scholarly journals Σύνθεση και μελέτη αναστολέων λιπολυτικών ενζύμων

2016 ◽  
Author(s):  
Αικατερίνη Νικολάου
Keyword(s):  
Fatty Acids ◽  
Lysophosphatidic Acid ◽  
Inhibitory Activity ◽  
Functional Group ◽  
Inflammatory Diseases ◽  
Hydroxamic Acids ◽  
Pharmacological Properties ◽  
Ester Bond ◽  
Phospholipases A2 ◽  
Inflammatory Conditions

Phospholipases A2 (PLA2) are enzymes that hydrolyze the sn-2 ester bond of phospholipids releasing free fatty acids and lysophospholipids. Among them, arachidonic acid can be converted into a variety of eicosanoids by metabolic enzymes, while lysophosphatidylcholine (LPC), the most abundant lysophospholipid in plasma and tissues, can be converted into lysophosphatidic acid (LPA) by a secreted enzyme that exhibits lysophospholipase D activity, known as autotaxin (ATX). Both enzymes are involved in inflammatory conditions and, as a consequence, constitute attractive targets for the development of novel agents for the treatment of inflammatory diseases. Due to the fact that molecules which bear the 2-oxoamide functional group and long aliphatic chains exhibit inhibitory activity against cytosolic GIVA cPLA2, 2-oxoamideswith reduced lipophilicity were designed and synthesized. Taking into consideration that in recent years hydroxamic acids have attracted considerable attention due to their pharmacological properties, hydroxamic acids and derivatives there of were designed and synthesized, so as to evaluate their inhibitory activity against ATX.

Potent and selective 2-oxoamide inhibitors of phospholipases A2 as novel medicinal agents for the treatment of inflammatory diseases

2012 ◽  
Vol 84 (9) ◽  
pp. 1877-1894 ◽  
Author(s):  
Efrosini Barbayianni ◽  
Georgia Antonopoulou ◽  
George Kokotos
Keyword(s):  
Amino Acids ◽  
Fatty Acids ◽  
Inflammatory Diseases ◽  
Ester Bond ◽  
Selective Inhibitors ◽  
Phospholipases A2 ◽  
Hydrolysis Of ◽  
Major Target ◽  
Phospholipases A

Phospholipases A2 (PLA2s) are enzymes that are capable of catalyzing the hydrolysis of the sn-2 ester bond of glycerophospholipids, releasing free fatty acids, including arachidonic acid (AA), and lysophospholipids. Both products are precursor signaling molecules involved in inflammation. Among the various PLA2s, cytosolic GIVA cPLA2 is considered a major target for inflammatory diseases, while secreted GIIA sPLA2 is involved in cardiovascular diseases. We have developed lipophilic 2-oxoamides based on (S)-γ- or δ-amino acids as potent and selective inhibitors of GIVA cPLA2, which present interesting in vivo anti-inflammatory activity. 2-Oxoamides based on natural α-amino acids are selective inhibitors of GIIA sPLA2. The mode of binding of 2-oxoamides with either GIVA cPLA2 or GIIA sPLA2 has been studied by various techniques.

scholarly journals Chlorinated Phospholipids and Fatty Acids: (Patho)physiological Relevance, Potential Toxicity, and Analysis of Lipid Chlorohydrins

2016 ◽  
Vol 2016 ◽  
pp. 1-26 ◽  
Author(s):  
Jenny Schröter ◽  
Jürgen Schiller
Keyword(s):  
Fatty Acids ◽  
Hypochlorous Acid ◽  
Inflammatory Diseases ◽  
Fatty Acyl ◽  
Head Group ◽  
Inflammatory Conditions ◽  
First Case ◽  
Physiological Relevance ◽  
Fatty Aldehydes

Chlorinated phospholipids are formed by the reaction of hypochlorous acid (HOCl), generated by the enzyme myeloperoxidase under inflammatory conditions, and the unsaturated fatty acyl residues or the head group. In the first case the generated chlorohydrins are both proinflammatory and cytotoxic, thus having a significant impact on the structures of biomembranes. The latter case leads to chloramines, the properties of which are by far less well understood. Since HOCl is also widely used as a disinfecting and antibacterial agent in medicinal, industrial, and domestic applications, it may represent an additional source of danger in the case of abuse or mishandling. This review discusses the reaction behavior of in vivo generated HOCl and biomolecules like DNA, proteins, and carbohydrates but will focus on phospholipids. Not only the beneficial and pathological (toxic) effects of chlorinated lipids but also the importance of these chlorinated species is discussed. Some selected cleavage products of (chlorinated) phospholipids and plasmalogens such as lysophospholipids, (chlorinated) free fatty acids andα-chloro fatty aldehydes, which are all well known to massively contribute to inflammatory diseases associated with oxidative stress, will be also discussed. Finally, common analytical methods to study these compounds will be reviewed with focus on mass spectrometric techniques.

Hyperferritinaemia: An Iron Sword of Autoimmunity

2019 ◽  
Vol 25 (27) ◽  
pp. 2909-2918 ◽  
Author(s):  
Joanna Giemza-Stokłosa ◽  
Md. Asiful Islam ◽  
Przemysław J. Kotyla
Keyword(s):  
Immune Response ◽  
Macrophage Activation ◽  
Inflammatory Diseases ◽  
Acute Phase Reactant ◽  
Catastrophic Antiphospholipid Syndrome ◽  
Inflammatory Conditions ◽  
Phase Reactant ◽  
Signalling Molecule ◽  
Cytokine Synthesis

Background:: Ferritin is a molecule that plays many roles being the storage for iron, signalling molecule, and modulator of the immune response. Methods:: Different electronic databases were searched in a non-systematic way to find out the literature of interest. Results:: The level of ferritin rises in many inflammatory conditions including autoimmune disorders. However, in four inflammatory diseases (i.e., adult-onset Still’s diseases, macrophage activation syndrome, catastrophic antiphospholipid syndrome, and sepsis), high levels of ferritin are observed suggesting it as a remarkable biomarker and pathological involvement in these diseases. Acting as an acute phase reactant, ferritin is also involved in the cytokine-associated modulator of the immune response as well as a regulator of cytokine synthesis and release which are responsible for the inflammatory storm. Conclusion:: This review article presents updated information on the role of ferritin in inflammatory and autoimmune diseases with an emphasis on hyperferritinaemic syndrome.

Lipids and Free Fatty Acids of Red Sea Avrainvillea amadelpha, Holothuria atra, and Sarcocornia fruticosa Inhibit Marine Bacterial Biofilms

2020 ◽  
Vol 17 (6) ◽  
pp. 466-471
Author(s):  
Usama W. Hawas ◽  
Fekri Shaher ◽  
Mohamed Ghandourah ◽  
Lamia T. Abou El-Kassem ◽  
Sathianeson Satheesh ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Free Fatty Acids ◽  
Red Sea ◽  
Inhibitory Activity ◽  
Sea Cucumber ◽  
Bacterial Biofilms ◽  
Antibiofilm Activity ◽  
Bacterial Strains ◽  
Holothuria Atra ◽  
Sarcocornia Fruticosa

This study aimed at evaluating the antibiofilm activity of the Red Sea metabolites from green alga Avrainvillea amadelpha, sea cucumber Holothuria atra and costal plant Sarcocornia fruticosa against three biofilm bacterial strains isolated from Jeddah coast. Free fatty acids (FFAs) and other lipoidal matters were extracted from these organisms and analyzed by GC-MS. The composition of lipoidal fractions showed that A. amadelpha is rich by 74% saturated FAs, while sea cucumber H. atra revealed high content (60%) of unsaturated FAs. Palmitic acid is the major FA component in all species ranging from 14.5 to 26.7%. Phytol, sterols and hydrocarbons (C8-C29) were represented in the alga A. amadelpha as high contents with values 25.8, 21.9 and 18.5%, respectively. The extracts and lipoidal contents showed biofilm inhibitory activity against the isolated bacterial strains, where the unsaponified lipoidal fraction of S. fruticosa exhibited highest inhibitory activity against Planomicrobium sp. at concentration of 200 µg/mL.

Ternary complexes of N-carboxymethylaminoacetohydroxamic acid

1981 ◽  
Vol 46 (5) ◽  
pp. 1107-1115 ◽  
Author(s):  
Rolf Karlíček ◽  
Miroslav Polášek ◽  
Vladimír Jokl
Keyword(s):  
Complex Formation ◽  
Ternary System ◽  
Binuclear Complex ◽  
Functional Group ◽  
Hydroxamic Acids ◽  
Ternary Complexes ◽  
Hydrogen Ions ◽  
Ligand Structure ◽  
Excess Copper

The formation of N-carboxymethylaminoacetohydroxamic acid complexes in solutions with excess copper(II) or iron(III) ions or both of them was studied. In the presence of Cu(II), the binuclear complex Cu2H-1L+ was identified; in the ternary system, the complex CuFeH-1L+ was found. This complex formation is necessarily associated with the ligand structure >N-CH2.CO-NHOH and with a new property of hydroxamic acids of this type - detachment of two hydrogen ions from one carbohydroxamic functional group.

scholarly journals In Vitro Antimicrobial, Antioxidant and Anticancer Activities of Egyptian Citrus Beebread

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2433
Author(s):  
Nesren Elsayed ◽  
Hatem Sharaf El-Din ◽  
Ammar B. Altemimi ◽  
Hanaa Y. Ahmed ◽  
Anubhav Pratap-Singh ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Inhibitory Activity ◽  
Nutritive Value ◽  
Antioxidant Properties ◽  
Antitumor Agent ◽  
Monounsaturated Fatty Acids ◽  
Free Sugar ◽  
Natural Food ◽  
Anticancer Activities

In this study, Egyptian beebread (EBB) was investigated for its nutritive value, chemical composition, antioxidant properties, antimicrobial and antitumor activities. Results indicated that EBB was a good source of protein (23.58 ± 0.183 g/100 g BB), total free sugar (20.266 ± 0.930) and potassium (290.202 ± 2.645 mg/100 g). Additionally, 14 fatty acids were identified in EBB, wherein polyunsaturated and monounsaturated fatty acids represented 51.06% ± 0.09% and 9.86% ± 0.01%, respectively. The EBB extract exhibited almost 400% better antiradical activity than BHT, with IC50 of EBB extract being 10.7 µg/mL compared to 39.5 µg/mL for BHT. EBB exhibited higher inhibitory activity than the reference compound against Staphylococcus aureus and Escherichia coli, followed by Bacillus subtilis. No inhibitory activity was observed against Aspergillus Niger. Additionally, the highest inhibitory activity was recorded against Caco-2 cells, followed by PC3 and HepG-2 cancer cell lines with IC50 values 262, 314 and 386 μg/mL, respectively. These findings establish the potential of EBB as an antioxidant, antimicrobial and antitumor agent, with possible applications as natural food supplements and natural preservatives.

scholarly journals Illuminating an Invisible Epidemic: A Systemic Review of the Clinical and Economic Benefits of Early Diagnosis and Treatment in Inflammatory Disease and Related Syndromes

2019 ◽  
Vol 8 (4) ◽  
pp. 493 ◽  
Author(s):  
Wylezinski ◽  
Gray ◽  
Polk ◽  
Harmata ◽  
Spurlock
Keyword(s):  
Healthcare System ◽  
Inflammatory Diseases ◽  
The United States ◽  
Economic Benefits ◽  
Systemic Review ◽  
Best Interest ◽  
Delayed Treatment ◽  
Inflammatory Conditions ◽  
Slow Development ◽  
The U.S

Healthcare expenditures in the United States are growing at an alarming level with the Centers for Medicare and Medicaid Services (CMS) projecting that they will reach $5.7 trillion per year by 2026. Inflammatory diseases and related syndromes are growing in prevalence among Western societies. This growing population that affects close to 60 million people in the U.S. places a significant burden on the healthcare system. Characterized by relatively slow development, these diseases and syndromes prove challenging to diagnose, leading to delayed treatment against the backdrop of inevitable disability progression. Patients require healthcare attention but are initially hidden from clinician’s view by the seemingly generalized, non-specific symptoms. It is imperative to identify and manage these underlying conditions to slow disease progression and reduce the likelihood that costly comorbidities will develop. Enhanced diagnostic criteria coupled with additional technological innovation to identify inflammatory conditions earlier is necessary and in the best interest of all healthcare stakeholders. The current total cost to the U.S. healthcare system is at least $90B dollars annually. Through unique analysis of financial cost drivers, this review identifies opportunities to improve clinical outcomes and help control these disease-related costs by 20% or more.

Inflammatory and Obstructive Disorders of Salivary Glands

1987 ◽  
Vol 66 (1_suppl) ◽  
pp. 675-679 ◽  
Author(s):  
A. Blitzer
Keyword(s):  
Salivary Glands ◽  
Fine Needle Aspiration ◽  
Chronic Conditions ◽  
Viral Infections ◽  
Inflammatory Diseases ◽  
Needle Aspiration ◽  
Ct Scans ◽  
Fine Needle ◽  
Inflammatory Conditions ◽  
Chronic Sialadenitis

Obstructive and inflammatory diseases of the salivary glands can have a congenital, traumatic, metabolic, or infectious-inflammatory cause. The acute inflammatory conditions include bacterial and viral infections, and the chronic conditions include sialoliths, strictures, chronic sialadenitis, sialectasis, and lymphoepithelial disease. The neoplastic diseases can cause obstruction and/or infection and often make the diagnosis elusive. In addition to a working knowledge of possible etiology, one needs experience with clinical examination, salivary analysis, sialography, CT scans, MRI, and fine-needle aspiration and cytology in order successfully to evaluate and manage patients with these conditions.

scholarly journals Metabolite and Elastase Activity Changes in Beach Rose (Rosa rugosa) Fruit and Seeds at Various Stages of Ripeness

Plants ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1283
Author(s):  
Seung-Hun Chae ◽  
Young-Sang Lee ◽  
Jin-Hee Kim ◽  
Tae-Ho Han ◽  
Kang-Mo Ku
Keyword(s):  
Fatty Acids ◽  
Ursolic Acid ◽  
Inhibitory Activity ◽  
Ethanol Extract ◽  
Dry Weight ◽  
Total Phenolic ◽  
Rosa Rugosa ◽  
Optimal Harvest ◽  
Rose Hip ◽  
The Rose

Rose hips are the fruits of the beach rose (Rosa rugosa). To determine the optimal harvest time and to obtain the maximum functional compounds, rose hips at various stages of ripeness (immature, early, mid, and late) were harvested, and the flesh tissue and seeds were separated. The rose hip flesh showed the highest total phenolic content at the mid-ripeness stage (8.45 ± 0.62 mg/g gallic acid equivalent concentration (dry weight)). The early-, mid-, and late-ripeness stages of rose hip flesh did not show significantly different 2,2-diphenyl-1-picrylhydrazyl antioxidant capacities. The elastase inhibitory activity of the 95% ethanol extract from the rose hip seeds was highest at the mid-ripeness stage; however, the elastase inhibitory activity of the rose hip tissue was not significantly different from that of the seeds. Pathway analysis using MetaboAnalyst showed that sucrose, fructose, and glucose gradually increased as the fruit ripened. Ursolic acid was detected in the seeds but not in the flesh. Of the fatty acids, linoleic acid concentrations were highest in rose hip seeds, followed by linolenic acid, oleic acid, and palmitic acid. Fatty acids and ursolic acid might be the active compounds responsible for elastase inhibitory activity and can be utilized as a functional cosmetic material.

Inflammatory and Obstructive Disorders of Salivary Glands

1987 ◽  
Vol 66 (2_suppl) ◽  
pp. 675-679 ◽  
Author(s):  
A. Blitzer
Keyword(s):  
Salivary Glands ◽  
Fine Needle Aspiration ◽  
Chronic Conditions ◽  
Viral Infections ◽  
Inflammatory Diseases ◽  
Needle Aspiration ◽  
Ct Scans ◽  
Fine Needle ◽  
Inflammatory Conditions ◽  
Chronic Sialadenitis

Obstructive and inflammatory diseases of the salivary glands can have a congenital, traumatic, metabolic, or infectious-inflammatory cause. The acute inflammatory conditions include bacterial and viral infections, and the chronic conditions include sialoliths, strictures, chronic sialadenitis, sialectasis, and lymphoepithelial disease. The neoplastic diseases can cause obstruction and/or infection and often make the diagnosis elusive. In addition to a working knowledge of possible etiology, one needs experience with clinical examination, salivary analysis, sialography, CT scans, MRI, and fine-needle aspiration and cytology in order successfully to evaluate and manage patients with these conditions.

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