• The levels of prostaglandin E2 (PGE2), PGF2 alpha, PGI2, thromboxane A2 (TXA2), and leukotriene B4 (LTB4), which represent the cyclooxygenase and 5-lipoxygenase pathways, were determined in 21 pairs of surgically excised human colon cancer and histologically normal mucosa samples 5 to 10 cm away from the tumor. (nih.gov)
  • The data indicated that inhibition of the cyclooxygenase pathway alone was less effective than inhibition of both the lipoxygenase and cyclooxygenase pathways of arachidonic- acid metabolism in blocking A23187 mediated chemiluminescence. (cdc.gov)
  • inhibition of 5-lipoxygenase (5-LO), which is expected to be involved in DHEA- and NALA-degradation pathway, also partially blocked the ability of DHEA and NALA to inhibit cell proliferation and phosphorylated Akt. (biomedcentral.com)
  • It was previously reported that proadifen (SKF-525A), a well-known cytochrome P450 monooxygenase inhibitor, not only has anti-proliferative potential in some cancer cell lines, but it is also able to inhibit BCRP and MRP1 transporter proteins ( 8 ). (spandidos-publications.com)
  • Liver transcriptomic analysis indicated that GE mainly influenced the primary bile acid (PBA) biosynthesis and bile secretion pathways. (bvsalud.org)
  • A total of 99 potential targets were identified in the network pharmacology analysis of CQD, indicating its involvement in the regulation of inflammatory and apoptotic signaling pathways, and potential value for treating HUA and alleviating kidney injury. (bvsalud.org)
  • The prostaglandin and leukotriene families of lipid mediators are formed via two distinct biosynthetic pathways that are initiated by the oxygenation of arachidonic acid by either cyclooxygenase-2 (COX-2) or 5-lipoxygenase (5-LOX), respectively. (elsevierpure.com)
  • Effect of dietary stilbenes on 5-lipoxygenase and cyclooxygenases activities in vitro. (cas.cz)
  • This includes lipoxygenases, which incorporate one molecule of O2 into the carbon framework and cyclooxygenases, which incorporate two molecules of O2. (vanderbilt.edu)
  • We have conducted extensive functional studies with lipoxygenases and cyclooxygenases based on available crystal structures and employing exhaustive site-directed mutagenesis. (vanderbilt.edu)
  • The relationship between cultivated soybean and perennial soybean seed proteins were examined by immunoblot analyses using antibodies raised against G. max ß-conglycinin, glycinin A3 subunit, lipoxygenase, leginsulin, Kunitz trypsin inhibitor and Bowman-Birk protease inhibitor. (usda.gov)
  • Compounds that bind to and inhibit that enzymatic activity of LIPOXYGENASES. (bvsalud.org)
  • As we previously described, proadifen, a P450 monooxygenase inhibitor, might also be able to inhibit some ABC transporters, including breast cancer resistance protein (BCRP). (spandidos-publications.com)
  • and the 5α-reductase inhibitors [which inhibit the development of BPH through a reduction in dihydrotestosterone (DHT) production]. (frontiersin.org)
  • and Q702, an Axl/Mer/CSF1R triple kinase inhibitor for the treatment of drug resistant non-small cell lung cancer and other cancer types. (pharmaceutical-technology.com)
  • The mainstay of treatment for advanced hepatocellular carcinoma (HCC) was the tyrosine kinase inhibitor (TKI) sorafenib [ 5 ]. (biomedcentral.com)
  • 3-[3-Amino-4-(indan-2-yloxy)-5-(1-methyl-1 H -indazol-5-yl)-phenyl]-propionic acid (AK106-001616) is a novel, potent, and selective inhibitor of the cytosolic phospholipase A 2 (cPLA 2 ) enzyme. (aspetjournals.org)
  • Kaithwas, Gaurav 2019-10-24 00:00:00 Background: This study evaluates the anti-cancer effects of Tadalafil (potent PDE-5 inhibitor) in female albino wistar rats against n-methyl n-nitrosourea induced mammary gland carcinogenesis. (sagepub.com)
  • These results pave the way for the rational design of 5-LOX/sEH dual inhibitors and for further investigation of their potential use as anti-inflammatory agents. (inrae.fr)
  • Antileukotrienes include leukotriene receptor antagonists (e.g. montelukast, zafirlukast and pranlukast) and leukotriene synthesis inhibitors (e.g. zileuton) [6]. (roma2024.com)
  • Assessment of in vivo 5-lipoxygenase activity by analysis of leukotriene B4 in saliva: effects of treatment with zileuton. (findmedarticle.com)
  • Effects of 5-lipoxygenase inhibitor zileuton on airway responses to inhaled swine house dust in healthy subjects. (findmedarticle.com)
  • While conventional drugs such as the α1-adrenergic receptor antagonists and 5α-reductase inhibitors have been found to be useful in the treatment of BPH, the adverse side effects associated with their usage, have led to increased search for alternative means of managing this disease. (frontiersin.org)
  • Unlike traditional nonsteroidal anti-inflammatory drugs and selective cyclooxygenase-2 inhibitors, AK106-001616 reduced prostaglandin E 2 (PGE 2 ) and leukotriene B 4 (LTB 4 ) production by stimulated cells. (aspetjournals.org)
  • The mechanism of the anti-lipolytic effect of two anti-cachectic agents, eicosapentaenoic acid, an ω-3 polyunsaturated fatty acid (PUFA), and N-(3-phenoxycinnamyl)acetohydroxamic acid (BW A4C), a 5-lipoxygenase inhibitor, has been investigated. (aston.ac.uk)
  • and lipoxygenase analysis based on product principle resulted hydro per oxyeicosatetraenoic acid (HPETE). (envirobiotechjournals.com)
  • previously named ML3000) is a substrate analogue of arachidonic acid which inhibits cyclooxygenase type 1 and 2 (COX1 and COX2) and 5-lipoxygenase (5-LOX), decreasing prostaglandins and leukotrienes production. (j-epilepsy.org)
  • The metabolic pathway of arachidonic acid (AA) has two main branches: 1) AA is converted by COX-1 and COX-2 into prostaglandins (PG) and thromboxane (TX), and 2) the actions of 5-lipoxygenase (5-LO) and 5-Lipoxygenase Activating Protein (FLAP) create leukotrienes (LT) in the other arm of the pathway [ 16 ]. (biomedcentral.com)
  • 5-Lipoxygenase, Human, Recombinant, S. fruigiperda 5-Lipoxygenase, Human, Recombinant, S. frugiperda E.C 1.13.11.34, catalyzes the formation of 5(S)-HpETE from arachidonic acid and its subsequent conversion to leukotriene A4. (sigmaaldrich.com)
  • Funk and co-investigators localized COX-1 to 9q32-q33.3 via somatic hybrid deoxyribonucleic acid (DNA) analysis. (medscape.com)
  • These compounds underwent extensive in vitro investigation revealing dual 5-LOX/sEH inhibitors, with 73 showing the most promising activity (IC(50)s of 0.41 +/- 0.01 and 0.43 +/- 0.10 microM for 5-LOX and sEH, respectively). (inrae.fr)
  • HKD2 and HKE2 were formed in human blood leukocytes activated with bacterial lipopolysaccharide and calcium ionophore A23187, and biosynthesis was blocked by inhibitors of 5-LOX or COX-2. (elsevierpure.com)
  • Enzymatic and cellular assays revealed the indoline derivative 43 as a notable 5-LOX inhibitor, guiding the design of new analogues. (inrae.fr)
  • Abnormal expression of 5-Lipoxygenase Activating Protein (FLAP) has been detected in many tumor cells. (biomedcentral.com)
  • The phospholipase-A2 inhibitor, quinacrine, completely blocked A23187 induced chemiluminescence but only partially blocked FMLP stimulated chemiluminescence. (cdc.gov)
  • Our results show that maternal dietary n-3 PUFA deficiency increases microglia-mediated phagocytosis of synaptic elements in the rodent developing hippocampus, partly through the activation of 12/15-lipoxygenase (LOX)/12-HETE signaling, altering neuronal morphology and affecting cognitive performance of the offspring. (nature.com)
  • aminoguanidine (100 mg/kg, i.p.), as an inducible NOS (iNOS) inhibitor and 7-nitroindazole (60 mg/kg, i.p.), as a neuronal NOS inhibitor were injected 15 min before licofelone. (j-epilepsy.org)
  • The Pharmacology of TNF Inhibitors - August 17, 2001. (powershow.com)
  • Upregulation of NOS was assessed by measuring enzyme levels in lung homogenates by Western blot analysis and enhancement of the COX-related pathway was judged from perfusate concentrations of 6‐ketoprostaglandin F 1α . (ersjournals.com)
  • Sjögren-Larsson syndrome (SLS) is diagnosed by demonstrating the enzyme deficiency or by mutation analysis of the FALDH gene. (medscape.com)
  • TNF inhibitors may increase the risk of skin cancer, particularly non-melanoma skin cancers like squamous cell carcinoma. (powershow.com)
  • however, studies provide some data on leukotriene synthesis inhibitors as possible therapeutic agents for patients with Sjögren-Larsson syndrome. (medscape.com)
  • TNF Alpha Inhibitors Market Overview 2023-2032 - Market Growth Analysis, Trends And Drivers - TNF alpha inhibitors refer to medications that are used to treat inflammatory diseases such as rheumatoid arthritis (RA), psoriatic arthritis, and juvenile idiopathic arthritis and that help to reduce or eliminate inflammation. (powershow.com)
  • Few human studies in the past have also examined the role of metformin Epirubicin Hydrochloride tyrosianse inhibitor in sepsis and lung diseases. (biobender.com)
  • Effects of selective and non-selective COX inhibitors on antigen-induced release of prostanoid mediators and bronchoconstriction in the isolated perfused and ventilated guinea pig lung. (findmedarticle.com)
  • of ELISA assessment and European Blot analyses performed on anti-PA, anti-pXO2-60 and anti-LF antibodies. (biobender.com)
  • The work on lipid mediators is focused on endocannabinoid oxygenation products of COX-2 and 15-lipoxygenase whereas the work on lipid peroxidation products is focused on malondialdehyde, 4-hydroxynonenal, and structurally related molecules. (vanderbilt.edu)
  • Repurposing mechanistic insight of PDE-5 inhibitor in cancer chemoprevention through. (sagepub.com)
  • The in vitro result displayed the sea plumes gorgonian extract was less potential as xanthine oxidase and lipoksigenase inhibitor. (envirobiotechjournals.com)
  • Eicosanoids may participate in colon carcinogenesis, as evidenced from work in animal tumor models showing prevention of colon cancer by inhibitors of their synthesis and epidemiologic studies demonstrating reduced risk of colon cancer in long-term users of aspirin and other nonsteroidal antiinflammatory drugs (NSAIDs). (nih.gov)
  • Here we identify two cyclic hemiketal (HK) eicosanoids, HKD 2 and HKE 2 , as the major nonenzymatic rearrangement products of the diendoperoxide using liquid chromatography-mass spectrometry analyses as well as UV and NMR spectroscopy. (elsevierpure.com)
  • The GC-MS analysis of the methanolic extract of BG revealed 23 compounds which are reported to possess different biological activities. (biomedcentral.com)
  • Several other software tools exist that address the challenges regarding the organization and analysis of chemical and biological data. (biomedcentral.com)
  • Our 2-D gel and immunoblot analyses demonstrate significant differences in the protein composition and size heterogeneities of the 7S and 11S seed storage proteins of soybean and perennial Glycine species. (usda.gov)
  • Electrophoretic mobility shift analysis using nuclear extracts obtained from RAW264 cells and from the promonocytic cell line U-937 revealed the formation of at least three distinct protein-DNA complexes at each of these sites, one of which was found to contain the transcription factor Sp1. (uni-frankfurt.de)
  • Quantitative real-time PCR and Western blot analyses showed that compared with the Model group, adenosine triphosphate (ATP)-binding cassette efflux transporter G2 (ABCG2) expression in the CQD group was significantly upregulated (P (bvsalud.org)
  • Expression of 15-lipoxygenase type-1 in human mast cells. (findmedarticle.com)
  • The result of lipoxygenase inhibitor showed that IC50 value of bark nhexane extract and bark ethyl acetate extract were 2.14 μg/mL and 11.65 ug/mL respectively compared tobaikelain standard IC50 of 0.01ug/mL. (envirobiotechjournals.com)
  • The animal tissue and serum samples were evaluated for the presence of antioxidant parameters and the cellular morphology was studied using carminic staining, haematoxylin staining and scanning electron microscopy followed by immunoblotting analysis. (sagepub.com)
  • It also covers disease epidemiology, treatment algorithms, treatment patterns, in-depth analysis of the pipeline, and deal analysis. (powershow.com)
  • Tadalafil is a known phosphodiesterase-5 Distinct metastasis and resistance development by self- (PDE-5) inhibitor, which have anti-cancer effects in vari- renewing nascent cancer cells in response with the ous types of cancer [2]. (sagepub.com)
  • The GC-MS analysis showed 27 bioactive compounds. (ijpsr.com)
  • In silico analysis of an in-house library identified nine compounds as potential 5-LOX inhibitors. (inrae.fr)
  • by Gas Chromatography-Mass Spectrometry (GC-MS) analysis by ethanol extract. (ijpsr.com)
  • The extract was subjected to GC-MS analysis 13 . (ijpsr.com)
  • and selective CDK7 inhibitors to treat cancer. (pharmaceutical-technology.com)
  • Dans une étude cas-témoins non appariés en milieu hospitalier, 108 personnes atteintes d'un cancer et 105 témoins ont été interrogés sur leurs apports alimentaires en recourant à la version en langue arabe d'un questionnaire validé sur la fréquence de consommation alimentaire. (who.int)
  • The same extracts were assessed for their antioxidative potentials with the use of DPPH free radical scavenging assay followed by determination of HRBC membrane stabilization method, Brine Shrimp Lethality Assay (BSLA) and GC-MS analysis. (biomedcentral.com)
  • Additionally, we have measured the trypsin and chymotrypsin inhibitor activities from cultivated soybean and perennial Glycine species, and have found marked differences between them. (usda.gov)
  • Licofelone is a cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibitor, which its effectiveness to treat osteoarthritis has been approved. (j-epilepsy.org)
  • Today, Scaffold Hunter supports a wide range of analysis tasks independent from the underlying molecular scaffolds, while scaffold based approaches still remain an integral part of the software. (biomedcentral.com)
  • Cyclooxygenase-2 (COX-2) is the molecular target of non-steroidal anti-inflammatory drugs (NSAIDs) and selective COX-2 inhibitors. (vanderbilt.edu)
  • Our laboratory has combined structural analysis with functional studies to define the molecular determinants of the interaction of ligands (substrates and inhibitors) with COX-2. (vanderbilt.edu)
  • Comparative analysis of the effect of site-directed mutation of active site residues on the binding of substrates and inhibitors to COX-1 and COX-2 led us to hypothesize that neutral derivatives of esters and amides would bind selectively to COX-2. (vanderbilt.edu)
  • All other studies experienced unclear or higher overall risk of bias and meta-analyses were consequently deemed unfeasible. (roma2024.com)