- |||||||||| Review, Journal: COX 2-inhibitors; a thorough and updated survey into combinational therapies in cancers. (Pubmed Central) - Jan 6, 2024
Additional studies and well-designed clinical trials are required to completely elucidate the efficacy of COX inhibition and combination therapy in enhancing cancer treatment outcomes. This narrative review study provides a detailed summary of COX-2 monotherapy and combination targeted therapy in cancer treatment.
- |||||||||| celecoxib oral / Generic mfg.
Journal: Design, synthesis, pharmacological evaluation, and in silico studies of the activity of novel spiro pyrrolo[3,4-d]pyrimidine derivatives. (Pubmed Central) - Jan 4, 2024
All compounds exhibit significant antiinflammatory activity, and they inhibited both COX-1 and COX-2 enzymes with a selectivity index higher than celecoxib as a reference drug...Our findings are promising in the area of medicinal chemistry for further optimization of the newly designed and synthesized compounds regarding the discussed structure-activity relationship study (SAR), in order to obtain a superior antioxidant lead compound in the near future. All chemical structures of the novel synthesized candidates were unequivocally elucidated and confirmed utilizing spectroscopic and elemental investigations.
- |||||||||| piroxicam / Generic mfg.
Journal: Preparation of Piroxicam nanosuspensions by high pressure homogenization and evaluation of improved bioavailability. (Pubmed Central) - Dec 22, 2023
The anti-inflammatory effect of PRX nanosuspension was also investigated in rabbits and it was observed that PRX nanosuspension treatment significantly improved the inhibition of COX-2 and NF?B expression as compared to the PRX treatment (p?<?0.05). The results in this study indicate that PRX nanosuspension is a promising nanomedicine for enhancing the anti-inflammatory activity of PRX and has a high potential for the treatment of inflammation.
- |||||||||| Review, Journal: Pyridazine derivatives as selective COX-2 inhibitors: A review on recent updates. (Pubmed Central) - Dec 18, 2023
This article summarizes some methods for the synthesis of pyridazine derivatives. Furthermore, it covers all of the pyridazine derivatives that have appeared as selective COX-2 inhibitors, making it useful as a reference for the rational design of novel selective COX-2 inhibitors.
- |||||||||| glibenclamide / Generic mfg., indomethacin / Generic mfg., Farxiga (dapagliflozin) / Ono Pharma, AstraZeneca
Preclinical, Journal: Investigating the Cardiovascular Benefits of Dapagliflozin: Vasodilatory Effect on Isolated Rat Coronary Arteries. (Pubmed Central) - Dec 17, 2023
The application of a Ca-activated K channel (K) blocker (TEA, 2 mM), voltage-dependent K channel (K) blocker (4-AP, 2 mM), ATP-sensitive K channel blocker (K) glibenclamide (3 ?M), and inward-rectifier K channel (K) blocker (BaCl, 30 ?M) did not affect the dapagliflozin-induced vasodilation either...In the present study, we found that dapagliflozin has a significant vasodilatory effect on rat coronary arteries. Our findings suggest a novel pharmacologic approach for the treatment of cardiovascular diseases in diabetic patients through the modulation of Ca homeostasis via dapagliflozin administration.
- |||||||||| aspirin / Generic mfg.
Journal: BmPxt1 mediated immune response by regulating PGE in silkworm, Bombyx mori. (Pubmed Central) - Dec 17, 2023
Hemocyte-spreading, nodule formation, phenoloxidase (PO) and AMP genes (attacin, defencin and moricin) were also inhibited by aspirin, a COX inhibitor...Injection of recombinant BmsPxt1 into larvae resulted in increased transcript levels of AMP genes. Our results confirmed that BmPxt1 was involved in the synthesis of PGs in the innate immune response of silkworm larvae, and provided new information for the role of BmsPxt1 secreted by silkworm in activating PO and antimicrobial peptides.
- |||||||||| Review, Journal: Diclofenac for acute postoperative pain in children. (Pubmed Central) - Dec 17, 2023
Healthcare providers should weigh the benefits and risks based on what is known of their respective pharmacological effects, rather than known efficacy. For surgical interventions in which bleeding or nausea and vomiting are a concern postoperatively, the risks of adverse events using opioids or diclofenac for managing pain should be considered.
- |||||||||| aspirin / Generic mfg., rofecoxib (TRM-201) / Tremeau Pharma
Journal: Inhibition of endogenous nitric oxide activity impairs the colonic sparing effect of rofecoxib, the cyclooxygenase-2 inhibitor and resveratrol, the preferential cyclooxygenase-1 inhibitor in the course of experimental colitis. Role of oxidative stress biomarkers and proinflammatory cytokines. (Pubmed Central) - Dec 17, 2023
levels, SOD activity and GSH content exerted by NO-ASA- or L-arginine treatment of the respective control TNBS-rats without L-NNA administration. These observations suggest that 1) the increase of NO availability either from NO-releasing donors such as NO-ASA or NO precursors such as L-arginine, can inhibit the inflammatory and microvasculature alterations, as well as increase in lipid peroxidation due to the enhanced efficacy of these compounds to increase the antioxidative properties of colonic mucosa, 2) unlike ASA which exacerbated the severity of colitis, the treatment with rofecoxib, the specific 'safer' COX-2 inhibitor or resveratrol, the polyphenolic compound known to act as the dual COX-1 and COX-2 inhibitor, can attenuate the colonic damage during course of TNBS colitis possibly via anti-inflammatory and antioxidative properties, and 3) the blockade of endogenous NO activity by L-NNA which also exacerbated the severity of mucosal damage in colitis, can abolish the sparing effect of rofecoxib and resveratrol indicating the NO bioavailability plays an important role in enhanced efficacy of both specific and dual COX inhibitors to ameliorate the experimental colitis.
- |||||||||| naproxen (IP 890) / Iroko
Journal: Investigation of Gold Nanoparticle Naproxen-Derived Conjugations in Ovarian Cancer. (Pubmed Central) - Dec 13, 2023
The proposed system demonstrated an increased chemotherapeutic effect than the free drug counterparts with at least 5 times lower IC50 values. NDC@AuNP nanosystems induced higher apoptosis rates, which established a simple and novel way to investigate activity of prospective drugs in drug discovery research.
- |||||||||| indomethacin / Generic mfg.
Journal: Supramolecular nanofiber of indomethacin derivative confers highly cyclooxygenase-2 (COX-2) selectivity and boosts anti-inflammatory efficacy. (Pubmed Central) - Dec 5, 2023
Moreover, a rabbit model of endotoxin-induced uveitis (EIU) reveals that the Idm-Nal-Nal-Asp hydrogel outperforms clinically used 0.1?wt% diclofenac sodium eye drops in terms of in vivo anti-inflammatory efficacy via topical instillation route. As a rational approach to designing and applying COX-2 selective inhibitors, this work presents a simple method for converting non-selective nonsteriodal anti-inflammatory drugs (NSAIDs) into highly selective COX-2 inhibitors that can self-assemble into supramolecular hydrogel for anti-inflammation applications.
- |||||||||| Vampex (carbenoxolone gel) / York Pharma
Journal: Roles of endothelial prostaglandin I in maintaining synchronous spontaneous Ca transients in rectal capillary pericytes. (Pubmed Central) - Dec 4, 2023
As a rational approach to designing and applying COX-2 selective inhibitors, this work presents a simple method for converting non-selective nonsteriodal anti-inflammatory drugs (NSAIDs) into highly selective COX-2 inhibitors that can self-assemble into supramolecular hydrogel for anti-inflammation applications. Spontaneous Ca transients arising from endoplasmic reticulum Ca release were synchronously developed amongst capillary pericytes in a gap junction blocker (3
- |||||||||| dasatinib / Generic mfg., celecoxib oral / Generic mfg.
Journal: New pyrazolyl-thiazolidinone/thiazole derivatives as celecoxib/dasatinib analogues with selective COX-2, HER-2 and EGFR inhibitory effects: design, synthesis, anti-inflammatory/anti-proliferative activities, apoptosis, molecular modelling and ADME studies. (Pubmed Central) - Dec 1, 2023
= 2.72) and doxorubicin (S.I?=?3.88). Derivatives 16a, 18c, 18d, 18f inhibit EGFR and HER-2 IC50 for EGFR of 0.043, 0.226, 0.388, 0.19??M respectively and for HER-2 of 0.032, 0.144, 0.195, 0.201??M respectively.
- |||||||||| indomethacin / Generic mfg.
Preclinical, Journal: Role of CB1 Cannabinoid Receptors in Vascular Responses and Vascular Remodeling of the Aorta in Female Mice. (Pubmed Central) - Nov 29, 2023
Vascular effects of phenylephrine (Phe), angiotensin II, acetylcholine (Ach) and estradiol (E2) were obtained and repeated with inhibitors of nitric oxide synthase (NOS, N?-nitro-L-arginine) and of cyclooxygenase (COX, indomethacin)...CBR KO female mice are characterized by increased vasorelaxation associated with increased utilization of endothelial NO and a decreased impact of constrictor prostanoids. Our results indicate that the absence or inhibition of CBRs may have beneficial vascular effects.
- |||||||||| indomethacin / Generic mfg., thalidomide / Generic mfg., carbamazepine / Generic mfg.
Preclinical, Journal: In vivo analgesic activity of new N-arylphthalimides derivatives in mice. (Pubmed Central) - Nov 27, 2023
Our results indicate that the absence or inhibition of CBRs may have beneficial vascular effects. This information may be useful in the development of a more potent phthalimide as an analgesic agent that acts as a sodium channel blocker and COX inhibitor.
- |||||||||| indomethacin / Generic mfg.
Preclinical, Journal: Deficiency of long-chain acyl-CoA synthetase 4 leads to lipopolysaccharide-induced mortality in a mouse model of septic shock. (Pubmed Central) - Nov 24, 2023
The increased mortality observed in LPS-treated Acsl4 KO mice was significantly improved by treatment with the general cyclooxygenase inhibitor indomethacin with a partial reduction in the severity of illness index for hypothermia, diarrhea score, and intestinal permeability. These results suggest that ACSL4 deficiency enhances susceptibility to endotoxin at least partly through the overproduction of cyclooxygenase-derived eicosanoids.
- |||||||||| etoricoxib / Generic mfg.
Journal: Etoricoxib enhances aryl hydrocarbon receptor activity. (Pubmed Central) - Nov 20, 2023
Etoricoxib has a synergistic effect on ITE-induced CYP1A1 expression in human cells. The effect of etoricoxib on AhR and ITE on endothelial cells and cardiomyocytes should be further elucidated to in hope to clarify the mechanism of increased cardiovascular events in COX-2 inhibitors and etoricoxib.
- |||||||||| Miostat (carbachol) / Novartis
Preclinical, Journal: Assessment of In Vitro Airway Smooth Muscle Relaxant Activity of Rhus coriaria L. Fruit Ethanolic Extract and Its Possible Mechanisms. (Pubmed Central) - Nov 10, 2023
The direct relaxant effect of RCE (0.1-0.7?mg/mL) was tested in the rat bronchi and trachea rings precontracted by carbachol (CCh)...In addition, the cyclooxygenase inhibitor indomethacin and the nitric oxide synthase inhibitor N(G)-nitro-l-arginine methyl ester (L-NAME), respectively, were used for exploring the mechanisms of RCE-induced relaxation and reduction of reactivity...In summary, we have shown that RCE displayed relaxant activities in the in vitro airway smooth muscles, and the possible mechanisms seems to involve the prostaglandin, nitric oxide, and Ca pathways. Taken together, our findings indicate the potential role of RCE in the treatment of respiratory diseases with limited airflow, or obstructive respiratory diseases, and could justify its traditional use in the respiratory diseases.
- |||||||||| Preclinical, Journal: Endothelium-Independent Vasorelaxant Effects of Sudachitin and Demethoxysudachitin, Polymethoxyflavone from the Peel of Citrus sudachi on Isolated Rat Aorta. (Pubmed Central) - Nov 5, 2023
Both the adenylate cyclase activator forskolin- and soluble guanylate cyclase activator sodium nitroprusside-induced relaxant effects were potentiated by preincubation of sudachitin...Phosphodiesterase inhibitors (3-isobutyl-1-methylxanthine, cilostamide or sildenafil) alone, sudachitin alone, and a combination of phosphodiesterase inhibitors with sudachitin exhibited relaxant effects, while the lack of any interaction between each phosphodiesterase inhibitor and sudachitin indicated an additive effect between the two substance categories. These results suggest that sudachitin and demethoxysudachitin cause endothelial-independent relaxation, and that the mechanism of vasorelaxation by sudachitin is associated with the enhancement of cAMP- and guanosine 3',5'-cyclic monophosphate (cGMP)-dependent pathways.
- |||||||||| celecoxib oral / Generic mfg.
Journal: Bioequivalence of Celecoxib Capsules in Chinese Healthy Volunteers. (Pubmed Central) - Nov 3, 2023
The main pharmacokinetic parameters were logarithmically converted and analyzed for variance. The 90% confidence interval for the bioavailability of the T compared to the R was calculated using maximum drug plasma concentration, area under the plasma concentration-time curve from time zero to the last quantifiable concentration point, and area under the plasma concentration-time curve from time zero to infinity for a single oral dose in volunteers, and the data obtained were all between 80% and 125%, indicating that the T and R have bioequivalence and good safety during fasting and fed administration.
- |||||||||| Journal: Biological Evaluation of Xanthene and Thioxanthene Derivatives as Antioxidant, Anticancer, and COX Inhibitors. (Pubmed Central) - Oct 24, 2023
Nevertheless, additional research is necessary to create more analogues, develop a more distinct comprehension of the structure-activity relationship (SAR), and perform in vivo experiments to evaluate the pharmacokinetic and pharmacodynamic characteristics of the compounds under examination. Such research may pave the way for the development of novel therapeutic agents with potential applications in cancer and inflammatory diseases.
- |||||||||| Tectin (tetrodotoxin) / CK Life Sci
Preclinical, Journal: Regional characterisation of TRPV1 and TRPA1 signalling in the mouse colon mucosa. (Pubmed Central) - Oct 22, 2023
Antagonism of the calcitonin gene-related peptide (CGRP) receptor had no effect on mucosal TRPV1 signalling, while tetrodotoxin and antagonists of the 5-hydroxytryptamine-3 and 4 receptors, CGRP receptor, and EP1/2/3 receptors had no effect on mucosal TRPA1 signalling. Our data demonstrates the regional-specificity and side-dependence of colonic TRPV1 and TRPA1 signalling, with involvement of submucosal neurons and mediation by epithelial NK1 receptor activation for TRPV1, and endogenous prostaglandins and EP4 receptor activation for TRPA1 mucosal responses.
- |||||||||| Journal: EP2 inhibition restores myeloid metabolism and reverses cognitive decline. (Pubmed Central) - Oct 2, 2023
Studies suggest that inhibition of EP2 restores age-associated spatial memory deficits and synaptic proteins and impairs tumorigenesis. The data indicate that EP2 signaling is important in myeloid cell metabolism and support its candidacy as a therapeutic target.
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