- |||||||||| midazolam hydrochloride / Generic mfg.
Journal: Phytochemical quercetin alleviates hyperexcitability of trigeminal nociceptive neurons associated with inflammatory hyperalgesia comparable to NSAIDs. (Pubmed Central) - Jun 24, 2022
The mean discharge frequency of SpVc wide-dynamic range (WDR) neurons to both non-noxious and noxious mechanical stimuli in inflamed rats was significantly decreased after quercetin or diclofenac administration under combination of three anesthetic agents (medetomidine, midazolam and butorphanol)...Together, these results suggest that administration of quercetin attenuates inflammatory hyperalgesia associated with hyperexcitability of nociceptive SpVc WDR neurons via inhibition of the peripheral cyclooxygenase-2 signaling cascade and voltage-gated ion channels. These findings support the proposed potential of quercetin as a therapeutic agent in complementary alternative medicine strategies for preventing trigeminal inflammatory mechanical hyperalgesia.
- |||||||||| Review, Journal: Kidney Angiotensin in Cardiovascular Disease: Formation and Drug Targeting. (Pubmed Central) - Jun 22, 2022
SIGNIFICANCE STATEMENT: Angiotensin formation in the kidney is widely accepted but little understood, and multiple, often contrasting concepts have been put forward over the last two decades. This paper offers a unifying view, simultaneously explaining how existing and novel drugs exert renoprotection by interfering with kidney angiotensin formation.
- |||||||||| aspirin / Generic mfg.
Journal, PD(L)-1 Biomarker, IO biomarker: Does the Combined Use of Aspirin and Immunotherapy Result in Better Outcomes in Non-Small Cell Lung Cancer Than Immunotherapy Alone? (Pubmed Central) - Jun 22, 2022
Low-PD-L1 expression in NSCLC was associated with an increased likelihood of survival; this could be of clinical significance, especially with previous studies suggesting better outcomes of using ASA in PD-L1 low tumors. These findings suggest that daily ASA use with PD-L1 inhibitors is associated with more favorable outcomes in NSCLC. More studies are needed to investigate further the potential benefits vs. risks of using ASA with different immunotherapies and the other possible variables affecting treatment outcomes.
- |||||||||| lovastatin / Generic mfg., cisplatin / Generic mfg.
Journal: THSD7B Mutation Induces Platinum Resistance in Small Cell Lung Cancer Patients. (Pubmed Central) - Jun 19, 2022
Several cases of small cell lung cancer (SCLC) patients demonstrate resistance to the treatment initiatives such as cisplatin after platinum chemotherapy...Lovastatin and cyclooxygenase inhibitors could be used as potential target compounds in THSD7B mutant patients, which provides reference for future research on platinum resistance. THSD7B can be considered a reliable biomarker that effectively facilitates the prediction of poor survival in SCLC platinum-treated patients.
- |||||||||| paclitaxel / Generic mfg., ibuprofen / Generic mfg.
Journal: Design, synthesis and molecular docking studies of new azomethine derivatives as promising anti-inflammatory agents. (Pubmed Central) - Jun 14, 2022
Herein, we synthesized a series of Ibuprofen-based 4a-k, quinoxaline-based 9a-f and pyridine-based 13a-h azomethine derivatives and studied their anti-inflammatory potency...Due to their antioxidant properties, compounds were screened for their cytotoxicity against cervical cancer derived HeLa and breast cancer derived MCF-7 cell with the drug Paclitaxel as the standard...Also, the late apoptosis in cervical HeLa cancer cells did not show the expected results, as the compounds proved to be weakly cytotoxic. Thus, the major findings of the work demonstrates the Schiff bases to be promising anti-inflammatory agents compatible with NSAIDs, having moderate anti-oxidant properties with minimal cytotoxicity.
- |||||||||| celecoxib oral / Generic mfg.
Preclinical, Journal: New tilomisole-based benzimidazothiazole derivatives as anti-inflammatory agents: Synthesis, in vivo, in vitro evaluation, and in silico studies. (Pubmed Central) - Jun 14, 2022
Compounds 13, 20, 30, 40, 43, and 46 demonstrated values of inhibition of induced edema in the in vivo assay comparable to celecoxib...In silico studies, including ADMET prediction, compliance to Lipinski's rule of five, and molecular docking into the active site of both COX isozymes were conducted for the synthesized compounds. The results suggested that these compounds are good candidates for orally active drugs, and docking revealed higher number of interactions with COX-2 for 13 as the most active compound compared with COX-1 reflecting its advantageous selectivity and explaining its extreme potency.
- |||||||||| metformin / Generic mfg.
Review, Journal: Drug repurposing-an emerging strategy in cancer therapeutics. (Pubmed Central) - Jun 14, 2022
Clinical trials are vital for determining medication safety and effectiveness, and hence the clinical studies for each repurposed medicine in cancer, including their stages, status, and National Clinical Trial (NCT) identification, are reported in this review article. Various emerging evidences imply that repurposing drugs is critical for the faster and more affordable discovery of anti-cancerous drugs, and the advent of artificial intelligence-based computational tools can accelerate the translational cancer-targeting pipeline.
- |||||||||| gentamicin sulfate / Generic mfg., celecoxib oral / Generic mfg.
Preclinical, Journal: Celecoxib has Preventive and Therapeutic Benefits against Nephrotoxicity Caused by Gentamicin in Mice. (Pubmed Central) - Jun 11, 2022
It is noteworthy that celecoxib therapy after gentamicin administration brought about substantially the same results as celecoxib treatment before gentamicin injection in mice. Our results showed the role of celecoxib as a therapeutic tool for gentamicin-induced nephrotoxicity as well as raised its beneficial prophylactic role in this medical challenge by attenuating oxidative stress and inflammation.
- |||||||||| Review, Journal: Non-steroidal anti-inflammatory drugs (NSAIDs), pain and aging: Adjusting prescription to patient features. (Pubmed Central) - Jun 8, 2022
A narrative review of papers published from January 2011 to December 2021, after a literature search in selected databases using the terms "pharmacokinetics", "ibuprofen", "diclofenac", "acemetacin", "naproxen", "etodolac" and "etoricoxib" was performed...Young patients, patients dealing with acute pain, or with active and/or chronic symptomatic gastritis, selective COX-2 inhibitors (celecoxib or etoricoxib) may be a better option (level of evidence 2)...PERSPECTIVE: Although there are several NSAIDs options to treat pain, physicians usually take special care to its prescription regarding cardiovascular and gastrointestinal side effects, despite the age of the patient. In this paper, based on the best evidence, the authors present a review of the safest NSAIDs to use in the elderly.
- |||||||||| indomethacin / Generic mfg.
Cyclooxygenase Signaling Promotes Control Of A. Fumigatus Invasive Growth By Macrophages And Neutrophils (Exhibit and Poster Hall) - Jun 4, 2022 - Abstract #ASMMicrobe2022ASM_Microbe_3147;
Instead, cyclooxygenase inhibition decreases the ability of innate immune cells to inhibit spore germination and the fungal transition from early germling to tissue-invasive growth. The effects of indomethacin treatment can be rescued by exogenous PGE2 and treatment with an EP2 receptor antagonist phenocopies the effects of indomethacin, demonstrating that a cyclooxygenase-PGE2-EP2 signaling pathway promotes innate immune responses to A. fumigatus.
- |||||||||| indomethacin / Generic mfg.
Understanding the Impact of Nonsteroidal Anti-Inflammatory Drugs During Clostridioides Difficile Infection (Exhibit and Poster Hall) - Jun 4, 2022 - Abstract #ASMMicrobe2022ASM_Microbe_2979;
Mice infected with C. difficile and pre-treated with Indomethacin, a non-selective COX inhibitor, showed dramatic exacerbation of disease and disruption of the epithelial cell barrier...I hypothesize that during CDI, NSAIDs uncouple mitochondrial functions leading to an increase in epithelial cell death and permeability. Impairment of epithelial cell barrier functions allows for microbes to translocate into the lamina propria leading to a robust pro-inflammatory response.
- |||||||||| indomethacin / Generic mfg.
Journal: Neural circuits mediating circulating interleukin-1β-evoked fever in the absence of prostaglandin E2 production. (Pubmed Central) - Jun 4, 2022
In anesthetized rats, pretreatment with indomethacin, a non-selective COX inhibitor, did not prevent BAT thermogenesis or cutaneous vasoconstriction (CVC) induced by intravenous IL-1β (2 µg/kg)...Therefore, our data suggests that COX-independent mechanisms elicit activation of neurons within the DMH and rRPa, which is sufficient to trigger and mount inflammatory fever. These data provide a foundation for elucidating the brain circuits responsible for COX-independent, IL-1β-elicited fevers.
- |||||||||| capecitabine / Generic mfg.
Journal: Randomized double-blind, placebo-controlled study of topical diclofenac in the prevention of hand-foot syndrome in patients receiving capecitabine (the D-TORCH study). (Pubmed Central) - May 29, 2022
Apart from oral cyclooxygenase-2 (COX-2) inhibitor (celecoxib), there are no proven strategies for the prevention of HFS...In this study, we aim to compare topical 1% diclofenac gel with placebo in the prevention of capecitabine-induced HFS...To date, there have been a lot of trials for hand-foot syndrome prevention using agents like pyridoxine, vitamin E, carvedilol, and various polyherbal formulations, but none has been found successful...Clinical Trials Registry of India CTRI/2021/01/030592 . Prospectively registered on January 19, 2021.
- |||||||||| indomethacin / Generic mfg., ibuprofen / Generic mfg.
Journal: Synthesis of salicylic acid phenylethyl ester (SAPE) and its implication in immunomodulatory and anticancer roles. (Pubmed Central) - May 26, 2022
A marked increase of anti-oxidative enzymes viz., catalase, GGT, and GST, and a decrease of pro-inflammatory cytokines IL-6 and TNF-α in the intestinal tissue extracts of the treated groups was noted. The results of this study have sufficient credence to support that the synthesised ester (SAPE) be considered as an anti-oxidative and anti-inflammatory compound with therapeutic potential for the effective management of cancer.
- |||||||||| celecoxib oral / Generic mfg.
Journal: Antiinflammation Derived Suzuki-Coupled Fenbufens as COX-2 Inhibitors: Minilibrary Construction and Bioassay. (Pubmed Central) - May 21, 2022
Both the para-amino and para-hydroxy mono substituents display the most substantial COX-2 inhibition, particularly the latter one showing a comparable activity as celecoxib...In silico simulation and modeling for three COX-2 active-p-fluoro, p-hydroxy and p-amino-fenbufens show a preferable docking to COX-2 than COX-1. The most stabilization by the p-hydroxy fenbufen with COX-2 predicted by theoretical simulation is consistent with its prominent COX-2 inhibition resulting from experiments.
- |||||||||| indomethacin / Generic mfg., ibuprofen / Generic mfg.
Journal: Factorial design in the optimization and study "in combo" of derivatives of imidazo[1,2-a]azines in the COX´s isoforms inhibition. (Pubmed Central) - May 20, 2022
COX1: 4a = 2.72 μM, 4b = 3.94 μM, 5a = 7.29μM, 5b = 63.26 μM, 6a = 12.93 μM, indomethacin = 0.13 μM, ibuprofen = 0.2 μM; COX 2: 4a = 1.89 μM, 4b = 2.39 μM, 5a = 8.08 μM, 5b = 41.15 μM, 6a = 5.86 μM, indomethacin = 0.09 μM, ibuprofen = 0.125 μM. Through factorial design it was possible to optimize the inhibitory response on therapeutic targets, obtaining molecule 4a as a result of factorial analysis.
- |||||||||| tamoxifen / Generic mfg., naproxen / Generic mfg.
Preclinical, Journal: Loss of Endothelial Cytochrome P450 Reductase Induces Vascular Dysfunction in Mice. (Pubmed Central) - May 18, 2022
POR expression in endothelial cells maintains eNOS activity and its loss results in an overactivation of the vasoconstrictor prostanoid system. Through these mechanisms, loss of endothelial POR induces vascular dysfunction and hypertension.
- |||||||||| meloxicam / Generic mfg., risperidone / Generic mfg., paracetamol / Generic mfg.
Journal: Risperidone in analgesia induced by paracetamol and meloxicam in experimental pain. (Pubmed Central) - May 17, 2022
This suggests that COX inhibition is only a partial explanation of the increased analgesic potency of paracetamol and meloxicam since the effects of NSAIDs in the CNS are mediated by multiple mechanisms. These results indicate that the combination of risperidone with paracetamol or meloxicam could be a new and effective alternative for the management of inflammatory pain.
- |||||||||| ibuprofen / Generic mfg.
Clinical data, Retrospective data, Journal: NSAID use and clinical outcomes in COVID-19 patients: a 38-center retrospective cohort study. (Pubmed Central) - May 17, 2022
A conservative interpretation in light of the quantitative bias analysis is that there is no evidence that NSAID use is associated with risk of increased severity or the other measured outcomes. Our results confirm and extend analogous findings in previous observational studies using a large cohort of patients drawn from 38 centers in a nationally representative multicenter database.
- |||||||||| isoflurane / Generic mfg.
Journal: A Foundation for the Neural Control of Viral Fever. (Pubmed Central) - May 14, 2022
Female and male Sprague Dawley rats anesthetized with urethane and α-chloralose (for BAT sympathetic nerve recording, n=3) or isoflurane (for cutaneous vasoconstriction experiments, n=3) received iv poly I:C (1mg/kg for experiments with sympathetic nerve recording, or 500μg/kg for experiments for cutaneous vasoconstriction)...These data suggest that the activity of neurons in the rRPa and the DMH are necessary for poly I:C-induced activation of BAT thermogenesis and cutaneous vasoconstriction. These data define critical components of the neural circuits for poly I:C-induced fever, highlight differences between the neural circuitry mediating bacterial fever and viral fever, and provide a foundation for elucidating additional brain mechanisms responsible for viral fever.
- |||||||||| metformin / Generic mfg.
Journal: Countermeasure Analysis for Galactic Cosmic Radiation Induced Damage. (Pubmed Central) - May 14, 2022
Surprisingly, some anti-diabetic medications observed to be useful including metformin...We also observed that this increase was partially ameliorated by some of the lead candidates. That no one class of drug dominated the response to radiation exposure speaks to the complexity of managing GCR exposure.
- |||||||||| ketorolac / Generic mfg., nitroprusside / Generic mfg.
Journal: Effect of Oral Contraceptive Phase on Mechanisms of Cutaneous Microvascular Function. (Pubmed Central) - May 14, 2022
Maximal vasodilation was induced by heating the skin to 43°C and infusing 28 mM sodium nitroprusside...During the HH phase, a large effect size was observed between control and ketorolac (69 ± 17 %NO; d = 0.94) sites...While overall endothelial function (i.e., magnitude of local heating plateau) is similar between OC phases, there may be basal constriction (i.e., increased baseline with COX inhibition) and reduced NO-dependent dilation during the HH phase. This shift in mechanisms underlying endothelial function in women using OC may contribute to cardiovascular health outcomes.
- |||||||||| nitroprusside / Generic mfg., indomethacin / Generic mfg.
Preclinical, Journal: Aortic Relaxation in Castrated Male Rats and Responses to Estrogen Treatment. (Pubmed Central) - May 14, 2022
Endothelium-independent vasorelaxation was assessed by measuring sodium nitroprusside (SNP)-induced relaxation response in endothelium-denuded rings in addition to the contractile response curves to PE before and after pretreatment with L-NAME in aortic rings...Furthermore, the comparison of current data in the CAS male rats with our recently published data on the aortic reactivity in the intact males appears to rule out any effect of testosterone deprivation on the stimulated release of NO in male rat aortas. Additional studies will be needed to document the direction and magnitude of CSHT interaction with vasculatures.
- |||||||||| indomethacin / Generic mfg., celecoxib oral / Generic mfg.
Journal: Near-Infrared Fluorescent Heptamethine Cyanine Dyes for COX-2 Targeted Photodynamic Cancer Therapy. (Pubmed Central) - May 10, 2022
I-IR799-CXB and I-IR799-IMC were tested for their cancer targeting and photodynamic efficiency towards liver hepatocellular carcinoma cells (HepG2) compared to normal liver cell, alpha mouse liver 12 cells (AML12). Interestingly, after conjugation, I-IR799-IMC exhibited superior tumour targetability and PDT efficiency than I-IR799-CXB .
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