to the Stern-Volmer plots, the NOR was quenched both by collisions and complex formation with the same quencher. However, the static quenching had a more important effect on the emission. Large static and dynamic quenching constants support significant ion-dipole and orbital-orbital interactions between NOR and cations. The both quenching constants by Cu2+ were the largest among quenchers. Also, quenching mechanism of Cu2+ was somewhat different. The change in the absorption spectra due to the quencher provided information on static quenching. The fluorescence of NOR was relatively insensitive to both the dynamic and static quenching compared with other quinolone antibiotics. This property can be explained by the twisted intramolecular charge transfer.

• 한국동물위생학회지
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• 제30권3호
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• pp.363-374
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• 2007

A biochemical characterization and antimicrobial drugs susceptibility study was conducted in four breeding kennel which was canine abortion caused by Brucella canis in Gyeongbuk province in 2003-2006. Total of 267 dogs domesticated in the four kennel were examination. Among them, 143 (53.6%) dogs were sero-positive and 25 of blood samples were isolated to Brucella canis. At amplification of 35KDa-BCSP gene using PCR, 711 bp DNA fragment was same visible in 25 isolates and B canis RM6/66. Biochemical characterization of B canis isolated was non-hemolytic, no production of $H_2S$, no fermentation of carbohydrates, catalase-positive, oxidase-positive, indol-negative, hydrolyzation of urea, reduction of nitrate and development of thionin dye medium. Using disk-diffusion method, all of 25 strains tested were found to be highly susceptible to tetracycline, aminoglycoside, quinolone, macrolide antibiotics, rifampin and ampicillin in vitro. Using PFGE with restriction enzyme Smi I, 25 isolates tested were typed to 2 pattern, S1 and S2.