Rosa heckeliana, as one of the wild-growing species of the family Rosacea, has a wide use in the folk medicine; however, scientifically there is very little known about it. Our objective was to examine the antioxidative and antiproliferative properties of Rosa heckeliana root extract and its phenolics. The phenolic constituents, namely catechin, caffeic acid, and ellagic acid, were obtained by the methods of extraction, fractionation, and purification through column chromatography. The DPPH and ABTS radical scavenging assays and total flavonoid content analysis were employed as the current antioxidant methods over the crude extract and fractionated parts. Among the extracts/fractions, the ethyl acetate fraction exhibited the highest amount of flavonoid content (4.58 +/- 0.018 mu g CE/mg of extract). The ethyl acetate fraction also displayed high antioxidative properties for DPPH (EC50 value: 2.78 +/- 0.01 mu g/mL) and ABTS scavenging capacities (586 +/- 6.64 mu M trolox as TEAC value). Additionally, the antiproliferative properties of the crude extract and the ethyl acetate fraction and its isolated constituents were evaluated for two breast cancer cell lines (MCF-7 and MDA-MB-231) using the XTT method. Acetate fraction over the cells of MCF-7 and MDA-MB-231 resulted in ED50 values of 61.18 +/- 0.99 mu g/mL and 62.54 +/- 2.01 mu g/mL, respectively. The isolated phenolic constituents were twice as effective as the ethyl acetate fraction on both MCF-7 and MDA-MB-231 cells.