scholarly journals Basic Pharmacological Characterization of EV-34, a New H2S-Releasing Ibuprofen Derivative

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 599
Author(s):  
Alexandra Gyöngyösi ◽  
Vivien Verner ◽  
Ilona Bereczki ◽  
Attila Kiss-Szikszai ◽  
Rita Zilinyi ◽  
...  
Keyword(s):  
Cytotoxic Effect ◽  
High Dose ◽  
Pharmacological Characterization ◽  
Rat Serum ◽  
Diphenyltetrazolium Bromide ◽  
Oxidative Condition ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Background: Cardioprotective effects of H2S are being suggested by numerous studies. Furthermore, H2S plays a role in relaxation of vascular smooth muscle, protects against oxidative stress, and modulates inflammation. Long-term high-dose use of NSAIDs, such as ibuprofen, have been associated with enhanced cardiovascular risk. The goal of the present work is the synthesis and basic pharmacological characterization of a newly designed H2S-releasing ibuprofen derivative. Methods: Following the synthesis of EV-34, a new H2S-releasing derivative of ibuprofen, oxidative stability assays were performed (Fenton and porphyrin assays). Furthermore, stability of the molecule was studied in rat serum and liver lysates. H2S-releasing ability of the EC-34 was studied with a hydrogen sulfide sensor. MTT (3-(4,5-dimethylthiazol 2-yl)-2,5-(diphenyltetrazolium bromide)) assay was carried out to monitor the possible cytotoxic effect of the compound. Cyclooxygenase (COX) inhibitory property of EV-34 was also evaluated. Carrageenan assay was carried out to compare the anti-inflammatory effect of EV-34 to ibuprofen in rat paws. Results: The results revealed that the molecule is stable under oxidative condition of Fenton reaction. However, EV-34 undergoes biodegradation in rat serum and liver lysates. In cell culture medium H2S is being released from EV-34. No cytotoxic effect was observed at concentrations of 10, 100, 500 µM. The COX-1 and COX-2 inhibitory effects of the molecule are comparable to those of ibuprofen. Furthermore, based on the carrageenan assay, EV-34 exhibits the same anti-inflammatory effect to that of equimolar amount of ibuprofen (100 mg/bwkg). Conclusion: The results indicate that EV-34 is a safe H2S releasing ibuprofen derivative bearing anti-inflammatory properties.

scholarly journals Characterization of fluoroquinolone-induced Achilles tendon toxicity in rats: comparison of toxicities of 10 fluoroquinolones and effects of anti-inflammatory compounds.

1997 ◽  
Vol 41 (11) ◽  
pp. 2389-2393 ◽  
Author(s):  
Y Kashida ◽  
M Kato
Keyword(s):  
Nitric Oxide ◽  
Body Weight ◽  
Methyl Ester ◽  
Achilles Tendon ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
High Dose ◽  
Juvenile Rats ◽  
Anti Inflammatory

Fluoroquinolone antibacterial agents have been reported to induce tendon lesions in juvenile rats. In the present study, we characterized fluoroquinolone-induced Achilles tendon lesions by comparing the effects of 10 fluoroquinolones and examining the potential of one of these antimicrobial agents, pefloxacin, to induce tendon lesions when coadministered with one of nine anti-inflammatory compounds. Among the 10 fluoroquinolones tested, fleroxacin and pefloxacin were the most toxic, inducing lesions at a dose of 100 mg/kg of body weight or more, while lomefloxacin, levofloxacin, and ofloxacin or sparfloxacin and enoxacin induced lesions at 300 mg/kg or more and 900 mg/kg, respectively. In contrast, norfloxacin, ciprofloxacin, and tosufloxacin had no effect even at the high dose of 900 mg/kg. The severity of the Achilles tendon lesions appeared to correlate with the structure of the substituent at the seventh position. Furthermore, pefloxacin-induced tendon lesions were inhibited by coadministration with dexamethasone and N-nitro-L-arginine methyl ester. Phenidone (1-phenyl-3-pyrazolidinone) and 2-(12-hydroxydodeca-5,10-diynyl)3,5,6-trimethyl-1,4-benzoqui none (AA861) also decreased the incidence of tendon lesions. In contrast, catalase, dimethyl sulfoxide, indomethacin, pyrilamine, and cimetidine did not modify these tendon lesions. These results suggest that nitric oxide and 5-lipoxigenase products partly mediate fluoroquinolone-induced tendon lesions.

Anti-nociceptive and anti-inflammatory activity of synthesized novel benzoxazole derivatives

2021 ◽  
Vol 20 ◽  
Author(s):  
Mansi L. Patil ◽  
Swati S. Gaikwad ◽  
Naresh J. Gaikwad
Keyword(s):  
Cytotoxic Activity ◽  
Research Study ◽  
Ex Vivo ◽  
Immunological Response ◽  
Inflammatory Activity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Introduction: Pain is an immunological response to any infection or inflammation and long term use of pain management therapy includes use of Nonsteroidal anti-inflammatory drugs which is associated with occurrence of toxicity as well as gastrointestinal bleeding. Therefore, the investigation of new analgesic and anti-inflammatory agents remains a major challenge. Aims: The objective of this research study is to undergo the pharmacological evaluation of newly synthesized benzoxazole derivatives. These novel derivatives were evaluated for anti-nociceptive, anti-inflammatory and cytotoxic activity using various in-vivo and ex-vivo methods. Methods: The study was carried out using swiss mice (adult male) weighing between 20gm to 30gm and were divided into groups containing (n=6) six animals in each group for treatment. The anti-nociceptive activity was performed by using 0.1ml of 0.6% v/v acetic acid as nociception inducer and evaluated by the diminished number of abdominal writhes. The anti-inflammatory activity was done using 0.1 ml of 2% w/v Carrageenan induced paw edema method was observed which was evaluated by calculating the percent maximum possible effect. Histopathological evaluation and cytotoxic activity of the compounds was carried out. Results: The results of this research study revealed that synthesized derivatives (a, b, c, d and e) showed promising anti-nociceptive and anti-inflammatory effect along significantly higher cytotoxic activity in MCF-7 cell lines. Conclusion: It can be concluded that synthesized derivatives (a, b, c, d and e) have potential anti-nociceptive and anti-inflammatory effect along with cytotoxic activity and certain modification in structure may result in potent activity.

Long Term Gastric Electrical Stimulation has an Anti-inflammatory Effect

2017 ◽  
Vol 152 (5) ◽  
pp. S729 ◽  
Author(s):  
Thomas Abell ◽  
Archana Kedar ◽  
Abigail Stocker ◽  
Karen Beatty ◽  
Lindsay McElmurray ◽  
...  
Keyword(s):  
Electrical Stimulation ◽  
Gastric Electrical Stimulation ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Cannabidiol produces a long-term anti-inflammatory effect in a murine model of acute lung injury

2011 ◽  
Vol 25 ◽  
pp. S210 ◽  
Author(s):  
A. Ribeiro ◽  
V. Ferraz-de-Paula ◽  
M.L. Pinheiro ◽  
W.M. Quinteiro-Filho ◽  
A.T. Akamine ◽  
...  
Keyword(s):  
Acute Lung Injury ◽  
Lung Injury ◽  
Murine Model ◽  
Anti Inflammatory ◽  
Inflammatory Effect

scholarly journals Synthesis and Characterization of New Etodolac Derivatives with Possible Anti-Inflammatory Activity

2019 ◽  
Vol 28 (1) ◽  
pp. 107-113
Author(s):  
Omeed Muhsin Hassan ◽  
Susan Sarsam
Keyword(s):  
Ir Spectroscopy ◽  
Egg White ◽  
Inflammatory Activity ◽  
Synthesis And Characterization ◽  
Paw Edema ◽  
Ft Ir ◽  
Anti Inflammatory ◽  
Ft Ir Spectroscopy ◽  
Inflammatory Effect

A series of Etodolac hydrazone derivatives were synthesized and evaluated for their anti-inflammatory activity by using egg white induced paw edema method. All the synthesized target compounds were characterized by CHN- microanalysis, FT-IR spectroscopy and 1HNMR analysis. The synthesized target compounds (P1-P3) were found to be active in reducing paw edema thickness and their anti-inflammatory effect was comparable to that of the standard (Etodolac). Keywords: Etodolac hydrazone derivatives, anti-inflammatory, paw edemamethod.

scholarly journals The Effect of 630 nm Photobiomodulation on the Anti-Inflammatory Effect of Human Gingival Fibroblasts

Photonics ◽  
2021 ◽  
Vol 8 (9) ◽  
pp. 360
Author(s):  
Zeqing Chen ◽  
Xuwen Liu ◽  
Haokuan Qin ◽  
Zhicheng Lu ◽  
Shijie Huang ◽  
...  
Keyword(s):  
Red Light ◽  
Chronic Inflammatory Disease ◽  
Human Gingival Fibroblasts ◽  
High Dose ◽  
Oxygen Species ◽  
Gingival Fibroblasts ◽  
Anti Inflammatory ◽  
Different Doses ◽  
Selection Of ◽  
Inflammatory Effect

Periodontal disease is the most common oral chronic inflammatory disease in humans. Recent studies have indicated that red light Photobiomodulation (PBM) could inhibit cell inflammation effectively, but the effect of different doses of PBM on the treatment of inflammation has to be improved. Thus, this study was aimed to investigate the effects of various doses of PBM (630 ± 30 nm, (1) 5 mW/cm2, 1 J/cm2, 200 s; (2) 5 mW/cm2, 3 J/cm2, 600 s; (3) 5 mW/cm2, 9 J/cm2, 1800 s; (4) 5 mW/cm2, 18 J/cm2, 3600 s; (5) 5 mW/cm2,36 J/cm2, 7200 s) on the anti-inflammatory response of human gingival fibroblasts. Our results suggested that PBM (630 ± 30 nm) with doses of 18 J/cm2 and 36 J/cm2 could significantly inhibit the production of inflammatory cytokines such as Prostaglandin E2 (PGE2) and IL-8, presumably due to the fact that a high dose of PBM treatment could reduce intracellular Reactive oxygen species (ROS) in human gingival fibroblasts, thus reducing the expression of COX-2 enzyme. In addition, it was found that treatment with different doses of PBM (630 ± 30 nm) did not result in reduced mitochondrial membrane potential and mitochondrial dysfunction in human gingival fibroblasts. Our study provides a theoretical reference for the selection of PBM parameters and the application of PBM in the clinical treatment of periodontitis.

Characterization of Moringa oleifera roots polysaccharide MRP-1 with anti-inflammatory effect

2019 ◽  
Vol 132 ◽  
pp. 844-851 ◽  
Author(s):  
Can Cui ◽  
Song Chen ◽  
Xinyu Wang ◽  
Guangwei Yuan ◽  
Feng Jiang ◽  
...  
Keyword(s):  
Moringa Oleifera ◽  
Anti Inflammatory ◽  
Inflammatory Effect

INVESTIGATION OF NEW NSAIDS FOR THE TREATMENT OF INFLAMMATORY DISEASES OF KIDNEY AND URINARY TRACT

2016 ◽  
Vol 78 (5-6) ◽  
Author(s):  
Murashko Tatyana ◽  
Ivanov Alexey ◽  
Smirnov Ivan ◽  
Bondarev Alex ◽  
Alexey Nemtsev ◽  
...  
Keyword(s):  
Benzoic Acid ◽  
High Efficiency ◽  
Inflammatory Diseases ◽  
Pain Syndrome ◽  
Test Substance ◽  
Peptic Ulcers ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used in the world, primarily due to their high efficiency for the treatment of inflammatory induced pain syndrome. The main feature of NSAIDs is a combination of anti-inflammatory, analgesic, antipyretic, and anticoagulant properties. However, their long-term use is associated with side effects in the gastrointestinal tract including peptic ulcers and other. We developed and synthesized molecule of methyl (4-О-β-glucopyranosyloxy)-benzoic acid. The anti-inflammatory effect of methyl (4-О-β-glucopyranosyloxy)-benzoic acid evaluated using the carrageenan-induced hindpaw edema model. The study shows that the intragastrically administration of test substance to animals reduces inflammatory process.

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