Cooperative Behavior of Fluoroquinolone Combinations against Escherichia coli and Staphylococcus aureus.

The effects of different combinations of ciprofloxacin (CIP) and norfloxacin (NOR) against Escherichia coli and Staphylococcus aureus were studied using checkerboard, fractional inhibitory concentration (FIC) and time-kill analysis methods. Results obtained by the checkerboard method showed that the more effectives combinations against Escherichia coli were 0.0009 µg/mL CIP+0.0312 µg/mL NOR and 0.0037 µg/mL CIP+0.0075 µg/mL NOR with a FIC index of 0.62. For Staphylococcus aureus, the combination of 0.0625 µg/mL CIP+0.2500 µg/mL NOR showed a synergistic effect, with a FIC index of 0.50. The results of the time-kill method demonstrated either indifference or additivity of the combinations 0.0009 µg/mL CIP+0.0312 µg/mL NOR, 0.0018 µg/mL CIP+0.0312 µg/mL NOR, 0.0037 µg/mL CIP+0.0075 µg/mL NOR and 0.0037 µg/mL CIP+0.0156 µg/mL NOR at 24 h against E. coli. The combination 0.0037 µg/mL CIP+0.0312 µg/mL NOR showed synergistic activity. All the analyzed combinations evidenced bactericidal effects at 4 h. The combinations 0.0625 µg/mL CIP+0.2500 µg/mL NOR and 0.0625 µg/mL CIP+0.0625 µg/mL NOR showed indifference or additivity against S. aureus. None of them generated bactericidal effect at 4 h. Moreover, this last equimolecular combination (equivalent to 1/4 minimum inhibitory concentration (MIC) CIP+1/16 MIC NOR) generated higher reduction of nitro blue tetrazolium than drugs alone. By another way, combinations not equimolecular of CIP and NOR assayed, generated less levels of reactive oxygen species (ROS) than the components alone.

Evaluation of Antibacterial Activity and Reactive Species Generation of N-Benzenesulfonyl Derivatives of Heterocycles.

Two N-benzenesulfonyl (BS) derivatives of 1,2,3,4-tetrahydroquinoline (THQ) were designed, prepared, and screened for antibacterial activity. This approach was based on combining the two privileged structures, BS and THQ, which are known to be active. The objective of this study was to evaluate the antibacterial activity of BS-THQ and its analogue 4-NH2BS-THQ, and to investigate the roles of reactive oxygen species and reactive nitrogen species in their lethality. Both showed bactericidal activity against Staphylococcus aureus ATCC 29213 and methicillin-resistant S. aureus (MRSA) ATCC 43300, with transmission electron microscopy revealing a disturbed membrane architecture. Furthermore, an increase of reactive oxygen species (ROS) in strains treated with BS-THQ with respect to the control was detected when fluorescent microscopy and spectrophotometric techniques were used. The analogue 4-NH2BS-THQ demonstrated a broader spectrum of activity than BS-THQ, with a minimum inhibitory concentration of 100 µg/mL against reference strains of S. aureus, Escherichia coli and Pseudomonas aeruginosa. The assayed compounds represent promising structures for the development of new synthetic classes of antimicrobials.

Intoxicación por plomo y su tratamiento farmacológico / Lead poisoning and pharmacological treatment

La intoxicación por plomo es un problema de saludpública. La evidencia de poblaciones afectadas por nivelestóxicos de plomo en sangre, confirma que hay que seguirtrabajando desde una visión pluridisciplinar. Es necesariodefinir políticas para la prevención, detección, diagnosticoy tratamiento de los efectos nocivos del plomo sobre lasalud. Los niños constituyen el segmento de la poblaciónmás vulnerable, con consecuencias de alto impactosocial, como una disminución del coeficiente intelectual ydeficiente desarrollo neurológico. En la práctica clínica, haycuatro medicamentos que se usan para el tratamiento de laintoxicación crónica, son el edetato cálcico disódico IV e IM,el dimercaprol IM, la penicilamina VO y el succímero VO.Si se tiene en cuenta que sólo penicilamina está autorizadaen nuestro país, el problema se torna mayor. Esta breverevisión pretende brindar información sobre la intoxicaciónpor exposición al plomo, los tratamientos recomendados ylos disponibles en nuestro país.(AU)

Lead exposure and poisoning is a public health concern.Evidence of people with toxic level of lead in blood confirmsINTOXICACION PORPLOMO Y SU TRATAMIENTOFARMACOLOGICORecibido: 25 de Setiembrede 2012. Aprobado: 4 denoviembre de 2012Lead poisoning and pharmacological treatmentFontana Daniela,Lascano Valeria María,Solá Nancy,Martinez Samanta,Virgolini Miriam,Mazzieri Maria Rosa.Departamento de Farmacia,Facultad de Ciencias Químicas,Universidad Nacional deCórdoba.Medina Allende y Haya de laTorre, Ciudad Universitaria,(5000) Córdoba, ArgentinaTEL/FAX +54 351 535 3850(int 53351). E-mail: mrmazzie@fcq.unc.edu.ar that it is necessary to keep on working from a multidisciplinary approach. There shouldbe a well-defined policy for the prevention, detection, diagnosis and treatment of theharmful effects of lead. Children are the population at major risk, with high social impactconsequences such as lower IQ and inadequate neurological development. There arefour drugs used to treat chronic toxicity: sodium calcium edetate IV and IM, succimer(oral), dimercaprol IM, and penicillamine (oral). If we consider that the last one is theonly authorized drug in our country, the problem grows bigger. This brief review offersinformation about lead exposure and poisoning, the recommended drug treatments andtheir market availability.(AU)

Intoxicación por plomo y su tratamiento farmacológico / Lead poisoning and pharmacological treatment

La intoxicación por plomo es un problema de saludpública. La evidencia de poblaciones afectadas por nivelestóxicos de plomo en sangre, confirma que hay que seguirtrabajando desde una visión pluridisciplinar. Es necesariodefinir políticas para la prevención, detección, diagnosticoy tratamiento de los efectos nocivos del plomo sobre lasalud. Los niños constituyen el segmento de la poblaciónmás vulnerable, con consecuencias de alto impactosocial, como una disminución del coeficiente intelectual ydeficiente desarrollo neurológico. En la práctica clínica, haycuatro medicamentos que se usan para el tratamiento de laintoxicación crónica, son el edetato cálcico disódico IV e IM,el dimercaprol IM, la penicilamina VO y el succímero VO.Si se tiene en cuenta que sólo penicilamina está autorizadaen nuestro país, el problema se torna mayor. Esta breverevisión pretende brindar información sobre la intoxicaciónpor exposición al plomo, los tratamientos recomendados ylos disponibles en nuestro país.

Lead exposure and poisoning is a public health concern.Evidence of people with toxic level of lead in blood confirmsINTOXICACIÓN PORPLOMO Y SU TRATAMIENTOFARMACOLOGICORecibido: 25 de Setiembrede 2012. Aprobado: 4 denoviembre de 2012Lead poisoning and pharmacological treatmentFontana Daniela,Lascano Valeria María,Solá Nancy,Martinez Samanta,Virgolini Miriam,Mazzieri Maria Rosa.Departamento de Farmacia,Facultad de Ciencias Químicas,Universidad Nacional deCórdoba.Medina Allende y Haya de laTorre, Ciudad Universitaria,(5000) Córdoba, ArgentinaTEL/FAX +54 351 535 3850(int 53351). E-mail: mrmazzie@fcq.unc.edu.ar that it is necessary to keep on working from a multidisciplinary approach. There shouldbe a well-defined policy for the prevention, detection, diagnosis and treatment of theharmful effects of lead. Children are the population at major risk, with high social impactconsequences such as lower IQ and inadequate neurological development. There arefour drugs used to treat chronic toxicity: sodium calcium edetate IV and IM, succimer(oral), dimercaprol IM, and penicillamine (oral). If we consider that the last one is theonly authorized drug in our country, the problem grows bigger. This brief review offersinformation about lead exposure and poisoning, the recommended drug treatments andtheir market availability.