Abstract: OBJECTIVE To study the different effects and molecular mechanism of Alisol acetates(alisol B 23-acetate and alisol A 24-acetate)on the decrease of the hyperlipidemia of fat mice. METHODS Established a hyperlipidemic mice model，measured the level of TC， TG and HDL-C after the administration of Alisol acetates，detected the activity of LCAT， which is a key enzyme in lipid metabolism，obtained the molecular structure of LCAT by homology modeling and studied the interaction between LCAT and Alisol acetates using molecular modeling. RESULTS Alisol acetates played a hypolipidemic effect by reducing TG， TC level and increasing HDL-C level. lisol acetates decreased the LCAT activity. Alisol acetates binding regions are in the range of Leu201~Phe305. CONCLUSION Alisol acetates elevated HDL-C mechanism may not be by modulating LCAT activity. The region of Leu201~Phe305 may be the suppression positions. Ile227， Arg217， Gly229 may be the critical amino acid residues for the interaction.