Arylxanthones with anti-inflammator potential in cellular systems
Conference Paper
Overview
Overview
abstract
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.
