• Therefore, COX - also known as prostaglandin-endoperoxide synthase (PTGS), fatty acid COX, prostaglandin H (PGH) synthase, and EC 1.14.99.1 - is implicated in the production of fever, inflammation, and pain. (medscape.com)
  • Cyclooxygenase conversion of arachidonic acid into prostaglandin H2 (PGH2). (medscape.com)
  • Methoxy-8-(2-hydroxy-3-buthoxy-3-methylbutyloxy)-psoralen has been shown to regulate the cyclooxygenase-2 (COX-2)-dependent phase of prostaglandin D(2) generation in bone marrow-derived mast cells (IC50, 23.5 mM). (pureprescriptions.com)
  • PTGS2 (COX-2), converts arachidonic acid (AA) to prostaglandin endoperoxide H2. (wikipedia.org)
  • Their mechanism of action is unknown but may involve inhibition of cyclooxygenase activity and prostaglandin synthesis. (medscape.com)
  • This drug inhibits inflammatory reactions and pain, probably by decreasing the activity of the enzyme cyclooxygenase, which results in decreased prostaglandin synthesis. (medscape.com)
  • This agent acts by inhibiting inflammatory reactions and pain via decreasing the activity of cyclooxygenase, which results in a decrease of prostaglandin synthesis. (medscape.com)
  • Lungs and AM were analysed for pro- and anti-inflammatory lipid mediators, namely leukotriene B 4 (LTB 4 ), prostaglandin E 2 (PGE 2 ), 15(S)-hydroxy-eicosatetraenoic acid (15(S)-HETE), lipoxin A 4 (LXA 4 ) and oxidative stress marker 8-isoprostane by enzyme immunoassays and immunohistochemistry. (biomedcentral.com)
  • The AA, a normal component of cell membrane phospholipids, serve as substrate for prostaglandin endoperoxide (PGH) syntases-1 and -2, also known as cycloxygenase (COX)-1 and -2, lipoxygenase (5-, 12-, or 15) (LO), or cytochrome p450 enzymes [ 18 ]. (hindawi.com)
  • 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)
  • Free AA can be metabolized to eicosanoids through three major pathways: the cyclooxygenase (COX) pathway, the lipoxygenase (LOX) pathway, and the cytochrome P450 (CYP) pathway. (frontiersin.org)
  • 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)
  • Changes in dietary fatty acids, specifically the polyunsaturated fatty acids of the ω-3 and ω-6 families and some derived eicosanoids from lipoxygenases, cyclooxygenases, and cytochrome P-450, seem to control the activity of transcription factor families involved in cancer cell proliferation or cell death. (springer.com)
  • Selective COX-2 inhibitor NSAIDs that do not block COX-1, such as the celecoxib and rofecoxib, also are regarded as safe. (wikipedia.org)
  • 3 In an in vitro study using canine cell cultures, Carprofen demonstrated selective inhibition of COX-2 versus COX-1. (drugs.com)
  • 3 The existence of the d -receptor was subsequently proposed to explain the profile of activity in vitro of the enkephalins (the first endogenous opioid peptides), and on the basis of the relative potency of the non-selective opioid antagonist naloxone to reverse endogenous opioid peptide inhibition of the nerve-evoked contractions of the mouse vas deferens. (opioids.wiki)
  • Equally exciting are opportunities for effective chemoprevention with nonsteroidal anti-inflammatory agents, both synthetic and naturally occurring, or selective cyclooxygenase-2 inhibitors. (aacrjournals.org)
  • Cyclooxygenase-2 (COX-2) is the molecular target of non-steroidal anti-inflammatory drugs (NSAIDs) and selective COX-2 inhibitors. (vanderbilt.edu)
  • 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)
  • 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)
  • Inhibitors of protein kinases and calmodulin-dependent enzyme system did not prevent the PUFA-induced migration inhibition, which was also independent of phospholipase D-catalyzed hydrolysis of phospholipids. (jci.org)
  • In addition to aspirin, patients also react to other NSAIDs such as ibuprofen, and to any medication that inhibits the cyclooxygenase-1 (COX-1) enzyme, although paracetamol (acetaminophen) in low doses is generally considered safe. (wikipedia.org)
  • Regardless of the etiology, a deficiency of cyclooxygenase (COX), a key regulatory enzyme in the synthetic pathway of eicosanoid production, results in beneficial and detrimental physiologic conditions relative to imbalances of the eicosanoids. (medscape.com)
  • HGNC ID, HGNC:9605), also known as cyclooxygenase-2 or COX-2, is an enzyme that in humans is encoded by the PTGS2 gene. (wikipedia.org)
  • Each monomer of the enzyme has a peroxidase and a PTGS (COX) active site. (wikipedia.org)
  • Other mechanisms may also play a role, such as inhibition of leukotriene synthesis, lysosomal enzyme release, lipoxygenase activity, neutrophil aggregation, and various cell membrane functions. (medscape.com)
  • The major pharmacologic action of agents in this class is noncompetitive inhibition of the enzyme carbonic anhydrase. (medscape.com)
  • Urine volume increases with enzyme inhibition (proximal tubule reabsorption of water is reduced by approximately one third), which promotes an alkaline pH. (medscape.com)
  • It was concluded that the PUFA rather than their metabolites were responsible for the inhibition since: (a) antioxidants did not prevent the PUFA-induced migration inhibition and the hydroxylated intermediates were less active, and (b) inhibitors of the cyclooxygenase and lipoxygenase pathways were without effect. (jci.org)
  • These compounds are synthesized in vivo through what can now be regarded as the "orthodox" cyclooxygenase pathways, which came to light largely through the work of Sune Bergström, who led a team then based at the Karolinska Institutet in Stockholm. (jci.org)
  • Here, we focus on newly uncovered pathways, involving either the cyclooxygenases (COXs) or nonenzymatic chemical transformations, that lead to the formation of bioactive prostanoids and of previously unknown lipid mediators produced by COX-2. (jci.org)
  • Also, we suggest that COX/5-LOX activation is possibly required in the initial stage of onset but SE recruits extra excitatory pathways with prolongation. (j-epilepsy.org)
  • AD is associated with enhanced β-A production and accumulation resulting in neuroinflammation probably via activation of lipoxygenase (LOX) and cyclooxygenase (COX) pathways. (afpm.org.my)
  • GSE-related anti-cancer activity mostly relies on the induced increase in reactive oxygen species, followed by the orchestrated down- and up-regulation of several key-molecular pathways, including MAPK kinases, PI3K/Akt, NF-kB, cytoskeleton proteins and metalloproteinases. (oatext.com)
  • Aspirin-exacerbated respiratory disease (AERD), also called NSAID-exacerbated respiratory disease (NERD/N-ERD) or historically aspirin-induced asthma and Samter's Triad, refers to the triad of asthma, chronic rhinosinusitis with nasal polyps, and intolerance of aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs). (wikipedia.org)
  • Cardiac inflammation is easily accompanied by hypoxia, while hypoxia-induced injury and microenvironmental variations limit the efficacy of common anti-inflammatory drugs. (bvsalud.org)
  • The inducible cyclooxygenase, COX-2, generates prostaglandins involved in inflammation. (drugs.com)
  • Indeed, a number of studies have demonstrated that EET analogs and sEH inhibitors induce vasodilation, lower blood pressure and decrease inflammation. (frontiersin.org)
  • These include regulation of cell cycle, activation of mitochondrial pathway, induction of mitochondrial outer membrane permeabilization, induction of apoptosis, modulation of oxidative stress, amelioration of inflammation, modulation of insulin signaling and inhibition of angiogenesis. (mdpi.com)
  • Recently we demonstrated in a mouse model for allergic airway inflammation that particle-derived oxidative stress plays a crucial role during augmentation of allergen-induced lung inflammation by ultrafine carbon particle (UfCP) inhalation. (biomedcentral.com)
  • In sensitized and challenged mice UfCP exposure induced highest significant levels of all lipid mediators in the lungs together with the peak of allergic airway inflammation on day 7 after UfCP inhalation. (biomedcentral.com)
  • Inflammation induced a reduction in parvalbumin-positive interneuron density in the cortex, which was normalised with high-dose montelukast. (biomedcentral.com)
  • The effects of single or daily application of 0.1-100 µM curcumin on cell apoptosis in ultraviolet B (UVB)-induced mice were tested using an experimental double-blind posttest design with a control group and two research models: a single application of curcumin before a single UVB exposure and daily application of curcumin for 7 days before a single UVB exposure on the seventh day. (bvsalud.org)
  • In HL-60 leukaemia cells, di-GA activated caspase 3 and dose-dependently induced apoptosis. (nature.com)
  • These data show that di-GA exhibits three distinct anticancer activities: induction of apoptosis, cell-cycle arrest and disruption of cancer cell-induced lymphendothelial disintegration. (nature.com)
  • This proadifen-MTX synergism was also mediated by the inhibition of various cellular proteins engaged in apoptosis, including Mc-1, Bcl-xL, survivin and activation of procaspase-3. (spandidos-publications.com)
  • Conclusion: The results confirm that Tadalafil treatment restored all the biological markers to the normal and its involvement in mitochondrial mediated death apoptosis pathway along with inhibition of inflammatory markers. (sagepub.com)
  • Grape-related anti-tumoral activity encompasses a wide array of biological mechanisms and cellular targets, eventually leading to inhibition of cell growth and to enhanced apoptosis in several cancer cell lines, including lung, colon, breast, bladder, leukemia and prostate tumors. (oatext.com)
  • In the case of therapeutic options two and three by inducing lethal toxicity and thus killing the cancer cells, predominately via a form of programmed cell death termed apoptosis. (touchoncology.com)
  • Prostanoids, as they are known today, are a specific class of bioactive mediators generated via initial actions of cyclooxygenase. (jci.org)
  • 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)
  • In non-sensitized mice UfCP exposure induced a light non-significant increase of all lipid mediators. (biomedcentral.com)
  • Similarly but significantly in rat AM all lipid mediators were induced already within 1 h of UfCP stimulation. (biomedcentral.com)
  • The arachidonic acid, released by phospholipase A2, is an important substrate for the production of a group of lipid mediators known as leukotrienes, which induce proinflammatory signaling through the activation of specific BLT and CysLT receptors. (hindawi.com)
  • 2 The constitutive cyclooxygenase, COX-1, synthesizes prostaglandins necessary for normal gastrointestinal and renal function. (drugs.com)
  • Carprofen has also been shown to inhibit the release of several prostaglandins in two inflammatory cell systems: rat polymorphonuclear leukocytes (PMN) and human rheumatoid synovial cells, indicating inhibition of acute (PMN system) and chronic (synovial cell system) inflammatory reactions. (drugs.com)
  • The PTGS (COX) enzymes catalyze the conversion of arachidonic acid to prostaglandins in two steps. (wikipedia.org)
  • Leukotrienes and prostaglandins are involved in multiple physiological and pathophysiological events, and inhibition of their action is the molecular basis for the pharmacological activities of several important drugs. (vanderbilt.edu)
  • 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)
  • This article reviews the anti-inflammatory relative and anti-infectious effects of Evodia rutaecarpa and its major bioactive components and the involvement of the nitric oxide synthases, cyclooxygenase, NADPH oxidase, nuclear factor kappa B, hypoxia-inducible factor 1 alpha, reactive oxygen species, prostaglandins, tumor necrosis factor, LIGHT, amyloid protein and orexigenic neuropeptides. (biomedcentral.com)
  • Meanwhile, the inhibitory effect of AK106-001616 was more effective than that of naproxen in the mouse collagen antibody-induced arthritis model with leukotrienes contributing to the pathogenesis. (aspetjournals.org)
  • The tertiary and quaternary structures of PTGS1 (COX-1) and PTGS2 (COX-2) enzymes are almost identical. (wikipedia.org)
  • PTGS1 (COX-1) and PTGS2 (COX-2) are bifunctional enzymes that carry out two consecutive chemical reactions in spatially distinct but mechanistically coupled active sites. (wikipedia.org)
  • Increasing evidence suggests an involvement of COX and LOX enzymes in epileptic disorders. (j-epilepsy.org)
  • In order to effectively attenuate myocardial injury caused by hypoxic and inflammatory injury, we designed and synthesized a kind of anti-inflammatory compounds by coupling cyclooxygenase (COX) and carbonic anhydrase (CA) inhibitors, and evaluated the activity and their mechanism in vitro and in vivo. (bvsalud.org)
  • Hydrochloric acid (HCl) and carbonic anhydrase inhibitors may be used in some acute situations. (medscape.com)
  • For these, reasons both leukotriene synthesis inhibitors and leukotriene receptor antagonists have been suggested for inducing beneficial effects at different stages of the atherosclerosis process and may represent a new therapeutic target in the treatment of atherosclerotic vessel diseases, in particular in acute coronary syndrome. (hindawi.com)
  • The mechanism of action of Carprofen, like that of other NSAIDs, is believed to be associated with the inhibition of cyclooxygenase activity. (drugs.com)
  • As a class, cyclooxygenase inhibitory NSAIDs may be associated with gastrointestinal, renal and hepatic toxicity. (petsupplies4less.com)
  • PTGSs are targets for NSAIDs and PTGS2 (COX-2) specific inhibitors called coxibs. (wikipedia.org)
  • Foremost among these are non-steroidal anti-inflammatory drugs (NSAIDs) and cyclooxygenase-2 (COX-2) inhibitors. (vanderbilt.edu)
  • We tested this hypothesis by synthesizing a series of neutral derivatives of NSAIDs and demonstrating increases in selectivity for COX-2 of several orders of magnitude. (vanderbilt.edu)
  • A correlation was seen among bortezomib dose, proteasome inhibition, and positive modulation of serum prostate-specific antigen. (aacrjournals.org)
  • 2008). Clinical imatinib mesylate treatment induces early normalisation of aberrant neutrophil leukotriene C4 synthase expression and activity in chronic myeloid leukaemia. (findmedarticle.com)
  • Furthermore, di-GA inhibited the generation of lymphendothelial gaps by cancer cell spheroid-secreted lipoxygenase metabolites. (nature.com)
  • The results of the present study indicate that protective effects of zafirlukast and valdecoxib are achieved through the blockade of release of LOX and COX metabolites therefore, representing a new therapeutic target for treating AD and other neurodegenerative disorders. (afpm.org.my)
  • The symptoms of NSAID-induced reactions are hypersensitivity reactions rather than allergic reactions that trigger other allergen-induced asthma, rhinitis, or hives. (wikipedia.org)
  • Inhibition of COX-1 is thought to be associated with gastrointestinal and renal toxicity while inhibition of COX-2 provides anti-inflammatory activity. (drugs.com)
  • 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)
  • stitute of 11 distinct gene families, which initiate the Carcinogenesis was induced by single tail vein injection of st sequential lcleavage of cyclic adenosine monophosphate MNU on day 1 in each animal. (sagepub.com)
  • Similar to COX-2, 5-LO is expected to be a promising target for molecular targeted cancer therapy because 5-LO has been identified as being related to carcinogenesis due to its ability to promote cell proliferation and angiogenesis [ 17 - 19 ]. (biomedcentral.com)
  • Furthermore, using sequence analysis of human genomic DNA, researchers concluded that the amino acids important for catalysis by COX-1 are conserved and are equally important for catalysis by COX-2. (medscape.com)
  • Figure 2) While metabolizing arachidonic acid primarily to PGG2, COX-2 also converts this fatty acid to small amounts of a racemic mixture of 15-Hydroxyicosatetraenoic acids (i.e., 15-HETEs) composed of ~22% 15(R)-HETE and ~78% 15(S)-HETE stereoisomers as well as a small amount of 11(R)-HETE. (wikipedia.org)
  • 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)
  • Biological in vitro assays demonstrated that several of the synthesized compounds possess pronounced inhibitory activities against HDAC and COX isoforms. (bvsalud.org)
  • Chemotherapy in particular is also frequently associated with significant side effects, which are often perceived by patients as worse than the actual disease, and have in the past led to the termination of treatment, particularly in under-aged patients.16 However, even with treatment success, long-term adverse effects and treatment-induced secondary cancers are, with extended life expectancies, also becoming increasingly a problem. (touchoncology.com)
  • By inhibiting the activity of overexpressed CA under hypoxia, the acidic microenvironment can be regulated to inhibit the hypoxic injury, in which the pH-dependent primary drug resistance can be overcome to improve the anti-inflammatory effect of the COX inhibitor. (bvsalud.org)
  • Volatile oils from Centipeda have been shown to modulate anti-inflammatory action by inhibition of pro-inflammatory cytokines in rat model. (pureprescriptions.com)
  • We are exploiting this discovery to prepare novel COX-2 inhibitors as anti-inflammatory drugs and cancer preventive agents. (vanderbilt.edu)
  • New anti-inflammatory agents possessing dual cyclooxygenase/lipoxygenase (COX/LOX) inhibition were discovered by PASS prediction of biological activity for 573 virtually designed chemical compounds. (way2drug.com)
  • Eight tested compounds exhibited anti-inflammatory activity in the carrageenan-induced paw edema. (way2drug.com)
  • Genetic ablation and pharmacological inhibition of NLRP3 inflammasome dampen inflammatory responses to particulates. (cdc.gov)
  • Preexposure of neutrophils for 15-30 min to 1-10 micrograms/ml PUFA reduced the random and chemotactic migration to both FMLP- and fungi-activated complement. (jci.org)
  • For example, we recently reported the identification of a critical H-bonding interaction that leads to the selectivity of aspirin for acetylation of Ser-530 in COX-2. (vanderbilt.edu)
  • The membrane permeability and inhibition of cellular HDAC activity of selected compounds were confirmed by whole-cell HDAC inhibition assays and immunoblot experiments. (bvsalud.org)
  • In contrast to previous reports, the simultaneous inhibition of HDAC and COX activity by dual HDAC-COX inhibitors or combination treatments with vorinostat and celecoxib did not result in additive or synergistic anticancer activities. (bvsalud.org)
  • In addition, this compound consistently modulated the production of leukotriene C(4), demonstrating the ability to modulate both cyclooxygenase-2 and 5-lipoxygenase activity. (pureprescriptions.com)
  • Digalloyl-resveratrol (di-GA) is a synthetic compound aimed to combine the biological effects of the plant polyhydroxy phenols gallic acid and resveratrol, which are both radical scavengers and cyclooxygenase inhibitors exhibiting anticancer activity. (nature.com)
  • It further inhibited cell-cycle progression in the G1 phase by four different mechanisms: rapid downregulation of cyclin D1, induction of Chk2 with simultaneous downregulation of Cdc25A, induction of the Cdk-inhibitor p21 Cip/Waf and inhibition of ribonucleotide reductase activity resulting in reduced dCTP and dTTP levels. (nature.com)
  • We show for the first time that proadifen is able to enhance the cytotoxic properties of MTX in cBCRP cells, particularly through the inhibition of BCRP expression and activity. (spandidos-publications.com)
  • We examined not just the effect of proadifen and MTX on the expression of BCRP, but we were also interested in other molecular mechanisms involved in the possible antitumour activity of proadifen alone and in combination with MTX, such as the expression of anti-apoptotic proteins, proteins involved in the regulation of BCRP and proteins involved in the reparation of chemotherapeutic drug-induced DNA damage. (spandidos-publications.com)
  • Assessment of in vivo 5-lipoxygenase activity by analysis of leukotriene B4 in saliva: effects of treatment with zileuton. (findmedarticle.com)
  • Several computer programs were used for prediction of the biological activity of 29 compounds concerning CYP1A2, 2C9, and 3A4 inhibition. (way2drug.com)
  • 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)
  • It is also shown that PUFA decrease the FMLP-induced Ca2+ mobilization. (jci.org)
  • First, hydrogen is abstracted from carbon 13 of arachidonic acid, and then two molecules of oxygen are added by the PTGS2 (COX-2), giving PGG2. (wikipedia.org)
  • This includes lipoxygenases, which incorporate one molecule of O2 into the carbon framework and cyclooxygenases, which incorporate two molecules of O2. (vanderbilt.edu)
  • It was demonstrated that intraperitoneal administration of BHMC (0.03, 0.1, 0.3 and 1.0mg/kg) exhibited dose-dependent inhibition of chronic constriction injury-induced neuropathic pain in mice, when evaluated using Randall-Selitto mechanical analgesiometer. (afpm.org.my)
  • Administration of zafirlukast (15 and 30mg/kg), and valdecoxib (5 and 10mg/kg) significantly improved the behavioral performances and showed significant reversal of mito-oxidative damage declining the neuroinflammation in β-A1-42 oligomer treated rats. (afpm.org.my)
  • The specificity of a particular NSAID for COX-2 versus COX-1 may vary from species to species. (drugs.com)
  • COX-2 is naturally inhibited by calcitriol (the active form of Vitamin D). Both the peroxidase and PTGS activities are inactivated during catalysis by mechanism-based, first-order processes, which means that PGHS-2 peroxidase or PTGS activities fall to zero within 1-2 minutes, even in the presence of sufficient substrates. (wikipedia.org)
  • BMC Cancer (2019) 19:996 Page 2 of 15 PDE-5, PDE-6, PDE-9 are the predominant active iso- Sciences, Naini Allahabad, India. (sagepub.com)
  • Vascular endothelium is an active endocrine, paracrine, and autocrine organ, indispensable for the maintenance of vascular homeostasis [ 15 ]. (hindawi.com)
  • Evidence suggests that COX-1 and COX-2 are similar in structure and function but that they exist as 2 distinct enzymatic entities. (medscape.com)
  • Staphylococcal enterotoxin B (SEB) is one of at least 15 antigenically distinct enterotoxin proteins ( 3 , 4 ). (cdc.gov)
  • 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)
  • Effects of 5-lipoxygenase inhibitor zileuton on airway responses to inhaled swine house dust in healthy subjects. (findmedarticle.com)
  • 15 Our only available responses to treatment failure are altering the treatment and increasing the dosage until the maximal tolerable dose is reached. (touchoncology.com)
  • The most promising dual inhibitors, C3 and C4, evoked antiproliferative effects in the low micromolar concentration range and caused a significant increase in apoptotic cells. (bvsalud.org)
  • [ 1 ] Thus, tracing research of the COX pathway is essential to an understanding of COX deficiency, and examining the variable effects of COX inhibition are advantageous. (medscape.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)
  • These anti-proliferative effects seemed to be mediated in a cannabinoid receptor-independent manner, since the antagonist of cannabinoid receptor-1 (CB1) and vanilloid receptor-1 (VR1), two endocannabinoid receptors, did not reverse the ability of DHEA and NALA to induce cell death. (biomedcentral.com)
  • From these findings, we suggest that ROS production induced by the 5-LO pathway mediates the anti-cancer effects of DHEA and NALA on HNSCC cells. (biomedcentral.com)
  • Since both histone deacetylases (HDACs) and cyclooxygenase-2 (COX-2) are known to be overexpressed in several cancer types, we herein report the design, synthesis, and biological evaluation of a library of dual HDAC-COX inhibitors. (bvsalud.org)
  • The two 15-HETE stereoisomers have intrinsic biological activities but, perhaps more importantly, can be further metabolized to a major class of agents, the lipoxins. (wikipedia.org)
  • 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)
  • Taken together, the present study demonstrated that the systemic administration of BHMC attenuated chronic constriction, injury-induced neuropathic pain. (afpm.org.my)