Antimicrobial resistance to antibiotic treatment has significantly increased during recent years, causing this to become a worldwide public health problem. More than 70% of pathogenic bacteria are resistant to at least one of the currently used antibiotics. Polymyxin E (colistin) has recently been used as a “last line” therapy when treating Gram-negative multi-resistant bacteria. However, little is known about these molecules’ pharmacological use as they have been discontinued because of their high toxicity. Recent research has been focused on determining colistimethate sodium’s pharmacokinetic parameters to find the optimal dose for maintaining a suitable benefit–risk balance. This review has thus been aimed at describing the use of colistin on patients infected by multi-drug resistant bacteria and the importance of measuring this drug’s plasma levels in such patients.
In this study, we report the synthesis and biological evaluation of four 6- and 17-substituted progesterone derivatives (7-10). These compounds were prepared from the commercially available 17alpha-acetoxyprogesterone. The biological effect of these steroids was demonstrated in in vivo as well as in vitro experiments. In the in vivo experiments, we measured the activity of 6-10 on the weight of the prostate glands of gonadectomized hamsters treated with testosterone (T). For the studies in vitro, we determined the IC(50) value by measuring the concentration of steroidal derivative that inhibited 50% of the activity of 5alpha-reductase present in the human prostate. The results from this work indicated that compounds 6-9 significantly decreased the weight of the prostate as compared to testosterone-treated animals and this reduction of prostate weight was comparable to that produced by finasteride. Steroid 8 was the most effective of the tested compounds. However, compound 10 did not exhibit this capacity. On the other hand, 6-9 exhibited a high inhibitory activity for the human 5alpha-reductase enzyme with IC(50) values of 10, 70, 22, and 19 nM, respectively. However, 10 was not effective for the inhibition of 5alpha-reductase activity. In conclusion, the compounds that contained the acetate ester moiety in the molecule (6, 7, 8, and 9) inhibited the activity of 5alpha-reductase and decreased the weight of the prostate. Nevertheless, the double bond in ring B seems to diminish the inhibitory potency (7 and 9), since 6, which does not possess a double bond at C-6, had the highest inhibitory activity (the lowest IC(50) value).
Este estudio analiza el efecto del entrenamiento de la fuerza muscular abdominal y flexibilidad de isquiotibiales sobre el equilibrio dinámico valorado a través de la oscilación del centro de presión en mujeres sedentarias. Material y método: la muestra corresponde a 51 mujeres, 21 de ellas pertenecen al grupo control (GC) y 30 al grupo experimental (GEXP). La obtención de los datos fue a través de una entrevista personal, firma de consentimiento informado, mediciones de peso, talla, edad, IMC y encuesta de la actividad física. Además previo a la intervención se aplicaron evaluaciones de flexibilidad de musculatura isquiotibial y de fuerza muscular abdominal. La intervención duró ocho semanas al cabo de las cuales se realizaron reevaluaciones. Conclusiones: postintervención el atributo de flexibilidad mejoró un 32 %, y la fuerza abdominal incrementó en un 31 %. Finalmente, al contrastar las oscilaciones del centro de presión del grupo control y del grupo experimental a través del Sistema de Balance SD Biodex se obtuvo que la oscilación centro presión anteroposterior disminuyó un 17 %, y la oscilación centro presión medial lateral disminuyó un 26 %. Entrenar estos grupos musculares mejora el equilibrio dinámico, aspecto importante al momento de querer reducir lesiones.
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