Background: Cancer is a life threatening deadly disease considered as a major health concern globally. Hepatocellular Carcinoma (HCC) is a foremost health anxiety in developing and developed nations due to a variety of etiologies factors, including Hepatitis virus, superfluous storage of iron in the body, exposure to toxins and carcinogens which directly affect the cellular mechanism. Objective: The present investigation involved in analyzing anti-cancer potential of diosmin through in vitro and in vivo examination. Materials and methods: The present study absorbed the anti-cancer activity of diosmin at 50, 100, 150, 200 μM/ml for 24 hours of treatment on dose dependent manner. Group II animals were administrated 0.01% NDEA to induce primary liver carcinoma. Cancer bearing experimental animals were treated orally with the drug diosmin at the dosage level of 200 mg per kg/body weight for 28 successive days. Results: Diosmin treatment on HepG2 cells constrains nearly half of the cell population and proliferation at the dose of 100 μM/ml and in vivo experimental studies showed remarkable repossession in biochemical and morphological characteristics. Conclusion: These results summarizes that both in vivo and in vitro anti-carcinogenic activity of diosmin could be an outstanding flavonoid in the treatment of HCC because of its therapeutic and pharmacological properties.