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Many medicinal plants found in Africa, such as <i>Dovyallis caffra</i>, have been reported to contain various bioactive compounds, which have been found to reduce metal salts into their corresponding metal-based nanoparticles. In this paper, the evaluation of synthesis, characterization, and biological properties of <i>Dovyallis caffra</i>-mediated cassiterite (SnO₂) nanoparticles was carried out. The physicochemical properties of the synthesized material were investigated using X-ray diffraction (XRD), energy dispersive X-ray analysis (EDX), scanning electron microscopy (SEM), and transmission electron microscopy (TEM) techniques. The characterization studies revealed that the material possessed a single tetragonal cassiterite SnO₂ phase, having a cluster-like foam appearance and an irregular spherical morphology with diameters ranging from 6.57 to 34.03 nm. The biological screening revealed that the prepared cassiterite (SnO₂) nanoparticles exhibited cytotoxicity against the MCF-7 breast cancer cells, with an IC₅₀ value of 62.33 µg mL⁻¹, better than the standard drug 5-fluorouracil, with an IC₅₀ value of 71.21 µg mL⁻¹. The radical scavenging potential of the nanoparticles, using the DPPH assay, showed that it possessed a slightly better activity than ascorbic acid, a common antioxidant. These results suggest that the <i>Dovyallis caffra</i>-mediated cassiterite (SnO₂) nanoparticles possess the potential to simultaneously generate and scavenge excess ROS, which in turn results in the exhibition of good cytotoxicity and antioxidant properties.