• Biomolecules & Therapeutics
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• 제5권2호
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• pp.187-193
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• 1997

The in vivo and in vivo antibacterial activity of DW-116, a newly synthesized fluoroquinolone, were compared with those of other quinolones. DW-116 exhibited more potent antibacterial activity than rufloxacin and lower activity than ofloxacin and ciprofloxacin in in vivo assay But, DW-116 particularly showed strong activity against the family of staphylococci including methicillin-sensitive staphylococcus and its activity was more active than that of ciprofloxacin. The time-kill curve studies showed rapid bactericidal activity for DW-116. The post-antibiotic effect of DW-116 was observed between 0.66 and 5 hours. The therapeutic efficacy of DW-116 against respiratory infection with P. aeruginosa was as strong as that of ciprofloxacin and its effect against urinary tract in(traction with E. coli was more effective than rufloxacin. The excellent therapeutic efficacy of DW-116 against these local infections is due to its good pharmacokinetic profiles.

• Journal of Microbiology and Biotechnology
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• 제20권4호
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• pp.798-802
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• 2010

Recently, a total of 74 Staphylococcus pseudintermedius isolates were collected from clinical cases of canine pyoderma and otitis externa in Korea. In this study, we examined in vitro fluoroquinolone resistance among those isolates using a standard disc diffusion technique. The results demonstrated that, except for one isolate, approximately 18.9% to 27.0% of the isolates possessed bacterial resistance to both veterinary- and human-licensed fluoroquinolones including moxifloxacin (18.9% resistance), levofloxacin (20.3% resistance), ofloxacin (24.3% resistance), ciprofloxacin (25.7% resistance), and enrofloxacin (27.0% resistance). Most surprisingly, 14 out of 74 (18.9%) isolates were resistant to all the five fluoroquinolones evaluated. Moreover, a PCR detection of the methicillin resistance gene (mecA) among the 74 isolates revealed that 13 out of 25 (52.0%) mecApositive isolates, but only 7 out of 49 (14.3%) mecA-negative isolates, were resistant to one or more fluoroquinones. Taken together, our results imply that bacterial resistance to both veterinary- and human-use fluoroquinolones becomes prevalent among the S. pseudintermedius isolates from canine pyoderma and otitis externa in Korea, as well as that the high prevalence of the mecA-positive S. pseudintermedius isolates carrying multiple fluoroquinolones resistance could be a potential public health problem.

• Biomolecules & Therapeutics
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• 제15권2호
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• pp.102-107
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• 2007

Cimetidine, a substrate for P-glycoprotein (P-gp), is a well known drug interacting with a variety of drugs and results in alteration of pharmacokinetic parameters by concomitant administration. The aim of present study was to investigate whether cimetidine affects the transport of various quinolone antibiotics in human colorectal cancer cell line (Caco-2) system which has been typically used to investigate drug transport via P-gp. The apparent permeability coefficients (P$_{app}$) value of 9 quinolone antibiotics in the co-treatment with cimetidine was examined. Apical to basolateral (AP-to-BL) transport of fleroxacin in the co-treatment with cimetidine was increased to 1.5-fold (p<0.01) compared with that of fleroxacin alone, whereas basolateral to apical (BL-to-AP) transport of fleroxacin was decreased to 0.83-fold significantly (p<0.05). Ofloxacin was decreased to 0.8-fold (p<0.01) and 0.72-fold (p<0.01) significantly in AP-to-BL and BL-to-AP direction, respectively by cimetidine cotreatment. The P$_{app}$ values of gatifloxacin, moxifloxacin, ciprofloxacin and rufloxacin also were changed by cimetidine. These results have a potential that cimetidine influences on the pharmacokinetics of quinolone antibiotics. It suggests that careful drug monitoring and dosage adjustment may be necessary during the co-administration of quinolone antibiotics with cimetidine.

• 한국동물위생학회지
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• 제32권3호
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• pp.281-286
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• 2009

Fluoroquinolones in muscle and egg were separated by liquid extraction and determined. The analysis was carried out using following conditions; C18 column ($150{\times}4.6mm$, $5{\mu}m$), mobile phase composed of D.W. (containing 0.4% triethylamine and phosphoric acid) : methanol : acetonitrile (780:100:120, v/v/v), quarternary pump at a flow rate of 0.9ml/min and $20{\mu}l$ of injection volume, fluorescence detector with EX 278nm/Em 456nm. The calibration range of seven fluoroquinolones showed linearity ($r^2{\geq}0.999$) at concentration range of $0.025{\sim}0.8{\mu}g/ml$. The recoveries in fortified muscle and egg represented more than 81.3%. The detection limits for ofloxacin, norfloxacin, ciprofloxacin, enrofloxacin, danofloxacin, saraloxacin and orbifloxacin were 3.1, 2.5, 3.6, 1.7, 0.9, 2.5 and $2.1{\mu}g/kg$, respectively. We also monitored fluoroquinolones residue in the sample (chicken muscle 182, cattle muscle 140, pig muscle 139, egg 212) using EEC-plate (E. coli ATCC 11303) screening and HPLC confirmation methods. The screening test results, fluoroquinolones, antibacterial substances were all negative.

• 약학회지
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• 제38권3호
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• pp.265-273
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• 1994

ln vitro and in vivo antibacterial activities of DWQ-013(1-cyclopropyl-6,8-difluoro-7-(3-methylthiomethylpyrrolidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid), a new fluoroquinolone antibacterial agent, were compared with those of ciprofloxacin, sparfloxacin and ofloxacin against aerobic and anaerobic standard strains and clinical isolates. DWQ-013 had a broad spectrum and potent antibacterial activity against Gram-positive and Gram-negative bacteria. The antibacterial activity of DWQ-013 against Staphylococcus aureus was equal to that of sparfloxacin(SPFX) and superior to those of ciprofloxacin(CPFX). The antibacterial activity against Gram-negative bacteria was slightly lower than those of ciprofloxacin and sparfloxacin. MIC of DWQ-013 against Pseudomonas aeruginosa$(0.781{\sim}1.563\;{\mu}g/ml)$ was usually equal to that of sparfloxacin$(0.781\;{\mu}g/ml)$ and was inferior to that of ciprofloxacin$(0.098\;{\mu}g/ml)$. The number of viable cells was decreased rapidly after addition of DWQ-013 at concentration of $1{\sim}2$ folds of MIC.

• 약학회지
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• 제41권2호
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• pp.225-232
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• 1997

The in vitro antibacterial activity of DWP20367 (1-Cyclopropyl-6-fluoro-8-chloro-7-(2,7-diazabicyclo[3,3,0]oct-4-ene-7-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid), a new broad-spectrum fluoroquinolone, was compared with those of ciprofloxacin (CPFX), sparfloxacin (SPFX) and ofloxacin (OFLX). DWP20367 was showed antibacterial activity much higher than CPFX, SPFX and OFLK against gram-positive bacteria, while it was slightly more superior to quinolones against gram-negative bacteria. DWP20367 was particularly effective against MRSA, and its $MlC_{90}$ against clinical isolates of methicillin-susceptible S. aureus, low methicillin-resistant S. aureus and high methicillin-resistant S. aureus were 0.098, 0.781 and 1.563 micro g/ml, respectively. Against S. pneumoniae, MIC90 of DWP20367 was 2- to 8-fold higher than those of CPFX. With a view of MIC90, DWP20367 showed slightly more potent activity against P. aeruginosa and E. coli isolates than the control quinolones. DWP20367 activity was not affected by inoculum size and medium pH. But addition of $Mg^{2+}, \;Ca^{2+} $Mg2+, Ca2+ or horse serum (25%) decreased its antibacterial activity. DWP20367 was showed rapidly bactericidal activity within 2 to 4 h, and regrowth was not observed even after 24 h incubation at concentrations near the 4-fold of MIC.

• 한국동물위생학회지
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• 제26권4호
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• pp.313-321
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• 2003

During the period of December 2000 to November 2001, a total of 419(10.9%) Salmonella was isolated from 3,850 slaughtered pig samples(2,732 lymph nodes and 1,118 caecal contents) in Korea. Three hundred and seventy(13.5%) and 49(4.4%) Salmonella were isolated from lymph nodes and caecal contents, respectively. In the isolation ratio of Salmonella spp originated from each class of season, summer(15.7%), autumn(11.5%), spring(10.0%) and winter(8.3%), in order. As the result of serotyping, B group(67.5%) were the most common, in order of C$_1$(14.6%), D$_1$(6.0%), C$_2$(4.1%) and E$_1$(3.3%). 32 serovars were found, the major serotypes were as follows; S typhimurium(21.7%), S schwarzengrund(16.0%), S derby(15.8%), S typhimurium variant copenhagen(9.8%), S enteritidis (6.0%) and S mbandaka(6.0%). All of the isolates were susceptible to norfloxacin and ofloxacin. The isolates were resistant in order of doxycycline(69.2%), tetracycline(68.7%), penicliin(54.9%) and streptomycin(52.5%).

• 한국어병학회지
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• 제21권3호
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• pp.229-239
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• 2008

The aim of this study was to acquire level on the occurrence of five fluoroquinolones(FQs) residue among cultured eels in Jeonbuk province. Samples were collected from the four local area(Kunsan, Gochang, Wanju and Osu) and surveyed on the distribution of FQs residual level in edible muscle using HPLC method. A total of 90 samples of eel was monitored for detection of the FQs residue. Among them, 30 eels(33.3%) were detected the FQs single or paired, respectively. The detection ratios were showed Osu(40%, 8/20), Gochang(33%, 13/44), Wanju(30%, 6/20) and Kunsan(30%, 3/10) in order, respectively. The ratio was equivalent to over 30% of overall in sampled area. The most frequently detected FQs were perfloxacin(PF) followed by enrofloxacin(EF), ciprofloxacin(CF), ofloxacin(OF) and norfloxacin(NF). Eight different combinations of FQ residual patterns were observed as single(5 type, 21%) or as paired(3type, 12,5%) respectively and frequently encountered patterns were PF(37%) and PF-EF(23%). The residual level of FQs was evaluated in the range of 1-75 ug/kg and the most prevalent levels of FQs was found in 1-25 ug/kg(35 fish, 85%) followed by 26-50 ug/kg(5 fishes, 11%) and 51-75 ug/kg(1 fishes, 3.3%). These results could be possible that the cultured eels were mostly exposed with PF, EF and CF, and might be treated with a variety of fluoroquinolones for prevention of bacterial disease.

• Journal of Microbiology and Biotechnology
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• 제18권11호
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• pp.1853-1857
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• 2008

Salmonella contamination in chicken meat was studied with 100 chicken meat samples purchased from 55 shops located in various regions. A total of 21 isolates of Salmonella enterica were isolated from 21 chicken meat samples from four shops located at open markets, whereas there were none from supermarkets with well-equipped cold systems. Among these, 18 isolates were identified as Salmonella enterica serotype Haardt (S. Haardt) and three isolates were S. enterica serotype Muenchen. When the minimal inhibitory concentrations of the S. Haardt isolates were assayed with the agar dilution method to determine susceptibility to ampicillin, chloramphenicol, sulfisoxazole, tetracycline, and nalidixic acid, all 18 isolates were resistant to tetracycline and nalidixic acid and nine of these were resistant to ampicillin. These isolates showed reduced susceptibility to eight fluoroquinolones including ciprofloxacin, enrofloxacin, levofloxacin, gatifloxacin, gemifloxacin, moxifloxacin, norfloxacin, and ofloxacin. When quinolone resistance determining regions of gyrA and gyrB were sequenced, every isolate had the same missense mutation Ser83$\rightarrow$Tyr (TCC$\rightarrow$+TAC) in gyrA, whereas no mutation was found in gyrB. Pulsed-field gel electrophoresis with XbaI revealed a close relationship among these isolates, suggesting a contamination of raw chicken meat with clonal spread of nalidixic acid-resistant and quinolone-reduced susceptibility S. Haardt in chickens. Results in this study show the importance of a well-equipped cold system and the prudent use of fluoroquinolone in chickens to prevent the occurrence of quinolone-resistant isolates.

• 약학회지
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• 제40권3호
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• pp.357-368
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• 1996

The in vitro antibacterial activity of a novel fluoroquinolone, DWP20373(1-Cyclopropyl-6-fluoro-8-methoxy-7-(2,7-diazabicyclo[3,3,0]oct-4-ene-7-yl)-1,4-dihydro-4 oxoquino line-3carboxylic acid) was compared with those of ciprofloxacin (CPFX), sparfloxacin (SPFX) and ofloxacin (OFLX). DWP20373 was more active than SPFX and OFLX but was less potent than CPFX against gram-negative bacteria. DWP20373 showed an excellent activity against L-MRSA and H-MRSA ($MlC_{90}=0.781{\sim}1.563{\mu}g/ml$).The activity of DWP20373 decreased moderately in the presence of 5mM $Mg^{2+}$. However, pH and serum had no effect on the activity of DWP20373. DWP20373 possessed a rapid bactericidal activity against gram-positive and gram-negative strains.