• Proceedings of the Korean Society of Applied Pharmacology
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• 1997.04a
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• pp.57-63
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• 1997

Animal and clinical investigations have shown that fluoroquinolones, new quinolone antibacterial agents (NQs), are well absorbed across the intestinal tract, with a bioavailability of 60-90% after oral administration. Although some types of carrier-mediated intestinal transport mechanisms have been reported for enoxacin (ENX), ofloxacin (OFLX) and sparfloxacin (SPFX), recent results using a human intestinal epithelial cell line, Caco-2, indicated a passive or nonsaturable transport of SPFX, one of the most hydrophobic NQs. The mechanism underlying the intestinal absorption of NQs is still largely unknown. The distribution of NQs into peripheral tissues including erythrocytes is very rapid and their tissue-to-plasma concentration ratios (Kp) are considerably larger than those of inulin (an extracellular fluid space marker), in spite of almost complete ionization of NQs at the physiological pH. Our findings suggest that OFLX and lomefloxacin (LFLX) are taken up by rat erythrocytes via a transport system common to that of a water-soluble vitamin, nicotinic acid.

• Archives of Pharmacal Research
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• v.21 no.2
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• pp.106-112
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• 1998

Structure-activity relationship of 20 fluoroquinolones was studied using the susceptible and 4 resistant Escherichia coli which were developed against 4 fluoroquinolones [ciprofloxacin (1), KR-10755 (6), norfloxacin (2), and ofloxacin (3)] in our laboratory. The C-7 and C-8 substituents of fluoroquinolone were important in various functions such as the inhibitory activity on DNA gyrase, permeability, and efflux. Among 20 fluoroquinolones, compounds with a 3-methyl-3,7-diazabicyclo[3.3.0]octan-1(5)-ene-7-yl substituent at the C-7 position or a chlorine substituent at the C-8 position showed a good inhibitory activity on DNA gyrase (especially a mutated DNA gyrase). Compounds with a 3,7-diazabicyclo [3.3.0]octan-1(5)-ene-7-yl substituent at the C-7 position showed good permeability in the susceptible and resistant strains, while compounds with a fluorine substituent at the C-8 position were less eff luxed from cells.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.106-106
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• 1993

DWC-751은 그람양성 및 음성균주에 대하여 광범위한 항균스펙트럼을 가지는 것으로 나타났다. 그람양성균 S. aureus에 대하여는 cefpirome과 동등하며, cefotaxime 보다 4배, ceftazidime보다 16배 우수하였고 그람음성균에 대하여 DWC-751의 항균력은 cefpirome, cefotaxime보다 2배, ceftazidime보다 4-8배 우수하였다. Ps. aeruginosa에 대한 DWC-751의 항균력은 ceftazidime과 거의 동등한 항균력을 나타내었고, cefpirome보다 2배, cefotaxime보다 4-8배 우수한 항균력을 나타내었다. 임상분리균주 및 ofloxacin 내성균주에 대한 DWC-751의 항균력은 표준균주에 대한 결과와 같이 대조약물보다 우수하였다. 전신감염치료효과에 있어서 Streptococcus pyogenes, Serratia marcescens, Acinetobacter calcoaceticus, Morganella morganii, Proteus mirabilis에 대한 동물실험 결과, ED$_{50}$치에 의한 효능은 cefotaxime 보다 우수하였으며,Enterobacter cloacae, Pseudomonas aeruginosa에 대하여는 ceftazidime과 거의 동등하였다.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.278.2-278.2
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• 2003

A column-switching semi-micro HPLC method with fluorescence detection was developed for the direct analysis of rebamipide in human plasma. Plasma was filtered through a 0.45 $\mu\textrm{m}$ membrane filter and 5 ${\mu}\ell$ of the filtrate was directly injected onto the pre-column. After elution of the plasma proteins to waste, the retained rebamipide and internal standard(ofloxacin) were transferred to a C18 semi-microcolumn (5$\mu\textrm{m}$, 150 ${\times}$2.0mm) where they were separated using acetonitrile-1.4％ acetic acid (40:60, v/v) as mobile phase. (omitted)

• Journal of fish pathology
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• v.9 no.2
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• pp.185-193
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• 1996

Extensive acquirement of drug resistance to traditional antibacterial agents poses a serious problem to eel aquaculturists. To collect the basic information for new drug development in the future, we assessed the in vitro antibacterial efficacy of 14 new quinolones with 75 isolates of Edwardsiella tarda from local aquaculture tanks of Anguilla japonica. Of all tested quinolones under development or marketed for human use, DU-6859 was most potent with its $MIC_{50}$ value of $0.05{\mu}g$/ml in broth microdilution assay. The drugs whose $MIC_{50}$ values ranged from 0.2 to $0.78{\mu}g$/ml were T-3762, Bay-y3118, ciprofloxacin, norfloxacin, ofloxcin and tosufloxacin. The weakest group of drugs, with their $MIC_{50}$ being 1.56-$3.13{\mu}g$/ml, were difloxacin, sparfloxacin, fleroxacin, Q-35, amifloxacin, lomefloxacin and enoxacin. The number of resistant strains, when arbitrarily defined with their MICs of $\geq6.25{\mu}g$/ml, was : 3 to T-3762, 3 to Bay-y3118, 44 to difloxacin, 16 to sparfloxacin, 13 to ciprofloxacin, 19 to fleroxacin, 36 to Q-35). 31 to amifloxacin, 5 to norfloxacin, 13 to ofloxacin, 31 to lomefloxacin, 41 to enoxacin, 12 to tosufloxacin and 0% to DU-6859, respectively. This information can be taken into consideration for the future development of fisheries antibacterial quinolones.

• Journal of fish pathology
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• v.20 no.3
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• pp.221-227
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• 2007

In this study, one hundred strains of bacterial flora were isolated from the intestine of cultured and wild black rockfish Sebastes inermis collected in Yeosu and examined for drug resistance to 9 antibiotics. From cultrued fish, the isolated bacteria were Photobacterium group (26 strains) and Acinetobacter group (18 strains) of Gram-negative, and unidentified marine sediment bacterium (6 strains) of Gram-positive. From wild fish, Photobacterium group (18 strains), Acinetobacter group (12 strains) and Shewanella group (5 strains) of Gram-negative and Bacillus group (8 strains), Staphylococcus group (4 strains), and unidentified marine sediment bacterium (3 strains) of Gram-positive. Intestine flora of wild black rockfish was more diverse than that of one cultured. The drugs tested were tetracyclines (oxytetracycline), aminoglycosides (gentamicin), macrorides (erythromycin) and quinolones (flumequine, oxolinic acid, norfloxacin, ofloxacin, enrofloxacin and ciprofloxacin). Sensitivity to all seven antibiotics except oxytetracycline and oxolinic acid was higher in bacteria from wild fish than from cultured ones, although wild isolates were more resistant than control strain Escherichia coli ATCC9637. This suggests that use of antibiotics in the fish farm might have some resistance in intestinal flora of wild fish.

• Journal of Food Hygiene and Safety
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• v.30 no.1
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• pp.51-58
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• 2015

Thirty one of Staphylococcus aureus isolated from perilla leaf cultivation areas in Miryang were investigated on the characteristics, such as enterotoxin genes and antibiotic susceptibility. Five toxin genes (sea, seb, sec, sed, and see) were examined by PCR method. Disc diffusion method was used to examine the antibiotic susceptibility of S. aureus by using 18 types of antibiotic discs with different concentrations. Among enterotoxin-encoding genes, sea and sed genes were co-detected from 4 isolates (12.9%), sed gene was founded in 9 isolates (29.0%), and see gene was founded in 1 isolate (3.2%). However seb and sec and tsst were not detected in any isolates. As a result of antibiotic susceptibility test, 7 isolates (22.6%) were resistant to 12 antibiotics (penicillin, ampicillin, oxacillin, amoxicillin-clavulanic acid, cefazolin, cephalothin, imipenem, gentamicin, tetracycline, ofloxacin, norfloxacin, and erythromycin). 2 isolates (6.5%) were resistant to 5 antibiotics (penicillin, ampicillin, amoxicillin-clavulanic acid, gentamycin, and telithromycin). MRSA (Methicilline Resistant Staphylococcus aureus) was founded in packing vinyl, hands, and perilla leaves.

• Journal of fish pathology
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• v.20 no.1
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• pp.49-60
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• 2007

Non-hemolytic Streptococcus parauberis isolated from diseased olive flounder, Paralichthys olivaceus in the South coast of Korea were identified by physiological, biochemical and genetic analysis in order to define the different characteristics geographically. First, twelve strains of S. parauberis were isolated from catalase-negative gram-positive cocci by multiplex PCR assay. Phenotypic identifications were performed with commercially available kit (API 20 Strep and API ZYM system). Analysis of API profiles of the isolates showed that strains were identified as either of Lactococcus lactis, S. constellatus or S. uberis. Moreover, S. parauberis isolated from olive flounder differed from that of turbot (X89967) to the test of not Voges-Proskauer, arginine, hippurate, alkiline phosphatase and pyrroidonyl arylamidase but β-glucuronidase. All S. parauberis isolates were sensitive to florfenicol, ampicillin, ofloxacin and vancomycin but were resistant to oxolinic acid, flumequine, nalidixic acid and sulfisoxazol. However, the 16S rDNA sequences of the isolates showed 99% similarity to S. parauberis KCTC 3651 (AY584477) and a great homogenecity among the flounder isolates.

• Korean Journal of Microbiology
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• v.30 no.5
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• pp.360-365
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• 1992

Clinical isolates of 8 ofloxacin resistant Staphylococcus auresu (ORSA) were subjected to MIC test, Southern analysis on gyrA locus and nucleotide sequence analysis of 290 bp of gyrA gene (gyrA-290) spanning amino acid 26 to 121 in order to understand the mechanism of quinolone resistance in Staphylococcus aureus. ORSAs showed highlevel resistance against quinolones (8-250 fold increase of MICs) and also significant resistance agianst ${\beta}-lactams$ (2-32 fold increase of MICs). However, ORSs did not show any change in sensitivity agianst vancomycin. Southern analysis of ORSAs with HindIII, PstI and AluI revealed RFLPs on gyrA locus. In order to further analyze the gyrA gene, gyrA-290 was amplified by PCR and cloned to pTZ vector. Subsequent nucleic acid sequence analysis of gyrA-290 demonstrated a point mutation of C to T resulting amino acid change of Ser-84 to Leu-84 in all 8 ORSA strains. The substitution at 84th amino acid of tyrase A might confer one mechanism of high level quinolone resistance in Staphylococcus aureus.

• 한국생물공학회:학술대회논문집
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• 2001.11a
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• pp.662-665
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• 2001

Enantioselective production of levofloxacin from ofloxacin butyl ester by porcine liver esterase was enhanced with the addition of ${\alpha}$-cyclodextrin(${\alpha}-CD$) and pH change. The conversion yield was increased from 27 to 64% and 100% with 150 mM substrate when the molar ratio of ${\alpha}-CD$ to substrate was 1 and 2, respectively. When 100 mM of substrate was added with the same molar ratio of ${\alpha}-CD$ at pH 5.6, the solubility was increased 3.8 times and the conversion yield was increased 4.4 times.