[Effect of biologically active substances of animal and plant origin on prooxidant-antioxidant balance in rats with experimental prostatic hyperplasia].

The effect of biologically active complexes of animal (prostatilen) and plant (permixon) origin on physiological indices of prostate and prooxidant-antioxidant balance in prostate and blood was studied in rats with the hyperprolactinemia-induced prostatic hyperplasia. It was shown that both prostatilen (1 mg of the total peptides per kg) and permixon (100 mg of Serenoa repens extract per kg) prevent increase in the prostate mass and volume, in the content of lipid hydroperoxides, and in the glutathione peroxidase activity in prostate. Prostatilen, in contrast to permixon, normalized the content of lipid hydroperoxides (increased under hyperplazia conditions) and increases glutathione peroxidase activity (reduced under hyperplazia conditions).

Prooxidant-antioxidant balance in the prostate and blood of rats with sulpyride[corrected]-induced prostatic hyperplasia corrected with prostatilen.

We studied the effects of 30-day injections of sulpyride and treatment with Prostatilen on the development of prostatic hyperplasia and LPO in rats. Sulpyride induced proliferation of lateral lobes, increased the content of lipid hydroperoxides and glutathione peroxidase activity in the gland; in the blood this preparation increased lipid hydroperoxide concentration and decreased glutathione peroxidase and total antioxidant activity. Prostatilen prevented the development of hyperplasia and normalized the prooxidant-antioxidant balance in tissues, except total antioxidant activity of the blood.

[Effect of cinnarizine on the brain mitochondrial oxidative system, antioxidant blood activity, and the rat behavior in hypoxia]. / Vliianie tsinnarizina na mitokhondrial'nuiu sistemu okisleniia mozga, antiokislitel'nuiu aktivnost' krovi i povedenie krys pri gipoksii.

The effect of cinnarizine on the functional state of brain mitochondria, the activity of blood antioxidant system, and the behavior of rats was studied under model hypoxic hypoxia conditions. A four-day treatments with cinnarizine (50 mg/kg, twice per day via a gastric tube) prevents the hypoxic brain edema development, restores NAD+ dependent oxidation of a succinate substrate, normalizes emotional-exploratory activity, and causes hyperlocomotion of the experimental animals, while not influencing a high level of activity of the blood antioxidant system.

[Comparative study of the effect of paracetamol, phenacetin and amidopyrine on mitochondrial function in isolated rat hepatocytes]. / Sravnitel'noe izuchenie deistviia paratsetamola, fenatsetina i amidopurina na funktsiiu mitokhondrii v izolirovannykh gepatotsitakh krys.

Effects of amidopyrine, phenacetin and paracetamol on the viability and energetic state of isolated rat hepatocytes were compared. During incubation in minimal salt solution all drugs in concentrations above 1 mM in dose-dependent manner decreased the viability of hepatocyte suspension assessed by trypan blue dye inclusion and inhibited the ATP synthesis and the respiratory activity. Cytotoxic effect of chemicals decrease in the order: amidopyrine-->phenacetin-->paracetamol. The inhibition of the rate of endogenous respiration were accompanied by stimulation of oxygen consumption in nonmitochondrial systems. An uncoupler of oxidative phosphorylation, 2,4-dinitrophenol, and disruption of plasma membrane by digitonin followed by substrate succinate addition did not restore the respiratory activity of hepatocytes up to the level of control cells. These data show that cytotoxicity of the chemicals is determined by their interaction with enzymes of mitochondrial respiratory chain.

[The effect of paracetamol and its combinations with acetylsalicylic and ascorbic acids on lipid peroxidation processes in the rat liver]. / Vliianie paratsetamola, ego kombinatsii s atsetilsalitsilovoi i askorbinovoi kislotami na protsessy perekisnogo okisleniia lipidov v pecheni krys.

Paracetamolum (PC) after i.p. administration to rats at the therapeutic (100.0 mg/kg) and subtoxic (500.0 mg/kg) doses was shown to induce significant and dose-dependent elevation of the level of malone dialdehyde (MDA) as well as the increase in a certain extent of chemiluminescence (CL) being injected at the higher dose. Acetylsalicylic acid (ASA) at the same doses being injected at the lower one, induced the tendency toward the reduction of MDA level, while at the higher dose the rise of MDA content and CL intensity compared to PC have been observed. PC combination with ASA at therapeutic doses range (50.0 + 50.0 mg/kg) significantly diminished MDA formation, while at subtoxic doses range (250.0 + 250.0 mg/kg) such effect was not detected, although subsequent tendency toward CL intensity reduction was observed. Ascorbinic acid being administered in combination with PC and ASA had no influence on MDA formation but significantly weakened CL intensity when subtoxic doses of indicated drugs were used.

[The effect of local corticosteroid therapy on ophthalmic tonus and ocular hydro- and hemodynamics in experimental inflammatory pathology]. / Vliianie mestnoi terapii kortikosteroidami na oftal'motonus, gidro- i gemodinamiku glaza pri éksperimental'noi vospalitel'noi patologii.

The laboratory samples of 0.1% dexamethasone and 1% hydrocortisone eye drops which had been designed at the State Research Center of Drugs were investigated for their effects on intraocular pressure in the presence of photokeratitis caused by UV irradiation. Producing pronounced antiinflammatory effects, the daily triple instillations of corticosteroids for 9 days tended to gradually increase the ophthalmotone induced both by the imbalance of production and outflow of intraocular fluid and by ocular hemodynamic disorders associated with the enhanced blood filling of the choroidal vessels and with the higher intensity of pulse oscillations.

[Analgesic action and pharmacokinetics of lysine acetylsalicylate administered intramuscularly]. / Anal'geticheskoe deistvie i farmakokinetika lizina atsetilsalitsilata pri vnutrimyshechnom vvedenii.

The analgesic effect, acute toxicity and pharmacokinetics of lysine acetylsalicylate (LAS), a water-soluble salt of acetylsalicylic acid (ASA) were studied as compared with a 50% solution of analgin and a 4% solution of amidopyrine at intramuscular administration and ASA administered intragastrically. During inflammation-induced pain in rats LAS exerts a pronounced analgesic effect exceeding the activity of other agents. LD50 of LAS was similar to that of analgin and ASA. LAS toxicity was significantly less than that of amidopyrine. Bioavailability of ASA at intramuscular administration to rabbits was close to that at intravenous injection and significantly higher as compared with intragastric administration.

[Antiaggregation action and pharmacokinetics of lysine acetylsalicylate]. / Antiagregatsionnoe deistvie i farmakokinetika atsetilsalitsilata lizina.

Lysine acetylsalicylate, a water-soluble salt of acetylsalicylic acid, administered intravenously to rabbits (15 and 100 mg/kg) and also in vitro (2-10 mg/ml) produced antiaggregational and anticoagulant effects pertaining to acetylsalicylic acid. Pharmacokinetics of acetylsalicylic acid injected intravenously to rabbits in the form of lysine acetylsalicylate is formalized by a biexponential equation for a two-compartment model. The main pharmacokinetic constants of acetylsalicylic acid in these experiments were found to be similar to those in humans.

[Mechanism of the microcirculatory effects of ethyl-3,5,6-tri-O-benzyl-D-glucofuranoside]. / O mekhanizme mikrotsirkuliatornykh éffektov étil-3,5,6-tri-O-benzil-D-gliukofuranozida.

According to the rheo- and photoplethysmography data, ethyl-3,5,6-tri-O-benzyl-D-glucofuranoside (glivenol, tribenol; 25,250 and 4000 mg/kg i.p.) markedly increases the blood content in hind limbs of rabbits, displaying a tendency towards a decrease in systemic arterial pressure and negligibly raises the body temperature when given in maximal doses, without affecting cardiac activity and respiration. The mechanism of the drug hemodynamic effect revealed is determined by activation of the blood flow in precapillary vessels. This plays an essential role in pathogenetic therapy of microcirculatory and trophic disorders in chronic venous failure.

[Effect of tribenol on the activity of certain redox enzymes in inflamed venous walls]. / Vliianie tribenola n aktivnost' nekotorykh okislitel'no-vosstanovitel'nykh fermentov v venoznoi stenke pri ee vospalenii.

A study was made on the mechanism of action of the antivaricose agent tribenol (ethyl-3,5,6-tri-O-benzyl-D-glucofuranozide; glivenol) on the activity of hydroxyreductase on the Krebs cycle and glycolysis during occlusion of the femoral vein and its inflammation in rats. It was shown histochemically that on the 5th day of traumatic phlebitis after ligation of the vein, its wall shows a substantial rise in the activity of succinate- and malate dehydrogenase (SDH and MDH), a slight increase in the activity of lactate dehydrogenase (LDH) and a pronounced lowering of the activity of alpha-glycerophosphate dehydrogenase (alpha-GPDH). The treatment with tribenol in a dose of 25 mg/kg for 5 days makes the activity of SDH and alpha-GPDH return to normal, drastically increases the activity of LDH and produces no significant effect on MDH. In a dose of 250 mg/kg tribenol makes the activity of all hydroxyreductases studied return to normal or reduces it.

[Effects of strophanthin, mefenamic acid and dexamethasone on the inflammatory and reparative processes in the heart in experimental myocarditis]. / Vliianie strofantina, mefenamovoi kisloty i deksametazona na vospalitel'no-reparativnye protsessy v serdtse pri éksperimental'nom miokardite.

In isadrin-induced myocarditis, the rat heart shows an increase in the activity of acid phosphatase, glucose-6-phosphate dehydrogenase. The heart weight also rises, whereas ATPase activity and magnesium content fall. Under these conditions strophanthin produces a marked decrease in acid phosphatase activity, stimulates the activity of glucoso-6-phosphate dehydrogenase, and demonstrates a tendency to increasing the activity of ATP-splitting enzymes, to reducing the activity of ATP-synthetase, and to the recovery of the magnesium content. Mefenamic acid and dexamethasone also decrease the activity of acid phosphatase but this decrease is less pronounced as compared with that induced by strophanthin. They exhibit the same tendency to the inhibition of glucoso-6-phosphate dehydrogenase. Mefenamic acid affects the remaining parameters similarly to strophanthin, while dexamethasone inhibits them.

[Membrane stabilizing effect of medicinal substances used for the treatment of chronic venous insufficiency]. / Membranostabiliziruiushchii éffekt lekarstvennykh sredstv, primeniaemykh dlia lecheniia khronicheskoi venoznoi nedostatochnosti.

Experiments "in vitro" have brought evidence that butadion, escinol, esculetin, glyvenol, rutin, escin and the summary flavor noid preparation are capable of stabilizing erythrocytes membranes with the cells subjected to hypotonic hemolysis. Depending upon optimal concentrations the activity of the substances was within the range of 10(-3) to 10(-8). As concerns the intensity of the effect in the optimal concentration (10(-5) M), that corresponds to the one built up in the blood of patients given the therapeutic dose of the drug, the action of glyvenol was 1.6-3.5 times superior to that of the other compounds.