Eksp Klin Farmakol [journal]
- [REPARATIVE ACTIVITY OF ORIGINAL SUBSTANCE BASED ON ALGINIC ACID]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2016; 79(1):38-44.
The influence of an original substance based on enzymatically destructed alginic acid on the reparative activity has been studied using an experimental model of planar aseptic wound. Toxicity of the test compound was evaluated and its effective dose was determined using curiozin as the reference drug. It is found that the test compounds is non-toxic. It is established that the pharmacological activity of the reference drug (curiozin) is lower on the average by 3.5% (δ = 0.021) than that of the original pharmaceutical substance based on destructed alginic acid
- [ANTIOXIDANT ACTIVITY OF XYMEDONE IN RATS WITH CHRONIC AUTOIMMUNE INFLAMMATION]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2016; 79(1):33-7.
Effects of drug xymedone (in comparison to ionol) in a group of 32 white rats with experimental model of chronic autoimmune inflammation of rat paws (induced by Freund's adjuvant) were studied by measuring the volume of paw edema and determining the levels of lipid peroxidation (LPO) products and the activity of antioxidant enzymes in various tissues. Chronic autoimmune inflammation induced by Freund's adjuvant was characterized by the LPO intensification and disturbances of the level of antioxidant enzymes. Intragastric administration of xymedone (2,2-dihydro-4,6-dimethyl,-N-(β-oxy-ethyl)-2-pyrimidon) at a dose of 169 mg/kg and reference drug ionol (2,6-ditretbutyl-4-methylphenol) at a dose of 220 mg/kg increased the activity of serum antioxidant enzymes by 19% and 11%, respectively, decreased the serum level of nitrite ion by 62% and 50%, and reduced the levels of LPO products in rat blood and homogenates of liver, kidney, and spleen by up to 80% (p < 0.05).
- [PHARMACOLOGICAL CORRECTION OF METABOLIC DISORDERS IN CHILDREN WITH ACUTE EPSTEIN--BARR VIRAL INFECTION]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2016; 79(1):28-32.
The study was aimed to investigate the influence of drug reamberin inclusion in the treatment regimen of patients with acute Epstein-Barr virus (EBV) infection on the effectiveness of therapy. Treatment results were analyzed in a group of 70 children aged 4-15 with a diagnosis of moderate to severe EBV infection. By the method of random sampling distribution, patients were divided into two comparable groups of 35 children, which were representative with respect to gender, age, date of admission, and conducted basic therapy. Patients in the control group were treated by the conventional scheme, while the main group received basic therapy with antibacterial drug (according to indication) and symptomatic agents (antipyretics, desensitizing agents, and local antiseptics for the treatment of rotor and nasopharynx) and, in addition, obtained 1.5% reamberin solution intravenously, 10 mL/kg body weight once a day at a rate of 3-4 mL/min (the treatment course did not exceed 3 days). Treatment efficacy was assessed by a decrease in the duration of intoxication symptoms, relief of their clinical manifestations, and normalization of laboratory data (including, in addition to commonly accepted data, the levels of malonic dialdehyde, ferritin, transferrin and catalase before and after treatment).The inclusion of reamberin in the therapy of acute EBV infection in children favors (in comparison to conventional treatment regimen) more pronounced and rapid decrease the intensity of the oxidative process and improves the functioning of the antioxidant system. This was manifested by normalization of immunobiochemical indicators (reduction of malonic dialdehyde and ferritin and increase in the level of catalase) and decrease in the inflammatory response (leukocytosis, ESR, and the number of atypical mononuclear cells in the blood), This resulted in more rapid relief of the clinical manifestations of infection (sore throat, hyperthermia, lymphadenopathy, and hepatomegaly) and shortened the hospital stay by 38.5% (p < 0.05).
- [GLUTATHIONE SYSTEM ACTIVITY IN RAT TISSUES UNDER PHENYLETHYL BIGUANIDE ACTION ON THE BACKGROUND OF EXPERIMENTAL BRAIN ISCHEMIA/REPERFUSION DEVELOPMENT]. [English Abstract, Journal Article, Research Support, Non-U.S. Gov't]
- Eksp Klin Farmakol 2016; 79(1):23-7.
It was studied the total antioxidant activity, content of primary lipid peroxidation (LPO) products and reduced glutathione, and the activity of glutathione peroxidase, glutathione reductase, glucose-6-phosphate dehydrogenase, and NADP-isocitrate dehydrogenase in rat tissues under phenylethyl biguanide (phenfor- min) action on the background of experimental brain ischemia/reperfusion development. It is stablished the analyzed parameters, increasing under ischemia/reperfusion conditions in the brain and blood serum of animals, exhibit a decrease upon the introduction of this biguanide derivative. The obtained data can be explained by a decrease in degree of mobilization of the antioxidant system--in particular, of its glutathione chain--in the pathologic state. Hence, there is a need in NADPH supply for the system functioning compared with the pathology. Thus, phenylethyl biguanide demonstrates its antioxidant and protective properties under oxidative stress development that is accompanied by accumulation of the products of free radical oxidation of biomolecules during the ischemic brain injury.
- [DIURETIC ACTIVITY OF 4-O-CARBOXYPHENYL-D-GLUCOPYRANOSIDE SODIUM SALT ADMINISTERED VIA DIFFERENT ROUTES]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2016; 79(1):20-2.
It was compared the diuretic activity of the sodium salt of 4-(O-β-D-glucopyranosyloxy)benzoic acid for enteral (intragastric) and parenteral ways of administration. The test substance was administered enterally and parenterally (subcutaneously in the region of the withers) in a daily dose of 18 µmol/kg for the first seven days and in a dose of 54 mmol/kg for the next seven days. Diuretic activity of the sodium salt of 4-(O-β-D-glucopyranosyloxy)benzoic acid was evaluated in terms of urine volume. Urine was analyzed for creatinine and the concentration of sodium, potassium and chloride ions. Experiments showed that the sodium salt of 4-(O-β-D-glucopyranosyloxy)benzoic acid produced a diuretic effect only for the enteral administration route.
- [ESTIMATING THE EFFECTIVENESS OF HYPOLIPIDEMIC THERAPY WITH ROSUVASTATIN IN PATIENTS WITH CORONARY HEART DISEASE DEPENDING ON THE GENOTYPE OF LIPOPROTEIN LIPASE]. [Clinical Trial, English Abstract, Journal Article, Research Support, Non-U.S. Gov't]
- Eksp Klin Farmakol 2016; 79(1):15-9.
Taking into account the genetic heterogeneity of hyperlipidemias, polymorphic genes involved in the regulation of lipid metabolism may explain differences in the efficacy of hypolipidemic therapy. In the present prospective and randomized study, we have investigated the efficacy of rosuvastatin (10 mg/day) in the therapy of atherogenic hyperlipidemias in a group of 62 patients with coronary heart disease (CHD), depending on the genotype of lipoprotein lipase (LPL). The pharmacological correction was carried out during one year under control of lipid metabolism parameters (total cholesterol, LDL-C, HDL-C, HDL-unrelated cholesterol, triglycerides, atherogenic index) at the baseline and on 4th, 8th, 24th and 48th week. The HindIII polymorphism (+495T > G, rs320) of the LPL gene was genotyped in all patients studied through a real-time PCR TaqMan assay. Rosuvastatin produced a significant hypolipidemic effect with respect to all investigated lipid metabolism parameters for 24 weeks of treatment. Changes in the parameters of lipid metabolism upon rosuvastatin treatment differed in patients with genotype +495GG as compared to the rest LPL genotypes. In comparison to the +495TT and TG genotypes, the genotype +495GG showed a greater reduction in total cholesterol on 8th week, and in LDL-C, HDL-unrelated cholesterol, and atherogenic index on the 48th week of rosuvastatin therapy (p <0.01). It can be suggested that the pronounced hypolipidemic effect of rosuvastatin in homozygotes +495GG of the LPL gene is associated with modulation of the LPL activity, as it has been previously reported for other statin drugs.
- [COMPARISON OF CYTOPROTECTIVE EFFECTS OF HEMANTANE AND AMANTADINE UNDER CONDITIONS OF 6-HYDROXYDOPAMINE NEUROTOXIN ACTION ON CULTURED HUMAN NEUROBLASTOMA CELLS]. [Comparative Study, English Abstract, Journal Article]
- Eksp Klin Farmakol 2016; 79(1):12-4.
Potential neuroprotective activity of the novel antiparkinsonian drug hemantane (hydrochloride N-2-(adamantyl)-hexamethylenimine) in comparison to amantadine has been studied in various regimes of administration on human neuroblastoma SH-SY5Y cell line injury induced by 6-hydroxydopamine (6-OHDA), which is used as in vitro model of dopaminergic neurons for Parkinson's disease. Two regimes of hemantane and amantadine administration in a range of final concentrations 10⁻⁶-10⁻⁸ M were used either prior to or immediately after 6-OHDA introduction. MTT colorimetric assay was used to assess the viability of test cells. Significant decrease in viability of SH-SY5Y cells treated with 6-OHDA was observed. The addition of hemantane to cell medium produced cytoprotective effects in both regimes of administration--before and after 6-OHDA--at concentrations 10⁻⁷ M and 10⁻⁶-10⁻⁸ M, respectively. Amantadine in con- centrations 10⁻⁷-10⁻⁸ M was effective to increase cell survival only when administered after 6-OHDA. These results show that hemantane has a greater neu-roprotective potential in comparison to amantadine.
- [PHARMACOLOGICAL STUDY OF NEW COMPOUNDS ACTING AS REGULATORS OF 18-KDA TRANSLOCATOR PROTEIN LIGANDS]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2016; 79(1):7-11.
The interaction of new original 1-arylpyrrolo[1,2-a]pyrazine-3-carboxamide derivatives with mitochondrial translocator protein (MTP) 18 kDa has been studied by radioligand binding assay. Compounds GML-1 (Ki = 5.2 x 10⁻⁸ M) and GML-3 (Ki = 5.3 x 10⁻⁷ M) exhibit high binding affinity for MTP. GML-1 and GML-3 in a dose range of 0.1-1 mg/kg (i.p.) demonstrated anxiolytic-like effects in the elevated plus-maze test in CD-1 mice, which were blocked by the MTP selective antagonist PK11195. The data obtained on the molecular target, anxiolytic-like effects and low toxicity GML-1 and GML-3 suggest that these compounds are promising for further investigation as anxiolytics.
- [NEUROCHEMICAL STUDY OF TROPOXIN EFFECTS ON THE CONTENT OF MONOAMINES AND ITS METABOLITES IN WISTAR RAT BRAIN STRUCTURES]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2016; 79(1):3-6.
The influence of perspective anti-migraine drug tropoxin on the content of monoamines and related metabolites in Wistar rat brain structures, including frontal cortex (FC), hypothalamus, nucleus accumbens (NA), striatum, and hippocampus, has been studied using HPLC/ED technique. Tropoxin (10 mg/kg) induced a 30% decrease (p < 0.05) in dopamine (DA) level in FC as well as norepinephrine content in NA, while the concentrations of DA metabolites DOPAC and HVA in the hypothalamus were found to increase. The injection of tropoxin in a dose of 20 mg/kg led to an increase in HVA level in hypothalamus as well as seroto- nin metabolite 5-HIAA content in NA. The obtained data provide evidence that tropoxin predominantly influenced the activity of dopaminergic system while the drug effects on the parameters of serotoninergic link seem to be rather mild.