- |||||||||| Journal: Therapeutic Use of Scoparia dulcis Reduces the Progression of Experimental Osteoarthritis. (Pubmed Central) - Feb 14, 2020
The experiment was performed with Wistar rats divided into 4 groups with 5 animals each: healthy, saline, crude extract, and meloxicam groups...The highest inhibition of cyclooxygenase 2 in the crude extract occurred at 50 µg/mL. The crude extract of S. dulcis presents therapeutic potential for the treatment of osteoarthritis due to its anti-inflammatory and anti-nociceptive action.
- |||||||||| ibuprofen / Generic mfg.
A case of quad fever which responded to oral ibuprofen () - Feb 11, 2020 - Abstract #ISPRM2020ISPRM_337; Ibuprofen act via inhibiting cyclooxygenase enzyme thus reduce production of prostaglandin H2 which has contributed to fever. Conclusions : Oral ibuprofen, a readily available drug, is a potential treatment agent to treat quad fever
- |||||||||| Journal: Map and model-moving from observation to prediction in toxicogenomics. (Pubmed Central) - Feb 7, 2020
The design and analysis pipeline described here could serve as a blueprint for creating comparable toxicogenomic fingerprints of chemicals. It integrates, aggregates, and models time- and concentration-resolved toxicogenomic data.
- |||||||||| celecoxib oral / Generic mfg.
Journal: 1,4-Dihydroquinazolin-3(2H)-yl benzamide derivatives as anti-inflammatory and analgesic agents with an improved gastric profile: Design, synthesis, COX-1/2 inhibitory activity and molecular docking study. (Pubmed Central) - Jan 17, 2020 Compounds 4b, 4d, 4h, 4l, 4n and 4o showed the best in vitro COX-2 inhibitory activity (IC 0.04-0.07 μM), which was nearly the same as that of the reference drug celecoxib (IC 0.049 μM), but had a lower selectivity index, as dictated in our target design...The docking study results agreed with the in vitro COX inhibition assay results. Moreover, the predicted in silico studies of all the compounds support their potential as drug candidates.
- |||||||||| Journal: BPTF cooperates with p50 NF-κB to promote COX-2 expression and tumor cell growth in lung cancer. (Pubmed Central) - Jan 16, 2020
Moreover, we showed that the expressions of BPTF and COX-2 in tumor tissues of lung cancer patients were positively correlated, and high co-expression of BPTF and COX-2 predicted poor prognosis in lung cancer patients. Collectively, our results indicated that BPTF cooperated with p50 NF-κB to regulate COX-2 expression and lung cancer growth, suggesting that the BPTF/p50/COX-2 axis could be a potential therapeutic target for lung cancer.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
Clinical, Journal, Real-World Evidence: Comparison of cholinesterase inhibitor safety in real-world practice. (Pubmed Central) - Jan 11, 2020 Compared with low-dose donepezil, galantamine use was associated with a lower risk of mortality (adjusted hazard ratio: 0.84, 95% confidence interval: 0.60-1.18), cardiovascular serious adverse events (adjusted hazard ratio: 0.78, 95% confidence interval: 0.62-0.98), and entry into a residential care facility (adjusted hazard ratio: 0.72, 95% confidence interval: 0.59-0.89). Given the absence of randomized trial data showing clinically meaningful benefit of ChEI therapy in Alzheimer's disease, our study suggests preferential use of galantamine may at least be associated with fewer adverse events than treatment with donepezil or rivastigmine.
- |||||||||| Journal: Endometriosis. (Pubmed Central) - Jan 11, 2020
Endometriosis-associated pelvic pain is managed by suppression of ovulatory menses and estrogen production, cyclooxygenase inhibitors, and surgical removal of pelvic lesions, and in vitro fertilization is frequently used to overcome infertility. Although novel targeted treatments are becoming available, as endometriosis pathophysiology is better understood, preventive approaches such as long-term ovulation suppression may play a critical role in the future.
- |||||||||| Journal: Increased coronary arteriolar contraction to serotonin in juvenile pigs with metabolic syndrome. (Pubmed Central) - Jan 10, 2020
MetS exhibited significant increases in tissue levels of TXA synthase and TP receptors (P < 0.05 vs. lean), respectively. MetS is associated with increased contractile response of porcine coronary arterioles to serotonin, which is in part via upregulation/activation of PLA, COX, and subsequent TXA, suggesting that alteration of vasomotor function may occur at an early stage of MetS and juvenile obesity.
- |||||||||| Entyvio (vedolizumab) / Takeda
New onset spondyloarthropathy in vedolizumab treated IBD patients (Hall C - Poster exhibition) - Jan 7, 2020 - Abstract #ECCOIBD2020ECCO_IBD_1611; On re-challenge with vedolizumab, the arthropathy recurred in 2 out of the 3 patients.Conclusion This case series demonstrates the potential risk for development of spondyloarthropathy with vedlizumab in IBD patients which is unrelated to the activity of IBD and can have significant impact including need for use for systemic steroids and hospitalisation. Larger prospective cohorts are needed to confirm these results.
- |||||||||| Dynastat (parecoxib) / Pfizer, etoricoxib / Generic mfg., celecoxib oral / Generic mfg.
Journal: A review of dexketoprofen trometamol in acute pain. (Pubmed Central) - Jan 1, 2020 Larger prospective cohorts are needed to confirm these results. In conclusion, dexketoprofen trometamol appears to provide similar analgesic efficacy to COX-2 inhibitors when used to treat acute pain, has a rapid onset of action, is well tolerated, and has an opioid-sparing effect when used as part of a multimodal regimen in the acute pain setting.
- |||||||||| celecoxib oral / Generic mfg.
Journal: Nanoliposomal formulation encapsulating celecoxib and genistein inhibiting COX-2 pathway and Glut-1 receptors to prevent prostate cancer cell proliferation. (Pubmed Central) - Jan 1, 2020 The mechanistic study suggests that enhanced reactive oxygen species (ROS) formation and a decrease in cellular GSH concentration, along with inhibition of COX-2 synthesis and Glut-1 receptors are the key processes behind the inhibition of prostate cancer cells. Overall, these results provide strong evidence for the role of COX-2 and Glut-1 proteins for the progression of prostate cancer and highlighting the potential of celecoxib and genistein as a useful and combinatorial pharmacological agent for chemotherapeutic purposes in prostate cancer.
- |||||||||| Endometriosis (Room 157) - Dec 14, 2019 - Abstract #ENDO2020ENDO_1002;
Endometriosis-associated pelvic pain is managed by suppression of ovulatory menses and estrogen production, cyclooxygenase inhibitors, and surgical removal of pelvic lesions, and in vitro fertilization is frequently used to overcome infertility. Although novel targeted treatments are becoming available, as endometriosis pathophysiology is better understood, preventive approaches such as long-term ovulation suppression may play a critical role in the future.
- |||||||||| Journal: Cyclooxygenase-2 inhibitors as a therapeutic target in inflammatory diseases. (Pubmed Central) - Dec 6, 2019
COX-2 selective inhibitors happen to show equivalent efficacy with that of conventional NSAIDs, but they have reduced gastrointestinal side effects. This review would elucidate the most recent findings on selective COX-2 inhibition and their relevance to human pathology, concretely in inflammatory pathologies characterized by a prolonged pro-inflammatory status, including autoimmune diseases, metabolic syndrome, obesity, atherosclerosis, neurodegenerative diseases, chronic obstructive pulmonary disease, arthritis, chronic inflammatory bowel disease and cardiovascular pathologies.
- |||||||||| Brilinta (ticagrelor) / AstraZeneca, Cangrelor (ARC69931MX) / The Medicines Company, Effient (prasugrel) / Eli Lilly, Daiichi Sankyo
Journal: Structure Activity Relationship of 4-Amino-2-thiopyrimidine Derivatives as Platelet Aggregation Inhibitors. (Pubmed Central) - Dec 6, 2019 These negative findings demonstrated that this heterocyclic nucleus is not a useful common pharmacophore for developing P2Y-dependent inhibitors of platelet aggregation. Nevertheless, compounds 2c and 2h could represent a new chemotype to further develop inhibitors of platelet aggregation.
- |||||||||| nitroprusside / generics
Journal: Linoleic acid reduces vascular reactivity and improves the vascular dysfunction of the small mesentery in hypertension. (Pubmed Central) - Dec 2, 2019 LA treatment reduced the contractile response to phenylephrine, although there were no changes observed in MRA in regard to the acetylcholine or sodium nitroprusside responses...In conclusion, these findings show that LA treatment decreases blood pressure. In addition, the improvement of endothelial dysfunction and structural changes in this hypertension model may be responsible for the reduction in blood pressure.
- |||||||||| glibenclamide / generics
Journal: Chrysophyllum cainito (apple-star): a fruit with gastroprotective activity in experimental ulcer models. (Pubmed Central) - Nov 30, 2019 Regarding the mode of action, the gastroprotective effect of MEPe was decreased by the pre-administration of N-ethylmaleimide (NEM, a sulfhydryl group chelator, 10 mg/kg, i.p), glibenclamide (a potassium channel blocker, 10 mg/kg, i.p), yohimbine (10 mg/kg, i.p, an alpha-adrenergic receptor antagonist, 10 mg/kg, i.p) and indomethacin (a cyclooxygenase inhibitor, 10 mg/kg, i.p)...Together, the antiulcer effect of extracts of the C. cainito fruit in different experimental models was confirmed by the favoring of mucosal protective mechanisms among different, but complementary, modes of action. In parallel, the gastroprotective effects of the flour from C. cainito fruit were also described.
- |||||||||| Journal: Cysteinyl leukotriene receptor antagonism: a promising pharmacological strategy for lowering the severity of arthritis. (Pubmed Central) - Nov 29, 2019
Paw inflammation, RA markers (RF and CRP), eicosanoids (PGE, LTB, and LTC), cytokines (IL-1β and MCP-1), activity of hydrolytic enzymes (collagenase, elastase, and hyaluronidase), expression of matrix metalloproteinases (MMP), and EP-4 receptor were significantly (p < 0.05) reduced in montelukast administered rats. This study established that leukotriene inhibition through montelukast lowered the severity of arthritis and thus a potential strategy for reducing the severity of arthritis.
- |||||||||| dalfampridine / Generic Mfg.
Preclinical, Journal: GLP-1 Relaxes Rat Coronary Arteries by Enhancing ATP-Sensitive Potassium Channel Currents. (Pubmed Central) - Nov 29, 2019 Furthermore, GLP-1 increased outward K currents by enhancing the K channel in rat coronary arterial smooth muscle cells (RCASMCs). These results show that GLP-1 is an endothelial-dependent vasospasmolytic agent in the RCA and imply that the relaxant effect is regulated by enhancing K rather than K or K currents in RCASMCs.
- |||||||||| aspirin / Generic Mfg., Tarceva (erlotinib) / Astellas, Roche
Journal: Reconsidering the Role of Cyclooxygenase Inhibition in the Chemotherapeutic Value of NO-Releasing Aspirins for Lung Cancer. (Pubmed Central) - Nov 19, 2019 Nitric oxide-releasing aspirins (NO-aspirins) are aspirin derivatives that are safer than the parent drug in the gastrointestinal context and have shown superior cytotoxic effects in several cancer models...NCX4040 was more potent in decreasing NSCLC cell viability and migration and exhibited significant synergistic effects in combination with erlotinib (an epidermal growth factor receptor inhibitor) in erlotinib-resistant cells...Furthermore, misoprostol reversed the antimigratory effects of NCX4040. Overall, these results indicate that PGE inhibition is important in the mode of action of NO-aspirins.
- |||||||||| ibuprofen / Generic mfg.
Polyunsaturated Fatty Acid (PUFA) Signaling Induces Ferroptosis-Mediated Cell-Death in Multiple Myeloma (Hall B, Level 2 (Orange County Convention Center)) - Nov 7, 2019 - Abstract #ASH2019ASH_4302; Mice were then treated with daily localized injections of vehicle, 100µg/g AA, 500µg/g of AA, or IV with 2mg/kg/biweekly Carfilzomib (CFZ), or CFZ with 500µg/g of AA (COMBO)...To identify the primary apoptosis-inducing AA signaling pathway in MM cells, we used specific inhibitors of each of these signaling pathways including ibuprofen (Cox inhibitor), baicalein (12-LOX inhibitor), BW B70C (5,15-LOX inhibitor), 1-aminobenzotriazole (CYP450 inhibitor), and ferrostatin (Ferroptosis/lipid peroxidation inhibitor)...Taken together, we show that BM adipocytes promote myeloma cell proliferation at least in part through secreted FFAs. Therapeutically targeting members of this signaling pathway, such as ferroptosis, is a potential novel treatment strategy for MM especially in the MGUS and SMM stages.
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