In recent years, Biophytum umbraculum Welw. (Oxalidaceae) has undergone several phytochemical and pharmacological investigations. Although its major phytochemical clas-ses have been characterized, few isolated compounds have been reported. The previously detected phytoconstituents, along with the documented antioxidant and an-ti-inflammatory activities, both align with a potential antiproliferative effect. This study aims to complement the existing chemotaxonomic profile of B. umbraculum through isola-tion and identification of phytoconstituents and to evaluate the antiproliferative potential of its extracts. Hexane, ethyl acetate, and methanolic extracts of B. umbraculum were screened against two human adherent cell lines: breast (MCF-7) and cervical (SiSo) ade-nocarcinomas, by using the crystal violet staining (CVS) assay. The hexane extract inhib-ited both MCF-7 and SiSo cell proliferation with IC50 values of 8.93 ± 0.07 and 14.59 ± 0.08 µg/mL, respectively. The ethyl acetate extract showed activity against both cell lines with IC50 values of 12.60 ± 0.14 and 13.10 ± 0.04 µg/mL, respectively. The methanolic extract was inactive on the MCF-7 cell line and only slightly active on the SISO cell line. Chromatographic fractionations led to the isolation of ursolic acid from the active ethyl acetate extract, and rutin from the methanolic extract. A further antiproliferative evalua-tion is warranted to confirm the contribution of ursolic acid on the effect of the ethyl acetate extract. Additional fractionations may uncover more phytoconstituents of diverse pharmaceutical interests