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841 Trials |  |
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- | Journal: Two new phenolic compounds and some biological activities of Scorzonera pygmaea Sibth. & Sm. subaerial parts. (Pubmed Central) - Apr 12, 2020
COX inhibition test was used to evaluate the anti-inflammatory activity and all the fractions showed low inhibition in comparison with indomethacin. [Formula: see text].
- | Lacromid (bezafibrate) / Remedica
Journal: PPARα ligand, AVE8134, and cyclooxygenase inhibitor therapy synergistically suppress lung cancer growth and metastasis. (Pubmed Central) - Apr 12, 2020
In this study, we found that the degrees of inhibition on LC growth and metastasis by PPARα ligands depended on their bidirectional regulation on EETs and 11-HETE. Considering their safety and efficacy, the novel PPARα ligand, AVE8134, is a potentially ideal anti-angiogenesis drug for cancer treatment when jointly applied with the COX inhibitor indomethacin.
- | Preclinical, Journal: High salt intake shifts the mechanisms of flow-induced dilation in the middle cerebral arteries of Sprague-Dawley rats. (Pubmed Central) - Apr 10, 2020
These results suggest that HS intake impairs FID and changes FID mechanisms to entirely NO-dependent, in contrast to the LS group where FID is NO, prostanoid and epoxyeicosatrienoic acids (EET's) dependent. Those changes were accompanied by increased lipid peroxidation products in the plasma of HS-fed rats, increased vascular superoxide/reactive oxygen species levels and decreased NO levels; together with increased expression of HIF-1α and VEGF.
- | Journal: Cyclooxygenase inhibition does not impact the pressor response during static or dynamic mechanoreflex activation in healthy decerebrate rats. (Pubmed Central) - Apr 10, 2020
We found that indomethacin had no effect (p>0.05, n=9) on the pressor or cardioaccelerator responses during 30 seconds of either static or dynamic stretch. We conclude that, despite skeletal muscle stretch-induced reductions in blood flow and the possibility of increased COX metabolite concentration, COX metabolites do not activate or sensitize thin fiber muscle afferents stimulated during 30 seconds of static or dynamic mechanoreflex activation in healthy rats.
- | Preclinical, Journal: Investigation of the mechanisms of cyclooxygenase-mediated mechanoreflex sensitization in a rat model of simulated peripheral artery disease. (Pubmed Central) - Apr 10, 2020
Femoral artery ligation had no effect on skeletal muscle COX protein expression or activity, or concentration of the COX metabolite prostaglandin E. Conversely, femoral artery ligation increased expression of the COX metabolite receptors endoperoxide 4 and thromboxane A-R in dorsal root ganglia tissue. We conclude that, in ligated rats, the COX pathway sensitizes the peripheral endings of mechanoreflex afferents which occurs principally as a result of increased expression of COX metabolite receptors.
- | aspirin / Generic mfg.
Journal: Pharmaco-Genetic Screen To Uncover Actin Regulators Targeted by Prostaglandins During Drosophila Oogenesis. (Pubmed Central) - Apr 10, 2020
Here we describe a pharmaco-genetic interaction screen that takes advantage of the fact that Stage 10B follicles will mature in culture and COX inhibitors, such as aspirin, block this in vitro follicle maturation...Here we present the screen results and initial follow-up studies on three strong enhancers - Enabled, Capping protein, and non-muscle Myosin II Regulatory Light Chain. Overall, these studies provide new insight into how PGs regulate both actin bundle formation and cellular contraction, properties that are not only essential for development, but are misregulated in disease.
- | Journal: Enteric neuroplasticity and dysmotility in inflammatory disease: key players and possible therapeutic targets. (Pubmed Central) - Apr 10, 2020
Other cells implicated in inflammation-induced neuroplasticity include muscularis macrophages and enteric glia. Targeted treatments that are discussed include 5-HT agonists, cyclooxygenase inhibitors, antioxidants, B cell depletion therapy, and activation of anti-inflammatory pathways.
- | Journal: Synthesis and Cyclooxygenase Inhibition of Sulfonamide-Substituted (Dihydro)Pyrrolo[3,2,1-hi]indoles and Their Potential Prodrugs. (Pubmed Central) - Apr 10, 2020
The N-propionamide-substituted analogs showed a significantly decreased lipophilicity and, as expected, lower or no COX-inhibition potency. Hence, the N-(sulfonyl)propionamides can be regarded as potential prodrugs, which represents a potential approach for more sophisticated radiotracer developments.
- | quercetin (LY294002) / Eli Lilly
Journal, IO Biomarker: The Role of the LY294002 - A Non-Selective Inhibitor of Phosphatidylinositol 3-Kinase (PI3K) Pathway- in Cell Survival and Proliferation in Cell Line SCC-25. (Pubmed Central) - Apr 10, 2020
Our results demonstrated that activation of the PI3K/AKT pathway is directly related to members of the Bcl-2 family and GLUT1, but not the inflammatory mediators COX1 and COX2. Our data suggest that the PI3K/AKT pathway is related to cell survival and proliferation in oral squamous cell carcinoma through its interaction with Bcl-2 family members..
- | Journal: Suppression of inflammatory mediators and matrix metalloproteinase (MMP)-13 by Morus alba stem extract and oxyresveratrol in RAW 264.7 cells and C28/I2 human chondrocytes. (Pubmed Central) - Apr 9, 2020
The MSE demonstrates the potential to be used as an alternative treatment for reducing inflammation and preventing cartilage degradation. Its component, oxyresveratrol, may exert these effects to some extent.
- | Journal: Cyclooxygenase-2 as a Biomarker with Diagnostic, Therapeutic, Prognostic, and Predictive Relevance in Small Animal Oncology. (Pubmed Central) - Apr 9, 2020
It is also overexpressed in humans presenting various types of tumours and in selected types of tumours in animals, particularly in dogs. This article discusses the expression of COX-2 in canine and feline tumours, the importance of COX-2 as a biomarker with diagnostic, therapeutic, prognostic and predictive relevance in oncology, and the clinical significance of inhibiting COX-2 overexpression in tumours.
- | celecoxib oral / Generic mfg.
Journal: Synthesis and biological evaluation of 2-(4-methylsulfonyl phenyl) indole derivatives: multi-target compounds with dual antimicrobial and anti-inflammatory activities. (Pubmed Central) - Apr 9, 2020
Compounds 9a-c were found to release moderate amounts of NO to decrease the side effects associated with selective COX-2 inhibitors. A molecular modeling study for compounds 7b, 7h, and 7i into COX-2 active site was correlated with the results of in vitro COX-2 inhibition assays.
- || Clinical, Journal: Prescription of pain medication among older cancer patients with and without an intellectual disability: a national register study. (Pubmed Central) - Apr 4, 2020
In the studied cohort of older people surviving or living with cancer, prescriptions for pain-treatment was less common in patients with ID compared to the general population. These results may suggest that pain is not sufficiently treated among cancer patients with ID, a situation that most likely would compromise the quality of life in this group.
- | Journal, IO Biomarker: Ellagitannins from Punica granatum leaves suppress microsomal prostaglandin E synthase-1 expression and induce lung cancer cells to undergo apoptosis. (Pubmed Central) - Apr 3, 2020
The ellagitannins also down-regulated tumor necrosis factor α, inducible nitric oxide synthase, and anti-apoptotic factor B-cell chronic lymphocytic leukemia/lymphoma 2, and induced A549 cells to undergo apoptosis. These findings indicate that the ellagitannins have anti-inflammatory and anti-carcinogenic effects, due to their specific suppression of mPGES-1.Abbreviations: Bcl-2: B-cell chronic lymphocytic leukemia/lymphoma 2; COX: cyclooxygenase; CRE: cAMP response element; DHHDP: dehydrohexahydroxydiphenoyl; EtO: diethyl ether; EtOAc: ethyl acetate; GAPDH: glyceraldehyde 3-phosphate dehydrogenase; iNOS: inducible nitric oxide synthase; mPGES-1: microsomal prostaglandin E synthase-1; n-BuOH: water-saturated n-butanol; NSAIDs: non-steroidal anti-inflammatory drugs; NF-κB: nuclear factor-κB; PG: prostaglandin; TNF: tumor necrosis factor; TUNEL: terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling.
- | allopurinol / Generic mfg.
Journal: Anti-Inflammatory and Anti-Hyperuricemic Functions of Two Synthetic Hybrid Drugs with Dual Biological Active Sites. (Pubmed Central) - Apr 1, 2020
The present study aimed to test the anti-inflammatory and xanthine oxidase inhibitory activities of two synthesized molecules and compare them to routinely prescribed nonsteroidal anti-inflammatory drugs (NSAIDs), such as diclofenac and the serum urate-lowering drug, allopurinol...In addition, the tested compounds markedly decreased paw swelling, mobilization of inflammatory cells, iNOS-, and NF-κB-immunoreactive cells in a mouse model of paw edema. Interestingly, both compounds were potent xanthine oxidase inhibitors as well as Cox inhibitors with higher activity in favor of compound B providing potential dual acting series of anti-hyperuricemic and anti-inflammatory therapeutic agents.
- | nitroprusside / Generic mfg.
Journal: Sulodexide Promotes Arterial Relaxation via Endothelium-Dependent Nitric Oxide-Mediated Pathway. (Pubmed Central) - Mar 31, 2020
SDX did not affect aortic or mesenteric artery endothelium-independent relaxation to the NO donor sodium-nitroprusside. Thus, SDX promotes arterial relaxation via a mechanism involving endothelium-dependent NO production; an effect that could enhance vasodilation and decrease vasoconstriction in vascular disorders.
- || Clinical, Observational data, Journal: The utility/futility of medications for neuropathic pain - an observational study. (Pubmed Central) - Mar 29, 2020
Patients probably differ in many respects from those subjects in clinical trials. This is not to negate the use of recommended medications for NP but an indication that success rates of treatment are likely to be worse than the data coming from those trials published by the pharmaceutical industry.
- | furosemide / Generic mfg., Alverix (amiloride hydrochloride) / Remedica
Preclinical, Journal: Effects of myricetin-3-O-α-rhamnoside (myricitrin) treatment on urinary parameters of Wistar rats. (Pubmed Central) - Mar 29, 2020
This is not to negate the use of recommended medications for NP but an indication that success rates of treatment are likely to be worse than the data coming from those trials published by the pharmaceutical industry. Taking together, although the results of this study point to the diuretic potential of myricitrin, the reduction in urinary Cl and excretion should be considered in future approaches, as well as for therapeutic applicability.
- || Review, Journal: Brief Story on Prostaglandins, Inhibitors of their Synthesis, Hematopoiesis, and Acute Radiation Syndrome. (Pubmed Central) - Mar 29, 2020
Progress in these efforts was obtained after discovery of selective inhibitors of inducible selective cyclooxygenase-2 (COX-2) inhibitors. Recent studies have been able to suggest the possibility to find combined therapeutical approaches utilizing joint administration of prostaglandins and inhibitors of their synthesis at optimized timing and dosing of the drugs which could be incorporated into the therapy of patients with acute radiation syndrome.
- furosemide / Generic mfg.
NSAID-induced hyperkalemia despite normal renal function () - Mar 27, 2020 - Abstract #NKFCSM2020NKF_CSM_38;
The opioid crisis has led to the liberal use of NSAIDS for managing pain. This unique case demonstrates the risks associated with this therapeutic trend in patients even with an otherwise low chance of renal, cardiovascular, or electrolyte abnormalities.
- | Preclinical, Journal: The mechanism of Tyk2 deficiency-induced immunosuppression in mice involves robust IL-10 production in macrophages. (Pubmed Central) - Mar 26, 2020
Tyk2 KO macrophages showed an enhanced CREB phosphorylation induced by P. acnes plus PGE. Taken together, these results showed that Tyk2 deficiency potentiates the PGE-protein kinase A-IL-10 pathway in macrophages, and thereby contributes to potentiation of the immunosuppressive phenotype.
- || aspirin / Generic mfg.
Clinical, Journal: Effects of Aspirin on Growth Factor Release From Freshly Isolated Leukocyte-Rich Platelet-Rich Plasma in Healthy Men: A Prospective Fixed-Sequence Controlled Laboratory Study. (Pubmed Central) - Mar 24, 2020
Reduction in growth factor release attributed to daily use of low-dose ASA or other COX inhibitors can be mitigated when PRP samples are activated with TBN. Clinical studies are needed to determine whether activation before PRP injection is needed in all applications where ASA is in use and to what extent ASA may inhibit growth factor release in vivo at the site of injury.
- | Journal: The protein tyrosine phosphatase PTPN7 is a negative regulator of ERK activation and thromboxane generation in platelets. (Pubmed Central) - Mar 24, 2020
Although bleeding times did not significantly differ between PTPN7-null and WT mice, time to death was significantly faster in PTPN7-null mice than in WT mice in a pulmonary thromboembolism model. We conclude that PTPN7 regulates platelet functional responses downstream of GPCR agonists, but not GPVI agonists, through inhibition of ERK activation and thromboxane generation.
- | glibenclamide / Generic mfg.
Preclinical, Journal: Relaxation Effect of Patchouli Alcohol in Rat Corpus Cavernous and Its Underlying Mechanisms. (Pubmed Central) - Mar 21, 2020
The relaxant response to PA was not influenced by tetrodotoxin and atropine while it was significantly inhibited by removal of endothelium...The treatment of endothelium-deprived corpus cavernosum with several potassium channel blockers including tetraethylammonium (TEA), 4-aminopyridine (4-AP), and glibenclamide had no effect on PA-induced relaxation...Also, PA improved relaxant capacity of sildenafil in rat corpus cavernosum...In conclusion, PA relaxed the rat corpus cavernosum attributed to both endothelium-dependent and -independent properties. While the former component was mostly involved in nitric oxide signaling pathway, the endothelium-independent mechanism involved in PA-induced relaxation was probably linked to calcium antagonism.
- | ibuprofen / Generic mfg.
Journal: The COX-2/PGE pathway suppresses apical elimination of RasV12-transformed cells from epithelia. (Pubmed Central) - Mar 21, 2020
Moreover, caerulein-induced chronic inflammation substantially suppresses apical elimination of RasV12 cells. These results indicate that intrinsically or extrinsically mediated inflammation can promote tumour initiation by diminishing cell competition between normal and transformed cells.
- | Journal: Fluorination as tool to improve bioanalytical sensitivity and COX-2-selective antitumor activity of cobalt alkyne complexes. (Pubmed Central) - Mar 19, 2020
The higher quantification of fluorine by HR CS MAS makes this method about 5-fold more sensitive than HR CS AAS measuring cobalt. As a further positive result, 3/4/5/6-Co-ASS demonstrated high selectivity to tumor cells due to lack of antimetabolic activity against the non-tumorigenic bone marrow stromal cell line HS-5.
- | ibuprofen / Generic mfg.
Preclinical, Journal: Nonsteroidal anti-inflammatory drugs and acetaminophen ameliorate muscular mechanical hyperalgesia developed after lengthening contractions via cyclooxygenase-2 independent mechanisms in rats. (Pubmed Central) - Mar 19, 2020
In contrast, acetylsalicylic acid, ibuprofen, loxoprofen sodium, and acetaminophen increased the withdrawal threshold, which had decreased by lengthening contractions, in a dose-dependent manner. These results demonstrate the analgesic actions of nonsteroidal anti-inflammatory drugs and acetaminophen in the maintenance process of lengthening contraction-induced muscular mechanical hyperalgesia, which may occur through cyclooxygenase-2 independent mechanisms.
- | Preclinical, Journal: Impaired Fluid Intake, but Not Sodium Appetite, in Aged Rats Is Mediated by the Cyclooxygenase-Prostaglandin E Pathway. (Pubmed Central) - Mar 19, 2020
These data indicate that the reduced fluid intake that occurs in aging is due to increased COX-PGE-mediated inflammation. However, the reduced sodium intake in these animals appears to occur via an alternate mechanism.
- | aspirin / Generic mfg.
Journal: Cyclooxygenase 1 mediates IL-33-induced extracellular signal regulated kinase activation in mast cells; Implications for aspirin sensitivity. (Pubmed Central) - Mar 18, 2020
However, the reduced sodium intake in these animals appears to occur via an alternate mechanism. MC-intrinsic COX-1 amplifies IL-33-induced activation in the setting of innate type 2 immunity, and may help explain the phenomenon of therapeutic desensitization to aspirin by nonselective COX inhibitors in AERD.
- Human Rhinovirus Infection of Primary Bronchial Epithelial Cells Upregulates Prostaglandin E2 Production That Attenuates Transforming Growth Factor Beta-1-Induced Fibroblast-to-Myofibroblast Transition (PENNSYLVANIA CONVENTION CENTER, Room 126 A-B (100 Level)) - Mar 15, 2020 - Abstract #ATS2020ATS_3506;
Lack of FMT-stimulation by HRV may be because HBEC and HBF were from healthy donors who did not display airway remodeling when infected in vivo with HRV. Future studies using HBEC and HBF from asthmatic individuals are planned to determine if a different pattern is observed.
- lorazepam / Generic mfg.
Chronic Lorazepam-Induced Pro-Relaxant Signaling in ASM Cells Is Cyclooxygenase Dependent (PENNSYLVANIA CONVENTION CENTER, Room 204 A-B (200 Level)) - Mar 15, 2020 - Abstract #ATS2020ATS_2581;
Chronic, but not necessarily acute, treatment of human ASM cells with lorazepam activates both COX-1 and COX-2-mediated pathway. Future studies will be aimed at examining downstream synthesis of prostaglandin E2 and the role of E-type prostanoid receptor subtypes in mediating lorazepam-induced pro-relaxant signals in ASM cells.
- | etodolac / Generic mfg.
Journal: Fingerprinting, Antimicrobial, Antioxidant, Anticancer, Cyclooxygenase and Metabolic Enzymes Inhibitory Characteristic Evaluations of Stachys viticina Boiss. Essential Oil. (Pubmed Central) - Mar 14, 2020
Moreover, the S. viticina EO showed high cyclooxygenase inhibitory activity against COX-1 and COX-2 with IC values of 0.25 and 0.5 µg/mL, respectively, similar to those of the positive control (the NSAID etodolac). Outcomes amassed from this investigation illustrate that S. viticina EO represents a rich source of pharmacologically active molecules which can be further validated and explored clinically for its therapeutic potential and for the development and design of new natural therapeutic preparations.
- | quercetin (LY294002) / Eli Lilly
Preclinical, Journal: Shenfu Injection Promotes Vasodilation by Enhancing eNOS Activity Through the PI3K/Akt Signaling Pathway In Vitro. (Pubmed Central) - Mar 13, 2020
Furthermore, it promoted the expression of total eNOS and the phosphorylation of eNOS at serine (Ser) 1177 but inhibited the phosphorylation at threonine (Thr) 495, which was significantly reversed by PI3K-specific inhibitor LY294002. In conclusion, our study showed the vasodilation effect of SFI in thoracic aorta is mediated entirely by enhancing eNOS activity through the PI3K/Akt signaling pathway, providing novel knowledge on the effect of SFI on shock and HF for future clinical applications.
- | glibenclamide / Generic mfg.
Journal: Vasorelaxing Activity of R-(-)-3'-Hydroxy-2,4,5-trimethoxydalbergiquinol from Dalbergia tonkinensis: Involvement of Smooth Muscle CaV1.2 Channels. (Pubmed Central) - Mar 8, 2020
R-(-)-3'-Hydroxy-2,4,5-trimethoxydalbergiquinol-induced vasorelaxation was antagonized by (S)-(-)-Bay K 8644 and unaffected by tetraethylammonium plus glibenclamide...R-(-)-3'-Hydroxy-2,4,5-trimethoxydalbergiquinol likely stabilized the channel in its closed state, as suggested by molecular modelling and docking simulation to the Ca1.2 channel α subunit. In conclusion, D. tonkinensis species may represent a source of agents potentially useful for the development of novel antihypertensive drugs.
- imrecoxib (BAP 909) / Jiangsu Hengrui Medicine, celecoxib oral / Generic mfg.
[VIRTUAL] EFFICACY AND SAFETY OF IMRECOXIB, CELECOXIB AND DICLOFENAC IN PATIENTS WITH OSTEOARTHRITIS- A NETWORK META-ANALYSIS () - Mar 8, 2020 - Abstract #ISPOR2020ISPOR_1902;
Since there were sparse RCTs have been reported for imrecoxib, the conclusion should be adopted with caution. Meanwhile, a nocebo effect was observed in the analysis of the rate of adverse events, which need further discussion.
- | ibuprofen / Generic mfg.
Journal: Synthesis, chemical characterization and DNA interaction study of new diclofenac and ibuprofen zinc (II)-nicotinamide ternary complexes as cyclooxygenase inhibitor prototypes. (Pubmed Central) - Mar 3, 2020
Thus, two new compounds were synthesized, characterized and had their previous toxicities determined. These compounds are promising new drugs, with the next step being evaluations of their activity.
- | Journal: Anti-inflammatory and antiproliferative compounds from Sphaeranthus africanus. (Pubmed Central) - Mar 2, 2020
For the first-time, the diastereomeric carvotacetones (6-7) were isolated as separate compounds, and their anti-proliferative activity was determined. Selective COX-2 inhibitory, COX-2 mRNA expression and NO production inhibitory activities by some of the major constituents of S. africanus supports the traditional medical application of this plant for the treatment of inflammation-related disorders.
- | glibenclamide / Generic mfg.
Preclinical, Journal: Marjoram Relaxes Rat Thoracic Aorta Via a PI3-K/eNOS/cGMP Pathway. (Pubmed Central) - Feb 26, 2020
Blockers of ATP-sensitive or Ca2+-activated potassium channels such as glibenclamide or tetraethylamonium (TEA), respectively, did not significantly affect OME-induced relaxation...Our findings further support the medicinal value of marjoram and provide a basis for its beneficial intake. Although consuming marjoram may have an antihypertensive effect, further studies are needed to better determine its effects in different vascular beds.
- | Review, Journal: Prostaglandin-cytokine crosstalk in chronic inflammation. (Pubmed Central) - Feb 25, 2020
In addition, PGs are also involved in tissue remodelling such as fibrosis and angiogenesis. In this article, we review these findings and discuss their relevance to human diseases.
- | cisplatin / Generic mfg.
Journal: Synthesis and evaluation of bi-functional 7-hydroxycoumarin platinum(IV) complexes as antitumor agents. (Pubmed Central) - Feb 24, 2020
The incorporation of 7-hydroxycoumarin leads to significantly enhanced platinum accumulation in both whole tumor cells and DNA. The HSA interaction investigation reveals that the tested coumarin platinum(IV) compound could effectively combine with HSA via van der Waals force and hydrogen bond.
- | aspirin / Generic mfg.
Retrospective data, Journal: Association of Aspirin Use With Postoperative Hematoma and Bleeding Complications in Foot and Ankle Surgery: A Retrospective Study. (Pubmed Central) - Feb 24, 2020
Postoperative hematomas were evacuated in the clinic under sterile conditions and healed by secondary intention. Perioperative aspirin use appears to be safe and effective in foot and ankle surgery, and patients taking aspirin had good surgical outcomes with minimal postoperative complications.
- | Journal: Evaluation of the neurotoxic effects of intrathecal administration of (S)-(+)-Ketoprofen on rat spinal cords: randomized controlled experimental study (Pubmed Central) - Feb 21, 2020
Perioperative aspirin use appears to be safe and effective in foot and ankle surgery, and patients taking aspirin had good surgical outcomes with minimal postoperative complications. Intrathecal (S)-(+)-Ketoprofen caused dose-dependent neurohistopathological changes in rats on days 3 and 7 after injection, suggesting that (S)-(+)-Ketoprofen should not be intrathecally administered.
- | Journal: Optimization of pyrrolizine-based Schiff bases with 4-thiazolidinone motif: Design, synthesis and investigation of cytotoxicity and anti-inflammatory potency. (Pubmed Central) - Feb 21, 2020
Additionally, compounds 12, 19 and 22 also exhibited higher affinity for CDK2 than CAN508. To sum up, the above-mentioned data highlight these compounds as promising anti-inflammatory and anticancer agents.
- | Journal: The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors. (Pubmed Central) - Feb 20, 2020
A systematic substitution of the amine moiety of 1d, utilizing structural information and array chemistry, with modifications to improve inhibitor stability, resulted in the identification of the 300-fold more active H-PGDS inhibitor tool compound 1bv (IC = 9.9 nM, LE = 0.42). This selective inhibitor exhibited good murine pharmacokinetics, dose-dependently attenuated PGD production in a mast cell degranulation assay and should be suitable to further explore H-PGDS biology.
- | Journal: Inflammation-linked adaptations in dermal microvascular reactivity accompany the development of obesity and type 2 diabetes. (Pubmed Central) - Feb 16, 2020
We demonstrate that the development of obesity, metabolic dysfunction and type 2 diabetes, in HCD-fed mice, is accompanied by increased dermal adiposity and associated metaflammation in dWAT. Importantly, these temporal changes are also linked to disease stage-specific dermal microvascular reactivity, which may reflect adaptive mechanisms driven by metaflammation.
- | Journal: Antibacterial, anti-inflammatory and peroxidase-mediated cyclooxygenase-1 inhibitory properties of Fusarium solani extract. (Pubmed Central) - Feb 16, 2020
This study design can be adapted in soil fungi metabolomic investigations. We report for the first time the potent anti-inflammatory property of the ethyl acetate extract of soil strain of F. solani with a possible mechanism of action that involves the inhibition of COX enzyme.
- | celecoxib oral / Generic mfg.
Journal: Altered cyclooxygenase-1 and enhanced thromboxane receptor activities underlie attenuated endothelial dilatory capacity of omental arteries in obesity. (Pubmed Central) - Feb 15, 2020
We report for the first time the potent anti-inflammatory property of the ethyl acetate extract of soil strain of F. solani with a possible mechanism of action that involves the inhibition of COX enzyme. The results show that the depot-specific reduction in endothelial dilatory capacity of omental compared with subcutaneous arteries in obesity is in large part due to altered cyclooxygenase-1 and enhanced thromboxane receptor activities, which cause EDHF deficiency.
- | Journal: Fluorescent indomethacin-dansyl conjugates utilize the membrane-binding domain of cyclooxygenase-2 to block the opening to the active site. (Pubmed Central) - Feb 14, 2020
Inhibition kinetics of compound 2were similar to those of the indomethacin parent compound against wild-type COX-2, and the R120A substitution reduced the time dependency of COX inhibition. These results provide a structural basis for the further design and optimization of conjugated COX reagents for imaging of malignant or inflammatory tissues containing high COX-2 levels.
- | methotrexate / Generic mfg.
Journal: Accelerated Atherosclerosis in Rheumatoid Arthritis: Mechanisms and Treatment. (Pubmed Central) - Feb 14, 2020
These results provide a structural basis for the further design and optimization of conjugated COX reagents for imaging of malignant or inflammatory tissues containing high COX-2 levels. Greater understanding of the pharmacologic activity of RA treatments on the atherosclerotic process may lead to improved care, addressing both damage to the joints and damage to the heart.
- | ibuprofen / Generic mfg.
Journal: Vascular endothelial growth factor polymorphism rs2010963 status does not affect patent ductus arteriosus incidence or cyclooxygenase inhibitor treatment success in preterm infants. (Pubmed Central) - Feb 14, 2020
Our results indicate that there is no association between vascular endothelial growth factor polymorphism rs2010963 status and the occurrence of patent ductus arteriosus or the response to cyclooxygenase inhibitor treatment in a large cohort of preterm infants. Additional studies are needed to determine the role of genetic factors on patent ductus arteriosus incidence and treatment response.