Investigation of the whole plant of Agastache rugosa resulted in the isolation of two new lignan compounds. Their structures were elucidated as (8S,7'R,8'S)-4-hydroxybenzoic acid 4-(4-hydroxy-3-methoxybenzyl)-2-(4-hydroxy-3-methoxyphenyl)tetrahydrofuran-3-ylmethyl ester (agastinol, 1) and (7'R,8'S)-4-hydroxybenzoic acid 4-(hydroxy-3-methoxybenzylidene)-2-(4-hydroxy-3-methoxyphenyl)-tetrahydrofuran-3-ylmethyl ester (agastenol, 2). Agastinol and agastenol inhibited etoposide-induced apoptosis in U937 cells with IC50 values of 15.2 and 11.4 microg/mL, respectively.