scholarly journals Suspicion of quinolone active metabolite following discrepancy between predicted and experimental urine bactericidal activities.

1997 ◽  
Vol 41 (5) ◽  
pp. 927-930 ◽  
Author(s):  
L Aguilar ◽  
M J Giménez ◽  
J Costa ◽  
R Dal-Ré ◽  
J Prieto

The prediction of urine antibacterial activity from pharmacological and microbiological parameters was assessed by using experimental urine levels and urine bactericidal titers determined up to 72 h after a 400-mg single dose of two quinolones in a phase I study. The area under the bactericidal curve (AUBC) was accurately predicted for norfloxacin but significantly (P < 0.001) underestimated for rufloxacin (actual value was four times higher than the predicted value against Escherichia coli and two times higher against Staphylococcus aureus). In vitro susceptibility differences between the two strains predicted the ex vivo AUBC differences for norfloxacin but not for rufloxacin, where ex vivo differences were greater than expected. Urine bactericidal titers for up to 72 h were accurately predicted for norfloxacin against E. coli and S. aureus and for rufloxacin against S. aureus, but experimental activity for up to 48 h was four times higher (P < 0.001) than the predicted activity for rufloxacin against E. coli. In the case of norfloxacin, the duration of adequate urine antibacterial activity against S. aureus was overestimated. Inaccurate estimations of ex vivo antibacterial activity of a suspected active metabolite (as with rufloxacin) when an adequate cutoff is not established may have dosing implications.

2016 ◽  
Vol 5 (04) ◽  
pp. 4512
Author(s):  
Jackie K. Obey ◽  
Anthoney Swamy T* ◽  
Lasiti Timothy ◽  
Makani Rachel

The determination of the antibacterial activity (zone of inhibition) and minimum inhibitory concentration of medicinal plants a crucial step in drug development. In this study, the antibacterial activity and minimum inhibitory concentration of the ethanol extract of Myrsine africana were determined for Escherichia coli, Bacillus cereus, Staphylococcus epidermidis and Streptococcus pneumoniae. The zones of inhibition (mm±S.E) of 500mg/ml of M. africana ethanol extract were 22.00± 0.00 for E. coli,20.33 ±0.33 for B. cereus,25.00± 0.00 for S. epidermidis and 18. 17±0.17 for S. pneumoniae. The minimum inhibitory concentration(MIC) is the minimum dose required to inhibit growth a microorganism. Upon further double dilution of the 500mg/ml of M. africana extract, MIC was obtained for each organism. The MIC for E. coli, B. cereus, S. epidermidis and S. pneumoniae were 7.81mg/ml, 7.81mg/ml, 15.63mg/ml and 15.63mg/ml respectively. Crude extracts are considered active when they inhibit microorganisms with zones of inhibition of 8mm and above. Therefore, this study has shown that the ethanol extract of M. africana can control the growth of the four organisms tested.


Author(s):  
Lina Y Alkaissi ◽  
Martin E Winberg ◽  
Stéphanie DS Heil ◽  
Staffan Haapaniemi ◽  
Pär Myrelid ◽  
...  

Abstract Background The first visible signs of Crohn’s disease (CD) are microscopic erosions over the follicle-associated epithelium (FAE). The aim of the study was to investigate the effects of human α-defensin 5 (HD5) on adherent-invasive Escherichia coli LF82 translocation and HD5 secretion after LF82 exposure in an in vitro model of human FAE and in human FAE ex vivo. Methods An in vitro FAE-model was set up by the coculture of Raji B cells and Caco-2-cl1 cells. Ileal FAE from patients with CD and controls were mounted in Ussing chambers. The effect of HD5 on LF82 translocation was studied by LF82 exposure to the cells or tissues with or without incubation with HD5. The HD5 secretion was measured in human FAE exposed to LF82 or Salmonella typhimurium. The HD5 levels were evaluated by immunofluorescence, immunoblotting, and ELISA. Results There was an increased LF82 translocation across the FAE-model compared with Caco-2-cl1 (P &lt; 0.05). Incubation of cell/tissues with HD5 before LF82 exposure reduced bacterial passage in both models. Human FAE showed increased LF82 translocation in CD compared with controls and attenuated passage after incubation with sublethal HD5 in both CD and controls (P &lt; 0.05). LF82 exposure resulted in a lower HD5 secretion in CD FAE compared with controls (P &lt; 0.05), whereas Salmonella exposure caused equal secretion on CD and controls. There were significantly lower HD5 levels in CD tissues compared with controls. Conclusions Sublethal HD5 reduces the ability of LF82 to translocate through FAE. The HD5 is secreted less in CD in response to LF82, despite a normal response to Salmonella. This further implicates the integrated role of antimicrobial factors and barrier function in CD pathogenesis.


2021 ◽  
Author(s):  
Allyson E. Shea ◽  
Jolie A. Stocki ◽  
Stephanie D. Himpsl ◽  
Sara N. Smith ◽  
Harry L. T. Mobley

Uropathogenic Escherichia coli (UPEC) causes the majority of uncomplicated urinary tract infections (UTI), which affect nearly half of women worldwide. Many UPEC strains encode an annotated intimin-like adhesin ( ila ) locus in their genome related to a well-characterized virulence factor in diarrheagenic E. coli pathotypes. Its role in UPEC uropathogenesis, however, remains unknown. In prototype UPEC strain CFT073, there is an ila locus that encodes three predicted intimin-like genes sinH , sinI , and ratA . We used in silico approaches to determine the phylogeny and genomic distribution of this locus among uropathogens. We found that the currently annotated intimin-encoding proteins in CFT073 are more closely related to invasin proteins found in Salmonella . Deletion of the individual sinH , sinI , and ratA genes did not result in measurable effects on growth, biofilm formation, or motility in vitro . On average, sinH was more highly expressed in clinical strains during active human UTI than in human urine ex vivo . Unexpectedly, we found that strains lacking this ila locus had increased adherence to bladder cells in vitro , coupled with a decrease in bladder cell invasion and death. The sinH mutant displayed a significant fitness defect in the murine model of ascending UTI including reduced inflammation in the bladder. These data confirmed an inhibitory role in bladder cell adherence to facilitate invasion and inflammation; therefore, the ila locus should be termed invasin-like, rather than intimin-like. Collectively, our data suggest that loss of this locus mediates measurable interactions with bladder cells in vitro and contributes to fitness during UTI.


2021 ◽  
Vol 74 (9) ◽  
pp. 2109-2111
Author(s):  
Evheniia A. Shtaniuk ◽  
Oleksandra O. Vovk ◽  
Larisa V. Krasnikova ◽  
Yuliia I. Polyvianna ◽  
Tetiana I. Kovalenko

The aim: Study of antibacterial activity of the preparations, containing antiseptic dioxidine and antibiotic levofloxacin in vitro on standard strains of main optional-anaerobic pathogens of purulent-inflammatory processes of surgical wounds S. aureus, E. coli, P. aeruginosa and definition of more effective ones on them. Materials and methods: Solutions of dioxidine 1.2 %, dioxidine 1.2% with decamethaxin, Dioxisole, water soluble ointment with dioxidine 1.2% and levofloxacin 0.1% with decamethaxin were used in experiment. Antibacterial activity was studied on standard strains of S. aureus АТСС 25923, E. coli АТСС 25922, P. aeruginosa АТСС 27853. Distinguishing and identification of pure cultures of bacteria was done according to generally accepted microbiological methods. Determination of purulent-inflammatory processes pathogens sensitivity was done by disco-diffuse method on Mueller-Hinton medium. Antibacterial activity of solutions and ointments was studied with the help of agar diffusion method (“well” method) according to methodic recommendations. Each investigation was repeated 6 times. Method of variation statistics was used for the research results analysis. Results: All antibacterial preparations under study are effective and highly effective on S. aureus АТСС 25923, E. coli АТСС 25922, P. aeruginosa АТСС 27853. Solution with 1.2 % dioxidine with decamethaxin and ointment with 0.1 % levofloxacin and decamethaxin have larger growth retardation zones towards S. aureus and P. aeruginosa. E. coli strains are more sensitive to the solution of Dioxisole and ointment with 1.2 % dioxidine. Conclusions: All strains are sensitive, most of them are highly sensitive, up to 5 antibacterial preparations under study in vitro.


2002 ◽  
Vol 1 (2) ◽  
pp. 100-106
Author(s):  
M. Zakir Sultan ◽  
Naznin Ara Khatune ◽  
Zakia Sultana Sathi ◽  
Md. Shah Alam Bhuiyan ◽  
M. Golam Sadik ◽  
...  

2019 ◽  
Vol 24 ◽  
pp. 2515690X1988627 ◽  
Author(s):  
Mekonnen Sisay ◽  
Negussie Bussa ◽  
Tigist Gashaw ◽  
Getnet Mengistu

Medicinal plants are targeted in the search for new antimicrobial agents. Nowadays, there is an alarmingly increasing antimicrobial resistance to available agents with a very slow development of new antimicrobials. It is, therefore, necessary to extensively search for new agents based on the traditional use of herbal medicines as potential source. The antibacterial activity of 80% methanol extracts of the leaves of Verbena officinalis (Vo-80ME), Myrtus communis (Mc-80ME), and Melilotus elegans (Me-80ME) was tested against 6 bacterial isolates using agar well diffusion technique. In each extract, 3 concentrations of 10, 20, and 40 mg/well were tested for each bacterium. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were also determined. Vo-80ME and Mc-80ME exhibited promising antibacterial activity against Staphylococcus aureus with the highest zone of inhibition being 18.67 and 26.16 mm, respectively at concentration of 40 mg/well. Regarding gram-negative bacteria, Vo-80ME exhibited an appreciable activity against Escherichia coli and Salmonella typhi. Mc-80ME displayed remarkable activity against all isolates including Pseudomonas aeruginosa with the maximum zone of inhibition being 22.83 mm. Me-80ME exhibited better antibacterial activity against E coli, but its secondary metabolites had little or no activity against other gram-negative isolates. The MIC values of Vo-80ME ranged from 0.16 to 4.00 mg/mL. The lowest MIC was observed in Mc-80ME, with the value being 0.032 mg/mL. Mc-80ME had bactericidal activity against all tested bacterial isolates. Mc-80ME showed remarkable zone of inhibitions in all tested bacterial isolates. Besides, Vo-80ME showed good antibacterial activity against S aureus, E coli, and S typhi. Conversely, Me-80ME has shown good activity against E coli only. Generally, M communis L and V officinalis have good MIC and MBC results.


2020 ◽  
Vol 2020 ◽  
pp. 1-13 ◽  
Author(s):  
Naheed Zafar ◽  
Bushra Uzair ◽  
Muhammad Bilal Khan Niazi ◽  
Shamaila Sajjad ◽  
Ghufrana Samin ◽  
...  

Treatment of pandrug resistant (PDR) Escherichia coli strain is the leading causative agent of bovine mastitis worldwide. Hence, becoming a potential threat to veterinary and public health. Therefore, to control the infection new nontoxic, biocompatible antimicrobial formulation with enhanced antibacterial activity is massively required. Current study was planned to synthesize chitosan coated titanium dioxide nanoparticles (CS-NPs coated TiO2). Coating was being done by chitosan nanoparticles (CS-NPs) using ionic gelation method. Aqueous solution of Moringa concanensis leaf extract was used to synthesize titanium dioxide nanoparticles (TiO2 NPs). The synthesized nanoformulations were characterized by using XRD, SEM, and FTIR. X-ray diffraction (XRD) analysis indicated the crystalline phase of TiO2 NPs and CS-NPs coated TiO2 NPs. Scanning Electron Microscopy (SEM) confirmed spherical shaped nanoparticles size of chitosan NPs ranging from 19–25 nm and TiO2 NPs 35–50 nm. Thesize of CS-NPs coated TiO2 NPs was in the range of 65–75 nm. The UV-Vis Spectra and band gap values illustrated the red shift in CS-NPs coated TiO2 NPs. Fourier transform infrared (FTIR) spectroscopy confirmed the linkages between TiO2 NPs and chitosan biopolymer, Zeta potential confirmed the stability of CS-NPs coated TiO2 NPs by showing 95 mV peak value. In-vitro antibacterial activity of CS-NPs coated TiO2 NPs and Uncoated TiO2 NPs was evaluated by disc diffusion method against PDR strain of E. coli isolated from mastitic milk samples. The antibacterial activity of all the synthesized nanoformulations were noted and highest antibacterial activity was shown by CS-NPs coated TiO2-NPs against pandrug resistant (PDR) E. coli strain with the prominent zone of inhibition of 23 mm. Morphological changes of E. coli cells after the treatment with MIC concentration (0.78 μg/ml) of CS-NPs coated TiO2 NPs were studied by transmission electron microscopy TEM showedrigorous morphological defectand has distorted the general appearance of the E. coli cells. Cytotoxicity (HepG2 cell line) and hemolytic (human blood) studies confirmed nontoxic/biocompatible nature of CS-NPs coated biologically synthesized TiO2 NPs. The results suggested that biologically synthesized and surface modified TiO2 NPs by mucoadhesive polysaccharides (e.g. chitosan) coating would be an effective and non-toxic alternative therapeutic agent to be used in livestock industry to control drug resistant veterinary pathogens.


2005 ◽  
Vol 73 (9) ◽  
pp. 6005-6016 ◽  
Author(s):  
Francis Girard ◽  
Isabelle Batisson ◽  
Gad M. Frankel ◽  
Josée Harel ◽  
John M. Fairbrother

ABSTRACT The ileal in vitro organ culture (IVOC) model using tissues originating from colostrum-deprived newborn piglets has proven to be an effective way to study the attaching and effacing (A/E) phenotype of porcine enteropathogenic Escherichia coli (EPEC) ex vivo. The aim of this study was to investigate the role of intimin subtype and Tir in the adherence of EPEC and Shiga-toxin-producing E. coli (STEC), isolated from different animal species, to porcine intestinal IVOC. Moreover, the role of intimin in Tir-independent adherence of the human EPEC strain E2348/69 was investigated using intimin and Tir-deficient derivatives. Our results demonstrated that A/E E. coli strains (AEEC) from various animal species and humans induce the A/E phenotype in porcine ileal IVOC and that intimin subtype influences intestinal adherence and tropism of AEEC strains. We also showed that a tir mutant of EPEC strain E2348/69 demonstrates close adherence to the epithelial cells of porcine ileal IVOC segments, with microvillous effacement but with no evidence of actin polymerization or pedestal formation, and that intimin seems to be involved in this phenotype. Overall, this study provides further evidence for the existence of one or more host-cell-encoded intimin receptor(s) in the pig gut.


Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2126 ◽  
Author(s):  
Alla V. Lipeeva ◽  
Danila O. Zakharov ◽  
Liubov G. Burova ◽  
Tatyana S. Frolova ◽  
Dmitry S. Baev ◽  
...  

Synthesis of 1,2,3-triazole-substituted coumarins and also 1,2,3-triazolyl or 1,2,3-triazolylalk-1-inyl-linked coumarin-2,3-furocoumarin hybrids was performed by employing the cross-coupling and copper catalyzed azide-alkyne cycloaddition reaction approaches. The synthesized compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus, Bacillius subtilis, Actinomyces viscosus and Escherichia coli bacterial strains. Coumarin-benzoic acid hybrids 4с, 42с and 3-((4-acetylamino-3-(methoxycarbonyl)phenyl)ethynyl)coumarin (29) showed promising activity against S. aureus strains, and the 1,2,3-triazolyloct-1-inyl linked coumarin-2,3-furocoumarin hybrid 37c was endowed with high selectivity against B. subtilis and E. coli species. The in vitro antibacterial activity of 4с, 29, 37c and 42с can potentially be compared with that of a number of modern antibiotic drugs used in the clinic, suggesting promising prospects for further research. A detailed study of the molecular interactions with the targeted protein MurB was performed using docking simulations and the obtained results are quite promising.


2016 ◽  
Vol 87 (11) ◽  
pp. 1377-1386 ◽  
Author(s):  
Xihui Zhao ◽  
Qun Li ◽  
Xiaowen Li ◽  
Yanzhi Xia ◽  
Bing Wang ◽  
...  

Biopolymer nanocomposites containing metal nanoparticles have attracted much attention due to their excellent properties and broad applications. In this work, alginate fibers embedded with silver nanoparticles (AgNPs) were prepared. The as-obtained alginate-AgNP fibers exhibited antibacterial activity against both Gram microorganisms of model microbes Escherichia coli (Gram-negative) and Staphylococcus aureus (Gram-positive). A growth kinetic study with S. aureus and E. coli displayed the inhibition of bacterial growth at the logarithmic phase. The cytotoxic effect of the fibers in human cervical cancer (HeLa) cells was assessed by cell counting kit-8 (CCK-8) assay and flow cytometry. The as-prepared alginate-AgNP fibers, particularly with high amount and long treatment time, showed high cell-killing efficiency. These findings emphasize that such alginate-AgNP fibers with multifaceted biological activities are a promising material for applications in the textile or biomedical fields.


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