Effect of the type of N-substituent in the benzo-18-azacrown-6 compound on copper(II) chelation: complexation, radiolabeling, stability in vitro, and biodistribution in vivo.

In this work, we synthesized two new benzo-18-azacrown-6 ethers bearing picolinate and pyridine pendant arms and studied the copper complexes of these ligands, as well as those of an acetate analog. All considered ligands were capable of forming mono- and dinuclear complexes due to their large size and large number of donor sites. Among all forms of complexes, the coordination of cations inside the macrocycle has only been shown for the mononuclear form of the acetate complex, while out-cage coordination has been observed for other forms. Electrochemical studies have shown the instability of the mononuclear form of the complex with the pyridine ligand to the reduction in the range of redox potentials of bioreductants. The stabilities of labeled acetate complexes with "in-cage" coordination of the cation and picolinate with "out-cage" coordination were compared in an excess of serum and superoxide dismutase; while the former turned out to be unstable to transchelation, the latter was stable throughout the experiment. Additional studies in biologically relevant media were performed for the picolinate complex and demonstrated its stability in vitro. The biodistribution of this complex in mice after 6 hours post-injection demonstrates a slow excretion from the body; however, the accumulation is noticeably lower than that of free copper cations.

[The comparative analysis of the parameters used for diagnostics of lowering mineralization of osteous tissue].

With the purpose of a choice of optimal biochemical parameters for individual diagnostics of bone tissue mineralization disturbances bone mineral density (T-criterion), a blood serum level of the transport form of vitamin D (25-OH D), osteocalcin and calcitonin, and also calcium daily urine excretion and calcium excretion in morning urinary portion per creatinin has been determined. The most informative parameters have appeared T-criterion, blood serum level of 25-OH D3) or osteocalcin due their interchangeability, and also calcium urine excretion per creatinin.

[Vitamin and mineral supply of patients with cardiovascular diseases].

Analysis of dietary intake for the month before admission using the food frequency method in patients with cardiovascular diseases (CVD) showed high level consumption of vitamin C, excessive consumption of phosphorus and deficiency in consumption of vitamins A, B1, B2. 82% of patients had low calcium excretion per 1 kg of body mass, 16% of people had high level of bone resorption. In the group of patients with low calcium consumption, content of all the vitamins in daily ration was significantly lower, than that in the group with adequate calcium consumption. High spread of osteopenia among patients with CVD was expected because of deficiency in calcium consumption and their lowe supply with vitamin D, that appears risk factors of osteoporosis. But, actually, only 10% of patients had osteopenia and only 2 from 132 osteoporosis. Knowing that 95% of patients were overweighted, we suppose that low spread of osteopenia may be caused by estrogen-producing ability of fatty tissue.

[Energy expenditures in patients with insulin-dependent diabetes mellitus in a hospital and ambulatory environment (computer analysis)]. / Energotraty u bol'nykh insulinzavisimym sakharnym diabetom v statsionarnykh i ambulatornykh usloviiakh (komp'iuternyi analiz).

Original computer programs for assessment of energetic value of nutrition and daily energy expenditures of man based on physical activity protocols have been developed. The programs were tried in 16 patients with insulin-dependent diabetes, and essential individual differences from tentative table estimations of energy expenditures were detected. Correlations between treatment efficacy and individual energy expenditures of patients were observed; a moderate deficit of nutrition calories was found more detrimental for metabolic control than their moderate excess. The regularities detected even in such a nonrepresentative sample permit us evaluate high the potentialities and significance of the suggested method for assessment of energy expenditures.

[Nutrition factor in the treatment and prevention of ischemic heart disease under ambulatory care]. / Faktor pitaniia v lechenii i profilaktike IBS pri dispansernom nabliudenii.

Study of the influence of a long-term staged use of diet therapy during prophylactic medical observation of post-myocardial infarction patients has shown that the anti-sclerosis diet used under clinical conditions was effective for relieving the angina pectoris syndrome and obtaining favourable dynamic changes in a number of metabolic parameters. Among the out-patients the diet was used by only 76 per cent. A comparative study of the results of diet therapy during the 3-year medical observation has shown a clear tendency to a gradual reduction of hyperlipoproteinemia and excessive body weight in patients who adhered to the diet. The parameters under study in the group of patients who violated the diet returned to the original level. The incidence of recurrent myocardial infarctions in patients on a diet was twice as low as in those who violated it. Prolonged diet therapy considerably improved parameters of IHD patients' working capacity. A special model has been elaborated for adequate use of the nutritional factor at all stages of the rehabilitation program.

[High density lipoprotein cholesterol and iodine-accumulating function of thyroid gland in patients with alimentary obesity as well as patients with ischemic heart disease with excessive body mass]. / Kholesterin lipoproteidov vysokoi plotnosti i iodnakopitel'naia funktsiia shchitovidnoi zhelezy u bol'nykh alimentarnym ozhireniem i ishemicheskoi bolezn'iu serdtsa s izbytochnoi massoi tela.

Accumulation of 131I was decreased in patients with heart ischemic disease and excessive body mass whereas this decrease occurred more seldom in patients with metabolic-alimenatary obesity. Increase in the ratio of alpha-cholesterol/cholesterol in blood serum was more typical for the patients with heart ischemic disease as compared with corpulent patients. Deterioration of iodine-accumulating function of thyroid gland in the ischemic disease was accompanied by decrease in content of cholesterol as well as by increase of alpha-cholesterol. These alterations were not found in the patients with obesity. In the decrease of iodine-accumulating function of thyroid gland contents of cholesterol and alpha-cholesterol were dissimilarly altered in the patients with excessive body mass and heart ischemic disease as well as in the patients with metabolic-alimentary obesity.

[Effect of a reducing diet on metabolic disorders in ischemic heart disease patients having excess weight]. / Vliianie redutsirovannoi diety na nekotorye metabolicheskie narusheniia u bol'nykh ishemicheskoi bolezn'iu serdtsa, imeiushchikh izbytochnuiu massu.

The paper concerns the effect of the diet with a strongly reduced content of carbohydrates, with a restriction of table salt and extractive substances on lipid and carbohydrate metabolism, on catecholamine secretion and exocrine pancreatic function in patients with ischemic heart disease accompanied by overweight and disturbed carbohydrate tolerance. Dietetics has a normalizing action on the body overweight, lipid composition and lipoproteid spectrum, as well as on the enhanced activity of serum trypsin. Moreover, it makes the blood content of immunoreactive insulin return partially to normal.