Oxidative stress, a contributing factor to numerous diseases such as inflammation, has sparked increased interest in the search for natural antioxidants known for their biodegradability and low toxicity. In this study, we investigated Aristolochia trilabiata, a plant native to the Brazilian Amazon, as a potential source of bioactive compounds. Using the "reverse ethnopharmacology" method, we collected valuable information on the medicinal uses of A. trilabiata. A total of 15 families were interviewed, and remarkably 40% reported medicinal uses of decoction and infusion of its leaves mainly to treat inflammation, pain, and urinary issues. Otherwise, 27% were aware without details, and 33% had no knowledge about the species. Since inflammation was described as medicinal use, our study focused on the antioxidant capacities of the aqueous extract (ExtH2O) and its methanolic (FrMeOH) and aqueous (FrH2O) fractions from the leaves of A. trilabiata, associated with their molecular profiles. Thus, the antioxidant capacities of aqueous extract and its fractions were evaluated by oxygen radical absorbance capacity (ORAC) assays. The molecular profile was assessed via Liquid chromatography-mass spectrometry (LC-MS/MS) and nuclear magnetic resonance (NMR) analysis. As a result, FrMeOH exhibited a potent antioxidant capacity (4.94 mmol TE/g), confirmed promising ability against oxygen-derived free radicals, and it was associated mainly with eriodictyol and blumenol C-derived compounds, which beyond potent antioxidant effects, could be associated with anti-inflammatory properties, making A. trilabiata a promising natural source of bioactive that opens exciting avenues for further research and utilization in medicine and natural product discovery.