Author(s)

Farah Mukhtar¹, Kimberly Stieglitz², Shamsher Ali³, Asma Ejaz⁴, Muhammad Iqbal Choudhary^5,6,7, Muhammad Imran Fakhri⁷, Uzma Salar⁷, Khalid Mohammed Khan⁷

¹Department of Chemistry, University of Karachi, Karachi, Pakistan.
²STEM Biotechnology Division, Roxbury Community College, Roxbury, MA, USA.
³Department of Environmental Health, Harvard University TH Chan School of Public Health, Harvard-MIT Division of Health Sciences and Technology, Department of Medicine, Brigham and Women’s Hospital, Boston, MA, USA.
⁴Vascular Surgery Research, Harvard Medical School, Boston, MA, USA.
⁵Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Ka-rachi, Karachi, Pakistan.
⁶Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia.
⁷H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.

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.

Coumarin, Sulphonated Coumarin, Biscoumarin, Adipocyte Differentiation and Docking Studies

Mukhtar, F. , Stieglitz, K. , Ali, S. , Ejaz, A. , Choudhary, M. , Fakhri, M. , Salar, U. and Khan, K. (2016) Coumarin and Biscoumarin Inhibit in Vitro Obesity Model. Advances in Biological Chemistry, 6, 152-168. doi: 10.4236/abc.2016.65014.