Hypericum androsaemum L. ethanol:water extract acted as a lipid peroxidation inhibitor and free radical scavenger. A marked inhibition of the growth of breast, lung, cervical and hepatocellular human carcinoma cell lines was also observed, whereas no toxicity was shown against non-tumor porcine liver cells (>400μg/mL). The extract was also effective in inhibiting nitric oxide production, as an indicator of the anti-inflammatory potential. The anti-Candida effects varied among different strains of the same species, C. glabrata and C. tropicalis being the most sensible species with an effect directly related with the extract concentrations tested. A significant anti-biofilm formation potential was also observed, namely for C. glabrata and C. tropicalis (biofilm reduction >90%). 5-O-Caffeoylquinic and 3-O-caffeoylquinic acids were the most abundant phenolic compounds identified in the extract, and might be related with the observed bioactive effects. Nevertheless, future studies should be carried out to obtain dose-response curves of the isolated active compounds, in order to perform further pre-clinically testing to quantify the presence of the most active compounds in the extract.