المؤلفون: Shevchenko, K. V., Nagaev, I. Yu., Kulikova, O. I., Stvolinsky, S. L., Shevchenko, V. P., Myasoedov, N. F.

المصدر: Russian Journal of Bioorganic Chemistry; Apr2024, Vol. 50 Issue 2, p401-407, 7p

مصطلحات موضوعية: CARNOSINE, CELL membranes, CARBOXYPEPTIDASES, BLOOD plasma, SALICYLIC acid

مستخلص: Objective: The resistance of carnosine, pyrrolylcarnosine (PC) and salicylcarnosine (SC) to the action of leucine aminopeptidase and carboxypeptidases B and Y was evaluated. Methods: Proteolysis of carnosine and its derivatives under the action of leucine aminopeptidase, carboxypeptidases Y and B, or under the action of enzyme systems of plasma membranes of rat brain cells or blood plasma. Results and Discussion: It was found that proteolysis of carnosine, PC and SC under the action of leucine aminopeptidase does not occur. Carboxypeptidases B and Y, as well as the enzyme systems of blood plasma and plasma membranes of rat brain cells, degraded peptides containing β-alanyl, N-pyrrolyl, N-salicylic fragments to varying degrees. In all cases, histidine was formed. The formation of pyrrole or salicylic acid did not occur. Conclusions: It was found that carnosine, PC and SC showed high resistance to the action of amino- and carboxypeptidases in invitro experiments. [ABSTRACT FROM AUTHOR]

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المؤلفون: Shevchenko, V. P., Shevchenko, K. V., Andreeva, L. A., Nagaev, I. Yu., Myasoedov, N. F.

المصدر: Radiochemistry; Feb2024, Vol. 66 Issue 1, p97-104, 8p

مصطلحات موضوعية: DEUTERIUM, TRIFLUOROACETIC acid, GABA, CATALYTIC converters for automobiles, ACIDS, ISOTOPE exchange reactions

مستخلص: The efficiency of incorporating deuterium into 4-aminobutanoic acid (GABA) has been studied. The use of D2O at 200°C makes it possible to introduce into GABA an average of about 0.5 deuterium atoms, D2O with trifluoroacetic acid (1 : 1) at 250°C, an average 1.49 deuterium atoms with a yield of 15%. The solid-phase method permits introducing about 3 deuterium atoms per GABA molecule. During isotopic exchange with D2O, the use of a palladium–rhodium mixture pretreated with deuterium gas made it possible to produce [D]GABA with the deuterium content of 4.5–4.6 atoms. But in both cases, the yields of [D]GABA were low. Preparative amounts of [D]GABA were produced engaging additional supports. The best result was obtained when applying GABA to zeolite. Using D2O with 5% Pd/BaSO4–GABA–zeolite pretreated with deuterium gas, allows producing [D]GABA with an average content of 1.5–2.0 deuterium atoms and a yield of about 30%. [ABSTRACT FROM AUTHOR]

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المؤلفون: Shevchenko, V. P., Nagaev, I. Yu., Shevchenko, K. V., Myasoedov, N. F.

المصدر: Radiochemistry; Aug2023, Vol. 65 Issue 4, p442-447, 6p

مصطلحات موضوعية: DEUTERIUM, ISOTOPE exchange reactions, TRITIUM, HYDROGEN isotopes, DEUTERIUM oxide

مستخلص: The influence of various factors on the efficiency of introducing deuterium into 3-(N-pyrrolyl)-propanoyl-L-histidine and 3-(N-salicyl)-propanoyl-L-histidine was studied. Heavy water was used as a source of deuterium. It is shown that the content of deuterium atoms in the substance can be increased by pretreating the reaction mixture with deuterium gas. The new approach opens up additional possibilities both for obtaining high labeled pharmaceuticals by introducing hydrogen isotopes into organic compounds, and theoretically for a deeper understanding of the role in this process of activated deuterium or tritium particles solvated on the carrier and in the pool of matter. [ABSTRACT FROM AUTHOR]

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المؤلفون: Dmitriev, M. E., Shevchenko, K. V., Shevchenko, V. P., Nagaev, I. Yu., Kalashnikova, I. P., Ragulin, V. V., Myasoedov, N. F.

المصدر: Russian Journal of General Chemistry; Aug2023, Vol. 93 Issue 8, p2022-2028, 7p

مصطلحات موضوعية: URETHANE, PEPTIDES, GLUTAMIC acid, PROPIONALDEHYDE, HYDROLYSIS

مستخلص: The amidoalkylation of a phosphonous acid containing a structural isostere of diethyl glutamiate, using ethyl carbamate and 3-(methylthio)propionaldehyde, was proposed for the synthesis of NC(O)OEt-protected phosphinic pseudo-Met-Glu-peptide. Subsequent adamantyl protection of the phosphorylic function and hydrolysis of carboxylic groups made it possible to obtain phosphinic Met-[P]-Glu peptide in the form of cyclic glutamate anhydride. It was found that the latter reacts with the third amino acid component histidine to form the phosphinic Met-[P]-Glu-γ-His tripeptide. [ABSTRACT FROM AUTHOR]

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المؤلفون: Manchenko, D. M., Glazova, N. Yu., Sebentsova, E. A., Andreeva, L. A., Dolotov, O. V., Kamensky, A. A., Myasoedov, N. F., Levitskaya, N. G.

المصدر: Neuroscience and Behavioral Physiology ; volume 53, issue 1, page 132-141 ; ISSN 0097-0549 1573-899X

مصطلحات موضوعية: General Neuroscience

الإتاحة: https://doi.org/10.1007/s11055-023-01397-6Test

المؤلفون: Shevchenko, V. P., Nagaev, I. Yu., Lopachev, A. V., Myasoedov, N. F.

المصدر: Pharmaceutical Chemistry Journal ; volume 56, issue 11, page 1491-1495 ; ISSN 0091-150X 1573-9031

مصطلحات موضوعية: Drug Discovery, Pharmacology

الإتاحة: https://doi.org/10.1007/s11094-023-02819-yTest

المؤلفون: Shevchenko, V. P., Nagaev, I. Yu., Kulikova, O. I., Myasoedov, N. F.

المصدر: Doklady Chemistry; Jul2023, Vol. 511 Issue 1, p181-185, 5p

مصطلحات موضوعية: DEUTERIUM, DEUTERIUM oxide, BIOACTIVE compounds, ISOTOPE exchange reactions

مستخلص: Effect of temperature on the efficiency of deuterium introduction into a new biologically active compound salicylcarnosine (SC) has been studied. Gaseous deuterium and heavy water were used as deuterium sources. The synthesis of labelled SC by a solid-phase method at 190°C leads to formation of [D]SC in 53% yield and deuterium content about 4.8 atoms per molecule. It has been shown that isotope exchange between SC protons and deuterium water proceeds more efficiently after preliminary treatment of catalyst with gaseous deuterium at ambient temperature. [D]SC forms in 46% yield and contains about 7.3 deuterium atoms per molecule. The preparative synthesis of labelled SC by this procedure at 190°C results in [D]SC yield of 60–70% at deuterium content about 6.2 atoms per molecule. The new procedure for the activation of deuterium inclusion in peptides opens additional opportunities for preparing highly labelled compounds. [ABSTRACT FROM AUTHOR]

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المؤلفون: Shevchenko, V. P., Andreeva, L. A., Shevchenko, K. V., Nagaev, I. Yu., Myasoedov, N. F.

المصدر: Pharmaceutical Chemistry Journal ; volume 56, issue 5, page 602-606 ; ISSN 0091-150X 1573-9031

مصطلحات موضوعية: Drug Discovery, Pharmacology

الإتاحة: https://doi.org/10.1007/s11094-022-02683-2Test

المؤلفون: Manchenko, D. M., Glazova, N. Yu., Sebentsova, E. A., Andreeva, L. A., Dolotov, O. V., Kamensky, A. A., Myasoedov, N. F., Levitskaya, N. G.

المصدر: Neuroscience & Behavioral Physiology; Jan2023, Vol. 53 Issue 1, p132-141, 10p

مصطلحات موضوعية: LABORATORY rats, PEPTIDES, ADRENOCORTICOTROPIC hormone, DISEASE complications, CORTICOSTERONE

مستخلص: Tetrapeptide KKRR, corresponding to the ACTH15-18 sequence, is the shortest fragment with high-affinity binding with the ACTH receptor; it does not activate this receptor and prevents the whole hormone molecule from binding to it, and thus exhibits the properties of an ACTH receptor antagonist. The aim of the present work was to study the effects of peptide ACTH15-18 (KKRR) and its analog ACTH15-18PGP on behavior in Wistar rats in normal conditions and after acute stress produced by inescapable electrical foot shock. The peptides studied here did not affect the anxiety levels in white rats in normal conditions. Prior administration of ACTH15-18 (250 μg/kg) and its analog ACTH15-18PGP (50 and 250 μg/kg) decreased anxiety and corticosterone release in rats which had received a acute electrical foot shock stress. The extent and duration of the anti-stress effects of ACTH15-18PGP were significantly greater than the extent and duration of the effects of its natural prototype. [ABSTRACT FROM AUTHOR]

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المؤلفون: Glazova, N. Yu., Manchenko, D. M., Vilensky, D. A., Sebentsova, E. A., Andreeva, L. A., Kamensky, A. A., Dergunova, L. V., Limborska, S. A., Myasoedov, N. F., Levitskaya, N. G.

المصدر: Journal of Evolutionary Biochemistry & Physiology; Jan2023, Vol. 59 Issue 1, p200-212, 13p

مصطلحات موضوعية: OPIOID receptors, CURIOSITY, PAIN threshold, LABORATORY rats, PAIN tolerance, NALOXONE, ANXIETY

مستخلص: Acute stress exposure triggers a cascade of neurochemical reactions, leading, specifically, to behavior changes and increased pain tolerance in humans and animals. ACTH/MSH-like peptides play an important role in regulating the organism's response to stressful exposures. The aim of the present study was to assess the effects of the heptapeptide Semax, a synthetic ACTH4–10 analog, in various models of acute stress. The effect of intraperitoneal Semax administration at doses of 0.05 and 0.5 mg/kg on changes in behavior and pain sensitivity of Wistar rats was investigated in models of inescapable intermittent footshock stress and forced cold-water swim stress. To assess the involvement of the endogenous opioid system in the effects of stress, there was studied an impact of the preadministration with the opioid receptor antagonist Naloxone (1 mg/kg). The stressors used led to an increase in the pain threshold in the paw-pressure test, which indicates the development of stress-induced analgesia (SIA). In addition, rats exposed to stress showed decreased exploratory behavior and increased anxiety-like behavior in the hole board test. Both Semax and Naloxone attenuated SIA in the model of inescapable footshock stress, but did not affect pain threshold values in the model of forced cold-water swim stress. Both drugs did not affect rat behavior in the above models of acute stress. It can be concluded that Semax attenuates the opioid form of SIA, but does not affect behavior changes in rats exposed to acute stress. [ABSTRACT FROM AUTHOR]

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