High-pressure NMR characterization of triacetyl-beta-cyclodextrin in supercritical carbon dioxide.

Cyclodextrins are used in many drug formulations since their cavities provide microenvironments where drug molecules can enter and form inclusion complexes for controlled drug delivery. Supercritical carbon dioxide (scCO(2)) is an alternative to organic solvents and a very attractive medium for the preparation of these inclusion complexes. The potential ability of triacetyl-beta-cyclodextrin (TA-beta-CD) to form inclusion complexes in addition to its high miscibility in liquid and scCO(2) could offer a chance for an economical and environmental friendly chemical processing. In this work, high-pressure NMR studies were performed in order to obtain information on the molecular structure and dynamics of TA-beta-CD in scCO(2) at 313.15 K and 20 MPa and its ability to form inclusion complexes under these conditions was studied. The influence of scCO(2) on a number of NMR spectral parameters, such as chemical shifts, spin-spin coupling constants, nuclear Overhauser effect (NOE) and spin-lattice relaxation (T(1)) has been studied. We unequivocally show for the first time structural changes of TA-beta-CD in scCO(2), like acetyl chain orientation and overall shape distortions that can affect its inclusion capability in this medium. The possibility of cavity self-closure is discussed and the results of two inclusion studies that support cavity self-closure, with the angiotensin-converting enzyme inhibitor, captopril, and the nonsteroid anti-inflammatory drug, flufenamic acid, are presented.

Structures of the chain metaphosphates NaM(PO3)3 (M = Ca or Sr).

Solid-state (23)Na and (31)P magic-angle spinning nuclear magnetic resonance spectroscopy and X-ray crystallography have been used to study the structures of the chain metaphosphates NaCa(PO(3))(3) and NaSr(PO(3))(3). The compounds are isostructural and crystallise in space group P(-1) with the following parameters: NaCa(PO(3))(3), a = 6.711 A, b = 6.934 A, c = 7.619 A, alpha = 83.44 degrees , beta = 81.41 degrees , gamma = 82.80 degrees ; NaSr(PO(3))(3)a = 6.805 A, b = 7.133 A, c = 7.720 A and alpha = 83.71 degrees , beta = 80.48 degrees , gamma = 82.87 degrees . Both structures contain anionic metaphosphate chains of (PO(3))(n) (n) with ionic contacts to Na(+) ions in distorted octahedral sites and Ca(2+) (or Sr(2+)) in distorted dodecahedral sites. (31)P and (23)Na NMR are entirely consistent with the crystallographic data and an empirical method for assigning (31)P resonances to particular crystallographically unique P atoms is described.

[Season and age related structure of acute intestinal infections morbidity in the Russian Federation].

AIM: To study seasonal and age features of etiological structure of acute intestinal infections (AII) in the territory of the RF. MATERIAL AND METHODS: A total of 7388 AII inpatients aged from 1 day to 90 years from 7 cities (Moscow, St-Petersburg, Nizhniy Novgorod, Chelyabinsk, Tyumen, Makhachkala and Khabarovsk) of the RF participated in a trial conducted from December 2001 to September 2006 The patients were examined with diagnostic tests based on polymerase chain reaction (PCR) for detection of rotaviruses of group A (RVA), noroviruses, astroviruses, adenoviruses, salmonella, termophilic campilobacteria, shigella and enteroinvasive Escherichia coli (EIEC). RESULTS: The above agents were detected in 72% children and 52% adults. In children RVA and noroviruses occurred most frequently (29.5% and 11%, respectively). The adults carried most often salmonella (9.3%), noroviruses (8.4%), RVA (7.8%) and Schigella in combination with EIEC (7.0%). CONCLUSION: Viral agents are essential or prevailing causative agents of AII at different ages. Seasonal and age-related trends of AII morbidity are characterized.

Synthesis and beta-lactamase inhibitory activity of new 6beta-cysteinesulfonamidopenicillanic acids.

New 6beta-cysteinesulfonamidopenicillanic acids and their sulfoxides were synthesized by sulfonylation of 6beta-aminopenicillanic acid or its (S)-sulfoxide with (R)-N-benzyloxycarbonylcysteinesulfonyl chloride ethyl ester (2a, 1b) and (R)-N-benzyloxycarbonylcysteinesulfonyl chloride benzyl ester (2a, 2b). The corresponding 6beta-cysteinesulfonamidopenicillanic acids sulfones 1c and 2c were prepared by oxidation of the sulfoxides 1b and 2b with potassium permanganate in aqueous medium. When combined with ampicillin some of the compounds reduced the minimal inhibitory concentrations of ampicillin against beta-lactamase producing strains.

[Reorganization of chromatin superstructure during marked changes in the rate of protein synthesis]. / Reorganizatsiia superstruktur khromatina v usloviiakh rezkikh kolebanii skorosti sinteza belkov.

The changes in the structure and RNA-polymerase activity of rat liver cell chromatin after a single injection of cycloheximide (3 mg/kg of body mass) were studied. The cycloheximide-induced fluctuations in protein synthesis rates are concomitant with episodes of drastic changes in the chromatin structure. The reorganization of the general protein structure is associated with an increase or a decrease of the RNA-polymerase II activity. The data obtained suggest that the activation-inactivation of RNA-polymerase II in cell nuclei is due to reorganization of chromatin infrastructures--from higher levels of the electron-dense chromatin package to the unfolded nucleosomes of the transcriptionally active protein.

[The effect of chondroitin sulfate preparations on wound healing and the strength of the surgical scar]. / Vliianie preparatov khondroitinsul'fata na zazhivlenie ran i prochnost' khirurgicheskogo rubtsa.

An experimental investigation of the ability of the chondroitinsulphate preparation produced from cattle tracheas, of rumalon and chonsuride to stimulate the regeneration of cutaneous coverings in case of their injury was carried out. A strength of the surgical cicatrix and its elongation at rupture in two weeks' injections of chondroitinsulphate increased in comparison with control. A stimulating effect of chondroitinsulphate to regeneration of flesh wound in case of local single action didn't differ essentially from the effect of chonsuride. In case of application of the preparations, an area of wound for the rats received chondroitinsulphate was already on the eighth day twice as less in comparison with the animals treated with chonsuride. Thus, a stimulating effect of chondroitinsulphate preparation to the regeneration of damaged cutaneous coverings by both parenteral and local administration was shown.

[Effect of blood plasma and serum and its fractions on the activity of the sodium channels in neuroblastoma cells]. / Vliianie plazmy, syvorotki krovi i ee fraktsii na aktivnost' natrievykh kanalov neiroblastomy.

Blood plasma, serum and its fractions containing components of different molecular masses obtained by dialysis and gradual ultrafiltration were tested for their action on the sodium currents of voltage clamped internally perfused neuroblastoma cells. Blood plasma free of platelet factor 4, serum and its fractions containing components of molecular masses more than 50 kD produced an increase in sodium channel currents and shifts in activation and inactivation curves along the voltage axis towards more negative or positive potentials, respectively. Moreover, the serum deficient in components with the molecular masses less than 50 kD produced a more prominent effect on all the parameters tested. Thus, the low-molecular fractions were suggested to exert an inhibitory activity on the stimulatory effects produced by the high-molecular components of the serum.

[Changes in the properties of the enzymes of energy allowance resulting from heat shock in lake frogs]. / Izmenenie svoistv fermentov énergoobespecheniia ozernykh liagushek v rezul'tate teplovogo shoka.

A study was made of the activity and heat resistance of preparations of Na, K-ATPase, Mg-ATPase and succinate dehydrogenase of the lake frog R. ridibunda caused by the heat shock of animals. A decrease in the activity and an increase in the heat resistance of all the three enzymes studied were observed. The level of individual correlations between these parameters remained unchanged. An increase in the heat resistance of Na, K-ATPase occurs at the expense of a higher threshold of its thermal inactivation without changes in the affinity of this enzyme to Na+ and K+. Under discussion is the question of the functional significance of the changes observed.

[Correlations of the individual levels of the activity and heat resistance of energy-support enzymes in the lake frog]. / Issledovanie korreliatsii individual'nykh urovnei aktivnosti i teploustoichivosti fermentov énergoobespecheniia ozernoi liagushki.

A study was made of the correlation between the levels of the activity and heat resistance of Na,K-ATPase, Mg-ATPase and succinate dehydrogenase (SDG) in Rana ridibunda. A correlation was observed between the activities of two ATPases, and between either of them and the activity of liver SDG. The correlation coefficient between the heat resistance levels was statistically significant only in SDG of liver and muscles. The question whether the criterion of T50% inactivation may be good for a comparative appraisal of the heat resistance of enzymes is under discussion.

[Properties of the enzymes of energy supply in the common frog under various physiological states. II. Changes in the heat resistance of adenosine triphosphatases and succinate dehydrogenase]. / Issledovanie svoistv fermentov énergoobespecheniia travianoi liagushki pri raznykh fiziologicheskikh sostoianiiakh organizma. II. Izmenenie teploustoichivosti adenozintrifosfataz i suktsinatdegidrogenazy.

The heat resistance of SDG, Na, K-ATPase and Mg-ATPase of the grass frog was determined in January, March and May, the number of animals examined being 30-40 in either experiment. It was found that the average level of the heat resistance of the enzymes studied shows significant, often differently directed changes, which depend on the physiological state of an organism. Negligible correlation between the thermal sensitivity of different enzymes of an organism during hibernation, completely disappear during the activity state.

[Properties of the energy-allowance enzymes of the common frog in different physiological body states. I. Adenosine triphosphatase and succinate dehydrogenase activities]. / Issledovanie svoistv fewrmentov énergoobespecheniia travianoi liagushki pri raznykh fiziologicheskikh sostoianiiakh organizma. I. Aktivnost' adenozintrifosfataz i suktsinatdegidrogenazy.

The activity of SDG, Na, K-ATPase and Mg-ATPase of the grass frog was determined in January, March and May, the number of animals examined being 30-40 in either series of experiments. In May (period of reproduction) the average activity of the above enzymes was higher than in January and March. This was observed both in males and females. A correlation between enzymatic activities of each single organism in March and May significantly increased. The role of these changes in the increase of viability of the organism is discussed.

[Dependence of Na, K-ATPase enzyme activity on the surface properties and charge of the substances interacting with the cell membrane]. / Zavisimost' fermentativnoi aktivnosti Na, K-ATFazy ot poverkhnostnykh svoistv i zariada vzaimodeistvuiushchikh s kletochnoi membranoi veshchestv.

The surface activity and effect of histone, sodium deoxycholate and Triton X-100 on N+,K+-ATPase have been compared. It has been found that the coefficient of surface tightness on the borderline of suspension of ATPase containing membranes/air decreases with the increase in concentrations of these agents. The enzyme activity undergoes biphasic modification increasing with lower and decreasing with higher concentrations of the agents. The effectiveness of the agents depends on the charge of their molecules. The mechanism of interaction between Na+,K+-ATPase and the above modifiers is discussed.

[Activity and thermal stability of the enzymes of energy support in the common frog]. / Izuchenie aktivnosti i teploustoichivosti nekotorykh fermentov energoobespecheniia travianoi liagushki.

The activity and heat resistance of succinate dehydrogenase (SDG), Na, K-ATPase and Mg-ATPase of the grass frog (39 specimens) have been determined. No correlation was found between individual levels of heat resistance both of either enzyme examined and of the same enzyme but taken from different tissues (SDG of liver and muscles). The average level of heat resistance of SDG in liver is significantly higher than that in m. gastrocnemius. A statistically significant correlation was observed between individual levels of enzyme activity in the internal organs (SDG of liver, Na, K-ATPase and Mg-ATPase of kidney). The activity of SDG of muscles does not correlate with that of either partner.

[Comparison of the heat resistance of ATP-hydrolyzing enzymes in 2 species of frogs]. / Sravnenie teploustoichivosti ATF-gidrolizuiushchikh fermentov u dvukh vidov liagushek.

A comparison was made between the heat resistance levels of two enzymatic preparations: the actomyosinic and the transport ATPases of two species of frogs (grass and lake frogs) differing in their thermophilia. The interspecies differences in the heat resistance were found to be 6 degrees C for the actomyosinic and 3 degrees C for the transport ATPase in favour of the more thermophilic lake frog. In both species the myosinic ATPase is more sensitive to heat than the transport one. The high heat resistance of the transport ATPase is due to a higher threshold of its sensitivity to temperature.

[Stimulatory effect of lactin combined with hyphotocin on galactopoiesis in rats]. / O stimuliruiushchem vliianii na galaktopoéz u krys laktina v sochetanii s gifototsinom.

Specific features of the effect of lactin and hyphotocin or their combinations on lactopoiesis were studied in experiments on female white rats being in the stage of fading lactation. In a morphological examination of the mammary gland it was discovered that changes characteristic of galactopoiesis increase under the influence of lactin are accompanied by milk delay in lactopoietic lobules. Hyphotocin that intensifies lactation increases milk secretion without inhibiting the physiological involution of the gland. Simultaneous injection of lactin and hyphotocin stimulates lactation and inhibits the morphological involution of the mammary gland.

[Localization of ubiquinone-9 in electron transport chain of Candida guilliermondii]. / Uchastie ubikhinona-9 v tsepi perenosa élektronov u Candida guilliermondii

The activity of ubiquinone-dependent enzyme systems was studied in mitochondrial fractions of the yeast Candida guilliermondii cultivated on the medium containing carbohydrates of hydrocarbons as a source of carbon. The activity of NADH2-oxidase and succinate-CoQ-reductase was higher in systems with mitochondrial fractions from the cells grown on the medium with n-paraffins than in mitochondrial fractions from the cells cultivated on the medium with glucose. About 30% of intracellular ubiquinone is located in the mitochondrial fraction of hydrocarbon oxidizing yeast cells; however, the activity of enzymes was stimulated upon introduction of exogeneous ubiquinones into the systems. Therefore, exogeneous ubiquinones may be involved in the electron transport chain during oxidation of reduced substrates. Both ubiquinone-dependent enzyme systems are resistant to storage.