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PubMed2001

Linezolid: an oxazolidinone antimicrobial agent.

BACKGROUND: Linezolid is the first oxazolidinone anti-infective agent marketed in the United States. It is indicated for the treatment of nosocomial pneumonia, complicated skin and skin-structure infections caused by methicillin-sensitive or methicillin-resistant Staphylococcus aureus and other susceptible organisms, and vancomycin-resistant Enterococcus faecium infections. It also is indicated for the treatment of uncomplicated skin and skin-structure infections caused by methicillin-sensitive S. aureus or Streptococcus pyogenes, and community-acquired pneumonia caused by penicillin-sensitive Streptococcus pneumoniae. OBJECTIVE: This article reviews the pharmacologic properties and clinical usefulness of linezolid. METHODS: Using the terms linezolid, PNU-100766, and oxazolidinone, we performed a literature search of the following databases: MEDLINE (1966 to September 2000), HealthSTAR (1993 to September 2000), Iowa Drug Information Service (1966 to September 2000), International Pharmaceutical Abstracts (1970 to September 2000), PharmaProjects (January 2000 version), and meeting abstracts of the Infectious Diseases Society of America and the Interscience Conference on Antimicrobial Agents and Chemotherapy (1996 to 2000). RESULTS: Linezolid has a unique structure and mechanism of action, which targets protein synthesis at an exceedingly early stage. Consequently, cross-resistance with other commercially available antimicrobial agents is unlikely. It is primarily effective against gram-positive bacteria. To date, resistance to linezolid has been reported in patients infected with enterococci. The pharmacokinetic parameters of linezolid in adults are not altered by hepatic or renal function, age, or sex to an extent requiring dose adjustment. Linezolid is metabolized via morpholine ring oxidation, which is independent of the cytochrome P450 (CYP450) enzyme system; as a result, linezolid is unlikely to interact with medications that stimulate or inhibit CYP450 enzymes. Compassionate-use trials and other clinical studies involving mainly adult hospitalized patients with gram-positive infections have shown that linezolid administered intravenously or orally is effective in a variety of nosocomial and community-acquired infections, including those caused by resistant gram-positive organisms. Reported adverse effects include thrombocytopenia. diarrhea, headache, nausea, vomiting, insomnia, constipation, rash, and dizziness. Preliminary pharmacoeconomic data indicate that a significantly higher percentage of patients receiving linezolid therapy versus comparator could be discharged from the hospital by day 7 (P = 0.005). CONCLUSIONS: Linezolid appears to be effective while maintaining an acceptable tolerability profile. Due to the risk of bacterial resistance, linezolid should be reserved for the treatment of documented serious vancomycin-resistant enterococcal infections.

Acetamides↗
PubMed2004

Results of a multicenter, randomized, open-label efficacy and safety study of two doses of tigecycline for complicated skin and skin-structure infections in hospitalized patients.

BACKGROUND: Tigecycline is a broad-spectrum glycylcycline antibiotic being investigated for the treatment of serious infections in hospitalized patients. Tigecycline has been shown to be efficacious against serious infections in animals, and preliminary studies in healthy adults have shown that tigecycline has an acceptable tolerability profile. OBJECTIVE: This study compared the clinical and microbiological efficacy, pharmacokinetic properties, and tolerability of 2 doses of tigecycline in hospitalized patients with a complicated skin and skin-structure infection (cSSSI). METHODS: This Phase II, randomized, open-label study was conducted between September 1999 and March 2001 at 14 investigative centers across the United States. Patients were randomized to receive tigecycline 25 or 50 mg IV q12h for 7 to 14 days. The primary efficacy end point was the clinically observed cure rate among clinically evaluable (CE) patients at the test-of-cure visit. Secondary end points were the clinical cure rate at the end of treatment and bacteriologic response in microbiologically evaluable (ME) patients. Also, in vitro tests of susceptibility to tigecycline were performed for selected pathogens known to cause skin infections, including methicillin-resistant and methicillin-susceptible Streptococcus pyogenes, Staphylococcus aureus, Escherichia coli, Enterococcus faecalis, and Enterococcus faecium. Tolerability assessments also were conducted. RESULTS: A total of 160 patients received > or =1 dose of tigecycline; 109 patients were CE, and 91 were ME. The majority of patients (74%) were men, and the mean (SD) age was 49.0 (14.8) years. At the test-of-cure visit, the clinical cure rate in the 25-mg group was 67% (95% CI, 53.3%-79.3%) and in the 50-mg group was 74% (95% CI, 60.3%-85.0%). In the 25-mg group, 56% of the patients had eradication (95% CI, 40.0%-70.4%) of the pathogens compared with 69% (95% CI, 54.2%-82.3%) in the 50-mg group. Values for the minimum concentration of tigecycline that is inhibitory for 90% of all isolates ranged from 0.06 to 0.50 microg/mL for the selected pathogens. Both tigecycline doses were generally well tolerated. Nausea and vomiting were the most common adverse events. CONCLUSIONS: In this study, tigecycline appeared efficacious and showed a favorable pharmacokinetic profile and an acceptable safety profile in the treatment of hospitalized patients with cSSSI. In patients who received 50-mg doses of tigecycline q12h, the clinical cure rates and microbial eradication rates were 74% and 70%, respectively, and were 67% and 56% in patients who received 25-mg doses.

Adolescent↗
PubMed2003

Enterocin CRL35 inhibits late stages of HSV-1 and HSV-2 replication in vitro.

The replication of herpes simplex virus (HSV) type 1 and 2 in Vero cells is inhibited in the presence of enterocin CRL35 (ECRL), a bacteriocin produced by Enterococcus faecium CRL35. Attempts to resolve the mode of action of ECRL indicate that virus adsorption and penetration are not affected. Instead, a late step of virus multiplication is hindered since the addition of 100 microg/ml of ECRL at 8h post infection still causes a 90% inhibition of virus release. The effect of ECRL on HSV antigen expression was studied by immunofluorescence using a polyclonal serum and a monoclonal antibody against glycoprotein D (gamma protein). These studies indicated that ECRL impeded the second round of infection, apparently as a consequence of the inhibition of glycoprotein D expression. The replication of syncytial mutants of HSV-1 was significantly inhibited at a ECRL concentration of 25 microg/ml. Both the percentage of fused cells and the polykaryocyte size were affected. Studies on the effect of ECRL on viral protein synthesis showed that in the presence of ECRL, HSV late gamma proteins were not synthesized. From these findings, it is concluded that inhibition of HSV spreading by ECRL is due to the prevention of mainly late glycoprotein synthesis.

Animals↗
PubMed2003

Construction and use of a computerized DNA fingerprint database for lactic acid bacteria from silage.

Efficient selection of new silage inoculant strains from a collection of over 10,000 isolates of lactic acid bacteria (LAB) requires excellent strain discrimination. Toward that end, we constructed a GelCompar II database of DNA fingerprint patterns of ethidium bromide-stained EcoRI fragments of total LAB DNA separated by conventional agarose gel electrophoresis. We found that the total DNA patterns were strain-specific; 56/60 American Type Culture Collection strains of 33 species of LAB could be distinguished. Enterococcus faecium strains ATCC19434 and ATCC35667 had identical total DNA patterns and RiboPrints. Lactobacillus rhamnosus strains ATCC7469 and ATCC27773 also had identical total DNA patterns, but different RiboPrints. EcoRI RiboPrint patterns could distinguish only about 9/23 Lactobacillus plantarum strains and about 6/10 Lactobacillus buchneri strains, whereas all 33 strains could be distinguished by EcoRI total DNA patterns. Despite gel-to-gel variation, new DNA patterns can be readily grouped with existing patterns using GelCompar II. The database contains large homogenous clusters of L. plantarum, E. faecium, L. buchneri, Lactobacillus brevis and Pediococcus species that can be used for tentative taxonomic assignment. We routinely use the DNA fingerprint database to identify and characterize new strains, eliminate duplicate isolates and for quality control of inoculant product strains. The GelCompar II database has been in continuous use for 7 years and contains more than 3600 patterns representing approximately 700 unique patterns from over 300 gels and is the largest computerized DNA fingerprint database for LAB yet reported.

DNA Fingerprinting↗
PubMed2003

Identification and antibiotic susceptibility of bacterial isolates from probiotic products.

In the present study, a total of 55 European probiotic products were evaluated with regard to the identity and the antibiotic resistance of the bacterial isolates recovered from these products. Bacterial isolation from 30 dried food supplements and 25 dairy products, yielded a total of 268 bacterial isolates selected from several selective media. Counts of food supplements showed bacterial recovery in 19 (63%) of the dried food supplements ranging from 10(3) to 10(6) CFU/g, whereas all dairy products yielded growth in the range of 10(5)-10(9) CFU/ml. After identification of the isolates using whole-cell protein profiling, mislabeling was noted in 47% of the food supplements and 40% of the dairy products. In six food supplements, Enterococcus faecium was isolated whereas only two of those products claim this species on their label. Using the disc diffusion method, antibiotic resistance among 187 isolates was detected against kanamycin (79% of the isolates), vancomycin (65%), tetracycline (26%), penicillinG (23%), erythromycin (16%) and chloramphenicol (11%). Overall, 68.4% of the isolates showed resistance against multiple antibiotics including intrinsic resistances. Initially, 38% of the isolated enterococci was classified as vancomycin resistant using the disc diffusion method, whereas additional broth dilution and PCR assays clearly showed that all E. faecium isolates were in fact vancomycin susceptible.

Anti-Bacterial Agents↗
PubMed2003

Synthesis and utilisation of folate by yoghurt starter cultures and probiotic bacteria.

Thirty-two bacterial isolates from species commonly used in yoghurts and fermented milks were examined for their ability to synthesise or utilise folate during fermentation of skim milk. The organisms examined included the traditional yoghurt starter cultures, Lactobacillus delbrueckii subsp. bulgaricus and Streptococcus thermophilus, and probiotic lactobacilli, bifidobacteria, and Enterococcus faecium. Folate was synthesised by S. thermophilus, bifidobacteria, and E. faecium. S. thermophilus was the dominant producer, elevating folate levels in skim milk from 11.5 ng g(-1) to between 40 and 50 ng g(-1). Generally, lactobacilli depleted the available folate in the skim milk. Fermentations with mixed cultures showed that folate production and utilisation by the cultures was additive. Fermentations using a combination of Bifidobacterium animalis and S. thermophilus resulted in a six-fold increase in folate concentration. Although increased folate levels in yoghurts and fermented milks are possible through judicious selection of inoculum species, the folate levels remain relatively low in terms of recommended daily allowance.

Bifidobacterium↗
PubMed2004

Lactobacillus casei, dominant species in naturally fermented Sicilian green olives.

This study investigated the phenotypic and genotypic characteristics of lactic acid bacteria in naturally fermented green olives, collected from different areas of Sicily. Both classical biochemical tests and PCR/Restriction Fragments Length Polymorphism (RFLP) of 16S rDNA were used to characterize the isolates. The identity of the isolates was obtained by the partial sequencing analysis of the 16S rDNA. The BioMerieux software assigned the 13 heterofermentative strains to the Lactobacillus brevis species; 24 homofermentative strains were classified as Lactobacillus casei and the remaining 11 homofermentative lactobacilli were identified as Lactobacillus plantarum. The rapid ID 32 STREP test identified coccal-shaped strains as Enterococcus faecium species. The PCR/RFLP analysis showed a remarkable bacterial heterogeneity within the isolates. The 16S rDNA partial sequencing did not confirm biochemical identification, revealing a strong dominance of isolates belonging to the L. casei species. It is noteworthy that this species has never been reported as dominant species in fermented vegetables.A combination of molecular and biochemical analysis allowed the identification of species involved in natural food fermentations.

Fermentation↗
PubMed2000

A new rapid automated method for the detection of Listeria from environmental swabs and sponges.

Many food and meat processors test environmental swabs and sponges to confirm the absence of Listeria spp. Spectral pattern changes in a liquid growth medium, resulting from esculin hydrolysis by Listeria in contaminated swabs and sponges, were automatically monitored by the BioSys instrument in a semifluid layer (SFL). The blackening of SFL in modified MOX broth resulted in sharply declining curves, which were easily detected by the instrument. The instrument detected all nine strains of Listeria monocytogenes tested. None of the gram negative organisms (Proteus, Escherichia coli, Pseudomonas, Citrobacter and Yersinia) were detected by the system, nor were most gram positive organisms, including Bacillus, Streptococcus, and Lactobacillus strains, Staphylococcus aureus, Enterococcus faecium and E. faecalis, which hydrolyze esculin, produced black colonies on PALCAM and Oxford media and were also detected in the system. A total of 122 sponges and swabs collected at food processing plants were evaluated by this method. Of these, 99 were negative, and 11 were positive. L. innocua was the dominant Listeria species in these environmental samples. Good correlation was obtained between numbers of Listeria and detection times of esculin hydrolysis: 1000 CFU/swab were detected in 10-13 h, whereas 1-10 CFU/swab were detected in less than 22 h. The total assay time was 26 h.

Animals↗
PubMed2003

Efficacy of some neutralizers in suspension tests determining the activity of disinfectants.

The ability of six mixtures to neutralize glutaraldehyde, o-phthalaldehyde and peracetic acid was tested using four reference strains: Pseudomonas aeruginosa CIP A22, Escherichia coli CIP 54127, Staphylococcus aureus CIP 53154, and Enterococcus faecium CIP 5855. Glutaraldehyde was the hardest to neutralize, and peracetic acid the easiest. The most effective mixture was Tween 80 with sodium bisulphate, sodium thioglycolate, lecithin and cysteine, and the least effective was Tween 80, lecithin and histidine. The efficacy of the neutralizers may indicate a propensity loss of activity from interfering substances when disinfectants are used in practice.

Colony Count, Microbial↗
PubMed2003

A standardized test to assess the impact of different organic challenges on the antimicrobial activity of antiseptics.

This paper presents a suggestion for determining the antimicrobial efficacy of antiseptics in a phase 2/step 1 assay. Emphasis is placed on specific organic challenges to evaluate the efficacy of antiseptics used to rinse the oral cavity, mucous membranes, or wounds for either prophylactic or therapeutic reasons. Basic data are given concerning ready-to-use products based on Poly(1-vinyl-2-pyrrolidone-)iodine-complex (PVP-iodine), chlorhexidine, octenidine, or cetylpyridinium chloride. Hydrogen peroxide (3.0%) was included to assess a product with known limited efficacy only. Using Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Enterococcus faecium, and Candida albicans, a 10(5)-fold reduction can be achieved in 10 min without interfering substances. In the presence of 10% albumin, 10% sheep blood, or 1% mucin, a 10(3)-fold reduction is yielded using products based on PVP-iodine, octenidine, or chlorhexidine. The combination of 4.5% albumin, 4.5% sheep blood, and 1% mucin was the most difficult organic challenge and only the products based on PVP-iodine, octenidine, or chlorhexidine remained active. The cetylpyridinium-based product and hydrogen peroxide were less effective. Based on these data, a proposal for a phase 2/step 1 assay for antiseptics is presented to promote the standardization efforts.

Albumins↗
PubMed1998

Role of antimicrobial-impregnated polymer and Teflon in the prevention of biliary stent blockage.

Biliary stent blockage and microbial colonization is a common complication associated with polyurethane stents used for the relief of bile-duct obstruction caused by benign or malignant disease. In an attempt to overcome this problem the application of a 'Teflon' (polytetrafluoroethylene) stent and an antimicrobial benzalkonium chloride (BZC) impregnated polymer were investigated. The effects of these materials on microbial colonization were compared to a polyurethane stent in vitro in broth or bile. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of BZC for three commonly isolated biliary stent pathogens, Staphylococcus epidermidis, Enterococcus faecium and Enterobacter cloacae were also determined. All the isolates were sensitive to BZC. The growth kinetics of the three organisms in broth and in human pooled bile were similar. Adherence to the BZC impregnated polymer was significantly reduced as compared to the polyurethane and Teflon stents (P < 0.05) in nutrient broth. In bile, fewer organisms attached to the Teflon as compared with the polyurethane stent (P < 0.05) for all organisms. For two of the three test organisms there was less bacterial adherence to the Teflon than to the BZC impregnated polymer. The Teflon and antimicrobial stent materials studied may prevent biliary stent blockage resulting from microbial colonization.

Anti-Infective Agents, Local↗
PubMed2003

The tyrosine decarboxylase operon of Lactobacillus brevis IOEB 9809: characterization and conservation in tyramine-producing bacteria.

Bacterial genes of tyrosine decarboxylases were recently identified. Here we continued the sequencing of the tyrosine decarboxylase locus of Lactobacillus brevis IOEB 9809 and determined a total of 7979 bp. The sequence contained four complete genes encoding a tyrosyl-tRNA synthetase, the tyrosine decarboxylase, a probable tyrosine permease and a Na+/H+ antiporter. Rapid amplification of cDNA ends (RACE) was employed to determine the 5'-end of mRNAs containing the tyrosine decarboxylase gene. It was located only 34-35 nucleotides upstream of the start codon, suggesting that the preceding tyrosyl-tRNA synthetase gene was transcribed separately. In contrast, reverse transcription-polymerase chain reactions (RT-PCRs) carried out with primers designed to amplify regions spanning gene junctions showed that some mRNAs contained the four genes. Homology searches revealed similar clusters of four genes in the genome sequences of Enterococcus faecalis and Enterococcus faecium. Phylogenetic analyses supported the hypothesis that these genes evolved all together. These data suggest that bacterial tyrosine decarboxylases are encoded in an operon containing four genes.

Amino Acid Sequence↗
PubMedDate not supplied

Multi-laboratory assessment of the linezolid spectrum of activity using the Kirby-Bauer disk diffusion method: Report of the Zyvox Antimicrobial Potency Study (ZAPS) in the United States.

The in vitro activity of linezolid against common Gram-positive pathogens was compared to that of penicillin or ampicillin or oxacillin (depending upon genus), cefazolin, erythromycin, clindamycin, quinupristin/dalfopristin, levofloxacin, nitrofurantoin and vancomycin by disk diffusion methods. One hundred and six centers (31 states in US) tested recent clinical isolates of Staphylococcus aureus, coagulase-negative staphylococci, Enterococcus faecium, E. faecalis, Streptococcus pneumoniae, and other streptococci. Testing was conducted using the standardized disk diffusion method and concurrent quality control testing was performed. Strains with linezolid zone diameters of < or = 20 mm were requested for referral to the microbiology monitor for confirmation. A total of 3,100 isolates (97% compliance) were tested. Susceptibility (zone diameters, > or = 21 mm) of staphylococci and streptococci to linezolid was reported in 100% and 99.4% of staphylococci and streptococci, respectively. Susceptibility (zone diameters, > or = 23 mm) of enterococci to linezolid was 96.0% with only three isolates (0.4%) reported as resistant (zone diameters, < or = 20 mm; unconfirmed). Among a total of nine isolates (0.3%) reported to have zone diameters 20 mm, six were not submitted for further testing, two were contaminated with Gram-negative bacilli and one was determined to be linezolid-susceptible. There were no differences in linezolid susceptibility in the vancomycin- or oxacillin- or penicillin-resistant subsets of strains. This susceptibility pattern for US medical centers is indicative of the excellent and nearly complete in vitro activity against the key Gram-positive pathogens for which linezolid has received US Food and Drug Administration indications for clinical use.

Acetamides↗
PubMed2002

A multicenter evaluation of linezolid antimicrobial activity in North America.

Overall, 141 centers in North America enrolled in this international surveillance study designed to evaluate the in vitro antimicrobial activity and spectrum of linezolid, a new oxazolidinone. Each participant tested the susceptibility of clinical isolates of staphylococcal species (n = 85) against 12 drugs, and enterococcal species (n = 40) against 6 drugs using reference broth microdilution trays; and of streptococcal species (n = 25) against 6 drugs using Etests (AB BIODISK, Solna, Sweden). Quality control testing was conducted using recommended strains, and verification of resistance to linezolid and select other agents was performed by a regional monitor. Of the 20,161 isolates collected from sites across the United States (US; n = 132) and Canada (n = 9), 18,307 were included in this analysis. Oxacillin resistance occurred in 38.7 and 70.6% of Staphylococcus aureus and coagulase-negative staphylococcal (CoNS) isolates, respectively. Vancomycin resistance was reported in 65.9 and 2.6% of Enterococcus faecium and E. faecalis, respectively. Penicillin resistance occurred in 37.2% of Streptococcus pneumoniae, 17.5% constituting high-level resistance (MIC, > or =2 microg/ml). The MIC(90) for linezolid was 1 microg/ml for streptococci, 2 microg/ml for enterococci and CoNS isolates, and 4 microg/ml for S. aureus. Using the US FDA-recommended susceptible breakpoints for linezolid, there were no confirmed reports of linezolid resistance (i.e., MIC > or =8 microg/ml). The occurrence of linezolid MICs was unimodal and generally varied between, 1-4 microg/ml for staphylococci (94% of recorded results), 1-2 microg/ml for enterococci (93%), and 0.5-1 microg/ml for streptococci (85%). Susceptibility to linezolid was not influenced by susceptibility to other antiicrobials such as vancomycin, beta-lactams or macrolides. Only linezolid was universally active against essentially all tested Gram-positive specimens. The unimodal susceptibility pattern is indicative of excellent and near complete activity against key Gram-positive pathogens including multiply resistant strains, but surveillance for emerging resistances (rare) and the performance of routine susceptibility tests to guide patient therapy seems prudent.

Acetamides↗
PubMed1997

In vitro antimicrobial activity of RU-59863, a C-7 catechol substituted cephalosporin.

The in vitro activity of RU-59863, a so-called "fifth generation" catechol cephalosporin, was evaluated against 606 bacterial isolates and compared with the activities of cefotaxime, ceftazidime, cefepime, and cefpirome. RU-59863 demonstrated a broad spectrum of inhibition and superior overall activity than comparators when tested against Enterobacteriaciae (MIC90s, 0.015 to 2 micrograms/ml), Pseudomonas aeruginosa (MIC90, 0.5 microgram/ml), Stenotrophomonas maltophilia (MIC90, 0.25 microgram/ml), Acinetobacter ssp. (MIC90, 4 micrograms/ml), and oxacillin-susceptible Staphylococcus ssp. (MIC90s, 0.5 to 8 micrograms/ml). Potent RU-59863 activity was also observed against beta-haemolytic and viridans gr. streptococci (MIC90s, 0.12-0.5 microgram/ml), Streptococcus pneumoniae (MIC90s, 0.03 to 0.5 microgram/ml), Haemophilus influenzae (MIC90, 0.06 microgram/ml), and Neisseria gonorrhoeae (MIC90, 0.06 micrograms/ml). RU-59863 demonstrated marginal potency against Enterococcus faecalis (MICs 2 to 16 micrograms/ml) and was inactive against Enterococcus faecium (MIC90, > 128 micrograms/ml). Oxacillin-resistant staphylococci were not inhibited by RU-59863 (MIC90s, 32 to 128 micrograms/ml). Among the cephalosporins tested, RU-59863 performed best versus ceftazidime-resistant Bush group 1 isolates and strains producing extended spectrum beta-lactamases. RU-59863 was also effective against many fluoroquinolone-, aminoglycoside-, and imipenem-resistant isolates. RU-59863 seems to be a significant advance in cephalosporin chemistry and activity, especially against Gram-negative pathogens resistant to current beta-lactam therapeutic agents. Further studies of human pharmacokinetics and against clinical infections are encouraged.

Bacteria↗
PubMed1999

In vitro activity of moxifloxacin, a new 8-methoxyquinolone, against gram-positive bacteria.

The in vitro activity of moxifloxacin, formerly BAY 12-8039, against gram-positive bacteria was tested by the agar dilution method. A total of 189 isolates that included Staphylococcus aureus, Enterococcus faecalis, Enterococcus faecium, streptococci, rhodococci, leuconostocs, pediococci, lactobacilli, and diphtheroids were tested. Moxifloxacin showed greater potency than ciprofloxacin against S. aureus, streptococci, and enterococci, having Minimal Inhibitory Concentrations (MICs) lower than those of ciprofloxacin by 2- to 64-fold. This improved activity was most prominent for S. aureus. Moxifloxacin was active against Leuconostoc and Rhodococcus species. Time-kill studies using moxifloxacin at a concentration of 3 micrograms/mL against one isolate each of methicillin-resistant S. aureus (MSSA) (MIC, 0.031 microgram/mL), MRSA (MIC, 1 microgram/mL), two isolates of E. faecalis (MICs, 0.25 and 2 micrograms/mL), and two isolates of vancomycin-resistant E. faecium (MICs, 0.25 and 2 micrograms/mL) revealed an average decrease in colony forming unit (CFU) by 3.8, 0.4, 4.0, 2.0, 4.2, and 1.8 log10 CFU/mL at 24 h, respectively. Moxifloxacin is a new 8-methoxyquinolone with improved in vitro activity against gram-positive bacteria. Further studies of the in vivo activity of this compound appear warranted.

Anti-Infective Agents↗
PubMed2003

Growth inhibition of intestinal bacteria and mutagenicity of 2-, 3-, 4-aminobiphenyls, benzidine, and biphenyl.

2-Aminobiphenyl (2-ABP), 3-aminobiphenyl (3-ABP) and 4-aminobiphenyl (4-ABP), but not benzidine (Bz) and biphenyl (Bp), were found to be inhibitory to the growth of human intestinal bacteria Bifidobacterium infantis ATCC 15697, B. bifidium ATCC 11863, Clostridium perfringens ATCC 13124, Escherichia coli ATCC 25922, E. coli ATCC 35218, Enterobacter cloacae ATCC 13047 and Salmonella typhimurium TA98, TA100, YG1041 at 10-200 microg/ml in culture broth. Bacteroides distasonis ATCC 8503, B. fragilis ATCC 25285, B. theataiotaomicron ATCC 29741, C. paraputrificum ATCC 26780, C. clostridiiforme ATCC 25537, Lactobacillus acidophilus ATCC 4356 and Enterococcus faecium ATCC 19434 were not inhibited by the above mentioned compounds in concentrations up to 200 microg/ml. The Ames Salmonella/microsome assay was employed to test the mutagenicity of the above-mentioned compounds using strains TA98 and TA100 in the presence and absence of Aroclor 1254-induced rat S9 mix. It was found that 4-ABP was mutagenic to both TA98 and TA100, and Bz was mutagenic to TA98 in the presence of rat S9 mix. 2-Aminobiphenyl, 3-ABP, and Bp were not mutagenic to both strains tested. 2-Aminobiphenyl and 3-ABP are chemical isomers of 4-ABP and are as strong as 4-ABP in inhibiting the growth of intestinal bacteria but not as mutagenic as 4-ABP. Evidence suggested that the mechanism of growth inhibition is not involved with the interaction of DNA that causes mutations, but rather on the electron transport system of these organisms.

Aminobiphenyl Compounds↗
PubMed2000

Ecological impact of antibiotic use in animals on different complex microflora: environment.

Different means of interaction between microecological systems in different animal hosts (including humans) and the environment may occur during the transfer of resistant bacteria and their resistance genes. Spread of resistance takes place in different ways with respect to clonal spread of resistance strains by the spread of wide host range plasmids and translocatable elements. Commensals in ecosystems have a special significance and a pronounced capacity for acquisition and transfer of resistance genes as with Enterococcus faecium and Escherichia coli in the gut flora or Pseudomonas spp. in aquatic environments. The route of transmission from animals to humans by meat products is well established. Other routes via water and food plants (vegetables) have been investigated less, although resistance genes transfer in aquatic environments as evidenced from sequence comparison of such genes (e.g. tetR, floR in Salmonella typhimurium DT104). Whether this is due to rare but important transfer events or whether there is a more frequent exchange in aquatic or terrestrial environments needs further elucidation.

Animal Feed↗