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Vol 25, No 2 (2022)

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Peptide therapy in clinical pharmacology: current state and promising directions of development

Arkhincheeva N.T., Balkhaev I.M.


Insulin therapy initiated the use of peptides in incurable diseases at the beginning of the 20th century. Over time, peptide science has evolved in sync with other scientific discoveries and has finally expanded its view beyond the traditional focus on human endogenous peptides to reveal a broader range of peptide agents identified from other resources or through medicinal chemistry. The article is a literary review of publications in the Russian scientific electronic library eLIBRARY and in the PubMed library of the USA National Center for Biotechnology Information (NCBI). As a result of the analysis, the formulation of peptide therapy, the current state of the development of peptide therapy, the strengths and weaknesses of peptides as drugs, and emerging new opportunities in the design and development of peptide drugs are outlined.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(2):3-6
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Investigation of phenolic compounds of the jerusalem artichoke herbs (Helianthus tuberosum L.)

Saybel O.L.


Relevance. Jerusalem artichoke (Helianthus tuberosum L.), is a valuable food crop grown in many countries of the world and has multiple uses in the food industry and animal husbandry. The main raw material of Jerusalem artichoke is tubers, when harvesting the grass, as a rule, is utilized. The herb has a significant biomass and contains phenolic compounds. The aim of the study was to analyze the phenolic complex of Jerusalem artichoke herb and assess the prospects for its use as a medicinal plant material. Material and Methods. As a result of the studies carried out by HPLC-UV-MS/MS, 18 compounds related to hydroxycinnamic acids and flavonoids were identified. The dominant substances are chlorogenic, isochlorogenic A and isochlorogenic C acids. Results. Using the method of direct spectrophotometry, a method has been developed for the quantitative determination of the sum of phenolic compounds in terms of chlorogenic acid. The content of these compounds ranges from 4.88 ± 0.22 % to 7.47 ± 0.35 %, the accumulation is carried out mainly in the leaves. Conclusion. The highest content of chlorogenic acid is also observed in Jerusalem artichoke leaves and is 2.65 ± 0.08 %. Thus, Jerusalem artichoke herb harvested at the end of the growing season is of interest for further research and creation on pharmaceutical substances. At the same time, this will make it possible to purposefully process the secondary raw materials formed during the cultivation of tubers and ensure the comprehensive use of Jerusalem artichoke.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(2):7-13
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Investigation and validation of quantitative analysis of phenolic compounds and chlorogenic acid in the Vaccinium uliginosum leaves

Shamilov A.A., Bubenchikova V.N., Garsiya E.R., Ibaeva K.A., Larsky M.V.


Relevance. The modern requirements of qualitative control of medicinal plant raw material recommends to evaluate total amount of biological active compounds and amount of major substances. Aim. Investigation and validation of quantitative analysis of total amount of phenolic compounds and major substance chlorogenic acid in the Vaccinium uliginosum leaves. Materials and methods. Quantitative analysis of total amount of phenolic compounds in the V. uliginosum leaves was carried out by spectrophotometry. Amount of chlorogenic acid was measured by capillary electrophoresis as main method and by high-performance liquid chromatography as comparative method. Developed methods were validated. Results. We investigated and validated methods of spectrophotometric analysis of total amount of phenolic compounds and quantitative analysis of chlorogenic acid by capillary electrophoresis. Total amount of phenolic compounds were 4.94±0.17% - 9,09±0,17%, amount of chlorogenic acid - 1.75±0.08% - 4.34±0.16% Conclusions. Medicinal plant raw material - Vaccinium uliginosum leaves -are recommended to be standardized by total amount of phenolic compounds and amount of major substance - chlorogenic acid - using spectrophotometry and capillary electrophoresis respectively. Total amount of phenolic compounds calculated to g chlorogenic acid at 100 g of raw material should be no less 4.5%, amount of chlorogenic acid - no less 1.5%.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(2):14-23
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The study of the physico-chemical properties of the substance efavirenz

Zolotov S.A., Ponomarev E.S., Dain I.A., Demina N.B., Zolotova A.S., Retivov V.M., Buzanov G.A.


The aim of the work was to study the physicochemical properties of the domestic active pharmaceutical substance efavirenz produced by AMEDART LLC of the Russian Federation. Modern methods are used: differential scanning calorimetry, X-ray powder diffraction, spectral emission microscopy, high performance liquid chromatography, etc. The melting point, lipophilicity coefficient, wave numbers, shape and size of crystal particles, solubility in the biological pH range and in some organic solvents were determined. It has been established that the studied API has a minimum endothermic peak in the region of 140°C, the obtained lipophilicity coefficient is 4.67, it is practically insoluble in aqueous media in the biological pH range, but it is well soluble in most polar organic solvents, such as: methanol, ethyl alcohol, acetone and tetrahydrofuran, has a crystalline structure in the form of sticks from 3 to 18 microns and irregularly shaped particles from 1 to 7 microns in size, as well as wave numbers - angles of 6.1, 6.4, 10.4, 11.0, 12.3, 13.3, 14.2, 16.9, 20.1, 21.3, 24.9. DSC, IR spectrometry and X-ray powder diffraction data showed that the substance is a polymorph form I.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(2):24-29
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Comparison of the rate of release of active substances from solutions of hydroxymethylpropyl cellulose and hydroxyethyl cellulose for selecting the optimal polymer for the development of ear drops

Ghadeer B., Martceva D.S., Zhilyakova E.T., Boyko N.N., Abdulhadi A.B., Wissam M.D.


Drops are a liquid dosage form, which can go out of target place, so the use of a substance that gives the drops viscosity which prevents solution of drops to go out of place of applications, as polymers which are very important but that use may effect on release of active ingredients in drops, so in this study we studied the effect of used HPMC which is polymer used for viscoelastic, as well as an excipient and controlled-delivery component in ear drops. The aim of the work was to compare the rate of release of active substances from solutions of hydroxymethylpropyl cellulose and hy-droxyethyl cellulose, as the choice of the optimal polymer for the development of ear drops. We have studied the use of HPMC and HEC polymer for obtaining viscoelastic liquid dosage forms in the form of ear drops, as excipients that control the release. For the analysis, ofloxacin was chosen as active substances, in view of its high activity on microorganisms that cause otitis media, and HPMC and HEC, ethyl alcohol 96% and purified water were used as auxiliary substances in the analyzed compositions. To determine the viscosity of solutions, we have chosen a glass capillary viscometer VPZH-2, in accordance with the recommendation of the State Pharmaceutical Organization. The release was carried out by equilibrium dialysis through a semiper-meable membrane using a regenerated cellulose tubular membrane (model T3). The HPLC method was used to identify the active substance. In view of the data obtained on the release of the active substance, for the development of the composition and technology of ear drops, as an auxiliary component, we chose HPMC.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(2):30-34
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Effect of metabolic type of obesity on blood microbiome

Shestopalov A.V., Kolesnikova I.M., Gaponov A.M., Grigoryeva T.V., Khusnutdinova D.R., Kamaldinova D.R., Volkova N.I., Makarov V.V., Yudin S.M., Rumyantsev A.G., Rumyantsev S.A.


Background. Recent studies have shown a significant role of the gut microbiome in various pathologies including obesity. It is assumed that the gut microbiome is one of the sources for the formation of the blood microbiome. Obesity is associated with changes in the gut microbiome, which may also affect the blood microbiome. It is customary to distinguish between metabolically healthy obesity (MHO) and metabolically unhealthy obesity (MUHO) depending on the metabolic complications risk. Aim. To study the influence of the metabolic phenotype of obesity on the blood microbiome formation. Materials and methods. The study included 116 healthy donors and 101 obese patients. Depending on the metabolic type of obesity, the obese patients were divided into subgroups with metabolically healthy obesity (MHO, n=36) and metabolically unhealthy obesity (MUHO, n=53). Quantitative and qualitative assessment of the blood microbiome was based on metagenomic analysis. Blood samples were used to isolate DNA and perform sequencing of the variable v3-v4 region of the 16S rRNA gene. Results. In patients with MHO, the characteristics of the alpha-diversity of the blood microbiome were like those of healthy donors. However, MUHO is associated with an increase in the blood microbial diversity. The main phyla of the blood microbiome were Bacteroidetes, Firmicutes, Proteobacteria, and Actinobacteria. Cyanobacteria, TM7, Thermi, Verrucomicrobia, Chloroflexi, Acidobacteria, Planctomycetes, Gemmatimonadetes, and Tenericutes were found to be less significant phyla of the blood microbiome. Phyla Acidobacteria, TM7 and Verrucomicrobia were more often isolated in blood samples of patients with MUHO compared with healthy donors. Conclusion. MUHO linked to increased diversity of the blood microbiome. This appears to be due to increased microbial translocation from the intestine and non-intestinal sources.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(2):35-41
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Estimation of enzyme catalytic activity in bioptates of lower limb varicose deformed veins depending on the severity of chronic venous insufficiency

Minaev A.V., Vavilova T.P., Alekberova G.I., Yamaletdinova G.F., Abduvosidov K.A.


Relevance. Varicose veins of the lower extremities are recognized as one of the most common pathologies of the venous system of the lower extremities. Along with various involutive and morphological changes occurring in the venous wall, changes at the molecular level play a key role in pathogenesis. The content of various biologically active substances directly in the varicose vein wall, reflecting the speed of biochemical processes, has not been practically studied. Aim. To study the catalytic activity of lactate dehydrogenase and creatine kinase in biopsy specimens of the vein wall in patients with varicose disease of the lower extremities of different classes of chronic venous insufficiency according to the CEAP classification. Matherials and Methods. In the experiment, tissue of the venous wall taken from 141 patients with varicose disease of the lower extremities of classes C2-C6 (according to the CEAP classification) was studied. All examined patients were divided into 4 groups depending on the severity of the disease. Determination of enzyme activity was performed by spectrophotometric method. Results. An increase in the activity of lactate dehydrogenase and a decrease in the activity of creatine kinase were revealed as the disease progressed. A positive correlation was found between lactate dehydrogenose activity and the class of chronic venous insufficiency and a negative correlation between creatine kinase activity and the class of chronic venous insufficiency. Conclusions. An increase in the catalytic activity of lactate dehydrogenase and a decrease in the activity of creatine kinase in biopsies of varicose veins of the lower extremities are directly related to the progression of the disease, which is explained by the predominance of anaerobic processes over aerobic ones in the varicose deformed venous wall, an increase in tissue hypoxia and a decrease in energy supply.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(2):42-48
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Dipeptide BDNF mimetic GSB-106 prevents depression-like behavior and cognitive impairment caused by ischemic stroke in rats

Povarnina P.Y., Nikiforov D.M., Vorontsova O.N., Gudasheva T.A.


Relevance. Depression and cognitive impairment are common complications of acute cerebrovascular accidents. Disorders of hippocampal neuroplasticity associated with a decrease in BDNF expression are considered as one of the causes of these complications. A dimeric dipeptide mimetic of the BDNF loop 4, (bis (N-monosuccinyl-L-seryl-L-lysine) hexamethylenediamide) (GSB-106) was created at the V.V. Zakusov Research Institute of Pharmacology. GSB-106 demonstrated antidepressant, neuroprotective and neuroregenera-tive properties in in vivo experiments. Objective. Experiments were performed on 40 male rats Wistar weighing 240-280 g. Purpose of the study is to investigate the effect of GSB-106 on depression-like behavior and memory impairments in rats induced by middle cerebral artery occlusion (MCAO). Material and methods. GSB-106 was injected intraperitoneally at a dose of 0.1 mg/kg for 21 days after surgery. Depressive-like be havior was detected in the forced swimming test, and memory impairments - in the novel object recognition test. Conclusions. GSB-106 is a promising compound for further development as a drug for the treatment of post-stroke depression and cognitive impairment.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(2):49-53
pages 49-53 views

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