Actein, a 9,19-cyclobutane triterpenoid from Cimicifuga spp., ameliorates atherosclerosis via ABCG1 and LXR upregulation.

Introduction: Considering the global burden of atherosclerosis-related cardiovascular mortality, this study investigates the anti-atherosclerotic potential of Actein, a 9,19-cyclobutane triterpenoid isolated from Cimicifuga spp.

Methods: The study employed both in vitro and in vivo experiments. In vitro, the effect of Actein on oxLDL-induced macrophage foam cells was examined. In vivo, ApoE-deficient mice were fed a high-fat diet to induce atherosclerosis and were then treated with Actein (10 mg/kg) or Atorvastatin for 8 weeks.

Results: Actein significantly reduced lipid accumulation in oxLDL-induced foam cells. In the in vivo model, Actein treatment significantly lowered serum levels of total cholesterol, triglycerides, and low-density lipoprotein cholesterol, while increasing high-density lipoprotein cholesterol. Furthermore, Actein diminished the levels of inflammatory markers (IL-6, IL-1β, TNF-α, and MMP-9) and upregulated the expression of ABCG1 and LXR proteins in liver tissue. The efficacy of Actein was comparable to, and in some aspects superior to, that of Atorvastatin.

Conclusion: These findings establish Actein as a promising natural compound for the treatment of atherosclerosis, warranting further investigation into its therapeutic potential.