Scielo RSS <![CDATA[Brazilian Journal of Pharmaceutical Sciences]]> vol. 54 num. 1 lang. es <![CDATA[SciELO Logo]]> <![CDATA[The role of selenium in insulin resistance]]> ABSTRACT In recent years, there has been growing interest in clarifying the pathogenesis of some chronic diseases, such as obesity and type 2 diabetes mellitus. Metabolic alterations in these diseases are characterized by chronic hyperglycemia and insulin resistance. Studies have demonstrated the participation of minerals in the pathogenesis of insulin resistance, more specifically their involvement in the synthesis and regulation of insulin. Selenium is an anti-inflammatory and antioxidant micronutrient that is essential for the activity of selenoproteins. Two selenoproteins (glutathione peroxidase and selenoprotein P) are known to be involved in the insulin signaling pathway. The aim of this review is to provide an update on the role of selenium in insulin resistance mechanisms. Evidence shows that adequate concentrations of selenium play a key role in the secretion and action of insulin, but an excess of selenium in the body is associated with the pathogenesis of insulin resistance and the development of diabetes mellitus. <![CDATA[Phage therapy: progress in pharmacokinetics]]> ABSTRACT The concept of phage therapy exists in the history and it has been ignored for a long time, but the consequence of drug resistance in pathogen bacteria has forced the forgotten kingdom of phage therapy to be re-explored. However, for the successful implementation and acceptance of phage therapy worldwide, the number of factors need to be addressed. In pharmacology of phage therapy, pharmacodynamics is a straightforward concept, on the other hand, owing to the unique feature of phages to replicate and their high sensitivity, pharmacokinetics is rather complex. In this review, we have discussed pharmacokinetics and some recent advances in delivery systems as to achieve the therapeutically effective concentrations of phage in their activated form. <![CDATA[Intravenous immunoglobulin therapy among pediatric patients: labeled and off-labeled indications]]> ABSTRACT This study was designed to evaluate utilization patterns and clinical outcome of intravenous immunoglobulin (IVIG) therapy among pediatric patients in a tertiary hospital. Demographic data, IVIG prescribed, and clinical outcome were retrospectively reviewed from the pharmacy dispensing data and patient medical records between 2007 and 2014. One hundred and fifteen instances of IVIG administration to 108 pediatric patients were recorded. A total of 61 cases (53%) and 54 cases (47%) of the IVIG administered were for labeled and off-labeled indications, respectively. Age, weight, specialty, total IVIG usage, length of hospital stays, and mortality rate were found to be significantly associated with the indication being labeled or off-labeled (p&lt;0.05). However, there was no significant difference in terms of adverse reactions between labeled and off-labeled indications (p&gt;0.05). Guidelines should be developed and implemented for rational and evidence-based use of IVIG to avoid unnecessary wastage. <![CDATA[Fast detection of Mycobacterium tuberculosis in culture-positive sputum samples by nitrate reductase activity]]> ABSTRACT Microscopy and bacterial culture are the main tools in the diagnosis of tuberculosis. Since the slow growth of Mycobacterium tuberculosis impairs rapid diagnosis strategies, especially in countries where the latter are the only available resources, the ongoing development of new and inexpensive tools based on mycobacterial metabolism optimizing growth detection with preliminary identification is greatly welcome. When compared to the other species from the M. tuberculosis complex, M. tuberculosis is a strong nitrate reducer. Current assay compares the nitrate reductase activity of M. tuberculosis from pulmonary specimens cultivated in nitrate-supplemented media. Fifty-five sputum samples were decontaminated and inoculated in conventional (Middlebrook 7H9, Ogawa Kudoh-OK) and in nitrate-supplemented media (Middlebrook 7H9-N, Ogawa Kudoh-N). An aliquot from the media directly reacted with Griess reagent (7H9-N and OK-N) every five days, or transferred to a nitrate substrate solution (7H9, OK). Nitrate to nitrite reduction was considered positive, revealed by the pink color, indicating bacterial growth. As reference method, the Mycobacteria Growth Indicator Tube (MGIT) was used for sensitivity calculations and statistical analysis. 7H9-N and OK-N assays proved to perform better in detecting M. tuberculosis than conventional assays (7H9 and OK). Indeed, broth nitrate-supplemented medium (7H9-N) was comparable to MGIT to detect M. tuberculosis, except in growth detection time. Results show that 7H9-N may be used as an alternative tool particularly in low-income countries since it is a simple and cheap technique, and does not restrict diagnosis to single-source products. <![CDATA[In vitro cytotoxicity of chemical preservatives on human fibroblast cells]]> ABSTRACT Preservatives are widely used substances that are commonly added to various cosmetic and pharmaceutical products to prevent or inhibit microbial growth. In this study, we compared the in vitro cytotoxicity of different types of currently used preservatives, including methylparaben, imidazolidinyl urea (IMU), and sodium benzoate, using the human newborn fibroblast cell line CCD1072Sk. Of the tested preservatives, only IMU induced a reduction in cell viability, as shown using the MTT assay and propidium iodide staining (IMU&gt;methylparaben&gt;sodium benzoate). IMU was shown to promote homeostatic alterations potentially related to the initiation of programed cell death, such as decreased mitochondrial membrane potential and caspase-3 activation, in the treated cells. Methylparaben and sodium benzoate were shown to have a very low cytotoxic activity. Taken together, our results suggest that IMU induces programed cell death in human fibroblasts by a canonical intrinsic pathway via mitochondrial perturbation and subsequent release of proapoptotic factors. <![CDATA[Evaluation of the influence of fluoroquinolone chemical structure on stability: forced degradation and in silico studies]]> ABSTRACT Fluoroquinolones are a known antibacterial class commonly used around the world. These compounds present relative stability and they may show some adverse effects according their distinct chemical structures. The chemical hydrolysis of five fluoroquinolones was studied using alkaline and photolytic degradation aiming to observe the differences in molecular reactivity. DFT/B3LYP-6.31G* was used to assist with understanding the chemical structure degradation. Gemifloxacin underwent degradation in alkaline medium. Gemifloxacin and danofloxacin showed more degradation perceptual indices in comparison with ciprofloxacin, enrofloxacin and norfloxacin in photolytic conditions. Some structural features were observed which may influence degradation, such as the presence of five member rings attached to the quinolone ring and the electrostatic positive charges, showed in maps of potential electrostatic charges. These measurements may be used in the design of effective and more stable fluoroquinolones as well as the investigation of degradation products from stress stability assays. <![CDATA[Pharmacists in dispensing drugs (PharmDisp): protocol for a clinical trial to test the effectiveness of distance education in training pharmacists for dispensing drugs]]> ABSTRACT Dispensing drug is a moment in which the pharmacist is able to analyze pharmacotherapy and contribute to its rational use. However, research has shown that some pharmacists lack adequate knowledge to perform this service. This study aims to describe a research protocol for a clinical trial to test the effectiveness of a distance learning program to train pharmacists in dispensing drugs. This is a protocol for an open diagnostic, non-randomized, single group clinical trial. A 12-week duration distance learning course was structured on the Moodle platform for training community pharmacists who are registered in the Regional Board of Pharmacy and work as employees or owners in Brazilian community pharmacies. The course curricula involves concepts and practice of dispensing drugs applied to the treatment of hypertension, diabetes mellitus, dyslipidemia and asthma. Pharmacists are divided randomly into groups, to which previously selected tutors give directions to the discussion and clarify questions. A validated questionnaire is being used before and after the course to measure participants’ knowledge. Participant satisfaction with the course is also being measured. Pharmacists who work in the study headquarters municipality receive two visits from a mystery shopper, before and after the course, to evaluate their performance in dispensing drugs. The virtual platform and the content of the course material were evaluated by judges. The study has been approved by the Research Ethics Committee of the School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo. The sample size was estimated to provide desired power for testing the significance of the difference between baseline-to-endpoint change scores. Information about the course is being released through channels such as social networks. The results will be submitted for publication in scientific journals, but information enabling the identification of the study subjects will be kept confidential. The trial has been registered in The Brazilian Clinical Trials Registry with number RBR7mbrp3 on January 15th, 2015. <![CDATA[Alpha amylase and Alpha glucosidase inhibitory effects of aqueous stem extract of Salacia oblonga and its GC-MS analysis]]> ABSTRACT Our present investigation deals with the phytochemical screening, estimation of total flavonoids, terpenoids and tannin contents to evaluate the anti-diabetic activities of Salacia oblonga stem followed by GC-MS analysis. It explores the natural compounds and the potential α-amylase and α-glucosidase inhibitory actions of stem extracts. The aqueous stem extract was selected from other extracts (ethanol, acetone, petroleum ether and chloroform) for the in vitro study of anti-diabetic activity by alpha amylase and alpha glucosidase inhibitory assays. The stem extract was also analyzed by gas chromatography mass spectrometry to identify the natural chemical components. Phytochemical analysis of aqueous stem extract showed major classes of secondary metabolites such as phenols, flavonoids, alkaloids, terpenoids, tannins, saponins. The total flavonoid, terpenoid, and tannin contents were quantified as 19.82±0.06 mg QE/g, 96.2±0.20 mg/g and 11.25±0.03 mg TAE/g respectively. The percentage inhibition of assays showed maximum inhibitory effects (59.46±0.04% and 68.51±0.01%) at a concentration of 100 mg/mL. The IC50 values of stem extract was found to be 73.56 mg/mL and 80.90 mg/mL for alpha amylase and alpha glucosidase inhibition. Fifteen chemical constituents were found by GC-MS analysis. This study suggest the aqueous stem extract of Salacia oblonga might be considered as potential source of bio active constituents with excellent antidiabetic activity. <![CDATA[Effects of high fat diet on kidney lipid content and the Na,K-ATPase activity]]> ABSTRACT It is widely known that high fat diet (HFD) can contribute to the advent of health problems. Recent studies have indicated that obesity imposes a hemodynamic overload to the kidneys. In order to further investigate such injuries, two groups of six Swiss mice each were fed with a controlled AIN93G diet or a high fat (AIN93G modified) diet for eight weeks. Blood samples were collected to determine the hormonal, lipid profile, glucose, urea, and creatinine levels. Histopathological and immunohistochemical analysis were carried out to analysis the kidney damage. Fractions of renal membranes were prepared to assess the Na,K-ATPase activity, lipid peroxidation, total cholesterol, and phospholipid content. The results indicated that the blood lipid profile, urea and creatinine was not altered by the HFD. On the other hand, it was observed in HFD diet mice elevated glucose blood levels along with an augment on insulin and a decrease on corticosterone release. HFD provoked a reduction in the diameter of the convoluted tubules and cell volume in Bowman’s capsule and an increased number of positive cells with Na,K-ATPase, but reduced the Na,K-ATPase activity and the cholesterol content in the kidney cell membrane but favored the lipid peroxidation.