Ethanolic and aqueous leaf extracts of Ficus cyathistipula significantly reduced blood-glucose level, improved triglycerides and cholesterol levels of dyslipidemia in diabetic-rats. They similarly reduced the inflammation of paw-edema and stomach-ulcers in rats. Fractions obtained by successive partition of ethanolic extract were assessed for their cytotoxicity, antioxidant and antimicrobial activities; Petroleum ether fraction was the most cytotoxic (IC(50) = 4.43 ± 0.2, 17.3 ± 2.22 and 15.5 ± 3.67 μg/ml on MCF7, HepG2 and HeLa cell lines, respectively). Ethyl acetate fraction was the strongest antioxidant in DPPH assay (IC(50) = 100 μg/ml). All samples exhibited low to strong antimicrobial activity. Chemical investigation of leaf extracts led to the isolation of α-amyrin palmitate (1), lupeol acetate (2), taraxerol (3), β-sitosterol (4), protocatechuic acid (5) and 3-O-caffeoyl quinic acid (6) that were identified via spectral and chromatographic analyses. Metabolite profiling was performed via UPLC-PDA-MS and revealed the presence of flavonoid glycosides, phenolic acids, isoflavones, coumarins and fatty acids. Quantitative determination revealed 593 ± 0.5 mg BSE, 348.1 ± 0.09 mg GAE, 238.7 ± 0.5 mg rutin and 9 ± 0.5 g tannins per 100 g d.wt. of leaves. GLC analysis of lipid fraction revealed identification of phytosterols (15.6%), saturated (51.71%) and unsaturated (41.9%) fatty acids. Galactose, glucose, arabinose and glucoronic acid (36.98%, 28.86%, 22.56% and 1.06%, respectively) were identified by HPLC analysis of mucilage-hydrolysate.