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This study was aimed to evaluate the pharmacological potential of various extracts (hexane, chloroform, methanol and aqueous) of dried shoots of Triticum aestivum (wheat grass) in terms of antiproliferative and hepatoprotective potential of T. aestivum. The total chlorophyll content in dried shoots of T. aestivum was 0.54 ± 0.016 g/L (chlorophyll-a: 0.288 ± 0.05 g/L; and chlorophyll-b; 0.305 ± 0.05 g/L), while total carotene content was 0.42 ± 0.066 g/L. In addition, the chloroform extract of dried shoots of T. aestivum (250 μg/mL) exhibited 87.23% inhibitory effect with potent cytotoxicity against human hepatocellular carcinoma (HepG2) cancer cell line. Moreover, chloroform and methanol extracts significantly reduced the levels of SGOT, and SGPT enzymes, as well as total bilirubin content, while raised the level of total protein in a concentration-gradient manner, confirming the potent hepatoprotective effect of T. aestivum. A possible mechanism of apoptosis of the chloroform extract of dried shoots of T. aestivum in terms of its potent antiproliferative activity against HepG2 cancer cell line can also be proposed in this study. Our findings clearly demonstrate that T. aestivum has a significant pharmacological potential that night be used for antiproliferative and hepatoprotective purposes.