scholarly journals In Vitro and In Vivo Antibacterial Activities of DW-224a, a New Fluoronaphthyridone

2006 ◽  
Vol 50 (6) ◽  
pp. 2261-2264 ◽  
Author(s):  
Hee-Soo Park ◽  
Hyun-Joo Kim ◽  
Min-Jung Seol ◽  
Dong-Rack Choi ◽  
Eung-Chil Choi ◽  
...  
Keyword(s):  
Antibacterial Activities ◽  
The Other ◽  
Vitro Activity ◽  
Gram Negative Bacteria ◽  
In Vitro Activity ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria

ABSTRACT DW-224a showed the most potent in vitro activity among the quinolone compounds tested against clinical isolates of gram-positive bacteria. Against gram-negative bacteria, DW-224a was slightly less active than the other fluoroquinolones. The in vivo activities of DW-224a against gram-positive bacteria were more potent than those of other quinolones.

scholarly journals In Vitro and In Vivo Antibacterial Activities of DW286, a New Fluoronaphthyridone Antibiotic

2002 ◽  
Vol 46 (9) ◽  
pp. 3071-3074 ◽  
Author(s):  
Hee-Jeong Yun ◽  
Yu-Hong Min ◽  
Jung-A Lim ◽  
Jin-Wook Kang ◽  
So-Young Kim ◽  
...  
Keyword(s):  
Staphylococcus Epidermidis ◽  
Systemic Infection ◽  
Antibacterial Activities ◽  
The Other ◽  
Gram Negative Bacteria ◽  
In Vitro Activity ◽  
Gram Negative ◽  
Gram Positive Bacteria

ABSTRACT The in vitro and in vivo activities of DW286, a novel fluoronaphthyridone with potent antibacterial activity, were compared with those of ciprofloxacin, gemifloxacin, sparfloxacin, and trovafloxacin. Against gram-positive bacteria, such as Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, and Enterococcus faecalis, the in vitro activity of DW286 was stronger than that of any other reference antibiotic. Against gram-negative bacteria, the activity of DW286 was similar to those of trovafloxacin and gemifloxacin but was weaker than that of ciprofloxacin. In a mouse systemic infection caused by three S. aureus strains, including methicillin-resistant S. aureus and quinolone-resistant S. aureus (QRSA), DW286 demonstrated the most potent activity, as found in vitro. Specially, DW286 is ≥8-fold more active against QRSA than the other fluoroquinolones. And the 50% protective doses for DW286 were correspondent with the in vitro activities.

Comparative in vitro activity of A-56268 (TE-031) against gram-positive and gram-negative bacteria andChlamydia trachomatis

1987 ◽  
Vol 6 (2) ◽  
pp. 173-178 ◽  
Author(s):  
C. Benson ◽  
J. Segreti ◽  
H. Kessler ◽  
D. Mines ◽  
L. Goodman ◽  
...  
Keyword(s):  
Vitro Activity ◽  
Gram Negative Bacteria ◽  
In Vitro Activity ◽  
Gram Positive ◽  
Gram Negative

scholarly journals In vitro activity of para-guanidinoethylcalix[4]arene against susceptible and antibiotic-resistant Gram-negative and Gram-positive bacteria

2007 ◽  
Vol 60 (3) ◽  
pp. 575-581 ◽  
Author(s):  
Marion Grare ◽  
Maxime Mourer ◽  
Stéphane Fontanay ◽  
Jean-Bernard Regnouf-de-Vains ◽  
Chantal Finance ◽  
...  
Keyword(s):  
Vitro Activity ◽  
In Vitro Activity ◽  
Gram Positive ◽  
Antibiotic Resistant ◽  
Gram Negative ◽  
Gram Positive Bacteria

scholarly journals Bacterial Induction of Beta Interferon in Mice Is a Function of the Lipopolysaccharide Component

2000 ◽  
Vol 68 (3) ◽  
pp. 1600-1607 ◽  
Author(s):  
Andreas Sing ◽  
Thomas Merlin ◽  
Hans-Peter Knopf ◽  
Peter J. Nielsen ◽  
Harald Loppnow ◽  
...  
Keyword(s):  
Mouse Strains ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Necrosis Factor Alpha ◽  
Gram Negative ◽  
Protein Levels ◽  
Gram Positive Bacteria ◽  
Beta Interferon

ABSTRACT We investigated the reason for the inability of lipopolysaccharide (LPS)-resistant (Lps-defective [Lpsd ]) C57BL/10ScCr mice to produce beta interferon (IFN-β) when stimulated with bacteria. For this purpose, the IFN-β and other macrophage cytokine responses induced by LPS and several killed gram-negative and gram-positive bacteria in LPS-sensitive (Lps-normal [Lpsn ]; C57BL/10ScSn and BALB/c) and Lpsd (C57BL/10ScCr and BALB/c/l) mice in vitro and in vivo were investigated on the mRNA and protein levels. In addition, double-stranded RNA (dsRNA) was used as a nonbacterial stimulus. LPS and all gram-negative bacteria employed induced IFN-β in the Lpsn mice but not in theLpsd mice. All gram-positive bacteria tested failed to induce significant amounts of IFN-β in all four of the mouse strains used. As expected, all other cytokines tested (tumor necrosis factor alpha, interleukin 1α [IL-1α], IL-6, and IL-10) were differentially induced by gram-negative and gram-positive bacteria. Stimulation with dsRNA induced IFN-β and all other cytokines mentioned above in all mouse strains, regardless of their LPS sensitivities. The results suggest strongly that LPS is the only bacterial component capable of inducing IFN-β in significant amounts that are readily detectable under the conditions used in this study. Consequently, in mice, IFN-β is inducible only by gram-negative bacteria, but not in C57BL/10ScCr or other LPS-resistant mice.

scholarly journals Small subunits of RNA polymerase: localization, levels and implications for core enzyme composition

Microbiology ◽  
2010 ◽  
Vol 156 (12) ◽  
pp. 3532-3543 ◽  
Author(s):  
Geoff P. Doherty ◽  
Mark J. Fogg ◽  
Anthony J. Wilkinson ◽  
Peter J. Lewis
Keyword(s):  
Fluorescent Protein ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
The Core ◽  
Bacterial Rna ◽  
Green Fluorescent

Bacterial RNA polymerases (RNAPs) contain several small auxiliary subunits known to co-purify with the core α, β and β′ subunits. The ω subunit is conserved between Gram-positive and Gram-negative bacteria, while the δ subunit is conserved within, but restricted to, Gram-positive bacteria. Although various functions have been assigned to these subunits via in vitro assays, very little is known about their in vivo roles. In this work we constructed a pair of vectors to investigate the subcellular localization of the δ and ω subunits in Bacillus subtilis with respect to the core RNAP. We found these subunits to be closely associated with RNAP involved in transcribing both mRNA and rRNA operons. Quantification of these subunits revealed δ to be present at equimolar levels with RNAP and ω to be present at around half the level of core RNAP. For comparison, the localization and quantification of RNAP β′ and ω subunits in Escherichia coli was also investigated. Similar to B. subtilis, β′ and ω closely associated with the nucleoid and formed subnucleoid regions of high green fluorescent protein intensity, but, unlike ω in B. subtilis, ω levels in E. coli were close to parity with those of β′. These results indicate that δ is likely to be an integral RNAP subunit in Gram-positives, whereas ω levels differ substantially between Gram-positives and -negatives. The ω subunit may be required for RNAP assembly and subsequently be turned over at different rates or it may play roles in Gram-negative bacteria that are performed by other factors in Gram-positives.

scholarly journals In Vitro and In Vivo Antibacterial Activities of OPC-20011, a Novel Parenteral Broad-Spectrum 2-Oxaisocephem Antibiotic

1998 ◽  
Vol 42 (11) ◽  
pp. 2943-2949 ◽  
Author(s):  
Makoto Matsumoto ◽  
Hisashi Tamaoka ◽  
Hiroshi Ishikawa ◽  
Mikio Kikuchi
Keyword(s):  
Serum Proteins ◽  
Systemic Infection ◽  
Antibacterial Activities ◽  
Gram Negative Bacteria ◽  
Murine Models ◽  
Penicillin Binding Protein ◽  
Gram Positive ◽  
Gram Positive Bacteria

ABSTRACT OPC-20011, a new parenteral 2-oxaisocephem antibiotic, has an oxygen atom at the 2- position of the cephalosporin frame. OPC-20011 had the best antibacterial activities against gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), Enterococcus faecalis, and penicillin-resistant Streptococcus pneumoniae: MICs at which 90% of the isolates were inhibited were 6.25, 6.25, and 0.05 μg/ml, respectively. Its activity is due to a high affinity of the penicillin-binding protein 2′ in MRSA, an affinity which was approximately 1,050 times as high as that for flomoxef. Against gram-negative bacteria, OPC-20011 also showed antibacterial activities similar to those of ceftazidime. The in vivo activities of OPC-20011 were comparable to or greater than those of reference compounds in murine models of systemic infection caused by gram-positive and -negative pathogens. OPC-20011 was up to 10 times as effective as vancomycin against MRSA infections in mice. This better in vivo efficacy is probably due to the bactericidal activity of OPC-20011, while vancomycin showed bacteriostatic activity against MRSA. OPC-20011 produced a significant decrease of viable counts in lung tissue at a dose of 2.5 mg/kg of body weight, an efficacy similar to that of ampicillin at a dose of 10 to 20 mg/kg on an experimental murine model of respiratory tract infection caused by non-ampicillin-susceptibleS. pneumoniae T-0005. The better therapeutic efficacy of OPC-20011 was considered to be due to its potent antibacterial activity and low affinity for serum proteins of experimental animals (29% in mice and 6.4% in rats).

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