Hesperidin a natural flavanoglycoside, has demonstrated a wide variety of biological activities which make it a good candidate for the treatment of many oxidative stress mediated diseases. The present study was aimed to evaluate its therapeutic potential by assaying the activities of lipid peroxidation and various membrane bound marker enzymes in 7, 12-Dimethybenz (a) anthracene induced breast cancer rats. The daily oral treatment of hesperidin (30mg/kg body weight) to breast cancer bearing rats for 45 days demonstrated a significant (p<0.05) decline in lipid peroxidation and membrane bound marker enzyme levels. The altered activities of membrane bound key marker enzymes such as AST, ALT, ALP, ACP, 5’ND, γ-GT, and LDH in serum of control and experimental breast cancer rats were significantly (p<0.05) reverted to near normal levels by the administration of hesperidin. Further, hesperidin administration to breast cancer bearing rats improved the macromolecular structure such as total protein content in breast, liver tissues and serum suggesting the maintenance of cell structure and integrity and also modulation of nucleic acids thereby exhibiting anticancer potential of hesperidin in breast cancer bearing rats. Thus, the modulatory effects of hesperidin on attenuating the lipid peroxidation and down regulation of key membrane bound marker enzyme activities and up regulation of protein content afford an assurance for widespread use for treatment of breast cancer in the future.