Combinations of Piperine with Hydroxypropyl-β-Cyclodextrin as a Multifunctional System

Piperine is an alkaloid that has extensive pharmacological activity and impacts other active substances bioavailability due to inhibition of CYP450 enzymes, stimulation of amino acid transporters and P-glycoprotein inhibition. Low solubility and the associated low bioavailability of piperine limit its potential. The combination of piperine with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) causes a significant increase in its solubility and, consequently, an increase in permeability through gastrointestinal tract membranes and the blood–brain barrier. X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR) were used to characterize interactions between piperine and HP-β-CD. The observed physicochemical changes should be combined with the process of piperine and CD system formation. Importantly, with an increase in solubility and permeability of piperine as a result of interaction with CD, it was proven to maintain its biological activity concerning the antioxidant potential (2,2-diphenyl-1-picryl-hydrazyl-hydrate assay), inhibition of enzymes essential for the inflammatory process and for neurodegenerative changes (hyaluronidase, acetylcholinesterase, butyrylcholinesterase).     

Magnetic Resonance Signal Amplification by Reversible Exchange of Selective PyFALGEA Oligopeptide Ligands Towards Epidermal Growth Factor Receptors

The biorelevant PyFALGEA oligopeptide ligand, which is selective towards the epidermal growth factor receptor (EGFR), has been successfully employed as a substrate in magnetic resonance signal amplification by reversible exchange (SABRE) experiments. It is demonstrated that PyFALGEA and the iridium catalyst IMes form a PyFALGEA:IMes molecular complex. The interaction between PyFALGEA:IMes and H₂ results in a ternary SABRE complex. Selective 1D EXSY experiments reveal that this complex is labile, which is an essential condition for successful hyperpolarization by SABRE. Polarization transfer from parahydrogen to PyFALGEA is observed leading to significant enhancement of the ¹H NMR signals of PyFALGEA. Different iridium catalysts and peptides are inspected to discuss the influence of their molecular structures on the efficiency of hyperpolarization. It is observed that PyFALGEA oligopeptide hyperpolarization is more efficient when an iridium catalyst with a sterically less demanding NHC ligand system such as IMesBn is employed. Experiments with shorter analogues of PyFALGEA, that is, PyLGEA and PyEA, show that the bulky phenylalanine from the PyFALGEA oligopeptide causes steric hindrance in the SABRE complex, which hampers hyperpolarization with IMes. Finally, a single-scan ¹H NMR SABRE experiment of PyFALGEA with IMesBn revealed a unique pattern of NMR lines in the hydride region, which can be treated as a fingerprint of this important oligopeptide.     

New 1,3,4-Oxadiazole Derivatives of Pyridothiazine-1,1-Dioxide with Anti-Inflammatory Activity

Numerous studies have confirmed the coexistence of oxidative stress and inflammatory processes. Long-term inflammation and oxidative stress may significantly affect the initiation of the neoplastic transformation process. Here, we describe the synthesis of a new series of Mannich base-type hybrid compounds containing an arylpiperazine residue, 1,3,4-oxadiazole ring, and pyridothiazine-1,1-dioxide core. The synthesis was carried out with the hope that the hybridization of different pharmacophoric molecules would result in a synergistic effect on their anti-inflammatory activity, especially the ability to inhibit cyclooxygenase. The obtained compounds were investigated in terms of their potencies to inhibit cyclooxygenase COX-1 and COX-2 enzymes with the use of the colorimetric inhibitor screening assay. Their antioxidant and cytotoxic effect on normal human dermal fibroblasts (NHDF) was also studied. Strong COX-2 inhibitory activity was observed after the use of TG6 and, especially, TG4. The TG11 compound, as well as reference meloxicam, turned out to be a preferential COX-2 inhibitor. TG12 was, in turn, a non-selective COX inhibitor. A molecular docking study was performed to understand the binding interaction of compounds at the active site of cyclooxygenases.     

Polymer derived ceramic materials from Si,B and MoSiB filler-loaded perhydropolysilazane precursor for oxidation protection

Silica-based coating systems were developed using polymer derived ceramics (PDCs) technology. Ceramic composites on the base of a SiO₂ and SiNO matrix and homogeneously distributed Mo₅SiB₂, SiB₆, Si and B fillers were manufactured. The coating systems have low porosity and provide a high oxidation resistance up to 100 h at 800 °C and 1100 °C in air. The influence of temperature and atmosphere of pyrolysis on the polymer precursor, the volume fraction of filler materials on the chemical composition of compacts as well as their high-temperature oxidation protection was investigated.     

Effect of complexation of oxidised corn starch with mineral elements on physicochemical properties

The objective of this study was to determine the effect of complexation of oxidised starch with mineral elements on its physicochemical properties. Corn starch was oxidised with sodium hypochlorite and, afterwards, modified with ions of potassium, magnesium and iron. Thus, native and modified starches were analysed for: contents of mineral elements, colour parameters (L*a*b*), water binding capacity and solubility in water at temperature of 60 and 80 °C. Thermodynamic characteristics of gelatinisation by DSC, molecular weight distribution by GPC, intrinsic viscosity and pasting properties by RVA were studied. The efficiency of incorporation of metal ions into oxidised corn starch was about 30%, 20% and 20% for potassium, magnesium and iron ions, respectively. The complexation with potassium ions caused the greatest changes in the molecular weight distribution and the intrinsic viscosity of starches and viscosity of starch pastes. Only modification of starch with iron ions affected the colour parameters of the starch. Incorporation of metal ions into starch resulted also in changes in its water binding capacity and solubility in water.     

Impact of adhesive ingredients on adhesion between rubber and brass-plated steel wire in tire

Proficiency on underlying mechanism of rubber-metal adhesion has been increased significantly in the last few decades. Researchers have investigated the effect of various ingredients, such as hexamethoxymethyl melamine, resorcinol, cobalt stearate, and silica, on rubber-metal interface. The role of each ingredient on rubber-metal interfacial adhesion is still a subject of scrutiny. In this article, a typical belt skim compound of truck radial tire is selected and the effect of each adhesive ingredient on adhesion strength is explored. Out of these ingredients, the effect of cobalt stearate is found noteworthy. It has improved adhesion strength by 12% (without aging) and by 11% (humid-aged), respectively, over control compound. For detailed understanding of the effect of cobalt stearate on adhesion, scanning electron microscopy and energy dispersive spectroscopy are utilized to ascertain the rubber coverage and distribution of elements. X-ray photoelectron spectroscopy results helped us to understand the impact of Cu_XS layer depth on rubber-metal adhesion. The depth profile of the Cu_XS layer was found to be one of the dominant factors of rubber-metal adhesion retention. Thus, this study has made an attempt to find the impact of different adhesive ingredients on the formation of Cu_XS layer depth at rubber-metal interface and establish a correlation with adhesion strength simultaneously.     

Purification of the cardiac sarcoplasmic reticulum membrane protein phospholamban from recombinant Escherichia coli

Phospholamban (PLN) was expressed in Escherichia coli as a protein fusion with glutathione S-transferase (GST). GST-PLN was mostly present in the insoluble protein fraction and accounted for approximately 50% of total insoluble protein. Attempts to suppress inclusion body formation or to use GST as an affinity-purification tag failed. A successful purification method is based on preparative SDS/PAGE and electrodialysis. From 1 g cells we typically purified 13.5 mg fusion protein with a PLN content of 2.8 mg. We genetically inserted an enterokinase (EK) protease site just in front of the PLN sequence and demonstrated the proteolytical liberation of PLN from the carrier protein. The approach described represents a substantial advancement in PLN expression and purification.     

An artificial neural network approach on parametric optimization of laser micro-machining of die-steel

In the present research, laser micro machining (LMM) of tungsten-molybdenum general purpose high speed steel (Rex M2) has been studied. Selection of optimum machining parameter combinations for obtaining higher depth of groove and smaller height of recast layer is a challenging task in LMM due to the presence of a large number of process variables. There is no perfect combination of parameters which can simultaneously result in both the highest depth of groove and lowest height of recast layer. This paper presents an attempt to develop a strategy for predicting the optimum machining parameter setting for the generation of the maximum depth of groove with minimum height of recast layer. A feed forward back-propagation neural network has been developed to model the machining process. The model, after proper training, is capable of predicting the response parameters as a function of four different control parameters. Experimental results demonstrate that the machining model is suitable and the optimization strategy satisfies practical requirements. The developed model has been found to be quite unique, powerful and flexible.