<p>Chestnut shell polyphenols are widely known as antioxidants, but there are few studies on the inhibition of α-amylase to control postprandial blood glucose. This study aimed to evaluate the inhibitory effect of chestnut shell ethanol extract (CSEE) on postprandial blood sugar-related α-amylase and elucidate its underlying mechanism. Twenty-three polyphenols in CSEE were identified via ultra-high performance liquid chromatography with tandem high resolution orbitrap mass spectrometry. CSEE exhibited a strong inhibitory effect on α-amylase in a mixed type inhibition mode (IC<sub>50</sub> = 16.50&#xa0;µg/mL), and two or three polyphenols with high abundance in CSEE exhibited positive synergistic effects on α-amylase after mixing. Further, analysis by molecular docking and spectroscopy indicated that CSEE binding with active site through hydrogen bonding and hydrophobic forces, via changing conformation and microenvironment of α-amylase, eventually reducing the enzyme activity. In vitro starch digestion suggested that CSEE decreases the rapidly digestible starch content and increases the resistant starch content, thereby decreasing starch digestibility and the glycaemic index of starch hydrolysis. These results represent that chestnut shells may be a new potential source of α-amylase inhibitor, as well as a valuable resource for managing postprandial blood glucose levels.</p>

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Chestnut shell polyphenols as a new potential α-amylase inhibitor: Inhibition mechanism (interaction, kinetic, molecular docking), in vitro digestibility of starches, and identification of phenolic compounds by UHPLC-QE

  • Xiyue Yang,
  • Bowei Dong,
  • Sibo Shen,
  • Weiwei Liu,
  • Caihong Cheng,
  • Bin Du

摘要

Chestnut shell polyphenols are widely known as antioxidants, but there are few studies on the inhibition of α-amylase to control postprandial blood glucose. This study aimed to evaluate the inhibitory effect of chestnut shell ethanol extract (CSEE) on postprandial blood sugar-related α-amylase and elucidate its underlying mechanism. Twenty-three polyphenols in CSEE were identified via ultra-high performance liquid chromatography with tandem high resolution orbitrap mass spectrometry. CSEE exhibited a strong inhibitory effect on α-amylase in a mixed type inhibition mode (IC50 = 16.50 µg/mL), and two or three polyphenols with high abundance in CSEE exhibited positive synergistic effects on α-amylase after mixing. Further, analysis by molecular docking and spectroscopy indicated that CSEE binding with active site through hydrogen bonding and hydrophobic forces, via changing conformation and microenvironment of α-amylase, eventually reducing the enzyme activity. In vitro starch digestion suggested that CSEE decreases the rapidly digestible starch content and increases the resistant starch content, thereby decreasing starch digestibility and the glycaemic index of starch hydrolysis. These results represent that chestnut shells may be a new potential source of α-amylase inhibitor, as well as a valuable resource for managing postprandial blood glucose levels.