- |||||||||| morphine sulphate / Generic mfg.
EVALUATION OF INTRAVENOUS KETOROLAC IN CARDIOTHORACIC SURGERY PATIENTS ([VIRTUAL]) - Mar 23, 2022 - Abstract #SCCM2022SCCM_1934; The use of IV ketorolac did not reduce post-operative opioid use in CABG patients compared to CPM at POD2. Further studies are warranted to fully understand if ketorolac plays a meaningful role in the post-operative pain management of patients undergoing CABG.
- |||||||||| cisplatin / Generic mfg.
Preclinical, Journal: Development of methylated cobalt-alkyne complexes with selective cytotoxicity against COX-positive cancer cell lines. (Pubmed Central) - Mar 12, 2022 The reduced growth-inhibitory potency in T-24 cells, which express distinctly fewer COX enzymes (COX-1/COX-2 = 50/1) than HT-29 cells (COX-1/COX-2 = 50/50), and the only marginal activity in COX-negative MCF-7 breast cancer cells point to an interference in the arachidonic acid cascade through COX-2 inhibition as part of the mode of action, especially as the cellular uptake was even higher in MCF-7 cells than in T-24 cells. These findings clearly demonstrate that the methylated cobalt-alkyne complexes possess promising potential for further development as reasonable alternatives to the limited platinum-based antitumor agents.
- |||||||||| ibuprofen / Generic mfg.
Review, Journal: Management of the patent ductus arteriosus in preterm infants. (Pubmed Central) - Mar 12, 2022 High-dose ibuprofen may be preferable, especially for preterm infants beyond the first 3 to 5 days of age. If pharmacotherapy fails (after two courses) or is contraindicated, procedural closure may be considered for infants with a persistent PDA with significant clinical symptoms in addition to echocardiographic signs of a large PDA shunt volume and pulmonary over-circulation.
- |||||||||| Quantification of oxylipins as biomarkers of inflammation and cancer risk in breast tissue (E-Poster Website) - Mar 9, 2022 - Abstract #AACR2022AACR_5298;
We conclude that eicosanoids can be readily measured in small frozen breast tissue samples obtained via percutaneous biopsy or at surgery. Future studies to assess the associations of eicosanoid levels with BC risk factors and development of BC after a benign biopsy may inform risk prediction and potentially inhibitable inflammatory mechanisms of breast carcinogenesis.
- |||||||||| In vivo CRISPR screening identifies mediators of immune evasion in KRAS-mutant lung cancer (Section 37) - Mar 9, 2022 - Abstract #AACR2022AACR_3378;
Together these data suggest that targeting KRAS-driven mechanisms of immune evasion could broaden the clinical efficacy of immunotherapy in KRAS-mutant NSCLC.Since the approval of immunotherapy, a novel class of mutant-specific KRAS-G12C inhibitors have recently been approved for the treatment of KRAS-mutant NSCLC, however acquired drug resistance is common. We are therefore also currently investigating whether the inhibition of the COX-2/PGE2 axis enhances the therapeutic benefit of KRAS-G12C inhibitors.
- |||||||||| Journal: Flavonoids: Antiplatelet Effect as Inhibitors of COX-1. (Pubmed Central) - Mar 5, 2022
The results obtained showed that quercetin and diosmetin aglycones have a greater antiplatelet effect and inhibit the COX enzyme activity to a greater extent than their heterosides; however, the fact that greater inhibition of the pure recombinant enzyme was achieved by heterosides suggests that these compounds may have difficulty in crossing biological membranes. In any case, in view of the results obtained, it can be concluded that flavonoids could be useful as coadjuvants in the treatment of cardiovascular pathologies.
- |||||||||| indomethacin / Generic mfg.
Preclinical, Journal: Cyclooxygenase-dependent mechanisms mediate in part the anti-dilatory effects of perivascular adipose tissue in uterine arteries from pregnant rats. (Pubmed Central) - Mar 3, 2022 Arteries were exposed to Krebs-Henseleit solution (control) or PVAT-conditioned media (PVATmedia) in the presence of the following inhibitors: L-NAME (NOS inhibitor), indomethacin (COX inhibitor), SC560 (COX-1 inhibitor), NS398 (COX-2 inhibitor), SQ 29,548 (thromboxane receptor (TP) inhibitor)...Incubation of uterine arteries from pregnant rats with PVATmedia increased production of thromboxane B (TxB, p=0.01) but thromboxane receptor (TP) inhibition did not affect the anti-dilatory properties of PVATmedia. In conclusion, inhibition of COX signaling suppressed the anti-dilatory effects of PVATmedia, while PVATmedia had no effect on the contribution of the NOS/NO pathway to ACh-induced relaxation in uterine arteries from pregnant rats, indicating that the anti-dilatory effects of uterine PVAT are mediated in part by COX-dependent mechanisms.
- |||||||||| celecoxib oral / Generic mfg.
Review, Journal: New horizons in the roles and associations of COX-2 and novel natural inhibitors in cardiovascular diseases. (Pubmed Central) - Feb 24, 2022 The combination of galangin-like flavonol compounds with these prodrug metabolites may lead to the development of novel COX-2 inhibitors. This review focuses on the most compelling evidence regarding the role and mechanism of COX-2 in cardiovascular diseases and demonstrates that quercetin-like compounds exert potential cardioprotective effects by serving as cofactors of COX-2.
- |||||||||| fluconazole oral / Generic mfg., ibuprofen / Generic mfg., voriconazole / Generic mfg.
Journal: Fluconazole-COX Inhibitor Hybrids: A Dual-Acting Class of Antifungal Azoles. (Pubmed Central) - Feb 19, 2022 The hybrids were active against a mutant lacking CYP51, the target of azole drugs, indicating that these agents act via a dual mode of action. This study established that azole-COX inhibitor hybrids are a novel class of potent antifungals with clinical potential.
- |||||||||| Journal: Antiarthritic activity of OA-DHZ; a gastroprotective NF-κB/MAPK/COX inhibitor. (Pubmed Central) - Feb 17, 2022
In contrast to the results obtained from in vivo experimentation, there is a disparity in the pharmacokinetic profile of OA-DHZ, where it showed low oral exposure and high clearance rate. OA-DHZ being antiarthritic acting via NF-κB /MAPK/ COX inhibition while showing gastroprotective effects, can be a suitable candidate to be in the drug pipeline and further exploration.
- |||||||||| Journal: Activity-Guided Characterization of COX-2 Inhibitory Compounds in Waltheria indica L. Extracts. (Pubmed Central) - Feb 17, 2022
The results of the predictive models further suggested that the compounds contribute to COX-2 inhibition in the order linoleic acid > alpha linolenic acid > steroidal saponins > triterpenoid saponins. The characterization of substances contributing to COX-2 inhibition in this study enables a more targeted development of extraction processes to obtain Waltheria indica extracts with superior anti-inflammatory properties.
- |||||||||| celecoxib oral / Generic mfg.
Journal: Effects of Celecoxib Adjunct to Selective Serotonin Reuptake Inhibitors on Obsessive-Compulsive Disorder. (Pubmed Central) - Feb 15, 2022 There was a significant difference between the study groups in obsession (F= 49.19, df= 1, P≤0.001), compulsion (F= 13.78, df= 1, P= 0.001), and OCD (F= 57.25, df= 1, P≤0.001), i.e., higher in the celecoxib group. This study showed that adjuvant treatment with celecoxib can further improve the symptoms of OCD in individuals receiving SSRIs.
- |||||||||| paracetamol / Generic mfg.
Review, Journal: Pharmacological hypotheses: Is acetaminophen selective in its cyclooxygenase inhibition? (Pubmed Central) - Feb 12, 2022 Thus, we suggest with specificity to human in vivo physiology that ACT: (i) does not act on a third COX isoform; (ii) is not selective in its COX inhibition; and (iii) inhibition of COX isoforms are determined by subtle and nuanced physiological variations. Robust research designs are required in humans to objectively confirm these hypotheses.
- |||||||||| celecoxib oral / Generic mfg.
Review, Journal: Recent advances in molecular pathways and therapeutic implications targeting neuroinflammation for Alzheimer's disease. (Pubmed Central) - Feb 12, 2022 Non-selective COX inhibitor indomethacin is also potent inhibitor of inflammatory mediators released from microglia...Mitophagy induction is also beneficial in the removal of damaged mitochondria and reduction of infiltration of inflammatory molecules at the site of accumulation of the damaged mitochondria. Targeting these pathways and eventually ameliorating the activation of microglia can mitigate neuroinflammation and come out as a better therapeutic option for the treatment of Alzheimer's disease.
- |||||||||| ibuprofen / Generic mfg.
Preclinical, Journal: Airway hyperresponsiveness induced by intermittent hypoxia in rats. (Pubmed Central) - Feb 10, 2022 IH-induced AHR and lung inflammation were completely abolished by daily intraperitoneal injection of N-acetylcysteine (an antioxidant) or ibuprofen (a cyclooxygenase inhibitor), but not by apocynin (an inhibitor of NADPH oxidase) or vehicle. In conclusion, AHR and lung inflammation occur after 14-day IH exposure, with endogenous reactive oxygen species and cyclooxygenase metabolites being responsible for these responses.
- |||||||||| meloxicam / Generic mfg., etoricoxib / Generic mfg.
Journal: The hyperthermic effect of central cholecystokinin is mediated by the cyclooxygenase-2 pathway. (Pubmed Central) - Feb 9, 2022 Finally, the CCK receptor antagonist YM022 (10 µg/kg; icv) attenuated the late phases of fever induced by bacterial lipopolysaccharide (10 µg/kg; intravenously). We conclude that centrally administered CCK causes hyperthermia through changes in the activity of "classical" thermoeffector pathways, and that the activation of COX-2 is required for the development of this response.
- |||||||||| meloxicam / Generic mfg., piroxicam / Generic mfg.
Journal: Biological Evaluation and Molecular Docking Studies of Novel 1,3,4-Oxadiazole Derivatives of 4,6-Dimethyl-2-sulfanylpyridine-3-carboxamide. (Pubmed Central) - Feb 8, 2022 Furthermore, the results of cytotoxicity assay indicated that all of the tested compounds exhibited potent anti-cancer activity against A549, MCF-7, LoVo, and LoVo/Dx cell lines, compared with piroxicam and meloxicam. Moreover, our experimental study was supported by density functional theory (DFT) and molecular docking to describe the binding mode of new structures to cyclooxygenase.
- |||||||||| celecoxib oral / Generic mfg.
Journal: Docking Study, Synthesis, and Anti-Inflammatory Potential of Some New Pyridopyrimidine-Derived Compounds. (Pubmed Central) - Feb 8, 2022 Moreover, the gastric ulcerogenic potential assay of compounds IIIf-h revealed their lower ulcerogenic liability than indomethacin with comparable effect to celecoxib. Virtual docking investigation of the most active candidates IIId, IIIf, IIIg and IIIi in the active site of COX-2 enzyme showed that these compounds implied interaction and binding motif similar to the cocrystallized ligand bromocelecoxib.
- |||||||||| indomethacin / Generic mfg.
Preclinical, Journal: Design, synthesis, and in vitro antiplatelet aggregation activities of taiwanin C. (Pubmed Central) - Feb 8, 2022 These results demonstrate that taiwanin C acts very efficiently in two different signaling pathways of platelet aggregation. Although preliminary, these results indicate that taiwanin C has potential for further studies on its use for the development of new antiplatelet.
- |||||||||| Journal: Automatic evaluation of cyclooxygenase 2 inhibition induced by metal-based anticancer compounds. (Pubmed Central) - Feb 3, 2022
The results obtained in this work provide significant information about the mechanism of the studied compounds, mostly ruthenium-based compounds, and the role of COX-2 in their mode of action. Moreover, this work confirmed the potential of the μSIA-LOV system as a simple, versatile, robust, and rapid analytical tool for automating the determination of IC values of metal-based compounds.
- |||||||||| Vampex (carbenoxolone gel) / York Pharma
Preclinical, Journal: Involvement of Gap Junctions in Acetylcholine-Induced Endothelium-Derived Hyperpolarization-Type Dilation of Retinal Arterioles in Rats. (Pubmed Central) - Feb 1, 2022 Moreover, the retinal arteriolar response to ACh was attenuated by 18β-glycyrrhetinic acid under treatment with a combination of N-nitro-L-arginine methyl ester (a nitric oxide (NO) synthase inhibitor; 30 mg/kg) and indomethacin (a cyclooxygenase inhibitor; 5 mg/kg)...Treatment with 18β-glycyrrhetinic acid revealed no significant effect on NOR3 (an NO donor)-induced retinal vasodilator response. These results suggest that gap junctions contribute to the ACh-induced, EDH-type dilation of rat retinal arterioles in vivo.
- |||||||||| Journal: Comparison of bioactive compounds and health promoting properties of fruits and leaves of apple, pear and quince. (Pubmed Central) - Jan 28, 2022
Leaves of apples and pears most effectively inhibited COX-1, COX-2, α-amylase, and α-glucosidase enzyme but quince leaves showed the most effective inhibition of pancreatic lipase, AChE and BuChE, 15-LOX, and antioxidant capacity, which particularly correlated with bioactive compounds. Present study shows that leaves are promising sources of valuable compounds and may be used to produce functional foods as well as for medical purposes.
- |||||||||| Selective dietary plant extract as inhibitors of cyclooxygenase -1 and cyclooxygenase-2 activities (Zoom Room 1 (Virtual Room)) - Jan 28, 2022 - Abstract #ACSSp2022ACS_Sp_8086;
Selective inhibition of COX2 over COX1 were found to be better by minimizing gastrointestinal effects associated with COX-1. This study of screening of various food product as potential inhibitors against COX1 and CO2 is expected to guide us to develop effective natural dietary plant products that provide anti-inflammatory properties with limited or no side effects.
- |||||||||| glibenclamide / Generic mfg., nifedipine immediate release / Generic mfg.
Preclinical, Journal: Mechanisms of inhibitory activity of root extract of Carpolobia lutea G. Don on in vitro contractile responses of rabbit corpus carvernosum. (Pubmed Central) - Jan 27, 2022 This study of screening of various food product as potential inhibitors against COX1 and CO2 is expected to guide us to develop effective natural dietary plant products that provide anti-inflammatory properties with limited or no side effects. Concentration-dependent relaxant effect of CLRE in rabbit CC involves the soluble guanylate cyclase/cyclase Guanosine Monophosphate system, and activation of ATP-dependent K channels.
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