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1.
Viruses ; 13(10)2021 09 25.
Article in English | MEDLINE | ID: mdl-34696362

ABSTRACT

Modern bacteriophage encapsulation methods based on polymers such as alginate have been developed recently for their use in phage therapy for veterinary purposes. In birds, it has been proven that using this delivery system allows the release of the bacteriophage in the small intestine, the site of infection by Salmonella spp. This work designed an approach for phage therapy using encapsulation by ionotropic gelation of the lytic bacteriophage S1 for Salmonella enterica in 2% w/v alginate beads using 2% w/v calcium chloride as crosslinking agent. This formulation resulted in beads with an average size of 3.73 ± 0.04 mm and an encapsulation efficiency of 70%. In vitro, the beads protected the bacteriophages from pH 3 and released them at higher pH. To confirm that this would protect the bacteriophages from gastrointestinal pH changes, we tested the phage infectivity in vivo assay. Using a model chicken (Gallus gallus domesticus) infected with Salmonella Enteritidis, we confirmed that after 3 h of the beads delivery, infective phages were present in the chicken's duodenal and caecal sections. This study demonstrates that our phage formulation is an effective system for release and delivery of bacteriophage S1 against Salmonella Enteritidis with potential use in the poultry sector.


Subject(s)
Phage Therapy/methods , Salmonella Phages/metabolism , Alginates/chemistry , Animals , Bacteriophages , Cecum/metabolism , Cell Encapsulation/methods , Chickens/microbiology , Gastrointestinal Tract/metabolism , Microspheres , Poultry/virology , Salmonella Phages/genetics , Salmonella enterica/metabolism , Salmonella enterica/virology
2.
Nat Prod Commun ; 9(10): 1449-55, 2014 Oct.
Article in English | MEDLINE | ID: mdl-25532220

ABSTRACT

Five hydrazone derivatives of streptomycin were synthetized (D0h, D1ph, D2bt, D3dctf, D4ag) and characterized by IR, 1H and 13C NMR spectroscopy, mass spectrometry and elemental analysis. Protonation constants were determined by potentiometry for all derivatives. D1ph and D2bt derivatives were investigated as receptors of dicarboxylates and adenine nucleotides in aqueous solution by potentiometric and 1H NMR titrations. D1ph and D2bt derivatives have the highest affinity with AMP and ATP, respectively, which shows that electrostatic forces are not always the dominant factor in binding of streptomycin derivatives with nucleotides, but the conformational fit between them. Calculated structures at the DFT level of the D1ph derivative bonded with either AMP or ADP showed that the complexes are stabilized by the formation of multiple interactions with the receptors. The antibiotic activity of the derivatives was explored and compared with native streptomycin.


Subject(s)
Hydrazones/chemistry , Streptomycin/chemistry , Magnetic Resonance Spectroscopy
3.
Bioorg Med Chem ; 21(15): 4550-8, 2013 Aug 01.
Article in English | MEDLINE | ID: mdl-23787289

ABSTRACT

In our search for new antiamoebic agents, a new series of ethyl and methyl quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives have been synthesized using the Beirut reaction. All compounds were characterized by spectroscopic techniques and elemental analysis. Antiamoebic activity was evaluated in vitro against Entamoeba histolytica strain HM1:IMSS by the microdilution method, and the structure-activity relationship was analyzed. We found that eleven quinoxaline derivatives showed greater activity than metronidazole and nitazoxanide with IC50 values in the range 1.99-0.35 µM. Compounds T-001 and T-016 shows IC50 values of 1.41 and 1.47 µM, respectively, with a value of selectivity index >60.


Subject(s)
Antiprotozoal Agents/chemistry , Antiprotozoal Agents/pharmacology , Entamoeba histolytica/drug effects , Quinoxalines/chemistry , Quinoxalines/pharmacology , Antiprotozoal Agents/chemical synthesis , Cyclic N-Oxides/chemical synthesis , Cyclic N-Oxides/chemistry , Cyclic N-Oxides/pharmacology , Models, Molecular , Molecular Structure , Quinoxalines/chemical synthesis , Spectrum Analysis , Structure-Activity Relationship
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