In this study, we isolated and characterized dichloromethane and hexane extracts, complexed with hydroxypropyl-β-cyclodextrin (HP-β-CD), of Schinus terebinthifolius fruits. Such complexation may be useful in the formulation of herbal medicines, by improving solubility, or increasing stability by reducing the loss of volatile compounds. The cytotoxicity in osteoblasts, antifungal against Malassezia furfur and antitumor activities were evaluated in Caco-2 cells. The antifungal activity of the extracts and the essential oil in natura or complexed with HP-β-CD against the fungus M. furfur was evaluated by agar diffusion methods and quantitatively by inhibitory concentration (IC). All samples inhibited fungus growth and, when complexed with HP-β-CD, the IC was reduced by 50%. Osteoblast cell viability was not affected by the presence of extracts and oil. The antitumor activity of the extract in dichloromethane was evaluated using Caco-2 cells. The results demonstrated significant reduction in cell viability in the presence of the extract, which makes it a promising candidate for cancer treatment.