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Purpose: To determine the bioactive compounds in Moringa oleifera (MO) and Acanthospermum hispidum (AH) with antioxidant, anticancer, antifungal and antibacterial potentials. Methods: Fresh leaves of these plants were collected from Akinmoorin and Awe, Oyo State, Nigeria. Particle-induced x-ray emission (PIXE) technique was performed using a 2.5MeV proton beam (a non- destructive elemental analysis). Phytochemicals were qualitatively analyzed using High-performance liquid chromatography (HPLC), gas chromatographic-mass spectrophotometer (GC-MS) and standard procedures. Disc diffusion method was used to determine the minimum inhibitory concentration (MIC) for fungi and bacteria. Antioxidant properties were carried out by DPPH radical scavenging activity. Cancer cells (MDAMB 231 and HTC 15) were cultivated in the presence of the extracts at body temperature with 5 % CO2 and 95 % air in 100 % relative humidity. Thereafter, adherent cells were seeded and treated with increasing concentrations of the plant extracts for 48 - 72 h. Results: Phytochemical analysis showed that both plants contain alkaloids, flavonoids, anthraquinones, steroids and terpenoids, saponins, tannins, phenols and glycosides. The MIC for MO on fungi was 21.0 and 12.0 mg/mL for AH. Furthermore, MO MIC for bacteria was 25.25 mg/mL and 9.75 mg/mL for AH. Antioxidant properties revealed MO having 80.02 % and AH, 76 % at 32.00 µL. The ethanolic extracts showed a 50 % reduction in cancer cell viability at 24.5 µg/mL for MO and 16.0 µg/mL for AH, respectively, on MDAMB 231 and HTC 15 cells. Conclusion: Moringa oleifera (MO) and Acanthospermum hispidum (AH) extracts exhibit significant antioxidant, antitumor, antifungal and antibacterial activities. Further studies will require that the active constituents be isolated and formulated into suitable dosage forms. [ABSTRACT FROM AUTHOR]