Kaempferol (3,5,7,4′-tetrahydroxy flavone), a naturally occuring flavonoid, distributed all over the world tremendously essential because of its biological and health beneficial properties. The present study was aimed to investigate its curative prospective by estimating the lipid peroxidation (LPO) activities, levels of antioxidants enzymes and phase I and II biotransformation enzymes against Aflatoxin B₁ (AFB₁) induced experimental hepatocarcinogensis. In the developing countries, 80% of the burden of hepatocellular carcinoma (HCC) due to the occurrence of HCC in regions where aflatoxin exposure is high. After inducing primary liver cancer by Aflatoxin B₁ (AFB₁), group III animals were administrated with kaempferol (100mg/kg/bw p.o) dissolved in 1ml of DMSO for a period of 28 successive days. The disturbed activities of lipid peroxidation, declined levels of enzymic and non enzymic antioxidants and altered levels of xenobiotic enzymes were significantly (P<0.01) reverted to near standard levels by the treatment of natural flavonoid kaempferol. Thus, results undoubtedly prove the modulatory property of kaempferol through significantly restored all the altered biochemical analysis. Furthermore, histopathological changes of liver sample were compared with respective control which strongly indicates antioxidant and anticancer properties of kaempferol which afford a guarantee for prevalent use for treatment of hepatocellular carcinoma in the upcoming.