The synthesis and antiviral activity of glycyrrhizic acid conjugates with alpha-D-glucosamine and some glycosylamines

Glycyrrhizic acid and its 30-methyl ester were conjugated with 2-amino-1,3,4,6-tetra-O-acetyl-2-deoxy-alpha-D-glucopyranose, 2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl amine, 2,3,4-tri-O-acetyl-apha-L-arabinopyranosyl amine, 2-acetamido-2-deoxy-beta-D-glucopyranosyl amine, and beta-D-galactopyranosyl amine using N,N'-dicyclohexylcarbodiimide and its mixtures with N-hydroxybenzotriazole. Structures of the conjugates were confirmed by IR, UV, 1H, and 13C NMR spectroscopy. The glycoconjugate with the residues of 2-acetamido-2-deoxy-beta-D-glucopyranosyl amine in the carbohydrate part of its molecule exhibited antiviral activity (ID50 4 microg/ml) toward the herpes simplex type 1 virus (HSV-1) in the VERO cell culture. Two compounds demonstrated anti-HIV-1 activity (50-70% inhibition of p24) in a culture of MT-4 cells at concentrations of 0.5-20 microg/ml. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2004, vol. 30, no. 3; see also http://www.maik.ru.     

Cone-beam tomography of congenital fissures of the alveolar process and palate

Cone-beam tomography is one of the current radiodiagnostic techniques, which allows patients with congenital fissures of the alveolar process and soft and hard palates to be examined, by minimizing the radiation load. On surgical treatment planning, cone-beam tomography makes it possible to estimate the extent of a bone defect in the alveolar process, its sizes, the presence or absence of oronasal fistulas, the position of the intermaxilla, the state of bone tissue (sizes, density characteristics) in the genial area for an autograft, the degree of a maxillofacial deformity, and occlusive features. Postoperative cone-beam tomography permits one to estimate the degree of alveolar process recovery, the sizes of a regenerate, the processes of osteointegration, and the state of fixing elements and the donor bed.     

Influence of omeprasole and lansoprasole on Na+, K+ -ATPase and Mg2+ -ATPase activity of the plasmatic membrane of myometrium smooth muscle cells

The paper deals with the influence of the proton pump inhibitors - omeprasole and lansoprasole on the enzymatic activity of the ouabain-sensitive Na+, K+ -ATPase and the ouabain-resistant Mg2+ - ATPase in the suspension of the myometrium cell plasmatic membranes treated with 0.1% digitonin solution. It was found, that omeprasole and lansoprasole inhibited Na+, K+ -ATPase in the range from 10 to 100 microM. The maximal effect was observed at a concentration of 100 microM with the percentage of inhibition of 81 and 86% at an average as compared with the control for omeprasole and lansoprasole, respectively. The magnitudes of the inhibition coefficient I(0.5) for omeprasole and lansoprasole were 35.60 +/- 0.81 and 29.40 +/- 1.79 microM respectively. Meanwhile cooperative effects on the Na+, K+ - ATPase activity were not found, as the Hill coefficient n(H) for omeprasole was 1.00 +/- 0.08, while for lansoprasole it was 1.20 +/- 0.03. These substances had also insignificant influence on Mg2+ -ATPase: the enzymatic activity was decreased to 84 and 82% as compared with the control with omeprasole and lansoprasole, respectively, in concentration of 100 microM for each inhibitor. The inhibition of Na+, K+ -ATPase activity can evidence for the possible side effects of omeprasole and lansoprasole when they are used for treatment of acid-dependent diseases of the stomach. In addition, obtained experimental data can be useful for further research of the membrane mechanisms of omeprasole and lansoprasole action on cationic exchange in the smooth muscle cells.     

The role of beta-adrenoreceptors in the mechanism of the hemodynamic action and radiation-protective activity of the copolymer of 2-methyl-5-vinylpyridine with 2-methyl-5-vinylpyridinium-N-oxide

In experiment on anesthetized dogs and cats in was shown that the new water-soluble copolymer initiated depressive reaction characteristic for beta-adrenomimetics. This effect was levelled with the help of non-selective adrenoblockator--propranololum. In experiment on dogs the preliminary treatment with propranololum decreased the therapeutic antiradiation efficiency of the copolymer from 68.4 to 8.3%.     

Neuroprotective effect of N-acylethanolamines in chronic morphine dependence. II. Effect on the rat brain fatty acid composition

The effect of N-acylethanolamines mixture (NAE) with saturated and unsaturated acyl chains on the fatty acid composition of the rat brain under chronic morphine dependence was investigated. Long-term administration of NAE reduced morphine-induced decrease of mono- and polyunsaturated fatty acids in the rat brain crude lipid extract. Furthermore, NAE restored the acyl chain spectrum, especially the content of docosahexaenoic acid in essential phospholipids--phosphatidylcholine and phosphatidylethanolamine. Pharmacological activity of NAE depended on a dose.     

Mechanism of direct cell interactions. Self-organization of protein synthesis rhythm

Primary 24-hour cultures of hepatocytes on slides in a serum-free medium were studied. Circahoralian rhythm of protein synthesis served as a marker of cell cooperation. Stimulation of protein kinase activities by phorbol 12-myristate 13-acetate at 0.5 or 1.0 microM or forskolin at 10 microM led to visualization of the protein synthesis rhythm in sparse cultures, which were asynchronous in the control and with linear kinetics of protein synthesis. Inhibitors of protein kinase activities H7 (1-(5-isoquinolinylsulfonyl)-5-methylpiperasine dihydrochloride) at 40 microM or H8 (N-(2-[methylamino]ethyl)-5-isoquinolinesulfonamide hydrochloride) at 25 microM eliminated the protein synthesis rhythm in dense cultures, which are normally synchronous with oscillatory kinetics of protein synthesis. After inhibition of the protein kinase activities, gangliosides or phenylephrine did not synchronize the protein synthesis rhythm. Phorbol 12-myristate 13-acetate modulated the protein synthesis rhythm, shifted the rhythm phase, i.e., stimulation of the protein kinase activities, and, correspondingly, protein phosphorylation may be a factor of synchronization of synthesis oscillations in individual cells and of population rhythm formation. Thus, a cascade of processes leading to self-organization of hepatocytes during formation of summarized protein synthesis was revealed in a series of studies: signal of gangliosides or other calcium agonists-->changes in the level of calcium ions in cytoplasm-->increased protein kinase activities-->protein phosphorylation-->modulation of individual oscillations in the intensity of protein synthesis and their coordination in a summarized rhythm. cAMP-dependent protein kinases also affect the protein synthesis rhythm. Protein phosphorylation is a key process. The mechanisms of cell self-organization are similar in vitro and in vivo, specifically in the liver in situ.     

Participation of the cava vein blood flow in forming the total venous return under influence of different modality stimuli on the circulation system

Participation of the anterior and posterior veins cava in forming the total venous return under pressor and depressor effects, stimulation of depressing foci of the medulla's ventral part, enhancement of pulmonary ventilation, hypoxia, hypothermia, administration of acetylcholine, histamine, corinfar, was shown to depend on the blood flow shift direction in each of the veins cava, dynamics of shifts' development in time, and intensity of the stimulus. In systemic responses, the blood flow shifts in the vena cava anterior much contribute to the total venous return at the maximum of the systemic arterial pressure rise (r = 0.87) whereas contribution of the vena cava posterior is the greatest during a later occurring increase in the venous return (r = 0.84). Along with increase in the stimulus intensity the vena cava anterior's part in forming the venous return becomes more limited whereas that of the vena cava posterior is enhanced.     

Local disinhibition with bicuculline does not break the trained relationship between afferent input and efferent output in cat motor cortex

Neurons of the cat motor cortex related to the lifting-withdrawal phase of forepaw placing reaction are preferentially activated by tactile stimulation of the dorsal surface of the forepaw. The placing reaction was altered in such a way that the innate "dorsal placing" was subjected to extinction and was substituted for the newly acquired conditioned reaction in response to the ventral side stimulation. This alteration of placing reaction led to the inversion of the innate input-output relationship in the motor cortex. The neurons related to forepaw lifting-withdrawal began to be activated by tactile stimulation of the ventral rather than dorsal forepaw surface. Local cortical disinhibition by bicuculline application at the recording site qualitatively changed neither normal input-output relationships nor inverse relationships after placing reaction alteration. This suggests that alteration of the sensorimotor coordination in cat motor cortex is underlain by changes in excitatory rather than inhibitory connections.     

Aerobic methanotrophic communities in the bottom sediments of Lake Baikal

The results of the first methodical investigation into the aerobic methanotrophic communities inhabiting the bottom sediments of Lake Baikal are reported. Use of the radioisotopic method revealed methane consumption in 12 10- to 50-cm-long sediment cores. The maximum methane consumption rates (495-737 microl/(dm3 day) were recorded in sediments in the regions of hydrothermal vents and oil and gas occurrence. Methane consumption was most active in the surface layers of the sediments (0-4 cm); it decreased with the sediment depth and became negligible or absent at depths below 20 cm. The number of methanotrophic bacteria usually ranged from 100 to 1000 cells/cm3 of sediment and reached 1 million cells/cm3 in the regions of oil and gas occurrence. The 17 enrichment cultures obtained were represented mainly by morphotype II methanotrophs. Phylogenetic analysis of the enrichment cultures in terms of the amino acid sequence of the alpha subunit of the membrane-bound methane monooxygenase revealed the predominance of methanotrophs of the genus Methylocystis. The results obtained suggest the presence of an active aerobic methanotrophic community in Lake Baikal.     

Some electrophysiological and hemodynamic characteristics of auditory selective attention in norm and schizophrenia

Six patients in the state of remission after the first episode ofjuvenile schizophrenia and seven sex- and age-matched mentally healthy subjects were examined by fMRI and ERP methods. The auditory oddball paradigm was applied. Differences in P300 parameters didn't reach the level of significance, however, a significantly higher hemodynamic response to target stimuli was found in patients bilaterally in the supramarginal gyrus and in the right medial frontal gyrus, which points to pathology of these brain areas in supporting of auditory selective attention.