[Activity of cytochrome P-450 aromatase, nitric oxide synthase and level of S-nitrosothiols in rat ovaries and uterus under oxidative stress caused by cobalt chloride]. / Aktivnost' tsitokhorma P-450 aromatazy, sintazy oksida azota i soderzhanie S-nitrozotiolov v iaichnikakh i matke krys pri oksidativnom stresse, vyzvannom khloridom kobal'ta.

Cytochrome P-450 aromatase and nitric oxide syntase activities were established to decrease in the ovaries and uteri of CoCl2 injected Wistar female rats. Respectively the S-nitrosothiols concentration was also decreased. The quantity of malonic dialdehyde was increased in the ovaries and uteri of rats injected by CoCl2. It's assumed that reactive oxygen species formed by CoCl2 inhibit the activities of aromatase and nitric oxide syntase as haem ligands and inhibitors of it's biosynthesis.

[Effect of nonsteroidal estrogen-like substances on aromatase activity]. / Vliianie nesteroidnykh veshchestv s éstrogenopodobnym éffektom na aktivnost' aromatazy.

The effects in vitro of DDT, DDE and genistein on rat uterine purified aromatase activity were studied. It was established that all these compounds were competitive aromatase inhibitor. In the studies in vivo DDT and genistein decrease the rat ovarian and rat uterine aromatase activity. They were identified to decrease the quantity of the aromatase in these organs by inhibiting the expression of corresponding genes.

[In vitro study of regulation of rat liver xanthine oxidase activity by antioxidant reducing agents]. / Issledovanie in vitro reguliatsii aktivnosti ksantinoksidazy pecheni krys vosstanoviteliami-antioksidantami.

It was learned the regulation of xanthine oxidase activity from rat liver in the partly purified prepared by ascorbic acid, glutathione-SH, dithiothreitol, cysteine++ and hydrocortisone++. It was shown that ascorbic acid glutathione-SH, dithiothreitol, and cysteine++ can be activators and uncompetitor inhibitors of xanthine oxidase in dependence from concentration. As far as hydrocortisone is concerned, it is a powerful uncompetitor inhibitor of xanthine oxidase, that is bind with it. It was considered the mechanism of activation and inhibition of xanthine oxidase by these reductors-antioxidants.

[Effect of caffeine on xanthine oxidase activity]. / Vliianie kofeina na aktivnost' ksantinoksidazy.

The effect of caffeine on the xanthine oxidase activity in human organism has been studied. It was revealed that caffeine calls the inconsiderable reliable increase of the level of uric acid and the reliable lowering of levels of hypoxanthine and xanthine in urine. The isosteric inhibition of xanthine oxidase activity by caffeine was revealed in the experiments in vitro. It was proved that caffeine cannot be the inhibitor of xantine oxidase in vivo because it demethylases to I-methylxanthine.

[The effect of calcium chloride on the distribution, protein binding and catabolism of 14C-biotin in the body of white mice]. / Vplyv khlorydu kal'tsiiu na rozpodil, proteïdyzatsiiu ta katabolizm 14C-biotynu v orhanizmi bilykh myshei.

Calcium chloride injected intramuscularly to white mice in the therapeutical dose of 50 mM/kg, influences considerably distribution, proteidization, enterohepatic recycling level, elimination from the blood, excretion with urine and catabolism of 14C-biotin injected simultaneously in the physiological dose of 0.5 mM/kg. CaCl2 decreases and retards inflow of the 14C-biotin general radio-label to the analyzed tissues and organs, with the simultaneous increase of its proteidization in the same tissues. At the same time permeability of histohematic barriers of these tissues for 14C-biotin under the CaCl2 effect falls markedly. Calcium chloride increases the level of complete catabolism of 14C-biotin to 14CO2 by 51% 480 min after their simultaneous injection. A conclusion is made that calcium introduced as CaCl2 in the mentioned dose inhibits enterohepatic recycling of 14C-biotin in the white mice organism with the simultaneous of 14C-biotin assimilation in the analyzed tissues.

[The effect of parenterally administered alcohol on the riboflavin balance in the tissues of white mice]. / Vplyv parenteral'noho vvedeniia alkoholiu na balans ryboflavinu u tkanynakh bilykh myshei.

Accumulation of general flavins and distribution of 14C-riboflavin, intensity of this vitamin renewal in organs and tissues of white mice under conditions of parenteral injection of ethanol have been studied. It is shown that alcoholic intoxication has intensified renewal of riboflavin in tissues of the digestive system and in some other organs due to increased excretion of endogenous forms of the vitamin with following filling of the vacant depots by an exogenous vitamin.

[Metabolism and catabolism to CO2 of [14C] gamma-aminobutyric acid conjugates with pyridoxal phosphate, nicotinate and biotin]. / Obmen i katabolizm do CO2 kon"iugatov [14C]gamma-aminomaslianoi kisloty s piridoksal'fosfatom, nikotinatom i biotinom.

Pharmacokinetics and catabolism to CO2 in the mice organism and metabolic transformation by the tissues homogenates of [1-14C] GABA and its conjugates with nicotinate, pyridoxal phosphate and biotin have been studied. The permeability of nicotinoyl-GABA through the hemato-encephalic barrier was 10 times as much as the corresponding value for GABA and its conjugates with other vitamins. PLP-GABA is eliminated more rapidly from the brain in comparison with GABA, biotinyl-GABA is retained to a higher degree in kidneys, the entero-hepatic recycling takes place more actively for nicotinoyl-GABA. The latter, in contrast to biotinyl-GABA, remains unaffected by the liver, intestine mucose membrane and brain proteases and is catabolized to CO2 to a considerably lower extent as compared with GABA, perhaps due to the intestine bacterial microflora.

[The possible participation of the GABA metabolic system in the mechanisms of the protective action of L-aspartate in hypoxia in an enclosed space]. / O vozmozhnom uchastii sistemy metabolizma GAMK v mekhanizmakh zashchitnogo deistviia L-aspartata pri gipoksii zamknutogo prostranstva.

L-Aspartate given intradermally in a dose of 100 mg.kg-1 to mice 2-3 minutes before placement to a hypoxic chamber was shown to prolong the mean animal lifespan by 38% and to delay hypoxic convulsions by 38-40%. The agent was ascertained to maintain the higher glutamate decarboxylase (GD) activity and GABA levels in the brain during hypoxia and prevent GD activity and GABA levels from their drastic diminution when hypoxic convulsions occurred.

[The role of transaminases in realizing the protective effect of L-aspartate in hypoxia]. / Rol' transaminaz v realizatsii zashchitnogo éffekta L-aspartata pri gipoksii.

Activation of aspartate aminotransferase and alanine aminotransferase of mitochondria introduced to the incubation medium of pyridoxal-5'-phosphate (40 microM) is approximately 2 times higher than that of the corresponding cytoplasmic forms. At hypoxia aspartate aminotransferase activity in mitochondria and postmitochondrial supernatant tends to an increase while that of alanine aminotransferase decreases (above 2 times). The protection from hypoxic damage when using L-aspartate (100 mg/kg subcutaneously 3-5 min before hypoxia) intensifies an adaptive increase of aspartate aminotransferase activity and removes a decrease of alanine aminotransferase activity. Under these conditions stimulating effect of pyridoxal-5'-phosphate on transaminases activity in vitro weakens. A simultaneous administration of vitamin-coenzyme complex (thiamine pyrophosphate, lipoate, sodium 4-phospho-pantothenate, flavin-mononucleotide, nicotinate) intensifies these metabolic shifts and protective action of L-aspartate.

[The interaction of lipoic acid and its metabolites with aspartate and alanine aminotransferases in a multienzyme complex from rat liver and brain mitochondria]. / Vzaiemodiia lipoievoï kysloty ta ïï metabolitiv z aspartat- i alaninaminotransferazoiu u mul'tienzymnomu kompleksi mitokhondrii pechinky i mozku shchuriv.

It is shown that lipoic acid and its metabolites--lipoamide and 4,6-dithiohexanoic acid can interact and inhibit the mitochondrial aspartate- and alanine-aminotransferase activities. This effect is much more pronounced in the case of multienzyme complexes--metabolon.

[Effect of preliminarily administered aspartate to the body and its combination with a vitamin-coenzyme complex on the catabolism of L-[14C]-aspartate in tissues of various mouse organs in hermetically closed space]. / Vliianie predvaritel'no vvedennogo v organizm aspartata i ego sochetaniia s vitaminno-kofermentnym kompleksom na katabolizm L-[14C]-aspartata v tkaniakh nekotorykh organov myshei v usloviiakh germozamknutogo prostanstva.

Effect of factors of sealed non-aired space on the organism leads to the enhancement of catabolism of L-4-[14C]-aspartate in the mice encephalon to 14CO2. Preliminary administration of L-aspartate to the organism (100 mg/kg) leads to the intensification of these adaptative reactions and prolongs life of animals under these conditions. Accumulation of the introduced aspartate in the liver and encephalon gets more intensive and its supply to the blood is more rapid under these conditions. Simultaneous (together with L-aspartate) administration of the vitamin-coenzyme complex (pentapyruvate) which includes thiamine pyrophosphate, lipoate, sodium 4-phosphopantotenate, nicotinate and riboflavin-mononucleotide and stimulates the function of the key links of the Krebs cycle to animals has induced intensification of the protective effect of L-aspartate and evoked further activation of the L-aspartate catabolism in the encephalon, mainly at late, preagonal stages of the developing pathological state. The data presented confirm that protective effect of L-aspartate, provided the effect of the closed space factors on the organism, is a result of its quick introduction, into energy mebolism of tissues, in particular, of the nervous tissue.

[Experimental substantiation of the method of pharmaco-metabolic brain protection against hypoxia in severe craniocerebral injury]. / Eksperimental'noe obosnovanie sposoba farmakometabolicheskoi zashchity mozga ot gipoksii pri tiazheloi cherepno-mozgovoi travme.

The experiment has shown that a complex of functionally related vitamins including thiamine, lipoate, D-pantothenate, nicotinate and riboflavine in "pyruvate-dehydrogenase" ratios decreases inhibition of the activity of alpha-keto acid dehydrogenases in the brain and liver with thiopental anesthesia, intensifies arrival of [35S]-lipoate to the brain and decreases acute toxicity of sodium thiopental (TnNa). The same complex (where thiamine, pantothenate and riboflavine are substituted by the corresponding coenzyme forms) complemented by the components stimulating the function of GABA-bypath of the brain as administered to rats with serious craniocerebral injury on the background of prolonged anaesthesia effect improves recovery of the brain functions, that is followed by normalization of ketoglutarate-dehydrogenase activity, maintenance of GABA-bypath function and by a decrease of GABA and glutamate content in the brain. The results obtained substantiate the advisability to use vitamin-coenzyme-metabolic complex in the acute period of traumatic brain disease aimed to increase efficiency of the antihypoxic TnNa effect and to correct its undesirable effects.

[Supermolecular organization of aminotransferases and dehydrogenases of alpha-ketoacid from rat brain mitochondria]. / Hadmolekuliarnaia organizatsiia aminotransferaz i degidrogenaz alpha- ketokislot mitochondrii golovnogo mozga krys.

A fraction of coarse mitochondria from the rat brain was deposited after short-term effect of supersound to obtain "metabolones". Activity of dehydrogenases of alpha-ketoacids, succinate dehydrogenase, aspartate-, alanine- and GABA-alpha-ketoglutarate amino-transferases has been determined in the supernatant liquid and in "metabolones". It is shown that dehydrogenase activity is mainly (93-100%) localized in "metabolones", while the level of aminotransferase activity in the latter is lower (72-94%). Nonproportionally high activity of aminotransferases in the supernatant liquid is found to considerably suprpass a decrease in activity of these enzymes in "metabolones" against a background of extremely scanty losses of protein (within 5%) induced by the supersound effect. A hypothetic model of a "metabolone" containing the enzymes of the Krebbs cycle and GABA-shunt is suggested.

[Distribution and replenishing of riboflavin in albino mice with acute alcoholic intoxication]. / Raspredelenie i obnovliaemost' riboflavina v organizme belykh myshei v usloviiakh ostroi alkogol'noi intoksikatsii.

It is shown that acute alcohol intoxication in the tissues of white mice accelerates riboflavin metabolism. In this case arrival of the exogenous vitamin with accompanying depletion of its endogenous resources is observed to intensify.

[Neurometabolic effects and antihypoxic activity of a vitamin-coenzyme complex, including thiamine pyrophosphate, lipoate, 4-phosphopantothenate, nicotinate and flavinadenine mononucleotide]. / Izuchenie neirometabolicheskikh éffektov i antigipoksicheskoi aktivnosti vitaminno-kofermentnogo kompleksa, vkliuchaiushchego tiaminpirofosfat, lipoat, 4-fosfopantotenat, nikotinat i flavinadeninmonanukleotid.

Administration of the vitamin-coenzyme complex containing thiamin pyrophosphate:lipoate:4-phosphopantothenate:nicotinate:flavinad enine mononucleotide (0.2:3:5:8:1) led to increased utilization of alpha-ketoglutarate in nervous tissue via alpha-ketoglutarate dehydrogenase and GABA-transaminase pathways. In these systems content of glutamate and GABA was decreased, suggesting their elevated consumption as energy-providing substrates. If 4-phosphopantothenate was substituted by CoASH and nicotinate--by NAD+, increased decarboxylation of 5(-14)C-alpha-ketoglutarate, 1(-14)C-GABA and 4(-14)C-Asp was detected in brain homogenates in vitro. The neurometabolic effects were accompanied by pronounced antihypoxic effects as shown by the test "hypoxy of closed space".

[Catabolism of labelled alpha-ketoglutarate, succinate, aspartate and gamma-aminobutyric acid in nerve tissue; the effect of pyridoxal-5'-phosphate in vitro]. / Katabolizm mechenykh alpha-ketoglutarate, suktsinata, aspartata i gamma-aminomaslianoi kisloty v nervnoi tkani; vliianie piridoksal'-5'-fosfata in vitro.

Proceeding from estimation of the 14CO2 release from [5-14C]alpha-ketoglutarate, [1-14C] gamma-aminobutyric acid (GABA), [1,4-14C] succinate and [4-14C] aspartate (0.4-1 mM) during their incubation with homogenates of different brain areas with regard for the label position and stereospecificity of decarboxylation of citrate formed due to the metabolism, the relative intensity of their catabolism is determined: [1,4-14C] succinate much greater than [4-14C]aspartate greater than [5-14C] alpha-ketoglutarate much greater than [1-14C]GABA. The label release with catabolism of [1-14C] alpha-ketoglutarate considerably exceeds the intensity of decarboxylation of the above enumerated substrates. In all cases the maximum release of 14CO2 has been registered in the cortex homogenates, the minimum--in the medulla homogenates, and only under long-term incubation with high concentration of GABA (50 mM) maximum catabolism was registered in the medulla. Preincubation of nervous tissue with pyridoxal-5'-phosphate (40 microM) results in significant acceleration of catabolism of [1-14C] alpha-ketoglutarate, [5-14C] alpha-ketoglutarate and [4-14C] aspartate with an inconsiderable increase of catabolism of the rest of labelled substrates.

[The protective effect of energy substrates, vitamins, coenzymes and their complexes in the action on the body of the factors of an enclosed space]. / Zashchitnyi éffekt énergeticheskikh substratov, vitaminov, kofermentov i ikh kompleksov pri deistvii na organizm faktorov zamknutogo prostranstva.

Experiments on mice were performed to study a protective action of amino acids and other oxidation substrates (L-aspartic acid, pyruvate, succinate, GABA, alpha-ketoglutarate), metabolites (pyridoxal-5'-phosphate) as well as vitamin-coenzyme complexes in combination with oxidation substrate while being under closed space conditions. GABA, aspartate, glutamate possessed the highest protective effect as against alpha-ketoglutarate and succinate.

[Dynamics of absorption of C-14-biotin by blood cells and plasma protein binding in ontogenesis]. / Dinamika pogloshcheniia 14C-biotina kletkami krovi i sviazyvanie belkami plazmy v ontogeneze.

Age peculiarities of absorption of 14C-biotin by the blood cells and plasma proteins in vitro are studied. The phase dynamics of 14C-biotin absorption by the blood cells and binding by plasma proteins is found. The reliable ontogenetic differences in absorption of 14C-biotin by the blood cells and plasma proteins are determined. The biotin-binding in vitro by the blood cells and plasma proteins decreases and becomes slower in old rats as compared with young ones.

[Study of the restoration and balance of thiamine in the tissues of albino mice in alcoholic intoxication]. / Izuchenie obnovliaemosti i balansa tiamina v tkaniakh belykh myshei pri deistvii étanolovogo narkoza.

Acute inhalative alcoholic intoxication has been studied for its effect on the influx and level of free and bound thiamine in tissues of white mice. It is established that acute inhalative ethanol intoxication increases 35S-thiamine incorporation in tissues and decreases the level of endogenic free and bound thiamine. The results obtained permit a conclusion on intensification of the thiamine renewal in tissues with its sufficient influx from outside as affected by the ethanol narcosis.

[The effect of thiamine and its metabolites on pepsin and trypsin activity]. / Vplyv tiaminu ta iogo metabolitiv na aktyvnist' pepsynu i trypsynu.

The presence of thiochrome in the incubation medium increases the pepsin activity. Thiamine pyrophosphate decrease the pepsin and trypsin activity. The established facts may be important for the physiological regulation of proteases activity in the stomach-intestine tract.