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Advisor(s)
Abstract(s)
The purpose of this study was the evaluation of the
xanthine oxidase (XO) inhibition produced by some
synthetic 2-styrylchromones. Ten polyhydroxylated
derivatives with several substitution patterns were
synthesised, and these and a positive control, allopurinol,
were tested for their effects on XO activity by
measuring the formation of uric acid from xanthine. The
synthesised 2-styrylchromones inhibited xanthine oxidase
in a concentration-dependent and non-competitive
manner. Some IC50 values found were as low as 0.55mM,
which, by comparison with the IC50 found for allopurinol
(5.43 mM), indicates promising new inhibitors.
Those 2-styrylchromones found to be potent XO
inhibitors should be further evaluated as potential
agents for the treatment of pathologies related to the
enzyme’s activity, as is the case of gout, ischaemia/
reperfusion damage, hypertension, hepatitis and cancer.
Description
Keywords
2-Styrylchromones Allopurinol Benzopyrone Xanthine oxidase inhibition
Citation
Fernandes, Eduarda; Carvalho, Félix; Silva, Artur; Santos, Clementina; Pinto, Diana; Cavaleiro, José; Bastos, Maria de Lourdes (2002). 2-Styrylchromones as novel inhibitors of xanthine oxidase. A structure-activity study. ISSN 1475-6366. 17:1, p. 45-48
Publisher
Taylor & Francis