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Vol 25, No 7 (2022)
- Year: 2022
- Articles: 8
- URL: https://journals.eco-vector.com/1560-9596/issue/view/5742
Articles
Studying of the anti-ischemic effect of Orostachys spinosa dry extract in carotid arteries bilateral occlusion in white rats
Abstract
The aim of the study to evaluate the anti-ischemic effect of Orostachys spinosa dry extract in common carotid arteries bilateral occlusion in albino rats. Material and methods. The studies were carried out on 67 Wistar rats. O. spinosa extract was used as research object at doses 50, 100, 200 mg/kg. Introductory extract solution was administered intragastrically for 14 days prior to carotid arteries bilateral occlusion. The anti-ischemic effect of the O. spinosa extract was evaluated total mortality, dynamics of survival, mean life time, as well as the neurological status of animals using the modified McGraw scale and the degree of rats brain hydration. Results. It was found that the lowest animals mortality rate was observed in the experimental groups treated with O. spinosa extract at doses 100 and 200 mg/kg in carotid arteries common bilateral occlusion. The most pronounced statistically significant increase in life expectancy was observed in animals treated with O. spinosa extract at doses 50 and 100 mg/kg (by 38%, p<0.05) arelative to that of control animals. The least pronounced neurological deficit degree was observed in animals treated with O. spinosa extract at doses 50 and 100 mg/kg. The most pronounced statistically significant decrease in the brain hydration level was observed in animals receiving O. spinosa extract at a dose 100 mg/kg. Life expectancy in animals, treated with dry O. spinosa extract at doses 50 and 100 mg/kg was incresed by 38% (p<0.05) that of animals in the control group. The neurological deficit least pronounced degree was observed in animals treated with O. spinosa extract at doses of 50 and 100 mg/kg. The most pronounced statistically significant decrease in the level of brain hydration was observed in animals treated with dry O. spinosa extract at a dose 100 mg/kg. Conclusion. O. spinosa extract has a neuroprotective effect in cerebral ischemia, reducing the animals death percentage, increasing animals life expectancy, and reducing the neurological deficit degree and the cerebral edema severity.
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Study of pharmacological activity micronized purified flavonoid fractions of sea buckthorn meal
Abstract
Relevance. The research and comprehensive study of the therapeutic effects of flavonoids isolated from plant raw materials and waste products of its processing in modern conditions is becoming important. One of the available raw materials sources is advisable to consider the multi-tonnage waste of processing the fruits of buckthorn buckthorn (Hippophae rhamnoides L.) - meal. The aim of the work is to investigate the pharmacological activity of the micronized form of the composition of bio-flavonoids of fat-free sea buckthorn meal causing the phleboprotective activity in vitro and in vivo in comparison with the Detralex® preparation. Material and methods. The micronized purified flavonoid fraction from the fat-free buckthorn buckthorn meal (MPFF S-BM) was obtained by extraction of a bioflavonoid complex from the fat-free meal with ethyl alcohol concentration of 90% in the Soxlet apparatus, removal of solvent from the extract under vacuum, washing of a viscous syrupy mass of vacuum concentrate with water in a ratio of 1:3, filtration and drying sediment, followed by ultrasonic micronization of the flavonoid fraction in a liquid dispersion medium at an ultrasonic radiation power of 50 watts. The therapeutic effects of MPFF S-BM were studied: in vitro - using specific enzyme biotest systems based on glutathione reductase, catalase and iNO-synthase - antioxidant and anti-inflammatory activity, in vivo - on 30 male Wistar rats weighing 150-270 g according to the indicators of vascular-platelet and coagulation hemostasis. Results. With the help of specific enzyme biotest systems in vitro, it was revealed that the MPFF S-BM sample has an antioxidant and anti-inflammatory effect. In vivo experiments have established that MPFF S-BM after a preliminary course of administration at a dose of 25 mg / kg causes partial activation of the hemostasis system in rats, accelerating the onset of the initiation phase of blood clotting. Conclusions. Further research by MPFF S-BM is of great practical importance, since it opens up the prospect of creating new drugs of phleboprotective action.
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Evaluation of anti-ulcer activity of biologically active compounds in alder leaves
Abstract
Relevance. Erosive and ulcerative lesions of the stomach and duodenal ulcers are very common patology. Relevant is the development of new effective gastroprotective herbal remedies. Alder leaves contain a complex biologically active compounds, which causes antioxidant, antimicrobial, wound healing and anti-inflammatory action. In folk medicine alder is used to treat diseases of the gastrointestinal tract, however, there are no experimental data on gastroprotective properties of alder leaves. Material and methods. The objects of the study were black alder leaves and gray alder leaves harvested July 2020. The gastroprotective effect of black and gray alder leaf extracts was studied on the model of indomethacin erosive-hemorrhagic mucosal lesions membranes of the stomach, which was caused by a single intragastric administration to Wistar rats of indomethacin at a dose of 35 mg/kg per os. Results. It was established that the index of antiulcer activity for water extracts from black alder leaves in case of administering before the damage to the mucous membrane by the ulcerogen was 2.74, in case of administering after modeling the pathology - 2.65. For decoctions of gray alder leaves, the index of antiulcer activity in case of administering before indomethacin exposure was 2.02, in case of using after indomethacin administration was 2.5. The value of the index of antiulcer activity in all experimental groups is more than 2 confirms the presence of antiulcerogenic activity of biologically active compounds of black alder and gray alder leaves. Conclusion. Administration to white rats of water extracts of alder leads to a significant decrease in the amount ulcers in all experimental groups. Proven possibility of using for the treatment and prevention of erosive ulcerative lesions of the gastric mucosa of rats decoctions of black and gray alder leaves on the model of "acute" indomethacin ulcer.
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Study of Cichorium intybus L. Herb extract hepatoprotective activity in vitro and in vivo
Abstract
Relevance. According to the World Health Organization recommendations it is advisable to use herbal medicines in the treatment of approximately 75% of patients with digestive system diseases. Medicinal plant raw materials contain significant amounts of biologically active substances (e.g. flavonoids, phenolic acids, etc.), that are of substantial interest. One of these biologically active substances sources is Cichorium intybus L. herb. The aim of research is the hepatoprotective activity comparative study of the of biologically active substances fractions different polarity of the Cichorium intybus L.herb extract using specific enzyme biotest systems in vitro and confirmation attained results using in vivo models. Material and methods. Common Cichorium intybus L. herb extract fractions have been under study in this research. The Silimar substance was chosen as the reference drug. Аntioxidative and antitoxic activity was studied using specific enzyme biotest-systems in vitro. The identified in vitro protective effect was manifested through the activity of enzymes marking of the morphofunctional state of hepatocytes in rats and histopathological examination, against the background of toxic hepatitis induced by one-time tetrachloro-methane injection. Results. As a result of the research, it was shown that the aqueous fraction of the extract had the highest antioxidative and antitoxic activity in vitro using specific enzyme biotest-systems. Based on in vitro results it was provided the hepatoprotective activity of aqueous fraction. In vitro results were confirmed in vivo: prophylactic repeated administration of common chicory herb fractions into the body of rats with toxic liver damage caused a decrease in the activity of AST, ALT and AP. The greatest inhibitory effect on the activity of enzymes marking the functional state of rat livers had silymar (by 15%, ALT by 33% and AP by 14%, p<0.05) and aquatic (by 20.5%, 40.9% and II.8%, respectively; p<0.05) fraction. The research design was approved by the Bioethical Commission of the FGBNU VILAR. Conclusion. It was found the antioxidative and antitoxic activity BAS fractions of different polarity of the Cichorium intybus L. herb extract using specific enzyme biotest systems in vitro based on key homeostasis enzymes (catalase, glutathione reductase, cytochrome P450 and glutathione transferase). As a result of in vitro experiments, it was established and confirmed by the biochemical and pathohistological studies that the aqueous fraction had the most obvious biological activity This fraction contains chicoric and chlorogenic acids; and these compounds can play dominant role in the hepatoprotective effect of the fraction.
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Structure confirmation and enantiomeric composition of a phenyltetrahydroquinolinedione derivative with TRPA1-antagonistic activity
Abstract
Relevance. Chemical structure data on a new active pharmaceutical ingredient (API) is mandatory information submitted during registration of the original medicinal product. Spectral properties study makes it possible to confirm the structure of the new compound, and it is also the basis for the further development of the API quality control methods. Some organic compounds can exist in the form of several stereoisomers, which may either not differ in therapeutic effect or be responsible for various biological effects, including toxic ones. Therefore, it is extremely important at the early stages of drug development to establish the enantiomeric composition of a potential API for its further quality control. The aim of this study was to confirm the structure and determination of the enantiomeric composition of a potential API - the phenyltetrahydroquinolinedione derivative with TRPAl-antagonistic activity. Material and methods. 1H NMR, 13C NMR, IR, UV methods were used to confirm the structure of the API; the enantiomeric composition was determined on a liquid chromatograph with a chiral column. Results and conclusions. The studied compound structure was confirmed, IR and UV spectrophotometry methods can be used in quality control of the API in attribute "Identification", the API test sample is a mixture of four stereoisomers in equal proportions.
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Synthesis and evaluation of antimicrobial activity of new 1,3,5-triazine derivatives
Abstract
Aim. Synthesis of new 1,3,5-triazine derivatives (studied compounds, target compounds) and evaluation of their antimicrobial activity in silico and in vitro. Material and methods. The target compounds were obtained as a result of the reaction of 2,5-disubstituted-4-hydroxy-6H-1,3-oxazin-6-ones and S-methylisothiourea hemisulfate in the presence of an equimolar amount of sodium methylate in a methanol medium. The structure has been proven using modern physico-chemical analysis methods. Computer screening of biological activity was carried out using the PASS program located on the web service and accessible via the Internet. Experimentally, the antimicrobial activity of the compounds was studied in relation to the test culture of the microorganism - Staphylococcus aureus P209. Results. New derivatives of 1,3,5-triazine were synthesized with a yield of 66-72%. The structure of the obtained compounds was proved using 1H and 13C NMR spectroscopy, IR spectroscopy. As a result of screening of biological activity using the PASS program, data on a pronounced antimicrobial effect were obtained. The study of antimicrobial activity in vitro showed that the target compounds have an effect on Staphylococcus aureus P209. Conclusion. New derivatives of 1,3,5-triazine - 2-(methylthio)-4-(4-nitrophenyl)-6-ethyl-1,3,5-triazine, 2-(methylthio)-4-phenyl-6-ethyl-1,3,5-triazine, 2-(methylthio)-4-(4-methylphenyl) were synthesized-6-ethyl-1,3,5-triazine. Their structure has been proved using modern physico-chemical analysis methods. The results of computer prediction made it possible to determine the potential biological activity. Experimental microbiological studies have proved that the studied compounds have antimicrobial activity against Staphylococcus aureus P209.
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Peculiarities of essential oil accumulation by millet grass of common flora of Voronezh region
Abstract
Relevance. An important and little-studied aspect of the effects of human economic activity on medicinal plants is that in response to increased anthropogenic load, additional synthesis of secondary metabolites, is induced, which play an important role in the adaptation of plants to changing conditions. The purpose of the study was to study the features of the accumulation of essential oil in the grass of a thousand-leaf common, prepared in the agro- and urbocenoses of the Voronezh region. Material and methods. In the Voronezh region, 13 raw material harvesting points were selected to study the content of essential oil in it. Correlation coefficients were analyzed to examine in detail the effect of basic pollutants (heavy metals and arsenic) on the accumulation of essential oil. Results. All analyzed vegetable raw materials are considered benign in terms of essential oil content. The maximum amount of essential oil (0.76%) is noted in a sample of grass of an ordinary thousand leaf growing on the territory of the Khopersky Reserve. The minimum amount of essential oil is noted in the sample collected along the M4 route in the Pavlovsky district (0.18%). In general, for samples of control territories and agrobiocenoses, a higher content of essential oil can be noted than in samples of urbobiocenoses. The content of essential oil in the grass of bitter wormwood collected in territories deprived of human economic activity amounted to 0.68-0.76%, near agricultural land - 0.36-0.48%. In a number of urbanized territories, samples of grass of an ordinary thousand tree with a much lower content of essential oil - 0.18-0.39% - were harvested on the street of the cities of Voronezh, Ostrogozhsk, Borisoglebsk, along the M4 highway in Ramonsky and Pavlovsky districts, along the railway. Conclusion. The calculated values of correlation coefficients showed a strong negative effect of lead, cadmium, nickel, cobalt, zinc on the accumulation of essential oil in the grass of the bitter wormwood. The lowest content of essential oil was found in samples harvested on the streets of large cities of the region, along road routes and the railway. This makes it possible to conclude that the anthropogenic load has a negative effect on the accumulation of this group of compounds in the grass of the common thousand leaf.
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Experimental morphogenesis of Amomum tsao-ko Crevost & Lemarie. In vitro culture
Abstract
Relevance. A promising area of research in the field of biotechnology is the in vitro study of endemic plants used in folk medicine. Such plants include black cardamom (Amomum tsao-ko Crevost & Lemarie) - a medicinal plant. Extracts and essential oil are used in the treatment of respiratory diseases, have an antimicrobial effect, and also inhibit the development of human cancer cells. The main method of reproduction of A. tsao-ko is seed and vegetative. However, these methods have both advantages and disadvantages. Therefore, it is necessary to develop a technology for rapid reproduction of this culture in vitro. Purpose of the study. To study A. tsao-ko Crevost & Lemarie in vitro. Material and methods. The object of the study was A. tsao-ko seeds collected in the cardamom forest in the village of Sin Cau (22° 23'04.5"N 103 ° 32'44.0" VD), Giang Ma commune, Tam Duong district, Lai Chau province, Northwestern region of Vietnam. The seeds were superficially sterilized with 0.1% sulema solution for 10 minutes, then scarification was performed, after which the seeds were cultivated on a nutrient medium containing various concentrations of mineral salts according to Murashige and Skoog (MS). At the breeding stage, the effect of BAP (0.5-4 mg/l) and kinetin (0.5-2 mg/l) in combination with NAA (0.5-1 mg/l) on the proliferation of shoots and the formation of adventitious buds was studied. At the third stage of clonal micropropagation, the effect of NAA and IBA (0.25-1 mg/L) on the rooting of A. tsao-ko microbeads was studied. Results. It was found that scarification leads to an increase in seed germination by 12% compared to the control variant. Cultivation of isolated explants on a nutrient medium containing 1/16 of the norm of mineral salts according to MS, BAP 4 mg/l and NAA 0.5 mg/l contributed to obtaining the highest rates in terms of the number of adventitious shoots, their growth and the number of roots per explant. The best result for rooting microshoots was obtained on a medium containing 0.5 mg/l of IBA.
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