Tubulin inhibitors. Selected scaffolds and main trends in the design of novel anticancer and antiparasitic agents.

Design of tubulin inhibitors as anticancer drugs dynamically developed over the past 20 years. The modern arsenal of potential tubulin-targeting anticancer agents is represented by small molecules, monoclonal antibodies, and antibody-drug conjugates. Moreover, targeting tubulin has been a successful strategy in the development of antiparasitic drugs.

Click chemistry in the synthesis of antibody-drug conjugates.

Antibody-Drug Conjugates (ADC) are a new class of anticancer therapeutics with immense potential. They have been rapidly advancing in the last two decades. This fast speed of development has become possible due to several new technologies and methods.

Multi-Targeting Anticancer Activity of a New 4-Thiazolidinone Derivative with Anti-HER2 Antibodies in Human AGS Gastric Cancer Cells.

Combining chemotherapy with immunotherapy still remains a regimen in anticancer therapy. Novel 4-thiazolidinone-bearing hybrid molecules possess well-documented anticancer activity, and together with anti-HER2 antibodies, may represent a promising strategy in treating patients with gastric cancer with confirmed human epidermal growth factor receptor 2 (HER2) expression. The aim of the study was to synthesize a new 4-thiazolidinone derivative (Les-4367) and investigate its molecular mechanism of action in combination with trastuzumab or pertuzumab in human AGS gastric cancer cells.

Changes in mental health during three waves of the COVID-19 pandemic: a repeated cross-sectional study among polish university students.

Background: Research indicates that mental health worsened during the Coronavirus crisis, in particular among women and university students. However, few longitudinal studies have so far investigated the changes in mental health outcomes across three subsequent waves of the COVID-19 pandemic. Therefore, this study aims to examine changes in mental health among university students.

New Perspectives for the Use of Potentilla alba Rhizomes to Treat Thyroid Gland Impairments.

is a valuable medicinal plant that has been highly praised even before its first appearance in herbal books; however, it has now been forgotten in Western Europe. Currently, this species is used in Eastern Europe as a remedy to treat dysentery and various thyroid gland dysfunctions. The present review summarizes the advances in the phytochemical, pharmacological, and toxicological research related to this plant species.

The influence of occupants' body mass on carbon dioxide mass flow rate inside a university classroom - case study.

From 2014 to 2017, through the cold season, 37 experimental measurements of carbon dioxide (CO) concentration were done inside a selected university classroom, during the same type of activity, namely written examination. Based on the data obtained from the experimental measurements, the article sought to primarily establish a correlation between the body mass of the students and the intensity of carbon dioxide releases inside the experimental classroom. This relationship was determined by using statistical analysis (general least-square estimation of the regression line).

Effect of chlorotriphenyl derivatives of Sn and Pb upon biophysical properties of membranes.

Biophysical activity of two twin organometallic compounds Triphenyltin chloride (TPhT) and Triphenyllead chloride (TPhL) in their interreaction with model membranes, as well as with yeast cells Saccharomyces cerevisiae, was investigated. Four measurement methods were used in the experiments: two physical methods (spin probes method and the electric method); two biological methods (minimal inhibitory concentration /MIC/ and yeast survival test). It has been found that the activity of TPhT in interaction with model membranes and yeast cells is distinctly greater than that of TPhL.

Tin compounds interaction with membranes of egg lecithin liposomes.

This work is a continuation of earlier research concerning the influence of tin compounds on the dynamic properties of liposome membranes produced with lecithin hen egg yolks (EYL). The experiments were carried out at room temperature (about 25 degrees C). Four tin compounds were chosen, including three organic ones, (CH3)4Sn, (C2H5)4Sn and (C3H7)3SnCl, and one inorganic, SnCl2.

Effect of organic tin compounds on electric properties of model membranes.

The objective of the present work was to investigate the effect of selected organic tin compounds and potassium chloride (used as a reference substance) on the trans-membrane electric voltage and electric resistance of model membranes, the latter being nitrocellulose filters impregnated with butylene ester of lauric acid. The increasing KCl concentration (in the measurement chambers) caused a rapid rise of the negative trans-membrane voltage, whose value stabilized afterwards. In the case of (C3H7)3SnCl an abrupt maximum of the negative voltage was observed followed by a monotonic drop to zero.

The influence of tin compounds on the dynamic properties of liposome membranes: a study using the ESR method.

The influence of organic and inorganic compounds of tin on the dynamic properties of liposome membranes obtained in the process of dipalmitoylphosphatidylcholine (DPPC) sonication in distilled water was investigated. This was carried out by means of the spin ESR probe method. The probes were selected in such a way as to penetrate different areas of the membrane (a TEMPO probe, 5-DOXYL stearic acid, 16-DOXYL stearic acid).

Comparison of the blood plasma catecholamines level in thoroughbred and Arabian horses during the same-intensity exercise.

The aim of this study was to compare changes in epinephrine (E), norepinephrine (NE) and dopamine (DA) levels in blood plasma of two racehorses breeds: Arabian and Thoroughbred during moderate intensity exercise performed in the same conditions. The increase in plasma E level just after exercise was higher in Thoroughbreds than in Arabians. During the whole test, the Arabians showed the higher levels of NE and DA as compared to those found in Thoroughbreds.

Electric interactions at the lipid membrane surface.

This work presents the results of an experimental study and of computer simulations concerning electric interactions in the surface layer of egg yolk lecithin (EYL) liposome membranes. The surface layer is formed by EYL polar heads, which possess features of electric dipoles, and positive charged polar heads belonging to admixtures of quaternary ammonium salts (AS). The results of the experimental study are in good agreement with the ones of the computer simulations.

Computer simulations of the electric interactions between the phospholipid head-groups and ionic admixtures in the membrane surface.

Some phospholipids (e.g. lecithin) form a system of electric dipoles on the membrane surface layer.

ESR study of the liposome membrane physical parameters in the heating-cooling cycles.

Changes of dynamic and structural parameters of egg yolk lecithin (EYL) liposome membranes in the heating-cooling cycles have been studied using the ESR spin probe method. The investigations were conducted in the range of temperatures from -18 degrees C to +60 degrees C. It has been found that in the range of temperatures -15 degrees C to +45 degrees C in both the heating and the cooling run the spectroscopic parameters changed practically along the same curve (reversible changes).

Biological indicators for the assessment of human exposure to organophosphorous compounds.

Unlabelled: The aim of the present study is to review selected biological effects of organophosphorous compounds used as pesticides and to discuss their significance in terms of occupational exposure. The results of a long-term study of the red cells and plasma ChE in group of workers engaged in the production of pesticides are also presented. Cholinesterase activity in plasma and red blood cells was determined spectrophotometrically by the Ellman modified method.

Bimodal effect of amphiphilic biocide concentrations on fluidity of lipid membranes.

Using the spin label method (ESR) it has been shown that biologically active, amphiphilic compounds (quaternary ammonium salts (AS) containing polar heads with single and double positive charge caused, at low concentrations, decrease fluidity of liposome membranes formed with egg yolk lecithin (EYL). At higher concentrations an increase in fluidity was observed. With compounds having a single positive charge minimum fluidity of membrane structure occurs in the range of 1 to 3%, with compounds containing double positive charge-in the range of 4-6%.

Activity of placental glutathione peroxidase and superoxide dismutase in cows with and without retained fetal membranes.

Changes in the levels of the activity of two enzymes that neutralize free radicals-glutathione peroxidase [(EC.1.11.

Secondary processing of chondrules and refractory inclusions (CAIs) by gasdynamic heating.

A theoretical model of aerodynamic heating of a meteoric particle upon entry into a parent body atmosphere is presented. The model includes the effects of melting, vaporization, and heat conduction into the particle interior. Properties of chondrule rims are interpreted in the context of the model.

Are some chondrule rims formed by impact processes? Observations and experiments.

Observations and experimental evidence are presented to support the hypothesis that high-speed impact into a parent body regolith can best explain certain textures and compositions observed for rims on some chondrules. A study of 19 interclastic rimmed chondrules in the Weston (H 3/4) ordinary chondrite shows that two main rim types are present on porphyritic olivine-pyroxene (POP) and porphyritic pyroxene (PP) chondrules: granular and opaque rims. Granular rims are composed of welded, fine-grained host chondrule fragments.

Processing of refractory meteorite inclusions (CAIs) in parent-body atmospheres.

The refractory meteorite inclusions known as CAIs (calcium-aluminum rich inclusions) display melted rims that were produced by thermal events of only a few seconds duration. We show that gas dynamic deceleration in a temporary atmosphere around an accreting parent body, produced by gas release during accretion, could provide a regime of sufficiently high gas density and small scale height to achieve partial melting of the CAIs. In addition, the presence of dust in the atmosphere would increase the gradient of pressure with height (i.

Evaluation of flow through simulated vascular stenoses with gradient echo magnetic resonance imaging.

Magnetic resonance imaging using gradient echo sequences can quickly generate dynamic images of the cardiovascular system. We used a gradient echo sequence (repetition time = 21 milliseconds, echo time = 12 milliseconds, flip angle = 30 degrees) to evaluate how a simulated vascular stenoses affects the signal intensity of flowing fluid. Axial slices were obtained at regular intervals along a plastic tube containing a circular constriction (25%, 51%, or 73% reduction of cross-sectional area).

Radiogenic heating of comets by 26Al and implications for their time of formation.

The effect of radiogenic heating on the thermal evolution of spherical icy bodies with radii 1 km < R < 100 km was investigated. The radioisotopes considered were 26Al, 40K, 232Th, 235U, and 238U. Except for the 26Al abundance, which was varied, the other initial abundances were kept fixed, at values derived from those of chondritic meteorites and corresponding to a gas-to-dust ratio of 1.