The resistance of Plasmodium falciparum (P. falciparum) to well-recognized antimalarial drugs is now common in nearly every area of its prevalence; consequently, there is a need to explore therapeutic plants that have bioactive compounds which can be utilized in the manufacture of antimalarial drugs. The in vitro potency of the volatile oil (VO) of Xylopia aethiopica (X. aethiopica) was evaluated against P. falciparum 3D7 strain, a human malaria parasite, a good activity against the parasite P. falciparum was recorded with an IC50 of 14 µg/mL. The in vitro cytotoxicity of the fruit oil of X. aethiopica was determined at a concentration of 50 µg/mL against HeLa cells and was found to show no cytotoxicity effect at this concentration; this could be an indication of the safety of the fruit oil as a targeted drug for mammalian organisms. , The antibacterial property of the VO from the fruit of X. aethiopica, was evaluated in vitro; the fruit oil exhibited good antimicrobial activity against the tested microorganisms, with Klebsiella pneumoniae having the highest inhibition zone of 19.0 ± 1.4 mm. The result recorded for MBC/MFC confirms that VO of this plant can be used in therapeutic preparations, particularly in the infections brought about by some of these microorganisms as practiced by traditional healers in folkloric medicines. This appears to justify the numerous folkloric therapeutic uses of the aerial parts of this plant. The hydro distilled volatile oil from X. aethiopica was characterized by Gas Chromatography-Mass Spectrometry (GC-MS), an abundance of monoterpenes hydrocarbon (58.0%), followed by oxygenated monoterpenes (30.13%), sesquiterpene hydrocarbon (8.96%), and fatty acid (0.74%) were well represented. The significant quantitative constituents of the fruit oil are 1, 8-cineole (16.73%), β-pinene (11.59%), sabinene (10.76%), 1R-α-pinene (8.30%), α-phellandrene (8.34%).