Journal
MOLECULES
Volume 26, Issue 13, Pages -Publisher
MDPI
DOI: 10.3390/molecules26133940
Keywords
COX-1; COX-2; nabumetone; molecular docking; anti-enzymatic assays; cell toxicity
Funding
- special award Department of Excellence [232/2016]
- Sistema Integrato di Laboratori per l'Ambiente-(SILA) [PONa3_00341]
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This study compared the interaction of two prodrugs and their active metabolite with the COX binding site, and assessed their potential as antiproliferative agents through cytotoxicity, cytofluorimetry, and protein expression assays. Encouraging results suggest that the compounds could act not only as precursors of the anti-inflammatory metabolite, but also as direct antiproliferative agents.
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.
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