- |||||||||| indomethacin / Generic mfg.
Journal, IO biomarker: Systemic Nos2 Depletion and Cox inhibition limits TNBC disease progression and alters lymphoid cell spatial orientation and density. (Pubmed Central) - Nov 15, 2022 Consistent with a causative relationship between these observations, pharmacological inhibition of COX2 with indomethacin dramatically reduced tumor growth of the 4T1 model of TNBC in both WT and Nos2 mice...These findings are consistent with our observations in low NOS2/COX2 expressing breast tumors proving that COX2 activity is responsible for limiting the spatial distribution of effector T cells in TNBC. Together these results suggest that clinically available NSAID's may provide a cost-effective, novel immunotherapeutic approach for treatment of aggressive tumors including triple negative breast cancer.
- |||||||||| meloxicam / Generic mfg., celecoxib oral / Generic mfg.
Journal: Discovery of novel pyrazole and pyrazolo[1,5-a]pyrimidine derivatives as cyclooxygenase inhibitors (COX-1 and COX-2) using molecular modeling simulation. (Pubmed Central) - Nov 8, 2022 Besides, two pyrazole derivatives, 4c and 5b, displayed a COX-1/COX-2 SI of 2.14 and 1.49. Computational techniques such as molecular docking, density function theory (DFT) calculation, and chemical absorption, distribution, metabolism, excretion, and toxicity evaluation were applied to explain the molecules' binding mode, chemical nature, drug likeness, and toxicity prediction.
- |||||||||| ibuprofen / Generic mfg.
Journal: Basal extrusion of single-oncogenic mutant cells induces dome-like structures with altered microenvironments. (Pubmed Central) - Nov 8, 2022 Furthermore, the expression of COX-2 is profoundly elevated in RasV12 cells in dome-like structures, and treatment with the COX inhibitor ibuprofen suppresses the recruitment of activated fibroblasts and moderately diminishes the formation of dome-like structures. Hence, basal extrusion of single-oncogenic mutant cells can induce tumor microenvironment and EMT and generate characteristic precancerous lesions, providing molecular insights into the earlier step of cancer development.
- |||||||||| aspirin / Generic mfg., minocycline / Generic mfg.
Review, Journal: Current Perspectives on Pharmacological and Non-Pharmacological Interventions for the Inflammatory Mechanism of Unipolar Depression. (Pubmed Central) - Oct 28, 2022 Some of the non-pharmacological interventions (physical exercise and electroconvulsive therapy) have also showed beneficial effects for depressive patients with elevated inflammatory markers. Treatments with anti-inflammatory action may improve clinical outcomes in depression, at least for some categories of patients, thus opening the way for a future personalised approach to patients with unipolar depression regarding the inflammation-related mechanism.
- |||||||||| indomethacin / Generic mfg.
Preclinical, Journal: Role of Prostaglandins in Nitric Oxide-Induced Glial Cell-Mediated Vasodilation in Rat Retina. (Pubmed Central) - Oct 28, 2022 Male Wistar rats were used to examine the effects of intravitreal pretreatment with indomethacin, a cyclooxygenase inhibitor; PF-04418948, a prostanoid EP receptor antagonist; and CAY10441, a prostanoid IP receptor antagonist, on the changes in the retinal arteriolar diameter induced by intravitreal administration of NOR3, an NO donor...These results suggest that activation of the arachidonic acid cascade and subsequent stimulation of prostanoid EP receptors are involved in rat retinal vasodilatory responses evoked by NO-induced glial cell stimulation. Therefore, glial cell-derived PGE, similar to EETs, may play an important role in retinal vasodilatory mechanisms.
- |||||||||| ibuprofen / Generic mfg., celecoxib oral / Generic mfg.
Journal: Investigation of Embelin synthetic hybrids as potential COVID-19 and COX inhibitors: Synthesis, Spectral analysis, DFT calculations and Molecular docking studies. (Pubmed Central) - Oct 25, 2022 The compounds 3, 4, 7, and 8 demonstrated excellent COX inhibitions with IC50 values of 1.65, 1.54, 1.56, and 1.23 μM compared to standard drugs Celecoxib and Ibuprofen. Finally, the molecular docking studies carried out with Covid-19 and cyclooxygenase with all the newly synthesized embelin derivatives.
- |||||||||| Journal, BRCA Biomarker: The prognostic value of arachidonic acid metabolism in breast cancer by integrated bioinformatics. (Pubmed Central) - Oct 23, 2022
The study indicated that a high level of AA metabolism may be a biomarker for good prognosis in breast cancer, providing a possible explanation for the discouraging effect of cyclooxygenase inhibitors in cancer therapy. Moreover, a novel AA metabolic prognostic signature was constructed in the study, providing a novel strategy for breast cancer.
- |||||||||| acetylcysteine solution / Generic mfg., paracetamol / Generic mfg.
An early morning at Barbastro´s Hospital () - Oct 17, 2022 - Abstract #EUSEM2022EUSEM_1377; We should perform an exhaustive hepatic function control, as well as paracetamol blood levels.Youth is a stressful time in many people´s lives. As emergency doctors, we can draw up a protocol for those substances that are within everyone´s reach and that can have harmful consequences for health, such as paracetamol, due to overdose.
- |||||||||| acetylcysteine solution / Generic mfg., paracetamol / Generic mfg.
An early morning at Barbastro´s Hospital () - Oct 17, 2022 - Abstract #EUSEM2022EUSEM_1376; We should perform an exhaustive hepatic function control, as well as paracetamol blood levels.Youth is a stressful time in many people´s lives. As emergency doctors, we can draw up a protocol for those substances that are within everyone´s reach and that can have harmful consequences for health, such as paracetamol, due to overdose.
- |||||||||| acetylcysteine solution / Generic mfg., paracetamol / Generic mfg.
An early morning at Barbastro´s Hospital () - Oct 17, 2022 - Abstract #EUSEM2022EUSEM_1375; We should perform an exhaustive hepatic function control, as well as paracetamol blood levels.Youth is a stressful time in many people´s lives. As emergency doctors, we can draw up a protocol for those substances that are within everyone´s reach and that can have harmful consequences for health, such as paracetamol, due to overdose.
- |||||||||| acetylcysteine solution / Generic mfg., paracetamol / Generic mfg.
An early morning at Barbastro´s Hospital () - Oct 17, 2022 - Abstract #EUSEM2022EUSEM_1374; We should perform an exhaustive hepatic function control, as well as paracetamol blood levels.Youth is a stressful time in many people´s lives. As emergency doctors, we can draw up a protocol for those substances that are within everyone´s reach and that can have harmful consequences for health, such as paracetamol, due to overdose.
- |||||||||| Journal: Megastigmane sesquiterpenoids from whole plants of Viola kunawurensis. (Pubmed Central) - Oct 12, 2022
Their structures were established by comprehensive 1D, 2D-NMR and HRESIMS analyses, and their absolute configurations were determined by comparing their calculated ECD data with the experimental ones. Evaluations of the anti-inflammatory activity revealed that kunawuronoside A-D and compounds 14-15 inhibited COX-2 expression with inhibition rates ranging from 36.7% to 58.5%, while the NO production induced by lipopolysaccharide (LPS) was suppressed by the kunawuronoside A-D in a dose-dependent manner in RAW264.7 macrophage cell line.
- |||||||||| celecoxib oral / Generic mfg.
Preclinical, Journal: Effect of Selective Cyclooxygenase Inhibitors on Animal Behaviour and Monoaminergic Systems of the Rat Brain. (Pubmed Central) - Oct 8, 2022 Therefore, we studied the effects of SC560 (selective COX-1 inhibitor) and celecoxib (selective COX-2 inhibitor) on the activity of brain monoaminergic systems and animal behaviour...In turn, changes in the activity of the serotonergic system may be related to the activity of indoleamine-2,3-dioxygenase, which decreases because of the decreased concentration of pro-inflammatory compounds. We believe that behavioural changes induced by COX inhibitors are the result of the modified activity of monoaminergic CNS systems in the brainstem, hypothalamus, and medial prefrontal cortex.
- |||||||||| Repurposing NSAIDs for cancer immunotherapy: mechanisms beyond COX inhibition (Hall C) - Oct 6, 2022 - Abstract #SITC2022SITC_1110;
Conclusions Our results demonstrate that the pro-oxidative property of NSAIDs can be exploited to enhance death receptor signaling in cancer cells, providing rationale for combining NSAIDs with genetically modified T cells to intensify tumor cell killing through the TRAIL-DR5 axis. Ethics Approval All animal experiments and procedures were performed in accordance with the institutional protocol and were approved by the Institutional Animal Care and Use Committee (IACUC) of Augusta University.
- |||||||||| aspirin / Generic mfg., sulindac / Generic mfg., celecoxib oral / Generic mfg.
Review, Journal: Colorectal Carcinoma, Cyclooxygenases, and COX Inhibitors. (Pubmed Central) - Oct 4, 2022 Aspirin and Sulindac were two drugs to be initially proven to halt the progression and cause regression of the polyps. Celecoxib, a selective COX-2 inhibitor besides NSAIDs, was also used in experimental studies.
- |||||||||| aspirin / Generic mfg.
Review, Journal: Fifty Years with Aspirin and Platelets. (Pubmed Central) - Oct 4, 2022 What followed was a long, winding road of clinical research leading to the characterization of low-dose aspirin as a life-saving antiplatelet drug, that still represents the cornerstone of antithrombotic therapy. Having witnessed and participated in these 50 years of aspirin research, I thought of providing a personal testimony of how things developed and eventually led to a remarkable success story of independent research.
- |||||||||| Preclinical, Journal: Ehrlich Tumor Induces TRPV1-Dependent Evoked and Non-Evoked Pain-like Behavior in Mice. (Pubmed Central) - Sep 25, 2022
Intrathecal injection of AMG9810 (TRPV1 antagonist) reduced ongoing Ehrlich tumor-triggered mechanical and thermal hyperalgesia (p < 0.05). Therefore, the contribution of TRPV1 to Ehrlich tumor pain behavior was revealed by genetic and pharmacological approaches, thus, supporting the use of this model to investigate TRPV1-targeting therapies for the treatment of cancer pain.
- |||||||||| Review, Journal: Development and Challenges of Diclofenac-Based Novel Therapeutics: Targeting Cancer and Complex Diseases. (Pubmed Central) - Sep 25, 2022
In this article, we discuss why defining diclofenac-based mechanisms, pharmacological features, and its medicinal properties are needed to direct future drug development against neurodegeneration and imperfect ageing and to improve cancer therapy. In addition, we describe various advance molecular mechanisms and fundamental aspects linked with diclofenac which can strengthen and enable the better designing of new derivatives of diclofenac to overcome critical challenges and improve their applications.
- |||||||||| aspirin / Generic mfg.
Journal: Catalytic covalent inhibition of cyclooxygenase-1 by a biomimetic acyltransferase. (Pubmed Central) - Sep 24, 2022 In this study, a small molecule has been developed for the first time that can achieve catalytic covalent inhibition of the inflammatory response enzyme, cyclooxygenase-1, in cells using only endogenous acetyl-CoA as a co-substrate. By utilizing a catalytic inhibitor which can self-regenerate, a sustained inhibitory response is achieved in cells compared to the analogous non-catalytic covalent cyclooxygenase antagonist, acetylsalicylic acid (aspirin).
- |||||||||| rofecoxib (TRM-201) / Tremeau Pharma
Diagnosing the Cardiovascular Risk of VIOXX: A Place for Rofecoxib in Pain Management (Virtual Poster Hall) - Sep 17, 2022 - Abstract #ACRConvergence2022ACR_CONVERGENCE_3274; P3 Given its unique profile, rofecoxib ≤25 mg/day may be a viable treatment option in patients populations for whom tNSAIDs are avoided and where opioids are frequently used. Tremeau Pharmaceuticals is currently conducting a pivotal Phase III trial evaluating rofecoxib in the treatment of hemophilic arthropathy (NCT04684511) and is pursuing other indications
- |||||||||| dorsomorphin (Compound C) / EMD Serono
Preclinical, Journal: Vascular Functional Effect Mechanisms of Elabela in Rat Thoracic Aorta. (Pubmed Central) - Sep 10, 2022 Elabela exhibits a prominent vasodilator effect in rat thoracic aorta. Apelin receptor, prostanoids, adenosine monophosphate-activated protein kinase, protein kinase C, and calcium-activated potassium channels are involved in the vasorelaxant effect mechanisms of elabela.
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