TITLE:
Coumarin and Biscoumarin Inhibit in Vitro Obesity Model
AUTHORS:
Farah Mukhtar, Kimberly Stieglitz, Shamsher Ali, Asma Ejaz, Muhammad Iqbal Choudhary, Muhammad Imran Fakhri, Uzma Salar, Khalid Mohammed Khan
KEYWORDS:
Coumarin, Sulphonated Coumarin, Biscoumarin, Adipocyte Differentiation and Docking Studies
JOURNAL NAME:
Advances in Biological Chemistry,
Vol.6 No.5,
October
28,
2016
ABSTRACT: 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.