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Rumex roseus L. ( R. roseus ) is acknowledged as an aromatic plant. For its excellent biological properties, it was used as a traditional medicine. The aim of the present study is to evaluate the chemical components and their effect as the biological activities of Tunisian extracts of R. roseus . Consecutive extractions by cold maceration of the aerial part with solvents of increasing polarity (cyclohexane (CYH), dichloromethane (DCM), and methanol (MeOH)) were performed, and the different chemical groups (phenolics, flavonoids, tannins, anthocyanins, etc.) were identified. In addition, the volatile compounds of the obtained extracts were identified before and after derivatization. Moreover, their antioxidant and anticancer activities were evaluated. The analysis of HPLC-DAD revealed the identification of 18 components from organic extracts, among them are, for example, chlorogenic acid and shikonin, while GC-MS analysis allowed the detection of 34 volatile compounds. Some of those compounds were identified for the first time in plant extracts such as pyrazolo[3,4-d] pyrimidine-3,4(2H,5H)-dione (1); L-proline (16); 2-amino-3-hydroxybutanoic acid (19); L-(-)-arabitol (23); D-(-)-fructopyranose (25); and D-(+)-talopyranose (27). DPPH tests revealed that the most important antioxidant activity was found in the methanolic extract with 75.2% inhibition at 50 mg/L and that the highest cytotoxic activity against HCT-116 and MCF-7 was recorded in the dichloromethane extract with 62.1 and 80.0% inhibition at 50 mg/L, respectively. The biological activities were fully correlated with the chemical composition of the different extracts. So, we can suggest that R. roseus is a source of bioactive molecules that could be considered potential alternatives for use in dietary supplements for the prevention or treatment of diseases., Competing Interests: The authors declare that they have no conflicts of interest regarding the work described in this manuscript., (Copyright © 2021 Mohamed Marouane Saoudi et al.)