Background: Bioactive compounds from the fruit of S. elaeagnifolium were isolated since could be highly potential source to develop functional foods or pharmaceutical products. Objectives: In this study a bioguided fractionation of the methanolic extract from S. elaeagnifolium fruit was carried out to evaluate their cytotoxicity and antitumoral potential on several cell lines and breast tumor explants, respectively. Methods: Microdilution method with A. salina was used to isolate bioactive compounds. Fractionation was performed by vacuum liquid chromatography, and the monitoring from fractions was done by thin layer chromatography. The effect of the fractions on viability in Vero, HeLa, and MCF-7 cells was assessed using WST-1 assay, whereas in breast tumor explants was evaluated by Alamar blue assay. A qualitative phytochemical analysis was performed to partially identify the compounds contained in the fractions and a spectroscopic characterization by RP-HPLC-MS was done to identify the group of compounds responsible for the effect on the cell lines and the mammary explants. Results: Several fractions were isolated from the fruit of S. elaeagnifolim. Notwithstanding, the FVLC7 showed a higher activity in A. salina assay. This fraction reduced the viability at 39 ± 1.67, 15.05 ± 0.09 and 66.10 ± 4 % in Vero, HeLa and MCF-7 cells, at 100 mg/mL, respectively. On the other hand, showed an effect in breast tumor explants obtained from a patient in remission. Qualitative phytochemical analysis showed that FVLC7 contains alkaloids, coumarins, and sesquiterpene lactones. Characterization by RP-HPLC-MS detected quinic acid, chlorogenic acid, dicaffeoylquinic acid as well as presence of an alkaloid. Conclusion: On this basis, our results suggest that cytotoxic effect of FVLC7 isolated from the fruit of S. elaeagnifolium could be mediated by quinic, chlorogenic, and dicaffeoylquinic acids.