Journal
BIOFACTORS
Volume 38, Issue 5, Pages 378-386Publisher
WILEY
DOI: 10.1002/biof.1033
Keywords
hydroxyflavones; oxidative burst; reactive oxygen species; reactive nitrogen species; cyclooxygenase-1; cyclooxygenase-2; 5-lipoxygenase
Funding
- Reitoria da Universidade do Porto for Projectos Pluridisciplinares para estimulo a Iniciacao a Investigacao na U. Porto'
- FCT [SFRH/BPD/63179/2009, SFRH/BD/72856/2010]
- FSE
- national funds of MCTES
- Fundação para a Ciência e a Tecnologia [SFRH/BD/72856/2010, SFRH/BPD/63179/2009] Funding Source: FCT
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The classical anti-inflammatory therapies are frequently ineffective and present numerous and severe side effects, especially in long term use, which requires the development of anti-inflammatory drugs with different scaffolds and mechanisms of action. Owing to the high antioxidant potential and anti-inflammatory activities already inferred for hydroxyflavones, we found it would be relevant to evaluate the anti-inflammatory potential of a series of trihydroxyflavones by testing their ability to scavenge reactive oxygen species (ROS) and reactive nitrogen species (RNS) in cells and cell-free systems and to inhibit the proinflammatory pathways mediated by the enzymes cyclooxygenase (COX) and 5-lipoxygenase (5-LOX), in which reactive species have a proven involvement. The tested trihydroxyflavones proved to be effective inhibitors of neutrophils' oxidative burst and were shown to scavenge different ROS and RNS in cell-free systems. The most active compound in the majority of the assays was 3,3',4'-trihydroxyflavone, which was somehow expected due to the presence of the ortho-dihydroxy in the B-ring, an important structural feature in terms of free radical scavenging activity. Additionally, the studied compounds were able to inhibit the production of leukotriene B4 by 5-LOX in activated neutrophils. 3,5,7-Trihydroxyflavone was able to inhibit both COX-1 and COX-2, which makes it a dual inhibitor of COX and 5-LOX pathways and, therefore, a promising candidate for a new therapeutic option in the treatment of inflammatory processes.
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