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Minimal Inhibitory Concentration (minimal + inhibitory_concentration)
Selected AbstractsPharmacokinetic-pharmacodynamic integration of moxifloxacin in rabbits after intravenous, intramuscular and oral administrationJOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 4 2005E. FERNÁNDEZ-VARÓN The pharmacokinetics of moxifloxacin was studied following intravenous (i.v.), intramuscular (i.m.) and oral dose of 5 mg/kg to healthy white New Zealand rabbits (n = 6). Moxifloxacin concentrations were determined by HPLC assay with fluorescence detection. The moxifloxacin plasma concentration vs. time data after i.v. administration could best be described by a two-compartment open model. The disposition of i.m. and orally administered moxifloxacin was best described by a one-compartment model. The plasma moxifloxacin clearance (Cl) for the i.v route was (mean ± SD) 0.80 ± 0.02 L/h·kg. The steady-state volume of distribution (Vss) was 1.95 ± 0.18 L/kg. The terminal half-life (t1/2,z) was (mean ± SD) 1.84 ± 0.12, 2.09 ± 0.05 and 2.15 ± 0.07 h after i.v., i.m. and oral, respectively. Minimal inhibitory concentration (MIC) assays of moxifloxacin against different strains of S. aureus were performed in order to compute pharmacodynamic surrogate markers. From these data, it is concluded that a 5 mg/kg dose moxifloxacin would be effective by i.m. and oral routes in rabbits against bacterial isolates with MIC , 0.06 ,g/mL and possibly for MIC , 0.12 ,g/mL, but in the latter case a higher dose would be required. [source] Fungal endophytes from Dioscorea zingiberensis rhizomes and their antibacterial activityLETTERS IN APPLIED MICROBIOLOGY, Issue 1 2008L. Xu Abstract Aims:, The aim of the study was to isolate and characterize the endophytic fungi from the rhizomes of the Chinese traditional medicinal plant Dioscorea zingiberensis and to detect their antibacterial activities. Methods and Results:, After strict sterile sample preparation, nine fungal endophytes were isolated from rhizomes of the Chinese traditional medicinal plant D. zingiberensis. The endophytes were classified by morphological traits and internal transcribed spacer (ITS) rRNA gene sequence analysis. Their ITS rDNA sequences were 99,100% identical to Nectria, Fusarium, Rhizopycnis, Acremonium and Penicillium spp. respectively. Of these, the most frequent genera were Fusarium and Nectria. One isolate, Dzf7, was unclassified on the basis of its low sequence similarity. The next closest species was Alternaria longissima (c. 92·4% sequence similarity). Endophyte isolate Dzf5 showed the closest sequence similarity (c. 99·5%) to an uncultured soil fungus (DQ420800) obtained from Cedar Creek, USA. Bioassays using a modified broth dilution test were used to detect the antibacterial activity of n -butanol extracts of both mycelia and culture filtrates of D. zingiberensis showed biological activity against Bacillus subtilis, Staphylococcus haemolyticus, Escherichia coli and Xanthomonas vesicatoria. Minimal inhibitory concentration (MIC) values of the extracts were between 31·25 ,g ml,1 and 125 ,g ml,1. Conclusions:, Endophytic fungus Dzf2 (c. 99·8% sequence similarity to Fusarium redolens) isolated from D. zingiberensis rhizome showed the most potent antibacterial activities. Significance and Impact of the Study:, Endophytic fungi isolated from D. zingiberensis may be used as potential producers of antibacterial natural products. [source] Direct fluconazole susceptibility testing of positive Candida blood cultures by flow cytometryMYCOSES, Issue 3 2008Bernard Rudensky Summary The standard methods for yeast susceptibility testing require 24,48 h of incubation. As there has been an increase in incidence of non- albicans Candida species, the clinician is very often wary of initiating therapy with fluconazole until a final susceptibility report is generated, especially when treating very sick patients. A rapid reliable susceptibility testing method would enable the clinician to prescribe fluconazole, thus avoiding more toxic or expensive therapy. To determine the feasibility of direct susceptibility testing of Candida species to fluconazole by a rapid flow cytometric method, 50 Candida strains were seeded into blood culture bottles and were tested for susceptibility to fluconazole directly from the bottles after their being flagged as positive by the blood culture instrument. Minimal inhibitory concentration (MIC) determined by fluorescent flow cytometry (FACS) showed excellent agreement to that determined by macrodilution. Following the seeding experiments, 30 true patient specimens were tested directly from positive blood cultures, and MIC determined by both methods showed excellent agreement. Antifungal susceptibility testing by FACS directly from positive blood culture bottles is a reliable, rapid method for susceptibility testing of Candida to fluconazole. The method allows same-day results, does not require subculture to agar media, and can greatly assist in the selection of appropriate antifungal therapy. [source] Minimal inhibitory concentration of tilmicosin against isolates of Histophilus somni from Australian cattleAUSTRALIAN VETERINARY JOURNAL, Issue 12 2007PJ Blackall No abstract is available for this article. [source] Synthesis and in vitro Efficacy Studies of Silver Carbene Complexes on Biosafety Level 3 BacteriaEUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 13 2009Matthew J. Panzner Abstract A series of N-heterocyclic carbene silver complexes have been synthesized and tested against the select group of biosafety level 3 bacteria Burkholderia pseudomallei, Burkholderia mallei, Bacillus anthracis, methicillin-resistant Staphylococcus aureus and Yersinia pestis. Minimal inhibitory concentrations, minimal bactericidal and killing assays demonstrated the exceptional efficacy of the complexes against these potentially weaponizable pathogens. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009) [source] Frequent occurrence of multidrug-resistant CC17 Enterococcus faecium among clinical isolates in SwedenJOURNAL OF APPLIED MICROBIOLOGY, Issue 5 2010H. Billström Abstract Aims:, To screen for the globally spread cluster of Enterococcus faecium, clonal complex 17 (CC17) and characterize the genetic profile of Swedish clinical Ent. faecium isolates. Methods:, A total of 203 consecutive isolates collected from 2004 to 2007 from patients with bacteraemia in Sweden. All isolates were genotyped using multiple-locus variable-number tandem repeat analysis (MLVA) and 20 isolates representing different MLVA types (MT) were chosen for multilocus sequence typing (MLST). Minimal inhibitory concentrations against clinically relevant antibiotics were determined with agar dilution. Presence of the virulence genes esp and hyl was investigated using PCR. Results:, A total of 65% (n = 109) of all isolates belonged to MT-1, and the second most common MLVA type was MT-159 (13%, n = 21). MLST analysis confirmed the presence of CC17 during the entire study period. The number of isolates resistant to gentamicin and vancomycin, as well as the presence of hyl, increased significantly during the investigation period. Conclusions:, The present study demonstrates that nosocomial infections caused by Ent. faecium CC17 are commonly occurring in Sweden. Significance and Impact of the Study:, This is the first report of CC17 Ent. faecium in Sweden. The increase of antibiotic resistance and virulence indicates that these strains are further adapting to the hospital environment. [source] Pharmacokinetic,pharmacodynamic integration of orbifloxacin in rabbits after intravenous, subcutaneous and intramuscular administrationJOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 1 2008P. MARÍN The single-dose disposition kinetics of orbifloxacin were determined in clinically normal rabbits (n = 6) after intravenous (i.v.), subcutaneous (s.c.) and intramuscular (i.m.) administration of 5 mg/kg bodyweight. Orbifloxacin concentrations were determined by high performance liquid chromatography with fluorescence detection. Minimal inhibitory concentrations (MICs) assay of orbifloxacin against 30 strains of Staphylococcus aureus from several European countries was performed in order to compute pharmacodynamic surrogate markers. The concentration,time data were analysed by compartmental and noncompartmental kinetic methods. Steady-state volume of distribution (Vss) and total body clearance (Cl) of orbifloxacin after i.v. administration were estimated to be 1.71 ± 0.38 L/kg and 0.91 ± 0.20 L/h·kg, respectively. Following s.c. and i.m. administration orbifloxacin achieved maximum plasma concentrations of 2.95 ± 0.82 and 3.24 ± 1.33 mg/L at 0.67 ± 0.20 and 0.65 ± 0.12 h, respectively. The absolute bio-availabilities after s.c. and i.m. routes were 110.67 ± 11.02% and 109.87 ± 8.36%, respectively. Orbifloxacin showed a favourable pharmacokinetic profile in rabbits. However, on account of the low AUC/MIC and Cmax/MIC indices obtained, its use by i.m. and s.c. routes against the S. aureus strains assayed in this study cannot be recommended given the risk of selection of resistant populations. [source] Pharmacokinetic,pharmacodynamic integration of danofloxacin after intravenous, intramuscular and subcutaneous administration to rabbitsJOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 1 2007E. FERNÁNDEZ-VARÓN The pharmacokinetics of danofloxacin was studied following intravenous (i.v.), intramuscular (i.m.) and subcutaneous (s.c.) administration of 6 mg/kg to healthy rabbits. Danofloxacin concentration were determined by high-performance liquid chromatography assay with fluorescence detection. Minimal inhibitory concentrations (MICs) assay of danofloxacin against 30 strains of Staphylococcus aureus from several European countries was performed in order to compute pharmacodynamic surrogate markers. The danofloxacin plasma concentration versus time data after i.v. administration could best be described by a two-compartment open model. The disposition of i.m. and subcutaneously administered danofloxacin was best described by a one-compartment model. The terminal half-life for i.v., i.m. and s.c. routes was 4.88, 6.70 and 8.20 h, respectively. Clearance value after i.v. dosing was 0.76 L/kg·h. After i.m. administration, the absolute bioavailability was mean (±SD) 102.34 ± 5.17% and the Cmax was 1.87 mg/L. After s.c. administration, the absolute bioavailability was mean (±SD) 96.44 ± 5.95% and the Cmax was 1.79 mg/L. Danofloxacin shows a favourable pharmacokinetics profile in rabbits reflected by parameters such as a long half-life and a high bioavailability. However, in consideration of the low AUC/MIC indices obtained, its use by i.m. and s.c. route against the S. aureus strains assayed in this study cannot be recommended given the risk for selection of first mutant subpopulations. [source] In vitro and in vivo pharmacodynamic properties of the fluoroquinolone ibafloxacinJOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 6 2002M. Coulet The pharmacodynamic properties of a new veterinary fluoroquinolone antimicrobial agent, ibafloxacin, were evaluated. Minimal inhibitory concentrations (MIC), time-kill kinetics, postantibiotic effect (PAE) and postantibiotic subminimal inhibitory concentration effects (PA-SME) were determined against pathogenic canine Gram-negative and Gram-positive bacterial isolates from dermal, respiratory and urinary tract infections. The synergistic interactions between ibafloxacin and its main metabolite, 8-hydroxy-ibafloxacin were investigated. Finally, the efficacy of ibafloxacin was tested in in vivo canine infection models. Ibafloxacin had good activity against Pasteurella spp., Escherichia coli, Klebsiella spp., Proteus spp. and Staphylococcus spp. (MIC90=0.5 µg/mL), moderate activity against Bordetella bronchiseptica, Enterobacter spp. and Enterococcus spp. (MIC50=4 µg/mL) and low activity against Pseudomonas spp. and Streptococcus spp. The time-killing analysis confirmed that ibafloxacin was bactericidal with a broad spectrum of activity. The PAE and PA-SME were between 0.7,2.13 and 1,11.5 h, respectively. Finally, studies in dog models of wound infection and cystitis confirmed the efficacy of once daily oral ibafloxacin at a dosage of 15 mg/kg. Additional studies are needed to better define the importance of AUC/MIC (AUIC) and Cmax/MIC ratios on the outcome of fluoroquinolone therapy in dogs. [source] Selective growth of Staphylococcus aureus from flushed dairy manure wastewater using acriflavine-supplemented mannitol salt agarLETTERS IN APPLIED MICROBIOLOGY, Issue 6 2006J.A. Davis Abstract Aims:, To investigate the use of mannitol salt agar (MSA) supplemented with acriflavine for selective growth and quantification of Staphylococcus aureus from flushed dairy manure wastewater (FDMW). Methods and Results:, Minimal inhibitory concentrations of acriflavine in MSA were determined by comparing the growth of S. aureus subsp. aureus (ATCC 33591) and Staphylococcus epidermidis (ATCC 155) in pure culture. Acriflavine concentrations of 1·3, 1·4 and 1·5 mg l,1 reduced CFU of S. epidermidis by 43%, 55% and 87%, respectively, while CFU of S. aureus subsp. aureus were only reduced by 15%, 20% and 26% at the respective concentrations of acriflavine. MSA supplemented with 1·5 mg l,1 acriflavine was tested for selective growth of indigenous S. aureus from three grab samples of FDMW. Acriflavine concentrations of 1·5 mg l,1 reduced background flora without significantly reducing (P < 0·05) indigenous S. aureus counts. Conclusions:, Acriflavine-supplemented MSA provides an effective media for selective growth and quantification of indigenous S. aureus from FDMW in the presence of high levels of background microflora. Significance and Impact of the Study:,S. aureus is implicated for mastitis infections in dairy cows. Therefore, a reliable means for monitoring and detecting the organism in FDMW provides a tool for measuring the effectiveness of treatment for reducing S. aureus levels and implementing flushwater recycling without affecting herd health. [source] Effects of fluorides on Candida albicansORAL DISEASES, Issue 4 2008S Flisfisch Aims:, To assess whether a short exposure of Candida albicans to commonly used fluorides would affect growth, cell surface hydrophobicity, and adherence to buccal epithelial cells. Methods:,Candida albicans ATCC 90028 and 11 clinical isolates were used. Minimal inhibitory concentrations (MICs) of sodium fluoride (NaF) and of an amine fluoride,/,stannous fluoride combination (AmF,/,SnF2) were determined. Yeasts were exposed to MICs of tested agents for 1 h. Subsequently, their growth was recorded spectrophotometrically. Their cell surface hydrophobicity was assessed with n -hexadecane. Adherence to buccal epithelial cells was determined microscopically. Phosphate buffered saline (PBS) and chlorhexidine digluconate (CHX) served as controls. All results were analyzed by one-way ANOVA. Results:, MICs of AmF,/,SnF2 and CHX varied between 1 and 4 ,g ml,1, whereas those of NaF were 15 000 ,g ml,1. Statistically significant growth inhibition was detected after AmF,/,SnF2 (OD24 h ± SD 0.457 ± 0.059) and CHX (0.175 ± 0.065) in comparison with PBS (0.925 ± 0.087) and NaF (0.813 ± 0.081). All strains demonstrated uniform behavior. Only minor changes in cell surface hydrophobicity and adherence to buccal epithelial cells (BEC) were detected. Conclusion:, Growth inhibition of AmF,/,SnF2 was comparable with that of CHX whereas NaF had a weaker effect. Exposure to the fluorides did not seem to alter the cell surface hydrophobicity nor adherence to BEC. [source] Epidemiology of Candidemia in a Turkish tertiary care hospital,APMIS, Issue 9 2006MUSTAFA BAKIR In order to determine the local epidemiology of candidemia, Candida strains isolated between 1994 and 2000 were identified to species level; antifungal resistance patterns and DNA fingerprints were analyzed. Identification of Candida strains (n: 140) was performed with germ tube test and carbohydrate assimilation reactions. Minimal inhibitory concentrations were determined using a commercial test for 5-flucytosine and the broth macrodilution method according to NCCLS for fluconazole and amphotericin B. Molecular relatedness was determined by restriction endonuclease analysis of genomic DNA followed by probe hybridization. C. albicans (37.2%), C. parapsilosis (32.2%), and C. tropicalis (12.2%) comprised 114 (81.4%) of 140 isolates. Susceptibility tests did not reveal resistance to amphotericin B in any of the Candida isolates. Fluconazole resistance was detected in one isolate of C. krusei, and 5-flucytosine resistance in two C. tropicalis isolates and one C. albicans isolate. Significantly higher frequency of clusters with identical strains in C. parapsilosis and C. tropicalis was detected compared to C. albicans. Pediatric wards are particularly important in the nosocomial transmission of non- albicans candida species. [source] Kinetic bactericidal activity of telithromycin, azithromycin and clarithromycin against respiratory pathogens,APMIS, Issue 10 2005L. DRAGO The present study assessed the comparative in vitro killing kinetics of telithromycin, azithromycin and clarithromycin. Minimal inhibitory concentrations (MIC) and minimal bactericidal concentrations (MBC) were determined against Streptococcus pneumoniae, ,-haemolytic streptococci, Haemophilus influenzae and Moraxella catarrhalis strains characterized by different susceptibilities to ,-lactams and macrolides. For each bacterial species, representative strains were chosen for time-kill studies. Telithromycin showed high activity against all the tested strains with MIC ranging from ,0.004 to 0.5 mg/L for streptococci, from 0.008 to 8 mg/L for H. influenzae, and from 0.008 to 0.5 mg/L for M. catarrhalis. In time-kill studies, telithromycin showed an overall superior bactericidal activity in respect to macrolides, particularly against resistant strains. In conclusion, telithromycin proved to possess bactericidal activity against a wide range of respiratory pathogens, including strains resistant to common macrolides. [source] Original Article: Pulmonary function, airway cytology and bronchoalveolar lavage fluid drug concentration after aerosol administration of cefquinome to horsesEQUINE VETERINARY EDUCATION, Issue 9 2010T. Art Summary The administration of antibiotics by aerosol to horses suffering from respiratory infections may partially circumvent the limitations of antimicrobial therapy, e.g. large injection volumes, low bioavailability and risk of diarrhoea. Only injectable formulations are available currently and usually contain other substances that could irritate the mucosa and induce coughing and bronchospasm. In addition, the quality of the aerosol, particularly in terms of the delivery of antibiotics to the deep parts of the lung, is unknown. Although used under field conditions, cefquinome delivered by aerosol has never been studied in horses. This study examined the safety of cefquinome injectable solution, administered by aerosol at a dose of 225 mg/inhalation to 7 healthy horses, by assessing (1) pulmonary function before and 15 min after a single inhalation, at the first day (Day 1) and the fifth day (Day 5) of a 5 day period treatment; and (2) the inflammatory status of the lung, i.e. percentage neutrophils and myeloperoxidase concentration, based on bronchoalveolar lavage (BAL) at D1 and D5. In addition, cefquinome concentrations were measured in bronchoalveolar lavage fluid after aerosol, intravenous (i.v.) and intramuscular (i.m.) administrations. A single aerosol of cefquinome injectable solution did not induce any immediate nor delayed pulmonary side effects in healthy horses and produced cefquinome concentrations in bronchoalveolar lavage (BAL) within 30 min that were higher than the minimal inhibitory concentration of the main equine respiratory pathogens. These results should stimulate further studies, especially in horses suffering from bronchial hyper-reactivity. Aerosol delivery of antibiotics may well have a role in equine therapeutics. [source] Adhesion of Enterococcus faecalis 1131 grown under subinhibitory concentrations of ampicillin and vancomycin to a hydrophilic and a hydrophobic substratumFEMS MICROBIOLOGY LETTERS, Issue 1 2001Amparo M Gallardo-Moreno Abstract The effect of two subinhibitory antibiotic concentrations of ampicillin and vancomycin during growth on the adhesion of Enterococcus faecalis 1131 to glass and silicone rubber was studied in a parallel plate flow chamber. Initial deposition rates and numbers of adhering bacteria after 4 h were higher on hydrophilic glass than on hydrophobic silicone rubber, regardless of growth conditions. The presence of 1/4 minimal inhibitory concentration (MIC) of ampicillin during growth reduced enterococcal adhesion to both substrata, but growth in the presence of 1/4 MIC vancomycin did not affect the adhesion of E. faecalis. Moreover, enterococcal adhesion increased after growth in the presence of 1/8 MIC vancomycin. The increased adhesion after growth in the presence of subinhibitory concentrations of vancomycin may have strong implications for patients living with implanted biomaterials, as they may suffer adverse effects from use of this antibiotic, especially since bacteria once adhered are less sensitive to antibiotics. [source] Amoxicillin Resistance in Helicobacter pylori: Studies from Tokyo, Japan from 1985 to 2003HELICOBACTER, Issue 1 2005Kazuhiro Watanabe ABSTRACT Background., Previous reports revealed no resistant strains of amoxicillin (AMPC), which is usually used in eradication therapy for H. pylori infection. However, the frequency and evolution of natural AMPC-resistant strains in the Japanese population remains unknown. Aim., To assess the prevalence of H. pylori resistance against AMPC in the Tokyo area, a collection of 648 H. pylori strains isolated from patients with GI diseases from 1985 to 2003 was tested for their sensitivity to AMPC. Methods., The susceptibility of the strains was assessed by determination of the minimal inhibitory concentration (MIC) using the E -test and/or the Dry-plate method. The susceptibility breakpoints of AMPC for H. pylori were: sensitive (AMPC-S); MIC < 0.04 µg/ml, intermittent resistance (AMPC-I); 0.04,1, resistant (AMPC-R); > 1. Results., No AMPC-R strains were detected in the strains isolated between 1985 and 1996, while the rate of resistance was determined to be 1.1%, 2.1%, 5.4%, 5.6%, 0%, 8.8%, and 1.5% every year, respectively, from 1997 to 2003. The percentage of AMPC-I strains increased from 2000 to 2003. The total eradication rate of H. pylori in the patients who received triple therapy containing AMPC was 81.4% (214/263). Classified as above, the rates of AMPC-S, AMPC-I, and AMPC-R were 84.6%, 77.8%, 25%, respectively. Conclusion.,H. pylori resistance to AMPC is still rare in Japan, although the percentage of AMPC-I strains has increased over the last 4 years. The frequency of isolation of strains showing true resistance to AMPC may increase in the future, along with an increase in the frequency of isolation of AMPC-I strains. [source] A century of the synthesis of dapsone: its anti-infective capacity now and thenINTERNATIONAL JOURNAL OF DERMATOLOGY, Issue 10 2000Ronni Wolf MD Background Although dapsone was first synthesized in 1908, a quarter of a century was to pass before it was used in the treatment of bacterial infections. Dapsone was, however, too toxic for humans (because of the excess dosage which was administered at that time) and was thus considered to be of no value in the treatment of common bacterial infections. Since the early 1950s, dapsone has been recognized as being uniquely effective against a number of noninfectious, inflammatory diseases and, today, this is its main indication. Thus, the reason why dapsone was first introduced into medicine, namely the treatment of bacterial infections, has been set aside and its main current applications are the treatment of noninfectious, inflammatory, autoimmune, and bullous diseases. Objective To study the anti-infective capacity of dapsone against common bacterial infections. As many patients who receive dapsone for the treatment of noninfectious, inflammatory diseases have a concomitant bacterial infection or a superinfection of their skin disease, we thought that, if dapsone proved to be effective against common bacterial infections, it may obviate the need for an additional antimicrobial drug in these patients. Methods Three bacterial ATCC> strains (Streptococcus pyogenes, Staphylococcus aureus, and Escherichia coli) were tested by a macrodilution minimal inhibitory concentration (MIC) test for dapsone. Dapsone concentrations were between 0.06 and 1125 ,g/mL. Results Even the highest concentration of dapsone of 1125 ,g/mL did not inhibit bacterial growth. Conclusions Our results indicate that dapsone has no antibacterial effects whatsoever. Even at very high concentrations, it does not suppress the growth of most susceptible strains of bacteria. The story of dapsone (i.e. the long time that elapsed between its synthesis to its use for the chemotherapy of infectious diseases) will not repeat itself this time. [source] Investigation of the anti-fungal activity of coptisine on Candida albicans growth by microcalorimetry combined with principal component analysisJOURNAL OF APPLIED MICROBIOLOGY, Issue 4 2009W.-J. Kong Abstract Aims:, This study investigated the anti-fungal activity of coptisine on Candida albicans growth. Methods and Results:, The metabolic power-time curves of Candida albicans growth at 37°C affected by coptisine were measured by microcalorimetry using an LKB-2277 Bioactivity Monitor with stop-flow mode. Then, the diameter of inhibitory zones in the agar layer was observed using agar cup method, and the minimal inhibitory concentration (MIC) of coptisine on Candida albicans growth was determined by serial dilution method. From the principal component analysis on nine quantitative parameters obtained from the power-time curves, we could easily evaluate the anti-fungal activity of coptisine by analysing the change of values of the main two parameters, growth rate constant k and maximum power output in the log phase Pm, log. The results showed that coptisine had strong anti-fungal activity: at a low concentration (45 ,g ml,1) began to inhibit the growth of Candida albicans and at a high concentration (500 ,g ml,1) completely inhibited Candida albicans growth. Coptisine gave big inhibitory zones with diameters between 11 and 43 mm within test range, and the MIC of it was 1000 ,g ml,1. Conclusions:, Coptisine had strong anti-fungal activity on Candida albicans growth. The method of microcalorimetry applied for the assay of anti-fungal activity of coptisine was quantitative, sensitive and simple. Significance and Impact of the Study:, This work will provide useful information for the development of chemical biology policy in the use of anti-microbials in food and drug production. [source] Efficient removal of hexavalent chromium by a tolerant Streptomyces sp. affected by the toxic effect of metal exposureJOURNAL OF APPLIED MICROBIOLOGY, Issue 6 2007D.K. Morales Abstract Aims:, To isolate and analyse chromium-resistant micro-organisms suitable for bioremediation. Methods and Results:, Strain CG252, with a minimal inhibitory concentration of 500 ,g ml,1, was isolated from contaminated soils and identified as a Streptomyces sp. by 16S rDNA sequence analysis. Assays carried out at various Cr(VI) concentrations indicated that chromium removal was more efficient at lower concentrations and that this activity resulted in accumulation of Cr(III). Atomic adsorption analysis indicated that the chromium removed was not associated with cell mass and activity assays showed that the capacity to reduce Cr(VI) was most probably due to a soluble cytosolic enzyme. Cells grown as biofilms showed enhanced removal of Cr(VI) with respect to planktonic cells, while analysis of growth and colony morphology indicated that Cr(VI) had a toxic effect on this strain. Conclusions:,Streptomyces sp. CG252 tolerated heavy metals and elevated levels of chromium, despite its negative effect on growth and development, and was efficient at removing Cr(VI) by promoting reduction to Cr(III). Significance and Impact of the Study:, Strain CG252's capacity to tolerate heavy metals and to reduce Cr(VI) to the less toxic Cr(III), especially when forming biofilms, makes it a promising candidate for detoxification of sites containing this heavy metal. [source] Effects of vancomycin, daptomycin, fosfomycin, tigecycline, and ceftriaxone on Staphylococcus epidermidis biofilmsJOURNAL OF ORTHOPAEDIC RESEARCH, Issue 10 2009Stefan Hajdu Abstract Infection of medical implanted material is associated with considerable morbidity and costs. In the following work, we investigated the effects of vancomycin, daptomycin, fosfomycin, tigecycline, and ceftriaxone on biofilms formed by Staphylococcus epidermidis isolates causative for implant infection and catheter-associated bacteremia. Biofilms were studied using the static microtiter plate model and incubated with the antibiotics increasing the concentration from 1× to 128× the minimal inhibitory concentration (MIC) of the respective isolate tested. To quantify the reduction of the biomass, the optical density ratio (ODr) of stained biofilms and the number of growing bacteria were determined. Incubation of the staphylococcal biofilms with the antibiotics decreased the biofilm ODr (at baseline,=,1) for ceftriaxone (0.83,±,0.48) but minimally only for fosfomycin (0.96,±,0.64), daptomycin (1.05,±,0.59), tigecycline (1.18,±,0.66), and vancomycin (0.98,±,0.44) at exceedingly high concentrations of 128,×,MIC. The significant reduction of the bacterial growth was not achieved for all antibiotics, not even at the highest concentrations tested. Using higher doses of the antibiotics may be of some value in the treatment of biofilm-associated infections, although effects are seen only at clinically unachievable doses. However, to eradicate the staphylococcal biofilm, additional measures like debridement and/or removal of the implant are needed. © 2009 Orthopaedic Research Society. Published by Wiley Periodicals, Inc. J Orthop Res 27:1361,1365, 2009 [source] Membrane permeability and antimicrobial kinetics of cecropin P1 against Escherichia coli,JOURNAL OF PEPTIDE SCIENCE, Issue 6 2009Steven Arcidiacono Abstract The interaction of cecropin P1 (CP1) with Escherichiacoli was investigated to gain insight into the time-dependent antimicrobial action. Biophysical characterizations of CP1 with whole bacterial cells were performed using both fluorescent and colorimetric assays to investigate the role of membrane permeability and lipopolysaccharide (LPS) binding in lytic behavior. The kinetics of CP1 growth inhibition assays indicated a minimal inhibitory concentration (MIC) of 3 µM. Bactericidal kinetics at the MIC indicated rapid killing of E.coli (<30 min). Membrane permeability studies illustrated permeation as a time-dependent event. Maximum permeability at the MIC occurred within 30 min, which correlates to the bactericidal action. Further investigation showed that the immediate permeabilizing action of CP1 is concentration-dependent, which correlates to the concentration-dependent nature of the inhibition assays. At the MIC and above, the immediate permeability was significant enough that the cells could not recover and exhibit growth. Below the MIC, immediate permeability was evident, but the level was insufficient to inhibit growth. Dansyl polymyxin B displacement studies showed LPS binding is essentially the same at all concentrations investigated. However, it does appear that only the immediate interaction is important, because binding continued to increase over time beyond cell viability. Our studies correlated CP1 bactericidal kinetics to membrane permeability suggesting CP1 concentration-dependent killing is driven by the extent of the immediate permeabilizing action of the peptide. Copyright © 2009 European Peptide Society and John Wiley & Sons, Ltd. [source] Antifungal activity of Thymus oils and their major compoundsJOURNAL OF THE EUROPEAN ACADEMY OF DERMATOLOGY & VENEREOLOGY, Issue 1 2004C Pina-Vaz ABSTRACT The increasing recognition and importance of fungal infections, the difficulties encountered in their treatment and the increase in resistance to antifungals have stimulated the search for therapeutic alternatives. Essential oils have been used empirically. The essential oils of Thymus (Thymus vulgaris, T. zygis subspecies zygis and T. mastichina subspecies mastichina) have often been used in folk medicine. The aim of the present study was to evaluate objectively the antifungal activity of Thymus oils according to classical bacteriological methodologies , determination of the minimal inhibitory concentration (MIC) and the minimal lethal concentration (MLC) , as well as flow cytometric evaluation. The effect of essential oils upon germ tube formation, an important virulence factor, was also studied. The mechanism of action was studied by flow cytometry, after staining with propidium iodide. The chemical composition of the essential oils was investigated by gas chromatography (GC) and gas chromatography/mass spectroscopy (GC/MS). The antifungal activity of the major components (carvacrol, thymol, p -cymene and 1,8-cineole) and also possible interactions between them were also investigated. The essential oils of T. vulgaris and T. zygis showed similar antifungal activity, which was greater than T. mastichina. MIC and MLC values were similar for all the compounds tested. At MIC values of the essential oils, propidium iodide rapidly penetrated the majority of the yeast cells, indicating that the fungicidal effect resulted primarily from an extensive lesion of the cell membrane. Concentrations below the MIC values significantly inhibited germ tube formation. This study describes the potent antifungal activity of the essential oils of Thymus on Candida spp., warranting future therapeutical trials on mucocutaneous candidosis. [source] Effect of benzyl isothiocyanate on tomato fruit infection development by Alternaria alternataJOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE, Issue 9 2005R Troncoso-Rojas Abstract Benzyl isothiocyanate (BITC) is known to be a strong antifungal compound in vitro against different fungi. The effectiveness of benzyl isothiocyanate to control Alternaria alternata growth in vitro and in vivo was tested. BITC in vitro activity was evaluated in A alternata growing on potato dextrose agar and exposed to 0.025, 0.05, 0.1, 0.2 or 0.4 mg ml,1. In vivo activity was evaluated by exposing A alternata -inoculated tomato fruits for either 18 or 36 h to 0.28 or 0.56 mg ml,1 BITC packed on low-density polyethylene film (LDPF) bags. Additionally, the effect of BITC on post-harvest physiology and tomato quality throughout storage at 20 °C was evaluated daily by monitoring respiration rate and ethylene production, whereas total soluble solids, pH, titratable acidity and fresh weight loss were measured every 3 days. Results showed that the minimal inhibitory concentration of BITC in vitro was 0.1 mg ml,1. A combined use of 0.56 mg ml,1 BITC with LDPF for 18 h was the optimum treatment to control Alternaria rot in packed tomato fruit. No effect of BITC on respiration rate, ethylene production, total soluble solids, pH, weight loss and titratable acidity was observed. Results suggest that BITC can be used as a post-harvest treatment to control Alternaria rot in tomato fruit without detrimental effects on the tomato post-harvest quality. Copyright © 2005 Society of Chemical Industry [source] Usefulness and pharmacokinetic study of oral terbinafine for hyperkeratotic type tinea pedisMYCOSES, Issue 1 2008Izumi Kikuchi Summary To study and establish an optimal administration method of oral antifungal, terbinafine (TBF), for hyperkeratotic type tinea pedis, from the pharmacokinetic point of view, 20 patients with hyperkeratotic type tinea pedis were given TBF 125 mg once daily for 4 weeks and observed over time for improvement in dermatological symptoms and mycological efficacy. Targeting five of the patients, TBF concentration in the stratum corneum was measured using the liquid chromatography/tandem mass spectrometry (LC-MS/MS) method. TBF was detected in the stratum corneum of the sole 1 week after beginning the treatment in some cases and reached its peak 1 week after the completion of the treatment with a concentration of 247.8 ng g,1, which was approximately more than 50 times higher than its minimal inhibitory concentration against dermatophytes. TBF was not detected at 8 weeks post-treatment, although its concentration was 50.73 ng g,1 at 6 weeks post-treatment. Its effectiveness rate (effective + markedly effective) was 95% (19/20) with no adverse reactions, including abnormal changes in the laboratory test values, in any patient. These results suggest that TBF is a useful drug to treat hyperkeratotic tinea pedis from the pharmacokinetic point of view. [source] Screening of herbal extracts against multi-drug resistant Acinetobacter baumanniiPHYTOTHERAPY RESEARCH, Issue 8 2010Yoko Miyasaki Abstract Antibiotic resistance is increasing resulting in a decreasing number of fully active antimicrobial agents available to treat infections with multi-drug resistant (MDR) bacteria. Herbal medicines may offer alternative treatment options. A direct inoculation method simulating the standard disc diffusion assay was developed to determine in vitro antimicrobial activity of sixty herbal extracts against MDR- Acinetobacter baumannii (A. baumannii). Eighteen herbal extracts inhibited MDR- A. baumannii on agar plates, although the magnitude and quality of bacterial inhibition differed considerably among the antibacterial herbal extracts. Next, minimal inhibitory concentration (MIC) of these antibacterial herbal extracts was calculated using a broth microdilution assay. For most herbal extracts, the larger the zone of inhibition on agar plates, the lower the MIC. In general, hetero-resistance on agar plates correlated with higher MIC. The skip well phenomenon was seen with two herbal extracts. In conclusion, 30% of the screened herbal extracts demonstrated in vitro antibacterial activity against MDR- A. baumannii using similar rigorous testing methods as those commonly employed for assessing antimicrobial activity of synthetic antibacterial agents. Characterization of a specific compound conferring this antibacterial activity of the herbal extracts may help to identify novel antimicrobial agents active against highly resistant bacteria. Copyright © 2010 John Wiley & Sons, Ltd. [source] Mutations in 23S rRNA and ribosomal protein L4 account for resistance in Chlamydia trachomatis strains selected in vitro by macrolide passageANDROLOGIA, Issue 4 2010H. Zhu Summary Thirteen strains of Chlamydia trachomatis were exposed to subinhibitory concentrations of erythromycin (0.5 ,g ml,1), azithromycin (0.5 ,g ml,1) and josamycin (0.04 ,g ml,1) to select macrolide-resistant mutants with serial passages. The C. trachomatis mutants presented with low-level resistance to erythromycin, azithromycin and josamycin for which a 16-fold increase, a 16-fold increase and an 8-fold increase respectively in the minimal inhibitory concentration (MICs) for the mutant strains compared with the MIC for the susceptible strains were found. The results of chemosensitivity showed that josamycin had the highest susceptibility rate compared with erythromycin and azithromycin in the treatment of C. trachomatis. The ribosomal protein L4 and 23S rRNA genes of the susceptible and resistant strains of C. trachomatis were partially sequenced. A double mutation was found in ribosomal protein L4 of the mutants, leading to Pro109(CCG),Leu(CTG), and Pro151(CCG),Ala(GCC) (Escherichia coli numbering) in the corresponding protein, but these mutations were also found in parent strains. An investigation into the sequences of 23S rRNAs in the mutants revealed point mutations of A2057G, A2059G and T2611C (E. coli numbering). These results suggest that point mutations located in 23S rRNA were associated with macrolide resistance in C. trachomatis. [source] Synthesis and Evaluation of Novel Indolylthiadiazinoazetidinones and Indolylthiadiazinothiazolidinones as Antimicrobial AgentsARCHIV DER PHARMAZIE, Issue 2 2010Vikas Kumar Abstract Some new 5-methoxy/ethoxy-2,3-[2,-(3,,-chloro-2,,-oxo-4,,-substituted-aryl-1,,-azetidinyl)-1,,3,,4,-thiadiazino]indoles 13,20 and 5-methoxy/ethoxy-2,3-[2,-(2,,-substituted-aryl-4,,-oxo-1,,,3,,-thiazolidin-3,,-yl)-1,,3,,4,-thiadiazino]indoles 21,28 have been synthesized from 5-methoxy/ethoxy-2,3-[2,-(substituted-benzylidinylimino)-1,,3,,4,-thiadiazino]indoles 5,12. These newly synthesized compounds were characterized by elemental and spectral analysis. Further, compounds 5,28 of the present series have been screened for their antibacterial and antifungal activities. Both minimal inhibitory concentration (MIC) and inhibition zones were determined in order to monitor the efficacy of the synthesized compounds. Compounds 14 and 16 were found to be the most potent members of the present series, they showed maximal antibacterial and antifungal properties much better than the standard drugs. [source] Sensitivity to Hydrogen Peroxide of Growth and Hyaluronic Acid Production by Streptococcus zooepidemicus ATCC 39920ASIA-PACIFIC JOURNAL OF CHEMICAL ENGINEERING, Issue 5-6 2005M.D. Mashitah Abstract The sensitivity to hydrogen peroxide (H2O2) of growth and hyaluronic acid (HA) production by Streptococcus zooepidemicus ATCC 39920 was studied under various conditions. In sheep blood agar-plates, no detectable zone was observed even when the concentration of H2O2 was increased to 0.15 mM. With brain heart infusion-agar and chemically defined medium-agar plates, a profound zone was detected at 0.015 mM concentration of H2O2. To determine the minimal inhibitory concentration (MIC) of the strain in culture broth, various concentrations of H2O2 (0-200 mM) were maintained in the medium prior to fermentation. The result showed that for higher concentrations of H2O2 in the medium, the greater was the inhibition. Streptococcus is catalase-negative and known to produce H2O2 which may affect growth, HA production and glucose utilization. In order to determine at which growth phase H2O2 had the maximum inhibitory activity, a batch fermentation of S. zooepidemicus was conducted in shake flask culture. It was found that H2O2 production took place during the growth phase, and HA production started after the growth had reach late exponential phase when H2O2 in the culture media was depleted. This indicates that H2O2 produced by the cells did not affect cell growth but influenced HA production. [source] Palladium-Catalysed Amination of Electron-Deficient or Relatively Electron-Rich Benzo[b]thienyl Bromides , Preliminary Studies of Antimicrobial Activity and SARsEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 17 2004Maria-João R. P. Queiroz Abstract Several diarylamines in the benzo[b]thiophene series were prepared in good to high yields by palladium-catalysed amination of ethyl 3-bromobenzo[b]thiophene-2-carboxylate with anilines and 5-aminoindole in the presence of Pd(OAc)2, BINAP and Cs2CO3 in toluene. The presence of the ester group at the 2-position of the benzo[b]thiophene moiety increases the yields and lowers the heating times relative to the reactions performed with 3-bromobenzo[b]thiophene. When aminopyridines were used instead of anilines, the ligand and the solvent need to be changed to XANTHPHOS and dioxane in the amination reaction. With 2-aminopyridine a one-pot C,N coupling and intramolecular cyclization involving the nitrogen atom of the pyridine ring occurred, with loss of ethanol, giving an interesting fluorescent tetracyclic heteroaromatic compound. The antimicrobial activity, the minimal inhibitory concentrations (MICs) and the structure-activity relationships (SARs) were evaluated. A selectivity with low MICs was observed against Bacillus Cereus, and good results were also obtained against Candida albicans. The acids obtained by hydrolysis of the ester group, as non-proteinogenic ,,,-unsaturated ,-amino acids, can be incorporated into peptide chains to induce conformational constraints. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004) [source] In Candida albicans, resistance to flucytosine and terbinafine is linked to MAT locus homozygosity and multilocus sequence typing clade 1FEMS YEAST RESEARCH, Issue 7 2009Frank C. Odds Abstract A panel of 637 isolates of Candida albicans that had been typed by multilocus sequence typing (MLST) and tested for susceptibility to amphotericin B, caspofungin, fluconazole, flucytosine, itraconazole, ketoconazole, miconazole, terbinafine and voriconazole was the material for a statistical analysis of possible associations between antifungal susceptibility and other properties. For terbinafine and flucytosine, the greatest proportion of low-susceptibility isolates, judged by two resistance breakpoints, was found in MLST clade 1 and among isolates homozygous at the MAT locus, although only three isolates showed cross-resistance to the two agents. Most instances of low susceptibility to azoles, flucytosine and terbinafine were among oropharyngeal isolates from HIV-positive individuals. Statistically significant correlations were found between terbinafine and azole minimal inhibitory concentrations (MICs), while correlations between flucytosine MICs and azole MICs were less strong. It is concluded that a common regulatory mechanism may operate to generate resistance to the two classes of agent that inhibit ergosterol biosynthesis, terbinafine and the azoles, but that flucytosine resistance, although still commonly associated with MAT homozygosity, is differently regulated. [source] | ||||||||||||||||||||||||||||