Problems of Biological Medical and Pharmaceutical Chemistry

Introduction. The development and validation of analytical methods are one of the most important stages in the development of a new drug. As part of the implementation of the scientific research plan, the VILAR has developed a method for obtaining a dry extract Serratula coronata herb and its adaptogenic activity has been proven.

The purpose of the study was to develop and validate a method for the quantitative determination of 20-hydroxyecdysone to control the quality of the Serratula coronata herbal dry extract.

Materials and methods. The object of the study is a dry extract obtained by extracting dried herb with 70% ethyl alcohol, subsequent concentration, purification with chloroform, liquid-liquid extraction with n-butanol and drying of butanol extracts.

Results. As a result of the research, optimal analysis conditions were selected and validation was carried out, which made it possible to characterize it positively in terms of specificity, linearity, accuracy, reproducibility, and intra-laboratory precision.

Conclusions. The developed method is suitable for the quantitative determination of 20-hydroxyecdysone in the Serratula coronata herbal dry extract and can be used in drawing up a regulatory document for this substance.

Purpose. To conduct a comparative analysis of the qualitative composition and quantitative content of components of essential oils isolated from different organs of Artemisia santolinofolia, and also to study the influence of weather conditions on the accumulation and composition of essential oils.

Material and methods. The object of the study is the aerial part of A. santolinifolia, collected in the Okinsky district of the Republic of Buryatia during the flowering phase, in August 2016, 2017, 2019. Essential oils were isolated by hydrodistillation. The component composition was determined by chromatography-mass spectrometry with an Agilent Packard HP 6890 gas chromatograph with a quadrupole mass spectrometer (HP MSD 5973N).

Results. The highest content of essential oils is in inflorescences (0.7%) and leaves (0.7%), less in the aerial parts (0.5%) and stems (0.4%). Monoterpenoids mainly accumulate in inflorescences, sesquiterpenoids are mostly found in leaves and stems. Dominant components characteristic of all parts of the plant: 1,8-cineole (1.5–9.1%), terpineol-4 (0.7–2.8%), bornyl-2-methylbutonoate (1.5–1.8), camphor (0.4–39.5%), borneol (0.7–6.4%), bornyl acetate (3.1–5.0%), davana ether (isomer 1) (1.9–5.3%), davana ester (isomer 2) (1.1–3.2%), davanone (0.6–12.4%), caryophiollene (0.5–2.0%), bicyclogermacrene ( 0.7–6.2%), spatulenol (0.8–19.9%). The hydrothermal coefficient (HTC) was calculated and a positive correlation between HTC and the content of essential oil in the raw material was shown.

Conclusions. For the first time, the component composition of essential oils isolated from the inflorescences, leaves, and stems of Artemisia santolinofolia was studied; 60 compounds related to mono- and sesquiterpene compounds were identified. The dominant components of essential oils were identified. A study of the dynamics of accumulation showed that oils are contained in all organs of the plant, therefore the entire above-ground part of the plant is collected; the optimal period for collecting raw materials is the flowering phase. The content of essential oils depends more on the amount of precipitation than on the average monthly temperature.

Introduction. When producing alcohol, only the starch is extracted from the grain; the remainder of the grain containing various biologically active substances (BAS): proteins and amino acids, reducing substances, uronides, flavonoids, lipids, vitamins and provitamins, with added enzymes is called post-alcohol grain grains, its volume is 12-13 times greater than the volume of alcohol and practically not used. To substantiate the prospects for the pharmaceutical use of grains, two areas of processing have been proposed: to obtain total biologically active substances (“Biobardins”) and individual betaine hydrochlorides with different pharmacological properties. The assumption that the cause of grains spoilage is labile biologically active substances, the isolation of which will determine the stability of grains, requires experimental confirmation.

The purpose of the work is to study the chemical and microbiological safety of grains (wheat, corn, barley, millet) before and after its processing (after obtaining Biobardins and betaines).

Material and methods. The object of the study is various types of grain grounds (wheat, corn, barley, millet) produced in 2021–2022 by distilleries in the Stavropol Territory. We studied the chemical safety of industrial waste according to the integral and most informative indicator of anthropogenic environmental pollution - the indicator “chemical oxygen consumption” (COC), determined by dichromatometry. Microbiological quality control of grain grounds was carried out in accordance with the requirements of general pharmacopoeial monograph GPM.1.2.4.0002.18 “Microbiological purity” of the State Pharmacopoeia of the Russian Federation XIV.

Results. The indicator of “chemical oxygen consumption” (COC), which characterizes the chemical safety of waste and determined by dichromatometry, decreased by 4.1 times (by 75.6%) when obtaining Biobardinov from stillage (from 54503 to 13205 mg O/l), and when obtaining betaines - 3.5 times (by 71.4%) (from 54503 to 15490 mg O/l). In both options, the recycled grains corresponds to non-hazardous industrial waste. According to the results of specific qualitative reactions, the processed grains contains no biologically active substances characteristic of the original grains: proteins and amino acids, reducing sugars, uronides. Microbiological control of the processed grains also confirmed its microbiological safety in terms of the content of aerobic bacteria, enterobacteria, fungi and the absence of Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella.

Conclusion. Thus, the use of various types of post-alcohol grain grains as pharmaceutical raw materials for the production of total and individual medicines made it possible to solve 2 problems: to use grains as a medicinal raw material and to reduce the technogenic impact of grains on the environment.

Objective is a study of the effectiveness and safety of using a "Florenta" dietary supplement based on Siberian fir extract as an interferon inducer in the complex therapy of acute respiratory viral infections.

Material and methods. The object of the study was a biologically active food supplement based on a concentrated aqueous extract of Siberian fir needles (Abies sibirica L.). The patients under observation were adults with various manifestations of acute respiratory viral infection (ARVI). The patients were matched in age, gender and concomitant pathology.

During the study, vital signs were monitored and tolerability and possible adverse events were recorded. The results of laboratory parameters were assessed and an overall evaluation of the effectiveness of therapy and patient satisfaction with treatment results was made.

Results. It has been established that the Siberian fir extract included into the treatment of patients with mild to moderate ARVI allows managing the clinical symptoms of the disease in a shorter time and increasing the effectiveness of complex therapy. At the same time, the risk of complications is reduced and the prognosis for the disease course becomes positive. The drug under study has been proven to be well tolerated and safe. Analysis of interferon status has revealed a significant improvement in the parameters of interferons under study.

Conclusions. As a result of the studies, it has been found out that a biologically active food supplement based on Siberian fir extract as part of complex therapy for ARVI reduces the severity and intensity of symptoms of the disease, accelerates the recovery of patients and leads to the normalization of their interferon status.

Introduction. It is urgent to search for plants that can become sources of biologically active substances for the creation of new highly effective and safe medicines. One of these plants is the crowned sickle (Serratula coronata L.). The value of crowned serpuha is determined by its high content of phytoecdysteroids and flavonoids.

The purpose of the work is to study the acute toxicity, anti-inflammatory activity and capillary-strengthening effect of the flavonoid fraction of the herb Serpucha crown.

Material and methods. In the Department of Experimental Pharmacology of the Federal State Budgetary Institution VILAR, a study of the pharmacological activity of the flavonoid fraction of the herb Serpucha crowned was carried out. Acute toxicity parameters were assessed using the Kerber method. The toxicity class of the test substance was determined according to GOST 12.1.007-76 "Harmful substances. Classification and general safety requirements." The anti-inflammatory effect of the flavonoid fraction of the herb Serpucha crown was studied in models of formaldehyde edema and interstitial edema. The effectiveness of the anti-inflammatory effect of the flavonoid fraction of the herb crowned serpentine in vitro experiments was assessed by the rate of the enzymatic reaction catalyzed by inducible NO synthase. The activity of the iNOS enzyme in experiments was assessed by the rate of the reaction catalyzed by iNOS in vitro at 37 ^oC. The study of the capillary-strengthening effect of the flavonoid fraction of the herb Serpucha crowned was carried out according to the "Method for determining the reactivity of skin capillaries to inflammatory stimuli" on a model of local inflammatory reaction (xylene inflammation) in rats.

Results. When studying the acute toxicity of the flavonoid fraction of the herb Serpucha crown, LD₅₀ values were not established, since doses of the studied extract administered into the stomach of mice did not cause death of the animals. In accordance with the classification of toxicity of chemical substances according to GOST 12.1.007-76 "Harmful substances. Classification and general safety requirements", the flavonoid fraction of the herb crowned Serpucha is a low-hazard substance. As a result of the analysis of the data obtained, it was established that the flavonoid fraction of the herb serpukha crowned in doses of 100 and 200 mg/kg has an anti-inflammatory effect, significantly reducing formaldehyde edema in animals by 18 and 20%, respectively, compared with the control group of animals. It was established that the flavonoid fraction of the herb Serpucha crowned at a dose of 200 mg/kg has a pronounced anti-exudative effect, significantly reducing interstitial edema in animals by 22% compared to the control group of animals. In vitro experiments, the flavonoid fraction of the herb Serpucha crown inhibits the rate of the iNOS reaction by 1.5 times compared to the control, which indicates the presence of pronounced anti-inflammatory activity of this sample. The studied fraction has a pronounced capillary-strengthening effect under the conditions of an experimental model of xylene inflammation, reducing the permeability of the vascular wall.

Conclusions. The results of the studies indicate that the flavonoid fraction of the herb Serpucha crown, in terms of acute toxicity, belongs to the category of low-hazard substances and has a pronounced anti-inflammatory and capillary-strengthening effect.

Introduction. An important direction in the biotechnology of plant cell cultures is the search for factors and influences that contribute to increasing the accumulation of pharmacologically valuable metabolites in them, including polyphenols. These factors include light, the effect of which activates the processes of photomorphogenesis in in vitro cultures, regulates their differentiation and metabolic processes. All this depends on the intensity of the light flux, the origin of the cells and tissues cultivated in vitro, as well as the economic value of the synthesized plant metabolites. One of the promising pharmacologically valuable crops are tea plants (Camellia sinensis L.), as well as callus cultures initiated from them, which are characterized by the accumulation of various polyphenols, including flavans – substances with P-vitamin capillary-strengthening activity.

The aim of the study was to compare the effect of different light intensity on the morpho-physiological characteristics of tea callus cultures, as well as the accumulation and localization of polyphenols in them.

Material and methods. The object of the study was tea callus cultures of stem origin grown for 40 days at light intensity: 50 µmol·m^-2·s^-1, 75 µmol·m^-2·s^-1 and 100 µmol·m^-2·s^-1 (low, medium and high intensity, respectively). Morphophysiological parameters of calluses (color, density, water content), the total phenolics and flavans content in them, as well as their localization were analyzed.

Results. The cultivation of tea calluses in the light was accompanied by their changing-over to photomorphogenesis, which manifested itself in the greening of the cultures and the chloroplasts formation in cells. The greatest efficiency of this process was noted at the high light intensity, which correlated with the maximum accumulation of polyphenols and flavans, exceeding that in cultures grown at lower light flux values. Consequently, the cultivation of tea callus cultures at different light intensities makes it possible to regulate the polyphenols accumulation in them – biologically active plant metabolites with antioxidant activity.