Open Access Open Access  Restricted Access Access granted  Restricted Access Subscription or Fee Access

Vol 24, No 1 (2021)


Standardization of medicinal drug with original substance of benzophenone derivative for HIV-1 infection treatment

Kosman V.M., Jain (Korsakova) E.A., Demchenko D.V., Makarov V.G., Balabanyan V.Y.


Synthetic pyrimidine derivative of benzophenone l-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil was proposed as an original pharmaceutical substance for the development of antiretroviral drugs. The aim of the study was to develop and validate methods for gualitative and guantitative standardization of the drug dosage form (tablets) with the original pharmaceutical substance of the benzophenone derivative for the treatment of HIV-1 infection. Material and methods. Experimental tablets were obtained in laboratory conditions of RMC "HOME OF PHARMACY" (Russia) in accordance with laboratory guidelines and analyzed by various pharmacopoeia methods. Results. In order to evaluate the identification and guantify the active substance in the drug high-performance liguid chromatography with UV detection was proposed, acceptance criteria for guality control were established, methods were validated according to modern reguirements and met them in all parameters. To assess the tablets guality tests on the characteristics of appearance, average weight and uniformity in weight, abrasion, disintegration, excipients (aerosil) were proposed. Conclusion. Methods of standardization based on HPLC with UV-detection for dosage form with original pharmaceutical substance based on benzophenone derivative for treatment of HIV-1 infection were proposed and validated.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(1):4-10
pages 4-10 views

Influence 3-formylchromone derivatives in vitro at aggregation of p-amyloid plagues and tyrosinase activity

Pozdnyakov D.I., Rukovitsyna V.M., Larskij M.V.


Objectives. Alzheimer's disease is one of the most common terminal forms of dementia, characterized by a complex pathogenesis with the formation of amyloid plagues in the brain structures. At the same time, one of the new and promising areas of Alzheimer's disease therapy is the influence on the amyloidogenic cascade. Aim of the study. In vitro to evaluate the effect of ten 3-formylchromone derivatives on the formation of p-amyloid aggregates and tyrosinase activity. Materials and methods. The effect of the studied compounds on tyrosinase activity was evaluated using the Mapunyamethod, using L-tyrosine as a substrate and kojic acid as a reference. Aggregation of amyloid plagueswas studied spectrophotometrically in reaction with Congo red after three and six days of incubation. Results. Among the test-objects, the most significant antithyrosinase properties were found in the 6-acetyl substituted derivative of 3-formylchromone, whose IC50 value was comparable to kojic acid (32±1.913 pg/ml versus 30.2±1.599 pg/ml). Also, this compound most significantly inhibited the aggregation of amyloid plagues on the third day of incubation-31.0% (p<0.05) and 61% (p<0.05) - on the sixth day. It should be noted that 3-formylchromone and oxime of this compound had no significant effect on tyrosinase activity and amyloidogenesis. Conclusion. This study suggests the relevance of further study of 6-acetyl-substituted 3-formylchronome as a potential means of pathogenetic therapy of Alzheimer's disease.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(1):11-15
pages 11-15 views

Features of accumulation of biologically active substances by leaves of the large plantain growing in various urban and agrobiocenoses of Voronezh region

Dyakova N.A.


Relevance. An important and little-researched aspect of the effect of human economic activity on medicinal plants is that in response to an increase in anthropogenic load, additional synthesis of secondary metabolites is induced with different intensities. The purpose of the study was to study the accumulation of biologically active substances in the leaves of the large plantain, collected in various agricultural and urbobiogeocenoses of the Voronezh region from the point of view of anthropogenic impact. Material and methods. In the framework of the study, 51 samples of plantain leaves of a large scale determined the content of polysaccharides and extractive substances extracted by 70% alcohol. Results. All samples meet the existing reguirements of regulatory documentation on the content of determined groups of biologically active substances. The lowest content of polysaccharides was noted for samples collected under high-voltage power lines, near the industrial enterprises of Minudobrenia 0JSC, along and at a distance of 100 m from the A144 route in the Anninsky district, along and at a distance of 200 m from the M4 highway in the Ramonsky district. The decrease in the content of this group of biologically active substances can be associated with the suppression of biosynthetic processes in the plant as a result of significant anthropogenic effects. At the same time, leaves of a large plantain with a high polysaccharide content (more than 20%) were harvested in a number of urboce-noses - in Ostrogozhsk, Elan-Koleno, at a distance of more than 100 m from a non-fast highway, at a distance of 300 m from the railway, where, probably, human economic activity has less impact on the habitat of the producing plant. In a number of urbanized areas, large plantain leaves were selected with a content of extractive substances extracted by 70% alcohol exceeding their concentration in samples of protected areas, which can be associated with induction of synthesis in conditions of habitat contamination stressful for the plant as a result of anthropogenic effects of biologically active compounds extracted by 70% alcohol. In this case, we are probably talking about stimulating the biosynthesis of polyphenol compounds (flavonoids, etc.), which are key secondary metabolites that have membrane-stabilizing effects under conditions of oxidative stress.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(1):16-21
pages 16-21 views

The role of PCSK9 in the regulation of lipoprotein transport (review)

Chaulin A.M., Duplyakov D.V.


The article summarizes the role of the new type 9 subtilisin-Kexin protein convertase (PCSK9) in the regulation of lipoprotein transport. Impaired transport, characterized by excessive serum cholesterol and low-density atherogenic lipoproteins, is a key risk factor for the development of atherosclerosis and cardiovascular diseases. Due to the fact that PCSK9 causes degradation of low-density lipoprotein receptors and increases the level of atherogenic low-density lipoproteins, PCSK9 has become a new target for the development of therapeutic drugs for the treatment and prevention of cardiovascular diseases. At the same time, review articles on PCSK9 do not pay enough attention to ITS additional role in regulating lipoprotein transport. In this regard, this review discusses the effects of PCSK9 on other receptors involved in lipid metabolism, further study of which is of great practical importance in the future.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(1):22-30
pages 22-30 views

Prospects for applications of nanodiamonds in medicine (review)

Berdichevskiy G.M., Vasina L.V., Ryumina E.V., Sharoyko V.V., Semenov K.N.


Nowadays, detonation nanodiamonds are considered by researchers as promising nanocarriers in the fields of biologically active substances and drug delivery systems. The possibility of using detonation nanodiamonds in biomedicine is due to the presence of a set of unigue physicochemical properties, namely: nanodiamonds have a large specific surface area, stable fluorescence, biocompatibility, the ability to adsorb or conjugate with drugs. These properties of detonation nanodiamonds determine their use to create biomarkers, biosensors, highly effective adsorbents, catalysts for deactivation of toxins, dental composite materials. The procedure for standardisation and unification of industrially produced detonation nanodiamonds significantly expands the prospects for their application in medicine. The purpose of this review is to analyse the works of domestic and foreign scientists, which consider the use of detonation nanodiamonds not only as nanocarriers in delivery systems of cytostatics for the treatment of cancer, but also for the targeted delivery of a number of drugs for the treatment of other pathologies. The review article will be useful for specialists working in the field of nanomedicine and nanoengineering.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(1):31-37
pages 31-37 views

Changes in the composition of complex proteins in subcellular fractions of syncytiotrophoblast in placental insufficiency

Pogorelova T.N., Gunko V.O., Nikashina A.A., Palieva N.V., Kaushanskaya L.V., Degtyareva A.S.


Relevance. Regulatory processes in the placenta, controlled by the metabolism of its proteins, play an important role in ensuring the normal course of pregnancy and fetal development. Violations of these processes can lead to failure of the placenta, which occupies a leading place among complications of gestation. The aim of study: to study the composition of complex proteins in the subcellular fractions of placental syncytiotrophoblast in placental insufficiency (PI). Material and methods. The material of the study was the placental tissue, the subcellular fractions of syncytiotrophoblast of which were obtained by differential ultracentrifugation in a sucrose gradient. Proteins were separated by polyacrylamide gel electrophoresis. Quantification of glyco-, lipo- and nucleoproteins was carried out densitometrically after their specific staining. Results. Disruption of the production of these proteins in PI was established, depending on their nature and the nature of the cell fraction. Most of all proteins are characterized not only by a decrease in the level, but also by redistribution in zones with different molecular weights, as well as a modification of electrophoretic mobility. Along with differences in the composition and properties of apoproteins, disorders also affect non-protein components that are part of complex proteins: nucleic acids, phospholipids, oligosaccharide structures of glycoproteins. These changes are reflected in the regulatory functions of complex proteins in the placenta. Conclusion. The revealed damages are obviously important links in the chain of molecular-cellular disorders, accompanied by the development of PI.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(1):38-42
pages 38-42 views

Development of a method for selective assessment of complement microbicidal activity in human blood serum

Legkovoy S.V., Umnyakova E.S., Berlov M.N.


Background. The ability of blood serum to suppress viability of microorganisms is primarily implemented by the presence of cationic factors (e.g. lysozyme, p-lysine, etc.) and complement system proteins. The complement itself is only able to cause lysis of some gram-negative bacteria, while cationic factors are predominantly active against gram-positive ones. The study of the contribution of individual antimicrobial components of blood serum and their combined action to its microbicidal activity would help to expand the understanding of the molecular mechanisms of innate immunity. The aim of the study. Development of a method for selective depletion of cationic factors from serum while preserving the functional activity of the complement system. Materials and methods. Pooled blood serum from healthy donors was used as the starting material. The depletion of cationic molecules from blood serum was performed by its incubation with a suspension of carboxymethylcellulose. In order to find the optimal conditions for binding of cationic proteins and peptides, either the NaCI concentration in the sample or the volume of the applied polymer suspension were varied. Removal of cationic factors from the serum was evaluated by the residual activity of lysozyme. The retention of complement was evaluated by serum hemolytic activity against rabbit red blood cells. The bactericidal activity of native and depleted serum against the gram-positive bacterium Listeria monocytogenes EGD was also compared. Results. Incubation of serum with carboxymethylcellulose suspension taken in egual volume in the presence of 0.1 M NaCI allowed effective removal of cationic polypeptides without evident changes in complement functional activity. Antimicrobial activity of the serum depleted of cationic factors was remarkably lower compared with the native blood serum. Conclusions. A method for selective removal of cationic factors from blood serum was developed. The described procedure allows evaluation of the complement microbicidal activity independently on the action of antimicrobial serum cationic polypeptides.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(1):43-48
pages 43-48 views

Antioxidant activity of the dry extract from Silene jeniseensis Willd at experimental immunodeficiency

Khalzanova A.V., Toropova A.A., Khobrakova V.B.


Rationale. Many vital metabolic and physiological processes occurring in the body are closely related to free radical oxidation. Toxic peroxide free radicals and reactive oxygen species damage important structural and functional proteins and lipids, enzyme and membrane systems of cells that results in the suppression of the functional activity of immunocompetent cells and emergence of various immunopathological processes. The use of new immunomodulators based on plant raw materials with antioxidant activity is relevant for their correction. The aim of this work is to evaluate the antioxidant properties of the dry Silene jeniseensis Willd extract in experimental immunodeficiency. Material and methods. Studies were conducted on Fl(CBAxC57BI/6) mice. Immunodeficiency was simulated by intraperitoneal administration of cyclophosphamide. S. jeniseensis extract was administered at a dose of 100 mg/kg in association with cyclophosphamide. The intensity of lipid peroxidation and the state of the endogenous antioxidant system were evaluated by determining of the malonic dialdehyde (MDA) and reduced glutathione (GSH) content and catalase activity in the spleen homogenate. The membrane-stabilizing activity was evaluated using a model of peroxide hemolysis with a suspension of red blood cells from donor blood. Antiradical activity was determined by the ability of the remedy to bind 2,2'-diphenyl-l-picrylhydrazyl (DPPH'), 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS,+), superoxide anion radical (О2”) and Fe2+. Results. The introduction of S. jeniseensis extract reduced the severity of oxidative stress in immunosuppression: the MDA content decreased by 2.0 times; the catalase activity and GSH content increased by 2.3 and 1.5 times, respectively, compared to the level of suppression. S. jeniseensis is characterized by pronounced membrane-stabilizing activity, shows the anti-radical effect against DPPH1, ABTS’+ and O2” radicals, also it has Fe2+- chelating activity. Conclusions. S. jeniseensis extract has a pronounced antioxidant activity in experimental immunodeficiency which is manifested by the decrease of the malonic dialdehyde concentration, increase of catalase activity and increase of the reduced glutathione content, also it has the membrane-stabilizing and anti-radical effects.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(1):49-55
pages 49-55 views

ANDREY ROBERTOVICh GRABEKLIS (k 50-letiyu so dnya rozhdeniya)

- -.
Problems of Biological Medical and Pharmaceutical Chemistry. 2021;24(1):56-56
pages 56-56 views

This website uses cookies

You consent to our cookies if you continue to use our website.

About Cookies