Abstract: Mikania cordata is a medicinal plant traditionally used as an antibacterial, anti-ulcer, anti-inflammatory, antihelmintic and analgesic agent. The potential of M. cordata as an anti-cancer agent has not been explored thus far. This study aims to assess M. cordata as a possible anti-cancer agent, specifically against MCF-7 breast cancer cells. Ethanol extract-vacuum liquid chromatography fractions inhibited proliferation of the MCF-7 cells via different mechanisms. Fraction 6 induces non-specific cytotoxicity via apoptosis and oxidative pathways demonstrated by the TUNEL and DPPH assays. Fractions 7, 10 and 11 exhibit selective cytotoxicity against MCF-7 breast cancer cells but does so through mechanisms other than apoptosis and oxidation. The results suggest that novel mechanisms of action may be at work, imparting cancer-specific cytotoxicity properties of these fractions. Phytochemical screening suggests terpenes and saponins as the possible anti-cancer agent in M. cordata.