Open Access Open Access  Restricted Access Access granted  Restricted Access Subscription or Fee Access

Vol 27, No 3 (2024)

Cover Page

Full Issue

Open Access Open Access
Restricted Access Access granted
Restricted Access Subscription or Fee Access

Pharmaceutical chemistry

The effect of flavonoids on the α-tocopherol compositions antioxidant activity

Ilyasov I.R., Braun A.V., Olicheva V.V., Fateenkova O.V., Fateenkov V.N., Zhevlakova A.K., Voskoboynikova I.V., Kolkhir V.K., Beloborodov V.L.

Abstract

Introduction. Flavonoids are a family of biologically active substances, representatives of which are often found in the human diet, in particular quercetin, rutin, and morin. When ingested with food, these compounds exhibit their antioxidant properties within the biomolecular system, where α-tocopherol is an important component. Systems formed by antioxidants are characterized by a certain total antioxidant effect, which often differs from the simple sum of their antioxidant capacities to a greater extent in the case of synergy or to a lesser extent in the case of subadditive interaction. From this point of view, the nature of the studied flavonoid's interaction with the endogenous antioxidant α-tocopherol is interesting. The identified interaction effects can serve as a basis for improved antioxidant formulations, as well as the subsequent study of the cooperation mechanisms in vivo.

Aim. The study aims to determine the interaction effects of the α-tocopherol compositions with quercetin, rutin, and morin at their different ratios.

Material and methods. Solutions of individual substances and flavonoid–α-tocopherol compositions in ratios from 1:1 to 1:20 were assessed. The antioxidant capacity was evaluated by the ABTS/PP method, implemented in the form of decolorization and kinetic approaches.

Results. The values of the TEAC index of the studied flavonoids obtained by the decolorization and kinetic method are close and lie in the range of 0.85–3.73 (decolorization) and 0.94–3.22 (kinetic method). Antioxidant capacity increased in the next order: α-tocopherol, rutin, morin, and quercetin. In the first 10 minutes of incubation, flavonoids captured 50–80% of the total number of ABTS•+ radical cations, while α-tocopherol showed the maximum of its antioxidant capacity already in the 1st minute. The composition effects were additive and slightly subadditive for the studied compositions of rutin, morin, and quercetin with α-tocopherol demonstrating maximum values up to –13% in the composition of morin–α-tocopherol 1:10 and quercetin–α-tocopherol 1:20. No dependence of the component’s ratios on the composition effect was found.

Conclusions. The studied compositions of bioflavonoids and α-tocopherol exhibit additive and minor subadditive effects.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(3):3-9
pages 3-9 views

Microcapsules in medicine: review of scientific literature and prospects of application in microencapsulation of anticancer drugs

Sapronova A.K., Denisyuk T.A., Lositskaya O.S.

Abstract

Microcapsules are an innovative form of drug delivery into the human body, which has attracted attention due to its great capabilities in various fields of healthcare. These small particles with a special shell have the potential to improve the processes of drug therapy, diagnosis, and treatment of diseases (for example, cancer), during which the effectiveness increases and the toxicity of many drugs decreases. Due to their small size (from 100 to 500 microns), microcapsules can transfer and protect the active components of drugs, ensuring their accurate and targeted delivery to the site of action in the body. Currently, a promising area is the study of microcapsules in which antitumor drugs are placed. The active substance is delivered directly to cancer cells, which increases the concentration of the drug in the tumor and at the same time reduces its effect on healthy tissues. This approach will help improve cancer treatment outcomes and increase the chances of a successful recovery for patients without any dangerous side effects.

The purpose of the work is to analyze modern research related to the microcapsulation of various drugs, especially in the field of oncology.

The literature is analyzed, including scientific domestic and foreign publications that have been written over the past ten years. The analysis of existing studies related to the use of microcapsules in medicine is presented. Some methods of obtaining a new form, its types, and applications in medicine, in particular in oncology, are considered. This review provides valuable information on a variety of research methods and promising uses of a process such as microcapsulation for the delivery of anticancer drugs, and can be one of the important resources for researchers developing new therapeutic approaches, as well as for doctors applying advanced cancer treatments through innovative therapies.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(3):10-15
pages 10-15 views

Comparative chromatographic and spectral study of the alkaloid composition of the biomass of tissue culture and the herb of Glaucium Flavum

Kurkin V.A., Kurkina A.V., Trifonova P.V., Tukhbatullina R.G., Matygullina L.I.

Abstract

Introduction. The culture of plant cells and tissues is an effective technology for obtaining various secondary metabolites, including for use in the pharmaceutical industry. Compounds synthesized in callus and suspension cultures may be identical to plant ones, and the yield of secondary metabolites, in some cases, exceeds plant sources. In this regard, yellow hornpoppy (Glaucium flavum Crantz.) is of great interest, containing glaucin, which has a unique antitussive effect and is a source of a number of medications.

The purpose of this study is a comparative phytochemical study of the alkaloid composition of the tissue culture and the herb of Glaucium flavum.

Material and methods. Callus tissue cultures of yellow hornpoppy yellow hornpoppy (Glaucium flavum Crantz.) were obtained in the laboratory of the Institute of Pharmacy of Kazan State Medical University. The herb of the Glaucium flavum cultivated on the territory of the Botanical Garden of Samara University was collected during the flowering period of plants in 2021. A comparative study of the alkaloid composition of the callus culture and the herb of Glaucium flavum was carried out by methods of luminescent microscopy on an Altami LUM-2 microscope (Russia), thin-layer chromatography (TLC) on Sorbfil-PTSH-AF-A-UV plates, as well as spectrophotometry. A mixture of solvents n-butanol-acetic acid-water 4:1:2 was used as a solvent system. The detection of separated substances was carried out by scanning chromatographic plates in UV light at a wavelength of 366 and 254 nm, followed by the manifestation of Dragendorf reagent. The identification of the isolated glaucin hydrochloride was carried out on the basis of UV, 1H-NMR, 13C-NMR spectroscopy data. 1H NMR spectra were obtained on the "JNM-ECX 400" device (399.78MHz), 13C NMR spectra were obtained on the "JNM–ECX 400" device (100.52 MHz). The spectra were recorded using a Specord 40 spectrophotometer (Analytik Jena AG, Germany) in the wavelength range of 190-500 nm.

Results. During the luminescent analysis of the tissue culture of the Glaucium flavum Crantz., as well as intact plants, the type of luminescence characteristic of isoquinoline alkaloids was noted. Using TLC analysis, isoquinoline alkaloids, including glaucin, were found in samples of callus cultures and the aerial parts of Glaucium flavum, however, a lower glaucin content was noted in the sample of the callus culture compared to that of the intact plant. The spectrophometric analysis of the studied samples showed that the nature of the absorption curve in intact plants and crops of the so-called Glaucium flavum has both common and distinctive features. The UV spectrum of water-alcohol extraction from a sample of Glaucium flavum tissue culture has a similar spectrophotometric profile, however, it contains only one absorption maximum (288 nm), coinciding with that of the UV spectrum of water-alcohol extraction from the herb of this plant.

Conclusions. Therefore, the final conclusion regarding the content of glaucin in the studied samples can be made only during the preparative isolation of substances from the biomass of Glaucium flavum using column chromatography.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(3):16-22
pages 16-22 views

Relationship between biochemical indicators and phenotypical characteristics of thyme (Thymus vulgaris L.)

Malankina E.L., Tkatchova E.N., Al Karavi H.A.

Abstract

Introduction. Thyme (Thymus vulgaris L.) is a sought-after medicinal crop, the raw materials of which are included in the Pharmacopoeias of several countries and are widely used in scientific medicine. Due to the presence of strong intraspecific diversity in thyme, it seems interesting to identify phenotypic characteristics that most likely indicate the presence of certain pharmacologically significant compounds. The presence of such information will allow targeted selection both in natural populations and during the hybridization of cultivars and the development of new varieties.

The purpose of the work was to identify phenotypic traits indicating a high content of essential oil and thymol in thyme, the amount of phenolic compounds, flavonoids and tannins.

Material and methods. Samples and varieties of thyme from different geographical origins were selected as objects. Biometric, anatomical indicators and yield were determined in the flowering phase. The essential oil content was determined by Clevenger hydrodistillation method. Component composition was determined by gas chromatography. The amount of phenolic compounds and tannins according to the Folin-Ciocalteu method in aqueous-alcoholic extract calculated as gallic acid. The determination of flavonoids in the aqueous-alcoholic extract was carried out using the spectrophotometryс method calculated as rutin.

Results. As a result of the research, no signs were found indicating a high content of essential oil. Flavonoid content calculated as rutin had a negative correlation (−0.72) with stomatal density. A negative relationship was noted between the intensity of coloring of the pistil and anthers and the content of the total phenolic compounds calculated as gallic acid (0.71 and 0.72, respectively). Large stomata on both the underside and upper side of the leaf may indicate a high tannin content (0.8 and 0.88). All studied components of common thyme belonged to the thymol type, and the content of this component ranged from 37.6 to 80.8%. An increased content of thymol in essential oil is observed such signs as an elongated leaf shape (leaf index R = 0.78), lack of downward curling of the edges of the leaf blade (R = –0.78) and pronounced veins on the underside of the leaf (R = 0.92). Large stomata on the lower epidermis also indicate an increased proportion of thymol in the essential oil (R = 0.78). When analyzing the interdependence between the content of the main components of essential oil, it was noted that there is a close negative correlation between the content of p-cymene and thymol (R = –0.91) and carvacrol (R = –0.88).

Conclusion. As a result of the research, phenotypic and anatomical characteristics were identified that make it possible to diagnose promising samples of common thyme, which will help speed up the selection process.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(3):23-29
pages 23-29 views

Quality assessment of Silybum marianum fruits grown in the Republic of Buryatia

Saybel O.L., Konyaeva E.A., Kulyak O.Y., Dul V.N., Tsybikova O.M., Tsydypov B.D.

Abstract

Introduction. Medicines of plant origin are widely used in the complex therapy of various diseases. Among the medicines of plant origin used for the treatment of chronic liver diseases, the most popular are preparations based on Silybum marianum (L.) Gaertn.).

The aim of this work was to Silybum marianum fruits to evaluate the possibility of obtaining raw materials of pharmacopoeial quality in the dry-steppe zone of the Republic of Buryatia.

Material and methods. The object of the study was Silybum marianum fruits of the varieties Debut and Start, obtained from experimental fields in Ivolginsky district of the Republic of Buryatia, as well as samples of Silybum marianum fruits received for analysis at the Testing Center of FGBNU VILAR from different regions of the Russian Federation.

Results. As a result of the research it was found that climatic and geographical conditions of the dry-steppe zone of the Republic of Buryatia allow successful cultivation of Silybum marianum and obtaining raw materials (fruits) of pharmacopoeial quality.

Conclusion. Silybum marianum fruits obtained from plants of the Start variety are not inferior to similar raw materials harvested in other regions of the Russian Federation in the content of the sum of flavolignans.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(3):30-34
pages 30-34 views

Analysis of the possibility of using medical clays to obtain sorption dosage forms

Bondarev A.V., Zhilyakova E.T., Riffi M., Novikova N.B.

Abstract

Introduction. Currently, medical clays in Russia are represented by the drug "Smectite dioctahedral", which accounts for 25% of all enterosorbents. Compared to 2014, the share of medical clays in the total structure of enterosorbents has increased fourfold. The search for new sources of medicinal mineral raw materials for the production of sorption dosage forms is an urgent task of pharmaceutical technology.

The purpose of the work is to analysis of the possibility of using medical clays to obtain sorption dosage forms.

Material and methods. Two medical clays were selected as objects of research: sample "X" – clinoptilolite clay of the Kholinsky deposit (Russia, Trans-Baikal Territory), sample "I" – zeolite clay of the Western Aftar deposit (Iran). The determination of the specific surface area and porosity was carried out by low-temperature nitrogen sorption on a TriStar II 3020 analyzer, microscopy was carried out on an electron–ion scanning microscope FEI Quanta 600 FEG.

Results. A comparative analysis of technological and adsorption characteristics of clays was carried out. It was found that the clinoptilolite clay of the Kholinsky deposit is symmetrical equiaxed particles in the form of spherical formations, the average particle size is 6.33 microns, the specific surface area is 20.9227 m2/g, the pore volume is 0.058435 cm3/g, the average pore size is 11 nm, has mesopores (17-50 nm) and macropores. A study of the morphological characteristics of the zeolite clay of the Western Aftar deposit (Iran) shows that the clay consists of agglomerates of irregularly shaped particles with an average size of 2.00 microns. According to the obtained adsorption characteristics, clay has a specific surface area of 20.4654 m2/g, a pore volume of 0.065848 cm3/g, an average pore size of 13 nm, has mesopores (18-50 nm) and macropores.

Conclusions. The studied clays are mesomacroporous sorbents with a predominance of mesopores. Satisfactory adsorption indicators show the prospects of using medical clays to obtain sorption dosage forms.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(3):35-40
pages 35-40 views

Problems of experimental biology and medicine

Selection of methodology for Thiophan M isolation from animal organs

Ligostaev A.V., Ivanovskaya Y.A., Terentyeva S.V., Pashkova L.V., Zherebtcova E.Y., Prosenko O.I., Pitukhin M.P.

Abstract

Introduction. An important preparatory stage of collecting information for the registration of a new drug is the study of its pharmacokinetic parameters in accordance with the requirements of good laboratory practice. The preparatory stage of such a study consists in the selection of optimal conditions for sample preparation of biological objects to determine the test substance in them.

The purpose of this study is to select optimal conditions for sample preparation, including the pH value of the extractant, and isolation of Thiophane M from the organs of laboratory animals (rats) for its further voltammetric determination according to the previously developed method.

Material and methods. The object of the study was the substance Thiophane M [dodecyl(3,5,-dimethyl-4-hydroxybenzyl)sulfide], which is a promising biologically active compound with antioxidant properties, developed on the basis of the Department of Chemistry of Novosibirsk State Pedagogical University together with the Research Institute of Antioxidant Chemistry. Experimental data were obtained using 5 male rats weighing from 350-380 g, which were injected with an intragastrically tested sample of Thiophane M at a dose of 500 mg/kg in the form of an oil solution in olive oil.

Results. The total number of samples obtained and examined is 180. Based on the data obtained with their subsequent statistical processing by the indirect differences method according to the State Pharmacopoeia of the XIV edition, it was established that the optimal condition for the extraction of Thiophane M is a single extraction with diethyl ether, which is confirmed by the results of voltammetric analysis. We have found that the greatest number Thiophane M localized in the brain, heart and lungs (364.0±8.20, 332.0±16.47 and 275.0±25.40 µcg/g, respectively), fewer Thiophane M detected in kidney, spleen and liver (146.0±15.50, 81.0±8.66 56.0±14.53 µcg/g, respectively).

Conclusions. Of all the methods of Thiophan M isolation from rat organs, the method using diethyl ether as an extractant was chosen, which gave stable results due to the maximum extraction of the substance.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(3):41-48
pages 41-48 views

Effect of ACTG(4-7)-PRO-GLY-PRO and ACTG(6-9)-PRO-GLY-PRO on the intensity of redox processes and behavioural status of rats under thyroid hyperfunction conditions

Sergalieva M.U., Tsibizova A.A., Murtalieva V.K., Andreeva L.A., Myasoedov N.F., Samotrueva M.A.

Abstract

The aim of the work is to study the effect of melanocortins on the intensity of redox processes in the prefrontal region of the brain and the behavioral status of rats against the background of thyroid hyperfunction.

Material and methods. In the experiment, the test animals were divided into the following groups (n = 10): intact rats (control); animals treated with sodium salt pentahydrate L-thyroxine (hyperthyroidism); rats receiving ACTH (4-7)-Pro-Gly-Pro and individuals receiving ACTH (6-9)-Pro-Gly-Pro, respectively, intraperitoneally daily for 21 days, starting from day 22 of administration of sodium salt pentahydrate L-thyroxine. Hyperthyroidism was simulated in animals by intragastric administration of L-thyroxine sodium salt pentahydrate for 42 days. The intensity of lipoperoxidation processes was studied by the content of diene and triene conjugates in the prefrontal zone tissue, the initial level of TBА-reactive products, and the rates of spontaneous and ascorbic peroxidation of lipids. The level of protein peroxidation products was determined by the reaction of oxidized amino acid residues of proteins with 2,4-dinitrophenyl hydrazone. Evaluation of the enzymatic unit of the antioxidant system of the prefrontal region was carried out by determining the activity of superoxide dismutase and catalase. The behavioral status of laboratory rodents was studied using the «Hole board» test.

Results. The use of ACTH(4-7)-Pro-Gly-Pro and ACTH(6-9)-Pro-Gly-Pro compounds under experimental hyperthyroidism led to a decrease in the intensity of the processes of peroxidation of lipids, proteins and the restoration of levels of activity of antioxidant enzymes – superoxide dismutase and catalase in the tissue of the prefrontal region of the brain of animals, as well as correction behavioral indicators in the «Hole board» test.

Conclusion. The obtained experimental data indicate that ACTH(4-7)-Pro-Gly-Pro and ACTH(6-9)-Pro-Gly-Pro show antiperoxy and antioxidant activity against lipoperoxidation parameters and oxidative modification of proteins and enzymatic protection systems in the prefrontal brain zone tissue, as well as exert psychocorregating action on behavioral responses of white rats against the background of thyroid hyperfunction.

Problems of Biological Medical and Pharmaceutical Chemistry. 2024;27(3):49-55
pages 49-55 views

This website uses cookies

You consent to our cookies if you continue to use our website.

About Cookies