Chromatographic investigation of the Citharexylum quadrangulare leaves led to isolation of nine compounds viz., stigmasterol (1), β-sitosterol (2), oleanolic acid (3), duranterectoside B (4), durantoside I (5), cirsimaritin 4'-O-β-D-glucopyranoside (6), 5-deoxypulchelloside (7), lamiide (8) and cirsimaritin 4'-O-β-D-glucopyranoside 4"-sodium sulphate (9). The compounds (1, 3 and 4) were isolated for the first time from genus Citharexylum. The structures of the isolated compounds were determined by interpretation of their spectroscopical data and comparison with published literature. The aqueous fraction exhibited the most significant anti-inflammatory activity. Its effect was more potent than the reference drug. While, the most significant anti-pyretic sample was the total methanol extract. Also, it showed a gastroprotective activity with preventive index (78%). Finally, the ethyl acetate fraction demonstrated a significant decrease in blood glucose level on hyperglycemic alloxaned rats.