scholarly journals Avermectin Derivatives, Pharmacokinetics, Therapeutic and Toxic Dosages, Mechanism of Action, and Their Biological Effects

2020 ◽  
Vol 13 (8) ◽  
pp. 196 ◽  
Author(s):  
Gaber El-Saber Batiha ◽  
Ali Alqahtani ◽  
Omotayo B. Ilesanmi ◽  
Abdullah A. Saati ◽  
Amany El-Mleeh ◽  
...  
Keyword(s):  
Respiratory Failure ◽  
Mechanism Of Action ◽  
Chloride Channel ◽  
Metabolic Disorders ◽  
Biological Effects ◽  
Streptomyces Avermitilis ◽  
Minor Components ◽  
Electrical Impulse ◽  
Current Review ◽  
Parasitic Worms

Avermectins are a group of drugs that occurs naturally as a product of fermenting Streptomyces avermitilis, an actinomycetes, isolated from the soil. Eight different structures, including ivermectin, abamectin, doramectin, eprinomectin, moxidectin, and selamectin, were isolated and divided into four major components (A1a, A2a, B1a and B2a) and four minor components (A1b, A2b, B1b, and B2b). Avermectins are generally used as a pesticide for the treatment of pests and parasitic worms as a result of their anthelmintic and insecticidal properties. Additionally, they possess anticancer, anti-diabetic, antiviral, antifungal, and are used for treatment of several metabolic disorders. Avermectin generally works by preventing the transmission of electrical impulse in the muscle and nerves of invertebrates, by amplifying the glutamate effects on the invertebrates-specific gated chloride channel. Avermectin has unwanted effects or reactions, especially when administered indiscriminately, which include respiratory failure, hypotension, and coma. The current review examines the mechanism of actions, biosynthesis, safety, pharmacokinetics, biological toxicity and activities of avermectins.

Screening of Synthetic Heterocyclic Compounds as Antiplatelet Drugs

2021 ◽  
Vol 17 ◽  
Author(s):  
Marcel Hrubša ◽  
Khondekar Nurjamal ◽  
Alejandro Carazo ◽  
Nayana Nayek ◽  
Jana Karlíčková ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Biological Effects ◽  
Antiplatelet Drugs ◽  
Antiplatelet Drug ◽  
Breast Adenocarcinoma ◽  
Antiplatelet Activity ◽  
Major Mechanism ◽  
Treatment And Prevention ◽  
Impedance Aggregometry ◽  
Thromboxane Receptors

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.

scholarly journals Mushroom Compost Worker's Lung

1987 ◽  
Vol 80 (11) ◽  
pp. 674-677 ◽  
Author(s):  
M S Phillips ◽  
A A Robinson ◽  
T W Higenbottam ◽  
I M Calder
Keyword(s):  
Respiratory Failure ◽  
Acute Respiratory Failure ◽  
Mechanism Of Action ◽  
Mushroom Compost ◽  
Occupational History ◽  
Serological Investigation

This study draws attention to difficulties in the diagnosis and the understanding of the mechanism of action of mushroom compost worker's lung. Descriptions are given of 4 workers in one factory who developed acute respiratory failure within a 6-month period; 13 others who were unaffected were also studied. Serological investigation appears to be largely unhelpful, and the evidence against the condition being included amongst the extrinsic allergic alveolitides is discussed. A detailed clinical and occupational history is essential for diagnosis.

Lithium - Pharmacological and Toxicological Aspects: The Current State of the Art

2020 ◽  
Vol 27 (3) ◽  
pp. 337-351 ◽  
Author(s):  
Branislava Medić ◽  
Marko Stojanović ◽  
Bojan V. Stimec ◽  
Nevena Divac ◽  
Katarina Savić Vujović ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Glycogen Synthase ◽  
Tissue Injury ◽  
Current Knowledge ◽  
Biological Effects ◽  
Therapeutic Index ◽  
Adjunctive Treatment ◽  
Renal Diseases ◽  
Protective Effects ◽  
Organ Systems

: 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.

scholarly journals Antidiabetic Effects of Bisamide Derivative of Dicarboxylic Acid in Metabolic Disorders

2020 ◽  
Vol 21 (3) ◽  
pp. 991 ◽  
Author(s):  
Angelina Vladimirovna Pakhomova ◽  
Vladimir Evgenievich Nebolsin ◽  
Olga Victorovna Pershina ◽  
Vyacheslav Andreevich Krupin ◽  
Lubov Alexandrovna Sandrikina ◽  
...  
Keyword(s):  
Metabolic Syndrome ◽  
Stem Cells ◽  
Dicarboxylic Acid ◽  
Metabolic Disorders ◽  
Biological Effects ◽  
Treatment Options ◽  
The Metabolic Syndrome ◽  
Pancreatic Stem Cells ◽  
The Impact

In clinical practice, the metabolic syndrome can lead to multiple complications, including diabetes. It remains unclear which component of the metabolic syndrome (obesity, inflammation, hyperglycemia, or insulin resistance) has the strongest inhibitory effect on stem cells involved in beta cell regeneration. This makes it challenging to develop effective treatment options for complications such as diabetes. In our study, experiments were performed on male C57BL/6 mice where metabolic disorders have been introduced experimentally by a combination of streptozotocin-treatment and a high-fat diet. We evaluated the biological effects of Bisamide Derivative of Dicarboxylic Acid (BDDA) and its impact on pancreatic stem cells in vivo. To assess the impact of BDDA, we applied a combination of histological and biochemical methods along with a cytometric analysis of stem cell and progenitor cell markers. We show that in mice with metabolic disorders, BDDA has a positive effect on lipid and glucose metabolism. The pancreatic restoration was associated with a decrease of the inhibitory effects of inflammation and obesity factors on pancreatic stem cells. Our data shows that BDDA increases the number of pancreatic stem cells. Thus, BDDA could be used as a new compound for treating complication of the metabolic syndrome such as diabetes.

scholarly journals An Overview of the Biological Effects of Some Mediterranean Essential Oils on Human Health

2017 ◽  
Vol 2017 ◽  
pp. 1-14 ◽  
Author(s):  
Hazem S. Elshafie ◽  
Ippolito Camele
Keyword(s):  
Essential Oils ◽  
Biological Effects ◽  
Human Pathogens ◽  
Factors Affecting ◽  
Current Review ◽  
Mediterranean Plants ◽  
Pharmaceutical Industries ◽  
Mediterranean Plant ◽  
Pharmaceutical Agents ◽  
Common Plant

Essential oils (EOs), extracted from aromatic plants, are interesting natural products and represent an important part of the traditional pharmacopeia. The use of some EOs as alternative antimicrobial and pharmaceutical agents has attracted considerable interest recently. Most of the EOs and their single constituents have been reported to inhibit several phytopathogens, human pathogens, and insects as well as their effective uses in food and pharmaceutical industries. The current review discussed the chemical composition and bioactivity of some important EOs extracted from some Mediterranean plants and their principal bioactive single constituents. Information has been furnished on the mechanisms, mode of actions, and factors affecting the bioactivity of some single constituents from different Mediterranean plant EOs. The current review gives an insight into some common plant EOs belonging to Lamiaceae, Apiaceae, Rutaceae, and Verbenaceae families commonly growing in Mediterranean region. Further information has been provided about the medical uses of some EOs for several human diseases covering the pharmacological effects (anti-inflammatory, antioxidant, and anticarcinogenic). The antimicrobial effects have been also considered in the current review. Although plant EOs are considered promising natural alternatives for many chemical drugs, they still need more specific research for wide application especially in food and pharmaceutical industries.

scholarly journals Biological effects of ubiquitin-specific peptidase 22 on thyroid papillary cancer cells and its mechanism of action

2020 ◽  
Vol 9 (5) ◽  
pp. 3703-3711
Author(s):  
Hong-Qun Wang ◽  
Ying Li ◽  
Shan-Shan Ding ◽  
Ying-Xue Li ◽  
Ai-Chun Wang ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Mechanism Of Action ◽  
Biological Effects ◽  
Papillary Cancer ◽  
Thyroid Papillary ◽  
Thyroid Papillary Cancer

scholarly journals Caffeic acid phenethyl ester (CAPE): cornerstone pharmacological studies and drug delivery systems

Pharmacia ◽  
2019 ◽  
Vol 66 (4) ◽  
pp. 223-231 ◽  
Author(s):  
Yordan Yordanov
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Biological Effects ◽  
Caffeic Acid Phenethyl Ester ◽  
Delivery Systems ◽  
Large Contribution ◽  
Current Review ◽  
Pharmacological Studies

Propolis is a natural product with a plethora of biological effects, utilized by traditional medicine since antiquity. However, its application as a pharmaceutical is hindered by its variable composition and difficult standardization. CAPE has been shown to be a major component of propolis, with a large contribution to its pharmacological effects, among which the anti-inflammatory, antioxidant and antineoplastic have been attracting most attention. The current review article aims to present the cornerstone pharmacological studies of CAPE throughout the years, following its discovery, which confirmed its primary importance among propolis constituents and opened the path to its intensive research as a potential pharmaceutical. We present the diversity of drug delivery systems of CAPE, which have been developed to improve its efficacy in in vitro and in vivo disease models and discuss their primary promises and weaknesses. The increased interest in recent years over more practical approaches of CAPE research such as its pharmaceutical formulation comes to show that it has a potential to become commercialized as a pharmaceutical.

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