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78 Companies | 115 Products |
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- || Clinical, Review, Journal: Cyclooxygenase Inhibition Safety and Efficacy in Inflammation-Based Psychiatric Disorders. (Pubmed Central) - Apr 7, 2021
In this review, a broad overview of the use of COX inhibitors in the treatment of inflammation-based psychiatric disorders is provided. For this purpose, a critical analysis of the use of COX inhibitors in the last ten years of clinical trials of the major psychiatric disorders was carried out.
- | CBT-1 (tetrandrine) / CBA Pharma
Journal: Antibacterial and COX-2 Inhibitory Tetrahydrobisbenzylisoquinoline Alkaloids from the Philippine Medicinal Plant Phaeanthus ophthalmicus. (Pubmed Central) - Apr 7, 2021
A limited number of drugs with COX-2 inhibitory properties like celecoxib also confer antibacterial activity. Thus, tetrahydrobisbenzyl alkaloids, especially 2, are promising pharmaceutical inspirations for developing treatments of bacterial/inflammation-related infections.
- [VIRTUAL] TREATMENT PATTERNS AND CLINICAL CHARACTERISTICS OF PATIENTS WITH OSTEOARTHRITIS OF THE HIP AND/OR KNEE TREATED WITH TRADITIONAL NSAIDS VS COX-2S: A REAL-WORLD STUDY OF COMMERCIALLY-INSURED PATIENTS (Room 6) - Apr 6, 2021 - Abstract #EULAR2021EULAR_1864;
However, patients who start treatment with topical tNSAIDs switch to other types of NSAIDs; oral tNSAIDs were the most frequently prescribed treatment across the cohorts. Thus, despite the safety concerns with oral tNSAIDs and COX-2s, patients are still placed on these treatments to manage their OA pain.
- | ibuprofen / Generic mfg.
Journal: Polygalactan from bivalve Crassostrea madrasensis attenuates nuclear factor-κB activation and cytokine production in lipopolysaccharide-activated macrophage. (Pubmed Central) - Apr 2, 2021
Western blot experiment revealed that the polygalactan attenuated the migration of nuclear factor-κB-p to the nucleus from cytoplasm, and suppressed the phosphorylation of α-subunit of κB inhibitor. Greater selectivity index of sulfated polygalactan (3.93) towards inducible cyclooxygenase-2 as compared with the anti-inflammatory agent ibuprofen (1.11), and the potential to inhibit nuclear factor-κB cascade to generate chemokine production manifested its utilization in the development of functional food attenuating inflammation-related disorders.
- | Journal: Inhibiting Mitochondrial Cytochrome c Oxidase Downregulates Gene Transcription After Traumatic Brain Injury in Drosophila. (Pubmed Central) - Apr 2, 2021
Inhibiting COX by exposure to NIR downregulates gene expression in injured females but has minimal effect in injured males. Our results suggest that mitochondrial COX modulation with NIR alters gene expression in Drosophila following TBI and the response to injury and NIR exposure varies by biological sex.
- | aspirin / Generic mfg.
Journal: Aspirin for the prevention and treatment of preeclampsia: a matter of COX-1 and/or COX-2 inhibition? (Pubmed Central) - Mar 30, 2021
Therefore, we conclude that more functional and biochemical tests are needed to unravel the contribution of prostanoids in the mechanisms implicated in the pathogenesis of preeclampsia and the potential of dual COX and/or selective COX-2 inhibition for the prevention and treatment of preeclampsia. This information is vital if we are to deduce the suitability, optimal timing and dose of aspirin and/or a specific COX-2 inhibitor (most likely using modified forms that do not cross the placenta) that can then be tested in a randomised, controlled trial instead of the current practice of empirical dosing regimens.
- | Journal: Discrimination of Naturally-Occurring 2-Arylbenzofurans as Cyclooxygenase-2 Inhibitors: Insights into the Binding Mode and Enzymatic Inhibitory Activity. (Pubmed Central) - Mar 30, 2021
A three-dimensional quantitative activity-structure relationship (3D-QSAR) was also demonstrated, which showed some crucial structural requirements for enhanced enzyme inhibition. Therefore, four hits are proposed as lead structures for the development of COX-2 inhibitors based on 2-arylbenzofurans in further studies.
- | meloxicam / Generic mfg.
Journal: Synthesis, Cyclooxygenases Inhibition Activities and Interactions with BSA of N-substituted 1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones Derivatives. (Pubmed Central) - Mar 27, 2021
The intrinsic fluorescence of BSA was quenched by tested compounds due to the formation of A/E-BSA complex. The results of the experiment and molecular docking confirmed the main interaction forces between studied compounds and BSA were hydrogen bonding and van der Waals force.
- | dizocilpine (MK801) / Merck (MSD)
Journal: Pharmacological evaluation underlying the antinociceptive activity of 2 new hybrids NSAIDs tetrahydropyran derivatives. (Pubmed Central) - Mar 26, 2021
In summary, hybrid compounds presented central antinociceptive effect, demonstrating participation of the NO-cGMP-K ATP pathway, κ-opioid and NMDA receptors. In addition the compounds showed inhibition of cyclooxygenase enzymes and adverse effects were not observed with dose 300 times greater than the dose used experimentally.
- | Nimi-Rapitab (nimesulide) / Shreya Life Sciences
Preclinical, Journal: Vasodilatory effects of cannabidiol in human pulmonary and rat small mesenteric arteries: modification by hypertension and the potential pharmacological opportunities. (Pubmed Central) - Mar 25, 2021
The CBD effect in rats was CB1-sensitive and dependent on the hypertension model. Thus, modification of CBD-mediated responses in disease should be considered when CBD is used for therapeutic purposes.
- | indomethacin / Generic mfg., propranolol / Generic mfg.
Preclinical, Journal: Underlying mechanism of vasorelaxant effect exerted by 3,5,7,2',4'-pentahydroxyflavone in rats aortic ring. (Pubmed Central) - Mar 25, 2021
It was also found to be able to reduce the intracellular calcium level by blocking VOCC and calcium intake from the extracellular environment and the intracellular release of calcium from the sarcoplasmic reticulum. The present study showed that the vasorelaxant effect of morin potentially involves the NO/sGC, muscarinic receptors, β-adrenegic receptors, and calcium channels.
- || Clinical, Journal: Use of cyclooygenase inhibitor and the risk of hepatocellular carcinoma in patients with chronic hepatitis B: a nested case-control study using a nationwide population-based data. (Pubmed Central) - Mar 23, 2021
The adjusted ORs were 0.75 (95% CI: 0.63-0.90), 0.41 (95% CI: 0.31-0.56), 0.38 (95% CI: 0.25-0.57), and 0.49 (95% CI: 0.31-0.79) for the 28-90, 91-180, 181-360, and >360 cDDDs, respectively (p<0.001In conclusion, the use of COX inhibitors was associated with a reduced risk of HCC in CHB. COX-inhibitor may have a chemopreventive role in HCC development in patients with chronic liver disease.
- | indomethacin / Generic mfg.
Preclinical, Journal: COX Inhibition Increases Alternaria-Induced Pulmonary Group 2 Innate Lymphoid Cell Responses and IL-33 Release in Mice. (Pubmed Central) - Mar 23, 2021
Mice were treated with the COX inhibitors indomethacin, flurbiprofen, or vehicle and challenged intranasally with Alternaria extract for four consecutive days to induce innate lung inflammation...This is supported by the in vitro finding that the COX product PGE and the PGI analogs cicaprost decreased Alternaria extract-induced IL-33 release by human bronchial epithelial cells. Although contrasting effects of PGD, PGE, and PGI on ILC2 responses have been previously reported, the overall effect of the COX pathway on ILC2 function is inhibitory in Alternaria-induced innate airway inflammation.
- | Journal: Deciphering the Pharmacological Mechanisms of Guizhi-Fuling Capsule on Primary Dysmenorrhea Through Network Pharmacology. (Pubmed Central) - Mar 23, 2021
Consequently, GZFLC presented pain relief and sustained benefits for primary dysmenorrhea. This study could provide a scientific approach for deciphering pharmacological mechanisms of herbal formulae through network pharmacology.
- | Journal: Inhibition of cyclooxygenase by blocking the reducing cosubstrate at the peroxidase site: discovery of galangin as a novel cyclooxygenase inhibitor. (Pubmed Central) - Mar 20, 2021
Further experimental studies confirm that galangin can inhibit, both in vitro and in vivo, quercetin-mediated activation of the peroxidase activity of the COX-1/2 enzymes. The results of the present study demonstrate that galangin is a novel naturally-occurring inhibitor of COX-1 and COX-2, acting by blocking the function of the reducing cosubstrates at the peroxidase sites.
- | Journal: The fatty acid amide hydrolase and cyclooxygenase-inhibitory properties of novel amide derivatives of carprofen. (Pubmed Central) - Mar 19, 2021
Both compounds inhibited the cyclooxygenation of arachidonic acid by ovine COX-1, and were more potent inhibitors of human recombinant COX-2 when 2-arachidonoylglycerol was used as substrate than when arachidonic acid was used. It is concluded that Carpro-AM1 and Carpro-AM6 are dual-acting FAAH/substrate-selective COX inhibitors.
- | aspirin / Generic mfg.
Journal: PGE deficiency predisposes to anaphylaxis by causing mast cell hyper-responsiveness. (Pubmed Central) - Mar 18, 2021
Homeostatic levels of PGE attenuate MC activation via EP2/EP4 and protect against ANA. Relative deficiency of PGE predisposes to ANA in humans and mice, while PGE stabilization protects against anaphylactic reactions.
- | meloxicam / Generic mfg.
Journal: Design, Synthesis and Comprehensive Investigations of Pyrrolo[3,4-d]pyridazinone-Based 1,3,4-Oxadiazole as New Class of Selective COX-2 Inhibitors. (Pubmed Central) - Mar 16, 2021
Moreover, all derivatives reduce the increased level of reactive oxygen and nitrogen species and prevent DNA strand breaks caused by oxidative stress. Finally, performed spectroscopic and molecular docking studies demonstrated that new compound interactions with bovine serum albumin (BSA) are moderate, formation of complexes is in one-to-one ratio, and binding site II (subdomain IIIA) is favorable.
- || Review, Journal: Current Controversy on Platelets and Patent Ductus Arteriosus Closure in Preterm Infants. (Pubmed Central) - Mar 16, 2021
However, these platelet effects on PDA seem to be of only moderate clinical significance. Furthermore, platelet transfusions in thrombocytopenic preterm infants in order to facilitate PDA closure appear to cause more harm than good.
- indomethacin / Generic mfg.
[VIRTUAL] APELIN/AJP SYSTEM PROTECTS THE GASTRIC MUCOSA AGAINST ISCHEMIA-REPERFUSION INJURY VIA ACTIVATION OF CNOS/NO SYSTEM, SENSORY NEUROPEPTIDES AND SUPPRESSION OF OXIDATIVE STRESS (DDW Virtual) - Mar 15, 2021 - Abstract #DDW2021DDW_4441;
We determined the effect of intraperitoneal (i.p.) treatment with apelin-13 with or without the concomitant treatment with AJP antagonist ML221 (10 - 100 µg/kg i.p.) against ischemia-reperfusion (I/R)-induced gastric mucosal lesions induced by clamping of celiac artery for 30 min (ischemia) followed by release of the clamp to allow for 3 h of reperfusion (I/R) and accompanying changes in the gastric blood flow (GBF) in rats pretreated with L-NAME (5 mg/kg i.g.) to inhibit NO-synthase, 2) indomethacin (2 mg/kg i.g.) to suppress PG-COX-1 pathway and 3) capsaicin (125 mg/kg s.c.) to induce functional ablation of sensory nerves...The increase in mRNA expression of IL-6, IL-1, TNF-α, HIF-1α, Nrf2, HO-1 in gastric mucosa of I/R rats was inhibited by apelin while the upregulation of cNOS and CGRP mRNA was observed in apelin-pretreated rats exposed to I/R, this latter effect being inhibited in ML221-dependent manner. We conclude that 1) apelin/APJ signaling suppresses the formation of gastric mucosal I/R injury by enhancement in gastric microcirculation, downregulation of proinflammatory cytokines and biomarkers and by inhibition of lipid peroxidation and oxidative stress induced by I/R, and 2) apelin-induced gastroprotection is possibly mediated by NO and sensory neuropeptides but seems to be independent from PG/COX biosynthetic pathway.
- hydrogen sulfide-releasing derivative of ketoprofen (ATB-352) / Antibe
[VIRTUAL] IMPACT OF NOVEL HYDROGEN SULFIDE-RELEASING KETOPROFEN (ATB-352) ON MOLECULAR PATHWAYS AND MICROBIOME PROFILE IN GASTROINTESTINAL (GI) TRACT WITH POSSIBLE DEVELOPMENT OF GI-SAFE POLYPHARMACY WITH OTHER NON-STEROIDAL ANTI-INFLAMMATORY DRUGS (NSAIDS) (DDW Virtual) - Mar 15, 2021 - Abstract #DDW2021DDW_3519;
We conclude that GI-safety of H2S-releasing ketoprofen does not require polypharmacy with PPIs and involves maintenance of intestinal microbiota profile and HMOX-1, CREB and SOCS3 pathways activation. [
- aspirin / Generic mfg.
[VIRTUAL] Glucagon-Like Peptide-1 Receptor Agonists Decrease Platelet-Mediated Airway Inflammation () - Mar 14, 2021 - Abstract #ATS2021ATS_2564;
GLP-1RAs are already U.S. Food and Drug Administration-approved for the treatment of type 2 diabetes mellitus and obesity. Prospective study of the impact of GLP-1RAs in human asthma phenotypes is warranted.
- | aspirin / Generic mfg., indomethacin / Generic mfg., celecoxib oral / Generic mfg.
Journal: Effects of COX Inhibitors on Responsiveness of the Tracheal Tract to Acetylcholine and Histamine and their Relationship with LTC4 and PGE2 Levels of Bronchoalveolar Lavage Fluid in Allergic Guinea Pigs. (Pubmed Central) - Mar 13, 2021
Inflammatory cells including eosinophils and neutrophils corresponded to the changes observed for each treatment group. Ketoprofen and indomethacin increased the tracheal sensibility to Ach and His; therefore, their administration is not recommended in patients susceptible to allergy.
- | Preclinical, Journal: Valuing Bioactive Lipids from Green, Red and Brown Macroalgae from Aquaculture, to Foster Functionality and Biotechnological Applications. (Pubmed Central) - Mar 12, 2021
Ulva rigida, C. tomentosum, P. palmata and P. dioica inhibited COX-2 activity by up to 80%, while P. dioica and P. palmata extracts showed the highest cytotoxic potential in the MDA-MB-231 breast cancer cells. This work enhances the valorization of macroalgae as functional foods and promising ingredients for sustainable and healthy diets and fosters new applications of high-valued algal biomass, in a species-specific context.
- | Journal: Laser light as a promising approach to improve the nutritional value, antioxidant capacity and anti-inflammatory activity of flavonoid-rich buckwheat sprouts. (Pubmed Central) - Mar 12, 2021
Also, laser light boosted the antioxidant capacity and anti-inflammatory activities through inhibiting cyclooxygenase-2 and lipoxygenase activities, particularly in TBW sprouts. Accordingly, laser light could be recommended as a promising method to improve the nutritional and health-promoting values of buckwheat sprouts.
- MCI-030 / ChemomAb
[VIRTUAL] PDE10A as a novel target to suppress Wnt/β-catenin signaling and other oncogenic pathways in ovarian cancer () - Mar 11, 2021 - Abstract #AACR2021AACR_797;
Our data demonstrate that PDE10A has pro-tumorigenic effects in ovarian cancer cells and its high expression in ovarian cancer patients is associated with poor prognosis. Altogether, our results warrant future studies of PDE10A as a novel target for ovarian cancer chemoprevention and/or treatment.
- | Journal: Kirenol, darutoside and hesperidin contribute to the anti-inflammatory and analgesic activities of Siegesbeckia pubescens Makino by inhibiting COX-2 expression and inflammatory cell infiltration. (Pubmed Central) - Mar 11, 2021
Altogether, our results warrant future studies of PDE10A as a novel target for ovarian cancer chemoprevention and/or treatment. ESM and its active ingredients can effectively attenuate the expression of inflammatory factors induced by chemical inflammation, prevent the infiltration of inflammatory cells, and exert good anti-inflammatory and antinociceptive activities.
- || indomethacin / Generic mfg., celecoxib oral / Generic mfg.
Clinical, Journal: New pyrazole derivatives possessing amino/methanesulphonyl pharmacophore with good gastric safety profile: Design, synthesis, cyclooxygenase inhibition, anti-inflammatory activity and histopathological studies. (Pubmed Central) - Mar 9, 2021
The obtained ulcerogenic liability data revealed the gastric safety of these derivatives which was confirmed by the histopathological studies. Docking study was performed for all synthesized derivatives to explain their interaction with COX-2 receptor active site.
- | meloxicam / Generic mfg.
Journal: Design, synthesis, biological evaluation and in silico studies of novel pyrrolo[3,4-d]pyridazinone derivatives withpromising anti-inflammatory and antioxidant activity. (Pubmed Central) - Mar 9, 2021
Moreover, every examined derivative of pyrrolo[3,4-d]pyridazinone demonstrates better inhibitory activity towards COX-2 and a superior COX-2/COX-1 selectivity ratio compared to the reference drug meloxicam...Finally, a study of the binding mechanism between compounds 7a,b-13a,b and bovine serum albumin (BSA) was carried out. According to spectroscopic and molecular docking studies, all examined derivatives interact with BSA, which suggests their potential long half-life in vivo.
- | meloxicam / Generic mfg.
Journal: New 1,3,4-Oxadiazole Derivatives of Pyridothiazine-1,1-Dioxide with Anti-Inflammatory Activity. (Pubmed Central) - Mar 9, 2021
TG12 was, in turn, a non-selective COX inhibitor. A molecular docking study was performed to understand the binding interaction of compounds at the active site of cyclooxygenases.
- | Journal: Morel mushroom, Morchella from Kashmir Himalaya: a potential source of therapeutically useful bioactives that possess free radical scavenging, anti-inflammatory, and arthritic edema-inhibiting activities. (Pubmed Central) - Mar 9, 2021
HPTLC analysis revealed that EAE is composed of several chemical components. The mushroom is a source of therapeutically useful functional food that can provide relief in arthritis.
- || pregabalin / Generic mfg.
Review, Journal: Narrative review of acute post-craniotomy pain. Concept and strategies for prevention and treatment of pain. (Pubmed Central) - Mar 6, 2021
Performing a scalp block prior to surgical incision or after surgery, the use of intraoperative dexmedetomidine, and the perioperative administration of pregabalin are just some alternatives that are gaining ground. The management of post-craniotomy pain should be based on perioperative multimodal analgesia in the framework of an "enhaced recovery after surgery" (ERAS) approach.
- || aspirin / Generic mfg.
Review, Journal: Mechanisms of Colorectal Cancer Prevention by Aspirin-A Literature Review and Perspective on the Role of COX-Dependent and -Independent Pathways. (Pubmed Central) - Mar 5, 2021
We suggest that the preferential chemopreventive effect of aspirin against CRC may be related to direct exposure of aspirin/salicylic acid or its metabolites to the colorectal tissues. Future investigations should shed light on the role of aspirin, its metabolites and the role of the gut microbiota in cancer prevention against CRC.
- | Cognex (tacrine) / Shionogi
Journal: Synthesis, biological evaluation and modeling of hybrids from tetrahydro-1H-pyrazolo[3,4-b]quinolines as dual cholinestrase and COX-2 inhibitors. (Pubmed Central) - Mar 4, 2021
Furthermore, their anti-inflammatory activity using in vitro (COX-1/COX-2) inhibitory assay demonstrated superior activity to celecoxib with higher selectivity indices for some compounds...In conclusion, this work provides an extension of the chemical space of tetrahydro-1H-pyrazolo[3,4-b]quinoline chemotype for the anticholinestrase and anti-inflammatory activity. This would aid to minimize the possible neuroinflammation linked to the pathogenesis of Alzheimer's disease.
- | Journal: Synthesis and anti-hepaticfibrosis of glycyrrhetinic acid derivatives with inhibiting COX-2. (Pubmed Central) - Mar 3, 2021
Thirdly, for the rats which induced with (carbontetrachloride) CCl, the symptoms of liver fibrosis in rats were significantly alleviated after successive administration the tested compound for 14d; the α-SMA level in liver tissue decreased in a concentration dependent manner; and the liver cell necrosis and the fat collagen fiber decreased significantly compared with the positive control group; furthermore, inflammatory infiltration was significantly lower than that of the control. This suggests the compounds possibly are candidates for hepatic fibrosis with promising application in clinic.
- | tezosentan (ACT-050089) / Roche
Preclinical, Journal: Effects of endothelin receptor blockade and COX inhibition on intestinal I/R injury in a rat model: Experimental research. (Pubmed Central) - Mar 3, 2021
This suggests the compounds possibly are candidates for hepatic fibrosis with promising application in clinic. It is suggested that NO-ASA, TS, and FLUR can be introduced as promising therapeutics to improve intestinal I/R injury.
- | indomethacin / Generic mfg.
Journal: The gastroprotective effect of red propolis extract from Northeastern Brazil and the role of its isolated compounds. (Pubmed Central) - Mar 3, 2021
The compounds MV and MD may have an essential role in the activity of HERP. Our data contribute to validate the traditional use of propolis for gastric disorders.
- | indomethacin / Generic mfg., celecoxib oral / Generic mfg.
Journal: New pyridazine derivatives as selective COX-2 inhibitors and potential anti-inflammatory agents; design, synthesis and biological evaluation. (Pubmed Central) - Mar 2, 2021
Furthermore, the selective COX-2 inhibitor 3g exhibited a superior gastrointestinal safety profile compared to the reference drugs celecoxib and indomethacin with less number of ulcers and milder ulcer score. The molecular docking study of this compound with COX-2 protein revealed more favorable binding mode compared to celecoxib, explaining its remarkable COX-2 inhibitory potency.
- | Journal: Characteristics of New Peptides GQLGEHGGAGMG, GEHGGAGMGGGQFQPV, EQGFLPGPEESGR, RLARAGLAQ, YGNPVGGVGH, and GNPVGGVGHGTTGT as Inhibitors of Enzymes Involved in Metabolic Syndrome and Antimicrobial Potential. (Pubmed Central) - Mar 2, 2021
Peptide RQ-9 was characterized by the highest COX inhibitory activity (0.31 and 4.77 µg/mL for COX-1 and COX-2, respectively). Only peptide RQ-9 inhibited S. enteritidis ATCC 4931 growth (42%-48%) in all tested concentrations (15.62-250 mg/mL).
- | naproxen / Generic mfg.
Journal: Synthesis and biological evaluation of RGD conjugated with Ketoprofen/Naproxen and radiolabeled with [Tc] via N4(GGAG) for αβ integrin-targeted drug delivery. (Pubmed Central) - Feb 27, 2021
Provided that NSAID drugs are conjugated to RGD, there will be a selective delivery to target tissues as well as synergetic anti-tumor effects which reduce systemic doses and toxicity. Graphical abstract.
- | Journal: Synthesis and Evaluation of New Coumarin Derivatives as Antioxidant, Antimicrobial, and Anti-Inflammatory Agents. (Pubmed Central) - Feb 27, 2021
Regarding the anti-inflammatory testing, pyranocoumarins 2b, 3a,b and 5c and coumarin-sulfonamide compound 9a showed more potent antiproteinase activity than aspirin in vitro; however, five compounds were as potent as aspirin...For in vitro COX-inhibitory activity of coumarin derivatives, pyranocoumarin derivative 5a was the most selective (SI = 152) and coumarin-sulfonamide derivative 8d was most active toward COX-2 isozyme. The most active derivatives met the in silico criteria for orally active drugs; thus, they may serve as promising candidates to develop more potent and highly efficient antioxidant, antimicrobial, and/or anti-inflammatory agents.
- | Preclinical, Journal: Mechanism of Huang-lian-Jie-du decoction and its effective fraction in alleviating acute ulcerative colitis in mice: Regulating arachidonic acid metabolism and glycerophospholipid metabolism. (Pubmed Central) - Feb 26, 2021
The most active derivatives met the in silico criteria for orally active drugs; thus, they may serve as promising candidates to develop more potent and highly efficient antioxidant, antimicrobial, and/or anti-inflammatory agents. Our experiments revealed that HLJDD and HLJDD-NBA can alleviate UC of mice by regulating arachidonic acid metabolism and glycerophospholipid metabolism, which points out the direction for further research and development of HLJDD as a new anti-ulcer drug.
- || Review, Journal: Herbal Medications Used to Treat Fever. (Pubmed Central) - Feb 26, 2021
In addition, herbs have known antipathogenic properties and can be effective in the treatment of infection from numerous microorganisms. Last, in traditional Chinese medicine, herbs are used to restore imbalances between the nonpathogenic and the pathogenic clearing interior heat and treating heat patterns in a variety of ways.
- | ibuprofen / Generic mfg., celecoxib oral / Generic mfg.
Journal, IO biomarker: New 1,2,4-triazole/pyrazole hybrids linked to oxime moiety as nitric oxide donor celecoxib analogs: Synthesis, cyclooxygenase inhibition anti-inflammatory, ulcerogenicity, anti-proliferative activities, apoptosis, molecular modeling and nitric oxide release studies. (Pubmed Central) - Feb 25, 2021
Regarding EGFR inhibition, docking was carried out with ID: 1M17. The internal oxime serious was more active as anticancer because of their ability to form extra HBs with receptor cleft.
- | Journal: Girinimbine from curry leaves promotes gastro protection against ethanol induced peptic ulcers and improves healing via regulation of anti-inflammatory and antioxidant mechanisms. (Pubmed Central) - Feb 25, 2021
In addition, significantly upregulated HSP70 and downregulated iNOS were observed in girinimbine treated rat tissue at both the transcriptional and translational level. Our results clearly indicated that girinimbine displayed a significant gastro-protection effect, via the capacity to inhibit inflammatory responses and antioxidant potential.
- | resiniferatoxin (MCP-101) / Sorrento
Journal: Involvement of TRPV1 and the efficacy of α-spinasterol on experimental fibromyalgia symptoms in mice. (Pubmed Central) - Feb 24, 2021
The reserpine-induced mechanical allodynia and the thermal hyperalgesia were abolished by TRPV1-positive fibers desensitisation induced by previous resiniferatoxin (RTX) administration. In summary, the TRPV1 channel is involved in the development and maintenance of nociception and depressive-like behaviours in a fibromyalgia model, while the α-spinasterol has therapeutic potential to treat the pain and depression symptoms in fibromyalgia patients.
- | Preclinical, Journal: Novel bisthiolane polysulfides from lachrymatory factor synthase-suppressed onion and their in vitro cyclooxygenase-1 inhibitory activity. (Pubmed Central) - Feb 24, 2021
On the basis of spectroscopic and mass spectrometric analyses, it was found that these bisthiolane polysulfides were bis(5-hydroxy-3,4-dimethylthiolan-2-yl)-tri/tetra/pentasulfide with the general formulas of CHOS (tri-), CHOS (tetra-) and CHOS (penta-), and they were confirmed to exist in authentic tearless onion juice. Thiolanotrisulfide (1) and thiolanotetrasulfide (2) inhibited cyclooxygenase-1 activity with IC values of 720 ± 78 and 464 ± 48 μM respectively, compared with 3282 ± 188 μM for aspirin.
- | Journal: Further insight into the dual COX-2 and 15-LOX anti-inflammatory activity of 1,3,4-thiadiazole-thiazolidinone hybrids: The contribution of the substituents at 5th positions is size dependent. (Pubmed Central) - Feb 23, 2021
Compounds 3a, 4r and 4q showed comparable in vivo anti-inflammatory activity to the reference drug (celecoxib)...Docking study was performed to explore the possible mode of interaction of the new compounds with the active site of human 15-LOX and COX-2. This study discloses some structural features for binding to 15-LOX and COX, thus pave the way to design anti-inflammatory agents with balanced dual inhibition of these enzymes.
- | Tyvaso (treprostinil) / United Therapeutics Corp
Journal: Characterisation of cough evoked by inhaled treprostinil and treprostinil palmitil. (Pubmed Central) - Feb 23, 2021
The mechanisms inducing cough with inhaled TRE likely involves the activation of prostanoid IP receptors on jugular C-fibres in the tracheobronchial airways. Cough induced by inhaled dry powder and nebulised formulations of TP occurs at higher inhaled doses than TRE, presumably due to the slow, sustained release of TRE from the prodrug resulting in lower concentrations of TRE at the airway sensory nerves.
- | Neforex (nefopam) / Incepta
Journal: Predicting Acute Pain After Surgery: A Multivariate Analysis. (Pubmed Central) - Feb 20, 2021
The presented analysis offers detailed insight into current practice patterns and reveals modifications that can be implemented in today's clinical practice. Our results also suggest that parameters other than those currently studied are relevant for postoperative pain including biological and psychological variables.