The invention relates to the application of gynostemma pentaphylla saponin LVII in preparation of anti-hepatoma drugs, particularly to gynostemma pentaphylla saponin. The gynostemma pentaphylla saponin LVII is known as 2-hydroxyl-3-O-Beta-D- glucopyranose-20(S)-protopanoxadiol-20-O-Beta-D-xylopyranose(1-6)-Beta-D-glucopyranoside, the molecular formula is C47H80O18, and the molecular weight is 932; the gynostemma pentaphylla saponin LVII is obtained by separating and purifying gynostemma pentaphylla total saponins in a step-by-step manner through adopting the enzymatic conversion method, therefore, the preparation method is simple and the cost is low. When the hepatoma is taken as an example, the testing result of the extracorporeal anti-hepatoma model indicates that the gynostemma pentaphylla saponin LVII has inhibiting effect on growth of hepatoma cell line SMMC7721, Bel7402, and can degrade the DNA in the human hepatoma carcinoma cell Bel7402 into small fragments, so as to facilitate death of human hepatoma carcinoma cells and inhibit the growth of hepatoma, as a result, the gynostemma pentaphylla saponin LVII can be applied in the preparation of anti-hepatoma drugs.