Бібліотека Вінницького національного медичного університету ім. М.І.Пирогова

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Synthesis and investigation of the derivatives of amidinohydrazonelated aromatic compounds as furin inhibitors / T. V. Osadchuk [et al.] // The Ukrainian Biochemical Journal. - 2017. - Том 89, N 6. - P3-12

MeSH-главная:
ФУРИН -- FURIN (терапевтическое применение)
Аннотация: The proprotein convertase furin plays a crucial role in a variety of pathogenic processes such as cancer, bacterial and viral diseases, neurodegenerative disorders and diabetes. Thus, furin inhibitors are promising therapeutics for the treatment of many diseases. In this study we synthesized some new non-peptide of furin inhibitors, with positively charged amidinohydrazone groups present in ortho-, meta– or para-positions in the benzene rings relative to the linker. From the results of biological testing it followed that the position of amidinohydrazone groups in aromatic rings was significant for the manifestation of antifurin activity. The replacement of linkers containing a propoxy group by a “bridge” with a benzene ring was found to cause an increase in the inhibitory effect of the compounds. The effect of synthesized bisamidinohydrazones on furin also depended on the substitution of the hydrogen atom in the amidinohydrazone group by the methyl group. These compounds were shown to block the enzyme activity mainly by the mechanism of mixed inhibition, and their Ki values were at the micromolar level
Доп.точки доступа:
Osadchuk, T. V.
Semyroz, A. V.
Shybyryn, O. V.
Kibirev, V. K.

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Kolas, I. K.
Copurification of chicken liver soluble htiamine monophosphatase and low molecular weight acid phosphatase / I. K. Kolas, A. F. Makarchikov // The Ukrainian Biochemical Journal. - 2017. - Том 89, N 6. - P13-21

MeSH-главная:
ТИАМИНМОНОФОСФАТ -- THIAMINE MONOPHOSPHATE (метаболизм)
ПЕЧЕНЬ -- LIVER (ультраструктура, цитология)
ЭУКАРИОТЫ -- EUKARYOTA
Аннотация: Thiamine monophosphatase (ThMPase) is an enzyme of thiamine metabolism in animals whose molecular nature has still to be elucidated. In this study we have achieved a 714-fold purification of a soluble enzyme possessing ThMPase activity from a chicken liver extract. In addition to ThMPase, acid phosphatase activity was traced during purification. Both activities proved to have coincident elution profiles at all chromatographic steps implying the same enzyme involved. The molecular weight of the enzyme was 18 kDa as estimated by gel filtration. Along with ThMP and p-nitrophenyl phosphate, the purified enzyme was capable of hydrolyzing flavin mononucleotide as well as phosphotyrosine. Subcellular distribution of ThMPase activity was also explored indicating its cytosolic localization. The results of the present work imply the involvement of low molecular weight acid phosphatase in thiamine metabolism in the chicken liver
Доп.точки доступа:
Makarchikov, A. F.

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Antioxidant activity of melatonin and glutathione interacting with hydroxyl and superoxide anion radicals / T. Y. Kuznetsova [et al.] // The Ukrainian Biochemical Journal. - 2017. - Том 89, N 6. - P22-30

MeSH-главная:
МЕЛАТОНИН -- MELATONIN (вредные воздействия)
ГЛУТАТИОН -- GLUTATHIONE (вредные воздействия)
КИСЛОРОД -- OXYGEN
Аннотация: Based on the analysis of the results obtained by quantum chemical modeling of interaction between reduced glutathione (GSH) and melatonin (MLT) molecules with oxygen radicals (•OH and • OOˉ) it was found that this interaction occured following the acid-base mechanism, where MLT and GSH acted as a base in respect of •OH, and as acid in respect of •OOˉ. We have carried out the correlation of the results of quantum chemical calculations (density redistribution, energetic characteristics) under the interaction of MLT and GSH molecules with •OH and •OOˉ in changing macroscopic properties of the process of electroreduction of free oxygen radicals in the presence of antioxidants (potential and maximal current wave reduction waves). This was a direct experimental macroscale evidence of the results of theoretical modeling at the nanoscale level that pointed to a marked antioxidant activity of glutathione compared with melatonin
Доп.точки доступа:
Kuznetsova, T. Y.
Solovyova, N. V.
Solovyov, V. V.
Kostenko, V. O.

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Changes in proHB-EGF expression after functional activation of the immune system cells / T. O. Chudina [et al.] // The Ukrainian Biochemical Journal. - 2017. - Том 89, N 6. - P31-38

MeSH-главная:
ИММУНОГЕНЕТИЧЕСКИЕ ПРОЦЕССЫ -- IMMUNOGENETIC PROCESSES (действие лекарственных препаратов)
ЛИПОПОЛИСАХАРИДЫ -- LIPOPOLYSACCHARIDES (вредные воздействия)
Аннотация: The level of proHB-EGF expression on J774, Raji, KG-1 cells derived from different types of human and mouse immune system cells under the standard in vitro culture conditions and during functional activation of these cells was investigated. Changes in the proHB-EGF expression on the cell surface were found to depend on the density of cell population, the content of fetal bovine serum in the culture medium, the effect of mitogenic factors – bacterial lipopolysaccharide, an inactive full-size form of diphtheria toxin (CRM197) and recombinant soluble HB-EGF – rsHB-EGF. The results obtained are important for the understanding of the functional role of proHB-EGF receptor on the surface of macrophage-like cells and B lymphocytes and indicate the involvement of this receptor in immune response regulation in an organism
Доп.точки доступа:
Chudina, T. O.
Labintsev, A. J.
Romaniuk, S. I.
Kolybo, D. V.
Komisarenko, S. V.

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Gonchar, O. A.
Time-dependent effect of severe hypoxia/reoxygenation on oxidative stress level, antioxidant capacity and p53 accumulation in mitochondria of rat heart / O. A. Gonchar, I. N. Mankovska // The Ukrainian Biochemical Journal. - 2017. - Том 89, N 6. - P39-47

MeSH-главная:
СЕРДЦЕ -- HEART (патофизиология)
АНОКСИЯ -- ANOXIA (патофизиология)
Аннотация: The intensity of oxidative stress, protein expression of antiapoptotic Bcl-2 as well as antioxidant enzymes manganese superoxide dismutase (MnSOD) and glutathione peroxidase (GPx) and their regulator p53 were studied in the mitochondria of rat heart. Sessions of repeated hypoxia/reoxygenation ((H/R), 5 cycles of 10 min hypoxia (5.5% O₂ in N₂) alternated with 10 min normoxia, daily) were performed in our study. It was shown that short-term sessions of H/R (during 1-3 days) caused a significant increase in the oxidative stress markers (ROS formation and lipid peroxidation), mitochondrial p53 translocation, a decrease in MnSOD protein expression/activity and Bcl-2 protein content, but up-regulated GPx. We have demonstrated that prolonged H/R (7-14 days) induced myocardial tolerance to fluctuation in oxygen levels that was associated with the reduction in mitochondrial p53 protein content, elevation of mitochondrial Bcl-2 protein level, and increase in antioxidant capacity. A close correlation between the mitochondrial p53 accumulation and ROS formation as well as the activity and protein content of MnSOD and GPx allowed us to assume that p53 took an active part in the regulation of prooxidant/antioxidant balance in mitochondria of rat heart during repeated H/R
Доп.точки доступа:
Mankovska, I. N.

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Effect of L-carnitine administration on serum insulin and adiponectin levels, and AMPK, APPL1 and PPAR? gene expression in STZ-induced diabetic rat liver / B. Shahouzehi [et al.] // The Ukrainian Biochemical Journal. - 2017. - Том 89, N 6. - P48-55

MeSH-главная:
ДИАБЕТ САХАРНЫЙ ЭКСПЕРИМЕНТАЛЬНЫЙ -- DIABETES MELLITUS, EXPERIMENTAL (метаболизм)
КРОВЬ -- BLOOD (действие лекарственных препаратов)
ПЕЧЕНЬ -- LIVER (действие лекарственных препаратов)
КАРНИТИН -- CARNITINE (фармакокинетика)
Аннотация: Diabetes is considered as a metabolic disease in which insulin secretion and functions are disturbed and characterized by hyperglycemia. L-carnitine is synthesized in most mammals and plays critical role in fatty acid oxidation and energy production. Data about the L-carnitine hypoglycemic effects are controversial. We evaluated long-term oral L-carnitine administration effects on blood glucose, insulin and adiponectin levels, as well as expression of AMPK, APPL1 and PPARγ genes in liver of STZ-induced diabetic rats. Group 1 (control), did not receive any treatment, group 2 received 50 mg/kg STZ by i.p injection, group 3 received single dose of 50 mg/kg STZ by i.p injection and also 600 mg/kg/day L-carnitine orally for 5 weeks. Our results showed that L-carnitine long-term oral supplementation significantly reduced blood glucose and normalized insulin levels in diabetic rats. Also, we found that L-carnitine significantly increased AMPK and APPL1 expression, and showed a mild elevation of PPARγ expression. In sum, we suggest that long-term L-carnitine supplementation has beneficial effects on diabetic rats which showed hypoglycemic effects. Probably the beneficial effects of L-carnitine are contributed to the upregulation of insulin sensitizers such as AMPK and adiponectin
Доп.точки доступа:
Shahouzehi, B.
Barkhordari, K.
Aminizadeh, S.
Masoumi-Ardakani, Y.

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Effects of thiosulfonates on the lipid composition of rat tissues / A. Z. Pylypets [et al.] // The Ukrainian Biochemical Journal. - 2017. - Том 89, N 6. - P56-62

MeSH-главная:
ЛИПИДЫ (кровь)
ТИОСУЛЬФАТЫ -- THIOSULFATES (фармакокинетика)
Аннотация: Thiosulfonates are synthetic analogs of organic sulfur-containing compounds isolated from plants. Recent studies have shown that these substances lowering cholesterol content in the body, are effective against hyperlipidemia. Therefore, the aim of our investigation was to study the effect of synthesized thiosulfonates on the content of lipids and their spectrum in rats blood, liver and kidney. The amount of total lipids and their fractional profile were determined by thin-layer chromatography. The administration of methyl-, ethyl-, and allylthiosulfonates at a dose of 300 mg/kg of body weight did not cause significant changes in the content of total lipids and phospholipids, but led to the redistribution of their classes in the examined tissues. The content of triacylglycerols in the blood plasma under the action of ethyl- and allylthiosulfonates was decreased by 29.14 and 23.19% (P 0.05-0.01), respectively, whereas the injection with methyl- and ethylthiosulfonates was accompanied by a significant decrease in mono-, di-, triglycerides and free fatty acids in the liver compared to control. The most significant changes in the lipid profile of kidney tissue were detected under the action of methylthiosulfonate
Доп.точки доступа:
Pylypets, A. Z.
Iskra, R. Ya.
Havryliak, V. V.
Nakonechna, A. V.
Novikov, V. P.
Lubenets, V. I.

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Комісаренко, С. В.
Для чого потрібні циркадні ритми, або як змінити хід "біологічного годинника" / С. В. Комісаренко, С. І. Романюк // The Ukrainian Biochemical Journal. - 2017. - Том 89, N 6. - С. 63-73

MeSH-главная:
ЦИРКАДНЫЙ РИТМ -- CIRCADIAN RHYTHM (физиология)
БИОЛОГИЧЕСКИЕ ЧАСЫ -- BIOLOGICAL CLOCKS (физиология)
Аннотация: 2 жовтня Нобелівський комітет при Каролінському медичному інституті оголосив імена лауреатів Нобелівської премії з фізіології і медицини за 2017 рік. Ними стали троє американських учених: Джеффрі Холл (Jeffrey C. Hall), майкл росбаш (Michael Rosbash) і майкл Янг (Michael W. Young). Нагороду їм присуджено «за відкриття молекулярних механізмів, що контролюють циркадний ритм»
Доп.точки доступа:
Романюк, С. І.

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