Does inhibition of aldose reductase contribute to the anti-inflammatory action of setipiprant?
Jazyk angličtina Země Česko Médium print-electronic
Typ dokumentu časopisecké články
PubMed
28406694
DOI
10.33549/physiolres.933516
PII: 933516
Knihovny.cz E-zdroje
- MeSH
- aldehydreduktasa antagonisté a inhibitory metabolismus MeSH
- antiflogistika chemie farmakologie MeSH
- indoly chemie farmakologie MeSH
- inhibitory enzymů metabolismus farmakologie MeSH
- krysa rodu Rattus MeSH
- lidé MeSH
- NADP metabolismus MeSH
- naftaleny chemie farmakologie MeSH
- potkani Wistar MeSH
- simulace molekulového dockingu metody MeSH
- vazebná místa fyziologie MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- lidé MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido(4,3-b)indol-5(2H)-yl)acetic acid MeSH Prohlížeč
- AKR1B1 protein, human MeSH Prohlížeč
- aldehydreduktasa MeSH
- antiflogistika MeSH
- indoly MeSH
- inhibitory enzymů MeSH
- NADP MeSH
- naftaleny MeSH
The aim of this study was to investigate aldose reductase inhibitory action of setipiprant as a potential additional mechanism contributing to its anti-inflammatory action. Aldose reductase activity was determined by spectrophotometric measuring of NADPH consumption. Setipiprant was found to inhibit aldose reductase/NADPH-mediated reduction of 4-hydroxynonenal, 4-hydroxynonenal glutathione and prostaglandin H2 substrates, all relevant to the process of inflammation. Molecular modeling simulations into the aldose reductase inhibitor binding site revealed an interaction pattern of setipiprant. Considering multifactorial etiology of inflammatory pathologies, it is suggested that, in addition to the antagonizing prostaglandin D2 receptor, inhibition of aldose reductase may contribute to the reported anti-inflammatory action of setipiprant.
Institute of Experimental Pharmacology and Toxicology Slovak Academy of Sciences Bratislava Slovakia
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