Investigation of the non-polar (rich in chlorophyll) and polar fractions of the ethyl acetate extract of Gymnosporia senegalensis (Lam.) Loes. leaves led to the isolation of nine compounds, including one new megastigmane derivative, (3R*,5S*,6R*,7E,9ξ)-7-megastigmene-3,6,9-triol-3-O-β-D-(6′-O-galloyl)glucopyranoside (1), four known galloylated derivatives (2, 3, 8, 9), three known chlorophyll derivatives (4–6), and one known fatty acid (7). The structures of the isolates were determined by means of spectroscopic and spectrometric data, as well as by comparison with literature values. The extracts and isolated compounds were tested for their antibacterial, antifungal, and antioxidant activities. The isolates showed weak to high antimicrobial activities with phaeophytin A (4) being the most active one whereas phaeophorbide-a (5) and Chlorine e6 trimethyl ester (6) exhibited the highest antioxidant activities.