In the course of a search for acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors from natural sources, new types of ACAT inhibitors were isolated from the extract of Magnolia obovata leaves, and identified as obovatol, honokiol, and magnolol. The active compounds inhibit rat liver ACAT with IC50 values of 42, 71, and 86 μM, respectively.