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We analyzed changes in activities of enzymes of phases I and II of xenobiotic biotransformation and parameters of NO metabolism in liver microsomes of rats with toxic CCl

It is established that arabinogalactan and pectinaceous polysaccharides isolated from Ferula kuchistanica are capable of stimulating a primary immune response in mice by increasing the number of antibody-producing cells in the spleen in response to immunization with sheep red blood cells in both intact animals (on average by 51.0%; p0.005) and those with secondary immunodeficiency caused by irradiation (on average by 164.4%; p0.005). The treatment with compounds studied also significantly increased the functional condition of cells of the mononuclear phagocyte system (on average by 27.0%; p0.005).

Significant muscle loading in elite athletes result in considerable changes in their physiological and immune status. There can be variations in the concentrations of serum IgM, IgG and IgA – from significant decrease to elevation, reduction of total serum IgE, an increase in the level of proinflammatory cytokines, etc. (5, 13, 10). Therefore, health status monitoring is of great importance, especially in the diagnosis of diseases. The intense training of an athlete can cause a negative influence on the immune state, raise susceptibility to bacterial and viral infections, induce functional disorders of the hepatobiliary system. Intestinal parasitic diseases (IPD) induce such changes (4, 6). Their timely diagnosis and adequate therapy are of peculiar importance in regions endemic with IPD. Uzbekistan belongs to such a region (1).Object of the study: To characterize the prevalence of intestinal parasites in junior wrestlers with an estimation of clinical manifestations, detect immunological shifts a...

It was established that steroidal genins and their glycosides of the spirostan series and (especially) furostan series show anticestodal activity against Hymeiolepis nana species. Search for anthelminthic agents in the indicated series of compounds is a promising direction of research.

Introduction of phytoecdysteroids (ecdysterone, turkesterone and ñyasterone) to rats subjected to prolonged immobilization stress significantly decreased involution of the thymus and spleen, contributed to normalization of increased mass of adrenal glands, and restored their content of ascorbic acid and cholesterol. In the liver of stressed animals, phytoecdysteroids prevented sharp decrease in the glycogen concentration, showed a clear trend toward normalization of the ratio of lactic and pyruvic acids, maintained homeostasis of macroergic phosphorus compounds, and increased the activity of antioxidant enzymes that inhibit lipid peroxidation. With respect to the stress-protective activity, the studied phytoecdysteroids are in some cases superior to eleutherococcus extract.

The efficacy of albendazole (400 mg taken once), mebendazole (100 mg taken once), and metronidazole (0.5 g thrice daily for 7 days) was evaluated when treating ascariasis, enterobiosis, and blastocystosis, respectively, in patients with HIV infection and in those with pulmonary tuberculosis. Metronidazole-resistant lambliasis was treated with exdisten (5 mg four times for 10 days) in 30.4% of the patients with HIV infection and in 43.3% of those with tuberculosis. Most HIV infected patients received antiretroviral therapy (ARVT). All the tuberculosis patients took isoniazid, ethambutol, pyrazinamide, rifampicin, and streptomycin. Efficiency was monitored by triple coproscopy at an interval of 5-7 days and by additional examinations using the method of Ritchii et al. There was parasitological cure (decreased infection rate for blastocystosis) and clinical improvement as positive changes in symptoms, such as nausea, weakness, headache, weight loss, and others, in all the patients with concomitant ascariasis, enterobiosis, and lambliasis. ARVT and antituberculosis drugs were observed to be better tolerated in all cases.

The technological isolation of turkesterone from the epigeal part ofAjuga turkestanica (Rgl.) Brig. is described, a method is proposed for the quantitative determination of turkesterone, and the results of an investigation of its biological activity are given.

Galactomannan, a nontoxic compound that exhibits in experiments with intact rats a slight hypocholesterinemic and hypoglycemic activity, was isolated from the coating of Gleditsia macracantha seeds. It prevents significantly the development of experimental hyperglycemia and diabetes when administered simultaneously with alloxan.

A series of phytoecodysteroids, including alpha-ecdysone, 2-deoxy-alpha-ecdysone, and 2-deoxyecdysterone isolated from Silene praemixta, integristerone A and ecdysterone isolated from Rhaponticum carthamoides and 22-acetylcyasterone and turkesterone isolated from Ajuga turkestanica, exhibit a pronounced hypoglycemic effect in experiments on intact male rats. The most active compounds--ecdysteron and turkesterone--also produce an expressed hypoglycemic effect in animals with model hyperglycemia induced by the administration of glucose, adrenalin and alloxan. Phytoecdysteroids are substances possessing protein-anabolic activity and are somewhat similar to steranobols in this aspect. Phytoecdysteroids exhibit unidirectional effect and are well comparable with steranabol actionon the carbohydrate metabolism.

The introduction of polyprenols isolated from fir (Abies) tree in male rats weighing 170 - 180 g with alcohol-induced hepatitis favored reduction in hepatocyte cytolysis and cholestasis and led to an improvement of the protein- and glycogen-synthesizing function of liver. A clear tendency to normalization of the maintenance of total lipids, triglycerides and phospholipids and the inhibition of lipid peroxidization processes in the damaged organ was observed. The introduction of Abies polyprenols also improved the process of bile secretion and its chemical composition.

Ecdisten, the drug designed on the basis of the phytoecdisteroid ecdisterone isolated from Rhaponticum carthamoides, was used in the treatment of first diagnosed (primary) and persistent (resistant to traditional lambliacides) lambliasis. A control group received metronidazole. Daily parasitological monitoring of lamblia elimination while treating with ecdisten in a daily dose of 20 mg for 10 days indicated the absence of lamblia in 70% of the patients with primary lambliasis on days 3 to 5; in the remaining 30%, parasitic elimination was accomplished on days 6-7 of treatment. In the patients with persistent lambliasis, the parasites were eliminated in 43.2% of cases on days 4-5 and in 56.6% on days 6-10. Metronidazole just on the second day of therapy caused parasitic elimination in 28.6% of the patients. All the patients were freed from lamblia within 5 days. Improvement occurred more rapidly with ecdisten treatment; immunological normalization was seen when ecdisten was used. Seven-ten-day course of ecdisten is sufficient for the treatment of primary lambliasis; when persistent lambliasis is treated, its course should be prolonged. If required, the course may be repeated, by increasing the daily dose.

Influence of phytoecdysteroids (isolated from Ajuga turkestanica) and bemithyl on the duration of swimming of laboratory animals (mice, rats) under various experimental conditions was studied. Turkesteron and cyasteron increased duration of dynamic work carried out by animals, decreased fatigue, and accelerated recovery processes to a greater extent that did bemithyl. The positive influence of phytoecdysteroids on the working capacity is based on the activation of metabolic processes in skeletal muscles, directed to support the homeostasis of energy production. Phytoecdysteroids also accelerate recovery of immune reactions which are decreased due to the exhausting physical work.

Intramuscular injection of an oil solution of tefestrol, as well as the oral administration of tefestrol tablets and the parenteral administration of sinestron in doses of 0.01, 0.1, 1, and 5 mg/kg led to a pronounced estrogen effect in both nonpubertate and pubertate (intact and ovariectomized) rats. In the minimum dose, the estrogen activity of the injection preparation exceeded that of tablets. Preliminary tefestrol injections accelerated the fertilization and pregnancy. The injection form has a shorter latent period and produces a longer estrogen effect, while not violating fetus implantation, producing no toxic action, and having no negative influence on the pregnancy terms and the development of fetus.

The properties of ecdysten, an exdysterone-based preparation, were studied under experimental (of heliotrine induced hepatitis model in rats) and clinical (chronic viral hepatitis B) conditions. A 2-week treatment with ecdysten in a daily dose of 5 mg/kg (p.o.) significantly improved the state of rat liver, as manifested by normalization of the enzymatic activity of blood serum, stimulation of the protein and glycogen synthesis, inhibition of lipid peroxidation, and activation of all chains of microsomal oxidation of hepatocytes. The inclusion of ecdysten into a complex therapy scheme for patients with chronic viral hepatitis B (5-mg tablets twice per day over a period of 30 days) substantially improved the clinical and biochemical indices of the functional state of liver, positively influenced the humoral and cell immunity and the resistance factors, and normalized the course of autoimmune processes accompanying the liver pathology.

The sum of bufadienolides (bacagin) isolated from the poison of Bufo viridis toad occurring in Central Asia produces a selective strophanthin-K-like action upon the heart function, increasing myocardial contractility, retarding cardiac rhythm, and positively influencing the parameters of myocardial metabolism. The mechanism of realization of the positive ionotropic effect of bacagin is probably related to the ability of increasing the basal level of cytosol calcium at the expense of inhibiting the activity of Na+/K(+)-ATPase and, to some extent, Ca(2+)-ATPase in endoplasmic reticulum.

The drug ecdisten as tablets is the natural compound ecdisteron was extracted from Rhaponticum carthamoides (Willd.) Jljin. Ecdisten was tested in the treatment of 32 and 3 patients with persistent and acute giardiasis, respectively. A ten-day course of ecdisten, 5 mg 3 or 4 times a day, resulted in a clinical and parasitological recovery in 22 (68.7%) and 3 patients, respectively. After the reuse of a ecdisten course in 4 patients with persistent giardiasis wherein its initial dose was increased, recovery was achieved in 3 cases, the efficacy of the agent was 78.1%. Ecdisten should be used to treat giardiasis, in its chronic pattern or resistance to conventional giardicial agents.

Phytoecdysteroids ecdysteron and turkesteron isolated from Ajuga turkestanica (Rgl.) Brig. decrease the manifestations of uremic intoxication in rats with experimental renal pathology induced by a nephrotoxic mixture (containing uranyl acetate and glycerol). Injected in a dose of 5 mg/kg, the drugs restore glomerular filtration level, favor the disappearance of the albuminuria and normalize urinary sediments. The nephroprotector effect of the phytoecdysteroids studied resembles the action of a steroidal anabolic drug nerobol.

The effects of ecdysterone and the related drug ecdysten on the sexual activity were studied under experimental and clinical conditions. A 10-day administration of ecdysterone (5 and 10 mg/kg, p.o.) improved behavioral characteristics of the sexual function in rats, the effect being especially pronounced during the fist days of experiment. The administration of ecdysten to men with the infertility diagnosis (disturbed spermatogenesis as a complication of some urologic diseases) increased the copulative function and improved the sperm quality. The administration of ecdysten to patients in the stage of recovery upon myocardial infarction also improved the sexual function.

Phytoecdysteroids alpha-ecdysone, 2-desoxyecdysterone, ecdysterone, sileneoside A, and turkesterone isolated from Rhaponticum carthamoides (Willd.) IIjin, Silene brahuica Boiss and Ajuga turkestanica (Rgl.) Repeated administration of brig increased the content of erythrocytes and hemoglobin in the blood of intact rats. The most active of them--ecdysterone, sileneoside A, and, particularly turkesterone, cause also a marked effect on red blood regeneration in hemotoxic phenylhydrazine anemia. In its capacity for simulating erythropoiesis turkesterone resembles the well-known steroidal anabolic drug nerobol.

Administration of cycloartane (askendoside D-10 mg/kg, cyclosiversioside F-25 mg/kg) and heart glycosides (strophanthin K-0.36 mg/kg, celanide-1 mg/kg) for 3-10 days is found to exert unidirectional effect on the indices of carbon, lipid and adenine nucleotide metabolism in animal myocardium under study. Glycogen and ATP content increases under parallel decrease of lactate and nonesterified fatty acid content. Differences in the effect of cycloorthane and heart glycosides and especially on the indices of myocardial carbon metabolism were registered under more prolonged administration. Administration of heart glycosides in contrast to cycloorthane ones promotes a decrease of glycogen level and redox potential and increase of lactate content.

Phytoecdysteroids: ecdysterone and turkesterone, introduced orally to male rats with the body mass 180-120 g in a dose of 5 mg/l kg of mass and nerobol in a dose of 10 mg per 1 kg of the mass for 15 days against a background of the developed alloxan diabetes cause a considerable decrease in the content of free fatty acids of the blood serum, sharply increased after the subcutaneous injection of alloxan to the animals (150 mg per 1 kg of the mass). The content of glycogen, malonic dialdehyde, pyruvic acid and calcium transporting function of the liver mitochondria are also normalized. These changes are closely interrelated (and may be mutually conditioned) with the preparation-induced reduction of phospholipid spectrum of the liver mitochondrial membranes pathologically changed owing to insulin insufficiency. In this case phytoecdysteroids in the first turn normalize the fractions of phospholipids which play the structural role in the mitochondrial membranes, and nerobol normalizes the level of minor and monoacylic phospholipids.

The phytoecdisteroids ecdisterone, turkesterone and cyasterone were administered in a dose of 5 mg/kg per os to rats with hepatitis induced by subcutaneous injections of CCl4. Similarly to the anabolic drug nerobol (10 mg/kg), the above agents not only interfere with the manifestation of the hepatic action of CCl4 (in this case the effect of the phytoecdisteroids is more remarkable) but also favour a more rapid normalization, as compared to the control, of functional and metabolic disorders in the liver. The phytoecdisteroids and nerobol noticeably stimulate the recovery of bile secretion, the synthesis of bilirubin and bile acids, cholesterol excretion.

Peroral administration of salvipholin in a dose of 50 mg/kg to intact male rats (the body weight 180-220 g) had a positive effect on the carbohydrate-lipid metabolism in the liver and blood serum of animals. Administration of the same dose to rats with alloxan diabetes induced a significant decrease in the content of glucose, free fat acids, triglycerides and lysophospholipids of the liver and blood serum. The level of these components has sharply increased after subcutaneous alloxan administration in a dose of 150 mg/kg, the content of glycogen and pyruvic acid being normalized and insulin deficiency removed. These changes are closely related to salvipholin-promoted restoration of phospholipid spectra of the blood serum and liver of experimental animals disturbed under conditions of insulin deficiency. The possible mechanism of the salvipholin action is analyzed.

Biocyclic diterpenoids--salvin, salvicin and salvifolin, administered per os to rats at a dose of 50 mg/kg show marked hypoglycemic activity in intact animals as well as in animals with experimental hyperglycemia developing against a background of GTT (3000 mg/kg intraperitoneally) or alloxan (150 mg/kg subcutaneously). They are superior to adebit but inferior to maninil. Prophylactic and therapeutic administration of these compounds ensure the preservation of islet beta-cells in animals with alloxan diabetes.

Studies into the effects of metandrostenolone and ecdisterone, anabolic steroids of different classes, on the content of hormones in blood plasma made it possible to establish that metandrostenolone produces appreciable changes in the hormonal background: a short-term increase in the content of corticosterone but a decline in the concentration of somatotropic hormone (STH). The long-term administration of metandrostenolone brings about a reduction of the content of testosterone. Unlike metandrostenolone, ecidsterone provoked but an increase in the content of corticosterone both on single and long-term administration. It is concluded that the rise of the content of corticosteroids in blood plasma under the influence of the tested drugs may be a factor favoring mobilization of biochemical processes in skeletal muscles in response to physical exercise. Meanwhile the change in the corticosterone:testosterone:STH ratio in blood may cause side effects due to the long-term use of metandrostenolone and other anabolic derivatives of androgens.

Administration of galbanic acid isolated from the roots of Ferula kopetdaghensis Eug. Kor. to rats orally in a dose of 50 mg/kg was found to improve the course of toxic hepatitis induced by fourfold subcutaneous injections of a 50% oil solution of CCl4. Galbanic acid produced much more earlier than in control normalization of the activity of the enzymes alanine- and aspartataminotransferase in blood serum, increased glycogen content and improved the parameters of the redox potential of lactic acid-pyruvic acid system in the liver. Galbanic acid exerted the antioxidant effect. In the animals with a developed hepatitis receiving galbanic acid there was a more rapid restoration of intensity of bile secretion, synthesis of bile acids and bilirubin, cholesterol excretion as compared with control.

The natural lignin of kenaf stems and fractions of the dioxane lignin of kenaf stems isolated previously were cleaved by sodium in liquid ammonia in order to study their structure. It was established that the kenaf lignins consist of three types of structural units: p-coumaryl, guaiacyl, and syringyl, with a predominance of the guaiacyl types. An antioxidation activity of the monomeric products of the degradation of the kenaf lignins has been found.

In experiments with white mice it has been established that phytoecdisteroides turkesteron, ecdisteron and 2-desoxy-alpha-ecdison in the dose of 5 mg on 1 kg of body mass stimulate the protein synthesis. Using the model of protein synthesis from mice liver it has been shown that the action of phytoecdisteroides is connected with the rise of poliribosome functional activity and rate increase of protein macromolecules formation. Preliminary administration of actinomycin D does not prevent the effect of protein synthesis stimulation. It has been concluded that the anabolic effect of phytoecdisteroides in mammals organism is connected not with induction of RNA synthesis but with the acceleration of translocation processes.

Phytoecdysteroids from Rhaponticum carthemoides (Willd) Iljin and Ajuga turkestanica (Rgl.) Brig in a dose of 5 mg/kg per os markedly stimulate the bile secretion in normal rats treated with single (cyasterone) and 7-day-long (ecdysterone, cyasterone) administration. The chemical composition of the bile is significantly improved because of increased levels of bile acids and bilirubin and a decreased cholesterol content. Phytoecdysteroids (ecdysterone) exert more beneficial effect on the parameters under study in rats with toxic hepatitis induced by heliotrine.

The results of the comparative study on the myotropic activity of methandrostenolone and ecdysterone and their effects on physical endurance of animals suggested that ecdysterone possessing a wider spectrum of the anabolic action on the contractile proteins of the skeletal muscles exerts a more pronounced influence on physical endurance of animals without their preliminary training.

After administration of phytoecdisteroids (ecdisterone, turkesterone) at a dose of 5 mg/kg and the anabolic steroid preparation nerobol at a dose of 10 mg/kg into rats with experimental hepatitis caused by CCl4 poisoning, positive alterations were found in activity of the polyenzymatic systems in membranes of liver mitochondria simultaneously with an increase in their stability and resistance to the effect of exogenous factors producing the mitochondria degradation (controlled heating, treatment with phospholipase A2 or trypsin). These alterations, which appear to occur due to development of strong binds between phospholipids and proteins of inner mitochondrial membrane, promoted normalization of the respiratory chain and the outer pathway of electron transport in hepatocytes of rats with hepatitis.

Oral ratibol (10 mg/kg) produced in rabbits a decrease of blood coagulability (increased the time of thromboelastogram reaction, reduced the activity of prothrombin complex according to Quick, tolerance to heparin and activity of factors II, VII, XIII and concentration of factor I). The drug administration (1 mg/kg) for 20 days caused at the first stage a decrease and at the second stage an increase of blood coagulability. At a single and 20-day administration ratibol enhanced the fibrinolytic activity, reduced the resistance of fibrin clot to streptokinase and increased the antithrombin activity.

Introduction of phytiexdizone-exdisterone (0.5 mg/100 g) to rats for 7 days is shown to be attended by an accelerated body weight gain and also by a rising weight of the liver, heart, kidneys and musculus tibialis anterior. In these organs the total amount of protein increases. All of the above-stated changes are more marked when the substance is given to growing rats (70--80 g). In experiments on castrated sexually immature rats the androgenic action of exdisterone, unlike that of methandrostenolone, is not demonstrable.

It is shown that 6-ketoderivatives of natural sapogenins, viz. agigenin, diosgenin and alliogenin, display the anabolic activity and do not manifest any androgenic properties. The compoud IV/(25 R)-5alpha-spirostan-2alpha, 3beta, 5alpha-triol-6-OH/produces an accelerated gain of weight in rats, and also an increase in the weight of the liver, heart, kidneys, musculus tibiliasis anterior and augments the total amount of protein therein. All of the above-mentioned changes become more pronounced with the study substance introduced to young animals. Castration of sexually immature rats greatly mitigates the anabolic effect of the compound IV.

The effect of substances with anabolic activity (metandienone and ecdysterone phytoecdysteroid) on the manifestation of insulin effects was studied on a model of insulin resistance in rats induced by injections of hydrocortisone or by insulin insufficiency caused by alloxan. The sensitivity of the body to i. v. infusion of insulin and the reactivity of isolated fatty tissue to the hormone were increased after administration of these substances to test animals. The above effects of steroids were determined by nonspecific synthesis of total proteins in cells rather than by an increase in insulin secretion.

Administration of phytoecdisteroides ecdisterone and turkesterone in the dose of 5 mg/kg and anabolic steroid preparation nerobol in the dose 10 mg/kg in rats with experimental diabetes removes the activation of respiration under all metabolic conditions of rats liver mitochondria revealing at given pathology. The normalized effect of phytoecdisteroides on the cells energetic processes is observed on the 7th day of the administration. The same effect of nerobol is revealed at more prolonged (15 days) administration.

Oxidative phosphorylation and Ca2+-transport functions of liver mitochondria were normalized in rats with alloxane diabetes after peroral administration of phytoecdisteroids - ecdisterone and turkesterone (5 mg/kg) or nerobol (10 mg/kg) within 15 days. These drugs normalized the activity of NADH dehydrogenase and succinate dehydrogenase in respiratory chain of mitochondria, increased distinctly stability of the enzymes to the effect of such factors as heating, effect of phospholipase A2 or trypsin.

Protein biosynthesis was stimulated in liver tissue in vivo and in vitro after administration into mice of either phytoecdizone of turkesterone (0.5 mg/100 g) or of anabolic steroid compound nerobole (1 mg/100 g). Stimulation of protein biosynthesis was due to an increase in functional activity of polyribosomes and to elevation in the synthesis of protein molecules. Actinomycin D, which inhibited the stimulation of protein biosynthesis in liver tissue of mice treated with nerobole, did not affect the phenomenon in mice treated with turkesterone.