Introduction. Today, one of the reliably known causes of mortality in the Russian Federation is diseases of the cardiovascular system, a significant part of which is associated with atherosclerotic disease. Combination therapy for diseases of the cardiovascular system includes, among other things, the use of modern lipid-lowering drugs, the use of which is often limited due to their pronounced side effects. In this regard, it seemed appropriate to search for new compounds of natural origin that potentially have lipid-lowering activity with minimal side effects. According to the scientific literature, natural phenolic compounds, namely substances from the group of flavonoids and isoflavonoids, have a set of such characteristics. In this regard, steelgrass (Ononis arvensis L.), the chemical composition of which is extremely rich and diverse in terms of flavonoids and isoflavonoids, can be a ra-ther promising source for searching and screening compounds with a given activity. The aim of the study. The purpose of the work was to study and predict the hypolipidemic activity of flavonoids and isoflavonoids of Ononis arvensis L. using in silico methods. Material and methods. The objects of the study were the structural formulas of flavonoids and isoflavonoids of field steelhead. Calculation of mo-lecular properties was carried out using the Molinspiration chemoinformatic software. Computer prediction of lipid-lowering activity was carried out us-ing the PASS-online service. Molecular docking was performed using the CB-Dock2 services for blind docking and Webina 1.0.5 for active site docking. Hepatotoxicity, mutagenicity and cytotoxicity of the analyzed biologically active substances were studied using the ProTox-II resource. Results. As a result of in silico studies, it was found that most of the studied flavonoids and isoflavonoids correspond to the Lipinski rule and the drug-likeness concept. In addition, for all studied biologically active substances, activities associated with a decrease in lipid fractions in the body were predicted. The results of molecular docking indicate that all analyzed compounds are capable of potentially inhibiting the enzyme HMG-CoA reductase, which makes it possible to predict the required lipid-lowering effect. Studying the toxicity of the research objects, most of them in silico demonstrated a high level of safety. Conclusions. The prospects for further research on the development of targeted technology for obtaining herbal preparations from steelhead, enriched with flavonoids and isoflavonoids, as well as subsequent tests to confirm hypolipidemic activity in in vitro and in vivo experiments are shown.
Relevance. In many countries plants have long been used in folk medicine as a source of medicines, as they are well tolerated, gradual development of therapeutic effect and a mild effect on the body. Due to these features such medicines are being safely used in the treatment and prevention of exacerbations of chronic diseases: of cardiovascular system, respiratory system, digestive system, pathologies of the urinary tract, etc., and also as a rehabilitation therapy after past diseases. The purpose of the study is to systematize and generalize the data of world literature concerning the general health-improving and tonic properties study of plants growing in the Republic of Buryatia. Material and methods. In this work used publication materials from the PubMed and е-library databases, search.rsl. The keyword search: restorative, tonic effect, herbal medicines, medicinal plants of Buryatia, biologically active substances, Astragalus membranaceus, Saposhnikovia divaricatа, Scutellaria baicalensis, Sedum roseum, Crataegus sangunea. The survey comprises the data of foreign and national articles, published on the topic during last 20 years. Conclusions. All the plants listed in this review are used for thousands of years in the Tibetan medicine. Based on the analysis of the presented literature data, their range of medicinal use is much wider, then the applications in modern clinical practice. The information reported in this review may be the basis for the development of new herbal medicines, including officinal mixture, with specified pharmacological properties.
Introdction. Herpesvirus infections are one of the leading medical and social problems and are defined as a "global problem of humanity". Currently, the most common are simple (HSV-1, HSV-2) and herpes zoster (VVO). For the prevention and treatment of herpesvirus infections, antiviral drugs are prescribed, one of which is the herbal drug Flakozid, 0.1 g tablets for oral administration. The aim of the work was a retrospective analysis of the results of an experimental and clinical study of Flakozid in simple recurrent and herpes zos-ter, chickenpox. Material and methods. The antiviral properties of Flakozid were studied in in vitro experiments, in the culture of chicken embryo fibroblast cells against three strains of herpes virus (2 strains geratogenic "10", "90" and dermatogenic strain "64") and in vivo − on a model of experimental herpetic encephalitis of white mice in doses from 20 mg/kg to 500 mg/ kg with the administration of per os and subcutis. The results of the clinical study of Flakozid were analyzed in 313 patients (adults and children) with simple recurrent herpes 202 patients, including genital – 65, with herpes zoster – 45, chickenpox – 66. The criteria for the effectiveness of antiviral therapy of herpes were the duration of inflammatory phenomena, a reduction in the number and duration of relapses; in chickenpox – the severity of symptoms of intoxication, the nature and spread of rashes, the degree of their re-verse development. Flakozid was prescribed 0.2–0.6 g per day. Results. Experimental studies have shown that Flakozid had a high viral inhibitory effect against Herpes simplex. Treatment with Flakozid led to a high therapeutic effect: complete resolution of rashes in simple recurrent herpes after an average of 6-14 days, genital – 8-15 days, shingles – 7-15 days and shortening the duration of relapses by 2 times. The therapeutic effect of Flakozid in the treatment of genital herpes was noted in 91.6% of cases and exceeded the effect of Alpizarin (40%); in chickenpox –74%. Conclusions. The high therapeutic effect of Flakozid in the treatment of viral infectious and inflammatory dermatoses in adults and children allowed it to be recommended in a wide clinical practice in the treatment of simple recurrent herpes, including genital and extragenital localization; herpes zoster, chickenpox.
Intriduction. Currently, the antibiotic resistance development in pathogenic microorganisms remains a global problem. To solve this problem, an active search and development of new antimicrobial drugs, including those of plant origin, is underway. In the many years course of experience in this area, methods used to determine antimicrobial activity are being developed and improved, however, not all of them are suitable for determining the activity of biologically active substances of plant origin. The purpose of the study. To summarize information about existing methods for determining antimicrobial activity under in vitro experimental conditions. Material and methods. The article is based on publication materials from the PubMed and E-library databases, search.rsl. The literary search was carried out by keywords: antimicrobial activity, antibacterial effect, antibiotic, herbal preparations. The review includes articles that are relevant to the research topic and have been published over the past 10 years. Results and discussion. The article describes the main methods for determining antimicrobial activity in vitro and determines the possibility of using these methods in relation to herbal remedies. Conclusions. The findings indicated that the choice of the research method should depend primarily on the object under study and the type of microorganism in respect of which the activity is determined. Most of the developed and widely used methods for determining antimicrobial activity do not allow an adequate assessment of the activity of herbal remedies. Thus, when working with herbal remedies, the methods of double serial dilutions in liquid nutrient media with the use of indicators and the developing direction of activity research on biofilms can be considered the most accurate.
In ethnomedicine of European and Asian countries, both the roots and herbs of the restharrow are used to treat a number of diseases. The purpose of the study is to assess the qualitative and quantitative composition of tinctures based on the content of saponins. Research was carried out to confirm the presence of saponins and make their quantitative determination in experimental samples of tinctures of herbs and roots of field restharrow (Ononis arvensis L.) collected in the Altai Region and in tinctures of herbs and roots of intermediate restharrow (Ononis intermedia L.) and field restharrow (Ononis arvensis L.) growing in the Nakhchivan Autonomous Republic. Experimental samples of tinctures from the roots and herbs of the field restharrow and the roots and herbs of the intermediate restharrow were made by maceration using 70 % ethyl alcohol as an extractant. Studies were carried out to confirm the presence of triterpenoid saponins in the studied samples of tinctures by the foaming reaction using the Fontan-Kandel method, the qualitative Lafon reaction, and the qualitative Salkowski test. A technique has been adapted for the quantitative determination of saponins in terms of glycyrrhizinic acid using spectrophotometry at a wavelength of 258 nm. A technique has been adapted for the quantitative determination of saponins in terms of the ammonium salt of aralosides using spectrophotometry at a wavelength of 510 nm. The tests carried out confirmed the presence of triterpenoid saponins in the tested samples of tinctures from the roots and herbs of the field restharrow and the intermediate restharrow. The presence of saponins was significantly higher in the tested samples of tinctures from the roots of both field restharrow and intermediate restharrow.
The pharmacological activities of wild common chicory herb extract and cultivated chicory leaf extract were compared to reveal promising sources of antioxidant, hepatoprotective, and immunomodulatory biologically active substances (BAS). The bioactivities of common chicory extracts were examined in vitro using four specific enzyme bioassay systems (SEBS) based on glutathione reductase (GR) and catalase (CAT), cytochrome P450 and glutathione transferase (GTF), and NADPH-oxidase. The addition of wild common chicory herb extract at a concentration of 3.3 µg/mL to the incubation medium increased the rate of the GR reaction by 91
Relevance. The leaves of the Plantago major are a pharmacopeic medicinal plant raw materials, quite well studied in relation to the chemical compo-sition and spectrum of medical use, but the list of drugs based on them today is limited. In this regard , it seemed to be relevant to study the possibil-ity of developing a drug in the form of a medicinal pencil containing an extraction complex of Plantago major leaves, enriched with flavonoids. To solve this problem, it was necessary to choose an extragent that selectively extracts the biologically active substances of the Plantago major leaves, with a predominance of flavonoids. The aim of the work was a comparative study of the chemical composition and immunotropic effects of the in vitro heteropoly fractions of the leaves of the Plantago major leaves. Material and methods. The object of research was the leaves of the Plantago major. The content of extractive substances in the raw materials was determined by the pharmacopeic method of single extraction using extractants of various polarity: purified water, 40 %, 70 % and 95 % of ethyl alco-hol. The content of the amount of flavonoids in extracts in terms of cinaroside was carried out by differential spectrophotomeria. Heteropoly fractions were obtained by the method of reperculation in a battery from 3 laboratory percolators with subsequent condensation and drying. The assessment of the phagocytic and microbicidal function of neutrophilic granulocytes carried out in vitro on the samples of peripheral blood of conditionally fast-ash persons. Results. It was revealed that the content of extractive substances was reduced with a decrease in the polarity of the extractant, while the content of the extracted amount of flavonoids increased. Comparative immunological studies included the extracts of Plantago major leaves, obtained with the use of 70 % and 95 % of ethyl alcohol. An analysis of their immunotropic effects showed that the fraction extracted by 70% alcohol, statistically sig-nificantly increased the indicators of the phagocytic number, phagocytic index and the relative number of neutrophilic granulocytes that absorb bacte-ria. In addition, in its presence, the digestive ability of neutrophilic granulocytes and the digestion index relative to indicators of the control group in-creased, the activity of NADPH-oxidase and the number of formsan-positive neutrophil granulocytes increased. Conclusions. A comparative assessment of the effect of heteropoly fractions of Plantago major leaves on the phagocytic and microbicidal functions of neutrophilic granulocytes showed that the most pronounced positive immunotropic effect was demonstrated by the fraction extracted with 70% ethanol.
Проведено сравнительное изучение фармакологической активности экстракта травы дикорастущего и экстракта листьев культивируемого цикория обыкновенного как перспективных источников антиоксидантных, гепатопротекторных и иммуномодулирующих биологически активных веществ. Первичный скрининг биологической активности экстрактов изучали с использованием специфических ферментных биотест-систем in vitro на основе глутатионредуктазы (ГР) и каталазы (КАТ); цитохрома Р450 и глутатионтрансферазы (ГТ); НАДФН-оксидазы. При внесении экстракта травы дикорастущего цикория обыкновенного в концентрации 3,3 мкг/мл в инкубационную среду скорость ГР-реакции увеличивалась на 91 %, КАТ – на 37 % по сравнению с контролем. С применением специфических ферментных биотест-систем на основе цитохрома Р450 и ГТ установлено, что экстракт листьев культивируемого растения в концентрациях 2,0 мкг/мл обладал менее выраженным действием по сравнению с экстрактом травы дикорастущего растения на активность ключевых ферментов системы биотрансформации. Полученные результаты подтверждены на модели токсического поражения печени крыс, вызванного тетрахлорметаном in vivo. В экспериментах использовали нелинейных крыс самцов массой тела 200 ± 20 г. С использованием специфической ферментной биотест-системы на основе НАДФН-оксидазы из лейкоцитов крови кроликов показано, что экстракт листьев культивируемого цикория в концентрации 3,3 мкг/мл проявлял более выраженные иммуномодулирующие свойства по сравнению с экстрактом травы дикорастущего растения.
Введение. Поиск растительных источников БАВ адаптогенного действия представляет научный и практический интерес. Однако, важной проблемой их использования как источника БАВ, является доступность исходного сырья, так как часто оно невелико. Одним из решений данной проблемы является культивирование перспективных в качестве сырья растений in vitro. Изучение биологической активности субстанций, полученных из клеточных культур, заслуживает особого внимания. Цель исследования – изучение в опытах in vivo адаптогенных свойств комплекса БАВ из суспензионных клеточных культур женьшеня обыкновенного и родиолы розовой полученных в ФГБНУ ВИЛАР. Методика. Объекты исследования: экстракты из суспензионной клеточной культуры женьшеня обыкновенного и родиолы розовой, входящие в состав Биологической коллекции ФГБНУ ВИЛАР. Фармакологические исследования проводили на белых нелинейных мышах и белых нелинейных крысах. Острую токсичность изучали по методу Кербера. Влияние экстрактов на нервную систему изучали на модели «открытое поле норкового типа». Проведено изучение влияния экстракта на продолжительность жизни мышей на модели гипоксии с гиперкапнией в гермообъеме, а также на выносливость и работоспособность на модели «вынужденное плавание с грузом» на мышах. Результаты. Было показано, что экстракты из суспензионных клеточных культур женьшеня обыкновенного и родиолы розовой малотоксичны, обладают адаптогенной активностью, оказывают антигипоксическое действие в условиях модели гипоксии с гиперкапнией в гермообъеме, повышают физическую работоспособность и выносливость в условиях модели «вынужденное плавание с грузом», а также не оказывают отрицательного влияния на нервную систему и поведение опытных животных. Заключение. Клеточные культуры женьшеня обыкновенного и родиолы розовой являются перспективным биотехнологическим сырьем для разработки на их основе безопасных лекарственных средств, повышающих неспецифическую сопротивляемость организма к негативным воздействиям окружающей среды и стрессу. The search for phytocomponents with adaptogenic activity is an important task of modern pharmacology. At the same time, an important problem for their use is the availability of raw materials, plant-to-plant variability in medicinal content, etc. An efficient and well suited solution to these problems is in vitro systems for production of medicinal plants and their extracts. Therefore, the biological activity of such in vitro-produced substances should be studied. Aim of the study: to determine in in vivo experiments the pharmacological activity of Panax ginseng and Sedum roseum cell culture extracts obtained in the All-Russian Research Institute of Medicinal and Aromatic Plants. Methods. Extracts of Panax ginseng C.A. Mey and Sedum roseum (L.) Scop. cell cultures (from the All-Russian Research Institute of Medicinal and Aromatic Plants Biological Collection) were studied. Pharmacological studies were performed on white, outbred mice and rats. The studies were approved by the local Bioethical Committee. Acute toxicity was studied using the Kerber method. The effect of the cell culture extracts on the nervous system was studied using the forced swim test with weight load and open field test. Experimental studies of the adaptogenic effect of the cell culture extracts were performed in animal model of hypoxia with hypercapnia. Results. Panax ginseng and Sedum roseum cell culture extracts have low toxicity and have adaptogenic activity. Effects of both cell culture extracts in the forced swim test with weight load demonstrated increased performance efficiency and fitness. In the hypoxia-with-hypercapnia study of antihypoxic adaptogenic action, there was no negative impact on the animals’ nervous system. Conclusion. Extracts of Panax ginseng and Sedum roseum cell cultures are a promising biotechnological raw material for developing drugs to increase the body’s nonspecific resistance to adverse environmental influences and stress.
В настоящее время в медицине широко применяются лекарственные препараты растительного происхождения. Однако они отличаются сложным химическим составом, содержание отдельных компонентов может меняться в зависимости от погодных условий, мест произрастания, изменений состава почвы и т.д. Всё это указывает на необходимость контроля каждой партии лекарственного растительного сырья по химическому составу или целевой биологической активности. Контроль биологической активности чаще всего проводят с использованием лабораторных животных. Во всех странах мира такие эксперименты строго контролируются законами и могут проводиться только с их соблюдением. Основываясь на принципах «трех R» в ФГБНУ ВИЛАР разработан альтернативный метод с использованием специфических ферментных биотест-систем (СФБТС) in vitro на основе ключевых ферментов гомеостаза. Целью работы являлось экономическое обоснование возможности использования СФБТС в оценке биологической активности растительных лекарственных средств на примере четырех экстрактов красных листьев винограда культурного (Vitis vinifera L.) различных сортов. При оценке их венотропной активности с применением СФБТС in vitro по сравнению с методами in vivo сокращаются затраты: временные в 2 раза, финансовые в 2,8 раз, количество лабораторных животных в 4 раза.
Relevance. One of the important directions of medical science and practice remains the introduction and improvement of existing methods and means for the treatment of dermatological diseases of various etiologies. At the same time, the search for new wound-healing drugs that can com-prehensively affect the wound process is relevant. Practical dermatology has an extensive range of synthetic antimicrobial, anti-inflammatory and wound healing agents. However, despite their known effectiveness, many of them are characterized by the presence of undesirable reactions for the body, such as allergies, dry skin, the formation of resistance, the development of withdrawal syndrome, a decrease in the local and general immuno-logical response of the body. The solution of this problem can be facilitated by the use of an ointment based on a dry extract of the herb Eupatorium cannabinum L., for which, along with known antimicrobial properties, there are grounds for predicting a wound-healing effect. The aim of the study was to study the wound-healing activity of antimicrobial ointment with a dry extract of cannabis herb in order to predict the possibility of use in medical practice as a polyvalent agent for the treatment of wound processes. Material and methods. An ointment was developed with a dry extract of cannabis herb, the wound-healing activity of which was determined on a simulated «linear» skin wound in male rats weighing 200.0 ± 20.0 g. An assessment of the restoration of the skin in experimental groups of animals and in control was carried out. Results. It was revealed that the restoration of the epithelium with the formed dry, pink, natural tissue and wool coating in the groups of rats treated with an experimental soft dosage form occurs earlier than in the control groups treated with a control ointment for an average of 6–8 days. Conclusions. The results obtained allow us to recommend an ointment with an extract of the herb Eupatirum cannabinum as a means of plant origin, which has a polyvalent, including the wound-healing effect revealed in experiments.
Introduction. One of the most common bacterial infections includes acute and chronic tonsillitis, affecting 10 to 15 % of adults and approximately 20–25 % of children worldwide, according to the World Health Organization. The focus of this study was an original substance, sangviritrin, containing no less than 96.5 % of the sum of bisulfates of two alkaloids: sanguinarine and chelerythrine. Given the high antimicrobial activity of sangviritrin, the research aimed to develop a local delivery system based on this medicinal substance.Aim. The aim of this work was to develop an oral medicinal form of sangviritrin.Materials and Methods. Sangviritrin, produced by the All-Russian Scientific Research Institute of Medicinal and Aromatic Plants, was used as the active pharmaceutical ingredient. The selection of auxiliary components was carried out in accordance with the methodologies specified in the State Pharmacopoeia XV edition. The organoleptic properties of the substance and spray samples were studied using A. I. Tenzova's method. The local irritant action of the spray was assessed using the conjunctival test method on chinchilla rabbits weighing 3.5–4.3 kg. Quantitative determination of sangviritrin in the medicinal form was performed using spectrophotometric methods at a wavelength of 321 ± 2 nm on a spectrophotometer SPECORD® 200 PLUS (Analytik Jena GmbH+Co. KG, Germany).Results and Discussion. Optimal auxiliary component compositions were selected based on measurements of spray technological parameters. A comprehensive approach was justified for correcting the organoleptic properties of the substance, involving the introduction of a minimal amount of sweeteners and additional use of β-cyclodextrin. Examination of the local irritant action indicated a "weak or absent" degree of local irritation.Conclusion. A local delivery system for sangviritrin has been developed for the treatment of infectious and inflammatory diseases of the oral cavity.
Introduction. The use of a combined herbal extract of chamomile flowers, calendula flowers and yarrow herb (patent RU 1 561 262 C) can be effective against various microbial strains, including those causing inflammatory diseases of the oral cavity. The article presents the results of a comparative pharmaceutical and technological study of an adsorbed liquid plant extract on sorbents of various nature for subsequent introduction into the composition of orodispersible tablets.Aim. To select the optimal sorbent of liquid plant extract of chamomile flowers, calendula and yarrow herb ensuring the suitability of the active pharmaceutical ingredient for direct compression, by analyzing using the SeDeM expert system method.Materials and methods. Active pharmaceutical ingredient was adsorbed on organic (microcrystalline celluloses of various brands) and inorganic (colloidal silicon dioxide of various brands) sorbents, a liquid combined plant extract of anti-inflammatory and antibacterial action of chamomile flowers, calendula flowers and yarrow herb. Pharmaceutical-technological analysis included the study of such technological parameters as: Bulk Density (Da = m/Va), Tapped Density (Dc = m/Vc), Inter-particle Porosity (Ie = (Dc – Da)/(Dc · Da)), Carr index (IC = (Dc – Da)/(Dc · 100)), Cohesion Index (Icd), Hausner Index ratio (IH = Dc/Da), Angle of Repose (Tgα = h/r), Powder Flow (t), Loss of Drying (%LoD), Hygroscopicity (%H), Particles <50 μm (%Pf), Homogeneity Index (IΘ = Fm/100 + ∆Fmna).Results and discussion. A comprehensive pharmaceutical-technological study of sorbents of liquid plant extract before and after adsorption was carried out, the results of which were processed and presented by the SeDeM expert system method. It was found that the adsorption of the extract has a positive effect on the Dimension (ID = (Da · Dc)/2) of all studied sorbents which may be related to change in the fractional composition due to the aggregation of small particles during adsorption and destruction of large ones when sifting the finished mixtures through a sieve with a mesh diameter of 200 μm (recommended insoluble particle size for use in the oral cavity). A negative effect on the Stability (IS = (%LoD · %H)/2) was also recorded for all samples, regardless of their nature, which is probably explained by residual moisture after drying and high hygroscopicity of adsorbed plant bioactive substances. Changes in the Compressibility (IC = (Ie · IC · Icd)/3), Flowability (IF = (IH · α · t)/3) and Dosage (IDos = (%Pf · IΘ)/2) are individual.Conclusion. The SeDeM expert system method makes it possible to characterize bulk materials from the point of view of suitability for direct compression, to establish the factors that need to be primarily corrected by the introduction of auxiliary substances. As a result of the conducted studies, Aeroperl 300 (inorganic sorbent) and Pharmacel 112 (organic sorbent) can be recommended for the introduction of liquid plant extract of chamomile flowers, calendula flowers and yarrow herb into the composition of orodispersible tablets.
Aim. To evaluate the antitoxic activity of chicory herb extract fractions in rats with toxic hepatitis.Materials and methods. There were 64 male rats were divided into groups of 6 animals that received the whole chicory herb extract, its fractions, or the reference drug (RD) and 2 groups did not receive any drug. The Silimar substance (a dry purified extract obtained from the fruits of milk thistle [Silybum marianum]) was chosen as RD. Animals from one of the groups that did not receive the drug (control group) and the groups that received drugs were injected with CCl4 to simulate toxic liver damage. The last group of animals received neither drugs nor CCl4 (intact animals). The changes in the activity of biotransformation enzymes (cytochrome P450 [cytР450] and glutathione transferase [GT]) in hepatocytes and serum liver enzymes (AST, ALT and AP) were assessed.Results. There was a decrease in cytР450 and GT activity in the liver microsomes of control rats (having CCl4 hepatitis without treatment) compared with intact animals. These parameters were more in the animals that were administrated with chicory herb extract, its fractions, and RD than in control animals. The administration of the whole extract, aqueous fraction, and RD led to an increase in the activity of cytP450 and GT enzymes almost to the level of the same indicators in intact animals. Pronounced grown in the activity of serum liver enzymes (ALT, AST and AP) were found after CCl4 injection. Administration of common chicory herb fractions before toxic liver damage caused a decrease in the grown of the activity of these enzymes. The greatest inhibitory effect on the grown of the activity of these liver enzymes had RD, aqueous and butanolic fractions of chicory herb. Despite a significant decrease in hyperfermentemia found in groups of animals treated with fractions of chicory herb, AST, ALT and AP activities did not reach the level that was in the intact animal group.Conclusion. The aqueous and butanolic fractions of the chicory herb extract had the highest antitoxic activity in experimental animal toxic liver injury.