Background: It is estimated that in Brazil 59,700 new cases of breast and 68,220 new cases of prostate cancer will occur, in 2018, in Brazil. For that reason, there is a need for introducing new antitumor drugs in therapy. Objective: The objective of the study is to bioguide fractionate the organic/aqueous extracts from the aerial organs of Picrolemma sprucei (EB1151 and EB1152) aiming the identification of antitumor compounds and to evaluate the influence of EB1151 on mice behavioral phenotype. Materials and Methods: The breast (MCF-7) and prostate (PC-3) cancer cell lines cytotoxicity assay were assessed using the sulforhodamine B method. Fractionation was carried out by thin layer and column chromatographic techniques. The influence of the intraperitoneal administration of nonlethal dose (NLD, 39.1 mg/kg) of EB1151 to Balb-c male mice was assessed in open cage and open-field (OF) apparatuses. Results: FCHCl3partition phases from EB1151 and EB1152 showed cytotoxic activity against both cancer cells, as did fractions UNIP343, which contains sergeolide and isobruceine B, and UNIP344, which contains sergeolide and 15-deacetylsergeolide. Higher doses of EB1151 showed significant alterations in response to touch, hindquarter fall, irritability, auricular and corneal reflexes, ataxia, micturition, ptosis, piloerection, hypothermia, and cyanosis, and NLD showed alterations in general activity and response to touch, but recovery was obtained up to the end of the experiment. Conclusions: Quassinosides from the aerial organs of P. sprucei showed significant cytotoxicity against MCF-7 and PC-3 cell lines. Extract EB1151 has impaired general activity and activity in the OF apparatus, but recovery was observed.