Phenylalanine-Based AMPA Receptor Antagonist as the Anticonvulsant Agent with Neuroprotective Activity—In Vitro and In Vivo Studies

Trying to meet the multitarget-directed ligands strategy, a series of previously described aryl-substituted phenylalanine derivatives, reported as competitive antagonists of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, were screened in vitro for their free-radical scavenging and antioxidant capacity in two different assays: ferric reducing antioxidant power (FRAP) and oxygen radical absorbance capacity fluorescent (ORAC-FL) assays. The most active antioxidants 1 and 8 were further examined to evaluate their neuroprotective properties in vitro. In this study, compound 1 showed a significant neuroprotective effect against the neurotoxin 6-hydroxydopamine in neuroblastoma SH-SY5Y and IMR-32 cell lines. Both compounds also showed prevention from high levels of reactive oxygen species (ROS) in SH-SY5Y cells. Furthermore, the desired monoamine oxidase B (MAO-B) inhibition effect (IC₅₀ = 278 ± 29 nM) for 1 was determined. No toxic effects up to 100 µM of 1 and 8 against neuroblastoma cells were observed. Furthermore, in vivo studies showed that compound 1 demonstrated significant anticonvulsant potential in 6-Hz test, but in neuropathic pain models its antiallodynic and antihyperalgesic properties were not observed. Concluding, the compound 1 seems to be of higher importance as a new phenylalanine-based lead candidate due to its confirmed promise in in vitro and in vivo anticonvulsant activity.     

Postdiagenetic Changes in Kerogen Properties and Type by Bacterial Oxidation and Dehydrogenation

A significant part of organic carbon found on the earth is deposited as fossil organic matter in the lithosphere. The most important reservoir of carbon is shale rocks enriched with organic matter in the form of kerogen created during diagenesis. The purpose of this study was to analyze whether the bacterial communities currently inhabiting the shale rocks have had any impact on the properties and type of kerogen. We used the shale rock located on the Fore-Sudetic Monocline, which is characterized by oil-prone kerogen type II. We were able to show that shale rock inhabited by bacterial communities are characterized by oxidized and dehydrated kerogen type III (gas-prone) and type IV (nonproductive, residual, and hydrogen-free). Bacterial communities inhabiting shale rock were dominated by heterotrophs of the Proteobacteria, Firmicutes, and Actinobacteria phyla. Additionally, we detected a number of protein sequences in the metaproteomes of bacterial communities matched with enzymes involved in the oxidative metabolism of aliphatic and aromatic hydrocarbons, which may potentially contribute to the postdiagenetic oxidation and dehydrogenation of kerogen. The kerogen transformation contributes to the mobilization of fossil carbon in the form of extractable bitumen dominated by oxidized organic compounds.     

The Effect of Antiretroviral Therapy on SIRT1, SIRT3 and SIRT6 Expression in HIV-Infected Patients

Human Immunodeficiency Virus (HIV) infection and the chronic use of combined antiretroviral therapy (cART) may affect the occurrence of certain disturbances in the body. There is growing interest in sirtuins–enzymes involved in the regulation of many metabolic processes in the organism and in the pathogenesis of many diseases which also exhibit potential antiviral activity. The aim of the study was to investigate the connection of cART to the expression of Sirtuin 1 (SIRT1), Sirtuin 3 (SIRT3) and Sirtuin 6 (SIRT6) in HIV-infected men. The plasma levels of sirtuins were measured before and one year after cART, and related to HIV viral load, lymphocytes T CD4+ and CD8+ count as well as the applied cART. The levels of sirtuins in plasma were measured in HIV-infected patients (n = 53) and the control group (n = 35) by immunoassay methods. There were statistically significant (p < 0.05) differences between SIRT6 in the HIV-infected patients before therapy and in the subgroups, depending on the count of lymphocytes T CD8+. There were significant differences in the levels of SIRT1 depending on the applied treatment regimen. The obtained results indicate the most significant changes in the expression of SIRT6 in the course of HIV infection and suggest an influence of the type of cART on the level of SIRT1, which indicates its important role in the course of HIV.     

The Current State of Knowledge on Salvia hispanica and Salviae hispanicae semen (Chia Seeds)

Chia seeds (Salviae hispanicae semen) are obtained from Salvia hispanica L. This raw material is distinguished by its rich chemical composition and valuable nutritional properties. It is currently referred to as “health food”. The purpose of the present work was to perform a literature review on S. hispanica and chia seeds, focusing on their chemical composition, biological properties, dietary importance, and medicinal uses. The valuable biological properties of chia seeds are related to their rich chemical composition, with particularly high content of polyunsaturated fatty acids, essential amino acids, polyphenols, as well as vitamins and bioelements. The available scientific literature indicates the cardioprotective, hypotensive, antidiabetic, and antiatherosclerotic effects of this raw material. In addition, studies based on in vitro assays and animal and human models have proven that chia seeds are characterized by neuroprotective, hepatoprotective, anti-inflammatory, and antioxidant properties. These properties indicate a valuable role of chia in the prevention of civilization diseases. Chia seeds are increasingly popular in functional food and cosmetic and pharmaceutical industries. That is attributed not only to their desirable chemical composition and biological activity but also to their high availability. Nevertheless, S. hispanica is also the object of specific biotechnological studies aimed at elaboration of micropropagation protocols of this plant species.     

Effect of heat treatment on the structure and morphology of ZnO nanorod array and its composite with titania precursor

ABSTRACT

Effects of the elevated temperature on the structure evolution of the ZnO nanorod array (ZNA) and their hybrid nanocomposite with layered (tetramethyl)ammonium titanate (LTMAT) prepared by the liquid phase deposition were investigated. The vertically oriented ZnO nanorods were deposited on a quartz plate by a chemical bath deposition method and then they were penetrated by the LTMAT using the dip-coating method from the water solution. As a result of such an experimental procedure, an assembly composed of the ZNA with LTMAT was obtained and called hybrid nanocomposite. Since the LTMAT converts to TiO₂ upon subsequent sintering at 350 °C, it can be regarded as TiO₂ precursor for the thermal treatment experiments. The experiments with ZNA and their hybrid nanocomposite at the elevated temperature revealed coalescence of the deposited ZnO nanorods and crystallization of zinc titanate with Zn₂TiO₄ stoichiometry.     

Removal of graffiti from the mortar by using Q-switched Nd:YAG laser

This paper presents part of the larger study on microstructural features of mortars and it's effects on laser cleaning process. It focuses on the influence of surface roughness, porosity and moisture content of mortars on the removal of graffiti by Nd:YAG laser. The properties of this laser are as follows: wavelength (λ) 1.06 μm, energy: 500 mJ per pulse, pulse duration: 10 ns. The investigation shows that the variation of laser fluence with the number of pulses required for the laser cleaning can be divided into two zones, namely effective zone and ineffective zone. There is a linear relationship observed between number of pulses required for laser cleaning and the laser fluence in the effective zone, while the number of pulses required for the laser cleaning is almost constant even though the laser fluence increases in the ineffective zone. Moreover, surface roughness, porosity and moisture content of mortar samples have influence on the laser cleaning process. The effect of these parameters become however negligible at the high level of laser fluence. The number of pulses required for the laser cleaning is low for smooth surface or less porous mortar. Furthermore, the wetness of the samples facilitates the cleaning process.     

A Hierarchical Model of Quantum Anharmonic Oscillators: Critical Point Convergence

We study the two-dimensional gauge theory of the symmetric group S_n describing the statistics of branched n-coverings of Riemann surfaces. We consider the theory defined on the disc and on the sphere in the large-n limit. A non trivial phase structure emerges, with various phases corresponding to different connectivity properties of the covering surface. We show that any gauge theory on a two-dimensional surface of genus zero is equivalent to a random walk on the gauge group manifold: in the case of S_n, one of the phase transitions we find can be interpreted as a cutoff phenomenon in the corresponding random walk. A connection with the theory of phase transitions in random graphs is also pointed out. Finally we discuss how our results may be related to the known phase transitions in Yang-Mills theory. We discover that a cutoff transition occurs also in two dimensional Yang-Mills theory on a sphere, in a large N limit where the coupling constant is scaled with N with an extra logN compared to the standard t Hooft scaling.     

Examining the possibilities of applying high pressure to preserve yoghurt supplemented with probiotic bacteria

Natural yoghurt was subject to pressures of 200 and 250 MPa/4 and 18°C/15 min, after which milk-activated inocula of Lactobacillus acidophilus and Bifidobacterium sp. were added. The yoghurts were stored for 4 weeks at refrigeration temperature. After preparation and each week of storage, the count of bacteria, acidity, antibacterial property and an organoleptic assessment was determined. The highest survival rate was demonstrated by the bacteria of Lactobacillus delbrueckii ssp. bulgaricus, Streptococcus thermophilus and Bifidobacterium sp. in the yoghurt pressurised 200 MPa/15min at 4°C. Acidity increases in the control yoghurts were higher than in the pressurised ones. Pressurised yoghurts demonstrated weaker antibacterial effect in comparison to control yoghurts. Slight changes in the smell and taste were observed after pressurisation. Yoghurts pressurised at 18°C were characterised by more favourable organoleptic properties. Better conciseness of the curd and lower whey seep out were observed in pressurised yoghurt.     

Molecular properties with dual basis set methods

The dual basis set approach has proven to be very successful for accurately estimating total energies with large basis sets. This study extends the applications of this technique to the calculation of molecular properties, including energy derivatives with respect to nuclear positions and to an external electric field. All energy derivatives have been calculated numerically via finite-differences. Molecular gradients and Hessians as well as dipole moments and polarizabilites have been calculated at the HF and MP2 levels using two alternative versions of the dual basis set method. The accuracy of these approaches is discussed in the context of quality of basis sets used in calculations. It is shown that even quite poor results obtained with the 6-311G basis set are significantly improved in dual basis set calculations with the 6-311G(d,p) and 6-311G(3df,3dp) basis sets.     

Multi-dimensional scalar balance laws with discontinuous flux

We consider scalar balance laws with a dissipative source term. The flux function may be discontinuous with respect to both the space variable x and the unknown quantity u. We formulate the definition of entropy weak solutions and provide existence and uniqueness to the considered problem. The problem is formulated in the framework of multi-valued mappings. The notion of entropy measure-valued solutions is used to prove the so-called contraction principle and comparison principle.