XO is a xanthine oxidoreductase enzyme that generates reactive oxygen species, catalyzes the oxidation of hypoxanthine to xanthine, and further catalyzes the oxidation of xanthine to uric acid. This enzyme has been reported to play a potential role in the progression and development of various cancers. Curcumin has been reported to inhibit PMA-induced XO activation. In contrast, another study reported that curcumin had no effect on XO activity. Computational and molecular docking studies have shown that curcumin directly interacted with XO. Curcumin bounds and interacts with XO on residues Phe914, Phe1009, and Thr1010, thus reducing their activation. Curcumin metabolites have been shown to bind XO more efficiently than the parent compound, curcumin. This study highlighted the activity of the metabolites curcumin, which exhibited greater biological activity than the parent compound against XO.