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Published on: February 15, 2019
Inhibition of human intestinal α-glucosidases by calystegines
Nebojša Jocković1, Wiebke Fischer, Matthias Brandsch
1Institute of Pharmacy, Faculty of Sciences I, Martin-Luther-University Halle-Wittenberg , Hoher Weg 8, 06120 Halle (Saale), Germany.
Calystegines from potatoes show potential for managing blood glucose. Calystegine B2 weakly inhibits sucrase, suggesting dietary vegetables may help prevent post-meal glucose spikes.
Area of Science:
- Biochemistry
- Plant Science
- Nutritional Science
Background:
- Calystegines are plant alkaloids found in common fruits and vegetables.
- Their sugar-like structure suggests interaction with carbohydrate-metabolizing enzymes.
- Inhibition of alpha-glucosidases like maltase and sucrase is a strategy for type 2 diabetes management.
Purpose of the Study:
- To investigate the inhibition of human maltase and sucrase by calystegines A3 and B2.
- To assess the potential of these alkaloids as dietary components for glucose management.
Main Methods:
- Purification of calystegines A3 and B2 from potatoes.
- In silico docking studies to predict enzyme-alkaloid interactions.
- In vitro enzyme inhibition assays.
- Caco-2 cell transport studies to evaluate systemic availability.
Main Results:
- In silico studies confirmed calystegine binding to maltase and sucrase active sites.
- Calystegine A3 exhibited low in vitro inhibition of both enzymes.
- Calystegine B2 showed inhibition primarily against sucrase.
- Both calystegines demonstrated low transport by Caco-2 cells, indicating limited systemic absorption.
Conclusions:
- Calystegine B2's inhibition of sucrase warrants further investigation for dietary interventions.
- Vegetables containing calystegine B2 may help mitigate postprandial hyperglycemia.
- Low systemic availability suggests a localized effect in the gastrointestinal tract.
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