Uptake and intracellular activity of an optically active ofloxacin isomer in human neutrophils and tissue culture cells

The penetration of an optically active ofloxacin isomer [(-)-ofloxacin] into human neutrophils and different tissue culture cells (HEp-2, McCoy, MDCK, and Vero) was studied and compared with that of ofloxacin by a fluorometric assay. The cellular-to-extracellular-concentration ratios (C/E) of (-)-ofloxacin were always higher than 6, significantly greater than those of ofloxacin at extracellular concentrations of 5 and 10 mg/liter. The penetration of (-)-ofloxacin and ofloxacin was doubled when neutrophils were stimulated by phorbol myristate acetate but not affected after ingestion of opsonized Staphylococcus aureus. The C/E ratios of (-)-ofloxacin and ofloxacin for different tissue culture epithelial cells and fibroblasts were lower than those of neutrophils but still higher than 2. Both compounds produced a significant reduction in viable intraphagocytic S. aureus during 3 h of exposure to antimicrobial agents. We conclude that (-)-ofloxacin appears to reach higher intracellular concentrations than ofloxacin, remaining active inside the neutrophils

Intracellular penetration and activity of BAY Y 3118 in human polymorphonuclear leukocytes

The penetration of a new quinolone (BAY Y 3118) into human polymorphonuclear leukocytes (PMNs) was evaluated by a fluorometric assay. The cellular concentration-to-extracellular concentration (C/E) ratio was higher than 6.3 at extracellular concentrations ranging from 2 to 100 mg/liter. The uptake of BAY Y 3118 was rapid, reversible and nonsaturable. The intracellular penetration of BAY Y 3118 was significantly affected by environmental temperature (C/E ratio at 4°C, 5.4 ± 0.5; control, 7.5 ± 0.9; P < 0.05) and cell viability (C/E ratio in dead PMNs, 5.5 ± 0.8; control, 7.5 ± 0.9; P < 0.05), but it was not affected by metabolic inhibitors. The ingestion of opsonized zymosan or opsonized Staphylococcus aureus significantly decreased the levels of PMN-associated BAY Y 3118. Cell stimulation by a membrane activator, however, significantly increased the intracellular concentration of this quinolone. At therapeutic extracellular concentrations (0.5, 2, and 5 mg/liter), BAY Y 3118 showed intracellular activity greater than that of ciprofloxacin against S. aureus in human PMNs. It was concluded that BAY Y 3118 reaches high intracellular concentrations within human PMNs and remains active intracellularly

Rendimiento de los estudiantes de primer curso de universidad en las tareas orales en la simulación de un examen de acceso a la Universidad. Performance of first year university students in the speaking tasks of a simulated University Entrance Examination

El debate sobre la Prueba de idiomas (inglés) en el Examen de Acceso a la Universidad (PAU) se ha convertido en un tema crítico en el sistema educativo español. A pesar del interés del Ministerio de Educación en el cambio de una prueba que tiene su fuerte énfasis en la lectura, la escritura y la gramática, sino una negligencia general hacia la comprensión y expresión oral, las administraciones regionales han hecho pocos cambios. El hecho de no evaluar los aspectos orales en la prueba puede disminuir la importancia que estos aspectos reciben en los últimos niveles del ámbito educativo, y por ende, en el nivel oral de los alumnos. Para comprobar la competencia oral de los egresados de la escuela secundaria, un conjunto de tareas de habla fueron diseñadas y administradas a 169 estudiantes de primer semestre de tres universidades españolas diferentes que habían realizado recientemente el PAU para observar su competencia oral. Los resultados mostraron que la gran mayoría de los estudiantes en la investigación tienen un nivel B1 con un enorme porcentaje de estudiantes en el nivel A1- A2. Estos resultados no difieren significativamente de un estudio previo del Ministerio de Educación y muestran la necesidad de incluir las tareas que hablan en la Prueba de Acceso a la Universidad o el Examen Final de Bachillerato. Los estudios cualitativos también sugirieren que la forma de realizar las tareas y el enfoque de las pruebas podría tener un efecto sobre el rendimiento de los estudiantes

Filmed clinical cases improved communication skills of student of Pharmacology in Podiatry degree

Solving clinical case by writing-report lacks of students sympathies and interest in many cases. Make a short film is a novelty that really like to the students and may improve their arguing and planning capacities and their communication skills. Aim: To evaluate the impact of presenting and resolving clinical cases through filming a short-film in the communication skills development and in the learning of medicines in Podiatry undergraduate students. Methods: A two-year study in which students were invited to voluntarily form groups (3 students maximum). Each group has to design and film a short-film (8 min maximum) showing a clinical case in which medicines’ use was needed to treat feet pathology. A camera, a mobile-phone's video editor or whatever they may use was allowed. The job of each group was supervised and helped by a teacher. The students were invited to present their work to the rest of the class. After each short-film projection the students were encouraged to ask questions if they wanted to do it. After all the projections the students voluntarily answered a satisfaction survey. Results: Students of Pharmacology of Podiatry Degree, N=101, 55.6% female, 20±1.3 years old were enrolled. 37 short-films showing a clinical case were made. The average time spent by students in making the film was 12.4±8 h. The percentage of students which were satisfied with this way of presentation of the clinical cases was 75.2%. Conclusion: Filmed clinical cases performed by student of Pharmacology of the Podiatry Degree improved their communication skills.Universidad de Málaga. Campus de Excelencia Internacional Andalucía Tech. Convocatoria de Ayudas de la Universidad de Málaga a Proyectos de Innovación Educativa, convocatoria 2013-2015, PIE 13-156 en Área de Ciencias de la Salud

In vitro effect photodynamic therapy with differents photosensitizers on cariogenic microorganisms

Background Antimicrobial photodynamic therapy has been proposed as an alternative to suppress subgingival species. This results from the balance among Streptococcus sanguis, Streptococcus mutans and Candida albicans in the dental biofilm. Not all the photosensitizers have the same photodynamic effect against the different microorganims. The objective of this study is to compare in vitro the photodynamic effect of methylene blue (MB), rose Bengal (RB) and curcumin (CUR) in combination with white light on the cariogenic microorganism S. mutans, S. sanguis and C. albicans. Go to: Results Photodynamic therapy with MB, RB and CUR inhibited 6 log 10 the growth of both bacteria but at different concentrations: 0.31–0.62 μg/ml and 0.62–1.25 μg/ml RB were needed to photoinactivate S. mutans and S. sanguis, respectively; 1.25–2.5 μg/ml MB for both species; whereas higher CUR concentrations (80–160 μg/ml and 160–320 μg/ml) were required to obtain the same reduction in S. mutans and S. sanguis viability respectively. The minimal fungicidal concentration of MB for 5 log10 CFU reduction (4.5 McFarland) was 80–160 μg/ml, whereas for RB it ranged between 320 and 640 μg/ml. For CUR, even the maximum studied concentration (1280 μg/ml) did not reach that inhibition. Incubation time had no effect in all experiments. Go to: Conclusions Photodynamic therapy with RB, MB and CUR and white light is effective in killing S. mutans and S. sanguis strains, although MB and RB are more efficient than CUR. C. albicans required higher concentrations of all photosensitizers to obtain a fungicidal effect, being MB the most efficient and CUR ineffective.España, Ministerio de Ciencia e Innovación CTQ2013-48767-C3-2-

Intracellular penetration and activity of gemifloxacin in human polymorphonuclear leukocytes

The intracellular penetration and activity of gemifloxacin in human polymorphonuclear leukocytes (PMN) were evaluated. Gemifloxacin reached intracellular concentrations eight times higher than extracellular concentrations. The uptake was rapid, reversible, and nonsaturable and was affected by environmental temperature, cell viability, and membrane stimuli. At therapeutic extracellular concentrations, gemifloxacin showed intracellular activity against Staphylococcus aureus

Photodynamic Therapy Combined with Antibiotics or Antifungals against Microorganisms That Cause Skin and Soft Tissue Infections: A Planktonic and Biofilm Approach to Overcome Resistances

The present review covers combination approaches of antimicrobial photodynamic therapy (aPDT) plus antibiotics or antifungals to attack bacteria and fungi in vitro (both planktonic and biofilm forms) focused on those microorganisms that cause infections in skin and soft tissues. The combination can prevent failure in the fight against these microorganisms: antimicrobial drugs can increase the susceptibility of microorganisms to aPDT and prevent the possibility of regrowth of those that were not inactivated during the irradiation; meanwhile, aPDT is effective regardless of the resistance pattern of the strain and their use does not contribute to the selection of antimicrobial resistance. Additive or synergistic antimicrobial effects in vitro are evaluated and the best combinations are presented. The use of combined treatment of aPDT with antimicrobials could help overcome the difficulty of fighting high level of resistance microorganisms and, as it is a multi-target approach, it could make the selection of resistant microorganisms more difficult

Uptake and intracellular activity of moxifloxacin in human neutrophils and tissue-cultured epithelial cells

The penetration by moxifloxacin of human neutrophils (polymorphonuclear leukocytes [PMN]) and tissue-cultured epithelial cells (McCoy cells) was evaluated by a fluorometric assay. At extracellular concentrations of 5 mg/liter, the cellular-to-extracellular concentration ratios (C/E) of moxifloxacin in PMN and McCoy cells were 10.9 ± 1.0 and 8.7 ± 1.0, respectively (20 min; 37°C). The uptake of moxifloxacin by PMN was rapid, reversible, nonsaturable (at extracellular concentrations ranging from 1 to 50 μg/ml), and not affected by cell viability. The uptake of moxifloxacin was affected by external pH and the environmental temperature. The incubation of PMN in the presence of sodium fluoride, sodium cyanide, and carbonyl cyanide m-chlorophenylhydrazone significantly decreased the C/E of this agent. Neither PMN stimulation nor phagocytosis of opsonized Staphylococcus aureus significantly affected the uptake of moxifloxacin by human PMN. This agent, at concentrations of 0.5, 1, and 5 mg/liter, induced a significant reduction in the survival of intracellular S. aureus in human PMN. In summary, moxifloxacin reaches much higher intracellular concentrations within phagocytic and nonphagocytic cells than extracellular ones, remaining active inside the neutrophils

Uptake and intracellular activity of sparfloxacin in human polymorphonuclear leukocytes and tissue culture cells

The penetration of sparfloxacin into human neutrophils (PMN) and different tissue culture cells (HEp-2 and McCoy) was evaluated. The cellular to extracellular concentration ratios (C/E) of sparfloxacin were always higher than 4 at extracellular concentrations ranging from 0.5 to 25 mg/liter. The uptake of sparfloxacin by PMN was rapid, nonsaturable, reversible, not energy dependent, and significantly reduced at pH 8. The penetration of this agent into PMN was similar when viable and Formalin-killed cells were used and was not affected by environmental temperature. Ingestion of opsonized zymosan significantly increased the amount of PMN-associated sparfloxacin. Sparfloxacin at a concentration of 0.5 mg induced a significant reduction in the survival of intracellular Staphylococcus aureus. It is concluded that sparfloxacin reaches intracellular concentrations within leukocytic cells much higher than extracellular concentrations, while remaining active intracellularly