Saponifiable and unsaponifiable fractions of Ficus microcarpa leaves hexane extract have been phytochemically studied and evaluated for its hypolipidaemic and antioxidant effects in hypercholesterolemic rats. The effect of the extract on the lipid profile was assessed by measuring the levels of total cholesterol, high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C), triglycerides, phospho and total lipids. Lipid peroxides, glutathione and superoxide dismutase were measured as antioxidants. The work was extended to evaluate liver function indices as well as the histopathological picture of the liver after treatment. Treatment with leaves extract (500 mg kg⁻¹ body weight) 5 times/week for 9 weeks at the same time of cholesterol administration (30 mg/0.3 mL 0.7% tween/animal) recorded an improvement of lipid profile, antioxidants, liver function enzymes and the liver histopathological picture. The lipoidal matters of the unsaponifiable fraction of the hexane extract by GC/MS led to the identification of 22 compounds, while saponifiable fraction by (MS/MS) technique led to identification of 13 unsaturated and saturated fatty acid methyl ester derivatives. It can be concluded that the hexane extract of F. microcarpa L has been proved to have hypolipidaemic and antioxidant effects in hypercholesterolemic rats through its role in counteracting LDL oxidation, enhancement of HDL synthesis and inhibition of lipid peroxidation.