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View article: Evaluation of molecular mechanisms of (Z)-3-(pentadec-10′-enyl)-catechol (litreol) and synthetic derivatives as inhibitors of human leukotriene biosynthesis
Evaluation of molecular mechanisms of (Z)-3-(pentadec-10′-enyl)-catechol (litreol) and synthetic derivatives as inhibitors of human leukotriene biosynthesis Open
View article: Uncovering anti-inflammatory natural products that synergize with supplemented omega-3 PUFA for eliciting endogenous inflammation resolution signals
Uncovering anti-inflammatory natural products that synergize with supplemented omega-3 PUFA for eliciting endogenous inflammation resolution signals Open
Inflammation resolution is governed by specialized pro-resolving mediators (SPM), mainly formed from omega-3 polyunsaturated fatty acids (n-3 PUFA) by lipoxygenases (LOX), which terminate inflammatory processes and facilitate healing and t…
View article: Sex hormone deprivation abolishes sex‐specific differences in murine colon inflammation and related lipid mediator production
Sex hormone deprivation abolishes sex‐specific differences in murine colon inflammation and related lipid mediator production Open
Unresolved inflammation, due to unfavorable imbalances between pro‐inflammatory and pro‐resolving mediators, leads to chronic inflammatory pathologies that are often sex‐biased and regulated by sex hormones, including inflammatory bowel di…
View article: A Comprehensive <i>In Vitro</i> Characterization of a New Class of Indole-Based Compounds Developed as Selective Haspin Inhibitors
A Comprehensive <i>In Vitro</i> Characterization of a New Class of Indole-Based Compounds Developed as Selective Haspin Inhibitors Open
Haspin is an emerging, but rather unexplored, divergent kinase involved in tumor growth by regulating the mitotic phase. In this paper, the in-silico design, synthesis, and biological characterization of a new series of substituted …
View article: Cannabidiol acts as molecular switch in innate immune cells to promote the biosynthesis of inflammation-resolving lipid mediators
Cannabidiol acts as molecular switch in innate immune cells to promote the biosynthesis of inflammation-resolving lipid mediators Open
View article: Glucocorticoids regulate lipid mediator networks by reciprocal modulation of 15-lipoxygenase isoforms affecting inflammation resolution
Glucocorticoids regulate lipid mediator networks by reciprocal modulation of 15-lipoxygenase isoforms affecting inflammation resolution Open
Glucocorticoids (GC) are potent anti-inflammatory agents, broadly used to treat acute and chronic inflammatory diseases, e.g., critically ill COVID-19 patients or patients with chronic inflammatory bowel diseases. GC not only limit inflamm…
View article: Allosteric Activation of 15‐Lipoxygenase‐1 by Boswellic Acid Induces the Lipid Mediator Class Switch to Promote Resolution of Inflammation
Allosteric Activation of 15‐Lipoxygenase‐1 by Boswellic Acid Induces the Lipid Mediator Class Switch to Promote Resolution of Inflammation Open
Specialized pro‐resolving mediators (SPM), primarily produced in innate immune cells, exert crucial bioactions for resolving inflammation. Among various lipoxygenases (LOX), 15‐LOX‐1 is key for SPM biosynthesis, but cellular activation pri…
View article: Identification of 2-Aminoacyl-1,3,4-thiadiazoles as Prostaglandin E<sub>2</sub> and Leukotriene Biosynthesis Inhibitors
Identification of 2-Aminoacyl-1,3,4-thiadiazoles as Prostaglandin E<sub>2</sub> and Leukotriene Biosynthesis Inhibitors Open
The application of a multi-step scientific workflow revealed an unprecedented class of PGE2/leukotriene biosynthesis inhibitors with in vivo activity. Specifically, starting from a combinatorial virtual library of ∼4.2 × …
View article: Discovery and Optimization of Indoline-Based Compounds as Dual 5-LOX/sEH Inhibitors: <i>In Vitro</i> and <i>In Vivo</i> Anti-Inflammatory Characterization
Discovery and Optimization of Indoline-Based Compounds as Dual 5-LOX/sEH Inhibitors: <i>In Vitro</i> and <i>In Vivo</i> Anti-Inflammatory Characterization Open
The design of multitarget drugs represents a promising strategy in medicinal chemistry and seems particularly suitable for the discovery of anti-inflammatory drugs. Here, we describe the identification of an indoline-based compound inhibit…
View article: Modulation of Inflammation-Related Lipid Mediator Pathways by Celastrol During Human Macrophage Polarization
Modulation of Inflammation-Related Lipid Mediator Pathways by Celastrol During Human Macrophage Polarization Open
Depending on the timing and concentration, CS not only favorably affects LOX activities in macrophages but also the expression of LM-biosynthetic enzymes during macrophage polarization connected to changes of inflammation-related LM which …
View article: Mycobacterium tuberculosis-Induced Upregulation of the COX-2/mPGES-1 Pathway in Human Macrophages Is Abrogated by Sulfasalazine
Mycobacterium tuberculosis-Induced Upregulation of the COX-2/mPGES-1 Pathway in Human Macrophages Is Abrogated by Sulfasalazine Open
Macrophages are the primary human host cells of intracellular Mycobacterium tuberculosis ( M.tb ) infection, where the magnitude of inflammatory reactions is crucial for determining the outcome of infection. Previously, we showed that the …
View article: <i>Staphylococcus aureus</i> controls eicosanoid and specialized pro‐resolving mediator production via lipoteichoic acid
<i>Staphylococcus aureus</i> controls eicosanoid and specialized pro‐resolving mediator production via lipoteichoic acid Open
Staphylococcus aureus causes severe infections associated with inflammation, such as sepsis or osteomyelitis. Inflammatory processes are regulated by distinct lipid mediators (LMs) but how their biosynthetic pathways are orchestrated in S …
View article: Sex Hormone–Dependent Lipid Mediator Formation in Male and Female Mice During Peritonitis
Sex Hormone–Dependent Lipid Mediator Formation in Male and Female Mice During Peritonitis Open
Introduction: Sex differences in inflammation are obvious and contribute to divergences in the incidence and severity of inflammation-related diseases that frequently preponderate in women. Lipid mediators (LMs), mainly produced by lipoxyg…
View article: The α-tocopherol-derived long-chain metabolite α-13′-COOH mediates endotoxin tolerance and modulates the inflammatory response via MAPK and NFκB pathways
The α-tocopherol-derived long-chain metabolite α-13′-COOH mediates endotoxin tolerance and modulates the inflammatory response via MAPK and NFκB pathways Open
CCL2 is suppressed in murine macrophages by α-13'-COOH and the indirect suppression of MAPK and NFκB pathways is likely a relevant process contributing to anti-inflammatory actions of α-13'-COOH. These results improve the understanding of …
View article: Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation
Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation Open
Endogenous long-chain metabolites of vitamin E (LCMs) mediate immune functions by targeting 5-lipoxygenase (5-LOX) and increasing the systemic concentrations of resolvin E3, a specialized proresolving lipid mediator. SAR studies on semisyn…
View article: Beneficial Modulation of Lipid Mediator Biosynthesis in Innate Immune Cells by Antirheumatic Tripterygium wilfordii Glycosides
Beneficial Modulation of Lipid Mediator Biosynthesis in Innate Immune Cells by Antirheumatic Tripterygium wilfordii Glycosides Open
Tripterygium wilfordii glycosides (TWG) is a traditional Chinese medicine with effectiveness against rheumatoid arthritis (RA), supported by numerous clinical trials. Lipid mediators (LM) are biomolecules produced from polyunsaturated fatt…
View article: From Vietnamese plants to a biflavonoid that relieves inflammation by triggering the lipid mediator class switch to resolution
From Vietnamese plants to a biflavonoid that relieves inflammation by triggering the lipid mediator class switch to resolution Open
View article: Staphylococcus aureus-Derived α-Hemolysin Evokes Generation of Specialized Pro-resolving Mediators Promoting Inflammation Resolution
Staphylococcus aureus-Derived α-Hemolysin Evokes Generation of Specialized Pro-resolving Mediators Promoting Inflammation Resolution Open
Underlying mechanisms of how infectious inflammation is resolved by the host are incompletely understood. One hallmark of inflammation resolution is the activation of specialized pro-resolving mediators (SPMs) that enhance bacterial cleara…
View article: Editorial: Role of Blood Cells in Inflammatory and Vascular Disorders
Editorial: Role of Blood Cells in Inflammatory and Vascular Disorders Open
EDITORIAL article Front. Pharmacol., 11 September 2020Sec. Inflammation Pharmacology Volume 11 - 2020 | https://doi.org/10.3389/fphar.2020.585705
View article: Impact of Androgens on Inflammation-Related Lipid Mediator Biosynthesis in Innate Immune Cells
Impact of Androgens on Inflammation-Related Lipid Mediator Biosynthesis in Innate Immune Cells Open
Rheumatoid arthritis, asthma, allergic rhinitis and many other disorders related to an aberrant immune response have a higher incidence and severity in women than in men. Emerging evidences from scientific studies indicate that the activit…
View article: The Anti-Inflammatory and Antimicrobial Potential of Selected Ethnomedicinal Plants from Sri Lanka
The Anti-Inflammatory and Antimicrobial Potential of Selected Ethnomedicinal Plants from Sri Lanka Open
Traditional folk medicine in Sri Lanka is mostly based on plants and plant-derived products, however, many of these medicinal plant species are scientifically unexplored. Here, we evaluated the anti-inflammatory and antimicrobial potency o…
View article: Region-Specific Proteome Changes of the Intestinal Epithelium during Aging and Dietary Restriction
Region-Specific Proteome Changes of the Intestinal Epithelium during Aging and Dietary Restriction Open
The small intestine is responsible for nutrient absorption and one of the most important interfaces between the environment and the body. During aging, changes of the epithelium lead to food malabsorption and reduced barrier function, thus…
View article: Communication between human macrophages and epithelial cancer cell lines dictates lipid mediator biosynthesis
Communication between human macrophages and epithelial cancer cell lines dictates lipid mediator biosynthesis Open
View article: Myxochelin- and Pseudochelin-Derived Lipoxygenase Inhibitors from a Genetically Engineered <i>Myxococcus xanthus</i> Strain
Myxochelin- and Pseudochelin-Derived Lipoxygenase Inhibitors from a Genetically Engineered <i>Myxococcus xanthus</i> Strain Open
Precursor-directed biosynthesis was used to introduce selected aryl carboxylic acids into the pseudochelin pathway, which had recently been assembled in Myxococcus xanthus. Overall, 14 previously undescribed analogues of the natural…
View article: Synthesis, biological evaluation and molecular modeling of novel selective COX-2 inhibitors: sulfide, sulfoxide, and sulfone derivatives of 1,5-diarylpyrrol-3-substituted scaffold
Synthesis, biological evaluation and molecular modeling of novel selective COX-2 inhibitors: sulfide, sulfoxide, and sulfone derivatives of 1,5-diarylpyrrol-3-substituted scaffold Open
View article: Vacuolar (H+)-ATPase Critically Regulates Specialized Proresolving Mediator Pathways in Human M2-like Monocyte-Derived Macrophages and Has a Crucial Role in Resolution of Inflammation
Vacuolar (H+)-ATPase Critically Regulates Specialized Proresolving Mediator Pathways in Human M2-like Monocyte-Derived Macrophages and Has a Crucial Role in Resolution of Inflammation Open
Alternative (M2)-polarized macrophages possess high capacities to produce specialized proresolving mediators (SPM; i.e., resolvins, protectins, and maresins) that play key roles in resolution of inflammation and tissue regeneration. Vacuol…
View article: Protective effect of piceatannol and bioactive stilbene derivatives against hypoxia-induced toxicity in H9c2 cardiomyocytes and structural elucidation as 5-LOX inhibitors
Protective effect of piceatannol and bioactive stilbene derivatives against hypoxia-induced toxicity in H9c2 cardiomyocytes and structural elucidation as 5-LOX inhibitors Open
View article: The standardized herbal combination BNO 2103 contained in Canephron® N alleviates inflammatory pain in experimental cystitis and prostatitis
The standardized herbal combination BNO 2103 contained in Canephron® N alleviates inflammatory pain in experimental cystitis and prostatitis Open
View article: Gliotoxin from Aspergillus fumigatus Abrogates Leukotriene B4 Formation through Inhibition of Leukotriene A4 Hydrolase
Gliotoxin from Aspergillus fumigatus Abrogates Leukotriene B4 Formation through Inhibition of Leukotriene A4 Hydrolase Open
View article: Targeting biosynthetic networks of the proinflammatory and proresolving lipid metabolome
Targeting biosynthetic networks of the proinflammatory and proresolving lipid metabolome Open
Nonsteroidal anti‐inflammatory drugs interfere with the metabolism of arachidonic acid to proinflammatory prostaglandins and leukotrienes by targeting cyclooxygenases (COXs), 5‐lipoxygenase (LOX), or the 5‐LOX–activating protein (FLAP). Th…