For the development of novel hepatoprotective agents, C11, C28, C2,3,23 or C2,23,28 functional groups on asiatic acid were modified, and their hepatoprotective effects were evaluated. Most of the prepared compounds displayed potent hepatoprotective activities against CCl4- and galactosamine (GaIN)-induced hepatotoxicity. Especially, compounds 16 and 20 showed the most significant hepatoprotective effects against GaIN-induced hepatotoxicity (54.2% and 46.4% protection at 50 mM, respectively).