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Background: Pequi (Caryocar brasiliense Camb.) is a fruit from Brazilian Cerrado rich in bioactive compounds, such as phytosterols and tocopherols, which can modulate the death of cancer cells. Objective: In the present study, the main bioactive compounds of hydrophilic and lipophilic extracts of pequi oil and pulp were identified and were verified if they exert modulatory effects on oxidative stress of mononuclear cells cocultured with MCF-7 breast cancer cells. Study design: Identification and quantification of the main compounds and classes of bioactive compounds in pequi pulp and oil, hydrophilic, and lipophilic extracts were performed using spectroscopy and liquid chromatographic methods, while the beneficial effects, such as antioxidant capacity in vitro, were determined using methods based on single electron transfer reaction or hydrogen atom transfer, while for antioxidant and antiproliferative activities ex vivo, 20 healthy volunteers were recruited. Human peripheral blood mononuclear cells (MN) were collected, and cellular viability assay by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide), superoxide anion evaluation, and CuZn-superoxide dismutase determination (CuZn-SOD) in MN cells, MCF-7 cells, and coculture of MN cells and MCF-7 cells in the presence and absence of pequi pulp or oil hydrophilic and lipophilic extracts were performed. Results: In the hydrophilic extract, the pequi pulp presented the highest phenolic content, while in the oil lipophilic extract, it had the highest content of carotenoids. The main phytosterol in pequi oil was β-sitosterol (10.22 mg/g), and the main tocopherol was γ-tocopherol (26.24 µg/g sample). The extracts that had highest content of bioactive compounds stimulated blood mononuclear cells and also improved SOD activity. By evaluating the extracts against MCF-7 cells and coculture, they showed cytotoxic activity. Conclusion: The results support the anticarcinogenic activity of pequi extracts, in which the pequi pulp hydrophilic extracts presented better immunomodulatory potential. [ABSTRACT FROM AUTHOR]