Wounds are classified as neglected tropical diseases. Herbal medicines are widely used and play a significant role in the alternative management of infectious diseases, including chronic wounds, ulcers and injuries. The overall aim of this study is to evaluate the antioxidant activity and major compounds of the hydroethanolic extract of the leafy stems of Ageratum conizoides, following in vitro testing for cytotoxic activity. Phytochemical analysis was carried out using the standard differential reaction method. The major compounds with proven pharmacological properties were identified using UV-visible absorption spectrophotometry at characteristic maximum absorption wavelengths. Antioxidant activity was determined using the DPPH radical scavenging assay. Cytotoxic activity was determined using the Artemia salina cell mortality rate assay. The hydroethanolic crude extract contains higher amounts of saponins (957.2±2.42 mgEqAG/g), condensed tannins (491.02±1.03 mgEqCAT/g) and alkaloids (411.15±10.66 mgEqAG/g) than phenolic compounds (389.70 ± 0.36 mgEqAG/g), flavonoids (380.57 ± 2.15 mgEqAG/g) and triterpenes (310.50 ± 0.26 mgEqAG/g). The hydroethanolic extract significantly reduced the DPPH radical with a half-maximal inhibitory concentration (IC₅₀) of 6.98 mg/mL. No cellular safety was observed for the extract with an LC50 of 1.62 mg/ml.