Objective: Dysphania ambrosioides (L.) Mosyakin & Clemants (Amaranthaceae), is a medicinal plant traditionally used for the treatment of pain, skin inflammations, fractures, and cardiac diseases. This study aimed to review the main phytochemical constituents from D. ambrosoides leaves, and the structure-activity relation of different compounds. Methodology: literature review, carried out between December 2022 and April 2023, through a bibliographic survey, in accordance with the recommended guidelines of PRISMA. The following descriptors were used “Dysphania ambrosioides”, “Chenopodium ambrosioides”, “leaves”, “traditional uses”, and “phytochemical constituents”, combining them with Boolean operators “AND” e “OR”, using electronic databases PubMed, and Google Scholar, published in the last 20 years and that addressed the theme. Results: D. ambrosioides is a promising ethnomedicinal plant and its leaves are a source of bioactive compounds such as α-terpinene, α-terpinenyl-acetate, beta-cymene, p-cymene, piperitone, carvyl acetate, piperitol acetate, trans-ascaridol, carvacrol, thymol, and limonene. In addition, chrysin, patulin, piperoylpiperidine, and scopoletin are present in this species. For these, the literature reports different mechanisms of action: PPAR –y agonist, Inhibitor of aromatase, Activation of the L-arginine/NO/cGMP/KATP pathway, an inhibitor of fatty acid synthase, Increase in glutathione peroxidase, and superoxide dismutase. Final considerations: more extensive number of preclinical pharmacological studies are performed to elucidate the molecular mechanisms of the components of the Phyto complex (bioactive constituents) isolated from D. ambrosioides leaves so that there is greater progress in the scientific validation for the use of the leaves as a source of therapeutic agents.