• Title/Summary/Keyword: cephalosporin

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Synthesis and in Vitro Antibacterial Activity of Cephalosporins with a Pyridiniume Substituent Carrying an Isoxazole Moiety at the C-3 Position

  • Park, Hae-Il;Choi, Hyun-Joo;Jang, Jin-Hee;Choi, Sung-Hak;Rhee, Jae-Keol;Chang, Min-Sun
    • Archives of Pharmacal Research
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    • v.24 no.2
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    • pp.89-94
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    • 2001
  • Several quaternary pyridinium cephalosporin analogues were prepared analogues were Prepared and evaluated in vitro for antibacterial activity against selected Gram-positive and Cram-negative organisms. Most of the synthesized analogues were either as effective or less effective against the tested bacterial organ isms than the reference com pounds, Cefpirome and Ceftazidime.

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Isolation and Resistance Patterns of E. coli from Domestic Animals and Dranage in 1987 (가축 및 하천에서 분리한 대장균의 항균제내성)

  • Chung, Kyu-Sun;Lee, Yeon-Tae;Pio, Seog-Youn
    • YAKHAK HOEJI
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    • v.33 no.2
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    • pp.73-79
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    • 1989
  • One hundred and sixteen strains of E. coli isolated from drainage in Seoul city in 1987 and 104 strains of E. coli isolated from stools of domestic animals in suburb of Seoul in 1987 were examined for susceptibilities to 10 antimicrobial agents by the agar dilution method. The susceptibilities of the two groups to each antimicrobial agent were compared and correlations in the antimicrobial susceptibility of the 220 strains of E. coli among the 10 antimicrobial agents were also analyzed. The frequency of resistance strains was highest to tetracycline with 77%, and followed by chloramphenicol, streptomycin, ampicillin, kanamycin and cephalosporin in the descreasing order, tanging from 62% to 10%. Strains resistant to tobramycin, nalidixic acid, gentamicin and amikacin occupied 3 strains, 2 strains, 2 strains and 1 strain respectively.

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Vibrio vulnificus infection: a persistent threat to public health

  • Yun, Na Ra;Kim, Dong-Min
    • The Korean journal of internal medicine
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    • v.33 no.6
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    • pp.1070-1078
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    • 2018
  • Vibrio vulnificus is a gram-negative bacterium that can cause serious, potentially fatal infections. V. vulnificus causes three distinct syndromes: an overwhelming primary septicemia caused by consuming contaminated seafood, wound infections acquired when an open wound is exposed to contaminated warm seawater, and gastrointestinal tract-limited infections. Case-fatality rates are higher than 50% for primary septicemia, and death typically occurs within 72 hours of hospitalization. Risk factors for V. vulnificus infection include chronic liver disease, alcoholism, and hematological disorders. When V. vulnificus infection is suspected, appropriate antibiotic treatment and surgical interventions should be performed immediately. Third-generation cephalosporin with doxycycline, or quinolone with or without third-generation cephalosporin, may be potential treatment options for patients with V. vulnificus infection.

Immuno-modulation effects of cefodizime, a cephalosporin, in rat dendritic cells

  • Joo, Seong-Soo;Won, Tae-Joon;Lee, Do-Ik
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.129.1-129.1
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    • 2003
  • According to recent reports, cefodizime (CEF), a third generation cephalosporin has the capability of chemotactic activity of neutrophils and monocytes and may act as the strong immuno-modulator. This study was planned to demonstrate whether CEF has the proposed effect on rat dendritic cells in vitro. Dendritic cells were taken from rat spleen tissue and cultured for a week. The obtained dendritic cells were treated with 10$\mu$g/ml, 50$\mu$g/ml, 100$\mu$g/ml cefodizime and 10IU/$m\ell$ IFN-Υ+1$\mu$g/ml LPS. (omitted)

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Distribution of Pseudomonas-Derived Cephalosporinase and Metallo-β-Lactamases in Carbapenem-Resistant Pseudomonas aeruginosa Isolates from Korea

  • Cho, Hye Hyun;Kwon, Gye Cheol;Kim, Semi;Koo, Sun Hoe
    • Journal of Microbiology and Biotechnology
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    • v.25 no.7
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    • pp.1154-1162
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    • 2015
  • The emergence of carbapenem resistance among Pseudomonas aeruginosa is an increasing problem in many parts of the world. In particular, metallo-$\beta$-lactamases (MBLs) and AmpC $\beta$lactamases are responsible for high-level resistance to carbapenem and cephalosporin. We studied the diversity and frequency of $\beta$-lactamases and characterized chromosomal AmpC $\beta$lactamase from carbapenem-resistant P. aeruginosa isolates. Sixty-one carbapenem-resistant P. aeruginosa isolates were collected from patients in a tertiary hospital in Daejeon, Korea, from January 2011 to June 2014. Minimum inhibitory concentrations (MICs) of four antimicrobial agents were determined using the agar-dilution method. Polymerase chain reaction and sequencing were used to identify the various $\beta$-lactamase genes, class 1 integrons, and chromosomally encoded and plasmid-mediated ampC genes. In addition, the epidemiological relationship was investigated by multilocus sequence typing. Among 61 carbapenem-resistant P. aeruginosa isolates, 25 isolates (41.0%) were MBL producers. Additionally, 30 isolates producing PDC (Pseudomonas-derived cephalosporinase)-2 were highly resistant to ceftazidime (MIC50 = $256{\mu}g/ml$) and cefepime (MIC50 = $256{\mu}g/ml$). Of all the PDC variants, 25 isolates harboring MBL genes showed high levels of cephalosporin and carbapenem resistance, whereas 36 isolates that did not harbor MBL genes revealed relatively low-level resistance (ceftazidime, p < 0.001; cefepime, p < 0.001; imipenem, p = 0.003; meropenem, p < 0.001). The coexistence of MBLs and AmpC $\beta$-lactamases suggests that these may be important contributing factors for cephalosporin and carbapenem resistance. Therefore, efficient detection and intervention to control drug resistance are necessary to prevent the emergence of P. aeruginosa possessing this combination of $\beta$-lactamases.

Isolation, Identification and Drug Susceptibility of Bacteria from Cow Genital Organs (한우(韓牛) 및 유우(乳牛)의 생식기내(生殖器內) 세균분리(細菌分離) 동정(同定) 및 약제감수성(藥劑感受性))

  • Kang, Byung-kyu;Park, Choon-ho
    • Korean Journal of Veterinary Research
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    • v.27 no.1
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    • pp.61-68
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    • 1987
  • This study was conducted to determine the microorganisms inhabitating in cow genitalia and their antimicrobial drug susceptibility. During the period between July, 1985 and February, 1986, a total of 111 cow genitalia, 58 from Korean native and 53 from dairy cow, were sampled at three abattoirs. Gross pathological examination and bacterial isolation and identification were performed from the genital samples. In addition antimicrobial drug susceptibility test for the microorganisms isolated, some synergistic activity among drugs were examined on the major organism isolated from the cases of endometritis and pyometra. The results are summerized as follows: 1. Among the bacteria isolated from the genitalia, Staphylococcus spp., C. pyogenes, E. coli, Proteus spp., Streptococcus spp., Bacillus spp. were most frequently isolated whereas the genera of Pasteurella, Pseudomonas, Klebsiella and Yersina were detected far less frequently. 2. In Korean native cow the genera of Straphylococcus and Steptococcus were more isolated than dairy cow while in dairy cow the genera of Corynebacterium, Proteus, Escherichia were more of ten isolated than Korean native cow. 3. From cow genital organs showing lesions of endometritis and prometra, C. pyogenes was most frequently isolated, the isolation rate being 60 percent, and follow by Staphylococcus spp., Proteus spp., E. coli and Pasteurella spp. in the order. 4. Antimicrobial drug susceptibility test conducted on the major organisms isolated showed that all the isolates were susceptible to gentamicin, cephalosporin and sulfisoxazole, but resistant to tetracycline and penicillin. 5. Twenty-nine isolates of C. pyogenes were submitted to the synergistic activity test of cephalosporin, kanamycin and streptomycin with penicillin. Synergists were demonstrated in 90 percent, 31 percent and 27 percent of isolates examined by the combined use of penicillin and cephalosporin, penicillin and kanamycin, penicillin and streptomycin, respectively. About 10 percent of the isolates were found to be indifferent by the synergism test.

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In Vitro and in Vivo Antibacterial Activities of a New Parenteral Cephalosporin, LB10522 (주사제용 세파로스포린계 항생제 LB10522의 in vitro 및 in vivo 항균력)

  • Paek, Kyung-Sook;Oh, Jeong-In;Kim, Mu-Yong;Kim, In-Chull;Kwak, Jin-Hwan
    • YAKHAK HOEJI
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    • v.40 no.1
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    • pp.95-101
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    • 1996
  • The in vitro antibacterial activities of LB10522, a new catechol-substituted cephalosporin, were compared with those of cefpirome, ceftazidime, ceftriaxone, and cefoperaz one against clinical isolates and laboratory standard anaerobes. LB10522 had broad spectrum antibacterial activities against both gram-positive and gram-negative microorganisms. It was most active against gram-positve bacteria among the reference cephalosporins tested. Against gram-negative strains such as the family Enterobacteriaceae, LB10522 showed an activity comparable to that of cefpirome. But LB10522 was more potent than ceftazidime, ceftriaxone and cefoperazone. In particular, Pseudomonas aeruginosa was highly susceptible to LB10522, which was 32-fold and 64-fold more active than ceftazidime and cefpirome, respectively. Against anaerobic strains, the activity of LB10522 was similar to those of reference compounds. LB10522 exhibited potent therapeutic activities against experimental local infections in mice. The therapeutic effect of LB10522 against urinary tract infection (UTI) caused by P. aeruginosa 1912E in mice was superior to that of cefpirome. Against experimental respiratory tract infection (RTI) caused by K. pneumoniae DT-S in mice, LB10522 was as effective as cefpirome. The in vivo efficacy of LB10522 was correlated well with its in vitro activity.

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Action Mechanism of LB10522, a New Catechol-Substituted Cephalosporin (카테콜 치환체를 가진 세파로스포린계 항생제 LB10522의 작용기전)

  • Kim, Mu-Yong;Oh, Jeong-In;Paek, Kyoung-Sook;Kim, In-Chull;Kwak, Jin-Hwan
    • YAKHAK HOEJI
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    • v.40 no.1
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    • pp.102-111
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    • 1996
  • LB10522 is a new parenteral broad spectrum cephalosporin with a catechol moiety at C-7 position of beta-lactam ring. This compound can utilize tonB-dependent iron transp ort system in addition to porin proteins to enter bacterial periplasmic space and access to penicillin-binding proteins (PBPs) which are the lethal targets of ${\beta}$-lactam antibiotics. The chelating activity of LB10522 to metal iron was measured by spectrophotometrically scanning the absorbance from 200 to 900nm. When $FeCl_3$ was added, optical density was increased between 450 and 800nm. LB10522 was more active against gram-negative strains in iron-depleted media than in iron-replete media. This is due to the increased expression of iron transport channels in iron-depleted condition. LB10522 showed a similar activity against E. coli DC2 (permeability mutant) and E. coli DCO (wild type strain) in both iron-depleted and iron-replete media, indicating a minimal permeaility barrier for LB10522 uptake. LB10522 had high affinities to PBP 3 and PBP 1A, 1B of E. coli. By blocking these proteins, LB10522 caused inhibition of cell division and the eventual death of cells. This result was correlated well with the morphological changes in E. coli exposed to LB10522. Although the in vitro MIC of LB10522 against P. aeruginosa 1912E mutant (tonB) was 8-times higher than that of the P. aeruginosa 1912E parent strain, LB10522 showed a similar in vivo protection efficacy against both strains in the mouse systemic infection model. This result suggested that tonB mutant, which requires a high level of iron for normal growth, might have a difficulty in surviving in their host with an iron-limited environment.

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