title: Flavonoids inhibit COX-1 and COX-2 enzymes and cytokine/chemokine production in human whole blood.
abstract: Cyclooxygenase 2 (COX-2) and the production of cytokines/chemokines are important targets for the modulation of the inflammatory response. Although a large variety of inhibitors of these pathways have been commercialized, some of those inhibitors present severe side effects, governing the search for new molecules, as alternative anti-inflammatory agents. This study was undertaken to study an hitherto not evaluated group of flavonoids, concerning its capacity to inhibit COX-1 and COX-2 enzymes, as well as to inhibit the production of the cytokines and a chemokine, in a complex matrix involved in the systemic inflammatory process, the blood, aiming the establishment of a structure-activity relationship. The results obtained reveal promising flavonoids for the modulation of the inflammatory process, namely the ones presenting a catechol group in B ring, as some flavonoids were able to simultaneously inhibit the production of inflammatory prostaglandin E2 and pro-inflammatory cytokines.
authors.affiliation: REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira n 228, 4050-313, Porto, Portugal.
authors.forename: Daniela
authors.initials: D
authors.lastname: Ribeiro
authors.forename: Marisa
authors.initials: M
authors.lastname: Freitas
authors.forename: Sara M
authors.initials: SM
authors.lastname: Tomé
authors.forename: Artur M S
authors.initials: AM
authors.lastname: Silva
authors.forename: Stefan
authors.initials: S
authors.lastname: Laufer
authors.forename: José L F C
authors.initials: JL
authors.lastname: Lima
authors.forename: Eduarda
authors.initials: E
authors.lastname: Fernandes
mesh_terms: D018925:Chemokines / Q000037:antagonists & inhibitors* / Q000097:blood; D051545:Cyclooxygenase 1 / Q000097:blood; D051546:Cyclooxygenase 2 / Q000097:blood; D052246:Cyclooxygenase 2 Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D016207:Cytokines / Q000037:antagonists & inhibitors* / Q000097:blood; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans
chemical_list: D018925:Chemokines; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D016207:Cytokines; D005419:Flavonoids; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; C496511:PTGS1 protein, human; C496540:PTGS2 protein, human