- |||||||||| Preclinical, Journal: Synthesis and In Vitro Biological Evaluation of p-Carborane-Based Di-tert-butylphenol Analogs. (Pubmed Central) - Jun 14, 2023
Interestingly, R-830-Cb did not affect the viability of primary cells and suppressed HCT116 cell proliferation more potently than its carbon-based R-830 counterpart. Considering all the advantages of boron cluster incorporation for enhancement of drug biostability, selectivity, and availability of drugs, R-830-Cb can be tested in further mechanistic and in vivo studies.
- |||||||||| AM 095 / BMS
Preclinical, Journal: TXA2 mediates LPA1-stimulated uterine contraction in late pregnant mouse. (Pubmed Central) - Jun 12, 2023 Moreover, selective thromboxane receptor (TP) antagonist, SQ-29548, and Rho kinase inhibitor, Y-27632 almost eliminated LPA-induced uterine contractions. LPA1 stimulation elicits contractions in the late pregnant mouse uterus using the contractile prostanoid, TXA2 and may be targeted to induce labor in uterine dysfunctions/ dystocia.
- |||||||||| simvastatin / Generic mfg.
Journal: New insights on mode of action of vasorelaxant activity of simvastatin. (Pubmed Central) - Jun 1, 2023 Furthermore, simvastatin was found to attenuate the release of calcium (Ca) from intracellular stores in the presence of ruthenium red (ryanodine receptor, RyR inhibitor) and extracellular stores via nifedipine (voltage-operated Ca channels, VOCC blocker) and SK&F96365 (receptor-operated Ca channel, ROCC blocker). Thus, it can be concluded that the vasorelaxant effect of simvastatin involves NO/cGMP pathways, ATR receptors, Ca channels, and K channels.
- |||||||||| indomethacin / Generic mfg., captopril / Generic mfg.
Preclinical, Journal: Pulegone Prevents Hypertension through Activation of Muscarinic Receptors and Cyclooxygenase Pathway in L-NAME-Induced Hypertensive Rats. (Pubmed Central) - May 26, 2023 Secondly, the mechanism involved in hypotensive activity was determined in the presence of pharmacological drugs such as atropine/muscarinic receptor blocker (1?mg/kg), L-NAME/NOS inhibitor (20?mg/kg), and indomethacin/COX inhibitor (5?mg/kg) in anesthetized rats...Rats were divided into six groups which were treated orally with tween 80 (placebo), captopril (10?mg/kg), and different doses of pulegone (20?mg/kg, 40?mg/kg, and 80?mg/kg)...Plasma mRNA expression of eNOS was reduced, whereas ACE, ICAM1, and EDN1 levels were high in the L-NAME group, which was facilitated by pulegone treatment. To conclude, pulegone prevented L-NAME-induced hypertension by demonstrating a hypotensive effect through muscarinic receptors and cyclooxygenase pathway, indicating its use as a potential candidate in managing hypertension.
- |||||||||| rofecoxib (TRM-201) / Tremeau Pharma
Journal: Discovery of andrographolide hit analog as a potent cyclooxygenase-2 inhibitor through consensus MD-simulation, electrostatic potential energy simulation and ligand efficiency metrics. (Pubmed Central) - May 24, 2023 In this study, chemical and bio-informatics approaches have been employed to find a novel potent andrographolide (AGP) analog as a COX-2 inhibitor having better pharmacological properties than aspirin and rofecoxib (controls). In-depth analysis revealed that AGP analog A3 (3-[2-[(1R,4aR,5R,6R,8aR)-6-hydroxy-5,6,8a-trimethyl-2-methylidene-3,4,4a,5,7,8-hexahydro-1H-naphthalen-1-yl]ethylidene]-4-hydroxyoxolan-2-one) forms the most stable complex with the AF-COX-2 showing the least RMSD value (0.37?
- |||||||||| Journal: Hybrids of carbonic anhydrase and cyclooxygenase inhibitors attenuate cardiac hypoxic inflammatory injuries. (Pubmed Central) - May 22, 2023
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. Consequently, this study provides a new strategy for the treatment of cardiac inflammation accompanied by hypoxia.
- |||||||||| STUDY OF ADVERSE REACTIONS TO COVID-19 VACCINATION IN PATIENTS WITH RHEUMATIC DISEASES () - May 19, 2023 - Abstract #EULAR2023EULAR_4167;
Based on the results of this study, we believe that adverse reactions to vaccination are acceptable. We plan to accumulate more cases and analyze them in the future.The exacerbation of disease after the first vaccination would predict the exacerbation after the second vaccination.
- |||||||||| Preclinical, Journal: Carborane-based Tebufelone Analogs and their Biological Evaluation In Vitro. (Pubmed Central) - May 9, 2023
Cell viability studies on HT29 colon adenocarcinoma cells revealed that the observed antiproliferative effect of the para-carborane analogs of tebufelone is enhanced by structural modifications that include chain elongation in combination with introduction of a methylene spacer resulting in higher anticancer activity compared to tebufelone. Hence, this strategy proved to be a promising approach to design potent 5-LO inhibitors with potential application as cytostatic agents.
- |||||||||| Review, Journal: Antiplatelet drugs: Potential therapeutic options for the management of neurodegenerative diseases. (Pubmed Central) - May 3, 2023
Apart from this, the review also emphasizes the recent developments of selected natural antiplatelet phytochemicals belonging to key classes of plant-based bioactive compounds, including polyphenols, alkaloids, terpenoids, and flavonoids as potential therapeutic candidates in NDDs. We believe that the broad analysis of contemporary strategies and specific approaches for plausible therapeutic treatment for NDDs presented in this review could be helpful for further successful research in this area.
- |||||||||| glibenclamide / Generic mfg., indomethacin / Generic mfg.
Preclinical, Journal: Vasorelaxant Effect of Moroccan Cannabis sativa Threshing Residues on Rat Mesenteric Arterial Bed is Endothelium and Muscarinic Receptors Dependent. (Pubmed Central) - May 1, 2023 Chemical investigation of EFCS identified potential active components namely apigenin and derivatives of luteolin skeleton and also additional components such as neophytadiene, squalene, and ?-sitosterol. In conclusion, the vasorelaxant effect of EFCS on rat mesenteric arterial bed, which is dependent of muscarinic receptor activation, nitric oxide, and EDHF, can account for potential therapeutic use against high blood pressure related cardiovascular diseases.
- |||||||||| Review, Journal: PDE5 inhibitors and gastric mucosa: implications for the management of peptic ulcer disease. (Pubmed Central) - Apr 29, 2023
In recent years, studies have mentioned tremendous pleiotropic effects of PDE5 inhibitors on gastrointestinal, urogenital, musculoskeletal, reproductive, cutaneous, and neurologic disorders. Recent data shows that PDE5 inhibition augments gastric mucosa protection, and here, we review the most recent findings regarding the use of PDE5 inhibitors for the prevention and management of PUD.
- |||||||||| clarithromycin / Generic mfg., celecoxib oral / Generic mfg.
Preclinical, Journal: Promising anti-Helicobacter pylori and anti-inflammatory metabolites from unused parts of Phoenix dactylifera CV 'Zaghloul': in (Pubmed Central) - Apr 28, 2023 The anti-inflammatory response of isolated compounds was evaluated by inhibiting cyclooxygenase-2 enzyme using TMPD Assay followed by an in silico study to validate their mechanism of action using celecoxib as a standard drug...These results were verified by molecular docking studies, where 4, 7 and 8 showed the best interactions with key amino acid residues of COX-2 active site. The present study characterizes a new sesquiterpene lactone and recommends 4 and 8 for future in
- |||||||||| nimesulide / Generic mfg.
Journal: Synergistic Combination of Citrus Flavanones as Strong Antioxidant and COX-Inhibitor Agent. (Pubmed Central) - Apr 28, 2023 Indeed, DFM proves to be the most powerful anti-inflammatory and antioxidant agent reducing, synergistically and in a statistically significant manner (p < 0.05), PGE2 release than the oxidative stress markers, also with respect to the nimesulide and trolox used as reference compounds. This leads to the hypothesis that FM could be an excellent antioxidant and COX inhibitor candidate to counteract intestinal inflammation.
- |||||||||| ticagrelor / Generic mfg., aspirin / Generic mfg., ibrutinib / Generic mfg.
Journal: Effect of antiplatelet agents and tyrosine kinase inhibitors on oxLDL-mediated procoagulant platelet activity. (Pubmed Central) - Apr 17, 2023 Studies of washed human platelets, as well as platelets from mouse and non-human primate models of hyperlipidemia, further determined that P2YR antagonists (e.g., ticagrelor) and BTK inhibitors (e.g., ibrutinib) reduced oxLDL-mediated platelet responses and procoagulant activity, whereas COX inhibitors (e.g., aspirin) had no significant effect. Together, our results demonstrate that oxLDL enhances GPVI-mediated platelet procoagulant activity in a manner that may be more effectively reduced by P2YR antagonists and tyrosine kinase inhibitors compared to COX inhibitors.
- |||||||||| Review, Journal, Surgery: Can Anti-inflammatory Drugs used in Plastic Surgery Procedures Increase the Risk of Hematoma? (Pubmed Central) - Apr 5, 2023
Together, our results demonstrate that oxLDL enhances GPVI-mediated platelet procoagulant activity in a manner that may be more effectively reduced by P2YR antagonists and tyrosine kinase inhibitors compared to COX inhibitors. Based on available data, there is no significant risk of hematoma with use of anti-inflammatory drugs in plastic surgery.
- |||||||||| aspirin / Generic mfg., ibuprofen / Generic mfg.
Journal: Non-steroidal anti-inflammatory drugs as a targeted therapy for bone marrow failure in Ghosal Hematodiaphyseal Dysplasia. (Pubmed Central) - Apr 3, 2023 Mass spectrometry analysis demonstrated that urinary PG metabolites were increased along with proinflammatory lipoxygenase (LOX) products 5-Hydroxyeicosatetraenoic acid and leukotriene E4. Our data show that NSAIDs at standard doses surprisingly reduced both COX and LOX products, leading to the resolution of cytopenias, and should be considered for first-line treatment for Ghosal syndrome.
- |||||||||| indomethacin / Generic mfg.
Preclinical, Journal: Cuminaldehyde Effects in a MIA-Induced Experimental Model Osteoarthritis in Rat Knees. (Pubmed Central) - Mar 30, 2023 Cuminaldehyde was found to be as effective as indomethacin in reducing pain in all evaluated tests, including forced walking, functional disability of weight distribution on the legs, and spontaneous pain in animals with osteoarthritis...Its nociceptive activity occurs via central and peripheral mechanisms. Cuminaldehyde modulates the immune response of the inflammatory process and may be considered a leading compound for the development of new anti-inflammatory and analgesic drugs.
- |||||||||| paracetamol / Generic mfg.
Clinical, Journal: Combination Pharmacotherapy for Patent Ductus Arteriosus: Rationale and Evidence. (Pubmed Central) - Mar 27, 2023 Combination therapy with acetaminophen and ibuprofen is a novel strategy for PDA treatment in ELGANs, as it may facilitate higher ductal closure rates via additive action on two separate pathways inhibiting prostaglandin production...In this review, we examine the potential clinical impact of treatment failure in ELGANs with significant PDA, highlight the biological rationale in support of studying combination therapy, and review the randomized and non-randomized studies to date. With the rising number of ELGANs receiving neonatal intensive care, who are vulnerable to PDA-related morbidities, there is an urgent need for adequately powered clinical trials to systematically investigate the efficacy and safety of combination therapy for PDA treatment.
- |||||||||| Anaphylactic Shock With Ketorolac-rare Case (Walter E. Washington Convention Center, Area G, Hall C (Lower Level)) - Mar 25, 2023 - Abstract #ATS2023ATS_6107;
He was treated in ER for gastroenteritis with ondansetron, Pepcid and IV fluids and Ketorolac 15 mg IV for pain...He was given Benadryl, dexamethasone, 2L IVF, 0.5mg of IM epinephrine... Ketorolac anaphylactic shock is rare but life threatening and must be considered in all who receives it.
- |||||||||| ibuprofen / Generic mfg.
Journal: Expectant Management or Early Ibuprofen for Patent Ductus Arteriosus. (Pubmed Central) - Mar 20, 2023 P=N/A Expectant management for PDA in extremely premature infants was noninferior to early ibuprofen treatment with respect to necrotizing enterocolitis, bronchopulmonary dysplasia, or death at 36 weeks' postmenstrual age. (Funded by the Netherlands Organization for Health Research and Development and the Belgian Health Care Knowledge Center; BeNeDuctus ClinicalTrials.gov number, NCT02884219; EudraCT number, 2017-001376-28.).
- |||||||||| setanaxib (GKT831) / Calliditas
Journal: Food Restriction Augmented Alpha1-Adrenergic Mediated Contraction in Mesenteric Arteries. (Pubmed Central) - Mar 20, 2023 Augmentation of ?1-adrenergic-mediated contraction via the inhibition of the eNOS-NO pathway increased the activation of ROS through NOX2/4 in response to FR. Reduced eNOS-NO signaling may be a pathophysiological counterbalance to prevent hypovolemic shock in response to FR.
- |||||||||| Clinical, Preclinical, Journal: Disconnect between COX-2 selective inhibition and cardiovascular risk in preclinical models. (Pubmed Central) - Mar 16, 2023
In addition, the vascular ring model suggested possible adverse cardiovascular effects by COX-2 inhibitors, although these effects were not seen in vivo studies. These results may also suggest that COX-2 inhibition alone is not responsible for rofecoxib-mediated adverse cardiovascular outcomes.
- |||||||||| metformin / Generic mfg., bleomycin / Generic mfg.
Review, Journal, IO biomarker: Chemoprevention of oral cancer: A review and future perspectives. (Pubmed Central) - Mar 15, 2023 In the era of personalized medicine, future studies will focus on identifying specific biomarkers and molecular profile to monitor and to prevent malignant transformation. Larger trials are warranted to validate the effect of chemopreventive agents.
|