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Inhibition of protein tyrosine phosphatase 1B by flavonoids: A structure - activity relationship study

Carina Proença1, Marisa Freitas1, Daniela Ribeiro1

  • 1UCIBIO, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal.

Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association
|November 28, 2017
PubMed

Insights

Certain flavonoids show promise as inhibitors of protein tyrosine phosphatase 1B (PTP1B), a key target for type 2 diabetes. These compounds may improve insulin sensitivity and aid in managing type 2 diabetes mellitus (T2DM).

Area of Science:

  • Biochemistry
  • Pharmacology
  • Endocrinology

Background:

  • Protein tyrosine phosphatase 1B (PTP1B) is a critical negative regulator of insulin signaling.
  • Dysregulation of PTP1B activity contributes to insulin resistance and type 2 diabetes mellitus (T2DM).
  • PTP1B represents a significant therapeutic target for T2DM management.

Purpose of the Study:

  • To investigate the in vitro inhibitory activity of structurally related flavonoids against recombinant human PTP1B.
  • To evaluate the inhibition type of the most potent flavonoid inhibitors.
  • To identify structural features of flavonoids that enhance PTP1B inhibition.

Main Methods:

  • In vitro enzyme inhibition assays were performed using recombinant human PTP1B.
  • A panel of structurally related flavonoids was screened for inhibitory activity.
  • Kinetic studies were conducted to determine the type of inhibition for active compounds.

Main Results:

  • Flavonoid C13 emerged as the most potent PTP1B inhibitor among the tested compounds.
  • Flavonoid inhibitory activity is significantly influenced by the nature, position, and number of substituents.
  • Specific substituents, including 7- and 8-OBn groups (A ring), 3' and 4'-OMe groups (B ring), and a 3-OH group (C ring), enhance PTP1B inhibition.

Conclusions:

  • Several tested flavonoids demonstrate significant PTP1B inhibitory potential.
  • These flavonoids may serve as novel therapeutic agents for T2DM by enhancing insulin sensitivity.
  • Structural optimization of flavonoids could lead to more effective PTP1B inhibitors for diabetes treatment.
Keywords:
Diabetes mellitusEnzymatic inhibition typeFlavonoidsPTP1B inhibition

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