Procyanidin effects on adipocyte-related pathologies

Procyanidins, a class of flavonoids, have clear and well-defined beneficial effects against several pathologies including cardiovascular heart disease. Now, studies in vivo are revealing the effects of procyanidins against obesity, where they prevent weight gain and adipose tissue mass increase, and against diabetes and insulin resistance, where they act as antihiperglycemic agents. Several mechanisms may be responsible for these effects. One of these, due to the key role of adipose tissue in the development of obesity and insulin resistance, is their effect on adipocytes. In this review we compile the studies that indicate a protective role for procyanidins in obesity and insulin resistance, focusing on their effects on the adipocyte, where procyanidins modify lipid synthesis, lipid degradation, glucose uptake, and adipose differentiation.     

pH-responsive drug delivery system based on hollow silicon dioxide micropillars coated with polyelectrolyte multilayers

We report on the fabrication of polyelectrolyte multilayer-coated hollow silicon dioxide micropillars as pH-responsive drug delivery systems. Silicon dioxide micropillars are based on macroporous silicon formed by electrochemical etching. Due to their hollow core capable of being loaded with chemically active agents, silicon dioxide micropillars provide additional function such as drug delivery system. The polyelectrolyte multilayer was assembled by the layer-by-layer technique based on the alternative deposition of cationic and anionic polyelectrolytes. The polyelectrolyte pair poly(allylamine hydrochloride) and sodium poly(styrene sulfonate) exhibited pH-responsive properties for the loading and release of a positively charged drug doxorubicin. The drug release rate was observed to be higher at pH 5.2 compared to that at pH 7.4. Furthermore, we assessed the effect of the number of polyelectrolyte bilayers on the drug release loading and release rate. Thus, this hybrid composite could be potentially applicable as a pH-controlled system for localized drug release.     

Testing for Panel Cointegration Using Common Correlated Effects Estimators

Spurious regression analysis in panel data when the time series are cross section dependent is analysed in the article. We show that consistent estimation of the long‐run average parameter is possible once we control for cross section dependence using cross section averages in the spirit of the common correlated effects approach proposed by Pesaran. This result is used to design a panel cointegration test statistic accounting for cross section dependence. The performance of the proposal is investigated in comparison with factor‐based methods to control for cross section dependence when strong, semi‐weak and weak cross section dependence may be present.     

Fenton and photo‐Fenton oxidation of a model mixture of dyes – overall kinetic analysis

The decolorisation and mineralisation of a model mixture of reactive dyes, under Fenton and photo‐Fenton conditions, have been investigated. A kinetic study was performed and rate constants and half‐life times determined from batch experimental data according to a pseudo‐first‐order degradation kinetic model. Moreover, the use of natural or artificial light, as well as the effect of temperature, was evaluated with the aim of finding the best Fenton process to promote the efficient degradation of the standard trichromatic system. The experimental results showed that the Fenton process run under solar light was the most effective. It is suggested that Fenton‐ and photo‐Fenton‐type reactions are viable techniques for the treatment of these types of dye mixtures, according to the high levels of colour, chemical oxygen demand and total organic carbon removal.     

BMS Derivatives C7-Linked to β-Cyclodextrin and Hyperbranched Polyglycerol Retain Activity against R5-HIV-1NLAD8 Isolates and Can Be Deemed Potential Microbicides

Amides from indole-3-glyoxylic acid and 4-benzoyl-2-methylpiperazine, which are related to entry inhibitors developed by Bristol-Myers Squibb (BMS), have been synthesized with aliphatic chains located at the C7 position of the indole ring. These spacers contain an azido group suitable for the well-known Cu(I)-catalyzed (3+2)-cycloaddition or an activated triple bond for the nucleophilic addition of thiols under physiological conditions. Reaction with polyols (β-cyclodextrin and hyperbranched polyglycerol) decorated with complementary click partners has afforded polyol-BMS-like conjugates that are not cytotoxic (TZM.bl cells) and retain the activity against R5-HIV-1_NLAD8 isolates. Thus, potential vaginal microbicides based on entry inhibitors, which can be called of 4^th generation, are reported here for the first time.     

Study of Resonances in 1 × 25 kV AC Traction Systems

AC traction systems are 1 × 25 or 2 × 25 kV 50-Hz single-phase, non-linear, time-varying loads that can cause power quality problems. One of the main concerns about these systems is voltage distortion, because adjustable-speed drives for trains may inject harmonic currents of frequencies below 2 kHz. Since the presence of parallel resonances in the contact feeder section of the traction circuit worsens the scenario, traction system resonance phenomena should be analyzed to prevent problems. Several works addressed these phenomena, but they only drew weak numerical conclusions based on the frequency scan method. This article studies 1 × 25 kV traction system resonances at pantograph terminals and provides more effective analytical expressions to locate them and determine the impact of traction system parameters on them. These expressions are validated from several traction systems in the literature.     

N‐Benzyl‐4‐((heteroaryl)methyl)benzamides: A New Class of Direct NADH‐Dependent 2‐trans Enoyl–Acyl Carrier Protein Reductase (InhA) Inhibitors with Antitubercular Activity

Isoniazid (INH) remains one of the cornerstones of antitubercular chemotherapy for drug‐sensitive strains of M. tuberculosis bacteria. However, the increasing prevalence of multidrug‐resistant (MDR) and extensively drug‐resistant (XDR) strains containing mutations in the KatG enzyme, which is responsible for the activation of INH into its antitubercular form, have rendered this drug of little or no use in many cases of drug‐resistant tuberculosis. Presented herein is a novel family of antitubercular direct NADH‐dependent 2‐trans enoyl–acyl carrier protein reductase (InhA) inhibitors based on an N‐benzyl‐4‐((heteroaryl)methyl)benzamide template; unlike INH, these do not require prior activation by KatG. Given their direct InhA target engagement, these compounds should be able to circumvent KatG‐related resistance in the clinic. The lead molecules were shown to be potent inhibitors of InhA and showed activity against M. tuberculosis bacteria. This new family of inhibitors was found to be chemically tractable, as exemplified by the facile synthesis of analogues and the establishment of structure–activity relationships. Furthermore, a co‐crystal structure of the initial hit with the enzyme is disclosed, providing valuable information toward the design of new InhA inhibitors for the treatment of MDR/XDR tuberculosis.