Solvates of New Arylpiperazine Salicylamide Derivative-a Multi-Technique Approach to the Description of 5 HTR Ligand Structure and Interactions.

A new ligand for 5-HT1A and 5-HT7 receptors, an arylpiperazine salicylamide derivative with an inflexible spacer, is investigated to identify preferred fragments capable of creating essential intermolecular interactions in different solvates. To fully identify and characterize the obtained crystalline materials, various methods including powder and single-crystal X-ray diffraction, solid-state NMR, and thermal analysis were employed, supplemented by periodic ab initio calculations. The molecular conformation in different solvates, types, and hierarchy of intermolecular interactions as well as the crystal packing were investigated to provide data for future research focused on studying protein-ligand interactions. Based on various methods of crystal structure analysis, including the interaction energy calculation and programs using an artificial neural network, a salicylamide fragment was found to be crucial for intermolecular contacts, mostly of dispersion and electrostatic character. A supramolecular 2D kite-type layer of {4,4} topology was found to form in crystals. The closed voids between layers contain disordered solvents, very weakly interacting with the molecule and the layer. It has been postulated that the separation of the layers might be influenced by an increase in temperature or the size of the solvent; hence, only methanol and ethanol hemi-solvates could be obtained from a series of various alcohols.

Production of cytokines and stimulation of resistance to viral infection in human leukocytes by Scutellaria baicalensis flavones.

Extracts of Scutellaria baicalensis display a wide spectrum of antiviral activity. It was of great interest to check the effect of baicalein and wogonin preparations on two important mechanisms of innate immunity: the secretion of cytokines and the natural resistance of human leukocytes to viral infection. To study the effect of S. baicalensis extracts on interferons (IFNs), tumor necrosis factor alpha (TNF-alpha), and interleukin (IL) production and virus replication, uninfected and vesicular stomatitis virus (VSV)-infected human peripheral blood leukocytes (PBLs) were used. Four pulverized preparations obtained from roots of Scutellaria and a Sigma-Aldrich preparation of purified baicalein were used in the study. RPMI extracts containing different amounts of baicalein and wogonin were used to study the effect on VSV replication in PBLs. PBLs express ex vivo individually differentiated cytokine-dependent resistance/innate immunity to viral infections. The degree of resistance was estimated on the basis of VSV replication in PBLs. The results obtained indicate that baicalein- and wogonin-containing extracts modulate cytokine production, that is inhibit IFN-alpha and IFN-gamma and stimulate TNF-alpha and IL (IL-12, IL-10) production. They also augment the resistance of PBLs to VSV. Extract from S. baicalensis containing baicalein and wogonin regulates the innate antiviral immunity by modulation of cytokine production and stimulation of human leukocyte resistance.

Mechanisms ensuring optimal conditions of implantation and embryo development in the pig.

The paper summarizes results of a series of studies concerning luteolysis and early pregnancy in pigs. The involvement of the oxytocin (OT)/OT receptor system in the mechanism of corpus luteum (CL) protection during early pregnancy as well as the implication of luteinizing hormone (LH) in the endometrial prostaglandin (PG) release and synthesis are described. In addition, the role of leptin in the regulation of ovarian steroidogenesis and the expression of leptin and its receptor (OB-Rb) genes in hypothalamus, pituitary and reproductive tissues are reported. Moreover, a strong emphasis was placed on the mechanism of PGE2 participation in the local endocrine regulations of reproductive processes occurring in the utero-ovarian area as well as on the vascular endothelial growth factor (VEGF) ligand-receptor system in the ovary and uterus.

[Selected risk factors for coronary heart disease in a group of women aged 30-65 in Kraków]. / Wybrane czynniki ryzyka choroby niedokrwiennej serca w grupie kobiet w wieku 30-65 lat mieszkajacych w Krakowie.

Mortality rates due to cardiovascular diseases (CD) in Poland are almost twice higher than in the European Union countries. The mortality caused by CD has paid the attention on the fact that it increases relatively among women in comparison to men. Epidemiological observations conducted in female groups indicated that the ischaemic heart disease (IHD) appears more frequently after menopause. The aim of the study was to evaluate some IHD risk factors in the group of women aged 30-65 from Kraków. The study included 95 women, without IHD diagnosis, voluntarily registered to the practice of nurses group. The menopause occurrence and selected possible to modify CD risk factors as a concentration of the total cholesterol, LDL cholesterol, fasting glucose, C-reactive protein (CRP) and also blood pressure, body mass index and waist circumference were assessed. The smoking of tobacco was estimated by an objective method (the level of carbon monoxide in breath out--smoke check). The level of depression was evaluated with the use of Beck Inventory Scale. The results were calculating using Statistica Pl 6.0 programme. The investigated group, especially women after natural menopause, had higher CD risk factors such as: hypercholesterolemia, systolic hypertension, overweight, tobacco smoking, CRP and depression. The tobacco smoking appeared more often in the group after menopause because of other reasons and in the group of women with regular menstruation. The rate of depression was also higher among women after menopause because of other reasons.