Background: Gossypium herbaceum (G. herbaceum), a plant commonly found in the wild in Nigeria, is said to possess some therapeutic activities. However, there is a dearth of information on its chemical constituents. Also,there is a need to investigate its therapeutic activities. Objective: To investigate the qualitative and quantitative phytochemical components of the leaf extracts of G.herbaceum, as well as its antioxidant, antimalarial and cytotoxic activity. Methods: Gas chromatography-mass spectrometry (GC-MS) analysis was used to determine the components of ethanol and hexane extracts of G. herbaceum leaf while 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide assays were used to determine the antioxidant potential. Malaria parasites viability was examined using parasite lactate dehydrogenase (pLDH) technique and HeLa cell was used for the cytotoxicity evaluation. Results: Bioactive compounds identified in ethanol and hexane extracts of G. herbaceum were 37 and 30 kinds, respectively, with major components as linoleic acid (36.10% and 33.82%), vitamin E (7.15% and 5.98%) and caryophyllene (4.21% and 5.08%). It also has tannins, saponins, alkaloids, flavonoids steroids, phenols and terpenoids. In antibacterial test, significant inhibitory potentials against multidrug-resistant bacteria strains were present. In vitro antioxidant potentials (IC50) of ethanol and hexane extracts were 3.33 and 4.12 μg/mL for DPPH assays, and 3.87 and 5.00 μg/mL for nitric oxide assays, respectively. Antiplasmodial activities (IC50) were 9.99 and 9.76 μg/mL for ethanol and hexane extracts, respectively. Conclusion: G. herbaceum leaf may provide novel plant-derived therapeutic agents, effective in treating infectious diseases arising from multiple drug-resistant bacteria and a target in the management of oxidative stress.