3,260 results match your criteria Bioorganicheskaia khimiia[Journal]


[The Point Mutation in NOGGIN2 Protein That Enhances Its Ability to Bind Activin].

Bioorg Khim 2015 Nov-Dec;41(6):749-51

Earlier we have revealed the ability of Noggin family proteins to bind a member of the TUF-β superfamily, ActivinB, and to repress the Activin-dependent Smad2 signaling cascade. In the present work we have characterized a mutant of the Xenopus laevis Noggin2, bearing the substitution W203R. We have shown that this point mutation enhances the affinity of Noggin2 to ActivinB, while weakens its affinity to BMP. Read More

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[The Cytoskelrtal Protein Zvxin Interacts with the Hedgehog Receptor Patched].

Bioorg Khim 2015 Nov-Dec;41(6):744-8

Earlier, we demonstrated Zyxin influence upon Hedgehog (Hh)-signaling pathway during early patterning of the central neural system (CNS) anlage of the Xenopus laevis embryo. Now we show that Zyxin can physically interact with the transmembrane receptor of Hh, Patched2 (Ptc2). Binding of Hh by this receptor activates signaling pathway, which regulates many events, including numerous types of cell differentiation during the embryonic development. Read More

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May 2016
5 Reads

[Synthesis and Neurotropic Activity of 2,4-pyrano[4',3':4,5]pyrido[2,3-b]thieno[3,2-d] Pyrimidines].

Bioorg Khim 2015 Nov-Dec;41(6):737-43

2,4-Disubstituted derivatives of pyrano[4',3':4,5]pyrido[2,3-b]thieno[3,2-d] pyrimidines were synthesized and their pharmacological studies was carried out at animals by the tests of antagonism with subcutaneous administration of corazol and behavior of "open field" model. The method of "rotating rod" was used to evaluate of neurotoxicity. The neurotropic properties were found in the new synthesized compounds. Read More

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[Inhibitory Properties of Nitrogen-Containing Adamantane Derivatives with Monoterpenoid Fragments Against Tyrosyl-DNA Phosphodiesterase I].

Bioorg Khim 2015 Nov-Dec;41(6):731-6

It was found that compounds combining diazaadamantane and monoterpenoid fragments are potent inhibitors of new structural type of human recombinant DNA repair enzyme Tyrosyl-DNA phosphodiesterase I (Tdp1). It was demonstrated that the inhibition efficiency depended on the length and flexibility of the aliphatic chain of the substituent. Read More

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May 2016
3 Reads

[Modulation of Ca(2+)-Dependent Proteiolysis under the Action of Weak Low-Frequency Magnetic Fields].

Bioorg Khim 2015 Nov-Dec;41(6):725-30

The study aimed to determine the molecular targets of magnetic fields in living objects. Time-dependent effects of weak low-frequency magnetic field tuned to the parametric resonance for calcium ions were studied on model organisms (fish, whelk). The dynamics of Ca(2+)-dependent proteinase activity under the exposure to magnetic fields with given parameters was determined and minimal time of exposure in order to achieve inactivation of these proteinases was find out as well. Read More

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[Intracellular Protein Degradation in Growth of Atlantic Salmon, Salmo salar L].

Bioorg Khim 2015 Nov-Dec;41(6):717-24

A brief review on the common characteristics and specific features of proteolytic machinery in fish skeletal muscles (based on Atlantic salmon, Salmo salar L., Salmonidae) has been given. Among a variety of proteases in the muscle tissue, those determining protein degradation level in developing and intensively growing muscles in salmon young and by this way regulating protein retention intensity and growth at all namely lysosomal cathepsins B and D and calcium-dependent proteases (calpains) were comprehensively studied. Read More

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[Fragment of Receptor for Advanced Glycation End Products Improves Memory State in a Model of Alzheimer's Disease].

Bioorg Khim 2015 Nov-Dec;41(6):709-16

A number of synthetic peptides corresponding to potentially important regions in the sequence of the four membrane proteins known as beta-amyloid cell receptors have been investigated on their ability to improve memory state in experimental model of Alzheimer's disease. Nine fragments repeating all the exposed nonstructural regions of the RAGE protein according to X-ray data, have been synthesized. The activity of these peptides and synthesized earlier immunoprotective fragments of other three proteins (acetylcholine receptor alpha7-type, prion protein and neurotrophin receptor p75) has been investigated under intranasal administration, without immune response to the peptide. Read More

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[Preparation of Transmembrane Fragments Growth Hormone Receptor GHR in a Cell-Free Expression System for Structural Studies].

Bioorg Khim 2015 Nov-Dec;41(6):701-8

Growth hormone somatotropin and its membrane receptor GHR, belonging to a superfamily of the type I receptors possessing tyrosine kinase activity, are involved in the intercellular signal transduction cascade and regulate a number of important physiological and pathological processes in humans. Binding with somatotropin triggers a transition of GHR between two alternative dimer states, resulting in an allosteric activation of JAK2 tyrosine kinase in the cell cytoplasm. Transmembrane domain of GHR directly involved in this complex conformational transition. Read More

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[Interaction of DNA Aptamers with the ATP-Dependent Lon Protease from Escherichia coli].

Bioorg Khim 2015 Nov-Dec;41(6):696-700

ATP-dependent Lon protease of E. coli (Ec-Lon) is a key enzyme of the quality control system of the cell proteome. Ec-Lon subunit comprises N-terminal non-catalytic region, ATPase module and proteolytic domain (serine-lysine endopeptidase). Read More

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[Protein Identification of Blood Nucleoprotein Complexes].

Bioorg Khim 2015 Nov-Dec;41(6):686-95

Circulating nucleoprotein complexes were isolated-from blood plasma by affinity chromatography using immobilized polyclonal anti-histone antibodies. It was found, that the main part of DNA from histone-contained nucleoprotein complexes have size 170-180 b.p. Read More

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May 2016
3 Reads

[Functionalized Metal Chelates Based on Diethylenetriaminetetraacetic Acids for Chemical Modification of Proteins and Small Biomolecules].

Bioorg Khim 2015 Nov-Dec;41(6):675-85

Bifunctional reagents based on diethylenetriaminetetraacetic acid containing a bound metal ion and a reactive functional group for the interaction with proteins and low-molecular-weight substances have been synthesized. An Amino-derivative of a complexonate was obtained by acylation of monosubstituted diamine with diethylenetriaminepentaacetic acid dianhydride followed by deprotection ofthe amino group, purification by anion exchange chromatography and chelation of Eu3+. This metal chelate derivative was used for labeling 17α-hydroxyprogesterone 3-(O-carboxymethyl)oxime and horseradish peroxidase. Read More

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May 2016
2 Reads

[Ph-Sensor Properties of a Fluorescent Protein from Dendronephthya sp].

Bioorg Khim 2015 Nov-Dec;41(6):669-74

Genetically encoded biosensors based on fluorescent proteins are now widely applicable for monitoring pH changes in live cells. Here, we have shown that a fluorescent protein from Dendronephthya sp. (DendFP) exhibits a pronounced pH-sensitivity. Read More

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May 2016
2 Reads

[Interaction of Arenicin-1 with C1q Protein].

Bioorg Khim 2015 Nov-Dec;41(6):664-8

The interaction between arenicin-1, that is an antimicrobial peptide from polychaeta Arenicola marina, and human complement system protein C1q was studied using enzyme-linked receptor sorbent assay and ELISA. We revealed that arenicin-1 and C1q form complex that is stable in high ionic strength condition 0.5 M NaCl. Read More

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[Anti-Inflammatory Activity of the Polypeptide of the Sea Anemone, Heteractis crispa].

Bioorg Khim 2015 Nov-Dec;41(6):657-63

The anti-inflammatory effect of the recombinant polypeptide HCGS 1.20, a Kunitz-type serine protease inhibitor of the sea anemone Heteractis crispa, was investigated. It was shown that the polypeptide inhibits the increase of the concentration of calcium ions in mouse bone marrow derived macrophages elicited by histamine, and reduces the content of NO in lipopolysaccharide stimulated macrophages. Read More

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May 2016
10 Reads

[The Qualitative Analysis of the Amide Derivative of HLDF-6 Peptide and Its Metabolites with the Use of Tritium- and Deuterium-Labeled Derivatives].

Bioorg Khim 2015 Nov-Dec;41(6):644-56

The goal of the study was to elaborate the pharmacokinetics methods of the amide derivative of peptide HLDF-6 (TGENHR-NH2) and its range of nootropic and neuroprotective activity is wide. The hexapeptide 41TGENHR46 is a fragment of the HDLF differentiation factor. It forms the basis for the development of preventive and therapeutic preparations for treating cerebrovascular and neurodegenerative conditions. Read More

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May 2016
2 Reads

[Pioneer Transcription Factors in Normal Development and in Carcinogenesis].

Bioorg Khim 2015 Nov-Dec;41(6):636-43

Pioneer transcription factors constitute a heterogeneous group of regulatory proteins of animals, which, unlike other transcription factors, are able to recognize and bind target DNA sequences within closed chromatin. This binding can change the local chromatin structure and facilitate binding of other proteins, thus establishing competence for gene expression. The ability to bind silent genes in the closed environment makes the pioneer factors very useful in the processes leading to cardinal alteration of cell phenotype, such as differentiation in embryonic development or cell reprogramming. Read More

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SYNTHESIS AND CHARACTERIZATION OF POLYSIALIC ACID/CARBOXYMETHYL CHITOSAN HYDROGEL WITH POTENTIAL FOR DRUG DELIVERY.

Bioorg Khim 2015 Sep-Oct;41(5):627-32

A novel hydrogel was prepared from polysialic acid (PSA) and carboxymethyl chitosan (CMCS) using glutaraldehyde as the cross-linking agent. The resulting PSA-CMCS hydrogel exhibited pH sensitivity, in which the swelling ratio under acidic conditions was higher than those under neutral or alkaline conditions. The swelling ratio of PSA-CMCS hydrogel at equilibrium depended on the medium pH, the cross-linking agent concentration, and the ratio of PSA to CMCS (w/w). Read More

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SYNTHESIS AND BIOLOGICAL EFFICACY OF NOVEL PIPERAZINE ANALOGUES BEARING QUINOLINE AND PYRIDINE MOIETIES.

Bioorg Khim 2015 Sep-Oct;41(5):619-26

A series of novel piperazine analogues bearing quinolin-8-yloxy-butan--ones/pyridin-2-yloxy-ethanones were synthesized by a simple and convenient approach based on various substituted piperazine incorporating quinoline and pyridine moieties. The analogues were evaluated for in vitro antioxidant activity against 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and ferrous ion radical scavenging activities and anti-inflammatory activity by inhibition of Vipera russelli venom (PLA2) and gastric K+/H(+)-ATPase activities. Most of the title compounds exhibited promising activity. Read More

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April 2016
3 Reads

[Enantioselective Synthesis of (R)- and (S)-3-Methylspermidines].

Bioorg Khim 2015 Sep-Oct;41(5):612-8

Earlier unknown enantiomerically pure (R)- and (S)-1,8-diamino-3-methyl-4-azaoctane's (3-MeSpd's) were synthesized with high overall yields and optical purity starting from commercially available R- and S-isomers of N-Boc-2-aminopropanol-1. Application of R- and S-isomers of 3-MeSpd for the investigation of the stereospecificity of spermidine transporter and peculiarities of deoxyhypusine synthase reaction are discussed. Read More

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April 2016
1 Read

[The Biological Activity of the Sevanol and Its Analogues].

Bioorg Khim 2015 Sep-Oct;41(5):606-11

Previously, from the plant Thymus armeniacus a new lignan sevanol was isolated, it's structure was elucidated and was shown that it effectively inhibits the acid-sensing channel ASIC3 and also exhibits a pronounced analgesic and anti-inflammatory effect. In this work biological activity of the sevanol analog obtained by chemical synthesis from simple precursors, the stereoisomer of sevanol and a precursor molecule represents a half of sevanol was measured in electrophysiological experiments on human ASIC3 channels expressed in Xenopus laevis oocytes. Measured inhibitory activity of a synthetic analogue coincided with the activity ofthe natural molecule. Read More

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April 2016
2 Reads

[Targeted Delivery of Quantum Dots to HER2-Expressing Tumor Using Recombinant Antibodies].

Bioorg Khim 2015 Sep-Oct;41(5):599-605

Targeted delivery of semiconductor quantum dots (Q Ds) to tumors overexpressing HER2 cancer marker has been. demonstrated on immunocompromised mice bearing human breast cancer xenografts. To obtain targeted QDs complexes we applied the approach based on the use of protein adaptor system, RNAase barnase and its inhibitor barstar. Read More

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April 2016
3 Reads

[Radioligand Method of Assessment of β-Adrenoceptor's Activity on Human T-Lymphocytes].

Bioorg Khim 2015 Sep-Oct;41(5):592-8

We proposed a new method of evaluation of beta-receptor's activity on the surface of human T-lymphocytes based on the radioligand method. Optimal conditions for evaluation of specific binding to β2-adrenoceptors of 0.5 fmol ligand per 1 million cells using [125I]-cyanopindolol were found. Read More

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[Differences of Nonsense-Mediated mRNA Degradation Activity in Mammalian Cell Lines Revealed by a Fluorescence Reporter].

Bioorg Khim 2015 Sep-Oct;41(5):587-91

Activity of nonsense-mediated mRNA degradation (NMD) was studied in several mammalian cell cultures using recently developed genetically encoded fluorescence sensor [Pereverzev et al., Sci. Rep. Read More

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April 2016
2 Reads

[The Effect of Mutations in the Inserted Domain of ATP-Dependent Lon Protease from E. coli on the Enzyme Function].

Bioorg Khim 2015 Sep-Oct;41(5):579-86

ATP-Dependent protease LonA from E. coli (Ec-Lon), belonging to the superfamily of AAA+ proteins, is a key member of the protein quality control system in bacterial cells. Ec-Lon functions as homohexamer and degrades abnormal and defective polypeptides as well as a number of regulatory proteins by the processive mechanism. Read More

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[Streptokinase and Staphylokinase: Differences in the Kinetics and Mechanism of Their Interaction with Plasminogen, Inhibitors and Fibrin].

Bioorg Khim 2015 Sep-Oct;41(5):565-78

Comparative in vitro study of the kinetics of various reactions involved in the process of thrombolysis initiated by streptokinase (SK) and staphylokinase (STA) was carried out. It was shown that at the interaction of an equimolar ratio of plasminogen (Pg) with SK or STA the rate of formation and the specific esterase activity of the complex plasmin (Pm) · SK are higher than those of the complex Pm · STA. The catalytic efficiency (kcat/Km) of hydrolysis of the chromogenic plasmin substrates by Pm · SK complex was 2 times higher than by Pm · STA complex. Read More

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April 2016
2 Reads

[Identification of Target Extracellular Proteases--Activators of Proteins of Haemostasis System Produced by Micromycetes Aspergillus ochraceus and Aspergillus terreus].

Bioorg Khim 2015 Sep-Oct;41(5):559-64

Effects of extracellular proteases of Aspergillus ochraceus and Aspergillus terreus on plasma hemostasis proteins, consist of initiating the activation of prothrombin complex proteins, was detected. Was discovered, that A. ochraceus proteases have a direct influence on protein C and coagulation factor X, and A. Read More

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[Affine Haemosorbents Based on Aromatic Peptides for Binding of the Immunoglobulin G].

Bioorg Khim 2015 Sep-Oct;41(5):553-8

Affinity haemoadsorbents based on WY, WTY, WNY ligands and polysaccharide matrix were developed for the human immunoglobulin G binding. The characteristics of new sorbents such as the binding of total IgG and binding of IgG subclasses were compared. It was found that all new sorbents well extract the IgG from the blood plasma. Read More

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April 2016
3 Reads

[Supramolecular Agents for Theranostics].

Bioorg Khim 2015 Sep-Oct;41(5):539-52

This mini-review summarizes recent data obtained in the process of creation of a versatile module platform suitable for construction of supramolecular theranostic agents. As an example, we consider multifunctional hybrid agents for imaging and elimination of cancer cells. The use of an adapter protein system barnase:barstar for producing targeted multifunctional hybrid structures on the basis of highly specific peptides and mini-antibodies as addressing modules and recombinant proteins and/or nanoparticles of different nature (quantum dots, nanogold, magnetic nanoparticles, nanodiamonds, upconverting nanophosphores, polymer nanoparticles) as agents visualizing and damaging cancer cells is described. Read More

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April 2016
5 Reads

[Tyrosyl-DNA Phosphodiesterase 1 Is a New Player in Repair of Apurinic/Apyrimidinic Sites].

Bioorg Khim 2015 Sep-Oct;41(5):531-8

Genomic DNA is constantly damaged by the action of exogenous factors and endogenous reactive metabolites. Apurinic/apyrimidinic sites (AP sites), which occur as a result of DNA glycosylase induced or spontaneous hydrolysis of the N-glycosidic bonds, are the most common damages of DNA. The chemical reactivity of AP sites is the cause of DNA breaks, and DNA-protein and DNA-DNA crosslinks. Read More

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April 2016
2 Reads

[Octarphin--Nonopioid Peptide of the Opioid Origin].

Authors:
E V Navolotskaya

Bioorg Khim 2015 Sep-Oct;41(5):524-30

The data on the properties and mechanism of action of the peptide octarphin (TPLVTLFK, the fragment 12-19 of β-endorphin)--a selective agonist of nonopioid (insensitive to the action of the opioid antagonist naloxone) β-endorphin receptor found on n immune cells (peritoneal macrophages, T and B lymphocytes of spleen and blood), endocrine (adrenal cortex, hypothalamus), cardiovascular (cardiomyocytes) systems are analyzed and systematized. Binding to the receptor octarphin increases increases the mitogen-induced pro- liferation of human and mouse T and B lymphocytes in vitro, activates murine peritoneal macrophages in vitro and in vivo, stimulates growth of human T-lymphoblast cell lines Jurkat and MT-4, inhibits adenylate cyclase activity of rat adrenal cortex membranes and suppresses the secretion of glucocorticoids from the adrenal gland into the blood. It was shown that in a concentration range of 1-1000 nM the peptide increases the activity of inducible NO-synthase (iNOS), and the content of NO and cGMP in lipopolysaccharide-activated murine peritoneal macrophages. Read More

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[Structural Features of Cysteine-Stabilized Polypeptides from Sea Anemones Venoms].

Bioorg Khim 2015 Sep-Oct;41(5):511-23

Nowadays, venom-based drug discovery becomes popular again: pharmaceutical companies evaluate animal venom potential as a combinatory library of biologically-active compounds. Collaborations with research groups from academia are intensified, new toxins are being investigated, among which polypeptides are of paramount importance. Sea anemones produce the most diversified, from structural point of view, polypep- tide venom components among other animals. Read More

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[The Development and Application of BODIPY-Labeled Oligonucleotides in Real-Time Polymerase Chain Reaction].

Bioorg Khim 2015 Jul-Aug;41(4):505-8

A BODIPY-based (4,4-difluoro-1,3,5,7-tetramethyl-4-bora-3a,4a-diaza-s-indacene, TMB) green fluorescent probe for quantitative real-time polymerase chain reaction (qPCR) was synthesized by azide-alkyne cycloaddition reaction. Comparative studies with analogous fluorescein-based probe were carryed out. We demonstrate that fluorescent probes with TMB fluorophore can be used in qPCR experiments as well. Read More

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December 2015

SYNTHESIS, REACTIONS, AND BIOLOGICAL ACTIVITY OF SOME TRIAZINE DERIVATIVES CONTAINING SULFA DRUG MOIETIES.

Bioorg Khim 2015 Jul-Aug;41(4):491-504

Thienyl-triazine-sulphonamide conjugates were prepared from their precursor amines using triethyl orthoformate or ethyl chloroformate as cross coupling reagents. The progress of these reactions was investigated by spectral (IR, NMR, MS) and microanalytical techniques. The synthesized compounds were in vitro screened for antibacterial, antifungal, antioxidant, and anticancer activity. Read More

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December 2015

SYNTHESIS AND REACTIVITY OF ENAMINONE OF NAPHTHO[B] 1,4-OXAZINE: ONE POT SYNTHESIS OF NOVEL ISOLATED AND HETEROCYCLE-FUSED DERIVATIVES WITH ANTIMICROBIAL AND ANTIFUNGAL ACTIVITIES.

Bioorg Khim 2015 Jul-Aug;41(4):475-90

The synthesis of the multifunctional, hitherto unreported 3-(3-(dimethylamino)acryloyl)-2H-naphtho[1,2- b] [1,4]oxazin-2-one was described and its utility as a versatile building block was demonstrated for the synthesis of some new pyrimidines, pyrazoles, isoxazoles, pyrazolo[a]pyrimidines, triazolo[a]pyrimidines, pyrido[d]pyrimidines, pyrido[d]pyrimidines, piperidines, pyrido[a]benzimidazoles, 2H-pyran-3-carboxamides, benzofurans, naphtho[b]furans and pyrazolo[c] [1,2,4]triazines of potential biological activities. The synthesized compounds were characterized by IR, 1H NMR, 13C NHR and mass spectral data. Some of the compounds were evaluated for antimicrobial activities. Read More

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December 2015
1 Read

SYNTHESIS AND EVALUATION OF NEW PHTHALAZINE SUBSTITUTED β-LACTAM DERIVATIVES AS CARBONIC ANHYDRASE INHIBITORS.

Bioorg Khim 2015 Jul-Aug;41(4):468-74

A new series of phthalazine substituted β-lactam derivatives were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA I and II) were evaluated. 2H-Indazolo[2,1-b]phthala- zine-trione derivative was prepared with 4-nitrobenzaldehyde, dimedone, and phthalhydrazide in the presence of TFA in DMF, and the nitro group was reduced to 13-(4-aminophenyl)-3,3-dimethyl-3,4-dihydro- 2H-indazolo[1,2-b]phthalazine-1,6,11(13H)-trione with SnCl2 · 2H2O. The reduced compound was re- acted with different aromatic aldehydes, and phthalazine substituted imines were synthesized. Read More

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December 2015
14 Reads

[Genotoxic and Mutagenic Properties of Synthetic Betulinic and Betulonic Acids].

Bioorg Khim 2015 Jul-Aug;41(4):462-7

Synthesis of betulinic acid was performed from the birch bark extract (Betula pendula). Betulonic acid was intermediate of the synthesis. Both acids were isolated with purity 95%. Read More

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December 2015
2 Reads

[Synthesis and Pharmacological Activity of N-Hetaryl-3(5)-Nitropyridines].

Bioorg Khim 2015 Jul-Aug;41(4):454-61

Reacting a number chlorosubstituted 3(5)-nitropyridine with some diazoles or 3-chloropyridazin-6-one synthesized previously undescribed various 2-, 4- or 6-substituted hetaryl-3(5)-nitropyridines. Furthermore, pyrazolyl-3-nitropyridine prepared by cyclizing hydrazinopyridine resulting from the nucleophilic substitution of chlorine in chlorosubstituted 3-nitropyridine by hydrazine. It has been shown that these compounds have moderate antibacterial activity against some pathogenic Gram-positive and Gram-negative bacteria (Staphylococcus aureus, Escherichia coli), as well as a strong effect on protistocidal action form Colpoda steinii, surpassing clinically used reference drugs. Read More

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December 2015

[The Analysis for Probable Reasons of Cd4+ T-Cell Activation Non-Linear Dependence on Extra Cellular Calcium Ion Concentration in Human Peripheral Blood in vitro].

Authors:
I S Litvinov

Bioorg Khim 2015 Jul-Aug;41(4):443-53

The analysis for probable reasons of CD4+ T-cell activation non-linear dependence on [Ca2+]o in HPB in vitro is the general aim of current work. At the beginning we pursued the analysis of receptor-dependent (the mixture of monoclonal antibodies (mAbs) to CD3 and CD28 molecules) and receptor-independent (phorbol-myristate-acetate and ionomycin mixture) means to activate T cells in vitro with different [Ca2+]o in HPB. The key role of intracellular T-cell signaling systems in activated T cells in their non-similar sensitivity to calcium ions in the blood was shown. Read More

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December 2015

[The Role of Extracellular Calcium Ions Reduction in T Cell Activation in Human Peripheral Blood].

Bioorg Khim 2015 Jul-Aug;41(4):432-42

Calcium plays a fundamental role in many essential live functions. It is well-known that many infections can lead to hypocalcaemia in humans. The importance of extracellular calcium concentration ([Ca2+]o) in T-cell activation is well recognized, but [Ca2+]o levels necessary for lymphocyte activation have not been investigated in detail. Read More

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December 2015
1 Read

[ag1 Is Required for the Fin Regeneration in Danio rerio].

Bioorg Khim 2015 Jul-Aug;41(4):427-31

In the current research, we have demonstrated that Ag1 protein is necessary for the fin regeneration in the fish Danio rerio. Robust activation of gene ag1 expression in cells of the wound epithelium is observed after caudal fin amputation. Besides, inhibition of translation of ag1 mRNA leads to retardation of the caudal tail fin regeneration. Read More

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December 2015

IDENTIFCATION AND VALIDATION OF NOVEL microRNA MOLECULE FROM THE PELODISCUS SINENSIS BY BIOINFORMATICS APPROACHES.

Bioorg Khim 2015 Jul-Aug;41(4):416-26

MicroRNAs (miRNAs) are a group of endogenous, short non-coding RNAs with the length of about 22 nt, which mediate gene expression at the post-transcriptional level through mRNA degradation or translational repression. Among them, some are highly evolutionally conserved in the animal kingdom; this provides a powerful strategy for identifying miRNAs in new species. The Chinese soft-shelled turtle (Pelodiscus sinensis) is one of the most important freshwater aquaculture reptilian species in China, but related miRNAs have not been identified up to now. Read More

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December 2015
11 Reads

[A New Simple Technique for Producing Labeled Monoclonal Antibodies for Antibody Pair Screening in Sandwich-ELISA].

Bioorg Khim 2015 Jul-Aug;41(4):411-5

A simple and fast method for obtaining biotin-labeled monoclonal antibodies was developed usingcontent of hybridoma culture supernatant sufficient to select antibody pairs in sandwich ELISA. The method consists in chemical biotinylation of antigen-bound antibodies in a well of ELISA plate. Using as an example target Vaccinia virus A27L protein it was shown that the yield of biotinylated reactant is enough to set comprehensive sandwich ELISA for a moderate size panel of up to 25 monoclonal antibodies with an aim to determine candidate pairs. Read More

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December 2015

[Solubilization Specificities Interferon beta-1b from Inclusion Bodies].

Bioorg Khim 2015 Jul-Aug;41(4):403-10

A new solubilization method of recombinant interferon beta-1b (IFNβ-1b) from the inclusion bodies was developed. This method allows to extract the target protein selectively in the solutions of different alcohols, such as ethanol, propanol and isopropanol. It was shown that the more effective IFNβ-1b solubilization was achieved in the 55% propanol solution. Read More

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December 2015

[Main Cellular Redox Couples].

Bioorg Khim 2015 Jul-Aug;41(4):385-402

Most of the living cells maintain the continuous flow of electrons, which provides them by energy. Many of the compounds are presented in a cell at the same time in the oxidized and reduced states, forming the active redox couples. Some of the redox couples, such as NAD+/NADH, NADP+/NADPH, oxidized/reduced glutathione (GSSG/GSH), are universal, as they participate in adjusting of many cellular reactions. Read More

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December 2015

[Novel Water-Soluble Substrate for Silicateins].

Bioorg Khim 2015 May-Jun;41(3):380-2

We suggested to use tetrakis(2-hydroxyethyl)orthosilicate (THEOS) as a substrate for silicateins--an enzyme family playing a key role in formation of skeleton in marine sponges. We compared THEOS with tetraethylorthosilicate (TEOS)--a commonly used substrate for silicateins. These substrates were tested in reaction of amorphous silica formation in vitro catalyzed by silicatein Al from sponge Latrunculia oparinae. Read More

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November 2015
1 Read

[Protective Effects of Myelopeptides in Neuroblastoma C-1300 Cell Culture].

Bioorg Khim 2015 May-Jun;41(3):375-9

The effects of bone marrow regulatory peptides--myelopeptides 1-6--in mouse neuroblastoma C-1300 were studied. Cultivation in presence of myelopeptides stimulated morphological differentiation of neuroblasts. Neuroprotective abilities of myelopeptides were shown on the models of morphine toxity and oxygen-glucose deprivation in neuroblastoma cell culture. Read More

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November 2015

SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL COUMARIN DERIVATIVES AS ANTIOXIDANT AGENTS.

Bioorg Khim 2015 May-Jun;41(3):366-74

Coumarins have been isolated from plants and reported for antioxidant properties. In the present study, we report synthesis of new coumarin derivatives as prospective therapeutic agents and investigate their antioxidant properties. Read More

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November 2015
2 Reads

ONE-POT THREE-COMPONENT MICROWAVE-ASSISTED SYNTHESIS OF NOVEL THIAZOLIDINONE DERIVATIVES CONTAINING THIENO[d]PYRIMIDINE-4-ONE MOIETY AS POTENTIAL ANTIMICROBIAL AGENTS.

Bioorg Khim 2015 May-Jun;41(3):357-65

New 2-methyl-5-(4-oxo-2-(substituted phenyl)thiazolidin-3-yl)thieno[3,4-d]-pyrimidin-4-one, 5-(2,7-diphenyl-5-thioxo-5,6,7,7a-tetrahydrothiazolo[4,5-d]pyrimidin-3(2H)-yl)-2-methylthieno[3,4-d]pyrimidin-4(3H)-one, and 2-methyl-5-(5-phenyl-thiazolo[5,4-d]soxazol-6(5H)-yl)thieno[3,4-d]pyrimidin-4(3H)-one have been prepared under microwave-assisted and conventional conditions. The new compounds were screened for their in vitro antimicrobial activity against two gram-positive bacteria (Bacillus subtilis NCI M-2063 and Staphylococcus aureus NCIM-2901), one gram-negative bacteria (Escherichia coli NCIM-2256), and.three fungal strains (Candida albicans NCIM-3471, Aspergillusfiavus NCIM-539, and Aspergillus niger NCIM-1196) and showed promising biological activity. Read More

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November 2015
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[Synthesis and Anticancer Activity of Betulonic Acid Imidazolides].

Bioorg Khim 2015 May-Jun;41(3):346-56

Synthesis of lupane C28-imidazolides, contained 3-oxo-, 3-oximino- and 2-cyano-2,3-seco-4(23)-en-frag ments in cycle A was carried out. The most antitumor activity at. in vitro testing showed 3-oximino-lup- 20(29)-en-28-yl-1H-imidazole-1-carboxylate; which inhibited the growth or induced apoptosis of non-small lung cancer, colon cancer, breast cancer, CNS cancer, ovarian cancer, prostate cancer, leucosis, melanoma cells. Read More

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November 2015
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[Search of (-)-Cytisine Derivatives as Potential Inhibitors of NF-κB and STAT1].

Bioorg Khim 2015 May-Jun;41(3):336-45

Design and synthesis ofnew derivatives of (-)-cytisine with a wide spectrum of pharmacological activity, represents the potential therapeutic interest for development of drug candidates for neurodegenerative disorders, inflammatory diseases, and treatment of nicotine addiction. We used HEK293 cell line transiently transfected with N F-κB and STATI luciferase reporter constructs to screen the (-)-cytisine derivatives for their potency to modulate basal and induced NF-κB and STAT1 activity. Currently, NF-κB, STAT1 and components of their signaling pathways are considered as attractive targets for pharmacological intervention, primarily in chronic inflammation, cancer, autoimmune, neurodegenerative and infectious diseases. Read More

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November 2015
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