ABSTRACT
An 11-month-old infant was hospitalized for his first episode of severe bronchiolitis, with pneumomediastinum on the chest x-ray performed in the emergency room before hospitalization. After a few days, the occurrence of a feverish torticollis motivated a CT scan, revealing mediastinitis. An iatrogenic perforation was objectified in the posterior wall of the esophagus, probably caused by nasopharyngeal aspiration. This exceptional case has never been reported before, except in premature infants. This encouraged us to report this case to change systematic aspiration practices and prefer nasal suctioning in healthy infants with bronchiolitis presenting to the emergency department.
Subject(s)
Bronchiolitis/therapy , Esophagus/injuries , Mediastinitis/etiology , Suction/adverse effects , Humans , Infant , Male , Mediastinitis/diagnosisABSTRACT
"Purple drank" is a dangerous hallucinogenic cocktail commonly used by teenagers, made popular by American rappers and social networks. It combines codeine-based cough syrup, antihistamines such as promethazine, and soda. Unknown by caregivers, it may be responsible for serious neuropsychological complications. We report the effects of this new risky behavior in three patients: a 14-year-old girl and her boyfriend, both found in an initial state of drowsiness, followed by hallucinations and anticholinergic toxidrome; and another teenager whose chronic use led to addiction with increasing doses. It is important to identify signs of such intoxication and to inform patients about the risks of respiratory depression, drowsiness, and delirium linked to acute medication misuse.
Subject(s)
Antitussive Agents/adverse effects , Beverages/adverse effects , Codeine/adverse effects , Histamine Antagonists/adverse effects , Opioid-Related Disorders/complications , Adolescent , Anticholinergic Syndrome/etiology , Female , Hallucinations/chemically induced , Humans , MaleABSTRACT
The structural basis of the binding of the polyamine spermine to the monoclonal antibody SPM8-2 was studied using computer modelling, ELISA methods and chemical modifications of the binding site residues. Paratope modelling showed that the antibody combining site forms a highly negatively charged cavity mainly shaped by aspartic acid and tyrosine residues which contact the tetra-positively charged spermine molecule by electrostatic interactions and hydrogen bondings. The importance of the electrostatic environment for spermine binding to SPM8-2 is emphasised by the strong dependency on pH and ionic strength. Specific chemical modifications of carboxylate groups and tyrosine residues of the antibody adsorbed to microtiter plates resulted in decreased binding of the N1-biotin-spermine conjugate used to monitor the activity of the antibody. These observations are consistent with a key role of aspartate and tyrosine residues in complex formation with spermine. These studies, important to our understanding of antibody-hapten specificity, may also shed light on important motifs responsible for protein-polyamine interactions.
Subject(s)
Antibodies, Monoclonal/chemistry , Antibodies, Monoclonal/immunology , Computer Simulation , Models, Molecular , Spermine/immunology , Amino Acid Sequence , Animals , Antibody Specificity , Mice , Models, Immunological , Molecular Sequence Data , Static Electricity , Structure-Activity RelationshipABSTRACT
Using solid phase synthesis techniques, we have rapidly obtained a series of eight aryl sulphonamides derived from putrescine. These conjugates with various aryl groups were evaluated for their affinity towards 5-HT6 receptors in man. This evaluation revealed the interest of two compounds which present the same activity level, in the submicromolar range, as two reference derivatives. The most potent will be considered as a new lead for further investigations.
Subject(s)
Receptors, Serotonin/metabolism , Sulfonamides/chemical synthesis , Sulfonamides/metabolism , Humans , Ligands , Lysergic Acid Diethylamide/metabolism , Putrescine/analogs & derivatives , Putrescine/chemical synthesis , Serotonin Antagonists/metabolismABSTRACT
Seven analogues of the bacterial osmoprotectant glycine betaine (GB, trimethylammonioacetate), in which the methyl groups of the Me3N+ moiety are replaced by various substituents, were obtained by SPOS using Wang resin. Their biological activities (osmoprotection vs toxicity), appeared closely related to their uptake efficiency and their catabolism in the betaine-demethylating model bacterium Sinorhizobium meliloti.
Subject(s)
Betaine/analogs & derivatives , Betaine/pharmacology , Chemistry, Organic/methods , Osmotic Pressure/drug effects , Sinorhizobium meliloti/drug effects , Betaine/chemical synthesis , Cell Division , Escherichia coli/drug effects , Escherichia coli/physiology , Sinorhizobium meliloti/physiology , Succimer/pharmacokinetics , Succimer/pharmacologyABSTRACT
Ofloxacin (OFX) is a fluorquinolone characterized by photochemical instability. With the goal to improve its photostability in aqueous solutions, the complexation of ofloxacin with beta-cyclodextrin was investigated. The complexes showed a water solubility enhancement of approximately 2.6 times; nevertheless, the photodegradation of ofloxacin was not reduced. The complexes obtained were characterized by thermal and 1H nuclear magnetic resonance (NMR) analysis, which revealed an interaction between ofloxacin and beta-cyclodextrin. The last analysis indicated that only partial inclusion of the N-methylpiperazinyl moiety occurred, which can explain the fact that photostabilization was not improved. This partial inclusion phenomenon could be explained also by computer-aided molecular modeling.
Subject(s)
Anti-Infective Agents/chemistry , Cyclodextrins/chemistry , Ofloxacin/chemistry , beta-Cyclodextrins , Calorimetry, Differential Scanning , Chromatography, High Pressure Liquid , Computer Graphics , Drug Stability , Kinetics , Light , Magnetic Resonance Spectroscopy , Models, Molecular , Solubility , Ultraviolet RaysABSTRACT
A series of N1-monosubstituted putrescine and spermine derivatives was synthesised using a solid phase methodology. We evaluated their cytotoxicity, calmodulin antagonism and polyamine uptake inhibition, pharmacological properties shared by some antitumoral agents.