Vol 24, No 1 (2021)

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.

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.

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.

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.