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.     

Ampacities of power cables wound on reels

This paper presents a mathematical model that is capable of calculating the ampacity of a wide variety of power cable designs consisting of an arbitrary number of layers on a cable reel. The model considers round cables with copper conductors. The validity and accuracy of the ampacity model were verified by comparing the predicted temperature distribution within the reel with measured temperatures collected during an extensive testing program conducted at the US Bureau of Mines (USBM). The mathematical model predicted a temperature distribution within the cable layers that was very close to the measured variation in temperature. The value of the program is illustrated by calculating ampacities for several copper conductor sizes     

Non-contact methods of measuring moisture concentration in external layers of building partitions: III—Water vapour condensation on the cementitious surfaces

This paper presents the results of the larger study into a potential application of laser radiation for the detection of phase transition processes in low temperatures occurring on the surface layers of cementitious materials. An attempt was made to identify relationships between the environmental conditions—temperature and air humidity, and the selected parameters of the reflected light. Onset of the condensation process and formation of water microdrops on the surface of the material leads to the phase displacement of individual laser rays, which are represented by different speckle images.

Although the analysis of parameters of the reflected light are very difficult in the case of porous materials because of highly developed roughness of the surface structure it has been proved that a dynamic study of the phase transition phenomena can be successfully carried out without mechanical intervention.     

Non-contact methods of measuring moisture concentration in external layers of building partitions II—Monitoring of the water vapour condensation on porous surfaces

This paper present the results of the investigation into a potential application of laser radiation for the detection of phase transition processes occurring on the surface layers of porous materials. An attempt was made to discuss in the approximation equations, the relationships between coefficients of the reflected light, the temperature and humidity of the surrounding environment. Laser light reflected from the porous surface carries information about the roughness of the structure. The presence of water microdrop on the surface of the porous material, as a result of condensation and thus a phase transition, leads to the phase displacement of individual rays, which is represented by different images. Therefore, a comprehensive analysis of the reflected light parameters allows a dynamic study of the phase transition phenomena without mechanical intervention.     

A mixture theory for heat conduction in heterogeneous media

A mixture theory based on the ensemble-averaging technique is proposed for studying the thermal behaviour of heterogeneous media. Balance equations with partial heat fluxes and interaction terms are introduced for a two-component medium. Relations between these quantities and the ensemble-averaged (mean) temperatures of separate components are derived. The limits of application of widely used postulates of proportionality of the interaction term of difference in mean temperature of components is discussed. The effective conductivities of components in the mixture and the interaction coefficient are introduced and related to the so-called microstructure functions, which are functions of the microgeometry of the medium and the thermal properties of its components. Examples of the application of the theory to the calculation of the mean properties of a heterogeneous medium are presented.