Novel cinnamic acid magnolol derivatives as potent α-glucosidase and α-amylase inhibitors: Synthesis, in vitro and in silico studies

In this study, twenty novel cinnamic acid magnolol derivatives were synthesized, and screened for their anti hyperglycemic potential. All synthesized compounds exhibited good to moderate alpha-glucosidase and alpha-amylase inhibitory activities with IC50 values: 5.11 +/- 1.46-90.26 +/- 1.85 mu M and 4.27 +/- 1.51-49.28 +/- 2.54 mu M as compared to the standard acarbose (IC50: 255.44 +/- 1.89 mu M and 80.33 +/- 2.95 mu M, respectively). Compound 6j showed the strongest inhibitory activity against alpha-glucosidase (IC50 = 5.11 +/- 1.46 mu M) and alpha-amylase (IC50 = 4.27 +/- 1.51 mu M). Kinetic study indicated that compound 6j was reversible and a mixed type inhibitor against alpha-glucosidase and alpha-amylase. In silico studies revealed the binding interaction between 6j and two enzymes, respectively. Finally, cells cytotoxicity assay revealed that compound 6j showed low toxicity against 3 T3-L1 cells and HepG2 cells.