[Potentiation of activation of soluble guanylate cyclase by YC-1, NO-donors and increase of the synergistic effect of YC-1 on NO-dependent activation of the enzyme by 1,2,3-triazolyl-1,2,5-oxadiazole derivatives].

The influence of (1H-1,2,3-triazol-1-yl)-1,2,5-oxadiazole derivatives: 4-amino-3-(5-methyl-4- ethoxycarbonyl-(1H-1,2,3-triazol-1-yl)-1,2,5-oxadiazole (TF4CH3) and 4,4'-bis(5-methel-4-ethoxycarbonyl-1H- 1,2,3-triazol-1-yl)-3,3'-azo-1,2,5-oxadiazole (2TF4CH3) on stimulation of human platelet soluble guanylate cyclase by YC-1, NO-donors (sodium nitroprusside, SNP, and spermine NONO) and on a synergistic increase of NO-dependent enzyme activation in the presence of YC-1 has been investigated. Both compounds increased guanylate cyclase activation by YC-1, potentiated guanylate cyclase stimulation by NO-donors and increased the synergistic effect of YC-1 on NO-dependent activation of soluble guanylate cyclase. The similarity in the properties of the examined TF4CH3 and 2TF4CH3 with that of YC-1 and the possible mechanism underlying the revealed properties of compounds used are discussed.

[Nutrition value of tropical and subtropical fruits].

The article is devoted to the study of the chemical composition of tropical and subtropical fruit (avocado, papaya and mango), which are now in great numbers are on the appeared on the Russian market. Due to use technology tropical and subtropical fruits can be implemented in almost all areas and regions of the country. Relatively low cost makes these products quite popular among the people. In domestic scientific literature there are no systematic data describing the chemical composition of these tropical and subtropical fruits sold in the domestic market, while the information needed to calculate food and energy value of diets and culinary products derived from tropical and subtropical fruit. Avocado fruits are sources of insoluble dietary fiber content of which was equal to 12.2%, as well as minerals. The study of the fatty acid composition of lipids avocados showed high content of oleic acid fruit, which accounts for 53.2% of total fatty acids in these fruits. Which makes them a valuable source of unsaturated fatty acids.

Synthesis and antineoplastic properties of (1H-1,2,3-triazol-1-yl)furazans.

A method of 3-amino-4-[5-aryl(heteroaryl)-1H-1,2,3-triazol-1-yl)]furazan synthesis was optimized. Condensation of these compounds with 2,5-dimethoxytetrahydrofuran resulted in a series of previously unknown 4-[5-aryl(heteroaryl)-1H-1,2,3-triazol-1-yl)]-3-(pyrrol-1-yl)furazans. All target compounds were evaluated for both antimitotic microtubule destabilizing effect in a phenotypic sea urchin embryo assay and cytotoxicity in a panel of 60 human cancer cell lines. Pyrrolyl derivatives of triazolylfurazans were determined as antiproliferative compounds. The most potent microtubule targeting compounds 7a and 7e are of interest for further trials as antineoplastic agents.

[Composition and content of biologically active substances in rose hips].

The paper studies the chemical composition of the powders obtained from the pulp with the skins and seeds of fruits of wild rose hips. Research results have shown that the main fraction of the powder is dietary fiber, powder of seeds of insoluble fiber in 1,6 and 2,3 higher than in the powder of the fruit with a thin skin and pulp, respectively. The greatest amount of carbohydrates and protein found in powders and pulp of the fruit with a thin skin, and lipids predominate in the powder from the seeds. Found that the lipid powder rosehip richest in oleic, linoleic and linolenic acids, the share of oleic acid has 6,4-19,2%, linoleic and linolenic 19,7-45,8 and 23,3-33,9% of the amount of fatty acids. Lipids powders of hips and seeds of rose have higher levels of essential linoleic acid and powder from the pulp with the skins - linolenic acid. In the study established the presence of sterols 7 fractions, the predominant of which is the beta-sitosterol. In the powder from the pulp with the skins found the greatest amount of ascorbic acid, carotenoids, and the powder of seeds - vitamin E. Carotenoids in powders are beta-carotene and lycopene. The high content of ascorbic acid, vitamin E and carotenoids in powder from wild rose hips makes them a good source of antioxidants. Therefore, we studied the possibility of using vegetable powders obtained from hips of wild rose, to enrich biologically active substances such as vitamins C, E and carotenoids, food supply, particularly of health care use. Rosehip powder from the pulp with the skins had the highest antioxidant activity, antioxidant activity of hips powders was 74% of the activity of powder from the pulp with the skins, the lowest antioxidant activity was observed in the powder from the wild rose seeds. That's way, based on the analysis of the chemical composition of rose hip powder found high levels they ascorbic acid, carotenoids, flavonoids,found their high antioxidant activity. It allows to recommend powders produced from the hips, as a source of physiologically functional ingredients for the production of fortified food products, especially medical and prophylactic purposes. The use of such additives will fill the gap in the body of P-active substances, vitamins C and E, beta-carotene, pectin substances.

[Comparative evaluation of zinc organic and inorganic form bioavailability in vivo].

Bioavailability of zinc complex with enzymatic hydrolysate of milk protein (EHMP) was studied in Wistar rats. Body mass, zinc content in os femoris and serum alkaline phosphatase activity were similar in rats receiving Zn-EHMP and zinc sulphate and were significantly higher than in animals fed with basal semi synthetic zinc-deficient diet. Apparent absorption of both Zn sources in rat's intestine was high (more than 70%) probably due to absence of plant dietary fiber in applied diet. Zinc organic form use in fortification of food is discussed.

[The homeostatic changes of mineral and trace elements during of year at rheumatoid arthritis].

Dietetic therapy on a basis of specially developed variant anti-inflammatory, hypoallergic, hyposodium diets 10 PA, applied in Clinic of Institute of Nutrition Russian Academy of Medical Science for treatment of patients rheumatoid an arthritis, has yielded the positive clinical results comparable to efficiency of medicinal therapy. Two-year-old researches have allowed to receive representative enough (756 element-definition) a material on macro- and to microelement structure of plasma of blood of patients and its seasonal dynamics determined by interaction two neurohumoral systems. For two elements--K and Zn, changes of concentration in whey of blood during one year it was revealed not, but for others five investigated elements--Na, Ca, Mg, Cu and Fe, curves with appreciable maxima and minima of contents which did not coincide with similar dependences for healthy people and about earlier investigated pathologies of other genesis were observed. The received data are interpreted for the benefit of adaptive, protective character of seasonal changes dynamic homeostasis.

[The season changes of mineral and trace elements contents in blood patients with ulcer pathology gastric and intestinal duodenal].

There are two concepts of homeostasis microelements: a traditional one, considering homeostasis as a constancy of internal media of alive organisms, and an alternative, examining the change of structure of these media in time as a consequence of change of external factors. In the first concept the deviation of concentration of a microelement from norm in whey of blood is considered a diagnostic attribute of microelementose (deficiency or surplus). In the second concept, on the contrary, it is supposed, that such deviations can have the adaptive character assisting to an organism in struggle against illness. At three-year research of 436 patients by a stomach ulcer and duodenal we have revealed precise patterns of seasonal changes of homeostasis the basic seven elements of whey of blood--Na, K, Ca, Mg, Zn, Cu and Fe which differ from similar time functions for healthy people and can be explained only on the basis of the assumption about protective adaptations an organism at the given pathology. As functions of time it is considered two homeostasis parameters--a level of concentration and capacity homeostasis which are determined not by processes of absorption, deducing and depositions, but requirements of a cellular level of a feed.

[Moscow schoolchildren zinc status: correction of zinc insufficiency by organic zinc compounds].

The paper presents the results of study of zinc hair content in 43 Moscow schoolchildren, aged 9-11 years of both sex (May 2003 to December 2003). Significant drop of zinc hair content was established in 67% of schoolchildren. It was shown that the organic form of zinc enchanted zinc hair content. The findings will be used to implement preventive and health-promoting measures among schoolchildren.

[Effect of a zinc-enriched diet on the clinical and metabolic parameters in type 2 diabetic patients]. / Vliianie BAD, soderzhashchei tsink, na kliniko-metabolicheskie pokazateli u bol'nykh sakharym diabetom 2 tipa.

It was investigated the influence of a diet with zinc supplementation on dynamic of glycaemia, lipid profile, blood pressure and weight in type 2 diabetic patients. Traditional hypocaloric diet was supplemented with zinc-spirulina (7.5 mg zinc per day). The results investigations indicated that a zinc-enriched diet has beneficial effects on basal and postprandial glycaemia, the content of cholesterol and triglycerides in serum in compared with a traditional hypocaloric diet.

Synthesis and vasodilating properties of N-alkylamide derivatives of 4-amino-3-furoxancarboxylic acid and related azo derivatives.

A series of N-alkylamide derivatives of 4-amino-3-furoxancarboxylic acids 5a-11a and their oxidation products, the azo derivatives 5b-11b, were synthesised and studied for their vasodilating properties. All the products were able to release rat aorta strips precontracted with (-)noradrenaline. Azo derivatives proved to be 20-200 times more potent than the parent amines. The large variation of lipophilicity within the two series does not seem to influence significantly the activity. Experiments carried out in the presence of oxyhaemoglobin (HbO(2)) suggest the involvement of nitric oxide (NO*) in the vasodilation.

[A study of the intake of zinc, copper and selenium by Moscow preschool children]. / Izuchenie obespechennosti tsinkom, med'iu i selenom moskovskikh detei doshkol'nogo vozrasta.

The paper presents the results of comprehensive study of the provision of Moscow preschool age children with zinc, copper, and selenium, which involved assessment of their dietary intake of these substances, analysis of the provision with these trace elements by using non-invasive biochemical studies, and examination of the children's physical development and morbidity. Comparison of the data on the levels of zinc, copper, and selenium in the hair, nail, and saliva with scanty data available in the literature leads to the conclusion that Moscow preschool children show subnormal provision with these trace elements, which is not accompanied by clinical symptoms of their deficiency.

Benzodifuroxan as an NO-dependent activator of soluble guanylate cyclase and a novel highly effective inhibitor of platelet aggregation.

The ability of benzodifuroxan (BDF) to activate human platelet guanylate cyclase was investigated. The maximal stimulatory effect (1160 +/- 86%) was observed at 0.01 mM concentration. Sodium nitroprusside produced the same stimulatory effect (1220 +/- 100%) but at a higher concentration (0.1 mM). 1-H-[1,2,4,]-Oxadiazolo[4, 3-alpha]quinoxalin-1-one (ODQ), an inhibitor of NO-dependent guanylate cyclase activation, attenuated the stimulatory effect of BDF (0.01 mM) by 75% and that of sodium nitroprusside (0.1 mM) by 80%. Increasing dithiothreitol concentration in the sample from 2. 10-6 to 2.10-4 M increased the stimulatory effect of BDF 2.7-fold. The possible involvement of sulfhydryl groups of low-molecular-weight thiols and guanylate cyclase in thiol-dependent activation of the enzyme is discussed. We have also found that BDF is a highly effective inhibitor of ADP-induced human platelet aggregation with IC50 of 6.10-8 M. The effect of sodium nitroprusside was much weaker (IC50, 5.10-5 M).

Vasorelaxant and antiplatelet activity of 4,7-dimethyl-1,2, 5-oxadiazolo[3,4-d]pyridazine 1,5,6-trioxide: role of soluble guanylate cyclase, nitric oxide and thiols.

1. Certain heterocyclic N-oxides are vasodilators and inhibitors of platelet aggregation. The pharmacological activity of the furoxan derivative condensed with pyridazine di-N-oxide 4,7-dimethyl-1,2, 5-oxadiazolo[3,4-d]pyridazine 1,5,6-trioxide (FPTO) and the corresponding furazan (FPDO) was studied. 2. FPTO reacted with thiols generating nitrite (NO), S-nitrosoglutathione and hydroxylamine (nitroxyl) and converted oxyHb to metHb. FPDO did not generate detectable amounts of NO-like species but reacted with thiols and oxyHb. 3. FPTO and FPDO haem-dependently stimulated the activity of soluble guanylate cyclase (sGC) and this stimulation was inhibited by 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) and by 0.1 mM dithiothreitol. 4. FPTO relaxed noradrenaline-precontracted aortic rings and its concentration-response curve was biphasic (pIC(50)=9. 03+/-0.13 and 5.85+/-0.06). FPDO was significantly less potent vasodilator (pIC(50)=5.19+/-0.14). The vasorelaxant activity of FPTO and FPDO was inhibited by ODQ. oxyHb significantly inhibited only FPTO-dependent relaxation. 5. FPTO and FPDO were equipotent inhibitors of ADP-induced platelet aggregation (IC(50)=0.63+/-0.15 and 0.49+/-0. 05 microM, respectively). The antiplatelet activity of FPTO (but not FPDO) was partially suppressed by oxyHb. The antiaggregatory effects of FPTO and FPDO were only partially blocked by sGC inhibitors. 6. FPTO and FPDO (10 - 20 microM) significantly increased cyclic GMP levels in aortic rings and platelets and this increase was blocked by ODQ. 7. Thus, FPTO can generate NO and, like FPDO, reacts with thiols and haem. The vasorelaxant activity of FPTO and FPDO is sGC-dependent and a predominant role is played by NO at FPTO concentrations below 1 microM. On the contrary, inhibition of platelet aggregation is only partially related to sGC activation.

[Lipid peroxidation and various parameters of mineral metabolism in patients with alimentary obesity during therapy with monosodium glutamate]. / Issledovanie perekisnogo okisleniia lipidov i nekotorykh pokazatelei mineral'nogo obmena u bol'nykh alimentarnym ozhireniem pri ispol'zovanii v dietoterapii mononatriia glutamata.

Lipid peroxidation and mineral metabolism were studied in patients with III degree of obesity and bad standing of sodium restricted diet before and after treatment with including in diet of monosodium glutamate (MSG). It was established well being of MSG and absence of negative effect on loss of body mass in course of dietary treatment. MSG caused normalization of level of diene conjugates and some minerals in serum of patients.

[Effect of diet on serum macroelement levels in patients with alcoholic lesions of the liver]. / Vliianie diety na soderzhanie makroélementov v syvorotke krovi u bol'nykh s alkogol'nym porazheniem pecheni.

The content of seven main biometals: sodium, potassium, calcium, magnesium, zinc, copper, iron was studied in the blood serum of patients with alcoholic affection of the liver verified clinically and morphologically. In contrast to literature data, it has been established that the levels of the main elements in the blood serum of patients with alcoholic affections of the liver may be normal, and concentrations of zinc, copper and iron are even elevated. The initial body mass of patients significantly influences the mineral spectrum of the blood serum: the levels of zinc and copper in patients with excessive body mass and obesity were significantly higher than in those with normal body mass. The content of the main elements in the blood serum was not changed in relation to the degree of the liver affection and alimentary therapy.

[Study of nutritive value of modified casein]. / Izuchenie pishchevoi tsennosti modifitsirovannogo kazeina.

It has been shown that modified casein purified from carbohydrate components contains several times less phosphorus and calcium as compared to initial casein. Figures close to experimental and potential biological value were obtained in experiments on growing rats with modified and initial casein as a protein component-milk substitute.

[Biological variability and accuracy in determining macro- and microelements in fish]. / O biologicheskoi izmenchivosti i tochnosti opredeleniia makro- i mikroélementov v rybakh.

The statistical analysis of 911 personal observations and literature findings on the mean content of ash, sodium, potassium, calcium, magnesium, iron, zinc, copper and manganese in different species of fish has brought to the conclusion on the absence of any reliable interspecies differences in the content of macro- and trace elements in fish muscle tissue (except for sodium and zinc). The evaluation of the analytical accuracy in the assessment and biological variability of the mineral composition of the fish muscles has shown that the values of both these components are comparable and should be taken into account in the development of new tables on the chemical composition of food products.

[Content of mineral substances in the internal organs of rats on intravenous feeding]. / Soderzhanie mineral'nykh veshchestv vo vnutrennikh organakh krys pri vnutrivennom pitanii.

The experiments on rats receiving a complete intravenous nutrition (group 1) during 15 days showed that the concentration of natrium, magnesium and iron was increased in the liver and decreased in the spleen as compared to that in controls given normal feeding (group 2). The content of zink and copper (mg%) was significantly lowered in both the organs of rats in group 1. The growth of the liver and spleen mass during parenteral feeding led to a significant rise in the content of natrium, potassium, magnesium, iron, zink and manganese in the whole liver tissue of group 1 rats, while the content of calcium and copper was similar in both groups of animals. The content of natrium, potassium, magnesium, iron and zink in the whole spleen tissue was significantly higher in group 1 rats, while the content of calcium, copper and manganese was similar in both groups of rats. A correlation was revealed between the content of iron and copper in the liver tissue (r = +0.87) and the levels of natrium and magnesium it the spleen tissue (r = +0.78) of group 1 rats. In group 2 rats a correlation was recorded between the content of calcium and manganese in the liver tissue an the levels of natrium and calcium in the spleen (r = +0.85 and +0.86, respectively).

[Dynamics of biometal distribution in breast milk]. / Dinamika raspredeleniia biometallov v grudnom moloke.

The results of 352 atomic-absorption measurements of the concentrations of 8 basic biometals in breast milk samples from women of different age were investigated by variation-statistical and correlative analysis. It was found that in all the cases the distribution patterns of biometals were asymmetric. K, Na, Fe and Mn were marked by logarithmic distributions, whereas Ca, Mg, Zn and Cu by power distributions with the index 1/2. That was determined most likely by the physicochemical nature of the mechanisms by which milk homeostasis was controlled. It was shown that in assumption about the normal distribution pattern, commonly accepted in practice, might lead to noticeable errors in quantitative assessments and to erroneous qualitative conclusions. The most probable concentrations of the metals and the width of their distribution showed alterations in time, dissimilar for different metals, including extremal alterations, with the concentrations of the test metals changing 1-5-fold and elementary relations up to 10-fold. For K-Na, Fe-Mn, Zn-Cu and Fe-Cu pairs the interelementary relations of the presumably biochemical nature were discovered, with the stability of those relations being dependent on the time of lactation. The data on variations in the balance of biometals can be used in the design of improved substitutes of breast milk and formula feeding adapted to babies of different age.