Beauveriolides are 13-membered cyclodepsipeptides isolated from Beauveria sp. Beauveriolide III inhibits acyl-CoA:cholesterol acyltransferase (ACAT) to block the synthesis of cholesteryl ester, leading to a reduction of lipid droplets in macrophages. Beauverolide III is more potent against ACAT1 than ACAT2 (IC50 5.5 vs. > 20 µM, respectively). Beauveriolide III is antiatherogenic activity in mouse models.