Extracts of the marine microalgae Nannochloropsis oculata were obtained using 80% methanol (MeOH) and water. The 80% MeOH extract was further fractionated with n-hexane, chloroform, ethyl acetate (EtOAc), n-butanol (n-BuOH), and water to isolate the active fraction. Seven samples were prepared and their angiotensin converting enzyme (ACE), $alpha$-glucosidase, and cancer cell growth inhibitory activities in vitro were determined. The most profound ACE inhibitory activity was observed in the chloroform fraction, while the others had moderate effects. By contrast, greater $alpha$-glucosidase inhibitory activity was found in the EtOAc fraction, n-hexane fraction, and water extract of N. oculata. The antiproliferative effects of the extracts and fractions against HL-60, U937, CT-26, and SK-Hep1 cancer cells were also determined. The n-BuOH fraction had the strongest antiproliferative effects on CT-26 cells in a time-dependant manner (P<0.05). These results suggest that the extracts and fractions from N. oculata could be used as a potential functional food or as pharmaceutical ingredients.