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Chemical investigation of the hydnoid fungus Sarcodontia setosa resulted in the isolation of five compounds, including two new sarcodontic acid derivatives - setosic acid (1) and 7,8-dehydrohomosarcodontic acid (2) along with three known benzoquinone pigments - sarcodontic acid (3), 4,5-dehydrosarcodontic acid (4) and dihydrosarcodontic acid (5). The structures were elucidated using spectroscopic methods (UV, NMR and HR-ESIMS). The biosynthetic relationship of the isolated compounds is proposed and discussed. Antibacterial activity screening of compounds 1-5 against ESKAPE bacterial strains in vitro with zones of inhibition was performed and MIC values were established for the most active compounds (3 and 5).
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One new compound isoembinin 1 along with ten known compounds 2-11 were isolated from the terrestrial parts of Iris lactea Pall. All of the compound structures were determined through extensive 1D and 2D NMR experiments along with HR-ESIMS analysis and comparison with literature data. Because many flavonoids exert antiplatelet and antioxidant activity we tested the effects of the isolated flavone C-glycosides 1-9 on platelet activation and reactive oxygen species (ROS) production. Platelet reactivity was assessed by activation of αIIbß3 integrins activation and ROS production by DCF-DA fluorescence. For the analysis of whether protein kinase A or G are involved in the platelet inhibition, the activity of these kinases was analyzed by phosphorylation of their common substrate in platelets. In all experiments apigenin, which inhibit platelet activation was used as a positive control. All isolated flavone C-glycosides inhibited platelet αIIbß3 integrins activation with IC50 in the µM range, however this inhibitory effect was found to not be mediated through the prevention of ROS formation or by the activation of cyclic nucleotide pathways. Structure-activity comparison between apigenin and compounds 1-9 shows that the presence of C-glycoside and O-glycoside residues on the aglycone apigenin diminish the degree of platelet inhibition.
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A new dihydrochalcone, 2',4'-dimethoxydihydrochalcone (1), together with 7 known compounds, 2',4'-dihydroxydihydrochalcone (2), 2'-hydroxy-4'-methoxydihydrochalcone (3), 2'-hydroxy-4'-methoxychalcone (4), 1-(3,5-dihydroxy-4-methoxyphenyl)-2-(3-hydroxyphenyl) ethane (5), 2,3,4,7-tetramethoxy-9,10-dihydrophenanthrene (6), 5-hydroxy-2,3,4-trimethoxy-9,10-dihydrophenanthrene (7) and 5,7-dihydroxy-6,8-dimethyl flavanone (8) were isolated from the shoots of Empetrum nigrum L. The structures of these compounds were elucidated using 1D and 2D NMR experiments along with HR-ESI-MS. Compound 6 is reported for the genus Empetrum for the first time.[Formula: see text].
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Chalconas , Ericaceae , Flavanonas , Ericaceae/química , Etano , Estructura MolecularRESUMEN
Two undescribed (1-2) and five known cyclic diarylheptanoids (3-7) were isolated from the false heartwood of white birch (Betula pubescens Ehrh.). All structures were elucidated through extensive 1D and 2D NMR experiments and HR-ESI-MS data, along with comparison of their spectroscopic data with those reported in the literature. The two new cyclic diarylheptanoids are betuladiol (1) and betulondiol (2). Extracts from false heartwood were evaluated for their antimicrobial activity against Klebsiella pneumoniae, Escherichia coli, Proteus mirabilis, Staphylococcus aureus and Cutibacterium acnes together with their antifungal activity against Candida albicans and Candida glabrata.
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Betula , Diarilheptanoides , Diarilheptanoides/química , Extractos Vegetales/química , Staphylococcus aureus , Escherichia coliRESUMEN
In the present study, we explored the therapeutic potential of bioreactor-grown cell cultures of the medicinal plant species Dioscorea deltoidea, Tribulus terrestris and Panax japonicus to treat carbohydrate metabolism disorders (CMDs) in laboratory rats. In the adrenaline model of hyperglycemia, aqueous suspensions of cell biomass pre-administered at a dose of 100 mg dry biomass/kg significantly reduced glucose level in animal blood 1-2.5 h (D. deltoidea and T. terrestris) or 1 h (P. japonicus) after adrenaline hydrochloride administration. In a streptozotocin-induced model of type 2 diabetes mellitus, the cell biomass of D. deltoidea and T. terrestris acted towards normalization of carbohydrate and lipid metabolism, as evidenced by a significant reduction of daily diuresis (by 39-57%), blood-glucose level (by 46-51%), blood content in urine (by 78-80%) and total cholesterol (25-36%) compared to animals without treatment. Bioactive secondary metabolites identified in the cell cultures and potentially responsible for their actions were deltoside, 25(S)-protodioscin and protodioscin in D. deltoidea; furostanol-type steroidal glycosides and quinic acid derivatives in T. terrestris; and ginsenosides and malonyl-ginsenosides in P. japonicus. These results evidenced for high potential of bioreactor-grown cell suspensions of these species for prevention and treatment of CMD, which requires further investigation.
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Diabetes Mellitus Tipo 2/tratamiento farmacológico , Dioscorea , Panax , Extractos Vegetales/farmacología , Tribulus , Animales , Biomasa , Reactores Biológicos , Glucemia/efectos de los fármacos , Metabolismo de los Hidratos de Carbono/efectos de los fármacos , Técnicas de Cultivo de Célula , Colesterol/sangre , Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Tipo 2/inducido químicamente , Diuresis/efectos de los fármacos , Hematuria/tratamiento farmacológico , Metabolismo de los Lípidos/efectos de los fármacos , Plantas Medicinales , RatasRESUMEN
Background: Polyherbal mixtures called "medical species" are part of traditional and officinal medicine in Russia. This review aimed to analyze medical species used in Russia for the treatment of diabetes and related disorders. The information relevant to medical species, diabetes, and obesity was collected from local libraries, the online service E-library.ru, and Google Scholar. The prediction of the antidiabetic activity for the principal compounds identified in plants was performed using the free web resource PASS Online. Results: We collected and analyzed information about the compositions, specificities of use, and posology of 227 medical species. The medical species represent mixtures of 2-15 plants, while the most frequently mentioned in the literature are species comprising 3-6 plants. The top 10 plants among the 158 mentioned in the literature include Vaccinium myrtillus L., Phaseolus vulgaris L., Taraxacum campylodes G.E. Haglund., Urtica dioica L., Rosa spp., Hypericum spp., Galega officinalis L., Mentha × piperita L., Arctium spp, and Fragaria vesca L. The leading binary combination found in medical species comprises the leaves of V. myrtillus and pericarp of P. vulgaris; leaves of V. myrtillus and leaves of U. dioica; and leaves of V. myrtillus and aerial parts of G. officinalis. In triple combinations, in addition to the above-mentioned components, the roots of T. campylodes are often used. These combinations can be regarded as basic mixtures. Other plants are added to improve the efficacy, treat associated disorders, improve gastrointestinal function, prevent allergic reactions, etc. Meanwhile, an increase in plants in the mixture necessitates advanced techniques for quality control. A feature of medical species in Russia is the addition of fresh juices, birch sap, seaweeds, and adaptogenic plants. Modern studies of the mechanisms of action and predicted activities of the principal compounds from medicinal plants support the rationality of polyherbal mixtures. Nevertheless, the mechanisms are not well studied and reported due to the limited number of compounds. Further investigations with calculations of synergistic or additive indices are important for strengthening the scientific fundamentals for the wider use of medical species in the therapy of diabetes. Two medical species, "Arfazetin" (7 medicinal plants) and "Myrphasinum" (12 medicinal plants), are approved for use in officinal medicine. The efficacy of these species was confirmed in several in vivo experiments and clinical trials. According to modern regulatory rules, additional experiments and clinical trials are required for more detailed investigations of the mechanisms of action and confirmation of efficacy. Conclusion: We believe that the scientifically based utilization of rich plant resources and knowledge of Russian herbal medicine can significantly contribute to the local economy as well as to the sectors seeking natural healing products.
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ETHNOPHARMACOLOGICAL RELEVANCE: Herbal medicine in Russia has a long history starting with handwritten herbalist manuscripts from the Middle Ages to the officinal Pharmacopoeia of the 21st century. The "herbophilious" Russian population has accumulated a lot of knowledge about the beneficial effects of local medicinal plants. Yet, for a long time, Russian traditional and officinal herbal medicine was not well known to the international audience. In our previous comprehensive review, we discussed the pharmacological effects of specific plants included in the 11th edition of the Pharmacopoeia of the USSR, which was also for a while used in Russia. The 14th edition of the Russian Federation's State Pharmacopoeia was implemented in 2018. AIM OF THE REVIEW: The aims of the present review are: (i) to trace the evolution of medicinal plant handling from handwritten herbalist manuscripts to Pharmacopoeias; (ii) to describe the modern situation with regulatory documents for herbal medicinal products and their updated classification; (iii) to summarize and discuss the pharmacology, safety, and clinical data for new plants, which are included in the new edition of the Pharmacopoeia. METHODS: New medicinal plants included in the 14th edition of the Russian Federation's State Pharmacopoeia were selected. We carefully searched the scientific literature for data related to traditional use, pharmacological, clinical application, and safety. The information was collected from local libraries in Saint-Petersburg, the online databases E-library.ru, Scopus, Web of Science, and the search engine Google scholar. RESULTS: Investigating the evolution of all medicinal plants referred to in the Russian Pharmacopoeias led us to the identification of ten medicinal plants that were present in all editions of civilian Russian Pharmacopoeias starting from 1778. In the 14th edition of the modern Russian Pharmacopoeia, medicinal plants are described in 107 monographs. Altogether, 25 new monographs were included in the 14th edition, and one monograph was excluded in comparison to the 11th edition. Some of the included plants are not endemic to Russia and do not have a history of traditional use, or on the other hand, are widely used in Western medicine. For 15 plants, we described the specificity of their application in Russian traditional medicine along with the claimed dosages and indications in officinal medicine. The pharmacology, safety, and clinical data are summarized and assessed for nine plants, underlining their therapeutic potential and significance for global phytopharmacotherapy. CONCLUSIONS: In this review, we highlight the therapeutical potential of new plants included in the modern edition of the Russian Pharmacopoeia. We hope that these plants will play an imperative role in drug development and will have a priority for future detailed research.
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Medicina Tradicional/métodos , Farmacopeas como Asunto/clasificación , Extractos Vegetales/clasificación , Extractos Vegetales/uso terapéutico , Plantas Medicinales/clasificación , Humanos , Medicina Tradicional/tendencias , Plantas Medicinales/química , Federación de Rusia/etnologíaRESUMEN
Chemical diversity of secondary metabolites provides a considerable variety of pharmacological actions with a significant extension due to their combinations in plant extracts. Production of plant-derived medicinal products in cell cultures has advantages because of the efficient use of different biotic and abiotic elicitors and better control of the developmental processes. Using PASS software, we predicted biological activity spectra for phytoconstituents identified in cell cultures of Panax japonicus (12 molecules), Tribulus terrestris (4 molecules), and Dioscorea deltoidea (3 molecules). Mechanisms of action associated with the antihypoxic effect were predicted for the majority of molecules. PharmaExpert software allowed analyzing possible synergistic or additive effects of the combinations of phytoconstituents associated with the antihypoxic action. Experimental studies of the antihypoxic effect of the plants' extracts in water and ethanol have been performed in 3 animal models: Acute asphyctic hypoxia (AAH), Acute haemic hypoxia (AHeH), and Acute histotoxic hypoxia (AHtH). Effects of Panax japonicus and Tribulus terrestris preparations exceeded the activity of the reference drug Mexidol in the AHtH model. In the AHeH model, all preparations demonstrated moderate activity; the most potent has been observed for Dioscorea deltoidea. Thus, we found that experimental studies in animal models have confirmed the in silico prediction.