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1.
Spectrochim Acta A Mol Biomol Spectrosc ; 267(Pt 2): 120597, 2022 Feb 15.
Article in English | MEDLINE | ID: mdl-34802932

ABSTRACT

We present complex spectroscopic data of the synthetic brunogeierite (Fe2+)2Ge4+O4 with space group Fd3¯m of spinel structure: a = 8.3783 (6) Å, V = 588.12 (13) Å3. Brunogeierite crystals up to 200 µm in size were crystallized by the interaction of a boric acid solution on a metal iron wire in the presence of germanium oxide (GeO2) at 600/650 °C and 100 MPa. Mössbauer spectrum of synthetic brunogeierite consists of the symmetric doublet with the parameters IS = 1.104(1) mm/s and QS = 2.845(1) mm/s, that corresponds to the octahedral position of iron ions ([VI]Fe2+). The Raman spectra of Fe2GeO4 crystal consist of an intense main band at 756 cm-1 and four less intense bands at ∼644, 472, 302, and ∼205 cm-1 at ambient conditions. All five bands inherent in the spectrum of cubic spinel are present and gradual change in high pressure spectra up to 30 GPa. The color of the crystal changes from brown-orange to reddish at the center at 22.7 GPa and became opaque black up to 30.2 GPa. Herewith, in the high pressure spectra, we observed the splitting of some bands and the appearance of additional bands in a wide pressure range (from 1.6 to 30 GPa). The factor group analysis with the lattice dynamics calculation of potential crystal structure distortions shows the decreasing of the structure symmetry to tetragonal or rhombohedral in this pressure range.

2.
Dokl Biochem Biophys ; 488(1): 313-315, 2019 Sep.
Article in English | MEDLINE | ID: mdl-31768849

ABSTRACT

Selective anxiolytic fabomotizole (Afobazol®) has affinity for the Sigma-1 chaperone receptor site, quinone reductase 2 (NQO2) and MAO-A regulatory sites, and melatonin receptor type 1 (MT1 receptor). The analysis of the effect of fabomotizole on the gene expression profile in the brain of MR (Maudsley Reactive) rats was carried out when modeling emotional stress in the open field test. A change in the expression of 14 genes was found, the results of the functional annotation of which showed that the mechanisms of action of fabomotizole may be associated with the regulation of translation of proteins (Rpl5, Rpl15, Ncl, and Ybx1), synaptic functions (Cplx2, Dlg4, Syngap1, Add1, Rab8b, Klc1, and Chn1), and cellular metabolism (Akr1d1, Bcat1, and Pkm).


Subject(s)
Anti-Anxiety Agents , Behavior, Animal/drug effects , Benzimidazoles/pharmacology , Brain , Gene Expression Regulation/drug effects , Morpholines/pharmacology , Nerve Tissue Proteins/biosynthesis , Stress, Psychological , Animals , Anti-Anxiety Agents/chemistry , Anti-Anxiety Agents/pharmacology , Brain/metabolism , Brain/pathology , Brain/physiopathology , Kinesins , Microtubule-Associated Proteins , Rats , Receptors, Melatonin , Stress, Psychological/drug therapy , Stress, Psychological/metabolism , Stress, Psychological/pathology , Stress, Psychological/physiopathology
3.
J Helminthol ; 93(1): 42-49, 2019 Jan.
Article in English | MEDLINE | ID: mdl-29382411

ABSTRACT

Trichinellosis, a zoonotic disease caused by nematodes of the genus Trichinella, is still a public health concern in the Arctic. The aims of this study were to investigate the seroprevalence of anti-Trichinella IgG in aboriginal peoples of two settlements in the Chukotka Autonomous Okrug (Russian Federation) on the Arctic coast of the Bering Sea, and to evaluate the survival of Trichinella nativa larvae in local fermented and frozen meat products. A seroprevalence of 24.3% was detected in 259 people tested by an enzyme-linked immunosorbent assay (ELISA). The highest prevalence was detected among people who consumed traditional local foods made from the meat of marine mammals. Trichinella nativa larvae were found to survive for up to 24 months in a fermented and frozen marine mammal meat product called kopalkhen. Since the T. nativa life cycle can be completed in the absence of humans, it can be expected to persist in the environment and therefore remain a cause of morbidity in the human populations living in Arctic regions.


Subject(s)
Frozen Foods/parasitology , Meat/parasitology , Trichinellosis/epidemiology , Animals , Antibodies, Helminth/blood , Aquatic Organisms/parasitology , Arctic Regions/epidemiology , Enzyme-Linked Immunosorbent Assay , Humans , Immunoglobulin G/blood , Larva/physiology , Prevalence , Russia/epidemiology , Seroepidemiologic Studies , Trichinella/immunology , Trichinellosis/ethnology
4.
Bull Exp Biol Med ; 165(5): 649-652, 2018 Sep.
Article in English | MEDLINE | ID: mdl-30225697

ABSTRACT

Using the streptozotocin model of type 2 diabetes mellitus in Wistar rats, we compared antidiabetic activity of anxiolytic Afobazole with that of metformin. Afobazole in a dose of 10 mg/kg reduced streptozotocin-induced hyperglycemia and polyphagia and prevented accumulation of malonic dialdehyde, being not inferior to metformin in a dose of 300 mg/kg, and was even more effective than metformin in body weight recovery, elimination of polydipsia, and preservation of these effects after treatment withdrawal.


Subject(s)
Benzimidazoles/pharmacology , Diabetes Mellitus, Experimental/drug therapy , Hyperglycemia/drug therapy , Hyperphagia/prevention & control , Hypoglycemic Agents/pharmacology , Metformin/pharmacology , Morpholines/pharmacology , Animals , Anti-Anxiety Agents/pharmacology , Blood Glucose/drug effects , Body Weight/drug effects , Diabetes Mellitus, Experimental/chemically induced , Diabetes Mellitus, Experimental/metabolism , Diabetes Mellitus, Experimental/pathology , Drug Repositioning , Hyperglycemia/chemically induced , Hyperglycemia/metabolism , Hyperglycemia/pathology , Male , Rats , Rats, Wistar , Streptozocin
5.
Bull Exp Biol Med ; 159(1): 44-7, 2015 May.
Article in English | MEDLINE | ID: mdl-26033588

ABSTRACT

Cell damage depending on activity of quinone reductase 2 (MT3 receptor) was simulated in experiments on bone marrow cell suspension and assessed by menadione-induced DNA breaks measured by comet assay. We analyzed the protective effect of afobazole interacting with MT1, MT3, σ1 receptors, and monoamine oxidase A and its main metabolite M11 that specifi cally binds to MT3 receptors. Both compounds reduced the level of menadione-induced DNA damage (afobazole was effective in lower concentrations in comparison with M-11). Conclusion was made on the contribution of MT3 receptors to the protective effect of afobazole, but the observed concentration differences indicate possible contribution of other targets of anxiolytic drug to the protective mechanisms.


Subject(s)
Anti-Anxiety Agents/pharmacology , Benzimidazoles/pharmacology , Bone Marrow Cells/drug effects , DNA Breaks/drug effects , Morpholines/pharmacology , Neuroprotective Agents/pharmacology , Quinone Reductases/antagonists & inhibitors , Receptors, Melatonin/drug effects , Animals , Anti-Anxiety Agents/metabolism , Benzimidazoles/metabolism , Biotransformation , Cells, Cultured , Comet Assay , Dicumarol/pharmacology , Drug Evaluation, Preclinical , Metallothionein 3 , Mice , Monoamine Oxidase , Monoamine Oxidase Inhibitors , Morpholines/metabolism , NAD(P)H Dehydrogenase (Quinone)/antagonists & inhibitors , Neuroprotective Agents/metabolism , Quinone Reductases/metabolism , Receptor, Melatonin, MT1/drug effects , Receptors, sigma/drug effects , Vitamin K 3/toxicity
6.
Mater Sci Eng C Mater Biol Appl ; 38: 143-50, 2014 May 01.
Article in English | MEDLINE | ID: mdl-24656362

ABSTRACT

Two novel macrocyclic 6-methyluracilic amphiphiles (uracilophanes) with four (UP1) and two (UP2) uracil moieties and ammonium groups have been synthesized. Tetracationic multi-uracilophane is composed of two macrocyclic units bridged each other with an external methylene spacer, while in the cryptand-like dicationic uracilophane pyrimidinic moieties are connected with an internal methylene spacer. This internal spacer provided a conformational rigidity to the macrocycle. The self-assembly of the uracilophanes is studied and compared with a reference dicationic uracilophane (UP3) with no spacer fragment. Compounds UP1 and UP3 are capable of aggregating, which is characterized by the analogous critical micelle concentration of 1mM, although the former has four decyl tails versus two decyl tails in UP3 molecule. NMR self-diffusion, fluorimetry and DLS techniques revealed that bimodal size distribution occurs in the UP1 solution, with small (≤2nm) and large (ca. 30-50 nm) aggregates contributed. Unexpectedly, the cryptand-like uracilophane UP2 with the same hydrophobicity as UP3 does not form aggregates. The balance of the geometry and energetic factors was analyzed and compared with those contributing to the aggregation of the reference compound UP3. It was established that it is the geometry that controls the packing of the cryptand-like uracilophanes upon aggregation, while hydrophobic effect plays a minor role. In contrast, both factors control the aggregation of oligomeric macrocycle, with energetic factor prevailing. These findings are of importance for (i) the understanding the diverse structural behavior of bioamphiphiles that have very similar chemical structure, but different conformations; and (ii) the design of amphiphiles with controlled model of self-assembly. Supramolecular systems studied can be recommended for biotechnological applications.


Subject(s)
Macrocyclic Compounds/chemistry , Macrocyclic Compounds/chemical synthesis , Surface-Active Agents/chemistry , Surface-Active Agents/chemical synthesis , Uracil/chemistry , Conductometry , Diffusion , Electric Conductivity , Hydrolysis , Light , Magnetic Resonance Spectroscopy , Nitrophenols/chemistry , Particle Size , Scattering, Radiation , Solutions , Spectrometry, Fluorescence , Surface Tension , Temperature
7.
Bull Exp Biol Med ; 155(3): 370-2, 2013 Jul.
Article in English | MEDLINE | ID: mdl-24137606

ABSTRACT

Antimutagenic effects of polypeptides isolated from Triticum kiharae wheat plantule extracts have been studied on human cells exposed to cadmium chloride. The most effective polypeptide Tk-AMP-BP ß -purothionin exhibited higher antimutagenic activity than wheat water extract and another peptide isolated from the same wheat species, Tk-AMP-γ 2 defensin; it also produced a pronounced antioxidant effect. This polypeptide can be used as a preventive agent for reducing the mutagenic potential of some environmental pollutants and for correction of human diseases associated with the defense system defects.


Subject(s)
Antimicrobial Cationic Peptides/pharmacology , Antimutagenic Agents/pharmacology , Antioxidants/pharmacology , Plant Extracts/pharmacology , Plant Proteins/pharmacology , Triticum/chemistry , Cadmium Chloride/adverse effects , Cells, Cultured , Defensins/pharmacology , Humans , Luminescent Measurements , Lymphocytes/drug effects
9.
Med Parazitol (Mosk) ; (3): 10-5, 2011.
Article in Russian | MEDLINE | ID: mdl-21932540

ABSTRACT

The structure of a parasite system is formed and its functioning takes place in qualitatively different environments. The aquatic environment serves as a source of new elements and modules, energy, and information for parasite systems. And the parasite systems, for their part, affect the physical and biological parameters of the environment. Many intestinal infections caused by pathogenic microorganisms generally characterized by an acute disease course are related to a water factor. Such are typhus, typhoids, dysentery, cholera, salmonellosis, virus hepatitis, and others. Many parasitic diseases caused by pathogenic intestinal protistae (lambliasis, amebiasis, balantidiasis), blood parasite protistae (malaria), helminthes (opisthorchiasis, fascioliasis, diphyllobothriasis, cercariosis, pseudoamphistomosis) are also closely related to a water factor. Ascaridiasis, hymenolepiasis, trichocephalosis, and echinococcosis have a less close but still self-evident relationship to a water factor. The clbse relationships of many parasitic diseases to a water factor are also determined by the fact that the life cycles of many parasites necessarily include various intermediate hosts and parasite vectors, such as fishes, mollusks, crustaceans, and insects, which are aquatic organisms at some stages of their life. The results of continuous exposure of people to parasitic diseases are quite similar to the suppressive effects of the environment in the ecologically troublesome regions. The most prognostically useful information is formed while mapping by medical and ecological regions, by employing a combination of current mathematical and cartographical methods. The former include cluster analysis, quartering method, informational logical analysis, which are all described in this article and others. Regional mapping using the parasitological criteria should achieve at least two goals: 1) a scientific one that aids in finding causative connections and to prognosticate a situation; 2) a practical one that assists in developing regional programs for disease control and prevention. It is necessary to use the recommendations described in detail in the article in order to have the maximum results during medical and ecological mapping by the regions with a future goal of obtaining useful prognostic information.


Subject(s)
Aquatic Organisms/physiology , Ecology/organization & administration , Parasites/physiology , Parasitic Diseases/epidemiology , Parasitic Diseases/prevention & control , Animals , Aquatic Organisms/microbiology , Aquatic Organisms/parasitology , Aquatic Organisms/virology , Cluster Analysis , Ecosystem , Host-Parasite Interactions , Humans , Information Theory , Parasites/microbiology , Parasites/parasitology , Parasites/virology , Parasitic Diseases/microbiology , Parasitic Diseases/parasitology , Parasitic Diseases/virology , Research Design , Russia , Water/physiology
11.
Genetika ; 46(7): 981-9, 2010 Jul.
Article in Russian | MEDLINE | ID: mdl-20795503

ABSTRACT

Polymorphism of a 8 10-bp mitochondrial cox1 gene region was studied in 16 cercaria isolates of bird schistosomes (family Schistosomatidae), which were collected in water bodies of Moscow and Moscow oblast and represented three species: Trichobilharzia szidati, T. franki, and T. regenti. A substantial predominance of AT (65.4%) was characteristic of the cox1 sequences in all three species. Rare single nucleotide substitutions determined low (0.2-0.9%) intraspecific nucleotide and amino acid sequence diversity. Haplotype diversity h was high (80-100%) in all three species, suggesting a unique character for almost all cox1 sequences in the sample. Phylogenetic trees based on the nucleotide and amino acid sequence variations were constructed to study the relationships of the three schistosome species. A high support was observed for the main branching node that reflects differentiation of the monophyletic group Trichobilharzia and species of the genera Bilharziella (B. polonica), Dendritobilharzia (D. pulverulenta), and Gigantobilharzia (G. huronensis). Based on the nucleotide substitutions and amino acid polymorphisms, two groups of isolates, which infect Lymnaea stagnalis (T. szidati) and snails of the group Radix (T. franki and T. regenti) respectively, were isolated in the genus Trichobilharzia. The time of divergence between the two schistosome groups infecting snails of the genera Radix and Lymnaea was calculated from the cox1 nucleotide substitution rate, which is known for Asian and Indian blood flukes from the genus Schistosoma and is 2-3% per million years on average. Divergence of the three bird schistosome species under study and divergence of the Asian species of mammalian schistosome were almost concurrent, dating back to 2.5-3.8 Myr ago. Factors responsible for the lack of intraspecific subdivision with respect to the cox1 gene in bird schistosomes and the lack of separation between two species (T. franki and T. regenti) are discussed.


Subject(s)
Electron Transport Complex IV/genetics , Helminth Proteins/genetics , Mitochondrial Proteins/genetics , Phylogeny , Polymorphism, Genetic , Schistosoma/genetics , Animals , Birds/parasitology , Moscow
12.
Med Parazitol (Mosk) ; (2): 53-9, 2010.
Article in Russian | MEDLINE | ID: mdl-20608188

ABSTRACT

According updates on molecular genetics, the development of human schistosomes in Asia with subsequent migration to the African continent is considered to be the most probable course of events. Generally, there are 2 hypotheses of the genus Schistoma. A hypothesis of Gondvana origin was based on snail host phylogeny and paleonthology and considered first schistosomes to originate on this continent to and appear in Asia from the Indian subcontinent platform 70-150 million years ago and in South America before Gondvana's split 60-120 million years ago. The recent data of molecular genetics show a high similarity between ITS2 sequences of S.bovis and S.intercalatum, with slightly lesser one between S.bovis and S.matthei. The similar pattern with slightly fewer differences can be seen in variability of cytochrome C subunit 1. Webster et al. 2006 noted a generally high similarity among species of the African group of schistosomes and considered it to originate from interspecies hybridization inside this group. Such hydridization occurring in both nature and a laboratory can make uncertain the determination of schistosome species based on a certain single gene marker.


Subject(s)
Schistosomatidae/classification , Trematode Infections/parasitology , Africa/epidemiology , Americas/epidemiology , Animals , Asia/epidemiology , Cytochromes c1/genetics , DNA, Helminth/genetics , DNA, Ribosomal Spacer/genetics , Evolution, Molecular , Humans , Phylogeny , Schistosomatidae/genetics , Sequence Analysis, DNA , Trematode Infections/epidemiology
13.
Bull Exp Biol Med ; 148(1): 23-5, 2009 Jul.
Article in English | MEDLINE | ID: mdl-19902087

ABSTRACT

Selective anxiolytic afobazole (1 mM) inhibits monoamine oxidase A activity in mitochondria from rat brain and liver (IC(50) 0.36 and 0.43, respectively). Effect of the compound does not depend on the time of preincubation with mitochondria. Triple washout of mitochondria is followed by complete recovery of initial enzyme activity.


Subject(s)
Anti-Anxiety Agents/pharmacology , Benzimidazoles/pharmacology , Brain/drug effects , Liver/drug effects , Mitochondria/drug effects , Monoamine Oxidase/drug effects , Morpholines/pharmacology , Animals , Brain/enzymology , Liver/enzymology , Mitochondria/enzymology , Rats
14.
Bull Exp Biol Med ; 148(1): 42-4, 2009 Jul.
Article in English | MEDLINE | ID: mdl-19902093

ABSTRACT

In vitro radioligand assay revealed interaction of afobazole with sigma(1)-receptors (Ki=5.9x10(-6) M). Translocation of sigma(1)-receptors from the endoplasmic reticulum to the outer membrane was demonstrated by confocal microscopy. Experiments were performed on the model of HT-22 immortalized hippocampal cells after incubation with afobazole in a concentration of 10(-8) M.


Subject(s)
Anti-Anxiety Agents/pharmacology , Benzimidazoles/pharmacology , Morpholines/pharmacology , Neuroprotective Agents/pharmacology , Receptors, sigma/drug effects , Animals , Cell Line, Transformed , Fluorescent Antibody Technique , Hippocampus/cytology , Hippocampus/drug effects , Humans , Jurkat Cells , Mice , Radioligand Assay , Sigma-1 Receptor
15.
Eksp Klin Farmakol ; 72(1): 3-11, 2009.
Article in Russian | MEDLINE | ID: mdl-19334502

ABSTRACT

The interaction of afobazole (5-ethoxy-2-[2-(morpholino)-ethylthio]benzimidazole dihydrochloride) and its main metabolite M-11 (2-[2-(3-oxomorpholine-4-yl)-ethylthio]-5-ethoxy benzimidazole hydrochloride) with neuroreceptors was studied using the method of radioligand analysis. The binding of afobazole with s1 (Ki =5.9 x 10(-6) M), MTI (Ki =1.6 x 10(-5) M), and MT3 (Ki =9.7 x 10(-7) M) receptors, as well as with a regulatory site of MAO-A (Ki = 3.6 x 10(-6) M) was revealed. The binding of M-11 with MT3 receptors (Ki = 3.9 x 10(-7) M) was demonstrated. The translocation of s1 receptor from endoplasmatic reticulum to the external membrane was revealed by the confocal microscopy technique on the immmortalized hippocampal HT-22 cells under the condition of 30- and 60-min-long afobazole (10(-8) M) application. Afobazole was shown to inhibit MAO-A reversibly. These properties of afobazole are consistent with our previous findings of the anxiolytic and neuroprotective effects of this drug.


Subject(s)
Anti-Anxiety Agents/pharmacology , Benzimidazoles/pharmacology , Monoamine Oxidase/metabolism , Morpholines/pharmacology , Receptor, Melatonin, MT1/metabolism , Receptors, Melatonin/metabolism , Receptors, sigma/metabolism , Animals , Anti-Anxiety Agents/metabolism , Benzimidazoles/metabolism , Binding, Competitive , Brain/cytology , Brain/metabolism , Cell Line , Cell Membrane/metabolism , Cricetinae , Cricetulus , Endoplasmic Reticulum/metabolism , Fluorescent Antibody Technique , Metallothionein 3 , Mice , Mitochondria/drug effects , Mitochondria/metabolism , Monoamine Oxidase Inhibitors/pharmacology , Morpholines/metabolism , Neurons/drug effects , Neurons/metabolism , Protein Transport/drug effects , Radioligand Assay , Rats , Rats, Sprague-Dawley
16.
Eksp Klin Farmakol ; 72(1): 15-8, 2009.
Article in Russian | MEDLINE | ID: mdl-19334504

ABSTRACT

Experiments on mice showed that a single intraperitoneal administration of anxiolytic afobazole (10 mg/kg) increases the effect of haloperidol in the apomorphine-induced climbing test and does not influence the catalepsy caused by the neuroleptic agent. The daily dose of afobazole 10 mg/kg during a five-day preliminary test reduced the extrapyramidal effects of haloperidole on rats and mice without significant change of the apomorphine-induced climbing test results. The ability of afobazole to reduce extrapyramidal disturbances caused by haloperidol can be related to the agonist effect of afobazole with respect to sigma 1 receptors.


Subject(s)
Antipsychotic Agents/adverse effects , Benzimidazoles/pharmacology , Haloperidol/adverse effects , Morpholines/pharmacology , Motor Activity/drug effects , Animals , Anti-Anxiety Agents/pharmacology , Behavior, Animal/drug effects , Catalepsy/drug therapy , Male , Mice , Rats , Receptors, sigma/metabolism
17.
Eksp Klin Farmakol ; 72(1): 19-21, 2009.
Article in Russian | MEDLINE | ID: mdl-19334505

ABSTRACT

Anxiolytic afobazole was shown in the experiments on outbred rats to decrease the immobility in the Porsolt and Nomura swim tests. The degree of afobazole effect in a dose of 5 mg/kg (i.p.) is similar to that of the standard antidepressant amitriptyline administered in doses of 10 mg/kg. Data obtained are testifying to the antidepressant activity of afobazole.


Subject(s)
Antidepressive Agents/pharmacology , Benzimidazoles/pharmacology , Morpholines/pharmacology , Motor Activity/drug effects , Animals , Male , Rats
18.
Vestn Ross Akad Med Nauk ; (9): 45-51, 2008.
Article in Russian | MEDLINE | ID: mdl-19062578

ABSTRACT

The involvement of paraoxonase family in antiathrogenesis has recently attracted attention of many researchers to these enzymes. Type 1 paraoxonase (PON 1) is a Ca-dependent hydrolase with a broad spectrum of substrate specificity. It is tightly bound to plasma high density lipoproteins (HDLP) and exhibits antioxidative and antiatherogenic activities. This review analyses publications concerning the structure, biological activity, and clinical significance ofparaoxonases, in the first place PON 1. Consideration of genetic and regulatory aspects of PON 1 is important for better understanding clinical and prognostic implications of this enzyme. These data are supplemented by the results of original observations of 60 patients with systemic lupus erythematosus and 20 with rheumatoid arthritis admitted to the Institute of Rheumatology. They confirm the published reports indicating reduced activity of this enzyme in patients compared with healthy donors.


Subject(s)
Arthritis/enzymology , Aryldialkylphosphatase/metabolism , Animals , Biomarkers/metabolism , Disease Progression , Humans
20.
Eksp Klin Farmakol ; 69(3): 3-6, 2006.
Article in Russian | MEDLINE | ID: mdl-16878488

ABSTRACT

Changes in the BDNF content in brain structures--hippocampus, hypothalamus, striatum, and frontal cortex--were determined in mice of different emotional-stress reaction phenotypes, which were subjected to emotional stress and treated by the selective anxiolytic afobazole. The changes were different in BALB/c and C57BL/6 mice. Afobazole exhibited a significant protector action against a decrease in the brain BDNF level caused by emotional stress in BALB/c mice.


Subject(s)
Behavior, Animal/drug effects , Benzimidazoles/pharmacology , Brain Chemistry/drug effects , Brain-Derived Neurotrophic Factor/metabolism , Brain/metabolism , Morpholines/pharmacology , Stress, Psychological/metabolism , Animals , Male , Mice , Mice, Inbred BALB C , Phenotype
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