Ficus natalensis Subsp. leprieurii (miq) (F. natalensis) is an evergreen tree belonging to the family Moraceae and is widely distributed in Africa. The leaves of F. natalensis are well-known for their nutritional value and health benefits and were used traditionally to treat several ailments. The objective of this study was to identify the major classes of phytoconstituents, isolate some of them, and investigate the free radical scavenging potential of F. natalensis leaves. The leaves methanol extract of F. natalensis revealed an abundance of flavonoids, tannins, carbohydrates and/or glycosides, sterols, saponins, and triterpenes. Additionally, the total phenolic content (TPC) of F. natalensis methanol extract was 54.8 mg GAE/g and the total flavonoid content (TFC) was 14.78 mg RE/g. Moreover, three triterpenoid saponins were isolated from the methanol extract using different chromatographic techniques and identified by using 1D NMR together with mass spectrometry as 3-methoxy-quinovic acid-28-O-α-L-rhamnopyranoside ester (1), quinovic acid 3-O-methoxy (2), and 3-O-α-L-rhamnopyranoside-quinovic acid (3). Finally, the leaves methanol extract of F. natalensis revealed 2,2-diphenyl-1-picryhydrazyl (DPPH•) free radical scavenging capacity with IC50=80.22 μg/mL, compared to that of standard rutin (37.5 μg/mL) which suggests that F. natalensis could be a good source for phytochemical leads with higher antioxidant potential and health benefits.