- |||||||||| Journal: Isolation, characterization and anti-inflammatory mechanism of probiotics in lipopolysaccharide-stimulated RAW 264.7 macrophages. (Pubmed Central) - Sep 23, 2020
Further, these selected LAB isolates reduced the level of pro-inflammatory cytokines, TNF-α, IL-1β and IL-6, inhibited the phosphorylation of Mitogen Activated Protein Kinases (MAPKs) i.e. p38 MAPK, ERK1/2 and SAPK/JNK and expression of cyclooxygenase-2 (COX-2) in LPS stimulated RAW 264.7 cells. The in vitro analysis suggested that the selected probiotic isolates attenuated the LPS-induced inflammation by downregulating MAPK pathway vis-a-vis inhibiting COX-2 and can be employed as anti-inflammatory agents in various inflammatory diseases.
- |||||||||| indomethacin / PLx Pharma Inc, Generic mfg.
Preclinical, Journal: Bothrops leucurus venom induces acute hypotension in rats by means of its phospholipase A (blD-PLA). (Pubmed Central) - Sep 10, 2020 These effects were partially counteracted by pre-treatment with indomethacin (cyclooxygenase inhibitor)...Taken together, our results show that, at low doses, the venom of B. leucurus induces transient, acute hypotension in anesthetized rats following systemic vasodilation in a dose-dependent way. In addition, we provide clear evidence of the involvement of the enzymatic activity of blD-PLA in this cardiovascular response, acting via the production of vasodilating prostanoids.
- |||||||||| indomethacin / PLx Pharma Inc, Generic mfg.
Preclinical, Journal: Targeting cyclooxygenase by indomethacin decelerates progression of acute lymphoblastic leukemia in a xenograft model. (Pubmed Central) - Sep 2, 2020 The progression was monitored by noninvasive in vivo imaging of the engrafted leukemic cells, as well as by analyses of CD19+CD10+ leukemic blasts present in spleen or bone marrow at the termination of the experiments. The indomethacin treatment increased the level of p53 in the leukemic cells, implying that COX inhibition might reduce progression of ALL by attenuating protective paracrine PGE2 signaling from bone marrow stroma to leukemic cells.
- |||||||||| celecoxib oral / Generic mfg.
Clinical, Journal: Anti-inflammatory compound shows therapeutic safety and efficacy against flavivirus infection. (Pubmed Central) - Sep 1, 2020 Furthermore, administering 5 mg/kg compound 2d to DENV-2-infected AG129 mice prolonged survival and reduced viremia and serum cytokine levels. Overall, compound 2d showed therapeutic safety and efficacy in vitro and in vivo and could be further developed as a potential therapeutic agent for flavivirus infection.
- |||||||||| indomethacin / PLx Pharma Inc, Generic mfg.
Journal: Gastroprotective effect of the alkaloid boldine: Involvement of non-protein sulfhydryl groups, prostanoids and reduction on oxidative stress. (Pubmed Central) - Sep 1, 2020 The gastroprotective effect of Boldine was evaluated on gastric ulcer induced by 60% ethanol/0.3 M HCl or indomethacin (100 mg/kg) in mice...Moreover, the alkaloid reduced oxidative stress and inflammatory mediators in ethanol-ulcerated tissue, beyond has increased mucin-like glycoprotein amount. Finally, Boldine effect is dependent on non-protein sulfhydryl groups and prostanoids but does not involve the inhibition of H+/K + -ATPase activity, being a promising natural resource for gastric ulcer treatment.
- |||||||||| clopidogrel / Generic mfg.
Preclinical, Journal: Disorders on cardiovascular parameters in rats and in human blood cells caused by Lachesis acrochorda snake venom. (Pubmed Central) - Aug 29, 2020 Acetylsalicylic acid (ASA, a cyclooxygenase inhibitor) or clopidogrel (an ADP receptor blocker) inhibited the aggregating effect of SVLa...Altogether, under experimental conditions, SVLa induced blood coagulation, platelet aggregation, hypotension and bradycardia. Part of the effects presented here may be explained by the presence of snake venom metalloproteinases (SVMPs) and snake venom serine proteases (SVSPs), constituents of SVLa.
- |||||||||| ibuprofen / Generic mfg.
Journal: Interplay between inflammation and neural plasticity: both immune activation and suppression impair LTP and BDNF expression. (Pubmed Central) - Aug 15, 2020 We tested this hypothesis experimentally, by acute treatment of C57BL/6 adult male mice with different doses of two inflammatory modulators: lipopolysaccharide (LPS), an endotoxin, and ibuprofen (IBU), a nonselective cyclooxygenase inhibitor, which are respectively a pro- and an anti-inflammatory agent...Such effect appears to be dose-dependent since only the higher, but not the lower, dose of both compounds led to a plasticity impairment. Overall, the present findings indicate that acute treatment with pro- and anti-inflammatory agents impair neural plasticity in a dose dependent manner.
- |||||||||| dexamethasone / Generic mfg.
Journal: Anti-Inflammatory Polymeric Nanoparticles Based on Ketoprofen and Dexamethasone. (Pubmed Central) - Aug 6, 2020 The RT-qPCR analysis shows that the ketoprofen nanoparticles were able to reduce to almost basal levels the expression of tested pro-inflammatory markers and increase the gene expression of anti-inflammatory cytokines under inflammatory conditions. However, the synergistic inhibition of Il12b observed in nanoparticles that combine dexamethasone and naproxen was not observed in nanoparticles that combine dexamethasone and ketoprofen, suggesting that the synergistic trans-repression of Il12b observed in the first case was not mediated by cyclooxygenase-dependent pathways.
- |||||||||| [VIRTUAL] Anti-Amyloidogenic and Cyclooxygenase Inhibitory Activity of Indigofera zollingeriana Miq () - Aug 2, 2020 - Abstract #AAIC2020AAIC_3417;
This offers a novel perspective for understanding the anti-inflammatory mechanism of CAI and suggests its potential use as a therapeutic treatment in inflammatory diseases with excessive macrophage activation. The results suggest that Indigofera zollingeriana Miq possesses anti-inflammatory and anti-neurodegenerative properties and a promising lead as a source of pharmacologically active compounds.
- |||||||||| indomethacin / PLx Pharma Inc, Generic mfg., Tectin (tetrodotoxin) / WEX
Journal: TRPA1 causes rapid bronchodilation via non-epithelial PGE. (Pubmed Central) - Jul 29, 2020 Finally, AITC blocked airway hyperreactivity in two animal models of allergic asthma. These data demonstrate that stimulation of TRPA1 causes bronchodilation of intact airways and suggest that the TRPA1 pathway is a potential pharmacologic target for bronchodilation.
- |||||||||| sulindac / Generic mfg.
Journal: Ellagic Acid Inhibits Extracellular Acidity-Induced Invasiveness and Expression of COX1, COX2, Snail, Twist 1, and c-myc in Gastric Carcinoma Cells. (Pubmed Central) - Jul 21, 2020 In addition, acidity increased the mRNA protein expression of transcription factors snail, twist1, and c-myc; these were also reduced by ellagic acid. Together, these results suggest that ellagic acid suppresses acidity-enhanced migration and invasion of gastric cancer cells via inhibition of the expression of multiple factors (COX1, COX2, snail, twist1, and c-myc); for this reason, it may be an effective agent for cancer treatment under acidosis.
- |||||||||| Preclinical, Journal: Inhibition of lipolysis: a novel explanation for the hypothermic actions of Acetaminophen in Non-Febrile Rodents. (Pubmed Central) - Jul 21, 2020
These novel observations combined with the known limited inhibition of the COX enzymes by acetaminophen suggest both the antipyretic and hypothermia induced by acetaminophen and related compounds could be attributed to the direct inhibition of lipolysis and mitochondrial function, rather than cyclooxygenase inhibition centrally. Further these observations could provide new drug targets for reducing fever with the added bonus of fewer individuals being hospitalized by accidental acetaminophen overdose.
- |||||||||| verapamil / Generic mfg.
Preclinical, Journal: Vasorelaxant effect of osthole on isolated thoracic aortic rings in rats. (Pubmed Central) - Jul 21, 2020 Further these observations could provide new drug targets for reducing fever with the added bonus of fewer individuals being hospitalized by accidental acetaminophen overdose. Osthole has a vasorelaxant effect on isolated rat thoracic aortic rings, via inhibition of both receptor-operated and voltage-dependent Ca2+ channels in arterial smooth muscle, leading to decreased Ca2+ influx, and via inhibition of nitric oxide release on arterial endothelial cells.
- |||||||||| celecoxib oral / Generic mfg.
Preclinical, Journal: Anti-nociceptive and Anti-inflammatory Activities of Asparacosin A Involve Selective Cyclooxygenase 2 and Inflammatory Cytokines Inhibition: An in-vitro, in-vivo, and in-silico Approach. (Pubmed Central) - Jul 16, 2020 However, in formalin test, Asparacosin A (10-40 mg/kg, p.o) produced anti-nociceptive effects only in the late phase, similar to the effect observed with the reference drug celecoxib (50 mg/kg, p.o)...In conclusion, Asparacosin A exhibits anti-inflammatory and peripheral anti-nociceptive activities which are likely mediated via inhibition of COX-2 enzyme and inflammatory cytokines. Furthermore, Asparacosin A can serve as a model to obtain new and more selective potent anti-inflammatory and anti-nociceptive drugs.
- |||||||||| ibuprofen / Generic mfg.
Journal: Ester coupling of ibuprofen in hydrogel matrix: a facile one-step strategy for controlled anti-inflammatory drug release. (Pubmed Central) - Jul 16, 2020 In particular, we tested the biological activity of cleaved ibuprofen in terms of cyclooxygenase inhibition, reporting that chemical tethering did not alter the efficiency of the NSAID. Moreover, due to the sol-gel transition of the hydrogel matrix, these ibuprofen-functionalized hydrogels could be used as injectable tools in several clinical scenarios, performing a localized drug release and opening advanced avenues for in situ treatments.
- |||||||||| aspirin / Generic mfg.
Journal: Cardiovascular Biology of Prostanoids and Drug Discovery. (Pubmed Central) - Jul 16, 2020 Substantial variation in clinical responses to aspirin exists and is associated with cardiovascular risk...mPGES-1-derived PGE critically regulates microcirculation via its receptor EP (receptor for prostanoid E) 4. This review summarizes the actions and associated mechanisms for modulating the biosynthesis of prostanoids in thrombosis, vascular remodeling, and ischemic heart disease as well as their therapeutic relevance.
- |||||||||| cisplatin / Generic mfg., methotrexate / Generic mfg., sulfasalazine / Generic mfg.
Clinical, Journal, Relative risk: Relative risk of end-stage renal disease requiring dialysis in treated ankylosing spondylitis patients compared with individuals without ankylosing spondylitis: A nationwide, population-based, matched-cohort study. (Pubmed Central) - Jul 16, 2020 This review summarizes the actions and associated mechanisms for modulating the biosynthesis of prostanoids in thrombosis, vascular remodeling, and ischemic heart disease as well as their therapeutic relevance. The risk of ESRD was not significantly different between treated AS patients and non-AS individuals matched for age, sex, year of index date and dose of NSAID.
- |||||||||| Prexige (lumiracoxib) / Novartis, indomethacin / PLx Pharma Inc, Generic mfg.
[VIRTUAL] A novel protective role of prostaglandin D2 in antigen-induced bronchoconstriction (Pre-congress content) - Jul 15, 2020 - Abstract #ERS2020ERS_2155; In GPT, challenge with OVA (100 µg/mL) induced a constrition (Emax of 54±6%) that was enhanced by the unselective COX inhibitor indomethacin (Emax:94±2%; p<0.05)...Selective inhibition of COX-2 by lumiracoxib did not inhibit release of PGD2 or TXA2... Endogenous PGD2 is generated via COX-1 and mediates a previously unknown inhibitory effect of the antigen-induced bronchoconstriction via DP1 receptors inhibiting mast cell release.
- |||||||||| glibenclamide / Generic mfg., dalfampridine / Generic mfg.
Preclinical, Journal: 4-Aminopyridine, a Voltage-Gated K Channel Inhibitor, Attenuates Nitric Oxide-Mediated Vasodilation of Retinal Arterioles in Rats. (Pubmed Central) - Jul 3, 2020 Intravitreal injection of indomethacin (a non-selective cyclooxygenase inhibitor) also reduced the NOR3-induced retinal vasodilator response...These results suggest that the vasodilatory effects of NO are mediated, at least in part, through the activation of 4-aminopyridine-sensitive K channels in the retinal arterioles of rats. NO exerts its dilatory effect on the retinal vasculature of rats through at least two mechanisms, activation of the K channels and enhancement of prostaglandin production.
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