The present investigation on this study was to assess the antioxidant and toxicological potentials of Tapinanthus globiferus leaf extract and its effects on inherent antioxidant enzymes. The leaf extracts of the plant were prepared with both aqueous and ethanolic solvents at 5% concentration levels. Antioxidant indices such as free radical scavenging ability [DPPH], iron chelation ability [Fe2+], hydroxyl radical scavenging ability [OH*], which are indices for radical scavenging potential of Tapinanthus globiferus were assessed. Toxicological effect of the plant extract was equally investigated on defensive antioxidant enzymes in rat liver. The results indicate that the extracts exhibited antioxidant properties at significant (P<0.05) levels where the radical scavenging ability of the extracts were ascertained with percentage inhibition in the range (65 – 41.1) % DPPH, (60 – 77.5) % Fe2+ chelation, (17.5 – 34.2) % OH*. Hence, highest percentage inhibition was observed against Fe2+ where the extract demonstrated high level of iron chelating ability at relatively low extract concentration (1.0mg/ml). Also the results from toxicological assay indicate synergistic effect of the extract on defensive antioxidant enzymes with concomitant increase in their activities corresponding to increase in extract concentration. The results suggest that Tapinanthus globiferus could serve as reliable antioxidant dietary supplement and perhaps not toxic at the concentrations investigated.