scholarly journals Antimicrobial Activities of Daptomycin, Vancomycin, and Oxacillin in Human Monocytes and of Daptomycin in Combination with Gentamicin and/or Rifampin in Human Monocytes and in Broth against Staphylococcus aureus

2007 ◽  
Vol 51 (4) ◽  
pp. 1559-1562 ◽  
Author(s):  
Aldona L. Baltch ◽  
William J. Ritz ◽  
Lawrence H. Bopp ◽  
Phyllis B. Michelsen ◽  
Raymond P. Smith
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Drug Combination ◽  
Human Monocyte ◽  
Antimicrobial Activities ◽  
Human Monocytes ◽  
Antistaphylococcal Activity

ABSTRACT We investigated the antistaphylococcal activity of daptomycin, vancomycin, oxacillin, gentamicin, and rifampin in human monocyte-derived macrophages. Compared with vancomycin and oxacillin, daptomycin had the most rapid and greatest antibacterial activity, but that of oxacillin was most sustained. The combination of daptomycin, gentamicin, and rifampin was most effective intracellularly, while daptomycin plus gentamicin and the three-drug combination were most effective extracellularly, completely eliminating viable Staphylococcus aureus.

scholarly journals Synthesis and antimicrobial activities of novel n-substituted 8-(1-alkyl/alkylsulphonyl/alkoxycarbonyl-benzimidazol-2-ylmethoxy)-5-chloroquinolines

2011 ◽  
Vol 76 (9) ◽  
pp. 1199-1206 ◽  
Author(s):  
Raju Chaudhari ◽  
Sahebrao Rindhe
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Nitrogen Heterocycles ◽  
Antimicrobial Activities ◽  
Mass Spectral Data ◽  
Antifungal Activities ◽  
Mass Spectral ◽  
Electrophilic Reagents ◽  
Almost All ◽  
And Staphylococcus Aureus

Herein the synthesis of a series of novel 8-(1- alkyl/alkylsulphonyl/alkoxycarbonyl-benzimidazol-2-ylmethoxy)-5- chloroquinoline derivatives is reported. These derivatives were prepared by the condensation of o-phenylenediamine with [(5-chloroquinolin-8- yl)oxy]acetic acid, followed by substitution at nitrogen with different electrophilic reagents in presence of an appropriate base to give a series of nitrogen heterocycles containing the benzimidazole and quinoline nuclei. The structures of the compounds were confirmed based on 1H-NMR, 13CNMR, IR and mass spectral data. Almost all the compounds exhibited promising antibacterial activity against Salmonella typhimurium and Staphylococcus aureus. Some of the compounds showed good antifungal activities against Aspergillus niger but the antifungal activities against Candida albicans were disappointing.

scholarly journals Antibacterial Effects of Levofloxacin, Erythromycin, and Rifampin in a Human Monocyte System againstLegionella pneumophila

1998 ◽  
Vol 42 (12) ◽  
pp. 3153-3156 ◽  
Author(s):  
Aldona L. Baltch ◽  
Raymond P. Smith ◽  
Mary A. Franke ◽  
Phyllis B. Michelsen
Keyword(s):  
Antibacterial Activity ◽  
Legionella Pneumophila ◽  
Human Monocyte ◽  
Antibacterial Activities ◽  
Human Monocytes ◽  
Antibacterial Effects ◽  
In Vitro System ◽  
Time Period ◽  
Time Periods

ABSTRACT The antibacterial activities of levofloxacin, erythromycin, and rifampin against intracellular Legionella pneumophilaL-1033, serogroup 1, were studied. In an in vitro system utilizing adherent human monocytes, L. pneumophila L-1033, a phagocytosis time period of 1 h, and antibiotic (levofloxacin, erythromycin, and/or rifampin) at 1 to 10 times the MIC, the CFU/ml values for the monocyte lysate were determined during 0- to 4-day time periods. The decrease in CFU/ml with levofloxacin at pH 7.4 was rapid, occurring within 24 h, and was drug concentration dependent (P < 0.01). The decrease in CFU with rifampin was first observed at 48 h (P < 0.01), while only a minimal decrease in CFU/ml was observed with erythromycin. Combination of levofloxacin and rifampin and of levofloxacin and erythromycin at ten times their MICs significantly decreased the CFU/ml value (P < 0.01), to the value attained by levofloxacin alone, while combination of rifampin and erythromycin did not. Removal of levofloxacin after 24 h of incubation resulted in regrowth ofL. pneumophila L-1033, while a continued slow decrease in CFU/ml was seen following rifampin removal; CFU/ml values were unaffected by the removal of erythromycin. At 4 days, and even in assays performed following antibiotic removal, the CFU/ml value continued to be lower in the levofloxacin and rifampin assays than in the assays with erythromycin. Levofloxacin had a significantly higher bactericidal activity against L. pneumophila L-1033 than erythromycin or rifampin. In these assays, the addition of erythromycin or rifampin did not affect the antibacterial activity of levofloxacin.

scholarly journals Synthesis of New Oxindoles and Determination of Their Antibacterial Properties

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Pablo E. Romo ◽  
Braulio Insuasty ◽  
Rodrigo Abonia ◽  
María del Pilar Crespo ◽  
Jairo Quiroga
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Neisseria Gonorrhoeae ◽  
Room Temperature ◽  
Antibacterial Properties ◽  
Analytical Techniques ◽  
Toluenesulfonic Acid ◽  
Antistaphylococcal Activity ◽  
New Compounds

A versatile method for the synthesis of new oxindoles was developed by the reaction between substituted isatins and 5-aminopyrazoles. The reaction was carried out at room temperature in ethanol using p-toluenesulfonic acid as the catalyst. The products were obtained with acceptable to excellent yields (44–96%). Structures of the new compounds were unambiguously established by spectroscopic and analytical techniques. The antibacterial activity was determined by microdilution assays. Compounds 3b, 3e, and 3g showed antistaphylococcal activity, particularly compound 3e displayed a potent activity against the vancomycin intermediate Staphylococcus aureus (VISA). Compounds 3i, 3j, and 3o inhibited Neisseria gonorrhoeae growth.

scholarly journals Characterization and Antimicrobial Activity of Erbium(III) Complexes of C-3 Substituted 2-hydroxy-1,4-naphthalenedione-1-oxime Derivatives

2001 ◽  
Vol 8 (3) ◽  
pp. 159-164 ◽  
Author(s):  
S. B. Jagtap ◽  
N. N. Patil ◽  
B. P. Kapadnis ◽  
B. A. Kulkarni
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Magnetic Susceptibility ◽  
Candida Albicans ◽  
Xanthomonas Campestris ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Oxime Derivatives

Erbium(III) complexes of 2-hydroxy-l,4-naphthalenedione-1-oxime and its C-3 substituted derivatives are synthesized and characterized by elemental analysis, thermogravimetric analysis, infrared spectroscopy, magnetic susceptibility measurements 2-hydroxy-1,4-naphthalenedione-1-oxime derivatives are analysed using H1 and C13 NMR spectroscopy. The molecular composition of the synthesized complexes is found to be [ML3(H2O)2]. The antimicrobial activity of these complexes is determined by well diffusion method against the target microorganisms- Staphylococcus aureus, Xanthomonas campestris, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger. The antimicrobial activities of 2- hydroxy-1,4-naphthalenedione-1-oximes and their complexes are compared. It is observed that 2-hydroxy-1,4-naphthalenedione-l-oximes exhibit higher antifungal activity as compared to antibacterial activity. These activities are reduced upon complexation of these oximes with Erbium.

Synthesis and Antimicrobial Evaluation of Amino Acid Naphthoquinone Derivatives as Potential Antibacterial Agents

Chemotherapy ◽  
2021 ◽  
Author(s):  
Lluvia Itzel López-López ◽  
Ernesto Rivera-Ávalos ◽  
Cecilia Villarreal-Reyes ◽  
Fidel Martínez-Gutiérrez ◽  
Denisse de Loera
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Amino Acid ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Culture Collection ◽  
Anticancer Activities ◽  
Broth Microdilution Method

Background: The synthesis and biological evaluation of 1,4-naphthoquinone derivatives are of great interest since these compounds exhibit strong antibacterial, antifungal, antimalarial, and anticancer activities. The electronic properties of naphthoquinones are usually modulated by attaching functional groups containing nitrogen, oxygen and sulfur atoms, which tune their biological potency and selectivity. Methods: A series of 13 amino acid 1,4-naphthoquinone derivatives were synthesized under assisted microwave and ultrasound conditions. The antibacterial activity compounds was tested against American type Culture Collection (ATCC): Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Enterococcus faecalis, as well two multidrug resistant pathogens: Escherichia coli and Staphylococcus aureus from clinical isolated. Minimal inhibitory concentration (MIC) was determined using the broth microdilution method. Results: MIC of derivatives 4–11, 14 and 16 showed antimicrobial activity against gram-positive and gram-negative bacteria. Antimicrobial activities of the compounds 4–8 and 14 were ≤MIC 24.7 μg∙mL-1 against all the reference strain, even more the compound 6 showed the most potent activity with a MIC of 3.9 μg∙mL-1 on S. aureus. On the clinical isolated the compounds 7, 8 and 14 showed a MIC of 49.7 and 24.7 μg∙mL-1 against S. aureus y E. coli respectively. About ADME properties and Osiris analysis, the compounds 4-16 presented high gastrointestinal absorption and good characteristics for oral bioavailability and the compound 14 was the less toxic. Conclusion: amino acid 1,4-naphthoquinone derivatives showed good in vitro antibacterial activity against clinical strains, and modifications on C-3 with cloride atom enhanced the efficiency against same pathogens.

scholarly journals Enhancing the Solubility of Curcumin Metal Complexes and Investigating Some of Their Biological Activities

2019 ◽  
Vol 2019 ◽  
pp. 1-8 ◽  
Author(s):  
Tran Quang Hieu ◽  
Doan Thi Thanh Thao
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Zinc Complex ◽  
Biological Activities ◽  
Tween 80 ◽  
Antimicrobial Activities ◽  
Maximum Solubility ◽  
Optimum Parameters ◽  
Complexes With Metal Ions

This article describes the synthesis of curcumin complexes with metal ions. Properties of these complexes such as spectra IR and UV-Vis and solubility were investigated. The optimum parameters of ultrasound to enhance the solubility was figured out as follows: the capacity of ultrasound: 750 W/g; the time of ultrasound: 7 min; the concentration of the surfactant Tween 80 : 2%. The maximum solubility (mg/ml) of complexes was as follows: Cur-Fe(III): 0.162 ± 0.01; Cur-Zn(II): 0.267 ± 0.02; and Cur-Ca(II): 0.417 ± 0.05. Antioxidant capacity (DPPH, %I) of curcumin complexes was higher than that of curcumin-free complexes. All of these curcumin complexes revealed antimicrobial activities, in which calcium complex had the best resistance against Salmonella, followed by Fe(III) complexes. Meanwhile, the zinc complex was not resistant to this bacterium. These complexes showed antibacterial activity on Staphylococcus aureus, in which Cur-Ca (II) complexes had the highest antibacterial activity. For Escherichia coli, the Cur-Zn (II) complex had no resistance, while the Cur-Ca (II) complex showed the highest antibacterial activity.

scholarly journals Activities of Daptomycin and Comparative Antimicrobials, Singly and in Combination, against Extracellular and Intracellular Staphylococcus aureus and Its Stable Small-Colony Variant in Human Monocyte-Derived Macrophages and in Broth

2008 ◽  
Vol 52 (5) ◽  
pp. 1829-1833 ◽  
Author(s):  
Aldona L. Baltch ◽  
William J. Ritz ◽  
Lawrence H. Bopp ◽  
Phyllis Michelsen ◽  
Raymond P. Smith
Keyword(s):  
Staphylococcus Aureus ◽  
Drug Combination ◽  
Human Monocyte ◽  
Drug Combinations ◽  
Small Colony Variants ◽  
Small Colony Variant ◽  
Small Colony

ABSTRACT We investigated the antistaphylococcal activities of daptomycin, gentamicin, and rifampin against two Staphylococcus aureus strains and their stable small-colony variants, singly and in combination, in human monocyte-derived macrophages and in broth. Intracellularly, the three-drug combination and two-drug combinations with rifampin were most effective. Extracellularly, daptomycin, daptomycin plus gentamicin, gentamicin plus rifampin, and the three-drug combination had similar activities.

scholarly journals Antimicrobial activity of essential oils extracted from leaves of native Moroccan plants against clinical bacterial isolates

10.3823/819 ◽  
2018 ◽  
Vol 8 (1) ◽  
Author(s):  
Fatima El Malki ◽  
Kamal Eddaraji ◽  
Rajae Alloudane ◽  
Hassane Greche ◽  
Haiat Essalmani ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Essential Oils ◽  
Bactericidal Effect ◽  
Antimicrobial Activities ◽  
Acinetobacter Baumanii ◽  
And Staphylococcus Aureus

Introduction: Medicinal plants are plentiful of bioactive molecules effective against multi-resistance bacteria. The aims of this study were to assess the in vitro antimicrobial activities of essential oils extracted from three Moroccan aromatic plants. Methodology: Analysis of essential oils of Origanum compactum, Rosmarinus officinalis and Pelargonium asperum, collected from different localities in Morocco, were performed using a GC-MS spectrophotometry. Antibacterial activity was evaluated in vitro for five clinical multi-resistant isolates. Results: Origanum showed strong antibacterial activity against tested strains except Pseudomonas aeruginosa while Rosmarinum showed a bactericidal effect against Acinetobacter baumanii, Escherichia coli and Staphylococcus aureus. Pelargonium presented only slight growth inhibition of Staphylococcus aureus on solid medium, but provided bactericidal effect against Acinetobacter baumanii and Staphylococcus aureus. Interestingly, fractions F7 and F8 of Pelargonium which represented only 0.3% and 0.1% of the total mass were found bactericidal respectively against Klebsiella pneumoniae and Pseudomonas aeruginosa. Conclusions: Ours results showed that the antimicrobial activities were variables depending on the chemical composition of essential oils, the fraction used and the microorganism tested.Essential oils fractionation allows detection of bioactive substances, especially those owning antimicrobial activity, present in small quantities.

scholarly journals Antimicrobial Activities of BMS-284756 Compared with Those of Fluoroquinolones and β-Lactams against Gram-Positive Clinical Isolates

2002 ◽  
Vol 46 (1) ◽  
pp. 234-238 ◽  
Author(s):  
Matteo Bassetti ◽  
Louise M. Dembry ◽  
Patricia A. Farrel ◽  
Deborah A. Callan ◽  
Vincent T. Andriole
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Active Agent ◽  
Antimicrobial Activities ◽  
Clinical Isolates ◽  
Coagulase Negative Staphylococci ◽  
Gram Positive ◽  
Amoxicillin Clavulanic Acid ◽  
In Vitro Antibacterial Activity

ABSTRACT The in vitro antibacterial activity of BMS-284756 was compared to those of ciprofloxacin, gatifloxacin, moxifloxacin, ceftriaxone, imipenem, piperacillin-tazobactam, and amoxicillin-clavulanic acid against 492 gram-positive clinical isolates. BMS-284756 was the most-active agent against Streptococcus pneumoniae, Streptococcus viridans, beta-hemolytic streptococci, methicillin-sensitive and -resistant Staphylococcus aureus, methicillin-sensitive and -resistant coagulase-negative staphylococci, and enterococci.

scholarly journals Degradation of Human Antimicrobial Peptide LL-37 by Staphylococcus aureus-Derived Proteinases

2004 ◽  
Vol 48 (12) ◽  
pp. 4673-4679 ◽  
Author(s):  
Magdalena Sieprawska-Lupa ◽  
Piotr Mydel ◽  
Katarzyna Krawczyk ◽  
Kinga Wójcik ◽  
Magdalena Puklo ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Innate Immune System ◽  
Peptide Bond ◽  
Innate Immune ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Peptide Bonds ◽  
Antistaphylococcal Activity ◽  
Initial Cleavage

ABSTRACT Cathelicidin LL-37 is one of the few human bactericidal peptides with potent antistaphylococcal activity. In this study we examined the susceptibility of LL-37 to proteolytic degradation by two major proteinases produced by Staphylococcus aureus, a metalloproteinase (aureolysin) and a glutamylendopeptidase (V8 protease). We found that aureolysin cleaved and inactivated LL-37 in a time- and concentration-dependent manner. Analysis of the generated fragments by mass spectroscopy revealed that the initial cleavage of LL-37 by aureolysin occurred between the Arg19-Ile20, Arg23-Ile24, and Leu31-Val32 peptide bonds, instantly annihilating the antibacterial activity of LL-37. In contrast, the V8 proteinase hydrolyzed efficiently only the Glu16-Phe17 peptide bond, rendering the C-terminal fragment refractory to further degradation. This fragment (termed LL-17-37) displayed antibacterial activity against S. aureus at a molar level similar to that of the full-length LL-37 peptide, indicating that the antibacterial activity of LL-37 resides in the C-terminal region. In keeping with LL-37 degradation by aureolysin, S. aureus strains that produce significant amounts of this metalloprotease were found to be less susceptible to LL-17-37 than strains expressing no aureolysin activity. Taken together, these data suggest that aureolysin production by S. aureus contributes to the resistance of this pathogen to the innate immune system of humans mediated by LL-37.

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