Ludwigia hyssopifolia was used in folk practices to treat jaundice diseases in many Asian countries. This study aims to evaluate the antioxidant and anti-cancerous properties of the solvent extractives. The crude ethanolic extract and its fractions (chloroform, ethyl acetate, and methanol) were prepared from the whole plants. These extracts were subjected to DPPH assay to determine the antioxidant properties. An MTT assay was performed to investigate the cytotoxic activity against HepG2 cells. The volatile compounds from the ethanolic extract were identified by GC-MS technique. Total polyphenol and total flavonoid contents were determined by the spectrophotometric method. From the ethanolic extract of the whole plant, 15 phytoconstituents were analyzed. Crocetane (19.40%), heneicosane (14.85%), and 3,5-di-tert-butylphenol (14.82%) were identified as the main phytoconstituents. The ethyl acetate and methanolic fraction had the highest total polyphenol and flavonoid contents. Ethyl acetate and methanolic fractions had the best DPPH radical scavenging activity. Ethanolic extract and chloroform fraction showed the most potential anti-HepG2 activity. Ludwigia hyssopifolia represents a promising resource for developing of potential antioxidant and hepatoprotective products.