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Vol 73, No 1 (2024)

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Pharmaceutical chemistry and pharmacognosy

Quantitative determination of procyanidins in spruce cones

Semakin D.O., Gulyaev D.K., Belonogova V.D.

Abstract

Introduction. The common spruce Picea abies (L.) of the pine family (Pinaceae) is a widespread woody plant. Fir cones are waste products of wood harvesting and seed harvesting by forestry. Also, cones are promising sources of biologically active substances.

Objective: to determine the content of procyanidins in spruce cones.

Material and methods. Spruce cones for the research were harvested on the territory of the Ilyinsky district of Perm Krai, which belongs to territories with low anthropogenic load. The preparation of samples for the study was carried out from July to March. The determination of the procyanidin content was carried out by the Porter method. Procyanidins during the reaction are oxidized to anthocyanins, colored red.

Results. Research was conducted to determine the optimal conditions for the extraction of procyanidins from spruce cones. The largest amount of procyanidins are extracted from raw materials when used as an extractant, ethyl alcohol 80%, when the raw materials are crushed to 0.5 mm, the ratio of raw materials and extractant is 1:30 and the extraction time is 40 minutes. The seasonal dynamics of the procyanidin content in spruce cones has been studied. It is established that the content of procyanidins is subject to seasonal fluctuations. The maximum content of procyanidins is observed in February, and the lowest content in July.

Conclusion. Optimal conditions for determining the content of procyanidins in spruce cones have been established. The dynamics of procyanidin accumulation in spruce cones harvested in different seasons of the year is determined. The content of procyanidins increases significantly in the autumn months and remains high until March.

Farmaciya (Pharmacy). 2024;73(1):5-9
pages 5-9 views

Investigation of the chemical composition of the domestic apple tree fruits by x-ray fluorescence analysis

Kuzmenko K.N., Krasnyuk I.I., Bokov D.O., Plahotnaya O.N., Evgrafov A.A., Rodin M.N., Kuzmenko I.A., Nesterova N.V., Samylina I.A.

Abstract

Introduction. Apple fruits are widely used in the food industry and as non-pharmacopoeial medicinal raw materials. The value of this plant is due to the presence of a large number of biologically active compounds, namely: phenols, flavonoids and tannins. Despite the abundance of information on the chemical composition of this raw material, the study of the elemental composition of apple fruits remains relevant for potential use in the treatment of element deficiency conditions.

Objective: to study the content of chemical elements using X-ray fluorescence analysis in three different parts of apple fruits – in the exocarp, mesocarp and endocarp for four varieties, as well as to identify the nitrate content and measure acidity for these apple varieties.

Material and methods. Apple tree fruits for research were harvested in the Moscow region. After preliminary ashing of the samples, the content of chemical elements was determined by X-ray fluorescence analysis with a silicon drift detector. pH and nitrate ion concentrations were measured using an EXPERT-001 pH meter.

Results. Using X-ray fluorescence analysis (XFA), the elemental composition of four varieties of domestic apple fruits was studied for various parts of the fruit. An increased content of lead was noted in the exocarp of apples of the Spartan variety. A study of the content of nitrate ions and pH was also carried out.

Conclusion. The chemical composition of domestic apple fruits was studied using X-ray fluorescence. The content of chemical elements was different in different parts of the fruit. The lowest content of chemical elements was determined in the mesocarp of the fruit. It is also worth noting the high lead content in the exocarp of Spartan apples.

Farmaciya (Pharmacy). 2024;73(1):10-15
pages 10-15 views

Antimicrobial activity of essential oil fractions of siberian fir and scotch pine

Saveleva E.E., Efremov A.A., Rukosueva T.V., Bulgakova N.A., Logunova A.K.

Abstract

Introduction. Plants of the pine family, growing mainly in the Northern Hemisphere, are of interest both from an economic and medical point of view. The antimicrobial properties of essential oils of coniferous plants are being actively studied.

Objective: to study the antimicrobial activity of the essential oil fractions of Siberian fir and Scotch pine growing in the Krasnoyarsk Territory.

Material and methods. Essential oils were isolated by hydrosteam distillation on an all-metal installation with a Clevenger nozzle. The component composition of the essential oil fractions was determined by gas chromatography-mass spectrometry. The disc diffusion method was chosen to detect the antimicrobial activity of essential oil fractions. The following test cultures were used: Staphylococcus aureus (MSSA), Staphylococcus aureus (MRSA), Escherichia coli, Pseudomonas aeruginosa, Candida albicans.

Results. In all fractions of the essential oil of Siberian fir and Scotch pine, monoterpenoids predominate, the dominant components are bornylacetate and pinene, respectively. All fractions of both oils showed antimicrobial activity against Staphylococcus aureus (MRSA), Staphylococcus aureus (MSSA) and Candida albicans. Isolated individually dominant compounds bornylacetate (Siberian fir) and pinene (Scots pine) also showed antimicrobial activity.

Conclusion. The antimicrobial activity of individual fractions of essential oils of Siberian fir and Scotch pine and the dominant components of the fractions against Staphylococcus aureus (MSSA and MRSA), Escherichia coli, Pseudomonas aeruginosa, Candida albicans was studied. The activity of the fractions is largely due to the dominant components. The fractions enriched in monoterpenoids showed the highest activity. The strain of Staphylococcus aureus (MRSA) turned out to be the most sensitive to the fractions of essential oils.

Farmaciya (Pharmacy). 2024;73(1):16-21
pages 16-21 views

Control of organic impurities in antibiotics

Kovaleva E.L., Arkhipova A.S., Terentieva O.O.

Abstract

Introduction: the international, as well as Russian Pharmacopoeia criteria for organic impurity assessment are not applicable to medicinal products obtained by fermentation, therefore the setting of limits for product-related impurities in antibiotics is not regulated by any commonly shared rules.

The aim of the study was to analyse and summariese pharmacopoeial requirements for and methodological approaches to organic impurities control in active substances and finished products of semisynthetic antibiotics, peptide antibiotics, and antibiotics obtained by fermentation.

Material and methods: the authors analysed the requirements for organic impurities control, as established by the leading world pharmacopoeias and the State Pharmacopoeia of the Russian Federation, using the example of three different groups of antibiotics (semisynthetic antibiotics, antibiotics obtained by fermentation, and peptide antibiotics). The study used comparative analysis and content analysis methods.

Results: the study demonstrated that the product-related impurity profiles of the analysed active substances and corresponding finished products often differ significantly across the leading pharmacopoeias, either qualitatively or quantitatively, and do not necessarily comply with the EMA Guideline on setting specifications for related impurities in antibiotics. The methodological approaches to product-related impurity control also differ a lot in terms of pharmacopoeial reference standards used, accelerated stability studies, etc.

Conclusion: the complex composition of product-related compounds does not always allow for their unambiguous classification as either impurities or active moieties (e.g. in the case of bleomycin). Most Russian Pharmacopoeia antibiotic monographs are harmonised with the European Pharmacopoeia (Ph. Eur.), which is fraught with problems regarding reference standards (RSs) use, since the composition of Ph. Eur. RSs includes both the active substance and several (sometimes up to 8) impurities. The Russian Pharmacopoeia monographs on antibiotics obtained by a process involving the fermentation stage, include the abnormal toxicity test, which seems redundant in comprehensive impurity control, at least for semisynthetic antibiotics.

Farmaciya (Pharmacy). 2024;73(1):22-34
pages 22-34 views

Organization and economy

Innovations and methodologies in research on problematic issues of drug supply

Kabakova T.I., Goryachev A.B., Barkaev G.S., Iyro I.N., Magomedova F.T.

Abstract

Introduction. Increasing the efficiency of research in the field of organizing drug supply to the population is a priority task of pharmaceutical science. The study of the structure of scientific knowledge seems to be a relevant direction for its development. However, a methodological analysis of scientific works on the problems of drug supply has not previously been carried out as an independent study.

Purpose of the study: analysis of theoretical and methodological solutions in scientific works on the problems of drug supply.

Material and methods. Using the PICO tool, we formed an array of 61 dissertations defended in the period from 1991 to the present, on the problems of drug supply. The resulting array was studied using the methods of content analysis, grouping, graphical, comparative and scientometric analysis.

Results and discussion. It was found that during the study period, 34 types of innovations were used with a total frequency of their use in 53 cases. The average number of innovation types used was 2.97 per study. In total, scientists used 53 types of methodologies, of which 14 types were directly related to the field of drug supply. 226 cases of using various types of methodologies were identified, with the average number of their use per study being 3.68. The analyzed array contains 81 names of methods and groups of methods. The total frequency of their use was 531 cases, and the average number of methods per 1 dissertation was 8.69. In works on the problems of drug supply, 242 names of scientists and predecessors of the dissertation candidates were mentioned. 313 cases of their mention were identified, which amounted to an average of 5 names per dissertation. As a result, a methodological profile of scientific research on the problems of drug supply was formed using four analytical blocks.

Conclusion. Data were obtained on the constant scientific interest of scientists in problematic issues of improving the drug supply system. The presence of reserves for expanding the boundaries of the scientific field of pharmaceutical science has been established.

Farmaciya (Pharmacy). 2024;73(1):35-43
pages 35-43 views

Modern methodological approach to the assessment of the individual quality of life of hiv-infected patients

Petrov A.G., Glembotskaya G.T., Khoroshilova O.V.

Abstract

Introduction. The study of the quality of life (QOL) of HIV-infected patients in the system of personalized and specialized pharmaceutical care is a fundamentally new method that allows us to study the multidimensional picture of the patient's subjective experiences caused by the disease. Integral information about the physical, psychological, spiritual and social aspects of the disease makes it possible to identify individual characteristics of the patient's reaction to the disease, evaluate the effectiveness of treatment in a particular patient according to individual monitoring data and use these data to correct the treatment and prevention program.

Objective: development of modern methodological approaches to assessing the individual quality of life of HIV–infected patients to determine the effectiveness of treatment of a particular patient with subsequent correction of the therapy and prevention program.

Material and methods. The object of the study is HIV-infected patients undergoing treatment at the State Medical Institution “Kuzbass Center for Prevention and Control of AIDS” (n=250). The QL research methodology includes key components: selection of a research tool; collection and formation of a database; scaling of questionnaire data; statistical processing of collected information; analysis and interpretation of results.

Results. A modern modified method for assessing the individual quality of life of HIV-infected patients based on the use of relationship type indices has been developed. Each indicator represents the ratio of satisfaction with a certain aspect of life to the corresponding level of psychological claims. The sum of the index values is an indicator of quality of life.

Conclusion. A modified widely used method has been developed to assess the individual quality of life of HIV–infected patients in the system of specialized pharmaceutical care to determine the effectiveness of treatment of a particular patient with subsequent correction of the therapy and prevention program. It has been established that one of the main factors determining the quality of life of HIV–infected patients is a subjective assessment of health, which proves the importance of assessing quality of life as an integral indicator closely related to health.

Farmaciya (Pharmacy). 2024;73(1):44-51
pages 44-51 views

Pharmacology: Experiment and clinic

Approach to synthesis and study of pharmacological effects of new 1,3,5-triazine derivatives

Levshukova P.O., Kolesnik D.A., Kuvaeva E.V., Kirillova E.N., Ivkin D.Y.

Abstract

 

Introduction. Among the derivatives of 1,3,5-triazine, compounds with different biological activity are known, but there are few drugs of this structure on the pharmaceutical market. Thus, the production of new medicines based on a triazine core, as well as the study of their biological activity is an urgent direction.

Objective: synthesis of new 1,3,5-triazine derivatives using the reaction of recycling of 2,5-disubstituted-4-hydroxy-6H-1,3-oxazine-6-ones by 1,3-binucleophiles to obtain different substituents at positions 2,4,6 in one stage, as well as assessment of acute toxicity, diuretic activity in silico and in vivo for synthesized products.

Material and methods. The target compounds were obtained as a result of the interaction of 2,5-disubstituted-4-hydroxy-6H-1,3-oxazine-6-ones and S-methylisothiourea of hemisulfate in the presence of an equimolar amount of sodium methylate in a methanol medium. Prediction of acute toxicity of the studied compound was carried out using the local version of the GUSAR software. Computer screening of biological activity was carried out using the PASS program. Acute toxicity in vivo was determined on white male mice. For experimental evaluation of the diuretic activity of the obtained compounds in vivo, the Taylor, Topliss model was included in the work.

Results. 2-(methylsulfanyl)-4-(4-nitrophenyl)-6-ethyl-1,3,5-triazine, 2-(methylsulfanyl)-4-(4-nitrophenyl)-6-(pentane-1-yl)-1,3,5-triazine were obtained with a yield of 72% and 69%, respectively. The structure of the obtained compounds was proved using 1H and 13C NMR spectroscopy. The predicted and experimental data of acute toxicity correlate with each other, and the studied compounds belong to the class "low-toxic". During the screening of biological activity using the PASS program, data on the estimated diuretic activity were obtained. Studies of biological activity in vivo have shown that the target compounds have pronounced diuretic activity.

Conclusion. New compounds have been synthesized, their structure has been proved using modern physico-chemical analysis methods. The results of computer prediction made it possible to determine the potential class of toxicity and identify potential biological activity. With the help of experimental pharmacological studies, it has been proved that the studied compounds have low toxicity and exhibit pronounced diuretic activity.

Farmaciya (Pharmacy). 2024;73(1):52-56
pages 52-56 views

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