The main aim and objective of the present research work was the extraction, isolation and characteriza tion of bioactive molecule resveratrol (RVTL) from the blac k grapes (Vitis vinefera) and in vivo evaluation of hepatocytes regenerator potentiality against CCl 4 induced rat hepatocytes and in vitro cytotoxic act ivity against both human colon cancer cell line HT-29 and human breast cance r HS 578T Cell line. Based on this a new series of constituents had been planned to extract by Ethanol (ENL) from b lack grapes. The isolation and characterization of bioactive molecule resveratrol (RVTL) were carried out from t he ENL extract of the black grapes (Vitis vinefera) by modern analytical techniques such as U.V, I.R, 1 H-NMR and 13 C-NMR, JEOL GCmate and HPLC–ESI–MS/MS spectroscopy. In-vivo hepatoprotective activity was carried out by using albino rats. The results disp layed that the elevated levels of SGOT, SGPT, ALP and Serum biliru bin were mainly due to CCl 4 intoxication, reduced significantly (*P<0.05) in rats, after treatment wi th ENL extract containing RVTL of black grapes (Vit is vinefera). Treatment with ENL extract of black grapes (Vitis v inefera) at a both doses of 250 and 500 mg/kg b.w. significantly decreased the SGOT, SGPT, ALP, Serum Bilirubin leve ls by 23.5%, 28.9%, 8.9%, and 17.2% (at low dose) a nd 26.9%, 35.9%, 14.5% and 22.3% (at high dose) respec tively. Silymarin used as standard drug showed a re duction of 56.09%, 69.89%, 57.46% and 19.04% ns receiving CCl 4 alone. Histopathological investigation displayed t hat at both doses (250 mg/kg b.w. and 500 mg/kg b.w.), the ENL extract of black grapes (Vitis vinefera) was p ossessed very good hepatoprotective activity, but at 500 mg/ kg b.w. executed excellent hepatoprotective activit y against CCl4 induced damaged hepatocytes. The in vitro cytotoxic activity was carried out by SRB assay. The results obtained from the in-vitro studies performed by SRB assay us ing the HT-29 cell lines and HS 578T displayed that the ENL extract containing RVTL of black grapes (Vitis vini fera) possessed a very good cytotoxic activity. Fro m the present studied it had been concluded that ENL extract cont aining RVTL of black grapes (Vitis vinifera) exhibi ting the potential capability to kill the neoplastic cell wh en compared with standard drug 5-FU and doxorubicin . The ENL extract containing RVTL of black grapes (Vitis vini fera) displayed with the highest 93.43% growth inhi bition at 12.5 μ g (IC 50 = 2.2 μ g/ml) against human colon cancer cell line HT-29 and 93.6% growth inhibition at 25 μ g (IC 50 = 1.9 μ g/ml) against human breast cancer HS 578T Cell lin e.