EUROMEDICA  Hanover 29-30  Mai 2006	Advanced methods of diagnosis, treatment and prophylactics
	European Academy of Natural Sciences, Hanover European Scientific Society, Hanover Russian Academy of Natural Sciences, Moscow

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In 1981, selenopyran, an organic selenium compound with selenium mass percent amounting to 24 (C19H22Se, 9-phenyl-symmetrical octa-hydroselenoxanthene) was produced as a result of the research directed by Professor A.F. Blinokhvatov. The scientist neutralized the compound toxicity by binding a selenium atom to the heterocyclic ring. Trials on chicken showed a 77-time toxicity decrease as against that of sodium selenite, and a 490-time decrease in the trials on white mice (LD50 – 1600 mg per 1 kg body mass). Being soluble in oils and spirit, selenopyran is insoluble in water due to which has a longer retention time, thus, serving as a kind of “selenium depot” in the organism.

Selenopyran proved to reduce the intensity of methyl oleate oxidization which became apparent in the decrease of fatty acid peroxides. Selenopyran demonstrated its advantageous properties as an antioxidant compared to buthyhydoxytoulene (BHT) and tocopherol. Selenopyran which was either introduced intramuscularly or supplemented to the diets of the laboratory animals (chicken, calves, piglets, lambs, and Wistar’s rats) under oxidative stress, provided a decrease in levels of diene conjugates and malonic dialdehydes in blood, liver, myocardium, aorta and tunica mucosa of small intestines. Selenopyran introduced (per os) to a combination vitamin enrichment therapy in patients with coronary heart disease and myocardial infarctions was found to reduce plasma and erythrocyte levels of malonic dialdehyde.

Selenopyran is supposed to be absorbed with fats in the intestines and transferred as a constituent part of lipoproteins. Selenopyran is further metabolized in the cytochrome-450 monooxygenase system, at the same time the number and catalytic activity of monooxygenases having molecular weights of about 49 000 D are found to increase. Later on, upon opening of the covalent bond, the reduced tetravalent selenium is released. The selenopyran metabolites appear to conjugate with proteins, thus, stimulating the immune response. The reduced selenium is involved in formation of glutathione peroxidase and other selenoproteins. Selenopyran is a double-action antioxidant. It was found that upon an increase of peroxide concentration in a system (in vitro), selenopyran gets recycled forming a carbocyclic compound (β-cycloketol) and eliminating a heteroatom. Thus, an increase of peroxide level in vitro and in vivo systems initiates both activation of a system and a prompt supply of selenium essential for stimulation of antioxidative enzymes. Therefore, we define selenopyran as a self-contained antioxidant and “emergency-call selenium”.

During a further study of the preparation a selenopyran-related dose-dependent decrease of intracellular cholesterol level was registered both in human macrophage and aorta intimae unstriped muscle cell cultures pretreated with the atheriogenic plasma. The antiatherogenic effect of selenopyran was proved both by experimental studies and clinical trials. Introduction of selenopyran in rats’ special atherogenic diet, caused a reduction of total

and β-cholesterol levels and an increase of α-cholesterol levels. The antiatherogenic effect of selenopyran was demonstrated by histological examinations. A reliable inhibition of atherogenic changes was indicated in aorta. Similar results were obtained in two clinical placebo-controlled trials of selenopyran-containing preparations introduced to myocardial infarction and coronary heart disease patients.

In summary, the range of application of selenopyran in clinical and dietary nutrition in Russia is to a considerable degree determined by its chemical and biological properties. Due to supplementation of oils rich in polyunsaturated fatty acids with selenopyran the food is found to acquire both stabilizing and antiatherogenic properties. Selenopyran combined with vitamin and microelement complexes available either in the form of tablets or in food substances adds immunostimulating and antioxidative effects to their properties