Inhibitory Effect of Persimmon Tannin on Pancreatic Lipase and the Underlying Mechanism in Vitro

J Agric Food Chem. 2018 Jun 20;66(24):6013-6021. doi: 10.1021/acs.jafc.8b00850. Epub 2018 Jun 11.

Abstract

Pancreatic lipase (PL) is a critical enzyme associated with hyperlipidemia and obesity. A previous study of ours suggested that persimmon tannin (PT) was the main component accounting for the antihyperlipidemic effects of persimmon fruits, but the underlying mechanisms were unclear. In this present study, the inhibitory effect of PT on PL was studied and the possible mechanisms were evaluated by fluorescence spectroscopy, circular dichroism (CD) spectra, isothermal titration calorimetry (ITC), and molecular docking. PT had a high affinity to PL and inhibited the activity of PL with the half maximal inhibitory concertation (IC50) value of 0.44 mg/mL in a noncompetitive way. Furthermore, molecular docking revealed that the hydrogen bonding and π-π stacking was mainly responsible for the interaction. The strong inhibition of PT on PL in the gastrointestinal tract might be one mechanism for its lipid-lowering effect.

Keywords: A-ECG and EGCG dimers; fluorescence spectroscopy; molecular docking; obesity; pancreatic lipase; persimmon tannin (PT).

MeSH terms

  • Animals
  • Diospyros / chemistry*
  • Enzyme Inhibitors / chemistry*
  • Kinetics
  • Lipase / antagonists & inhibitors*
  • Lipase / chemistry
  • Molecular Docking Simulation
  • Pancreas / enzymology
  • Plant Extracts / chemistry*
  • Swine
  • Tannins / chemistry*

Substances

  • Enzyme Inhibitors
  • Plant Extracts
  • Tannins
  • Lipase