Coumarin and Biscoumarin Inhibit <i>in Vitro</i> Obesity Model

Coumarin, sulphonated coumarin, and biscoumarin compounds were examined for their effects on suppressing the adipocyte differentiation in 3T3-L1 cells. Many of them inhibited the adipocyte differentiation in a dose dependent manner, amongst them compounds (7), (28), and (33) significantly suppressed the adipogenic differenti-ation, and also exhibited lipolytic effect on mature adipocytes. The active compounds potentially imitate the AMP-activated protein kinase (AMPK) ligands, there- fore, binding of these compounds with AMPK possibly shuts down the anabolic pathways. Furthermore, these compounds were docked into binding pockets with reasonable pre-dicted binding constants in the low micromolar range. These results indicate that compounds (7), (28), and (33) inhibit adipogenic development in pre- adipocytes, having lipolytic effect on mature adipocytes, and can be potent activators of human AMPK.