Human Acyl-CoA:Cholesterol Acyltransferase(hACAT)Inhibitory Activities of Triterpenoids from Roots of Glycine max(L.)Merr.

摘要

Eight triterpenoids,six lanostanes 1-6,one lupenane 7,and one oleanane 8,were isolated by bioactivity-guided fractionation of the ethylacetate extract from roots of Glycine max(L.)Merr.All isolated compounds were examined for their inhibitory activities against human ACAT-1(hACAT-1)and human ACAT-2(hACAT-2).Among them,three triterpenoids showed potent hACAT inhibitory activities,(24R)-ethylcholest-5-ene-3,7-diol(1)and 3beta-hydroxylup-20(29)-en-28-oic acid(7)exhibited more potent inhibitory activity against hACAT-1(1:IC50=25.0±1.2 and 7:IC50=11.5±0.4 mu M)than hACAT-2(1:IC50=102.0±5.4 and 7:IC50=33.9±3.7 mu M),respectively.Interestingly,5 alpha,8 alpha-epidioxy-24(R)-methylcholesta-6,22-diene-3beta-ol(4)has proven to be a specific inhibitor against hACAT-1(IC50=38.7±0.8 mu M)compared to hACAT-2(IC50>200).In conclusion,this is the first study to demonstrate that triterpenoids of G.max have potent inhibitory activities against hACAT-1 and hACAT-2.