Vol 7, No 6 (2019)


11-amino acid peptide imitating the structure of erythropoietin α-helix b improves endothelial function, but stimulates thrombosis in rats.

Korokin M.V., Soldatov V.O., Tietze A.A., Golubev M.V., Belykh A.E., Kubekina M.V., Puchenkova O.A., Denisyuk T.A., Gureyev V.V., Pokrovskaya T.G., Gudyrev O.S., Zhuchenko M.A., Zatolokina M.A., Pokrovskiy M.V.


The aim of the study was to test whether P-αB can be positioned as a preventing and treating agent for cardiovascular diseases.Materials and methods. The study was performed on sexually mature male Wistar rats. Endothelial dysfunction was modulated by a 7-days intraperitoneal administration of L-NAME at the dose of 2.5 mg/100 g. P-αB, or erythropoietin (EPO), was used for therapy at the dose of 2.5 µg/100 g × 3 times for 7 days, the total dose was 7.5 µg/100 g. The function of endothelium was estimated by an endothelium-dependent and endothelium-independent vasodilation. In addition, a histological assessment of the abdominal aortic wall state and the analysis of eNos, Tnf and Il-1β genes expression were performed. To estimate prothrombotic properties, P-αB and EPO were administered, at the doses of 2.5 and 5 µg/100 g (3 times a day for 7 days, the total doses were 7.5 µg/100 g and 15 µg/100 g, respectively) and on the 8th day, the time of ferric (III) chloride-induced carotid artery thrombosis was estimated.Results. Theresults of the functional tests for endothelium-dependent and endothelium-independent vasodilatation, as well as the histological picture of the aorta have evidenced that P-αB and EPO do not affect L-NAME-induced hypertension but improve the endothelium function. At the same time, P-αB shows a significantly higher endothelial-protective activity, reducing the coefficient of endothelial dysfunction from 5.1±0.15 to 2.72±0.12. In addition, P-αB has significantly increased the expression of eNos and reduced the expression level of Tnf and Il-1β mRNA genes. Carrying out Ferric (III) chloride-induced carotid artery thrombosis has revealed that P-αB (5 µg/100 g × 3 times a day for 7 days, total dose was 15 µg/100 g) has a lower but statistically significant prothrombotic activity than EPO.Conclusion. P-αB can be positioned as an atheroprotector because of its ability to prevent the death of endothelial cells, as well as to reduce remodeling and proinflammatory activation of the vascular wall. However, the prothrombotic properties of P-αB limit its use as a preventing and treating agent for atherosclerosis-associated diseases.
Pharmacy & Pharmacology. 2019;7(6):312-320
pages 312-320 views

Structural transformations of thermal burn wounds in rats under the influence of Semax and Selank neuropeptides

Azhikova A.K., Feldman B.V., Andreeva A.A., Teply D.D., Samotrueva M.A., Myasoedov N.F.


The morphological features of the skin of rats under the stress exposure, such as burn injury and against the background of the correction by the drugs of the peptide structure, have been studied.The aim of the study was to investigate the regulatory effect of the neuropeptide drugs Semax (Met-Glu-His-Phe-Pro-Gly-Pro) and Selank (Thr-Lys-Pro-Arg-Pro-Gly-Pro) under the conditions of thermal burn exposure.Materials and methods. The object of the study was integumentary tissues (skin, subcutaneous tissue) of laboratory non-linear male rats (n = 36) excised from the thermal injury zone. A thermal burn of the skin had been caused by the application of a copper object in the interscapular in the interscapular dorsal area. Starting from the first day after the injury, neuropeptide drugs Semax (Met-Glu-His-Phe-ProGly-Pro) and Selank (Thr-Lys-Pro-Arg-Pro-Gly-Pro) had been administered intraperitoneally at the doses of 100 μg/kg daily during the entire period of the experiment. To assess the condition of the skin tissues, histological sections 5-6 μm thick were prepareв, stained afterwards with hematoxylin and eosin. The consistency of the systemic effect of the neuropeptide drugs was estimated by a change in some indicators of the immune system.Results. The thermal exposure led to the development of significant degenerative and dystrophic changes in the skin. The recovery of the burn wounds on rats’ skins proceeded according to the type of the delayed partial reparative regeneration, accompanied by destructive phenomena and the formation of the scar tissue.Under the influence of the drugs based on the regulatory peptides of Semax (Met-Glu-His-Phe-Pro-Gly-Pro) and Selank (Thr-Lys-Pro-Arg-ProGly-Pro), the recovery of burn wounds in rats proceeded more intensively, compared with the animals from the group without any correction. This fact was confirmed by the earlier signs of the beginning of the reparative skin regeneration: the restriction of destructive processes within the epidermis and dermis, the absence of purulent-necrotic complications, the initial phases of granulation and epithelization, an early scab rejection and a partial closure of the defect.Conclusion. The use of the neuropeptide drugs Semax and Selank as systemic remedies for the correction of wound skin defects in experimental animals proves their polypotent effectiveness, expands the therapeutic possibilities and opens up new prospects for their use.
Pharmacy & Pharmacology. 2019;7(6):321-331
pages 321-331 views

Cerebroprotective effect of some phenolic acids under conditions of experimental brain ischemia

Voronkov A.V., Pozdnyakov D.I., Nigaryan S.A.


The aim of the study was to evaluate the cerebroprotective effect of some phenolic acids under the conditions of experimental cerebral ischemia in rats.Materials and methods. The experiment was conducted on male Wistar rats weighing 220-240 g. Focal cerebral ischemia was modeled by irreversible right-sided thermocoagulation of the middle cerebral artery under chloral hydrate anesthesia (350 mg/kg, intraperitoneally). The experimental compounds (4-hydroxy-3.5-di-tert-butyl cinnamic acid, caffeic acid and gallic acid 100 mg/kg each compound) and a reference drug (Mexicor - 100 mg/kg) were administered intragastrically next day after the surgery and then for three daysrunning. The effect of the test-compounds on the cognitive functions of the rats was evaluated by CRPA and TEA tests. The influence of the compounds on the changes in the concentration of lactate, pyruvate, homocysteine, as well as the degree of cerebral edema formation and necrosis of the brain tissue, were studied.Results. In the study, it has been established that against the background of the focal cerebral ischemia, the administration of caffeic, 4-hydroxy-3,5-di-tert-butylcinnamic and gallic acid, contributed to the preservation of a memorable trace in rats, as well as a decrease in lactate concentration (by 40.37% (p<0.05), 151.26% (p<0.05), 48.02% (p<0.05)) and pyruvate (by 96.6,% (p<0.05), 38, 78% (p<0.05), 33.3% (p<0.05)), homocysteine (by 59.6% (p<0.05), 102.18% (p<0.05), 28.8% (p<0.05)), аnecrosis zone (by 122.79% (p<0.05), 165.11% (p<0.05), 12.38% (p<0,05)) and cerebral edema (by 10.47% (p<0.05), 11.08% (p<0.05), 9.92% (p<0.05)) relative to the NC group of rats.Conclusion. The obtained data indicate the possibility of further detailed investigation of the cerebroprotective effect of 4-hydroxy-3,5-di-tert-butylcinnamic, caffeic and gallic acids.
Pharmacy & Pharmacology. 2019;7(6):332-339
pages 332-339 views

Antiulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate in ethanol-prednisolone damage to gastric mucosa

Chernikov M.V., Oganova M.A., Kalashnikova S.A., Polyakova L.V., Khromova N.A.


Nowadays, the search for new effective and safe medicines for the treatment of acid-dependent gastrointestinal diseases remains an urgent problem of modern pharmacology.The aim of this study was an experimentally study of the anti-ulcer activity of 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole dinitrate on the model of damage to the gastric mucosa caused by the administration of 80% ethanol and prednisolone combination (20 mg/kg).Materials and methods. To simulate the damage to the gastric mucosa, the experimental animals (white male Wistar rats) were administrated with prednisone at the rate of 20 mg/kg and 80% ethyl alcohol at the dose of 0.6 ml/100 g of the animal body weight. Prednisolone was dissolved in 80% alcohol. Antisecretory antiulcer agents actively used in clinical practice, were selected as reference drugs: ranitidine (30 mg/kg, 10 mg/kg and 3 mg/kg) and omeprazole (3 mg/kg, 1 mg/kg and 0.3 mg/kg). The studied compound was used at the doses of 30 mg/kg, 10 mg/kg and 3 mg/kg. All the substances under study were administered intragastrically with the use of an atraumatic probe. Results. It has been established that the benzimidazole derivative in the studied doses contributes to a dose-dependent reliable reduction in the area and depth of ulcerative lesions of the gastric mucosae relative to the control and reference drugs (ranitidine and omeprazole). In addition, in the maximum studied dose (30 mg/kg), the proportion of the animals with ulcerative lesions significantly decreases by more than 2 times. The calculated ED50 values for the benzimidazole derivative and ranitidine were 5.09 mg/kg and 38.23 mg/kg, respectively.Conclusion. The obtained experimental data indicate that the benzimidazole derivative has a pronounced dose-dependent antiulcer effect on the model of ethanol-prednisolone erosive-ulcerous defects of the rats’ gastric mucosae, which is superior to the effects of the reference preparations. It makes its further study promising.
Pharmacy & Pharmacology. 2019;7(6):339-345
pages 339-345 views

Phytochemical study of Tribulus Terrestris L.

Affaf A., Karpenko Y.N., Gulyaev D.K., Belonogova V.D., Molokhova E.I., Blinova O.L., Gileva A.A.


Tríbulus terrestris L., an annual herb belonging to the Zygophyllaceae family and growing in moderate and tropical climates, has a rich chemical composition of biologically active substances and chemical elements.The aim of the work is a phytochemical study of Tribulus terrestris L. growing in different geographical zones.Materials and methods. The objects of study were herb specimens of Tribulus terrestris L. collected in different habitats. The samples of the raw materials were shade-dried. The determination of saponins in the raw materials, was carried out by high performance liquid chromatography with a mass spectrometric detection (HPLC-MS / MS). The study of the qualitative and quantitative composition of the elements was carried out on an X-ray fluorescence spectrometer.Results. The saponins had been studied by HPLC-MS/MS, according to which in all the studied samples, dioscin and protodioscin were found. Their retention times coincided with the retention times of dioscin and protodioscin standards. It has been established that among the macroelements of Tríbulus terrestris L., potassium and calcium are mostly accumulated. They account for about 90% of the total content of the elements in the plant. It has been revealed that the distribution of macroand microelements in the plant, varies significantly depending on their place and growing conditions.Conclusion. The maximum dioscin content was observed in the samples harvested in Moldova, and the minimum - in the samples from the nursery garden of the All-Russian Scientific Research Institute of medicinal and aromatic plants. The largest amount of protodioscin was found out in the samples from the Crimea, and the minimum - in the samples from Moldova. The carried out study of the elements content of Tríbulus terrestris L. showed that the habitats (geographical zones) in which the studied samples of raw materials had been were collected, affect the accumulation of the elements by the plant. Based on the data obtained, biological absorption series have been compiled for the samples from each habitat.
Pharmacy & Pharmacology. 2019;7(6):346-355
pages 346-355 views

Dynamics of the acute viral hepatitises morbidity and range of medicinal preparations for treatment in hospital environment in the Volgograd region (the Russian Federation), 2016-2018.

Ganicheva L.M., Ioannidi E.A., Panfilova O.A., Tyurenkov I.N., Knyazeva Y.S., Kaisheva N.S.


The aim of the study was to investigate the prevalence of acute viral hepatitises A, B and C in the Volgograd region; the range and identification of the most frequently prescribed pharmacological groups to be used in hospital environment; and analyzing the price dynamics of medicines. These factors will make it possible to assess the state of the medicine provision for the patients with this disease in hospital environment. Materials and methods. In the study, the following methods have been used: comparison, a method of grouping indicators and a structurallogical method. The materials were the hepatological department patients’ treatment sheets (Volgograd Regional Clinical Infectious Diseases Hospital N1).Results. Acute hepatitis A is the most common (46.9%), acute hepatitis B occupies the second position (27.4%), and acute hepatitis C - the third one (25.7%), where in 46.2%, 23.5% and 14.7%, respectively, are accounted for by icteric viral hepatitis. Hepatoprotectors, symptomatic medications and rehydration and detoxification medicinal preparations are prescribed for all forms and degrees of the disease severity.Conclusion. The study has revealed a decreased morbidity of acute viral hepatitises A, B and an increased morbidity of acute viral hepatitis C in the Volgograd region. Among all the types of hepatitises, the prevailing one is the icteric form of moderate severity. The range of medicinal preparations prescribed for the treatment of acute viral hepatitises has been studied. Most often, doctors prescribe hepatoprotectors, rehydration and detoxification medicinal preparations. The study of price dynamics, showed a predominant increase in hepatoprotectors and a decrease in medicines for rehydration and detoxification. The results obtained indicate a tendency towards the improvement of drug provision in the Volgograd Region, for the patients with acute viral hepatitises. Besides, the results of the study give an opportunity to consider the ways of its further optimization.
Pharmacy & Pharmacology. 2019;7(6):356-362
pages 356-362 views

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