scholarly journals STUDIES ON THE MECHANISM OF ACTION OF THERMAL NEUTRONS IN PRODUCTING BIOLOGICAL EFFECTS. I. LACK OF EFFECT OF HYPOXIA AND GLUTATHIONE IN ALTERING MORTALITY IN MICE

1953 ◽  
Author(s):  
J Storer ◽  
L Ellinwood ◽  
W Langham ◽  
P Sanders
2021 ◽  
Vol 17 ◽  
Author(s):  
Marcel Hrubša ◽  
Khondekar Nurjamal ◽  
Alejandro Carazo ◽  
Nayana Nayek ◽  
Jana Karlíčková ◽  
...  

Background: Antiplatelet drugs represent the keystone in the treatment and prevention of diseases of ischemic origin, including coronary artery disease. The current palette of drugs represents efficient modalities in most cases, but their effect can be limited in certain situations or associated with specific side effects. In this study, representatives of compounds selected from series having scaffolds with known or potential antiplatelet activity were tested. These compounds were previously synthetized by us, but their biological effects have not yet been reported. Objective: The aim of this study was to examine the antiplatelet and anticoagulation properties of selected compounds and determine their mechanism of action. Methods: Antiplatelet activity of compounds and their mechanisms of action were evaluated using human blood by impedance aggregometry and various aggregation inducers and inhibitors and compared to appropriate standards. Cytotoxicity was tested using breast adenocarcinoma cell cultures and potential anticoagulation activity was also determined. Results: In total, four of 34 compounds tested were equally or more active than the standard antiplatelet drug acetylsalicylic acid (ASA). In contrast to ASA, all 4 active compounds decreased platelet aggregation triggered not only by collagen, but also partly by ADP. The major mechanism of action is based on antagonism at thromboxane receptors. In higher concentrations, inhibition of thromboxane synthase was also noted. In contrast to ASA, the tested compounds did not block cyclooxygenase-1. Conclusion: The most active compound, 2-amino-4-(1H-indol-3-yl)-6-nitro-4H-chromene-3-carbonitrile (2-N), which is 4-5x times more potent than ASA, is a promising compound for the development of novel antiplatelet drugs.


2020 ◽  
Vol 27 (3) ◽  
pp. 337-351 ◽  
Author(s):  
Branislava Medić ◽  
Marko Stojanović ◽  
Bojan V. Stimec ◽  
Nevena Divac ◽  
Katarina Savić Vujović ◽  
...  

: Lithium is the smallest monovalent cation with many different biological effects. Although lithium is present in the pharmacotherapy of psychiatric illnesses for decades, its precise mechanism of action is still not clarified. Today lithium represents first-line therapy for bipolar disorders (because it possesses both antimanic and antidepressant properties) and the adjunctive treatment for major depression (due to its antisuicidal effects). Beside, lithium showed some protective effects in neurological diseases including acute neural injury, chronic degenerative conditions, Alzheimer's disease as well as in treating leucopenia, hepatitis and some renal diseases. Recent evidence suggested that lithium also possesses some anticancer properties due to its inhibition of Glycogen Synthase Kinase 3 beta (GSK3β) which is included in the regulation of a lot of important cellular processes such as: glycogen metabolism, inflammation, immunomodulation, apoptosis, tissue injury, regeneration etc. : Although recent evidence suggested a potential utility of lithium in different conditions, its broader use in clinical practice still trails. The reason for this is a narrow therapeutic index of lithium, numerous toxic effects in various organ systems and some clinically relevant interactions with other drugs. Additionally, it is necessary to perform more preclinical as well as clinical studies in order to a precise therapeutic range of lithium, as well as its detailed mechanism of action. The aim of this review is to summarize the current knowledge concerning the pharmacological and toxicological effects of lithium.


2020 ◽  
Vol 9 (5) ◽  
pp. 3703-3711
Author(s):  
Hong-Qun Wang ◽  
Ying Li ◽  
Shan-Shan Ding ◽  
Ying-Xue Li ◽  
Ai-Chun Wang ◽  
...  

2000 ◽  
Vol 13 (10) ◽  
pp. 949-952 ◽  
Author(s):  
Hena R. Ashar ◽  
Lydia Armstrong ◽  
Linda J. James ◽  
Donna M. Carr ◽  
Kimberley Gray ◽  
...  

Scientifica ◽  
2018 ◽  
Vol 2018 ◽  
pp. 1-14 ◽  
Author(s):  
León Jesús German-Ponciano ◽  
Gilberto Uriel Rosas-Sánchez ◽  
Eduardo Rivadeneyra-Domínguez ◽  
Juan Francisco Rodríguez-Landa

Flavonoids are phenolic compounds found commonly in plants that protect them against the negative effects of environmental insults. These secondary metabolites have been widely studied in preclinical research because of their biological effects, particularly as antioxidant agents. Diverse flavonoids have been studied to explore their potential therapeutic effects in the treatment of disorders of the central nervous system, including anxiety and depression. The present review discusses advances in the study of some flavonoids as potential antidepressant agents. We describe their behavioral, physiological, and neurochemical effects and the apparent mechanism of action of their preclinical antidepressant-like effects. Natural flavonoids produce antidepressant-like effects in validated behavioral models of depression. The mechanism of action of these effects includes the activation of serotonergic, dopaminergic, noradrenergic, andγ-aminobutyric acid-ergic neurotransmitter systems and an increase in the production of neural factors, including brain-derived neurotrophic factor and nerve growth factor. Additionally, alterations in the function of tropomyosin receptor kinase B and activity of the enzyme monoamine oxidase A have been reported. In conclusion, preclinical research supports the potential antidepressant effects of some natural flavonoids, which opens new possibilities of evaluating these substances to develop complementary therapeutic alternatives that could ameliorate symptoms of depressive disorders in humans.


1971 ◽  
Vol 64 (5) ◽  
pp. 1002-1008 ◽  
Author(s):  
H. M. Flint ◽  
E. L. Walk ◽  
W. Klassen ◽  
D. Greenberg

Author(s):  
Karlen O Hovnanyan

The search for new derivatives of benzoimidazole with an active center that have a wide range of biological effects (antifungal, antiflammatory, antibacterial, antiviral, antitumor, antidiabetic, etc.) is the subject of modern pharmaceutical science. To determine the mechanism of action of benzoimidazole, a search is underway for more. We have previously carried out the Ultrastructural characterization of various prokaryotes and protists, as well as the mechanism of action of antibiotics and chemical preparations on them. From a series of heterocyclic drugs, a drug with a wide spectrum of action was chosen as derivatives of benzimidazole and a model of a free-living unicellular eukaryote Endameba moshkovskii with a vegetative and cystic form. The purpose of this work is the nature of the action of drugs of the benzimidazole series and in the ultrastructural visualization of the mechanism of action of benzimidazole using electron microscopic and electron-cytochemical methods on the model of polyxenic cultures of unicellular eukaryotes Entamoeba moshkovskii. We have established for the first time the excising effect of benzimidazole and the functional-ultrastructural mechanism of the action of benzimidazole on entameoba cells. As a result, the ultrastructural and functional morphology of benzimidazole action in the process of excysting entamoeba was established.


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