Arylxanthones with anti-inflammator potential in cellular systems Conference Paper uri icon


  • Sincere thanks are expressed to Faculdade de Farmácia da Universidade do Porto, Universidade de Aveiro, Instituto Politécnico de Bragança, Fundação para a Ciência e a Tecnologia (FCT, Portugal), European Union, FEDER, PT 2020, QREN, and COMPETE funding UCIBIO, REQUIMTE [(PT2020 UID/MULTI/04378/2013 - POCI/01/0145/FEDER/007728), (NORTE-01-0145-FEDER-000024), and (PTDC/QEQ-QAN/1742/2014 – POCI- 01-0145-FEDER-016530)] and QOPNA (FCT UID/QUI/00062/2013) Research Units.
  • Xanthones are a family of naturally-occurring oxygenated heterocyclic compounds. A wide range of natural and synthetic analogues are known to possess diverse biological activities including antifungal, antimalarial, antioxidant and antitumor, among others [1]. There are only a few publications related to arylxanthones [2], most of them focused on arylxanthones synthetic strategies and their biomedical potential, mainly highlighting them as effective scavengers of reactive oxygen species (ROS) and reactive nitrogen species (RNS) [3,4]. As far as we know, the anti-inflammatory potential of xanthones bearing an aryl group has not been studied so far. With this idea in mind, our purpose was to evaluate the putative anti-inflammatory effects of several arylxanthones bearing hydroxyl groups in certain positions of their main core, namely through their ability to inhibit 5-lipoxygenase (5-LOX) and cyclooxygenase 1 (COX-1) and 2 (COX-2), both enzymes involved in the arachidonic acid metabolism [5,6]. Preliminary results showed that some of the studied arylxanthones were able to prevent leukotriene B4 production in human neutrophils, the xanthone with a catechol group at position 2 being the most active one. The inhibition of prostaglandin E2 production was assessed in human whole blood and the majority of the tested compounds were able to inhibit COX-1 while being completely ineffective in COX-2.

publication date

  • January 1, 2016