Research Results in Pharmacology最新文献

{"title":"Synthesis, molecular docking, ADMET study and in vitro pharmacological research of 7-(2-chlorophenyl)-4-(4-methylthiazol-5-yl)-4,6,7,8-tetrahydroquinoline-2,5(1H,3H)-dione as a promising non-opioid analgesic drug","authors":"A. D. Kravchenko, N. Pyatigorskaya, G. Brkich, L. Yevsieieva, A. Kyrychenko, S. Kovalenko","doi":"10.3897/rrpharmacology.8.80504","DOIUrl":"https://doi.org/10.3897/rrpharmacology.8.80504","url":null,"abstract":"Introduction: The discovery of novel drugs that can block the transmission of pain signals for treating the pain of various etiologies is an urgent topic in pharmaceutics. The aim of this paper is to synthesize and to investigate in vitro and in silico characteristics of a promising novel compound: 7-(2-chlorophenyl)-4-(4-methylthiazol-5-yl)-4,6,7,8-tetrahydroquinoline-2,5(1H,3H)-dione (HSV-DKH-0450).\u0000 Materials and methods: The specific activity and the inhibitory mechanism of HSV-DKH-0450 were studied using the HEK293 culture cells expressing the IPTG-induced TRPA1 ion channels. Cardiotoxicity was determined by estimating the binding of HSV-DKH-0450 to the hERG channel. Inhibition of human liver cytochromes was determined by the effect on the activity of cytochromes 1A2, 2C9, 2D6, 2C8, and 3A4. Cellular toxicity was assessed by the effect on the viability of human hepatocytes. ADMET properties were evaluated using admetSAR and SwissADME web-based tools. Molecular docking was carried out using AutoDock Vina tools to predict the binding affinity of all HSV-DKH-0450 stereoisomers toward the TRPA1 and TRPV1 receptors.\u0000 Results and discussion: In silico predictions of ADMET properties of HSV-DKH-0450 showed that it has optimal pharmaceutical profiles. A series of in vitro pharmacological studies revealed that HSV-DKH-0450 is a promising antagonist of the TRPA1 ion channel with the IC50 of 91.3 nM. The molecular docking of HSV-DKH-0450 stereoisomers against the TRPA1 and TRPV1 receptors demonstrates that they all are characterized by an approximately similar high binding affinity.\u0000 Conclusion: The obtained data for substance HSV-DKH-0450 look promising for its further development as a potential therapeutic agent for pain relief.\u0000 Graphical abstract:","PeriodicalId":21030,"journal":{"name":"Research Results in Pharmacology","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41360835","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of novel effective agents from 1H-indolylammonium trifluoroacetates effective against conditionally pathogenic microorganisms","authors":"I. S. Stepanenko, S. A. Yamashkin, T. N. Platkova, A. I. Kiryutina, I. Sorokvasha","doi":"10.3897/rrpharmacology.8.73329","DOIUrl":"https://doi.org/10.3897/rrpharmacology.8.73329","url":null,"abstract":"Introduction: The problem of antibiotic resistance of microorganisms is becoming more urgent in the twenty-first century. More and more pathogenic microbes are becoming resistant to two or more antibiotics. This problem has become worse into the COVID-19 pandemic. The search for new compounds with antimicrobial activity is one of the principles for overcoming the antibiotic resistance of microorganisms. Materials and methods: Methods for the preparation, isolation, and identification of salts of 2,3,5-trimethyl-, 1,2,3,5-tetramethyl-, 2,3-dimethyl-5-methoxy-, 5-methoxy-1,2,3-trimethyl-1H-indole-6-amines and trifluoroacetic acid were developed and laboratory microbiological studies of them for antimicrobial activity were carried out. Sensitivity of the test-strains of microorganisms to the new compounds was studied. A method of serial dilutions to determine the minimal inhibitory concentration (MIC) of the compounds under study was used in the study. Results and discussion: The compounds 5-8 showed a pronounced antibacterial activity against the test strains of microorganisms in vitro with MIC from 0.98 μg/mL to 125.0 μg/mL. The prospects for targeted synthesis of biologically active compounds which are derivatives of 1H-indolylamines with a trifluoromethyl group in the molecule were determined, and after additional studies, the compounds 5-8 may find application as water-soluble synthetic antimicrobial agents. Conclusion: The laboratory microbiological screening of showed that they have an antimicrobial effect that exceeds the activity of the reference drug, dioxidine. The presence of molecular mechanisms predicted in silico in the spectrum of biological activity of the studied compounds, such as Pseudolysin inhibitor, Omptin inhibitor, Undecaprenyldiphospho-muramoylpentapeptide beta-N-acetylglucosaminyltransferase inhibitor, UDP-epimerase inhibitor, Bacterial efflux pump inhibitor, suggests the presence of antimicrobial activity against gram-positive and gram-negative microorganisms. Trifluoroacetates 2,3,5-trimethyl-1H-indole-6-ammonium (5), 1,2,3,5-tetramethyl-1H-indole-6-ammonium (6), 2,3-dimethyl-5-methoxy-1H-indole-6-ammonium (7), 1,2,3-trimethyl-5-methoxy-1H-indole-6-ammonium (8), after additional studies, may find application as water-soluble synthetic antimicrobial agents.","PeriodicalId":21030,"journal":{"name":"Research Results in Pharmacology","volume":"8 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"70415229","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design and evaluation of pharmacological properties of a new 1,3,4-thiadiazolylamide derivative of 2-propylpentanoic acid","authors":"A. S. Malygin, V. Yasnetsov","doi":"10.3897/rrpharmacology.7.70179","DOIUrl":"https://doi.org/10.3897/rrpharmacology.7.70179","url":null,"abstract":"Introduction: The use of the pharmacophoric approach is a promising direction for modifying the chemical structure of 2-propylpentanoic (valproic) acid in order to obtain new drugs.\u0000 Materials and methods: In the experiments on mice, acute toxicity, neurotoxicity, antiepileptic activity and analgesic effect of N-(5-ethyl-1,3,4-thiadiazol-2-yl)-2-propylpentanamide (valprazolamide) were evaluated. LD50 was determined by probit analysis. Neurotoxicity was determined in a rotarod test and a bar test in mice. The effects of valprazolamide on the exploratory behavior of mice in open field test and in a light/dark transition test were evaluated. Its antiepileptic activity was tested in mice against seizures induced by maximal electroshock, pentylenetetrazole (scPTZ); isoniazid, thiosemicarbazide, pilocarpine, and camphor. The analgesic effect was studied in a hot plate test.\u0000 Results and discussion: N-(5-ethyl-1,3,4-thiadiazol-2-yl)-2-propylpentanamide was obtained by introducing pharmacophores into the structure of 2-propylpentanoic acid: a substituted amide group and an electron-donor domain of 1,3,4-thiadiazole. The LD50 value for intraperitoneal administration of a new 2-propylpentanoic acid: derivative to mice was 924.8 mg/kg, and the TD50 value in the rotarod test and the bar test were 456.7 mg/kg and 546.7 mg/kg, respectively. The suppression of orienting responses in the animals was noted when it was administered in neurotoxic doses. Valprazolamide showed the most antiepileptic activity on models of MES, scPTZ and isoniazid antagonism tests. The ED50 values were 138.4 mg/kg, 74.5 mg/kg, and 126.8 mg/kg, respectively. The therapeutic indices for these models of epilepsy were 6.7; 12.4; 7.3, and protective index – 3.3; 6.1 and 3.6, respectively. In the hot plate test, valprazolamide increased the latency period before a defensive response to a thermal stimulus (ED50 165 mg/kg).\u0000 Conclusion: N-(5-ethyl-1,3,4-thiadiazol-2-yl)-2-propylpentanamide is a new 1,3,4-thiadiazolylamide derivative of 2-propylpentanoic acid with antiepileptic and analgesic activities, which belongs to the group of low-toxic agents.\u0000 \u0000 Graphic abstract\u0000 \u0000 \u0000 \u0000 \u0000 N-(5-ethyl-1,3,4-thiadiazol-2-yl)-2-propylpentanamide (3D)\u0000 LD50=924.8 mg/kg (mice, intraperitoneally)\u0000 TD50=456.7 mg/kg (rotarod, mice, intraperitoneally)\u0000 ED50=138.4 mg/kg (MES, mice, intraperitoneally)\u0000 ED50=74.5 mg/kg (scPTZ, mice, intraperitoneally)","PeriodicalId":21030,"journal":{"name":"Research Results in Pharmacology","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"70415174","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Impact of organotin compounds on the growth of epidermoid Lewis carcinoma","authors":"M. Dodokhova, A. V. Safronenko, I. Kotieva, M. Alkhuseyn-Kulyaginova, D. Shpakovsky, E. Milaeva","doi":"10.3897/rrpharmacology.7.71455","DOIUrl":"https://doi.org/10.3897/rrpharmacology.7.71455","url":null,"abstract":"Introduction: Search for new compounds with a broad antitumor and antimetastatic potency due to multiple targeting remains important in medicinal chemistry, pharmacology and oncology. We report the efficacy of hybrid organotin agents bis-(3,5-di-tert-butyl-4-hydroxyphenylthiolate) dimethyltin (Ме3) and (3,5-di-tert-butyl-4-hydroxyphenylthiolate) triphenyltin (Ме5).\u0000 Materials and methods: The compounds were administered to mice bearing the spontaneously metastatic epidermoid Lewis lung carcinoma (LLC). The efficacy of the treatment was evaluated by mean life span, percentage of tumor growth inhibition, number of lung metastases, frequency of metastasis, tumor weight 21 days after tumor cell inoculation, and a degree of lung damage according to the method of D. Tarin and J.E. Price.\u0000 Results and discussion: For new organotin compounds containing an antioxidant protective fragment of 2,6-di-tert-butylphenol, moderate antitumor and pronounced antimetastatic effects were revealed in the Lewis model of epidermoid lung carcinoma; more active for Me5. Some features of the development of the process of metastasis were recorded with the introduction of various doses of hybrid organotin compounds.\u0000 Conclusion: Substances Ме3 and Ме5 possess specific activity on the model under investigation, which allows one to suggest these organotins as promising series of antitumor and antimetastatic agents with multiple targeting mode of action.","PeriodicalId":21030,"journal":{"name":"Research Results in Pharmacology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44088265","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Optimization of premedication of patients with arterial hypertension and severe ventricular rhythm disturbances with Amiodarone-associated thyrotoxicosis","authors":"A. Safronenko, S. V. Lepyavka, I. A. Demidov, M. I. Nazheva, Yu. S. Maklyakov","doi":"10.3897/rrpharmacology.7.78137","DOIUrl":"https://doi.org/10.3897/rrpharmacology.7.78137","url":null,"abstract":"Introduction: The effectiveness of premedication of patients with arterial hypertension and severe ventricular rhythm disturbances against the background of Amiodarone-associated thyrotoxicosis, high anxiety and cyclothymiae disorders should be based on the pharmacological positions of the need to reduce the risk of dangerous adverse cardiovascular reactions.\u0000 Materials and methods: During the research, a clinical group of 114 patients with arterial hypertension, severe ventricular arrhythmias and Amiodarone-associated type I thyrotoxicosis was formed: four subgroups were identified. In Subgroup 1 (n=22), no premedication was given. In Subgroup 2 (n=32), premedication was given with Diazepam and magnesium sulfate in a prolonged mode. In Subgroup 3 (n=30), the patients received Diazepam the day before surgery. In Subgroup 4 (n=30), premedication was given with Midazolam. A dynamic assessment of the severity of anxiety, depression, sedation and daily monitoring of blood pressure and ECG were carried out.\u0000 Results and discussion: After surgery, in Subgroup 1, the level of anxiety and depression increased. In all other Subgroups, regardless of the type of premedication, the use of benzodiazepines was accompanied by a decrease in the level of anxiety after surgery. A decrease in pressure load and an increase in the stability of the parameters of systemic hemodynamics were registered in Subgroup 2 of patients, whereas in Subgroup 4 of patients, the pressure load increased while limiting the differences in blood pressure values during the day. After surgery, in Subgroup 2, cardiac rhythm disturbances were less common; in Subgroup 3, the structure of rhythmogenesis disturbances in the heart almost did not change, and in Subgroup 4, there was an unfavorable trend of an increase in the frequency of supraventricular, single and group ventricular extrasystoles.\u0000 Conclusion: The prolonged premedication with long-acting benzodiazepines and magnesium preparations in patients with arterial hypertension, ventricular rhythm disturbances against the background of Amiodarone-associated thyrotoxicosis reduces the level of anxiety, as well as the risk of developing cardiovascular complications and instability of systemic hemodynamics.","PeriodicalId":21030,"journal":{"name":"Research Results in Pharmacology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42560531","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Study of analgesic activity and effects of new dipharmacophores – nebracetam and cyclooxygenase-2 inhibitors derivatives on the cognitive abilities of rats","authors":"V. S. Slyusarenko, I. S. Koklin, S. Kovalenko, V. Chuev, Alexey A. Shabalin, V. Gureev, M. Korokin","doi":"10.3897/rrpharmacology.7.78463","DOIUrl":"https://doi.org/10.3897/rrpharmacology.7.78463","url":null,"abstract":"Introduction: The aim of the present study was to research the analgesic activity and effect of new dipharmacophore compounds consisting of substances with proven therapeutic activity, namely nebracetam–ibuprofen (NRIP), nebracetam–dexibuprofen (NRDIP), nebracetam–niflumic acid (NRNFA), and nebracetam–mefenamic acid (NRMFA), on the cognitive abilities of rats.\u0000 Materials and methods: The experimental study was performed in 110 Wistar rats (male/female ratio 50/50%), weighing 180–200 g, and 50 laboratory mice (male/female ratio 50/50%) weighing 18–22 g. The study of the analgesic activity was carried out using the acetic acid writhing test and the hot plate test. The effect on the cognitive abilities of rats was studied using the pattern recognition test in a model of neurotrauma caused by a drop-weight.\u0000 Results and discussion: It has been shown that the administration of dipharmacophores nebracetam–ibuprofen (NRIP), nebracetam–dexibuprofen (NRDIP), nebracetam–niflumic acid (NRNFA) as well as nebracetam–mefenamic acid (NRMFA) in the tested dosages leads to a statistically significant (p<0.05) analgesic action in acetic acid writhing tests and hot plate tests. At the same time, the analgesic activity of the compounds has been shown to conjoin with a statistically significant influence on cognitive functions in the experimental animal groups after simulating a neurotrauma.\u0000 Conclusion: The dipharmacophore compounds studied in the present research, having analgesic and nootropic effects, can be used as effective and safe analgesics and can also be used for the treatment and prevention of pain syndrome, enhancing the cognitive abilities of healthy people in complicated professional conditions.","PeriodicalId":21030,"journal":{"name":"Research Results in Pharmacology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41603462","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"“The obesity paradox” in patients with atrial fibrillation according to the results of the REKUR-AF study","authors":"I. L. Polshakova, S. Povetkin, Alexey Y. Gaponov","doi":"10.3897/rrpharmacology.7.78134","DOIUrl":"https://doi.org/10.3897/rrpharmacology.7.78134","url":null,"abstract":"Introduction: to evaluate the effect of excess body weight (EBW) and obesity on the survival of patients with atrial fibrillation (AF) in the REKUR-AF study.\u0000 Materials and methods: A subanalysis of patients with AF included in the REKUR-AF (382 people) study was performed. Survival rates were analyzed in three patient groups: patients with normal body mass index (BMI), EBW and obesity. Then the nature and significance of the influence of the studied factor on the prognosis in patients with AF were assessed.\u0000 Results and discussion: Patients with AF and normal BMI were significantly older than those with obesity and EBW (p<0.001 and p=0.021, respectively). Among obese patients, hypertension was significantly (p=0.0015) more common (93.9%) compared to the group of patients with a normal BMI level (80.5%). The frequency of type 2 diabetes in obese patients prevailed over the same indicator in the groups of people with normal BMI and EBW (p=0.007 and p=0.020, respectively).\u0000 The analysis of the survival rate of patients with AF depending on the BMI level showed that this factor had a significant impact (p=0.013) on the prognosis. The group of individuals with a normal BMI level had a significantly lower survival rate than the cohort of patients with EBW (p=0.011) and OB (p=0.025). The final model for Cox regression analysis (χ2=53.06, p<0.001) included the following factors: age, form of AF, BMI, presence/absence of type 2 diabetes, presence/absence of previous hospitalizations, presence/absence of hypertension, and presence/absence of oral anticoagulant (OAC) intake.\u0000 Conclusion: The obtained results do not make it possible to unambiguously interpret obesity as a predictor of a positive outcome in this category of individuals.","PeriodicalId":21030,"journal":{"name":"Research Results in Pharmacology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43038074","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Modern approaches to pharmacotherapy of tuberculosis infection in children","authors":"V. Novikov, N. E. Usacheva, T. Myakisheva","doi":"10.3897/rrpharmacology.7.66627","DOIUrl":"https://doi.org/10.3897/rrpharmacology.7.66627","url":null,"abstract":"Anti-TB drugs for children: Aetiotropic therapy is used for the treatment of tuberculosis (TB) in children, as well as in adult patients. Anti-tuberculosis drugs (anti-TB drugs) are divided into 3 lines, taking into account drug sensitivity in Mycobacterium tuberculosis (MBT). First-line anti-TB drugs (basic) are used to treat TB caused by drug-susceptible MBT. Second- and third-line (reserve) drugs are recommended for the treatment of MBT-induced multidrug-resistant (MDR) and extensively drug-resistant (XDR) TB, respectively.\u0000 Stages and regimens to treat tuberculosis: Chemotherapy of tuberculosis in children is carried out in 2 stages (intensive treatment and continuation of treatment) and includes 5 regimens. Each regimen assumes a certain combination of anti-TB drugs, indicating the duration and frequency of their administration. The final chemotherapy regimen is chosen only according to the results of determining the drug sensitivity. To improve the TB epidemic among children, it is important to improve the regimens for the use of anti-TB drugs. The effectiveness of anti-tuberculosis pharmacotherapy is largely determined by the MBT sensitivity and the rational choice of the chemotherapy regimen. The wrong choice of a chemotherapy regimen or its violation threatens to reduce the effectiveness of pharmacotherapy and expand the spectrum of resistance of the pathogen. The development of fixed-dose combination anti-TB drugs and special dosage forms for children will improve the quality of chemotherapy and adherence to treatment. Pharmacoeconomic studies are needed to increase the effectiveness of drug pharmacotherapy for tuberculosis infection in children and to optimize the costs of its implementation.","PeriodicalId":21030,"journal":{"name":"Research Results in Pharmacology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41631778","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Is antibiotics overuse justified when immediate intervention is not possible? A rapid evidence review","authors":"Nour Ibrahim, Z. Noujeim, G. Aoun, Abbass El-Outa","doi":"10.3897/rrpharmacology.7.77709","DOIUrl":"https://doi.org/10.3897/rrpharmacology.7.77709","url":null,"abstract":"Introduction: This review revisits clinical use of antibiotics for most common acute oro-dental conditions; we aim to provide evidence governing antibiotics use when access to oral healthcare is not available, as during the ongoing outbreak of the severe acute respiratory syndrome coronavirus 2.\u0000 Materials and methods: In this rapid review, articles were retrieved after conducting a search on PubMed and Google Scholar. Relevant publications were selected and analyzed. Most recent systematic reviews with/without meta-analyses and societal guidelines were selected. Data were extracted, grouped, and synthesized according to the respective subtopic analysis.\u0000 Results and discussion: There was evidence supporting the use of antibiotics in common oro-dental conditions as temporary measure when immediate care is not accessible, such as in case of localized oral swellings as well as to prevent post-extraction complications. No sufficient evidence could be found in support of antibiotic use for pain resulting from pulpal origin.\u0000 Conclusion: Antibiotic use may be justified to defer treatment temporarily or reduce risk of complications in case of localized infection and tooth extraction, when no access to immediate dental care is possible.\u0000 Graphical abstract:\u0000 \u0000 \u0000","PeriodicalId":21030,"journal":{"name":"Research Results in Pharmacology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48752070","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacological properties of selenium and its preparations: from antioxidant to neuroprotector","authors":"I. Belenichev, Nadia O. Gorchakov, I. Samura, N. Savchenko, N. Bukhtiyarova, O. Popazova","doi":"10.3897/rrpharmacology.7.73051","DOIUrl":"https://doi.org/10.3897/rrpharmacology.7.73051","url":null,"abstract":"Selenium is an essential component of more than two dozen enzymes and other selenoproteins that play critical roles in reproduction, DNA synthesis, thyroid hormone metabolism, and protection from oxidative damage and infection. Selenium has a protective action against some forms of cancer and cardiovascular diseases, modulates levels of inflammatory mediators, promotes to maintain bone homeostasis and protects against bone loss. Selenium significance as a cardioprotective agent may be associated not only with its antioxidant properties, but also with its ability to prevent inflammation, autophagy, as well as the intrinsic and extrinsic apoptosis pathways. Signaling pathways, such as p-AMPK, PARP, Nrf2, STAT, are involved in the protective effects of selenium. Selenium protects against cardiovascular damage by increasing the survival rate of cardiomyocytes, including a mitochondria-dependent pathway and autophagy through peroxisome proliferator-activated receptors. Research demonstrating neuroprotective and cardioprotective effects of selenium preparations – selenoline, selenocysteine and selenomethionine – is growing at a rapid rate. It has been established that these compounds are able to normalize the levels of heat shock proteins (HSP70), which limit the cytotoxic effects of free radicals, produce energotropic action, prevent a decrease in the membrane mitochondria charge, and the opening of the mitochondrial pore. Also regulate the expression of transmembrane factors NF-kB, c-fos, which is associated with their main biological function of chaperone proteins, providing protection of neurons from damage. In this review, we want to emphasize pharmacological role of Selenium and its derivatives on human health is very complex and has yet to be fully understood.","PeriodicalId":21030,"journal":{"name":"Research Results in Pharmacology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49503186","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}