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Trihydroxyflavones with antioxidant and anti-inflammatory efficacy.
MedLine Citation:
PMID:  22806885     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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 B(4) 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.
Authors:
Ana Gomes; Diana Couto; Andreia Alves; Irene Dias; Marisa Freitas; Graça Porto; José Alberto Duarte; Eduarda Fernandes
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-7-17
Journal Detail:
Title:  BioFactors (Oxford, England)     Volume:  -     ISSN:  1872-8081     ISO Abbreviation:  -     Publication Date:  2012 Jul 
Date Detail:
Created Date:  2012-7-18     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8807441     Medline TA:  Biofactors     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012 International Union of Biochemistry and Molecular Biology, Inc.
Affiliation:
REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal; CIAFEL, Departamento de Biologia do Desporto, Faculdade de Desporto, Universidade do Porto, Rua Dr. Plácido Costa, 91, 4200-450 Porto, Portugal.
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