• Toxicological Research
• /
• 제8권2호
• /
• pp.161-170
• /
• 1992

The objectives of this sutdy were to investigate the effects of 8-fluorociprofloxacin(8-FCP) on the central nervous system (CNS) and to compare with those of ciprofloxacin(CP). The $LD_{50}$ values of intravenous 8-FCP were similar or slightly lower in rat (M;203.6mg/kg, F;186.1mg/kg)and markedly lower in mice (M;126.5mg/kg, F;163.1mg/kg), as compared to those of CP. However, no recognizable differences in the clinical signs and recovery were found between 8-FCP and CP in both species. In combination with fenbufen, the convulsive liability of 8-FCP was higher than that of CP. At an intravenous dose of 10mg/kg, 8-FCP provoked convulsive signs and subsequent death in mice, whereas CP produced convulsion at a dose of 40mg/kg. The hexobabital -induced sleeping time was markedly lengthened by the oral administration of 8-FCP, but slightly increased by CP. In addition, the two quinolone derivatives had analgesic effects. The analgesic activity of 8-FCP was approximately two times higher than that at CP. However, both 8-FCP and CP had little effects of pentylenetetrazole-or strychnine-induced convulsion and muscle relaxation. Our finding that 8-FCP had more remarkable CNS effects than CP strongly suggests that there should be differences in the pharmacokinetic characteristics and/or in the binding affinity for specific biologic targets, or receptors, in the CNS.

• 대한수의학회지
• /
• 제37권1호
• /
• pp.147-154
• /
• 1997

국내에서 많이 사용되고 있는 제2세대 quinolone 항생제인 norfloxacin(NFX)에 대한 약역학적인 특성을 구명하기 위하여 국내에서 분리된 동물유래 병원성 세균에 대하여 시험관내에서 실험을 수행하여 다음과 같은 결과를 얻었다. 즉, E coli(n=89) 대한 NFX의 $MIC_{50}$와 $MIC_{90}$는 공히 0.02g/ml이었으며, Streptococcus spp.(n=36)에 대한 NFX의 $MIC_{50}$는 2g/ml 그리고 $MIC_{90}$는 4g/ml로 나타났다. Salmonella spp.(n=56)에 대한 NFX의 $MIC_{50}$와 $MIC_{90}$ 모두 0.2g/ml로 강한 항균력을 보였으며, Streptococcus spp.(n=24)에 대한 NFX의 $MIC_{50}$는 2g/ml 그리고 $MIC_{90}$가 4g/ml로 나타났다. Bacillus spp.(n=34)는 NFX의 $MIC_{50}$와 $MIC_{90}$는 모두 0.4g/ml으로서 대부분의 병원성 세균에 대해서 $MIC_{50}$와 $MIC_{90}$치가 동일하든지 또는 매우 비슷한 수치를 보여주었다. 그러나 NFX는 혐기성세균인 Clostridium spp.(n=34)에 대해서는 항균력이 매우 낮았다. 현재 수의임상에서 항균제 병용요법이 많이 응용되고 있는 것을 고려하여 NFX와 다른 항생물질간의 분획억제농도 (FICs)를 E coli 88ac을 시험균주로 하여 실험한 결과, NFX와 colistin과 병용할 때 FIC 값이 0.38로서 상승작용을 그리고 gentamicin, trimethoprim, amikacin, penicillin 및 tylosin과의 병용시 FIC 값이 각각 0.52, 0.56, 0.63, 1.00 및 1.02로서 상가작용을 보여주었으며, tetracyclin과의 병용시의 FIC값은 1.49로서 길항작용을 나타냄을 알 수 있었다. 한편 실제 항균제의 임상적용시 매우 주요한 요소인 항균활성후 저농도유효성(PAE)을 알아보기 위하여 E coli AB1157을 시험균주로 측정한 결과 PAE은 0.90~1.02 시간 그리고 S aureus R-209에 대해서는 PAE가 1.58~1.99 시간으로서 그람음성균 및 그람양성균 모두에 대해서 긴 PAE를 갖고 있음을 알 수 있었다.

• 대한한의학회지
• /
• 제26권1호
• /
• pp.195-205
• /
• 2005

Objective & Methods: To evaluate the in vitro synergic effect of Eunkyo-san, a traditional poly-herbal formula used in the treatment of respiratory diseases in oriental medicine with quinolone antibiotics, represented by ciprofloxacin (CPFX), which was used in the minimal concentration (MIC), $MIC_{50}$ and $MIC_{90}$. of single use of quinolones in concomitant treatment with Eunkyo-san against 9 strain$ of gram positive bacteria. Results: In. the case of aerobic gram positive bacteria, the MIC, $MIC_{50}$ and $MIC_{90}$ against Staphylococcus aureus, Staphylococcus aureus smith, Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae Type I, Type II and Type III were significantly decreased in concomitant treated groups with Eunkyo-san compared to those of single treated groups of CPFX, respectively. However, no significant changes were demonstrated against Bacillus subtilis and Enterococcus faecalis. Conclusion: The in vitro antibacterial activity of CPFX were increased against some strains of gram positive strains, especially, pneumococcus such as Staphylococcus and Streptococcus, by concomitant use of Eunkyo-san.

• 약학회지
• /
• 제37권2호
• /
• pp.136-142
• /
• 1993

To a suspension of 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-{3,7-diazabicyclo[3.3.0]oct-1(5)-en-3-yl}-4-oxo-3-quinoline carboxylic acid(C1) in sodium hydroxide solution and water is added dropwise with stirring carbon disulfide. [6R-[6$\alpha$, 7$\beta$(Z)]]-7-[[[2-Amino-4-thiazoly)methoxyimino]-acetyl]amino]-3-[[[[7-( 3-carboxy-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-7-guinolonyl)-3,7-diazabicyclo[3.3.0]oct-1(5)-en-3-yl]thioxomethyl]thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-2-carboxylic acid (DACD) was synthesized from 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-[7-(mercapto) thioxomethyl-[3,7-dia zabicyclo[3.3.0]oct-1(5)-en-3-yl}]-4-oxo-3-quinoline carboxylic acid disodium salt(C2) and cefotaxime. The invitro activity of novel dual-action cephalosporin, DACD, was compared with the in vitro activities of CENO(cefotaxime 3'-norfloxacin dithiocarbamate), cefotaxime, and norfloxacin against a variety of bacterial species. In vitro activity of DACD was superior to that of norfloxacin against Streptococcus pyogenes. Against Gram-positive and Gram-negative bacteria, its activity was almost equal to that of CENO.

• 한국동물위생학회지
• /
• 제31권1호
• /
• pp.17-29
• /
• 2008

In this study, antimicrobial resistance of E coli isolated from domestic beef on sale in Busan and Gyeongnam province was investigated from March to October 2007. A total of 600 beef samples were collected for the monitoring of antimicrobial resistance, and 92 (15.3%) strains of E coli were isolated. Antimicrobial resistance test was carried out by agar disc diffusion method with 17 antimicrobials. In general, E coli isolates showed the highest antimicrobial resistance to doxycycline (73.9%), followed by tetracycline (70.7%) andcefazolin (63.0%). Then they showed higher resistance to several antimicrobials like norfloxacin (48.9%). However, They had low antimicrobial resistance to amikacin (4.3%), colistin (1.1%). Of 92 isolates, 82 (89.1%) were resistant to more than 2 antimicrobials. Among 17 antimicrobials examined, tetracyclines were the most resistant, followed by cephalosporins, quinolone. The resistance was seemed to be correlated to amounts of antimicrobial use. In the result of this study, we suggest that there be need to regulate the abuse of antimicrobial on food-producing animals in Korea because the concern on antimicrobial resistant is gradually increased worldwide.

• Archives of Pharmacal Research
• /
• 제19권1호
• /
• pp.52-59
• /
• 1996

The in vitro activity of LB20304 was evaluated against clinical isolates and compared with those of Q-35, ciprofloxacin, sparfloxacin, lomefloxacin and ofloxacin. LB20304 demonstrated 16-to 64-fold more potent activity than ciprofloxacin against gram-positive bacteria. LB20304 inhibited 90% of the isolates of methicillin-susceptible Staphylococcus aureus(MSSA) at a concentration of $0.016\mug/ml\; (MIC_{90}). MIC_{90}$ values of LB20304 against methicillin-resistant Staphylococcus aureus (MRSA), methicillin-susceptible Staphylococcus epidermidis (MSSE), methicillin-resistant S. epidermidis (MRSE) and Streptococcus pneumoniae were $2\mug/ml,\; 0.016\mug/ml,\; 0.5\mug/ml \;and\; 0.031\mug/ml,$ respectively. LB20304 was also very active against gram-negative bacteria. Against Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, Pseudomonas aeruginosa and Acinetobacter calcoaceticus, $MIC_{90}s of\; LB20304 were\; 0.031\mug/ml,\; 0.25\mug/ml,\; 2\mug/ml,\; 8\mug/ml\; and\; 0.5\mug/ml$, respectively. Its activity was comparable to that of ciprofloxacin but much better than those of Q-35, sparfloxacin, ofloxacin and lomefloxacin. LB20304 also exhibited the most potent acitvity among quinolones tested against laboratory standard strains, ofloxacin-resistant strains, .betha.-lactamase-producing strains and anaerobic strains. The inhibitory effect$ (IC_{50)$ of LB20304 on DNA gyrase from Micrococcus luteus, determined by the supercoiling assay, was 8-fold more potent than that of ciprofloxacin. LB20304 did not induce topoisomerase-associated DNA cleavage even at a concentration of 10 mg/ml, although ciprofloxacin induced DNA cleavage at a concentration of 1 mg/ml.

• 약학회지
• /
• 제43권6호
• /
• pp.716-728
• /
• 1999

Whole oil and ketonic fraction (KF) of Leptospermum scoparium have been tested for their antimicrobial activity and combination effect with several antibiotics against various bacterial strains and fungi by using microbiological assay methods. Antibacterial activities of KF against a number of test strains were 2-3 fold stronger than those of whole oil. MICs of the KF were $65~125{\;}{\mu\textrm{g}}/ml$ against seven gram positive bacterial strains, $65~250{\;}{\mu\textrm{g}}/ml$ against 19 methicillin resistance Staphylococcus aureus strains, and $65~50{\;}{\mu\textrm{g}}/ml$ against 14 quinolone resistance strains. However, KF showed little or no activity against gram negative bacteria. MICs of the KF were $16~250{\;}{\mu\textrm{g}}/ml$ against more than 50% of the anaerobic bacterial strains tested. KF showed the higher antibacterial activity than bacitracin against 10 strains of Bacteroids thetaiotaomicron, or three strains of Bacteroides ovatus, and the more active than ciprofloxacin against one strain of Bacteroides thetaiotaomicron and three strains of Bacteroids ovatus. The MICs of KF was 63 and $250{\;}{\mu\textrm{g}}/ml$ against Aspergillus niger and Candida albicans, respectively. Antibacterial activities of KF in combination with 19 antibiotics against 14 strains and with four antifungal agents against one fungal strain were determined by paper strip diffusion method. While most of combination showed additivity, KF showed synergism with bacitracin, exfadroxil, cephradin, and meropenem for 29~57% of the strains tested. However, ofloxacin, enoxacin, sparfloxacin showed antagonism with KF for 43~71% of the strains. KF alone and in combination with bacitracin, gentamycin, neomycin, itraconazole, fluconazole, terfinafine and ketoconazole against five bacterial strains or one fungus strain synergistic effect was demonstrated against 33% of strains examined with FIC index value below 0.5 by checkerboard study. Synergistic effect of KF with gentamicin against Staphylococcus epidermidis 329 (QRS) was found by time-kill study.

• Childhood Kidney Diseases
• /
• 제23권1호
• /
• pp.22-28
• /
• 2019

Purpose: We studied the pathogens and trends in antibiotic sensitivity pattern in children with urinary tract infection (UTI) over 8 years in order to evaluate adequate treatment. Methods: We performed a retrospective review of medical records of children with UTI from January 2009 to December 2016 in Daegu Fatima Hospital. Uropathogens and antibiotic sensitivity patterns were selected. Only 1 bacterial species with a colony count of ${\geq}105CFU/mL$ was considered a positive result. We compared 2 periods group (A: 2009~2012, B: 2013~2016) to investigate trends of antibiotic sensitivity pattern. Results: During the 8 year period, 589 cases are identified (E. coli was cultured in 509 cases, 86.4%). Among all patients, this study investigated the antibiotic sensitivity of E. coli. Antimicrobial susceptibility to ampicillin was steadily low for both periods (A: 32.6%, B: 40.1%, P=0.125), and to amikacin was consistently high for both periods (A: 99.4%, B: 99.3%, P=1.000). Antibiotic sensitivity to third-generation cephalosporin decreased from period A to B (A: 91.7%, B: 75.5%, P=0.000). Antibiotic sensitivity to quinolone significantly decreased from A to B (A: 88.4%, B: 78.2%, P=0.003). The prevalence of extended-spectrum ${\beta}$-lactamase-producing E. coli increased from period A to B (A: 6.1%, B: 17.1%, P=0.000). Conclusion: This study showed that conventional antibiotic therapy for the treatment of pediatric UTI needs to be reevaluated. A careful choice of antibiotic is required due to the change in antibiotic sensitivity and the emergence of antibiotic-resistant bacteria.

• Infection and chemotherapy
• /
• 제50권4호
• /
• pp.357-361
• /
• 2018

While carbapenems are the drug of choice to treat extended-spectrum-${\beta}$-lactamase (ESBL)-producing strains, some alternative carbapenem-sparing regimens are suggested for antibiotic stewardship. We experienced a case of ciprofloxacin treatment failure for acute pyelonephritis caused by an apparently susceptible Escherichia coli. A 71-year-old woman presented the emergency department with fever for 7 days and bilateral flank pain for 2 days. The laboratory results and abdominopelvic computed tomography finding were compatible with acute pyelonephritis. During 3-day ciprofloxacin therapy, the patient remained febrile with persistent bacteremia. After the change in antibiotics to ertapenem, the patient's clinical course started to improve. ESBL-producing E. coli isolates were identified in all three consecutive blood samples. Pulsed-field gel electrophoresis (PFGE) patterns, serotypes, and sequence types showed the three isolates were derived from the identical strain. The isolates produced CTX-M-14 type ESBL belonging to the ST69 clonal group. Despite in vitro susceptibility, the failure was attributed to a gyrA point mutation encoding Ser83Leu within quinolone resistance-determining regions. This case suggests that ciprofloxacin should be used cautiously in the treatment of serious infections caused by ciprofloxacin-susceptible, ESBL-producing E. coli, even in acute pyelonephritis because in-vitro susceptibility tests could fail to detect certain genetic mutations.

• The Plant Pathology Journal
• /
• 제38권5호
• /
• pp.482-489
• /
• 2022

Fire blight caused by Erwinia amylovora (Ea) is a devastating disease in apple and pear trees. Oxolinic acid (OA), a quinolone family antibiotic that inhibits DNA gyrase, has been employed to control fire blight in South Korea since 2015. The continuous use of this bactericide has resulted in the emergence of OA-resistant strains in bacterial pathogens in other countries. To investigate the occurrence of OA-resistant Ea strains in South Korea, we collected a total of 516 Ea isolates from diseased apple and pear trees in 2020-2021 and assessed their sensitivities to OA. We found that all isolates were susceptible to OA. To explore the possibility of emerging OA-resistant Ea by continuous application of OA, we exposed Ea stains to a range of OA concentrations and constructed OA-resistant mutant strains. Resistance was associated with mutations in the GyrA at codons 81 and 83, which result in glycine to cysteine and serine to arginine amino acid substitutions, respectively. The in vitro growth of the mutants in nutrient media and their virulence in immature apple fruits were lower than those of wild-type. Our results suggest that OA-resistance decreases the fitness of Ea. Future work should clarify the mechanisms by which OA-resistance decreases virulence of this plant pathogen. Continuous monitoring of OA-resistance in Ea is required to maintain the efficacy of this potent bactericide.