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Vol 25, No 8 (2022)

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The main directions of pharmaceutical development of phytoecdy-steroid preparations (review)

Molokhova E.I., Lipin D.E., Sorokina Y.V.


Phytoecdysteroids (phytoecdysones) are polyhydroxylated sterols identical to arthropod hormones that have a wide range of pharmacological effects. Goal of review is to systematize information sources on the search for promising sources of raw materials for the isolation of phytoecdysteroids and the creation of drugs based on them. It has been found that plants representatives of families Caryophyllaceae, Lamiaceae genus Ajuga, Asteraceae genus Serratula are of interest as traditional medicinal plant raw materials representatives. The prospects of producing of phytoecdysteroids using the hairy roots culture are shown. The review shows the nomenclature of medicinal products and BAA based on phytoecdysteroids. Trends in the creation of effective dosage forms that increase the biological availability of phytoecdysones, including the development of nanoscale complexes, are highlighted.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(8):3-9
pages 3-9 views

Biocatalysis as a tool for optimizing pharmaceutical synthesis of drugs (review)

Pechinskii S.V.


Relevance. Competitiveness and recognition of Russian drugs in the pharmaceutical market is possible only if the domestic product and its technology are inscribed in the paradigm of the development of advanced global pharmaceutical production, the priority drivers of which are environmental friendliness and economic efficiency. The introduction of "green technologies", and in particular the principles of "green chemistry", is a clear manifestation of the current trend and demand for the future in the development and production of medicines. The most interesting from a theoretical point of view and promising in practical terms is the optimization of the processes of synthesis of pharmaceutical substances through the introduction of enzyme synthesis. The goal is to show the prospects for the use of biocatalysis in the synthesis of drugs. Material and methods. The materials were scientific publications and patents devoted to modern problems and ways to solve them in the field of "green chemistry", "biocatalysis" and "synthesis of pharmaceutical substances". When writing the review, the following methods were used: systematization, comparison, analysis and generalization. Results. The review gives a brief historical description of the "waves of biocatalysis", considers the most striking examples of the modern application of enzyme catalysis in the world practice of pharmaceutical synthesis, generalizes the general prospects for the use of biocatalysis in the synthesis of drugs. The article shows that chemoenzymatic synthesis is economical, increases the purity of the target product, especially its "stereopurity", allows the synthesis of new drugs, which were previously difficult or even impossible to obtain according to classical schemes. It is concluded that, despite sufficient experimental material in related scientific fields, in our country there is practically no development of the direction on the use of enzyme synthesis in the development and production of medicines.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(8):10-23
pages 10-23 views

The development of the method to quantify the amount of the flavonoids of Leonurus deminutus v. Krecz. Herb

Sokolova Y.V., Mirovich V.M.


Relevance. Representatives of the genus Leonurus are sources of important biologically active compounds (BAQ, including phenolic ones. In the flora of Central Siberia, a plant of folk medicine is widespread - Leonurus deminutus V. Krez. To introduce a medicinal plant into medical practice, standardization of its medicinal plant raw materials (MPRM) is required. Objective. The development of the method to quantify the amount of the flavonoids in the aerial part of L. deminutus and validation evaluation of the developed method. Material and methods. The object of the study was samples of aerial organs of L. deminutus collected during the blooming period in 2021 on the territory of the Irkutsk region (near the village of Ust-Ordynsky). Quantitative determination of the amount of flavonoids was carried out by differential spectrophotometry, optimal extraction conditions were selected, contributing to the maximum yield of flavonoids. Validation was carried out according to the requirements of the OFS.1.1.0012.15 of the State Pharmacopoeia of the Russian Federation of the XIV edition. Results. Optimal extraction conditions for the quantitative determination of flavonoids in L. deminutus herb: extractant - ethyl alcohol 70%, the degree of grinding of raw materials - 1 mm, the ratio of "raw materials : extractant" - 1:100, extraction time - 60 minutes. When analyzing the extraction spectra, an analytical wave of 400±2 nm and a standard substance, cinaroside, were established. The relative error of the method was ±2,98%. Conclusion. The method to quantify the amount of the flavonoids in the aerial part of L. deminutus has been developed, a positive validation assessment of the developed method has been carried out. The validated method meets all the criteria of acceptability and can be recommended for inclusion in the regulatory documentation for this MPRM.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(8):24-30
pages 24-30 views

New thiadiazole derivatives with antituberculosis activity

Sharopov F.S., Rakhmonov R.O., Valiev A.K.


Despite to the existence of many antibiotics for the treatment of tuberculosis, the main obstacle on the way of complete liquidation of Mycobacterium tuberculosis is the acquiring of resistance for current drugs by bacteria. The search for new compounds exhibiting antituberculous activity is an important task of modern pharmacology. Molecular docking was used for the evaluation of antituberculous activity of forty thiadiazole derivatives and their interactions with the target protein CmaA1 (cyclopropanemycolic acid synthase 1). Finding out the results indicated that twenty four thiadiazole derivatives can have antituberculosis activity. Their molecular docking values were ranged from -7.4 to -9.4 kcal/mol, while the docking value of positive control (thioacetazone) was -7.3 kcal/mol. The molecules, namely 6-(4-bromophenyl)-N-cyclohexyl-imidazo[2,1-b][1,3,4]thiadiazole and 2-((6-(4-bromophenyl)imidazo[2,1-b][1,3,4]thiadiazol-2-yl)thio)-5-phenyl-1,3,4-oxodiazole have shown pronounced antituberculosis activity with values of -9.3 kcal/mol and -9.4 kcal/mol, respectively. These two molecules may be viable candidates for the development of the antituberculosis drugs.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(8):31-39
pages 31-39 views

Pharmacognostic study of the shoots of the Lespedeza bicolor growing in the Krasnodar region

Hochava M.R., Onbysh T.E., Bykova O.A.


Relevance. Be object Lespedeza bicolor Turcz. - shrub from the legume family (Fabaceae). As a medicinal vegetable raw material, shoots of Lespedeza bicolor wood as biologically active substances contain various classes of compounds (flavonoids, alkaloids, vitamins, etc.) that cause hypoazotemic, diuretic, antiviral and antimicrobial properties. The above makes it possible to consider timber shoots as a Lespedeza bicolor promising drug raw material. The purpose and object of the study: pharmacognostic study of the shoots of the Lespedeza bicolor forest growing in the Krasnodar Territory, in order to identify additional diagnostic signs that make it possible to reliably identify this raw material. Methods. The study of external and anatomical diagnostic signs and the quantitative content of extractive substances was carried out in accordance with the methods of the State Pharmacopoeia. The UV absorption spectra of the solutions were recorded on a two-beam UV-1800 spectrophotometer (Shimadzu). Results. Based on the morphological and anatomical analysis of several experimental samples of dried raw materials, a description of the morphological and anatomical signs of the shoots of the Lespedeza bicolor (leaf, leaf petiole, stem, flower) was compiled with the identification of additional diagnostic signs. It was found that the content of the sum of extractive substances in the shoots of Lespedeza bicolor timber extracted with water is 30,46%±0,81%, extracted with 40% ethyl alcohol - 32,33±0,22% and 70% ethyl alcohol -27,12±0,078%. Two minima at 260-262 nm and 310 nm are observed in the UV absorption spectrum of alcohol extraction of brine shoots; maximums at 270 nm and 315 nm, which is due to the absorption of flavonol glycosides of the quercetin series. Conclusion. The conducted studies made it possible to establish a number of diagnostic signs of authenticity and quality indicators of this vegetable raw materials, which can be considered from the point of view of their possible inclusion in the regulatory documentation.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(8):40-47
pages 40-47 views

Neuroprotective effects of hyperoside, under conditions of mitochondrial complex IV activity deficiency

Pozdnyakov D.I.


Relevance. Neuroprotection is one of the significant components of the therapy of the central nervous system diseases which are associated with a violation of energy metabolism. The immediate cause of the deficiency of the intracellular pool of macroergic compounds may be the dysfunction of the mitochondrial complex IV. Hyperoside is a flavonoid with an extensive spectrum of pharmacological activity, including potentially high neuroprotective properties. Material and methods. Mitochondrial complex IV activity deficiency was modeled in Wistar rats by intracerebral injection of 3M sodium azide solution, an inhibitor of mitochondrial complex IV. Hyperoside and the reference drug ethylmethylhydroxypyridine succinate were administered orally at a dose of 100 mg / kg, for 30 days from the moment of injection of sodium azide. After that, the intensity of pyruvate-dependent cellular respiration and changes in the concentration of mitochondrial hydrogen peroxide in the brain tissue of animals were evaluated. Results. In the course of the work, it was found that the course administration of hyperoside and a reference drug contributed to an increase in the intensity of cellular respiration, which was expressed in an increase in ATP-generating activity, the maximum level of respiration and respirometric capacity in relation to untreated animals. Also, the use of the referent and hyperoside contributed to a statistically significant (p<0.05) decrease in the content of mitochondrial hydrogen peroxide, while more pronounced changes were obtained when hyperoside was administered to animals. Conclusion. The obtained results indicate that the course administration of hyperoside in conditions of energy deficiency caused by mitochondrial complex IV deficiency increases the intensity of cellular respiration processes and prevents the generation of reactive oxygen species, which in turn may be evidence of the presence of neuroprotective action.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(8):48-52
pages 48-52 views

The effect of age-related changes on the toxicity of a dry extract of aerial part of chicory herb (Cichorium intybus L.)

Kuzina O.S., Borovkova M.V., Babenko A.N., Krepkova L.V., Lemyaseva S.V.


Relevance. Modern medicine widely uses herbal medicines in the treatment of various diseases, and the search for new medicines from plants continues to be relevant. Herbal drugs can be used for a long time in medical practice without significant side effects, however, at each stage of ontogenesis the human and animal body has a number of features affecting the metabolic processes of drugs. In this regard, there is a need for preclinical studies of drugs on animals of different ages. One of promising plants for the creation of new drugs is chicory (Cichorium intybus L.), which has a rich composition of biologically active substances, from which herb in All-Russian institute of medicinal and aromatic plants obtained dry extract. The aim to study the sensitivity of laboratory animals of different ages to a dry extract of chicory (Cichorium intybus L.) during a single injection. Methods. The study was conducted in accordance with the requirements of "Guidelines for conducting preclinical studies of drugs" on mature and immature laboratory animals of both sexes: Wistar rats aged 12 months and 3-week-old rats; BALB/c mice aged 12 months. A suspension of chicory extract was injected to animals once parenterally (intraperitoneally), then the signs of acute intoxication were recorded and the half-lethal dose (LD50) was determined using the Litchfield and Wilcoxon probit-analysis. Results. The study showed that the LD50 at a single intraperitoneal injection of the dry extract of aerial part of chicory to 12-month old mice and rats was decreased in comparison with analogous parameters in mature animals at the age of 3 months - 1,5 times on the average. For mice, these values were 2240 to 2129 mg/kg; for rats, 1443 to 2174 mg/kg. The sensitivity of immature (3-week-old) rats to the test extract was 20,6% lower than in mature animals, and the LD50 was determined to be 3280 mg/kg. Conclusion. Age-related changes in the sensitivity of laboratory animals to the dry extract of aerial part of chicory alter its toxicity parameters in different ways. Aging animals were more sensitive to the toxic effects of the extract under investigation, younger animals were less sensitive. The results obtained should be taken into consideration while developing new medicines based on these plant raw materials and their dosage forms as well as while drawing up instructions for medical use.

Problems of Biological Medical and Pharmaceutical Chemistry. 2022;25(8):53-57
pages 53-57 views

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