[Biological activity and mechanisms of therapeutic action of rosmarinic acid, luteolin and its sulphated derivatives].

The review considers recent experimental studies of biological activity and mechanisms of therapeutic action of rosmarinic acid, luteolin and its sulfated derivatives in diseases associated with disorders of carbohydrate and lipid metabolism. Particular attention is focused on the results of studies showing a high therapeutic potential of these phenolic compounds in their prophylactic and therapeutic use at experimental modeling of type 2 diabetes and hyperlipidemia. Based on the analysis of our results and the literature data putative mechanisms of therapeutic action of rosmarinic acid, luteolin and its sulfated derivatives have been proposed.

[Study of Antioxidant and Membranotropic Activities of Quinazoline Alkaloid Tryptanthrin Using Different Model Systems].

A comparative study of antioxidant (radical-interceptor) properties of tryptanthrin (quinazoline alkaloid shows a high anti-inflammatory activity and it is found in many types of different families of higher plants and microorganisms, including the human microbiome) in the systems of 2,2'-azo-bis(2-methylpropionamidin)dihydrochloride-luminol and hemoglobin-hydrogen peroxide-luminol has been conducted and the influence on the permeability of planar bilayer lipid membranes is evaluated. Trolox was used as a reference antioxidant, and ascorbic acid and dihydroquercetin were taken as standards. Tryptanthrin exhibits very weak antioxidant activity, being markedly inferior to the reference standard and antioxidants while testing antioxidant activity in both studied systems. By the efficacy of antioxidative action the substrates in the systems studied can be arranged in the following order: dihydroquercetin > trolox > ascorbic acid > tryptanthrin. Antioxidant potential of tryptanthrin is approximately 1000 and 3000 times lower than that of trolox and bioflavonoid dihydroquercetine, respectively. Tryptanthrin causes no significant changes in the permeability of planar bilayer membranes in a dose range of 0.5 to. 10 µg/ml. Our data show that tryptanthrin displays no significant radical-interceptor and membranotropic activities. It can be assumed that the observed high anti-inflammatory activity of tryptanthrin is not related to the neutralizing effect against reactive oxygen species and the influence on the permeability of cell membranes. The anticipated mechanisms of biological activity of tryptanthrin are discussed.

[Antioxidative and membranotropic activities of rosmarinic acid].

The metabolic damages and inflammatory diseases are closely connected with high increase of the contents of the reactive oxygen species (ROS) and lipid peroxidation products in organism. In connection with this natural antioxidants are actively used for efficient fight with oxidative stress. In current work we have estimated an antioxidative potential of rosmarinic acid (RA), which is broadly wide-spread amongst plants and possesses the useful spectrum of biological activities. It has been shown that RA noticeably exceeded known antioxidants in test on antioxidant activities in Hb-H2O2-luminol and 2,2'-azo bis (2-methylpropionamidine) dihydrochloride-luminol systems, as well as on inhibition of linoleic acid peroxidation. On antioxidant activities the investigated substances can be arranged in the following order: RA > dihydroquercetin > trolox > ascorbic acid. RA molecules are localized mainly in the lipid bilayer of polar groups, but have no significant effect on its structural and functional properties: RA does not cause significant changes in permeability of planar bilayer membranes in a dose range of 0.5 to 10 microg/ml. Spontaneous incorporating of 1 mol% of RA into the lipid bilayer is sufficient for the complete prevention of lipid peroxidation. Thus, the antioxidant activity of RA is based on its ability to inhibit the initiation stage of free radical reactions of lipid peroxidation, largely caused by the formation of ROS. In this regard RA, as a powerful and effective inhibitor of ROS and lipid peroxidation, has great potential for wide use not only in medicine but also in the food industry to preserve the quality of perishable food products.

[The effects of preparation "Histochrome" in biochemical parameters of blood for patients with cardiopathologies].

The effects of the small doses of the preparation Gistochrome, containing natural polyhydroxynaphtoquinoine echinochrom A from flat sea urchin Scaphechinus mirabilis, on blood biochemical parameters have been studied in patients with cardiovascular diseases. Gistochrome administration influenced the LPO-antioxidant protection system, indicating reinforcement of antioxidant protection mechanisms. Gistochrome modulated the immune status and the plasma cytokine profile. Thus, Gistochrome may be recommended as means of additional therapy for patients with cardiovascular diseases for correcting the metabolic, immunological and redox impairments.

[Study of antioxidant and membrane activity of rosmarinic acid using different model systems].

Rosmarinic acid is found in many species of different families of higher plants and its chemical structure is phenol propanoid with various biological activity. In this paper, we conducted a comparative study of antioxidant (radical-scavenging) properties of rosmarinic acid in systems of 2,2'-azo-bis(2-methylpropionamidin)dihydrochloride-luminol and hemoglobin-hydrogen peroxide-lu- minol, determined its protective potential in preventing peroxidation of linoleic acid, and evaluated the effect on the permeability of planar bilayer lipid membranes. Linoleic acid peroxidation was assessed by iron-thiocyanate method. In these studies, trolox was used as a reference antioxidant, and ascorbic acid, and dihydroquercetin were taken as standards. Rosmarinic acid is significantly superior to trolox, ascorbic acid and dihydroquercetin in the tests for antioxidant activity in the systems studied, as well as in inhibition of linoleic acid peroxidation. According to their activity the investigated substances can be arranged in the following order: rosmarinic acid > dihydroquercetin trolox > ascorbic acid. Rosmarinic acid does not cause significant changes in the permeability of planar bilayer membranes in a dose range of 0.5 to 10 mkg/mL. Antioxidant activity of rosmarinic acid is due to the neutralization of reactive oxygen species and/or luminol radicals generated in model systems. The observed features of the antioxidant and membrane activity of rosmarinic acid, which may underlie the previously mentioned pharmacological effects are discussed.

[Pharmacological activity echinochrome A singly and consisting of BAA "Timarin"].

Pharmacological activity of echinochrome A (EchA) alone and in the biologically active additives (BAA) "Timarin", administered per os has been investigated on volunteers. EchA decreased serum glutatione (GSH) and increased catalase activity 1 h after treatment; catalase activity normalized, while GSH exceeded the initial level 3 h after the treatment. Changes in serum lipid spectrum, demonstrating reduction of the risk atherogenesis were determined.

[Enhancing the immunogenic activity of influvac vaccine in the use of adjuvant TI complexes modified by echinochrome A].

The self-assembly of marine macrophyte glycolipids, holothurian saponin, and cholesterol gave rise to nanoscale morphological structures called tubular immunostimulating (TI) complexes. Whether the latter could be used on the basis of vaccine preparations containing the influenza virus subunit antigens was studied. There was an obvious increase in the immunogenicity of influenza virus hemagglutinin when the experimental animals were immunized with this antigen as part of TI complexes. It was shown that the adjuvant activity of the TI complex to influenza virus hemagglutinin could be enhanced by adding the known antioxidant echinochrome A from a sand-dollar (Echinarachnius parma) to the matrix of the TI complex.

[Particularities of corrective action of polar lipids and bioantioxidants from sea hydrobionts at imbalances of lipid and carbohydrate metabolism].

A total mixture of phospho- and glycolipids from sea macrophytes Sargassum pallidum, Ulva fenestrata, Zostera marina was separated and the fatty acid composition was determined. Biological activity of the mixtures of polar lipids and natural antioxidants echinochrome A from flat sea urchin Scaphechinus mirabilis and polyphenolic complex from sea grass Zostera marina was studied in rats with experimental model of atherosclerosis and diabetes. These experiments revealed optimal compositions for mixtures of polar lipids and antioxidants, which possess high medical-corrective activity. Proposed mechanisms of action of the polar lipids (containing different polyunsaturated fatty acids) and antioxidants studied are presented. These compositions may be used for creation of new biologically-active additives and drugs.

[The comparative study of the medical action of lyuteolin, rosmarinic acid and echinochrom A at experimental stress-induced cardiopathology].

The method of the physical load in condition of the coronary circulation of the blood disturbance, caused mesaton injection, induced development rat cardiopathology, bring about of the heart function decompensation and 40% death of experimenthal animals. Under electronic-microscopic study of rat cardiomyocytes are discovered signs to disorganizations of mitochondrial apparatus of these cells. Administration to therapeutic mode of luteolin and echinochrome A preparations has provided to 100% animal probability of survival. At the same time, mitochondrial apparatus of cardiomyocytes was characterized by the normal parameter i.e. given preparations have provided of defensive adative effect at cardiomyocytes level. Similar activities for rosmarinic acid have not shown. Study some metabolic parameter and endocrine status animal has also allowed revealing of therapeutic effect of luteolin and echinochrome A. Findings be evidence of that echinochrome A and luteolin capable to play the important positive role in metabolism of cardiomyocytes by stimulating of mitochondrial biogenesis and by changing of adaptative mechanisms of the organism cardiovascular system protection.