• 한국어병학회지
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• 제34권1호
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• pp.39-46
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• 2021

Tetracycline (TC)은 국내에서 세균 감염 치료에 반드시 필요한 대표적인 항생제로 알려져 있다. 그러나 부적절한 사용과 남용으로 인해 Tetracycline, Erythromycin, Fluoroquinolone 등과 같은 항생제에 대한 내성이 발생하고 있으며, 이는 국내 양식 분야에서 심각한 경제적 피해를 유발한다. 본 연구에서는 2015~2018년에 걸쳐 경기도 양식장의 양식생물에서 101개 균주를 분리하였다. 분리균주는 간이적인 생화학적 방법을 통해 동정하였으며, 최소 억제농도(MIC)의 확인을 통해 Oxytetracycline (OTC), Ampicillin (AMP), Clindamycin (CLI), Enrofloxacin (ENRO), Gentamycin (GEN)에 대한 내성 여부를 확인하였다. 이중 TC에 내성을 보이는 균주는 PCR법을 통해 tet 유전자의 분포를 조사하였다. 그 결과, 총 101개 균주 중에서 Aeromonas spp.가 44개(43.5%)로 가장 우점하였고, 그 다음으로 Pseudomonas spp. 4개(4.0%), Vibrio spp. 5개(5.0%)가 확인되었다. 또한, 다중 내성을 보이는 균주(77.2%)가 단일 내성균(22.8%)보다 많음을 확인하였다. tet(A), tet(D), tet(E), tet(G), tet(M), tet(S)가 TC 내성 균주에서 검출되었으며 tet(A)가 가장 우점적으로 확인되었다. Aeromonas spp.는 분리된 균주 중에서 가장 많았으며, 경기도 내 양식현장에서의 다양한 항생제 내성 유전자의 특성에 대한 추가적인 연구가 필요하다.

• 약학회지
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• 제52권3호
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• pp.219-224
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• 2008

Clinically isolated methicillin-resistant Staphylococcus aureus strains were exposed to subinhibitory concentration of DW286, DW-224a, gemifloxacin, trovafloxacin, sparfloxacin and ciprofloxacin during 26- to 39-days period. Subculturing led to resistance development, and most of the selected mutants were above susceptible breakpoints. Selected mutants had broad cross resistance to other quinolone antibiotics and only one mutant was completely susceptible to all fluoroquinolones. Twenty five among 42 mutants revealed mutations on DNA gyrase and topoisomerase IV by sequencing. Also 16 mutants had fluoroquinolones MICs that were 4-32 times lower in the presence of reserpine. In conclusion, alterations in DNA gyrase or topoisomerase IV and action of efflux pumping out system are the resistance mechanisms of DW-224a.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2002년도 Molecular and Cellular Response to Toxic Substances
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• pp.193-193
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• 2002

The subacute toxicities and toxicokinetics of a new fluoroquinolone antibiotics, DW-224a, were evaluated after single (at the 1st day) and 4-week (at the 28th day) oral administration of the drug, in doses of 0 (to serve as a control), 10, 30 and 90 mg/kg/day, to male and female dogs (n = 3 for male and female dogs for each dose).(omitted)

• 한국독성학회:학술대회논문집
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• 한국독성학회 2003년도 추계학술대회
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• pp.170-170
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• 2003

DW -224a is a fluoroquinolone antibiotics with a broad spectrum of activity against Gram-positive and Gram-negative bacteria. In order to clarify toxicokinetic profile of DW-224a, a 4-week repeated dose oral toxicokinetic study (dose level: 0, 63, 250, 1000 mg/kg) was conducted in groups of Sprague-Dawley rats.(omitted)

• 한국수산과학회지
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• 제39권2호
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• pp.66-71
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• 2006

Fluoroquinoles have a wide range of antimicrobial properties and are effective in the treatment of bacterial diseases in fish. The use of fluoroquinoles continues to grow steadily. Fluoroquinolone antibiotics are probably the most important class used among synthetic antibiotics in human and veterinary medicines because of their broad activity spectrum and good oral absorption. This study was conducted to estimate the residue of antibiotics in four species of farmed fishes, including olive flounder (Paralichthys olivaceus), black rock fish (Sebastes schlegeli), red sea bream (Pagrus major), and sea bass (Lateolabrax japonicus), collected from fish farms located in the southern coastal area of Korea. The residues of fluoroquinolones were determined using high performance liquid chromatography (HPLC) with a fluorescence detector. Residuals of five fluoroquinolones in muscle tissue of farmed fish were analyzed. We found that enrofloxacin was the most common agent in fish muscle, and that ciprofloxacin was the next most common. The range of detected concentrations of fluoroquinolones in olive flounder muscle was 0-0.859 mg/kg in 32.6% of all samples. Enrofloxacin was commonly detected in sea bass muscle at a range of 0-0.143 mg/kg in 38.9% of all samples. Fluoroquinolones were detected in 6.9% of black rock fish muscle and in 16.6% of sea bream, although the detected concentration was below 0.01 mg/kg. The maximum detection value of enrofloxacin and ofloxacin in olive flounder at the time of shipping was 0.102 mg/kg and 0.09 mg/kg, respectively; no other antimicrobials were detected. We detected no antimicrobial substances in red sea bream.

• 대한화학회지
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• 제54권6호
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• pp.744-748
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• 2010

Fluoroquinolone 항생제의 중요한 중간체인 2,3,4,5-tetrafluorobenzoic acid를 tetrachloride phthalic anhydride에서 출발 하여 imidation, fluorination, hydrolysis과 decarboxylation단계를 거쳐서 합성하였다. Imdation 단계에서는 상전이 촉매를 이용하여 98.2%의 수율로 합성하였으며, fluorination 단계에서는 81.3%, 가수분해 단계에서는 88.6%, 마지막으로 decarboxylation단계에서는 81.6%의 수율로 합성하였다.

• Journal of Microbiology and Biotechnology
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• 제26권9호
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• pp.1551-1556
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• 2016

Broiler meat production worldwide has been plagued by lethal food-poisoning bacteria diseases, including listeriosis. A fatality rate of 15.6% was recorded in human beings in the EU in 2015. During 2013, a total of 200 poultry farm samples, including litter, chicken breast, farm feed, and drinking water, were collected to generate baseline data for the characterization of the genus Listeria in broiler poultry farms. Listeria spp. were detected in a total of 95 (47.5%) poultry farm samples. The isolates of Listeria spp. included L. innocua (28.5%), L. ivanovii (12.5%), L. welshimeri (4.5%), and L. monocytogenes and L. seeligeri (1% each). Listeria spp. contamination rates were higher in farm feed (70%), followed by litter (52.5%), chicken breasts (42.2%), and drinking water (10%). Almost all Listeria spp. isolates were resistant to more than three classes of antibiotics (multidrug resistant). Besides this, we observed a significant resistance level to penicillin and fluoroquinolone drugs. However, lower resistance levels were recorded for broad-spectrum cephalosporins. The inlA, inlC, and inlJ virulence genes were detected in almost all of the L. monocytogenes isolates. Thus, food safety management approaches and interventions at all stages of the broiler rearing cycle were needed to control cross-contamination and the zoonotic potential of listeriosis.

• Genomics & Informatics
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• 제16권3호
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• pp.44-51
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• 2018

Fluoroquinolone (FQ) antibiotics are an important class of synthetic antibacterial agents. These are the most extensively used drugs for treating bacterial infections in the field of both human and veterinary medicine. Herein, the antibacterial and pharmacological properties of four fluoroquinolones: lomefloxacin, norfloxacin, ciprofloxacin, and ofloxacin have been studied. The objective of this study was to analyze the antibacterial characteristics of the different fluoroquinolones. Also, the pharmacological properties of the compounds including the Lipinski rule of five, absorption, distribution, metabolism, and excretion, LD50, drug likeliness, and toxicity were evaluated. We found that among all four FQ molecules, ofloxacin showed the highest antibacterial activity through in silico assays with a strong interaction (-38.52 kJ/mol) with the antibacterial target protein (topoisomerase-II DNA gyrase enzyme). The pharmacological and pharmacokinetic analysis also showed that the compounds ciprofloxacin, ofloxacin, lomefloxacin and norfloxacin have good pharmacological properties. Notably, ofloxacin was found to possess an IGC50 (concentration needed to inhibit 50% growth) value of $0.286{\mu}g/L$ against the Tetrahymena pyriformis protozoa. It also tested negative for the Ames toxicity test, showing its non-carcinogenic character.

• Journal of Veterinary Science
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• 제23권2호
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• pp.23.1-23.15
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• 2022

Background: Antibacterial agents play important roles in the treatment of bacterial infections. However, the development of antimicrobial resistance (AMR) and carry-over of substances into the environment are several problems arising during oral treatment of bacterial infections. We assessed AMR development in commensal Escherichia coli (E. coli) in enrofloxacin treated and untreated animals. In addition, we examined fluoroquinolone in the plasma and urine of treated and untreated animals, and in sedimentation dust and aerosol. Methods: In each trial, six pigs were treated with enrofloxacin via powder, granulate or pellet forms in two time periods (days 1-5 and 22-26). Four pigs served as untreated controls. The minimum inhibitory concentration (MIC) was determined to evaluate AMR development. Analysis of enro- and ciprofloxacin was performed with high performance liquid chromatography. Results: Non-wildtype E. coli (MIC > 0.125 ㎍/mL) was detected in the pellet treated group after the first treatment period, whereas in the other groups, non-wildtype isolates were found after the second treatment period. E. coli with MIC > 4 ㎍/mL was found in only the pellet trial. Untreated animals showed similar susceptibility shifts several days later. Bioavailability differed among the treatment forms (granulate > pellet > powder). Enro- and ciprofloxacin were detected in aerosols and sedimentation dust (granulate, powder > pellet). Conclusions: This study indicates that the kind of the oral dosage form of antibiotics affects environmental contamination and AMR development in commensal E. coli in treated and untreated pigs.

• Tuberculosis and Respiratory Diseases
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• 제38권4호
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• pp.372-378
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• 1991

Some kinds of newer fluoroquinolone antibiotics are known to interact with theophylline, which is widely used as a potent bronchodilator in asthma or chronic obstructive lung disease. To evaluate the effect of enoxacin and ciprofloxacin on the metabolism of theophylline, aminophylline was administered intravenously in bolus (6 mg/kg) over 30 minutes to 6 healthy volunteers (age: $23.3{\pm}4.2$ year, body weight: $63.2{\pm}9.0\;kg$, height: $169.0{\pm}6.5\;cm$, female 3, male 3) before and after per oral 5-day medication of enoxacin and ciprofloxacin, respectively and we measured the level of theophylline in serum. The results were as follows: 1) Enoxacin and ciprofloxacin did not influence the volume of distribution significantly. 2) Enoxacin decreased the clearance of theophylline significantly (from $42.9{\pm}14.6\;ml/min$ to $30.1{\pm}6.3\;ml/min$: p<0.05), but ciprofloxacin did not cause significant decrease (to $32.8{\pm}6.2\;ml/min$: p>0.005). 3) Enoxacin increased the elimination half life of theophylline significantly (from $496{\pm}83\;min$ to $693{\pm}32\;min$: p<0.001), but ciprofloxacin did not cause significant increase (to $687{\pm}222\;min$: p>0.05). These results suggested that enoxacin influenced clearance and elimination half life significantly and thorough monitoring of the level of theophylline in patients with coadminstration of enoxacin and theophylline was necessary. In case of ciprofloxacin, the influence on the metabolism of theophylline was not statistically significant, but one exceptionally large decrease of the clearance and increase of the elimination halflife of theophylline suggested the necessity of monitoring of theophylline level during coadministration of ciprofloxacin and theophylline.