The Open Conference Proceedings Journal

2013, 4 : 286 -286
Published online 2013 March 01. DOI: 10.2174/2210289201304010286
Publisher ID: TOPROCJ-4-4-286

Xanthine Oxidase Inhibitory Activity of Selected Chalcone Derivatives

Khairana Husain , Lam Kok Wai , Fadzureena Jamaluddin , Jamia Azdina Jamal and Nurnajmul Ummah Abu
Drug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur.

ABSTRACT

Xanthine oxidase (XO) is a key molybdoflavoprotein enzyme that functions in catalysing the oxidation of hypoxanthine and xanthine to uric acid. Excessive uric acid will results in hyperuricaemia which is the crucial cause of gout. In the present study, a series of thirty-five of chalcone derivatives were evaluated for inhibitory activity against xanthine oxidase in vitro. From the study, seventeen compounds (47.2%) exhibited XO inhibitory activity at 200 µg/mL which only four compounds (0.1%) inhibited XO activity at more than 50%. Compound 14, 1,3-bis(4-hydroxyphenyl)prop-2-en-1-one, showed the strongest activity more than 50% at 20 µg/mL with IC50 values of 15.31 µg/mL as compared to positive control of allopurinol (IC50 =12.86 µg/mL ). The results suggest that compounds 14 can be further investigated to be developed into a XO inhibitor.

Keywords:

Chalcone , Xanthine oxidase , Inhibitor .