1. Academic Validation
  2. α-Glucosidase inhibitory effect of Potentilla astracanica and some isoflavones: Inhibition kinetics and mechanistic insights through in vitro and in silico studies

α-Glucosidase inhibitory effect of Potentilla astracanica and some isoflavones: Inhibition kinetics and mechanistic insights through in vitro and in silico studies

  • Int J Biol Macromol. 2017 Dec;105(Pt 1):1062-1070. doi: 10.1016/j.ijbiomac.2017.07.132.
Didem Şöhretoğlu 1 Suat Sari 2 Arzu Özel 3 Burak Barut 3
Affiliations

Affiliations

  • 1 Hacettepe University, Faculty of Pharmacy, Department of Pharmacognosy, Sıhhiye, Ankara, TR-06100, Turkey. Electronic address: didems@hacettepe.edu.tr.
  • 2 Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Sıhhiye, Ankara, TR-06100, Turkey.
  • 3 Karadeniz Technical University, Faculty of Pharmacy, Department of Biochemistry, Trabzon, Turkey.
Abstract

α-Glucosidase Enzyme inhibitors are clinically used for the treatment of Type 2 diabetes mellitus. We tested α-glucosidase inhibitory effects of Potentilla astracanica Jacq. extracts (1, 2), two compounds isolated from these extracts, prunetin 5-O-β-glucopyranoside (3) and genistein 5-O-β-glucopyranoside (4), and their aglycon forms (5 and 6). All the tested Materials possessed remarkable α-glucosidase inhibitor activity compared to the positive control, acarbose. Genistein (6) showed the highest activity with an IC50 value of 1.47 (±0.11) μg/ml. An Enzyme kinetics analysis revealed that 3 and 6 were uncompetitive, 5 was noncompetitive, and 4 was competitive inhibitors. Using molecular modeling techniques we tried to provide insight into molecular mechanisms of their activity and how allosteric binding of 6 affected binding interactions between the agonist (maltose) and the Enzyme.

Keywords

Molecular dynamics; Potentilla; α-Glucosidase.

Figures
Products