 |
78 Companies | 115 Products |
|
|
115 Products | |
266 Diseases | |
841 Trials |  |
49644 News |  |
| «12...1516171819202122232425...3132» |
- | carbamazepine / Generic mfg.
Journal: Understanding mechanisms of drug resistance in epilepsy and strategies for overcoming it. (Pubmed Central) - Sep 15, 2021
Also, combinations of AEDs exerting synergy in preclinical and clinical studies (for instance, lamotrigine + valproate, levetiracetam + valproate, topiramate + carbamazepine) might be of importance in this respect. Preclinically antagonistic combinations must be avoided (lamotrigine + carbamazepine, lamotrigine + oxcarbazepine).
- | celecoxib oral / Generic mfg.
Journal, IO biomarker: Adipose-derived stem cells inhibit dermal fibroblast growth and induce apoptosis in keloids through the arachidonic acid-derived cyclooxygenase-2/prostaglandin E2 cascade by paracrine. (Pubmed Central) - Sep 14, 2021
To clarify the role of COX-2 in ADSC-CM-induced KFB apoptosis, a specific COX-2 inhibitor, celecoxib, was applied to KFBs cultured in ADSC-CM...We showed activation of the COX-2/PGE2 cascade in KFBs in response to ADSC-CM. By employing a specific COX-2 inhibitor, COX-2/PGE2 cascade activation played a crucial role in mediating the ADSC-CM-induced KFB apoptosis and anti-proliferation effects.
- || sulindac / Generic mfg.
Review, Journal: PDE5 and PDE10 inhibition activates cGMP/PKG signaling to block Wnt/β-catenin transcription, cancer cell growth, and tumor immunity. (Pubmed Central) - Sep 11, 2021
Thus, it might be feasible develop safer and more efficacious drugs for cancer indications by targeting PDE5 and PDE10, which are overexpressed in various tumors and essential for cancer cell growth. In this review, we describe the rationale for using the sulindac scaffold to design-out COX inhibitory activity, while improving potency and selectivity to inhibit PDE5 and PDE10 that activate cGMP/PKG signaling to suppress Wnt/β-catenin transcription, cancer cell growth, and tumor immunity.
- | Journal: New azaphilones from mangrove endophytic fungus Penicillium sclerotiorin SCNU-F0040. (Pubmed Central) - Sep 10, 2021
Compounds 1 and 2 have a-glucosidase inhibition activity with IC values of 102.3 and 217.5 μM. Compound 2 shows a moderate cyclooxygenase-2 inhibitory activity with an IC value of 47.8 μM.
- | meloxicam / Generic mfg.
Journal: Synthesis and biological evaluation as well as in silico studies of arylpiperazine-1,2-benzothiazine derivatives as novel anti-inflammatory agents. (Pubmed Central) - Sep 10, 2021
Moreover, the most selective compound 7b, towards COX-2, was non-toxic for the normal human cell line (in concentration of 10 µM) comparable to reference drug meloxicam. Additionally, investigation of influence on model membranes confirmed the ability of the compound 7b to penetrate lipid bilayers which seemed to be important to the influence with membrane protein-cyclooxygenase.
- | Journal: Design and Synthesis of N-Substituted 3,4-Pyrroledicarboximides as Potential Anti-Inflammatory Agents. (Pubmed Central) - Sep 9, 2021
Theoretical modeling was also applied to describe the binding properties of compounds towards COX-1 and COX-2 cyclooxygenase isoform. The data were supported by QSAR study.
- | Preclinical, Journal: Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents In Vitro and In Vivo. (Pubmed Central) - Sep 9, 2021
Integrated approaches of molecular simulation, organic synthesis, and biochemical/physical experiments identified 15 inhibiting COX-2 and LOX with respective IC 4 and 7 nM. At a dose of 5 mg kg to Swiss albino mice, 15 reversed algesia by 65% and inflammation by 33% in 2-3 h. We find good agreement between experiments and simulations and use the simulations to rationalize our observations.
- Quantifying Risk Factors for Microscopic Colitis: A Nationwide, Retrospective Cohort Study (Shoreline Exhibit Hall) - Sep 8, 2021 - Abstract #ACG2021ACG_1520;
Among medications, non-steroidal anti-inflammatory agents (OR, 20.2) and proton pump inhibitors (OR, 12.1) were associated with the highest odds of MC. Among medical comorbidities, infectious gastroenteritis (OR, 26.6) and celiac disease (OR, 22.5) had the highest odds of being associated with MC.
- pantoprazole / Generic mfg., aspirin / Generic mfg.
Peptic Ulcers and Decompensated Heart Failure Induced by Excessive Alka-Seltzer® Use (Shoreline Exhibit Hall) - Sep 8, 2021 - Abstract #ACG2021ACG_638;
Introduction: Alka-Seltzer ® is an over the counter medication that contains acetylsalicylic acid (aspirin) and is advertised to treat heartburn, acid indigestion, sour stomach and pain...He was placed on pantoprazole and subsequently underwent upper endoscopy which revealed large clean based (Forrest III) ulcers in the antrum with negative immunohistochemical staining for H.pylori...It's imperative that patients and physicians are educated regarding supplement contents and their potential effects and interactions. Figure: Endoscopic visualization of pre-pyloric ulcers.
- | mefenamic acid / Generic mfg., celecoxib oral / Generic mfg.
Journal: Mefenamic Acid can attenuate depressive symptoms by suppressing microglia activation induced upon chronic stress. (Pubmed Central) - Sep 3, 2021
Figure: Endoscopic visualization of pre-pyloric ulcers. MA inhibits microglia activation/phagocytosis induced upon chronic stress in the hippocampus, which might result in the improvement of depressive symptoms.
- | Journal: Aloe emodin shows high affinity to active site and low affinity to two other sites to result consummately reduced inhibition of lipoxygenase. (Pubmed Central) - Sep 2, 2021
ITC results indicate that the interaction of LOX with aloe emodin is endothermic in nature with a stoichiometry of n = 3. In conclusion, anti-inflammatory property of the plant could be assigned to the presence of aloe emodin.
- | Preclinical, Journal: Cycloarta-23-ene-3beta,25-diol a pentacyclic steroid from Euphorbia spinidens, as COX inhibitor with molecular docking, and in vivo study of its analgesic and anti-inflammatory activities in male Swiss mice and Wistar rats. (Pubmed Central) - Sep 2, 2021
In conclusion, anti-inflammatory property of the plant could be assigned to the presence of aloe emodin. Therefore, according to these findings, cycloart-23-ene-3beta,25-diol showed promising analgesic and anti-inflammatory effects with low toxicity against normal cells and can be suggested as a template lead for designing anti-inflammatory compounds with good selectivity index, and potency for COX-2 inhibitory activity.
- | Journal, IO biomarker: Design, synthesis and biological evaluation of N-anthraniloyl tryptamine derivatives as pleiotropic molecules for the therapy of malignant glioma. (Pubmed Central) - Sep 2, 2021
Finally, NP16 effectively inhibited tumor growth, promoted the survival rate, increased the expression of E-cadherin and reduced overproduction of PGE, MMP-9, VEGF-A and the level of p-STAT3 in tumor tissue, and improved the anxiety-like behavior in C6 glioma model. All these evidences demonstrated N-anthraniloyl tryptamine derivatives as multifunctional anti-glioma agents with high potency could drain the swamp to beat glioma.
- | Journal, Myeloid-derived suppressor cells, PD(L)-1 Biomarker, IO biomarker: Monocytic myeloid-derived suppressor cells reflect tuberculosis severity and are influenced by cyclooxygenase-2 inhibitors. (Pubmed Central) - Sep 1, 2021
We show novel data that COX-2i had limited effect in vivo but reduced M-MDSC cytokine production in vitro. The relevance of COX-2i in a HDT strategy needs to be further explored.
- | Journal: The inhibitory effects of Orengedokuto on inducible PGE2 production in BV-2 microglial cells. (Pubmed Central) - Aug 31, 2021
The inhibitory effects of OGT on PGE2 production in BV-2 cells were experimentally replicated in primary cultured astrocytes and mice brains. OGT can be useful in the treatment of neuroinflammatory diseases by modulating PGE2 expression.
- | Journal: Omega-3- and Resveratrol-Loaded Lipid Nanosystems for Potential Use as Topical Formulations in Autoimmune, Inflammatory, and Cancerous Skin Diseases. (Pubmed Central) - Aug 29, 2021
Liposomes provide sustained RSV release and their flexibility conferred by edge activator components enhances RSV diffusion, which is required to reach NO production cells and COX cell membrane enzymes. Overall, the inclusion of both lipid nanosystems in the same semisolid base constitutes a promising strategy for autoimmune, inflammatory, and cancerous skin diseases.
- | glibenclamide / Generic mfg., verapamil / Generic mfg.
Preclinical, Journal: Relaxation Effect of Schisandra Chinensis Lignans on the Isolated Tracheal Smooth Muscle in Rats and Its Mechanism. (Pubmed Central) - Aug 26, 2021
These results suggest that SCL has a significant relaxation effect on the isolated tracheal smooth muscle of rats, and the mechanism may be related to the inhibition of extracellular calcium influx and intracellular calcium release from the sarcoplasmic reticulum, as well as the activation of ATP-sensitive potassium channels. These findings may provide a pharmacological basis for the traditional use of S. chinensis to treat asthma.
- | Biomarker, Journal: Mechanistic definition of the cardiovascular mPGES-1/COX-2/ADMA axis. (Pubmed Central) - Aug 25, 2021
These findings may provide a pharmacological basis for the traditional use of S. chinensis to treat asthma. These data demonstrate that inhibition of mPGES-1 spares the renal COX-2/ADMA pathway and define mechanistically how COX-2 regulates ADMA.
- | Journal: Targeting Soluble Epoxide Hydrolase and Cyclooxygenases Enhance Joint Pain Control, Stimulate Collagen Synthesis, and Protect Chondrocytes From Cytokine-Induced Apoptosis. (Pubmed Central) - Aug 24, 2021
However, sEH-generated metabolites caused concentration-dependent apoptosis. Combined COX and sEH inhibition optimize pain control, attenuate loss of articular cartilage matrix during joint inflammation and cytokine-induced chondrocyte apoptosis.
- | Journal: Iminodibenzyl redirected cyclooxygenase-2 catalyzed dihomo-γ-linolenic acid peroxidation pattern in lung cancer. (Pubmed Central) - Aug 21, 2021
This D5D inhibition-based strategy selectively damaged lung cancer cells with a high COX-2 level, whereas it could avoid harassing normal lung epithelial cells. This finding challenged the COX-2 redox basis in cancer, providing a new direction for developing omega-6 (DGLA)-based diet/regimen in lung cancer therapy.
- | Journal: Picrorhizones A-H, Polyprenylated Benzoylphloroglucinols from the Stem Bark of Garcinia picrorhiza. (Pubmed Central) - Aug 20, 2021
The cytotoxicity results showed that compound 6 was active against KB, HeLa S3, MCF-7, and Hep G2 cancer cells, with IC values ranging from 5.9 to 9.4 μM. Among the compounds tested for cyclooxygenase inhibition, compound 8 possessed the highest inhibitory effect toward COX-1 (35.2 ± 9.6% inhibition at 20 μM).
- | Preclinical, Journal: Endothelial K 1.1 and K 3.1 channels mediate rat intrarenal artery endothelium derived hyperpolarization response. (Pubmed Central) - Aug 20, 2021
Among the compounds tested for cyclooxygenase inhibition, compound 8 possessed the highest inhibitory effect toward COX-1 (35.2 ± 9.6% inhibition at 20 μM). This study shows that K 1.1 and K 3.1 channels are functionally expressed at the renal vascular endothelium and play a central role in the EDH-mediated relaxation of kidney preglomerular arteries, which is important in the control of renal blood flow and glomerular filtration rate.
- | Journal: Contribution of Splenic Resistance Arteries to Splanchnic Blood Overflow in Cirrhosis. (Pubmed Central) - Aug 18, 2021
This study shows that K 1.1 and K 3.1 channels are functionally expressed at the renal vascular endothelium and play a central role in the EDH-mediated relaxation of kidney preglomerular arteries, which is important in the control of renal blood flow and glomerular filtration rate. In cirrhotic rats, a decreased splenic arterial response to vasoconstrictors, rather than an increased response to vasodilators, contributes to splanchnic vasodilation, while in mesenteric arteries also an increased response to vasodilators secondary to, but not only, eNOS and iNOS overexpression, plays a role.
- | Journal: Synthesis of New Tricyclic 1,2-Thiazine Derivatives with Anti-Inflammatory Activity. (Pubmed Central) - Aug 18, 2021
Finally, they neither have cytotoxic potency, nor demonstrate significant influence on the level of reactive oxygen species or nitric oxide. Overall, the tricyclic 1,2-thiazine derivatives are good starting points for future pharmacological tests as a group of new anti-inflammatory agents.
- | pentylenetetrazole (BTD-001) / Balance Therap
Preclinical, Journal: Involvement of N-Methyl-D-Aspartate Receptors in the Anticonvulsive Effects of Licofelone on Pentylenetetrazole-Induced Clonic Seizure in Mice. (Pubmed Central) - Aug 17, 2021
Notably, pre-treatment with the NMDAR co-agonist D-serine (30 mg/kg, i.p.) partially hindered the anticonvulsant effects of licofelone (20 mg/kg). Our data suggest a possible role for the NMDAR in the anticonvulsant effects of licofelone on the clonic seizures induced by PTZ in mice.
- || Zyclara (imiquimod) / Mochida, Viatris, Bausch Health
Clinical, Journal: Safety of topical interventions for the treatment of actinic keratosis. (Pubmed Central) - Aug 15, 2021
All these therapies have been proven efficient, yet they differ considerably regarding their safety profile.Expert opinion: In the future, safety concerns will relate to long-term and irreversible adverse drug events instead of application site reactions. In particular, the rate of treatment-associated non-melanoma skin cancers will increasingly come into focus and warrant investigation in postmarketing surveillance trials with a long-term follow-up.
- || Review, Journal: Inhibition of photodynamic therapy induced-immunosuppression with aminolevulinic acid leads to enhanced outcomes of tumors and pre-cancerous lesions. (Pubmed Central) - Aug 14, 2021
Given this pathway, there are three main methods to block immunosuppression: i) Inhibiting the proliferation of Tregs, which can be achieved with the administration of cyclophosphamide or inhibitors of indoleamine 2,3-dioxygenase 1, an activator of Tregs; ii) inhibiting MDSCs by reducing hypoxia around the tumor to create an unfavorable environment or administering all-trans-retinoic acid, which converts MDSCs to a non-immunosuppressive state; and iii) inhibiting COX-2 through selective or non-selective COX-inhibitors. In the present review article, strategies that have shown increased efficacy of PDT in treating tumors and pre-cancerous lesions by blocking the immunosuppressive side effects are outlined and discussed.
- Molecular hybridization of NSAIDs: Synthesis, computational studies, and evaluation of anti-inflammatory and analgesic properties (Room: Hall B4) - Aug 13, 2021 - Abstract #ACSFall2021ACS_Fall_4854;
The newly synthesized conjugates did not display any ulcerogenic liability. In vitro, COX-1, and COX-2 enzyme inhibition studies revealed some compounds are more selective toward COX-2 compared with reference drugs.
- [VIRTUAL] Design and synthesis of 6-hydroxyindole-7-carboxylates with anti-inflammatory and anti-cancer activities (Room: Zoom Room 19) - Aug 13, 2021 - Abstract #ACSFall2021ACS_Fall_3254;
Herein, we will discuss our efforts towards the design, synthesis and evaluation of 6-hydroxyindole-7-carboxylate derivatives as potential anti-inflammatory and anti-cancer compounds. Our discussion will also include an investigation on cell death mechanism and cell cycle arrest of selected compounds.
- | celecoxib oral / Generic mfg.
Journal: Novel 1,2,4-triazine-quinoline hybrids: The privileged scaffolds as potent multi-target inhibitors of LPS-induced inflammatory response via dual COX-2 and 15-LOX inhibition. (Pubmed Central) - Aug 13, 2021
The new triazine-quinoline hybrids (8a-n) exhibited potent COX-2 inhibitory profiles (IC = 0.047-0.32 μM, SI ∼ 20.6-265.9) compared to celecoxib (IC = 0.045 μM, SI ∼ 326)...Docking study of the synthesized hybrids into the active sites of COX-2 and 15-LOX enzymes ensures their favored binding affinity. To our knowledge, herein we reported the first 1,2,4-triazine-quinoline hybrids as dual COX/15-LOX inhibitors.
- | ibuprofen / Generic mfg.
Journal: Analysis of lung transcriptome in calves infected with Bovine Respiratory Syncytial Virus and treated with antiviral and/or cyclooxygenase inhibitor. (Pubmed Central) - Aug 12, 2021
Ibuprofen, when used alone, negatively affected the antiviral response and caused higher virus loads as shown by increased viral shedding. In contrast, when used with FPI Ibuprofen enhanced the specific antiviral effect of FPI, due to its ability to reduce the damaging effect of prostanoids and oxidative stress.
- | temozolomide / Generic mfg., celecoxib oral / Generic mfg.
Journal: COXIBs and 2,5-dimethylcelecoxib counteract the hyperactivated Wnt/β-catenin pathway and COX-2/PGE2/EP4 signaling in glioblastoma cells. (Pubmed Central) - Aug 12, 2021
In contrast, when used with FPI Ibuprofen enhanced the specific antiviral effect of FPI, due to its ability to reduce the damaging effect of prostanoids and oxidative stress. Not only celecoxib, but also 2,5-DMC, etori-, rofe- and valdecoxib should be further investigated as potential good anti-GBM therapeutics.
- | Journal: SCO-Spondin Defects and Neuroinflammation Are Conserved Mechanisms Driving Spinal Deformity across Genetic Models of Idiopathic Scoliosis. (Pubmed Central) - Aug 11, 2021
Through screening for chemical suppressors of sspo mutant phenotypes, we also identify potent agents capable of blocking severe juvenile spine deformity. Our work thus defines a new preclinical model of AIS and provides tools to realize novel therapeutic strategies.
- | Xefo (lornoxicam) - Old API Wind / down, Takeda
Journal: Immunomodulatory Effects of the Cyclooxygenase Inhibitor Lornoxicam on Phenotype and Function of Camel Blood Leukocytes. (Pubmed Central) - Aug 8, 2021
Flow cytometric analysis of cell vitality, including cell necrosis and apoptosis, revealed a pro-apoptotic effect of lornoxicam on camel leukocytes; (4) Lornoxicam administration, at the dose and intervals utilized herein, induces significant changes in the phenotype and function of camel blood leukocytes. The reduced cell numbers of all studied leukocyte subpopulations in lornoxicam-treated camels, which seems to be a result of enhanced cell apoptosis, indicates an inhibitory effect rather than a modulatory effect of lornoxicam on the camel immune system, which need to be considered when using lornoxicam in camel medicine.
- | Nexavar (sorafenib) / Bayer, Amgen
Journal: Abdominal Desmoid: Course, Severe Outcomes, and Unique Genetic Background in a Large Local Series. (Pubmed Central) - Aug 8, 2021
We also report a group of non-FAP abdominal desmoids, which includes patients with additional cancer-related gene alterations. This interesting group should be further explored.
- | cisplatin / Generic mfg., aspirin / Generic mfg.
Journal: Aspirin overcomes cisplatin resistance in lung cancer by inhibiting cancer cell stemness. (Pubmed Central) - Aug 8, 2021
This interesting group should be further explored. This study revealed that stemness is a latent inhibitor of the resistance of lung cancer cisplatin-resistant cells and might be effectively inhibited by aspirin.
- | flurbiprofen / Generic mfg.
Preclinical, Journal: Design, synthesis and in vitro and in vivo biological evaluation of flurbiprofen amides as new fatty acid amide hydrolase/cyclooxygenase-2 dual inhibitory potential analgesic agents. (Pubmed Central) - Aug 8, 2021
Thus, the present study identifies Flu-AM4 as a dual-action FAAH/substrate-selective COX inhibitor with anti-inflammatory and analgesic activity in animal pain models. These findings underscore the potential usefulness of such dual-action compounds.
- || Clinical, Journal: Covariation of changing patent ductus arteriosus management and preterm infant outcomes in Pediatrix neonatal intensive care units. (Pubmed Central) - Aug 7, 2021
These findings underscore the potential usefulness of such dual-action compounds. NICU-specific adjusted mortality, BPD, and pulmonary hemorrhage rates co-vary with changes in local COXI/ligation rates in some VLBW infant subgroups.
- | indomethacin / Generic mfg.
Journal: Mitochondrial HS-Mediated Anti-Inflammatory Theranostics. (Pubmed Central) - Aug 7, 2021
Here, we report a novel theranostic agent 1 (TA1), consisting of three parts: HS-mediated triggering part, a two-photon fluorophore bearing mitochondria targeting unit (Rhodol-TPP), and anti-inflammatory COX inhibitor (indomethacin)...In vivo experiments with inflammation-induced mouse models suggested that TA1 exhibits inflammation-site-elective drug release followed by significant therapeutic effects, showing its function as a theranostic agent, capable of both anti-inflammatory therapy and precise diagnosis. Theranostic behavior of TA1 is highly applicable in vivo model therapeutics for the inflammatory disease.
- || Review, Journal: Structure-Activity Relationship Analysis of Benzimidazoles as Emerging Anti-Inflammatory Agents: An Overview. (Pubmed Central) - Aug 7, 2021
For example, benzimidazole substituted with anacardic acid on C2 inhibits COX-2, and 5-carboxamide or sulfamoyl or sulfonyl benzimidazole antagonises the cannabinoid receptor, whereas the C2 diarylamine and C3 carboxamide substitution of the benzimidazole scaffold result in antagonism of the bradykinin receptor. In this review, we examine the insights regarding the SARs of anti-inflammatory benzimidazole compounds, which will be helpful for researchers in designing and developing potential anti-inflammatory drugs to target inflammation-promoting enzymes.
- || Review, Journal: Neuroinflammation in Major Depressive Disorder: A Review of PET Imaging Studies Examining the 18-kDa Translocator Protein. (Pubmed Central) - Aug 7, 2021
In this review, we examine the insights regarding the SARs of anti-inflammatory benzimidazole compounds, which will be helpful for researchers in designing and developing potential anti-inflammatory drugs to target inflammation-promoting enzymes. These findings supported the presence of neuroinflammation in MDD, suggesting that microgliosis may be an important pathophysiological mechanism that merits further investigation as a potential target for novel treatment strategies.
- Vincerinone (vatiquinone) / Sumitomo Dainippon, PTC Therap
[VIRTUAL] NEW TREATMENTS IN MITOCHONDRIAL DISORDERS (Topic D) - Aug 6, 2021 - Abstract #WCN2021WCN_710;
Other trials include EPI-743 and rAAV2-ND4 gene therapy in individuals who exhibit a “ window of opportunity” for directed ocular therapy. (6) Supplementation of nucleosides in mtDNA depletion syndromes is needed in TK2 and DGK deficiency.
- [VIRTUAL] Double-blind, Placebo-controlled Randomized Controlled Trial of NSAID Prior to Ureteral Stent Removal in Pediatric Patients () - Aug 5, 2021 - Abstract #AUA2021AUA_2799;
The incidence of severe pain before and after stent removal was low, ranging from 4.5–9.1%. Our study may have been underpowered given the low incidence of severe pain.
- | Journal: Analgesic, anti-inflammatory and toxic effects of ethanol extracts of Cucumis melo and Citrullus lanatus seeds. (Pubmed Central) - Aug 5, 2021
Analgesic and anti-inflammatory effects of extracts may be due to presence of cucurbitacin A, B or E in both seeds which are thought to inhibit COX 2. Results indicate that seeds of C. melo and C. lanatus may be effectively used as adjuvant analgesic and anti-inflammatory agents in situation of chronic pain and inflammation.
- | Journal: Identification of plant metabolite classes from Waltheria Indica L. extracts regulating inflammatory immune responses via COX-2 inhibition. (Pubmed Central) - Aug 5, 2021
Results indicate that seeds of C. melo and C. lanatus may be effectively used as adjuvant analgesic and anti-inflammatory agents in situation of chronic pain and inflammation. The data suggest that Waltheria Indica extracts inhibit the key inflammatory enzyme, COX-2, as a function of triterpenoid- and steroidal-saponin concentration and support the known efficacy of extracted Waltheria Indica leaves as a traditional treatment against inflammation related diseases.
- | Journal: Design, Synthesis and Pharmacological Evaluation of Gastro-protective Anti-inflammatory Analgesic Agents based on Dual Oxidative Stress / Cyclooxygenase Inhibition. (Pubmed Central) - Aug 4, 2021
The data suggest that Waltheria Indica extracts inhibit the key inflammatory enzyme, COX-2, as a function of triterpenoid- and steroidal-saponin concentration and support the known efficacy of extracted Waltheria Indica leaves as a traditional treatment against inflammation related diseases. From the above results, it can be concluded that designing of multifunctional molecules with COX-1/COX-2 inhibitory and anti-oxidant activities could hold a great promise for further development of GI-safer NSAIDs.
- | meloxicam / Generic mfg.
Preclinical, Journal: A New N-Substituted 1H-Isoindole-1,3(2H)-Dione Derivative-Synthesis, Structure and Affinity for Cyclooxygenase Based on In Vitro Studies and Molecular Docking. (Pubmed Central) - Aug 4, 2021
Three compounds showed greater inhibition of COX-2, three compounds inhibited COX-1 more strongly than the reference compound meloxicam...The newly synthesized phthalimide derivatives showed no cytotoxic activity in the concentration range studied (10-90 µM). A molecular docking study was used to determined interactions inside the active site of cyclooxygenases.
- || etoricoxib / Generic mfg.
Clinical, P1 data, Journal: Plasma LOX-Products and Monocyte Signaling Is Reduced by Adjunctive Cyclooxygenase-2 Inhibitor in a Phase I Clinical Trial of Tuberculosis Patients. (Pubmed Central) - Aug 4, 2021
Peripheral blood mononuclear cells isolated from TB patients included in a randomized phase I clinical trial of standard TB treatment with (n=21) or without (n=18) adjunctive COX-2i (etoricoxib) were analyzed at baseline, day 14 and day 56...COX-2i may reduce excess inflammation in TB via the LOX-pathway in addition to modulation of phosphorylation patterns in monocytes. Immunomodulatory effects of adjunctive COX-2i in TB should be further investigated before recommended for use as a HDT strategy.
- | Preclinical, Journal: Chemopreventive efficacy of juniper berry oil (Juniperus communis L.) on azoxymethane-induced colon carcinogenesis in rat. (Pubmed Central) - Aug 1, 2021
Additionally, JB oil supplementation ameliorated antioxidant defense systems and lipid peroxidation within the colon tissue of AOM + JB treated rats. These results reveal that the JB oil acted as a chemopreventive dietary agent, inhibiting cell proliferation and COX-2 expression and inducing apoptosis, resulting in a significant reduction in colon tumor formation.
- | indomethacin / Generic mfg.
Journal: Anti-platelet properties of Pim kinase inhibition is mediated through disruption of thromboxane A2 receptor signalling. (Pubmed Central) - Jul 31, 2021
Treatment with Pim kinase inhibitors caused reduced surface expression of the thromboxane A2 receptor and resulted in reduced responses to thromboxane A2 receptor agonists, indicating a role for Pim kinase in the regulation of thromboxane A2 receptor function. Our research identifies a novel, Pim kinase dependent regulatory mechanism for the thromboxane A2 receptor and represents a new targeting strategy that is independent of COX-1 inhibition or direct antagonism of the thromboxane A2 receptor that whilst attenuating thrombosis does not increase bleeding.