Arylxanthones with anti-inflammator potential in cellular systems
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resumo
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.
