Aged garlic extract (AGE) is one of the unique preparations standardized with 100% bioavailable active ingredients found in the bloodstream. The current research was aimed at exploring the role of AGE and its chief active constituent, s‐allyl cysteine (SAC) as antioxidant and hypolipidemic agent in rats. At the end of treatment of AGE and SAC, separated serum and freshly prepared liver tissue homogenate were analyzed for biochemical enzymes and biomarkers to evaluate and compare potencies of investigational agents. Both AGE and SAC significantly declined elevated levels of triglyceride, total cholesterol, ALP, AST, ALT, malondialdehyde, glutathione peroxidase enzyme activity, total glutathione and oxidised glutathione in serum and inclined superoxide dismutase, catalase, ferric reducing/antioxidant power, and total sulfhydryl values in liver tissue with reduction in thiobarbituric acid reactive species. The protective effects were superior with AGE compared with SAC indicating potential implication of other active constituents apart from SAC in AGE for combating hyperlipidemic stress.