Ruellia tuberosa L. (Acanthaceae) is a tropical perennial plant, native to Central America and widely distributed in Southeast Asia. In folkloric medicine, it has been used as diuretic, antidiabetic, antipyretic, analgesic, and anti-hypertensive, and as a thirst-quencher and antidote [1–3]. The leaves of R. tuberosa were collected in July 2007 from Orman Botanical Garden in Giza, Egypt. The air-dried and powdered leaves (3.10 kg) of R. tuberosa were extracted with 70% methanol (5 L 5), and then the extract was concentrated under reduced pressure to give a greenish residue (365 g). This residue was dissolved in water and successively extracted with n-hexane and n-BuOH. The n-BuOH fraction (150 g) was fractionated by various types of column chromatography to afford 13 known compounds. The compounds isolated were identified as -sitosterol glucoside (1) [4], 3-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-2-[4-(3-hydroxy-1-(E)-propenyl)-2-methoxyphenoxy]propyl--D-glucopyranoside (2) [5], syringaresinol 4,4-O-bis--Dglucopyranoside (3) [6], acteoside (verbascoside) (4) [7], (2R)-2-O--D-glucopyranosyl-2H-1,4-benzoxazin-3(4H)-one (HBOA-Glc, blepharin) (5) [8], syringin (6) [9], roseoside (7) [10], (+)-lyoniresinol 3-O--D-glucopyranoside (8) [11], pectolinargenin 7-O--D-glucopyranoside (9) [12, 13], cistanoside F (10) [14], (2R)-2-O--D-glucopyranosyl-4-hydroxy-2H-1,4-benzoxazin-3(4H)-one (DIBOA-Glc) (11) [15], nepetin (6-methoxyluteolin) 7-O--D-glucopyranoside (12) [16, 17], and demethoxycentaureidin 7-O--D-glucopyranoside (13) [18, 19] by comparison of their 1H and 13C NMR and mass spectra with those reported in the literature. All of these compounds were isolated for the first time from this plant.