scholarly journals Toward Multitasking Pharmacological COX-Targeting Agents: Non-Steroidal Anti-Inflammatory Prodrugs with Antiproliferative Effects

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3940
Author(s):  
Fedora Grande ◽  
Francesca Giordano ◽  
Maria Antonietta Occhiuzzi ◽  
Carmine Rocca ◽  
Giuseppina Ioele ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Active Metabolite ◽  
Docking Study ◽  
Antiproliferative Agents ◽  
Antiproliferative Effects ◽  
Slowing Down ◽  
Tricyclic Analog ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Effective Use

The antitumor activity of certain anti-inflammatory drugs is often attributed to an indirect effect based on the inhibition of COX enzymes. In the case of anti-inflammatory prodrugs, this property could be attributed to the parent molecules with mechanism other than COX inhibition, particularly through formulations capable of slowing down their metabolic conversion. In this work, a pilot docking study aimed at comparing the interaction of two prodrugs, nabumetone (NB) and its tricyclic analog 7-methoxy-2,3-dihydro-1H-cyclopenta[b]naphthalen-1-one (MC), and their common active metabolite 6-methoxy-2-naphthylacetic acid (MNA) with the COX binding site, was carried out. Cytotoxicity, cytofluorimetry, and protein expression assays on prodrugs were also performed to assess their potential as antiproliferative agents that could help hypothesize an effective use as anticancer therapeutics. Encouraging results suggest that the studied compounds could act not only as precursors of the anti-inflammatory metabolite, but also as direct antiproliferative agents.

Synthesize of New Ibuprofen and Naproxen Sulphonamide Conjugate with Anti-Inflammatory Study and Molecular Docking Study

2018 ◽  
Vol 9 (2) ◽  
Author(s):  
Tagreed N-A Omar ◽  
Monther F Mahdi ◽  
May Mohammed Jawad Al-Mudhafar ◽  
ZainabBassim .
Keyword(s):  
Pharmacological Study ◽  
Docking Study ◽  
Synthetic Approach ◽  
Molecular Docking Study ◽  
Nmr Data ◽  
Ft Ir ◽  
Inflammatory Drugs ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Gastric Irritation

Non-steroidal anti-inflammatory drugs (NSAIDs) contain free –COOH which thought to be responsible for the GI irritation associated with all traditional NSAIDs. The esterification of this group is one of an approach to ultimate aim for reduce the gastric irritation; so in this study we synthesized and preliminarily evaluated new ester compounds as new analogues with expected selectivity toward COX-2 enzyme. Synthetic procedures have been successfully developed for the generation of the target compounds (III a and b). The synthetic approach involved multi-steps procedures which include: Synthesis of 4-hydroxy benzene sulphonamide ( I b ), synthesis of Naproxen and Ibuprofen acyl chloride and then reacting them with 4-hydroxy benzene sulphonamide to form final compounds ( III a-b) .The structures of these compounds were identified and characterized using (TLC), infrared spectroscopy (FT-IR), 1H NMR data and microanalysis (CHN). Pharmacological study as anti-inflammatory activities for the final compounds were studied in rats by induced edema type of inflammation. Moreover, the results of a docking study of compounds III a-b into the COX-2 binding site revealed that its mechanism was possibly similar to that of naproxen, a COX-2 inhibitor. The effect of them on COX-2 antibody was showed it could significantly inhibit COX-2 activity.

scholarly journals Review: The choice and cardiovascular safety of particular nonsteroidal anti-inflammatory drugs

2018 ◽  
Vol 24 (1) ◽  
pp. 16-21
Author(s):  
Jonas Černeckis ◽  
Austėja Samuolytė ◽  
Greta Baltušytė ◽  
Rugilė Ivanickaitė ◽  
Kristijonas Puteikis
Keyword(s):  
Rheumatoid Arthritis ◽  
European Medicines Agency ◽  
Cardiovascular Safety ◽  
Menstrual Pain ◽  
Over The Counter ◽  
Wide Range ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Effective Use ◽  
Superiority Trials

Abstract Nonsteroidal anti-inflammatory drugs (NSAIDs) are authorized for the relief of pain and inflammation in a wide range of conditions including the discomfort associated with headaches, osteoarthritis, rheumatoid arthritis, and menstrual pain and are available by prescription or over-the-counter (OTC). We reviewed common adverse effects of NSAIDs (especially those related to cardiovascular [CV] system) along with NICE (National Institute for Health and Care Excellence), EMA (European Medicines Agency), and the FDA (U.S. Food and Drug Administration) guidelines for safe and effective use of particular NSAIDs. Furthermore, we examined the NSAIDs market in Lithuania in a period between June 2016 and May 2017 and discussed how well recommendations mentioned above were followed. We emphasized that there was a high percentage of diclofenac prescribed in Lithuania while international guidelines encourage prescribing ibuprofen or naproxen for their relatively lower CV risk. Reviewing past trials, we observed that despite existing guidelines no single NSAID could be considered to be the safest one due to a lack of superiority trials

Polyphenols from Cymbopogon citratus inhibit iNOS expression and NO production – a promising source of new anti-inflammatory drugs

Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
V Francisco ◽  
A Figueirinha ◽  
B Neves ◽  
C Garcia-Rodriguez ◽  
M Lopes ◽  
...  
Keyword(s):  
Inos Expression ◽  
No Production ◽  
Cymbopogon Citratus ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Promising Source

Heparin and proteoglycans as anti-inflammatory drugs

1996 ◽  
Vol 16 (01) ◽  
pp. 56-59
Author(s):  
D. J. Tyrrell ◽  
C. P. Page
Keyword(s):  
Inflammatory Diseases ◽  
Therapeutic Applications ◽  
Wide Range ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

SummaryEvidence continues to accumulate that the pleiotropic nature of heparin (beyond its anticoagulant potency) includes anti-inflammatory activities at a number of levels. It is clear that drugs exploiting these anti-inflammatory activities of heparin may offer exciting new therapeutic applications to the treatment of a wide range of inflammatory diseases.

Non-Steroidal Anti-inflammatory Drugs (NSAIDs): Synthesis of Ibuprofen, Naproxen and Nabumetone

2019 ◽  
pp. 19-27
Keyword(s):  
Review Paper ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Synthetic Approaches

This review paper covers the major synthetic approaches attempted towards the synthesis of some Non-Steroidal Anti-Inflammatory Drugs (Naproxen, Ibuprofen and Nabumetone)

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