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Structural Biology and Analytical Chemistry Approaches for Characterizing C-Glycoside Metabolic Enzymes in Human Gut Microbiota
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Inhibitory activity of flavonoids against human sucrase-isomaltase (α-glucosidase) activity in a Caco-2/TC7 cellular

Carina Proença1, Ana T Rufino1, José Miguel P Ferreira de Oliveira1

  • 1LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal. egracas@ff.up.pt.

Food & Function
|January 11, 2022
PubMed

Insights

Flavonoids show potential as new treatments for type 2 diabetes by inhibiting human alpha-glucosidase. Researchers found specific structural features enhance this activity, suggesting further study for developing novel antidiabetic drugs.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Metabolic Diseases

Background:

  • Type 2 diabetes (T2D) is a growing global health concern.
  • Alpha-glucosidase inhibitors are key for managing postprandial hyperglycaemia (PPHG) in T2D.
  • Current research often uses non-human enzyme sources, limiting physiological relevance.

Purpose of the Study:

  • To evaluate the inhibitory effects of flavonoids on human sucrase-isomaltase (SI).
  • To identify structural characteristics of flavonoids that enhance SI inhibition.
  • To advocate for the use of human enzyme sources in preclinical studies.

Main Methods:

  • A microassay was employed to test flavonoid inhibition against human SI.
  • Enzyme activity was assessed using natural substrates (sucrose, maltose) and a synthetic substrate (p-nitrophenyl-α-D-glucopyranoside).
  • Structure-activity relationships were analyzed based on flavonoid chemical structures.

Main Results:

  • Melanoxetin (compound 4) demonstrated significant inhibitory activity against human SI using natural substrates.
  • Flavonoid efficacy varied depending on the substrate used; they were less effective with the synthetic substrate.
  • Hydroxylation at specific positions (C-3, C-3', C-4', C-7, C-8) positively correlated with inhibitory potency.

Conclusions:

  • Flavonoids, particularly melanoxetin, show promise as potential therapeutic agents for T2D.
  • Specific hydroxyl group placements on flavonoid structures enhance alpha-glucosidase inhibitory activity.
  • Human enzyme sources are crucial for accurate in vitro assessment of alpha-glucosidase inhibitors.

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