In the present study, the phenolic (Folin-Dennis) and flavonoid (colorimetric assay) constituents, antioxidant [2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH) assay] and cytotoxic activities of an aqueous extract (AE) of Centella asiatica leaves were investigated. The aqueous extract (50 g/L) was obtained by infusion followed by cold maceration for 24 h. The levels of phenolic and flavonoid compounds were 2.86 g/100 g and 0.361 g/100 g, respectively. The AE showed elevated DPPH scavenging activity, with an IC50 value of 31.25 mu g/mL. The AE had a promising activity against mouse melanoma (B16F1), human breast cancer (MDA MB-231) and rat glioma (C-6) cell lines, with IC50 values of 698.0, 648.0 and 1000.0 mu g/mL, respectively. A positive correlation was established between the level of flavonoids, antioxidant and antitumor activities.