Cyclic diarylheptanoids inhibit cell mediated low-density lipoprotein oxidation.

Two cyclic diarylheptanoids, garugamblin-3 (1) and acerogenin L (2), isolated from the MeOH extract of the fruits of Alnus japonica Steud., inhibited human low-density lipoprotein (LDL) oxidation in the thiobarbituric acid-reactive substance assay with IC(50) values of 2.9 and 1.7 microM, respectively, and they also inhibited cell-mediated LDL oxidation more than 5 times more strongly than that of a well-known antioxidant, probucol, at a concentration of 10 microM. Compound (1) had no effect on the anti-atherogenesis in low-density lipoprotein receptor-deficient mice.