This study investigated the antiatherogenic activity and the chemical constituents of a triterpenoids-enriched extract from the aerial parts of Salvia miltiorrhiza Bunge. The extract displayed a significant, dose-responsive antiatherogenic effect on LDLR(-/-) mice after a 24-week application in a daily dose 50, 100, 200, 1000 mg/kg, respectively. Pronounced systemic inflammation and cutaneous xanthomatosis inhibition effects of the extract, combined with hypocholesteremic and plaque stable properties, were shown in this study. At 200 mg/kg in the high dose treated group, the percent inhibitions of two inflammatory markers in serum, CRP and MCP-1, were 47.6 +/- 4.2% and 36.8 +/- 5.0%, and significant reductions in aortic atherosclerotic lesion areas were 62.3 +/- 3.9% (en face) and 77.8 +/- 3.1% (cross section) compared with the model group. No abnormal behavior or lethality were observed with the extract up to 1000 mg/kg. Fifteen triterpenoids were separated and identified from the extract. This study provided new evidence of the antiatherogenic property of S. miltiorrhiza correlated with triterpenoids by an antiinflammatory mechanism.