• Journal of Microbiology
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• 제45권2호
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• pp.168-170
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• 2007

In this research 26 Shigella isolates were examined by PCR and direct nucleotide sequencing for genetic alterations in the quinolone-resistance determining regions (QRDRs). We tested for the presence of qnr genes by PCR in 91 strains, but no qnr genes were found. The results did show, however, some novel mutations at codon 83 of gyrA ($Ser{\rightarrow}Ile$) and codon 64 of parC ($Ala64{\rightarrow}Cys,\;Ala64{\rightarrow}Asp$), which were related to fluroquinolone resistance.

• 약학회지
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• 제39권4호
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• pp.351-359
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• 1995

The in vitro and in vivo antibacterial activities of DWQ-217 (1-cyclopropyl-6-fluoro-8-chloro-7-(3-amino-4-methylthiomethylpyrrolidinyl )-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid) were compared with those of ciprofloxacin (CPFX) and vancomycin(VCM). DWQ-217 was superior to those of CPFX and VCM against gram positive bacteria. DWQ-217 showed excellent activity against MRSA (MIC of methicillin; $\geq$12.5 $\mu\textrm{g}$/ml), MIC$_{90}$=0.013. DWQ-217 possessed strong bactericidal action against gram positive and gram negative strains by MIC/MBC test and killing curve. DWQ-217 and CPFX were administered orally and subcutaneously to mice infected systematically with S. aureus and S. pyogenes, DWQ-217 was $\geq$5-16 fold(p.o.) and $\geq$3-5 fold(s.c.) more active than CPFX.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 춘계학술대회
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• pp.12-12
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• 1997

CFC-222 is a novel fluoroqinolone antibacterial agent synthesized and under development by the Cheil Jedang Corporation, Korea. CFC-222 exerts the antibacterial activity by inhibition of bacterial DNA gyrase leading to bactericidal action. In in vitro and in vivo preclinical testing, CFC-222 has been shown to possess a broad spectrum of antibacterial activity. In particular CFC-222 is very potent against Gram-positive bacteria such as Staphylococcus spp., Streptocuccus spp. (in particular penicillin G-resistant and -susceptible S. pneumoniae) and Enterococcus spp. when compared to other quinolones (ciprofloxacin, ofloxacin or lomefloxacin). CFC-222 also showed potent activity against the methicillin resistant clinical isolates of S. aureus (MRSA). Against Gram-negative bacteria (E. coli, Pseudomonas and Sarcina) the activity of CFC-222 was slightly weaker than that of ciprofloxacin, but was more potent than that of ofloxacin or lomefloxacin. In urinary systemic infections caused by both Gram-positive and -negative bacteria, CFC-222 demonstrated a potent therapeutic efficacy in particular against Cram-positive bacteria S. aureus, S. pyrogen 203 and S. pneumonia TypeIII.

• Journal of Microbiology and Biotechnology
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• 제30권8호
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• pp.1180-1183
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• 2020

The prevalence and characterization of plasmid-mediated quinolone resistance (PMQR) determinants in ciprofloxacin-resistant Escherichia coli isolated from a Korean commercial layer farm were studied. A total of 45 ciprofloxacin-resistant E. coli isolates were recovered and all isolates were multidrug-resistant. Eight isolates have the PMQR genes aac(6')-Ib-cr, qnrS1, and qnrB4, and seven isolates exhibited double amino acid exchange at both gyrA and parC, and have high fluoroquinolone minimum inhibitory concentrations. Five transconjugants demonstrated transferability of PMQR and β-lactamase genes and similar antimicrobial resistance. Because PMQR genes in isolates from commercial layer chickens could enter the food supply and directly affect humans, control of ciprofloxacin resistance is needed.

• 약학회지
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• 제38권6호
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• pp.664-672
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• 1994

Eighteen new hybrid bivalent ligand quinolones that contain two different type of pharmacophores in a single molecule were prepared and evaluated for in viかo antibacterial activity. Hybrid bivalent ligands p-nitrobenzyloxycarbonyl quinolones were prepared by the treatment of active esters of succinyl fluoroquinolones with 1,7-disubstituted fluoroquinolone carboxylic acids in DMF. Eighteen final quinolone carboxylic acids were obtained by the reduction of compounds $25{\sim}42$ with hydrogen in the presence of 10% Pd-C. Among these derivatives, compound[56] showed the most potent antibacterial activity against a wide range of microoranisms.

• 대한의생명과학회지
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• 제10권4호
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• pp.507-514
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• 2004

The Pseudomonas aeruginosa isolated from the clinical specimens has a mutation on the QRDR (quinolone resistance determining region). There were obvious mutations in both gyrA and parC gene which are major targets of quinolone. Simultaneous mutations were found two sites or more on these genes in all of ten strains. GyrB or parE gene had only silent mutation without converted amino acids. We confirmed that P. aeruginosa from clinical specimens exhibited decreased sensitivity to fluroquiolone due to changed Thr-83→lle and Asp-87→Asn types on gyrA and altered Ser-87→Leu type on parC. This is the first finding that a new Met-93→Thr type on parC as well as mutations on gyrB or parE genes differed from existing patterns. This study showed more mutations of gyrA rather than parC, suggesting that change of Type Ⅳ topoisomerase is more serious than that of type Ⅱ (DNA gyrase).

• Natural Product Sciences
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• 제23권4호
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• pp.286-290
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• 2017

Multidrug-resistant Acinetobacter baumannii and Pseudomonas aeruginosa are highly dangerous nosocomial pathogens, cause the symptoms of skin infections, pressure sores, sepsis, blood stream and wound infections. Unfortunately, these pathogens are immune to the most common antibiotics, such as, carbapenem, aminoglycoside and fluoroquinolone. Therefore, it is imperative that new and effective antibiotics be developed. In the present study, the antimicrobial effects of Aloe vera MAP (modified Aloe polysaccharide) on Staphylococcus aureus and Bacillus subtilis, Escherichia coli and Enterobacter aerogenes, and clinical Pseudomonas aeruginosa and clinical Acinetobacter baumannii were comprehensibly investigated. Prior to the growth inhibition effect measurement and antibiotic disc diffusion assay on gram-positive and gram-negative bacteria and selected multidrug-resistant Pseudomonas aeruginosa and Acinetobacter baumannii, antimicrobial resistance screening was performed for the multidrug-resistant bacteria obtained from clinical isolates. The results for showed the Aloe vera MAP had a concentration-dependent effect on all of examined bacteria, particularly on Pseudomonas aeruginosa. Anti-inflammatory and anti-oxidant experiments were also performed dose dependently effects to confirm the beneficial physiological effects of Aloe vera MAP.

• 한국어업기술학회:학술대회논문집
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• 한국어업기술학회 2000년도 춘계수산관련학회 공동학술대회발표요지집
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• pp.457-458
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• 2000

Pefloxacine(PFX)은 기존 quinolone계 항균제의 단점을 보완한 fluoroquinolone계열의 합성 항균제로서 그람양성균과 그람음성균에 대해서도 살균효과가 뛰어날 뿐 아니라 내성균 출현 가능성이 비교적 낮은 장점이 있는 항균제로 보고되고 있다. 이러한 약리학적 특성 때문에 우리 나라에서도 양식어류 세균성 질병 치료제로 최근 사용량이 증가하고 있으나 현재까지도 어류를 대상으로 한 체내잔류 PFX의 정량분석방범과 PFX의 흡수, 분포, 해설 등 실제 약제 사용방법 설정에 필수적인 임상동태에 관해서는 연구가 되어 있지 않은 실정이다. 따라서 본 연구는 양식어류에 대한 PFX의 효과적인 사용방법을 확립하기 위하여 고속액체크로마토그라피(HPLC)를 사용하여 실험조건의 특이성 등을 검토하여 어체내 잔류 PFX의 최적 분석조건을 설정하였다. 그리고 주요 양식어류를 대상으로 PFX를 경구 투여한 후 시간경과에 따라 혈액을 채취하여 혈종에서의 약물동태학적 Parameter를 조사하였다. (중략)

• 약학회지
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• 제42권6호
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• pp.639-641
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• 1998

Minimal inhibitory concentrations (MICs) of Bifidobacterium spp. strains (Bifidobacterium breve K-110, B. breve K-111 and B. infantis K-525) isolated from healthy Korean against antituberculosis agents and fluoroquinolones were determined. From the MICs it was found that Bifidobacterium breve K-110, B. breve K-111 and B. infantis K-525 were susceptible to rifampicin and fluoroquinolenes and resistant to other antituberculosis agents.

• 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)