Synthesis and Purine P2X Receptor Antagonist Activity of Thiazole Derivatives

The ability of 12 new thiazole derivatives to influence the muscle contractility mediated by purine P2X receptors has been studied in vitro using isolated tissues of rats and guinea pigs. Most of the synthesized compounds did not cause significant effects, but two compounds exhibited pronounced antagonism with respect to P2X-mediated contractility response. These compounds offer a good starting point for the synthesis of new effective antagonists of P2 receptors. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 6, pp. 22 – 25, June, 2005.     

Demolition Waste Potential for Completely Cement-Free Binders

Due to renovation and fighting in the world, a huge accumulation of construction and demolition waste is formed. These materials are effectively used as aggregates, but there is very little information about the use of scrap concrete to create cementless binders. The purpose of the work is to be a comprehensive study of the composition and properties of concrete wastes of various fractions with the aim of their rational use as cementless binders. The scientific novelty lies in the fact that the nature of the processes of structure formation of a cementless binder based on sandy fractions of the screening of fragments of destroyed buildings and structures, as a complex polyfunctional system, has been theoretically substantiated and experimentally confirmed. Different percentages of non-hydrated clinker minerals in concrete scrap were determined. In the smallest fraction (less than 0.16 mm), more than 20% of alite and belite are present. Waste of the old cement paste is more susceptible to crushing compared to the large aggregate embedded in it, therefore, particles of the old cement paste and fine aggregate predominate in the finer fractions of the waste. Comprehensive microstructural studies have been carried out on the possibility of using concrete scrap as a completely cementless binder using scanning electron microscopy, X-ray diffraction analysis, and differential thermal analysis. It has been established that for cementless samples prepared from the smallest fractions (less than 0.315 mm), the compressive strength is 1.5–2 times higher than for samples from larger fractions. This is due to the increased content of clinker minerals in their composition. The compressive strength of the cementless binder after 28 days (7.8 MPa), as well as the early compressive strength at the age of 1 day after steaming (5.9 MPa), make it possible to effectively use these materials for enclosing building structures.     

Selected Properties of Veneered Lightweight Particleboards with Expanded Polystyrene

The aim of this study was to improve the properties of lightweight particleboards by their veneering. The industrially produced wood particles, rotary-cut birch veneer, expanded polystyrene (EPS) granules and urea-formaldehyde (UF) resin were used to manufacture non-veneered and veneered boards in laboratory conditions. The boards were manufactured with different densities of 350, 450 and 550 kg/m³ and with various levels of EPS content 4, 7 and 10%. Boards without EPS granules as the reference were also manufactured. Bending strength (MOR), modulus of elasticity in bending (MOE), internal bond (IB) strength, thickness swelling (TS) and water absorption (WA) of lightweight particleboards were determined. This study confirmed that veneering of lightweight particleboards by birch veneer improved mechanical properties significantly. The MOR and MOE of veneered boards throughout the whole density range of 350–550 kg/m³ meet the requirements of the CEN/TS 16368 for lightweight particleboards types LP1 and LP2. The IB strength of veneered boards only with density of 550 kg/m³ meets the requirements of CEN/TS 16368 (type LP1). The MOR, MOE and IB of non-veneered boards also meet the requirements of CEN/TS 16368 (type LP1) except boards with density of 350 kg/m³ for MOR and MOE, and except densities of 350 and 450 kg/m³ for IB.     

Induction of natural IgE by glucocorticoids

IgE mediates allergic responses by coating mast cell or basophil surfaces and inducing degranulation upon binding a specific allergen. IgE can also be spontaneously produced in the absence of foreign allergens; yet the origin, regulation, and functions of such “natural” IgE still remain largely unknown. Here, we find that glucocorticoids enhance the production of IgE in B cells both in vivo and ex vivo without antigenic challenge. Such IgE production is promoted by B cell–intrinsic glucocorticoid receptor signaling that reinforces CD40 signaling and synergizes with the IL-4/STAT6 pathway. In addition, we found that rare B cells in the mesenteric lymph nodes are responsible for the production of glucocorticoid-inducible IgE. Furthermore, locally produced glucocorticoids in the gut may induce natural IgE during perturbations of gut homeostasis, such as dysbiosis. Notably, mice preemptively treated with glucocorticoids were protected from subsequent pathogenic anaphylaxis. Together, our results suggest that glucocorticoids, classically considered to be broadly immunosuppressive, have a selective immunostimulatory role in B cells.     

Chronic biopsy proven post‐COVID myoendocarditis with SARS‐Cov‐2 persistence and high level of antiheart antibodies

PurposeTo study the clinical signs and mechanisms (viral and autoimmune) of myoendocarditis in the long‐term period after COronaVIrus Disease 2019 (COVID‐19).MethodsFourteen patients (nine male, 50.1 ± 10.2 y.o.) with biopsy proven post‐COVID myocarditis were observed. The diagnosis of COVID‐19 was confirmed by IgG seroconversion. The average time of admission after COVID‐19 was 5.5 [2; 10] months. An endomyocardial biopsy (EMB) of the right ventricle was obtained. The biopsy analysis included polymerase chain reaction diagnosis of viral infection, morphological, immunohistochemical (IHC) examination with antibodies to CD3, CD45, CD68, CD20, SARS‐Cov‐2 spike, and nucleocapsid antigens. Coronary atherosclerosis was ruled out in all patients over 40 years.ResultsThe new cardiac symptoms (congestive heart failure 3–4 New York Heart Association class with severe right ventricular involvement, various rhythm, and conduction disturbances) appeared 1–5 months following COVID‐19. Magnetic resonance imaging showed disseminated or focal subepicardial and intramyocardial late gadolinium enhancement, hyperemia, edema, and increased myocardial native T1 relaxation time. Antiheart antibodies levels were increased 3–4 times in 92.9% of patients. The mean left ventricular (LV) ejection fraction (EF) was 28% (24.5; 37.8). Active lymphocytic myocarditis was diagnosed in 12 patients, eosinophilic myocarditis in two patients. SARS‐Cov‐2 RNA was detected in 12 cases (85.7%), in association with parvovirus B19 DNA—in one. Three patients had also endocarditis (infective and nonbacterial, with parietal thrombosis). As a result of steroid and chronic heart failure therapy, the EF increased to 47% (37.5; 52.5).ConclusionsCOVID‐19 can lead to long‐term severe post‐COVID myoendocarditis, that is characterized by prolonged persistence of coronavirus in cardiomyocytes, endothelium, and macrophages (up to 18 months) in combination with high immune activity. Corticosteroids and anticoagulants should be considered as a treatment option of post‐COVID myoendocarditis.     

Formation of Micro- and Nanostructures on the Nanotitanium Surface by Chemical Etching and Deposition of Titania Films by Atomic Layer Deposition (ALD)

In this study, an integrated approach was used for the preparation of a nanotitanium-based bioactive material. The integrated approach included three methods: severe plastic deformation (SPD), chemical etching and atomic layer deposition (ALD). For the first time, it was experimentally shown that the nature of the etching medium (acidic or basic Piranha solutions) and the etching time have a significant qualitative impact on the nanotitanium surface structure both at the nano- and microscale. The etched samples were coated with crystalline biocompatible TiO₂ films with a thickness of 20 nm by Atomic Layer Deposition (ALD). Comparative study of the adhesive and spreading properties of human osteoblasts MG-63 has demonstrated that presence of nano- and microscale structures and crystalline titanium oxide on the surface of nanotitanium improve bioactive properties of the material.