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Introduction. The use of anticoagulants is relevant in therapeutic, cardiological, neurological practice, geriatrics, obstetrics and gynecology, as well as in complications associated with COVID-19 infection and vaccination. In-depth studies of additional pleiotropic effects of existing anticoagulants are being conducted. The anti-inflammatory effect of heparins and direct oral anticoagulants was found. Special emphasis is placed on the existing close relationship between coagulation and inflammatory processes. The interaction of anticoagulants with nonsteroidal anti-inflammatory drugs when taken together is actively discussed. The combination of anticoagulant and anti-inflammatory action in one chemical molecule can solve the problem of polypragmasia.Aim. To study the anti-inflammatory activity of promising 2-hydroxy-4-oxo-4-R-2-butenoates of heterylammonium, which have an effect on the blood clotting system.Materials and methods. For further study of anti-inflammatory activity, 2-hydroxy-4-oxo-4-R-2-butenoates of heterylammonium, which have an effect on the blood clotting system, were selected. The anti-inflammatory effect was studied on a model of acute inflammatory edema in mongrel rats of both sexes weighing 180–250 g. The studied compounds were administered intragastrically. Diclofenac sodium and nimesulide substances administered similarly were used as comparison drugs. Acute toxicity of substances that showed activity was studied on white nonlinear mice of both sexes weighing 18–22 g with the definition of LD50.Results and discussion. All the studied 2-hydroxy-4-oxo-4-R-2-butenoates of heterylammonium have anti-inflammatory effects of varying severity. Data on the study of acute toxicity during intragastric administration, allow us to attribute the studied compounds to the 4.5 class of the hazard classification of chemical products.Conclusion. The anti-inflammatory activity of 14 2-hydroxy-4-oxo-4-R2-butenoates of heterylammonium has been studied. Five butanoate have an effect lower than comparison drugs, eight compounds are comparable to the effect of reference drugs, one compound is superior to nimesulide. The studied compounds can be assigned to class 4,5 of the hazard classification of chemical products. Medicinal candidates have been selected for further pharmacological, toxicological and technological study.

Introduction. Interest in herbal preparations is increasing every year, as the variety of chemical composition and pharmacological action of plants makes it possible to discover and create drugs whose therapeutic effect is due to a complex of biologically active substances. It is important for the effective treatment of diseases to have a properly selected dosage form, which provides both ease of use and targeted use of the action of the pharmacologically active drug contained in it. Therefore, obtaining and introducing new plant extracts into medical practice can become promising in the field of creating soft dosage forms. Strawberry garden leaf extract dry (strawberry extract) is one of the potential substances for obtaining effective and safe medicines. According to the results of earlier studies conducted by the staff of the Perm State Pharmaceutical Academy of the Ministry of Health of the Russian Federation, a high anti-inflammatory activity of strawberry extract was proved, comparable to the activity of the synthetic drug Indomethacin. Studies of the chronic toxicity of the extract, allergenic, immunotoxic properties and reproductive toxicity in the framework of preclinical studies have shown the safety of the obtained extract and the possibility of using the substance for further development of medicines based on it. In this regard, the study of technological parameters and pharmacological activity of a soft dosage form based on strawberry extract is of practical interest for improving the drug supply of the population and expanding the range of medicines based on plant extracts with anti-inflammatory and antimicrobial effects.Aim. Development of a soft dosage form based on strawberry leaves of dry extract and study of its pharmacological activity.Materials and methods. For the study, gels with an active substance – strawberry leaves with dry extract (JSC "Biohimmash", Russia, shelf life – 2 years), the main components – sodium carboxymethylcellulose C75 (TU 2231-002-50277563-2000, LLC "Base chemical products "Yugreactive", Russia, 151118, term storage 3 years), methylcellulose 35 (TU 2231-107-57684455-2003, JSC "UZPH", Russia, 221218, shelf life 3 years), sodium alginate (TU 15-02-544-83, LLC "Base сhemical products "Yugreactive", Russia, 151018, shelf life 3 years), glycerol (FS.2.2.0006.15, JSC "Kupavnareaktiv", Russia, 082018, shelf life 3 years), purified water (FS FS.2.2.0020.18), obtained at the reverse osmosis unit UVOI-"MF" 1812S6 (JSC "NPK MEDIAN FILTER", Russia). Вiopharmaceutical and technological methods were used in the course of the research. Antimicrobial activity was determined according to the OFS.1.2.4.0010.15 by diffusion into agar. Anti-inflammatory activity was studied on a model of acute inflammatory edema caused by subplantar injection of 0.1 ml of 1 % aqueous solution of carrageenan into the hind paw of a rat. The obtained data were processed with the calculation of the Student's t-test for independent samples. The data were considered reliable at p < 0.05.Results and discussion. Based on technological, biopharmaceutical and pharmacological research methods, the composition of a gel from strawberry leaves with dry extract, which has antimicrobial and anti-inflammatory effects, was proposed and substantiated for the first time. The biopharmaceutical availability of the gel was determined by diffusion into agar gel. The antimicrobial activity of the gel from strawberry leaves with dry extract and its anti-inflammatory activity on the model of carrageenan edema with external application of the studied dosage forms were studied.Conclusion. The study shows the possibility of expanding the range of drugs for external use with antimicrobial and anti-inflammatory activity.

The article is devoted to examining anti-inflammatory activity of dry aqueous extract of European spruce (Picea abies) strobiles using different routes of administration. Strobiles of European spruce for extracts were harvested on the territory of the Perm region of the Russian Federation in a mixed forest with a predominance of European spruce and Scots pine (Pinus sylvestris). Dry aqueous extract was obtained according to the original patented method. Procyanidins content in spruce strobiles and dry extracts was determined by using acid cleavage of procyanidins to anthocyanidins according to the Porter method. Anti-inflammatory activity was established by using carrageenan-induced paw edema in rats. White laboratory outbred Wistar rats were used in the experiment. According to the results of the study, the procyanidin content was found to equal approximately 13 % in the samples of spruce strobiles. Intraperitoneal administration of dry extract of strobile spruce at a dose of 100 mg/kg was established to induce a pronounced anti-inflammatory activity. Intraperitoneal administration of smaller doses of strobile extract resulted in a pronounced anti-inflammatory activity at a dose of 50 mg/kg. A dose of 10 mg/kg successfully suppressed inflammation (50 % edema suppression) 1 and 3 hours after carrageenan administration (p < 0.05) according to hydrometric data, but this was not confirmed by photometric data. Oral administration of the extract showed no anti-inflammatory activity. With the rectal route of administration, no pronounced anti-inflammatory activity was found in the studied extract. The extract of spruce strobiles obtained by the original method contains 56 % procyanidins and exhibits pronounced anti-inflammatory activity when administered intraperitoneally. The use of the extract in oral and rectal routes of administration requires more in-depth study

Introduction. Sea buckthorn leaves are a promising object for the development of new medicinal herbal preparations due to an extensive list of biologically active substances (tannins, flavonoids, organic acids, etc.). However, despite the active study of biologically active substances of buckthorn buckthorn leaves, their use in medicine is limited to obtaining an antiviral drug "Hyporamine" containing a dry purified extract from the leaves of this plant.Aim. The aim of the work is to predict the pharmacological and toxic effects of decoction from buckthorn leaves in silico and to evaluate its anti-inflammatory activity in vivo in preclinical studies.Materials and methods. With the help of the PASS-online Internet resource, the prediction of promising pharmacological and possible toxic effects for the main biologically active substances of the phenolic complex of sea buckthorn leaves in silico was carried out. In preclinical studies in vivo (white outbred conventional male rats, 21 individuals, 210–240 g, 3 groups of 7 individuals each) on a model of formalin paw edema of rats (3.0 % aqueous formalin solution, 0.1 ml subplantarly), the anti-inflammatory activity of decoction of sea buckthorn leaves was evaluated. Animals of the experimental groups were administered: a comparison drug – an infusion of chamomile flowers or a decoction of sea buckthorn leaves at a dose of 10 ml/kg intragastrically daily for 7 days.Results and discussion. The analysis and systematization of data on the most likely pharmacological effects of the main biologically active substances of sea buckthorn leaves in silico using the PASS-online platform allow us to consider the most promising study of anti-inflammatory, hepatoprotective, cardioprotective, antibacterial, antifungal and antiviral activity, which opens up prospects for further preclinical and clinical studies in order to expand the list of indications for the use of extracts from the leaves of sea buckthorn. The prediction of the toxic effects of the main biologically active substances of sea buckthorn leaves showed that the smallest number of probable toxic effects is predicted for narcissin and quercetin, the largest for the substance strictinin I (including neurotoxicity, hematotoxicity, negative effects on the cardiovascular system, gastrointestinal toxicity, reproductive toxicity and carcinogenicity), which requires confirmations in preclinical toxicological studies. In preclinical studies in vivo on a model of rat paw edema, it was proved that a decoction of sea buckthorn leaves with a short-term oral course application of 7 days at a dose of 10 ml/kg (235 mg/kg based on the dry residue), it shows a sufficient anti-inflammatory effect, providing a significant, reliable decrease in the severity of rat paw edema, maximum 3 hours after phlogogen administration by 36.0 % compared with the control, which exceeds the effectiveness of the comparison drug (infusion of chamomile flowers).Conclusion. The main types of pharmacological activity (anti-inflammatory, hepatoprotective, cardioprotective, antibacterial, antifungal and antiviral) and toxic effects (neurotoxicity, hematotoxicity, negative effect on cardiovascular activity and gastrointestinal tract) have been established. Pronounced anti-inflammatory activity was reliably detected.

The Thymus L. genus is extremely widespread on the territory of Ukraine and includes up to 50 main species. Extracts from the official species of the Thymus L. genus are part of effective herbal preparations with pronounced anti-inflammatory, antimicrobial and antioxidant activities. A promising direction of modern phytochemical research is the determination of the accumulation of biologically active polyphenolic compounds in the Thymus vulgaris L. herb, which is widely cultivated in Ukraine and other countries. The aim of the work is to determine the accumulation of polyphenolic compounds in Thymus vulgaris L. herb at the end of flowering using TLC and HPLC methods. Materials and methods. For experimental studies, alcohol extracts from Thymus vulgaris L. herb (1:100) were used. The plants were cultivated in Volodymyrivka, Zaporizhzhia region during the period of maximum polyphenolic compounds accumulation (June – August 2022). The substances’ component composition was studied by TLC method Biostep CD 60 densitometer (Germany) and HPLC Agilent 1260 Infinity HPLC System Open LABCDS Software (Japan). Results. TLC and HPLC methods revealed up to 29 polyphenolic compounds. Experimentally determined flavonoids and hydroxycinnamic acids are known in phytotherapy for their pronounced anti-inflammatory, antimicrobial, and antioxidant activities. Conclusions. Considering the results obtained by TLC and HPLC methods, it can be concluded that Thymus vulgaris L. is a promising species for further phytochemical research.

Flavonoids are an extensive class of secondary metabolites present in varying concentrations in different parts of plants. Medicinal raw materials containing flavonoids have been used in traditional medicine in various countries for centuries and are also used in modern medicine for the production of drugs. Compared to other groups of secondary metabolites, flavonoids are often present in relatively large amounts. Interest in flavonoids is driven by constantly updated data on their biological activity and their wide distribution in the plant world. This review focuses on the two most commonly occurring polyphenolic compounds in plants, quercetin and kaempferol. The article describes the main glycosidic forms of the flavonoids under consideration and the modern results of studying their biological activity, namely their antioxidant, anti-allergic, anti-inflammatory, cardioprotective, and anti-tumor properties. In addition, some of the mechanisms for implementing the above types of biological activity are discussed. The analysis suggests that further in-depth pharmacological research on these flavonoids and the development of new advanced drugs based on them is promising. The cores of quercetin and kaempferol can be recommended for chemical modification to obtain highly active compounds with antioxidant, anti-allergic, anti-inflammatory, cardioprotective, and anti-tumor activities.

Background. In the majority of cases, contemporary pharmacological correction mainly focuses on the most effective analgesia. Therefore, the search for and research into new analgesic drugs are a priority in modern pharmacology.Objective — to establish the level of analgesic activity in eight novel heterocyclic compounds of 1,4-dihydropyridine derivatives synthesized in a classic test of orofacial trigeminal pain in animal experiments.Methods. An experimental preclinical randomized trial of the analgesic activity in 1,4-dihydropyridine derivatives was carried out. The experiment was conducted on 100 white male outbred rats in the laboratory of the Fundamental and Clinical Pharmacology Department, St. Luke Lugansk State Medical University, Lugansk People’s Republic. Novel 1,4-dihydropyridine derivatives were preliminarily investigated in a virtual biological screening by means of Swiss Target Prediction tool (Swiss Institute of Bioinformatics, Switzerland). The laboratory animals were divided into a control group (rats were exposed to acute pain syndrome by injecting 0.1 ml of 5% formalin solution into the vibrissae area without pharmacological correction), a comparison group (rats which received metamizole sodium (OOO Farmstandard) at a dose of 7 mg/kg 1.5 hour prior to acute pain syndrome modeling in the vibrissae area), and eight experimental groups (1.5 hours before formalin administration, novel 1,4-dihydropyridine derivatives under study at a dose of 5 mg/ kg were intragastrically injected). 10, 15 and 20 minutes after simulating acute pain, the number of scratching movements of the forelegs around orofacial region per minute was counted. Statistical processing of the results involved methods of mathematical statistics for quantitative variability and was carried out using Statistica 12.5 (IBM, USA).Results. Animals treated with 1,4-dihydropyridine derivatives d02-133 and d02-172 under the experimental conditions showed a significant (13–21 times) decrease in scratching movements frequency by the 10th minute of observation in comparison with the control group. By 15th minute, the analgesic activity of the cyanothioacetamide derivatives increased 14 and 11 times as compared to these indicators of the reference group. After 20 minutes, the analgesic activity of these compounds in terms of inhibiting nociceptive impulses, as compared to the control group, was also high, as the number of scratching movements in the vibrissae area in animals of these experimental groups was 8–9 times lower than in control group. The orofacial trigeminal pain test detected the most exhibited analgesic activity in novel cyanothioacetamide derivatives d02-139, d02-133, and d02-172, which appeared to be higher than that of metamizole sodium.Conclusion. It was found that novel original derivatives of 1,4-dihydropyridine showed a high degree of analgesic activity.

Introduction. New potential biologically active compounds with different pharmacological activities were found among pyrimidine derivatives. Simple and available synthesis of tetrahydropyrimidine-5-carboxamides was developed in Perm State Pharmaceutical Academy. Products of this reaction previously shown high analgesic and anti-inflammatory activities.Aim. To get previously unknown functionalized pyrimidines and to study their analgesic, anti-inflammatory and antipyretic activities.Materials and methods. 11 compounds N,6-diaryl-4-methyl-2-thioxo-1,2,3,6-tetrahydropyrimidine-5-carboxamides are objects of research. Their structure has been confirmed by spectroscopy methods. The biological activities were carried out by recommended methods for preclinical study of new pharmacological substances.Results and discussion. This paper presents the results of preclinical tests of the obtained compounds.Conclusion. Some compounds demonstrated high analgesic, anti-inflammatory and antipyretic activities and could be recommend for further study as perspective non-steroidal drugs.

Introduction. The defeat of hard tissues of the tooth, accompanied by inflammatory processes, remains today an urgent medical and social problem for the population. Inflammatory processes cause acute pain and often lead to loss of teeth, which causes significant damage to the aesthetic and functional state of the dental system. Despite the large number of drugs created to date, methods for their use, the search and testing of new drugs for the prevention and treatment of diseases of the oral cavity does not lose its relevance and relevance in practical healthcare.Aim. The purpose of this study was to study the anti-inflammatory activity of new dental dosage forms with Acyzol.Materials and methods. Serial samples of gels and films with an active pharmaceutical substance – acyzol bis-(1-vinylimidazole)zincdiacetate (ФС 000286 191211.2011, LLC "Makiz-Pharma", Russia, 101218, shelf life 3 years) were used for the study; basic and gel-forming components – Na-KMTs C75 (TU 2231-002-50277563-2000, LLC "Chemical Products Base "Yugreaktiv", Russia, 151119, shelf life 3 years), glycerol (FS.2.2.0006.15 "Glycerin", JSC "Kupavnareaktiv", Russia, 082019, shelf life 3 years), purified water (FS.2.2.0020.18 "Purified water"), nipagin (LLC "Alfa-Veta.com", Russia, 092018, shelf life 3 years), nipazol (LLC "ECOCHEM-INNOVATION", Russia, 071518, shelf life 3 years). The studies were carried out on a model of carrageenan edema during external application of the studied dosage forms of Acyzol, modified taking into account the specifics of the dosage forms.Results and discussion. An acute inflammatory reaction was induced by subplantar injection of 0.1 ml of a 1 % solution of carrageenin into the hind paw of a rat. An increase in the volume of the foot, indicating the development of edema, was assessed oncometrically before and 3 hours after the administration of the phlogogenic agent. The studied objects in the amount of 0.3 g were applied to the skin of the foot 0.5 hours before the introduction of carrageenan. Statistical processing was carried out according to Student's method using Microsoft Office Excel 2010 Professional software. Based on the results obtained, the effect of inflammation inhibition was determined as a percentage of the control level. The presence of anti-inflammatory action was judged by the severity of inhibition of the inflammatory response. If this indicator was more than 30 %, the result was taken into account as positive.Conclusion. It has been established that the films and the gel have an anti-inflammatory effect, which was found in the model of carrageenan edema. The results obtained indicate the feasibility of further pharmacological studies and make it possible to recommend the gel and films as an effective tool for the prevention and treatment of oral diseases.

The aim of the study is to determine antioxidant, anti-inflammatory and hypolipidemic activities of the extracts from Cosmos bipinnatus Cav. three varieties, obtained by the extraction with 70% ethyl alcohol.Materials and methods. The antioxidant effect was studied in vitro using a model of iron-induced lipid peroxidation in the lecithin liposome system. The study of the anti-inflammatory activity was carried out on 30 male rats of the “Wistar” line. Diclofenac was used as a reference drug (p. o., the dose of 13 mg/kg in terms of the weight of an adult). The substances were administered to animals in the form of an aqueous suspension stabilized with Tween-80. To simulate the inflammatory process, a model of “cotton granuloma” was created. A hypolipidemic activity of the extracts was studied on 36 white male rats of the “Wistar” line. To study the hypolipidemic activity of the studied extracts, a tween model was used to create a hyperlipidemic state in rats, the concentrations of total cholesterol and triglycerides was determined in the serum of the experimental animals.Results. The conducted model experiments made it possible to conclude that the alcohol extracts obtained from the dried inflorescences of the “Dazzler”, “Rosea” and “Purity” varieties of Cosmos bipinnatus Cav. have antioxidant, anti-inflammatory and hypolipidemic kinds of activities. It has been established that the extracts from the “Dazzler” and “Rosea” varieties (Cosmos bipinnatus Cav.) contribute to a better reduction in the accumulation of peroxide compounds, compared to the extract obtained from the “Purity” variety. The data analysis on the anti-inflammatory activity shows that all the studied objects significantly (p = 0.05) reduce the stage of exudation compared with the control group animals by 50% (the «Purity» variety), by 52% (the «Rosea» variety) and by 40% (the “Dazzler” variety).An experiment on the study of a hypolipidemic activity in the control group of the animals revealed a significant, in relation to the values of the intact group, increase in the cholesterol level of the blood serum by 78%, and in the level of triglycerides (TGCs) – by 64%.The administration of the extracts obtained from Cosmos bipinnatus Cav. “Purity”, “Rosea”, “Dazzler” varieties to the animals, led to a decrease in cholesterol in blood serum by 44%, 47%, 50%, and triglycerides by 52%, 52% and 57%, respectively. Both indicators reached the normal level and did not differ significantly from the values in healthy (intact) animals.Conclusion. According to the conducted studies, it can be concluded that alcohol extracts obtained from Cоsmos bipinnatus Cav., have pronounced antioxidant, anti-inflammatory and hypolipidemic kinds of effect.

Background. Over the past decades, scientific community is motivated on finding new anti-inflammatory agents with a safe and high-effective profile to manage pathology.Objectives. A study of the anti-inflammatory action of novel compounds, 1,4-dihydropyridine derivatives, in a classical formalin-induced paw oedema test in white rats.Methods. Originally synthesised 1,4-dihydropyridine derivatives were preliminarily subjected to virtual screening using the SwissTargetPrediction toolkit. White laboratory rats (130 animals) were divided into a control (formalin oedema) and intact group, 4 comparison (meloxicam, sodium metamizole, sodium diclofenac and indomethacin) and 7 experiment groups by the number of 1,4-dihydropyridine derivatives studied. The samples anti-inflammatory efficacy was evaluated in acute formalin-induced paw oedema model simulated by right hind limb subplantar injection of 0.1 mL 2% formalin. The studied substances were administered intragastrically at 5 mg/kg 1.5 h prior to oedema induction. Oncometry was assessed quantitatively by limb circumference. Animals were managed in compliance with GOST 33044–2014 “Principles of Good Laboratory Practice” at all experiment steps. Experimental data were analysed statistically to describe quantitative variability with variance σ2, mean limb girth a and standard deviation σ. Data homogeneity and reliability were estimated by variation coefficient V and the Wilcoxon T(W) criterion.Results. As the most anti-inflammatory effective, partially hydrogenated mar-040 pyridines (ethyl 4-({[5-cyano-6-{[2-(diphenylamino)-2-oxoethyl]thio}-4-(2-furyl)-2-methyl-1,4-dihydropyridin-3-yl]carbonyl}amino) benzoate) were shown 33-fold superior to indomethacin, 26-fold — to sodium diclofenac, 25-fold — to meloxicam and 30-fold — to sodium metamizole; mar-037 pyridines (ethyl 4-[({[3-cyano-5-({[4-(ethoxycarbonyl)phenyl]amino}carbonyl)-4-(2-furyl)-6-methyl-1,4-dihydropyridin-2-yl]thio}acetyl)amino] benzoate) — 17–23-fold superior vs. reference drugs. We also show that mаr-014 (ethyl 4-({[5-cyano-6-({2-[(3,5-dichlorophenyl) amino]-2-oxoethyl}thio)-4-(2-furyl)-2-methyl-1,4-dihydropyridin-3-yl]carbonyl}amino)benzoate) and mar033 (ethyl 2-[({[3-cyano-5-({[4-(ethoxycarbonyl)phenyl]amino}carbonyl)-4-(2-furyl)-6-methyl-1,4-dihydropyridin-2-yl]thio}acetyl)amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxylate) compounds are 2.7-fold more effective vs. reference drugs.Conclusion. The synthesised 1,4-dihydropyridine compounds reveal high efficacy in experimental assays. Selected novel 1,4-dihydropyridine derivatives exhibit a marked anti-inflammatory activity and offer value in future preclinical trials.

Non-steroidal anti-inflammatory drugs are among the top requested ones in the clinic of internal medicine. However, these drugs are associated with a wide range of adverse reactions involving a number of organs and systems, in particular the gastrointestinal tract, cardiovascular system and kidneys.The aim of the study is to characterize the effect of the combined use of cryopreserved placenta extract and diclofenac sodium on the prooxidant-oxidative system, the activity of inflammatory, destructive and cytolytic processes, as well as protein and lipid metabolism in rats with experimental rheumatoid arthritis.Results. The administration of diclofenac sodium and cryopreserved placenta extract to rats with adjuvant arthritis normalized the level of active products of thiobarbituric acid and hence was indicative of the neutralization of an arthritis-induced oxidative stress. A statistically significant (p=0.01) increase of in a superoxide dismutase activity (by 30.6% relative as compared with rats of the control group) has also been established. An increase in the anti-inflammatory properties of diclofenac sodium in the combined use of diclofenac sodium with a cryopreserved placenta extract has been found out. The level of C-reactive protein decreased (p

The raw material base of medicinal plants in Ukraine is sufficient only for half of the pharmacopoeial species. Most of them are growing in insufficient quantities and there is a need to import them. In the conditions of import dependence and scarcity of domestic raw materials, the search for new sources of biologically active substances among the representatives of the Ukrainian flora is an urgent aim of modern pharmaceutical science. The purpose of the research is to conduct comparative pharmacognostic and pharmacological studies of S. verticillata and S. officinalis leaves to determine the possibility of using non-pharmacopoeial species in pharmaceutical and medical practice. Materials and methods. The objects of the study are S. verticillata and S. officinalis leaves, which was harvested in the botanical garden of the I. Franko Lviv National University. The morphological and anatomical structure of the species leaves was studied by light microscopy. The study of macro- and microelement composition in the S. officinalis and S. verticillata leaves was carried out by atomic emission spectrographic method. Determination of the qualitative composition and quantitative content of the main groups of biologically active substances was carried out by HPLC. The quantitative determination of phenolic compounds was also carried out by spectrophotometric method. The anti-inflammatory activity of galenic extracts from the leaves of the studied species was studied using a model of acute inflammatory edema caused by subplant implantation of a carrageenin solution. Results. Using light microscopy, we studied the key microscopic and diagnostic signs of S. verticillata leaves. The content of 15 micro and macroelements was found in both studied species. 15 and 14 amino acids, 8 and 6 saponins, respectively, were identified in the S. officinalis and S. verticillata leaves. By HPLC, the qualitative composition and quantitative content of phenolic substances in the S. officinalis and S. verticillata leaves (13 and 12 compounds, respectively) was established. The maximum antiexudative effect of the dry extracts from the S officinalis and S. verticillata leaves was observed at a dose of 50 mg/kg. The dominant of elements are silicon, phosphorus, magnesium, calcium, sodium and potassium. The total content of trace elements in the leaves of S. verticillata is 1.78 times higher than in the pharmacopeia S. officinalis. The total content of saponins predominates in the leaves of S. verticillata and is 15.09 mg/g, which is 12.1 % more than in the pharmacopeia specie. The total flavonoid content in the leaves of S. verticillata is 1.57 times higher than in the pharmacopeia one S. officinalis, the content of hydroxycinnamic acids is highest in the S. officinalis leaves. The highest total content of all phenolic compounds is characteristic of S. verticillata leaves, which is 37.18 % (1.37 times) more than the pharmacopeia S. officinalis. At a dose of 50 mg/kg the anti-inflammatory effect of the dry extract from the S. verticillata leaves was comparable to the activity of the substance from the S. officinalis leaves. Conclusions. As a result of comparative pharmacognostic and pharmacological study of S. verticillata and S. officinalis leaves, it was found that S. verticillata is a promising species for introduction into medical and pharmaceutical practice, precisely as a source of phenolic compounds. The anti-inflammatory effect of the dry extract of S. verticillata leaves was compared with that of the substance of S. officinalis leaves, which indicates the possibility of creating a new anti-inflammatory medicine based on it.

Despite the popularity and efficiency of non-steroidal anti-inflammatory drugs and their widespread usage in clinical practice, this group of drugs is also characterized by numerous side effects, so obtaining of new safe NSAIDs is one of the priority tasks for modern pharmaceutical and medical chemistry. Aim. Studying of the anti-inflammatory activity of S-alkylated 1,3,4-oxadiazole-2-thiol derivatives with diclofenac fragment in the molecules. Materials and methods. The study of antiexudative activity of the compounds was carried out on the model of carrageenan-induced rat paw inflammation, quantitatively the effect was estimated by the index of inhibition of the inflammatory reaction. Results. During the research, highly active S-alkylated derivatives of 1,3,4-oxadiazole-2-thiol with antiexudative activity in the range of 42.4–44.6 % were identified, which is commensurate with the effects of the reference drugs diclofenac sodium and ketorolac. Conclusions. The obtained results indicate the presence of high antiexudative activity in a group of S-alkylated 1,3,4-oxadiazole-2-thiol derivatives, which actualizes the in-depth study of this class of heterocyclic compounds.

The biological activity of a number of N'-arylbenzenecarbоximidohydrazide hydrohalides in vitro against Staphylococcus aureus, Bacillus cereus, Escherichia coli and Candida albicans and Aspergillus brasiliensis fungi, as well as anti-inflammatory and analgesic activities in vivo has been studied. N'-(4-nitrophenyl)benzenecarboximidohydrazide hydrochloride (3c) exhibits marked antimicrobial activity against St. aureus, 4-nitro-N'-phenylbenzenecarboximidohydrazide hydrochloride (3b) is effective against C. albicans and A. brasiliensis fungi. Acute toxicity of the obtained compounds for mice with intragastric administration was 1000 to 2000 mg/kg and intraperitoneal administration was 200 to 400 mg/kg. 4-nitro-N'-phenylbenzenecarboximidohydrazide hydrochloride (3b) has anti-inflammatory and analgesic activities that do not exceed that of the reference preparations.

Medicinal plants have various pharmacological effects on a living organism due to their rich chemical composition. Therefore, a comprehensive study of herbal preparations in vivo is of great current interest. The grass of garden peony has a valuable complex of biologically active substances and is a promising raw material for extraction preparations. This work is devoted to the study of anti-inflammatory activity of the dry extract of the garden peony based on the model of “carrageenan edema”.

Abstract. Ascorbic acid (vitamin C, AA) is an essential nutrient of the human diet due to its participation on numerous regulatory and enzymatic processes. AA takes part in such vital physiological processes as hormone production, collagen synthesis, stimulation of the immune system, etc. In the present review the activities of AA are considered that provide its protective effect at influenza infection. This effect can be result of direct virus-inhibiting activity of AA as well as of anti-inflammatory and antioxidant properties. Oxidative stress during influenza infection leads to nonspecific damage of the pulmonary tissue and subsequent inflammation of the lungs. The antioxidant activity of AA results in alleviation of infection due to suppression of tissue damage as well as in inhibition of reactive oxygen species-mediated signal transduction and regulatory reactions. After oxidation by ROS, AA is converted to dehydroascorbic acid (DAA) and inhibits the key enzymes of NF-κB pathway, such as kinases IKKα and IKKβ. AA itself blocks the activity of another component of the NF-kB pathway, kinase IKKβ(SS/EE), whose activity is directed to the phosphorylation of the factor IκBα. As a result, activation of NF-κB and its transport to the nucleus does not occur. Thus, AA performs a dual function: first, it neutralizes free radicals, preventing them from activating NF-κB, and secondly, the product of its oxidation, DAA, further blocks the activation of this pathway. In addition, in some cases AA results in the decrease in the infectious activity of influenza virus that is not due to the antioxidant activity of AA, but to direct virus-inhibiting activity. Taken together, the presented data suggests that the use of drugs with antiviral and antioxidant activity, as a combination of individual drugs or, as in the case of AA, as a single drug with complex activity, for treatment of influenza has advantages over the etiotropic drug monotherapy scheme.

Аs a result of a set of scientific and experimental studies, gel and drug films have been developed that provide intensive mineralization of dentin. Previously conducted preclinical studies have studied the specific remineralizing activity and antimicrobial effect, as well as acute toxicity of dosage forms. To determine the anti-inflammatory activity, a model of acute inflammatory edema was used to evaluate the increase in the volume of the inflamed foot of rats, by introducing a phlogogenic agent. Based on the results obtained, it is established that the gel and the drug films have a sufficiently pronounced anti-inflammatory effect.

Aim. The approaches for creating novel agents with anti-inflammatory activity among sodium (3-R-2-oxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues were described in presented article. Methods and results. Mentioned methods have been based on combination of «in silico» screening with experimental studies. Affinity of studied compounds to the active center of COX-1 and COX-2 enzymes has been shown. Conducted visualization of compound – active site complex allowed to suppose the presence of anti-inflammatory activity of studied compounds. Conclusions. It was established, that sodium (3-R-2-oxo-2Н-[1,2,4]triazino[2,3-c]quinazoline-6-yl)alkylcarboxylates and their halogen-containing analogues reveal anti-inflammatory activity, the most active was compound DSK-38 (ED50 – 4 mg/kg as against 8 mg/kg of diclofenac sodium). «Structure–activity» relationships features among studied compounds have been discussed.

Nowadays all over the world there is an active search for new promising bioactive compounds and evaluation of their efficiency and safety for the usage in food for special dietary uses in order to form balanced healthy diets for different groups of consumers (children, pregnant and lactating women, etc.) or inclusion in diet therapy in order to increase the effectiveness of prevention and treatment of non-communicable diseases and reduce the need for medical care. Such substances can be cyclic peptides - compounds with a unique structure, thanks to which the stability of their configuration and high bioavailability are achieved, which, in turn, allows them to exhibit a wide range of biological effects. Basically, these bioactive compounds are extracted from the leaves and stems of medicinal plants or plants that have no tradition of food use in our country. Common flax (Linum usitatissimum), a crop widely used in nutrition, is practically their only food source. The purpose of the research was to generalize information on biological activity of flax cyclic peptides in order to assess the prospects of their food application. Material and methods . Systematic analysis of scientific literature was carried out using keywords (Linseed, or Flaxseed, or Flax, or Linum usitatissimum) and (Orbitide, or Cyclolinopeptide, or Linusorb, or LOMIX) in Google Scholar, PubMed systems. A total of 500 publications were identified and analyzed. Publish or Perish software was used for analysis. The topics of the publications were analyzed using KH Coder software. Results . Cyclic peptides are among the least studied components of flax, and the profile of cyclic peptides of domestic flax seed varieties has not been described so far. At the same time, the results of preclinical studies of flax cyclic peptides represent promising data that open prospects for their use in the therapy of various diseases. Immunosuppressive and anti-inflammatory activity, as well as hypocholesterolemic and antioxidant effects of flax cyclic peptides have been demonstrated. Conclusion . The current information on the biological activity of cyclic peptides is incomplete and should be expanded by new data obtained, in particular, in in vivo models and clinical trials. The study of the composition of flax cyclic peptides from domestic raw materials, the development and implementation of the methods of their extraction will contribute to the sustainable development of the industry and will allow reorienting the production of oilseed raw materials from its export to the introduction of knowledgeintensive technologies., Competing Interests: The authors have no conflict of interest to declare., (Copyright© GEOTAR-Media Publishing Group.)

It was shown in experiments on rats, that new complex phytoremedy, obtained from plants of Baikal region (regimen of administration. - 300 mg/kg daily, 1 week), demonstrate antialterative and antiexudative kinds of activity, as well as pharmacotherapeutical efficiency at conditions of aseptic inflammation.

Herbal medicines provide their versatile complex influence on the course of the pathological process in the kidneys due to biologically active compounds. Specifically, they cause the direct impact on the concrements formation. The search of drugs which would contain high biological compounds of plant origin is an actual issue of modern pharmacology. The aim of investigation was to study the anti-inflammatory activity of the new combined drug of urolytolytic action, which includes the total plant extract and succinate buffer complex. Materials and methods: aseptic exudative inflammation was caused by subplantar introduction of 0,1 ml of 1% solution of λ-karahenin in the right hind paw of rats, the investigated drug was administered at doses 1, 2 and 4 ml/kg. The influence of the studied drug was evaluated in terms of swelling limbs volume. It is shown that the severity of antiexudative action of flarosukcine had dose-dependent nature, increasing from dose of 1,0 ml/kg to 2,0 ml/kg (by 5,5%). Further dose increase to 4,0 ml/kg, was not defined by significant increase of activity. Anti-inflammatory activity of the drug ranged from 25 to 33%, which can be regarded as quite distinct, since in pharmacological study of anti-inflammatory drugs pharmacological activity level of at least 20% is significant. [ABSTRACT FROM AUTHOR]

Biomass of Arthrospira platensis has a long history of consumption as a source of protein, a number of micronutrients and minor biologically active compounds. Specific organoleptic properties of Arthrospira platensis biomass (pronounced bitter taste) limit its use as a source of phycocyanins. The developed modern methods of phycocyanin extraction from A. platensis biomass make it possible to obtain concentrates with improved sensory characteristics destined for the inclusion in foods for special dietary uses. The aim of this brief review was to analyze the results of the studies on the assessment of the biological activity of phycocyanin extracted from the Arthrospira platensis biomass, substantiating the prospects of using their concentrates for inclusion in foods for various dietary purposes. Material and methods . The PubMed Web Database, including MEDLINE article database, covering about 75% of the world's medical publications, was used for the main search for the literature. In addition, Scopus and Web of Science databases were used. Search depth - 15 years. Search keywords: Arthrospira platensis, phycocyanins, safety, antioxidant activity, immunomodulatory properties. Results and discussion. C-phycocyanin and allophycocyanin are complexes of proteins with the pigment phycocyanobilin, their total content is about 50% of the content of all proteins in the A. platensis biomass. A significant number of toxicological studies indicate that there are no risks to human health when using phycocyanin-containing extracts of A. platensis. Evidence of the antioxidant effect of phycocyanins extracted from A. platensis biomass, their anti-inflammatory activity, immunomodulatory properties, was obtained experimentally in vitro and in vivo, as well as in clinical studies. Conclusion . Toxicological studies and experimental in vivo tests have shown the safe and effective use of Arthrospira platensis biomass extracts with a high content of phycocyanins as an additional means of dietary prevention and diet therapy. These data indicate the prospects for conducting additional studies on the possibility of including phycocyanin concentrates in specialized foods for various purposes., Competing Interests: The authors declare no overt and potential conflict of interest related to the publication of this article., (Copyright© GEOTAR-Media Publishing Group.)