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Vol 25, No 3 (2022)

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Pharmaceutical chemistry

Physicochemical properties of zinc oxide nanoparticles modified with betulin diphosphate

Balakireva A.A., Panteleev D.A., Malygina D.S., Orekhov D.V., Spitskaya I.V., Melnikova N.B.


Relevance. Zinc oxide nanoparticles (ZnO NPs) are a promising component of drugs in the treatment of various dermatological diseases, due to the fact that they exhibit high antioxidant, prooxidant, and immunomodulatory properties. ZnO NPs are able to act on the bacterial cell membrane, causing apoptosis, and they are also capable of acting as a delivery vector for active pharmaceutical ingredients, because they are highly permeable through the skin. Immobilization of lupan triterpenoids on the surface of zinc oxide nanoparticles makes it possible to solve the main problem in creating wound dressings with ZnO NPs based on polymeric materials, such as the instability of nanoparticles, their aggregation, and the possibility of a "protein corona" forming when penetrating through the skin. As a triterpenoid of the lupane series, betulin diphosphate (BDP) was chosen, which exhibits wound healing, antioxidant, antitumor and anti-burn properties. BDP is a potential active pharmaceutical ingredient for the treatment of skin diseases. The aim of the work was to develop a method for the synthesis of stable ZnO NPs with immobilized betulin diphosphate, study their physicochemical properties, standardize and validate the procedure for the quantitative determination of ZnO NPs modified with betulin diphosphate (ZnO NPs-BDP). Material and methods. The physicochemical properties of the obtained ZnO NPs-BDP were studied by methods such as IR, UV, and photoluminescent spectroscopy, determination of the hydrodynamic diameter, zeta potential, and specific surface area. The identification of the studied nanoparticles was carried out using these methods. Results. Using powder X-ray diffraction and scanning electron microscopy, it was shown that the immobilization of BDP on the surface of ZnO NPs did not change the structure and practically did not affect the size of the nanoparticles. Conclusion. Thus, we experimentally substantiated the method of obtaining ZnO NPs with immobilized BDP by two methods (boiling zinc oxide nanoparticles in an alcoholic solution of BDP or in a solution of BDP disodium salt hydrate in the presence of a phosphate buffer). The method for the quantitative determination of zinc oxide in the ZnO NPs-BDP substance satisfies the criteria for accuracy and repeatability.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(3):3-9
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Biopharmaceutical study of berberine bisulphate dental gel

Palvinskiy A.G., Bakhrushina E.O., Kholina P.A., Krasnyuk I.I.


The lack of uniform design requirements for the pharmaceutical development of dental gels - especially in terms of common biorelevant approaches to assessing the release of an active ingredient in vitro - complicates the harmonization of international research results with each other and slows down the entry of new effective drugs into the market. Aim. To conduct approbation of a complex of biopharmaceutical tests - diffusion into an agar layer and biodegradation in a biological fluid using a sample of berberine bisulfate dental gel. Materials and methods. In the experiment, samples of dental gels of berberine bisulfate obtained in previous studies, based on hydroxyethyl cellulose and a combination of poloxamers, were compared. Diffusion was carried out in a layer of sterile agar gel, when 1.0 g of the gel was placed in a well with a diameter of 10.0 mm, according to the size of the diameter of the colored zone with thermostating (37 °C) for 60 minutes. Biodegradation in the oral cavity was studied on the "Dissolution" ERWEKA DT-800 tester, "Rotating paddle" apparatus (rotation speed 50 rpm) in a potassium-phosphate buffer solution pH 7.0 at 37 ± 0.1 C for 1.0 g of gel in 60 minutes. Results. In the course of the studies, the advantage of using a combined gel base of poloxamers over hydroxyethyl cellulose and its effect on the rate of release of berberine bisulfate was shown. An experimental sample of a gel based on poloxamers underwent biodegradation within an hour, which, together with high rates of mucoadhesion, makes it possible to assume a long exposure of the drug when used in vivo. Conclusion. For the analyzed compositions of dental gels of berberine bisulfate, made on the basis of a combination of poloxamers and hydroxyethyl cellulose, a difference in the kinetics and completeness of release by the method of diffusion into agar was shown. Biodegradation of the dental gel of berberine bisulfate based on the combination of poloxamers was evaluated within 60 minutes and was complete. It should also be noted that the sample remained adhesive to the substrate during the first half of the test and practically did not undergo degradation.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(3):10-14
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Medical chemistry

Remodeling of the left atrium in patients with 4-5 stage chronic kidney disease

Murkamilov I.T., Aitbaev K.A., Murkamilova Z.A., Fomin V.V., Kudaibergenova I.O., Yusupov F.A.


Purpose of the study. To investigate clinical and functional aspects of the left atrial remodeling in patients with stage 4-5 of the chronic kidney disease (CKD). Materials and methods. A total of 172 patients with CKD stage 4-5 at aged 16-74 years, were examined. Depending on the anterior-posterior size of the left atrium (LA) in diastole, all examined individuals (n = 172) were divided into two groups: 1st - individuals with CKD and normal size (less than 4.0 cm) of the LA (n = 126), 2nd - patients with CKD and increased anterior-posterior size (more than 4.0 cm) of the LA (n = 46). General physical examination and transthoracic echocardiography with the definition of the LA index in diastole was performed. Results. Statistically significant increase in the end systolic (4.20 ± 0.65 cm vs. 3.55 ± 0.47 cm, p < 0.01) and diastolic dimensions (5.97 ± 0.55 cm vs. 5,38 ± 0,43 cm, p < 0.01), thickness of interventricular septum (1,17 ± 0,16 cm vs 0,99 ± 0,14 cm, p < 0.01) and left ventricular posterior wall (1,13 ± 0.15 cm vs 0.97 ± 0.13 cm, p < 0.01) compared to CKD patients with normal size (less than 4.0 cm) of LA. In patients with left atrial dilatation, significantly higher values of the indexed mass of left ventricular myocardium (267 ± 62 g/m2 vs 198 ± 44 g/m2, p < 0.01) were registered. Eccentric type of the heart structural restructuring was significantly more often detected in the 1st group (87.3% vs 56.5%, p < 0.01) in comparison with the 2nd group. Frequency of the concentric type of left ventricular hypertrophy was significantly higher in the group with left atrial dilatation (43.5% vs 12.7%, p < 0.01) in comparison with the 1st group. In patients with CKD, left atrial dilatation was associated with a significant increase in the anterior - posterior dimension of the right ventricle (2.24 ± 0.47 cm vs 1.83 ± 0.37 cm, p < 0.01) and thickness of its anterior wall (0.41 ± 0.03 cm vs 0.39 ± 0.03 cm, p < 0.01). Patients of the 2nd group had higher body mass index values (25.5 ± 5.14 kg m vs 23.6 ± 3.91 kg/m, p < 0.01), systolic (168 ± 29 mm Hg vs 152 ± 27 mm Hg, p< 0.01) and diastolic (102 ± 20 mm Hg vs 94 ± 15 mm Hg, p < 0.01) arterial pressure, C-reactive protein (84.7% vs 20.6%, p < 0.01). Conclusion. In patients with at predialysis stage of CKD, left atrial remodeling is accompanied by increased levels of C-reactive protein and forming of concentric type of left ventricular hypertrophy.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(3):15-22
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Features of metabolism and spectrum of action of selenium, possibilities of application of selene-containing food supplements under SARS-CoV-2 pandemic conditions

Okladnikova E.V., Potupchik T.V., Evert L.S., Veselova O.F., Shirobokov Y.E.


This article provides a literary review of domestic and foreign sources reflecting the prevalence of selenium (Se) in the environment, its metabolism in the human body. It has been shown that Se deficiency is associated with cardiovascular diseases, disorders in the endocrine and reproductive system. The role of Se in the antioxidant defense system that supports the redox homeostasis of the cell and the body, for example, in viral infections, one of the causes of which is oxidative stress, is presented. The above sources also reflect the positive role of Se in viral infections, including, with a new coronavirus infection caused by the SARS-CoV-2 virus, since Se is necessary for the differentiation and proliferation of a number of immune cells involved in the processes of innate and adaptive immunity. It has been proven that in moderate doses, the Se supplement increases the proliferation of T cells and the activity of natural killer cells. In this regard, it is possible to recommend taking dietary supplements containing Se in high-risk areas and /or shortly after suspected infection with SARS-CoV-2. Positive research results, as well as a good safety profile, indicate the possibility of using biologically active food additives containing Se in complex therapy, in particular SELENBIO for women in disorders of the cardiovascular, endocrine, reproductive system, as well as in infectious diseases.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(3):23-33
pages 23-33 views

Problems of experimental biology and medicine

Inulin as a component of fortified foodstuffs: influence on the micronutrient status

Kodentsova V.M., Leonenko S.N., Beketova N.A., Kosheleva O.V., Vrzhesinskaya O.A., Sokolnikov A.A., Shevyakova L.V., Risnik D.V.


Elevance. Inulin is used as a source of polyfructosans in specialty foods for preventive nutrition to reduce the risk of chronic diseases. Along with the proven positive effect on the intestinal microbiota, the absorption of calcium, magnesium and zinc, data on the negative impact on the supply with vitamin E are emerging. The aim of the study was to evaluate the effect of introducing inulin into the diet on the assimilation of micronutrients in growing rats deficient in vitamins D and group B. Material and methods. To assess the effect of inulin on the micronutrient status of growing male Wistar rats (body weight 51.4 ± 0.5 g) in a semisynthetic diet deficient in vitamins D and group B for 7 days the missing vitamins were introduced with or without inulin enrichment of the diet (5%). The indices of micronutrient status were compared with the parameters of rats adequately provided with all vitamins throughout the experiment. The content of calcium and iron in the freeze-dried liver and brain was determined on a Z 5300 atomic absorption spectrophotometer (Hitachi High-Technologies Corporation (HHC), Japan), biochemical parameters of blood and urine were determined on a KoneLab 200i biochemical analyzer (ThermoScientific, Finland). Results. The presence of inulin in the diet slowed down the restoration of the normal supply with vitamins B1 and B6 (urine excretion), B2 (content in the brain), and also led to a 1.4-fold increase of the liver iron concentration, while simultaneously decreasing the concentration of liver vitamin E compared with the control group. Conclusions. Against the background of the existing multiple vitamin deficiency, the simultaneous presence of inulin and vitamins in the diet does not guarantee the complete absorption of all added vitamins and may lead to undesirable consequences. The effectiveness of n fortified product or dietary supplement for correcting the vitamin and mineral status may significantly depend on the composition of the product, which indicates the need for their clinical testing, confirming the bioavailability of the fortifying components and their effectiveness for maintaining health.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(3):34-42
pages 34-42 views

Pharmacological screening of Serratula coronata L. herbal extract

Lupanova I.A., Saybel O.L., Ferubko E.V., Kurmanova E.N., Radimitch A.I., Kolkhir V.K., Mizina P.G.


Relevance. Natural biologically active substances are currently relevant as an important source of new herbal medicines. Phytoecdysteroids are widely accepted in medicine: they increase the non-specific body's resistance to adverse environmental factors, physical and mental strain and stress. The most accessible phytoecdysteroids sources is the Serratula Coronata aboveground part. The purpose of the study. The pharmacological screening of dry purified Serratula Coronata extract for the development of new medicines. Materials and methods. The extract was obtained by three-fold dynamic maceration of raw materials with 70% ethyl alcohol (vol.) at a temperature of (50 ± 2) oC for 60 minutes. Five phytoecdysteroids were isolated in the extract and s a new compound - 20,22-propyledene 20-hydroxyecdysone. Pharmacological investigations were conducted with nonlinear white mice and nonlinear white rats. The research was approved by the VILAR Bioethical Commission. Acute toxicity was studied by the Kerber method. The Serratula Coronata extract effect on the nervous system was studied using "chloral hydrate sleep" and open field tests. The extract effect on the mice life time was studied using hypoxia with hypercapnia in the hermetic volume test. Results and discussion. It is found that that the dry purified Serratula Coronata extract is low-toxic, adaptogenic active, has a tonic effect in terms the "chloral hydrate sleep" model and antihypoxic effect in terms the "hypoxia model with hypercapnia in the hermetic volume" model., The extract does not negatively affect nervous system and experimental animals behavior. Conclusions. The dry purified Serratula Coronata extract is promising for further research to create adaptogenic herbal medicins.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(3):43-48
pages 43-48 views

Correction of structural changes in immune organs by genus Silene plants extracts at experimental cyclophosphamid immunosuppression

Khobrakova V.B., Razuvaeva Y.G., Khalzanova A.V., Olennikov D.N., Shobolov B.P.


The purpose of the study is to evaluate the effect of Silene jeniseensis and Silene repens dry extracts on structure of mice thymus and spleen at cyclophosphamide immunosuppression. Materials and methods. The experiments were carried out on F1 (CBAxC57Bl/6) mice. Immune deficiency was simulated by a single intraperitoneal introduction of cyclophosphamide in the dose 250 mg/kg. S. jeniseensis and S. repens dry extracts in the dose 100 mg/kg were administered to animals for 14 days intragastrically against cyclophosphamide. Morphological studies of the thymus and spleen were performed on day 16 after the extracts administration. The lobule area, cortex and medulla widths, cells density and composition of the cortex were measured in the thymus. The relative area of the white and red pulp was determined in the spleen. Results. S. jeniseensis and S. repens extracts limited the development of destructive processes in the mice thymus: lobule area was by 23 and 20% higher, the cortico-medullary ratio was by 28 and 25% higher. Cells density was higher in the cortical layer, due to a decrease in the number of destructive thymocytes and an increase in the number of mitotically dividing cells, blasts and large lymphocytes. The white pulp total area increased by 27 and 16% against the background of S. jeniseensis and S. repens extracts introduction. The mantle and marginal zones formed in the lymphoid follicles, which indicates of the lymphocyte differentiation processes restoration. Conclusions. S. jeniseensis and S. repens extracts limited the development of pronounced involutive processes in the immune organs at cyclophosphamid immunosuppression.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(3):49-56
pages 49-56 views

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