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HEPATOPROTECTIVE EFFECT OF GOLDEN VOLODUSHKA (BUPLEURUM AUREUM L.) HERB EXTRACT OF DRY IN EXPERIMENTAL TOXIC HEPATITIS IN RATS

Introduction. The search for new medicines, including those of plant origin, for the treatment of diseases of the hepatobiliary system is relevant and timely. A promising source for the development of hepatoprotective drugs is golden volodushka (Bupleurum aureum L.). To date, a large evidence base has been accumulated for the biochemical study of this plant, its pharmacological activity has been scien-tifically proven. Good stocks of golden volodushka in the wild, the simplicity of its harvesting and the possibility of cultivation were noted. The VILAR State Medical University has developed a method for obtaining volodushka golden herb extract of dry. Aim. The study of the pharmacotherapeutic efficacy of volodushka golden (Bupleurum aureum L.) herb extract of dry in case of liver damage under experimental conditions. Material and methods. In the studies, white non-linear male rats with a body weight of 180-200 g were used. Volodushka extract was studied at doses of 50 and 100 mg/kg. The comparison drug was silimar at a dose of 100 mg/kg. Experimental CCl4 – induced hepatitis in rats was caused by a single subcutaneous injection of 50% carbon tetrachloride oil solution one hour after the last administration of the studied extract and the comparison drug. After 48 hours, blood was taken from the tail vein of rats, serum was obtained and its biochemical analysis was carried out. Next, the rats eu-thanized in a CO2 chamber and the liver extracted for pathophysiological evaluation. Tetracycline hepatitis was caused by intragastric administration of tetracycline to animals at a dose of 500 mg/kg. Then, after 48 hours, blood was taken from the animals, serum was obtained and its biochemical analysis was carried out. Results. Volodushka golden grass dry extract on a model of carbon tetrachloride hepatitis exhibits a hepatoprotective effect, which is confirmed by a comparative pathophysiological study and a study of the activity of enzyme markers of the morphofunctional state of the liver in rat blood serum. In the tetracycline hepatitis model, the studied extract also has a hepatoprotective effect, which is confirmed by biochemical studies. Conclusions. Studies of volodushka extract in conditions of experimental liver lesions have shown that the studied extract in experimental therapeutic doses has a pronounced hepatoprotective effect and is promising for the creation of a herbal medicine for the prevention and treatment of diseases of the digestive system.

Development of emulgel formulation from Markhamia tomentosa leaf extract: Characterization and in vitro antimicrobial activity against skin isolates

Objectives: Skin infections are mild to severe infections often treated with antimicrobial agents. There is an increase in resistance to antimicrobial agents necessitating the search for new medicines. This study developed an emulgel formulation of Markhamia tomentosa leaf extract and evaluated its antimicrobial activity against skin isolates. Materials and Methods: A successive extraction of M. tomentosa leaves in five solvents – n-hexane, dichloromethane, ethyl acetate, ethanol, and distilled water was carried out. The activity of the extracts against skin isolates of Staphylococcus aureus, Staphylococcus epidermidis, and Bacillus subtilis was carried out. The distilled water extract was formulated into emulgel, characterized, and evaluated for antimicrobial activity. Results: The n-hexane and dichloromethane extracts of M. tomentosa were inactive against all organisms at concentrations used. The ethanol extract was active against S. aureus and S. epidermidis at 200 mg/mL. The ethyl acetate and distilled water extracts were active against S. epidermidis and B. subtilis at 100 and 50 mg/mL, respectively. All emulgel formulations of distilled water extract of M. tomentosa leaves were brown, smooth, and easy to spread on the skin and had a pH of 4.73–5.55. The formulation containing the distilled water extract was more viscous (7784cP) than the blank formulation (6328cP). The formulation was active against S. epidermidis. Conclusion: The distilled water extract of M. tomentosa leaves was the most active against S. epidermidis and B. subtilis. Its emulgel formulation had desirable physicochemical properties for application to the skin. Further studies can be carried out toward its development for the treatment of skin infection caused by organisms investigated.

MICROBIOLOGICAL CHARACTERISTICS OF THE EFFECTIVENESS OF THE TREATMENT OF RATS WITH AN EXPERIMENTAL INFECTED WOUND USING AN ANTISEPTIC AND AN IMMUNOMODULATOR

Despite the outstanding achievements in treating wounds, the question of the development and search of new medicines and new medicinal antimicrobial compositions, which would provide an opportunity to improve the treatment of infected and purulent wounds in modern conditions, is still relevant.Material and methods. On the basis of the Department of Microbiology and the veterinary medical clinic of National Pyrogov Memorial Medical University (Vinnytsya, Ukraine), an experimental study was conducted, which consisted of the microbiological evaluation of the use of the immunomodulator "Blastomunil" in the treatment of infected wounds in rats. Under anesthesia, a wound of 1.5x1.5 cm was made in the interscapular area of the animals. It was infected, and then it was treated by intramuscular injection of Blastomunyl, or its local application as monotherapy or in combination with Decamethoxine. The collection of material from the wounds for microbiological research was carried out for 3, 7, 10 and 14 days, followed by a microbiological study of the quantitative content of microorganisms in the wound and their species identification. Numerical values of the number of microorganisms in wounds were expressed as the decimal logarithm of colony-forming units per ml (lg CFU/ml).Research results. Indicators of S.aureus wound contamination on the third day decreased from the 3rd to the 6th group by 1.35, 1.32, 1.46, 1.49, 1.26. and 1.29 times, respectively, with the most significant indicators in 5 (3.74±0.14 lg CFU/ml) and 6 (2.48±0.45 lg CFU/ml) groups, which were significantly different from the control (p<0.05). Regarding P.aeruginosa, a significant logarithmic decrease in microbial contamination was observed in groups 3 (3.78±0.26 lg CFU/ml), 5 (3.12±0.17 lg CFU/ml), 6 (2.48±0.45 lg CFU/ml), and the reduction was respectively, 1.37, 1.66 and 2.09 times, and for the 6th group was reliably the most significant (p<0.05). On the 7th day, a decrease in the number of S.aureus and P.aeruginosa CFU was observed in all groups compared to the control. The most significant decrease in the level of microbial colonization of S.aureus wounds was found in group 5 (2.96±0.08 lg CFU/ml), and its multiplicity was 1.99 times, respectively, compared to the control (p<0.05). A significant reduction in the colonization of wounds by the opportunistic gram-negative bacillus P.aeruginosa was established on the 7th day in groups 5 (2.32±0.36 lg CFU/ml) and 6 (1.43±0.65 lg CFU/ml), the multiplicity of logarithmic reduction of contamination was significant and reliable ( p<0.05) and was 2.0 and 3.26, respectively. On the 10th day, the load of S.aureus in wounds in groups 3-6 significantly decreased. Multiplicity compared to the control was determined in 1.4, 1.54, 2.24, 2.2 times, respectively, with the best result in 5 (2.06±0.04 lg CFU/ml) and 6 (1.9±0.52 lg CFU/ml) groups. For P.aeruginosa, a reliable logarithmic decrease in microbial colonization was determined for groups 2-6, and the multiplicity compared to the control was 1.46, 1.38, 1.91, 1.86, 1.38 times with the best indicators in groups 5 (1.85±0.66 lg CFU/ml) and 6 (1.9±0.52 lg CFU/ml) (p<0.05). On the 14th day, complete eradication of S.aureus and P.aeruginosa was established in wounds of groups 3-6. In the second group, the level of contamination still remained at an insignificant level and was 1.55±0.49 lg CFU/ml S.aureus and 1.04±0.2 lg CFU/ml P.aeruginosa, which is 4.2 and 5 times less than in the control group.Conclusion. Blastomunyl indirectly, apparently due to its immunomodulatory effect, exhibits significant antimicrobial properties, both when administered intramuscularly and when used locally as monotherapy or in combination with Decasan.

The Effect of Whole Blood and Bone Marrow with the Addition of Pyrimidine-2,4(1h,3h)-dione Thietanyl Derivatives on Free Radical Oxidation.

It is relevant to study the general patterns and identify non-specific mechanisms of body protective and adaptive reactions violation, which can lead to the various pathological processes and develop principles for the correction of these disorders. One of the therapy and prevention directions is the search for new medicines. In recent years, new derivatives of pyrimidine bases have been synthesized and studied. Pyrimidine-based medicines have a membrane-stabilizing and immunomodulatory effect and can normalize metabolic disorders and increase the oxidative activity of leukocytes. Disruption of the free radical oxidation processes, the generation of reactive oxygen species and lipid peroxidation, including in whole blood and bone marrow, has gained importance in recent years. Each reaction was monitored by thin layer chromatography. 1H, 13C, and 15N NMR spectra were recorded (chemical shifts were expressed as δ-values). We studied the effect of 6-methyl-3-(thietan- 3-yl)pyrimidine-2,4(1H,3H)-dione on the generation of reactive oxygen species (ROS) in the whole blood and bone marrow using the study of whole blood spontaneous and stimulated chemiluminescence (CL). CL methods make it possible to quickly and easily assess the studied material (whole blood, bone marrow) effect on free radical oxidation. Using CL methods, it is possible to reveal the presence of medicines' pro- or antioxidant properties, opening up new possibilities in the search for substances with antioxidant properties and comparing their activity. Alkylation of 6-methylpyrimidine-2,4(1H,3H)-dione by 2-chloromethylthiirane in protic solvents in the presence of alkali leads to the formation of an N-thietane derivative. NMR spectroscopy showed that 6-methylpyrimidine-2,4(1H,3H)-dione was alkylated at position 3. The oxidation reactions of N-(thietan-3-yl)pyrimidine-2,4(1H,3H)-dione were studied, and it was determined that, depending on the excess of the oxidizing agent and the duration of the process, N-(1-oxothietan-3-yl)- or N-(1,1-- dioxothietan-3-yl)pyrimidine-2,4(1H,3H)-diones were formed. The effects of free radical oxidation processes of new biologically active pyrimidine-2,4(1H,3H)-diones were studied. New pyrimidine-2,4(1H,3H)-diones increase the general adaptive capabilities of the body and have protective effects in extreme conditions.

Antioxidant potential and antibacterial activities of Allium cepa (onion) and Allium sativum (garlic) against the multidrug resistance bacteria

BackgroundThe increase in the demand for synthetic drugs due to the surge in the cases of drug-resistant infectious organisms has led to the search for new medicines in plants. Some plants have phytochemicals that can serve medicinal purposes. This study focuses on the antibacterial activity and antioxidant potential of Allium sativum and Allium cepa extract on bacterial isolates isolated from the wound of diabetic patients. Agar well-diffusion method was used for the antibacterial susceptibility. Proteus mirabilis, Pseudomonas aeruginosa, Klebsiella pneumoniae, Staphylococcus aureus, and Escherichia coli were used for this study. The total phenolic content of the extract was determined using standard Spectrophotometric techniques.ResultsThe ethanolic extract of each plant had higher inhibitory effects against the bacterial isolates than the aqueous extracts. The zone of inhibition of each ethanolic section ranged from 3 to 12.5 mm, while the aqueous extracts ranged from 4 to 10 mm. The highest antimicrobial activity was observed at 150 mg/ml in A. sativum ethanolic extract when tested against Staphylococcus aureus, which resulted in a zone of inhibition of 12.5 mm. The aqueous and ethanolic extracts of A. cepa have higher phenolic content than that of A. sativum.ConclusionThis research showed that the ethanolic and aqueous extracts of both plants vary in their abilities to serve act as antioxidants and antimicrobials.

The Pandemic Response Box─Accelerating Drug Discovery Efforts after Disease Outbreaks.

The current Covid-19 pandemic has underlined the need for a more coordinated and forward-looking investment in the search for new medicines targeting emerging health care threats. Repositioning currently approved drugs is a popular approach to any new emerging disease, but it represents a first wave of response. Behind this would be a second wave of more specifically designed therapies based on activities against specific molecular targets or in phenotypic assays. Following the successful deployment and uptake of previous open access compound collections, we assembled the Pandemic Response Box, a collection of 400 compounds to facilitate drug discovery in emerging infectious disease. These are based on public domain information on chemotypes currently in discovery and early development which have been shown to have useful activities and were prioritized by medicinal chemistry experts. They are freely available to the community as a pharmacological test set with the understanding that data will be shared rapidly in the public domain.

Medicinal plants with potential antihypertensive properties: emphasis on natural products from the Brazilian Cerrado

ABSTRACT Arterial hypertension is a worldwide public health problem and the search for new medicines is one of the biggest challenges for the treatment of this pathology. Secondary metabolites of plants exhibit pharmacological properties of great phyto therapeutic interest. Cerrado is one of the largest biomes in Brazil and research with Cerrado plants as therapeutic resources is of growing interest. Our objective was to compile data regarding the Cerrado plants that already have some of their active compounds described and may potentially be used to treat arterial hypertension. We concluded that flavonoids, tannins, steroids and saponins exhibit important properties to low blood pressure. Thus, the species from Cerrado Brazilian such as pau-paraíba (Simarouba versicolor), pau-santo (Kielmeyera coriacea), abiu-do-cerrado (Pouteria torta), guarandi (Calophyllum brasiliense), bacaba (Oenocarpus bacaba), puçá-amarelo (Mouriri elliptica), fava-de-anta (Dimorphandramollis), murici (Byrsonima crassifolia) and cereja-do-cerrado (Eugenia calycina) are strong candidates for future herbal studies in this field.

Cytotoxicity Induced by Newly Synthesized Palladium (II) Complexes Lead to the Death of MCF-7 and MDA-MB-435 Cancer Cell Lines.

Purpose: Breast cancer is the most common female malignancy and melanoma is the most lethal type of skin cancer. Traditional therapy for cancer treatment is far from satisfactory due to drug resistance and side effects, thus a search for new medicines is being emphasized. Palladium(II) complexes have been reported as anticancer potential agents. In this work, the anticancer activities and cell death induction of a new series of square-planar Pd(II) complexes were evaluated against MCF-7 and MDA-MB-435 cancer cells. Methods: MCF-7 (breast carcinoma) and MDA-MB-435 (melanoma) cells were cultivated, and treated with ligand and Pd(II) complexes. Cell growth, migration and adhesion inhibition, morphological alterations, cell death induction and, DNA interaction upon treatment were studied. Results: Pd(II) complexes exhibited both short and long-term antiproliferative effects on both cell lines, reducing by 80% cell growth in the SRB assay and abolishing longterm proliferation, estimated by the clonogenic assay. Complexes reduced significantly (P<0.05) cell migration and adhesion when compared to the control group. Complexes induced morphological alterations in cell lines and significant (P<0.05) cellular shrinkage. Cell death was induced and the complexes were able to interact with DNA, inducing cleavage of double-stranded DNA, which may account for the complexes cytotoxic effects, observed against both MCF-7 and MDA-MB-435 cells. Conclusion: Overall, the complexes exhibited cytotoxic activities and induced cell death. These observations emphasize an anticancer role with a potential therapeutic value for Pd(II) complexes to improve the outcome of patients with breast cancer and melanoma.

ПРОТИВОАЛЛЕРГИЧЕСКАЯ АКТИВНОСТЬ ЧАЯ ТРАВЫ ФИАЛКИ

Widespread occurrence of allergic diseases requires the search for new medicines to solve this problem including their search through natural sources. The aim is to study anti-allergic activity of Viola herb tea in comparison with Bidens medicinal plant raw material. It was found that Viola herb tea containing polysaccharides and phenolic compounds has a pronounced dose-dependent and anti-anaphylactoid effect in vivo comparable to Bidens herb tea; a semi-effective dose of Viola herb tea made 342 mg/kg. The level of mast cell degranulation in the group studied in the presence of Viola herb tea was in the range of 14,5-21,0% and at all doses was significantly lower (p &lt; 0,05) than the level of mast cell degranulation in animals of the studied group in the presence of an allergen. The percentage of mast cell protection against degranulation in vitro of Viola herb tea is 31,2-65,7%. A semi-effective dose of Viola herb tea on the model of mast cell membranes stabilization is 433 ng/ml and is 1,6 times inferior to Bidens herb tea.

Precision cut lung slices: an ex vivo model for assessing the impact of immunomodulatory therapeutics on lung immune responses.

Chronic inflammatory diseases of the respiratory tract, such as chronic obstructive pulmonary disease (COPD) and asthma, are severe lung diseases that require effective treatments. In search for new medicines for these diseases, there is an unmet need for predictive and translatable disease-relevant in vitro/ex vivo models to determine the safety and efficacy of novel drug candidates. Here, we report the use of precision cut lung slices (PCLS) as a potential ex vivo platform to study compound effects in a physiologically relevant environment. PCLS derived from an elastase-challenged mouse model display key characteristics of increased inflammation ex vivo, which is exacerbated further upon challenge with LPS, mimicking the immune insult of a pathogen triggering disease exacerbation. Such LPS-induced inflammatory conditions are significantly abrogated by immunomodulatory agents targeting specific inflammatory signaling pathways in the absence of cytotoxic effects in lung slices. Thus, an ex vivo model of PCLS with a simulated pathogenic insult can replicate proposed in vivo pharmacological effects and thus could potentially act as a valuable tool to investigate the underlying mechanisms associated with lung safety, therapeutic efficacy and exacerbations with infection.

Worldwide Research Trends on Medicinal Plants.

The use of medicinal plants has been done since ancient times and may even be considered the origin of modern medicine. Compounds of plant origin have been and still are an important source of compounds for drugs. In this study a bibliometric study of all the works indexed in the Scopus database until 2019 has been carried out, analyzing more than 100,000 publications. On the one hand, the main countries, institutions and authors researching this topic have been identified, as well as their evolution over time. On the other hand, the links between the authors, the countries and the topics under research have been analyzed through the detection of communities. The last two periods, from 2009 to 2014 and from 2015 to 2019, have been examined in terms of research topics. It has been observed that the areas of study or clusters have been reduced, those of the last period being those engaged in unclassified drug, traditional medicine, cancer, in vivo study—antidiabetic activity, and animals—anti-inflammatory activity. In summary, it has been observed that the trend in global research is focused more on the search for new medicines or active compounds rather than on the cultivation or domestication of plant species with this demonstrated potential.

Оценка эффективности препарата Олифрин в лечении атрофического ринита с использованием русскоязычной версии опросника SNOT-25 в модификации Houser

Atrophic rhinitis at the same time significantly reduces the quality of life of patients suffering from it and is a refractory pathology. The current therapy for the disease includes conservative and sometimes surgical treatment. Nevertheless, the problem of effective therapeutic method remains to be relevant and requires the search for new medicines. Also, there is no tool for assessing the severity of symptoms and quality of life in patients with atrophic rhinitis. The internationally accepted SNOT-25 (Sino-Nasal Outcome Test-25) questionnaire with Houser’s modifications is used to assess the severity of symptoms of patients with empty nose syndrome and could be successfully applied for examination of patients with atrophic rhinitis. Research objectives. This research is aimed to evaluate the efficacy of the Russian nasal spray Olyfrin in the treatment of atrophic rhinitis. And also, to assess the possibility of using the SNOT 25 questionnaire with Houser’s modifications to determine symptom severity of atrophic rhinitis. Materials and Methods. At the first stage - validation of the SNOT-25 questionnaire modified by Houser - 64 patients were included in the study: 29 patients with atrophic rhinitis, 35 with other forms of chronic rhinitis. All patients filled in a prepared and adapted Russian-language version of the questionnaire. At the second stage - determination of the effectiveness of the spray Olyfrin in the treatment of atrophic rhinitis - the study included 29 patients with atrophic rhinitis. Olyfrin was used in 1 dose 3 times a day for 14 days. The dynamics of the severity of symptoms was assessed on the 7th and 14th days using the SNOT-25 questionnaire with Houser’s modifications. Analysis of the total number of points according to SNOT 25 with Houser’s modifications, along with the number of points scored for each of the questions, revealed a significant difference between the group of patients with atrophic rhinitis and the group of patients with other forms of chronic rhinitis (p &lt;0.05). When studying the efficacy of the spray Olyfrin, statistically significant differences were found in the sum of points on the questionnaire before treatment and on the 7th day after treatment (p = 0.005), as well as before treatment and on the 14th day after treatment (p &lt;0.001). A significant difference (p &lt;0.05) was also obtained depending on the day of treatment with a decrease in the number of points of the severity of dryness in the nose (3.75 ± 1.55 vs 1.76 ± 1.43), sensation of excessive openness of the nose (0, 62 ± 0.26 vs 0.41 ± 0.14) and the formation of crusts in the nasal cavity (3.45 ± 1.37 vs 1.76 ± 0.87) already on the 7th day of treatment, and for all these symptoms with an additional decrease in the severity of the feeling of suffocation (1.14 ± 0.29 vs 0.28 ± 0.1) and difficulty in nasal breathing (1.62 ± 0.33 vs 0.45 ± 0.12) on the 14th day of treatment. Conclusions. According to our study, Olyfrin nasal spray is advisable to use when prescribing empirical therapy for patients with atrophic rhinitis. And to assess the quality of life and the dynamics of treatment of patients with atrophic rhinitis, the Russian-language version of the SNOT-25 questionnaire with Houser’s modifications can be successfully used.

Piceatannol attenuates RANKL-induced osteoclast differentiation and bone resorption by suppressing MAPK, NF-κB and AKT signalling pathways and promotes Caspase3-mediated apoptosis of mature osteoclasts.

Osteoclasts are multinuclear giant cells that have unique ability to degrade bone. The search for new medicines that modulate the formation and function of osteoclasts is a potential approach for treating osteoclast-related bone diseases. Piceatannol (PIC) is a natural organic polyphenolic stilbene compound found in diverse plants with a strong antioxidant and anti-inflammatory effect. However, the effect of PIC on bone health has not been scrutinized systematically. In this study, we used RAW264.7, an osteoclast lineage of cells of murine macrophages, to investigate the effects and the underlying mechanisms of PIC on osteoclasts. Here, we demonstrated that PIC treatment ranging from 0 to 40 µM strongly inhibited osteoclast formation and bone resorption in a dose-dependent manner. Furthermore, the inhibitory effect of PIC was accompanied by the decrease of osteoclast-specific genes. At the molecular level, PIC suppressed the phosphorylation of c-Jun N-terminal kinase (JNK), extracellular signal-regulated kinase (ERK1/2), NF-κB p65, IκBα and AKT. Besides, PIC promoted the apoptosis of mature osteoclasts by inducing caspase-3 expression. In conclusion, our results suggested that PIC inhibited RANKL-induced osteoclastogenesis and bone resorption by suppressing MAPK, NF-κB and AKT signalling pathways and promoted caspase3-mediated apoptosis of mature osteoclasts, which might contribute to the treatment of bone diseases characterized by excessive bone resorption.

Medicinal Plants in the Diet of Golden Langur Trachypithecus geei in Kakoijana Reserve Forest, Western Assam, India. A Bio - Rational for the Search of New Medicines for Human Use?

Medicinal Plants in the Diet of Golden Langur Trachypithecus geei in Kakoijana Reserve Forest, Western Assam, India. A Bio - Rational for the Search of New Medicines for Human Use?

Comparing Medicinal Uses of Cochlospermaceae throughout Its Geographic Range with Insights from Molecular Phylogenetics

Species of the Cochlospermaceae, a small mostly pantropical plant family, were evaluated at a continental scale for medicinal uses in traditional medicine. This ethnobotanical information was placed in a phylogenetic framework to make informed predictions in the search for new medicines and bioactive compounds. Medicinal plant-use data were mapped onto a molecular phylogeny based on DNA sequences of nuclear and chloroplast markers. Associations of medicinal uses among closely related species occurring in different geographic regions and among diverse cultures were evaluated. The most common medicinal uses for these species are those used to treat skin ailments, gastro-intestinal problems, malaria, and liver issues. The plant species with the most numerous uses is Cochlospermum tinctorium, which occurs primarily in West Africa. Closely related species being used by cultural groups in different geographic regions to treat the same illnesses suggests the presence of bioactive compounds with potential biomedical value, since they may represent independent discoveries of similar medicinally-active compounds. This leads to the speculation that those closely related species not currently being used to treat these ailments may also contain identical or similar medicinally-active compounds and are worthy of laboratory investigations.

Flipping from E- to Z-alkenes

In their search for new medicines, chemists often choose the trusty Suzuki-Miyaura reaction to construct essential carbon-carbon bonds. This reliable reaction connects alkyl halides with various cl...

Medicinal plants in the diet of woolly spider monkeys (Brachyteles arachnoides, E. Geoffroy, 1806) – a bio-rational for the search of new medicines for human use?

The present study aimed to compare the plant food diet of woolly spider monkeys (Brachyteles arachnoides) inhabiting Intervales State Park in São Paulo, Brazil, with medicinal plant species used by humans in the surrounding areas of the park. The diet of a group of woolly spider monkeys living in an Atlantic forest area was recorded during 43 months of fieldwork. Fifty-three species (87 food items) were recorded. Plant specimens were collected and identified at the University of São Paulo and the Botanical Institute of São Paulo State. Using semi-structured interviews, ethnomedicinal data were also collected from four preselected respondents regarding the human therapeutic value of these plants. The study showed that 24.5% (13/53) of these species are used by residents around the park for medicinal purposes. Of these thirteen, seven species also have validated pharmacological properties, and three are utilized by local residents for similar medicinal purposes. Overlap in the plant food/medicinal diet of woolly spider monkey populations elsewhere were also noted, suggesting potential overlap in their medicinal value for humans and primates. The similarities between the ingestion of plants by primates and their medicinal use by humans provide a bio-rational for the search of bioactive plants in the primate diet. Further detailed investigation of their pharmacological and phytochemical value is warranted.

Antimicrobial and antifungal activity of some (5-(adamantane-1-yl)-4R-1,2,4-triazole-3-ylthiols substitutes

Lately adamantine containing substances have found wide use among the skeleton derivatives. The combination of adamantane and 1,2,4-triazole in one molecule creates significant preconditions to design new potential drugs with low toxicity and pronounced pharmacological activity. The aim of the research is the study of antimicrobial and antifungal activity of (5-(adamantane-1-yl)-4-R-1,2,4-triazole-3-ylthiols substitutes. Materials and methods. Determination of antimicrobial and antifungal activity has been carried out by 2-fold serial dilutions method in liquid nutrient media. The substance of the antibacterial drug Trimethoprim has been applied as a control in determining antimicrobial activity of the compounds against the investigated strains of microorganisms. Results . According to the data of experiments the 5-(((5-(adamantane-1-yl)-4-ethyl-4 H -1,2,4-triazole-3-yl)thio)methyl)-4-ethyl-4H-1,2,4-triazole-3-thiol shows the same activity as Trimethoprim against P. aeruginosa (MIC is 62.5 µg/ml, MBC – 125 μg/ml), marked activity towards S. aureus (MIC is 15.6 μg/ml, MBC – 31.25 μg/ml while trimethoprim – 31.25 μg/ml, MBC – 62.5 µg/ml), greater fungistatic and fungicidal activity towards C. albicans, which amounted to 31.25 µg/ml, MFC – 62.5 µg/ml (while trimethoprim 62.5 µg/ml, MFC – 125 µg/ml). Reconstration of benzyldenhydrazide group to hydrazide one leads to the slight increase of bacteriostatic activity. Replacing the radical R from -Н to -C 2 H 5 does not influence on the change of fungistatic activity. However, this resulted to the decrease in bacteriostatic activity against E. coli. The same is observed in relation to P. aeruginosa: from 62.5 μg/ml, MFC – 125 mcg/ml to 125 μg/ml, MFC – 125 µg/m respectively. Conclusion. The conducted study has showed that among the synthesized compounds there are some substances which strength of the antimicrobial and antifungal action in some cases exceeds the standard of comparison - Trimethoprim. The most active compound against the test strain of C. albicans was 2-(5-(((5-(adamantane-1-yl)-4 H -1,2,4-triazole-3-yl)thio)methyl)-1,3,4-thiodiazole(todosol)-2-amine), which activity in 8 times higher than the standard of comparison. The study of biological and pharmacological activity of the synthesized compounds, and also the determination of the regularities between structure and activity create a favorable basis for the search of new medicines in a number of 1,2,4-triazole derivatives.

Features of Modern Anticoagulant Therapy in Patients with Nonvalvular Atrial Fibrillation and Chronic Kidney Disease

Prevalence of atrial fibrillation (AF) in population is very high and continues to grow. According to the existing statistics its prevalence reaches about 2% so it is twice more, than it was considered in the last decade. Prevalence of AF among patients with chronic kidney disease (CKD) varies from 11 to 22% (according to other data – from 15 to 20%) and increases with age, considerably surpassing that in the general population among all age groups. Vast majority of patients with AF need in treatment with anticoagulants to prevent an ischemic stroke and systemic thromboembolisms. However, in case of combination AF and CKD, in addition to increase in frequency of strokes and the thromboembolic events, also the frequency of major bleedings significantly increases that considerably complicates the choice of adequate anticoagulant therapy in such situation. Many years the vitamin K antagonists were the only representatives of a class of anticoagulants for long-term therapy in patients with AF. Their well-known deficiencies (a narrow therapeutic window, need of frequent laboratory control, numerous drug-drug and dietary interactions, unpredictability of a pharmacodynamics and pharmacokinetics at certain patients) promoted search of new medicines, more convenient in use. Direct oral anticoagulants were easier to use, and by results of the main studies didn't yield or exceeded warfarin concerning balance of efficiency and safety. However, they were not specially studied in patients with the reduced kidney function. Features of modern anticoagulant therapy in patients with the nonvalvular AF and CKD are considered in the review. The possibility of the safest use of anticoagulants for patients with decreased creatinine clearance is analyzed.

Some Plant species of Tarai region of Kumaun, Uttarakhand, used in tuberculosis

Tuberculosis (TB) remains one of the most difficult ailments to control in the world today. The emergence of drug resistant strains has made previously effective and affordable remedies less effective (There are more than twenty drugs that are currently used for the treatment of TB and almost all of them were developed some years ago. The drugs are used in differing combinations in different circumstances, so that for example some TB drugs are only used for the treatment of new patients who are very unlikely to have resistance to any of the TB drugs). This has made the search for new medicines from local traditional medicines. The specific objectives of this study were to identify plant species used in the treatment of TB, parts used, their methods of preparation and administration. The present study was conducted in the central tarai region of Kumaun, Uttarakhand in the year 2008-2011. Total fifteen plant species were found to be used to cure tuberculosis. The different use of Adhatoda vasica was reported first time from the study area. Species Albizia lebbeck, Bauhinia variegata, Baliospermum montanum, Sida rhombifolia, Withania somnifera, Asclepias curassavica, Echinops echinatus, and Saccharum spontaneum were reported first time of the study area.